Free Opening Brief in Support - District Court of Delaware - Delaware

Case 1:04-cv-00833-KAJ

Document 253-6

Filed 06/21/2006

Page 1 of 29

EXHIBIT 5

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 2 of 29

I.

National Coordinating Committee on Large Volume Parenterais, "Recommendations to Pharmacists for Solving Problems with Large-Volume Parenterals", Am. J. Hosp. Pharm. 33:231 (1976). "United Kingdom Patent No. 1491184, (November, 1977). "Procede pour la preparacion d'heterosides de dihydroxyphenlalcanol heterosides, (January 1977), French Patent No. 2 314 725. The Pharmaceutical Codex 11th Ed., (1979), "Injections" p. 446-447. French Patent No. 2 405 957, (May 11, 1979). Pharmaceutical Sciences, Mack Publishing, (1980), p. 1365-1366. Chemical Abstracts, vol. 92, 99512c, (1980). The United States Pharmacopeia, Twentieth revision, p. 266, July 1, 1980. Chemical Abstracts, vol. 94 (1981), 214489f. Chemical Abstracts, vol. 99, 146022z. Chemical Abstracts, vol. 99 p. 345, Abst. No. 99:218014y. Nor. Pharm. Acta, 45, 61-67 (1983). Union Warns of Cancer Drug Dangers, Chemistry and Industry, (July 4, 1983). Drug Topics, "Cancer Drug Danger", (February 7, 1983), p. 99. Abstract of Medical Economics Co., Chemistry-Industry, (Feb. 7, 1983), p. 99. Chemical Abstracts, vol. 101, 122451x (1984). Journal of Chromatography 299, pp. 489-494 (1984). J. Pharm. Biomed Anal., 2,297-303 (1984). Japanese Patent No. 60-92212, (May, 1985). Adriamycin or Daunomycin composition having increased activity and decreased toxicity, European Patent No. 1 29 606. "Farmaceutische preparaten die antracycline glycosiden bevatten, alsmede een werkwijze ter bereiding daarvan, -Netherlands Patent No. 8 50 28 69. Epirubicin, Drugs of the Future, vol. 8, (5): p. 402, (1985). Chemical Abstracts, vol. 102 (1985), 209266k. et medicament de tels

2. 3.

4. 5. 6. 7. 8. 9. 10. 11. 12. 13. 14. 15. 16. 17. 18. 19. 20.

21.

22. 23.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 3 of 29

24. 25. 26. 27. 28. 29. 30. 31.

U.S. Pharmacopoeia (1985), p. 119. German Patent No. 29 27 452. Pharmaceutisch Weekbald, Scientific Edition, vol. 8, (Apr. 25, 1986), pp. 109-133. German Patent No. 3621844 A1 (March, 1987). Chemical Abstracts, vol. 104 (1986), 39716d. AHFS Drug Information (!990), p. 501-507. European Patent No. 0 401 896 A1, (December 12, 1990). Drug Information for the Health Care Professional USP DI (1991) 11th Edition, p. 12171222. Drug Information for the Health Care Professional USP DI (1991), 1lth Edition, p. 10801084. Pharmacol. 34:416-422 (1994). ABPI Data Sheet Compendium, (1994-1995), "Novantron Injection," Lederle Laboratories, pp. 752-754. German Patent Office Decision dated (10/8/96), revoking Patent No. 36 218844. Great Britain Patent No. 2 16 751, (April, 1996). Abdella (1985) A Chemical perspective on the Anthracycline Antitumor Antibiotics, Env. Health Persp. vol. 64, pp. 3-18. Adams (1987) Pharmaceutical Aspects of Home Infusion Therapy for Cancer Patients, (Apr. 1987), Pharm J., p. 476. Akbiyik (1979) "Total Lung Irradiation and Chemotherapy in Pulmonary Metastes from Carcinoma of the Uterine Cervix and Endometrium", J. Nat'l Medicinal Assn., Vol. 71, pp. 1061-1063. Alchas (1985)Self-Venting, Non-Coring Needle Assembly, (Aug. 1985), US Patent No. 4,537,593. Alfred N. Martin (1975) "Physikalische Pharmazie, p. 239. Amirjahed (1977) Simplified Method to Study Stability of Pharmaceutical Preparations, J. Pharm. Sci. p. (6):785 -788. Angiuli (1971) Structure of Daunomycin, X-Ray Analysis of N-Br-Acetyl-Daunomycin Solvate, Nature New Biol., 234:78-80, (Nov. 1971).

32.

33. 34.

35. 36. 37.

38.

39.

40.

41. 42.

43.

-2-

Case 1:04-cv-00833-KAJ
ATTACHMENT I 44. 45.

Document 253-6

Filed 06/21/2006

Page 4 of 29

Arcamone _' nx,,_ ,-, ·... ,_, · · _ _v, ) La _onstttuuon _mmlque de ia Daunomycine, Path. Biol. i 5(i9-20): 893. Arcamone (1969) Adriamycin (14-Hydroxydaunomycin), Tetrahedron Letters No. 13, p. 1007-1010. a Novel Antitumor Antibiotic

46.

Arcamone (1969) Adriamycin, 14-Hydroxydaunomycin, a New Antitumor Antibiotic from S. Peucetius Var. Caesius, Biotechnology and Bioengineering, vol. XI, pp. 1101-1110. Arcamone (1971) Structure of Daunomycin, X-Ray Analysis of N-Br-Acetyl-Daunomycin Solvate, Nature New Biol., 234:78. Arcamone (1971) Adriamycin Derivatives, (June, 29, 1971), US Patent No. 3,590,028. Arcamone (1972) "Dihydrodaunomycin Antibiotic and Derivatives Thereof, (Aug. 1972), US Patent No. 3,686,163. Arcamone (1972)"Structure and Physicochemical Properties of Andriamycin", International Symposium on Adriamycin "pp. 9-22. Arcamone (1974) "Process for the Preparation of Adriamyin and Adriamycinone and Adriamycin Derivatives", US Patent No. 3,803,124. Arcamone (1976) "Synthesis and Antitumour Activity of 4-Demethoxydaunorubicin, 4Demothoxy-7, 9-diepidaunorubicin, and their beta anomers", Cancer Treat Rep. 60(7):829. Arcamone (1976) "Synthesis and Antitumour Activity of 4-Deoxydaunorubicin 4Deoxyadriamycin", J. Med. Chem. 19(12): 1424. and

47.

48. 49.

50.

51.

52.

53.

54. 55.

Arcamone (1977) "Adriamycins and Uses Thereof, (Nov. 1977), US Patent No. 4,058,51. Arcamone (1977) "Daunomycins, Process for their Uses and Intermediates, US Patent No. 4,039,663. Arcamone (1977) Lloydia, "New Antitumor Anthracyclines," 40(1):45-66. Arcamone (1978) Topics in Antibiotic Chemistry, Vol. 2, 109-115. Arcamone (1978) Daunomycin and Related Antibiotics. Topics in Antibiotic Chemistry. vol. 2 (Sammes, ed.) (1978), pp. 103-278. Arcamone (1978) "U.S. Patent No. 4, 077,988 (March, 1978). Arcamone (1978) "Synthesis and Antitumour Activity of new Daunorubicin and Adriamycin Analogues", Experientia 34:1255. Arcamone (1979) Process for the Preparation of Adriamycins, Canadian Patent No. 1 046 507 (January, 1979). Arcamone (1979) Process for the Preparation of Daunomycins, Canadian Patent No. 1 046 508 (January 1979).
-3-

56. 57. 58.

59. 60.

61.

62.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 5 of 29

63.

Arcamone (I 98 I) Discovery & Development of Doxorubicin, Doxorubicin, Anticancer Antibiotics (Arcamone, eds.) Academic Press, pp. 1-47. Arena (1971) Analysis of the pharmacokinetic characteristics, pharmacological and chemotherapeutic activity of 14-hydroxy-daunomycin (adriamycin), a new drug endowed with an Antitumor activity, Drug Res. 21: 1258. Asker (1988) Effect of Glutathione on Photolytic Degradation of Doxorubicin Hydrochloride, J. Par. Sci. Tech., 42(5)193. Aubel Sadron (1984) Daunorubicin and doxorubicin, anthracycline antibiotics, a physicochemical and biological review Biochemie 66, pp. 333-352. Aulton (1988) Pharmaceutics--The science of dosage form design, pp. 242-244, 252253, 368-369, 374-375, 380. Bachur (1973), "Daunorubicin and adriamycin metabolism in the golden syrian hamster", Biochem. Med. vol. 8, p. 352. Bachur (1976), Cellular pharmacodynamics of several anthracycline antibiotics Journal of Medicinal Chemistry, Volume 19, Nov. 5, 1976 pps. 651-654. Bachur (1981), Daunomycin Metabolism in Rat Tissue Slices., J. Pharm. Exp. Ther. 175(2):331. B244. Banker & Chalmers (1982) Pharmaceutics & Pharmacy Practice, pp. 238-243, 275-278. Banks (1977) Topical Installation of Doxorubicin Hydrochloride in the Treatment of Recurring Superficial Transitional Cell Carinoma of the Bladder, J. Ulrol., vol. 118, p. 757. Barranco (1973) Survival and cell kinetics effects of adriamycin on mammalian cells, Cancer Res. 33:11. Barth (1977) Determination of Doxorubicin Hydrochloride., Pharmaceutical Preparations using High Pressure Liquid Chromatography, (1977) J. of Chromatography vol. 131, p. 375381. Barthelemy-Clavey (1974) Self-Association ofDaunorubicin, FEBS Lett., vol. 46(1), p. 5.

64.

65.

66.

67.

68.

69.

70.

71. 72.

73.

74.

75. 76.

Baurain (1980), "Nouveaux derive de la doxorubicine, leur preparacion et les compositions qui les contiennent" February, 1980, French Patent No. 2 432 525. Baurain (1981), "Derivatives of Doxorubicine, Their Preparation and Use", Oct. 1981, US Patent No. 4,296,105. Bean (1967) Advances in Pharmaceutical Services, (Bean, et al.), Vol. 2, pp. 62-75, 80-95. Beijnen (1985), "Aspects of the Chemical Stability of Doxorubicin and Seven Other Anthracyclines in Acidic Solution", Pharmaceutical Weekblad Scientific Editor, vol. 7, pp. 109-116.
-4-

77.

78. 79.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 6 of 29

80.

Beijncn (1985), "Stability of Anthracycline Antitumor Agents in Four Infusion Fluids", J. Parenteral Science and Technology, vol. 39, pp. 220-222. Beijnen (1986) "Stability of intravenous admixtures of doxorubicin and vincristine. Am. J. Hosp. Pharm., vol. 43, p. 3022. Beijnen (1986) Aspects of the Degradation Kinetics of Doxorubicin in Aqueous Solution (1986) 32 Int. J. Pharm. 123. Beijnen (1987) Structure Elucidation and Characterization of Daunorubicin Degradation Products (1987) Int. J. Pharm., vol. 34, p. 247. Bekers (1988) Effect of cyclodextrins on anthracycline stability in acidic aqueous media (1988) Pharm. Weekblad. S. Ed., vol. 10, 207. Benjamin (1973) Pharmacokinetics and Metabolism of Adriamycin in man, Clin. Pharm. Ther., 14(4) Part 1,592. Benvenuto (1981) Stability & Compatibility of Antitumor Agents in Glass & Plastic Containers, (Dec. 1981), Am. J. Hosp. Pharm., vol. 38, p. 1914-1918. Bernard (1969) "Rubidomycin, A New Agent Against Cancer", pp. ix-181. Bertazzoli (1972) Chronic toxicity of adriamycin: a new antineoplastic antibiotic (1972), Tox. Applied Pharm., vol. 2, pp. 287-301. Blum (1974) Adriamycin: A New Anticancer Drug with Significant Clinical Activity, Annals of Int. Med., 80:249-259. Bogardus (1979) "Solubility of Doxycycline in Aqueous Solutions", (Feb. 1979) vol. 68 (2) J. Pharm. Sci., pp. 188-194. Bohme (1979) "Equropaisches Arzneibuch III, Kommentar, Wissenschaftliche Verlagsgesellschatt mbH Stuggart, p. 654. Boiron (1969)Daunorubicin 330. in the Treatment of Acute Myelocytic Leukemia, The Lancet p.

81.

82.

83.

84.

85.

86.

87. 88.

89.

90.

91.

92.

93.

Bonadonna (1969) Clinical Evaluation of Adriamycin a New Antitumor Antibiotic, Br. Med. J., (3), 503 (August 1969). Bono (1980) "The Preclinical Development of Quelamycin and its Initial Clinical Trials.", Aruthracylines: Current Status and New Development, (1980) Academic Press, pp. 315. Bosanquet (1986) "Stability of Solutions of antineoplastic agents during preparation and storage for in vitro assay", Cancer Chemotherapy and Pharmacology, vol. 17, pp. 1-10. Bouma (1986) Anthracycline Antitumor agents: A review ofphyscicochemical, and stability properties Pharm. Weekblad Sc. Ed., vol. 8, p. 109-133. -5analytical

94.

95.

96.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 7 of 29

97.

Bradner (1977) The Journal of Antibiotics, "Boemic Acid Complex. Biological Characterization of the Antibiotics Marcellomycin and Musettamycin, (Aug. 1977). Brazhnikova (I 973) "Carminomycin, a New Antitumour Anthracycline", Antibiotiki 18:681. Brazhnikova (1974) "Physical and Chemical Characteristics and Structure of Carminomycin, a New Antitumour Antibiotic", J. Antibiot, 27(4):254 (1974). Brazhnikova (1986) Physicochemical Properties of Antitumour Antibiotic Rubomycin produced by Act. Cocruleorubidus (1986) Antibiotki 11:763. Brown (1978)Adriamycin and Related Anthracycline Antibiotics, Prog. Med. Chem. 15:124165. Calendi (1965) On Physico-Chemical Interactions between Daunomycin and Nucleic Acids; Biochem Biophys. Acta., vol. 103:25. Carlin (1968) "Incompatibilities of Parenteral Medications", Pharm. 271. (Jun. 1968) 25 Am. J. Hosp.

98. 99.

100.

101.

102.

103.

104.

Casazza (1977) Tumors and dental ocular abnormalities after treatment of infant rats with adriamycin, (1977) Tumor 63:331. Casazza (1984) Experimental Studies on New Anthracyclines (1984) (Proc. of Int. Symposium on Adriamycin: Ogawa et al. eds.). Cassinelli (1963) "La Daunomicina: Un Nuovo Antibiotico Ad Attivita Citostatica Isolamento E Proprieta (1963) Giorn. Microbial. 11:167. Cersosimo (1986) Epirubicin: A Review of the Pharmacology, Clinical Activity, and Adverse Effects of an Adriamycin Analogue, J. Clin. Onco14(3), 425. Cersosimo (1986) "Possible Strategies for the Formulation of Antineoplastic Drugs", Drug. Dev. Ind. Pharm. vol. 12(7) 1041. Connors (1979) Chemical Stability of Pharmaceuticals--a Handbook for Pharmacists (1979) Wiley, pp. 3-7, 44-63, 74-75. Crom (1987) Pharmacokinetics of Anticancer Drugs in Children, Clin. Pharm. 12:pp. 168213. Crommelin (1983) Preparation and characterization of doxorubicin-containing liposomes. II. Loading capacity, long-term stability and of doxorubicin-bilayer interaction mechanism (1983) Int. J. Phann. vol. 17, p. 135-144. Crommelin (1983) Preparation and characterization ofdoxorubicin-containing lipsomes: I. Influence of liposome charge and pH of hydration medium on loading capacity and particle size, (1983), Int. J. Pharm., vol. 16, pp. 79-92.

105.

106.

107.

108.

109.

110.

111.

112.

-6-

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 8 of 29

113.

Crooke (1977) "A Review ofCarminomycin, USSR", J. Med. 8(5):295.

A New Anthracycline Developed in the

114.

Dalmark (1981) A Fickian Diffusion Transport Process with Features of Transport Catalysis, J. Gen Physiol. 78:349. Daugherty (1981) "Photolytic Destruction of Adriamycin", J. Pharm. Pharmacol. Vol. 33, p. 556. Davignon (1984) Pharmaceutical Aspects of Antitumour Agents (1984) Pharm. Weekbt. 119:1144. De Luca (1984) Pharmaceutics & Pharmacy Practice, pp. 238-243,275-278. DeLuca & Boylan (1984) Pharmaceutical Dosage Forms: Parenteral Medications: vol. 1 (Edited by Avis et al., "Formulation for Small Volume Parenterals" (DeLuca & Boylan). Demorest (1984) Pharmaceutical Dosage Forms: Parenteral Medications: vol. 2 (Edited by Avis et al.,"Formulation for Large Volume Parenterals" (Demorest), pp. 55-63, 68-70, 73-76, 83. Depois (1967) "Isolement D'un nouvel antibiotique doue d'activite antitumorale la rubidomycine (13.057 R.P.), J. Preparation et properties, Arzicial Forsch. 17:934-939. Deprez-de Campanere (1979) Pharmacokinetic, Toxicologic, and Chemotherapeutic Properties of Detorubicin in Mice: A Comparative Study with Daunourubicin and Adriamycin, Cancer Treat. Rep., 63(5):861. Despois (1967) Isolement D'un Nouvel Antibiotique Doue D'Activite Antitumorale: La Rubidomycine (13.057 R.P.) Identite De La Rubidomycine et de La Daunomycine, Path. Biol., vol. 15, pp. 887-891. DeVries (1987) A Phase 1 and Pharmocokinetic Study with 21 day Continuous infusion of Epirubicin., J. Clin. Oncol., (1987), 5(9), 1445-1451. DeVroe (1990) "A Study on the stability of three antineoplastic drugs and on their sorption by i.v. delivery systems and end-line filters", (1990), Int. J. Pharm. vol. 65, p. 49-56. Di Marco (1964) Daunomycin, a New Antibiotic of the Rhodomycin Group, Nature 201: 706. Di Marco (1969) Adriamycin, a New Antibiotic, Antitumour, Activity, Cancer Chem. Reports, part 1, vol. 53, No. 1, p. 33. Di Marco (1972) Activity ofAdriamycin (NSC 123127) and Daunomycin (NSC 82151) Against Mouse Mammary Carcinoma, Cancer Chemother. Rep., part 1, vol. 56(2): 153. Dorr & Fritz (1980) Cancer Chemotherapy Handbook, pps. 388-401, "Doxorubicin".

115.

116.

117. 118.

119.

120.

121.

122.

123.

124.

125.

126.

127.

128.

-7-

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 9 of 29

i29.

Dorr (i979) incompatibilities with Parenteral Anticancer Drugs, The American Journal of intravenous Therapy, Feb./Mar., pp. 42, 45-46, 52. Dozier (1983) Practical Considerations in the Preparation and Administration of Cancer Chemotherapy (Sep. 1983) Am.J. Int. Ther. Clin. Nut., p. 6. Duarte-Karim (1976) Affinity ofadriamycin to phospholipids. A possible explanation for cardiac mirochonorial lesions. (1976) Biochem Biophy. Research Comm., 71(2), p. 658. Dubost (1963) "Un nouvel antibiotique a proprieties cytostatiques: la rubidomycine (1963) C.R. Acad. Sci. Paris, 257, p. 1813-1815. Ducep (1978) "Naphthacene Derivatives", (Feb. 1978), US Patent No. 4,075,328. Duma & Akers (1984) Pharmaceutical Dosage Forms, "Parenteral Medications: vol. 1 (Avis et al. Parenteral Drug Administration: Routes, Precautions, Problems & Complications" (Duma & Akers). Edward (1967) pH: An important Factor in the Compatibility of Additives In Intravenous Therapy (Aug. 1967) vol. 24 Am. J. Hosp. Pharm. 440. Eksborg (1978) "Extraction of Daunorubicin and Doxorubicin and Their Hydroxyl Metabolites: Self-Association in Aqueous Solution", Journal of Pharmaceutical Sciences, vol. 67, No. 6, pp. 782-785, (Jun., 1978). Eksborg (1984) "Liquid Chromatography in Anticancer Drug Research with Special Reference to Anthraquinone Glycosides", Journal of Pharmaceutical and Biomedical Analysis, vol. 2, No. 2, pp. 297-303. Falbe (1992) Rompp Chemic Lexikon, New York, 9th edition, Georg Thieme Verlag Stuttgart, "Buffers", pp. 3677-3678. Falk (1979) Mutagenicity in Urine of Nurses Handling Cytostatic Drugs, The Lancet, Jun. 9, 1979, pp. 1250-1251. Fandrich (1981) "Analysis of Carminomycin in Human Serum by Fluorometric HighPerformance Liquid Chromatography", J. Chromatogr. 223 115 (1981). Fischer (1989) The Cancer Chemotherapy Handbook 3rd edition, (1989), pp. 17-19, 65-69, 82-89. Flamberg (1986) Manufacturing Considerations in the Lyophilization of Parenteral Products Pharm. Manuf.3:29-31. Flora (1980) "The loss of Paraben Preservatives During Freeze Drying", J. Pharm. Pharmacol, Vol. 32, pp. 577-578. Florence & Atwood (1981) "Physiochemical Principles of Pharmacy" MacMillan Press, London, p. 475. -8-

130.

131.

132.

133. 134.

135.

136.

137.

138.

139.

140.

141.

142.

143.

144.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 10 of 29

i45.

Fynn (1980) "Buffers-pH Control within Pharmaceutical Systems", (Mar.-Apr. 1980) vol. 34, (2) J. Parenteral Drug Assoc. 139. Gaj (1984) Evaluation of growth in Five Microorganisms in Doxorubicin and Floxuridine Media, Pharm. Manuf, p. 50. Gaj (1984) Compatibility of Doxorubicin Hydrochloride and Vinblastine Sulfate--The Stability of a Solution Stored in Conned® Reservoir Bags or Monoject ® Plastic Syringes (May, 1984) Am. J. IV Ther. Clin. Nut., p. 8. Gamick (198i) Phase 1 Trial of Long Term Continuous Adriamycin Administration, Proc. Am. Soc. Clin. Oncol., C-106: p. 359, (Mar. 1981). Gamick (1983) "Clinical Evaluation of Long-Term, Continuous Infusion Doxorubicin" Cancer Treatment Reports, Vol. 67, pp. 133-142. Gatti (1986) "Anthracyclinglycoside enthaltende pharmazeutische Praparate, (April 1986), German Patent No. 35 36 896. Gatti (1987) "Pharmaceutical Compositions Containing Anthracycline Glycosides, (Jun. 1987), US Patent No. 4,675,311. Gatti (1987) "Injectable stabilised solutions containing an antitumor anthracycline glycoside, (February 1987), United Kingdom Patent No. 2 178 311. Gatti (1990) "injectable Ready-to-Use Solutions Containing an Antitumor Anthracyclien Glycoside, US Patent No. 4,946,831. Gatti (1991) "injectable Ready-to-Use Solutions Containing an Antitumor Anthracycline Gylcoside", Canadian Patent Application No. 1 291 037. Goormagtigh (1984) Anthracycline Glycoside-Membrane Acta: 271-288. Interactions, Biochem. Biophys.

146.

147.

148.

149.

150.

151.

152.

153.

154.

155.

156.

Gordon (1972) The Art and Science of Contemporary Drug Development, Prog. Drug. Res. 16:194. Gosalvez (1978) "Quelamycin, a New Derivative of Adriamycin with Several Possible Therapeutic Advantages", Eur. J. Cancer 14:1185. Graffiaer (1985) Preformulation Studies in a Drug Development Program for Tablet Formulations, J. Pharm. Sci. 74(1) 16. Greene (1979) "Stability ofcicplatin in aqueous solution", Am J. Hosp. Pharm. 36:38. Greidanus (1988) Continuous Infusion of Low-dose Doxorubicin, Epirubicin and Mitoxantrone, Cancer Chemotherapy: A Review, (1988)Pharrn. Weekblad. Sci. Ed., vol. 10, p. 237.

157.

158.

159. 160.

-9-

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 11 of 29

i61.

Gupta (i987) influence of Stabilization Temperature on the Entrapment of Adriamycin, Albumin Microspheres Drug. Dev. Int. Pharm., vol. 13, No. 8, pp. 1471-1482. Gupta (1988) investigation of the Stability of Doxorubicin Hydrochloride using Factorial Design, Drug Development & industrial Pharmacy, (1988) vol. 14(12) p. 1657-1671. Gustavasson (1986) "Fluid Transfer System, (Jan. 1986), US Patent No. 4,564,054. Gutteridge and Wilkens (1983) "Doxorubicin Degradation: Changes in Activity Compared by Bacterial Growth Inhibition and Free Radical-Dependent Damage to Deoxyribose", J. Biological Standardization, Vol. 11, pp. 359-364. Habib (1989) Photostabilization ofdoxorubicin Hydrochloride with Radioprotective and Photoprotective Agents: Potential Mechanism for Enhancing Chemotherapy during Radiotherapy (Nov.-Dec. 1989) 43 J. Parenteral Science & Technology, vol. 43, No. 6, p. 254, (Nov.-Dec,. 1989). Haneke (1981) Quanititation of Daunorubicin, Doxorubicin, and their Aglycones by IonPair Reversed-Phase Chromarography, Journal of Pharmaceutical Science vol. 70 No. 10, (October 1981), pps. 1112 - 1115. Harris (1978) "Novel Onium Surfactants, US Patent No. 4,093,663. Harris (1995) "Quantitive Chemical Analysis", 4th Edition, WH Freeman and Companyp. 23, p. 240. Henry (1976) "Adriamycin", Cancer Chemotherapy, American Cancer Society Symposium Series, pp. 15-57. Henry (1978) "5-Iminodaunomycin, US Patent No. 4,109,076. Herrick (1985) Monetary incentive for pharmacists to control drug costs; (Jul. 1985) vol. 42, Am. J. Hosp. Pharm. p. 1527-1532. "Ho & Shah Cartensen "Kinetic pH Profiles", pp. 59-121,380-385. Ho (1971) Prediction of Pharmaceutical Stability of Parenteral Solutions III (Feb. 1971) vol. 5, Drug, int. Clin. Pharm., pp. 47-50. Hoffman (1979) "Stability of Refrigerated and Frozen Solutions of Doxorubicin Hydrochloride". American Journal of Hospital Pharmacy, vol. 36, pp. 1536-1538. Horn (1981) Intravesical chemotherapy in a controlled trial with thio-tepa versus doxorubicin hydrochloride, J. Urol., 125:652. Hurteloup (1989) Phase II Trial of Idarubicin (4-Demethoxydaunorubicin) Breast Cancer, Eur. J. Cancer Clin. Oncol. 25(3)423. in Advanced

162.

163. 164.

165.

166.

167. 168.

169.

170. 171.

172. 173.

174.

175.

176.

177.

Israel (1977) N-Trifluoroacetyladriamycin-14- Alkanoates and Therapeutic Compositions Containing Same, Jul. 1977, US Patent No. 4,035,566. -10-

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 12 of 29

i 78.

Israel (1982) "Adriamycin Analogues: Preparation and Biological Evaulation of Some NPerfluoroacyl Analogues of Daunorubicin, Adriamycin, and N-(trifluoroacetyl) adriamycin 14-valerate and their 9, 10-Anhydro Derivatives", J. Med. Chem. 25:187. Jacobi (1980) "Studies on the intravesical action of topically administered G311-doxorubicin hydrochloride in men: plasma uptake and tumor penetration", J. Urol. 124:34. Jaenke (1976) "Delayed and progressive myocardial lesions after adriamycin administration in the rabbit", (1976) Cancer Res. vol. 36, pp. 2958-2966. Janssen (1985) "Doxorubicin Decomposition on Storage. Effect ofpH, Type of Buffer and Liposome Encapsulation", International Journal of Pharmaceutics, vol. 23, No. 1, pp. 1-11, Jan., 1985. Janssen (1985) Doxorubicin decomposition on storage. Effect ofpH., type of buffer and liposome encapsulation, (1985) Chemical Abstracts, vol. 102, No. 209226k. Jonkman-de Vries (1994) "Pharmaceutical Development of a Parental Lyophilized Formulation of the Novel Indoloquinone Antitumor Agent EO9", Cancer Chemotherapy and Pharmacology. Kalmas (1982) "Solubility Aspects in Parenteral Formulation" (May/Jun. 1982), Ind. J. Hosp. Pharm. 94, pp. 94-96, 98, Table I. Kaltofen (1994) "Tabellenbuch Chemic, 12th edition, pp. 172, 181. Kaniewska (1977) "A study of decomposition of Adriamycin", Pharmacia Polska, Vol. 9, 539-542. Kaniewska (1978) "Study of the Decomposition of Adriamycin", Chemical Abstracts, vol. 88, p. 396, No. 197, p. 396, No. 197526X. Kano (1984) Electrochemical Properties of Adriamycin Adsorbed on a Mercury Electrode Surface Bull. Chem. Soc. Japan. Kano (1985) The Effects of the pH and the Temperature on the Oxidation-reduction Properties of Adriamycin Adsorbed on a Mercury Electrode Surface Bull Chem. Soc. Japan, Feb, 1985, vol. 58, pp. 424-428. Kaplan et al. (1982) Phase I Trial of 4- Demethoxydaunorubicin Clin. Cancer Oncol., 18(12) 1303. with single i.v. doses, Eur. J.

179.

180.

181.

182.

183.

184.

185. 186.

187.

188.

189.

190.

191.

Karlsen (1983) "Stability of Cytotoxic Intravenous Solutions Subjected to Freeze-Thaw Treatment", Nor. Pharm Acta, vol. 45, pp. 61-67. Karlsen (1983) "Stability ofcytotoxic intravenous solutions subjected to freeze-thaw treatment", Chemical Abstracts, vol. 99, No. 146022, p. 374. Kawahara (1978) Stabilized S-Adenosyl-L-Methionine No. 4,109,079. -11Preparations, Aug. 1978, US Patent

192.

193.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 13 of 29

194.

Ketchmun (1981) "Cost Benefit and Stability Study of Doxorubicin Following Reconstitution", American Journal of Intravenous Therapy and Clinical Nutrition, vol. 8, No. 4, pp. 15-18, 1981. Keusters (1986) Stability of solutions ofdoxorubicin and epirubicin in plastic mini bags for intravesical use atter storage at -20.degree. C. and thawing by microwave radiation. (1986) Pharm. Weekblad Sc.Ed., vol. 8 p. 144. King (1982) Statistical Prediction of Drug Stability Based on Non-Linear Parameter Extension, J. Pharm. Sci. 73(5):657-662. Kirschenbaum (1976) Stability of injectable medications after reconstitution, Am. J. Hosp. Pharm.: 33:767-790. Kjeld Ilver (1971) Almen Galenisk Farmaci--Forel sningsnoter, Dansk Farmaceutforenings Forlag, (1971), pp. 132-136. Knoop (1988) The Pharmaceutical Drug Development Process: An Overview (1988) 22 Drug. Inf. J. 259. Koonsvitsky (1986)Non-Yellowing Patent No. 1 203 482. Pharmaceutical Composition, April 1986 Canadian

195.

196.

197.

198.

199.

200.

201.

Kovach (1979) Phase I Trial & Assay ofRubidozone (NSC 164011) in Patients with Advanced Solid Tumors, (Mar. 1979) Cancer Research vol. 39, p. 823. Kramer & Flynn (1972) "Solubility of Organic Hydrochlorides", (Dec. 1972) vol. 61 (12), J. Pharm. Sci. 1896. Gjelstrup (1983) Almen Farmaci II, "Parenteral Administration" Dansk Farmaceutforenings Forlag, Kobenhavn, pp. 404-408, 440, 442-443, 447, 451. (Kristensen & Moller 1983, pp. 408, 442, 447). Lachman (1986) The Theory & Practice of Industrial Pharmacy (Lachman et al.), 3rd Ed. 1986, p. 191, et seq., pp. 191-194, 195-196, 459-460, 471-472, 477-478, 764-765. Langone (1975) Adriamycin and Metabolites: Separation by High Pressure Liquid Chromatography and Qunitation by Radioimmunossay, Biochem Med. 12:283 (1975). Lankelma (1982) "Plasma Concentrations of Canninomycin and Canninomycinol in Man, Measured in High Pressure Liquid Chromatography", Eur. J. Cancer olin. Oncol. 18 (4):363. Lassila (1980) Immune Function in Nurses Handling cytostatic Drugs, The Lancet, (Aug. 30, 1980), p. 482. Legha (1982) Reduction ofDoxorubicin Cardiotoxicity by Prolonged Continuous Intravenous Infusion, Ann. Int. Med., vol. 96, No. 2, p. 133. Legha (1990) "The Anthracyclines and Mitoxantrone", Cancer Chemotheraphy by Infusion 2nd edition (Lokich et.) Precept Press. -12-

J

202.

203.

204.

205.

206.

207.

208.

209.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 14 of 29

210.

Lentner, (Editor i980) Geigy Scientific Tables, vol. 3, Physical Chemistry Composition of Blood Hematology Somatometric Data, 8th revised and enlarged edition, Edited by C. Lentner, pp. 54-60. Lin (1969) "Photochemical Considerations of Parenteral Products", Bull. Par. Drug. Assoc. 23 (4):149. Lin (1968) Kinetic Study in Formulation Investigation of New Compounds (1968). Lin (1969) "Parenteral Formulations I. Comparisons of Accelarated Stability Data with ShelfLife Studies", Bull. Par. Drug Assoc. 23(6):269. Lin (1970) "Parenteral Formulations II. A Stability Testing Program for Parenteral Products", Bull. Par. Drug. Assoc. 24(2):83. Lokich (1983) "Constant Infusion Schedule for Adriamycin: A Phase I-II Clinical Trial of a 30-Day Schedule by Ambulatory Pump Delivery System", J. Clin. Oncol., vol. 1 (1): 24-28. Lund (1994) The Pharmaceutical Codex 12th Ed. (Lund), (1994), p. 201. Maral (1967) "Etude Toxicologique et activite Antitumorale Experimentale de la Rubidomycine (13.057 R.P.) Path. Biol., vol. 15, No. 19-20, pp. 903-908 (1967). "Maral (1967) "Un nouvel antibiotique doue D'activite Antitumorale: La Rubidomycine (13.057 R.P.), II: Activite antitumorale experimentale Arzncimittel Forsch 17:934. Martindale (1982) "Doxorubicin Hydrochloride"", The Extra Pharmacopoeia (1982), pp. 205-208. Martindale (1989) "Mitotone", The Pharmaceutical Press, 29th Edition, London, Entry 1852x, pp. 643-645. Masuike (1984) "Determination of Adriamycin and its Metabolities in Biological Samples Using High Performance Liquid Chromatography. I. Analysis of Serum and Plasma by Direct Injection Method. II. Analysis of Tissues by Extraction Method", Pharmaceutical Society of Japan Journal, vol. 104, No. 6, pp. 614-623, Jun., 1984. Masuike (1984) Determination of Adriamycin and its Metabolities in Biological samples using high performance liquid chromatography Chemical Abstracts, vol. 101, p. 5. McEvoy (1984) AHFS Drug Information 84, p. 251-254. Mendenhall (1984) Stability of Parenterals (1984) Drugs Dev. Ind. Pharm. 10(8-9) pp. 12971342. Menozzi (1972) "Self-Association of Doxorubicin and Related Compounds in Aqueous Solution", Journal of Pharmaceutical Sciences, vol. 73, No. 6, pp. 766-770,. International Symposium on Adriamycin, pp. 9-22.

211.

212. 213.

214.

215.

216. 217.

218.

219.

220.

221.

222.

223. 224.

225.

-13-

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 15 of 29

226.

Merck Index (i983) i0th edition (i983), Edited by M. Windholz, et al. ), p. 499, entry 3,435 and 3,436. Merck Index (1989) "Aclacinymycins", S. Budavari, Ed. Merck & Co., Inc. Rahway, NJ, No. 108, p. 17. Merck Index (1996) Mitoxantrone, 12th Edition, Entry 6303, p. 1064. Miller (1987) "Clinical Pharmacology and Toxocology of 4.increment.Otetrahydropyranyladriamycin", Mar. 1, 1987, Cancer Research 47:1461-1465. Miyazaki (1981) "Precaution on Use of Hydrochloride Salts in Pharmaceutical Formulation", (Jun. 1981) 70(6) J. Pharm. Sci., pp. 594-596. Mollica (1978) Stability of Pharmaceuticals. J. Pharm. Sci. 67(4):443-465. Monkhouse (1985) Dosage Forms For Clinical Trials (1985) 11 (9 & 10) Drug. Dev. Ind. Phann. 1729. Mori (1980) Physicochemical Properties and Stability ofAclacinomycin (1980), Jpn. J. Antibiot 33:618. A Hydrochloride,

227.

228. 229.

230.

231. 232.

233.

234.

Moro (1988) "Pharmaceutical Compositions Consisting or Consisting Essentially of FreezeDried Drug-Carrying Liposomes, (May 1988), US Patent No. 4,746,516. Mortimer (1980) Chemi, 3rd Edition, Gerog Thieme Verlag Stuttgart, New York, pp. 490494. Mosher (1984) "Derivatives of daunorubicin and doxorubicin, (February, 1984), United Kingdom Patent No. 2 124 224. Motola (1984) Pharmaceutical Dosage Forms: Parenteral Medications: vol. 1 (Avis et al., 1984), "Preformulation Research of Parenteral Medications" (Motola & Agharkar). Motola & Agharkar (1984) Pharmaceutical Dosage Forms: Parenteral Medications: vol. 1 (Edited by Avis et al. 1984) "Biopharmaceutics of Injectable Medication". Naff (1982) Anthracycline Antibiotics, "Anthracyclines in the National Cancer Institute Program, Hassan S. E1Khadam, editor, Academic Press, pp. 1-57. Nettleton (1977) "New Antitumour Antibiotics: Musettamycin and Marcellomycin from Bohemic Acid Complex", 30(6) J. Antibiotics 525. Nettleton (1977) "Antibiotic Compounds marcellomycin and Musettamycin", US Patent No. 4,039,736. Newton (1978) "Physicochemical Determinants of Incompatibility and Instability in Injectable Drug Solutions and Admixtures", 35 Am. J. Hosp. Pharm., pp. 1213-1222. Newton (1987) Estimating shelf-life of drags in solution. Am. J. Hosp. Pharm. 44:1633. - 14-

235.

236.

237.

238.

239.

240.

241.

242.

243.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 16 of 29

244.

Niebergall (1990) Remington's Pharmaceutical Sciences, 18th edition, Ch. 17 Ionic Souluitons & Electolytic Equilibria. Nijker (1990) Carboplatin Composition, (December 1990) European Patent No. 0 401 896. Nikula (1984) "Chromosone Aberrations in Lymphocytes of Nurses Handling Cytostatic Agents", Scand. J. Work Environ. Health, Vol. 10, pp. 71-74. Noseworthy (1977) Stable Aqueous Solutions of Doxycycline, (Feb. 1977) Canadian Patent No. 1 005 760. Oki (1975) "New Antitumour Antibiotics, Aclacinomycins A and B", J. Antibiot, 28(10):830. Oki (1979) "Antitumour Anthracycline Antibiotics, Aclacinomycin A and Analogues: I. Taxonomy, Production, Isolation and Physicochemical Properties", J. Antibiot 32(8):791. Oki (1980) "Aclacinomycin A Anthracyclines: Current Status and New Developments", Academic Press. p. 323. Oppici (1980) Process of Purifying Anthracyclinonic Gylcosides by Selective Adsorption of Resins, May 1980 Canadian Patent No. 1 204 738. Ozturk (1988) Dissolution oflonizable Drugs in Buffered and Unbuffered Solutions (1988) 5(5) Pharm. Res. 272. Parrott & Saski (1965) Experimental Pharmaceutical Technology, 2nd Ed. pp. 132-134, 149-. 154. Parrott (1965) "Formulation ofParenterals", Durg and Cosmetic Industry, (March 1965). Patelli (1977) Daunomycin Analogues, Their Preparation and Use, (Sept. 1977), US Patent No. 4,046,878. Patelli (1978) "Process for the Preparation of Analogues of Daunomycin, (Oct. 1978), Canadian Patent No. 1 041 488. Pavlik (1984) Stability of Doxorubicin in Relation to Chemosensitivity Determinations: Loss of Lethality and Retention of Antiproliferative Activity, Cancer Investigation 2 (6), 449-458. Penco (1978) "Anthracycline Glycosides, Their Preparation and Use, (Jan. 10, 1978) B1841978, US Patent No. 4,067,969. Penco (1982) "4-Demethoxy-4 Deoxydoxorubicin, (Apr. 1982), US Patent No. 4,325,947. Poochikian (1981) Stability of anthracycline antitumor agents in four infusion fluids Chemical Abstracts, vol. 94.214489f. Poochikian (1981) "Stability ofAnthracycline Antitumor Agents in Four Infusion Fluids", American Journal of Hospital Pharmacy, vol. 38, pp. 483-486, (Apr., 1981). -15-

245. 246.

247.

248. 249.

250.

251.

252.

253.

254. 255.

256.

257.

258.

259. 260.

261.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 17 of 29

262.

Pope (1980) Accelerated Stability Testing for Prediction of Drug Product Stability--First of a Two-Part Article (Nov., 1980) D & CI 54, pp. 54, 56, 59, 60, 62, 116. Pope (1980) Accelerated Stability Testing for Prediction of Drug Product Stability--Second of a Two-Part Article (Dec., 1980) D & CI 48, pp. 48, 50, 55, 56, 58, 60, 62, 64-66, 110, 112-116. Rees (1973) Physico-Mechanical Pre-Formulation Studies 112 Boll. Chim. Farm. 216. Reich (1980) "Carminomycin, Arptheacyclines: Current Status and New Developments", (J. Cooke et al., eds.) Academic Press, p. 295. Reich (1980) "Marcellomycin Anthracyclines: Current Status and New Developments", (1980) Academic Press, p. 343. Rhone-Poulenc (1995) "Improvements in or relatingto Antibiotics and their preparation, (March 1995), United Kingdom Patent No. 985,598. Riley (1981) Review of New Drugs--1980, U. S. Pharm. 33 (Feb. 1981). Rosenkrantz (1982) "Stabilized Netilmicin Formulations, (Apr. 1982), US Patent No. 4,327,087. Rosenkratz (1982) Stabilized Antibiotic Formulations, (August 1982) Canadian Patent No. 1 129 344. Rote Liste (1984) Preparation No. 85 031, "Adriblastin". Rozencweig, "Preliminary Experience with Marcellomycin: Pre-Clinical and Clinical Aspects", p. 5499-561. Rubino (1987) "The Effects of Cosolvents on the Action of Pharmaceutical Buffers", (1987) 41 (2) J. Paren. Sci. Tech. 45. Salmon (1984) Antitumour Activity of Esorubicin in Human Tumour Clonogenic Assay with Comparison to Dexorubicin, J. Clin. Oncol. 2(4):282. Samuels (1971) "Daunorubicin Therapy in Advanced Neuroblastoma", (Apr. 1971), Cancer 27:831-834 Sandell (1967) Galenisk Farmaci, 2nd edition, Stockholm (1967). Savlov (1981) "Comparison of Doxorubicin with Cycloleucine in the treatment of Sarcomas", Cancer Treatment Sciences, Vol. 65, pp. 21-27. Schumacher (1966) Bulk Compounding Technology, Am. J. Hosp. Pharm. Vol. 23(11), (Nov. 1966), p. 628-629. Singh (1980) Effect of Solvents and Additives on the Stability of Drugs, Pharma Times 13. -16-

263.

264. 265.

266.

267.

268. 269.

270.

271. 272.

273.

274.

275.

276. 277.

278.

279.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 18 of 29

280.

Skovsgaard (1975) Adrimycin, an Antitumor Antibiotic: A Review with Special Reference to Daunomycin, Dan. Med. Bull 22(2):62-73. Snyder (editor) (1992) The Interpharm International Dictionary of Biotechnology and Pharmac_uticl Manufacturing edited by Dean E. Snyder, Publisher Buffalo Grove, IL, Interpharm Press, Inc.Speth Clinical Pharmacokinetics of Doxorubicin, Clin. Pharm., Vol. 15, pp. 15-31. Stella (1986) Chemical and Physical Bases Determining the Instability and Incompatibility of Formulated Injectable Drugs 40(4) J. Paren. Sci. Tech. 142. Stjernstrom (1978) Studies on the stability and compatibility of drugs in infusion fluids, Acta Pharm Spec. 15:33. Sturgeon (1977) Electronic Absorption Spectra and Protolytic Equlibria of Doxorubicin: Direct Spectrophotometric Determination ofMicroconstants, J. Pharm. Sci. 66(7):958. Suarato (1984) 4-Iododerivatives of Anthracycline Glycosides, Mar. 1984, US Patent No. 4,438,105. Suarato (1990) Antitumor Anthracyclines, The Chemistry of Antiumour Agents (Wilman, ed.). Svend Aage (1959) Troek of den flaeniske farmaci, Store Nordiske Videnskabsboghandel, p.220. Swinyard, EA (1980)"Introduction of New Drugs", Pharmaceutical Sciences, Mack Publishing Co., Easton, PA, pp. 1365-1376. Tan (1967) Daunomycin, an Anti-Tumor Antibiotic, in the Treatment of Neoplastic Disease, (Mar. 1967), Cancer 20:333-353. Tavoloni (1980) Photolytic Degradation of Adriamycin (1980) Comm. J. Pharm. Pharmacol. vol., 32, p. 860. Tencheva (1979) "New Approach of the Extrapolation Procedure in the Determination of Acid-Base Constants of Poorly Soluble Pharmaceuticals", (1979); Arzneim Forsch/Drug Res. 29 (II) #9, pp. 1331-1334. Tomlinson (1982) Concomitant Adsorption and Stability of Sonic Anthracycline Antibiotics (Oct. 1982) 71 (10) Journal of Pharmaceutical Sciences pp. 1121-1125. Tong (1979) "5-Iminodaunorubicin: Reduced Cardiotoxic Properties in an Antitumour Anthracycline", J. Med. Chem. 22(1): 36. Trissel Handbook on Injectable Drugs, 3rd Edition, p. 131-132, "Doxorubicin HCL". Trissel (1978) Investigational Drug Information Drug Intell. Clin. Pharm vol. 12, p. 404-406. Trissel (1980) Handbook on Injectable Drugs, 5th Edition, pp. 222-223; 259-264 and p. 707. -17-

281.

282.

283.

284.

285.

286.

287.

288.

289.

290.

291.

292.

293.

294. 295. 296.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 19 of 29

297. 298.

Trissei (1980) Handbook on Injectable Drugs, 2nd Edition, p. 196, 562. Trissel (1983) "Investigational Drugs" Handbook on Injectable Drugs. 3rd Edition American Society of Hospital Pharmacists. Trissel (1986) A Handbook on Injectable Drugs 4th Edition, p. 215-217. Turowski (1991) "Visual Compatability of Idarubicin Hydrochloride with selected drugs during simulated Y-site injection", (Oct. 1991), Ans. J. Hosp. Pharm., vol. 48, p. 2181. Umezawa (1979) "TetrahydropyTanyl Derivatives of Daunomycin and Adriamycin", J. Antibiot 32(10): 1082. Valentini (1986) Safety Device for Connection of a Syringe with the Mouth or Opening of Bottle Containing a Drug or a Small Tube for Drug Delivery from the Syringe. Mar. 1986, US Patent No. 4,576,211. Valentini (1988) Device for Connecting One End of a Liquid Medicament Delivery Cannula to an Appartus for Connecting a Syringe to a Vial Containing the Medicament, Nov. 1988, US Patent No. 4,786,281. Van Bommel (1984) Stability of Doxorubicin-Liposomes on Storage: as an Aqueous Dispersion, Frozen or Freeze dried (1984), Int. J. Pharm., vol. 22, pp. 299-310. Vigevani (1980) "Doxorubicin", Analytical Profiles of Drug Substances, vol. 9, pp. 245-274. Vilallonga (1978) Interaction of Doxorubicin with Phospholipid Monolayers, J. Pharm. Sci. 67(6), p. 773. Vogelzang (1984) Continuous Doxorubicin Infusion (CDI) Using an Implanted Lithium Battery-Powered Drug Administration Device System, Proc. Am.Soc. Clin.Uncol. C1030: p. 263, (Mar. 1984). Vogelzang (1985) Phase I Trial of an Implanted Battery-Powered, Programmable Drug Delivery System for Continuous Doxorubicin Administration, Journal of Clinical Oncology, vol. 3, No. 3, pp. 407-414. Vogenberg (1983) Stability Guidelines for Routinely Refrigerated Drug Products, Am. J. Hosp. Pharm. 40:101-102. Von Hoff (I 978) Daunomycin: An Anthracycline Antibiotic Effective in Acute Leukemia, Adv. Pharm. Chemo. 15:1-51. Walker (1991) Doxorubicin Stability in Syringes and Glass Vials and Evaluation of Chemical Contamination, Can J. Hosp. Pharm. 44(2): 71. Waller (1986) Documenting i.v. admixture product waste (Aug. 1986) vol. 43, Am. J. Hosp. Pharm. 1914-1915.

299. 300.

301.

302.

303.

304.

305. 306.

307.

308.

309.

310.

311.

312.

-18-

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 20 of 29

313.

Wang (1971) Therapeutic effect and toxicity of adriamycin in patients with neoplastic disease, (1971) Cancer, 28, p. 837.

314.

Wang & Kowal (1980) "Review of Excipients and pH's for Parenteral Products Used in the United States," Journal of the Parenteral Drug Association 14(6):452-462. Wasserman (1983) "Kinetics of the Acid-Catalyzed Hydrolysis of Doxorubicin", International Journal ofPharmaceutics, vol. 14, pp. 73-78. Watson (1976) Rapid analytic method for adriamycin and metabolites in human plasma by a thin tim fluorescence scanner (1976) Cancer Treat. Rep., vol. 60, No. 11, p. 1611. Weenen (1983) Pharmacokinetics of 4-Epi-doxorubicin in Man, lnvesi. New Drugs, vol. 1, p. 59. Weiss (1986) "Vented Syringe Adapter Assembly, (May 1986), US Patent No. 4,588,403Williams Photoinactivation of Anthracyclines (1981) Photochemistry & Photobiology, vol. 34, p. 131-134. Williams (1984) The Lyophilization of Pharmaceuticals: A Literature Review (1984), 38(2) J. Paren. Sci. Tech. 48-59. Williams (1990) Stabillity & Compatibility of Admixtures of Antineoplastic Drugs, Cancer Chemotherapyhy by Infusion. 2.sup.nd Edition (Lukich et.) (1990) Precept Press. Williamson (1980) "Doxorubicin Hydrochloride-Aluminum Pharmacy, Vol. 40, p. 214. Interaction", Am. J. Hospital

315.

316.

317.

318.

319.

320.

321.

322.

Windheuser (1963) "The Effect of Buffers on Parenteral Solutions", (Sep./Oct. 1963), vol. 17(5), Bull Parenteral Drug Assoc. Wood (1979) "Novel N-benzyl anthracyclines and pharmaceutical compositions containing them, (May 1979), United Kingdom Patent No. 2 007 645. Wood (1990) Stability ofDoxorubicin, Daunorubicin and Epirubxcin in Plastic Syringes and Minibags (1990) J. Clin. Pharm. Therapeutics vol. 15. p. 279-289. Wu (1981) "N-Benzyl Anthracyclines,( Feb. 1981), US Patent No. 4,250,303. Wu (1979) "N-Benzyl Anthracyclines, (Dec. 1979), US Patent No. 4,177,264. Yanagawa (1983) Stability and Releasibility of Adriamycin Ointment. Yee (1981) Adriamycin: A Brief Review (Apr., 1981) Am. J. Int. Ther. Clin Nut. pp. 7-12. Young (1981) The Anthracycline Antineoplastic Drugs vol. 305(3) New England J. Med pp. 139-153. Yuksel (1994) Determination of Cettriaxone in Aqueous Humour and Serum Samples by Differrential-pulse Adsorptive Stripping Voltammetry, Analyst, vol. 119, pp. 1575-1577. -19-

323.

324.

325. 326. 327. 328. 329.

330.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 21 of 29

33 i.

Zelinski (1977) "Coupling or Alkali Metal-Terminated Polymers, (Aug. 1977), US Patent No. 4,039, 633. Zellmer (1975) "Solving Problems with Large-Volume Parenterals, 1: Pharmacist Responsibility for Compounding Intravenous Admixtures", Am. J. Hosp. Pharm. 32:255. Zoglio (1968) Preformulation Stability Testing of Parenteral Products. The Guidelines for Examination for Each Industrial Field, Chapter "Medicament", 4. NCI Investigational Drugs Pharmaceutical Data 1982, pp. 48-50, 130-133, 148-151. NCI Investigational Drugs Pharmaceutical Data 1983, pp. 52-54, 148-151. NCI Investigational Drugs Pharmaceutical Data 1984, pp. 51-53, 134-137, 161-162. NCI Investigational Drugs Pharmaceutical Data 1985, pp. 46-48, 124-127. Benjamin R.S. 1974 Cancer Chemotherapy Reports 58:271-273. Bachur N.R. et al. 1970 Cancer Chemotherapy Reports 54:89-94. Franco R. et al. 1984 Intl. J. Cell Cloning 2:2-8. NL Patent No. 8502869, "Pharmaceutical preparations, containing anthracycline glycosides, and a method of preparing them." AHFS Drug Information 1990, p. 504-507. Lundgren PG et al. J. Clin. Hosp-Pharm. 1980. 5:279-297. Nakano M. (1968) J. Pharm Sci. 57:1865 Webb JW (1969) Am. J. Hosp. Pharm. 26:31-35. Horvath et al. Ann Immunol Hung. 1973;17:265-8. Pizzomo, G.; Trave, F.; Mazzoni, A.; Russello, O.; Nicolin, A. J. Liquid Chromat. (1985), 8(14), 2557-66. Couvreur, P.; Kante, B.; Roland, M.; Guiot, P.; Bauduin, P.; Speiser, P., J. Pharm. Pharmacol. (1979), 31(5), 331-2. Zweig, J. I.; Kabakow, B., J. Am. Med. Assoc., (1978) Vol. 239, p. 2116. D'Arcy P.F., Pharm. Int'l, (1985) 6/3 (59). DiBella N.J.; Garfield D.; Fink K.; et al., Oncology, (1984) 41/1 (1-3). Nishio M.; Kuroda A.; Suzuki M.; et al., Journal of Antibiotics, (1983) 36/7 (761-769). - 20 -

332.

333. 334. 335. 336. 337. 338. 339. 340. 341. 342.

343. 344. 345. 346. 347. 348.

349.

350. 351. 352. 353.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 22 of 29

354. 355. 356.

Collinsworth W., Clinical Chem., (1980) Vol. 26, No. 7, pp. 1047. Kimura, Yoshikazu; Suzuki, Michiyo; Terashima, Shiro, Chem.Lett. (1984) 2113-2116. Vigevani, Aristide; Ballabio, Marzia; Gandini, Elena; Penco, Sergio, Magn.Reson.Chem., 23(5), (1985) 344-352. Penco, Sergio; Cassinelli, Giuseppe; Vigevani, Aristide; Zini, Pierangelo; Rivola, Giovanni; Arcamone, Federico, Gazz.Chim.Ital. 115(3), (1985) 195-198. Israel, Mervyn; Potti, Gopalakrishnan, J.Med.Chem., 25(2), (1982) 187-191. Smith et al., J. Org. Chem. 42, (1977) 3653, 3658. Moshtev, Raphail V.; Khristova, Nadya Corrosion Science (1967), 7(5), 255-64. Matson SW; Fay PJ; Bambara RA Biochemistry, (1980) 19 (10) 2089-2096. Barr RD; Sertic J. Br J Cancer, (1981) 44 (2) 267-269. Kimura N T; Kanematsu T; Baba T. Gann, (1974) 65 (6) 513-522. Mitchell ID; Dixon PA; Gilbert PJ; White DJ Mutation Research, (1980) (79) 91-105. Wuest GP. Advan Antimicrob Antineoplastic Chemother Proc Int Congr Chemother, (1972) (2) 395-397. Li-Ying Yang and Benjamin Drewinko, Cancer Research 45, 1511-1515 April 1985. Edward M. Acton, George L. Tong, Carol W. Mosher, and Richard L. Wolgemuth, J. Med. Chem. 1984, 27, 638-645. Benjamin Drewinko, Li-Ying Yang, Barthel Barlogie, and Jose M. Trujillo, Cancer Research 43, 2648-2653, June 1983. Alvin N. Kotake, Nicholas J. Vogelzang, Richard A. Larson and Nick Choporis, Journal of Chromatography, 337 (1985) 194-200. Carol W. Mosher, Helen Y. Wu, Allan N. Fujiwara, and Edward M. Acton, J. Med. Chem. 1982, 25, 18-24. Sidney Weinhouse, Margaret Foti, Cancer Research, Inc. Vol. 12: (1971). Akiko Shimizu, Masaaki Mori, Tadashi Kawasaki, Byoin Yakugaku Vol. 11 no. 6:495-511 (1985). Masanori Iwata, Kozo Takayama, Yoshiharu Machida, Susumu Ito, Satoru Shimizu, Takashi Suda, Hiroshi Masuda, Akihiko Matsumoto Tsuneji Nagai, Yakuzaigaku Vol. 45:71-8 (1985).

357.

358. 359. 360. 361. 362. 363. 364. 365.

366. 367.

368.

369.

370.

371. 372.

373.

-21 -

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 23 of 29

374. 375. 376.

C.T. Plucker, Kingdom of Belgium, No. 632.391 (1963). Myhr K., Acta Anaesthesiologica Scandinavica, (1985) 29/Suppl. 82, 71-75. T. Vietti; F. Valeriote; J. Hudson; V. Averhart, Proceedings of the American Association for Cancer Research (1973) Vol. 14, 24. T. Vietti et al., J. Natl. Cancer Inst. (1981) 67:1283-9. T. Vietti et al., J. Natl. Cancer Inst. (1980) 64:801-5. T. Vietti et al., Cancer Res. (1972) 32:1496-1500. R. Franco, T. Miller, T. Kratt, M. Popp, O. Martelo, International Journal of Cell Cloning (1985) 3(6), 424-426. L.D. Protsenko, A.B. Shapiro, V.M. Ovrutskii, V.I. Suskina, L.S. Vasil'eva, L.K. Denisova, N.I. Sharykina, I.G. Kudryavtseva, Khimiko-Farmatsevticheskii Zhumal (1985), 19(10), 1199-202. K. Jauhiainen, L. Kangas, H. Kapyla, O. Altthan, Urological Research (1985), 13:19-21. Adnan E1-Yazigi, Iman A1-Saleh, Journal of Pharmaceutical Sciences (1985), 74(11), 12257. Mervyn Israel, P. iGopalakrishnan Potti, Ramakrishnan Seshadri, Journal of Medicinal Chemistry (1985) 28(9), 1223-8. E.J. Land, T. Mukherjee, A.J. Swallow, J.M. Bruce, British Journal of Cancer (1985) 51(4), 515-23. M.A. Van Lancker, H.J.C.F. Nelis, A.P. De Leenheer, Journal of Chromatography (1983) 254, 45-52. Larry P. Solomonson, Paul R. Halabrin, Cancer Research (1981) 41(2), 570-2. Edward N. Chaney, Jr., Richard P. Baldwin, Analytical Chemistry (1982) 54(14), 2556-60. V. Malatesta, F. Morazzoni, A. Gervasini, F. Arcamone, Anti-Cancer Drug Design (1985) 1(1), 53-7. Alan T. McGown, Timothy H. Ward, Brian W. Fox, Cancer Chemotherapy and Pharmacology (1983) 11(2), 113-16. H. Tapiero, A. Fourcade, G. Mathe,Recent Adv. Chemother., Proc. Int. Congr. Chemother., 14th (1985), Volume Anticancer Sect. 1,203-4. Luigi Valentini, Elisabetta Gianazza Pier Giorgio Righetti, Journal of Biochemical and Biophysical Methods (1980)3(6), 323-38.

377. 378. 379. 380.

381.

382. 383.

384.

385.

386.

\

387. 388. 389.

390.

391.

392.

- 22 -

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 24 of 29

393. 394. 395. 396. 397. 398. 399. 400.

LY Yang, American Association for Cancer Research, 24:315 (1983). B. Drewinko, LY Yang, Cancer Res. (1985), 45(4): 1511-5. B. Drewinko, LY Yang, B. Barlogie, JM Trujillo, Cancer Res. (1983), 43(6): 2648-53. M. Katz, New England Journal of Medicine (1969), 280(26): 1480-1. R. Barkman, Acta Ophthalmologica (1969) 47:461. T. Higucki, et al., Journal of Pharmaceutical Sciences (1964) 53(3):280-5. M. Nakano, Journal of Pharmaceutical Sciences (1968) 57(11):1865-8. T. Tsuji, M. Takezawa, H. Morioka, T. Kida, I. Horino, T. Eto and H. Shibai, Agricultural and Biological Chemistry 48(12), 3181-84 (1984). H. Umezawa, T. Takeuchi, M. Hamad, H. Naganawa, T. Sawa, T. Uchida, and M. Imoto, Anthracycline Compound, 84-148, 795, (1984). A. Trouet, D. Campeneere Deprez-de C. de Duve, Nature: New Biology (1972) 239(91) 110-112. E. Arlandini, A. Vigevani, F. Arcamone, Farmaco Ed. Sci., 35(1), 65-78 (1980). Roy J. Sturgeon, Stephen G. Schulman, European Journal of Medicinal Chemistry, 15(5), 469-472 (1980). R. Buehner, S. Biedert and DI Miura, Arzneim. Forsch., 30(7), 1065-1070 (1980). D. Vedaldi, F. Dall'acqua, S. Caffieri, G. Rodighiero, Farmaco Ed. Sci.37(9), 571-581 (1982). M.L. Schinetti, R. Greco, G. Lazzarino, G. Soldani, A. Bertelli, Arzneim. Forsch., 33(6), 834-836 (1983). G. Zbinden, A.K. Beilstein, E. Bachmann, Arzneim. Forsch., 34(10), 1298-1301 (1984). S. Miyazaki, S. Takeuchi, W. Hou, H. Norio, C. Yokouchi, M. Takada, M. Hosokawa, Y. Koga, and H. Kobayashi, Chemical & Pharmaceutical Bulletin 33(6) 2490-2498 (1985). T. Suzuki, E. Sato, K. Goto, Y. Katsurada, K. Unno, T. Takahashi, Chemical & Pharmaceutical Bulletin 29(3), 844-848 ( 1981). H. Tanizawa, Y. Sazuka, Y. Takino, Chemical & Pharmaceutical Bulletin 31(5), 1714-1718 (1983). L. Valentini, V. Nicolella, E. Vannini, M. Menozzi, S. Penco, F. Arcamone, Farmaco Ed.Sci. 40(6), 377-390 (1985).

401.

402.

403. 404.

405. 406.

407.

408. 409.

410.

411.

412.

- 23 -

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 25 of 29

413.

G. Buldain, J. Hurst, R.B. Frydman, and B. Frydman, J.Org.Chem., 42(23), 3653-3658 (1977). F. Arcamone, S. Penco, A. Vigevani, et al., Journal of Medicinal Chemistry 1975; 18 (7): 703-7. T. Takahashi, M. Nakano, H. Kaneshima and K. Mori, Hokkaidoritsu Eisei Kenkyushoho (1984), (34), 75-9. H. Sakamoto, T. Kitagawa, T. Sugiyama, Y. Miyake, and T. Yamano, Developments in Biochemistry (1982) 21,684-8. S. Eksborg, S O Nilsson and F. Edsmyr, European Urology (1980) 6 (4) 218-20. S Toyoshima, Radioisotopes (1980) 29(5) 252-260. P. Russo, M. Pala, L. Ottaggio, D. Vecchio, L. Santi, S. Parodi, Journal of Applied Toxicology (1983) (3) 58-62. A. Trouet, D. Deprez-de Campeneere, C. de Duve, Nature New Biology (1972) 239 (91) 110-112. A. Trouet, R. Baurain, M. Masquelier, D. DePrez-de Campeneere, Anthracyclines (1983) 101-4. G.P. Wiist, International Congress of Chemotherapy (2) 395-397 (1972). L.S. Pokras, L.P. Snezhnova, M.G. Brazhnikova, V.M. Grigor'eva, Antibiotiki 23(9), 788-92 (1978). D. Deprez-de Campeneere, Mem Acad R Med Belg, 47 (4) 214-255 (1974). F. Quadrifoglio, V. Crescenzi, G. Prota, L. Cariello, A. Di Marco, F. Zunino, Chemicobiological Interactions 11 (2) pp. 91-99 (1975). G. Ziglio, G. Beltramelli, Igiene Modema 83(1), 88-96 (1985). R. Mondelli, A. Amone, G. Fronza, G. Cassinelli, B. Gioia, A. Vigevani, Journal of Chemical Research (1984) 1717-1737. S. Fumero, G.P. Berruto, J. Meriggi, A. Mondino, S. Silvestri, R. Barale, Farmaco Ed.Sci., 36(10), 867-874 (1981). C. Dias Selassie, C. Hansch, T. A. Khwaja, C. B. Dias, S. Pentecost, Journal of Medicinal Chemistry 27(3), (1984) 347-357. S.A. Islam, S. Neidle, B. M. Gandecha, M. Partridge, L. H. Patterson, J. R. Brown,Journal of Medicinal Chemistry 28(7), (1985), 857-864.

414.

415.

416.

417. 418. 419.

420.

421.

422. 423.

424. 425.

426. 427.

428.

429.

430.

- 24 -

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 26 of 29

43 i.

Ramakrishnan Seshadri, Mervyn Israel, William J. Pegg,Journal of Medicinal Chemistry 26(1), (1983) 11-15. Tai-Shun Lin, Beverly A. Teicher, Alan C. Sartorelli, Journal of Medicinal Chemistry 23(11), (1980) 1237-1242. Mervyn Israel, John E. Airey, Robert J. Murray, John W. Gillard, Journal of Medicinal Chemistry 25(1), (1982) 28-31. Mervyn Israel, Robert J. Murray, Journal of Medicinal Chemistry 25(1), (1982) 24-28. K.C. Murdock, R.G. Child, Yang-i Lin, J.D. Warren, P.F. Fabio, Journal of Medicinal Chemistry 25(5), (1982) 505-518. Ronald G. Smith, Analytical Chemistry 54(12), (1982). 2006-2008. Smith et al., Journal of the American Chemical Society 98(6) (1976) 1969-1971. I.J. McLennan, R.E. Lenkinski, Journal of the American Chemical Society 106(23), (1984), 6905-6909. Z. Abdeen, J.M. Bruce, P.M. Guyan, E.J. Land, T. Mukherjee, A.J. Swallow, Journal of Chemical Research (1985) 8, 254-255. S.U. Hildegrand-Zanki, D.H. Kern, Proceedings of the 4th Conference on Human Tumor Cloning (1984) 451-458. Megumi Itoh, Masahiro Nakano, Kazuhiko Juni, Hitoshi Sekikawa, Chemical & Pharmaceutical Bulletin (1980) 28(4), 1051-5. P.K.Chakravarty, P.L. Carl, M.J. Weber, J.A. Katzenellenbogen, Journal of Medicinal Chemistry 26(5) (1983), 638-644. M. Volm, E. Maas, J. Mattem, Arzneim Forsch, 31(2) (1981), 300-302. Kenji Kano, Tomonori Konse, Tanekazu Kubota, Bulletin of the Chemical Society of Japan 58(7) (1985), 1879-1885. Amone et al., Tetrahedron Letters (1976), 3349. Edward M. Acton, George L. Tong, Journal of Medicinal Chemistry 24(6) (1981), 669-673. Y.Kimura, M. Suzuki, T. Matsumoto, R. Abe, S. Terashima, Chemistry Letters (1984), 501504. S. Penco, G. Cassinelli, A. Vigevani, P. Zini, G. Rivola, F. Arcamone, Gazzetta Chimica Italiana 115(3), (1985) 195-198. Michael J. Broadhurst, Cedric H. Hassall, Gareth J. Thomas, Journal of the Chemical Society (1982) 158-160. - 25 -

432.

433.

434. 435.

436. 437. 438.

439.

440.

441.

442.

443. 444.

445. 446. 447.

448.

449.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 27 of 29

450.

Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Sergio Penco, Giovanni Rivola, Gazzetta Chimica Italiana 114 (3/4), (1984), 185-188. DuVemay, et al., Biochemistry 18 (18), (1979), 4024-4027. D. Luedke, Y. Sunwoo, S. Luedke, R. Godefroid, Proceedings of the American Association of Cancer Research (1980) Vol. 21, p. 330. S.D. Aust, L.A. Morehouse, C.E. Thomas, Journal of Free Radicals in Biology & Medicine (1985) 1(1), 3-25. J.R. Powell, K.H. Donn, American Journal of Medicine (1984) 77/5 B, pp. 57-84. A.J. Zaloznik, S.G. Oswald, M. Langin, Cancer (1983) 51/4, 752-755. M. Anderson, D. Brassington, J. Bolger, British Medical Journal (1983) 286/6358, pp. 32-36. R.G. Stoller, S.A. Jacobs, J.C. Drake, Cancer Chemotherapy Reports (1975) 6/1, pp. 19-24. R.J. Sturgeon, C. Flanagan, D.V. Naik, S.G. Schulman, Journal of Pharmaceutical Sciences (1977) 66(9), 1346-1347. William R. Vincent, Leonard S. Rosenberg, Stephen G. Schulman, Journal of Pharmaceutical Sciences 73(9), (1984), pp. 1279-1284. Akira Tanaka, Junji Morita, Tohru Komano, Agricultural and Biological Chemistry 46(4), (1982), pp. 1013-1020. Theodore T. Otani, Mary R. Briley, Ruth I. Geran, Journal of Pharmaceutical Sciences 73(2), (1984), pp. 264-265. Seiichi Tanida, Toru Hasegawa, Masahiko Yoneda, Agricultural and Biological Chemistry 45(9), (1981), pp. 2013-2018. Shau-Fong Yen, W. David Wilson, Stevens W. Pearce, Edmond J. Gabbay.,Journal of Pharmaceutical Sciences 73(11), (1984), pp. 1575-1579. Tetsuya Terasaki, Tatsuki Iga, Yuichi Sugiyama, Manabu Hanano,Journal of Pharmacy and Pharmacology 34, (1982), pp. 597-600. Tetsuya Terasaki, Tatsuji Iga, Yuichi Sugiyama, Manabu Hanano, Journal of Pharmaceutical Sciences 73(10), (1984), pp. 1359-1363. Aldo Andreani, Daniela Bonazzi, Mirella Rambaldi, Iraklis Galatulas, Rosaria Bossa, Journal of Pharmaceutical Sciences 73(8), (1984), pp. 1175-1177. Edwin M. Uyeki, Akira Nishio, Philip J. Wittek, C.C. Cheng, Journal of Pharmaceutical Sciences 70(9), (1981), pp. 1011-1014.

451. 452.

453.

454. 455. 456. 457. 458.

459.

460.

461.

462.

463.

464.

465.

466.

467.

- 26 -

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 28 of 29

468.

Steven D. Averbuch, Theodore T. Finkelstein, Susan E. Fandrich, Steven D. Reich, Journal of Pharmaceutical Sciences 70(3), (1981), pp. 265-269. P. Couvreur, B. Kante, L. Grislain, M. Roland, P. Speiser, Journal of Pharmaceutical Sciences 71(7), (1982), pp. 790-792. Andrew E. Senyei, Steven D. Reich, Constance Gonczy, Kenneth J. Widder, Journal of Pharmaceutical Sciences 70(4), (1981), pp. 389-391. Jed, Fisher, K. Ramakrishnan, Kathryn E. McLane, Biochemistry (1982), 21(24), 6172-80. R. Supino; A. Necco; T. Dasdia; A.M. Casazza; A. Di Marco, Cancer Research (1977), 37(12), 4523-8. Jeffi'ey Cummings, Robert Milroy, Anticancer Research (1986), 6(5), 1177-9. J. Robert; B. Schott, S. Huet, Colloque INSERM (1988), 169, 587-93. F. Formelli; A. Di Marco; A.M. Casazza; G. Pratesi; R. Supino; A. Mariani, Curr. Chemother., Proc. Int. Congr. Chemother., 10th (1978), 2, 1240-2. J. Robert, Bulletin duCancer (1988), 75(2), 167-74. J. Robert; F. Rigal-Huguet; J.L. Harousseau; J. Pris; S. Huet; J. Reiffers; P. Hurteloup; V. Tamassia, Leukemia Research (1987), 11(11 ), 961-4. V. Tamassia; M.A. Pacciarini; E. Moro; E. Piazza; G. Vago; A. Libretti, International Journal of Clinical Pharmacology Research (1987), 7(5), 419-26. D.B. Smith; J.M. Margison; S.B. Lucas; P.M. Wilkinson; A. Howell, Cancer Chemotherapy and Pharmacology (1987), 19(2), 138-42. P.A. Speth; F.A. van de Loo; P.C. Linssen; H.M. Wessels; C. Haanen, Clinical Pharmacology and Therapeutics (1986), 40(6), 643-9. G. Zini, G.P. Vicario, M. Lazzati, F. Arcamone, Cancer Chemotherapy and Pharmacology (1986), 16(2), 107-15. J.J. Kavanagh; K.Y. Yeung; N. Savaraj; I.H. Krakoff, European Journal of Cancer & Clinical Oncology (1985), 21(10), 1187-9. S. Eridani; N.G. Slater; A.K. Singh; T.C. Pearson, Blut (1985), 50(6), 369-72. V. Bonfante; L. Ferrari; F. Villani; G. Bonadonna, Investigational New Drugs (1983), 1(2), 161-8. E. Berman; R.E. Wittes; B. Leyland-Jones; E.S. Casper; R.J. Gralla; J. Howard; L. Williams; R. Baratz; C.W. Young, Cancer Research (1983), 43 (12 Pt 1), 6096-101. A.M. Casazza; G. Pratesi; F. Giuliani; A. Di Marco, Tumori (1980), 66(5), 549-64. - 27 -

469.

470.

471. 472.

473. 474. 475.

476. 477.

478.

479.

480.

481.

482.

483. 484.

485.

486.

Case 1:04-cv-00833-KAJ
ATTACHMENT I

Document 253-6

Filed 06/21/2006

Page 29 of 29

487. 488. 489. 490. 491. 492. 493. 494. 495. 496. 497. 498. 499. 500. 501. 502.

Zimmerman et al., U.S. Patent No. 4,936,139 June 26, 1990. Shigeru, K. et al., CA Patent No. 2,014,244 (1990). Bargiotti et al., U.S. Patent No. 4,325,946 April 20, 1982. Cassinelli et al., U.S. Patent No. 4,276,289 June 30, 1981. Arcamone et al., U.S. Patent No. 4,107,423 August 15, 1978. Garland et al., U.S. Patent No. 4,348,388 September 7, 1982. Umezawa et al., U.S. Patent No. 4,355,026 October 19, 1982. Bargiotti et al., U.S. Patent No. 4,393,052 July 12, 1983. Angelucci et al., U.S. Patent No. 4,465,671 August 14, 1984. Angelucci et al., U.S. Patent No. 4,563,444 January 7, 1986. Penco et al., U.S. Patent No. 4,604,381 August 5, 1986. Bargiotti et al., U.S. Patent No. 4,684,629 August 4, 1987. Bargiotti et al., U.S. Patent No. 4,839,346 June 13, 1989. Morimoto, et al., JP Patent Publ. No. 61-254598 November 12, 1986. Venotti, et al., DE Patent No. No. DE 371 19 184 A1 December 7, 1987. M. Broggini, C. Italia, T. Colombo, L. Marmonti, M.G. Donelli, Cancer Treatment Reports (1984) 68(5), pp. 739-47.

153174.1

- 28 -