Crystalline forms of temozolomide

Details Crystalline forms of temozolomide Crystalline forms of temozolomide

2004-12-30

2009-11-10

Balasubramanian, Venkataraman (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

C514S183000

Reexamination Certificate

active

07615632

ABSTRACT:
Disclosed are novel crystalline forms of Temozolomide, methods of preparation thereof, medicaments including the novel crystalline forms of Temozolomide, and uses thereof in the treatment of medical conditions.

REFERENCES:
patent: 5260291 (1993-11-01), Lunt et al.
patent: 6844434 (2005-01-01), Kuo
patent: 6858631 (2005-02-01), Crocker et al.
patent: 2002/0095036 (2002-07-01), Kuo et al.
patent: 2004/0223951 (2004-11-01), Zaknoen
patent: 0262682 (1988-01-01), None
patent: 2511679 (1983-02-01), None
patent: WO 2005/063757 (2005-07-01), None
Lowe et al. “Antitumor Imidazotetrazines. 25. Crystal Structure of 8-Carbamoyl-3-Methylimidazo[5,1-d]-1,2,3,5-Tetrazin-4(3H)-One (Temozolomide) and Structural Comparisons With the Related Drugs Mitozolomide and DTIC”, Journal of Medicinal Chemistry, 35(8): 3377-3382, 1992. Compound 5, Figs.2-3, Table II.
Wang et al. “Preparation and Thermostability of Polymorphs of Temozolomide”, Zhongguo Yiyao Gongye Zazhi, 34(4): 178-180, 2003.
Britain et al. “Polymorphism in Pharmaceutical Solids Passage”, Polymorphism in Pharmaceutical Solids, p. 235-238, 1999. p. 236, 1. [18-22].
Caira “Crystalline Polymorphism of Organic Compounds”, Topics in Current Chemistry, 198: 163-208, 1998. p. 164, §1, p. 165, §2, p. 165, last §—p. 166, §1.
Baig et al. “Antitumour Imidazotetrazines. Part 12. Reactions of Mitozolomide and Its 3-Alkyl Congeners With Oxygen, Nitrogen, Halogen, and Carbon Nucleophiles”, J. Chem. Soc. Perkin Trans. I, p. 675-670, 1987.
Brown et al. “Antitumor Imidazotetrazines. 40. Radiosyntheses of [4-11C-Carbonyl]- and [3-N-11C-Methyl]-8-Carbamoyl-3-Methylimidazo[5,1-D]-1,2,3,5-Tetrazin-4(3H)-One (Temozolomide) for Positron Emission Tomography (PET) Studies”, Journal of Medicinal Chemistry, 45(25): 5448-5457, 2002.
Clark et al. “Antitumor Imidazotetrazines. 32. Synthesis of Novel Imidazotetrazinones and Related Bicyclic Heterocycles to Probe the Mode of Action of the Antitumor Drug Temozolomide”, Journal of Medicinal Chemistry, 38(9): 1493-1504, 1995.
Newlands et al. “Temozolomide: A Review of Its Discovery, Chemical Properties, Pre-Clinical Development and Clinical Trials”, Cancer Treatment Reviews, 23: 35-61, 1997.
Stevens et al. “Antitumor Imidazotetrazines. 1. Synthesis and Chemistry of 8-Carbamoyl-3-(2-Chloroethyl)Imidazo[5,1-D]-1,2,3,5-Tetrazin-4(3H)-One, A Novel Broad-Spectrum Antitumor Agent”, J. Med. Chem., 27(2): 196-201, 1984.
Wanner et al. “A New Synthesis of Temozolomide”, J. Chem. Soc. Perkin Trans. 1, p. 1877-1880, 2002.
Carlton “Microscopy in the Study of Polymorph Stability”, Microsc. Microanal., 10(Suppl.2): 1346-1347, 2004.
Haleblian “Characterization of habits and Crystalline Modification of Solids and Their Pharmaceutical Applications”, Journal of Pharmaceutical Sciences, 64(8): 1269-1288, Aug. 1975.
Haleblian et al. “Pharmaceutical Applications of Polymorphism”, Journal of Pharmaceutical Sciences, 58(8): 911-929, Aug. 1969.
Wang et al. “Alternative Syntheses of the Antitumour Drug Temozolomide Avoiding the Use of Methyl Isocyanate”, Journal of the Chemical Society, Chemical Communications, p. 1687-1688, 1994.
European Search Report Dated Sep. 10, 2008 From the European Patent Office Re.: Application No. 04806720.1.
Rodriguez-Hornedo et al. Significance of Controlling Crystallization Mechanisms and Kinetics in Pharmaceutical Systems, Journal of Pharmaceutical Sciences, XP001096590, 88(7): 651-660, Jul. 1, 1999.
Shekunov et al. “Crystallization Processes in Pharmaceutical Technology and Drug Delivery Design”, Journal of Crystal Growth, XP004193361, 211(1-4): 122-136, Apr. 1, 2000.
Wang et al., “Antitumor Imidazotetrazines. 35. New Synthetic Routes to the Antitumor Drug Temozolomide”, J.Org.Chem, vol. 62, No. 21, pp. 7288-7294 (1997).

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