US2005020836A1PendingUtilityA1
Crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4(3-ethynyl-phenyl)-1methyl-1h-quinolin-2-one, 2,3,-dihydroxybutanedioate salts and method of production
Est. expiryDec 19, 2020(expired)· nominal 20-yr term from priority
C07D 401/06A61P 35/00
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Claims
Abstract
The invention relates to crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3-dihydroxy butanedioate salts having the formula shown below: and to pharmaceutical compositions containing the above compound, methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above compound, and to methods of preparing the crystal forms of the above compound and related compounds.
Claims
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29 . A process for preparing a salt having the formula
comprising treating 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one with tartaric acid in a polar solvent at an elevated temperature to form an anhydrous crystal form which provides high-intensity diffraction peaks at diffraction angles (2θ) of about 3.6, 17.2, 17.6, 18.8, 19.2, 20.4 and 22.1 in the powder X-ray diffraction pattern.
30 . The process of claim 29 , wherein said salt is (+)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, (−)-2,3-dihydroxy butanedioate anhydrous salt.
31 . The process of claim 29 , wherein said salt is (−)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, (+)-2,3-dihydroxy butanedioate anhydrous salt.
32 . The process of claim 29 , wherein the polar solvent is ethyl acetate.
33 . A method of treating a hyperproliferative disorder in a mammal which comprises administering to the mammal a therapeutically effective amount of a crystal form of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3-dihydroxy butanedioate anhydrous salt.
34 . The method of claim 33 , wherein the method is for the treatment of a cancer selected from brain, squamous cell, bladder, gastric, pancreatic, breast, head, neck, oesophageal, prostate, colorectal, lung, renal, kidney, ovarian, gynecological and thyroid cancer.
35 . A method for the treatment of a hyperproliferative disorder in a mammal which comprises administering to the mammal a therapeutically effective amount of a polymorph of a crystal form of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3-dihydroxy butanedioate anhydrous salt in combination with an anti-tumor agent selected from the group consisting of mitotic inhibitors, alkylating agents, anti-metabolites, intercalating antibiotics, growth factor inhibitors, cell cycle inhibitors, enzymes, topoisomerase inhibitors, biological response modifiers, anti-hormones, and anti-androgens.
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