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    • 2. 发明申请
    • ANGIOTENSIN II RECEPTOR ANTAGONISTS
    • ANGIOTENSIN II受体拮抗剂
    • WO2006115834A1
    • 2006-11-02
    • PCT/US2006/014092
    • 2006-04-14
    • MERCK & CO., INC.ALANI, Laman, L.DUBOST, David, C.FOSTER, Bruce, S.GHOSH, SoumojeetJAHANSOUZ, HossainPOURKAVOOS, NazaneenREGE, BhagwantTATAVARTI, Aditya
    • ALANI, Laman, L.DUBOST, David, C.FOSTER, Bruce, S.GHOSH, SoumojeetJAHANSOUZ, HossainPOURKAVOOS, NazaneenREGE, BhagwantTATAVARTI, Aditya
    • A61K31/41C07D257/04
    • C07D403/10
    • The compounds of the present invention are polymorphic crystalline forms of the compound 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid, which has the structure (I). Specifically, the compounds of the invention are selected from the group consisting of 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid of Claim 3 selected from the group consisting of 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form I, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form II, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form III, and 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form IV, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form V, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VI, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VII, and 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VIII.
    • 本发明的化合物是2-丁基-4-氯-1 - ((2' - (1-H-四唑-5-基)联苯-4-基)甲基] - 咪唑-1-基的化合物的多晶型形式, 其具有结构(I)。 具体地说,本发明化合物选自2-丁基-4-氯-1 - [(2' - (1-H-四唑-5-基)联苯-4-基)甲基] - 咪唑 -5-羧酸,其选自2-丁基-4-氯-1 - [(2' - (1-H-四唑-5-基)联苯-4-基)甲基] - 咪唑 -5-甲酸盐酸盐形式I,2-丁基-4-氯-1 - [(2' - (1-H-四唑-5-基)联苯-4-基)甲基] - 咪唑-5-甲酸 盐酸盐形式II,2-丁基-4-氯-1 - [(2' - (1-H-四唑-5-基)联苯-4-基)甲基] - 咪唑-5-甲酸盐酸盐形式III和 2-丁基-4-氯-1 - [(2' - (1-H-四唑-5-基)联苯-4-基)甲基] - 咪唑-5-甲酸一水合物形式IV,2-丁基-4 - 氯 - 1 - [(2' - (1-H-四唑-5-基)联苯-4-基)甲基] - 咪唑-5-甲酸一水合物形式V,2-丁基-4-氯-1- 甲基] - 咪唑-5-羧酸一水合物形式VI,2-丁基-4-氯-1 - [(2' - (1H-四唑-5-基)联苯-4-基) (1-1H-四唑-5-基)联苯-4-基)甲基]咪唑-5--C 羧酸一水合物形式VII和2-丁基-4-氯-1 - [(2' - (1-H-四唑-5-基)联苯-4-基)甲基] - 咪唑-5-甲酸一水合物形式 八。