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AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
专利权人:
发明人:
申请号:
EP09793353.5
公开号:
EP2346872B1
申请日:
2009.10.08
申请国别(地区):
EP
年份:
2015
代理人:
摘要:
The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I, wherein R1, is selected from the group consisting of monocyclic aryl or monocyclic heteroaryl W is selected from the group consisting of a direct bond, -O-, and -N(R6)- provided that if W is a direct bond, D is a cyclic amine that is attached to A via the nitrogen atom of the cyclic amine D is selected from the group consisting of a direct bond, substituted or unsubstituted C1 to C4 alkyl, substituted or unsubstituted C3 to C7 cycloalkyl, cycloalkylalkyl, and 4- to 6-membered cyclic amines, provided that if D is a direct bond, R2a, R2b, and R2c must be selected from H, alkyl, or cycloalkyl E and G are independently N or CH provided that both are not N R1 is substituted or unsubstituted phenyl or substituted or unsubstituted monocyclic heteroaryl R2a, R2b, and R2c are independently selected from the group consisting of hydrogen, halo, cyano, hydroxyl, -NR5R5a, -SO2R34, -CO2R35 -NR5CO2R21, -NR5COR21, substituted or unsubstituted C1 to C4 alkyl, substituted or unsubstituted C3 to C7 cycloalkyl, substituted or unsubstituted 4- to 6-membered cyclic amines wherein said cyclic amine is optionally substituted with -OH, carbonylamino, alkoxycarbonylamino, or at least one of R2a, R2b, and R2c is a prodrug moiety selected from amino acid esters or phosphoric acid esters wherein said amino acid ester has the formula -OC(O)CH(NH2)R31, wherein R31 is H or C1 to C4 alkyl or any two of R2a, Rb, or R2c, may be taken together to form a ring R3 and R3a are each independently selected from the group consisting of hydrogen, hydroxyl, lower alkoxy, halo, CN, substituted or unsubstituted C1 to C4 alkyl, perfluoroalkyl, substituted or unsubstituted C3 to C7 cycloalkyl, cycloalkoxy, amino, alkylamino, dialkylamino, and aminoalkyl, wherein R3 or R3a and D
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