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    • 9. 发明申请
    • ELLIPTICINE COMPOUNDS FOR TREATING OBESITY
    • 用于治疗肥胖的化合物
    • WO2010107704A2
    • 2010-09-23
    • PCT/US2010/027337
    • 2010-03-15
    • OSTEOGENEX INC.ELLIES, DebraROSENBERG, William
    • ELLIES, DebraROSENBERG, William
    • A61K31/4738A61K31/47A61P3/04A61P3/00
    • A61K31/475
    • The present invention provides a method of reducing body weight in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I : In Formula I, R 1 is H, C 1-6 alkyl, or C 1-6 alkyl-aryl. Each of R 2 and R 4 of Formula I are independently H, halogen, C 1-6 alkyl, C 1-6 haloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkoxy, OR 2a , SR 2a , C(O)R 2a , C(O)OR 2a , C(O)NR 2a R 2b , NR 2a R 2b , C 1-6 alkyl NR 2a R 2b , N(R 2a )C(O)R 2b , N(R 2a )C(O)OR 2b , N(R 2a )C(O)NR 2a R 2b , OP(O)(OR 2a ) 2 , S(O) 2 OR 2a , S(O) 2 NR 2a R 2b , -CN, -NO 2 , cycloalkyl, heterocycloalkyl, aryl or heteroaryl. Each of R 2a and R 2b of Formula I are independently H, C 1-6 alkyl, C 1-10 heteroalkyl or C 1-6 alkyl-aryl. R 3 of Formula I is absent, C 1-6 alkyl or N-oxide. The compounds include the salts, hydrates and isomers thereof. The present invention also provides methods for the treatment of obesity and disorders related to obesity and higher than recommended percentage body fat, such as type II diabetes.
    • 本发明提供了一种通过向受试者施用治疗有效量的式I化合物来减少有需要的受试者的体重的方法:在式I中,R 1是H,C 1-6烷基或C 1-6 烷基 - 芳基。 式I的R 2和R 4各自独立地为H,卤素,C 1-6烷基,C 1-6卤代烷基,C 2-6烯基,C 2-6炔基,C 1-6卤代烷氧基,OR 2 a,SR 2 a,C(O)R 2a,C (O)OR2a,C(O)NR2aR2b,NR2aR2b,C1-6烷基NR2aR2b,N(R2a)C(O)R2b,N(R2a)C(O)OR2b,N(R2a)C(O)NR2aR2b,OP (O)(OR 2 a)2,S(O)2 OR 2 a,S(O)2 NR 2 R 2b,-CN,-NO 2,环烷基,杂环烷基,芳基或杂芳基。 式I的R2a和R2b各自独立地为H,C1-6烷基,C1-10杂烷基或C1-6烷基 - 芳基。 式I的R 3不存在,C 1-6烷基或N-氧化物。 化合物包括其盐,水合物和异构体。 本发明还提供了治疗与肥胖相关的肥胖症和高于推荐的体脂肪百分比(例如II型糖尿病)的方法。