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    • 8. 发明申请
    • PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
    • 吡咯烷酮类似物有效用于浓缩HORMONE受体-1拮抗剂的MELANIN
    • WO2010104830A1
    • 2010-09-16
    • PCT/US2010/026626
    • 2010-03-09
    • BRISTOL-MYERS SQUIBB COMPANYAHMAD, SaleemWASHBURN, William, N.HERNANDEZ, Andres, S.ROBL, Jeffrey, A.NGU, KhehyongWANG, Zhenghua
    • AHMAD, SaleemWASHBURN, William, N.HERNANDEZ, Andres, S.ROBL, Jeffrey, A.NGU, KhehyongWANG, Zhenghua
    • A61K31/4412A61P3/04C07D213/38C07D213/74C07D213/30C07D213/32C07D213/26C07D213/68C07D401/04A61K31/4409A61K31/4427
    • C07D213/38A61K31/4412A61K31/4427C07D213/26C07D213/30C07D213/32C07D213/68C07D401/04
    • MCHR1 antagonists are provided having the following Formula I: wherein A 1 and A 2 are independently C or N; E is C or N; D 1 is a bond, -CR 8 R 9 X-, -XCR 8 R 9 -, -CHR 8 CHR 9 -, -CR 10 =CR 10' -, -C≡C-, or 1,2-cyclopropyl; X is O, S or -NR 11 ; R 1 , R 2 , and R 3 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, lower cycloalkoxy, -CF 3 , -OCF 3 , -OR 12 and -SR 12 ; G is O or S; D 2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkycycloalkoxy; Z 1 and Z 2 are independently hydrogen, halogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF 3 , -OCONR 14 R 14' , -CN, -CONR 14 R 14' , -SOR 12 , -SO 2 R 12 , -NR 14 COR 14' , -NR 14 CO 2 R 14' , -CO 2 R 12 , NR 14 SO 2 R 12 or -COR 12 provided that if Z 1 is -CH 3 and one of R 1 , R 2 , or R 3 is F, then Z 2 cannot be H;; R 5 , R 6 , and R 7 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF 3 , -SR 12 , lower alkoxy, lower cycloalkoxy, -OCH 2 OMe, -CN, -CONR 14 R 14' , SOR 12 , SO 2 R 12 , NR 14 COR 14' , NR 14 CO 2 R 12 , CO 2 R 12 , NR 14 SO 2 R 12 and -COR 12 ; R 8 , R 9 , R 10 , R 10' , R 11 are independently hydrogen or lower alkyl; R 12 is lower alkyl or lower cycloalkyl; and R 14 and R 14' are independently H, lower alkyl, lower cycloalkyl or R 14 and R 14' together with the N to which they are attached form a ring having 4 to 7 atoms. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
    • 提供具有下式I的MCHR1拮抗剂:其中A1和A2独立地为C或N; E为C或N; D1是键,-CR8R9X-,-XCR8R9-,-CHR8CHR9-,-CR10 = CR10'-,-C = C-或1,2-环丙基; X是O,S或-NR 11; R 1,R 2和R 3独立地选自氢,卤素,低级烷基,低级环烷基,低级环烷氧基,-CF 3,-OCF 3,-OR 12和-SR 12; G为O或S; D2是低级烷基,低级环烷基,低级烷基环烷基,低级环烷基烷基,低级环烷氧基烷基或低级烷基环烷氧基; Z1和Z2独立地是氢,卤素,低级烷基,低级环烷基,低级烷氧基,低级环烷氧基,卤素,-CF3,-OCONR14R14',-CN,-CONR14R14',-SOR12,-SO2R12,-NR14COR14',-NR14CO2R14' ,-CO 2 R 12,NR 14 SO 2 R 12或-COR 12,条件是如果Z 1是-CH 3并且R 1,R 2或R 3中的一个是F,则Z 2不能是H。 R5,R6和R7独立地选自氢,卤素,低级烷基,低级环烷基,-CF3,-SR12,低级烷氧基,低级环烷氧基,-OCH2OMe,-CN,-CONR14R14',SOR12,SO2R12, NR14COR14',NR14CO2R12,CO2R12,NR14SO2R12和-COR12; R8,R9,R10,R10',R11独立地为氢或低级烷基; R12是低级烷基或低级环烷基; 并且R 14和R 14'独立地为H,低级烷基,低级环烷基或R 14和R 14'与它们所连接的N一起形成具有4至7个原子的环。 这些化合物可用于治疗MCHR1介导的疾病,例如肥胖症,糖尿病,IBD,抑郁症和焦虑症。