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    • 48. 发明授权
    • Substituted aniline derivatives useful as histamine H3 antagonists
    • 用作组胺H3拮抗剂的取代苯胺衍生物
    • US07879880B2
    • 2011-02-01
    • US11641153
    • 2006-12-19
    • Daniel M. SolomonRobert G. AslanianMichael Y. BerlinManuel de Lera RuizKevin D. McCormickMwangi W. MutahiWing C. Tom
    • Daniel M. SolomonRobert G. AslanianMichael Y. BerlinManuel de Lera RuizKevin D. McCormickMwangi W. MutahiWing C. Tom
    • A61K31/5377A61K31/496A61K31/4545C07D487/04C07D413/14C07D401/14C07D401/12
    • C07D401/12C07D213/73C07D213/74C07D401/14C07D471/04
    • Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein M1 is M2 is N; X is a bond, optionally substituted alkylene, alkenylene, —O—, —CH2N(R12)—, —N(R12)CH2—, —N(R12)—, —NHC(O)—, —OCH2—, —CH2O—, or —S(O)0-2—; and Y is —(CH2)1-2—, —C(═O)—, —C(═NOR13)— or —SO0-2—; or M1 is N; M2 is N or CH; X is a bond, alkylene, alkenylene, —C(O)—, —NHC(O)—, —OC(O)— or —S(O)1-2—; Y is —(CH2)1-2—, —C(═O)— or —SO0-2—; and when M2 is CH, Y is also Y is —O— or —C(═NOR13)—; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combination with other agents.
    • 公开了下式的化合物或其药学上可接受的盐,其中M 1为M 2为N; X是一个键,任选取代的亚烷基,亚烯基,-O - , - CH2-(R12) - , - N(R12)CH2-,-N(R12) - , - NHC(O) - , - OCH2 - - 或-S(O)0-2-; 并且Y是 - (CH 2)1-2 - , - C(= O) - , - C(= NOR 13) - 或-SOO 2 - ; 或M1为N; M2为N或CH; X是键,亚烷基,亚烯基,-C(O) - , - NHC(O) - , - OC(O) - 或-S(O)1-2 - Y是 - (CH 2)1-2 - , - C(= O) - 或-SOO 2 - ; 当M2是CH时,Y也是Y是-O-或-C(= NROR13) - ; Z是键或任选取代的亚烷基或亚烯基; U和W是CH,或一个是CH,一个是N; R 1是任选取代的烷基,环烷基,芳基,芳基烷基,杂芳基,杂环烷基; R 2是任选取代的烷基,烯基,芳基,芳基烷基,杂芳基,杂芳基烷基,环烷基或杂环烷基; 剩余的变量如规范中所定义; 以及单独或与其他药物组合治疗肥胖症,代谢综合征和认知缺陷障碍的组合物和方法。