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    Imidazole and benzimidazole derivatives useful as histamine H3 antagonists
    4.
    发明授权
    Imidazole and benzimidazole derivatives useful as histamine H3 antagonists 失效
    可用作组胺H3拮抗剂的咪唑和苯并咪唑衍生物

    公开(公告)号：US07482468B2

    公开(公告)日：2009-01-27

    申请号：US11334932

    申请日：2006-01-19

    申请人： Robert G. Aslanian ,  Wing C. Tom ,  Xiaohong Zhu

    发明人： Robert G. Aslanian ,  Wing C. Tom ,  Xiaohong Zhu

    IPC分类号： C07D403/10 ,  C07D403/14 ,  C07D221/04

    CPC分类号： C07D491/10 ,  C07D233/84 ,  C07D235/26 ,  C07D235/28 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14

    摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: n is 2-5; R is R3-aryl, R3-heteroaryl, R3-cycloalkyl, R3-heterocycloalkyl, alkyl, haloalkyl, —OR4, —SR4 or —S(O)1-2R5; R1 and R2 are H or optionally substituted phenyl or optionally substituted and X is —O— or —S—; or R1 and R2, together with the carbon atoms to which they are attached form optionally substituted and X is —O—, —S— or —NR7—; Z is and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I; also disclosed are methods of treating allergy, allergy-induced airway responses, congestion, obesity and metabolic syndrome using the compounds of Formula I, as well as combinations with other drugs useful for treating those diseases.

    摘要翻译： 公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中：n为2-5; R是R 3 - 芳基，R 3 - 杂芳基，R 3 - 环烷基，R 3 - 杂环烷基，烷基，卤代烷基，-OR 4，-SR 4或-S（O）1-2R 5; R1和R2是H或任选取代的苯基或任选取代的，X是-O-或-S-; 或R 1和R 2与它们所连接的碳原子一起形成任选被取代，X是-O - ， - S-或-NR 7 - ; Z是，其余变量如规范中所定义; 还公开了包含式I化合物的药物组合物; 还公开了使用式I化合物治疗过敏，过敏诱发的气道反应，充血，肥胖和代谢综合征的方法，以及与用于治疗这些疾病的其它药物的组合。

    Substituted aniline derivatives useful as histamine H3 antagonists
    7.
    发明授权
    Substituted aniline derivatives useful as histamine H3 antagonists 失效
    用作组胺H3拮抗剂的取代苯胺衍生物

    公开(公告)号：US07879880B2

    公开(公告)日：2011-02-01

    申请号：US11641153

    申请日：2006-12-19

    申请人： Daniel M. Solomon ,  Robert G. Aslanian ,  Michael Y. Berlin ,  Manuel de Lera Ruiz ,  Kevin D. McCormick ,  Mwangi W. Mutahi ,  Wing C. Tom

    发明人： Daniel M. Solomon ,  Robert G. Aslanian ,  Michael Y. Berlin ,  Manuel de Lera Ruiz ,  Kevin D. McCormick ,  Mwangi W. Mutahi ,  Wing C. Tom

    IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4545 ,  C07D487/04 ,  C07D413/14 ,  C07D401/14 ,  C07D401/12

    CPC分类号： C07D401/12 ,  C07D213/73 ,  C07D213/74 ,  C07D401/14 ,  C07D471/04

    摘要： 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.

    摘要翻译： 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。

    Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists
    9.
    发明授权
    Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists 失效
    碳链取代的哌啶及其衍生物可用作组胺H3拮抗剂

    公开(公告)号：US07408066B2

    公开(公告)日：2008-08-05

    申请号：US11455873

    申请日：2006-06-19

    申请人： Robert G. Aslanian ,  Michael Y. Berlin ,  Ying Huang ,  Kevin D. McCormick ,  Mwangi W. Mutahi ,  Neng-Yang Shih ,  Pauline C. Ting ,  Wing C. Tom ,  Junying Zheng

    发明人： Robert G. Aslanian ,  Michael Y. Berlin ,  Ying Huang ,  Kevin D. McCormick ,  Mwangi W. Mutahi ,  Neng-Yang Shih ,  Pauline C. Ting ,  Wing C. Tom ,  Junying Zheng

    IPC分类号： C07D401/04 ,  C07D401/14 ,  A61K31/495

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

    摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula: where ring A is a monoheteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.

    摘要翻译： 公开了下式的化合物或其药学上可接受的盐，其中：M 1和M 3是CH或N; M 2是CH，CF或N; Y是-C（-O） - ， - C（-S） - ， - （CH 2 CH 2）q - ， - C（-NOR 7） / SO 2 - ） - 或-SO 2 1-2。 Z是键或任选取代的亚烷基或亚烯基; R 1是H，烷基，烯基或任选取代的环烷基，芳基，杂芳基，杂环烷基或下式的基团：其中环A是单杂芳基环; R 2是任选取代的烷基，烯基，芳基，杂芳基，环烷基或杂环烷基; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应，充血，肥胖，代谢综合征非酒精性脂肪性肝病，肝脂肪变性，非酒精性脂肪性肝炎，肝硬化，肝细胞癌或认知缺陷障碍的组合物和方法。