Substituted aniline derivatives useful as histamine H3 antagonists
    2.
    发明申请
    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:US20070142394A1

    公开(公告)日:2007-06-21

    申请号:US11641153

    申请日:2006-12-19

    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是M 2是N; X是一个键,任选取代的亚烷基,亚烯基,-O - , - CH 2 N(R 12) - , - N(R 12) CH 2 - , - N(R 12) - , - NHC(O) - , - OCH 2 - , - O 2或-S(O)0-2 - ; 并且Y是 - (CH 2)2 - , - C( - ) - , - C(-NOR 13) - 或-SO <0-2 < - >。 或M 1是N; M 2是N或CH; X是键,亚烷基,亚烯基,-C(O) - , - NHC(O) - , - OC(O) - 或-S(O) Y是 - (CH 2)2 - , - C - ( - O) - 或-SO 0-2 - 。 当M 2是CH时,Y也是Y是-O-或-C(-NOR 13) - ; 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
    3.
    发明申请
    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:US20070010513A1

    公开(公告)日:2007-01-11

    申请号:US11455873

    申请日:2006-06-19

    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; R1 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 1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。

    Glaucoma surgery methods and systems

    公开(公告)号:US09642746B2

    公开(公告)日:2017-05-09

    申请号:US14191277

    申请日:2014-02-26

    申请人: Michael Berlin

    发明人: Michael Berlin

    IPC分类号: A61F9/007 A61F9/008 A61F9/00

    摘要: Methods and systems are disclosed for creating an aqueous flow pathway in the trabecular meshwork, juxtacanalicular trabecular meshwork and Schlemm's canal of an eye for reducing elevated intraocular pressure. Some embodiments described apparatus and methods useful in photoablation of tissues. In some embodiments, a photoablation apparatus is used to perforate a tissue, forming an aperture into a space behind the tissue. Gases formed during a photoablation process can be used to pressurize the space behind the tissue to enhance patency of the space. In some embodiments the tissue is the trabecular meshwork of the eye and a wall of Schlemm's canal, and the space behind the tissue is a portion of the lumen of Schlemm's canal. In some embodiments, the method is useful in the treatment of glaucoma by improving outflow from the anterior chamber of the eye into Schlemm's canal, reducing intraocular pressure.

    Glaucoma Surgery Methods and Systems
    10.
    发明申请

    公开(公告)号:US20170119579A9

    公开(公告)日:2017-05-04

    申请号:US14191277

    申请日:2014-02-26

    申请人: Michael Berlin

    发明人: Michael Berlin

    IPC分类号: A61F9/007 A61F9/008 A61F9/00

    摘要: Methods and systems are disclosed for creating an aqueous flow pathway in the trabecular meshwork, juxtacanalicular trabecular meshwork and Schlemm's canal of an eye for reducing elevated intraocular pressure. Some embodiments described apparatus and methods useful in photoablation of tissues. In some embodiments, a photoablation apparatus is used to perforate a tissue, forming an aperture into a space behind the tissue. Gases formed during a photoablation process can be used to pressurize the space behind the tissue to enhance patency of the space. In some embodiments the tissue is the trabecular meshwork of the eye and a wall of Schlemm's canal, and the space behind the tissue is a portion of the lumen of Schlemm's canal. In some embodiments, the method is useful in the treatment of glaucoma by improving outflow from the anterior chamber of the eye into Schlemm's canal, reducing intraocular pressure.