发明名称 Pyridonyl guanidine F<sub>1</sub>F<sub>0</sub>-ATPase inhibitors and therapeutic uses thereof
摘要 The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
申请公布号 US9370507(B2) 申请公布日期 2016.06.21
申请号 US201514675832 申请日期 2015.04.01
申请人 Lycera Corporation 发明人 Glick Gary D.;Hurd Alexander R.;Mattson Matthew N.;Taylor Clarke B.;Van Huis Chad A.
分类号 C07D401/12;C07D405/12;C07D413/12;A61K31/47;A61K31/44;A61K31/4439;A61K31/4433;A61K31/444;C07D213/75;C07D213/76 主分类号 C07D401/12
代理机构 Goodwin Procter LLP 代理人 Goodwin Procter LLP
主权项 1. A method of treating a disorder selected from the group consisting of an immune disorder and inflammatory disorder comprising administering to a human patient in need thereof a therapeutically effective amount of a compound of Formula I in order to ameliorate a symptom of the disorder, wherein Formula I is represented by: including all stereoisomers, geometric isomers, and tautomers; or a pharmaceutically acceptable salt or solvate of any of the foregoing; wherein: A1 is phenylene or a six-membered heteroarylene; A2 is X is —OP(O)(OR11)2; R1 represents independently for each occurrence halogen, alkyl, haloalkyl, hydroxyl, C1-C6alkoxy, or cyano; R2 is hydrogen; R3 is aryl, aralkyl, cycloalkyl, —(C(R6)2)m-cycloalkyl, heteroaryl, heteroaralkyl, or heterocycloalkyl, wherein said aryl, aralkyl, cycloalkyl, heteroaryl, heteroaralkyl, and heterocycloalkyl are each optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, cycloalkyl, C1-C6alkoxy, and cyano; R4 is hydrogen; R5 is hydrogen, halogen, alkyl, alkoxyl, or —C(O)R7; R6 represents independently for each occurrence hydrogen, alkyl, or cycloalkyl; R7 represents independently for each occurrence alkyl or cycloalkyl; R8 is hydrogen or alkyl; R9 is alkyl, cycloalkyl, haloalkyl, —(C(R6)2)m-cycloalkyl, —C(R6)2)m—CN, aryl, aralkyl heteroaryl, or heteroaralkyl; R10 is alkyl, cycloalkyl, —(C(R6)2)m-cycloalkyl, haloalkyl, or C1-C6alkoxy; R11 represents independently for each occurrence hydrogen or an alkali metal; n is 1 or 2; and m is 1, 2, 3, 4, or 5.
地址 Ann Arbor MI US
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