发明名称 Pyrazolyl guanidine F<sub>1</sub>F<sub>0</sub>-ATPase inhibitors and therapeutic uses thereof
摘要 The invention provides pyrazolyl guanidine compounds that inhibit F1Fo-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
申请公布号 US9580388(B2) 申请公布日期 2017.02.28
申请号 US201514800969 申请日期 2015.07.16
申请人 Lycera Corporation 发明人 Glick Gary D.;Hurd Alexander R.;Taylor Clarke B.;VanHuis Chad A.
分类号 A61K31/5377;A61K31/44;A61K31/4439;A61K31/425;A61K31/415;A61K31/42;C07D231/38;C07D231/40;C07D401/12;C07D405/12;C07D409/04;C07D409/12;C07D417/12;C07D487/14;C07D401/14;C07D413/12;C07D413/14;C07D403/12 主分类号 A61K31/5377
代理机构 Goodwin Procter LLP 代理人 Goodwin Procter LLP
主权项 1. A compound represented by Formula I: including all stereoisomers, geometric isomers, and tautomers; or a pharmaceutically acceptable salt or solvate of any of the foregoing; wherein: A1 is phenylene; A2 is R1 represents independently for each occurrence halogen or haloalkyl; R2 is hydrogen or alkyl; R3 is aryl, aralkyl, cycloalkyl, —(C(R8)2)m-cycloalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, —(C(R8)2)m-heterocycloalkyl, alkyl, haloalkyl, hydroxyalkyl, —(C(R8)2)m-alkoxyl, —(C(R8)2)m—O—(C(R8)2)m-alkoxyl, or —(C(R8)2)m—CN, 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, hydroxyalkyl, C1-C6alkoxy, cyano, and —C1-C6alkylene-CO2R8; R4 is hydrogen or alkyl; R5 is hydrogen or alkyl; R6 is alkyl, cycloalkyl, haloalkyl, cyano, aryl, aralkyl, heteroaryl, heteroaralkyl, —CO2R8, or —C(O)N(R10)(R11), wherein said cycloalkyl, aryl, aralkyl, heteroaryl, and heteroaralkyl are each optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, hydroxyalkyl, C1-C6alkoxy, —O-aralkyl, and cyano; R7 is hydrogen, halogen, alkyl, or haloalkyl; R8 represents independently for each occurrence hydrogen, alkyl, or cycloalkyl; or two occurrences of R8 attached to the same carbon atom are taken together with said carbon atom to form a saturated carbocylic ring; R10 and R11 each represent independently for each occurrence hydrogen, alkyl, or cycloalkyl; or R10 and R11 are taken together with the nitrogen atom to which they are attached to form a 3 to 7 membered heterocyclic ring optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, cycloalkyl, and C1-C6alkoxy; n is 1, 2, or 3; and m is 1, 2, 3, 4, or 5.
地址 Ann Arbor MI US
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