- 专利标题: Novel Potassium Channel Blockers
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申请号: US12550860申请日: 2009-08-31
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公开(公告)号: US20100087428A1公开(公告)日: 2010-04-08
- 发明人: Mushtaq Mulla , Derek Edward John , Richard John Hamlyn , Sasha Louise Garrett , Basil Hartzoulakis , David Madge , John Ford
- 申请人: Mushtaq Mulla , Derek Edward John , Richard John Hamlyn , Sasha Louise Garrett , Basil Hartzoulakis , David Madge , John Ford
- 申请人地址: GB Cambridge
- 专利权人: Xention Limited
- 当前专利权人: Xention Limited
- 当前专利权人地址: GB Cambridge
- 优先权: GB0815782.8 20080829
- 主分类号: A61K31/415
- IPC分类号: A61K31/415 ; C07D231/04 ; C07D233/66 ; C07D213/62 ; C07D265/36 ; A61K31/4164 ; A61K31/44 ; A61K31/538 ; A61P19/02 ; A61P17/06 ; A61P37/00
摘要:
The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein; X1 is selected from a group consisting of CH2, C(═O), C(═NH), NC(═O), R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl R2 is selected from the group consisting of optionally substituted alkyl, optionally substituted aryl or heteroaryl or NR24R25 R3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino sulfonyl or nitrile; R4 is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted sulfonyl, optionally substituted sulfamoyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl R5 may be hydrogen, an optionally substituted alkyl, preferably CH3 or, NR4R5 may form an optionally substituted saturated or partially saturated 4-7 membered ring with the general formula (II). Wherein; X2 is C(═O), CH2, CH(R6) or C(R6)(R6), X3 is CH2, CH(R7), C(R7)(R7), NH, N(R8), O or S Each R6 independently represents optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted heteroaryl; Each R7 independently represents optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted hetero aryl R8 is optionally substituted acyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R24 and R25 are the same or different and each represents hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl, n=1 or 2 m=1, 2 or 3 With the proviso that when X1 is C═O and R5 is H then R4 is not: Or Or Where R4a, R5a and R6a are each independently H, C1-6alkyl, aryl, heteroaryl, cycloalkyl, or aryl-C1-6alkyl; R10a is H or C1-6alkyl; and R11a is C1-6alkyl or aryl-C1-6alkyl and when X1 is C═O or CH2 and R5 is H then R4 is not: Where q is 0 to 5, R3b is H, OH or alkoxy and R4b is NH2, phenyl or a C3-10 heterocycle. The compounds are useful as potassium ion channel inhibitors.
公开/授权文献
- US08673901B2 Potassium channel blockers 公开/授权日:2014-03-18
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