首页> 外国专利> 4 - oxo - Derivatives of 1, 3, 8 - triaza 4.5 Deans as inhibitors of Potassium Channel Kv1.5, a composition that includes and its use in the treatment of heart disease.

4 - oxo - Derivatives of 1, 3, 8 - triaza 4.5 Deans as inhibitors of Potassium Channel Kv1.5, a composition that includes and its use in the treatment of heart disease.

机译:4-氧代-1,3,8-triaza的衍生物[4.5]迪恩斯作为钾通道Kv1.5的抑制剂,该组合物包括及其在心脏病治疗中的用途。

摘要

Derivatives of 4 - oxo - 1,3,8 triaza - spiro [4,5] Deans which are useful as inhibitors of 1.5 kV Potassium Channel activity and that provide for atrial Selective antiarrhythmic. Compositions and their use for treating atrial antiarritmia - selective.Claim 1: a compound having the formula (1), in which R is optionally substituted phenyl optionally substituted phenyl; r1 is alkyl; R2 is C1 - 6 linear or branched optionally substituted cycloalkyl, optionally substituted C3 - 6 or - C (o) R23,Where R23 is C1 - 6 linear or branched alkyl, optionally substituted cycloalkyl or C3 6 optionally substituted; R3 is Hydrogen; select between: 1) 2) C1 - 6 linear or branched alkyl, optionally substituted cycloalkyl, optionally substituted or C3 - 6; 3) - C (o) where alkyl R4, R4 is C1 - 6 Linear or branched optionally substituted cycloalkyl, optionally substituted C3 6,Optionally substituted heterocycle.Optionally substituted aryl or heteroaryl optionally substituted; 4) - C (o) where each nr5r6 R5 and R6 is selected regardless of: a) b) hydrogen; C1 - 6 linear or branched alkyl, optionally substituted cycloalkyl C3 - 7; c) optionally substituted; (d) - or7; R7 is Hydr Ogeno or C1 - 6 linear or branched alkyl, optionally substituted; e) nr8r9; where each R8 andR9 is independently Hydrogen, C1 - 6 linear or branched alkyl, optionally substituted C1 - 6 linear or branched alkoxy optionally substituted,- or Oh - co2r10; where R10 is C1 - 6 linear or branched alkyl, optionally substituted; or R8 and R9 can be taken together with e! Carbon Atom to which they are United to form a Ring optionally substituted has 3 to 7 Atoms in the ring and optionally containing one or more heteroatoms in the Ring selected independently among nO or s; or (f) R5 and R6 can be taken together with the carbon Atom to which they are United to form a Ring optionally substituted has 3 to 7 Atoms in the ring and optionally containing one or more heteroatoms in the Ring selected regardless of N, or S; 5) - C (R12, nr11)Where r11es to hydrogen); (b) C1 - 6 linear or branched alkyl, optionally substituted cycloalkyl, optionally substituted or C3 - 6; (c) - (d); or - ns; and R12) is a linear or branched alkyl C1 - 6 or optionally substituted cycloalkyl, optionally substituted C3 - 6; (b) - OR13, where R13 is Hydrogen C1 - 6, linear or branched alkyl, optionally substituted,C3 - optionally substituted cycloalkyl optionally substituted aryl or 6; or c) where each nr14r15 R14 and R15 is independently Hydrogen, optionally substituted aryl, alkyl C1 - 6 linear or branched or optionally substituted cycloalkyl, optionally substituted C3 - 8; 6) - so2r16; Donde R16 is optionally substituted aryl,C1 - 6 linear or branched alkyl, optionally substituted cycloalkyl, optionally substituted or C3 - 6; 7) - C (o) R17, where aryl or heteroaryl R17 is optionally substituted or optionally substituted; 8) - C (o) or18; where R18 is C1 - 6 linear or branched alkyl, optionally substituted, cicloalqui The C3 - 6 optionally substituted aryl or optionally substituted; L, L1 and L2 are units of Union,Each independently is a unit that has the formula: - [C (R19) 2] n -, in which each R19, in each case, Selected independently from Hydrogen, Methyl or Ethyl, N is 1 to 4; and each of X, y and Z is independently 0 OR 1; or a Pharmaceutical Salt form to Number of the same.
机译:4-氧代-1,3,8 triaza-spiro的衍生物[4,5]迪恩斯可用作1.5 kV钾离子通道活性的抑制剂,并提供心房选择性抗心律失常药。 1。一种具有式(1)的化合物,其中R是任选取代的苯基和任选取代的苯基; r1是烷基; R 2是C 1-6直链或支链的任选取代的环烷基,可选被取代的C 3-6或-C(o)R 23,其中R 23是C 1-6直链或支链的烷基,任选被取代的环烷基或C 3-6任选被取代; R3是氢;在以下之间选择:1)2)C1-6直链或支链烷基,任选取代的环烷基,任选取代或C3-6; 3)-C(o),其中烷基R 4,R 4为C 1-6直链或支链的任选取代的环烷基,任选取代的C 3 6,任选取代的杂环。任选取代的芳基或任选取代的杂芳基; 4)-C(o),其中每个nr5r6 R5和R6均被选择,而与:a)b)氢无关; C1-6直链或支链烷基,任选取代的环烷基C3-7; c)任选取代的; (d)-或7; R7是Hydr Ogeno或C1-6直链或支链烷基,任选被取代; e)nr8r9;其中每个R 8和R 9独立地为氢,C 1-6直链或支链的烷基,任选取代的C 1-6直链或支链的烷氧基,任选被取代的-或Oh-co2r10;其中R 10为C 1-6直链或支链烷基,任选取代;或R8和R9可以与e一起使用!它们被连接以形成任选取代的环的碳原子在环中具有3至7个原子,并且在环中任选地包含一个或多个独立地选自nO或s中的杂原子; (f)R5和R6可以与它们所连接的碳原子一起形成一个环,该环任选被取代,在环中具有3至7个原子,并且在选择的环中任选包含一个或多个杂原子,而与N无关,或S; 5)-C(R12,nr11),其中r11为氢); (b)C1-6直链或支链的烷基,任选取代的环烷基,任选取代的或C3-6; (c)-(d);或-ns; R12)为直链或支链的烷基C1-6或可具有取代基的环烷基,可具有取代基的C3-6; (b)-OR13,其中R13是氢C1-6,直链或支链的烷基,任选取代的,C3-任选取代的环烷基,任选取代的芳基或6; c)其中每个nr14r15的R14和R15独立地为氢,任选取代的芳基,烷基C1-6为直链或支链或任选取代的环烷基,任选取代的C3-8;或6)-so2r16; Donde R 16是任选取代的芳基,C 1-6直链或支链的烷基,任选取代的环烷基,任选取代的或C 3-6; 7)-C(o)R17,其中芳基或杂芳基R17是任选取代的或任选取代的; 8)-C(o)或18;其中R 18为C 1-6直链或支链的烷基,任选取代的,环氯基。C 3-6任选取代的芳基或任选取代的; L,L1和L2是Union的单元,每个独立地是具有以下公式的单元:-[C(R19)2] n-,其中每个R19在每种情况下均独立选自氢,甲基或乙基,N是1到4; X,y和Z各自独立地为0或1;或药用盐形式至相同编号。

著录项

  • 公开/公告号AR061522A1

    专利类型

  • 公开/公告日2008-09-03

    原文格式PDF

  • 申请/专利权人 WYETH;

    申请/专利号AR2007P102687

  • 发明设计人

    申请日2007-06-19

  • 分类号C07D471/10;A61K31/4747;A61P9/04;A61P9/06;C07D471/10;C07D221/00;

  • 国家 AR

  • 入库时间 2022-08-21 20:08:55

相似文献

  • 专利
  • 外文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号