发明授权
US08071651B2 5-amino-4-hydroxy-7-(imidazo [1,2-A] pyridin-6-ylmethyl)-8-methyl-nonamide derivatives and related compounds as renin inhibitors for the treatment of hypertension
失效
5-氨基-4-羟基-7-(咪唑并[1,2-A]吡啶-6-基甲基)-8-甲基 - 非酰胺衍生物和相关化合物作为治疗高血压的肾素抑制剂
- 专利标题: 5-amino-4-hydroxy-7-(imidazo [1,2-A] pyridin-6-ylmethyl)-8-methyl-nonamide derivatives and related compounds as renin inhibitors for the treatment of hypertension
- 专利标题(中): 5-氨基-4-羟基-7-(咪唑并[1,2-A]吡啶-6-基甲基)-8-甲基 - 非酰胺衍生物和相关化合物作为治疗高血压的肾素抑制剂
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申请号: US11992132申请日: 2006-09-14
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公开(公告)号: US08071651B2公开(公告)日: 2011-12-06
- 发明人: Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Aleksandar Stojanovic , Christiane Marti , Dirk Behnke , Stjepan Jelakovic
- 申请人: Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Aleksandar Stojanovic , Christiane Marti , Dirk Behnke , Stjepan Jelakovic
- 申请人地址: CH Basel
- 专利权人: Novartis AG
- 当前专利权人: Novartis AG
- 当前专利权人地址: CH Basel
- 代理机构: Wenderoth, Lind & Ponack, L.L.P.
- 优先权: CH1526/05 20050917
- 国际申请: PCT/EP2006/066369 WO 20060914
- 国际公布: WO2007/031558 WO 20070322
- 主分类号: A01N43/42
- IPC分类号: A01N43/42 ; A01N43/40 ; A01N43/58 ; A01N43/00 ; A01N43/64 ; A01N37/18 ; A01N35/00 ; A01N33/18 ; A01N33/24 ; C07C233/00 ; C07C235/00 ; C07C237/00 ; C07C239/00 ; A61K31/16 ; A61K31/12
摘要:
Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R6; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.p]alkyl, all of which may be substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino, or if m=0: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino, or if m=1: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, optionally substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6-alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino; have renin-inhibiting properties and can be used as medicines for the treatment of hypertension.
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