发明授权
US07208503B2 Angiogenesis inhibiting 5-substituted-1,2,4-thiadiazolyl derivatives
失效
血管发生抑制5-取代-1,2,4-噻二唑衍生物
- 专利标题: Angiogenesis inhibiting 5-substituted-1,2,4-thiadiazolyl derivatives
- 专利标题(中): 血管发生抑制5-取代-1,2,4-噻二唑衍生物
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申请号: US10387703申请日: 2003-03-13
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公开(公告)号: US07208503B2公开(公告)日: 2007-04-24
- 发明人: Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
- 申请人: Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
- 申请人地址: BE
- 专利权人: Janssen Pharmaceutica N.V.
- 当前专利权人: Janssen Pharmaceutica N.V.
- 当前专利权人地址: BE
- 主分类号: A01N43/40
- IPC分类号: A01N43/40 ; A61K31/445 ; C07D211/68
摘要:
This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH—, C3-6cycloalkyl, hydroxymethyl or benzoyloxymethyl; R2 is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; is Ar2, Ar2CH2— or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
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