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MACROCYCLIC UREA AND SULPHAMIDE DERIVATIVES AS TAFIa INHIBITORS
专利权人:
SANOFI-AVENTIS
发明人:
KALLUS Kristofer (DE),КАЛЛУС Кристофер (DE),BRENSTRUP Mark (DE),БРЕНСТРУП Марк (DE),EhFERS Andreas (DE),ЭФЕРС Андреас (DE),GLOBISh Anja (DE),ГЛОБИШ Аня (DE),ShROJDER Kherman (DE),ШРОЙДЕР Херман (DE),V,KALLUS KRISTOFER,КАЛЛУС Кристофер,BRENSTRUP MARK,БРЕНСТРУП Марк,EHFERS ANDREAS,ЭФЕРС Андреас,GLOBISH ANJA,ГЛОБИШ Аня,SHROJDER KHERMAN,ШРОЙДЕР Херман,VAGNER MIKHEL,ВАГНЕР Михель
申请号:
RU2010154089/04
公开号:
RU0002502736C2
申请日:
2009.05.22
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I) and/or stereoisomeric forms thereof and/or mixtures of said forms in any ratio and/or a physiologically tolerant salt of the compound of formula , where: X denotes -C(O)- or -SO2-, U denotes an oxygen atom or -(C0-C4)alkylene, A denotes an oxygen atom, -C(O)-NH-, -NH-C(O)- or -(C0-C4)alkylene, V denotes: 1) -(C2-C9)alkylene, where alkylene is unsubstituted or mono-, di- or tri-substituted, independently of each other, by an -OH group, 2) -(C3-C9)alkenylene, D denotes -(C1-C2)alkylene, Y denotes: 1) a covalent bond, 2) -(C6-C14)arylene-, or 3) Het, where Het denotes pyridyl or imidazolyl, R1 denotes: 1) a hydrogen atom, 2) -(C1-C6)alkyl, R3 denotes: 1) -(C2-C6)alkylene-NH2, 2) -(C1-C4)alkylene-SO2-(C1-C4) alkylene-NH2 or 3) -(C0-C4) alkylene-Het, where Het denotes pyridyl or piperidyl, where Het is unsubstituted or substituted with -NH2, R6 denotes: 1) a hydrogen atom, 2) -(C1-C6) alkyl, where the alkyl is unsubstituted or substituted, independently of each other, by a R16 group, 3) -(C0-C4) alkylene-Het, where Het denotes pyridyl, where -(C0-C4) alkylene and Het are unsubstituted or substituted, independently of each other, by a R16 group, 4) -(C0-C4) alkylene-phenyl, where -(C0-C4) alkylene and phenyl are unsubstituted or substituted, independently of each other, by a R16 group, or 5) -(C0-C4) alkylene-(C3-C8)cycloalkyl, R7 denotes a hydrogen atom, halogen or -(C1-C6)alkyl, R8 denotes a hydrogen atom or -(C1-C6)alkyl, R9 denotes a hydrogen atom, and R16 denotes -NH2, which are inhibitors of the active thrombin-activated fibrinolysis inhibitor, as well as a method for production thereof, a medicinal agent based thereon and use for prevention, secondary prevention and treatment of one or more disorders associated with thrombosis, embolism, hypercoagulation or fibrosis changes.EFFECT: improved properties of compounds.7 cl, 1 tbl, 9 exДанное изобретение относится к соединениям формулы (I), и/ил
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