ELAINE SOPHIE ELIZABETH STOKES,PATRICK PLE,DARREN MCKERRECHER,LAURENT FRANÇOIS ANDRE HENNEQUIN
申请号：
BR0017548
公开号：
BRPI0017548B1
申请日:
2000.02.08
申请国别(地区):
BR
年份:
2015
代理人:
摘要：
The invention relates to the use of compounds of the formula I: <；CHEM>； wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S； Z is -O-, -NH-, -S-, -CH2- or a direct bond； n is 0-5； m is 0-3； R<；2>； represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, -NR<；3>；R<；4>； (wherein R<；3>； and R<；4>；, which may be the same or different, each represents hydrogen or C1-3alkyl), or R<；5>；X<；1>；- (wherein X<；1>； and R<；5>； are as defined herein； R<；1>； represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N-C1-4alkylcarbamoyl, N,N-di(C1-4alkyl)carbamoyl, aminosulphonyl, N-C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N-(C1-4alkylsulphonyl)amino, N-(C1-4alkylsulphonyl)-N-(C1-4alkyl)amino, N,N-di(C1-4alkylsulphonyl)amino, a C3-7alkylene chain joined to two ring C carbon atoms, C1-4alkanoylaminoC1-4alkyl, carboxy or a group R<；56>；X<；10>； (wherein X<；10>； and R<；56>； are as defined herein)； and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
