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1. 发明申请

WO2005105097A3 PYRIDOPYRIMIDINES FOR TREATING INFLAMMATORY AND OTHER DISEASES 审中-公开
公开(公告)号：WO2005105097A3
公开(公告)日：2005-11-10
申请号：PCT/EP2005/051892
申请日：2005-04-27
申请人： GPC BIOTECH AG , DAUB, Henrik , WISSING, Josef , MISSIO, Andrea , KLEBL, Bert
发明人： DAUB, Henrik , WISSING, Josef , MISSIO, Andrea , KLEBL, Bert
IPC分类号： A61K31/513 , A61P29/00 , A61P37/00
摘要： The present invention relates to the use of pyridopyrimidine derivatives having the general formula (I) wherein X represents =NH, =N-Acyl, =O, or =S; R 1 represents -NR 3 R 4 , -SR 3 , -SO-R 3 , -SO 2 -R 3 , -OR 3 ; R 2 , R 3 , and R 4 are independently of each other hydrogen, -(CH 2 ) n Ph*, heteroaryl, C 3 -C 7 -cycloalkyl, C 1 -C 6 -alkyl, C 1 -C 6 -alkanoyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR 5 R 6 , phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R 5 and R 6 are independently of each other hydrogen, (CH 2 ) n Ph*, heteroaryl, C 3 -C 7 -cycloalkyl, C 1 -C 6 -alkyl, C 1 -C 6 -alkanoyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl; R 5 and R 6 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ph* represents phenyl or substituted phenyl; n is 0, 1, 2, or 3; R 4 can optionally be -CO-R 3 , -CO-OR 3 , -SO 2 -R 3 , -SO 2 -NR 5 R 6 , -CO-NR 5 R 6 , -CS-NR 5 R 6 , -C(=NH)-R 3 , -C(=NH)-NR 5 R 6 ; R 3 and R 4 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ar represents phenyl, substituted phenyl, or heteroaryl; and pharmaceutically acceptable salts thereof for prophylaxis and/or treatment of inflammatory diseases, neurodegenerative disorders, immunological diseases, neuroimmunological diseases, autoimmune diseases, diabetes, transplant rejection, infective diseases, prion diseases, cardiovascular diseases and disorders.

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