发明授权
- 专利标题: PHTHALAZINE DERIVATIVES FOR TREATING INFLAMMATORY DISEASES
- 专利标题(中): 酞炎症性疾病的治疗
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申请号: EP00920604.6申请日: 2000-03-28
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公开(公告)号: EP1165085B1公开(公告)日: 2006-06-14
- 发明人: BOLD, Guido , DAWSON KING, Janet , FREI, Jörg , HENG, Richard , MANLEY, Paul, William , WIETFELD, Bernhard , WOOD, Jeanette, Marjorie
- 申请人: Novartis AG , Novartis Pharma GmbH
- 申请人地址: Lichtstrasse 35 4056 Basel CH
- 专利权人: Novartis AG,Novartis Pharma GmbH
- 当前专利权人: Novartis AG,Novartis Pharma GmbH
- 当前专利权人地址: Lichtstrasse 35 4056 Basel CH
- 代理机构: de Weerd, Petrus G.W.
- 优先权: CH60399 19990330; GB9916064 19990708
- 国际公布: WO2000059509 20001012
- 主分类号: A61K31/50
- IPC分类号: A61K31/50 ; C07D401/06 ; C07D401/12 ; C07D401/14 ; C07D471/04 ; A61P29/00 ; A61P19/02
摘要:
The invention relates to the treatment of an inflammatory disease, and/or pain with an inhibitor of VEGF receptor tyrosine kinase of formula (I), wherein r is 0 to 2, n is 0 to 3, R1 and R2 a) are independently in each case lower alkyl; b) together form a bridge of subformula (I*), wherein the bond is achieved via the two terminal C atoms and m is 0 to 4, or c) together form a bridge of subformula (I**), wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen and the others are in each case CH, and the bond is achieved via atoms T1 and T4; G is -C(=O)-, CHF-, -CF2-, lower alkylene, C2-C6alkenylene, lower alkylene or C3-C6alkenylene substituted by acyloxy or hydroxy, -CH2-O-, -CH2-S-, -CH2-NH-, -CH2-O-CH2-, -CH2-S-CH2-, -CH2-NH-CH2-, oxa (-O-), thia (-S-), imino (-NH-), -CH2-O-CH2-, -CH2-S-CH2- or -CH2-NH-CH2-; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; Q is lower alkyl, lower alkoxy or halogen; Ra and Ra' are each independently H or lower alkyl; X is imino, oxa, or thia; Y is hydrogen, aryl, heteroaryl, or unsubstituted or substituted cycloalkyl; and Z is mono- or disubstituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono-or N, N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, alkylphenylsulfonyl, or (alternatively or, in a broader aspect of the invention, in addition) selected from the group consisting of ureido, halo-lower alkylthio, halo-lower alkansulfonyl, pyrazolyl, lower-alkyl pyrazolyl and C2-C7alkenyl; wherein - if more than 1 radical Z (m ≥ 2) is present - the substituents Z are selected independently from each other; and wherein the bonds characterized in subformula (I) by a wavy line are either single or double bonds; or an N-oxide of said compound, wherein 1 or more N atoms carry an oxygen atom; or a pharmaceutically acceptable salt thereof.
公开/授权文献
- EP1165085A1 PHTHALAZINE DERIVATIVES FOR TREATING INFLAMMATORY DISEASES 公开/授权日:2002-01-02
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