发明公开
- 专利标题： 5-AROYLNAPHTHALENE DERIVATIVES
- 专利标题（中）： 5-芳酰基萘衍生物
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申请号： EP98905325.0申请日： 1998-01-21
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公开(公告)号： EP0966437A1公开(公告)日： 1999-12-29
- 发明人: ROTSTEIN, David, Mark , SJOGREN, Eric, Brian
- 申请人： F.HOFFMANN-LA ROCHE AG
- 申请人地址： Grenzacherstrasse 124 4070 Basel CH
- 专利权人： F.HOFFMANN-LA ROCHE AG
- 当前专利权人： F.HOFFMANN-LA ROCHE AG
- 当前专利权人地址： Grenzacherstrasse 124 4070 Basel CH
- 代理机构： Löschner, Thomas, et al
- 优先权： US19970036466P 19970128
- 国际公布： WO1998032732 19980730
- 主分类号： C07D295
- IPC分类号： C07D295 ; A61K31 ; A61P29 ; A61P37 ; A61P43 ; C07C311 ; C07C317 ; C07C323 ; C07D207 ; C07D211 ; C07D213 ; C07D307 ; C07D333 ; C07D405
摘要：
The present invention relates to certain 5-aroylnaphthalene derivatives of formula (I), wherein A is a bond, -CH2-, -CH(OH)-, -C=NOR4-, -C(O)-, -NR5-, -O-, or -S(O)¿n?- where n is an integer from 0 to 2, R?4¿ is hydrogen or alkyl, and R5 is hydrogen, alkyl, or acyl; Z is a group represented by formula (B), (C), (D), or (E), where n1 is 0 to 3; X is O or S; R?6 and R7¿ are independently selected from hydrogen, alkyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, acyl, alkylthio, cycloalkylthio, cycloalkylalkylthio, alkoxy, cycloalkyloxy, cycloalkylalkyloxy, halogenalkyloxy, alkenyl, halogen, cyano, nitro, hydroxy, or -NR9R10 where R?9 and R10¿ are independently hydrogen, alkyl, or acyl; or R?6 and R7¿ when they are adjacent to each other form methylenedioxy or ethylenedioxy; R8 is hydrogen, alkyl, halogenalkyl, alkoxy, cycloalkyloxy, halogenalkyloxy, alkylthio, cycloalkylthio, nitro, cyano, hydroxy, or halogen; R1 is hydrogen, alkyl, alkenyl, alkynyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, alkoxy, alkenyloxy, cycloalkyloxy, cycloalkylalkyloxy, halogenalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, alkylthio, cycloalkylthio, cycloalkylalkylthio, hydroxy, halogen, cyano, carboxy, alkoxycarbonyl, acyl, -C=NOR?4, -NR9R10, -CONR9R10¿, -OCONR9R10, or -OSO¿2R?11 where R?4, R9, and R10¿ are as previously defined and R11 is alkyl, cycloalkyl, or halogenalkyl; R2 is hydrogen, alkyl, alkoxy, halogen, nitro, or -NR?9R10; and R3¿ is -SO¿2R?12 or -SO¿2?NR?13R14¿ where R12 is alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, or alkoxycarbonylalkyl; R13 is hydrogen, alkyl, or acyl; and R14 is hydrogen, alkyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonylalkyl, amino, aminoalkyl, aryl, aralkyl, heteroaralkyl, heterocyclo, heterocycloalkyl, acyl, hydroxy, or alkoxy; or R?13 and R14¿ together with the nitrogen atom to which they are attached optionally form a heterocycloamino group; that are inhibitors of prostaglandin G/H synthase, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
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