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INDOLINONES SUBSTITUEES EN POSITION 6, LEUR PREPARATION ET LEUR UTILISATION EN TANT QUE MEDICAMENTS
专利权人:
Boehringer Ingelheim Pharma GmbH & Co. KG
发明人:
HECKEL, Armin,ROTH, Gerald, Jürgen,WALTER, Rainer,VAN MEEL, Jacobus,REDEMANN, Norbert,TONTSCH-GRUNT, Ulrike,SPEVAK, Walter,HILBERG, Frank
申请号:
EP00971347.0
公开号:
EP1224170B9
申请日:
2000.10.09
申请国别(地区):
EP
年份:
2017
代理人:
摘要:
6-Carboxy-3-(anilino- or cycloalkylamino-methylene)-indolin-2-one or -thione derivatives (I) are new. 6-Carboxy-3-(anilino- or cycloalkylamino-methylene)-indolin-2-one or -thione derivatives of formula (I) and their tautomers, diastereomers, enantiomers (and mixtures) and salts are new. [Image] X : O or S; R 1H or prodrug residue; R 2COOH, (1-6C) alkoxycarbonyl (optionally substituted (os) terminally by Ph, heteroaryl, COOH, alkoxycarbonyl, CONH 2, mono- or dialkylaminocarbonyl or (in the case of (2-6C) alkoxycarbonyl) Cl, OH, alkoxy, NH 2 or mono- or dialkylamino), (5-7C) cycloalkoxycarbonyl, arylalkoxycarbonyl, CONH 2, CONHMe or ethylaminocarbonyl (os in the 2-position by OH or alkoxy); or di-(1-2C alkyl)-aminocarbonyl if R 4 is other than aminosulfonylphenyl or N-(1-5C alkyl)-alkylaminocarbonylphenyl; R 3H, 1-6C alkyl, 3-7C cycloalkyl, CF 3 or heteroaryl; or phenyl or naphthyl (both os by 1 or 2 of halo, CF 3, alkyl or alkoxy, and further os by OH, hydroxyalkyl, alkoxyalkyl, CN, carboxyalkyl, alkoxycarbonyl, CONH 2, mono- or dialkylaminocarbonyl, NO 2, NH 2, mono- or dialkylamino, aminoalkyl, alkylcarbonylamino, N-(alkyl)-alkylcarbonylamino, alkylcarbonylaminoalkyl, N-(alkyl)-alkylcarbonylaminoalkyl, alkylsulfonylamino, alkylsulfonylaminoalkyl, N-(alkyl)-alkylsulfonylamino, N-(alkyl)-alkylsulfonylaminoalkyl, arylalkylaminosulfonyl, 4-7C cycloalkylamino, Q, Q-CO-, Q-SO 2-, Q-alkyl-, Q-CO-alkyl-, Q-SO 2-alkyl-, heteroaryl or heteroarylalkyl); Q : 4-7 membered cycloalkyleneimino (CAI), where CH 2 in the 4-position of 6- or 7-membered CAI is optionally replaced by O, S, SO, SO 2, NH or N(alkyl); R 43-7C cycloalkyl (in which the CH 2 in the 4-position of 6-7 membered cycloalkyl is os by NH 2 or mono- or dialkylamino or replaced by NH or N(alkyl)); or phenyl substituted by R 6 and further os by 1 or 2 of halo, 1-5C alkyl, CF 3, alkoxy, COOH, alkoxycarbonyl, NH 2, NHCOMe, alkylsulfonylamino, CONH 2, mono- or dialkylaminocarbonyl, SO 2NH 2, mono- or dialkylaminosulfonyl,
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