发明名称 BIOLOGICALLY ACTIVE 3-SUBSTITUTED OXINDOLE DERIVATIVES USEFUL AS ANTI-ANGIOGENIC AGENTS
摘要 The new use of a compound of formula (I) wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole; n is zero or an integer of 1 to 3; R1 is hydrogen, C1-C6 alkyl or C2-C6 alkanoyl; R2 is hydrogen, halogen, C1-C6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C1-C6 alkyl; R3 is hydrogen or C1-C6 alkyl; R4 is hydrogen, hydroxy, C1-C6 alkoxy, C2-C6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above; R5 is hydrogen, C1-C6 alkyl or halogen; or a pharmaceutically acceptable salt thereof; and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR1, R2 and oxindolylidene may be independently on either of the aryl or heteroaryl moieties of said bicyclic ring, whereas only the benzene moiety is substituted when Y is tetralin; and wherein when Y is naphthalene, tetralin, quinoline or isoquinoline, then R2 is hydrogen, halogen, cyano or C1C6 alkyl and R3, R4 and R5 are hydrogen; whereas when Y is indole, then R2 is hydrogen, halogen, C1-C6 alkyl, cyano, carboxy, nitro or -NHR, in which R is as defined above, R3 is hydrogen or C1-C6 alkyl, R4 is hydrogen, hydroxy, C1C6 alkoxy, C2-C6 alkanoyloxy, carboxy, nitro or -NHR, wherein R is as defined above, and R5 is hydrogen, halogen or C1-C6 alkyl; as anti-angiogenic agent is disclosed.
申请公布号 CA2155098(A1) 申请公布日期 1995.06.29
申请号 CA19942155098 申请日期 1994.11.08
申请人 PHARMACIA S.P.A. 发明人 BUZZETTI, FRANCO;LONGO, ANTONIO;BRASCA, MARIA GABRIELLA;ORZI, FABRIZIO;CRUGNOLA, ANGELO;BALLINARI, DARIO;MARIANI, MARIANGELA
分类号 C07D401/06;A61K31/40;A61K31/403;A61K31/404;A61K31/47;A61K31/475;A61K31/505;A61K31/675;A61K31/70;A61K38/04;A61P27/02;A61P29/00;A61P35/00;C07D209/34;(IPC1-7):A61K31/40 主分类号 C07D401/06
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