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2. 发明公开

EP0711280A1 DERIVES DE PERHYDROISOINDOLE COMME ANTAGONISTES DE LA SUBSTANCE P 失效
标题翻译： DERIVES DE PERHYDROISOINDOLE COMME ANTAGONISTES DE LA物质P
公开(公告)号：EP0711280A1
公开(公告)日：1996-05-15
申请号：EP94923755.0
申请日：1994-07-28
申请人： RHONE-POULENC RORER S.A.
发明人： ACHARD, Daniel , GRISONI, Serge , JAMES-SURCOUF, Evelyne , MALLERON, Jean-Luc , MORGAT, Anne , PEYRONEL, Jean-François , SABUCO, Jean-François , TABART, Michel
IPC分类号： A61K31 , A61P11 , A61P29 , A61P37 , A61P43 , C07D209
CPC分类号： C07D209/44
摘要： Novel perhydroisoindole derivatives of general formula (I), wherein R1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl, R2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R3 is a phenyl radical optionally 2-substituted by C1-2 alkyloxy or alkyl or a fluorine atom, or disubstituted by trifluoromethyl, and R5 and R'5 are the same or different, one representing H or OH or alkyl while the other represents H or alkyl, R4 is OH, or else R4 is F when R5 and R'5 are H or alkyl, or R4 and R5 together form a bond, and R6 is H or alkyl, hydroxy or hydroxyalkyl; and one of the symbols R is H, alkyl, hydroxy or hydroxyalkyl while the other is H, alkyl, phenyl or hydroxyalkyl; isomeric forms with structure (Ia) or mixtures thereof; optionally salts thereof where applicable; and preparation thereof. Said novel derivatives are particularly suitable for use as P substance antagonists.
摘要翻译：其中R1为任选取代的苯基，环己二烯基，萘基，茚基或任选取代的杂环基，R2为H，卤素，OH，烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，烷氧基，烷硫基，酰氧基，羧基的新的全氢异吲哚衍生物，任选取代的烷氧基羰基，苄氧基羰基，氨基或酰氨基，R 3是任选地被C 1-2烷氧基或烷基或氟原子2取代或被三氟甲基二取代的苯基，并且R 5和R 15相同或不同，代表H或OH或烷基，而另一个代表H或烷基，R 4是OH，或者当R 5和R 15是H或烷基时，或者R 4和R 5一起形成键，并且R 6是H或烷基时，羟基或羟烷基; 并且其中一个符号R是H，烷基，羟基或羟烷基，而另一个是H，烷基，苯基或羟烷基; 具有结构（Ia）的异构形式或其混合物; 在适用的情况下任选地其盐和其制备。所述新衍生物特别适合用作P物质拮抗剂。

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