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    • 2. 发明公开
    • DERIVES DE PERHYDROISOINDOLE COMME ANTAGONISTES DE LA SUBSTANCE P
    • DERIVES DE PERHYDROISOINDOLE COMME ANTAGONISTES DE LA物质P
    • EP0794944A1
    • 1997-09-17
    • EP95941161.0
    • 1995-11-29
    • RHONE-POULENC RORER S.A.
    • ACHARD, DanielPEYRONEL, Jean-FrançoisTABART, Michel
    • A61K31A61P1A61P9A61P11A61P25A61P27A61P29A61P43C07D209C07D401C07D409
    • C07D401/06C07D209/44C07D409/06
    • New perhydroinsoindole having the general formula (I) wherein R1 is optionally substituted phenyl or is cyclohexadienyl, naphtyl, indenyl or mono or polycyclic heterocyclyl, saturated or unsaturated 5 to 9C and optionally substituted, R2 is H or halogen, OH, alkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, alkyloxycarbonyl, dialkylaminoalcyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R3 is phenyl optionally substituted in position -2 by a radical alkyl or alkyloxy 1 or 2C or by OH or F, or disubstituted by CF3, and R4 is an alkyl radical containing 1 or 2C substituted by halogen or CN, N3 or -NHCN, and the radicals R which are similar or different represent H, alkyl or phenyl, in their isomer forms having the structure (Ia) or mixtures thereof, optionally their salts when they exist and preparation thereof. The new derivatives of the invention are particularly useful as antagonists of substance P.
    • 具有通式(I)的新的全氢异吲哚:其中R 1是任选取代的苯基或是环己二烯基,萘基,茚基或单环或多环杂环基,饱和或不饱和的5至9℃和任选取代的,R 2是H或卤素,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,烷氧基羰基,二烷基氨基酰氧基羰基,苄氧基羰基,氨基或酰氨基,R3是在-2位任选被基团烷基或烷氧基1或2C或OH或F取代的苯基, (Ia)的异构体形式中,R4是含有被卤素或CN,N3或-NHCN取代的1或2C的烷基,且相同或不同的基团R表示H,烷基或苯基, 或它们的混合物,当它们存在时其任选的盐及其制备。 本发明的新衍生物作为物质P的拮抗剂特别有用。
    • 6. 发明公开
    • DERIVES DE PERHYDROISOINDOLE COMME ANTAGONISTES DE LA SUBSTANCE P
    • DERIVES DE PERHYDROISOINDOLE COMME ANTAGONISTES DE LA物质P
    • EP0711280A1
    • 1996-05-15
    • EP94923755.0
    • 1994-07-28
    • RHONE-POULENC RORER S.A.
    • ACHARD, DanielGRISONI, SergeJAMES-SURCOUF, EvelyneMALLERON, Jean-LucMORGAT, AnnePEYRONEL, Jean-FrançoisSABUCO, Jean-FrançoisTABART, Michel
    • A61K31A61P11A61P29A61P37A61P43C07D209
    • C07D209/44
    • 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.
    • 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。