Perhydroisoindole derivatives as substance P antagonists
    20.
    发明授权
    Perhydroisoindole derivatives as substance P antagonists 失效
    全氢异吲哚衍生物作为P物质拮抗剂

    公开(公告)号:US5739351A

    公开(公告)日:1998-04-14

    申请号:US849177

    申请日:1997-05-30

    摘要: New perhydroinsoindole having the general formula (I) wherein R.sub.1 is optionally substituted phenyl or is cyclohexadienyl, naphtyl, indenyl or mono or polycyclic heterocyclyl, saturated or unsaturated 5 to 9C and optionally substituted, R.sub.2 is H or halogen, OH, alkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, alkyloxycarbonyl, dialkylaminoalcyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R.sub.3 is phenyl optionally substituted in position -2 by a radical alkyl or alkyloxy 1 or 2C or by OH or F, or disubstituted by CF.sub.3, and R.sub.4 is an alkyl radical containing 1 or 2C substituted by halogen or CN, N.sub.3 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.

    摘要翻译: PCT No.PCT / FR95 / 01577 Sec。 371日期1997年5月30日 102(e)日期1997年5月30日PCT提交1995年11月29日PCT公布。 公开号WO96 / 16939 (Ia)具有通式(I)的新的全氢异吲哚,其中R 1为任选取代的苯基或环己二烯基,萘基,茚基或单环或多环杂环基,饱和或不饱和的5 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,二烷基氨基羰基氧基羰基,苄氧羰基,氨基或酰氨基,R3是任选被取代的苯基, 2或由OH或F取代或被CF 3二取代的烷基,R 4是含有1或2个被卤素或CN,N 3或-NHCN取代的烷基,基团R相同或相同, 不同的是代表具有结构(Ia)或其混合物的异构体形式的H,烷基或苯基,当它们存在时可以是它们的盐和它们的制备。 本发明的新衍生物特别可用作物质P的拮抗剂。