Spiro�heterocycle-imidazo�1,2-a!indeno�1,2-e!pyrazine!-4'-ones,
preparation thereof and drugs containing same
    3.
    发明授权
    Spiro�heterocycle-imidazo�1,2-a!indeno�1,2-e!pyrazine!-4'-ones, preparation thereof and drugs containing same 失效
    螺[杂环咪唑并[1,2-a]茚并[1,2-e]吡嗪] -4'-酮,其制备方法和含有它们的药物

    公开(公告)号:US5777114A

    公开(公告)日:1998-07-07

    申请号:US836410

    申请日:1997-06-30

    CPC分类号: C07D471/20 C07D487/20

    摘要: Compounds of formula (I): ##STR1## wherein R.sub.3 and R.sub.4, taken together with the carbon atom to which they are attached, form (a) a 2- or 3-pyrrolidine ring, a 2- or 4-piperidine ring or a 2-azacycloheptane ring, said rings being optionally substituted at the nitrogen atom by an alkyl, --CHO, --COOR.sub.11, --CO--alk--COOR.sub.6, --CO--alk--NR.sub.6 R.sub.12, --CO--alk--CONR.sub.6 R.sub.8, --CO--COOR.sub.6, --CO--CH.sub.2 --O--CH.sub.2 --COOR.sub.6, --CO--CH.sub.2 --S--CH.sub.2 --COOR.sub.6, --CO--CH.dbd.CH--COOR.sub.6, CO--alk, --CO--Ar", --CO--alk--Ar", --CO--NH--Ar", --CO--NH--alk--Ar", --CO--Het, --CO--alk--Het, --CO--NH--Het, --CO--NH--alk--Het, --CO--NH.sub.2, --CO--NH--alk, --CO--N(alk)alk', --CS--NH.sub.2, --CS--NH--alk, --CS--NH--Ar", --CS--NH--Het, --alk--Het, --alk--NR.sub.6 R.sub.8, --alk--COOR.sub.6, --alk--CO--NR.sub.6 R.sub.8, --alk--Ar", --SO.sub.2 --alk or --SO.sub.2 --Ar radical, or a --CO-cycloalkyl radical where the cycloalkyl is optionally 2-substituted by a carboxyl radical; or (b) a 2-pyrrolidin-5-one ring. The compounds of formula (I) have useful pharmacological properties and are .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and especially NMDA receptor glycine modulation site ligands.

    摘要翻译: PCT No.PCT / FR95 / 01430 Sec。 371日期:1997年6月30日 102(e)日期1997年6月30日PCT 1995年10月30日PCT PCT。 WO96 / 14318 PCT公开号 日期:1996年5月17日式(I)化合物:其中R 3和R 4与它们所连接的碳原子一起形成(a)2-或3-吡咯烷环, 或4-哌啶环或2-氮杂环庚烷环,所述环任选在氮原子上被烷基,-CHO,-COOR11,-CO-烷基-COOR6,-CO-alk-NR6R12,-CO- CONR6R8,-CO-COOR6,-CO-CH2-O-CH2-COOR6,-CO-CH2-S-CH2-COOR6,-CO-CH = CH-COOR6,-CO-烷基,-CO-Ar“ CO-NH-Ar“,-CO-NH-alk-Ar”,-CO-Het,-CO-alk-Het,-CO-NH-Het,-CO- NH-alk-Het,-CO-NH2,-CO-NH-alk,-CO-N(alk)alk',-CS-NH2,-CS-NH-alk,-CS-NH-Ar“ CS-NH-Het,-alk-Het,-alk-NR6R8,-alk-COOR6,-alk-CO-NR6R8,-alk-Ar“,-SO2-alk或-SO2-Ar基,或-CO - 环烷基,其中环烷基任选被羧基任意地2-取代; 或(b)2-吡咯烷-5-酮环。 式(I)化合物具有有用的药理学性质,并且是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体拮抗剂,所述受体也称为quisqualate受体。 此外,式(I)化合物是非竞争性N-甲基-D-天冬氨酸(NMDA)受体拮抗剂,特别是NMDA受体甘氨酸调节位点配体。

    1,4-Oxathiino[2,3-c]pyrrole derivatives
    9.
    发明授权
    1,4-Oxathiino[2,3-c]pyrrole derivatives 失效
    1,4-oxathiino {8,2,3- C {9吡咯衍生物

    公开(公告)号:US4021554A

    公开(公告)日:1977-05-03

    申请号:US628927

    申请日:1975-11-05

    CPC分类号: C07D215/38 C07D497/04

    摘要: 1,4-Oxathiino[2,3-c]pyrrole derivatives of the formula: ##STR1## wherein A represents a phenyl, 2-pyridyl, 3-pyridazinyl, 2-quinolyl or naphthyridinyl radical, or a said radical substituted by one or two atoms or radicals selected from halogen, alkyl of 1 through 4 carbon atoms, alkoxy of 1 through 4 carbon atoms and nitro, and R represents alkyl of 1 through 4 carbon atoms, cycloalkyl of 3 through 6 carbon atoms, alkenyl of 2 through 4 carbon atoms or alkynyl of 2 through 4 carbon atoms, possess pharmacological properties, and are especially useful as tranquillizers, anti-convulsant agents, decontracturants, and agents to produce hypnosis.

    摘要翻译: 其中A代表苯基,2-吡啶基,3-哒嗪基,2-喹啉基或萘啶基,或被一个或多个取代基取代的所述基团取代的下式的1,4-氧硫杂环丁烷并[2,3-c] 选自卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基和硝基的两个原子或基团,R表示1至4个碳原子的烷基,3至6个碳原子的环烷基,2至4的烯基 具有2至4个碳原子的碳原子或炔基具有药理学性质,并且特别可用作镇静剂,抗惊厥剂,脱保护剂和产生催眠剂的试剂。

    Complexes derived from platinum, their preparation and the
pharmaceutical compositions which contain them
    10.
    发明授权
    Complexes derived from platinum, their preparation and the pharmaceutical compositions which contain them 失效
    衍生自铂的复合物,其制备物和含有它们的药物组合物

    公开(公告)号:US5225207A

    公开(公告)日:1993-07-06

    申请号:US775410

    申请日:1991-10-15

    IPC分类号: C07F15/00

    CPC分类号: C07F15/0093

    摘要: New complexes of general formula (I) in whichR.sub.1 and R.sub.2 together form a saturated or unsaturated polycyclic carbocyclic radical containing 7 to 12 carbon atoms, or a saturated or partially saturated mono-, bi- or tricyclic heterocyclic radical containing 5 to 11 chain members and a hetero-atom chosen from oxygen, sulphur or nitrogen, which latter atom can optionally be substituted by an alkoxycarbonyl radical, and,X.sub.1 and X.sub.2 represent chlorine atoms or together formeither a radical of structure: ##STR1## in which n is 0 to 2 and R.sub.6 and R.sub.7, which are identical or different, are hydrogen atoms or, when n=1, can be alkyl radicals or form, together with the carbon atom to which they are attached, a cyclobutyl radical,or a radical of structure: ##STR2## in which n, R.sub.6 and R.sub.7 are defined as above, or their salts where such exist, and their hydrates, their preparation and the pharmaceutical compositions which contain them. ##STR3##

    摘要翻译: 通式(I)的新络合物,其中R 1和R 2一起形成含有7至12个碳原子的饱和或不饱和多环碳环基团,或含有5至11个链成员的饱和或部分饱和的单,双或三环杂环基团 和选自氧,硫或氮的杂原子,其后一个原子可任选被烷氧基羰基取代,并且,X 1和X 2表示氯原子或一起形成结构式如下的基团:其中 n为0〜2,R6和R7为相同或不同的氢原子,n = 1时,可以为烷基,也可以与它们所连接的碳原子一起形成环丁基或 结构基团:其中n,R6和R7如上所定义,或其盐,如此存在,以及它们的水合物,它们的制备和含有它们的药物组合物。 (一)