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    Novel 1,3-disubstituted pyrrolo[1,2-a]azepinone derivatives having anti-psychotic activity and pharmaceutical compositions containing them
    2.
    发明授权
    Novel 1,3-disubstituted pyrrolo[1,2-a]azepinone derivatives having anti-psychotic activity and pharmaceutical compositions containing them 失效
    具有抗精神病活性的新型1,3-二取代吡咯并[1,2-a]吖庚因衍生物和含有它们的药物组合物

    公开(公告)号：US4769366A

    公开(公告)日：1988-09-06

    申请号：US839101

    申请日：1986-03-13

    申请人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    发明人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    IPC分类号： A61K31/55 ,  A61P25/18 ,  C07D487/04 ,  A61K31/395 ,  C07D223/00

    CPC分类号： C07D487/04

    摘要： Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C,or (B) R is phenyl optionally substituted with one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals and R.sub.1 and R.sub.2 together form a piperazine or homopiperazine ring substituted by hydroxyalkyl (2 to 4 C), alkenyl (2 to 4 C), alkynyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CN, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, the said alkyls containing, except where otherwise stated, 1 to 4 C in a straight or branched chain,and the pharmaceutically acceptable salts thereof,are useful as antipsychotics.

    摘要翻译： 吡咯并[1,2-a]吖庚因酮衍生物，其中R 3为H或卤素，（A）R为苄基或苯硫基，其中苯基任选被一个或多个卤素或羟基取代 ，烷基，烷氧基或烷硫基，R 1和R 2可以相同或不同，表示任选被二烷基氨基取代的烷基，其中烷基任选地连接以形成被烷基取代的1-吡咯烷基，哌啶子基，吗啉代或1-哌嗪基环 或者R1和R2形成选自吡咯烷，哌啶，吗啉和哌嗪的杂环，被烷基，烯基（2至4 C），任选被卤素，烷基，烷氧基，烷硫基，CF 3，COOH取代的苄基或苯乙基取代， 羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或烷基羰氧基烷基，其中烷基羰基具有2至18个C，或（B）R是任选被一个或多个卤素或羟基，烷基，烷氧基或烷硫基取代的苯基， 和R2一起形成被羟烷基（2〜4 C），烯基（2〜4 C），炔基（2〜4 C），任选被卤素，烷基，烷氧基，烷硫基，CN取代的苄基或苯乙基取代的哌嗪或高哌嗪环 ，CF 3，COOH，羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或其中烷基羰基具有2至18个C的烷基羰氧基烷基，所述烷基除了另外说明的含有1至4个C的直链或支链以外， 其盐可用作抗精神病药。

    Process for preparing pyrrolo(1,2-A)azepinone derivatives
    3.
    发明授权
    Process for preparing pyrrolo(1,2-A)azepinone derivatives 失效
    制备吡咯（1,2-A）氮杂酮衍生物的方法

    公开(公告)号：US4826974A

    公开(公告)日：1989-05-02

    申请号：US116725

    申请日：1987-11-04

    申请人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    发明人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    IPC分类号： A61K31/55 ,  A61P25/18 ,  C07D487/04 ,  C07D487/06 ,  C07D403/14 ,  C07D413/14

    CPC分类号： C07D487/04

    摘要： Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, or (B) R is phenyl optionally substituted with one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals and R.sub.1 and R.sub.2 together form a piperazine or homopiperazine ring substituted by hydroxyalkyl (2 to 4 C), alkenyl (2 to 4 C), alkynyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CN, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, the said alkyls containing, except where otherwise stated, 1 to 4 C in a straight or branched chain, and the pharmaceutically acceptable salts thereof, are useful as antipsychotics.

    摘要翻译： 吡咯并[1,2-a]吖庚因酮衍生物，其中R 3为H或卤素，（A）R为苄基或苯硫基，其中苯基任选被一个或多个卤素或羟基取代 ，烷基，烷氧基或烷硫基，R 1和R 2可以相同或不同，表示任选被二烷基氨基取代的烷基，其中烷基任选地连接以形成被烷基取代的1-吡咯烷基，哌啶子基，吗啉代或1-哌嗪基环 或者R1和R2形成选自吡咯烷，哌啶，吗啉和哌嗪的杂环，被烷基，烯基（2至4 C），任选被卤素，烷基，烷氧基，烷硫基，CF 3，COOH取代的苄基或苯乙基取代， 羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或烷基羰氧基烷基，其中烷基羰基具有2至18个C，或（B）R是任选被一个或多个卤素或羟基，烷基，烷氧基或烷硫基取代的苯基， 和R2一起形成被羟烷基（2〜4 C），烯基（2〜4 C），炔基（2〜4 C），任选被卤素，烷基，烷氧基，烷硫基，CN取代的苄基或苯乙基取代的哌嗪或高哌嗪环 ，CF 3，COOH，羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或其中烷基羰基具有2〜18个碳原子的烷基羰氧基烷基，所述烷基除了另外说明的含有1〜4个C的直链或支链， 其盐可用作抗精神病药。

    1,4-Oxathiino[2,3-c]pyrrole derivatives
    5.
    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

    申请人： Claude Cotrel ,  Claude Jeanmart ,  Michel Barreau

    发明人： Claude Cotrel ,  Claude Jeanmart ,  Michel Barreau

    IPC分类号： C07D515/04 ,  A61K31/40 ,  A61K31/435 ,  A61K31/495 ,  A61K31/496 ,  A61K31/50 ,  A61P25/08 ,  A61P25/20 ,  C07D215/38 ,  C07D241/04 ,  C07D327/00 ,  C07D497/04 ,  C07D519/00 ,  C07D411/14

    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。

    Spiro�heterocycle-imidazo�1,2-a!indeno�1,2-e!pyrazine!-4'-ones, preparation thereof and drugs containing same
    7.
    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

    申请人： Jean-Claude Aloup ,  Fran.cedilla.ois Audiau ,  Michel Barreau ,  Dominique Damour ,  Arielle Genevois-Borella ,  Patrick Jimonet ,  Serge Mignani ,  Yves Ribeill

    发明人： Jean-Claude Aloup ,  Fran.cedilla.ois Audiau ,  Michel Barreau ,  Dominique Damour ,  Arielle Genevois-Borella ,  Patrick Jimonet ,  Serge Mignani ,  Yves Ribeill

    IPC分类号： C07D487/04 ,  A61K31/495 ,  A61P9/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/14 ,  A61P11/00 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D471/20 ,  C07D487/20 ,  C07D471/235 ,  C07D487/241

    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。

    Complexes derived from platinum, their preparation and the pharmaceutical compositions which contain them
    8.
    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

    申请人： Michel Barreau ,  Jean-Claude Chottard ,  Jean-Bernard Le Peco ,  Patrick Mailliet

    发明人： Michel Barreau ,  Jean-Claude Chottard ,  Jean-Bernard Le Peco ,  Patrick Mailliet

    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）

    1,2-Dithiole pyrimidines
    9.
    发明授权
    1,2-Dithiole pyrimidines 失效
    1,2-二硫杂环丁烷嘧啶

    公开(公告)号：US4144339A

    公开(公告)日：1979-03-13

    申请号：US855196

    申请日：1977-11-28

    申请人： Michel Barreau ,  Claude Cotrel ,  Claude Jeanmart

    发明人： Michel Barreau ,  Claude Cotrel ,  Claude Jeanmart

    IPC分类号： C07D237/08 ,  C07D237/14 ,  C07D237/20 ,  C07D237/24 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D241/12 ,  C07D241/16 ,  C07D241/20 ,  C07D241/24 ,  C07D241/26 ,  A61K31/505

    CPC分类号： C07D241/26 ,  C07D237/08 ,  C07D237/14 ,  C07D237/20 ,  C07D237/24 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D241/12 ,  C07D241/16 ,  C07D241/20 ,  C07D241/24

    摘要： 1,2-Dithiole derivatives of the formula: ##STR1## wherein Het represents an aromatic heterocyclic radical with six atoms in the ring two of which are nitrogen atoms, the heterocyclic radical optionally carrying a single substituent selected from halogen, alkyl, alkoxy, mercapto, alkylthio, dialkylamino, pyrrolidin-1-yl, piperidino, morpholino and 4-alkylpiperazin-1-yl, and R represents halogen, alkyl (optionally substituted by alkoxycarbonyl), carboxy, alkoxycarbonyl, carbamoyl, N-alkylcarbamoyl or a group R.sub.1 --CH(OH)-- in which R.sub.1 represents hydrogen or alkyl, the said alkyl, alkoxy and alkylthio radicals or alkyl or alkoxy moieties containing 1 to 4 carbon atoms except in the case of R.sub.1 which contains 1 to 3 carbon atoms when an alkyl radical, are new compounds useful in the treatment of bilharziasis.

    摘要翻译： 其中Het表示在其中两个为氮原子的六个原子的芳香族杂环基，杂环基任选地带有选自卤素，烷基，烷氧基，巯基的单个取代基的1,2-二硫杂衍生物 ，烷硫基，二烷基氨基，吡咯烷-1-基，哌啶子基，吗啉代和4-烷基哌嗪-1-基，R表示卤素，烷基（任选被烷氧基羰基取代），羧基，烷氧基羰基，氨基甲酰基，N-烷基氨基甲酰基或基团R1- CH（OH） - 其中R1代表氢或烷基，所述烷基，烷氧基和烷硫基或含有1-4个碳原子的烷基或烷氧基部分，除了当烷基含有1至3个碳原子的情况下， 是可用于治疗胆红病的新化合物。