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20 条记录 (耗时 0.021 秒)

    1-Spiro isobenzofuranic and 1-spiro isobenzothiophenic derivatives the process for preparing the same and their use in therapeutics
    8.
    发明授权
    1-Spiro isobenzofuranic and 1-spiro isobenzothiophenic derivatives the process for preparing the same and their use in therapeutics 失效
    1-螺异异佛尔酮和1-螺异苯并噻吩衍生物其制备方法及其在治疗中的应用

    公开(公告)号：US4395416A

    公开(公告)日：1983-07-26

    申请号：US341415

    申请日：1982-01-21

    申请人： Michel Langlois ,  Bernard P. Bucher ,  Philippe L. Dostert ,  Alain P. Lacour ,  Gerard H. Moinet

    发明人： Michel Langlois ,  Bernard P. Bucher ,  Philippe L. Dostert ,  Alain P. Lacour ,  Gerard H. Moinet

    IPC分类号： C07D307/94 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10 ,  A61K31/395

    CPC分类号： C07D491/10 ,  C07D307/94 ,  C07D495/10

    摘要： Derivatives of formula: ##STR1## in which Z N-R.sub.1 where R.sub.1 represents a linear or branched alkyl group with 1 to 5 carbon atoms or a phenyl group possibly substituted by a chlorine atom, in which case:n=1 or 2,the pair (A, C X) assumes the following values: (S, C.dbd.O), (S, CH.sub.2), (O, CH.sub.2), (O, CH--C.sub.6 H.sub.5), andR represents a hydrogen or halogen atom, one or more methoxy groups or the butadiene-1,3 ylene chain ##STR2## fixed in position 5,6 of the phenyhl nucleus and thus forming with this latter a naphthyl nucleus;or a methylene group (--CH.sub.2 --), in which case:n=1 or 2,A represents the oxygen atom,>C X represents a carbonyl group (>C.dbd.O) or thiocarbonyl group (>C.dbd.S), andR has the same meanings as previously,as well as the mineral or organic acid addition salts thereof. The compounds exhibit anti-convulsion and analgesic activity.

    摘要翻译： 式：其中Z <表示：其中R1表示具有1-5个碳原子的直链或支链烷基或可能被氯原子取代的苯基，其中Z <表示：结构的氨基> N-R1的衍生物， （S，C = O），（S，CH 2），（O，CH 2），（O，CH-C 6 H 5）和 R表示氢或卤素原子，一个或多个甲氧基或固定在苯基核的5,6位的丁二烯-1,3-亚苯基链，因此与后者形成萘基核; 或亚甲基（-CH 2 - ），在这种情况下：n = 1或2，A表示氧原子，> CX表示羰基（> C = O）或硫代羰基（> C = S），R 具有与之前相同的含义，以及其矿物或有机酸加成盐。 该化合物表现出抗惊厥和止痛活性。

    Dioxazabicyclic derivatives
    9.
    发明授权
    Dioxazabicyclic derivatives 失效
    二恶唑二环衍生物

    公开(公告)号：US4463004A

    公开(公告)日：1984-07-31

    申请号：US368924

    申请日：1982-04-16

    申请人： Patrick G. Guerret ,  Bernard P. Bucher ,  Philippe L. Dostert ,  Gisele C. Mocquet ,  Alain L. Nedelec

    发明人： Patrick G. Guerret ,  Bernard P. Bucher ,  Philippe L. Dostert ,  Gisele C. Mocquet ,  Alain L. Nedelec

    IPC分类号： C07D265/30 ,  C07D317/16 ,  C07D317/28 ,  C07D413/04 ,  C07D498/08 ,  A61K31/535 ,  C07D491/08

    CPC分类号： C07D265/30 ,  C07D317/16 ,  C07D317/28 ,  C07D413/04

    摘要： Compounds having analgesic activity are disclosed which have the general formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl having 1 to 4 carbon atoms, cyclohexyl or benzyl; R is selected from the group consisting of alkyl having at least 4 carbon atoms; cyclohexyl; unsubstituted phenyl or phenyl substituted with one or more halogen atoms, methyl, methoxy, hydroxy, cyano, nitro, trifluoromethyl, carboxyl, ethoxycarbonyl, acetamido, methylsulfonyl, phenoxy, benzoyl, phenyl, .alpha.-hydroxybenzyl, cyclohexyl or carbamoyl; thienyl; pyridyl; naphthyl; naphthyl substituted with methoxy; adamantyl; and benzyl; and n is 1, 2 or 3, with the provisos that (1) when R is carboxyphenyl, benzoylphenyl, or (.alpha.-hydroxybenzyl) phenyl, n is not 3, and (2) when R is (.alpha.-hydroxy benzyl) phenyl, R.sub.1 is not benzyl, and acid addition salts thereof.

    摘要翻译： 公开了具有镇痛活性的化合物，其具有以下通式：其中R 1是氢，具有1至4个碳原子的烷基，环己基或苄基; R选自具有至少4个碳原子的烷基; 环己基 甲基，甲氧基，羟基，氰基，硝基，三氟甲基，羧基，乙氧基羰基，乙酰氨基，甲基磺酰基，苯氧基，苯甲酰基，苯基，α-羟基苄基，环己基或氨基甲酰基取代的苯基或被一个或多个卤素原子取代的苯基。 噻吩基 吡啶基 萘基; 用甲氧基取代的萘基; 金刚烷 和苄基; 并且n为1,2或3，条件是（1）当R为羧基苯基，苯甲酰基苯基或（α-羟基苄基）苯基时，n不为3，和（2）当R为（α-羟基苄基）苯基 R1不是苄基，也可以是其酸加成盐。

    3-Aryl 2-oxazolidinones, their process of preparation and their therapeutical application
    10.
    发明授权
    3-Aryl 2-oxazolidinones, their process of preparation and their therapeutical application 失效
    3-芳基2-恶唑烷酮，其制备方法及其治疗应用

    公开(公告)号：US4150029A

    公开(公告)日：1979-04-17

    申请号：US771814

    申请日：1977-02-23

    申请人： Philippe L. Dostert ,  Colette A. Douzon ,  Guy R. Bourgery ,  Claude J. Gouret ,  Gisele C. Mocquet ,  Jean A. Coston

    发明人： Philippe L. Dostert ,  Colette A. Douzon ,  Guy R. Bourgery ,  Claude J. Gouret ,  Gisele C. Mocquet ,  Jean A. Coston

    IPC分类号： A61K31/42 ,  A61K31/421 ,  A61P25/24 ,  A61P25/26 ,  C07D263/24

    CPC分类号： C07D263/24

    摘要： Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or CONHR.sub.7 and R.sub.7 is methyl or isopropyl,And whereinWhen R.sub.1 is hydrogen: R is p-nitro, p-cyano; p-aldehydo; p-acetyl; m-ethyl; m-nitro; m-bromo; 3,4-dimethyl; m-NH.sub.2 ; p-methylamino; p-dimethylamino; p-diethylamino; p-methylbenzylamino; p-pyrrolidino; p-piperidino; SR.sub.4 in para position in which R.sub.4 is alkyl having 1 to 4 carbon atoms or cyclohexyl; OR.sub.5 is para position in which R.sub.5 is alkyl having 2 to 7 carbon atoms, cyclohexyl, cyclohexylmethyl, acetylmethyl; cyanomethyl, alkene-2 yl having 3 to 5 carbon atoms, butene-3 yl, cyclohexene-1 methyl, propargyl, butyne-2 yl, ##STR2## in which n is one or 2 and when n is one, R.sub.6 is hydrogen, o-fluoro, o-methyl, m-chloro, m-fluoro, m-methyl, m-trifluoromethyl, p-chloro, p-bromo-, p-fluoro, p-cyano, p-nitro or p-dimethylamino and when n is 2, R.sub.6 is hydrogen; and 3-methyl-4-benzyloxy:When R.sub.1 is CONHR.sub.7 and R.sub.7 is methyl: R is m-trifluoromethyl; m-bromo; p-chloro; p-fluoro; 3,4-dichloro; p-thiomethyl; p-acetyl; OR.sub.8 in para position wherein R.sub.8 is alkyl having 2 to 5 carbon atoms, cyanomethyl, acetylmethyl, propargyl or ##STR3## in which R.sub.9 is hydrogen, m-chloro, m-bromo, m-fluoro, p-fluoro, p-chloro or p-nitro;And when R.sub.1 is CONHR.sub.7 and R.sub.7 is isopropyl; R is m-trifluoromethyl or p-benzyloxy.The compounds are prepared by cyclizing 1-phenylamino-2,3-propandiol derivatives to form 5-hydroxymethyl-3 phenyl-2-oxozolidinone derivatives. The 5-hydroxymethyl group can be transformed to --CH.sub.2 OCONHR.sub.7 by reaction with methyl isocyanate or isopropyl isocyanate. The compounds possess psychotropic, particularly antidepressant, activity.

    摘要翻译： 具有式“IMAGE”的化合物，其中R1是氢或CONHR7，R7是甲基或异丙基，当R1是氢时，R是对硝基，对氰基; 对醛 对乙酰基; 甲基; 间硝基 溴代 3,4-二甲基 m-NH2; 对甲基氨基; 对二甲基氨基; 对二乙基氨基; 对甲基苄基氨基; 对 - 吡咯烷子; 对哌啶子 其中R4是具有1-4个碳原子的烷基的对位的SR4或环己基; OR5是R5是具有2至7个碳原子的烷基的对位，环己基，环己基甲基，乙酰基甲基; 氰基甲基，具有3至5个碳原子的烯-2，丁烯-3，环己烯-1甲基，炔丙基，丁炔-2基，其中n为1或2，当n为1时，R6为氢， 邻 - 甲基，间 - 氯，间氟，间甲基，间三氟甲基，对氯，对溴 - ，对氟，对氰基，对硝基或对二甲基氨基，当 n为2，R6为氢; 和3-甲基-4-苄氧基：