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    3-Aryl 2-oxazolidinones, their process of preparation and their therapeutical application
    5.
    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：

    1-Spiro isobenzofuranic and 1-spiro isobenzothiophenic derivatives the process for preparing the same and their use in therapeutics
    9.
    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。