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    4-pyrimidinone derivatives their preparation and their application in therapy
    23.
    发明授权
    4-pyrimidinone derivatives their preparation and their application in therapy 失效
    4-嘧啶酮衍生物的制备及其在治疗中的应用

    公开(公告)号：US5472967A

    公开(公告)日：1995-12-05

    申请号：US294023

    申请日：1994-08-24

    申请人： Christian Hoornaert ,  Marc Daumas ,  Michel Aletru ,  Jean-Claude Muller

    发明人： Christian Hoornaert ,  Marc Daumas ,  Michel Aletru ,  Jean-Claude Muller

    IPC分类号： C07D239/36 ,  C07D239/52 ,  C07D403/10 ,  A61K31/505

    CPC分类号： C07D239/36 ,  C07D239/52 ,  C07D403/10

    摘要： Compounds which can be expressed as tautomeric forms and having the formulas (I), (I') and (I") ##STR1## wherein R.sub.1 =a straight or branched (C.sub.1-7) alkyl group or a straight or branched (C.sub.3-9) alkenyl group or a cyclo(C.sub.3-7)alkyl(C.sub.1-6) alkyl group, R.sub.2 =an atom of hydrogen, or a straight or branched (C.sub.1-7)alkyl group, or a cyclo(C.sub.3-7)alkyl(C.sub.1-3)alkyl group, or an aryl(C.sub.1-3)alkyl group optionally substituted on the ring, or an aryloxy(C.sub.1-3)alkyl group optionally substituted on the ring, or an arylthio(C.sub.1-3)alkyl group optionally substituted on the ring, or an arylsulfonyl(C.sub.1-3)alkyl group optionally substituted on the ring, or a heteroaryl(C.sub.1-3)alkyl group optionally substituted on the ring, R.sub.3 =CO.sub.2 H, 1H-tetrazol-5-yl, NHCOR.sub.11, NHSO.sub.2 R.sub.11, CONHSO.sub.2 R.sub.11 or CONHOR.sub.12 group where R.sub.11 =a methyl, trifluoromethyl, or phenyl group optionally substituted, R.sub.12 =a hydrogen atom, or a methyl or a phenyl group optionally substituted. The compounds are useful for antagonizing angiotensin II.

    摘要翻译： 可以表示为互变异构形式并具有式（I），（I'）和（I“）的化合物其中R 1 =直链或支链（C 1-7）烷基 基团或直链或支链（C3-9）烯基或环（C3-7）烷基（C1-6）烷基，R2 =氢原子或直链或支链（C1-7）烷基， 或环（C 3-7）烷基（C 1-3）烷基或任选在环上取代的芳基（C 1-3）烷基或任意在环上取代的芳氧基（C 1-3）烷基，或 或环上任选取代的芳基磺酰基（C 1-3）烷基或环上任选取代的杂芳基（C 1-3）烷基，R 3 = CO 2 H ，1H-四唑-5-基，NHCOR 11，NHSO 2 R 11，CONHSO 2 R 11或CONHOR 12基团，其中R 11 =任选取代的甲基，三氟甲基或苯基，R 12 =氢原子或任选取代的甲基或苯基。 该化合物可用于拮抗血管紧张素II。

    9H-imidazo[1,2-A]benzimidazole-3-acetamide derivatives, their preparation and their therapeutic application
    24.
    发明授权
    9H-imidazo[1,2-A]benzimidazole-3-acetamide derivatives, their preparation and their therapeutic application 失效
    9H-咪唑并[1,2-A]苯并咪唑-3-乙酰胺衍生物，其制备及其治疗应用

    公开(公告)号：US5466706A

    公开(公告)日：1995-11-14

    申请号：US180998

    申请日：1994-01-14

    申请人： Pascal George ,  Danielle De Peretti ,  Jocelyne Roy ,  Jean-Paul Schmitt ,  Mireille Sevrin

    发明人： Pascal George ,  Danielle De Peretti ,  Jocelyne Roy ,  Jean-Paul Schmitt ,  Mireille Sevrin

    IPC分类号： A61K31/415 ,  A61P25/08 ,  A61P25/20 ,  A61P43/00 ,  C07D233/68 ,  C07D235/00 ,  C07D487/04 ,  C07D519/00 ,  A61K

    CPC分类号： C07D487/04

    摘要： Compound corresponding to the formula: ##STR1## in which X represents one or more of hydrogen, halogen, alkyl, trifluoromethyl, alkoxy, alkylthio, methylsulphonyl, cyano, ethoxycarbonyl, aminocarbonyl and carboxy, Y represents one or more of hydrogen, halogens, alkyl, trifluoromethyl, methoxy and trifluoromethoxy, R.sub.1 represents hydrogen, alkyl, phenylmethyl, 2-phenylethyl, acetyl or alkoxycarbonyl, R.sub.2 and R.sub.3 each represent hydrogen, alkyl which is optionally substituted, prop-2-enyl, prop-2-ynyl, phenyl, 1-(phenylmethyl)piperidin-4-yl, or 1-[(cyclohexen-1-yl)methyl]piperidin-4-yl, or alternatively R.sub.2 and R.sub.3 form, with the nitrogen atom carrying them, an optionally substituted heterocycle. These compounds are useful as hypnotic, anxiolytic and anticonvulsant agents.

    摘要翻译： 对应于下式的化合物：其中X表示氢，卤素，烷基，三氟甲基，烷氧基，烷硫基，甲基磺酰基，氰基，乙氧基羰基，氨基羰基和羧基中的一个或多个，Y表示一个或多个氢， 卤素，烷基，三氟甲基，甲氧基和三氟甲氧基，R1代表氢，烷基，苯基甲基，2-苯基乙基，乙酰基或烷氧基羰基，R2和R3各自表示氢，任选取代的烷基，丙-2-烯基，丙-2-炔基 ，苯基，1-（苯基甲基）哌啶-4-基或1 - [（环己烯-1-基）甲基]哌啶-4-基，或者R2和R3与带有氮原子一起形成任选取代的 杂环。 这些化合物可用作催眠，抗焦虑药和抗惊厥剂。

    Quinoline derivatives
    26.
    发明授权
    Quinoline derivatives 失效
    喹啉衍生物

    公开(公告)号：US5432283A

    公开(公告)日：1995-07-11

    申请号：US295469

    申请日：1994-08-25

    申请人： Gerard Cremer ,  Pascale Goberville ,  Jean-Claude Muller

    发明人： Gerard Cremer ,  Pascale Goberville ,  Jean-Claude Muller

    IPC分类号： C07D215/12 ,  C07D401/14 ,  C07D403/10 ,  C07D215/16

    CPC分类号： C07D401/14 ,  C07D215/12

    摘要： The present invention provides a compound which is a quinoline derivative of the formula (I) ##STR1## in which R.sub.1 represents either 1H-tetrazol-5-yl, or CO.sub.2 H,R.sub.2 represents either (C.sub.1-7)alkyl or (C.sub.2-6)alkenyl,R.sub.3 and R.sub.4 represent, independently of each other, hydrogen, halogen, cyano group, (C.sub.1-7)alkyl, (C.sub.3-7)cycloalkyl(C.sub.1-4)alkyl, aryl, aryl(C.sub.1-4)alkyl, aryl(C.sub.2-6)alkenyl, --(CH.sub.2).sub.m --COR.sub.5 in which m=0 to 4 and R.sub.5 represents hydrogen, --OH, --(C.sub.1-6)alkoxy, or --NR.sub.7 R.sub.8, R.sub.7 and R.sub.8 representing, independently of each other, hydrogen or --(C.sub.1-4)alkyl group, or a --(CH.sub.2).sub.n --R.sub.6 group in which n=1 to 4 and R.sub.6 represents --OH, --(C.sub.1-6)alkoxy, --(C.sub.1-4)alkoxy(C.sub.1-4)alkoxy, or (C.sub.3-7)cycloalkyl(C.sub.1-4)alkoxy group, or a pharmaceutically acceptable salt thereof and their therapeutic applications.

    摘要翻译： 本发明提供一种化合物，其为式（I）的喹啉衍生物，其中R 1表示1H-四唑-5-基或CO 2 H，R 2表示（C 1-7）烷基或（ C2-6）烯基，R3和R4彼此独立地表示氢，卤素，氰基，（C1-7）烷基，（C3-7）环烷基（C1-4）烷基，芳基，芳基（C1-4 ）烷基，芳基（C2-6）烯基， - （CH2）m-COR5，其中m = 0至4，R5表示氢，-OH， - （C1-6）烷氧基或-NR7R8，R7和R8表示， 氢或 - （C1-4）烷基或其中n = 1-4的R6为R6，R6为-OH的 - （CH2）n-R6基， - （C1-6）烷氧基， - （C1 -4）烷氧基（C 1-4）烷氧基或（C 3-7）环烷基（C 1-4）烷氧基或其药学上可接受的盐及其治疗应用。

    2-aminopyrazine-5-carboxamide derivatives, their preparation and their application in therapeutics
    27.
    发明授权
    2-aminopyrazine-5-carboxamide derivatives, their preparation and their application in therapeutics 失效
    2-氨基吡嗪-5-甲酰胺衍生物，其制备及其在治疗中的应用

    公开(公告)号：US5420130A

    公开(公告)日：1995-05-30

    申请号：US243315

    申请日：1994-05-16

    申请人： Pascal George ,  Benoit Marabout ,  Jacques Froissant

    发明人： Pascal George ,  Benoit Marabout ,  Jacques Froissant

    IPC分类号： A61K31/495 ,  A61K31/4965 ,  A61P13/02 ,  A61P13/08 ,  A61P15/00 ,  C07D241/26 ,  C07D241/28 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

    CPC分类号： C07D401/12 ,  C07D241/26

    摘要： Compounds corresponding to the general formula (I) ##STR1## in which n represents 0 or 1, R.sub.1 represents a methyl group, in which case R.sub.2 represents a phenoxy(C.sub.1 -C.sub.4)alkyl group (in which the phenoxy group is optionally substituted), or else R.sub.1 and R.sub.2 together form, and with the nitrogen atom which carries them, a 4-(phenoxymethyl)piperid-1-yl group (in which the phenoxy group is optionally substituted) or a 4-phenylpiperazin-1-yl group (in which the phenyl group is optionally substituted), R.sub.3 represents a hydrogen atom or a methyl group, R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydrogen atom or a group of general formula -CH.sub.2 -CH.sub.2 -NH-R.sub.6, R.sub.6 being a hydrogen atom or a tert-butyloxycarbonyl, 4-carbamoylpyrimidin-2-yl or 5-carbamoylpyrazin-2-yl group, are useful in the treatment of diseases and complaints involving hyperactivity of the .alpha.-adrenergic system at the level of the lower urinary apparatus.

    摘要翻译： 对应于通式（I）的化合物其中n表示0或1，R1表示甲基，其中R2表示苯氧基（C1-C4）烷基（其中苯氧基为 任选取代），或者R1和R2一起形成，并且与携带它们的氮原子一起形成4-（苯氧基甲基）哌啶-1-基（其中苯氧基任选被取代）或4-苯基哌嗪-1-基 - 基（其中苯基任选被取代），R 3表示氢原子或甲基，R 4表示氢原子，R 5表示氢原子或通式-CH 2 -CH 2 -NH-R 6基团， R6是氢原子或叔丁氧基羰基，4-氨基甲酰基嘧啶-2-基或5-氨基甲酰基吡嗪-2-基可用于治疗涉及α-肾上腺素能系统的多动症的疾病和投诉， 下尿路器

    2-(tetrazol-5-yl)-1,1'-biphenyl derivatives, their preparation and their use as synthetic intermediates
    29.
    发明授权
    2-(tetrazol-5-yl)-1,1'-biphenyl derivatives, their preparation and their use as synthetic intermediates 失效
    2-（四唑-5-基）-1,1'-联苯衍生物，其制备及其作为合成中间体的用途

    公开(公告)号：US5371233A

    公开(公告)日：1994-12-06

    申请号：US998055

    申请日：1992-12-29

    申请人： Marc Daumas ,  Christian Hoornaert ,  Isaac Chekroun ,  Manuel Bedoya-Zurita ,  Jose Ruiz-Montes ,  Guy Rossey ,  Helene Greciet

    发明人： Marc Daumas ,  Christian Hoornaert ,  Isaac Chekroun ,  Manuel Bedoya-Zurita ,  Jose Ruiz-Montes ,  Guy Rossey ,  Helene Greciet

    IPC分类号： C07D257/04 ,  C07D403/10

    CPC分类号： C07D257/04

    摘要： Compounds corresponding to the formula (I) ##STR1## in which X represents dibromomethyl, formyl, (C.sub.1-4)alkyl, or a group CH(OR.sub.5).sub.2 or CH(OH)OR.sub.5, wherein the or each R.sub.5 is hydrogen (C.sub.1-3)alkyl or the two R.sub.5 's in the case of CH(OR.sub.5).sub.2 are linked to provide a 1,3-dioxolane or 1,3-dioxane ring, and Y represents hydrogen, 1,1-dimethylethyl, triphenylmethyl, trimethylstannyl, tributylstannyl, (1,1-dimethylethyl)dimethylsilyl, (1,1-dimethylethyl)diphenylsilyl, 2-cyanoethyl, or a group CH.sub.2 OR.sub.6 wherein R.sub.6 is methyl, phenylmethyl, 1,1-dimethylethyl, 2,2,2-trichloroethyl, benzyloxycarbonyl or 2,2,2-trichloroethyloxycarbonyl, Y being in position 1 or 2 on the tetrazole ring. The compounds of formula (I) are useful as intermediates in the synthesis of compounds possessing therapeutic activity.

    摘要翻译： 对应于式（I）的化合物其中X表示二溴甲基，甲酰基，（C 1-4）烷基或CH（OR 5）2或CH（OH）OR 5基团，其中每个R 5为 氢（C 1-3）烷基或在CH（OR 5）2的情况下的两个R 5连接，得到1,3-二氧戊环或1,3-二恶烷环，Y代表氢，1,1-二甲基乙基，三苯基甲基 ，三甲基甲锡烷基，三丁基甲锡烷基，（1,1-二甲基乙基）二甲基甲硅烷基，（1,1-二甲基乙基）二苯基甲硅烷基，2-氰乙基或CH 2 OR 6，其中R 6是甲基，苯甲基，1,1-二甲基乙基， 三氯乙基，苄氧基羰基或2,2,2-三氯乙氧基羰基，Y在四唑环上位于1或2位。 式（I）的化合物可用作合成具有治疗活性的化合物的中间体。