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    Alpha-aminoamide derivatives useful as analgesic agents
    43.
    再颁专利
    Alpha-aminoamide derivatives useful as analgesic agents 有权
    用作止痛剂的α-氨基酰胺衍生物

    公开(公告)号：USRE40259E1

    公开(公告)日：2008-04-22

    申请号：US11359982

    申请日：1998-12-12

    申请人： Paolo Pevarello ,  Mario Varasi ,  Patricia Salvati ,  Claes Post

    发明人： Paolo Pevarello ,  Mario Varasi ,  Patricia Salvati ,  Claes Post

    IPC分类号： A61K31/275 ,  A61K31/165 ,  C07C255/50 ,  C07C233/05

    CPC分类号： C07C237/06 ,  A61K31/165 ,  C07C255/54

    摘要： The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents.In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain.Accordingly, one object of the present invention is to provide the use of a compound of formula (I) wherein: A is a —(CH2)m—, —(CH2)n—X— or —(CH2)v—O— group wherein m is an integer of 1 to 4, n is zero or an integer of 1 to 4, X is —S— or —NH—, and v is zero or an integer of 1 to 5; s is 1 or 2; R is a furyl, thienyl, or pyridyl ring or a phenyl ring optionally substituted by one or two substituents independently chosen from halogen, cyano, C1-C4 alkyl, C1-C4 alkoxy and trifluoromethyl; R1 is hydrogen or C1-C4 alkyl; one of R2 and R3 is hydrogen and the other is hydrogen or C1-C4 alkyl optionally substituted by hydroxy or phenyl; or R2 and R3 taken together with the carbon atom to which they are linked form a C3-C6 cycloalkyl ring; or R2 and R3 are both methyl; R4 is hydrogen or C1-C4 alkyl.

    摘要翻译： 本发明涉及新的和已知的α-氨基酰胺化合物，其制备方法，含有它们的药物组合物及其作为治疗剂的用途。 特别地，本发明的化合物具有止痛特性，特别可用于治疗和缓解慢性和神经性疼痛。 因此，本发明的一个目的是提供式（I）化合物的用途，其中：A是 - （CH 2）n - ， - （ CH 2 - （CH 2）n -X - 或 - （CH 2）2 -O - ，其中m是 1〜4的整数，n为0或1〜4的整数，X为-S-或-NH-，v为0或1〜5的整数。 s为1或2; R是呋喃基，噻吩基或吡啶基环或任选被一个或两个独立地选自卤素，氰基，C 1 -C 4烷基的取代基取代的苯环，C C 1 -C 4烷氧基和三氟甲基; R 1是氢或C 1 -C 4烷基; R 2和R 3中的一个是氢，另一个是氢或任选地是C 1 -C 4 - 被羟基或苯基取代; 或R 2和R 3与它们所连接的碳原子一起形成C 3 -C 6 - 环烷基环; 或R 2和R 3均为甲基; R 4是氢或C 1 -C 4烷基。

    Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines and process for their preparation
    44.
    发明授权
    Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines and process for their preparation 失效
    苯基取代的1,4-二氢吡啶的咪唑基和吡啶基衍生物及其制备方法

    公开(公告)号：US5514693A

    公开(公告)日：1996-05-07

    申请号：US92566

    申请日：1993-07-16

    申请人： Paolo Cozzi ,  Germano Carganico ,  Mariia Menichincheri ,  Patricia Salvati

    发明人： Paolo Cozzi ,  Germano Carganico ,  Mariia Menichincheri ,  Patricia Salvati

    IPC分类号： C07D401/10 ,  C07D521/00 ,  A61K31/44

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/10

    摘要： Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines of formula (I) ##STR1## wherein Het is ##STR2## A represents a direct linkage, --CH.sub.2 --, CH.sub.2 --CH.sub.2 -- or, when Het is ##STR3## A may also represent --CH.dbd.CH--; R is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy; each of R.sub.3 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group; one of R.sub.1 and R.sub.2 is a group --OR' wherein R' is a C.sub.1 -C.sub.6 alkyl either unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy or cyano, and the other is, independently,a) a group --OR";b) a group ##STR4## or c) a group --OR.sup.IV wherein R.sup.IV is hydrogen or a substituent selected from:(i) --(CH.sub.2).sub.m --CH.dbd.CH--Ph, ##STR5## are useful as Thromboxane A.sub.2 (TxA.sub.2) Synthase inhibitors and as calcium antagonists.

    摘要翻译： 式（I）的苯基取代的1,4-二氢吡啶的咪唑基和吡啶基衍生物其中Het为直链，-CH 2 - ，CH 2 -CH 2 - 或当Het为 A也可以表示-CH = CH-; R是氢，卤素，C 1 -C 3烷基或C 1 -C 3烷氧基; R 3和R 4各自为C 1 -C 3烷基; R1和R2之一是基团-OR'，其中R'是未被取代或被C1-C3烷氧基或氰基取代的ω-的C1-C6烷基，另一个独立地是a）基团-OR“; 或者c）基团-ORIV，其中RIV是氢或选自下列的取代基：（i） - （CH 2）m -CH = CH-Ph，（ii）图像（iii） ）和（iv）可用作Thromboxane A2（TxA2）合酶抑制剂和钙拮抗剂。

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    46.
    发明授权
    "N-imidazolyl derivatives of bicyclic compounds and pharmaceutical compositions containing the same" 失效
    “双环化合物的N-咪唑基衍生物和含有相同的”

    公开(公告)号：US4882347A

    公开(公告)日：1989-11-21

    申请号：US201909

    申请日：1988-06-02

    申请人： Paolo Cozzi ,  Corrado Ferti ,  Patricia Salvati ,  Germano Carganico ,  Antonio Pillan

    发明人： Paolo Cozzi ,  Corrado Ferti ,  Patricia Salvati ,  Germano Carganico ,  Antonio Pillan

    IPC分类号： C07D233/60 ,  A61K31/415 ,  A61P13/02 ,  A61P15/00 ,  C07D233/61 ,  C07D405/04

    CPC分类号： A61K31/415 ,  Y10S514/866

    摘要： A pharmaceutical compositon having activity against nephropathies comprising, as an active agent, a therapeutically effective amount of a compound of formula (I) ##STR1## wherein (a) ##STR2## wherein Y completes a single bond or is oxygen or a --CH.sub.2 -- group and the symbol ##STR3## represents a single bond or (b) ##STR4## ##STR5## and the symbol ##STR6## represents a double bond; one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is --CH.sub.2 OH, C.sub.2 -C.sub.4 acyl, ##STR7## in which each of R.sub.1, R.sub.8 and R.sub.9 is independently hydrogen or C.sub.1 -C.sub.4 alkyl and the others are independently chosen from hydrogen, hydroxy, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and --COOR, wherein R.sub.7 is as defined above, and one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier and/or diluent.

    摘要翻译： 具有抗肾病活性的药物组合物，其包含作为活性剂的治疗有效量的式（I）化合物（I），其中（a）其中Y完成单键或氧或氧 -CH 2 - 基，符号表示单键或（b） ，符号表示双键; R 1，R 2，R 3和R 4中的一个是-CH 2 OH，C 2 -C 4酰基，其中R 1，R 8和R 9各自独立地为氢或C 1 -C 4烷基，其余各自独立地选自氢， 羟基，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基和-COOR，其中R 7如上所定义，R 5和R 6之一是氢，另一个是氢，C 1 -C 6烷基或苯基; 或其药学上可接受的盐; 和药学上可接受的载体和/或稀释剂。

    Ergoline derivatives
    47.
    发明授权
    Ergoline derivatives 失效
    二元醇衍生物

    公开(公告)号：US4500712A

    公开(公告)日：1985-02-19

    申请号：US438259

    申请日：1982-11-01

    申请人： Luigi Bernardi ,  Aldemio Temperilli ,  Daniela Ruggieri ,  Giuliana Arcari ,  Patricia Salvati

    发明人： Luigi Bernardi ,  Aldemio Temperilli ,  Daniela Ruggieri ,  Giuliana Arcari ,  Patricia Salvati

    IPC分类号： A61K31/48 ,  A61P1/04 ,  A61P9/12 ,  C07D457/02 ,  C07D457/12 ,  C07D457/04

    CPC分类号： C07D457/02 ,  C07D457/12

    摘要： There are provided ergoline derivatives of formula ##STR1## wherein R.sub.1 .dbd.H, CH.sub.3 ; R.sub.2 .dbd.H or halogen atom, or CH.sub.3,CN, alkyl- or phenyl-thio; R.sub.3 .dbd.H, OCH.sub.3 ; R.sub.4 .dbd.C.sub.1 -C.sub.4 hydrocarbon group; X.dbd.O, S, NH; A.dbd.CO, SO.sub.2 ; B.dbd.C.sub.1 -C.sub.4 hydrocarbon group, aryl, aralkyl, heterocyclic ring group, alkoxy, aryloxy; n.dbd.0, 1, 2; and pharmaceutically acceptable salts thereof.A process for preparing said compounds is also provided. The compounds show anti-hypertensive activity and are active on the gastroenteric system.

    摘要翻译： 提供式（Ⅰ）的麦角灵衍生物，其中R1 = H，CH3; R2 = H或卤素原子，或CH3，CN，烷基或苯基 - 硫基; R3 = H，OCH3; R4 = C1-C4烃基; X = O，S，NH; A = CO，SO2; B = C1-C4烃基，芳基，芳烷基，杂环基，烷氧基，芳氧基; n = 0,1,2; 及其药学上可接受的盐。 还提供了制备所述化合物的方法。 这些化合物显示出抗高血压活性，并且对胃肠系统有活性。