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27 条记录 (耗时 0.019 秒)

    Substituted isoquinoline compounds, pharmaceutical composition and method of use in treating pain in mammals
    1.
    发明授权
    Substituted isoquinoline compounds, pharmaceutical composition and method of use in treating pain in mammals 失效
    取代的异喹啉化合物，药物组合物和用于治疗哺乳动物疼痛的方法

    公开(公告)号：US5254564A

    公开(公告)日：1993-10-19

    申请号：US553723

    申请日：1990-07-16

    申请人： Vittorio Vecchietti ,  Giuseppe Giardina ,  Roberto Colle

    发明人： Vittorio Vecchietti ,  Giuseppe Giardina ,  Roberto Colle

    IPC分类号： C07D217/06 ,  A61K31/47 ,  A61K31/472 ,  A61P7/10 ,  A61P9/00 ,  A61P9/10 ,  A61P25/04 ,  C07D217/14 ,  C07D221/16 ,  C07D221/20 ,  C07D217/26

    CPC分类号： C07D221/20 ,  C07D217/14 ,  C07D221/16

    摘要： A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, .sup.4 or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group;R.sub.4 and R.sub.5 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group; R.sub.6 and R.sub.7 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group;or R.sub.5 and R.sub.6 are together --CH.sub.2 -- when each of R.sub.4 and R.sub.7 is hydrogen or C.sub.1-6 alkyl;with the proviso that R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are not simultaneously hydrogen;R.sub.8 and R.sub.9, which may be the same or different, are each hydrogen, C.sub.1-6 alkyl, --CH.sub.2 OR.sub.10, halogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, thiol, C.sub.1-6 alkylthio, ##STR2## --NHCOR.sub.12, --NHSO.sub.2 R.sub.13, --CH.sub.2 SO.sub.2 NR.sub.14 R.sub.15, in which each of R.sub.10 to R.sub.15 is independently hydrogen, C.sub.1-6 alkyl, aryl or aralkyl, is useful for the treatment of pain, and or hyponatraemic disease states and/or cerebral ischaemia.

    Isoquinoline derivatives and their use as analgesics
    4.
    发明授权
    Isoquinoline derivatives and their use as analgesics 失效
    异喹啉衍生物及其用作镇痛药

    公开(公告)号：US4954509A

    公开(公告)日：1990-09-04

    申请号：US312648

    申请日：1989-02-17

    申请人： Vittorio Vecchietti ,  Giuseppe Giardina

    发明人： Vittorio Vecchietti ,  Giuseppe Giardina

    IPC分类号： A61K31/47 ,  A61K31/472 ,  A61P25/04 ,  C07D217/14 ,  C07D409/06

    CPC分类号： C07D409/06 ,  C07D217/14

    摘要： A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.sub.1-6 alkyl group.R.sub.6 and R.sub.6a, which may be the same or different, are each hydrogen, C.sub.1-6 alkyl, --CH.sub.2 OR.sub.6b, halogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, thiol, C.sub.1-6 alkylthio, ##STR2## --NHCOR.sub.6d, --NHSO.sub.2 R.sub.6e, --CH.sub.2 SO.sub.2 NR.sub.6f R.sub.6g, in which each of R.sub.6b to R.sub.6g is independently hydrogen, C.sub.1-6 alkyl, aryl or aralkyl;with the proviso that R.sub.4, R.sub.5, R.sub.6 and R.sub.6a are not simultaneously hydrogen,is useful for the treatment of pain.

    Heterocyclic ethylene diamine compounds and their pharmaceutical compositions and methods
    5.
    发明授权
    Heterocyclic ethylene diamine compounds and their pharmaceutical compositions and methods 失效
    杂环乙二胺化合物及其药物组合物和方法

    公开(公告)号：US4999359A

    公开(公告)日：1991-03-12

    申请号：US323617

    申请日：1989-03-14

    申请人： Vittorio Vecchietti ,  Giuseppe Giardina

    发明人： Vittorio Vecchietti ,  Giuseppe Giardina

    IPC分类号： A61K31/38 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4418 ,  A61P25/04 ,  C07D213/40 ,  C07D333/20 ,  C07D471/04 ,  C07D495/04

    CPC分类号： C07D213/40 ,  C07D333/20 ,  C07D471/04 ,  C07D495/04

    摘要： A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 is C.sub.1-6 alkyl, or phenyl;R.sub.5 is hydrogen or together with R.sub.4 forms a --(CH.sub.2).sub.n -- group in which n=1, 2 or 3; and `Het` is an optionally substituted single or fused ring heterocyclic group, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from oxygen, nitrogen and sulphur, with the proviso that when, simultaneously, R.sub.1 and R.sub.2 together are linear butylene, R.sub.3 is hydrogen, R.sub.4 is methyl, R.sub.5 is hydrogen and R is 3,4-dichlorophenyl, `Het` is not pyridyl, is useful for the treatment of pain.

    Hydroisoquinoline derivatives
    6.
    发明授权
    Hydroisoquinoline derivatives 失效
    氢异喹啉衍生物

    公开(公告)号：US5441956A

    公开(公告)日：1995-08-15

    申请号：US175371

    申请日：1994-01-05

    申请人： Vittorio Vecchietti ,  Giulio Dondio ,  Silvano Ronzoni ,  Roberto Colle

    发明人： Vittorio Vecchietti ,  Giulio Dondio ,  Silvano Ronzoni ,  Roberto Colle

    IPC分类号： A61K31/47 ,  A61K31/475 ,  A61P25/04 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/495

    CPC分类号： C07D471/04 ,  C07D491/04 ,  C07D495/04

    摘要： ##STR1## Compounds of formula (I) in which, R is linear or branched alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, aralkyl or furan-2-yl alkyl; R
    1 and R
    2 , which may be the same or different, are each hydrogen, hydroxy, alkoxy, or halogen; R
    3 is hydrogen, hydroxy or alkoxy; "Het" is optionally substituted single or fused heteroxyclic ring, containing from 5 to 10 ring atoms and comprising up to four heteratoms in the or each ring, selected from oxygen, nitrogen and sulphur; R
    4 and R
    5 , which may be the same or different, are each hydrogen alkyl, halogen, nitro; CF, cyano, alkoxy carbonyl, NH, alkylcarbonylamino, hydroxy, alkoxy, or benzyl, are selective delta receptor agonists and are useful in the treatment of pain.

    摘要翻译： PCT No.PCT / EP92 / 01483第 371日期1994年1月5日 102（e）日期1994年1月5日PCT提交1992年7月1日PCT公布。 公开号WO93 / 01186 （I）其中R为直链或支链烷基，环烷基，环烷基烷基，烯基，芳基，芳烷基或呋喃-2-基烷基的式（I）化合物; R 1和R 2可以相同或不同，分别为氢，羟基，烷氧基或卤素; R3是氢，羟基或烷氧基; “Het”是任选取代的单或稠环氧环，其含有5至10个环原子，并且在该环或每个环中包含至多四个杂原子，选自氧，氮和硫; R 4和R 5可以相同或不同，分别为氢烷基，卤素，硝基; CF，氰基，烷氧基羰基，NH，烷基羰基氨基，羟基，烷氧基或苄基是选择性δ受体激动剂，可用于治疗疼痛。

    2-aminoethylamine derivatives, compositions of the same and use of said compounds in medicine
    8.
    发明授权
    2-aminoethylamine derivatives, compositions of the same and use of said compounds in medicine 失效
    2-氨基乙胺衍生物，其组合物和所述化合物在医药中的用途

    公开(公告)号：US5030649A

    公开(公告)日：1991-07-09

    申请号：US598825

    申请日：1990-10-16

    申请人： Vittorio Vecchietti ,  Giuseppe Giardina

    发明人： Vittorio Vecchietti ,  Giuseppe Giardina

    IPC分类号： C07D295/125

    CPC分类号： C07D295/125

    摘要： A compound of formula (I): ##STR1## or a salt and/or solvate thereof, wherein R represents an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sup.1 and R.sup.2 each independently represents an alkyl, alkenyl or alkynyl group or R.sup.1 together with R.sup.2 represents a C.sub.3-6 polymethylene or alkenylene group;R.sup.3 represents hydrogen or alkyl;R.sup.4 represents hydrogen, halogen, alkyl, hydroxy, alkoxy, nitrile, nitro, amino or mono or disubstituted amino; andn represents O or an integer 1,is useful in the treatment of pain.