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    1-(2-arylethyl)-pyrrolidines
    1.
    发明授权
    1-(2-arylethyl)-pyrrolidines 失效
    1-（2-芳乙基） - 吡咯烷

    公开(公告)号：US5232978A

    公开(公告)日：1993-08-03

    申请号：US786674

    申请日：1991-11-01

    申请人： Rudolf Gottschlich ,  Karl-August Ackermann ,  Helmut Prucher ,  Andrew Barbar ,  Anton Haase ,  Hartmut Greiner ,  Gerd Bartoszyk

    发明人： Rudolf Gottschlich ,  Karl-August Ackermann ,  Helmut Prucher ,  Andrew Barbar ,  Anton Haase ,  Hartmut Greiner ,  Gerd Bartoszyk

    IPC分类号： C07D207/08 ,  C07D207/12 ,  C07D217/14 ,  C07D401/12 ,  C07D409/06 ,  C07D409/12

    CPC分类号： C07D207/08 ,  C07D207/12 ,  C07D217/14 ,  C07D401/12 ,  C07D409/06 ,  C07D409/12

    摘要： Novel 1-(2-arylethyl)-pyrrolidines of the formula ##STR1## in which, Ar is a phenyl group which is unsubstituted or monosubstituted by OH, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA or NH--SO.sub.2 --A,R.sup.1 is A,R.sup.2 is a phenyl, naphthyl, thienyl, benzothienyl or pyridyl group which is unsubstituted or mono- or disubstituted by A, Hal, CF.sub.3, OH, OA, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NO.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA, --NH--SO.sub.2 A, --CO--A, --CONH.sub.2, --CONHA, --CONA.sub.2, --CH.sub.2 --CONH.sub.2 and/or --O--CH.sub.2 --CONH.sub.2,R.sup.3 is OH or CH.sub.2 OH,A is alkyl with 1-4 C atoms andHal is F, Cl, Br or I,or a pharmaceutically acceptable salt thereof for use as an analgesic in humans and veterinary medicine.

    摘要翻译： 具有下式的新颖的1-（2-芳基乙基） - 吡咯啉其中，Ar是未被取代或被OH，-O-CO-NH 2，-O-CO-NHA，-O- CO-NA2，NH2，-NH-CHO，-NH-CO-A，-NH-CO-NH2，-NH-CO-NHA或NH-SO2-A，R1是A，R2是苯基，萘基，噻吩基 ，未取代或被A，Hal，CF 3，OH，OA，-O-CO-NH 2，-O-CO-NHA，-O-CO-NA 2，NO 2，NH 2 - 取代的苯并噻吩基或吡啶基， NH-CHO，-NH-CO-A，-NH-CO-NH2，-NH-CO-NHA，-NH-SO2A，-CO-A，-CONH2，-CONHA，-CONA2，-CH2-CONH2和/ 或-O-CH 2 -CONH 2，R 3是OH或CH 2 OH，A是具有1-4个C原子的烷基，Hal是F，Cl，Br或I，或其药学上可接受的盐，用作人类和兽医学中的止痛剂 。

    4-aryloxy- and 4-arylthiopiperidine derivatives
    5.
    发明授权
    4-aryloxy- and 4-arylthiopiperidine derivatives 失效
    4-芳氧基和4-芳硫基哌啶衍生物

    公开(公告)号：US5561145A

    公开(公告)日：1996-10-01

    申请号：US278210

    申请日：1994-07-21

    申请人： Helmut Prucher ,  Rudolf Gottschlich ,  Gerd Bartoszyk ,  Christoph Seyfried

    发明人： Helmut Prucher ,  Rudolf Gottschlich ,  Gerd Bartoszyk ,  Christoph Seyfried

    IPC分类号： A61K31/445 ,  A61K31/42 ,  A61K31/4465 ,  A61K31/4523 ,  A61P9/12 ,  A61P25/04 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  C07D211/54 ,  C07D263/20 ,  C07D413/06 ,  C07D413/14

    CPC分类号： C07D413/06

    摘要： Novel 4-aryloxy- or 4-arylthiopiperidine derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 are each, independently of one another, phenyl radicals which are unsubstituted or mono or disubstituted by A, OH, OA, aryloxy with 6-10 C atoms, aralkyloxy with 7-11 C atoms, --0--(CH.sub.2).sub.n --0--, Hal, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NA.sub.2, NHAc, NAAc, NHSO.sub.2 A and/or NASO.sub.2 A,X is O, S, SO or SO.sub.2,m is 1, 2 or 3,n is 1 or 2,A is an alkyl radical with 1-6 C atoms,Hal is F, Cl, Br or landAc is alkanoyl with 1-8 C atoms, aralkanoyl with 1-10 C atoms or aroyl with 7-11 C atoms,and the physiologically acceptable salts thereof, show an effect influencing the central nervous system, in particular neuroleptic effect, with a negligible cataleptic effect.

    摘要翻译： 式I的新型4-芳氧基 - 或4-芳硫基哌啶衍生物，其中R 1和R 2各自彼此独立地是未被取代的，被A，OH，OA，芳氧基与6- 10 C原子，具有7-11个碳原子的芳烷氧基，-O-（CH2）n-O-，Hal，CF3，NO2，NH2，NHA，NA2，NHAc，NAAc，NHSO2A和/或NASO2A，X是O，S ，SO或SO 2，m为1,2或3，n为1或2，A为具有1-6个C原子的烷基，Hal为F，Cl，Br或l，Ac为具有1-8个C原子的烷酰基 具有1-10个C原子的芳烷酰基或具有7-11个C原子的芳酰基及其生理上可接受的盐显示出影响中枢神经系统的作用，特别是抗精神病药效应，具有可忽略的催眠作用。

    Kappa-opiate agonists effective in the treatment of postoperative ileus
    10.
    发明授权
    Kappa-opiate agonists effective in the treatment of postoperative ileus 失效
    卡帕阿片激动剂有效治疗术后肠梗阻

    公开(公告)号：US5977161A

    公开(公告)日：1999-11-02

    申请号：US27228

    申请日：1998-02-20

    申请人： Andrew Barber ,  Christoph Seyfried ,  Gerd Bartoszyk ,  Rudolf Gottschlich

    发明人： Andrew Barber ,  Christoph Seyfried ,  Gerd Bartoszyk ,  Rudolf Gottschlich

    IPC分类号： C07D207/08 ,  A61K31/135 ,  A61K31/165 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61P1/00 ,  A61P1/04 ,  A61P29/00 ,  A61P43/00 ,  C07D207/12

    CPC分类号： A61K31/4025

    摘要： Disclosed herein are pharmaceutical preparations which are suitable for the treatment of postoperative ileus and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,R.sup.2 is Ar, orR.sub.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2,R.sup.5 is OH, CH.sub.2 OH,R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring,A is alkyl having 1-7 C atoms,Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.2, O, S, NH, NA, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 NH--, --CH.sub.2 --NA-- or a bondandHal is F, Cl, Br or I.

    摘要翻译： 本文公开了适用于治疗术后肠梗阻并含有至少一种其中R 1为Ar的式I化合物或具有3-7个C原子的环烷基或具有4-8个C原子的环烷基烷基，R2为Ar， 或R 1和R 2一起为R 3为H，OH，OA或A，R 4为A或可任选被Hal，OH，OA，CF 3，NO 2，NH 2，NHA，NHCOA，NHSO 2 A单取代或二取代的苯基和/或 NA2，R5分别为H，Hal，OH，OA，CF3，NH2，NHA，NA2，NHCOA，NHCONH2，NO2或亚甲二氧基的OH，CH2OH，R6和R7彼此独立地键合， A是具有1-7个C原子的烷基，Ar是可以在环中任选含有N，O或S原子的单环或双环芳族基团，并且可以被A， ，Hal，OH，OA，CF 3，NH 2，NHA，NA 2，NHCOA和/或NHCONH 2，D是CH 2，O，S，NH，NA，-CH 2 -CH 2 - ， - CH = CH-， - CH 2 NH-， CH2-NA-或键，Hal为F，Cl，Br或I.