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    Indol-3-yl derivatives
    1.
    发明授权
    Indol-3-yl derivatives 失效
    吲哚-3-基衍生物

    公开(公告)号：US06743810B2

    公开(公告)日：2004-06-01

    申请号：US10203406

    申请日：2002-08-09

    申请人： Matthias Wiesner ,  Simon Goodman ,  Rudolf Gottschlich

    发明人： Matthias Wiesner ,  Simon Goodman ,  Rudolf Gottschlich

    IPC分类号： A61K314439

    CPC分类号： C07D401/12 ,  C07D209/18 ,  C07D403/12 ,  C07D417/14

    摘要： Indol-3-yl derivatives of the general formula I in which A, B, X, R1, R2, R3, R4, R5, n and m are as defined in patent claim 1, and their physiologically acceptable salts or solvates are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumours, osteoporosis, rheumatic arthritis, macular degenerative disease, diabetic retinopathy, infections and restenosis after angioplasty or in pathological processes maintained or propagated by angiogenesis.

    摘要翻译： A，B，X，R 1，R 2，R 3，R 4，R 5，n和m的通式Iin的吲哚-3-基衍生物如 权利要求1，其生理上可接受的盐或溶剂化物是整联蛋白抑制剂，可用于对抗血栓形成，心肌梗死，冠心病，动脉硬化，炎症，肿瘤，骨质疏松症，风湿性关节炎，黄斑变性疾病，糖尿病性视网膜病变，感染和再狭窄 在血管成形术之后或通过血管发生维持或传播的病理过程中。

    Dibenzoazulene derivatives for treating thrombosis, osteoporosis, arteriosclerosis
    2.
    发明授权
    Dibenzoazulene derivatives for treating thrombosis, osteoporosis, arteriosclerosis 失效
    用于治疗血栓形成，骨质疏松症，动脉硬化的二苯并薁衍生物

    公开(公告)号：US06521646B1

    公开(公告)日：2003-02-18

    申请号：US09958812

    申请日：2001-10-15

    申请人： Wolfgang Stähle ,  Rudolf Gottschlich ,  Simon Goodman

    发明人： Wolfgang Stähle ,  Rudolf Gottschlich ,  Simon Goodman

    IPC分类号： A61K3144

    CPC分类号： C07D213/74 ,  C07C69/757 ,  C07C2603/40

    摘要： Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.

    摘要翻译： 式（I）化合物及其生理学上可接受的盐和溶剂合物可用作整合素抑制物质。 它们在预防和治疗心血管疾病，血栓形成，心肌梗死，冠心病，动脉硬化，骨质疏松症，通过血管发生引起或增殖的病理状况和肿瘤治疗中尤其有用。

    Sulfur-containing indole derivatives
    4.
    发明授权
    Sulfur-containing indole derivatives 失效
    含硫吲哚衍生物

    公开(公告)号：US4617309A

    公开(公告)日：1986-10-14

    申请号：US537621

    申请日：1983-09-30

    申请人： Henning Bottcher ,  Rudolf Gottschlich ,  Hans-Heinrich Hausberg ,  Christoph Seyfried ,  Klaus-Otto Minck

    发明人： Henning Bottcher ,  Rudolf Gottschlich ,  Hans-Heinrich Hausberg ,  Christoph Seyfried ,  Klaus-Otto Minck

    IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61P9/12 ,  A61P25/00 ,  A61P25/04 ,  C07D401/12 ,  C07D405/14 ,  C07D491/056

    CPC分类号： C07D401/12

    摘要： Sulfur-containing indole derivatives of the general formula I ##STR1## wherein Ind is a 3-indolyl radical which can be substituted once or twice by alkyl, O-alkyl, S-alkyl, SO-alkyl, SO.sub.2 -alkyl, OH, F, Cl, Br, CF.sub.3 and/or CN by a methylenedioxy group, A is --(CH.sub.2).sub.n --E--C.sub.m H.sub.2m -- or --(CH.sub.2).sub.n --E--C.sub.m-1 H.sub.2m-2 CO--, n is 0 or 1, m is 2, 3 or 4, E is S, SO or SO.sub.2 and Ar is a phenyl group which is unsubstituted or substituted once or twice by alkyl, O-alkyl, S-alkyl, SO-alkyl, SO.sub.2 -alkyl, OH, F, Cl, Br, CF.sub.3 and/or CN or by a methylenedioxy group and wherein the alkyl groups each have 1-4 C atoms, and their physiologically acceptable acid addition salts exhibit effects on the central nervous system.

    摘要翻译： 通式I的含硫吲哚衍生物其中Ind是可被烷基，O-烷基，S-烷基，SO-烷基，SO 2 - 烷基，OH取代一次或两次的3-吲哚基， （CH2）nE-CmH2m-或 - （CH2）nE-Cm-1H2m-2CO-，n为0或1，m为2，F，Cl，Br，CF3和/或CN为亚烷基二氧基， 3或4，E是S，SO或SO 2，Ar是未被取代或被烷基，O-烷基，S-烷基，SO-烷基，SO 2 - 烷基，OH，F，Cl， Br，CF 3和/或CN或亚甲二氧基，并且其中烷基各自具有1-4个C原子，并且其生理上可接受的酸加成盐对中枢神经系统表现出作用。

    Kappa-opiate agonists effective in the treatment of postoperative ileus
    7.
    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.

    Tetrahydrocarbazole derivatives
    8.
    发明授权
    Tetrahydrocarbazole derivatives 失效
    四氢咔唑衍生物

    公开(公告)号：US4547576A

    公开(公告)日：1985-10-15

    申请号：US568310

    申请日：1984-01-04

    申请人： Hans-Heinrich Hausberg ,  Henning Bottcher ,  Rudolf Gottschlich ,  Christoph Seyfried ,  Klaus-Otto Minck

    发明人： Hans-Heinrich Hausberg ,  Henning Bottcher ,  Rudolf Gottschlich ,  Christoph Seyfried ,  Klaus-Otto Minck

    IPC分类号： C07D401/06 ,  C07D405/14 ,  C07D409/14 ,  C07D491/04 ,  C07D491/056

    CPC分类号： C07D401/06 ,  C07D405/14 ,  C07D409/14 ,  C07D491/04

    摘要： Tetrahydrocarbazole derivatives of the general formula I ##STR1## in which Thc is a 1,2,3,4-tetrahydro-3-carbazolyl radical which can be substituted once or twice by alkyl, O-alkyl, S-alkyl, SO-alkyl, SO.sub.2 -alkyl, OH, F, Cl, Br, CF.sub.3 and/or CN or by a methylenedioxy group, the two radicals Y are each H or together are a C--C bond, one radical Z is Ar and the other radical Z is H, A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 -- and Ar is a phenyl group which is unsubstituted or substituted once or twice by alkyl, O-alkyl, S-alkyl, SO-alkyl, SO.sub.2 -alkyl, OH, F, Cl, Br, CF.sub.3 and/or CN or by a methylenedioxy group, or is a 2- or 3-thienyl radical, and in which the alkyl groups each have 1-4 C atoms, and their physiologically acceptable acid addition salts have effects on the central nervous system.

    摘要翻译： 其中Thc是1,2,3,4-四氢-3-咔唑基的四氢咔唑衍生物，其可以被烷基，O-烷基，S-烷基，SO- 烷基，SO 2 - 烷基，OH，F，Cl，Br，CF 3和/或CN或亚甲二氧基，两个基团Y各自为H或一起为CC键，一个基团Z为Ar，另一个基团Z为 H，A是-CH 2 - 或-CH 2 CH 2 - ，Ar是未被取代或被烷基，O-烷基，S-烷基，SO-烷基，SO 2 - 烷基，OH，F，Cl取代一次或两次的苯基， Br，CF 3和/或CN或亚甲二氧基，或是2-或3-噻吩基，其中烷基各自具有1-4个C原子，并且其生理上可接受的酸加成盐对中心具有影响 神经系统。

    Penicillins and their preparation
    9.
    发明授权
    Penicillins and their preparation 失效
    青霉素及其制备

    公开(公告)号：US4119631A

    公开(公告)日：1978-10-10

    申请号：US764786

    申请日：1977-02-02

    申请人： Rudolf Gottschlich ,  Werner Rogalski ,  Rolf Bergmann ,  Rosmarie Steinigeweg ,  Helmut Wahlig

    发明人： Rudolf Gottschlich ,  Werner Rogalski ,  Rolf Bergmann ,  Rosmarie Steinigeweg ,  Helmut Wahlig

    IPC分类号： C07D499/00 ,  C07D499/64 ,  C07D233/06

    CPC分类号： C07D499/00

    摘要： Carbamic acid lactones of the formula ##STR1## wherein Y is H or alkyl of 1-4 carbon atoms and R.sub.2 and R.sub.3 each are H or collectively with the carbon atoms to which they are attached form a first benzene or pyridine ring which is unsubstituted, substituted by up to two of alkyl, alkoxy of 1-4 carbon atoms, dialkylamino or halogen, wherein alkyl and alkoxy in each instance are of 1-4 carbon atoms, or is fused at two adjacent carbons to a second benzene or pyridine ring, are useful as intermediates for the production of penicillins by reaction with a penicillin of the formula ##STR2##

    摘要翻译： 其中Y是H或1-4个碳原子的烷基，R 2和R 3各自是H或与它们所连接的碳原子一起形成的第一个苯或吡啶环，其是未取代的， 被至多两个烷基，1-4个碳原子的烷氧基，二烷基氨基或卤素取代，其中每个实例中的烷基和烷氧基为1-4个碳原子，或者在两个相邻的碳上与第二个苯或吡啶环稠合， 可用作通过与式（IMAGE）的青霉素反应生产青霉素的中间体