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42 条记录 (耗时 0.012 秒)

    1,4-dihydropyridines
    3.
    发明授权
    1,4-dihydropyridines 失效
    1,4-二氢吡啶

    公开(公告)号：US4686229A

    公开(公告)日：1987-08-11

    申请号：US765908

    申请日：1985-08-14

    申请人： Ulrich Rosentreter ,  Elisabeth Perzborn ,  Friedel Seuter

    发明人： Ulrich Rosentreter ,  Elisabeth Perzborn ,  Friedel Seuter

    IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/50 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  C07C45/64 ,  C07C47/56 ,  C07D211/90 ,  C07D237/00 ,  C07D401/14 ,  C07D405/14

    CPC分类号： C07D401/14 ,  C07C45/64 ,  C07C47/56 ,  C07D211/90 ,  C07D405/14

    摘要： 1,4-Dihydropyridines of the formula ##STR1## in which R.sup.1 is hydrogen, or alkyl optionally substituted by halogen, nitro, cyano, alkoxy, carboxyl, alkoxycarbonyl or carboxamide,R.sup.2 is hydrogen or alkyl,R.sup.3 is hydrogen, alkyl, carboxyl, alkoxycarbonyl or aryl optionally substituted by hydroxyalkyl, carboxyl, sulphoxy, acloxyalkyl, or ##STR2## R.sup.4 is alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, ##STR3## X is oxygen, sulphur or NH, and n is 1 to 6,or physiologically acceptable salts thereof, which are active in combating thromboembolic and ischaemic disorders.

    摘要翻译： 式为“IMAGE”的1,4-二氢吡啶，其中R1为氢，或任选被卤素，硝基，氰基，烷氧基，羧基，烷氧基羰基或羧酰胺取代的烷基，R2为氢或烷基，R3为氢，烷基，羧基， 任选被羟烷基，羧基，磺氧基，酰氧基烷基取代的烷氧基羰基或芳基，或者R 4是烷基，芳基，杂芳基，芳烷基，杂芳烷基，X是氧，硫或NH，n是1至 6或其生理上可接受的盐，其对抗血栓栓塞和缺血性疾病是有活性的。

    Inhibiting lipoxygenase with pyrazolone derivatives
    4.
    发明授权
    Inhibiting lipoxygenase with pyrazolone derivatives 失效
    用吡唑啉酮衍生物抑制脂氧合酶

    公开(公告)号：US4670460A

    公开(公告)日：1987-06-02

    申请号：US808582

    申请日：1985-12-13

    申请人： Mithat Mardin ,  Friedel Seuter ,  Elisabeth Perzborn ,  Klaus Schlossmann ,  Dieter Mayer ,  Volker Fiedler

    发明人： Mithat Mardin ,  Friedel Seuter ,  Elisabeth Perzborn ,  Klaus Schlossmann ,  Dieter Mayer ,  Volker Fiedler

    IPC分类号： A61K31/415

    CPC分类号： A61K31/415

    摘要： A method of inhibiting lipoxygenase in a patient, for the prophylaxis and/or treatment of ischaemias and disorders in cardiac rhythm, inflammations of the skin and the eye, and of rheumatic, allergic and asthmatic diseases, oedemas, pulmonary embolisms, pulmonary hypertension, shock lung, oxygen intoxications and ulcerations which comprises administering to such patient an effective amount of a compound of the formula ##STR1## wherein R represents an aryl or heteroaryl radical which has 6 to 12 C atoms and optionally contains 1 to 3 identical or different substituents from the group comprising halogen, trifluoromethyl, alkyl, alkenyl, alkoxy, alkylamino, cyano, trifluoromethoxy, nitro, hydroxyl, SO.sub.n -alkyl (n=0 to 2) or SO.sub.n -trifluoromethyl (n=0 to 2), alkyl, alkenyl and alkoxy in each case being understood as meaning radicals with 1 to 4 C atoms,R.sup.1 represents hydrogen or a hydrocarbon radical which has 1 to 18 C atoms and optionally contains a hydroxyl, ether, ester or carboxyl group and optionally 1 to 3 halogen atoms,R.sup.2 has the meaning of R.sup.1 or represents radical ##STR2## R.sup.3 represents hydrogen or an acyl or sulphonyl radical with in each case 1 to 15 C atoms andX represents one of the groups --O--CH.sub.2 --CH.sub.2 --, --S--CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.sub.2 or ##STR3## the oxygen or sulphur atom being bonded to the radical R, and with the provisio that X does not represent --O--CH.sub.2 --CH.sub.2 -- if R=.beta.-naphthyl, R.sup.1 =CH.sub.3 and R.sup.2 =R.sup.3 =H.

    摘要翻译： 一种在患者体内抑制脂氧合酶的方法，用于预防和/或治疗心脏节律，皮肤和眼睛炎症以及风湿性，过敏性和哮喘性疾病，oedemas，肺栓塞，肺动脉高压，休克 肺，氧中毒和溃疡，其包括向此类患者施用有效量的式（I）化合物，其中R表示具有6至12个C原子并且任选地含有1至3个相同或相同或相同的1至3个的芳基或杂芳基， 硝基，羟基，SO1-烷基（n = 0至2）或SO 3 - 三氟甲基（n = 0至2）的不同取代基，烷基，环烷基， 烯基和烷氧基在每种情况下被理解为含有1至4个C原子的基团，R 1表示氢或具有1至18个C原子并且任选地含有羟基，醚，酯或羧基的烃基 p和任选的1至3个卤素原子，R 2具有R 1的含义或表示基团R 3表示氢或酰基或磺酰基，在每种情况下为1至15个C原子，X表示基团-O-CH 2 -CH 2 - ， - CH 2 -CH 2 - ， - CH 2 -CH 2 - ， - CH 2 -CH 2 - ， - CH 2或者 - 或者与基团R键合的氧原子或硫原子， 如果R =β-萘基，R1 = CH3，R2 = R3 = H，则不表示-O-CH2-CH2-。

    1-Substituted pyrazoles
    5.
    发明授权
    1-Substituted pyrazoles 失效

    公开(公告)号：US4117145A

    公开(公告)日：1978-09-26

    申请号：US766715

    申请日：1977-02-08

    申请人： Eike Moller ,  Karl-August Meng, deceased ,  Egbert Wehinger ,  Harald Horstmann ,  Friedel Seuter

    发明人： Eike Moller ,  Karl-August Meng, deceased ,  Egbert Wehinger ,  Harald Horstmann ,  Friedel Seuter

    IPC分类号： C07D231/20 ,  A61K31/415 ,  A61K31/445

    CPC分类号： C07D231/20 ,  Y10S514/822 ,  Y10S514/869

    摘要： Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, trifluoromethyl, aryl, aralkyl or a heterocycle;R.sup.1 is hydrogen, alkyl, aryl or aralkyl;R.sup.3 is an unsubstituted or substituted carboacyl or sulphonyl moiety;X is (a) methylene; (b) ethylene; (c) ethylene wherein 1 hydrogen atom on one or both of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms; (d) ethylene, or ethylene wherein 1 hydrogen atom on one or both of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, linked to R.sup.2 via an oxygen or sulphur atom; (e) propenyl; or (f) propenyl wherein a hydrogen atom on 1, 2 or 3 of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms; said propenyl moiety being linked to the N.sup.1 atom via a methylene moiety; andR.sup.2 is aryl unsubstituted or substituted by 1 or 2 of the same or different substituents selected from the group consisting of alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, cycloalkyl, cycloalkenyl, mono- or di-alkylamino, nitro, cyano, unsubstituted or substituted carboxamido, unsubstituted or substituted sulphonamido and SO.sub.n -alkyl wherein n is 0 to 2, or aryl having 2 substituents which together form a branched or unbranched, saturated or unsaturated 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring containing 1 or 2 oxygen or sulphur atoms, or pyridyl;Are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.

    Quinolinoxy phenylsulphonamides
    7.
    发明授权
    Quinolinoxy phenylsulphonamides 失效
    喹啉氧基苯酚

    公开(公告)号：US5070096A

    公开(公告)日：1991-12-03

    申请号：US614329

    申请日：1990-11-15

    申请人： Klaus Mohrs ,  Elisabeth Perzborn ,  Friedel Seuter ,  Romanis Fruchtmann ,  Christian Kohlsdorfer

    发明人： Klaus Mohrs ,  Elisabeth Perzborn ,  Friedel Seuter ,  Romanis Fruchtmann ,  Christian Kohlsdorfer

    IPC分类号： A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61K31/47 ,  A61K31/472 ,  A61P3/00 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P29/00 ,  A61P37/08 ,  C07D213/38 ,  C07D213/74 ,  C07D215/12 ,  C07D215/14 ,  C07D215/20 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D215/38 ,  C07D217/02 ,  C07D217/14 ,  C07D217/22

    CPC分类号： C07D213/74 ,  C07D213/38 ,  C07D215/14 ,  C07D215/20 ,  C07D215/227 ,  C07D215/26

    摘要： New phenylsulphonamide of the formula in which ##STR1## R.sup.1 represents a pyridyl, quinolyl or isoquinolyl radical which is unsubstituted or substituted by halogen, alkyl, cycloalkyl, alkoxy, cyano, nitro, halogenoalkyl, halogenoalkoxy, alkoxycarbonyl or alkylsulphonyl,R.sup.2 represents hydrogen, cyano, nitro, halogen, alkyl, alkoxy, halogenoalkyl, halogenoalkoxy or alkoxycarbonyl,R.sup.3 represents an aryl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted by halogen, halogenoalkyl, halogenoalkoxy, alkyl, alkoxy, alkylthio, alkylsulphonyl, cyano, nitro or alkoxycarbonyl, the substituents being identical or different, or represents pentafluorophenyl or represents a straight-chain, branched or cyclic alkyl which is unsubstituted or substituted by halogen, aryl, aryloxy, cyano, alkoxycarbonyl, alkoxy, alkylthio or trifluoromethyl, andX represents an --O--, --A--B-- or --B--A-- groupwhereA denotes --O--, ##STR2## and B denotes --CH.sub.2 -- or ##STR3## where R.sup.1 does not represent a pyridyl radical when x represents an --O-- group, and salts thereof are prepared by reacting appropriate amines with sulphonyl halides. The substituted phenylsulphonamides can be employed as active compounds for inhibiting enzymatic reactions and for inhibiting thrombocyte aggregations.

    摘要翻译： 新的具有下式的苯基磺酰胺，其中R 1表示未被取代或被卤素，烷基，环烷基，烷氧基，氰基，硝基，卤代烷基，卤代烷氧基，烷氧基羰基或烷基磺酰基取代的吡啶基，喹啉基或异喹啉基，R2表示 氢，氰基，硝基，卤素，烷基，烷氧基，卤代烷基，卤代烷氧基或烷氧基羰基，R3表示未被取代或被卤素，卤代烷基，卤代烷氧基，烷基，烷氧基，烷硫基，烷基磺酰基，氰基，硝基取代或三取代的芳基 或烷氧基羰基，取代基相同或不同，或表示五氟苯基，或表示未被取代或被卤素，芳基，芳氧基，氰基，烷氧基羰基，烷氧基，烷硫基或三氟甲基取代的直链，支链或环状烷基，X表示 -O-，-AB-或-BA-基团，其中A表示-O-，和B表示-CH2-或，其中R1不表示 当x表示-O-基团时，是一个吡啶基，其盐可以通过使适当的胺与磺酰卤反应来制备。 取代的苯基磺酰胺可用作抑制酶反应和抑制血小板聚集的活性化合物。

    Circulation-active substituted 5-nitro-1,4-dihydropyridines
    10.
    发明授权
    Circulation-active substituted 5-nitro-1,4-dihydropyridines 失效
    循环活性取代的5-硝基-1,4-二氢吡啶

    公开(公告)号：US4876254A

    公开(公告)日：1989-10-24

    申请号：US179102

    申请日：1988-04-08

    申请人： Gerhard Franckowiak ,  Michael Kayser ,  Matthias Schramm ,  Gunther Thomas ,  Rainer Gross ,  elisabeth Perzborn ,  Friedel Seuter

    发明人： Gerhard Franckowiak ,  Michael Kayser ,  Matthias Schramm ,  Gunther Thomas ,  Rainer Gross ,  elisabeth Perzborn ,  Friedel Seuter

    IPC分类号： A61K31/50 ,  A61K31/505 ,  A61P9/00 ,  C07D211/90 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    CPC分类号： C07D401/12 ,  C07D211/90 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14

    摘要： For the treatment of circulation disorders, the novel 5-nitro-1,4-dihydropyridines of the formula ##STR1## in which R represents C.sub.6 -C.sub.14 -aryl which can be mono- to pentasubstituted by identical or different substituents from the series comprising halogen, nitro, cyano, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, trifluoromethyl, trifluoromethoxy, difluoromethoxy, trifluoromethylthio and benzyl, benzyloxy or benzylthio optionally substituted by nitro, cyano, trifluoromethyl, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, orrepresents a heterocycle from the series pyrryl, thienyl, furyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidyl, quinolyl, benzoxadiazolyl, chromenyl or thiochromenyl optionally mono- to tetrasubstituted by halogen, phenyl or C.sub.1 -C.sub.4 -alkyl orrepresents straight-chain, branched or cyclic alkyl with up to 14 carbon atoms,and their physiologically acceptable salts.

    摘要翻译： 对于循环障碍的治疗，式“IMAGE”的新的5-硝基-1,4-二氢吡啶类，其中R代表C6-C14-芳基，其可以由包含卤素的系列的相同或不同的取代基单取代或五取代 硝基，氰基，C 1 -C 6烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷硫基，三氟甲基，三氟甲氧基，二氟甲氧基，三氟甲硫基和苄基，任选被硝基，氰基， 或C 1 -C 4 - 烷氧基，或代表吡啶基，噻吩基，呋喃基，吡唑基，咪唑基，恶唑基，噻唑基，吡啶基，哒嗪基，嘧啶基，喹啉基，苯并二唑基， 被卤素，苯基或C 1 -C 4烷基四取代，或代表具有至多14个碳原子的直链，支链或环状烷基，及其生理上可接受的盐。