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1. 发明授权

US4188395A 1,4-Dihydropyridine derivatives substituted in the 2 position, and their use as medicaments 失效
公开(公告)号：US4188395A
公开(公告)日：1980-02-12
申请号：US856559
申请日：1977-12-01
申请人： Friedrich Bossert , Egbert Wehinger , Horst Meyer , Arend Heise , Stanislav Kazda , Kurt Stoepel , Robertson Towart , Wulf Vater , Klaus Schlossmann
发明人： Friedrich Bossert , Egbert Wehinger , Horst Meyer , Arend Heise , Stanislav Kazda , Kurt Stoepel , Robertson Towart , Wulf Vater , Klaus Schlossmann
IPC分类号： A61K31/4427 , A61K31/455 , A61P3/06 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D211/90 , C07D401/04 , C07D401/06 , C07D401/14 , C07D213/55 , A61K31/44
CPC分类号： C07D401/04 , C07D211/90 , C07D401/14
摘要： The present invention provides 1,4-dihydropyridine derivatives of the formula in which ##STR1## R represents hydrogen, alkyl, alkenyl, alkoxyalkyl, aryl or aralkyl, the alkyl and aryl groups being optionally substituted,A represents a straight-chain or branched alkylene radical,R.sup.1 represents (a) an optionally substituted alkylthio group or (b) a group of the formula O--CO-alkyl, O--CO-aryl or O--CO-aralkyl, the alkyl and aryl groups being optionally substituted or (c) a phthalimido radical which is optionally substituted in the benzene ring, Y and Z are identical or different and each represents a group of the formula COOR.sup.2 or COR.sup.2,whereinR.sup.2 represents alkyl, alkenyl, alkinyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl or aralkyl, the alkyl and aryl radicals being optionally substituted, orY and Z are identical or different and each represents a cyano radical or a radical of the formula S(O).sub.n --R.sup.3,whereinR.sup.3 represents alkyl, alkenyl, alkoxyalkyl, aminoalkyl, alkylaminoalkyl, aryl or aralkyl, the alkyl and aryl radicals mentioned being optionally substituted, and n represents 0, 1 or 2,R.sup.4 represents hydrogen or alkyl, the alkyl radical being optionally substituted or interrupted by oxygen, or represents the radical A--R.sup.1,whereinA and R.sup.1 have the abovementioned meaning, and X represents an aryl radical, which optionally contains one to three identical or different substituents selected from phenyl, alkyl, alkenyl, alkinyl, alkoxy, alkinoxy, acyloxy, halogen, trifluoromethyl, trifluoromethoxy, hydroxyl, nitro, cyano, azido, amino, alkylamino, acylamino, carbalkoxy, carboxamido, sulphonamide and S(O).sub.n -alkyl (n=0 to 2), or represents a quinolyl, pyridyl, pyrimidyl, thienyl, furyl or pyrryl radical which is optionally substituted by alkyl, alkylamino, nitro or halogen, or represents an optionally substituted aralkyl, cycloalkyl, cycloalkenyl or styryl radical, and acid addition salts thereof.Also included in the invention are methods for the preparation of the 1,4-dihydropyridine derivatives of the invention, compositions containing said derivatives and methods for their use.

2. 发明授权

US4177278A 2-Alkyleneaminodihydropyridines compounds, their production and their medicinal use 失效
标题翻译： 2-亚氨基二氢吡啶类化合物，其生产及其药用
公开(公告)号：US4177278A
公开(公告)日：1979-12-04
申请号：US886971
申请日：1978-03-15
申请人： Friedrich Bossert , Egbert Wehinger , Arend Heise , Stanislav Kazda , Kurt Stoepel , Robertson Towart , Wulf Vater , Klaus Schlossmann
发明人： Friedrich Bossert , Egbert Wehinger , Arend Heise , Stanislav Kazda , Kurt Stoepel , Robertson Towart , Wulf Vater , Klaus Schlossmann
IPC分类号： A61K31/4427 , A61K31/455 , A61P3/06 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D211/90 , C07D401/04 , C07D213/55 , A61K31/44
CPC分类号： C07D211/90
摘要： The invention includes the provision of 2-alkyleneaminodihydropyridines and salts thereof and are useful, inter alia, as coronary dilators and antihypertensive agents. Also included in the invention are pharmaceutical compositions containing said 2-alkyleneaminodihydropyridines and methods of treatment involving the use of said compounds or compositions.
摘要翻译：本发明包括提供2-亚烷基氨基二氢吡啶及其盐，尤其可用作冠状动脉扩张剂和抗高血压药。本发明还包括含有所述2-亚烷基氨基二氢吡啶的药物组合物和涉及使用所述化合物或组合物的治疗方法。

3. 发明授权

US4976964A Medicament formulation containing dihydropyridines and a process for its preparation 失效
标题翻译：含有二氢吡啶类的药物制剂及其制备方法
公开(公告)号：US4976964A
公开(公告)日：1990-12-11
申请号：US852584
申请日：1986-04-16
申请人： Klaus Schlossmann , Alfred Zembrod , Stanislav Kazda , Peter Serno , Bernd Klinksiek
发明人： Klaus Schlossmann , Alfred Zembrod , Stanislav Kazda , Peter Serno , Bernd Klinksiek
IPC分类号： C07D211/90 , A61K9/127 , A61K31/44 , A61P9/00 , A61P9/08 , A61P9/10
CPC分类号： A61K31/44 , A61K9/127 , A61K9/1277 , Y10T428/2984
摘要： In the parenteral administration of a dihydropyridine, the improvement which comprises administering the dihydropyridine in an aqueous medium of pH 3 to 8.5 having dispersed therein liposomes with an average diameter of 20-1000 nm, the liposome membrane containng the following constituents by weight:(a) a part of a dihydropyridine, and(b) 5-500 parts of lipids.The aqueous medium is storage stable and readily injectable.
摘要翻译：在二氢吡啶的肠胃外给药中，包括将二氢吡啶在pH3〜8.5的水性介质中投入，其中分散有平均直径为20-1000nm的脂质体，脂质体膜含有以下重量份数：（a ）二氢吡啶的一部分，和（b）5-500份脂质。水性介质储存稳定且易于注射。

4. 发明授权

US5026714A Novel 1-alkyl-substituted 1,4-dihydropyridinelactone anti-diabetics 失效
标题翻译：新的1-烷基取代的1,4-二氢吡啶内酯抗糖尿病药
公开(公告)号：US5026714A
公开(公告)日：1991-06-25
申请号：US436157
申请日：1989-11-13
申请人： Siegfried Goldmann , Friedrich Bossert , Hilmar Bischoff , Dieter Petzinna , Walter Puls , Klaus Schlossmann
发明人： Siegfried Goldmann , Friedrich Bossert , Hilmar Bischoff , Dieter Petzinna , Walter Puls , Klaus Schlossmann
IPC分类号： A61K31/435 , A61P3/08 , A61P3/10 , C07D211/90 , C07D491/04 , C07D491/048
CPC分类号： C07D491/04 , C07D211/90
摘要： Novel blood sugar-lowering dihydropyridinelactones of the formula ##STR1## in which R represents halogen, C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.10 -alkoxy, C.sub.1 -C.sub.10 -alkylthio, C.sub.1 -C.sub.10 -alkylsulphinyl, C.sub.1 -C.sub.10 -alkylsulphonyl, cyano, C.sub.1 -C.sub.6 - mono- or polyfluoroalkyl, C.sub.1 -C.sub.6 -mono- or polyfluoroalkoxy or nitro,R.sup.1 represents hydrogen, halogen or C.sub.1 -C.sub.10 -alkyl or C.sub.1 -C.sub.10 -alkoxy,R.sup.2 represents a C.sub.1 -C.sub.20 hydrocarbon radical which can optionally be interrupted or substituted,R.sup.3 represents hydrogen NH.sub.2, CHO, CN or a C.sub.1 -C.sub.6 hydrocarbon radical which can be interrupted in the chain, andR.sup.4 represents a C.sub.1 -C.sub.10 -alkyl or C.sub.2 -C.sub.10 -alkenyl radical which can optionally be interrupted or substituted with the proviso that R is not CF.sub.3 if R.sup.2 represents C.sub.2 H.sub.5.
摘要翻译：式中，R表示卤素，C 1 -C 10 - 烷基，C 1 -C 10 - 烷氧基，C 1 -C 10 - 烷硫基，C 1 -C 10 - 烷基亚磺酰基，C 1 -C 10 - 烷基磺酰基，氰基， C 1 -C 6 - 单 - 或多氟烷基，C 1 -C 6 - 单 - 或多氟烷氧基或硝基，R 1表示氢，卤素或C 1 -C 10 - 烷基或C 1 -C 10 - 烷氧基，R 2表示可任选地为中间或取代的，R 3表示可在该链中中断的氢NH 2，CHO，CN或C 1 -C 6烃基，R 4表示可任选被中断或取代的C 1 -C 10 - 烷基或C 2 -C 10 - 烯基条件是如果R2表示C2H5，R不为CF3。

5. 发明授权

US4721719A Dihydropyridinelactols and their use as medicaments which influence blood sugar 失效
标题翻译：二氢嘧啶醇和它们作为影响血糖的药物的用途
公开(公告)号：US4721719A
公开(公告)日：1988-01-26
申请号：US900866
申请日：1986-08-27
申请人： Siegfried Goldmann , Friedrich Bossert , Hans J. Ahr , Hilmar Bischoff , Walter Puls , Dieter Petzinna , Klaus Schlossmann , Joachim Bender
发明人： Siegfried Goldmann , Friedrich Bossert , Hans J. Ahr , Hilmar Bischoff , Walter Puls , Dieter Petzinna , Klaus Schlossmann , Joachim Bender
IPC分类号： C07D307/33 , A61K31/435 , A61K31/4355 , A61K31/44 , A61P3/08 , A61P3/10 , C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D491/04
摘要： Reducing blood sugar with the novel dihydropyridinelactols, or salts thereof, of the formula ##STR1## in which R.sup.1 represents a phenyl, naphthyl, thienyl, pyridyl, chromonyl, thiochromonyl or thiochromenyl radical, the stated radicals optionally containing 1 or 2 identical or different substituents from the group consisting of fluorine, chlorine and bromine, alkyl, alkoxy and alkylthio, each having 1 to 6 carbon atoms, and fluoroalkyl or fluoroalkoxy, each having up to 3 carbon atoms and 3 fluorine atoms, and nitro and cyano,R.sup.2 represents a straight-chain, branched or cyclic alkyl having up to 12 carbon atoms which is optionally interrupted by 1 or 2 oxygen or sulphur atoms and which is optionally substituted by fluorine, chlorine, phenyl, cyano, hydroxyl, amino, C.sub.1 -C.sub.3 -alkylamino, di-C.sub.1 -C.sub.3 -alkylamino or N-benzylmethylamino,R.sup.3 represents cyano or straight-chain or branched alkyl which has up to 4 carbon atoms and is optionally interrupted in the chain by N-C.sub.1 -C.sub.3 -alkyl and/or oxygen, andR.sup.4 represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms and is optionally interrupted by 1 or 2 oxygen atoms and is substituted by one or more radicals from amongst fluorine, chlorine, hydroxyl, phenyl, amino, carboxyl and C.sub.1 -C.sub.4 -alkoxycarbonyl.
摘要翻译：其中R 1表示苯基，萘基，噻吩基，吡啶基，苯并二氢吡喃基或硫代色烯基的新颖的二氢吡啶类醇或其盐，降低血糖，所述基团任选地含有1或2个相同或不同的取代基由氟，氯和溴组成的组，每个具有1至6个碳原子的烷基，烷氧基和烷硫基，以及氟烷基或氟烷氧基，各自具有至多3个碳原子和3个氟原子，以及硝基和氰基，R2表示任选被1或2个氧原子或硫原子间隔的碳原子数为12的直链，支链或环状烷基，任选被氟，氯，苯基，氰基，羟基，氨基，C 1 -C 3 - 烷基氨基，二-C 1 -C 3 - 烷基氨基或N-苄基甲基氨基，R 3表示氰基或直链或支链烷基，其具有至多4个碳原子并且可选地被N-C 1 -C 3 - 烷基和/或氧中断， R4表示直链，支链或环状烷基，其具有多达6个碳原子，并且任选地被1或2个氧原子中断，并被氟，氯，羟基，苯基，氨基，羧基和C1中的一个或多个基团取代 -C 1-4 - 烷氧基羰基。

6. 发明授权

US4786641A Dihydropyridine compounds and their use in reducing blood sugar 失效
标题翻译：二氢吡啶化合物及其在降血糖中的应用
公开(公告)号：US4786641A
公开(公告)日：1988-11-22
申请号：US87491
申请日：1987-08-20
申请人： Siegfried Goldmann , Hans-Jurgen Ahr , Walter Puls , Hilmar Bischoff , Dieter Petzinna , Klaus Schlossmann , Joachim Bender
发明人： Siegfried Goldmann , Hans-Jurgen Ahr , Walter Puls , Hilmar Bischoff , Dieter Petzinna , Klaus Schlossmann , Joachim Bender
IPC分类号： A61K31/465 , A61K31/445 , A61K31/451 , A61P3/08 , C07D211/90 , C07D491/04 , C07D491/044 , C07D491/048 , A61K31/44
CPC分类号： C07D491/04 , C07D211/90
摘要： Blood-sugar-lowering dihydropyridines of the formula ##STR1## in which R.sup.1 represents phenyl, naphthyl, thienyl, pyridyl, chromenyl or thiochromenyl, it being possible for the radicals mentioned each to carry up to 2 identical or different substituents from the series comprising halogen, alkyl, alkoxy and alkylthio with in each case up to 6 carbon atoms, fluoroalkyl and fluoroalkoxy with in each case up to 3 carbon atoms and 3 fluorine atoms, nitro and cyano,R.sup.2 represents straight-chain, branched or cyclic alkyl which has up to 8 carbon atoms, can be interrupted in the alkyl chain by an oxygen or a sulphur atom and can be substituted by halogen, phenyl, cyano, hydroxyl, amino, alkylamino or dialkylamino with in each case up to 3 carbon atoms per alkyl group or by N-benzylmethylamino,R.sup.3 represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms, can be interrupted in the alkyl chain by an oxygen atom and can be substituted by halogen, hydroxyl, amino, phenyl, morpholino, carboxy or alkoxycarbonyl with up to 4 carbon atoms andR.sup.4 and R.sup.5 each represent hydroxyl, orR.sup.4 and R.sup.5 together represent --O--,or a physiologically acceptable salt thereof.
摘要翻译：其中R1代表苯基，萘基，噻吩基，吡啶基，色烯基或硫代色烯基的式“IMAGE”的降血糖二氢吡啶类，各自所提及的基团有可能从包含卤素的系列中携带多达2个相同或不同的取代基，烷基，烷氧基和烷硫基，在每种情况下最多6个碳原子，氟代烷基和氟代烷氧基，在每种情况下最多3个碳原子和3个氟原子，硝基和氰基，R2表示直链，支链或环状的烷基，至8个碳原子，可以通过氧或硫原子在烷基链中被中断，并且可以被卤素，苯基，氰基，羟基，氨基，烷基氨基或二烷基氨基取代，在每种情况下，每个烷基最多为3个碳原子，或通过N-苄基甲基氨基，R3表示具有多至6个碳原子的直链，支链或环状烷基，可以在烷基链中被氧原子中断，并可被卤素，羟基，氨基，苯基，具有至多4个碳原子的直链，羧基或烷氧基羰基，且R 4和R 5各自表示羟基，或者R 4和R 5一起表示-O-或其生理上可接受的盐。

7. 发明授权

US4657924A Nafazatrom as a lipoxygenase inhibitor 失效
标题翻译： Nafazatrom作为脂氧合酶抑制剂
公开(公告)号：US4657924A
公开(公告)日：1987-04-14
申请号：US715438
申请日：1985-03-25
申请人： Mithat Mardin , Wolf-Dieter Busse , Friedrich Hoffmeister , Friedel Seuter , Elisabeth Perzborn , Klaus Schlossmann , Dieter Mayer , Volker Fiedler
发明人： Mithat Mardin , Wolf-Dieter Busse , Friedrich Hoffmeister , Friedel Seuter , Elisabeth Perzborn , Klaus Schlossmann , Dieter Mayer , Volker Fiedler
IPC分类号： A61K31/415
CPC分类号： A61K31/415 , Y10S514/821 , Y10S514/826
摘要： A method of inhibiting lipoxygenase in a patient, for the prophylaxis and/or treatment of ischaemias and disorders in cardiac rhythm and of rheumatic, allergic and asthmatic diseases, oedemas, pulmonary embolisms, pulmonary hypertension, oxygen intoxications and ulcerations which comprises administering to such patient an effective amount of nafazatrom.
摘要翻译：一种抑制患者中脂质氧合酶的方法，用于预防和/或治疗心律和风湿性，过敏性和哮喘性疾病，oedemas，肺栓塞，肺动脉高压，氧中毒和溃疡中的局部缺血和疾病，其包括向该患者施用有效量的nafazatrom。

8. 发明授权

US4540707A Nafazatrom as a lipoxygenase inhibitor 失效
公开(公告)号：US4540707A
公开(公告)日：1985-09-10
申请号：US486175
申请日：1983-04-18
申请人： Mithat Mardin , Wolf-Dieter Busse , Friedrich Hoffmeister , Friedel Seuter , Elisabeth Perzborn , Klaus Schlossmann , Dieter Mayer , Volker Fiedler
发明人： Mithat Mardin , Wolf-Dieter Busse , Friedrich Hoffmeister , Friedel Seuter , Elisabeth Perzborn , Klaus Schlossmann , Dieter Mayer , Volker Fiedler
IPC分类号： A61K31/415
CPC分类号： A61K31/415 , Y10S514/821 , Y10S514/826
摘要： A method of inhibiting lipoxygenase in a patient, for the prophylaxis and/or treatment of ischaemias and disorders in cardiac rhythm and of rheumatic, allergic and asthmatic diseases, oedemas, pulmonary embolisms, pulmonary hypertension, oxygen intoxications and ulcerations which comprises administering to such patient an effective amount of nafazatrom.

9. 发明授权

US4894378A Lowering blood sugar with novel 4-thienyl-dihydropyridines 失效
标题翻译：用新的4-噻吩基 - 二氢吡啶降低血糖
公开(公告)号：US4894378A
公开(公告)日：1990-01-16
申请号：US210061
申请日：1988-06-22
申请人： Siegfried Goldmann , Hilmar Bischoff , Walter Puls , Joachim Bender , Dieter Petzinna , Klaus Schlossmann
发明人： Siegfried Goldmann , Hilmar Bischoff , Walter Puls , Joachim Bender , Dieter Petzinna , Klaus Schlossmann
IPC分类号： A61K31/435 , A61P3/08 , A61P3/10 , C07D491/04 , C07D491/048
CPC分类号： C07D491/04
摘要： Blood sugar levels are reduced by administration of novel 4-thienyl-dihydropyridines of the formula ##STR1## in which R.sup.1 represents 1 or 2 halogen atoms, or represents straight-chain, branched or cyclic alkyl with up to 8 carbon atoms,R.sup.2 represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical which has up to 15 carbon atoms, is optionally interrupted by one or two oxygen atoms, -N-phenyl or --SO.sub.n -- (n=0, 1 or 2) and is optionally substituted by halogen, phenyl, hydroxyl, cyano, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, pyridyl, piperidino, N-phenylpiperazino, N-methylpiperazino, morpholino or N-benzyl-N-methyl-amino,R.sup.3 represents hydrogen, or represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms and is optionally substituted by halogen, hydroxyl, amino or amino-C.sub.1 -C.sub.6 -alkoxy, or represents cyano or formyl andR.sup.4 represents hydrogen or a straight-chain, branched or cyclic alkyl radical which has up to 10 carbon atoms, is optionally interrupted by one or two oxygen atoms in the chain and is optionally substituted by halogen, cyano, hydroxyl, phenyl, carboxyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, amino, C.sub.1 14 C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, formyl, piperidino, morpholino or thiomorpholino, or physiologically acceptable salts thereof.

10. 发明授权

US4801715A Certain 4-thienyl-dihydropyridines 失效
标题翻译：某些4-噻吩基 - 二氢吡啶类
公开(公告)号：US4801715A
公开(公告)日：1989-01-31
申请号：US937870
申请日：1986-12-04
申请人： Siegfried Goldmann , Hilmar Bischoff , Walter Puls , Joachim Bender , Dieter Petzinna , Klaus Schlossmann
发明人： Siegfried Goldmann , Hilmar Bischoff , Walter Puls , Joachim Bender , Dieter Petzinna , Klaus Schlossmann
IPC分类号： A61K31/435 , A61P3/08 , A61P3/10 , C07D491/04 , C07D491/048
CPC分类号： C07D491/04
摘要： Blood sugar levels are reduced by administration of novel 4-thienyl-dihydropyridines of the formula ##STR1## in which R.sup.1 represents 1 or 2 halogen atoms, or represents straight-chain, branched or cyclic alkyl with up to 8 carbon atoms,R.sup.2 represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical which has up to 15 carbon atoms, is optionally interrupted by one or two oxygen atoms, -N-phenyl or --SO.sub.n --(n=0, 1 or 2) and is optionally substituted by halogen, phenyl, hydroxyl, cyano, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, pyridyl, piperidino, N-phenylpiperazino, N-methylpiperazino, morpholino or N-benzyl-N-benzyl-N-methyl-amino,R.sup.3 represents hydrogen, or represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms and is optionally substituted by halogen, hydroxyl, amino or amino-C.sub.1 -C.sub.6 -alkoxy, or represents cyano or formyl andR.sup.4 represents hydrogen or a straight-chain, branched or cyclic alkyl radical which has up to 10 carbon atoms, is optionally interrupted by one or two oxygen atoms in the chain and is optionally substituted by halogen, cyano, hydroxyl, phenyl, carboxyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, formyl, piperidino, morpholino or thiomorpholino,or physiologically acceptable salts thereof.
摘要翻译：通过给予式“IMAGE”的新型4-噻吩基 - 二氢吡啶，其中R1代表1或2个卤素原子，或代表具有至多8个碳原子的直链，支链或环状烷基，降低血糖水平，R2代表具有多至15个碳原子的直链，支链或环状饱和或不饱和烃基任选地被一个或两个氧原子间隔，-N-苯基或-SOn-（n = 0,1或2），并且是任选被卤素，苯基，羟基，氰基，氨基，C 1 -C 6 - 烷基氨基，二-C 1 -C 6 - 烷基氨基，吡啶基，哌啶子基，N-苯基哌嗪子基，N-甲基哌嗪基，吗啉代或N-苄基-N-苄基-N 甲基 - 氨基，R 3表示氢，或表示具有多至6个碳原子并且任选被卤素，羟基，氨基或氨基-C 1 -C 6 - 烷氧基取代的直链，支链或环状烷基，或表示氰基或甲酰基并且R 4表示氢或具有至多10个碳的直链，支链或环状烷基氰基，羟基，苯基，羧基，C 1 -C 6 - 烷氧基羰基，氨基，C 1 -C 6 - 烷基氨基，二-C 1 -C 6烷基氨基，C 1 -C 6 - 烷基氨基，，甲酰基，哌啶子基，吗啉代或硫代吗啉代，或其生理上可接受的盐。

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