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91. 发明申请

US20050004207A1 Substituted isoindoles and the use thereof 失效
公开(公告)号：US20050004207A1
公开(公告)日：2005-01-06
申请号：US10484369
申请日：2002-07-03
申请人： Alexander Straub , Thomas Lampe , Jens Pohlmann , Susanne Rohrig , Stephan Jordan , Elisabeth Perzborn , Karl-Heinz Schlemmer
发明人： Alexander Straub , Thomas Lampe , Jens Pohlmann , Susanne Rohrig , Stephan Jordan , Elisabeth Perzborn , Karl-Heinz Schlemmer
IPC分类号： C07D473/00 , A61K31/4025 , A61K31/4035 , A61K31/4155 , A61K31/4178 , A61K31/4184 , A61K31/422 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/52 , A61K31/5377 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P19/02 , A61P25/28 , A61P35/00 , C07D209/46 , C07D209/48 , C07D213/81 , C07D409/12 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/14 , C07D521/00 , A61K31/4015 , C07D207/40
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D409/12 , C07D409/14 , C07D471/14
摘要： The invention relates to the field of blood clotting, to novel compounds of formula (I), to a method for their production and to the use of these compounds as active ingredients in medicaments for preventing and/or treating diseases. The compounds are factor Xa inhibitors.

92. 发明授权

US06743798B1 Substituted pyrazole derivatives condensed with six-membered heterocyclic rings 有权
标题翻译：与六元杂环稠合的取代的吡唑衍生物
公开(公告)号：US06743798B1
公开(公告)日：2004-06-01
申请号：US09744830
申请日：2001-04-11
申请人： Alexander Straub , Achim Feurer , Cristina Alonso-Alija , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky , Elke Stahl
发明人： Alexander Straub , Achim Feurer , Cristina Alonso-Alija , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky , Elke Stahl
IPC分类号： C07D40304
CPC分类号： C07D471/04
摘要： The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.
摘要翻译：本发明涉及通式（I）的新的取代的吡唑衍生物，其中R 1，R 2，R 3和A各自如上所定义，并且其制备方法及其用途药物，特别是用于治疗心血管疾病的药物。

93. 发明授权

US06693102B2 Pyridine-substituted pyrazolopyridine derivatives 失效
标题翻译：吡啶取代的吡唑并吡啶衍生物
公开(公告)号：US06693102B2
公开(公告)日：2004-02-17
申请号：US10001569
申请日：2001-11-01
申请人： Johannes-Peter Stasch , Achim Feurer , Stefan Weigand , Elke Stahl , Dietmar Flubacher , Cristina Alonso-Alija , Frank Wunder , Dieter Lang , Klaus Dembowsky , Alexander Straub , Elisabeth Perzborn
发明人： Johannes-Peter Stasch , Achim Feurer , Stefan Weigand , Elke Stahl , Dietmar Flubacher , Cristina Alonso-Alija , Frank Wunder , Dieter Lang , Klaus Dembowsky , Alexander Straub , Elisabeth Perzborn
IPC分类号： C07D47104
CPC分类号： C07D471/04 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： The present invention relates to new pyrazolopyridine derivatives of the formula (I) in which R1 represents 4-pyridinyl or 3-pyridinyl; R2 represents H, NH2 or halogen; and salts, isomers and hydrates thereof as stimulators of soluble guanylate cyclase and for use as agents for the treatment of cardiovascular disorders, hypertension, of thromboembolic disorders and ischaemia, sexual dysfunction or inflammation, and for the treatment of disorders of the central nervous system.
摘要翻译：本发明涉及式（I）的新的吡唑并吡啶衍生物，其中R 1表示4-吡啶基或3-吡啶基; R 2表示H，NH 2或卤素; 其盐，异构体和水合物作为可溶性鸟苷酸环化酶的刺激剂，并用作治疗心血管疾病，高血压，血栓栓塞障碍和局部缺血，性功能障碍或炎症以及用于治疗中枢神经系统疾病的药剂。

94. 发明授权

US06414009B1 Heterocyclylmethyl-substituted pyrazol derivatives 失效
公开(公告)号：US06414009B1
公开(公告)日：2002-07-02
申请号：US09648082
申请日：2000-08-25
申请人： Alexander Straub , Chantal Fürstner , Ulrich Niewöhner , Thomas Jaetsch , Achim Feurer , Raimund Kast , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky , Dieter Arlt
发明人： Alexander Straub , Chantal Fürstner , Ulrich Niewöhner , Thomas Jaetsch , Achim Feurer , Raimund Kast , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky , Dieter Arlt
IPC分类号： A61K31416
CPC分类号： C07D401/04 , C07D263/32 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
摘要： The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of cardiovascular diseases.

95. 发明授权

US5998448A Combined preparations with vascular effect containing dihydropyridines acetylsalicylic acid nitroesters and vitamins 失效
标题翻译：含有二氢吡啶类乙酰水杨酸硝酸酯和维生素的血管作用的联合制剂
公开(公告)号：US5998448A
公开(公告)日：1999-12-07
申请号：US945516
申请日：1997-10-24
申请人： Eva Lesur , Dieter Neuser , Oswald Lockhoff , Elisabeth Perzborn , Johannes Peter Stasch , Peter Kurka
发明人： Eva Lesur , Dieter Neuser , Oswald Lockhoff , Elisabeth Perzborn , Johannes Peter Stasch , Peter Kurka
IPC分类号： A61K31/355 , A61K31/07 , A61K31/375 , A61K31/44 , A61K31/455 , A61K31/51 , A61K31/525 , A61K31/60 , A61K36/00 , C07D211/80 , A61K31/435
CPC分类号： A61K31/60 , A61K31/621
摘要： The invention relates to new combinations of dihydropyridines of the general formula (I) ##STR1## in which R.sup.1 to R.sup.5 have the meaning indicated in the description, for the prevention and treatment of vascular disorders, in particular of cardiovascular and cerebrovascular disorders, containing dihydropyridines having calcium antagonist activity, acetylsalicylic acid nitroesters and vitamins, and, if appropriate, also further auxiliaries or active compounds.
摘要翻译： PCT No.PCT / EP96 / 01631 Sec。 371 1997年10月24日第 102（e）1997年10月24日PCT PCT 1996年4月19日PCT公布。公开号WO96 / 34607 日期1996年11月7日本发明涉及通式（I）的二氢吡啶的新组合，其中R1至R5具有说明书中所示的含义，用于预防和治疗血管疾病，特别是心血管和脑血管障碍，具有钙拮抗剂活性的二氢吡啶类，乙酰水杨酸硝酸酯和维生素，以及如果合适的话，还可以是其他助剂或活性化合物。

96. 发明授权

US4876255A Substituted 1,4-dihydropyridines for control of circulation and thromboses 失效
标题翻译：用于控制循环和血栓形成的取代的1,4-二氢吡啶
公开(公告)号：US4876255A
公开(公告)日：1989-10-24
申请号：US178710
申请日：1988-04-07
申请人： Gerhard Franckowiak , Ulrich Rosentreter , Elisabeth Perzborn , Friedel Seuter , Michael Kayser , Gunther Thomas
发明人： Gerhard Franckowiak , Ulrich Rosentreter , Elisabeth Perzborn , Friedel Seuter , Michael Kayser , Gunther Thomas
IPC分类号： A61K31/50 , A61K31/505 , A61P7/02 , 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 control of coronary diseases and thromboses there are provided the novel compounds ##STR1## in which R.sup.1 is an optionally substituted phenyl or heterocyclic radical,R.sup.2 is a cyano, keto, carboxy, ester or amide group, andX is from 0 to 6,and physiologically acceptable salts thereof.
摘要翻译：为了控制冠状动脉疾病和血栓形成，提供了新的化合物（I），其中R 1是任选取代的苯基或杂环基，R 2是氰基，酮基，羧基，酯或酰胺基，X是 0至6，及其生理上可接受的盐。

97. 发明授权

US4698344A 1-Heteroaryl-4-aryl-pyrazolin-5-ones for use as medicaments 失效
标题翻译： 1-杂芳基-4-芳基 - 吡唑啉-5-酮，用作药物
公开(公告)号：US4698344A
公开(公告)日：1987-10-06
申请号：US800485
申请日：1985-11-21
申请人： Klaus Sasse , Michael Hammond , Friedel Seuter , Elisabeth Perzborn , Bernhard Pelster , Graham Sturton , Trevor Abram
发明人： Klaus Sasse , Michael Hammond , Friedel Seuter , Elisabeth Perzborn , Bernhard Pelster , Graham Sturton , Trevor Abram
IPC分类号： C07D213/77 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/505 , A61P7/02 , A61P29/00 , A61P37/08 , C07D231/22 , C07D251/46 , C07D317/00 , C07D401/04 , C07D403/04 , C07D405/14 , C12N9/99
CPC分类号： C07D401/04 , C07D403/04 , C07D405/14
摘要： The invention relates to 1-heteroaryl-4-aryl-pyrazolin-5-ones, a preparation process and the use in combating diseases, in particular for use as lipoxygenase inhibitors.
摘要翻译：本发明涉及1-杂芳基-4-芳基 - 吡唑啉-5-酮，其制备方法以及抗疾病特别用作脂氧合酶抑制剂的用途。

98. 发明授权

US4686229A 1,4-dihydropyridines 失效
标题翻译： 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。

99. 发明授权

US4670460A Inhibiting lipoxygenase with pyrazolone derivatives 失效
标题翻译：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-。

100. 发明授权

US07932278B2 2-aminoethoxyacetic acid derivatives and their use 有权
标题翻译： 2-氨基乙氧基乙酸衍生物及其用途
公开(公告)号：US07932278B2
公开(公告)日：2011-04-26
申请号：US11992396
申请日：2006-09-14
申请人： Christian R. Thomas , Susanne Röhrig , Elisabeth Perzborn
发明人： Christian R. Thomas , Susanne Röhrig , Elisabeth Perzborn
IPC分类号： A61K31/422 , A61P7/02 , C07D263/08
CPC分类号： C07D413/12
摘要： The present application relates to novel 2-aminoethoxyacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.
摘要翻译：本申请涉及新的2-氨基乙氧基乙酸衍生物，其制备方法，其用于治疗和/或预防疾病的用途，以及其用于制备用于治疗和/或预防疾病的药物的用途，特别是血栓栓塞性疾病

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