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61. 发明授权

US06759420B1 Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them 有权
标题翻译：芳基烷酰基衍生物，其制备方法，其用途和含有它们的药物组合物
公开(公告)号：US06759420B1
公开(公告)日：2004-07-06
申请号：US09472936
申请日：1999-12-28
申请人： Elisabeth Defossa , Uwe Heinelt , Otmar Klingler , Gerhard Zoller , Hans Matter , Fahad A. Al-Obeidi , Armin Walser , Peter Wildgoose
发明人： Elisabeth Defossa , Uwe Heinelt , Otmar Klingler , Gerhard Zoller , Hans Matter , Fahad A. Al-Obeidi , Armin Walser , Peter Wildgoose
IPC分类号： A61K3134
CPC分类号： C07D213/40 , A61K38/00 , C07C257/18 , C07C279/14 , C07C2601/14 , C07D211/26 , C07D213/56 , C07D233/20 , C07D233/74 , C07D271/07 , C07D413/12 , C07K5/0205 , C07K5/06078
摘要： The present invention is directed to new compounds for the inhibition of blood clotting proteins and factor Xa activity, and more particularly, to arylalkanoyl derivatives of the formula (I): wherein R(1), R(2), R(3), R(4), R(5), R(6a), and R(6b) have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula (I) in the treatment and prophylaxis of diseases whcih can be treated or prevented by the inhibition of factor Xa activity, such as cardiovascular or thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases.
摘要翻译：本发明涉及用于抑制凝血蛋白和因子Xa活性的新化合物，更具体地说，涉及式（I）的芳基烷酰基衍生物：其中R（1），R（2），R（3）， R（4），R（5），R（6a）和R（6b）具有权利要求中所示的含义。本发明还涉及制备式（I）化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，涉及使用式（I）化合物治疗和预防疾病的方法可以通过抑制因子Xa活性（例如心血管或血栓栓塞性疾病）以及式（I）化合物在制备用于这些疾病的药物中的用途来治疗或预防。

62. 发明授权

US06500811B2 Sulfonylaminophosphinic and sulfonylaminophosphonic acid derivatives, methods for their preparation and use 有权
标题翻译：磺酰氨基膦酸和磺酰氨基膦酸衍生物，其制备和使用方法
公开(公告)号：US06500811B2
公开(公告)日：2002-12-31
申请号：US09811698
申请日：2001-03-20
申请人： Manfred Schudok , Wilfried Schwab , Gerhard Zoller , Eckart Bartnik , Frank Büttner , Klaus-Ulrich Weithmann
发明人： Manfred Schudok , Wilfried Schwab , Gerhard Zoller , Eckart Bartnik , Frank Büttner , Klaus-Ulrich Weithmann
IPC分类号： C07F938
CPC分类号： C07F9/5728 , C07F9/3808 , C07F9/4006 , C07F9/572
摘要： Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.
摘要翻译：式I化合物适用于生产用于预防和治疗疾病的药物，其中涉及增加基质降解酶的活性。

63. 发明授权

US08470841B2 Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof 有权
标题翻译：杂环化合物，其制备方法，包含这些化合物的药物及其用途
公开(公告)号：US08470841B2
公开(公告)日：2013-06-25
申请号：US13002933
申请日：2009-07-07
申请人： Gerhard Zoller , Dieter Schmoll , Marco Mueller , Guido Haschke , Ingo Focken
发明人： Gerhard Zoller , Dieter Schmoll , Marco Mueller , Guido Haschke , Ingo Focken
IPC分类号： A01N43/40 , A61K31/435
CPC分类号： C07D213/69 , C07D237/16 , C07D319/06 , C07D405/12
摘要： Heterocyclic derivatives, processes for their preparation, medicaments comprising these compounds, and the use thereof. The invention relates to compounds of the formula I in which the radicals R1, R2, R3, R4, W, A, B, D, E, G, L, M, R, T and Y have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example for the treatment of the metabolic syndrome, insulin resistance, obesity and diabetes.
摘要翻译：杂环衍生物，其制备方法，包含这些化合物的药物及其用途。本发明涉及其中基团R 1，R 2，R 3，R 4，W，A，B，D，E，G，L，M，R，T和Y具有所述含义的式I化合物，其生理学耐受的盐。该化合物适用于例如治疗代谢综合征，胰岛素抵抗，肥胖和糖尿病。

64. 发明授权

US08399476B2 Imidazo[1,2-a]pyridines and their use as pharmaceuticals 有权
标题翻译：咪唑并[1,2-a]吡啶及其作为药物的用途
公开(公告)号：US08399476B2
公开(公告)日：2013-03-19
申请号：US12548636
申请日：2009-08-27
申请人： Gerhard Zoller , Hartmut Strobel , David William Will , Paulus Wohlfart
发明人： Gerhard Zoller , Hartmut Strobel , David William Will , Paulus Wohlfart
IPC分类号： A01N43/42 , A61K31/44 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04
摘要： The present invention relates to derivatives of imidazo[1,2-a]pyridines of formula I, in which R, R1 to R4 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的咪唑并[1,2-a]吡啶衍生物，其中R，R 1至R 4和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录和是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下使用。本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及式I化合物用于刺激内皮NO合成酶表达或用于治疗各种疾病，包括心血管疾病例如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全。

65. 发明申请

US20120028986A1 2-HETEROARYL-PYRROLO [3,4-C]PYRROLE DERIVATIVES, AND USE THEREOF AS SCD INHIBITORS 有权
标题翻译： 2-异丙基 - 吡咯并[3,4-C]吡咯烷酮衍生物及其作为SCD抑制剂的用途
公开(公告)号：US20120028986A1
公开(公告)日：2012-02-02
申请号：US13063088
申请日：2009-09-02
申请人： Gerhard Zoller , Marc Dietrich Voss , Hans Matter , Andreas Herling
发明人： Gerhard Zoller , Marc Dietrich Voss , Hans Matter , Andreas Herling
IPC分类号： A61K31/501 , A61K31/4439 , A61P3/06 , A61P9/10 , A61P35/00 , A61P1/04 , A61P29/00 , A61P25/16 , A61P25/28 , A61P17/10 , A61P17/00 , A61P31/20 , A61P3/04 , A61P11/06 , A61P19/02 , A61P19/06 , A61P31/12 , A61P21/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the formula (I), where the groups R1, M, A, B, D, L, and R have the specified meanings, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treating metabolic syndrome, insulin resistance, obesity, and diabetes.
摘要翻译：本发明涉及式（I）化合物，其中基团R 1，M，A，B，D，L和R具有特定含义，以及其生理上相容的盐。该化合物适用于例如治疗代谢综合征，胰岛素抵抗，肥胖症和糖尿病。

66. 发明授权

US08080569B2 Imidazo[2,1-b]thiazoles and their use as pharmaceuticals 有权
标题翻译：咪唑并[2,1-b]噻唑及其作为药物的用途
公开(公告)号：US08080569B2
公开(公告)日：2011-12-20
申请号：US12466576
申请日：2009-05-15
申请人： Gerhard Zoller , Hartmut Strobel , David William Will , Paulus Wohlfart
发明人： Gerhard Zoller , Hartmut Strobel , David William Will , Paulus Wohlfart
IPC分类号： A61K31/429 , C07D513/04
CPC分类号： C07D513/04
摘要： The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的咪唑并[2,1-b]噻唑衍生物，其中R，R 1至R 3和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录和是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于治疗的药物中的用途包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

67. 发明授权

US07772268B2 Diacyl indazole derivatives as lipase and phospholipase inhibitors 有权
标题翻译：二酰基吲唑衍生物作为脂肪酶和磷脂酶抑制剂
公开(公告)号：US07772268B2
公开(公告)日：2010-08-10
申请号：US12099337
申请日：2008-04-08
申请人： Gerhard Zoller , Stefan Petry , Gunter Müller , Hubert Heuer , Norbert Tennagels
发明人： Gerhard Zoller , Stefan Petry , Gunter Müller , Hubert Heuer , Norbert Tennagels
IPC分类号： C07D231/56 , A61K31/416
CPC分类号： C07D231/56 , C07D401/14 , C07D471/04 , C07D495/04
摘要： The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds to treat diabetes mellitus, dyslipidemia and atherosclerotic disorders.
摘要翻译：本发明涉及通式（I）或（II）的二酰基吲唑衍生物及其药学上可接受的盐：其中X，R 1和R 2如本文所定义。本发明还涉及这些化合物用于治疗糖尿病，血脂异常和动脉粥样硬化性疾病的用途。

68. 发明授权

US07718669B2 Triazolopyridine derivatives as inhibitors of lipases and phospholipases 有权
标题翻译：三唑并吡啶衍生物作为脂肪酶和磷脂酶的抑制剂
公开(公告)号：US07718669B2
公开(公告)日：2010-05-18
申请号：US12099922
申请日：2008-04-09
申请人： Stefan Petry , Gerhard Zoller , Günter Müller , Karl-Heinz Baringhaus , Hubert Heuer
发明人： Stefan Petry , Gerhard Zoller , Günter Müller , Karl-Heinz Baringhaus , Hubert Heuer
IPC分类号： A01N43/42 , A61K31/44 , C07D513/02 , C07D515/02
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to triazolopyridine derivatives of general formula (I), which are defined as cited in the description, to their pharmaceutically applicable salts and to their use as medicaments.
摘要翻译：本发明涉及通式（I）的三唑并吡啶衍生物，其定义如本说明书中引用的其药学上可应用的盐及其作为药物的用途。

69. 发明申请

US20090076068A1 IMIDAZOPYRIDIN-2-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES 有权
标题翻译：作为药物和磷脂抑制剂的咪达唑啶-2-酮衍生物
公开(公告)号：US20090076068A1
公开(公告)日：2009-03-19
申请号：US12235053
申请日：2008-09-22
申请人： Gerhard Zoller , Stefan Petry , Markus Follmann , Gunter Muller , Norbert Tennagels
发明人： Gerhard Zoller , Stefan Petry , Markus Follmann , Gunter Muller , Norbert Tennagels
IPC分类号： A61K31/4355 , C07D471/04 , A61K31/437 , A61P3/10 , A61P3/06 , A61P9/10
CPC分类号： C07D471/04
摘要： The present invention relates to imidazopyridin-2-one derivatives of the formula I with the definitions specified in the description, to their pharmaceutically usable salts and to their use as medicaments.
摘要翻译：本发明涉及式I的咪唑并吡啶-2-酮衍生物，其描述中定义的定义，其药学上可用的盐及其作为药物的用途。

70. 发明授权

US06500803B1 Factor VIIa inhibitors 有权
标题翻译：因子VIIa抑制剂
公开(公告)号：US06500803B1
公开(公告)日：2002-12-31
申请号：US09588651
申请日：2000-06-07
申请人： Otmar Klingler , Manfred Schudok , Gerhard Zoller , Uwe Heinelt , Elisabeth Defossa , Hans Matter , Pavel Safar
发明人： Otmar Klingler , Manfred Schudok , Gerhard Zoller , Uwe Heinelt , Elisabeth Defossa , Hans Matter , Pavel Safar
IPC分类号： A61K3805
CPC分类号： C07K5/06086 , A61K38/00
摘要： The present invention relates to compounds of formula I, in which R1, R2, R91, R92, R93, R94, R95, R96, R97, r, s, and t have the meanings indicated in the claims. Compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式Ⅰ化合物，其中R1，R2，R91，R92，R93，R94，R95，R96，R97，r，s和t具有权利要求中所示的含义。式I化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子VIIa的可逆抑制剂，并且通常可以在其中存在不需要的因子VIIa活性的条件下或用于治疗或预防预期因子VIIa的抑制的病症。本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

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