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41. 发明申请

US20110105454A1 SUBSTITUTED OXINDOLE-DERIVATIVES AND THE USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT ILLNESSES 有权
标题翻译：取代的氧化衍生物及其用于治疗依赖于依赖性依赖性的药物
公开(公告)号：US20110105454A1
公开(公告)日：2011-05-05
申请号：US12810561
申请日：2008-12-23
申请人： Wilfried Braje , Astrid Netz , Thorsten Oost , Wolfgang Wernet , Andrea Hager-Wernet , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch
发明人： Wilfried Braje , Astrid Netz , Thorsten Oost , Wolfgang Wernet , Andrea Hager-Wernet , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch
IPC分类号： A61K31/397 , C07D401/14 , A61K31/496 , A61P25/00
CPC分类号： C07D401/14 , C07D209/34 , C07D401/04
摘要： The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.
摘要翻译：本发明涉及式（I）的新型取代羟吲哚衍生物，含有所述衍生物的药物及其用于治疗加压素依赖性疾病的用途。

42. 发明申请

US20110071285A1 LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS 审中-公开
标题翻译：包含聚羟基 - 烷基和聚羟基 - 环烷基基团的低分子丝氨酸蛋白酶抑制剂
公开(公告)号：US20110071285A1
公开(公告)日：2011-03-24
申请号：US12850545
申请日：2010-08-04
申请人： Dieter Herr , Helmut Mack , Werner Seitz , Wilfried Hornberger
发明人： Dieter Herr , Helmut Mack , Werner Seitz , Wilfried Hornberger
IPC分类号： C07H15/26 , C07D277/30 , C07D409/12
CPC分类号： A61K31/155 , C07H7/00 , C07H15/00
摘要： The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or guanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.
摘要翻译：本发明涉及新型脒和喹啉，其生产及其用途及其作为胰蛋白酶型丝氨酸蛋白酶竞争性抑制剂的用途，特别是血栓素和补体蛋白酶CI和C1r。除了使用化合物作为血栓抑制剂，抗凝剂，补体抑制剂和抗炎剂之外，本发明还涉及含有所述化合物作为活性成分的药物组合物。该新型组合物的特征在于具有脒或胍功能的丝氨酸蛋白酶抑制剂与具有两个或多个羟基官能团的烷基基团的连接，其中所述烷基衍生自糖衍生物。因此，几种糖结构成分或来自糖的组分可以彼此连接。所述连接糖衍生物的原理使得能够获得口服活性化合物。

43. 发明申请

US20110071156A1 HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM 有权
公开(公告)号：US20110071156A1
公开(公告)日：2011-03-24
申请号：US12839612
申请日：2010-07-20
申请人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Andrea Hager-Wernet , Liliane Unger , Wilfried Lubisch
发明人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Andrea Hager-Wernet , Liliane Unger , Wilfried Lubisch
IPC分类号： A61K31/501 , C07D417/14 , A61K31/428 , C07D403/14 , A61K31/513 , C07D401/14 , A61K31/4439 , A61K31/497 , A61K31/4725 , A61K31/4709 , A61K31/4184 , A61K31/405 , A61K31/496 , A61P25/00
CPC分类号： C07D401/14 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.

44. 发明申请

US20100298326A1 Carboxamide compounds and their use as calpain inhibitors 有权
公开(公告)号：US20100298326A1
公开(公告)日：2010-11-25
申请号：US11990652
申请日：2007-12-28
申请人： Andreas Kling , Wilfried Hornberger , Helmut Mack , Achim Moeller , Volker Nimmrich , Dietmar Seemann , Wilfried Lubisch
发明人： Andreas Kling , Wilfried Hornberger , Helmut Mack , Achim Moeller , Volker Nimmrich , Dietmar Seemann , Wilfried Lubisch
IPC分类号： A61K31/5377 , C07D401/02 , A61K31/455 , C07D413/14 , C07D401/14 , A61K31/465 , A61P25/16 , A61P13/12 , A61P27/12 , A61P35/00 , A61P31/18
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D491/048 , C07D493/04 , C07D513/04
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a′ and I-A.a″ in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

45. 发明申请

US20070185126A1 Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing Them 有权
标题翻译：杂芳基取代的1,3-二氢吲哚-2-酮衍生物和含有它们的药物
公开(公告)号：US20070185126A1
公开(公告)日：2007-08-09
申请号：US10574211
申请日：2004-09-30
申请人： Wilfried Lubisch , Wilfried Hornberger , Thorsten Oost , Daryl Sauer , Liliane Unger , Wolfgang Wernet , Herve Geneste
发明人： Wilfried Lubisch , Wilfried Hornberger , Thorsten Oost , Daryl Sauer , Liliane Unger , Wolfgang Wernet , Herve Geneste
IPC分类号： A61K31/506 , A61K31/404 , C07D401/14 , C07D409/04 , C07D413/14 , C07D417/14 , A61K31/501 , A61K31/4709
CPC分类号： C07D401/14 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5 R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
摘要翻译：本发明涉及式（I）的新的1,3-二氢吲哚-2-酮（羟吲哚）衍生物，其中A，R 3，R 4，R 4，根据权利要求1定义5,6和7和R 7以及含有它们用于治疗疾病的药物。特别地，新型羟基吲哚衍生物可用于控制和/或预防各种加压素依赖性或催产素依赖性疾病。

46. 发明授权

US06900319B2 Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US06900319B2
公开(公告)日：2005-05-31
申请号：US10100099
申请日：2002-03-19
申请人： Hans-Joachim Boehm , Hans Wolfgang Höffken , Wilfried Hornberger , Stefan Koser , Helmut Mack , Thomas Pfeiffer , Werner Seitz , Thomas Zierke
发明人： Hans-Joachim Boehm , Hans Wolfgang Höffken , Wilfried Hornberger , Stefan Koser , Helmut Mack , Thomas Pfeiffer , Werner Seitz , Thomas Zierke
IPC分类号： A61K31/00 , A61K38/55 , A61P7/02 , C07D205/04 , C07D207/16 , C07D213/53 , C07D213/63 , C07D213/72 , C07D213/78 , C07D213/79 , C07D239/28 , C07D241/14 , C07D241/24 , C07D401/12 , C07K5/06 , C07K5/062 , C07K5/078 , C07D403/12
CPC分类号： C07D213/78 , C07D205/04 , C07D207/16 , C07D239/28 , C07D241/24 , C07D401/12 , C07K5/06165
摘要： The invention relates to a compound of the formula I: or a salt thereof with a physiologically tolerated acid, or stereoisomers thereof, wherein R1, R2, A, B, C and D have the meanings described in the specification.
摘要翻译：本发明涉及式I化合物或其盐与生理上耐受的酸或其立体异构体，其中R 1，R 2，A，B， C和D具有说明书中描述的含义。

47. 发明授权

US06444817B1 Thrombin inhibitors 有权
标题翻译：凝血酶抑制剂
公开(公告)号：US06444817B1
公开(公告)日：2002-09-03
申请号：US09414681
申请日：1999-10-08
申请人： Hans-Joachim Böhm , Hans Wolfgang Höffken , Wilfried Hornberger , Stefan Koser , Helmut Mack , Thomas Pfeiffer , Werner Seitz , Thomas Zierke
发明人： Hans-Joachim Böhm , Hans Wolfgang Höffken , Wilfried Hornberger , Stefan Koser , Helmut Mack , Thomas Pfeiffer , Werner Seitz , Thomas Zierke
IPC分类号： C07D23942
CPC分类号： C07D213/78 , C07D205/04 , C07D207/16 , C07D239/28 , C07D241/24 , C07D401/12 , C07K5/06165
摘要： Compounds of the formula where A, B, D, R1 and R2 have the meanings stated in the description, are described. The compounds are suitable for controlling diseases. The novel compounds are prepared via compounds of the formula H2N—CH2—G—M.
摘要翻译： A，B，D，R1和R2的化合物具有描述中所述的含义。该化合物适用于控制疾病。新化合物通过式H2N-CH2-G-M的化合物制备。

48. 发明授权

US09090592B2 Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors 有权
标题翻译：杂环化合物及其作为糖原合酶激酶-3抑制剂的用途
公开(公告)号：US09090592B2
公开(公告)日：2015-07-28
申请号：US13339884
申请日：2011-12-29
申请人： Sean Colm Turner , Helmut Mack , Margaretha Henrica Maria Bakker , Marcel Van Gaalen , Carolin Hoft , Wilfried Hornberger
发明人： Sean Colm Turner , Helmut Mack , Margaretha Henrica Maria Bakker , Marcel Van Gaalen , Carolin Hoft , Wilfried Hornberger
IPC分类号： C07D215/46 , C07D405/14 , C07D401/12 , C07D401/14
CPC分类号： C07D471/04 , A61P25/16 , A61P25/28 , C07D215/46 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention relates to novel heterocyclic compounds of formula I wherein the variables are as defined in the claims or the description, which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3β, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3β activity using the compounds.
摘要翻译：本发明涉及式I的新型杂环化合物，其中变量如权利要求或描述中所定义，其可用于抑制糖原合酶激酶3（GSK-3），含有该化合物的组合物，其用于制备药物的用途用于治疗易于用调节，优选抑制糖原合酶激酶3和bgr的活性的化合物治疗的医学疾病;以及治疗易于用调节糖原合酶激酶3和bgr的化合物治疗的医学病症的方法; 使用化合物的活性。

49. 发明授权

US08350055B2 Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them 有权
公开(公告)号：US08350055B2
公开(公告)日：2013-01-08
申请号：US12839612
申请日：2010-07-20
申请人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Andrea Hager-Wernet, legal representative , Liliane Unger , Wilfried Lubisch
发明人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Liliane Unger , Wilfried Lubisch
IPC分类号： C07D411/00
CPC分类号： C07D401/14 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.

50. 发明授权

US08129389B2 Substituted oxindole derivatives, medicaments containing the latter and use thereof 有权
标题翻译：取代的羟基吲哚衍生物，含有后者的药物及其用途
公开(公告)号：US08129389B2
公开(公告)日：2012-03-06
申请号：US11886729
申请日：2006-03-23
申请人： Wilfried Lubisch , Thorsten Oost , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Hervé Geneste
发明人： Wilfried Lubisch , Thorsten Oost , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Hervé Geneste
IPC分类号： A61K31/496 , A61K31/506 , C07D401/12 , C07D403/12 , C07D417/12
CPC分类号： C07D403/12 , C07D401/12 , C07D417/12
摘要： The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
摘要翻译：本发明涉及通式（I）的新型羟基吲哚衍生物，其中取代基A，B，R 1，R 2和R 3如权利要求1中所定义，含有所述衍生物的药物及其用于预防的药物和/或加压素依赖性和/或催产素依赖性疾病的治疗。

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