公开(公告)号：US20110263667A1

公开(公告)日：2011-10-27

申请号：US13125443

申请日：2009-10-21

Applicant: Stefan Abele ,  Stéphanie Combes ,  Jacques-Alexis Funel ,  Kurt Hilpert ,  Francis Hubler ,  Katharina Reichenbaecher ,  Dorte Renneberg ,  Markus Von Raumer

Inventor： Stefan Abele ,  Stéphanie Combes ,  Jacques-Alexis Funel ,  Kurt Hilpert ,  Francis Hubler ,  Katharina Reichenbaecher ,  Dorte Renneberg ,  Markus Von Raumer

IPC: A61K31/4184 ,  A61P9/10 ,  A61P9/00 ,  A61P9/06 ,  C07D235/14 ,  A61P9/12

CPC classification number: C07D235/14

Abstract: The invention relates to crystalline salts of isobutyric acid (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimethoxy-1H-benzoimidazol-2-yl)-propyl]-methyl-amino}-ethyl)-5-phenyl-bicyclo[2.2.2]oct-5-en-2-yl ester, processes for the preparation thereof, pharmaceutical compositions containing said crystalline salts, and their use as medicaments, especially as calcium channel blockers.

Abstract translation: 本发明涉及异丁酸（1R *，2R *，4R *）-2-（2 - {[3-（4,7-二甲氧基-1H-苯并咪唑-2-基） - 丙基] - 甲基 - 氨基} - 乙基）-5-苯基 - 双环[2.2.2]辛-5-烯-2-基酯，其制备方法，含有所述结晶盐的药物组合物及其作为药物的用途，特别是钙通道 阻滞剂

公开(公告)号：US08044055B2

公开(公告)日：2011-10-25

申请号：US12447039

申请日：2007-10-24

Applicant: Eva Caroff ,  Kurt Hilpert ,  Emmanuel Meyer

Inventor： Eva Caroff ,  Kurt Hilpert ,  Emmanuel Meyer

IPC: C07D239/34 ,  A61K31/506

CPC classification number: C07D409/12 ,  C07D239/34 ,  C07D401/12 ,  C07D405/12

Abstract: The invention relates to 2-phenyl-6-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. Formula (I).

Abstract translation: 本发明涉及2-苯基-6-氨基羰基 - 嘧啶衍生物及其作为P2Y12受体拮抗剂用于治疗和/或预防和/或治疗心脏和血管内脏，肝和肾血管的心血管和 脑血管疾病或与血小板聚集相关的病症，包括人类和其他哺乳动物的血栓形成。 式（I）。

公开(公告)号：US20110046089A1

公开(公告)日：2011-02-24

申请号：US12936661

申请日：2009-04-09

Applicant: Eva Caroff ,  Kurt Hilpert ,  Francis Hubler ,  Emmanuel Meyer ,  Dorte Renneberg

Inventor： Eva Caroff ,  Kurt Hilpert ,  Francis Hubler ,  Emmanuel Meyer ,  Dorte Renneberg

IPC: A61K31/675 ,  C07F9/6509 ,  A61P9/00

CPC classification number: C07F9/65583

Abstract: The present invention relates to compounds of formula I wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.

Abstract translation: 本发明涉及式I化合物，其中R 1，R 2，R 4，R 5，R a，R b，n，W和Z如本申请中所定义，其制备及其作为P2Y12受体拮抗剂在治疗和/或预防中的用途 的外周血管，内脏，肝和肾血管的心血管和脑血管疾病或与血小板聚集相关的病症，包括人和其他哺乳动物的血栓形成。

公开(公告)号：US20100261678A1

公开(公告)日：2010-10-14

申请号：US12745358

申请日：2008-11-28

Applicant: Eva Caroff ,  Kurt Hilpert ,  Francis Hubler ,  Emmanuel Meyer ,  Dorte Renneberg

Inventor： Eva Caroff ,  Kurt Hilpert ,  Francis Hubler ,  Emmanuel Meyer ,  Dorte Renneberg

IPC: A61K31/675 ,  C07F9/6512 ,  A61P9/00

CPC classification number: C07F9/65583 ,  C07F9/657181 ,  C07F9/65846

Abstract: The invention relates to 2-phenyl-pyrimidine derivatives containing a phosphonic acid motif and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. (I).

Abstract translation: 本发明涉及含有膦酸基序的2-苯基 - 嘧啶衍生物及其作为P2Y12受体拮抗剂用于治疗和/或预防心血管和脑血管疾病的内脏，肝和肾血管的外周血管的用途 或与血小板聚集相关的病症，包括人类和其他哺乳动物的血栓形成。 （一世）。

公开(公告)号：US20100130545A1

公开(公告)日：2010-05-27

申请号：US12597817

申请日：2008-04-25

Applicant: Kurt Hilpert ,  Francis Hubler ,  Dorte Renneberg

Inventor： Kurt Hilpert ,  Francis Hubler ,  Dorte Renneberg

IPC: A61K31/47 ,  A61K31/44 ,  A61K31/4184 ,  A61K31/417 ,  A61K31/343 ,  A61K31/135 ,  A61K31/165 ,  C07D217/12 ,  C07D215/14 ,  C07D215/12 ,  C07D401/12 ,  C07D213/24 ,  C07D235/06 ,  C07D233/61 ,  C07D307/78 ,  C07C229/00 ,  C07C231/02 ,  C07C209/60

CPC classification number: C07D235/14 ,  C07C215/42 ,  C07C217/62 ,  C07C219/24 ,  C07C233/34 ,  C07C235/10 ,  C07D213/36 ,  C07D215/12 ,  C07D217/14 ,  C07D233/64 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/06 ,  C07D491/04

Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 1a，R 2a，R 3，R 4，A，B，X，W和n如说明书中所定义。 这些化合物可用作钙通道阻滞剂。

公开(公告)号：US20070123510A1

公开(公告)日：2007-05-31

申请号：US10570517

申请日：2004-09-03

Applicant: Volker Breu ,  Anja Fecher ,  Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Valdenaire

Inventor： Volker Breu ,  Anja Fecher ,  Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Valdenaire

IPC: A61K31/55 ,  A61K31/519 ,  A61K31/517 ,  C07D498/02 ,  C07D491/02 ,  C07D487/02

CPC classification number: C07D239/84 ,  A61K31/517 ,  C07D239/70

Abstract: The invention relates to the guanine derivatives of general formula (I), and to hydrates or solvents thereof, for use as neuropeptide FF receptor antagonists in the treatment of pains and hyperalgesia, of withdrawal symptoms of addiction to alcohol, psychotropic drugs or nicotine and in the prevention of or recovery from these addictions, for the regulation of insulin release, food intake, memory functions, blood pressure, electrolyte and energy metabolism, and in the treatment of urinary incontinence.

Abstract translation: 本发明涉及通式（I）的鸟嘌呤衍生物及其水合物或溶剂，用作治疗痛苦和痛觉过敏的神经肽FF受体拮抗剂，对酒精，精神药物或尼古丁成瘾的戒断症状以及 预防或恢复这些成瘾，调节胰岛素释放，食物摄取，记忆功能，血压，电解质和能量代谢以及治疗尿失禁。

公开(公告)号：US20070037846A1

公开(公告)日：2007-02-15

申请号：US10562623

申请日：2004-06-16

Applicant: Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Houille ,  Markus Riederer ,  Oliver Valdenaire

Inventor： Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Houille ,  Markus Riederer ,  Oliver Valdenaire

IPC: A61K31/4152 ,  A61K31/4709 ,  A61K31/416

CPC classification number: A61K31/4152 ,  A61K31/416 ,  A61K31/4709

Abstract: The present invention relates to compounds of alkylidene pyrazolidinedione derivatives, which are effective platelet ADP receptor antagonists that prevent platelet aggregation and thrombosis. Thus, the present invention also relates to pharmaceutical compositions that contain the compounds as well as methods of preventing or treating peripheral, visceral, hepatic, renal, cardio- and cerebro-vascular diseases and conditions that are associated with platelet aggregation, including thrombosis, in humans and other mammals. The present invention further provides a process for manufacturing the alkylidene pyrazolidinedione derivatives.

Abstract translation: 本发明涉及亚烷基吡唑烷二酮衍生物的化合物，其是有效的血小板聚集和血栓形成的血小板ADP受体拮抗剂。 因此，本发明还涉及含有化合物的药物组合物以及预防或治疗外周，内脏，肝，肾，心脑血管疾病和与血小板聚集相关的病症的方法，包括血栓形成 人类和其他哺乳动物。 本发明还提供了制备亚烷基吡唑烷二酮衍生物的方法。

公开(公告)号：US07071212B2

公开(公告)日：2006-07-04

申请号：US10639030

申请日：2003-08-12

Applicant: Jean Ackermann ,  Leo Alig ,  Alexander Chucholowski ,  Katrin Groebke ,  Kurt Hilpert ,  Holger Kuehne ,  Ulrike Obst ,  Lutz Weber ,  Hans Peter Wessel

Inventor： Jean Ackermann ,  Leo Alig ,  Alexander Chucholowski ,  Katrin Groebke ,  Kurt Hilpert ,  Holger Kuehne ,  Ulrike Obst ,  Lutz Weber ,  Hans Peter Wessel

IPC: A61K31/445 ,  C07D265/30

CPC classification number: C07D207/27 ,  C07C257/18 ,  C07C259/18 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/12 ,  C07D209/48 ,  C07D211/46 ,  C07D211/58 ,  C07D211/96 ,  C07D213/30 ,  C07D213/55 ,  C07D213/65 ,  C07D213/74 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D235/18 ,  C07D249/08 ,  C07D261/04 ,  C07D271/06 ,  C07D277/24 ,  C07D295/155 ,  C07D307/12 ,  C07D307/20 ,  C07D307/54 ,  C07D309/12 ,  C07D309/14 ,  C07D317/64 ,  C07D319/18 ,  C07D321/10 ,  C07D333/24 ,  C07D335/04 ,  C07D403/12

Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.

Abstract translation: 本发明涉及下式的新型N-（4-甲脒基 - 苯基） - 甘氨酸衍生物：其中R 1，E，X 1至X 4 本说明书和权利要求书中所定义的，以及其水合物或溶剂合物及其生理上可用的盐。

公开(公告)号：US06320054B1

公开(公告)日：2001-11-20

申请号：US09526033

申请日：2000-03-15

Applicant: Leo Alig ,  Albrecht Edenhofer ,  Kurt Hilpert ,  Thomas Weller

Inventor： Leo Alig ,  Albrecht Edenhofer ,  Kurt Hilpert ,  Thomas Weller

IPC: C07D27720

CPC classification number: C07D417/12 ,  A61K38/00 ,  C07D277/48 ,  C07D277/56 ,  C07K5/1024

Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.

Abstract translation: 下式的化合物及其可药用的盐和酯，其中R1，R2和R3具有本文所述的含义，抑制粘合蛋白与不同类型细胞表面的结合，从而影响细胞和细胞基质 互动 这些化合物可以以药物制剂的形式用于控制或预防肿瘤，肿瘤转移，肿瘤生长，骨质疏松症，佩吉特氏病，糖尿病性视网膜病变，黄斑变性，血管干预后的再狭窄，牛皮癣，关节炎，纤维化，肾衰竭， 以及由病毒，细菌或真菌引起的感染。

公开(公告)号：US06297266B1

公开(公告)日：2001-10-02

申请号：US09420387

申请日：1999-10-19

Applicant: Leo Alig ,  Kurt Hilpert ,  Thomas Weller

Inventor： Leo Alig ,  Kurt Hilpert ,  Thomas Weller

IPC: C07D27748

CPC classification number: C07D277/48

Abstract: Compounds of formula (I) as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance described in the specification, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations in the control or prevention of neoplasms, tumor metastasizing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure as well as infections caused by viruses, bacteria or fungi.

Abstract translation: 式（I）化合物及其药学上可接受的盐和酯，其中R1，R2和R3具有说明书中描述的含义，抑制粘附蛋白与不同类型细胞表面的结合，从而影响细胞 和细胞 - 基质相互作用。 它们可以以药物制剂的形式用于控制或预防肿瘤，肿瘤转移，肿瘤生长，骨质疏松症，佩吉特氏病，糖尿病性视网膜病变，黄斑变性，血管干预后的再狭窄，牛皮癣，关节炎，纤维化，肾衰竭以及 作为病毒，细菌或真菌引起的感染。