公开(公告)号：US07696383B2

公开(公告)日：2010-04-13

申请号：US12143919

申请日：2008-06-23

Applicant: Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th. M. Tulp

Inventor： Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th. M. Tulp

IPC: C07C291/04 ,  A61K31/13

CPC classification number: C07C291/04

Abstract: Embodiments of the invention relate to a compound of formula (1), or a tautomer, stereoisomer, hydrate, or solvate thereof, wherein R1 is H or CH3. Other embodiments of the invention relate to a pharmaceutical composition containing these compound, to methods for preparing these compounds, and to methods for preparing compositions containing these compounds. Yet other embodiments of the invention relate to the uses of these compounds and compositions containing it, such as for the manufacture of medicaments and pharmaceutical compositions for treating a condition chosen from depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine and hot flashes.

Abstract translation: 本发明的实施方案涉及式（1）的化合物或其互变异构体，立体异构体，水合物或溶剂合物，其中R 1为H或CH 3。 本发明的其它实施方案涉及含有这些化合物的药物组合物，制备这些化合物的方法以及制备含有这些化合物的组合物的方法。 本发明的其它实施方案涉及这些化合物和含有它们的组合物的用途，例如用于制备用于治疗选自抑郁症，重度抑郁障碍，广泛性焦虑症，强迫症，社会焦虑症的药物和药物组合物 障碍，恐慌症，一般抑郁障碍，糖尿病性神经病，偏头痛和潮热。

公开(公告)号：US20090005455A1

公开(公告)日：2009-01-01

申请号：US12143919

申请日：2008-06-23

Applicant: Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th.M. Tulp

Inventor： Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th.M. Tulp

IPC: A61K31/135 ,  C07C217/74 ,  A61P25/00 ,  C07C215/56

CPC classification number: C07C291/04

Abstract: Embodiments of the invention relate to a compound of formula (1), or a tautomer, stereoisomer, hydrate, or solvate thereof, wherein R1 is H or CH3. Other embodiments of the invention relate to a pharmaceutical composition containing these compound, to methods for preparing these compounds, and to methods for preparing compositions containing these compounds. Yet other embodiments of the invention relate to the uses of these compounds and compositions containing it, such as for the manufacture of medicaments and pharmaceutical compositions for treating a condition chosen from depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine and hot flashes.

Abstract translation: 本发明的实施方案涉及式（1）的化合物或其互变异构体，立体异构体，水合物或溶剂合物，其中R 1为H或CH 3。 本发明的其它实施方案涉及含有这些化合物的药物组合物，制备这些化合物的方法以及制备含有这些化合物的组合物的方法。 本发明的其它实施方案涉及这些化合物和含有它们的组合物的用途，例如用于制备用于治疗选自抑郁症，重度抑郁障碍，广泛性焦虑症，强迫症，社会焦虑症的药物和药物组合物 障碍，恐慌症，一般抑郁障碍，糖尿病性神经病，偏头痛和潮热。

公开(公告)号：US20090005395A1

公开(公告)日：2009-01-01

申请号：US12143915

申请日：2008-06-23

Applicant: Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th.M. Tulp

Inventor： Lechoslaw A. Turski ,  Axel Stoit ,  Cornelis G. Kruse ,  Sander Vader ,  Martinus Th.M. Tulp

IPC: A61K31/519 ,  C07D487/04 ,  A61P15/10 ,  A61P9/12

CPC classification number: C07D487/04

Abstract: Embodiments of the present invention relate to a compound of formula (1A) or a pharmacologically acceptable salt, hydrate, or solvate thereof. Other embodiments of the present invention relate to a pharmaceutical composition containing this compound, to methods for preparing this compound, and to methods for preparing compositions containing this compound. Yet other embodiments of the invention relate to uses of this compound, and compositions containing it, for the manufacture of medicaments and pharmaceutical compositions for treating erectile dysfunction or pulmonary arterial hypertension.

Abstract translation: 本发明的实施方案涉及式（1A）化合物或其药理学上可接受的盐，水合物或溶剂化物。 本发明的其它实施方案涉及含有该化合物的药物组合物，该化合物的制备方法以及含有该化合物的组合物的制备方法。 本发明的其它实施方案涉及该化合物及其含有组合物用于制备用于治疗勃起功能障碍或肺动脉高压的药物和药物组合物的用途。

公开(公告)号：US07232813B2

公开(公告)日：2007-06-19

申请号：US11030043

申请日：2005-01-07

Applicant: Hrissanthi Ikonomidou ,  Lechoslaw A. Turski ,  Dieter Ziegler ,  Michael Weske

Inventor： Hrissanthi Ikonomidou ,  Lechoslaw A. Turski ,  Dieter Ziegler ,  Michael Weske

IPC: A61P25/00

CPC classification number: A61K31/675 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554

Abstract: The invention relates to a novel use of known benzazepine, benzoxazepine, benzo-thiazepine-N-acetic acid and phosphono-substituted benzazepinone derivatives having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity. The compounds of the invention are useful for the preparation of pharmaceutical compositions for prophylaxis and treatment of neurodegenerative disorders.The compounds of the invention are known from the European patents EP 0 733 642 and EP 0 916 679, and can be described by the general formulae (1): wherein the symbols have the meanings as given above in the description.

Abstract translation: 本发明涉及已知的苯并氮杂，苯并氧氮杂，苯并硫氮杂-N-乙酸和具有中性肽链内切酶（NEP）和（或）可溶性内肽酶（hSEP）抑制活性的膦酰取代苯并氮杂酮衍生物的新用途。 本发明的化合物可用于制备用于预防和治疗神经变性疾病的药物组合物。 本发明的化合物可以从欧洲专利EP 0 733 642和EP 0 916 679中得知，并且可以由通式（1）描述：其中符号具有上面在说明书中给出的含义。