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1. 发明申请

US20040198732A1 Aminoalkyl-substituted aromatic bicyclic compounds, methods for their preparation and their use as pharmaceuticals 审中-公开
公开(公告)号：US20040198732A1
公开(公告)日：2004-10-07
申请号：US10820736
申请日：2004-04-09
申请人： Aventis Pharma Deutschland GmbH
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Armin Walser , Gerard Rosse
IPC分类号： A61K031/53 , A61K031/497 , A61K031/4439 , C07D43/14
CPC分类号： C07D235/06 , C07D209/08 , C07D235/08 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/12
摘要： The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1 which are valuable pharmaceutically active compounds that are suitable, for example, for the treatment of obesity, type II diabetes, arteriosclerosis, high blood pressure, paresthesia, depression, anxiety, anxiety neuroses, schizophrenia, disorders associated with the circadian rhythm, and drug abuse, as well as normalizing lipid metabolism.

2. 发明申请

US20040132752A1 Substituted diaryl heterocycles, process for their preparation and their use as medicaments 有权
标题翻译：取代的二芳基杂环，其制备方法及其作为药物的用途
公开(公告)号：US20040132752A1
公开(公告)日：2004-07-08
申请号：US10626314
申请日：2003-07-24
申请人： Aventis Pharma Deutschland GmbH
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Thomas Boehme , Gerhard Hessler , Gerard Rosse , Armin Walser
IPC分类号： A61K031/513 , A61K031/4164
CPC分类号： C07D233/92 , C07D209/02 , C07D233/32 , C07D233/70 , C07D233/74 , C07D233/94 , C07D243/04 , C07D249/12 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D487/08 , C07D491/10
摘要： This invention discloses and claims diary heterocycles of formula (I) 1 and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using said compounds of formula (I) for the treatment or prevention of excessive weight or obesity, and for treatment of Type II diabetes, arteriosclerosis, high blood pressure, depression, anxiety, anxiety neuroses, and schizophrenia. Methods for treatment of excessive weight or obesity and for treatment of Type II diabetes with a mixture of a compound of formula I and antiobesity agents or appetite-regulating active ingredients, or with a mixture of a compound of formula I and antidiabetics or hypoglycemic active ingredients are also disclosed and claimed.
摘要翻译：本发明公开并要求式（I）的日记杂环及其药学上可接受的盐，其药物组合物，以及使用式（I）化合物治疗或预防过度体重或肥胖以及用于治疗II型糖尿病，动脉硬化，高血压，抑郁，焦虑，焦虑神经症和精神分裂症。用于治疗过度体重或肥胖以及用式I化合物与抗肥胖剂或食欲调节活性成分的混合物或与式I化合物与抗糖尿病药或降血糖活性成分的混合物治疗II型糖尿病的方法也被公开和要求保护。

3. 发明申请

US20040198733A1 Aminoalkyl-substituted aromatic bicyclic compounds, methods for their preparation and their use as pharmaceuticals 审中-公开
公开(公告)号：US20040198733A1
公开(公告)日：2004-10-07
申请号：US10820883
申请日：2004-04-09
申请人： Aventis Pharma Deutschland GmbH
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Armin Walser , Gerard Rosse
IPC分类号： A61K031/53 , A61K031/497 , A61K031/4439 , C07D43/14
CPC分类号： C07D235/06 , C07D209/08 , C07D235/08 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/12
摘要： The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1 which are valuable pharmaceutically active compounds that are suitable, for example, for the treatment of obesity, type II diabetes, arteriosclerosis, high blood pressure, paresthesia, depression, anxiety, anxiety neuroses, schizophrenia, disorders associated with the circadian rhythm, and drug abuse, as well as normalizing lipid metabolism.

4. 发明申请

US20040192693A1 Aminoalkyl-substituted aromatic bicyclic compounds, methods for their preparation and their use as pharmaceuticals 审中-公开
公开(公告)号：US20040192693A1
公开(公告)日：2004-09-30
申请号：US10820706
申请日：2004-04-09
申请人： Aventis Pharma Deutschland GmbH
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Armin Walser , Gerard Rosse
IPC分类号： A61K031/53 , A61K031/497 , A61K031/4439 , C07D43/14
CPC分类号： C07D235/06 , C07D209/08 , C07D235/08 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/12
摘要： The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1 which are valuable pharmaceutically active compounds that are suitable, for example, for the treatment of obesity, type II diabetes, arteriosclerosis, high blood pressure, paresthesia, depression, anxiety, anxiety neuroses, schizophrenia, disorders associated with the circadian rhythm, and drug abuse, as well as normalizing lipid metabolism.

5. 发明申请

US20040019114A1 4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
标题翻译： 4-氟-N-茚满-2-基苯甲酰胺及其作为药物的用途
公开(公告)号：US20040019114A1
公开(公告)日：2004-01-29
申请号：US10623775
申请日：2003-07-22
申请人： Aventis Pharma Deutschland GmbH
发明人： Paulus Wohlfart , Teri Suzuki , Ramalinga M. Dharanipragada , Alena Safarova , Armin Walser , Hartmut Strobel
IPC分类号： A61K031/165
CPC分类号： C07C233/65 , A61K31/166 , C07C2602/08
摘要： The present invention relates to the method of stimulating the expression of endothelial NO-synthase in a mammal, which method comprises administering a physiologically active amount of 4-fluoro-N-indan-2-yl benzamide according to the formula (I) 1 to the said mammal. The compound (I) can be used for the therapy and prophylaxis of cardiovascular diseases like stable and unstable angina pectoris, Prinzmetal angina (spasm), acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease PAOD, atherosclerosis, restenosis, endothelial damage after PTCA, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, and the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives, the therapy and prophylaxis of diabetes and diabetes complications (nephropathy, retinopathy), angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, restricted memory performance or a restricted ability to learn.
摘要翻译：本发明涉及刺激哺乳动物内皮细胞NO合成酶表达的方法，该方法包括将生理活性量的式（I）的4-氟-N-茚满-2-基苯甲酰胺给予哺乳动物说化合物（I）可用于治疗和预防心血管疾病如稳定和不稳定型心绞痛，Prinzmetal心绞痛（痉挛），急性冠状动脉综合征，心力衰竭，心肌梗死，中风，血栓形成，外周动脉闭塞性疾病PAOD，动脉粥样硬化，PTCA后再狭窄，内皮损伤，原发性高血压，肺动脉高压，继发性高血压，肾血管性慢性肾小球肾炎，勃起功能障碍，室性心律失常，绝经后妇女心血管危险降低或避孕药物摄入后，糖尿病和糖尿病的治疗和预防并发症（肾病，视网膜病变），血管生成，哮喘支气管炎，慢性肾功能衰竭，肝硬化，限制性记忆能力或受限的学习能力。

6. 发明申请

US20040198731A1 Aminoalkyl-substituted aromatic bicyclic compounds, methods for their preparation and their use as pharmaceuticals 审中-公开
标题翻译：氨基烷基取代的芳族双环化合物，其制备方法及其作为药物的用途
公开(公告)号：US20040198731A1
公开(公告)日：2004-10-07
申请号：US10820703
申请日：2004-04-09
申请人： Aventis Pharma Deutschland GmbH
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Armin Walser , Gerard Rosse
IPC分类号： A61K031/501 , A61K031/53 , A61K031/496 , A61K031/4439 , C07D43/14
CPC分类号： C07D235/06 , C07D209/08 , C07D235/08 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/12
摘要： The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1 which are valuable pharmaceutically active compounds that are suitable, for example, for the treatment of obesity, type II diabetes, arteriosclerosis, high blood pressure, paresthesia, depression, anxiety, anxiety neuroses, schizophrenia, disorders associated with the circadian rhythm, and drug abuse, as well as normalizing lipid metabolism.
摘要翻译：本发明涉及式I的氨基烷基取代的芳族二环化合物，其是有价值的药学活性化合物，其适用于例如治疗肥胖，II型糖尿病，动脉硬化，高血压，感觉异常，抑郁，焦虑，焦虑神经元，精神分裂症，与昼夜节律相关的疾病，药物滥用以及脂质代谢正常化。

7. 发明申请

US20030162967A1 Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them 有权
标题翻译：新型N-胍基烷基酰胺，其制备方法，用途及包含它们的药物制剂
公开(公告)号：US20030162967A1
公开(公告)日：2003-08-28
申请号：US10227222
申请日：2002-08-26
申请人： Aventis Pharma Deutschland GmbH
发明人： Otmar Klingler , Gerhard Zoller , Elisabeth Defossa , Fahad A. Al-Obeidi , Armin Walser , James Ostrem
IPC分类号： C07D417/02 , C07D413/02 , C07D43/02 , C07C237/38
CPC分类号： C07D213/30 , C07C279/14 , C07D213/40 , C07D215/48 , C07D239/28
摘要： The present invention relates to compounds of the formula I, 1 in which A, L, Y, and k have the meanings indicated in the specification and claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and/or factor VIIa and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula 1, 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A，L，Y和k具有说明书和权利要求书中所示的含义。式I的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心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子Xa和/或因子VIIa的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望的活性的条件或用于治愈或预防其中旨在抑制因子Xa和/或因子VIIa。本发明还涉及制备式1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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