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1. 发明授权

US08618304B2 Acylamino-substituted cyclic carboxylic acid derivatives and their use as pharmaceuticals 有权
标题翻译：酰氨基取代的环状羧酸衍生物及其作为药物的用途
公开(公告)号：US08618304B2
公开(公告)日：2013-12-31
申请号：US13461264
申请日：2012-05-01
申请人： Josef Pernerstorfer , Heinz-Werner Kleemann , Matthias Schaefer , Alena Safarova , Marcel Patek
发明人： Josef Pernerstorfer , Heinz-Werner Kleemann , Matthias Schaefer , Alena Safarova , Marcel Patek
IPC分类号： C07D401/00 , A61K31/44
CPC分类号： C07C235/54 , C07C231/00 , C07C231/02 , C07C235/42 , C07C235/84 , C07C255/50 , C07C255/54 , C07C255/57 , C07C307/10 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/22 , C07C2602/50 , C07D213/16 , C07D213/64 , C07D213/69 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/18 , C07D305/04 , C07D305/06 , C07D305/08 , C07D309/04 , C07D309/08 , C07D309/14 , C07D313/04 , C07D317/06 , C07D317/68 , C07D317/72 , C07D333/16 , C07D333/32 , C07D335/02 , C07D335/14 , C07D335/18 , C07D493/10
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are pharmaceutically active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物，其中A，Y，Z，R 20至R 22和R 50具有权利要求中所述的含义，其为药学活性化合物。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

2. 发明申请

US20050054729A1 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：US20050054729A1
公开(公告)日：2005-03-10
申请号：US10920395
申请日：2004-08-18
申请人： Paulus Wohlfart , Teri Suzuki , Ramalinga Dharanipragada , Alena Safarova , Armin Walser , Hartmut Strobel
发明人： Paulus Wohlfart , Teri Suzuki , Ramalinga Dharanipragada , Alena Safarova , Armin Walser , Hartmut Strobel
IPC分类号： A61K31/00 , A61K31/166 , A61K31/66 , A61P1/16 , A61P5/48 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P15/10 , A61P19/10 , A61P25/28 , A61P27/06 , A61P43/00 , C07C233/65 , A61K31/165
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) 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。

3. 发明授权

US07179839B2 Acylated indanyl amines and their use as pharmaceuticals 有权
标题翻译：酰化茚满胺及其作为药物的用途
公开(公告)号：US07179839B2
公开(公告)日：2007-02-20
申请号：US10073160
申请日：2002-02-13
申请人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schönafinger
发明人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schönafinger
IPC分类号： A61K31/357 , C07D317/46
CPC分类号： C07D213/81 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/76 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C255/57 , C07C255/60 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/16 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D207/34 , C07D213/56 , C07D213/82 , C07D215/48 , C07D235/08 , C07D241/24 , C07D249/04 , C07D261/18 , C07D295/185 , C07D307/78 , C07D307/84 , C07D317/60 , C07D333/24 , C07D401/06
摘要： The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1–R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1–C3-alkyl), B is CH2 or CH—(C1–C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
摘要翻译：本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有说明书中给出的含义，A是CH CH 2或CH-（C 1 -C 3 - 烷基），B是CH 2或CH-（C（C 1 -C 3） C 1 -C 3烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征，心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常，糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药。

4. 发明授权

US06617359B2 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：US06617359B2
公开(公告)日：2003-09-09
申请号：US10073330
申请日：2002-02-13
申请人： Paulus Wohlfart , Teri Suzuki , Ramalinga M. Dharanipragada , Alena Safarova , Armin Walser , Hartmut Strobel
发明人： Paulus Wohlfart , Teri Suzuki , Ramalinga M. Dharanipragada , Alena Safarova , Armin Walser , Hartmut Strobel
IPC分类号： A61K3165
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) 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。

5. 发明授权

US06287794B1 Factor Vlla inhibitors 有权
标题翻译：因子Vlla抑制剂
公开(公告)号：US06287794B1
公开(公告)日：2001-09-11
申请号：US09395572
申请日：1999-09-14
申请人： Pavel Safar , Alena Safarova , Peter Wildgoose
发明人： Pavel Safar , Alena Safarova , Peter Wildgoose
IPC分类号： C12Q156
CPC分类号： C07K5/1019 , A61K38/00 , C07K5/0815 , Y10T436/105831
摘要： The present invention relates to novel compounds and pharmaceutical composition, their preparation, and their use, having a antithrombotic effect through reversible inhibition of activated blood coagulation factor VIIa “FVIIa”.
摘要翻译：本发明涉及通过活化血液凝固因子VIIa“FVIIa”的可逆抑制具有抗血栓形成作用的新化合物和药物组合物，其制备及其应用。

6. 发明授权

US08362073B2 Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals 有权
标题翻译：酰氨基取代的稠环戊烷羧酸衍生物及其作为药物的用途
公开(公告)号：US08362073B2
公开(公告)日：2013-01-29
申请号：US12939650
申请日：2010-11-04
申请人： Matthias Schaefer , Josef Pernerstorfer , Dieter Kadereit , Hartmut Strobel , Werngard Czechtizky , L. Charlie Chen , Alena Safarova , Aleksandra Weichsel , Marcel Patek
发明人： Matthias Schaefer , Josef Pernerstorfer , Dieter Kadereit , Hartmut Strobel , Werngard Czechtizky , L. Charlie Chen , Alena Safarova , Aleksandra Weichsel , Marcel Patek
IPC分类号： A61K31/166 , C07C231/02
CPC分类号： C07C235/54 , A61K31/196 , A61K31/216 , A61K31/277 , A61K31/381 , A61K31/439 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/495 , A61K31/4965 , C07C231/02 , C07C235/62 , C07C235/84 , C07C237/38 , C07C255/54 , C07C255/57 , C07C255/58 , C07C307/10 , C07C309/73 , C07C311/08 , C07C315/04 , C07C317/22 , C07C317/46 , C07C319/12 , C07C319/20 , C07C321/26 , C07C323/12 , C07C323/19 , C07C323/42 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/08 , C07D207/09 , C07D207/263 , C07D209/12 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D221/04 , C07D231/12 , C07D233/54 , C07D233/64 , C07D233/84 , C07D235/12 , C07D235/18 , C07D241/38 , C07D249/06 , C07D261/04 , C07D261/20 , C07D263/32 , C07D271/08 , C07D277/24 , C07D277/56 , C07D285/06 , C07D295/08 , C07D295/20 , C07D305/06 , C07D307/12 , C07D309/06 , C07D319/06 , C07D319/12 , C07D319/20 , C07D333/16 , C07D333/38 , C07D333/56 , C07D333/78 , C07D413/04 , C07D417/04 , C07D453/02 , C07D471/08
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物，其中A，Y，Z，R 3至R 6，R 20至R 22和R 50具有权利要求中所示的含义，它们是有价值的药物活性化合物。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

7. 发明申请

US20110152290A1 ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： ACYLAMINO-取代的氟化环戊烷羧酸衍生物及其作为药物的用途
公开(公告)号：US20110152290A1
公开(公告)日：2011-06-23
申请号：US12939650
申请日：2010-11-04
申请人： Matthias SCHAEFER , Josef PERNERSTORFER , Dieter KADEREIT , Hartmut STROBEL , Werngard CZECHTIZKY , L. Charlie CHEN , Alena SAFAROVA , Aleksandra WEICHSEL , Marcel PATEK
发明人： Matthias SCHAEFER , Josef PERNERSTORFER , Dieter KADEREIT , Hartmut STROBEL , Werngard CZECHTIZKY , L. Charlie CHEN , Alena SAFAROVA , Aleksandra WEICHSEL , Marcel PATEK
IPC分类号： A61K31/495 , C07C69/757 , A61K31/216 , C07C62/14 , A61K31/196 , C07D213/36 , A61K31/4409 , C07D209/12 , A61K31/405 , C07D307/12 , A61K31/341 , C07D211/22 , A61K31/445 , C07D261/04 , A61K31/42 , C07D451/02 , A61K31/46 , C07D241/04 , C07D235/12 , A61K31/4184 , C07D263/32 , A61K31/421 , C07D417/04 , A61K31/426 , C07D285/06 , A61K31/433 , A61P9/00 , A61P29/00 , A61P13/12 , A61P35/00 , A61P19/00 , A61P11/00 , A61P25/00 , A61P17/06
CPC分类号： C07C235/54 , A61K31/196 , A61K31/216 , A61K31/277 , A61K31/381 , A61K31/439 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/495 , A61K31/4965 , C07C231/02 , C07C235/62 , C07C235/84 , C07C237/38 , C07C255/54 , C07C255/57 , C07C255/58 , C07C307/10 , C07C309/73 , C07C311/08 , C07C315/04 , C07C317/22 , C07C317/46 , C07C319/12 , C07C319/20 , C07C321/26 , C07C323/12 , C07C323/19 , C07C323/42 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/08 , C07D207/09 , C07D207/263 , C07D209/12 , C07D209/44 , C07D211/22 , C07D213/30 , C07D213/65 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D221/04 , C07D231/12 , C07D233/54 , C07D233/64 , C07D233/84 , C07D235/12 , C07D235/18 , C07D241/38 , C07D249/06 , C07D261/04 , C07D261/20 , C07D263/32 , C07D271/08 , C07D277/24 , C07D277/56 , C07D285/06 , C07D295/08 , C07D295/20 , C07D305/06 , C07D307/12 , C07D309/06 , C07D319/06 , C07D319/12 , C07D319/20 , C07D333/16 , C07D333/38 , C07D333/56 , C07D333/78 , C07D413/04 , C07D417/04 , C07D453/02 , C07D471/08
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物，其中A，Y，Z，R 3至R 6，R 20至R 22和R 50具有权利要求中所示的含义，它们是有价值的药物活性化合物。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

8. 发明授权

US07713963B2 Acylated indanyl amines and their use as pharmaceuticals 有权
标题翻译：酰化茚满胺及其作为药物的用途
公开(公告)号：US07713963B2
公开(公告)日：2010-05-11
申请号：US11548501
申请日：2006-10-11
申请人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schoenafinger , Ramalinga M. Dharanipragada
发明人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schoenafinger , Ramalinga M. Dharanipragada
IPC分类号： A61K31/541 , A61K31/5377 , C07D417/02 , C07D413/02
CPC分类号： C07D213/81 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/76 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C255/57 , C07C255/60 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/16 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D207/34 , C07D213/56 , C07D213/82 , C07D215/48 , C07D235/08 , C07D241/24 , C07D249/04 , C07D261/18 , C07D295/185 , C07D307/78 , C07D307/84 , C07D317/60 , C07D333/24 , C07D401/06
摘要： The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1—R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
摘要翻译：本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有在描述中给出的含义，A是CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B是CH 2或CH- （C 1 -C 3 - 烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征，心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常，糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药。

9. 发明申请

US20120264790A1 ACYLAMINO-SUBSTITUTED CYCLIC CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： ACYLAMINO取代的环状羧酸衍生物及其作为药物的用途
公开(公告)号：US20120264790A1
公开(公告)日：2012-10-18
申请号：US13461264
申请日：2012-05-01
申请人： Josef PERNERSTORFER , Heinz-Werner KLEEMANN , Matthias SCHAEFER , Alena SAFAROVA , Marcel PATEK
发明人： Josef PERNERSTORFER , Heinz-Werner KLEEMANN , Matthias SCHAEFER , Alena SAFAROVA , Marcel PATEK
IPC分类号： C07C61/40 , C07D231/12 , A61K31/415 , C07D213/82 , A61K31/44 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P7/02 , A61P29/00 , A61P19/02 , A61P13/12 , A61P11/00 , A61P11/06 , A61P37/00 , A61P37/08 , A61P35/04 , A61P3/00 , A61P17/06 , A61P25/00 , A61P17/04 , A61P27/02 , A61P25/18 , A61P25/28 , A61P5/00 , A61P5/16 , A61P17/02 , A61P35/00 , A61K31/196
CPC分类号： C07C235/54 , C07C231/00 , C07C231/02 , C07C235/42 , C07C235/84 , C07C255/50 , C07C255/54 , C07C255/57 , C07C307/10 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/22 , C07C2602/50 , C07D213/16 , C07D213/64 , C07D213/69 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/18 , C07D305/04 , C07D305/06 , C07D305/08 , C07D309/04 , C07D309/08 , C07D309/14 , C07D313/04 , C07D317/06 , C07D317/68 , C07D317/72 , C07D333/16 , C07D333/32 , C07D335/02 , C07D335/14 , C07D335/18 , C07D493/10
摘要： The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物，其中A，Y，Z，R20至R22和R50具有权利要求中所示的含义，它们是有价值的药物活性化合物。具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病梗死和心力衰竭。本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。

10. 发明授权

US08163751B2 Acylated indanyl amines and their use as pharmaceuticals 有权
标题翻译：酰化茚满胺及其作为药物的用途
公开(公告)号：US08163751B2
公开(公告)日：2012-04-24
申请号：US12748951
申请日：2010-03-29
申请人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schönafinger , Ramalinga M. Dharanipragada
发明人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schönafinger , Ramalinga M. Dharanipragada
IPC分类号： A61K31/495 , A61K31/44 , C07D241/36 , C07D513/02
CPC分类号： C07D213/81 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/76 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C255/57 , C07C255/60 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/16 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D207/34 , C07D213/56 , C07D213/82 , C07D215/48 , C07D235/08 , C07D241/24 , C07D249/04 , C07D261/18 , C07D295/185 , C07D307/78 , C07D307/84 , C07D317/60 , C07D333/24 , C07D401/06
摘要： The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
摘要翻译：本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有在描述中给出的含义，A是CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B是CH 2或CH- （C 1 -C 3 - 烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征，心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常，糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药。

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