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1. 发明申请

US20100183712A1 ACYLATED INDANYL AMINES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： ACYLATED INDANL AMINES及其作为药物的用途
公开(公告)号：US20100183712A1
公开(公告)日：2010-07-22
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： A61K9/48 , A61K9/36 , A61P9/00 , A61P9/04 , C07C233/01 , A61K31/165 , C07D241/38 , A61K31/498 , C07D471/02 , A61K31/437
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。

2. 发明申请

US20070082897A1 ACYLATED INDANYL AMINES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： ACYLATED INDANL AMINES及其作为药物的用途
公开(公告)号：US20070082897A1
公开(公告)日：2007-04-12
申请号：US11548501
申请日：2006-10-11
申请人： Hartmut STROBEL , Paulus WOHLFART , Alena SAFAROVA , Armin WALSER , Teri SUZUKI , Karl SCHONAFINGER , Ramalinga DHARANIPRAGADA
发明人： Hartmut STROBEL , Paulus WOHLFART , Alena SAFAROVA , Armin WALSER , Teri SUZUKI , Karl SCHONAFINGER , Ramalinga DHARANIPRAGADA
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/517 , A61K31/498 , A61K31/497 , A61K31/4709 , A61K31/428 , A61K31/423 , 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。

3. 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。

4. 发明申请

US20100113412A1 IMIDAZO[1,2-a]PYRIDINES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译：咪唑并[1,2-a]吡啶并用作药物
公开(公告)号：US20100113412A1
公开(公告)日：2010-05-06
申请号：US12548636
申请日：2009-08-27
申请人： Gerhard ZOLLER , Hartmut STROBEL , David William WILL , Paulus WOHLFART
发明人： Gerhard ZOLLER , Hartmut STROBEL , David William WILL , Paulus WOHLFART
IPC分类号： A61K31/437 , A61K31/397 , A61P3/10 , A61P9/00 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to derivatives of imidazo[1,2-a]pyridines of formula I, in which R, R1 to R4 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的咪唑并[1,2-a]吡啶衍生物，其中R，R 1至R 4和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录和是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下使用。本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及式I化合物用于刺激内皮NO合成酶表达或用于治疗各种疾病，包括心血管疾病例如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全。

5. 发明申请

US20100137321A1 IMIDAZO[1,2-a]AZINES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译：咪唑并[1,2-a]三嗪及其作为药物的用途
公开(公告)号：US20100137321A1
公开(公告)日：2010-06-03
申请号：US12548641
申请日：2009-08-27
申请人： Gerhard ZOLLER , Hartmut STROBEL , David William WILL , Paulus WOHLFART
发明人： Gerhard ZOLLER , Hartmut STROBEL , David William WILL , Paulus WOHLFART
IPC分类号： A61K31/5025 , A61K31/519 , C07D487/04 , A61P11/06 , A61P9/04 , A61P9/00 , A61P9/10 , A61P3/10
CPC分类号： C07D487/04 , A61K31/4188 , A61K31/4985 , A61K31/5025 , A61K31/519
摘要： The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的咪唑并[1,2-a]吖嗪衍生物，其中R，R 1至R 3，X，Y和n具有权利要求中所示的含义，其调节内皮一氧化氮的转录（ NO）合酶，是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下使用。本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及式I化合物用于刺激内皮NO合成酶表达或用于治疗各种疾病，包括心血管疾病例如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全。

6. 发明申请

US20100004299A1 Imidazo[2,1-b]thiazoles and their use as pharmaceuticals 有权
标题翻译：咪唑并[2,1-b]噻唑及其作为药物的用途
公开(公告)号：US20100004299A1
公开(公告)日：2010-01-07
申请号：US12466576
申请日：2009-05-15
申请人： Gerhard ZOLLER , Hartmut STROBEL , David William WILL , Paulus WOHLFART
发明人： Gerhard ZOLLER , Hartmut STROBEL , David William WILL , Paulus WOHLFART
IPC分类号： A61K31/429 , C07D513/04 , A61P9/10
CPC分类号： C07D513/04
摘要： The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的咪唑并[2,1-b]噻唑衍生物，其中R，R 1至R 3和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录和是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下使用。本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于治疗的药物中的用途包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

7. 发明申请

US20100016337A1 HETEROARYL-SUBSTITUTED CARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译：异氟醚取代的羧酰胺及其作为药物的用途
公开(公告)号：US20100016337A1
公开(公告)日：2010-01-21
申请号：US12486144
申请日：2009-06-17
申请人： Hartmut STROBEL , Paulus WOHLFART , Heinz-Werner KLEEMANN , Gerhard ZOLLER , David William WILL
发明人： Hartmut STROBEL , Paulus WOHLFART , Heinz-Werner KLEEMANN , Gerhard ZOLLER , David William WILL
IPC分类号： A61K31/505 , C07D401/12 , A61K31/4545 , C07D401/06
CPC分类号： C07D409/06 , C07D213/56 , C07D213/65 , C07D213/74 , C07D213/89 , C07D239/26 , C07D271/113 , C07D277/36 , C07D277/46 , C07D285/135 , C07D333/24 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12
摘要： The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的杂芳基取代的甲酰胺，其中Het，A，X，R 1，R 2和R 3具有权利要求所述的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

8. 发明申请

US20100016278A1 HETEROARYLCYCLOPROPANECARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译：异环戊二烯氧化酶及其作为药物的用途
公开(公告)号：US20100016278A1
公开(公告)日：2010-01-21
申请号：US12486118
申请日：2009-06-17
申请人： Hartmut STROBEL , Paulus WOHLFART , Gerhard ZOLLER , David William WILL
发明人： Hartmut STROBEL , Paulus WOHLFART , Gerhard ZOLLER , David William WILL
IPC分类号： A61K31/4418 , C07D211/70 , C07D413/12 , A61K31/5377 , A61K31/397 , A61P9/00 , A61P3/00 , A61P19/00 , A61P25/00
CPC分类号： C07D213/56 , C07D271/113 , C07D333/24 , C07D401/12 , C07D413/12 , C07D417/12 , C07D487/08
摘要： The present invention relates to heteroarylcyclopropanecarboxamides of the formula I, in which Het, X, Ra, Rb, Rc, Rd, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的杂芳基环丙烷甲酰胺，其中Het，X，Ra，Rb，Rc，Rd，R1，R2和R3具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

9. 发明申请

US20100016272A1 HETEROARYLACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译：异丙烯酰胺和它们作为药物的用途
公开(公告)号：US20100016272A1
公开(公告)日：2010-01-21
申请号：US12486117
申请日：2009-06-17
申请人： Hartmut STROBEL , Paulus WOHLFART , Heinz-Werner KLEEMANN , Gerhard ZOLLER , David William WILL
发明人： Hartmut STROBEL , Paulus WOHLFART , Heinz-Werner KLEEMANN , Gerhard ZOLLER , David William WILL
IPC分类号： A61K31/4709 , C07D401/06 , C07D267/10 , A61K31/496 , A61K31/553 , A61K31/397 , A61P25/00 , A61P9/00 , A61P3/00
CPC分类号： C07D213/56 , C07D213/64 , C07D213/73 , C07D213/75 , C07D215/12 , C07D233/64 , C07D233/68 , C07D239/26 , C07D277/30 , C07D277/46 , C07D333/24 , C07D333/60 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12
摘要： The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的杂芳基丙烯酰胺，其中Het，X，Ra，Rb，R 1，R 2和R 3具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理学活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

10. 发明申请

US20090239915A1 Substituted 2-phenyl-benzimidazoles and their use as pharmaceuticals 有权
标题翻译：取代的2-苯基 - 苯并咪唑及其作为药物的用途
公开(公告)号：US20090239915A1
公开(公告)日：2009-09-24
申请号：US12412481
申请日：2009-03-27
申请人： Gerhard ZOLLER , Hartmut STROBEL , David William WILL , Paulus WOHLFART
发明人： Gerhard ZOLLER , Hartmut STROBEL , David William WILL , Paulus WOHLFART
IPC分类号： A61K31/4245 , C07D235/18 , A61K31/4184 , C07D413/10 , A61P9/00
CPC分类号： C07D235/18 , C07D413/04
摘要： The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula I, in which X, R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要翻译：本发明涉及式I的2-苯基 - 苯并咪唑的衍生物，其中X，R，R 1至R 3和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录，并且是有价值的药理活性化合物。具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

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