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1. 发明授权

US08652785B2 Method of screening a modulator of endothelial NO synthase comprising the use of heme binding protein 1 失效
标题翻译：包括使用血红素结合蛋白1的内皮NO合成酶调节剂的筛选方法
公开(公告)号：US08652785B2
公开(公告)日：2014-02-18
申请号：US13131914
申请日：2009-11-27
申请人： Alexandra Krog , Jochen Kruip , Paulus Wohlfart , Johann Gassenhuber , Kathrin Heermeier , Hartmut Strobel , Natalie Karst , Alexandra Ferrier , Christian Viskov
发明人： Alexandra Krog , Jochen Kruip , Paulus Wohlfart , Johann Gassenhuber , Kathrin Heermeier , Hartmut Strobel , Natalie Karst , Alexandra Ferrier , Christian Viskov
IPC分类号： C12Q1/68
CPC分类号： G01N33/6893
摘要： The present invention relates to a method of screening for a modulator of endothelial NO synthase (eNOS) expression, a method of diagnosing a cardiovascular disease in a subject, the use of HEBP-1 for the identification of a medicament for preventing and/or treating a disease involving eNOS dysfunction, particularly a cardiovascular disease, the use of HEBP-1 for the detection of a component of eNOS signal transduction, and the use of HEBP1 for the regulation of eNOS promoter activity.
摘要翻译：本发明涉及一种筛选内皮细胞合成酶（eNOS）表达调节剂的方法，一种诊断受试者心血管疾病的方法，使用HEBP-1鉴定用于预防和/或治疗的药物涉及eNOS功能障碍，特别是心血管疾病的疾病，使用HEBP-1检测eNOS信号转导的成分，以及使用HEBP1来调节eNOS启动子活性。

2. 发明授权

US08299102B2 Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals 有权
标题翻译：杂芳基环丙烷甲酰胺及其作为药物的用途
公开(公告)号：US08299102B2
公开(公告)日：2012-10-30
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： C07D211/70 , A61K31/4418
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。

3. 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。

4. 发明申请

US20080167342A1 Heteroaryl-Substituted Amides Comprising An Unsaturated Or Cyclic Linker Group, And Their Use As Pharmaceuticals 有权
标题翻译：包含不饱和或环状连接基团的杂芳基取代的酰胺及其作为药物的用途
公开(公告)号：US20080167342A1
公开(公告)日：2008-07-10
申请号：US11958503
申请日：2007-12-18
申请人： Harmut STROBEL , Paulus WOHLFART , Gerhard ZOLLER , David William WILL
发明人： Harmut STROBEL , Paulus WOHLFART , Gerhard ZOLLER , David William WILL
IPC分类号： A61K31/4545 , C07D401/06 , A61K31/4439 , A61P9/00
CPC分类号： C07D401/14 , C07D401/06 , C07D401/08 , C07D409/14 , C07D417/06
摘要： The present invention relates to N-alkylamides of the formula I, in which A, Het, 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N-烷基酰胺，其中A，Het，X，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。

5. 发明授权

US08518976B2 Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals 有权
标题翻译：包含饱和连接基团的杂芳基取代的酰胺及其作为药物的用途
公开(公告)号：US08518976B2
公开(公告)日：2013-08-27
申请号：US11958483
申请日：2007-12-18
申请人： Harmut Strobel , Paulus Wohlfart , Gerhard Zoller , David William Will
发明人： Harmut Strobel , Paulus Wohlfart , Gerhard Zoller , David William Will
IPC分类号： C07D401/12 , C07D401/06
CPC分类号： C07D213/40 , C07D213/65 , C07D277/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/06 , C07D417/06 , C07D417/12
摘要： The present invention relates to N-alkylamides of the formula I, in which A, Het, 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N-烷基酰胺，其中A，Het，X，R 1，R 2和R 3具有权利要求中所述的含义，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。

6. 发明授权

US08168665B2 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：US08168665B2
公开(公告)日：2012-05-01
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： A01N43/50 , A01N43/52 , A61K31/415
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。

7. 发明授权

US07709478B2 Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents 有权
标题翻译：酰化6,7,8,9-四氢-5H-苯并环庚烯基胺及其作为药剂的用途
公开(公告)号：US07709478B2
公开(公告)日：2010-05-04
申请号：US10859773
申请日：2004-06-03
申请人： Hartmut Strobel , Paulus Wohlfart
发明人： Hartmut Strobel , Paulus Wohlfart
IPC分类号： A61K31/166
CPC分类号： C07C235/54 , C07C233/65 , C07C233/74 , C07C2602/12
摘要： The present invention relates to compounds 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, C and D are independently 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 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, diabetes complications, nephropathy, retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, or restricted memory performance or for a restricted ability to learn, or 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）的化合物，其中R 1 -R 4具有本说明书中给出的含义，A为CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B，C和D独立地为 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。这些化合物可用于制备用于治疗心血管疾病，稳定或不稳定心绞痛，冠心病，Prinzmetal心绞痛，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，内皮功能障碍的药物，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，糖尿病并发症，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，骨质疏松症或记忆障碍受限或受限制的学习能力，或降低绝经后妇女的心血管危险或摄入避孕药后。

8. 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。

9. 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。

10. 发明授权

US07338956B2 Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals 有权
标题翻译：酰氨基取代的杂芳族化合物及其作为药物的用途
公开(公告)号：US07338956B2
公开(公告)日：2008-03-04
申请号：US10634979
申请日：2003-08-05
申请人： Hartmut Strobel , Paulus Wohlfart , Peter Below
发明人： Hartmut Strobel , Paulus Wohlfart , Peter Below
IPC分类号： C07D417/12 , A61K31/428
CPC分类号： C07D215/38 , C07D235/30 , C07D263/58 , C07D277/82 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to acylamino-substituted heteroaromatic compounds of formula I, wherein R1, R2, R3, R4 and R5 and X are as defined herein, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.
摘要翻译：本发明涉及式I的酰氨基取代的杂芳族化合物，其中R 1，R 2，R 3，R 4，本文所述的X和X如本文所定义的药物组合物，包含这些化合物的药物组合物，刺激内皮NO合成酶表达的方法，以及包括施用这些化合物的治疗方法。

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