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    Heteroarylacrylamides and their use as pharmaceuticals
    1.
    发明授权
    Heteroarylacrylamides and their use as pharmaceuticals 有权
    杂芳基丙烯酰胺及其作为药物的用途

    公开(公告)号：US08304438B2

    公开(公告)日：2012-11-06

    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： C07D401/06 ,  A61K31/44

    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。

    Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals
    3.
    发明授权
    Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals 有权
    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。

    Substituted 2-phenyl-benzimidazoles and their use as pharmaceuticals
    4.
    发明授权
    Substituted 2-phenyl-benzimidazoles and their use as pharmaceuticals 有权
    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。

    Imidazo[1,2-a]pyridines and their use as pharmaceuticals
    5.
    发明授权
    Imidazo[1,2-a]pyridines and their use as pharmaceuticals 有权
    咪唑并[1,2-a]吡啶及其作为药物的用途

    公开(公告)号：US08399476B2

    公开(公告)日：2013-03-19

    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： A01N43/42 ,  A61K31/44 ,  C07D491/02 ,  C07D498/02

    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。

    Imidazo[2,1-b]thiazoles and their use as pharmaceuticals
    6.
    发明授权
    Imidazo[2,1-b]thiazoles and their use as pharmaceuticals 有权
    咪唑并[2,1-b]噻唑及其作为药物的用途

    公开(公告)号：US08080569B2

    公开(公告)日：2011-12-20

    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

    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应用。 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。

    Imidazo[1,2-a]azines and their use as pharmaceuticals
    7.
    发明授权
    Imidazo[1,2-a]azines and their use as pharmaceuticals 有权
    咪唑并[1,2-a]吖嗪及其作为药物的用途

    公开(公告)号：US08044050B2

    公开(公告)日：2011-10-25

    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

    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。

    Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents
    9.
    发明授权
    Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents 有权
    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。