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    Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals
    1.
    发明授权
    Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals 有权
    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：US08642620B2

    公开(公告)日：2014-02-04

    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

    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。

    Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals
    2.
    发明授权
    Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals 有权
    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。

    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。

    Heteroarylacrylamides and their use as pharmaceuticals
    4.
    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。

    Substituted 2-phenyl-benzimidazoles and their use as pharmaceuticals
    5.
    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]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。

    Imidazo[1,2-a]pyridines and their use as pharmaceuticals
    8.
    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
    9.
    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。

    Guanidine and amidine derivatives as factor Xa inhibitors
    10.
    发明授权
    Guanidine and amidine derivatives as factor Xa inhibitors 失效
    胍和脒衍生物作为因子Xa抑制剂

    公开(公告)号：US07435747B2

    公开(公告)日：2008-10-14

    申请号：US10886312

    申请日：2004-07-07

    申请人： Anuschirwan Peyman ,  David William Will ,  Uwe Gerlach ,  Marc Nazaré ,  Gerhard Zoller ,  Hans-Peter Nestler ,  Hans Matter ,  Fahad Al-Obeidi

    发明人： Anuschirwan Peyman ,  David William Will ,  Uwe Gerlach ,  Marc Nazaré ,  Gerhard Zoller ,  Hans-Peter Nestler ,  Hans Matter ,  Fahad Al-Obeidi

    IPC分类号： A61K31/445 ,  C07D211/26

    CPC分类号： C07D401/12 ,  C07D211/26 ,  C07D211/34

    摘要： The present invention relates to compounds of the formula I, in which R0; Q; X; Q′, D, R10 and V have the meanings indicated in the 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 (FXa) and/or factor VIIa (FVIIa), 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 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 I, 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R 0是 Q; X; Q'，D，R 10和V具有权利要求中所示的含义。 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（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈 或预防因子Xa和/或因子VIIa的抑制。 本发明还涉及式I化合物的制备方法，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。