公开(公告)号：US20080171739A1

公开(公告)日：2008-07-17

申请号：US11958483

申请日：2007-12-18

Applicant: Harmut STROBEL ,  Paulus WOHLFART ,  Gerhard ZOLLER ,  David William WILL

Inventor： Harmut STROBEL ,  Paulus WOHLFART ,  Gerhard ZOLLER ,  David William WILL

IPC: A61K31/541 ,  C07D401/06 ,  A61K31/444 ,  A61P9/00 ,  A61K31/4545

CPC classification number: C07D213/40 ,  C07D213/65 ,  C07D277/42 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20080167342A1

公开(公告)日：2008-07-10

申请号：US11958503

申请日：2007-12-18

Applicant: Harmut STROBEL ,  Paulus WOHLFART ,  Gerhard ZOLLER ,  David William WILL

Inventor： Harmut STROBEL ,  Paulus WOHLFART ,  Gerhard ZOLLER ,  David William WILL

IPC: A61K31/4545 ,  C07D401/06 ,  A61K31/4439 ,  A61P9/00

CPC classification number: C07D401/14 ,  C07D401/06 ,  C07D401/08 ,  C07D409/14 ,  C07D417/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08518976B2

公开(公告)日：2013-08-27

申请号：US11958483

申请日：2007-12-18

Applicant: Harmut Strobel ,  Paulus Wohlfart ,  Gerhard Zoller ,  David William Will

Inventor： Harmut Strobel ,  Paulus Wohlfart ,  Gerhard Zoller ,  David William Will

IPC: C07D401/12 ,  C07D401/06

CPC classification number: C07D213/40 ,  C07D213/65 ,  C07D277/42 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08642620B2

公开(公告)日：2014-02-04

申请号：US11958503

申请日：2007-12-18

Applicant: Harmut Strobel ,  Paulus Wohlfart ,  Gerhard Zoller ,  David William Will

Inventor： Harmut Strobel ,  Paulus Wohlfart ,  Gerhard Zoller ,  David William Will

IPC: A61K31/4545 ,  C07D401/06

CPC classification number: C07D401/14 ,  C07D401/06 ,  C07D401/08 ,  C07D409/14 ,  C07D417/06

Abstract: 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.

Abstract translation: 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。