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1. 发明申请

WO2009135590A1 ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 审中-公开
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：WO2009135590A1
公开(公告)日：2009-11-12
申请号：PCT/EP2009/002917
申请日：2009-04-22
申请人： SANOFI-AVENTIS , SCHAEFER, Matthias , PERNERSTORFER, Josef , KADEREIT, Dieter , STROBEL, Hartmut , CZECHTIZKY, Werngard , CHEN, L., Charlie , SAFAROVA, Alena , WEICHSEL, Aleksandra , PATEK, Marcel
发明人： SCHAEFER, Matthias , PERNERSTORFER, Josef , KADEREIT, Dieter , STROBEL, Hartmut , CZECHTIZKY, Werngard , CHEN, L., Charlie , SAFAROVA, Alena , WEICHSEL, Aleksandra , PATEK, Marcel
IPC分类号： A61K31/4402 , A61K31/38 , A61K31/16 , A61P9/00 , A61P29/00 , C07D333/80 , C07D333/32 , C07C323/19 , C07C235/54 , C07C235/84 , C07C323/62 , C07D213/64 , C07D277/56
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, R 3 to R 6 , R 20 to R 22 and R 50 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 LPA 1 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，其为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。

2. 发明申请

WO2004094425A1 Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals 审中-公开
标题翻译：三氮杂和四氮杂蒽醌二酮衍生物，其制备及其作为药物的用途
公开(公告)号：WO2004094425A1
公开(公告)日：2004-11-04
申请号：PCT/EP2004/003851
申请日：2004-04-13
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH , WEICHERT, Andreas , STROBEL, Hartmut , WOHLFART, Paulus , PATEK, Marcel , SMRCINA, Martin , WEICHSEL, Aleksandra
发明人： WEICHERT, Andreas , STROBEL, Hartmut , WOHLFART, Paulus , PATEK, Marcel , SMRCINA, Martin , WEICHSEL, Aleksandra
IPC分类号： C07D471/14
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to triaza- and tetraaza-anthracenedione derivatives of the formula (I), in which A, B and R 1 to R 5 have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmacologically active compounds. They are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (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 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）的三氮杂和四氮杂蒽并二酮衍生物，其中A，B和R 1至R 5具有权利要求中所示的含义。式（I）化合物是有价值的药理活性化合物。它们可用于治疗各种疾病状态，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。它们上调酶内皮一氧化氮（NO）合酶的表达，并且可以在需要所述酶的增加的表达或增加的NO水平或降低的NO水平的归一化的条件下应用。本发明还涉及式（I）化合物的制备方法，其用途，特别是药物中的活性成分，以及包含它们的药物制剂。

3. 发明申请

WO2008104278A1 IMIDAZO[1,2-A] PYRIDINES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：咪唑并[1,2-A]吡啶并用作药物
公开(公告)号：WO2008104278A1
公开(公告)日：2008-09-04
申请号：PCT/EP2008/001150
申请日：2008-02-15
申请人： SANOFI-AVENTIS , ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
发明人： ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
IPC分类号： A61K31/437 , C07D401/04 , A61P9/02 , A61P9/08 , A61P11/00 , A61P19/10
CPC分类号： C07D471/04
摘要： The present invention relates to derivatives of imidazo[1,2-a]pyridines of the 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 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 ）合成酶，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应用。本发明还涉及制备式（I）化合物，包含它们的药物组合物的方法，以及式（I）化合物在制备用于刺激内皮细胞表达的药物中的应用 NO合成酶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，高血压和心脏功能不全等各种疾病。

4. 发明申请

WO2008058641A1 IMIDAZO[2, 1-B]THIAZOLES AND THEIR USE AS PHARMACEUTICALS 审中-公开
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：WO2008058641A1
公开(公告)日：2008-05-22
申请号：PCT/EP2007/009539
申请日：2007-11-03
申请人： SANOFI-AVENTIS , ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
发明人： ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
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 the 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 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 ）合成酶，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。本发明还涉及用于制备式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诸如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等心血管疾病的各种疾病。

5. 发明申请

WO2008074413A3 HETEROARYLACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS FOR THE STIMULATION OF THE EXPRESSION OF ENDOTHELIAL NO SYNTHASE 审中-公开
公开(公告)号：WO2008074413A3
公开(公告)日：2008-06-26
申请号：PCT/EP2007/010709
申请日：2007-12-08
申请人： SANOFI-AVENTIS , STROBEL, Hartmut , WOHLFART, Paulus , KLEEMANN, Heinz-Werner , ZOLLER, Gerhard , WILL, David, William
发明人： STROBEL, Hartmut , WOHLFART, Paulus , KLEEMANN, Heinz-Werner , ZOLLER, Gerhard , WILL, David, William
IPC分类号： C07D213/50 , C07D401/06 , C07D407/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06 , A61P9/00 , A61K31/4523
摘要： The present invention relates to heteroarylacrylamides of the formula (I), in which Het, X, R a , R b , R 1 , R 2 and R 3 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.

6. 发明申请

WO2008037381A1 SUBSTITUTED 2-PHENYL-BENZIMIDAZOLES AND THEIR USE AS PHARMACEUTICALS 审中-公开
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：WO2008037381A1
公开(公告)日：2008-04-03
申请号：PCT/EP2007/008104
申请日：2007-09-18
申请人： SANOFI-AVENTIS , ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
发明人： ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
IPC分类号： C07D235/18 , C07D413/04 , A61K31/4184 , A61K31/4245 , 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使用。本发明还涉及制备式（I）化合物，包含它们的药物组合物的方法，以及式（I）化合物在制备用于刺激内皮细胞表达的药物中的应用 NO合成酶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，高血压和心脏功能不全等各种疾病。

7. 发明申请

WO2007000246A1 HETEROARYL-SUBSTITUTED AMIDES COMPRISING A SATURATED LINKER GROUP, AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：包含饱和连接剂组的HETEROARYL取代的氨基酸及其作为药物的用途
公开(公告)号：WO2007000246A1
公开(公告)日：2007-01-04
申请号：PCT/EP2006/005706
申请日：2006-06-14
申请人： SANOFI-AVENTIS DEUTSCHLAND GMBH , STROBEL, Hartmut , WOHLFART, Paulus , ZOLLER, Gerhard , WILL, David, William
发明人： STROBEL, Hartmut , WOHLFART, Paulus , ZOLLER, Gerhard , WILL, David, William
IPC分类号： C07D401/06 , C07D417/06 , C07D401/12 , C07D277/42 , C07D213/36 , C07D213/63 , A61P9/08 , A61K31/4439 , A61K31/444
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, R 1 , R 2 and R 3 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， SUP>具有权利要求书中所示的含义，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。

8. 发明申请

WO2008104279A1 IMIDAZO[1,2-A]AZINES AND THEIR USE AS PHARMACEUTICALS 审中-公开
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：WO2008104279A1
公开(公告)日：2008-09-04
申请号：PCT/EP2008/001151
申请日：2008-02-15
申请人： SANOFI-AVENTIS , ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
发明人： ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
IPC分类号： C07D487/04 , A61K31/4188 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61P1/16 , A61P3/10 , A61P3/14 , A61P7/02 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12
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 the 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 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）的咪唑并[1,2-a]吖嗪衍生物，其中R 1，R 3，R 3，X，Y和n具有权利要求中所示的含义，其调节内皮转录一氧化氮（NO）合成酶，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，包含它们的药物组合物的方法，以及式（I）化合物在制备用于刺激内皮细胞表达的药物中的应用 NO合酶或。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

WO2008080511A1 HETEROARYLCYCLOPROPANECARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
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：WO2008080511A1
公开(公告)日：2008-07-10
申请号：PCT/EP2007/010708
申请日：2007-12-08
申请人： SANOFI-AVENTIS , STROBEL, Hartmut , WOHLFART, Paulus , ZOLLER, Gerhard , WILL, David, William
发明人： STROBEL, Hartmut , WOHLFART, Paulus , ZOLLER, Gerhard , WILL, David, William
IPC分类号： C07D213/56 , C07D271/10 , C07D333/24 , C07D401/12 , C07D413/12 , C07D417/12 , C07D487/08 , A61K31/444 , A61P9/08
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, R a , R b , R c , R d , R 1 , R 2 and R 3 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，R a，R b，R c，R c，R R 1，R 2，R 2和R 3具有权利要求中指出的含义，其调节转录的内皮一氧化氮（NO）合成酶，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应用。本发明还涉及制备式（I）化合物，包含它们的药物组合物的方法，以及式（I）化合物在制备用于刺激内皮细胞表达的药物中的应用 NO合成酶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，高血压和心脏功能不全等各种疾病。

10. 发明申请

WO2007000248A1 HETEROARYL-SUBSTITUTED AMIDES COMPRISING AN UNSATURATED OR CYCLIC LINKER GROUP, AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：包含不饱和或循环链接组的HETEROARYL取代的氨基酸及其作为药物的用途
公开(公告)号：WO2007000248A1
公开(公告)日：2007-01-04
申请号：PCT/EP2006/005716
申请日：2006-06-14
申请人： SANOFI-AVENTIS DEUTSCHLAND GMBH , STROBEL, Hartmut , WOHLFART, Paulus , ZOLLER, Gerhard , WILL, David, William
发明人： STROBEL, Hartmut , WOHLFART, Paulus , ZOLLER, Gerhard , WILL, David, William
IPC分类号： C07D401/06 , C07D417/06 , C07D401/08 , C07D401/14 , C07D409/14 , A61P9/08 , A61K31/4439 , A61K31/444
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, R 1 , R 2 and R 3 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， SUP>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NO水平的标准化的条件下使用。本发明还涉及用于制备式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诸如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等心血管疾病的各种疾病。

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