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1. 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。

2. 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。

3. 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.

4. 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。

5. 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。

6. 发明申请

WO2014044738A1 BENZOIMIDAZOLE-CARBOXYLIC ACID AMIDE DERIVATIVES AS APJ RECEPTOR MODULATORS 审中-公开
标题翻译：苯甲酰胺唑羧酸酰胺衍生物作为APJ受体调节剂
公开(公告)号：WO2014044738A1
公开(公告)日：2014-03-27
申请号：PCT/EP2013/069432
申请日：2013-09-19
申请人： SANOFI
发明人： HACHTEL, Stephanie , WOHLFART, Paulus , WESTON, John , MÜLLER, Marco , DEFOSSA, Elisabeth , MERTSCH, Katharina , WENG, Jian-Hui , BINNIE, Robert A. , ABDUL-LATIF, Farid , BOCK, William Jerome , WALSER, Armin
IPC分类号： C07D235/08 , C07D403/06 , C07D405/06 , C07D409/14 , C07D411/06 , C07D413/14 , C07D417/06 , C07D451/04 , C07D487/06 , A61K31/4184 , A61P3/10 , A61P9/10
CPC分类号： C07D235/08 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D411/06 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D451/04 , C07D455/02 , C07D487/06 , C07D487/08
摘要： The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R', R", R"', R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I的苯并咪唑 - 羧酸酰胺化合物，其中R'，R“，R”'，R 1，R 2，R 3，R 4，R 5，R 6和Z定义如下。式I的化合物是APJ受体调节剂，并且可用于治疗例如与血压升高相关的疾病。本发明还涉及式I化合物，特别是作为药物中的活性成分的用途，以及包含它们的药物组合物。

7. 发明申请

WO2010063652A1 METHODS AND USES INVOLVING HEME BINDING PROTEIN 1 审中-公开
标题翻译：涉及HEME结合蛋白的方法和用途1
公开(公告)号：WO2010063652A1
公开(公告)日：2010-06-10
申请号：PCT/EP2009/065989
申请日：2009-11-27
申请人： SANOFI-AVENTIS , KRUG, Alexandra , KRUIP, Jochen , WOHLFART, Paulus , GASSENHUBER, Johann , HEERMEIER, Kathrin , STROBEL, Hartmut , KARST, Natalie , FERRIER, Alexandra , VISKOV, Christian
发明人： KRUG, Alexandra , KRUIP, Jochen , WOHLFART, Paulus , GASSENHUBER, Johann , HEERMEIER, Kathrin , STROBEL, Hartmut , KARST, Natalie , FERRIER, Alexandra , VISKOV, Christian
IPC分类号： G01N33/68 , A61K38/00
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。

8. 发明申请

WO2008077507A1 HETEROARYL-SUBSTITUTED CARBOXAMIDES AND USE THEREOF FOR THE STIMULATION OF THE EXPRESSION OF NO SYNTHASE 审中-公开
标题翻译：异氟醚取代的碳水化合物及其用于刺激无合成酶表达的用途
公开(公告)号：WO2008077507A1
公开(公告)日：2008-07-03
申请号：PCT/EP2007/010982
申请日：2007-12-14
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： C07D213/89 , C07D237/14 , C07D239/26 , C07D271/10 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/42 , C07D285/12 , C07D333/24 , C07D401/04 , C07D401/12 , C07D409/04 , C07D409/06 , C07D409/12
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, 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）的杂芳基取代的甲酰胺，其中Het，A，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，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。

9. 发明申请

WO2015055694A1 4-[5-(3-CHLORO-PHENOXY)-OXAZOLO[5,4-D]PYRIMIDIN-2-YL]-2,6-DIMETHYL-PHENOXY}-ACETIC ACID FOR USE IN THE PREVENTION OR TREATMENT OF ACUTE KIDNEY INJURY 审中-公开
标题翻译： 4- [5-（3-氯 - 苯氧基） - 氧杂] [5,4-D]嘧啶-2-YL] -2,6-二甲基 - 苯甲酸用于预防或治疗急性感染性损伤
公开(公告)号：WO2015055694A1
公开(公告)日：2015-04-23
申请号：PCT/EP2014/072078
申请日：2014-10-15
申请人： SANOFI
发明人： BRIAND, Véronique , GRATZER, Sabine , HUEBSCHLE, Thomas , JANIAK, Philip , KADEREIT, Dieter , PARKAR, Ashfaq , POIRIER, Bruno , SCHAEFER, Matthias , WOHLFART, Paulus
IPC分类号： A61K31/519 , A61P13/12
CPC分类号： A61K31/519 , Y02P20/582
摘要： {4-[5-(3-chloro-phenoxy)-oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethyl-phenoxy}-acetic acid or a pharmaceutically acceptable salt thereof for use in the prevention or treatmentof AKI (acute kidney injury). Medicament and pharmaceutical composition thereof.
摘要翻译： {4- [5-（3-氯 - 苯氧基） - 恶唑并[5,4-d]嘧啶-2-基] -2,6-二甲基 - 苯氧基} - 乙酸或其药学上可接受的盐预防或治疗AKI（急性肾损伤）。药物及其药物组合物。

10. 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。

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