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1. 发明申请

WO2008104278A8 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：WO2008104278A8
公开(公告)日：2009-01-29
申请号：PCT/EP2008001150
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 , A61P9/02 , A61P9/08 , A61P11/00 , A61P19/10 , C07D401/04
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。

2. 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.

3. 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。

4. 发明申请

WO2008000922A1 DERIVES SOUFRES D ' UREE CYCLIQUE, LEUR PREPARATION ET LEUR UTILISATION PHARMACEUTIQUE COMME INHIBITEURS DE KINASES 审中-公开
标题翻译：含硫的循环尿素衍生物，其制备及其作为激酶抑制剂的药物用途
公开(公告)号：WO2008000922A1
公开(公告)日：2008-01-03
申请号：PCT/FR2007/000080
申请日：2007-01-17
申请人： AVENTIS PHARMA S.A. , HALLEY, Frank , EL-AHMAD, Youssef , CERTAL, Victor , STROBEL, Hartmut , RITTER, Kurt , RUF, Sven , DAGALLIER, Anne , VENOT, Corinne
发明人： HALLEY, Frank , EL-AHMAD, Youssef , CERTAL, Victor , STROBEL, Hartmut , RITTER, Kurt , RUF, Sven , DAGALLIER, Anne , VENOT, Corinne
IPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , A61K31/41 , A61K31/4439 , A61K31/506
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14
摘要： L'invention concerne les nouveaux produits de formule (I) : dans laquelle n représente 0 ou 2; R représente pyridyle ou pyrimidinyle substitués par un radical NR1R2, avec l'un de R1 et R2 représente hydrogène ou alkyle, et l'autre de R1 et R2 représente hydrogène ou alkyle éventuellement substitué, cycloalkyle, hétérocycloalkyle, phényle, pyrimidinyle, pyridyle, et CO-R3 avec R3 choisi notamment parmi les radicaux aminés, alcoxy, hétérocycloalkyle, aryle, aryloxy et hétéroaryle; tous ces radicaux étant éventuellement substitués; et leurs sels.
摘要翻译：本发明涉及式（I）的新产物：其中n为0或2; R是被NR 1 R 2基取代的吡啶基或嘧啶基，其中R 1和R 2中的一个是氢或烷基，R 1和R 2中的另一个是氢或任选取代的烷基，环烷基，杂环烷基，苯基，嘧啶基，吡啶基和CO-R 3 R3特别选自氨基，烷氧基，杂环烷基，芳基，芳氧基和杂芳基; 所有这些基团任选被取代; 及其盐。

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

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。

7. 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。

8. 发明申请

WO2006010641A3 NOVEL CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS 审中-公开
标题翻译：新型环状尿素衍生物及其制备方法和作为激酶抑制剂的药物用途
公开(公告)号：WO2006010641A3
公开(公告)日：2006-10-26
申请号：PCT/EP2005008720
申请日：2005-07-25
申请人： AVENTIS PHARMA SA , STROBEL HARTMUT , RUF SVEN , LESUISSE DOMINIQUE , NEMECEK CONCEPTION , EL-AHMAD YOUSSEF , GUESSREGEN STEFAN , LEBRUN ANNE , RITTER KURT , BENARD DIDIER , HITTINGER AUGUSTIN , BOUCHARD HERVE
发明人： STROBEL HARTMUT , RUF SVEN , LESUISSE DOMINIQUE , NEMECEK CONCEPTION , EL-AHMAD YOUSSEF , GUESSREGEN STEFAN , LEBRUN ANNE , RITTER KURT , BENARD DIDIER , HITTINGER AUGUSTIN , BOUCHARD HERVE
IPC分类号： C07D401/06 , A61K31/4166 , C07D401/14
CPC分类号： C07D403/04
摘要： The invention relates to products of formula (I): in which p = 0, 1 and 2; A = aryl, heteroaryl, carbocycle or heterocycle; X = single bond; -N(R6)-; -NH-alk-; alkylene; -O-; -C(O)-; -S(O)n-; -N(R6)-C(O)-; -NH-CO-alk-, -N(R6)-C(O)-N(R6')-; -N(R6)-C(S)-N(R6')-; -N(R6)-C(O)O-; -N(R6)-SO2-; -N(R6)-SO2-N(R6')-; -C(O)-N(R6)-; -SO2-NR6-; and -C(O)O-; L1 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, heteroarylene; all optionally substituted; R1 = hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; -SO2R9, -C(O)R9; -C(O)OR9,-C(O)NR10R11, -C(S)NR10R11,-SO2NR10R11; R2 = hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, either R1 and R2 with N, or NR1R2 with L1 may form a saturated or unsaturated heterocycle possibly containing O, N, S; R3 = hydrogen; halogen; alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylenedioxy, heterocycle, aryl and heteroaryl, all optionally substituted; S(O)n-alkyl; amino, alkylamino, dialkylamino, with dialkylamino optionally forming with N a cycle, all optionally substituted; R4, R4' and R4''= hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, oxo; with two from among R4, R4' and R4'' possibly forming with C a ring possibly containing O, N or S; L2 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, -O-, -NR17-, -C(O)-, SO2; Y = N-heterocycle possibly containing O, N or S; R5 = hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl; all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products.
摘要翻译：本发明涉及式（I）的产物：其中p = 0,1和2; A =芳基，杂芳基，碳环或杂环; X =单键; -N（R 6） - ; -NH-烷 - ; 亚; -O-; -C（O） - ; -儿子-; -N（R 6）-C（O） - ; -NH-CO-alk-，-N（R 6）-C（O）-N（R 6'） - ; -N（R6）-C（S）-N（R6' ） - ; -N（R 6）-C（O）O-; -N（R 6）-SO 2 - ; -N（R6）-SO2-N（R6' ） - ; -C（O）-N（R6） - ; -SO 2 NR 6 - ; 和-C（O）O-; L1 =单键，亚烷基，亚烯基，亚炔基，亚环烷基，亚苯基，亚杂芳基; 全部任选被取代; R1 =氢，烷基，烯基，炔基或环烷基，芳基，杂芳基，芳基烷基，杂芳基烷基; -SO 2 R 9，-C（O）R 9; -C（O）OR 9，-C（O）NR 10 R 11，-C（S）NR 10 R 11，-SO 2 NR 10 R 11; R 2 =氢，烷基，烯基，炔基，环烷基，R 1和R 2与N或NR 1 R 2与L 1可以形成可能含有O，N，S的饱和或不饱和杂环; R3 =氢; 卤素; 烷基，烯基，炔基，环烷基，烷氧基，亚烷基二氧基，杂环，芳基和杂芳基，全部任选被取代; S（O）n-烷基; 氨基，烷基氨基，二烷基氨基，任选与N环形成的二烷基氨基，全部任选被取代; R4，R4'和R4“=氢，卤素，烷基，烯基，炔基，环烷基，芳基，杂芳基，氧代; 其中R4，R4'和R4“中的两个可能与C形成可能含有O，N或S的环; L2 =单键，亚烷基，亚烯基，亚炔基，亚环烷基，-O - ， - NR17-，-C（O） - ，SO2; Y =可能含有O，N或S的N-杂环; R5 =氢，卤素，烷基，烯基，炔基，环烷基，芳基，芳基烷基，杂芳基，杂芳基烷基; 所有这些基团任选地被取代，这些产物以所有异构形式和盐作为医药产品。

9. 发明申请

WO2006010641A2 NOVEL CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS 审中-公开
标题翻译：新型循环尿素衍生物，其制备方法及其作为激酶抑制剂的药物用途
公开(公告)号：WO2006010641A2
公开(公告)日：2006-02-02
申请号：PCT/EP2005/008720
申请日：2005-07-25
申请人： AVENTIS PHARMA S.A. , STROBEL, Hartmut , RUF, Sven , LESUISSE, Dominique , NEMECEK, Conception , EL-AHMAD, Youssef , GUESSREGEN, Stefan , LEBRUN, Anne , RITTER, Kurt , BENARD, Didier , HITTINGER, Augustin , BOUCHARD, Hervé
发明人： STROBEL, Hartmut , RUF, Sven , LESUISSE, Dominique , NEMECEK, Conception , EL-AHMAD, Youssef , GUESSREGEN, Stefan , LEBRUN, Anne , RITTER, Kurt , BENARD, Didier , HITTINGER, Augustin , BOUCHARD, Hervé
IPC分类号： C07D401/06 , C07D401/14
CPC分类号： C07D403/04
摘要： The invention relates to products of formula (I): in which p = 0, 1 and 2; A = aryl, heteroaryl, carbocycle or heterocycle; X = single bond; -N(R6)-; -NH-alk-; alkylene; -O-; -C(O)-; -S(O)n-; -N(R6)-C(O)-; -NH-CO-alk-, -N(R6)-C(O)-N(R6')-; -N(R6)-C(S)-N(R6')-; -N(R6)-C(O)O-; -N(R6)-SO2-; -N(R6)-SO2-N(R6')-; -C(O)-N(R6)-; -SO2-NR6-; and -C(O)O-; L1 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, heteroarylene; all optionally substituted; R1 = hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; -SO2R9, -C(O)R9; -C(O)OR9,-C(O)NR10R11, -C(S)NR10R11,-SO2NR10R11; R2 = hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, either R1 and R2 with N, or NR1R2 with L1 may form a saturated or unsaturated heterocycle possibly containing O, N, S; R3 = hydrogen; halogen; alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylenedioxy, heterocycle, aryl and heteroaryl, all optionally substituted; S(O)n-alkyl; amino, alkylamino, dialkylamino, with dialkylamino optionally forming with N a cycle, all optionally substituted; R4, R4' and R4''= hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, oxo; with two from among R4, R4' and R4'' possibly forming with C a ring possibly containing O, N or S; L2 = single bond, alkylene, alkenylene, alkynylene, cycloalkylene, -O-, -NR17-, -C(O)-, SO2; Y = N-heterocycle possibly containing O, N or S; R5 = hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl; all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products.
摘要翻译：本发明涉及式（I）的产物：其中p = 0,1和2; A =芳基，杂芳基，碳环或杂环; X =单键; -N（R 6） - ; -NH-烷 - ; 亚; -O-; -C（O） - ; -儿子-; -N（R 6）-C（O） - ; -NH-CO-烷基，-N（R 6）-C（O）-N（R 6'） - ; -N（R6）-C（S）-N（R6' ） - ; -N（R 6）-C（O）O-; -N（R 6）-SO 2 - ; -N（R6）-SO2-N（R6' ） - ; -C（O）-N（R6） - ; -SO 2 NR 6 - ; 和-C（O）O-; L1 =单键，亚烷基，亚烯基，亚炔基，亚环烷基，亚苯基，亚杂芳基; 全部任意取代; R 1 =氢，烷基，烯基，炔基或环烷基，芳基，杂芳基，芳基烷基，杂芳基烷基; -SO 2 R 9，-C（O）R 9; -C（O）OR 9，-C（O）NR 10 R 11，-C（S）NR 10 R 11，-SO 2 NR 10 R 11; R 2 =氢，烷基，烯基，炔基，环烷基，R 1和R 2与N或NR 1 R 2与L 1可以形成可能含有O，N，S的饱和或不饱和杂环; R3 =氢; 卤素; 烷基，烯基，炔基，环烷基，烷氧基，亚烷基二氧基，杂环，芳基和杂芳基，全部被取代; S（O）n-烷基; 氨基，烷基氨基，二烷基氨基，二烷基氨基，任选地以N a个周期形成，全部任选被取代; R 4，R 4'和R 4“=氢，卤素，烷基，烯基，炔基，环烷基，芳基，杂芳基，氧代; 其中R4，R4和R4之间的两个可能形成可能含有O，N或S的C环; L2 =单键，亚烷基，亚烯基，亚炔基，亚环烷基，-O-，-NR17-，-C（O） - ，SO2; Y =可能含有O，N或S的N-杂环; R5 =氢，卤素，烷基，烯基，炔基，环烷基，芳基，芳基烷基，杂芳基，杂芳基烷基; 所有这些基团任选被取代，这些产物是所有异构体形式和盐，作为药用产品。

10. 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。

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