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    • 1. 发明申请
    • IMIDAZO[1,2-A] PYRIDINES AND THEIR USE AS PHARMACEUTICALS
    • 咪唑并[1,2-A]吡啶并用作药物
    • WO2008104278A1
    • 2008-09-04
    • PCT/EP2008/001150
    • 2008-02-15
    • SANOFI-AVENTISZOLLER, GerhardSTROBEL, HartmutWILL, David, WilliamWOHLFART, Paulus
    • ZOLLER, GerhardSTROBEL, HartmutWILL, David, WilliamWOHLFART, Paulus
    • A61K31/437C07D401/04A61P9/02A61P9/08A61P11/00A61P19/10
    • C07D471/04
    • 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.
    • 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
    • IMIDAZO[2, 1-B]THIAZOLES AND THEIR USE AS PHARMACEUTICALS
    • 咪唑并[2,1-B]噻唑及其作为药物的用途
    • WO2008058641A1
    • 2008-05-22
    • PCT/EP2007/009539
    • 2007-11-03
    • SANOFI-AVENTISZOLLER, GerhardSTROBEL, HartmutWILL, David, WilliamWOHLFART, Paulus
    • ZOLLER, GerhardSTROBEL, HartmutWILL, David, WilliamWOHLFART, Paulus
    • A61K31/429C07D513/04A61P9/10
    • C07D513/04
    • 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.
    • 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。
    • 4. 发明申请
    • SUBSTITUTED 2-PHENYL-BENZIMIDAZOLES AND THEIR USE AS PHARMACEUTICALS
    • 取代的2-苯基苯并咪唑及其作为药物的用途
    • WO2008037381A1
    • 2008-04-03
    • PCT/EP2007/008104
    • 2007-09-18
    • SANOFI-AVENTISZOLLER, GerhardSTROBEL, HartmutWILL, David, WilliamWOHLFART, Paulus
    • ZOLLER, GerhardSTROBEL, HartmutWILL, David, WilliamWOHLFART, Paulus
    • C07D235/18C07D413/04A61K31/4184A61K31/4245A61P9/00
    • C07D235/18C07D413/04
    • 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.
    • 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。