相似化合物
1342836-25-2 632365-54-9 105434-90-0欧盟法规
C&L通报上下游产品
5-nitropyrazole-3-carboxylic acid 3-amino-5-methylpyrazole 5-pyridin-2-yl-7-trifluoromethyl-pyrazolo[1,5-a]pyrimidine-2-carboxylic acid 5-(3,4-dichloro-phenyl)-7-trifluoromethyl-pyrazolo[1,5-a]pyrimidine-2-carboxylic acid 7-amino-5-(3,4-dichloro-phenyl)-pyrazolo[1,5-a]pyrimidine-2-carboxylic acid 专利信息
专利号:US-2005239808-A1
优先权日:2002-05-10
标题 :Active substances for the treatment, diagnosis and prophylaxis of diseases in which abnormal protein structures occur
发明人:SCHRADER THOMAS; RIESNER DETLEV; RZEPECKI PETRA; NAGEL-STEGER LUITGARD; WEHNER MARK; KIRSTEN CHRISTIAN; MOLT OLIVER; ZADMARD REZA; ASCHERMANN KATJA
权利人:SCHRADER THOMAS; RIESNER DETLEV; RZEPECKI PETRA; NAGEL-STEGER LUITGARD; WEHNER MARK; KIRSTEN CHRISTIAN; MOLT OLIVER; ZADMARD REZA; ASCHERMANN KATJA
摘要:The invention on hand refers to diseases associated with abnormal protein structures, including Alzheimer's disease, Creutzfeldt-Jakob's disease, BSE and other prion-associated diseases. It is the task of the invention on hand to provide new active agents preventing the formation of amyloid plaques and to dissolve existing plaques, such agents being convenient for therapy, diagnosis and prophylaxis of diseases that are associated with abnormal protein structures. This task is performed in terms of the current invention by heterocyclic or aromatic agents with a rigid structure and a donor-acceptor-donor pattern (DAD), the latter being formed by donors and acceptors of hydrogen bridge linkages which comply with the β-sheet structure of the peptide or protein and thus fit as binding partners. The heterocyclic or aromatic agents are available at least as dimers. They recognise peptides and proteins with a β-sheet structure, form stable complexes with them and inhibit their aggregation to β-amyloid plaques. Furthermore, the new active agents are able to dissolve β-amyloid plaques that already exist. Another task of the current invention is to provide methods for the synthesis of said heterocyclic or aromatic compounds.
专利号:WO-2006127595-A1
优先权日:2005-05-23
标题:5-aminopyrazole carboxylic acid derivatives and methods of treatment of metabolic-related disorders thereof
发明人:SKINNER PHILIP J; SEMPLE GRAEME; WEBB PETER
权利人:ARENA PHARM INC; SKINNER PHILIP J; SEMPLE GRAEME; WEBB PETER
摘要:The present invention relates to certain pyrazole carboxylic acid or ester derivatives of Formula (I) and pharmaceutically acceptable salts thereof which exhibit useful pharmacological properties, for example, as agonists for the GPCR referred to herein as RUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, such as, dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.