专利号:US-10538490-B2 优先权日:2016-10-25 标题:Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof 发明人:ECKHARDT MATTHIAS; PETERS STEFAN; WAGNER HOLGER 权利人:BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of general formula I, n nwherein the groups R, R 1 , R 2 , R 3 , m and n are defined herein, which have valuable pharmacological properties, including binding to the GPR40 receptor and modulating its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-2010249192-A1 优先权日:2007-12-11 标 题 :Novel heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:LI CHUN SING; RAMTOHUL YEEMAN K; LECLERC JEAN-PHILIPPE 权利人:MERCK FROSST CANADA LTD 摘要:Heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer; liver steatosis; and non-alcoholic steatohepatitis. n HetAr − W − X − Ar  (I)
专利号:US-5654439-A 优先权日:1994-01-11 标 题:N-1-alkyl-2,5-Di(trialkyl silyl) pyrrolidines 发明人:PANDEY GANESH; BAGUL TRUSAR DAMU; LAKSHMAIAH GINGIPALLI 权利人:COUNCIL SCIENT IND RES 摘要:A novel 6-chloro-3-vinyl-pyridine of formula ##STR1## where X represents --H, --SO 2 Ph, --CO 2 Et, --COCH 3 and --CHO; which is used for the synthesis of Epibatidine of formula ##STR2## by reacting said 6-chloro-3-vinyl pyridine with N-1-alkyl-2,5-di(trialkyl silyl) pyrrolidine of formula ##STR3## to obtain N-alkyl Epibatidine which is hydrogenated to obtain the Epibatidine.
专利号:US-9617251-B2 优先权日:2015-08-07 标题:Indanylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof 发明人:ECKHARDT MATTHIAS; PETERS STEFAN; WAGNER HOLGER 权利人:BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of general formula I, n nwherein the groups R, R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-6844441-B2 优先权日:2000-03-31 标 题:Process for preparing substituted pyridines 发明人:DOW ROBERT L; SCHNEIDER STEVEN R 权利人:PFIZER 摘要:A process for preparing a compound of the formula: n n nwherein n, R 1 , R 2 , R 3 and X are as defined above, used as an intermediate in the synthesis of β-adrenergic receptor agonists.
专利号:US-2009137577-A1 优先权日:2007-06-29 标 题 :Heterocyclic compounds 发明人:DUPLANTIER ALLEN J; EFREMOV IVAN; ZHANG LEI; MAKLAD NOHA S; O'SULLIVAN THERESA 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n n n n n n n n n n as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 114. 摘要:Wessjohann, L. A.; Kaluđerović, G. N.; Neves Filho, R. A. W.; Morejon, M. C.; Lemanski, G.; Ziegler, T., Science of Synthesis: Multicomponent Reactions, (2013) 1, 416.