176508-81-9Relevant articles and documents
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity
Hangeland, Jon J.,Friends, Todd J.,Rossi, Karen A.,Smallheer, Joanne M.,Wang, Cailan,Sun, Zhong,Corte, James R.,Fang, Tianan,Wong, Pancras C.,Rendina, Alan R.,Barbera, Frank A.,Bozarth, Jeffrey M.,Luettgen, Joseph M.,Watson, Carol A.,Zhang, Ge,Wei, Anzhi,Ramamurthy, Vidhyashankar,Morin, Paul E.,Bisacchi, Gregory S.,Subramaniam, Srinath,Arunachalam, Piramanayagam,Mathur, Arvind,Seiffert, Dietmar A.,Wexler, Ruth R.,Quan, Mimi L.
, p. 9915 - 9932 (2015/02/05)
Novel inhibitors of FXIa containing an (S)-2-phenyl-1-(4-phenyl-1H-imidazol-2-yl)ethanamine core have been optimized to provide compound 16b, a potent, reversible inhibitor of FXIa (Ki = 0.3 nM) having in vivo antithrombotic efficacy in the rabbit AV-shunt thrombosis model (ID50 = 0.6 mg/kg + 1 mg kg-1 h-1). Initial analog selection was informed by molecular modeling using compounds 11a and 11h overlaid onto the X-ray crystal structure of tetrahydroquinoline 3 complexed to FXIa. Further optimization was achieved by specific modifications derived from careful analysis of the X-ray crystal structure of the FXIa/11h complex. Compound 16b was well tolerated and enabled extensive pharmacologic evaluation of the FXIa mechanism up to the ID90 for thrombus inhibition.
HETEROCYCLIC CARBONYL COMPOUNDS
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Page/Page column 59-60, (2008/06/13)
The invention relates to novel heterocyclic compounds of formula (I) wherein R1, D, W, T and T' have the meaning cited in the claim 1. Said compounds are SGK-inhibitors and can be used in the treatment of SGK-related diseases and disorders such as diabetes, obesity, metabolic syndrome (dyslipidemia), systemic and pulmonal hypertension, cardiovascular diseases and renal diseases, and generally for any kind of fibroses and inflammatory processes.
3-AMINOINDAZOLES
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Page/Page column 68, (2008/06/13)
Novel 3-aminoindazoles of formula (I) are SGK-inhibitors and can be used for treating SGK-related diseases and illnesses such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, and generally any type of fibroses and inflammatory processes.