Bicyclo under construction! The [RhCl(dppp)2]‐catalyzed intramolecular [6+2] cycloisomerization of alkyne–allenylcyclobutanes efficiently produced bicyclo[6.4.0]dodecatriene and bicyclo[6.3.0]undecatriene skeletons (see scheme). Straightforward cleavage of the unfunctionalized simple cyclobutane and construction of the bicyclo[6.m.0] frameworks could be achieved under mild conditions.
Pyrrolidine derivatives as prostaglandin modulators
申请人:Liao Yihua
公开号:US20050176800A1
公开(公告)日:2005-08-11
Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.
PYRROLIDINE DERIVATIVES AS PROSTAGLANDIN MODULATORS
申请人:LIAO Yihua
公开号:US20080114051A1
公开(公告)日:2008-05-15
Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteoporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.
Design and synthesis of an EP2-receptor selective agonist began with the chemical modification of alpha- and omega-chains of butaprost 1a, which exhibits an affinity for the IP-receptor. Two series of prostaglandin (PG) analogues with a 16-hydroxy-17,17-trimethylene moiety as an omega-chain were identified. Among those tested, 4a,b,e,f,h and 6a,b,e,f,h were found to be highly selective EP2-receptor agonists. Structure activity relationships are discussed. (C) 2002 Elsevier Science Ltd. All rights reserved.