专利号:US-12358903-B2 优先权日:2016-06-13 标题 :FXR (NR1H4) modulating compounds 发明人:BLOMGREN PETER A; CURRIE KEVIN S; FARAND JULIE; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN 权利人:GILEAD SCIENCES INC 摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
专利号:US-8952042-B2 优先权日:2009-08-19 标 题 :FXR (NR1H4) binding and activity modulating compounds 发明人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF 权利人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF; PHENEX PHARMACEUTICALS AG 摘要:The present invention relates to compounds of formula (1): n nwhere R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
专利号:US-8378104-B2 优先权日:2010-02-11 标 题 :7-aminofuropyridine derivatives 发明人:HORNBERGER KEITH R; BERGER DAN M; CHEN XIN; CREW ANDREW P; DONG HANQING; KLEINBERG ANDREW; LI AN-HU; MA LIFU; MULVIHILL MARK J; PANICKER BIJOY; SIU KAM W; STEINIG ARNO G; TARRANT JAMES G; WANG JING; WENG QINGHUA; SANGEM RAJARAM; GUPTA RAMESH C 权利人:OSI PHARMACEUTICALS LLC; HORNBERGER KEITH R; BERGER DAN M; CHEN XIN; CREW ANDREW P; DONG HANQING; KLEINBERG ANDREW; LI AN-HU; MA LIFU; MULVIHILL MARK J; PANICKER BIJOY; SIU KAM W; STEINIG ARNO G; TARRANT JAMES G; WANG JING; WENG QINGHUA; SANGEM RAJARAM; GUPTA RAMESH C 摘要:Compounds of Formula 1, as shown below and defined herein: n n n n n n n n n n n n pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.