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Double bond bridge compounds as modulators for farnesoid X receivers
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
ZHAO, GUOHUA,WU, XIMAO,SISTLA, RAMESH KUMAR,NARAYAN, RISHIKESH,NARA, SUSHEEL JETHANAND,MENG, WEI,JURICA, ELIZABETH ANNE,HUANG, YANTING,CHERUKU, SRINIVAS,ANUMULA, RUSHITH KUMAR,YOON, DAVID S.
申请号:
ARP180103177
公开号:
AR113820A1
申请日:
2018.10.31
申请国别(地区):
AR
年份:
2020
代理人:
摘要:
Formula compound (1),Or stereoisomer, Dow, or acceptable salts or solutions of drugs, all of which are defined according to this definition. These compounds modularize the activity of the farnesoid X (FXR) receiver.Like dying, for example Pharmaceutical ingredients including these compounds, and the use of pharmaceutical compounds and compounds to treat diseases, disorders or diseases associated with FXR deregulation, such as pathological fibrosis, rejection of transplantation, cancer, osteoporosis, and inflammation. 1. Claim 1: a compound characterized by formula (1),Among them, cyclo B is cyclohexane or cyclohexane on five to eight bridges; the polymerization point of 1 or Z is carbon atom; X1 and x8308son are C or N, respectively; x2 and X3 are carbon atoms; x 2 and x 3 are carbon atoms; Every one of themN. 830808,O O O O O S; E 1 and E 3 are respectively a covalent link, O, s, N, n 8310,c.Cr°83090 o Cr8309;-7491;-R8309;-7495;He's o, s, N, 831222,c.Cr°8311O Cr8311;-7491;-R8311;;7495;Where (E1 and E2) or (E3 and E2) form a simple link or two links; provided that the link between (E1 and E2) and (E3 and E2) is not two duplicate links; and there is no more than one E1,E2 and E3 are o, s, n or n831222;This is a covalent link, O, s, Nr. 8310a,-C(s)NH-,e. C83183318323lessor, c831833183323 isotar, c832283318324alquenileno, c83283318324a1, c832283318324a5-6, containing one to four heteroatoms selected from N and S; in these places, tar, isotar, arilo and heteroatom are replaced at the rate of 1830 to 833 respectively;Z was arilo, 6-10 members, 5-10 heterosexuals, 3-10 carbohydrates, 4-10 heterosexuals. Among arilo, heterosexuals, carbocyclo and heterosexuals, 0-5 r1830404 was substituted;Each of them is a covalent link o, s, Nr. 18311,1. In the case of c83321353183232323rentor or c831833183232323heterosexual, use 0-3r1 to replace the lessor and heterosexual;RX es - (CR1 square 7491; R1 square 749595) c833737-rz O-O (CR1 square 7491; R2 74295) c83377rz; e es 0 or 1; RZ se
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