Title:
NON-STEROIDAL FXR AGONISTS
Document Type and Number:
WIPO Patent Application WO2004046162
Kind Code:
A8
Abstract:
ABSTRACT Potent non-steroidal farnesoid X receptor (FXR) agonists are N-aryl-N-arylmethyl amido and ureido compounds having the chemical structure represented by the following formula (I): INSERT FORMULA wherein E1 is (C1-C8)alkyl, cyclohexyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, phenyl, or NH(C1-C8)alkyl; L1 and L2 are both H, or together form a pi-bond; X1 is C(O), or CH2; Y1 is H, NHZ1, NH(Z2)Z3, or OZ4; aryl moiety A1 is selected from the group of radicals consisting of: INSERT FORMULA A2 and G1 - G11 are as defined in the specification; and T1 and T2 are each independently O, S, NH, or N(C1-C8)alkyl. The FXR agonists are useful as therapeutic agents for the treatment of diseases linked to cholesterol, bile acids, and their metabolism and homeostasis.
Inventors:
NICOLAOU KYRIACOS C (US)
ROECKER ANTHONY J (US)
HUGHES ROBERT (US)
PFEFFERKORN JEFFREY A (US)
ROECKER ANTHONY J (US)
HUGHES ROBERT (US)
PFEFFERKORN JEFFREY A (US)
Application Number:
PCT/US2003/036195
Publication Date:
March 24, 2005
Filing Date:
November 14, 2003
Export Citation:
Assignee:
SCRIPPS RESEARCH INST (US)
NICOLAOU KYRIACOS C (US)
ROECKER ANTHONY J (US)
HUGHES ROBERT (US)
PFEFFERKORN JEFFREY A (US)
NICOLAOU KYRIACOS C (US)
ROECKER ANTHONY J (US)
HUGHES ROBERT (US)
PFEFFERKORN JEFFREY A (US)
International Classes:
C07C233/54; C07C233/63; C07C275/42; C07C323/40; C07C323/41; C07C323/44; C07D277/28; C07D311/04; C07D311/58; C07D317/58; C07D333/20; C07D405/12; C07D409/12; (IPC1-7): C07C233/61
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