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Biotech / Medical : Indications -- cardiovascular -- Ignore unavailable to you. Want to Upgrade?

To: scaram(o)uche who wrote (32)	5/14/2002 2:57:34 AM
From: scaram(o)uche	Respond to of 214

another work of Shan et al....... FXR MODULATORS Patent Number: WO0220463 Publication date: 2002-03-14 Inventor(s): HOUZE JONATHAN (US); KAYSER FRANK (US); MCKENDRY SHARON (US); SHAN BEI (US); XIA YI (US); GERGELY JOSHUA P (US) Applicant(s): TULARIK INC (US); HOUZE JONATHAN (US); KAYSER FRANK (US); MCKENDRY SHARON (US); SHAN BEI (US); XIA YI (US); GERGELY JOSHUA P (US) Requested Patent: WO0220463 Application Number: WO2001US27239 20010831 Priority Number(s): US20000230585P 20000905; US20000258092P 20001222 IPC Classification: C07C233/75; A61K31/16; A61P35/00; C07C237/22; C07C311/17; C07D241/44; C07D209/48; C07D279/02; C07K14/705 EC Classification: C07C237/22, C07C233/75, C07C311/19, C07C311/29 Equivalents: -------------------------------------------------------------------------------- Abstract -------------------------------------------------------------------------------- The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7 alpha -hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR gamma and PPAR alpha . Thus, compounds described herein are useful in treating other biological activities such as obesity, diabetes, lipid associated disorders, cancer, inflammatory disorders, disorders involving a disrupted or dysfunctional epidermal barrier, and various other metabolic disorders.