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Title:
METHODS FOR PREPARING SYNTHETIC BILE ACIDS AND COMPOSITIONS COMPRISING THE SAME
Document Type and Number:
WIPO Patent Application WO/2012/047495
Kind Code:
A3
Abstract:
This invention relates generally to methods for preparing certain bile acids from non-mammalian sourced starting materials as well as to synthetic bile acids and compositions comprising such acids wherein the acids are characterized by a different C14 population than naturally occurring bile acids as well as being free from any mammalian pathogens. This invention is also directed to the synthesis of intermediates useful in the synthesis of such bile acids. Accordingly, the C ring of the steroidal scaffold is oxidized to provide a synthetic route and intermediates to DCA. This invention also provides synthetic methods for preparing deoxycholic acid or a salt thereof starting from aromatic steroids such as estrogen, equilenin, and derivatives thereof. This invention is also directed to intermediates such as 12-oxo or delta-9,11-ene steroids as well as novel processes for their preparation. In preferred embodiments, bile acids are provided herein which have substituents on the B-ring and/or D-ring side chain and optionally on the hydroxy group of the A-ring.

Inventors:
MORIARTY, Robert M. (Inc.27200 West Agoura Road, Suite 20, Calabasas CA, 91301, US)
RAO, Photon (Inc.27200 West Agoura Road, Suite 20, Calabasas CA, 91301, US)
Application Number:
US2011/052204
Publication Date:
August 09, 2012
Filing Date:
September 19, 2011
Export Citation:
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Assignee:
KYTHERA BIOPHARMACEUTICALS, INC. (27200 West Agoura Road, Suite 200Calabasas, CA, 91301, US)
MORIARTY, Robert M. (Inc.27200 West Agoura Road, Suite 20, Calabasas CA, 91301, US)
RAO, Photon (Inc.27200 West Agoura Road, Suite 20, Calabasas CA, 91301, US)
International Classes:
C07J21/00; A61K31/56; A61P3/04; C07J9/00; C07J41/00; C07J75/00
Foreign References:
US20100160276A12010-06-24
US7601706B22009-10-13
US4762919A1988-08-09
US3891677A1975-06-24
US4226770A1980-10-07
US5304551A1994-04-19
US4681876A1987-07-21
US6610866B22003-08-26
US20070032464A12007-02-08
Attorney, Agent or Firm:
SWISS, Gerald F. et al. (Foley & Lardner LLP, 975 Page Mill RoadPalo Alto, CA, 94304, US)
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