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Title:
グルココルチコイド受容体アゴニストとしてのC-21チオエーテル
Document Type and Number:
Japanese Patent JP2011507879
Kind Code:
A
Abstract:
The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activity. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.

Inventors:
Antes, John Sea.
McCormick, Kevin Dee.
Hey, John A.
Aslanian, Robert G.
Biju, Praccat Le Jay.
Berlin, Michael Wye.
Solomon, Daniel M.
Application Number:
JP2010539763A
Publication Date:
March 10, 2011
Filing Date:
December 18, 2008
Export Citation:
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Assignee:
Schering Corporation
International Classes:
C07J31/00; A61K31/573; A61K31/58; A61K45/00; A61P1/04; A61P11/00; A61P11/02; A61P11/04; A61P11/06; A61P17/00; A61P17/04; A61P17/06; A61P19/02; A61P25/00; A61P27/02; A61P29/00; A61P37/02; A61P37/08; A61P43/00; C07J43/00; C07J71/00
Domestic Patent References:
JP2008546694A2008-12-25
JPS5030863A1975-03-27
JPH11501676A1999-02-09
JPS6289694A1987-04-24
JP2011507878A2011-03-10
Foreign References:
US5420120A1995-05-30
Other References:
JPN6013038029; Chemical & Pharmaceutical Bulletin 37(7), 1989, 1795-1801
JPN6013038031; Chemical & Pharmaceutical Bulletin 37(12), 1989, 3286-3293
JPN6013038017; Biochemistry 18(22), 1979, 4915-4922
JPN6013038019; Steroids 18(4), 1971, 421-432
JPN6013038022; Biochemical Pharmacology 12, 1963, 1081-1090
JPN6013038024; Journal of the Chemical Society 26, 1961, 5052-5054
JPN6013038026; Journal of Medicinal Chemistry 12(5), 1969, 810-818
Attorney, Agent or Firm:
Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita