抗炎症活性を持つ特定のグルココルチコステロイド化合物

Japanese Patent JP4709751

B2

A process for preparing a compound of formula (I): wherein X represents O or S; R 1 represents C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylmethyl or C 3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R 1 represents aryl, 4-(diethylamino)sulphonylphenyl, 2,6-difluorophenyl, 4-methoxyphenyl, 3-difluoromethylthiophenyl, 4-cyanophenyl, heteroaryl, 5-chloro-4-methoxy-thiophene-3-yl, 2-isopropyl-1,3-thiazol-4-yl, 5-trifluoromethylfuran-2-yl, 5-methylsulphonyl-thiophene-2-yl, 5-methylthio-thiophene-2-yl or 5-ethyl-isoxazol-3-yl; R 2 represents hydrogen, methyl, which may be in either the ± or ² configuration, or methylene; R 3 and R 4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond; or a physiologically acceptable salt or solvate thereof; comprising the reaction of a carboxylic acid (X=O) or carbothioic acid (X=S) of formula (II) wherein R 1 , R 2 , R 3 , R 4 , X and are as defined for formula (I) above; with a compound of formula L-CH 2 CN wherein L represents a leaving group.

Bigger dyke, keith
John, Matthew, Peter
Needham, Deborah

JP2006518180A

June 22, 2011

July 09, 2004

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GLAXO GROUP LIMITED

C07J41/00; A61K9/72; A61K31/569; A61K47/06; A61P1/00; A61P3/04; A61P5/44; A61P11/00; A61P11/02; A61P11/06; A61P17/00; A61P17/04; A61P17/06; A61P27/02; A61P27/16; A61P29/00; A61P37/08; A61P43/00; C07D215/26; C07D233/54; C07D451/02; C07J1/00; C07J3/00

JP2009514781A

WO2003072592A1
GB2137206B
WO2002000679A1
WO1989003390A1
US3856828
GB2079755B
GB1514476B
GB2137206A
GB1384372A

J. Med. Chem.,1994年,Vol.37, No.22,p.3717-3729
JOURNAL OF MEDICINAL CHEMISTRY,米国,AMERICAN CHEMICAL SOCIETY,1991年 8月 1日,V34 N8,P2468-2473

Yusuke Hiraki
Ishii Teiji
Satoshi Fujita

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