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Title:
【発明の名称】コレン酸アミドおよびその医薬組成物
Document Type and Number:
Japanese Patent JP2002505336
Kind Code:
A
Abstract:
Novel sterol derivatives of formula (I), in which: R1 represents a hydroxyl group or protected hydroxyl group, R2 represents a hydrogen atom and a double bond is present at c, or R1 and R2 together represent an oxo group and a double bond is present at b or double bonds are present at a and b; R3 represents a methyl group having alpha- or beta-configuration; R4 and R5, which may be the same or different, are selected from hydrogen atoms and aliphatic, cycloaliphatic, araliphatic and aryl groups, or together with the nitrogen atom to which they are attached form a heterocyclic group; and X represents a polymethylene group containing 2-5 carbon atoms, an oxa group-containing analogue thereof in which a methylene group other than that attached to the -CO.NR4R5 moiety is replaced by an oxygen atom, or an unsaturated analogue thereof containing up to two double bonds. Active compounds of the invention exhibit potent effects on the modulation of cell growth and differentiation and possess an advantageous therapeutic ratio by virtue of their low levels of calcaemic activity.

Inventors:
Robert Henry Hess
Sundara Categum Srinivasa Seti Seti
Marathi Ram Gopal
Application Number:
JP2000534566A
Publication Date:
February 19, 2002
Filing Date:
March 08, 1999
Export Citation:
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Assignee:
Research Institute for Medicine and Chemistry Incorporated
International Classes:
A61P1/04; A61P3/14; A61P5/18; A61P9/12; A61P11/06; A61P17/00; A61P19/02; A61P19/08; A61P21/00; A61P25/28; A61P29/00; A61P31/00; A61P35/00; A61P37/06; C07J41/00; C07J43/00; A61K31/575; (IPC1-7): C07J41/00; A61K31/575; A61P1/04; A61P5/18; A61P9/12; A61P11/06; A61P17/00; A61P19/02; A61P19/08; A61P21/00; A61P25/28; A61P29/00; A61P31/00; A61P35/00; A61P37/06; C07J43/00
Domestic Patent References:
JPH0672994A1994-03-15
Foreign References:
WO1997042215A11997-11-13
Other References:
NAKAGAWA,T. ET AL.: "Biosynthesis of 20-hydroxyecdysone in Ajuga hairy roots: stereochemistry of C-25 hydroxylation", TETRAHEDRON LETTERS, vol. 38, no. 15, JPN6009048878, 1997, pages 2701 - 2704, XP004058308, ISSN: 0001427120, DOI: 10.1016/S0040-4039(97)00433-4
SUCROW,W. ET AL.: "Synthesis of (24S)-ethylcholesta-5,22,25-trien-3β-ol", TETRAHEDRON LETTERS, JPN6009048880, 1971, pages 1883 - 1884, ISSN: 0001427121
KIRCHER,H.W. ET AL.: "Preparation of some unsaturated side chain derivatives of cholesterol", JOURNAL OF ORGANIC CHEMISTRY, vol. 47, no. 9, JPN6009048882, 1982, pages 1722 - 1724, ISSN: 0001427122
Attorney, Agent or Firm:
Chika Takagi (2 outside)