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Title:
【発明の名称】シトクロムp450活性に対する光学分子センサ
Document Type and Number:
Japanese Patent JP2002532487
Kind Code:
A
Abstract:
The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods. The optical probe of the invention is a compound having the generic structure Y-L-Q, wherein Y is selected from the group consisting of Q as herein defined, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; L is selected from the group of (-OCR2H)p-, wherein for each p, all R2 are separately selected from the group consisting of a hydrogen atom, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and p is a positive integer no greater than twelve; and Q is a chemical moiety that gives rise to optical properties in its hydroxy or hydroxylate, phenol or phenoxide form that are different from the optical properties that arise from its ether form. Most preferably, p is one, R2 is hydrogen, and Q is the ether form of a phenoxide fluorophore.

Inventors:
Markings, Lewis
Zlocarink, Grego
Application Number:
JP2000588160A
Publication Date:
October 02, 2002
Filing Date:
December 10, 1999
Export Citation:
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Assignee:
Aurora Biosciences Corporation
International Classes:
A61K45/00; A61P43/00; C07D219/06; C07D265/38; C07D311/16; C07D311/82; G01N37/00; C07D493/10; C12Q1/26; (IPC1-7): C07D219/06; A61K45/00; A61P43/00; C07D265/38; C07D311/16; G01N37/00
Domestic Patent References:
JPH09183776A1997-07-15
JPH10507203A1998-07-14
JPS59106300A1984-06-19
JPH11508355A1999-07-21
JPS63501941A1988-08-04
JPH02157273A1990-06-18
Foreign References:
GB2319250A1998-05-20
US5817693A1998-10-06
US5767144A1998-06-16
US5510357A1996-04-23
WO1998052926A21998-11-26
WO1998053790A21998-12-03
CA2506703A11997-09-18
Other References:
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MARY HAASCH, BIOCHEMICAL PHARMACOLOGY, vol. V47 N5, JPN5001024789, 2 March 1994 (1994-03-02), pages 893 - 899, ISSN: 0001893265
GRANT KRAFFT, JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. V110, JPN5001024790, 1988, pages 301 - 303, ISSN: 0001893266
JOURNAL OF MEDICINAL CHEMISTRY, vol. 34, JPN6011018157, 1991, pages 1049 - 1062, ISSN: 0001893267
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MACE, IN VITRO TOXICOLOGY,US,MARY ANN LIBERT, vol. V10 N1, JPN5001024784, 21 March 1997 (1997-03-21), pages 85 - 92, ISSN: 0001893260
R.T.MAYER, BIOCHEMICAL PHARMACOLOGY, vol. V40 N5, JPN5001024785, 1 September 1990 (1990-09-01), pages 1645 - 1655, ISSN: 0001893261
IAN N H WHITE, ANALYTICAL BIOCHEMISTRY, vol. V172 N2, JPN5001024786, 1988, pages 304 - 310, ISSN: 0001893262
JOROEN BUTERS, BIOCHEMICAL PHARMACOLOGY, vol. V46 N9, JPN5001024787, 2 November 1993 (1993-11-02), pages 1577 - 1584, ISSN: 0001893263
Attorney, Agent or Firm:
Nobuyuki Kaneda (2 others)