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1. WO2000040965 - FXR RECEPTOR-MEDIATED MODULATION OF CHOLESTEROL METABOLISM

Publication Number WO/2000/040965
Publication Date 13.07.2000
International Application No. PCT/US2000/000431
International Filing Date 06.01.2000
Chapter 2 Demand Filed 17.07.2000
IPC
A61K 31/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
A61K 31/575 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
575substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
G01N 33/68 2006.01
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48Biological material, e.g. blood, urine; Haemocytometers
50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
68involving proteins, peptides or amino acids
G01N 33/92 2006.01
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48Biological material, e.g. blood, urine; Haemocytometers
50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
92involving lipids, e.g. cholesterol
CPC
A61K 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
A61K 31/575
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
575substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
G01N 2333/70567
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
2333Assays involving biological materials from specific organisms or of a specific nature
435from animals; from humans
705Assays involving receptors, cell surface antigens or cell surface determinants
70567Nuclear receptors, e.g. retinoic acid receptor [RAR], RXR, nuclear orphan receptors
G01N 2500/04
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
2500Screening for compounds of potential therapeutic value
04Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
G01N 2800/044
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
2800Detection or diagnosis of diseases
04Endocrine or metabolic disorders
044Hyperlipemia or hypolipemia, e.g. dyslipidaemia, obesity
G01N 33/6872
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
48Biological material, e.g. blood, urine
50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
68involving proteins, peptides or amino acids
6872Intracellular protein regulatory factors and their receptors, e.g. including ion channels
Applicants
  • TULARIK, INC. [US/US]; Two Corporate Drive South San Francisco, CA 94080, US
Inventors
  • SHAN, Bei; US
  • OKAMOTO, Arthur, Y.; US
Agents
  • SMITH, Timothy, L. ; Townsend and Townsend and Crew LLP 8th floor Two Embarcadero Center San Francisco, CA 94111-3834, US
Priority Data
60/115,24907.01.1999US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) FXR RECEPTOR-MEDIATED MODULATION OF CHOLESTEROL METABOLISM
(FR) MODULATION DU METABOLISME DU CHOLESTEROL INDUITE PAR LE RECEPTEUR FXR
Abstract
(EN)
This invention provides methods and compositions that are useful for modulating cholesterol levels in a cell, and for identifying compounds that can tested for ability to modulate cholesterol levels in mammals. $i(In vitro) assays for prescreening to identify candidate therapeutic agents for modulation of cholesterol metabolism are provided. These methods involve analyzing the effect of a test compound on the binding of FXR to a ligand for FXR. Such ligands include, for example, bile acids, coactivators, and corespressors. The methods and compositions involve modulating FXR-mediated expression of genes involved in cholesterol metabolism.
(FR)
La présente invention concerne des procédés et des compositions convenant à la modulation des taux de cholestérol dans une cellule et à l'identification de composés dont on peut tester les capacités de moduler ces taux de cholestérol chez les mammifères. L'invention concerne également des dosages $i(in vitro) de présélection servant à identifier des agents thérapeutiques candidats convenant à la modulation du métabolisme du cholestérol. Ces procédés consistent à analyser les effets d'un composé test sur la fixation de FXR à un ligand du FXR. Parmi ces ligands figurent notamment des acides biliaires, des coactivateurs et des corépresseurs. Ces procédés et ces compositions mettent en oeuvre la modulation de l'expression de gènes impliqués dans le métabolisme du cholestérol induite par FXR.
Also published as
Latest bibliographic data on file with the International Bureau