WO2003060078A3 - Heterocyclic modulators of nuclear receptors - Google Patents

Heterocyclic modulators of nuclear receptors Download PDF

Info

Publication number
WO2003060078A3
WO2003060078A3 PCT/US2002/041224 US0241224W WO03060078A3 WO 2003060078 A3 WO2003060078 A3 WO 2003060078A3 US 0241224 W US0241224 W US 0241224W WO 03060078 A3 WO03060078 A3 WO 03060078A3
Authority
WO
WIPO (PCT)
Prior art keywords
nuclear receptors
heterocyclic modulators
compounds
heterocyclic
modulating
Prior art date
Application number
PCT/US2002/041224
Other languages
French (fr)
Other versions
WO2003060078A9 (en
WO2003060078A2 (en
WO2003060078A8 (en
Inventor
Richard Martin
Brenton Todd Flatt
Tie-Lin Wang
Jeffery Dean Kahl
Original Assignee
X Ceptor Therapeutics Inc
Richard Martin
Brenton Todd Flatt
Tie-Lin Wang
Jeffery Dean Kahl
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by X Ceptor Therapeutics Inc, Richard Martin, Brenton Todd Flatt, Tie-Lin Wang, Jeffery Dean Kahl filed Critical X Ceptor Therapeutics Inc
Priority to EP02806505A priority Critical patent/EP1465882B1/en
Priority to AU2002367060A priority patent/AU2002367060A1/en
Priority to AT02806505T priority patent/ATE521599T1/en
Publication of WO2003060078A2 publication Critical patent/WO2003060078A2/en
Publication of WO2003060078A9 publication Critical patent/WO2003060078A9/en
Publication of WO2003060078A8 publication Critical patent/WO2003060078A8/en
Publication of WO2003060078A3 publication Critical patent/WO2003060078A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Abstract

Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.
PCT/US2002/041224 2001-12-21 2002-12-20 Heterocyclic modulators of nuclear receptors WO2003060078A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP02806505A EP1465882B1 (en) 2001-12-21 2002-12-20 Hetrocyclic modulators of nuclear receptors
AU2002367060A AU2002367060A1 (en) 2001-12-21 2002-12-20 Heterocyclic modulators of nuclear receptors
AT02806505T ATE521599T1 (en) 2001-12-21 2002-12-20 HETEROCYCLIC MODULATORS OF NUCLEAR RECEPTORS

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34272001P 2001-12-21 2001-12-21
US60/342,720 2001-12-21

Publications (4)

Publication Number Publication Date
WO2003060078A2 WO2003060078A2 (en) 2003-07-24
WO2003060078A9 WO2003060078A9 (en) 2004-02-19
WO2003060078A8 WO2003060078A8 (en) 2004-04-29
WO2003060078A3 true WO2003060078A3 (en) 2004-06-24

Family

ID=23342988

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/041224 WO2003060078A2 (en) 2001-12-21 2002-12-20 Heterocyclic modulators of nuclear receptors

Country Status (6)

Country Link
US (2) US6696473B2 (en)
EP (1) EP1465882B1 (en)
AT (1) ATE521599T1 (en)
AU (1) AU2002367060A1 (en)
ES (1) ES2367539T3 (en)
WO (1) WO2003060078A2 (en)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI279401B (en) * 1999-08-31 2007-04-21 Incyte San Diego Inc Heterocyclic derivatives for the treatment of diabetes and other diseases
ES2367539T3 (en) * 2001-12-21 2011-11-04 X-Ceptor Therapeutics, Inc. HETEROCYCLIC MODULATORS OF NUCLEAR RECEPTORS.
US6987121B2 (en) 2002-04-25 2006-01-17 Smithkline Beecham Corporation Compositions and methods for hepatoprotection and treatment of cholestasis
US20040259948A1 (en) * 2003-01-10 2004-12-23 Peter Tontonoz Reciprocal regulation of inflammation and lipid metabolism by liver X receptors
WO2004113533A1 (en) * 2003-06-24 2004-12-29 Sumitomo Chemical Company, Limited LIVER X RECEPTOR α SPLICING VARIANT PROTEIN, GENE CODING FOR THE SAME AND USE THEREOF
EP1697413A2 (en) * 2003-08-18 2006-09-06 Wyeth Human lxr alpha variants
JP2008509912A (en) * 2004-08-10 2008-04-03 エグゼリクシス， インコーポレイテッド Heterocyclic compounds as pharmaceuticals
JP4553355B2 (en) * 2004-10-04 2010-09-29 富士フイルム株式会社 Pharmaceutical composition for prevention or treatment of Trypanosoma protozoan parasitic infection
US7618956B2 (en) * 2005-05-31 2009-11-17 The Gillette Company Reduction of hair growth
WO2009009139A2 (en) * 2007-07-11 2009-01-15 The General Hospital Corporation Rna ligase polypeptides and methods of selection and use thereof
WO2010045563A2 (en) * 2008-10-16 2010-04-22 Metabolous Pharmaceuticals, Inc. Combination therapies for the treatment of obesity
WO2010045529A2 (en) * 2008-10-16 2010-04-22 Metabolous Pharmaceuticals, Inc. Combination therapies for the treatment of obesity
US20100113583A1 (en) * 2008-10-16 2010-05-06 Aronne Louis J Combination therapies for the treatment of obesity
US20100113603A1 (en) * 2008-10-16 2010-05-06 Aronne Louis J Combination therapies for the treatment of obesity
US20100113580A1 (en) * 2008-10-16 2010-05-06 Aronne Louis J Combination therapies for the treatment of obesity
US20100331419A1 (en) * 2009-06-25 2010-12-30 Aronne Louis J Combination Therapies for the Treatment of Obesity
WO2010151565A2 (en) * 2009-06-26 2010-12-29 Metabolous Pharmaceuticals, Inc. Combination therapies for the treatment of obesity
WO2011008490A2 (en) * 2009-06-29 2011-01-20 Metabolous Pharmaceuticals, Inc. Combination therapies for the treatment of obesity
WO2011009115A2 (en) * 2009-07-17 2011-01-20 Metabolous Pharmaceuticals, Inc. Combination therapies for the treatment of obesity
WO2011041632A2 (en) * 2009-10-01 2011-04-07 Metabolous Pharmaceuticals, Inc. Combination therapies for the treatment of obesity
BR112013005425A2 (en) 2010-09-07 2018-05-02 Snu R&Db Foundation Three master teopin compounds and uses of these materials
JP6366721B2 (en) 2013-09-11 2018-08-01 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル Methods and pharmaceutical compositions for treating hepatitis B virus infection
AU2015204572B2 (en) 2014-01-10 2020-07-30 Inspirna, Inc. LXR agonists and uses thereof
WO2016198908A1 (en) 2015-06-09 2016-12-15 Abbvie Inc. Ror nuclear receptor modulators
JP7025022B2 (en) 2016-01-11 2022-02-24 ザ ロックフェラー ユニバーシティー Methods for the treatment of myeloid-derived inhibitory cell-related disorders
JP2020515564A (en) 2017-03-30 2020-05-28 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル Methods and pharmaceutical compositions for reducing episomal virus persistence and expression
BR112020006659B1 (en) 2017-10-04 2022-01-25 Bayer Aktiengesellschaft Derivatives of heterocyclic compounds, agrochemical formulation, method for controlling one or more animal pests, and product
WO2019104062A1 (en) 2017-11-21 2019-05-31 Rgenix, Inc. Polymorphs and uses thereof
CA3161274A1 (en) 2019-12-13 2021-06-17 Stephen Wald Metal salts and uses thereof
CN111041014B (en) * 2019-12-31 2022-03-18 浙江工业大学 Magnetic immobilized lipase and application thereof in resolution of 1-methyl-3-amphetamine
CN113181160A (en) * 2020-01-14 2021-07-30 无锡杰西医药股份有限公司 Application of isothiocyanate compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6541486B1 (en) * 1999-06-04 2003-04-01 Elan Pharma International Ltd. Bis-benzimidazole compounds and analogs thereof for inhibiting cell death
US6586453B2 (en) * 2000-04-03 2003-07-01 3-Dimensional Pharmaceuticals, Inc. Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1

Family Cites Families (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US228607A (en) * 1880-06-08 Door-hanger
US181420A (en) * 1876-08-22 Improvement in stove-platforms
US132223A (en) * 1872-10-15 Improvement in bale-ties
US120137A (en) * 1871-10-17 Improvement in mill-bolts
GB489335A (en) 1937-01-22 1938-07-22 Douglas James Fry Improvements in or relating to the manufacture and use of dyestuffs suitable for sensitising photographic emulsions
US2454629A (en) 1940-01-27 1948-11-23 Eastman Kodak Co Polymethine dyes
FR1449800A (en) 1964-07-02 1966-05-06 Kodak Pathe New chromatic sensitizing dyes
CA918992A (en) 1968-02-21 1973-01-16 Tsubota Motohiko Direct positive photographic emulsion
US3635964A (en) 1969-02-10 1972-01-18 Colgate Palmolive Co 5-morpholinyl-2 1-benzisothiazolines
US3710795A (en) 1970-09-29 1973-01-16 Alza Corp Drug-delivery device with stretched, rate-controlling membrane
FR2117337A5 (en) 1970-12-04 1972-07-21 Eastman Kodak Co Merocyanine dye sensitisers - contg basic and acidic gps for silver halide emulsions
GB1429184A (en) 1972-04-20 1976-03-24 Allen & Hanburys Ltd Physically anti-inflammatory steroids for use in aerosols
US4044126A (en) 1972-04-20 1977-08-23 Allen & Hanburys Limited Steroidal aerosol compositions and process for the preparation thereof
USRE28819E (en) 1972-12-08 1976-05-18 Syntex (U.S.A.) Inc. Dialkylated glycol compositions and medicament preparations containing same
IT1039699B (en) 1975-07-03 1979-12-10 Prephar SPERMICIDE COMPOSITION BASED ON BENZISOTHIAZOLIC DERIVATIVES
JPS53129633A (en) 1977-04-19 1978-11-11 Fuji Photo Film Co Ltd Silver halide photographic material
US4258185A (en) 1978-10-17 1981-03-24 Yoshitomi Pharmaceutical Industries, Ltd. Pyridazinone compounds
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
MX7065E (en) 1980-06-06 1987-04-10 Sankyo Co A MICROBIOLOGICAL PROCEDURE FOR PREPARING DERIVATIVES OF ML-236B
US4410545A (en) 1981-02-13 1983-10-18 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4328245A (en) 1981-02-13 1982-05-04 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4358603A (en) 1981-04-16 1982-11-09 Syntex (U.S.A.) Inc. Acetal stabilized prostaglandin compositions
US4409239A (en) 1982-01-21 1983-10-11 Syntex (U.S.A.) Inc. Propylene glycol diester solutions of PGE-type compounds
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
AU570021B2 (en) 1982-11-22 1988-03-03 Novartis Ag Analogs of mevalolactone
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
US4721721A (en) 1984-12-18 1988-01-26 Rorer Pharmaceutical Corporation 6-(4-thiazole) compounds, cardiotonic compositions including the same, and their uses
US5583024A (en) 1985-12-02 1996-12-10 The Regents Of The University Of California Recombinant expression of Coleoptera luciferase
US5221623A (en) 1986-07-22 1993-06-22 Boyce Thompson Institute For Plant Research, Inc. Use of bacterial luciferase structural genes for cloning and monitoring gene expression in microorganisms and for tagging and identification of genetically engineered organisms
US5071773A (en) 1986-10-24 1991-12-10 The Salk Institute For Biological Studies Hormone receptor-related bioassays
AU614965B2 (en) 1987-06-06 1991-09-19 Merck Patent Gesellschaft Mit Beschrankter Haftung Thiadiazinones
EP0303418A3 (en) 1987-08-11 1990-11-07 Smithkline Beecham Laboratoires Pharmaceutiques Substituted indolones, useful in the treatment of heart or asthmatic diseases
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5070012A (en) 1988-03-30 1991-12-03 The Board Of Trustees Of The Leland Stanford Junior University Monitoring of cells and trans-activating transcription elements
FI94339C (en) 1989-07-21 1995-08-25 Warner Lambert Co Process for the preparation of pharmaceutically acceptable [R- (R *, R *)] - 2- (4-fluorophenyl) -, - dihydroxy-5- (1-methylethyl) -3-phenyl-4 - [(phenylamino) carbonyl] -1H- for the preparation of pyrrole-1-heptanoic acid and its pharmaceutically acceptable salts
US5683888A (en) 1989-07-22 1997-11-04 University Of Wales College Of Medicine Modified bioluminescent proteins and their use
DE3932953A1 (en) 1989-10-03 1991-04-11 Boehringer Mannheim Gmbh NEW 2-BICYCLO-BENZIMIDAZOLES, METHOD FOR THEIR PRODUCTION AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS
US5283173A (en) 1990-01-24 1994-02-01 The Research Foundation Of State University Of New York System to detect protein-protein interactions
KR0164842B1 (en) 1990-03-24 1999-01-15 손정삼 Novel benzoxazine, benzothiazine derivatives and preparation thereof
TW203049B (en) 1990-04-13 1993-04-01 Yamanouchi Pharma Co Ltd
US5283179A (en) 1990-09-10 1994-02-01 Promega Corporation Luciferase assay method
US5177080A (en) 1990-12-14 1993-01-05 Bayer Aktiengesellschaft Substituted pyridyl-dihydroxy-heptenoic acid and its salts
EP0510235A1 (en) 1991-04-26 1992-10-28 Dong-A Pharm. Co., Ltd. Novel benzoxazine or benzothiazine derivatives and process for the preparation of the same
JPH0527356A (en) 1991-07-23 1993-02-05 Konica Corp Spectrally sensitized silver halide photographic sensitive material
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
JPH0620053A (en) 1992-07-03 1994-01-28 Sankyo Seiki Mfg Co Ltd Pattern recognizing method
JP2879395B2 (en) * 1992-10-26 1999-04-05 富士写真フイルム株式会社 Anticancer composition containing rhodacyanine compound and cyclodextrin
US5618831A (en) * 1992-11-17 1997-04-08 Fuji Photo Film Co., Ltd. Composition and method for treating cancer
US5476945A (en) * 1992-11-17 1995-12-19 Fuji Photo Film Co., Ltd. Water-soluble methine derivatives of thiazole
JPH06234639A (en) * 1993-02-10 1994-08-23 Fuji Photo Film Co Ltd Immunosuppressant
FR2707120B1 (en) 1993-07-02 1995-09-22 Lectra Systemes Sa Clothes grading system.
EP0743520A3 (en) 1993-12-30 1999-11-10 The Salk Institute For Biological Studies Novel uses for GAL4-receptor constructs
JP3466765B2 (en) 1994-07-27 2003-11-17 キッコーマン株式会社 Biotinylated firefly luciferase, biotinylated firefly luciferase gene, novel recombinant DNA, method for producing biotinylated firefly luciferase and bioluminescence analysis method
US6005086A (en) 1995-01-13 1999-12-21 The Salk Institute For Biological Studies Farnesoid activated receptor polypeptides, and nucleic acid encoding the same
US5741657A (en) 1995-03-20 1998-04-21 The Regents Of The University Of California Fluorogenic substrates for β-lactamase and methods of use
AUPN449295A0 (en) * 1995-07-28 1995-08-24 Inner And Eastern Health Care Network, The Radioprotectors
JP2000502988A (en) 1995-08-18 2000-03-14 オークランド ユニサーヴィスィズ リミテッド Radiation-activated cytotoxin therapy
US5955604A (en) 1996-10-15 1999-09-21 The Regents Of The University Of California Substrates for β-lactamase and uses thereof
US5707794A (en) 1996-11-22 1998-01-13 Sterling Diagnostic Imaging, Inc. Spectral sensitization of silver halide photographic elements
US6187797B1 (en) * 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
JP2001509165A (en) 1997-01-24 2001-07-10 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Use of FXR, PPARα and LXRα activators for restoring barrier function, promoting epidermal differentiation and inhibiting proliferation
US7101681B1 (en) 1997-11-21 2006-09-05 Amgen, Inc. Nuclear hormone receptor drug screens
MY153569A (en) 1998-01-20 2015-02-27 Mitsubishi Tanabe Pharma Corp Inhibitors of ?4 mediated cell adhesion
EP0985683A1 (en) 1998-09-09 2000-03-15 Fuji Photo Film Co., Ltd. Photosensitive composition and method for manufacturing lithographic printing plate
WO2000017334A2 (en) 1998-09-23 2000-03-30 Ludmila Solomin Analysis of ligand activated nuclear receptors i(in vivo)
EP1137940A4 (en) 1998-10-23 2004-06-02 Glaxo Group Ltd Assays for ligands for nuclear receptors
ES2326850T3 (en) 1998-12-23 2009-10-20 Glaxo Group Limited TESTS FOR NUCLEAR RECEPTORS LIGANDOS.
US6465258B1 (en) 1999-01-07 2002-10-15 Tularik, Inc. FXR receptor-mediated modulation cholesterol metabolism
ID30514A (en) 1999-01-14 2001-12-13 Bayer Ag 2-ARILIMINO SUBSTITUTIONAL HETEROSICLICS AND COMPOSITION CONTAINING IT, FOR USE AS A PROGESTERON RECEPTOR BINDING SUBSTANCES
US6071955A (en) 1999-02-25 2000-06-06 The Regents Of The University Of California FXR, PPARA and LXRA activators to treat acne/acneiform conditions
US6291676B1 (en) 1999-03-03 2001-09-18 University Of Kentucky Research Foundation Water-soluble derivatives of camptothecin/homocamptothecin
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
DE60029029T2 (en) 1999-03-26 2007-06-14 City Of Hope, Duarte Screen for FXR receptor modulators
US6316510B1 (en) 1999-04-13 2001-11-13 Henry Sperber Foamable binder composition and methods for producing the same
US6452032B1 (en) 1999-06-11 2002-09-17 Allergan Sales, Llc Organosilyl compounds having nuclear hormone receptor modulating activity
CN1368884A (en) 1999-06-11 2002-09-11 阿勒根销售公司 Method for modulating FXR receptor activity
JP2003508031A (en) 1999-06-18 2003-03-04 スィーヴィー セラピューティクス インコーポレイテッド Compositions and methods for increasing cholesterol efflux and elevating HDL using the ATP binding cassette transporter protein ABC1
JP2001013617A (en) 1999-06-29 2001-01-19 Konica Corp Silver halide emulsion, silver halide photosensitive material and heat developable photosensitive material
WO2001017994A1 (en) 1999-09-08 2001-03-15 Glaxo Group Limited Oxazole ppar antagonists
GB2354304A (en) 1999-09-16 2001-03-21 Barrus Ltd E P A valve and a marine propulsion unit incorporating a valve
US6458789B1 (en) 1999-09-29 2002-10-01 Lion Bioscience Ag 2-aminopyridine derivatives and combinatorial libraries thereof
AU2000235960A1 (en) 2000-02-14 2001-08-27 Tularik, Inc. Lxr modulators
AU2001262984A1 (en) 2000-05-03 2001-11-12 Tularik, Inc. Treatment of hypertriglyceridemia and other conditions using lxr modulators
GB0019290D0 (en) 2000-08-04 2000-09-27 Symphar Sa Methods for inducing apolipoprotein E secretion
US6777446B2 (en) 2000-09-05 2004-08-17 Tularik, Inc. FXR modulators
KR20030072614A (en) * 2001-01-31 2003-09-15 화이자 프로덕츠 인크. Thiazolyl-, Oxazolyl-, Pyrrolyl-, and Imidazolyl-Acid Amide Derivatives Useful as Inhibitors of PDE4 Isozymes
CA2469435A1 (en) 2001-12-21 2003-07-24 X-Ceptor Therapeutics, Inc. Modulators of lxr
ES2367539T3 (en) * 2001-12-21 2011-11-04 X-Ceptor Therapeutics, Inc. HETEROCYCLIC MODULATORS OF NUCLEAR RECEPTORS.
US20030228607A1 (en) 2002-04-15 2003-12-11 Wagner Brandee Lynn Screening method and modulators having an improved therapeutic profile

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6541486B1 (en) * 1999-06-04 2003-04-01 Elan Pharma International Ltd. Bis-benzimidazole compounds and analogs thereof for inhibiting cell death
US6586453B2 (en) * 2000-04-03 2003-07-01 3-Dimensional Pharmaceuticals, Inc. Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1

Also Published As

Publication number Publication date
AU2002367060A8 (en) 2003-07-30
ES2367539T3 (en) 2011-11-04
US20030212111A1 (en) 2003-11-13
EP1465882A2 (en) 2004-10-13
AU2002367060A1 (en) 2003-07-30
EP1465882B1 (en) 2011-08-24
US20040180942A1 (en) 2004-09-16
WO2003060078A9 (en) 2004-02-19
US6696473B2 (en) 2004-02-24
WO2003060078A2 (en) 2003-07-24
WO2003060078A8 (en) 2004-04-29
ATE521599T1 (en) 2011-09-15
EP1465882A4 (en) 2005-04-06
US7115640B2 (en) 2006-10-03

Similar Documents

Publication Publication Date Title
WO2003060078A8 (en) Heterocyclic modulators of nuclear receptors
AU2003228283A1 (en) Quinazolinone modulators of nuclear receptors
AU2003294264A1 (en) Non-steroidal farnesoid x receptor modulators and methods for the use thereof
AU2001280597A1 (en) Compositions for sustained release of analgesic agents, and methods of making and using the same
AU2002223185A1 (en) Method for developing business components
EP1569618A4 (en) Methods and compositions for applying pharmacologic agents to the ear
AU2004308299A1 (en) Compounds and methods for development of Ret modulators
EP1536812A4 (en) Methods for modulating activity of the fxr nuclear receptor
FI970328A (en) Heterocyclic compounds, useful as allosteric effectors at muscarinic receptors
TW200607798A (en) Progesterone receptor modulators comprising pyrrole-oxindole derivatives and uses thereof
AU2001279166A1 (en) Network emulator for testing voip connections
EE200100567A (en) Glucocorticoid receptor modulators
IL165990A0 (en) Methods and compositions for modulating T helper (TH) cell development and function
WO2006047269A3 (en) Pharmaceutical compositions
WO2007024744A3 (en) Heterocyclic carboxamide compounds as steroid nuclear receptor ligands
NO20013318D0 (en) Substituted 2-arylimino heterocyclic compounds and preparations containing them for use as progesterone receptor binding agents
WO2002064550A8 (en) Glucocorticoid receptor modulators
AU3196100A (en) Heterocyclic sulfonamide derivatives
AU2001280470A1 (en) Heterocyclic sulfonamide derivatives
AU2003213663A1 (en) Methods and compositions for regulating adipogenesis
EP1453496A4 (en) Composition and method for modulating bar/fxr receptor activity
AU2003218824A1 (en) Benzopyran derivatives substituted with secondary amines including tetrazole, method for the preparation thereof and pharmaceutical compositions containing them
AU2003258050A1 (en) 5-cycloalkenyl 5h-chromeno(3,4-f)quinoline derivatives as selective progesterone receptor modulator compounds
HUP0104588A3 (en) Substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators pharmaceutical compositions comprising thereof, method for their preparation and their use
AU3476599A (en) Indol-3-yl-cyclohexyl amine derivatives for the treatment of depression (5-ht1 receptor antagonists)

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SC SD SE SG SK SL TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR IE IT LU MC NL PT SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
COP Corrected version of pamphlet

Free format text: PAGES 107, 108, 117, 119, 120, 123, 164, 166, 175, 177, 194, 212, 315 AND 316, DESCRIPTION, REPLACED BY NEW PAGES 107, 108, 117, 119, 120, 123, 164, 166, 175, 177, 194, 212, 315 AND 316; AFTER RECTIFICATION OF OBVIOUS ERRORS AUTHORIZED BY THE INTERNATIONAL SEARCH AUTHORITY PAGES 107, 108, 117, 119, 120, 123, 164, 166, 175, 177, 194, 212, 315 ET 316,

CFP Corrected version of a pamphlet front page

Free format text: UNDER (54) PUBLISHED TITLE REPLACED BY CORRECT TITLE

WWE Wipo information: entry into national phase

Ref document number: 2002806505

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 2002806505

Country of ref document: EP

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
NENP Non-entry into the national phase

Ref country code: JP

WWW Wipo information: withdrawn in national office

Country of ref document: JP