WO2004024939A3 - Ligands for the peroxisome proliferator-activated receptor, and methods of use thereof - Google Patents

Ligands for the peroxisome proliferator-activated receptor, and methods of use thereof Download PDF

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Publication number
WO2004024939A3
WO2004024939A3 PCT/US2003/028931 US0328931W WO2004024939A3 WO 2004024939 A3 WO2004024939 A3 WO 2004024939A3 US 0328931 W US0328931 W US 0328931W WO 2004024939 A3 WO2004024939 A3 WO 2004024939A3
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WO
WIPO (PCT)
Prior art keywords
relates
certain embodiments
activated receptor
peroxisome proliferator
compounds
Prior art date
Application number
PCT/US2003/028931
Other languages
French (fr)
Other versions
WO2004024939A2 (en
Inventor
Alan P Kozikowski
Robert I Glazer
Pavel Petukhov
Zhi-Liang Wei
Original Assignee
Univ Georgetown
Alan P Kozikowski
Robert I Glazer
Pavel Petukhov
Zhi-Liang Wei
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 Univ Georgetown, Alan P Kozikowski, Robert I Glazer, Pavel Petukhov, Zhi-Liang Wei filed Critical Univ Georgetown
Priority to AU2003278814A priority Critical patent/AU2003278814A1/en
Publication of WO2004024939A2 publication Critical patent/WO2004024939A2/en
Publication of WO2004024939A3 publication Critical patent/WO2004024939A3/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

One aspect of the present invention relates to compounds that are active at a peroxisome proliferator-activated receptor (PPAR). In certain embodiments, the compound has a isoxazole or indole core. Another aspect of the present invention relates to a method of treating a mammal afflicted with cancer or non-insulin-dependent (type II) diabetes by administering a therapeutic amount of the compounds of the invention. In certain embodiments, the invention relates to a method of treating prostrate, stomach, or breast cancer. Another aspect of the invention relates to a method of identifying ligands active at a PPAR subtype using X-ray structural information. In certain embodiments, the method of identifying the ligand comprises using molecular modeling approaches including: in silico screening of chemical databases, de novo/rational drug design in which the ligand will be created computationally, and/or in silico screening of virtual combinatorial libraries.
PCT/US2003/028931 2002-09-13 2003-09-12 Ligands for the peroxisome proliferator-activated receptor, and methods of use thereof WO2004024939A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003278814A AU2003278814A1 (en) 2002-09-13 2003-09-12 Ligands for the peroxisome proliferator-activated receptor, and methods of use thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US41067702P 2002-09-13 2002-09-13
US60/410,677 2002-09-13

Publications (2)

Publication Number Publication Date
WO2004024939A2 WO2004024939A2 (en) 2004-03-25
WO2004024939A3 true WO2004024939A3 (en) 2004-10-14

Family

ID=31994180

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/028931 WO2004024939A2 (en) 2002-09-13 2003-09-12 Ligands for the peroxisome proliferator-activated receptor, and methods of use thereof

Country Status (2)

Country Link
AU (1) AU2003278814A1 (en)
WO (1) WO2004024939A2 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2529154C (en) 2003-06-20 2013-05-07 Galderma Research & Development, S.N.C. Novel compounds that modulate ppar.gamma. type receptors, and use thereof in cosmetic or pharmaceutical compositions
GB0403864D0 (en) 2004-02-20 2004-03-24 Ucl Ventures Modulator
BRPI0511099A (en) * 2004-05-14 2007-12-26 Irm Llc compounds and compositions as modulators of ppar
DK1852433T3 (en) 2004-10-29 2012-01-30 Zeria Pharm Co Ltd Carbazole derivatives, solvates thereof or pharmaceutically acceptable salt thereof
WO2006053791A2 (en) * 2004-11-19 2006-05-26 Galderma Research & Development Compounds that modulate ppary type receptors, and use thereof in cosmetic or pharmaceutical compositions
FR2878247B1 (en) * 2004-11-19 2008-10-03 Galderma Res & Dev NOVEL MODULATING COMPOUNDS OF PPARY RECEPTORS AND THEIR USE IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
TW200811164A (en) * 2006-05-12 2008-03-01 Jerini Ag New heterocyclic compounds for the inhibition of integrins and use thereof
US8044236B2 (en) 2006-10-12 2011-10-25 Institute Of Medicinal Molecular Design, Inc. Carboxilic acid derivatives
US8633245B2 (en) 2008-04-11 2014-01-21 Institute Of Medicinal Molecular Design, Inc. PAI-1 inhibitor
RU2010145916A (en) * 2008-04-11 2012-05-20 Инститьют Оф Медисинал Молекьюлар Дизайн, Инк. (Jp) PAI-1 INHIBITOR
JP5746864B2 (en) 2008-11-19 2015-07-08 ポーラ化成工業株式会社 Wrinkle improving agent
US8987514B2 (en) 2009-02-04 2015-03-24 President And Fellows Of Harvard College Compositions and methods for labeling and imaging phospholipids
KR20220162116A (en) * 2021-05-25 2022-12-07 주식회사 자이메디 Novel compounds inhibiting the binding between AIMP2-DX2 and KRAS and their uses

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 12, no. 16, 2002, pages 2141 - 2144 *
DATABASE CAPLUS [online] BING ET AL: "N-(arylacetyl)-biphenylalanines as Potent VLA-4 antagonists", Database accession no. 2002:543694 *

Also Published As

Publication number Publication date
WO2004024939A2 (en) 2004-03-25
AU2003278814A1 (en) 2004-04-30
AU2003278814A8 (en) 2004-04-30

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