WO2003106632A3 - Inhibiteurs de l'activite genique inflammatoire et de la synthese de cholesterol - Google Patents

Inhibiteurs de l'activite genique inflammatoire et de la synthese de cholesterol Download PDF

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Publication number
WO2003106632A3
WO2003106632A3 PCT/US2003/018651 US0318651W WO03106632A3 WO 2003106632 A3 WO2003106632 A3 WO 2003106632A3 US 0318651 W US0318651 W US 0318651W WO 03106632 A3 WO03106632 A3 WO 03106632A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
gene activity
cholesterol biosynthesis
inflammatory gene
methods
Prior art date
Application number
PCT/US2003/018651
Other languages
English (en)
Other versions
WO2003106632A2 (fr
Inventor
Mark J Evans
Douglas C Harnish
Original Assignee
Wyeth Corp
Mark J Evans
Douglas C Harnish
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
Priority to JP2004513445A priority Critical patent/JP2006505249A/ja
Application filed by Wyeth Corp, Mark J Evans, Douglas C Harnish filed Critical Wyeth Corp
Priority to CA002489594A priority patent/CA2489594A1/fr
Priority to EP03760319A priority patent/EP1560925A4/fr
Priority to EA200500012A priority patent/EA200500012A1/ru
Priority to US10/517,695 priority patent/US20050221328A1/en
Priority to BRPI0311772-3A priority patent/BR0311772A/pt
Priority to KR10-2004-7020311A priority patent/KR20050010916A/ko
Priority to AU2003247525A priority patent/AU2003247525A1/en
Priority to MXPA04012560A priority patent/MXPA04012560A/es
Priority to IL16569203A priority patent/IL165692A0/xx
Publication of WO2003106632A2 publication Critical patent/WO2003106632A2/fr
Publication of WO2003106632A3 publication Critical patent/WO2003106632A3/fr
Priority to NO20045536A priority patent/NO20045536L/no

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/0004—Oxidoreductases (1.)
    • C12N9/0071—Oxidoreductases (1.) acting on paired donors with incorporation of molecular oxygen (1.14)
    • C12N9/0073—Oxidoreductases (1.) acting on paired donors with incorporation of molecular oxygen (1.14) with NADH or NADPH as one donor, and incorporation of one atom of oxygen 1.14.13
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4702—Regulators; Modulating activity
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70567—Nuclear receptors, e.g. retinoic acid receptor [RAR], RXR, nuclear orphan receptors
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6897—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids involving reporter genes operably linked to promoters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/04—Endocrine or metabolic disorders
    • G01N2800/044—Hyperlipemia or hypolipemia, e.g. dyslipidaemia, obesity

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Immunology (AREA)
  • General Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Physics & Mathematics (AREA)
  • Biomedical Technology (AREA)
  • High Energy & Nuclear Physics (AREA)
  • Cell Biology (AREA)
  • Analytical Chemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)

Abstract

L'invention concerne des procédés pour identifier des agents efficaces en tant qu'inhibiteurs de la protéine d'hétérodimère courte (SHP) et du récepteur X farnésoïde (FXR) et promoteurs ainsi que des lignes cellulaires et vecteurs utilisés dans ces procédés. Les procédés de préparation et d'utilisation d'agents efficaces en tant qu'inhibiteurs de la protéine d'hétérodimère courte (SHP), y compris les procédés d'utilisation de ces procédés dans la prévention et/ou le traitement d'un état associé à l'activité de gène inflammatoire et/ou la biosynthèse de cholestérol chez un sujet. L'invention concerne des agents efficaces en tant qu'inhibiteurs de la protéine d'hétérodimère courte (SHP) et du récepteur X farnésoïde (FXR) ainsi que les compositions qu'ils comprennent, y compris les compositions efficaces pour réduire l'activité génique inflammatoire et/ou la biosynthèse de cholestérol chez un sujet.
PCT/US2003/018651 2002-06-13 2003-06-13 Inhibiteurs de l'activite genique inflammatoire et de la synthese de cholesterol WO2003106632A2 (fr)

Priority Applications (11)

Application Number Priority Date Filing Date Title
BRPI0311772-3A BR0311772A (pt) 2002-06-13 2003-06-13 inibidores da atividade do gene inflamatório e da biossìntese do colesterol
CA002489594A CA2489594A1 (fr) 2002-06-13 2003-06-13 Inhibiteurs de l'activite genique inflammatoire et de la synthese de cholesterol
EP03760319A EP1560925A4 (fr) 2002-06-13 2003-06-13 Inhibiteurs de l'activite genique inflammatoire et de la synthese de cholesterol
EA200500012A EA200500012A1 (ru) 2002-06-13 2003-06-13 Ингибиторы активности генов воспаления и биосинтеза холестерина
US10/517,695 US20050221328A1 (en) 2002-06-13 2003-06-13 Inhibitors of inflammatory gene activity and cholesterol biosynthesis
JP2004513445A JP2006505249A (ja) 2002-06-13 2003-06-13 炎症遺伝子活性およびコレステロール生合成の阻害剤
KR10-2004-7020311A KR20050010916A (ko) 2002-06-13 2003-06-13 염증 유전자 활성 및 콜레스테롤 생합성의 억제제
IL16569203A IL165692A0 (en) 2002-06-13 2003-06-13 Inhibitors of inflammatory gene activity and cholesterol biosynthesis
MXPA04012560A MXPA04012560A (es) 2002-06-13 2003-06-13 Inhibidores de la actividad genica inflamatoria y biosintesis de colesterol.
AU2003247525A AU2003247525A1 (en) 2002-06-13 2003-06-13 Inhibitors of inflammatory gene activity and cholesterol biosynthesis
NO20045536A NO20045536L (no) 2002-06-13 2004-12-17 Inhibitorer av inflammatorisk genaktivitet og kolesterol-biosyntese

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US38791502P 2002-06-13 2002-06-13
US60/387,915 2002-06-13
USNONE 2006-06-19

Publications (2)

Publication Number Publication Date
WO2003106632A2 WO2003106632A2 (fr) 2003-12-24
WO2003106632A3 true WO2003106632A3 (fr) 2004-06-10

Family

ID=29736382

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/018651 WO2003106632A2 (fr) 2002-06-13 2003-06-13 Inhibiteurs de l'activite genique inflammatoire et de la synthese de cholesterol

Country Status (4)

Country Link
AU (1) AU2003247525A1 (fr)
IL (1) IL165692A0 (fr)
WO (1) WO2003106632A2 (fr)
ZA (1) ZA200500296B (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060233873A1 (en) * 2003-01-24 2006-10-19 Julien Meissonnier Dispersion of taste masked crystals or granules of active substances, chewable soft capsules filled with said dispersion, and process for preparing same

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030083484A1 (en) * 2001-07-31 2003-05-01 Crooke Rosanne M. Antisense modulation of short heterodimer partner-1 expression
WO2003044167A2 (fr) * 2001-11-15 2003-05-30 Isis Pharmaceuticals, Inc. Modulation antisens destinee a l'expression d'un recepteur fxr humain

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030083484A1 (en) * 2001-07-31 2003-05-01 Crooke Rosanne M. Antisense modulation of short heterodimer partner-1 expression
WO2003044167A2 (fr) * 2001-11-15 2003-05-30 Isis Pharmaceuticals, Inc. Modulation antisens destinee a l'expression d'un recepteur fxr humain

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
CHEN ET AL.: "Nuclear receptor-mediated repression of human cholesterol 7-alpha hydroxylase gene transcription by bile acids", JOURNAL OF LIPID RESEARCH, vol. 42, 2001, pages 1402 - 1412, XP002970739 *
CUI ET AL.: "Guggelsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 278, 13 January 2003 (2003-01-13), pages 10214 - 10220, XP002970742 *
GOODWIN ET AL.: "A regulatory cascade of the nuclear receptors FXR, SHP-1 and LRH-1 represses bile acid biosynthesis", MOLECULAR CELL, vol. 6, 2000, pages 517 - 526, XP002209573 *
LAI ET AL.: "Estrogen receptor alpha regulates expression of the orphan receptor small heterodimer partner", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 278, 2 July 2003 (2003-07-02), pages 36418 - 36429, XP002970741 *
PARKS ET AL.: "Bile acids: Natural ligands for an orphan nuclear receptor", SCIENCE, vol. 284, 1999, pages 1365 - 1368, XP002927559 *
TU ET AL.: "FXR, a bile acid receptor and biological sensor", TRENDS IN CARDIOVASCULAR MEDICINE, vol. 10, 2000, pages 30 - 35, XP002970740 *

Also Published As

Publication number Publication date
IL165692A0 (en) 2006-01-15
WO2003106632A2 (fr) 2003-12-24
AU2003247525A1 (en) 2003-12-31
ZA200500296B (en) 2005-11-01

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