WO2009074969A3 - Spingosine-1-phosphate, analogues and antagonists for use as medicaments - Google Patents

Spingosine-1-phosphate, analogues and antagonists for use as medicaments Download PDF

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Publication number
WO2009074969A3
WO2009074969A3 PCT/IB2008/055253 IB2008055253W WO2009074969A3 WO 2009074969 A3 WO2009074969 A3 WO 2009074969A3 IB 2008055253 W IB2008055253 W IB 2008055253W WO 2009074969 A3 WO2009074969 A3 WO 2009074969A3
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Prior art keywords
treating
vascular
phosphate
antagonists
present
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PCT/IB2008/055253
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French (fr)
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WO2009074969A2 (en
Inventor
Noureddine Brakch
Frédéric BARBEY
Daniel Jean-Louis Hayoz
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University Of Lausanne
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Publication of WO2009074969A2 publication Critical patent/WO2009074969A2/en
Publication of WO2009074969A3 publication Critical patent/WO2009074969A3/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/47—Hydrolases (3) acting on glycosyl compounds (3.2), e.g. cellulases, lactases
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/92—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving lipids, e.g. cholesterol, lipoproteins, or their receptors
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening 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)
    • 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/32—Cardiovascular disorders
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/32—Cardiovascular disorders
    • G01N2800/323—Arteriosclerosis, Stenosis

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Microbiology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to compounds for treating and/or preventing cardiac and/or vascular symptoms in individuals suffering from Fabry disease. More generally, the present invention relates to compounds treating and/or preventing vascular and/or cardiac hypertrophy and/or hyperplasia, in particular in smooth muscle tissue / cells, such as vascular smooth muscle tissue. The present invention uses antagonists of sphingosine-1 -phosphate (SlP) for treating cardiac and vascular hypertrophy and/or hyperplasia, and SlP and its agonists for treating and/or preventing atherosclerosis.
PCT/IB2008/055253 2007-12-12 2008-12-12 Sphingosine-1-phosphate, analogs and antagonists for use as medicaments WO2009074969A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US731707P 2007-12-12 2007-12-12
US61/007,317 2007-12-12

Publications (2)

Publication Number Publication Date
WO2009074969A2 WO2009074969A2 (en) 2009-06-18
WO2009074969A3 true WO2009074969A3 (en) 2009-12-23

Family

ID=40456289

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2008/055253 WO2009074969A2 (en) 2007-12-12 2008-12-12 Sphingosine-1-phosphate, analogs and antagonists for use as medicaments

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Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ599595A (en) 2009-09-29 2014-03-28 Allergan Inc Condensed ring pyridine compounds as subtype-selective modulators of sphingosine-1-phosphate-2 (s1p2) receptors
EP2598126A2 (en) 2010-07-30 2013-06-05 Saint Louis University Methods of treating pain
FR2968556B1 (en) * 2010-12-13 2013-12-27 Centre Nat Rech Scient INHIBITORS OF HIV INFECTIONS AND USES THEREOF
EP2685971A2 (en) * 2011-03-18 2014-01-22 University Of Virginia Patent Foundation Compositions and methods for tissue engineering and cell based therapies
CA2953208C (en) 2014-06-02 2022-05-10 Dalhousie University Treatment of familial exudative vitreoretinopathy through s1pr2 inhibition
EP3154580B1 (en) 2014-06-12 2020-03-25 Andremacon S.r.l. Use of negative functional modulators of erythropoietin for therapy
JP6834098B2 (en) * 2015-06-01 2021-02-24 ダルハウジー ユニバーシティー S1PR2 antagonist and its use
US10487082B2 (en) 2015-06-01 2019-11-26 Dalhousie University S1PR2 antagonists and uses therefor
US10858358B2 (en) 2015-06-01 2020-12-08 Dalhousie University S1PR2 antagonists and uses therefor

Citations (10)

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Publication number Priority date Publication date Assignee Title
EP1325904A1 (en) * 2000-10-12 2003-07-09 Maruha Corporation Novel aliphatic compounds, process for their preparation and their usage
EP1522314A1 (en) * 2002-06-26 2005-04-13 Ono Pharmaceutical Co., Ltd. Remedies for diseases caused by vascular contraction or dilation
WO2006010379A1 (en) * 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
WO2006063033A2 (en) * 2004-12-06 2006-06-15 University Of Virginia Patent Foundation Aryl amide sphingosine 1-phosphate analogs
EP1698375A1 (en) * 2003-12-25 2006-09-06 Ono Pharmaceutical Co., Ltd. Azetidine ring compounds and drugs comprising the same
WO2007043568A1 (en) * 2005-10-12 2007-04-19 Toa Eiyo Ltd. S1p3 receptor antagonist
US20070167425A1 (en) * 2003-08-29 2007-07-19 Shinji Nakade Compound capable of binding s1p receptor and pharmaceutical use thereof
WO2007095561A2 (en) * 2006-02-15 2007-08-23 Allergan, Inc. Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (s1p) receptor antagonist biological activity
WO2007122401A1 (en) * 2006-04-21 2007-11-01 Astrazeneca Ab Imidazole derivatives for use as edg-1 antagonists
WO2008141013A1 (en) * 2007-05-08 2008-11-20 Allergan, Inc. S1p3 receptor inhibitors for treating pain

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1325904A1 (en) * 2000-10-12 2003-07-09 Maruha Corporation Novel aliphatic compounds, process for their preparation and their usage
EP1522314A1 (en) * 2002-06-26 2005-04-13 Ono Pharmaceutical Co., Ltd. Remedies for diseases caused by vascular contraction or dilation
US20070167425A1 (en) * 2003-08-29 2007-07-19 Shinji Nakade Compound capable of binding s1p receptor and pharmaceutical use thereof
EP1698375A1 (en) * 2003-12-25 2006-09-06 Ono Pharmaceutical Co., Ltd. Azetidine ring compounds and drugs comprising the same
WO2006010379A1 (en) * 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
WO2006063033A2 (en) * 2004-12-06 2006-06-15 University Of Virginia Patent Foundation Aryl amide sphingosine 1-phosphate analogs
WO2007043568A1 (en) * 2005-10-12 2007-04-19 Toa Eiyo Ltd. S1p3 receptor antagonist
WO2007095561A2 (en) * 2006-02-15 2007-08-23 Allergan, Inc. Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (s1p) receptor antagonist biological activity
WO2007122401A1 (en) * 2006-04-21 2007-11-01 Astrazeneca Ab Imidazole derivatives for use as edg-1 antagonists
WO2008141013A1 (en) * 2007-05-08 2008-11-20 Allergan, Inc. S1p3 receptor inhibitors for treating pain

Non-Patent Citations (5)

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Title
BARBEY FRÉDÉRIC ET AL: "Cardiac and vascular hypertrophy in Fabry disease: evidence for a new mechanism independent of blood pressure and glycosphingolipid deposition.", ARTERIOSCLEROSIS, THROMBOSIS, AND VASCULAR BIOLOGY APR 2006, vol. 26, no. 4, April 2006 (2006-04-01), pages 839 - 844, XP002536065, ISSN: 1524-4636 *
IKEDA H ET AL: "Sphingosine 1-phosphate enhances portal pressure in isolated perfused liver via S1P2 with Rho activation", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ACADEMIC PRESS INC. ORLANDO, FL, US, vol. 320, no. 3, 30 July 2004 (2004-07-30), pages 754 - 759, XP004518014, ISSN: 0006-291X *
ROBERT PHILIPPE ET AL: "EDG1 receptor stimulation leads to cardiac hypertrophy in rat neonatal myocytes", JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY, vol. 33, no. 9, September 2001 (2001-09-01), pages 1589 - 1606, XP002453937, ISSN: 0022-2828 *
WAMHOFF BRIAN R ET AL: "Pharmacological inhibition of the sphingosine-1-phosphate receptors type 1 and type 3 with VPC44116 prevents neointimal hyperplasia in the rat carotid artery injury model.", CIRCULATION, vol. 114, no. 18, Suppl. S, October 2006 (2006-10-01), & 79TH ANNUAL SCIENTIFIC SESSION OF THE AMERICAN-HEART-ASSOCIATION; CHICAGO, IL, USA; NOVEMBER 12 -15, 2006, pages 216, XP008108099, ISSN: 0009-7322 *
ZHU RAN ET AL: "Asymmetric synthesis of conformationally constrained Fingolimod analogues - Discovery of an orally active sphingosine 1-Phosphate receptor type-1 agonist and receptor type-3 antagonist", JOURNAL OF MEDICINAL CHEMISTRY, vol. 50, no. 25, 11 October 2007 (2007-10-11), pages 6428 - 6435, XP008108140, ISSN: 0022-2623 *

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