WO2011159550A3 - Lysophosphatidic acid receptor antagonist and uses thereof - Google Patents

Lysophosphatidic acid receptor antagonist and uses thereof Download PDF

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Publication number
WO2011159550A3
WO2011159550A3 PCT/US2011/039872 US2011039872W WO2011159550A3 WO 2011159550 A3 WO2011159550 A3 WO 2011159550A3 US 2011039872 W US2011039872 W US 2011039872W WO 2011159550 A3 WO2011159550 A3 WO 2011159550A3
Authority
WO
WIPO (PCT)
Prior art keywords
antagonist
lpal
pharmaceutically acceptable
receptor antagonist
acid receptor
Prior art date
Application number
PCT/US2011/039872
Other languages
French (fr)
Other versions
WO2011159550A2 (en
Inventor
Jason Edward Brittain
Thomas Jon Seiders
Christopher David King
Original Assignee
Amira Pharmaceuticals, Inc.
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 Amira Pharmaceuticals, Inc. filed Critical Amira Pharmaceuticals, Inc.
Publication of WO2011159550A2 publication Critical patent/WO2011159550A2/en
Publication of WO2011159550A3 publication Critical patent/WO2011159550A3/en

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Classifications

    • 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
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—Poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Pulmonology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Dermatology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Described herein is the LPAl antagonist {4'-[3-methyl-4-((R)-l-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-acetic acid (Compound 1), including pharmaceutically acceptable salts thereof. Also described are methods of preparing the LPAl antagonist, or pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions suitable for administration to a mammal that include the LPAl antagonist, or pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating LPA-dependent or LPA-mediated diseases or conditions.
PCT/US2011/039872 2010-06-14 2011-06-09 Lysophosphatidic acid receptor antagonist and uses thereof WO2011159550A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US35462210P 2010-06-14 2010-06-14
US61/354,622 2010-06-14

Publications (2)

Publication Number Publication Date
WO2011159550A2 WO2011159550A2 (en) 2011-12-22
WO2011159550A3 true WO2011159550A3 (en) 2012-04-05

Family

ID=45348798

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/039872 WO2011159550A2 (en) 2010-06-14 2011-06-09 Lysophosphatidic acid receptor antagonist and uses thereof

Country Status (1)

Country Link
WO (1) WO2011159550A2 (en)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20140879A1 (en) * 2010-12-07 2014-08-06 Amira Pharmaceuticals Inc LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS FOR THE TREATMENT OF FIBROSIS
EP2744807A4 (en) 2011-08-15 2015-03-04 Intermune Inc Lysophosphatidic acid receptor antagonists
MA37762B1 (en) * 2012-06-20 2018-04-30 Hoffmann La Roche N-aryltriazole compounds used as antagonists of lpar
US9321738B2 (en) * 2012-06-20 2016-04-26 Hoffman-La Roche Inc. N-alkyltriazole compounds as LPAR antagonists
WO2014058744A2 (en) 2012-10-09 2014-04-17 California Institute Of Technology In vivo and in vitro olefin cyclopropanation catalyzed by heme enzymes
WO2014058729A1 (en) * 2012-10-09 2014-04-17 California Institute Of Technology In vivo and in vitro carbene insertion and nitrene transfer reactions catalyzed by heme enzymes
US9399762B2 (en) 2014-02-18 2016-07-26 California Institute Of Technology Methods and systems for sulfimidation or sulfoximidation of organic molecules
US10118904B2 (en) 2015-06-05 2018-11-06 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of Demyelinating Diseases
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
AU2020384883B2 (en) 2019-11-15 2023-11-16 Gilead Sciences, Inc. Triazole carbamate pyridyl sulfonamides as LPA receptor antagonists and uses thereof
JP2023529369A (en) 2020-06-03 2023-07-10 ギリアード サイエンシーズ， インコーポレイテッド LPA receptor antagonists and their uses
CA3183097A1 (en) 2020-06-03 2021-12-09 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
CN113069460B (en) * 2021-03-24 2022-02-08 兰州大学 Application of halcinonide and derivatives thereof in preparation of drugs for treating and/or preventing cerebrovascular diseases
AU2022273631A1 (en) 2021-05-11 2023-11-02 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
US11939318B2 (en) 2021-12-08 2024-03-26 Gilead Sciences, Inc. LPA receptor antagonists and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040204383A1 (en) * 2003-04-11 2004-10-14 Gabor Tigyi Lysophosphatidic acid analogs and inhibition of neointima formation
US20060009507A1 (en) * 2003-10-09 2006-01-12 Miller Duane D LPA receptor agonists and antagonists and methods of use
WO2008014286A1 (en) * 2006-07-24 2008-01-31 University Of Virginia Patent Foundation Vinyl phosphonate lysophosphatidic acid receptor antagonists

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040204383A1 (en) * 2003-04-11 2004-10-14 Gabor Tigyi Lysophosphatidic acid analogs and inhibition of neointima formation
US20060009507A1 (en) * 2003-10-09 2006-01-12 Miller Duane D LPA receptor agonists and antagonists and methods of use
WO2008014286A1 (en) * 2006-07-24 2008-01-31 University Of Virginia Patent Foundation Vinyl phosphonate lysophosphatidic acid receptor antagonists

Also Published As

Publication number Publication date
WO2011159550A2 (en) 2011-12-22

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