WO2010011926A3 - A novel betaine cocrystal of epalrestat - Google Patents

A novel betaine cocrystal of epalrestat Download PDF

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Publication number
WO2010011926A3
WO2010011926A3 PCT/US2009/051693 US2009051693W WO2010011926A3 WO 2010011926 A3 WO2010011926 A3 WO 2010011926A3 US 2009051693 W US2009051693 W US 2009051693W WO 2010011926 A3 WO2010011926 A3 WO 2010011926A3
Authority
WO
WIPO (PCT)
Prior art keywords
novel betaine
betaine cocrystal
cocrystal
novel
epalrestat
Prior art date
Application number
PCT/US2009/051693
Other languages
French (fr)
Other versions
WO2010011926A2 (en
Inventor
Isabel Kalofonos
Patrick G. Stahly
William Martin-Doyle
Dimitris Kalofonos
Jeffrey S. Stults
Travis L. Houston
Original Assignee
Bionevia 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 Bionevia Pharmaceuticals, Inc. filed Critical Bionevia Pharmaceuticals, Inc.
Priority to EP09801070A priority Critical patent/EP2340245A4/en
Priority to EA201100246A priority patent/EA018905B1/en
Publication of WO2010011926A2 publication Critical patent/WO2010011926A2/en
Publication of WO2010011926A3 publication Critical patent/WO2010011926A3/en
Priority to US13/013,786 priority patent/US8697735B2/en
Priority to US14/251,039 priority patent/US9447056B2/en

Links

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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/25—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids with polyoxyalkylated alcohols, e.g. esters of polyethylene glycol
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D277/32—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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/36—Sulfur atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

The invention relates to a novel betaine cocrystal of 5-[(lZ,2E)-2-methyl-3- phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel betaine cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel betaine cocrystal and the therapeutic use of the novel betaine cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria, reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.
PCT/US2009/051693 2008-07-25 2009-07-24 A novel betaine cocrystal of epalrestat WO2010011926A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP09801070A EP2340245A4 (en) 2008-07-25 2009-07-24 A novel betaine cocrystal of epalrestat
EA201100246A EA018905B1 (en) 2008-07-25 2009-07-24 A novel betaine cocrystal of epalrestat
US13/013,786 US8697735B2 (en) 2008-07-25 2011-01-25 Solid forms of epalrestat
US14/251,039 US9447056B2 (en) 2008-07-25 2014-04-11 Solid forms of epalrestat

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8361908P 2008-07-25 2008-07-25
US61/083,619 2008-07-25

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2009/047060 Continuation-In-Part WO2009152347A2 (en) 2008-06-13 2009-06-11 Crystalline forms of zotepine hydrochloride

Related Child Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2009/051687 Continuation-In-Part WO2010011922A2 (en) 2008-07-25 2009-07-24 Novel crystalline salts of epalrestat
US13/013,786 Continuation-In-Part US8697735B2 (en) 2008-07-25 2011-01-25 Solid forms of epalrestat

Publications (2)

Publication Number Publication Date
WO2010011926A2 WO2010011926A2 (en) 2010-01-28
WO2010011926A3 true WO2010011926A3 (en) 2010-05-27

Family

ID=41570882

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2009/051693 WO2010011926A2 (en) 2008-07-25 2009-07-24 A novel betaine cocrystal of epalrestat

Country Status (3)

Country Link
EP (1) EP2340245A4 (en)
EA (1) EA018905B1 (en)
WO (1) WO2010011926A2 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8697735B2 (en) 2008-07-25 2014-04-15 Bionevia Pharmaceuticals, Inc. Solid forms of epalrestat
PL2326632T3 (en) 2008-09-06 2017-10-31 Bionevia Pharmaceuticals Inc Novel choline cocrystal of epalrestat
ES2555927T3 (en) 2011-01-20 2016-01-11 Bionevia Pharmaceuticals Inc. Compositions of modified release of epalrestat or a derivative thereof and methods for using them
ITMI20120586A1 (en) 2012-04-11 2013-10-12 Milano Politecnico CO-CRYSTALS OF 3-IODIOPROPINYL BUTYCARBAMMATE
CN113277962B (en) * 2021-06-01 2023-02-07 天津大学 Epalrestat-metformin salt hydrate and preparation method and application thereof
CN113336718B (en) * 2021-06-01 2023-02-28 天津大学 Epalrestat-metformin salt and preparation method and application thereof
CN115925650B (en) * 2022-12-13 2023-08-01 山东达因海洋生物制药股份有限公司 Epalrestat eutectic and preparation method and application thereof
CN115947699B (en) * 2023-01-16 2024-01-19 威海海洋职业学院 Epalrestat eutectic crystal taking nicotinamide as precursor and preparation method thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4831045A (en) * 1980-08-22 1989-05-16 Ono Pharmaceutical Co., Ltd. Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
US20050181041A1 (en) * 2003-12-09 2005-08-18 Medcrystalforms, Llc Method of preparation of mixed phase co-crystals with active agents

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE550022T1 (en) * 2003-02-28 2012-04-15 Mcneil Ppc Inc PHARMACEUTICAL MIXED CRYSTALS OF CELECOXIB-NICOTINAMIDE
JP4892915B2 (en) * 2005-10-04 2012-03-07 大日本印刷株式会社 Epalrestat manufacturing method

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4831045A (en) * 1980-08-22 1989-05-16 Ono Pharmaceutical Co., Ltd. Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
US20050181041A1 (en) * 2003-12-09 2005-08-18 Medcrystalforms, Llc Method of preparation of mixed phase co-crystals with active agents

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
AMY LAWSON-YUEN ET AL.: "The use of betaine in the treatment of elevated homocysteine.", MOLECULAR GENETICS AND METABOLISM., vol. 88, no. 3, 2006, pages 201 - 207, XP024947075 *
ENOKA P. WIJEKOON ET AL.: "Homocysteine Metabolism in ZDF (Type 2) Diabetic Rats.", DIABETES., vol. 5, no. 11, 2005, pages 3245 - 3251, XP008135285 *
See also references of EP2340245A4 *

Also Published As

Publication number Publication date
EP2340245A4 (en) 2011-09-28
EA018905B1 (en) 2013-11-29
EP2340245A2 (en) 2011-07-06
WO2010011926A2 (en) 2010-01-28
EA201100246A1 (en) 2011-10-31

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