EA200702274A1 - Твёрдые кристаллические и аморфные формы (-)-галофената и способ их получения, фармацевтическая композиция на их основе и способ лечения - Google Patents

Твёрдые кристаллические и аморфные формы (-)-галофената и способ их получения, фармацевтическая композиция на их основе и способ лечения

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Publication number
EA200702274A1
EA200702274A1 EA200702274A EA200702274A EA200702274A1 EA 200702274 A1 EA200702274 A1 EA 200702274A1 EA 200702274 A EA200702274 A EA 200702274A EA 200702274 A EA200702274 A EA 200702274A EA 200702274 A1 EA200702274 A1 EA 200702274A1
Authority
EA
Eurasian Patent Office
Prior art keywords
halophenate
basis
production
pharmaceutical composition
amorphous forms
Prior art date
Application number
EA200702274A
Other languages
English (en)
Inventor
Эдвард Д. Даугз
Эрик Дж. Хаген
Джейсон А. Хэнко
Дейвид Г. Лаукс
Original Assignee
Метаболекс, Инк.
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 Метаболекс, Инк. filed Critical Метаболекс, Инк.
Publication of EA200702274A1 publication Critical patent/EA200702274A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/82—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/83—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/17—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/18—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • 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
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • 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
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/82—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/76—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C235/78—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)

Abstract

Настоящее изобретение предлагает твердые кристаллические и аморфные формы (-)-галофената. Твердые кристаллические формы могут применяться в различных фармацевтических композициях и особенно эффективны для предупреждения и/или лечения заболеваний, связанных с осаждением липидов крови у млекопитающих, в частности против заболеваний, которые относятся к диабетам второго типа и гиперлипидемии. Изобретение также относится к способу предупреждения или лечения диабета II типа и гиперлипидемии у млекопитающих, включая стадию введения терапевтически эффективного количества твердой кристаллической и аморфной формы (-)-галофената.
EA200702274A 2005-04-20 2006-04-20 Твёрдые кристаллические и аморфные формы (-)-галофената и способ их получения, фармацевтическая композиция на их основе и способ лечения EA200702274A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US67365505P 2005-04-20 2005-04-20
PCT/US2006/015163 WO2006113917A1 (en) 2005-04-20 2006-04-20 Crystalline solid and amorphous forms of (-)- halofenate

Publications (1)

Publication Number Publication Date
EA200702274A1 true EA200702274A1 (ru) 2008-04-28

Family

ID=37115499

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200702274A EA200702274A1 (ru) 2005-04-20 2006-04-20 Твёрдые кристаллические и аморфные формы (-)-галофената и способ их получения, фармацевтическая композиция на их основе и способ лечения

Country Status (15)

Country Link
US (5) US8203019B2 (ru)
EP (1) EP1877362A1 (ru)
JP (1) JP2008538570A (ru)
KR (1) KR101372271B1 (ru)
CN (1) CN101163660A (ru)
BR (1) BRPI0610782A2 (ru)
CA (1) CA2606279C (ru)
CR (1) CR9516A (ru)
EA (1) EA200702274A1 (ru)
IL (1) IL186664A (ru)
MX (1) MX2007012991A (ru)
NO (1) NO20075831L (ru)
UA (1) UA96571C2 (ru)
WO (1) WO2006113917A1 (ru)
ZA (1) ZA200709015B (ru)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2606279C (en) * 2005-04-20 2015-01-06 Metabolex, Inc. Crystalline solid and amorphous forms of (-)- halofenate and methods related thereto
WO2009121940A1 (en) * 2008-04-03 2009-10-08 Janssen Pharmaceutica Nv Process for the preparation of (-)-(4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid 2-acetylamino-ethyl ester

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3953490A (en) 1972-07-13 1976-04-27 Merck & Co., Inc. Preparation of (3-trifluoromethylphenoxy)(4-chlorophenyl)acetonitrile
US6262118B1 (en) * 1999-06-04 2001-07-17 Metabolex, Inc. Use of (-) (3-trihalomethylphenoxy) (4-halophenyl) acetic acid derivatives for treatment of insulin resistance, type 2 diabetes and hyperlipidemia
CA2606279C (en) * 2005-04-20 2015-01-06 Metabolex, Inc. Crystalline solid and amorphous forms of (-)- halofenate and methods related thereto

Also Published As

Publication number Publication date
US9233914B2 (en) 2016-01-12
CR9516A (es) 2008-03-06
US8507719B2 (en) 2013-08-13
CA2606279C (en) 2015-01-06
WO2006113917A1 (en) 2006-10-26
BRPI0610782A2 (pt) 2017-01-31
EP1877362A1 (en) 2008-01-16
KR101372271B1 (ko) 2014-03-17
US20140024852A1 (en) 2014-01-23
WO2006113917A9 (en) 2008-02-14
US9845285B2 (en) 2017-12-19
UA96571C2 (ru) 2011-11-25
AU2006236153A2 (en) 2006-10-26
CA2606279A1 (en) 2006-10-26
US20150225333A1 (en) 2015-08-13
US20160280636A1 (en) 2016-09-29
MX2007012991A (es) 2008-03-13
IL186664A0 (en) 2008-01-20
CN101163660A (zh) 2008-04-16
US8993797B2 (en) 2015-03-31
NO20075831L (no) 2008-01-18
ZA200709015B (en) 2008-12-31
IL186664A (en) 2013-10-31
US20120232303A1 (en) 2012-09-13
KR20070122567A (ko) 2007-12-31
JP2008538570A (ja) 2008-10-30
US8203019B2 (en) 2012-06-19
US20080221018A1 (en) 2008-09-11
AU2006236153A1 (en) 2006-10-26

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