WO2007117791A2 - Combination treatment of metabolic disorders - Google Patents

Combination treatment of metabolic disorders Download PDF

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Publication number
WO2007117791A2
WO2007117791A2 PCT/US2007/063288 US2007063288W WO2007117791A2 WO 2007117791 A2 WO2007117791 A2 WO 2007117791A2 US 2007063288 W US2007063288 W US 2007063288W WO 2007117791 A2 WO2007117791 A2 WO 2007117791A2
Authority
WO
WIPO (PCT)
Prior art keywords
methyl
hydrogen
compound
phenyl
ethoxy
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2007/063288
Other languages
English (en)
French (fr)
Other versions
WO2007117791A3 (en
Inventor
Reid W. Von Borstel
Kirvin L. Hodge
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wellstat Therapeutics Corp
Original Assignee
Wellstat Therapeutics Corp
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 JP2009503119A priority Critical patent/JP2009532372A/ja
Priority to MX2008012506A priority patent/MX2008012506A/es
Priority to CA002647258A priority patent/CA2647258A1/en
Priority to EP07757896A priority patent/EP2001461A4/en
Priority to AU2007235145A priority patent/AU2007235145B2/en
Priority to NZ571118A priority patent/NZ571118A/en
Application filed by Wellstat Therapeutics Corp filed Critical Wellstat Therapeutics Corp
Priority to US12/294,530 priority patent/US8338480B2/en
Publication of WO2007117791A2 publication Critical patent/WO2007117791A2/en
Publication of WO2007117791A3 publication Critical patent/WO2007117791A3/en
Priority to IL194189A priority patent/IL194189A0/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • 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
    • A61K31/425—Thiazoles
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

Definitions

  • Rosiglitazone a direct PPAR-gamma agonist
  • AVAND AMET® rosiglitazone maleate and metformin hydrochloride
  • AVANDARYL® rosiglitazone maleate and glimepride
  • This invention concerns therapeutic uses of a combination of a direct PPAR-gamma agonist and a Compound of Formula I or a pharmaceutically acceptable salt thereof.
  • perfluoro as in perfluoromethyl or perfluoromethoxy, means that the group in question has fluorine atoms in place of all of the hydrogen atoms.
  • Insulin resistance syndromes and consequences of chronic hyperglycemia.
  • Dysregulation of fuel metabolism, especially insulin resistance which can occur in the absence of diabetes (persistent hyperglycemia) per se, is associated with a variety of symptoms, including hyperlipidemia, atherosclerosis, obesity, essential hypertension, fatty liver disease (NASH; nonalcoholic steatohepatitis), and, especially in the context of cancer or systemic inflammatory disease, cachexia. Cachexia can also occur in the context of Type I Diabetes or late- stage Type II Diabetes.
  • active agents of the invention are useful for preventing or amelioriating diseases and symptoms associated with insulin resistance.
  • EXAMPLE 1 Effects of Compound BI and rosiglitazone on body weight of mice with gold thioglucose-induced obesity
  • Drug preparation Compound BI was suspended in a vehicle comprising 1 % aqueous hydroxypropylmethylcellulose, using a tissue homogenizer to minimize particle size and maximize uniformity of the suspension. Rosiglitazone was suspended in the same vehicle. Drug concentrations in the dosing suspension for each treatment group were adjusted according to body weights so that a constant volume of 0.4 ml provided appropropriate drug doses in all groups.
  • the membrane was washed 6 x 7 min in TBST at room temperature, and then incubated with ECL (enhanced chemiluminescence) reagent (Amersham) for 1 min, and the relative amounts of UCPl in tissue samples were quantified by densitometry of the images on X-ray film resulting from exposure to light from the chemiluminescence reaction, and expressed as relative light units (RLU).
  • ECL enhanced chemiluminescence

Landscapes

  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
PCT/US2007/063288 2006-03-31 2007-03-05 Combination treatment of metabolic disorders Ceased WO2007117791A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
MX2008012506A MX2008012506A (es) 2006-03-31 2007-03-05 Tratamiento de combinacion de trastornos metabolicos.
CA002647258A CA2647258A1 (en) 2006-03-31 2007-03-05 Combination treatment of metabolic disorders
EP07757896A EP2001461A4 (en) 2006-03-31 2007-03-05 COMBINATION TREATMENT FOR METABOLISM DISEASES
AU2007235145A AU2007235145B2 (en) 2006-03-31 2007-03-05 Combination treatment of metabolic disorders
NZ571118A NZ571118A (en) 2006-03-31 2007-03-05 Combination treatment of metabolic disorders
JP2009503119A JP2009532372A (ja) 2006-03-31 2007-03-05 代謝障害の併用治療
US12/294,530 US8338480B2 (en) 2006-03-31 2007-03-05 Combination treatment of metabolic disorders
IL194189A IL194189A0 (en) 2006-03-31 2008-09-17 Combination treatment of metabolic disorders

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US74402106P 2006-03-31 2006-03-31
US60/744,021 2006-03-31

Publications (2)

Publication Number Publication Date
WO2007117791A2 true WO2007117791A2 (en) 2007-10-18
WO2007117791A3 WO2007117791A3 (en) 2008-08-21

Family

ID=38581719

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2007/063288 Ceased WO2007117791A2 (en) 2006-03-31 2007-03-05 Combination treatment of metabolic disorders

Country Status (11)

Country Link
US (1) US8338480B2 (enExample)
EP (1) EP2001461A4 (enExample)
JP (1) JP2009532372A (enExample)
KR (1) KR20080106455A (enExample)
CN (1) CN101410105A (enExample)
AU (1) AU2007235145B2 (enExample)
CA (1) CA2647258A1 (enExample)
IL (1) IL194189A0 (enExample)
MX (1) MX2008012506A (enExample)
NZ (1) NZ571118A (enExample)
WO (1) WO2007117791A2 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2085120A1 (en) * 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA The use of substances for the treatment of central or peripheral insulin receptor impairment and insulin resistance
JP2011515349A (ja) * 2008-03-13 2011-05-19 ウェルスタット セラピューティクス コーポレイション 尿酸を減少させる化合物及び方法
US8022249B2 (en) 2005-04-01 2011-09-20 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
EP2240024A4 (en) * 2008-01-15 2014-05-21 Wellstat Therapeutics Corp COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA03011558A (es) * 2001-06-12 2004-03-26 Wellstat Therapeutics Corp Compuestos para el tratamiento de desordenes metabolicos.
AU2007212104A1 (en) * 2006-02-02 2007-08-16 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
US7871785B2 (en) * 2007-09-07 2011-01-18 Children's Hospital Medical Center Use of secretor, Lewis and sialyl antigen levels in clinical samples as predictors of risk for disease
EP2451462B1 (en) 2009-07-06 2017-09-06 Children's Hospital Medical Center Inhibiting inflammation with milk oligosaccharides
WO2012033720A1 (en) 2010-09-08 2012-03-15 Wellstat Therapeutics Corporation Benzoic acid compounds for reducing uric acid
CN104885151B (zh) 2012-12-21 2017-12-22 杜比实验室特许公司 用于基于感知准则呈现基于对象的音频内容的对象群集
WO2014130789A1 (en) 2013-02-21 2014-08-28 Children's Hospital Medical Center Use of glycans and glycosyltransferases for diagnosing/monitoring inflammatory bowel disease
JP6553375B2 (ja) * 2014-06-24 2019-07-31 花王株式会社 Ｕｃｐ−１発現促進剤
JP6660668B2 (ja) * 2014-06-24 2020-03-11 花王株式会社 Ｕｃｐ−１発現促進剤
US10758519B2 (en) 2014-06-24 2020-09-01 Kao Corporation UCP-1 expression promoter
WO2015199097A1 (ja) * 2014-06-24 2015-12-30 花王株式会社 Ｕｃｐ－１発現促進剤
US10857167B2 (en) 2015-04-28 2020-12-08 Children's Hospital Medical Center Use of oligosaccharide compositions to enhance weight gain

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002100341A2 (en) 2001-06-12 2002-12-19 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
WO2004091486A2 (en) 2003-04-15 2004-10-28 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
WO2007003611A1 (fr) 2005-07-01 2007-01-11 Pierre Fabre Medicament Derives de pyrroloquinolines et leur utilisation comme inhibiteurs de proteines kinases

Family Cites Families (13)

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EP0842925A1 (en) * 1987-09-04 1998-05-20 Beecham Group Plc Substituted thiazolidinedione derivatives
TWI238064B (en) * 1995-06-20 2005-08-21 Takeda Chemical Industries Ltd A pharmaceutical composition for prophylaxis and treatment of diabetes
US6472373B1 (en) * 1997-09-21 2002-10-29 Schering Corporation Combination therapy for eradicating detectable HCV-RNA in antiviral treatment naive patients having chronic hepatitis C infection
US6172046B1 (en) * 1997-09-21 2001-01-09 Schering Corporation Combination therapy for eradicating detectable HCV-RNA in patients having chronic Hepatitis C infection
EA200400010A1 (ru) * 2001-06-07 2004-06-24 Эли Лилли Энд Компани Модуляторы рецепторов активаторов пролиферации пероксисом
WO2004041165A2 (en) * 2002-11-01 2004-05-21 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
BRPI0407506A (pt) * 2003-02-13 2006-02-14 Wellstat Therapeutics Corp compostos para o tratamento de distúrbios metabólicos, seu uso e composição farmacêutica compreendendo os mesmos
CN1777576A (zh) * 2003-04-22 2006-05-24 维尔斯达医疗公司 用于治疗代谢紊乱的化合物
AU2004237602B2 (en) * 2003-04-30 2009-05-28 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
WO2005018628A1 (en) * 2003-08-20 2005-03-03 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
WO2006127133A2 (en) 2005-04-01 2006-11-30 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
CN101374415A (zh) * 2006-01-25 2009-02-25 维尔斯达医疗公司 用于治疗代谢紊乱的化合物
CA2637375A1 (en) * 2006-01-25 2007-08-02 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002100341A2 (en) 2001-06-12 2002-12-19 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
WO2004091486A2 (en) 2003-04-15 2004-10-28 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
WO2007003611A1 (fr) 2005-07-01 2007-01-11 Pierre Fabre Medicament Derives de pyrroloquinolines et leur utilisation comme inhibiteurs de proteines kinases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP2001461A4

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8022249B2 (en) 2005-04-01 2011-09-20 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
EP2240024A4 (en) * 2008-01-15 2014-05-21 Wellstat Therapeutics Corp COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
EP2085120A1 (en) * 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA The use of substances for the treatment of central or peripheral insulin receptor impairment and insulin resistance
WO2009095265A1 (en) * 2008-02-01 2009-08-06 Merz Pharma Gmbh & Co. Kgaa The use of substances for the treatment of central or peripheral insulin receptor impairment and insulin resistance
JP2011515349A (ja) * 2008-03-13 2011-05-19 ウェルスタット セラピューティクス コーポレイション 尿酸を減少させる化合物及び方法

Also Published As

Publication number Publication date
IL194189A0 (en) 2009-08-03
US8338480B2 (en) 2012-12-25
AU2007235145A1 (en) 2007-10-18
AU2007235145B2 (en) 2011-09-22
KR20080106455A (ko) 2008-12-05
US20100292277A1 (en) 2010-11-18
CA2647258A1 (en) 2007-10-18
JP2009532372A (ja) 2009-09-10
NZ571118A (en) 2011-12-22
CN101410105A (zh) 2009-04-15
EP2001461A4 (en) 2010-06-09
MX2008012506A (es) 2008-10-14
WO2007117791A3 (en) 2008-08-21
EP2001461A2 (en) 2008-12-17

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