JP2009513563A - ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体 - Google Patents

ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体 Download PDF

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JP2009513563A
JP2009513563A JP2008525998A JP2008525998A JP2009513563A JP 2009513563 A JP2009513563 A JP 2009513563A JP 2008525998 A JP2008525998 A JP 2008525998A JP 2008525998 A JP2008525998 A JP 2008525998A JP 2009513563 A JP2009513563 A JP 2009513563A
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carboxylic acid
methyl
methylthiazole
amide
thiazole
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JP2008525998A
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Japanese (ja)
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JP2009513563A5 (https=
Inventor
チエンミン フー,
デュアンチエ ホー,
ラジェンダー カンボイ,
ビシュヌマーシー コドゥムル,
ナタリア ポクロフスカイア,
バンドナ ライナ,
シャオイ サン,
セルゲイ スビリドフ,
ザイホイ チャン,
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Xenon Pharmaceuticals Inc
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Xenon Pharmaceuticals Inc
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Publication of JP2009513563A publication Critical patent/JP2009513563A/ja
Publication of JP2009513563A5 publication Critical patent/JP2009513563A5/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/587Heterocyclic 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 aliphatic hydrocarbon radicals substituted by 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, said aliphatic radicals being substituted in the alpha-position to the ring by a hetero atom, e.g. with m >= 0, Z being a singly or a doubly bound hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/60Salicylic acid; Derivatives thereof
    • A61K31/612Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/26Glucagons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/28Insulins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • AHUMAN NECESSITIES
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/32Heterocyclic 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
    • C07D277/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2008525998A 2005-06-03 2006-06-05 ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体 Pending JP2009513563A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US68713305P 2005-06-03 2005-06-03
PCT/US2006/021660 WO2007130075A1 (en) 2005-06-03 2006-06-05 Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors

Related Child Applications (1)

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JP2013042546A Division JP2013100376A (ja) 2005-06-03 2013-03-05 ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体

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JP2009513563A true JP2009513563A (ja) 2009-04-02
JP2009513563A5 JP2009513563A5 (https=) 2009-07-02

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JP2008525998A Pending JP2009513563A (ja) 2005-06-03 2006-06-05 ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体
JP2013042546A Pending JP2013100376A (ja) 2005-06-03 2013-03-05 ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体

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JP2013042546A Pending JP2013100376A (ja) 2005-06-03 2013-03-05 ヒトのステアロイル−CoAデサチュラーゼ阻害剤としてのアミノチアゾール誘導体

Country Status (9)

Country Link
US (2) US8541457B2 (https=)
EP (2) EP2029138A1 (https=)
JP (2) JP2009513563A (https=)
CN (1) CN101208089A (https=)
AU (1) AU2006343359A1 (https=)
BR (1) BRPI0611187A2 (https=)
CA (1) CA2618646A1 (https=)
MX (1) MX2007015216A (https=)
WO (1) WO2007130075A1 (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009541367A (ja) * 2006-06-27 2009-11-26 インスティテュート オブ ファーマコロジー アンド トキシコロジー アカデミー オブ ミリタリー メディカル サイエンシス ピーエルエイ 2,4,5−三置換チアゾール化合物、それを含有する医薬組成物、並びにその調製及び医学的使用
WO2017099237A1 (ja) * 2015-12-11 2017-06-15 帝人ファーマ株式会社 アミノアゾール誘導体
JP2019513762A (ja) * 2016-04-11 2019-05-30 ジェンフィGenfit 胆汁うっ滞及び線維症の処置方法
JP2021519263A (ja) * 2018-03-23 2021-08-10 ユマニティ セラピューティクス,インコーポレーテッド 化合物及びその使用

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US20050119251A1 (en) * 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
JP5080256B2 (ja) * 2004-09-20 2012-11-21 ゼノン・ファーマシューティカルズ・インコーポレイテッド 二環式複素環誘導体およびステアロイル−CoAデサチュラーゼ(SCD)のインヒビターとしてのそれらの使用
CA2580857A1 (en) * 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
US7829712B2 (en) 2004-09-20 2010-11-09 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase
AR051091A1 (es) * 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
CA2580762A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
AU2005286648A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
EP1807085B1 (en) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
EP2289510A1 (en) * 2004-09-20 2011-03-02 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes
AU2006343359A1 (en) 2005-06-03 2007-11-15 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
WO2008139845A1 (ja) * 2007-04-24 2008-11-20 Daiichi Sankyo Company, Limited 新規アミド誘導体
EP2178852B9 (en) 2007-08-03 2016-06-22 Romark Laboratories, L.C. Alkylsulfonyl-substituted thiazolide compounds
WO2009103739A1 (en) * 2008-02-20 2009-08-27 Novartis Ag Heterocyclic inhibitors of stearoyl-coa desaturase
CA2716599A1 (en) * 2008-02-25 2009-09-03 Lars Thore Burgdorf Glucokinase activators
EP2307379A2 (en) * 2008-06-27 2011-04-13 Novartis AG Organic compounds
US20100113520A1 (en) * 2008-11-05 2010-05-06 Principia Biopharma, Inc. Kinase knockdown via electrophilically enhanced inhibitors
CA2750564A1 (en) 2009-02-17 2010-08-26 Merck Canada Inc. Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase
PE20121118A1 (es) 2009-05-12 2012-09-05 Romark Lab Lc Compuestos de haloalquil heteroaril benzamida
AP2012006064A0 (en) 2009-06-26 2012-02-29 Romark Lab Lc Compounds and methods for treating influenza.
EP2459568A4 (en) 2009-07-28 2013-02-27 Merck Frosst Canada Ltd NEW SPIRO COMPOUNDS AS AN INHIBITORS OF STEAROYL COENZYME A DELTA 9 DESATURASE
RU2013114390A (ru) 2010-08-31 2014-10-10 СНУ Ар энд ДиБи ФАУНДЕЙШН Применение фетального репрограммирования посредством ppar-дельта-агониста
EP2683705B1 (de) 2011-03-08 2015-04-22 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
WO2012120052A1 (de) 2011-03-08 2012-09-13 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2683699B1 (de) 2011-03-08 2015-06-24 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
WO2013056148A2 (en) 2011-10-15 2013-04-18 Genentech, Inc. Methods of using scd1 antagonists
WO2013134546A1 (en) 2012-03-07 2013-09-12 Mayo Foundation For Medical Education And Research Methods and materials for treating cancer
BR112014029365A2 (pt) 2012-05-22 2017-06-27 Hoffmann La Roche inibidores seletivos de células indiferenciadas
ME03455B (me) 2012-09-10 2020-01-20 Principia Biopharma Inc Jedinjenja pirazolopirimidina kao inhibitori kinaze
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WO2017099237A1 (ja) * 2015-12-11 2017-06-15 帝人ファーマ株式会社 アミノアゾール誘導体
JPWO2017099237A1 (ja) * 2015-12-11 2018-04-12 帝人ファーマ株式会社 アミノアゾール誘導体
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JP2019513762A (ja) * 2016-04-11 2019-05-30 ジェンフィGenfit 胆汁うっ滞及び線維症の処置方法
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EP2540296A1 (en) 2013-01-02
JP2013100376A (ja) 2013-05-23
US8541457B2 (en) 2013-09-24
CN101208089A (zh) 2008-06-25
US20100152187A1 (en) 2010-06-17
MX2007015216A (es) 2008-02-22
AU2006343359A1 (en) 2007-11-15
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US20130096056A1 (en) 2013-04-18
BRPI0611187A2 (pt) 2010-08-24

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