WO2003026661A1 - Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine - Google Patents

Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine Download PDF

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Publication number
WO2003026661A1
WO2003026661A1 PCT/JP2002/009350 JP0209350W WO03026661A1 WO 2003026661 A1 WO2003026661 A1 WO 2003026661A1 JP 0209350 W JP0209350 W JP 0209350W WO 03026661 A1 WO03026661 A1 WO 03026661A1
Authority
WO
WIPO (PCT)
Prior art keywords
pyrimidine derivative
insulin secretion
insulin
novel pyrimidine
secretion accelerator
Prior art date
Application number
PCT/JP2002/009350
Other languages
English (en)
Japanese (ja)
Inventor
Yasuhiro Yonetoku
Tatsuya Maruyama
Kenji Negoro
Hiroyuki Moritomo
Naoki Imanishi
Itsuro Shimada
Ayako Moritomo
Wataru Hamaguchi
Hana Misawa
Shigeru Yoshida
Takahide Ohishi
Original Assignee
Yamanouchi Pharmaceutical Co., Ltd.
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 Yamanouchi Pharmaceutical Co., Ltd. filed Critical Yamanouchi Pharmaceutical Co., Ltd.
Priority to JP2003530296A priority Critical patent/JPWO2003026661A1/ja
Publication of WO2003026661A1 publication Critical patent/WO2003026661A1/fr

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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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom

Landscapes

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

Abstract

L'invention concerne un dérivé de pyrimidine hautement efficace dans la promotion de la sécrétion d'insuline, l'accroissement de la teneur en insuline et l'inhibition de la croissance de la glycémie. Elle peut s'utiliser pour traiter le diabète insulino-dépendant, le diabète non insulino-dépendant, les maladies résistant à l'insuline et l'obésité.
PCT/JP2002/009350 2001-09-14 2002-09-12 Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine WO2003026661A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2003530296A JPWO2003026661A1 (ja) 2001-09-14 2002-09-12 インスリン分泌促進剤及び新規なピリミジン誘導体

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2001-279671 2001-09-14
JP2001279671 2001-09-14
JP2002121012 2002-04-23
JP2002-121012 2002-04-23

Publications (1)

Publication Number Publication Date
WO2003026661A1 true WO2003026661A1 (fr) 2003-04-03

Family

ID=26622233

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2002/009350 WO2003026661A1 (fr) 2001-09-14 2002-09-12 Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine

Country Status (2)

Country Link
JP (1) JPWO2003026661A1 (fr)
WO (1) WO2003026661A1 (fr)

Cited By (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005047268A2 (fr) * 2003-11-10 2005-05-26 X-Ceptor Therapeutics, Inc. Compositions de pyrimidine substituee et procedes d'utilisation associes
WO2005054199A1 (fr) 2003-12-03 2005-06-16 Cytopia Research Pty Ltd Inhibiteurs de la tubuline
EP1549316A1 (fr) * 2002-09-10 2005-07-06 Scios Inc. Inhibiteurs de tgf-$g(b)
JP2005520821A (ja) * 2002-03-15 2005-07-14 チバ　スペシャルティ　ケミカルズ　ホールディング　インコーポレーテッド ４−アミノピリミジン及び表面の抗菌処理のためのその使用
EP1610774A2 (fr) * 2003-04-09 2006-01-04 Exelixis, Inc. Modulateurs de tie-2 et procedes d'utilisation
WO2006076231A2 (fr) * 2005-01-10 2006-07-20 Arena Pharmaceuticals, Inc. Polytherapie destinee au traitement du diabete et de troubles lies au diabete et au traitement de troubles pouvant etre soignes par une augmentation du taux de glp-1 dans le sang
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2007120702A2 (fr) 2006-04-11 2007-10-25 Arena Pharmaceuticals, Inc. Agonistes du récepteur de gpr119 dans des procédés d'augmentation de la masse osseuse et de traitement de l'ostéoporose et autres états se caractérisant par une masse osseuse faible, et thérapie de combinaison associée
WO2008128984A1 (fr) * 2007-04-20 2008-10-30 Probiodrug Ag Dérivés d'aminopyrimidine utilisés comme inhibiteurs de la glutaminyl cyclase
JP2009526868A (ja) * 2006-02-15 2009-07-23 アボット・ラボラトリーズ 新規なアセチル−ＣｏＡカルボキシラーゼ（ＡＣＣ）阻害薬およびこれらの糖尿病、肥満および代謝症候群における使用
EP2108960A1 (fr) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Procédés d'utilisation d'un récepteur couplé à protéine G pour identifier les secrétagogues de peptide YY (PYY) et composés utiles dans le traitement des conditions modulées de secrétagogues BY (PYY) et composés utiles dans le traitement des conditions par PYY
JP2010195834A (ja) * 2001-12-07 2010-09-09 Vertex Pharmaceuticals Inc Ｇｓｋ−３阻害剤として有用なピリミジンベースの化合物
US20100298143A1 (en) * 2009-05-19 2010-11-25 Dow Agrosciences Llc Compounds and methods for controlling fungi
EP2107908A4 (fr) * 2007-02-02 2011-07-20 Redpoint Bio Corp Utilisation d'un inhibiteur de trpm5 pour réguler une sécrétion d'insuline et de glp-1
EP2402750A1 (fr) 2006-04-11 2012-01-04 Arena Pharmaceuticals, Inc. Procédés d'utilisation du récepteur GPR119 permettant d'identifier les composants utiles à l'augmentation de la masse osseuse chez un individu
CN103896856A (zh) * 2012-12-25 2014-07-02 叶龙 一种多取代单环嘧啶类jnk激酶抑制剂及其制备方法和用途
WO2014105952A3 (fr) * 2012-12-28 2014-10-09 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibiteurs du complexe usp1/uaf1 désubiquitinase et leurs utilisations
US8933083B2 (en) 2003-01-14 2015-01-13 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
US10894787B2 (en) 2010-09-22 2021-01-19 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
US11534424B2 (en) 2017-02-16 2022-12-27 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
US11884626B2 (en) 2015-06-22 2024-01-30 Arena Pharmaceuticals, Inc. Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1P1 receptor-associated disorders

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH1087492A (ja) * 1996-06-25 1998-04-07 Ono Pharmaceut Co Ltd 一酸化窒素産生阻害剤
WO1998037079A1 (fr) * 1997-02-19 1998-08-27 Berlex Laboratories, Inc. Derives n-heterocycliques utiles en tant qu'inhibiteurs de la no synthetase

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH1087492A (ja) * 1996-06-25 1998-04-07 Ono Pharmaceut Co Ltd 一酸化窒素産生阻害剤
WO1998037079A1 (fr) * 1997-02-19 1998-08-27 Berlex Laboratories, Inc. Derives n-heterocycliques utiles en tant qu'inhibiteurs de la no synthetase

Cited By (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010195834A (ja) * 2001-12-07 2010-09-09 Vertex Pharmaceuticals Inc Ｇｓｋ−３阻害剤として有用なピリミジンベースの化合物
JP2005520821A (ja) * 2002-03-15 2005-07-14 チバ　スペシャルティ　ケミカルズ　ホールディング　インコーポレーテッド ４−アミノピリミジン及び表面の抗菌処理のためのその使用
EP1549316A1 (fr) * 2002-09-10 2005-07-06 Scios Inc. Inhibiteurs de tgf-$g(b)
EP1549316A4 (fr) * 2002-09-10 2008-04-09 Scios Inc Inhibiteurs de tgf-$g(b)
US8933083B2 (en) 2003-01-14 2015-01-13 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
JP4895806B2 (ja) * 2003-04-09 2012-03-14 エクセリクシス， インク． Ｔｉｅ−２モジュレータと使用方法
JP2006523238A (ja) * 2003-04-09 2006-10-12 エクセリクシス， インク． Ｔｉｅ−２モジュレータと使用方法
EP1610774A4 (fr) * 2003-04-09 2008-07-16 Exelixis Inc Modulateurs de tie-2 et procedes d'utilisation
EP1610774A2 (fr) * 2003-04-09 2006-01-04 Exelixis, Inc. Modulateurs de tie-2 et procedes d'utilisation
US8410119B2 (en) 2003-07-14 2013-04-02 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US7625906B2 (en) 2003-07-14 2009-12-01 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2005047268A2 (fr) * 2003-11-10 2005-05-26 X-Ceptor Therapeutics, Inc. Compositions de pyrimidine substituee et procedes d'utilisation associes
WO2005047268A3 (fr) * 2003-11-10 2005-07-21 X Ceptor Therapeutics Inc Compositions de pyrimidine substituee et procedes d'utilisation associes
JP2011093930A (ja) * 2003-12-03 2011-05-12 Ym Biosciences Australia Pty Ltd チューブリン阻害剤
JP2007513093A (ja) * 2003-12-03 2007-05-24 サイトピア・リサーチ・ピーティーワイ・リミテッド チューブリン阻害剤
AU2004294354B2 (en) * 2003-12-03 2009-02-19 Ym Biosciences Australia Pty Ltd Tubulin inhibitors
US7981900B2 (en) 2003-12-03 2011-07-19 Ym Biosciences Australia Pty Ltd 2-phenyl pyrimidines which are tubulin inhibitors
JP4772690B2 (ja) * 2003-12-03 2011-09-14 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド チューブリン阻害剤
US9732046B2 (en) 2003-12-03 2017-08-15 Ym Biosciences Australia Pty Ltd. Substituted 1,2,4-triazines as tubulin inhibitors
EP2277865A1 (fr) * 2003-12-03 2011-01-26 YM BioSciences Australia Pty Ltd Azahétérocycles des six membres portant un substituant phényl comme inhibiteurs de polymérisation des microtubules
US9139560B2 (en) 2003-12-03 2015-09-22 Ym Biosciences Australia Pty Ltd. Substituted pyrazines as tubulin inhibitors
WO2005054199A1 (fr) 2003-12-03 2005-06-16 Cytopia Research Pty Ltd Inhibiteurs de la tubuline
US8394806B2 (en) 2003-12-03 2013-03-12 Ym Biosciences Australia Pty Ltd 2-phenyl pyrazines as tubulin inhibitors
WO2006076231A2 (fr) * 2005-01-10 2006-07-20 Arena Pharmaceuticals, Inc. Polytherapie destinee au traitement du diabete et de troubles lies au diabete et au traitement de troubles pouvant etre soignes par une augmentation du taux de glp-1 dans le sang
EP1808168A1 (fr) * 2005-01-10 2007-07-18 Arena Pharmaceuticals, Inc. Thérapie combinée pour le traitement du diabète et des conditions associées, et pour le traitement des conditions améliorées par l'augmentation du niveau de GLP-1 dans le sang
EP2116235A1 (fr) 2005-01-10 2009-11-11 Arena Pharmaceuticals, Inc. Thérapie combinée pour le traitement des diabètes et des conditions associées, et pour le traitement des conditions améliorées par l'augmentation du niveau de sang GLP-1
EP2322157A1 (fr) 2005-01-10 2011-05-18 Arena Pharmaceuticals, Inc. Composition pour le traitement des diabètes et des conditions associées, et pour le traitement des conditions améliorées par l'augmentation du niveau de sang GLP-1
EA011883B1 (ru) * 2005-01-10 2009-06-30 Арена Фармасьютикалз, Инк. Комбинированная терапия для лечения диабета и родственных ему состояний и для лечения состояний, улучшаемых увеличением уровня glp-1 крови
WO2006076231A3 (fr) * 2005-01-10 2007-01-18 Arena Pharm Inc Polytherapie destinee au traitement du diabete et de troubles lies au diabete et au traitement de troubles pouvant etre soignes par une augmentation du taux de glp-1 dans le sang
JP2009526868A (ja) * 2006-02-15 2009-07-23 アボット・ラボラトリーズ 新規なアセチル−ＣｏＡカルボキシラーゼ（ＡＣＣ）阻害薬およびこれらの糖尿病、肥満および代謝症候群における使用
EP2253311A2 (fr) 2006-04-11 2010-11-24 Arena Pharmaceuticals, Inc. Utilisation d'agonistes du récepteur de GPR119 dans des procédés d'augmentation de la masse osseuse et de traitement de l'ostéoporose, et thérapie de combinaison associée
WO2007120702A2 (fr) 2006-04-11 2007-10-25 Arena Pharmaceuticals, Inc. Agonistes du récepteur de gpr119 dans des procédés d'augmentation de la masse osseuse et de traitement de l'ostéoporose et autres états se caractérisant par une masse osseuse faible, et thérapie de combinaison associée
EP2402750A1 (fr) 2006-04-11 2012-01-04 Arena Pharmaceuticals, Inc. Procédés d'utilisation du récepteur GPR119 permettant d'identifier les composants utiles à l'augmentation de la masse osseuse chez un individu
EP2107908A4 (fr) * 2007-02-02 2011-07-20 Redpoint Bio Corp Utilisation d'un inhibiteur de trpm5 pour réguler une sécrétion d'insuline et de glp-1
US8188094B2 (en) 2007-04-20 2012-05-29 Probiodrug Ag Inhibitors of glutaminyl cyclase
WO2008128984A1 (fr) * 2007-04-20 2008-10-30 Probiodrug Ag Dérivés d'aminopyrimidine utilisés comme inhibiteurs de la glutaminyl cyclase
JP2010524896A (ja) * 2007-04-20 2010-07-22 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体
US8883714B2 (en) 2008-04-07 2014-11-11 Arena Pharmaceuticals, Inc. Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues
EP2108960A1 (fr) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Procédés d'utilisation d'un récepteur couplé à protéine G pour identifier les secrétagogues de peptide YY (PYY) et composés utiles dans le traitement des conditions modulées de secrétagogues BY (PYY) et composés utiles dans le traitement des conditions par PYY
US20100298143A1 (en) * 2009-05-19 2010-11-25 Dow Agrosciences Llc Compounds and methods for controlling fungi
JP2012527461A (ja) * 2009-05-19 2012-11-08 ダウ アグロサイエンシィズ エルエルシー 真菌を防除するための化合物および方法
CN102438993A (zh) * 2009-05-19 2012-05-02 陶氏益农公司 用于控制真菌的化合物和方法
US8759356B2 (en) * 2009-05-19 2014-06-24 Dow Agrosciences, Llc. Compounds and methods for controlling fungi
US10894787B2 (en) 2010-09-22 2021-01-19 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
CN103896856B (zh) * 2012-12-25 2016-06-08 叶龙 一种多取代单环嘧啶类jnk激酶抑制剂及其制备方法和用途
CN103896856A (zh) * 2012-12-25 2014-07-02 叶龙 一种多取代单环嘧啶类jnk激酶抑制剂及其制备方法和用途
US20150344443A1 (en) * 2012-12-28 2015-12-03 The United States Of America, As Represented By The Secretary, Department Of Health And Human Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
JP2016504365A (ja) * 2012-12-28 2016-02-12 アメリカ合衆国 Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用
US9802904B2 (en) * 2012-12-28 2017-10-31 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof
WO2014105952A3 (fr) * 2012-12-28 2014-10-09 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibiteurs du complexe usp1/uaf1 désubiquitinase et leurs utilisations
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
US11884626B2 (en) 2015-06-22 2024-01-30 Arena Pharmaceuticals, Inc. Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1P1 receptor-associated disorders
US11534424B2 (en) 2017-02-16 2022-12-27 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis

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