CN102395567A - 在治疗糖尿病和肥胖症中用作的tgr5激动剂的三唑和咪唑衍生物 - Google Patents

在治疗糖尿病和肥胖症中用作的tgr5激动剂的三唑和咪唑衍生物 Download PDF

Info

Publication number
CN102395567A
CN102395567A CN2010800163259A CN201080016325A CN102395567A CN 102395567 A CN102395567 A CN 102395567A CN 2010800163259 A CN2010800163259 A CN 2010800163259A CN 201080016325 A CN201080016325 A CN 201080016325A CN 102395567 A CN102395567 A CN 102395567A
Authority
CN
China
Prior art keywords
fluorophenyl
methyl
imidazoles
chloro
alkyl
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.)
Pending
Application number
CN2010800163259A
Other languages
English (en)
Chinese (zh)
Inventor
V.博鲁
B.C.博伦
J.E.达尔加德
B.T.弗拉特
N.哈克
S.哈德森
R.莫汉
M.莫里西
B.普拉特
王铁林
R.马丁
顾晓惠
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.)
Exelixis Inc
Original Assignee
Exelixis 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 Exelixis Inc filed Critical Exelixis Inc
Publication of CN102395567A publication Critical patent/CN102395567A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/84—Sulfur atoms
    • 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
    • A61K31/4164—1,3-Diazoles
    • 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
    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/12—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CN2010800163259A 2009-02-12 2010-02-12 在治疗糖尿病和肥胖症中用作的tgr5激动剂的三唑和咪唑衍生物 Pending CN102395567A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US15216309P 2009-02-12 2009-02-12
US61/152,163 2009-02-12
US28413909P 2009-12-11 2009-12-11
US61/284,139 2009-12-11
PCT/US2010/023981 WO2010093845A1 (en) 2009-02-12 2010-02-12 Triazole and imidazole derivatives for use as tgr5 agonists in the treatment of diabetes and obesity

Publications (1)

Publication Number Publication Date
CN102395567A true CN102395567A (zh) 2012-03-28

Family

ID=42102146

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2010800163259A Pending CN102395567A (zh) 2009-02-12 2010-02-12 在治疗糖尿病和肥胖症中用作的tgr5激动剂的三唑和咪唑衍生物

Country Status (8)

Country Link
US (1) US8785488B2 (https=)
EP (1) EP2396304A1 (https=)
JP (2) JP2012517479A (https=)
KR (1) KR20110119790A (https=)
CN (1) CN102395567A (https=)
AR (1) AR075255A1 (https=)
TW (1) TW201040168A (https=)
WO (1) WO2010093845A1 (https=)

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102781922A (zh) * 2009-12-11 2012-11-14 埃克塞利希斯股份有限公司 Tgr5激动剂
CN103755652A (zh) * 2013-12-20 2014-04-30 陕西理工学院 一种磺酰胺类化合物及其应用
CN103864754A (zh) * 2012-12-10 2014-06-18 中国科学院上海药物研究所 五元唑类杂环化合物及其制备方法、药物组合物和用途
CN104987313A (zh) * 2015-07-13 2015-10-21 佛山市赛维斯医药科技有限公司 一类末端取代的三氮唑亚砜类化合物、其制备方法及其用途
CN104987312A (zh) * 2015-07-13 2015-10-21 佛山市赛维斯医药科技有限公司 一类胺基苯三氮唑亚砜类11β-HSD1抑制剂及其用途
CN105001171A (zh) * 2015-07-13 2015-10-28 佛山市赛维斯医药科技有限公司 一类硝基苯三氮唑亚砜类11β-HSD1抑制剂及其用途
CN105017170A (zh) * 2015-07-13 2015-11-04 佛山市赛维斯医药科技有限公司 一类腈基苯三氮唑亚砜类11β-HSD1抑制剂及其用途
CN106432222A (zh) * 2016-09-19 2017-02-22 丹诺医药(苏州）有限公司 8‑氯‑1‑环丙基‑7‑氟‑9‑甲基‑4‑氧‑4‑氢‑喹嗪‑3‑羧酸酯及其制备方法
CN111039880A (zh) * 2019-12-10 2020-04-21 河南大学 咪康唑及其衍生物作为tgr5激动剂的应用
CN111763173A (zh) * 2020-07-14 2020-10-13 河南大学 苯乙基咪唑类衍生物及其用途
WO2025162114A1 (zh) * 2024-02-04 2025-08-07 成都麻沸散医药科技有限公司 一种杂环化合物及其用途

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
US9664677B2 (en) 2010-04-19 2017-05-30 Massachusetts Institute Of Technology Polymer-nanostructure composition for selective molecular recognition
CA2798610A1 (en) 2010-05-06 2011-11-10 Bristol-Myers Squibb Company Bicyclic heteroaryl compounds as gpr119 modulators
AU2011307289A1 (en) * 2010-09-29 2013-02-21 E. I. Du Pont De Nemours And Company Fungicidal imidazoles
WO2012082947A1 (en) * 2010-12-16 2012-06-21 Irm Llc Compounds and compositions as tgr5 agonists
WO2012109646A1 (en) 2011-02-11 2012-08-16 Vertex Pharmaceuticals Incorporated Treatment of hcv in hiv infection patients
WO2012149236A1 (en) 2011-04-28 2012-11-01 Bristol-Myers Squibb Company Novel bicyclic nitrogen containing heteroaryl tgr5 receptor modulators
WO2012174164A2 (en) * 2011-06-15 2012-12-20 Metabolex, Inc. Agonists of gpr131 and uses thereof
WO2013054338A1 (en) * 2011-07-06 2013-04-18 Cadila Healthcare Limited 2-thio-imidazole derivatives as tgr5 modulators
WO2013032939A1 (en) 2011-08-26 2013-03-07 Metabolex, Inc. Bicyclic agonists of gpr131 and uses thereof
WO2013062887A1 (en) * 2011-10-26 2013-05-02 Merck Sharp & Dohme Corp. Substituted pyridine derivatives useful as gpr131 agonists
WO2013102929A1 (en) 2011-12-26 2013-07-11 Cadila Healthcare Limited Novel compounds for treatment of diabetes, obesity or related disorders
WO2013164838A1 (en) * 2012-03-07 2013-11-07 Cadila Healthcare Limited Heterocyclic compounds and their use for treatment of diabetes, obesity or related disorders
LT6064B (lt) 2012-10-15 2014-08-25 Vilniaus Universitetas Fluorinti benzensulfonamidai kaip karboanhidrazės inhibitoriai
WO2014100025A1 (en) * 2012-12-17 2014-06-26 Exelixis, Inc. Tgr5 agonists having an imidazole or triazole core with subtituent having a quaternary nitrogen
WO2014100021A1 (en) * 2012-12-17 2014-06-26 Exelixis, Inc. Tgr5 agonists: imidazole and triazole compounds containing a quaternary nitrogen
US10323016B2 (en) 2014-06-12 2019-06-18 Universite De Lille 2 Droit Et Sante Imidazol- or 1,2,4-triazol-derivatives and their use
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
WO2016161003A1 (en) 2015-03-31 2016-10-06 Enanta Phamraceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
WO2017042380A1 (en) * 2015-09-11 2017-03-16 Universite De Lille 2 Droit Et Sante Novel 5-amino-2-thioimidazole compounds and their use
EP3210469A1 (de) 2016-02-23 2017-08-30 Bayer Cropscience AG Verwendung von substituierten thio-1,2,4-triazolen zur steigerung der stresstoleranz in pflanzen
WO2018005801A2 (en) * 2016-07-01 2018-01-04 Venenum Biodesign Llc Novel non-systemic tgr5 agonists
JP2022552655A (ja) 2019-10-07 2022-12-19 キャリーオペ，インク． Ｇｐｒ１１９アゴニスト
IL295825A (en) 2020-02-28 2022-10-01 Kallyope Inc gpr40 agonists
WO2021236617A1 (en) 2020-05-19 2021-11-25 Kallyope, Inc. Ampk activators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
ES2999626T3 (en) * 2020-10-09 2025-02-26 Bristol Myers Squibb Co Aminoimidazole fpr2 agonists
EP4377297A4 (en) * 2021-07-30 2025-05-28 The Regents of the University of California Compounds for modulating epithelial 15-(s)-lipoxygenase-2 and methods of use for same
US12221423B1 (en) 2023-10-23 2025-02-11 King Faisal University 3-(3-fluorophenyl)-5-(4-methoxybenzylthio)-4-phenyl-4H-1,2,4-triazole as an antimicrobial compound

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1158609A (zh) * 1994-09-26 1997-09-03 盐野义制药株式会社 咪唑衍生物
WO2005044192A2 (en) * 2003-10-28 2005-05-19 Amgen Inc. Triazole compounds and uses related thereto
WO2006068199A1 (ja) * 2004-12-22 2006-06-29 Mochida Pharmaceutical Co., Ltd. 代謝的に安定な３－オキシ－１，２，４－トリアゾール誘導体
CN1990474A (zh) * 2002-06-10 2007-07-04 默克公司 用于治疗糖尿病、肥胖和异常脂血症的11－β－羟甾醇脱氢酶1抑制剂

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL272996A (https=) * 1960-12-28
JPS61148176A (ja) * 1984-12-21 1986-07-05 Ota Seiyaku Kk 新規複素環式化合物
BR0214553A (pt) 2001-11-28 2004-10-13 Sod Conseils Rech Applic Compostos, processo de preparação, em fase lìquida, dos compostos, e, composições farmacêuticas
WO2004089367A1 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S Pharmaceutical use of substituted 1,2,4-triazoles
EP1635832A2 (en) * 2003-06-06 2006-03-22 Merck & Co., Inc. Combination therapy for the treatment of diabetes
JP2005170939A (ja) * 2003-11-20 2005-06-30 Takeda Chem Ind Ltd 糖尿病の予防・治療剤
JP2007527919A (ja) * 2004-03-08 2007-10-04 ワイス イオンチャンネルモジュレーター
JP2006063064A (ja) * 2004-07-27 2006-03-09 Takeda Chem Ind Ltd 受容体作動剤
WO2006080533A1 (ja) 2005-01-31 2006-08-03 Mochida Pharmaceutical Co., Ltd. ３－アミノ－１,２,４－トリアゾール誘導体
MX2007009388A (es) 2005-02-04 2007-09-25 Senomyx Inc Compuestos que comprenden porciones heteroarilo unidas y su uso como modificadores del sabor unami, saborizantes y mejoradores del sabor para composiciones comestibles.
JP5261176B2 (ja) 2005-08-16 2013-08-14 アイカジェン， インコーポレイテッド 電位作動型ナトリウムチャンネル阻害剤
EP1988083B1 (en) 2006-02-03 2014-04-02 Taisho Pharmaceutical Co., Ltd. Triazole derivative
JP2007210974A (ja) * 2006-02-13 2007-08-23 Sankyo Co Ltd 置換されたウレア化合物を含有する医薬
JP2009537564A (ja) 2006-05-17 2009-10-29 インサイト・コーポレイション １１−βヒドロキシルステロイドデヒドロゲナーゼタイプＩの複素環阻害剤およびそれを用いる方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1158609A (zh) * 1994-09-26 1997-09-03 盐野义制药株式会社 咪唑衍生物
CN1990474A (zh) * 2002-06-10 2007-07-04 默克公司 用于治疗糖尿病、肥胖和异常脂血症的11－β－羟甾醇脱氢酶1抑制剂
WO2005044192A2 (en) * 2003-10-28 2005-05-19 Amgen Inc. Triazole compounds and uses related thereto
WO2006068199A1 (ja) * 2004-12-22 2006-06-29 Mochida Pharmaceutical Co., Ltd. 代謝的に安定な３－オキシ－１，２，４－トリアゾール誘導体

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
IKUO KAWASAKI ET AL.: "New access to 1,3-dialkyl-2,3-dihydro-2-imino-1H-imidazoles and their application to the first total synthesis of naamine B, a marine 2,3-dihydro-2-imino-1,3-dimethyl-1H-imidazole alkaloid", 《J. CHEM. SOC., PERKIN TRANS. 1》 *
SHUNSAKU OHTA ET AL.: "Introduction of Carbogenic Substituent into the 4-Position of 1-Methyl-1H-imidazole", 《CHEM. PHARM. BULL.》 *

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102781922A (zh) * 2009-12-11 2012-11-14 埃克塞利希斯股份有限公司 Tgr5激动剂
CN103864754A (zh) * 2012-12-10 2014-06-18 中国科学院上海药物研究所 五元唑类杂环化合物及其制备方法、药物组合物和用途
CN103864754B (zh) * 2012-12-10 2016-12-21 中国科学院上海药物研究所 五元唑类杂环化合物及其制备方法、药物组合物和用途
CN103755652A (zh) * 2013-12-20 2014-04-30 陕西理工学院 一种磺酰胺类化合物及其应用
CN105017170A (zh) * 2015-07-13 2015-11-04 佛山市赛维斯医药科技有限公司 一类腈基苯三氮唑亚砜类11β-HSD1抑制剂及其用途
CN105001171A (zh) * 2015-07-13 2015-10-28 佛山市赛维斯医药科技有限公司 一类硝基苯三氮唑亚砜类11β-HSD1抑制剂及其用途
CN104987312A (zh) * 2015-07-13 2015-10-21 佛山市赛维斯医药科技有限公司 一类胺基苯三氮唑亚砜类11β-HSD1抑制剂及其用途
CN104987313A (zh) * 2015-07-13 2015-10-21 佛山市赛维斯医药科技有限公司 一类末端取代的三氮唑亚砜类化合物、其制备方法及其用途
CN106432222A (zh) * 2016-09-19 2017-02-22 丹诺医药(苏州）有限公司 8‑氯‑1‑环丙基‑7‑氟‑9‑甲基‑4‑氧‑4‑氢‑喹嗪‑3‑羧酸酯及其制备方法
CN111039880A (zh) * 2019-12-10 2020-04-21 河南大学 咪康唑及其衍生物作为tgr5激动剂的应用
CN111039880B (zh) * 2019-12-10 2022-06-21 河南大学 咪康唑及其衍生物作为tgr5激动剂的应用
CN111763173A (zh) * 2020-07-14 2020-10-13 河南大学 苯乙基咪唑类衍生物及其用途
CN111763173B (zh) * 2020-07-14 2022-11-01 河南大学 苯乙基咪唑类衍生物及其用途
WO2025162114A1 (zh) * 2024-02-04 2025-08-07 成都麻沸散医药科技有限公司 一种杂环化合物及其用途

Also Published As

Publication number Publication date
TW201040168A (en) 2010-11-16
JP2012517479A (ja) 2012-08-02
EP2396304A1 (en) 2011-12-21
KR20110119790A (ko) 2011-11-02
WO2010093845A1 (en) 2010-08-19
AR075255A1 (es) 2011-03-16
US8785488B2 (en) 2014-07-22
JP2014240421A (ja) 2014-12-25
US20120040985A1 (en) 2012-02-16

Similar Documents

Publication Publication Date Title
CN102395567A (zh) 在治疗糖尿病和肥胖症中用作的tgr5激动剂的三唑和咪唑衍生物
US8846739B2 (en) TGR5 agonists
EP3022202B1 (en) Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core
JP5180099B2 (ja) 置換イミダゾール誘導体、組成物ならびにｐｔｐアーゼ阻害剤としての使用方法
TWI490202B (zh) 昇糖素受體調節劑
CN114984003A (zh) 芳族磺酰胺衍生物
JP5451633B2 (ja) トリアゾールオキサジアゾール誘導体
JP2008536802A (ja) 代謝調節型グルタミン酸受容体のベンズアゾール増強剤
HK1206339A1 (en) N-aryltriazole compounds as lpar antagonists
EA020106B1 (ru) Производные l-(пиперидин-4-ил)пиразола в качестве модуляторов gpr119
CN101141957A (zh) 作为ppar调节剂的化合物和组合物
JP2015506382A (ja) オレキシンレセプターアンタゴニストとしての置換プロリン／ピペリジン
WO2004083190A1 (en) Biaryl substituted triazoles as sodium channel blockers
US20210317092A1 (en) Tetrazole containing compounds
JP2003505383A5 (https=)
US9376420B2 (en) 4,5-dihydro-1H-pyrazole derivative or salts thereof, and pharmaceutical composition comprising same
TW200424197A (en) Azole compounds
KR20060123739A (ko) 나트륨 채널 차단제로서의 치환된 트리아졸
US10214509B2 (en) Amino-substituted heterocyclic derivatives as sodium channel inhibitors
JP2008533193A (ja) オキシトシン拮抗薬としての置換トリアゾール誘導体
US20040029875A1 (en) Novel aminotriazolone compounds, method for preparing same and pharmaceutical compositions containing same
EP1954692A1 (en) Heterocycle-substituted 3-alkyl azetidine derivatives
JP2007505087A (ja) ベンゾオキサゾールアセトニトリル
KR101657594B1 (ko) 4,5-다이하이드로-1ｈ-피라졸 유도체 또는 그의 염 및 이를 포함하는 약학 조성물
HK40079811A (en) Aromatic sulfonamide derivatives

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20120328