CN102015676B - 作为amp-活化的蛋白激酶(ampk)活化剂的噻吩并吡啶酮衍生物 - Google Patents

作为amp-活化的蛋白激酶(ampk)活化剂的噻吩并吡啶酮衍生物 Download PDF

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Publication number
CN102015676B
CN102015676B CN200980116120.5A CN200980116120A CN102015676B CN 102015676 B CN102015676 B CN 102015676B CN 200980116120 A CN200980116120 A CN 200980116120A CN 102015676 B CN102015676 B CN 102015676B
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CN
China
Prior art keywords
dihydro
phenyl
thieno
hydroxyl
pyridine
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Expired - Fee Related
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CN200980116120.5A
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English (en)
Chinese (zh)
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CN102015676A (zh
Inventor
D·克拉沃
F·莱皮弗
S·哈莱库-波塞克
C·查隆
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Merck Patent GmbH
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Merck Patent GmbH
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN200980116120.5A 2008-05-05 2009-04-08 作为amp-活化的蛋白激酶(ampk)活化剂的噻吩并吡啶酮衍生物 Expired - Fee Related CN102015676B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08290423 2008-05-05
EP08290423.6 2008-05-05
PCT/EP2009/002606 WO2009135580A1 (en) 2008-05-05 2009-04-08 Thienopyridone derivatives as amp-activated protein kinase (ampk) activators

Publications (2)

Publication Number Publication Date
CN102015676A CN102015676A (zh) 2011-04-13
CN102015676B true CN102015676B (zh) 2014-05-28

Family

ID=40756916

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980116120.5A Expired - Fee Related CN102015676B (zh) 2008-05-05 2009-04-08 作为amp-活化的蛋白激酶(ampk)活化剂的噻吩并吡啶酮衍生物

Country Status (26)

Country Link
US (1) US8604202B2 (https=)
EP (1) EP2280952B1 (https=)
JP (1) JP5536757B2 (https=)
KR (2) KR20160038065A (https=)
CN (1) CN102015676B (https=)
AR (1) AR071530A1 (https=)
AU (1) AU2009243811B2 (https=)
BR (1) BRPI0910832B8 (https=)
CA (1) CA2723429C (https=)
CO (1) CO6331304A2 (https=)
CY (1) CY1113112T1 (https=)
DK (1) DK2280952T3 (https=)
EA (1) EA020773B1 (https=)
EC (1) ECSP10010654A (https=)
ES (1) ES2388485T3 (https=)
HR (1) HRP20120549T1 (https=)
IL (1) IL208988A (https=)
MX (1) MX2010011916A (https=)
MY (1) MY160357A (https=)
NZ (1) NZ589690A (https=)
PL (1) PL2280952T3 (https=)
PT (1) PT2280952E (https=)
SI (1) SI2280952T1 (https=)
UA (1) UA103617C2 (https=)
WO (1) WO2009135580A1 (https=)
ZA (1) ZA201008722B (https=)

Families Citing this family (25)

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WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US20130085169A1 (en) 2010-04-02 2013-04-04 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods and compositions comprising ampk activator (metformin/troglitazone) for the treatment of myotonic dystrophy type 1 (dm1)
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
JP5990170B2 (ja) * 2010-09-01 2016-09-07 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 除草活性を有するケトスルタム類及びジケトピリジン類
CA2830706A1 (en) * 2011-03-07 2012-09-13 Glaxosmithkline Llc Quinolinone derivatives
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
EP2679591A1 (en) 2012-06-29 2014-01-01 Poxel Thienopyridone derivatives useful as activators of AMPK
JP6064062B2 (ja) 2013-03-15 2017-01-18 ファイザー・インク Ａｍｐｋを活性化させるインダゾール化合物
US10143703B2 (en) 2014-01-02 2018-12-04 Massachusetts Eye And Ear Infirmary Treating ocular neovascularization
WO2015114663A1 (en) 2014-01-30 2015-08-06 Council Of Scientific & Industrial Research Novel thieno [2,3-d]pyrimidin-4(3h)-one compounds with antimycobacterial properties
WO2016205534A1 (en) * 2015-06-16 2016-12-22 Lazo John S Inhibitors of ptp4a3 for the treatment of cancer
RS61919B1 (sr) 2015-06-25 2021-06-30 Univ Health Network Inhibitori hpk1 i postupci za njihovo korišćenje
WO2017055925A2 (en) 2015-09-30 2017-04-06 Instituto De Medicina Molecular Methods for attenuating parasite virulence
US11584755B2 (en) 2017-09-26 2023-02-21 Ideaya Biosciences, Inc. Dihydrothieno[3,2-b]pyridine compounds
WO2019106087A1 (en) * 2017-11-29 2019-06-06 Syddansk Universitet Ampk inhibitors
WO2021236617A1 (en) 2020-05-19 2021-11-25 Kallyope, Inc. Ampk activators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
EP4221700A1 (en) 2020-09-30 2023-08-09 Bioverativ Therapeutics Inc. Ampk activators and methods of use thereof
WO2022106892A1 (en) 2020-11-17 2022-05-27 Instituto De Medicina Molecular Anti-malarial compounds
JP2024540522A (ja) 2021-11-19 2024-10-31 ザ・ブロード・インスティテュート・インコーポレイテッド キナーゼを標的結合部分で標識するための二官能性キメラ分子及びその使用方法

Citations (4)

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Publication number Priority date Publication date Assignee Title
CN87107975A (zh) * 1986-11-20 1988-06-01 布茨公司 治疗药物的制备方法
WO2003101979A1 (en) * 2002-05-31 2003-12-11 Pharmacia & Upjohn Company Llc Anthelmintic and insecticidal thiophene derivatives
US20050038068A1 (en) * 2003-05-16 2005-02-17 Iyengar Rajesh R. Thienopyridones as AMPK activators for the treatment of diabetes and obesity
WO2007019914A1 (en) * 2005-08-18 2007-02-22 Merck Patent Gmbh Use of thienopyridone derivatives as ampk activators and pharmaceutical compositions containing them

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DE4444815A1 (de) 1994-12-15 1996-06-20 Merck Patent Gmbh Thienopyridone
WO2006093518A2 (en) * 2004-06-25 2006-09-08 Apath, Llc Thienyl compounds for treating virus-related conditions
US7563813B2 (en) * 2005-05-13 2009-07-21 Wyeth Iminothiazolidinone derivatives as SFRP-1 antagonists
WO2007072094A1 (en) * 2005-12-20 2007-06-28 Richter Gedeon Nyrt. New compounds
MY155836A (en) * 2008-04-11 2015-12-15 Merck Patent Gmbh Thienopyridone derivatives as amp-activated protein kinase (ampk) activators

Patent Citations (4)

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CN87107975A (zh) * 1986-11-20 1988-06-01 布茨公司 治疗药物的制备方法
WO2003101979A1 (en) * 2002-05-31 2003-12-11 Pharmacia & Upjohn Company Llc Anthelmintic and insecticidal thiophene derivatives
US20050038068A1 (en) * 2003-05-16 2005-02-17 Iyengar Rajesh R. Thienopyridones as AMPK activators for the treatment of diabetes and obesity
WO2007019914A1 (en) * 2005-08-18 2007-02-22 Merck Patent Gmbh Use of thienopyridone derivatives as ampk activators and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
IL208988A0 (en) 2011-01-31
EA020773B1 (ru) 2015-01-30
BRPI0910832B1 (pt) 2020-09-15
DK2280952T3 (da) 2012-07-23
KR20160038065A (ko) 2016-04-06
PT2280952E (pt) 2012-09-28
EA201001733A1 (ru) 2011-06-30
JP2011519876A (ja) 2011-07-14
KR101648593B1 (ko) 2016-08-16
ECSP10010654A (es) 2011-01-31
MY160357A (en) 2017-02-28
WO2009135580A1 (en) 2009-11-12
BRPI0910832A8 (pt) 2016-07-12
MX2010011916A (es) 2010-11-26
HRP20120549T1 (hr) 2012-07-31
AU2009243811B2 (en) 2014-04-10
EP2280952B1 (en) 2012-06-27
ZA201008722B (en) 2012-01-25
PL2280952T3 (pl) 2012-10-31
CA2723429C (en) 2016-10-11
US8604202B2 (en) 2013-12-10
CN102015676A (zh) 2011-04-13
BRPI0910832A2 (pt) 2015-08-11
EP2280952A1 (en) 2011-02-09
CO6331304A2 (es) 2011-10-20
CY1113112T1 (el) 2016-04-13
HK1156313A1 (en) 2012-06-08
JP5536757B2 (ja) 2014-07-02
AR071530A1 (es) 2010-06-23
ES2388485T3 (es) 2012-10-15
US20110060001A1 (en) 2011-03-10
IL208988A (en) 2016-02-29
AU2009243811A1 (en) 2009-11-12
UA103617C2 (ru) 2013-11-11
SI2280952T1 (sl) 2012-09-28
CA2723429A1 (en) 2009-11-12
KR20110010757A (ko) 2011-02-07
NZ589690A (en) 2012-07-27
BRPI0910832B8 (pt) 2021-05-25

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