CN101115735B - 作为高血糖素受体拮抗剂的取代的噻吩衍生物、制备和治疗用途 - Google Patents

作为高血糖素受体拮抗剂的取代的噻吩衍生物、制备和治疗用途 Download PDF

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Publication number
CN101115735B
CN101115735B CN2006800046189A CN200680004618A CN101115735B CN 101115735 B CN101115735 B CN 101115735B CN 2006800046189 A CN2006800046189 A CN 2006800046189A CN 200680004618 A CN200680004618 A CN 200680004618A CN 101115735 B CN101115735 B CN 101115735B
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CN
China
Prior art keywords
thiophene
biphenyl
carbonyl
amino
dimethyl
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.)
Expired - Fee Related
Application number
CN2006800046189A
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English (en)
Chinese (zh)
Other versions
CN101115735A (zh
Inventor
M·D·沙佩尔
S·E·康纳
A·E·特里普
朱国新
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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Publication date
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Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN101115735A publication Critical patent/CN101115735A/zh
Application granted granted Critical
Publication of CN101115735B publication Critical patent/CN101115735B/zh
Expired - Fee Related legal-status Critical Current
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/26Heterocyclic 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
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2006800046189A 2005-02-11 2006-02-09 作为高血糖素受体拮抗剂的取代的噻吩衍生物、制备和治疗用途 Expired - Fee Related CN101115735B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US65249205P 2005-02-11 2005-02-11
US60/652,492 2005-02-11
PCT/US2006/004461 WO2006086488A2 (en) 2005-02-11 2006-02-09 Substituted thiophene derivatives as glucagon receptor antagonists, preparation and therapeutic uses

Publications (2)

Publication Number Publication Date
CN101115735A CN101115735A (zh) 2008-01-30
CN101115735B true CN101115735B (zh) 2013-01-09

Family

ID=36694345

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2006800046189A Expired - Fee Related CN101115735B (zh) 2005-02-11 2006-02-09 作为高血糖素受体拮抗剂的取代的噻吩衍生物、制备和治疗用途

Country Status (25)

Country Link
US (1) US8084489B2 (enExample)
EP (1) EP1856090B1 (enExample)
JP (1) JP4988604B2 (enExample)
KR (1) KR20070104409A (enExample)
CN (1) CN101115735B (enExample)
AT (1) ATE445609T1 (enExample)
AU (1) AU2006213894B2 (enExample)
BR (1) BRPI0607015A2 (enExample)
CA (1) CA2597073C (enExample)
CR (1) CR9304A (enExample)
CY (1) CY1109624T1 (enExample)
DE (1) DE602006009773D1 (enExample)
DK (1) DK1856090T3 (enExample)
EA (1) EA200701705A1 (enExample)
ES (1) ES2332470T3 (enExample)
IL (1) IL184932A0 (enExample)
MA (1) MA29432B1 (enExample)
MX (1) MX2007009661A (enExample)
NO (1) NO20074567L (enExample)
PL (1) PL1856090T3 (enExample)
PT (1) PT1856090E (enExample)
SI (1) SI1856090T1 (enExample)
TN (1) TNSN07313A1 (enExample)
WO (1) WO2006086488A2 (enExample)
ZA (1) ZA200706354B (enExample)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA013003B1 (ru) * 2004-06-14 2010-02-26 Эли Лилли Энд Компани Антагонисты рецептора глюкагона, их получение и терапевтическое применение
PT2129654E (pt) 2007-02-09 2014-09-04 Metabasis Therapeutics Inc Antagonistas do receptor de glucagina
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CN104803891B (zh) 2008-08-13 2017-10-20 症变治疗公司 胰高血糖素拮抗剂
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
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
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
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
CN103261165B (zh) 2010-12-23 2015-08-26 辉瑞公司 胰高血糖素受体调节剂
LT2673260T (lt) 2011-02-08 2016-10-25 Pfizer Inc. Gliukagono receptoriaus moduliatorius
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
WO2012120056A1 (de) 2011-03-08 2012-09-13 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8710050B2 (en) 2011-03-08 2014-04-29 Sanofi Di and tri- substituted oxathiazine derivatives, method for the production, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
WO2012120053A1 (de) 2011-03-08 2012-09-13 Sanofi Verzweigte 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
CN103732578B (zh) 2011-07-22 2015-08-12 辉瑞大药厂 喹啉基胰高血糖素受体调节剂
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
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
TW201427658A (zh) 2012-12-10 2014-07-16 Merck Sharp & Dohme 藉由投予升糖素受體拮抗劑及膽固醇吸收抑制劑治療糖尿病之方法
EP3065736B1 (en) 2013-11-04 2018-11-14 Merck Sharp & Dohme Corp. Glucagon receptor antagonist compounds, compositions thereof, and methods of use
EP3154956A4 (en) 2014-06-12 2018-01-17 Ligand Pharmaceuticals, Inc. Glucagon antagonists
WO2017049140A2 (en) 2015-09-18 2017-03-23 Wake Forest University Health Sciences Angiotensin (1-7) analogs and methods relating thereto
EP3821917A1 (en) 2015-10-05 2021-05-19 Hettwer Holding ApS Compositions and methods for treatment of bone defects
CA2914601A1 (en) * 2015-12-11 2017-06-11 Wake Forest University Health Sciences Angiotensin-(1-7) analogs and methods relating thereto
MA46089A (fr) 2016-08-30 2019-07-10 Regeneron Pharma Procédés de traitement de la résistance à l'insuline grave par interférence avec la signalisation du récepteur du glucagon
EP3529278A1 (en) 2016-10-20 2019-08-28 Regeneron Pharmaceuticals, Inc. Methods of lowering blood glucose levels
MX2020002057A (es) 2017-08-22 2020-07-13 Regeneron Pharma Metodos para tratar trastornos del ciclo de la urea mediante interferencia con la señalizacion del receptor del glucagon.
EP3752249A1 (en) 2018-02-13 2020-12-23 Ligand Pharmaceuticals, Inc. Glucagon receptor antagonists
MX2022007665A (es) 2019-12-20 2022-07-19 Bayer Ag Tiofenocarboxamidas sustituidas y sus derivados.

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005511683A (ja) * 2001-12-03 2005-04-28 ノボ ノルディスク アクティーゼルスカブ 新規なグルカゴンアンタゴニスト
AU2003233780A1 (en) * 2002-06-27 2004-01-19 Novo Nordisk A/S Novel glucagon antagonists/inverse agonists
ES2428538T3 (es) * 2004-05-28 2013-11-08 Eli Lilly And Company Antagonistas del receptor de glucagón, preparación y usos terapéuticos
EA013003B1 (ru) * 2004-06-14 2010-02-26 Эли Лилли Энд Компани Антагонисты рецептора глюкагона, их получение и терапевтическое применение

Also Published As

Publication number Publication date
PT1856090E (pt) 2009-11-18
CA2597073C (en) 2014-11-25
CY1109624T1 (el) 2014-08-13
EP1856090B1 (en) 2009-10-14
TNSN07313A1 (en) 2008-12-31
AU2006213894B2 (en) 2011-12-08
NO20074567L (no) 2007-11-08
MA29432B1 (fr) 2008-05-02
JP4988604B2 (ja) 2012-08-01
EA200701705A1 (ru) 2008-02-28
KR20070104409A (ko) 2007-10-25
ATE445609T1 (de) 2009-10-15
ZA200706354B (en) 2008-11-26
CN101115735A (zh) 2008-01-30
CA2597073A1 (en) 2006-08-17
MX2007009661A (es) 2007-09-25
US20100137417A1 (en) 2010-06-03
JP2008530102A (ja) 2008-08-07
WO2006086488A3 (en) 2006-12-14
AU2006213894A1 (en) 2006-08-17
EP1856090A2 (en) 2007-11-21
IL184932A0 (en) 2007-12-03
SI1856090T1 (sl) 2010-02-26
US8084489B2 (en) 2011-12-27
CR9304A (es) 2008-03-31
BRPI0607015A2 (pt) 2009-12-01
ES2332470T3 (es) 2010-02-05
WO2006086488A2 (en) 2006-08-17
DE602006009773D1 (de) 2009-11-26
DK1856090T3 (da) 2009-11-30
PL1856090T3 (pl) 2010-02-26

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Granted publication date: 20130109

Termination date: 20160209