CN101454310B - 11-β-羟类固醇脱氢酶1的抑制剂 - Google Patents

11-β-羟类固醇脱氢酶1的抑制剂 Download PDF

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Publication number
CN101454310B
CN101454310B CN2007800148990A CN200780014899A CN101454310B CN 101454310 B CN101454310 B CN 101454310B CN 2007800148990 A CN2007800148990 A CN 2007800148990A CN 200780014899 A CN200780014899 A CN 200780014899A CN 101454310 B CN101454310 B CN 101454310B
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halogen
alkyl
compound
mmol
dichloro
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CN101454310A (zh
Inventor
李仁华
T·E·马布里
L·L·小温纳罗斯基
徐彦平
欧文·布伦丹·华莱士
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Eli Lilly and Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • 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
    • A61P3/08—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • 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
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • C07D401/14—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 three or more hetero rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • General Health & Medical Sciences (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)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
CN2007800148990A 2006-04-25 2007-04-24 11-β-羟类固醇脱氢酶1的抑制剂 Expired - Fee Related CN101454310B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US74556906P 2006-04-25 2006-04-25
US60/745,569 2006-04-25
PCT/US2007/067296 WO2007127726A2 (en) 2006-04-25 2007-04-24 Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

Publications (2)

Publication Number Publication Date
CN101454310A CN101454310A (zh) 2009-06-10
CN101454310B true CN101454310B (zh) 2013-07-17

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CN2007800148990A Expired - Fee Related CN101454310B (zh) 2006-04-25 2007-04-24 11-β-羟类固醇脱氢酶1的抑制剂

Country Status (18)

Country Link
US (1) US7994176B2 (enExample)
EP (1) EP2021337B1 (enExample)
JP (1) JP5189079B2 (enExample)
CN (1) CN101454310B (enExample)
AT (1) ATE455110T1 (enExample)
AU (1) AU2007244904B2 (enExample)
BR (1) BRPI0710050A2 (enExample)
CA (1) CA2648236C (enExample)
CY (1) CY1109842T1 (enExample)
DE (1) DE602007004324D1 (enExample)
DK (1) DK2021337T3 (enExample)
EA (1) EA015516B1 (enExample)
ES (1) ES2336849T3 (enExample)
MX (1) MX2008013651A (enExample)
PL (1) PL2021337T3 (enExample)
PT (1) PT2021337E (enExample)
SI (1) SI2021337T1 (enExample)
WO (1) WO2007127726A2 (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ571175A (en) 2006-04-21 2011-10-28 Lilly Co Eli Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
BRPI0710273A2 (pt) 2006-04-21 2011-08-09 Lilly Co Eli composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, intermediário
US8088776B2 (en) * 2006-04-21 2012-01-03 Eli Lilly And Company Biphenyl amide lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
ATE472542T1 (de) 2006-04-24 2010-07-15 Lilly Co Eli 11-beta-hydroxysteroid-dehydrogenase-1-hemmer
ATE543798T1 (de) 2006-04-24 2012-02-15 Lilly Co Eli Cyclohexyl-substituierte pyrrolidinone als hemmer von 11-beta-hydroxysteroiddehydrogenase 1
CA2649650C (en) 2006-04-24 2014-01-14 Eli Lilly And Company Substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
AU2007244863B2 (en) * 2006-04-25 2012-01-19 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
US7968585B2 (en) 2006-04-25 2011-06-28 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
MX2008013844A (es) * 2006-04-28 2008-11-10 Lilly Co Eli Pirrolidinonas substituidas con pieridinilo como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1.
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US8507493B2 (en) 2009-04-20 2013-08-13 Abbvie Inc. Amide and amidine derivatives and uses thereof
US8440710B2 (en) * 2009-10-15 2013-05-14 Hoffmann-La Roche Inc. HSL inhibitors useful in the treatment of diabetes
WO2011068927A2 (en) * 2009-12-04 2011-06-09 Abbott Laboratories 11-β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 (11B-HSD1) INHIBITORS AND USES THEREOF
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
JP6023045B2 (ja) * 2010-05-27 2016-11-09 ファルマツェル、ゲーエムベーハー 新規７α−ヒドロキシステロイドデヒドロゲナーゼノックアウト突然変異体およびその使用
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
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
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, 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
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
WO2012120054A1 (de) 2011-03-08 2012-09-13 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
WO2012120055A1 (de) 2011-03-08 2012-09-13 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2766349B1 (de) 2011-03-08 2016-06-01 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2683704B1 (de) 2011-03-08 2014-12-17 Sanofi Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
CA2841932A1 (en) * 2011-07-13 2013-01-17 Novartis Ag 4 - piperidinyl compounds for use as tankyrase inhibitors
US9227982B2 (en) 2011-07-13 2016-01-05 Novartis Ag 4-oxo-3,5,7,8-tetrahydro-4H-pyrano[4,3-d]pyrminidinyl compounds for use as tankyrase inhibitors
US9181266B2 (en) 2011-07-13 2015-11-10 Novartis Ag 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors
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
JP6020459B2 (ja) 2011-10-18 2016-11-02 アステラス製薬株式会社 二環式ヘテロ環化合物
CN105793264B (zh) * 2014-03-10 2017-09-01 四川海思科制药有限公司 取代的二氢苯并呋喃‑哌啶‑甲酮衍生物、其制备及用途
CN108046988B (zh) * 2017-12-25 2021-04-16 云南民族大学 一种高效制备碘代醇的方法

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004056744A1 (en) 2002-12-23 2004-07-08 Janssen Pharmaceutica N.V. Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors
EP1747198B1 (en) 2004-05-07 2008-06-04 Janssen Pharmaceutica N.V. Adamantyl pyrrolidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
CA2565630C (en) * 2004-05-07 2013-05-28 Janssen Pharmaceutica N.V. Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
EP1802623A1 (en) 2004-10-12 2007-07-04 Novo Nordisk A/S 11beta-hydroxysteroid dehydrogenase type 1 active spiro compounds
WO2006049952A1 (en) 2004-10-29 2006-05-11 Eli Lilly And Company Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
SG161261A1 (en) 2004-11-10 2010-05-27 Incyte Corp Lactam compounds and their use as pharmaceuticals
ATE399546T1 (de) 2004-12-20 2008-07-15 Lilly Co Eli Cycloalkyl-lactam-derivate als inhibitoren von 11-beta-hydroxysteroiddehydrogenase 1
EP1830840B1 (en) 2004-12-21 2008-07-16 Eli Lilly And Company Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
EP1864971A4 (en) 2005-03-31 2010-02-10 Takeda Pharmaceutical PROPHYLACTIC / THERAPEUTIC AGENT AGAINST DIABETES
US7998959B2 (en) 2006-01-12 2011-08-16 Incyte Corporation Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
US8088776B2 (en) 2006-04-21 2012-01-03 Eli Lilly And Company Biphenyl amide lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
BRPI0710273A2 (pt) 2006-04-21 2011-08-09 Lilly Co Eli composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, intermediário
NZ571175A (en) 2006-04-21 2011-10-28 Lilly Co Eli Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
ATE543798T1 (de) 2006-04-24 2012-02-15 Lilly Co Eli Cyclohexyl-substituierte pyrrolidinone als hemmer von 11-beta-hydroxysteroiddehydrogenase 1
CA2649650C (en) 2006-04-24 2014-01-14 Eli Lilly And Company Substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
ATE472542T1 (de) 2006-04-24 2010-07-15 Lilly Co Eli 11-beta-hydroxysteroid-dehydrogenase-1-hemmer
AU2007244863B2 (en) 2006-04-25 2012-01-19 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
US7968585B2 (en) 2006-04-25 2011-06-28 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
MX2008013844A (es) 2006-04-28 2008-11-10 Lilly Co Eli Pirrolidinonas substituidas con pieridinilo como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1.
CL2008001839A1 (es) 2007-06-21 2009-01-16 Incyte Holdings Corp Compuestos derivados de 2,7-diazaespirociclos, inhibidores de 11-beta hidroxil esteroide deshidrogenasa tipo 1; composicion farmaceutica que comprende a dichos compuestos; utiles para tratar la obesidad, diabetes, intolerancia a la glucosa, diabetes tipo ii, entre otras enfermedades.

Also Published As

Publication number Publication date
US20090099182A1 (en) 2009-04-16
BRPI0710050A2 (pt) 2011-08-02
ATE455110T1 (de) 2010-01-15
EP2021337B1 (en) 2010-01-13
WO2007127726A2 (en) 2007-11-08
CA2648236A1 (en) 2007-11-08
ES2336849T3 (es) 2010-04-16
EP2021337A2 (en) 2009-02-11
JP5189079B2 (ja) 2013-04-24
EA015516B1 (ru) 2011-08-30
DK2021337T3 (da) 2010-03-29
WO2007127726A3 (en) 2008-01-03
AU2007244904A1 (en) 2007-11-08
CY1109842T1 (el) 2014-09-10
MX2008013651A (es) 2008-11-04
SI2021337T1 (sl) 2010-05-31
EA200870474A1 (ru) 2009-04-28
JP2009535356A (ja) 2009-10-01
AU2007244904B2 (en) 2012-05-31
PL2021337T3 (pl) 2010-06-30
DE602007004324D1 (en) 2010-03-04
US7994176B2 (en) 2011-08-09
CN101454310A (zh) 2009-06-10
PT2021337E (pt) 2010-02-22
CA2648236C (en) 2013-05-28

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