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

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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
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AU2007240450B2 (en) 2006-04-21 2011-12-22 Eli Lilly And Company Cyclohexylimidazole lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
AU2007240458B2 (en) 2006-04-21 2012-03-15 Eli Lilly And Company Biphenyl amide lactam derivatives as inhibitors of 11- beta-hydroxysteroid dehydrogenase 1
ES2533263T3 (es) 2006-04-21 2015-04-08 Eli Lilly And Company Derivados de ciclohexilpirazol-lactama como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1
PL2049475T3 (pl) 2006-04-24 2012-08-31 Lilly Co Eli Pirolidynony podstawione cykloheksylem jako inhibitory 11-betahydrokysterydu dehydrogenazy 1
PL2021336T3 (pl) 2006-04-24 2010-11-30 Lilly Co Eli Inhibitory dehydrogenazy 11-ß- hydroksysteroidowej typu 1
DK2029529T3 (da) 2006-04-24 2010-09-20 Lilly Co Eli Substitueret pyrrolidinone som inhibitor af 11-beta-hydroxysteroiddehydrogenase 1
WO2007127763A2 (en) 2006-04-25 2007-11-08 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP5101602B2 (ja) * 2006-04-25 2012-12-19 イーライ リリー アンド カンパニー １１−β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤
EA014719B1 (ru) * 2006-04-28 2011-02-28 Эли Лилли Энд Компани Пиперидинилзамещённые пирролидиноны в качестве ингибиторов 11-бета-гидроксистероид дегидрогеназы 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
US8871208B2 (en) * 2009-12-04 2014-10-28 Abbvie Inc. 11-β-hydroxysteroid dehydrogenase type 1 (11β-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
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
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
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
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2683699B1 (de) 2011-03-08 2015-06-24 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
US8901114B2 (en) 2011-03-08 2014-12-02 Sanofi Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof
CA2841932A1 (en) * 2011-07-13 2013-01-17 Novartis Ag 4 - piperidinyl compounds for use as tankyrase inhibitors
WO2013010092A1 (en) 2011-07-13 2013-01-17 Novartis Ag 4-oxo-3,5,7,8-tetrahydro-4h-pyrano {4,3-d} pyrminidinyl compounds for use as tankyrase inhibitors
CN103781776A (zh) 2011-07-13 2014-05-07 诺华股份有限公司 用作端锚聚合酶抑制剂的新的2-哌啶-1-基-乙酰胺化合物
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
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
BR112014009524A2 (pt) 2011-10-18 2017-05-09 Astellas Pharma Inc composto heterocíclico bicíclico
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
MXPA06012932A (es) * 2004-05-07 2007-01-26 Janssen Pharmaceutica Nv Derivados de pirrolidin-2-ona y piperidin-2-ona como inhibidores de 11-beta hidroxiesteroide deshidrogenasa.
ATE397586T1 (de) * 2004-05-07 2008-06-15 Janssen Pharmaceutica Nv Adamantyl pyrrolidin-2-on-derivate als 11-beta hydroxysteroid dehydrogenas inhibitoren
US8138342B2 (en) 2004-10-12 2012-03-20 High Point Pharmacueticals, LLC 11β-hydroxysteroid dehydrogenase type 1 active spiro compounds
EP1807072B1 (en) 2004-10-29 2009-01-07 Eli Lilly And Company Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
KR101368228B1 (ko) 2004-11-10 2014-02-27 인사이트 코포레이션 락탐 화합물 및 약제로서의 이의 용도
PT1830841E (pt) 2004-12-20 2008-12-15 Lilly Co Eli Derivados de cicloalquil-lactamas como inibidores da 11-beta-hidroxiesteróide desidrogenase 1
US7834194B2 (en) 2004-12-21 2010-11-16 Eli Lilly And Company Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
WO2006104280A1 (ja) 2005-03-31 2006-10-05 Takeda Pharmaceutical Company Limited 糖尿病の予防・治療剤
WO2007084314A2 (en) 2006-01-12 2007-07-26 Incyte Corporation MODULATORS OF 11-ß HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
AU2007240450B2 (en) 2006-04-21 2011-12-22 Eli Lilly And Company Cyclohexylimidazole lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
ES2533263T3 (es) 2006-04-21 2015-04-08 Eli Lilly And Company Derivados de ciclohexilpirazol-lactama como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1
AU2007240458B2 (en) 2006-04-21 2012-03-15 Eli Lilly And Company Biphenyl amide lactam derivatives as inhibitors of 11- beta-hydroxysteroid dehydrogenase 1
DK2029529T3 (da) 2006-04-24 2010-09-20 Lilly Co Eli Substitueret pyrrolidinone som inhibitor af 11-beta-hydroxysteroiddehydrogenase 1
PL2049475T3 (pl) 2006-04-24 2012-08-31 Lilly Co Eli Pirolidynony podstawione cykloheksylem jako inhibitory 11-betahydrokysterydu dehydrogenazy 1
PL2021336T3 (pl) 2006-04-24 2010-11-30 Lilly Co Eli Inhibitory dehydrogenazy 11-ß- hydroksysteroidowej typu 1
WO2007127763A2 (en) 2006-04-25 2007-11-08 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP5101602B2 (ja) 2006-04-25 2012-12-19 イーライ リリー アンド カンパニー １１−β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤
EA014719B1 (ru) 2006-04-28 2011-02-28 Эли Лилли Энд Компани Пиперидинилзамещённые пирролидиноны в качестве ингибиторов 11-бета-гидроксистероид дегидрогеназы 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
CA2648236A1 (en) 2007-11-08
EP2021337A2 (en) 2009-02-11
DK2021337T3 (da) 2010-03-29
MX2008013651A (es) 2008-11-04
SI2021337T1 (sl) 2010-05-31
ATE455110T1 (de) 2010-01-15
EA015516B1 (ru) 2011-08-30
WO2007127726A2 (en) 2007-11-08
CN101454310A (zh) 2009-06-10
JP5189079B2 (ja) 2013-04-24
CY1109842T1 (el) 2014-09-10
JP2009535356A (ja) 2009-10-01
WO2007127726A3 (en) 2008-01-03
AU2007244904B2 (en) 2012-05-31
DE602007004324D1 (en) 2010-03-04
ES2336849T3 (es) 2010-04-16
US7994176B2 (en) 2011-08-09
PT2021337E (pt) 2010-02-22
PL2021337T3 (pl) 2010-06-30
EP2021337B1 (en) 2010-01-13
BRPI0710050A2 (pt) 2011-08-02
EA200870474A1 (ru) 2009-04-28
CA2648236C (en) 2013-05-28
US20090099182A1 (en) 2009-04-16
AU2007244904A1 (en) 2007-11-08

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