CN101426783B - 作为11-β-羟基甾族化合物脱氢酶1的抑制剂的环己基吡唑-内酰胺衍生物 - Google Patents

作为11-β-羟基甾族化合物脱氢酶1的抑制剂的环己基吡唑-内酰胺衍生物 Download PDF

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Publication number
CN101426783B
CN101426783B CN2007800142829A CN200780014282A CN101426783B CN 101426783 B CN101426783 B CN 101426783B CN 2007800142829 A CN2007800142829 A CN 2007800142829A CN 200780014282 A CN200780014282 A CN 200780014282A CN 101426783 B CN101426783 B CN 101426783B
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China
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compound
alkyl
mmol
halogen
tetrahydro
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Expired - Fee Related
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CN2007800142829A
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English (en)
Chinese (zh)
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CN101426783A (zh
Inventor
T·D·艾歇尔
P·B·安泽维诺
R·李
A·P·克拉苏特斯基
T·E·马布里
A·萨伊德
N·J·斯奈德
G·A·斯蒂芬森
H·田
欧文·布伦丹·华莱士
L·L·小温纳罗斯基
Y·徐
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Eli Lilly and Co
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Eli Lilly and Co
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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2007800142829A 2006-04-21 2007-04-05 作为11-β-羟基甾族化合物脱氢酶1的抑制剂的环己基吡唑-内酰胺衍生物 Expired - Fee Related CN101426783B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US74532006P 2006-04-21 2006-04-21
US60/745,320 2006-04-21
PCT/US2007/066069 WO2007124254A2 (en) 2006-04-21 2007-04-05 Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

Publications (2)

Publication Number Publication Date
CN101426783A CN101426783A (zh) 2009-05-06
CN101426783B true CN101426783B (zh) 2013-10-30

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Country Status (29)

Country Link
US (1) US7981918B2 (enExample)
EP (1) EP2029579B1 (enExample)
JP (1) JP5161869B2 (enExample)
KR (1) KR101055576B1 (enExample)
CN (1) CN101426783B (enExample)
AR (1) AR060618A1 (enExample)
AU (1) AU2007240550B2 (enExample)
BR (1) BRPI0710229A2 (enExample)
CA (1) CA2647677C (enExample)
CO (1) CO6140026A2 (enExample)
CR (1) CR10400A (enExample)
DO (1) DOP2007000078A (enExample)
EA (1) EA015675B1 (enExample)
EC (1) ECSP088839A (enExample)
ES (1) ES2533263T3 (enExample)
IL (1) IL194835A (enExample)
JO (1) JO3042B1 (enExample)
MA (1) MA30476B1 (enExample)
MX (1) MX2008013484A (enExample)
MY (1) MY148128A (enExample)
NO (1) NO20084403L (enExample)
NZ (1) NZ571175A (enExample)
PE (1) PE20080362A1 (enExample)
SV (1) SV2008003070A (enExample)
TN (1) TNSN08405A1 (enExample)
TW (1) TWI347321B (enExample)
UA (1) UA95798C2 (enExample)
WO (1) WO2007124254A2 (enExample)
ZA (1) ZA200808686B (enExample)

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* Cited by examiner, † Cited by third party
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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
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
US7968585B2 (en) 2006-04-25 2011-06-28 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
EP2021337B1 (en) 2006-04-25 2010-01-13 Eli Lilly And Company 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
MX2008013844A (es) * 2006-04-28 2008-11-10 Lilly Co Eli Pirrolidinonas substituidas con pieridinilo como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1.
US8835426B2 (en) 2007-02-26 2014-09-16 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11β-hydroxysteroid dehydrogenase 1
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
CA2708303A1 (en) 2007-12-11 2009-06-18 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
KR20110002492A (ko) 2008-05-01 2011-01-07 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
WO2010011314A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1
US8846668B2 (en) 2008-07-25 2014-09-30 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2729993A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
US8598163B2 (en) * 2009-02-04 2013-12-03 Vitae Pharmaceuticals, Inc. Derivatives of [1,3]Oxazin-2-one useful for the treatment of metabolic diseases such as lipid disorders
JP5679997B2 (ja) 2009-02-04 2015-03-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 11β−ヒドロキシステロイドデヒドロゲナーゼ1の環状阻害剤
US8507493B2 (en) 2009-04-20 2013-08-13 Abbvie Inc. Amide and amidine derivatives and uses thereof
UA109255C2 (ru) 2009-04-30 2015-08-10 Берінгер Інгельхайм Інтернешнл Гмбх Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1
WO2011011123A1 (en) 2009-06-11 2011-01-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
WO2011002910A1 (en) 2009-07-01 2011-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2496589B1 (en) 2009-11-05 2014-03-05 Boehringer Ingelheim International GmbH Novel chiral phosphorus ligands
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
EP2576570A1 (en) 2010-05-26 2013-04-10 Boehringer Ingelheim International GmbH 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
EP2582698B1 (en) 2010-06-16 2016-09-14 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
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
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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
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
CA2813671A1 (en) 2010-11-02 2012-05-10 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
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
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
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
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
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
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
AR099936A1 (es) 2014-04-04 2016-08-31 Sanofi Sa Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y trastornos relacionados
US10858347B2 (en) 2015-12-31 2020-12-08 Karyopharm Therapeutics Inc. Multicyclic compounds and uses thereof
CN115916766A (zh) 2021-02-25 2023-04-04 阿普塔生物治疗公司 新型吡唑衍生物

Citations (2)

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WO2005108361A1 (en) * 2004-05-07 2005-11-17 Janssen Pharmaceutica N.V. Adamantyl pyrrolidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
WO2005108360A1 (en) * 2004-05-07 2005-11-17 Janssen Pharmaceutica N.V. Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors

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BRPI0710273A2 (pt) * 2006-04-21 2011-08-09 Lilly Co Eli composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, intermediário
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
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Patent Citations (2)

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WO2005108361A1 (en) * 2004-05-07 2005-11-17 Janssen Pharmaceutica N.V. Adamantyl pyrrolidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
WO2005108360A1 (en) * 2004-05-07 2005-11-17 Janssen Pharmaceutica N.V. Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors

Also Published As

Publication number Publication date
ZA200808686B (en) 2009-12-30
BRPI0710229A2 (pt) 2011-08-02
US20090111800A1 (en) 2009-04-30
CN101426783A (zh) 2009-05-06
AR060618A1 (es) 2008-07-02
CA2647677A1 (en) 2007-11-01
AU2007240550B2 (en) 2012-02-23
AU2007240550A1 (en) 2007-11-01
IL194835A0 (en) 2009-08-03
IL194835A (en) 2015-04-30
WO2007124254A3 (en) 2007-12-27
US7981918B2 (en) 2011-07-19
UA95798C2 (ru) 2011-09-12
SV2008003070A (es) 2010-01-18
TNSN08405A1 (en) 2010-04-14
EA015675B1 (ru) 2011-10-31
KR101055576B1 (ko) 2011-08-08
PE20080362A1 (es) 2008-04-25
JP2009534398A (ja) 2009-09-24
EA200870460A1 (ru) 2009-04-28
MX2008013484A (es) 2008-10-30
ECSP088839A (es) 2008-11-27
JP5161869B2 (ja) 2013-03-13
HK1126493A1 (en) 2009-09-04
EP2029579B1 (en) 2014-12-31
WO2007124254A2 (en) 2007-11-01
NO20084403L (no) 2008-11-14
JO3042B1 (ar) 2016-09-05
CR10400A (es) 2009-01-14
EP2029579A2 (en) 2009-03-04
MA30476B1 (fr) 2009-06-01
CA2647677C (en) 2014-03-18
TWI347321B (en) 2011-08-21
DOP2007000078A (es) 2007-11-15
TW200811141A (en) 2008-03-01
ES2533263T3 (es) 2015-04-08
MY148128A (en) 2013-02-28
CO6140026A2 (es) 2010-03-19
KR20080109867A (ko) 2008-12-17
NZ571175A (en) 2011-10-28

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