EA200870460A1 - Производные циклогексилпиразол-лактама в качестве ингибиторов 11-бета-гидроксистероиддегидрогеназы 1 - Google Patents

Производные циклогексилпиразол-лактама в качестве ингибиторов 11-бета-гидроксистероиддегидрогеназы 1

Info

Publication number
EA200870460A1
EA200870460A1 EA200870460A EA200870460A EA200870460A1 EA 200870460 A1 EA200870460 A1 EA 200870460A1 EA 200870460 A EA200870460 A EA 200870460A EA 200870460 A EA200870460 A EA 200870460A EA 200870460 A1 EA200870460 A1 EA 200870460A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
cyclogexylpyrazole
hydrogenase
hydroxysteroid
lactam
Prior art date
Application number
EA200870460A
Other languages
English (en)
Other versions
EA015675B1 (ru
Inventor
Томас Дэниел Айкер
Петер Бьяджо Анцевено
Жэньхуа Ли
Алексей Павлович Красутский
Томас Эдвард Мэбри
Ашраф Саеед
Нэнси Джун Снайдер
Грегори Алан Стефенсон
Хунци Тянь
Оуэн Брендан Уоллэйс
Леонард Лэрри мл. Виннероски
Яньпин Сюй
Original Assignee
Эли Лилли Энд Компани
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA200870460A1 publication Critical patent/EA200870460A1/ru
Publication of EA015675B1 publication Critical patent/EA015675B1/ru

Links

Classifications

    • 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

Abstract

В настоящем изобретении описаны новые соединения формулы, обладающие антагонистической активностью по отношению к 11 β-HSD первого типа, а также способы получения указанных соединений. Согласно другому варианту реализации в изобретении описаны фармацевтические композиции, содержащие соединения формулы I, a также способы применения указанных соединений и композиций для лечения диабета, гипергликемии, ожирения, гипертензии, гиперлипидемии, метаболического синдрома и других состояний, связанных с активностью 11β-HSD 1 типа.
EA200870460A 2006-04-21 2007-04-05 Производные циклогексилпиразол-лактама в качестве ингибиторов 11-бета-гидроксистероиддегидрогеназы 1 EA015675B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US74532006P 2006-04-21 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
EA200870460A1 true EA200870460A1 (ru) 2009-04-28
EA015675B1 EA015675B1 (ru) 2011-10-31

Family

ID=38595048

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200870460A EA015675B1 (ru) 2006-04-21 2007-04-05 Производные циклогексилпиразол-лактама в качестве ингибиторов 11-бета-гидроксистероиддегидрогеназы 1

Country Status (30)

Country Link
US (1) US7981918B2 (ru)
EP (1) EP2029579B1 (ru)
JP (1) JP5161869B2 (ru)
KR (1) KR101055576B1 (ru)
CN (1) CN101426783B (ru)
AR (1) AR060618A1 (ru)
AU (1) AU2007240550B2 (ru)
BR (1) BRPI0710229A2 (ru)
CA (1) CA2647677C (ru)
CO (1) CO6140026A2 (ru)
CR (1) CR10400A (ru)
DO (1) DOP2007000078A (ru)
EA (1) EA015675B1 (ru)
EC (1) ECSP088839A (ru)
ES (1) ES2533263T3 (ru)
HK (1) HK1126493A1 (ru)
IL (1) IL194835A (ru)
JO (1) JO3042B1 (ru)
MA (1) MA30476B1 (ru)
MX (1) MX2008013484A (ru)
MY (1) MY148128A (ru)
NO (1) NO20084403L (ru)
NZ (1) NZ571175A (ru)
PE (1) PE20080362A1 (ru)
SV (1) SV2008003070A (ru)
TN (1) TNSN08405A1 (ru)
TW (1) TWI347321B (ru)
UA (1) UA95798C2 (ru)
WO (1) WO2007124254A2 (ru)
ZA (1) ZA200808686B (ru)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2422165T3 (es) 2006-04-21 2013-09-09 Lilly Co Eli Derivados de ciclohexilimidazol lactama como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1
EA014718B1 (ru) * 2006-04-21 2011-02-28 Эли Лилли Энд Компани Производные бифениламидлактама в качестве ингибиторов 11-бета-гидроксистероиддегидрогеназы 1
BRPI0710262A2 (pt) 2006-04-24 2011-08-09 Lilly Co Eli composto, composição farmacêutica, e, intermediário
CA2646624C (en) * 2006-04-24 2013-08-06 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP5118692B2 (ja) 2006-04-24 2013-01-16 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の阻害剤としてのシクロヘキシル置換ピロリジノン
EP2021337B1 (en) 2006-04-25 2010-01-13 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
CA2649822C (en) * 2006-04-25 2013-08-13 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
DK2035379T3 (da) 2006-04-25 2010-09-06 Lilly Co Eli Inhibitorer af 11-beta-hydroxysteroiddehydrogenase 1
DK2049513T3 (da) * 2006-04-28 2012-02-27 Lilly Co Eli Piperidinylsubstituerede pyrrolidinoner som inhibitorer af 11-beta-hydroxysteroiddehydrogenase 1
WO2008106128A2 (en) 2007-02-26 2008-09-04 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
US8440658B2 (en) 2007-12-11 2013-05-14 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
RU2531272C2 (ru) 2008-05-01 2014-10-20 Вайтаи Фармасьютиклз, Инк. Циклические ингибиторы 11бета-гидроксистероид-дегидрогеназы 1
JP5777030B2 (ja) 2008-07-25 2015-09-09 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の阻害剤
US8487094B2 (en) 2008-07-25 2013-07-16 Boehringer Ingelheim International Gmbh Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1
EP2324018B1 (en) 2008-07-25 2013-09-04 Boehringer Ingelheim International GmbH Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1
CA2750517A1 (en) * 2009-02-04 2010-08-12 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8637505B2 (en) 2009-02-04 2014-01-28 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2243479A3 (en) 2009-04-20 2011-01-19 Abbott Laboratories Novel amide and amidine derivates and uses thereof
UA109255C2 (ru) 2009-04-30 2015-08-10 Берінгер Інгельхайм Інтернешнл Гмбх Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1
US8927539B2 (en) 2009-06-11 2015-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 based on the 1,3-oxazinan-2-one structure
JP5749263B2 (ja) 2009-07-01 2015-07-15 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
US8552212B2 (en) 2009-11-05 2013-10-08 Boehringer Ingelheim International Gmbh Chiral phosphorus ligands
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
EP2576570A1 (en) 2010-05-26 2013-04-10 Boehringer Ingelheim International GmbH 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
US8933072B2 (en) 2010-06-16 2015-01-13 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
EP2585444B1 (en) 2010-06-25 2014-10-22 Boehringer Ingelheim International GmbH Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders
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
EP2635268A1 (en) 2010-11-02 2013-09-11 Boehringer Ingelheim International GmbH Pharmaceutical combinations for the treatment of metabolic disorders
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
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
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
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
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
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
IN2014CN02949A (ru) * 2011-10-18 2015-07-03 Astellas Pharma Inc
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

Family Cites Families (21)

* 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
MXPA06012929A (es) 2004-05-07 2007-01-26 Janssen Pharmaceutica Nv Derivados de adamantil pirrolidin-2-ona como inhibidores de 11-beta hidroxiesteroide deshidrogenasa.
CN101001836B (zh) * 2004-05-07 2010-12-22 詹森药业有限公司 作为11-β羟基类固醇脱氢酶抑制剂的吡咯烷-2-酮和哌啶-2-酮衍生物
US8138342B2 (en) 2004-10-12 2012-03-20 High Point Pharmacueticals, LLC 11β-hydroxysteroid dehydrogenase type 1 active spiro compounds
DK1807072T3 (da) 2004-10-29 2009-03-16 Lilly Co Eli Cycloalkyllactamderivater som inhibitorer af 11-beta-hydroxysteroid-dehydrogenase 1
WO2006053024A2 (en) 2004-11-10 2006-05-18 Incyte Corporation Lactam compounds and their use as pharmaceuticals
DK1830841T3 (da) 2004-12-20 2008-10-13 Lilly Co Eli Cycloalkyllactamderivater som inhibitorer af 11-beta-hydroxysteroid-dehydrogenase 1
DE602005008282D1 (de) 2004-12-21 2008-08-28 Lilly Co Eli Cycloalkyl-lactam-derivate als inhibitoren von 11-beta-hydroxysteroiddehydrogenase 1
US20090264650A1 (en) 2005-03-31 2009-10-22 Nobuo Cho Prophylactic/Therapeutic Agent for Diabetes
ES2322727B1 (es) 2005-07-28 2010-04-22 Universidad Del Pais Vasco Metodo para cuantificar la union receptor acoplado a proteina g (gpcr)-proteina g mediante el empleo de un array de membranas celulares.
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
ES2422165T3 (es) * 2006-04-21 2013-09-09 Lilly Co Eli Derivados de ciclohexilimidazol lactama como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1
EA014718B1 (ru) * 2006-04-21 2011-02-28 Эли Лилли Энд Компани Производные бифениламидлактама в качестве ингибиторов 11-бета-гидроксистероиддегидрогеназы 1
BRPI0710262A2 (pt) 2006-04-24 2011-08-09 Lilly Co Eli composto, composição farmacêutica, e, intermediário
CA2646624C (en) 2006-04-24 2013-08-06 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP5118692B2 (ja) 2006-04-24 2013-01-16 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の阻害剤としてのシクロヘキシル置換ピロリジノン
DK2035379T3 (da) 2006-04-25 2010-09-06 Lilly Co Eli Inhibitorer af 11-beta-hydroxysteroiddehydrogenase 1
CA2649822C (en) 2006-04-25 2013-08-13 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
DK2049513T3 (da) 2006-04-28 2012-02-27 Lilly Co Eli Piperidinylsubstituerede pyrrolidinoner som inhibitorer af 11-beta-hydroxysteroiddehydrogenase 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
BRPI0710229A2 (pt) 2011-08-02
AU2007240550B2 (en) 2012-02-23
HK1126493A1 (en) 2009-09-04
EP2029579A2 (en) 2009-03-04
IL194835A0 (en) 2009-08-03
JP2009534398A (ja) 2009-09-24
IL194835A (en) 2015-04-30
EP2029579B1 (en) 2014-12-31
CA2647677A1 (en) 2007-11-01
US7981918B2 (en) 2011-07-19
ECSP088839A (es) 2008-11-27
EA015675B1 (ru) 2011-10-31
CR10400A (es) 2009-01-14
AR060618A1 (es) 2008-07-02
WO2007124254A3 (en) 2007-12-27
ZA200808686B (en) 2009-12-30
KR101055576B1 (ko) 2011-08-08
CO6140026A2 (es) 2010-03-19
US20090111800A1 (en) 2009-04-30
KR20080109867A (ko) 2008-12-17
TNSN08405A1 (en) 2010-04-14
CN101426783A (zh) 2009-05-06
MX2008013484A (es) 2008-10-30
TW200811141A (en) 2008-03-01
MY148128A (en) 2013-02-28
TWI347321B (en) 2011-08-21
NZ571175A (en) 2011-10-28
NO20084403L (no) 2008-11-14
UA95798C2 (ru) 2011-09-12
JO3042B1 (ar) 2016-09-05
ES2533263T3 (es) 2015-04-08
CA2647677C (en) 2014-03-18
DOP2007000078A (es) 2007-11-15
PE20080362A1 (es) 2008-04-25
SV2008003070A (es) 2010-01-18
JP5161869B2 (ja) 2013-03-13
WO2007124254A2 (en) 2007-11-01
MA30476B1 (fr) 2009-06-01
AU2007240550A1 (en) 2007-11-01
CN101426783B (zh) 2013-10-30

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