PE20081704A1 - Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa - Google Patents

Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa

Info

Publication number
PE20081704A1
PE20081704A1 PE2008000179A PE2008000179A PE20081704A1 PE 20081704 A1 PE20081704 A1 PE 20081704A1 PE 2008000179 A PE2008000179 A PE 2008000179A PE 2008000179 A PE2008000179 A PE 2008000179A PE 20081704 A1 PE20081704 A1 PE 20081704A1
Authority
PE
Peru
Prior art keywords
alkyl
tetrazol
piperidin
acetic
hydroxy
Prior art date
Application number
PE2008000179A
Other languages
English (en)
Inventor
Yves Leblanc
David Powell
Yeeman K Ramtohul
Serge Leger
Original Assignee
Merck Frosst Canada Ltd
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 Merck Frosst Canada Ltd filed Critical Merck Frosst Canada Ltd
Publication of PE20081704A1 publication Critical patent/PE20081704A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE AZACICLOALCANO DE FORMULA (I), DONDE q Y r SON 0 O 1; X-Y ES N-CRaRb, CR14-O, CR14-S(O)0-2 O CR13-CraRb; Ar ES FENILO, NAFTILO O HETEROARILO; Ra Y Rb SON H O ALQUILO C1-C3 SUSTITUIDO CON FLUOR O HIDROXI; R14 ES H O ALQUILO C1-C3; W ES UN HETEROARILO DE FORMULA a), b), c), ENTRE OTROS; R1 ES CIANO, HALOGENO, ALQUILO C1-C4, ENTRE OTROS; R2 ES H, HIDROXI, NITRO, ALQUILO C1-C4, ENTRE OTROS; R5, R6, R7, R8, R9, R10, R11 Y R12 SON H, FLUOR O ALQUILO C1-C3 OPCIONALMENTE SUSTITUIDO CON FLUOR O HIDROXI. SON COMPUESTOS PREFERIDOS: ACIDO (5-{5-[4-(2-BROMO-5-FLUOROFENOXI)PIPERIDIN-1-IL]PIRAZIN-2-IL}-2H-TETRAZOL-2-IL) ACETICO, ACIDO (5-{2-[4-(5-BROMO-2-CLOROFENOXI)PIPERIDIN-1-IL]PIRIMIDIN-5-IL}-2H-TETRAZOL-2-IL)ACETICO, ACIDO (5-{2-[4-(2-CLORO-5-FLUOROFENOXI)PIPERIDIN-1-IL]PIRIMIDIN-5-IL}-2H-TETRAZOL-2-IL)ACETICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE ESTEAROIL-CONZIMA A DELTA-9 DESATURASA (SCD) Y SON UTILES PARA LA PREVENCION Y TRATAMIENTO DE AFECCIONES Y ENFERMEDADES RELACIONADAS CON LA SINTESIS Y METABOLISMO ANORMALES DE LIPIDOS TALES COMO ENFERMEDADES CARDIOVASCULARES, DIABETES, OBESIDAD, ENTRE OTRAS
PE2008000179A 2007-01-26 2008-01-23 Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa PE20081704A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US89767507P 2007-01-26 2007-01-26

Publications (1)

Publication Number Publication Date
PE20081704A1 true PE20081704A1 (es) 2008-12-07

Family

ID=39644071

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000179A PE20081704A1 (es) 2007-01-26 2008-01-23 Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa

Country Status (11)

Country Link
US (2) US7582633B2 (es)
EP (1) EP2108015A4 (es)
JP (1) JP2010516714A (es)
CN (1) CN101641347A (es)
AR (1) AR064965A1 (es)
AU (1) AU2008209295A1 (es)
CA (1) CA2676199A1 (es)
CL (1) CL2008000198A1 (es)
PE (1) PE20081704A1 (es)
TW (1) TW200838533A (es)
WO (1) WO2008089580A1 (es)

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WO2007134457A1 (en) * 2006-05-22 2007-11-29 Merck Frosst Canada Ltd. Cyclic amine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
AU2007260527A1 (en) * 2006-06-12 2007-12-21 Merck Frosst Canada Ltd. Azetidine derivatives as inhibitors of stearoyl-coenzyme A delta-9 desaturase
CA2654098A1 (en) 2006-06-13 2007-12-21 Merck Frosst Canada Ltd. Azacyclopentane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
CA2660114A1 (en) * 2006-08-09 2008-02-14 Merck Frosst Canada Ltd. Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
TW200826936A (en) 2006-12-01 2008-07-01 Merck Frosst Canada Ltd Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
AR064965A1 (es) * 2007-01-26 2009-05-06 Merck Frosst Canada Inc Derivados de azacicloalcanos como inhibidores de estearoil - coenzima a delta -9 desaturasa
JP2010524861A (ja) * 2007-04-20 2010-07-22 メルク フロスト カナダ リミテツド ステアロイル−補酵素aデルタ−9デサチュラーゼの阻害剤としての新規な複素環式芳香族化合物
EP2152719A4 (en) * 2007-05-23 2011-01-19 Merck Frosst Canada Ltd BICYCLIC HETEROAROMATIC COMPOUNDS AS DELTA-9 DEATURASE STEAROYL COENZYME INHIBITORS
US7842696B2 (en) 2007-06-21 2010-11-30 Forest Laboratories Holdings Limited Piperazine derivatives as inhibitors of stearoyl-CoA desaturase
US20100197692A1 (en) * 2007-07-20 2010-08-05 Merck Frosst Canada Ltd. Bicyclic heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
CA2739466A1 (en) * 2008-10-17 2010-04-22 Merck Frosst Canada Ltd. Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
US20100160323A1 (en) * 2008-12-23 2010-06-24 Alexander Bischoff NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE
JP5597210B2 (ja) 2009-02-17 2014-10-01 メルク カナダ インコーポレイテッド ステアロイル−補酵素aデルタ−9デサチュラーゼの阻害剤として有用な新規スピロ化合物
EP2459568A4 (en) 2009-07-28 2013-02-27 Merck Frosst Canada Ltd NOVEL SPIRO COMPOUNDS USEFUL AS DELTA-9 DEATURASE STEAROYL COENZYME INHIBITORS
EP2532656A1 (en) * 2010-02-01 2012-12-12 Nippon Chemiphar Co., Ltd. Gpr119 agonist
FR2958935B1 (fr) 2010-04-19 2012-06-22 Pf Medicament Derives d'heterocycles azotes, leur preparation et leur application en therapeutique humaine
US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
US8530461B2 (en) * 2011-12-29 2013-09-10 Boehringer Ingelheim International Gmbh Azetidine derivatives
US9233102B2 (en) 2012-03-07 2016-01-12 Mayo Foundation For Medical Education And Research Methods and materials for treating cancer
JP6293127B2 (ja) 2012-05-22 2018-03-14 イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティー オブ エルサレム リミテッド 未分化細胞の選択的阻害剤
KR20150090100A (ko) * 2012-12-03 2015-08-05 에프. 호프만-라 로슈 아게 스테아로일-CoA 불포화화효소 1(에스씨디 1)의 억제제로서의 치환된 이속사졸 아마이드 화합물
WO2018081167A1 (en) * 2016-10-24 2018-05-03 Yumanity Therapeutics Compounds and uses thereof
EP3566055A4 (en) 2017-01-06 2020-12-02 Yumanity Therapeutics, Inc. TREATMENT METHODS FOR NEUROLOGICAL DISORDERS
EP3700934A4 (en) 2017-10-24 2021-10-27 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THESE COMPOUNDS

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WO2007134457A1 (en) 2006-05-22 2007-11-29 Merck Frosst Canada Ltd. Cyclic amine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
AU2007260527A1 (en) 2006-06-12 2007-12-21 Merck Frosst Canada Ltd. Azetidine derivatives as inhibitors of stearoyl-coenzyme A delta-9 desaturase
CA2654098A1 (en) 2006-06-13 2007-12-21 Merck Frosst Canada Ltd. Azacyclopentane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
CA2660114A1 (en) 2006-08-09 2008-02-14 Merck Frosst Canada Ltd. Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
JP2010506859A (ja) 2006-10-20 2010-03-04 メルク フロスト カナダ リミテツド ステアロイル−コエンザイムaデルタ−9デサチュラーゼの阻害剤としてのアザシクロアルカン誘導体
TW200826936A (en) 2006-12-01 2008-07-01 Merck Frosst Canada Ltd Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
AR064965A1 (es) * 2007-01-26 2009-05-06 Merck Frosst Canada Inc Derivados de azacicloalcanos como inhibidores de estearoil - coenzima a delta -9 desaturasa

Also Published As

Publication number Publication date
CL2008000198A1 (es) 2008-05-30
JP2010516714A (ja) 2010-05-20
AU2008209295A1 (en) 2008-07-31
EP2108015A1 (en) 2009-10-14
US20080182838A1 (en) 2008-07-31
EP2108015A4 (en) 2011-06-01
TW200838533A (en) 2008-10-01
US7582633B2 (en) 2009-09-01
WO2008089580A1 (en) 2008-07-31
CN101641347A (zh) 2010-02-03
US20090270434A1 (en) 2009-10-29
AR064965A1 (es) 2009-05-06
CA2676199A1 (en) 2008-07-31

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