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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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

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)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007134457A1 (en) * 2006-05-22 2007-11-29 Merck Frosst Canada Ltd. Cyclic amine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
WO2007143823A1 (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
EP2148878A4 (en) * 2007-04-20 2011-08-10 Merck Canada Inc NEW HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME-A-DELTA-9-DESATURASE
WO2008141455A1 (en) * 2007-05-23 2008-11-27 Merck Frosst Canada Ltd. Bicyclic heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
US7842696B2 (en) 2007-06-21 2010-11-30 Forest Laboratories Holdings Limited Piperazine derivatives as inhibitors of stearoyl-CoA desaturase
AU2008280784A1 (en) * 2007-07-20 2009-01-29 Merck Frosst Canada Ltd Bicyclic heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
AU2009304508A1 (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
WO2011011872A1 (en) 2009-07-28 2011-02-03 Merck Frosst Canada Ltd. Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase
KR20120130104A (ko) * 2010-02-01 2012-11-28 닛뽕 케미파 가부시키가이샤 Gpr119 작동약
FR2958935B1 (fr) * 2010-04-19 2012-06-22 Pf Medicament Derives d'heterocycles azotes, leur preparation et leur application en therapeutique humaine
WO2012027495A1 (en) 2010-08-27 2012-03-01 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
US8530461B2 (en) * 2011-12-29 2013-09-10 Boehringer Ingelheim International Gmbh Azetidine derivatives
WO2013134546A1 (en) 2012-03-07 2013-09-12 Mayo Foundation For Medical Education And Research Methods and materials for treating cancer
WO2013175474A2 (en) 2012-05-22 2013-11-28 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Selective inhibitors of undifferentiated cells
US9296711B2 (en) * 2012-12-03 2016-03-29 Hoffman-La Roche Inc. Substituted isoxazole amide compounds as inhibitors of stearoyl-CoA desaturase 1 (SCD1)
EP3177292B1 (en) 2014-08-07 2020-11-25 Mayo Foundation for Medical Education and Research Compounds and methods for treating cancer
WO2018081167A1 (en) 2016-10-24 2018-05-03 Yumanity Therapeutics Compounds and uses thereof
IL304017A (en) 2017-01-06 2023-08-01 Yumanity Therapeutics Inc Methods for treating neurological disorders
EP3700934A4 (en) 2017-10-24 2021-10-27 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THESE COMPOUNDS
SG11202009280RA (en) 2018-03-23 2020-10-29 Yumanity Therapeutics Inc Compounds and uses thereof
SG11202108079RA (en) 2019-01-24 2021-08-30 Yumanity Therapeutics Inc Compounds and uses thereof
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2162235T3 (es) 1996-01-15 2001-12-16 Janssen Pharmaceutica Nv Piridazinaminas inhibidoras de la angiogenesis.
US20050119251A1 (en) 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
US7754711B2 (en) 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
EP1651616B1 (en) 2003-07-30 2012-05-02 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
PT1651620E (pt) * 2003-07-30 2012-02-10 Xenon Pharmaceuticals Inc Derivados de piperizina e sua utilização como agentes terapêuticos
US7345043B2 (en) 2004-04-01 2008-03-18 Miikana Therapeutics Inhibitors of histone deacetylase
AR051026A1 (es) 2004-09-20 2006-12-13 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
CA2580857A1 (en) 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
AU2005286728A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
BRPI0515505A (pt) 2004-09-20 2008-07-29 Xenon Pharmaceuticals Inc derivados heterocìclicos e sua utilização como inibidores da estearoil-coa desaturase
AU2005286648A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
MX2007003321A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
WO2006034341A2 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
EP1804792A1 (en) 2004-09-20 2007-07-11 Xenon Pharmaceuticals Inc. Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-coa-desaturase (scd)
GT200600046A (es) * 2005-02-09 2006-09-25 Terapia de combinacion
WO2006125181A2 (en) 2005-05-19 2006-11-23 Xenon Pharmaceuticals Inc. Piperidine derivatives and their use as stearoyl-coa desaturase modulators
EP1902051A1 (en) 2005-06-09 2008-03-26 Merck Frosst Canada Ltd. Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
AU2006272334A1 (en) * 2005-07-20 2007-01-25 Merck Frosst Canada Ltd Heteroaromatic compounds as inhibitors of stearoyl-coenzyme A delta-9 desaturase
WO2007038865A1 (en) 2005-10-05 2007-04-12 Merck Frosst Canada Ltd. Substituted quinolines as inhibitors of leukotriene biosynthesis
AU2006315025A1 (en) 2005-11-15 2007-05-24 Merck Frosst Canada Ltd. Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
EP1966183A4 (en) 2005-12-20 2010-12-29 Merck Frosst Canada Ltd HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A-DELTA-9-DESATURASE
WO2007134457A1 (en) 2006-05-22 2007-11-29 Merck Frosst Canada Ltd. Cyclic amine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
WO2007143823A1 (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
US20100004245A1 (en) 2006-10-20 2010-01-07 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

Also Published As

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

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