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PE20081199A1 - 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
PE20081199A1
PE20081199A1 PE2007001699A PE2007001699A PE20081199A1 PE 20081199 A1 PE20081199 A1 PE 20081199A1 PE 2007001699 A PE2007001699 A PE 2007001699A PE 2007001699 A PE2007001699 A PE 2007001699A PE 20081199 A1 PE20081199 A1 PE 20081199A1
Authority
PE
Peru
Prior art keywords
alkyl
azacicloalkanes
desaturase
coenzyme
delta
Prior art date
Application number
PE2007001699A
Other languages
English (en)
Inventor
Nicolas Lachance
Chun Sing Li
Jean-Philippe Leclerc
Yeeman K Ramtohul
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 PE20081199A1 publication Critical patent/PE20081199A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE AZACICLOALCANOS DE FORMULA (I) DONDE q ES 0 O 1; r ES 0 O 1; X-Y ES N-C(O), N-CRaRb, CR14-O, ENTRE OTROS, EN DONDE Ra Y Rb SON CADA UNO H O ALQUILO(C1-C3) OPCIONALMENTE SUSTITUIDO CON F O HIDROXI; R14 ES H O ALQUILO(C1-C3); W ES UN HETEROARILO SELECCIONADO DE (a), (b), ENTRE OTROS, EN DONDE R1 ES HETEROARILO DE FORMULA (i), (ii), ENTRE OTROS, DONDE Rc ES -(CH2)mCO2H, -(CH2)mCO2ALQUILO(C1-C3), ENTRE OTROS; m ES DE 0 A 4; R5, R6, R7, R8, R9, R10, R11 Y R12 SON CADA UNO H, F O ALQUILO(C1-C3) OPCIONALMENTE SUSTITUIDO CON F O HIDROXI; Ar ES FENILO, NAFTILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON R3, DONDE R3 ES ALQUILO(C1-C6), HALOGENO, NITRO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO[5-(5-{4-[2-(TRIFLUOROMETIL)FENOXI]PIPERIDIN-1-IL}-1,3,4-TIADIAZOL-2-IL)-2H-TETRAZOL-2-IL]ACETICO, ACIDO[5-(5-{4-[2-(TRIFLUOROMETIL)FENOXI]PIPERIDIN-1-IL}-1,3,4-TIADIAZOL-2-IL)-1H-TETRAZOL-1-IL]ACETICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE ESTEAROIL-COENZIMA A DELTA-9-DESATURASA (SCD) SIENDO UTILES EN EL TRATAMIENTO DE ATEROSCLEROSIS, OBESIDAD, DIABETES DE TIPO 2, SINDROME METABOLICO, RESISTENCIA A INSULINA, CANCER, ESTEATOSIS HEPATICA
PE2007001699A 2006-12-01 2007-11-30 Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa PE20081199A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US87221606P 2006-12-01 2006-12-01
US89890007P 2007-02-01 2007-02-01

Publications (1)

Publication Number Publication Date
PE20081199A1 true PE20081199A1 (es) 2008-10-19

Family

ID=39467388

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007001699A PE20081199A1 (es) 2006-12-01 2007-11-30 Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa

Country Status (24)

Country Link
US (1) US8063224B2 (es)
EP (1) EP2099793B1 (es)
JP (1) JP5050061B2 (es)
KR (1) KR20090086623A (es)
AR (1) AR064026A1 (es)
AT (1) ATE543816T1 (es)
AU (1) AU2007327276B2 (es)
BR (1) BRPI0719702A2 (es)
CA (1) CA2670703C (es)
CL (1) CL2007003440A1 (es)
CO (1) CO6190521A2 (es)
CR (1) CR10858A (es)
EA (1) EA200970524A1 (es)
EC (1) ECSP099375A (es)
GT (1) GT200900144A (es)
IL (1) IL198824A0 (es)
MA (1) MA31017B1 (es)
MX (1) MX2009005713A (es)
NO (1) NO20092469L (es)
PE (1) PE20081199A1 (es)
SV (1) SV2009003275A (es)
TN (1) TN2009000212A1 (es)
TW (1) TW200826936A (es)
WO (1) WO2008064474A1 (es)

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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
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EP3177292B1 (en) 2014-08-07 2020-11-25 Mayo Foundation for Medical Education and Research Compounds and methods for treating cancer
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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
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
TW200826936A (en) 2008-07-01
TN2009000212A1 (en) 2010-10-18
MA31017B1 (fr) 2009-12-01
IL198824A0 (en) 2010-02-17
JP2010510993A (ja) 2010-04-08
GT200900144A (es) 2011-06-23
CL2007003440A1 (es) 2008-04-04
WO2008064474A1 (en) 2008-06-05
ECSP099375A (es) 2009-07-31
KR20090086623A (ko) 2009-08-13
EA200970524A1 (ru) 2009-12-30
JP5050061B2 (ja) 2012-10-17
SV2009003275A (es) 2009-11-18
CA2670703A1 (en) 2008-06-05
EP2099793A4 (en) 2010-12-29
CA2670703C (en) 2012-05-15
CO6190521A2 (es) 2010-08-19
ATE543816T1 (de) 2012-02-15
EP2099793B1 (en) 2012-02-01
AU2007327276B2 (en) 2011-06-09
EP2099793A1 (en) 2009-09-16
MX2009005713A (es) 2009-06-08
AR064026A1 (es) 2009-03-04
US8063224B2 (en) 2011-11-22
NO20092469L (no) 2009-08-27
AU2007327276A1 (en) 2008-06-05
US20080132542A1 (en) 2008-06-05
CR10858A (es) 2009-06-25
BRPI0719702A2 (pt) 2013-12-17

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