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AR070429A1 - Derivados de 1,3 tiazol como inhibidores de estearoil - coa -desaturasa - Google Patents

Derivados de 1,3 tiazol como inhibidores de estearoil - coa -desaturasa

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Publication number
AR070429A1
AR070429A1 ARP090100560A ARP090100560A AR070429A1 AR 070429 A1 AR070429 A1 AR 070429A1 AR P090100560 A ARP090100560 A AR P090100560A AR P090100560 A ARP090100560 A AR P090100560A AR 070429 A1 AR070429 A1 AR 070429A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
cycloalkyl
heterocyclyl
hetero
Prior art date
Application number
ARP090100560A
Other languages
English (en)
Original Assignee
Xenon Pharmaceuticals Inc
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40740143&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR070429(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Xenon Pharmaceuticals Inc, Novartis Ag filed Critical Xenon Pharmaceuticals Inc
Publication of AR070429A1 publication Critical patent/AR070429A1/es

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    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente proporciona derivados heterocíclicos que modulan la actividad de la estearoil-CoA-desaturasa. También se abarcan métodos para utilizar estos derivados con el fin de modular la actividad de la estearoil-CoA-desaturasa, y composiciones farmacéuticas que comprenden tales derivados. Reivindicacion 1: Un compuesto representado por la formula (1): en donde: Q es cualquiera de la formula (2); W es -N(R6)C(O)-, -R8-C(O)N(R6)-, -R8-OC(O)N(R6)-, -N(R6)C(O)O-, -N(R6)C(O)N(R6), -O-, -S-, -N(R6)-, -S(O)t-, -N(R6)S(O)t-, -S(O)tN(R6)-, -OS(O)tN(R6)-, -R8-C(O)-, -OC(O)-, -C(O)O-, -N(R6)C(=N(R6a))N(R6)-, -N(R6)-((R6a)N=)C-, -C(=N(R6a))N(R6)-, o un enlace directo; V es -C(O)N(R6)-, -S(O)t-, -S(O)2N(R6)-, -C(O)-, -R8-C(O)O-, -R8-C(O)N(R6)-, -R8-C(O)-, -C(=N(R6a))N(R6)-, o un enlace directo; t es 1 o 2; R1 es halogeno, hidrogeno, alquilo, alquenilo, alquinilo, alcoxilo, hidroxi-alquilo, alcoxi-alquilo, cicloalquilo, cicloalquil-alquilo, arilo, aralquilo, heterociclilo, heterociclil-alquilo, hetero-arilo, o hetero-aril-alquilo; o R1 es una estructura de multiples anillos que tiene de 2 a 4 anillos, en donde los anillos son independientemente cicloalquilo, heterociclilo, arilo o hetero-arilo, y en donde algunos o todos los anillos pueden estar fusionados unos con otros: R2 es hidrogeno, alquilo, alquenilo, alquinilo, alcoxilo, hidroxi-alquilo, alcoxi-alquilo, cicloalquilo, cicloalquil-alquilo, arilo, halo-alquilo, aralquilo, heterociclilo, heterociclil-alquilo, hetero-arilo o hetero-aril-alquilo; o R2 es una estructura de multiples anillos que tiene de 2 a 4 anillos, en donde los anillos son independientemente cicloalquilo, heterociclilo, arilo o hetero-arilo, y en donde algunos o todos los anillos pueden estar fusionados unos con otros; R3 es hidrogeno o alquilo; R4 y R4a son independientemente hidrogeno, alquilo, halo-alquilo, hidroxilo, hidroxi-alquilo, alcoxilo, cicloalquil-alquilo o aralquilo; o R4 y R4a se toman juntos para formar un grupo oxo (=O), cicloalquilo o heterociclilo; R5 y R5a son independientemente hidrogeno, alquilo o halo-alquilo; o R4 y R4a se toman juntos para formar un cicloalquilo, arilo, hetero-arilo o heterociclilo, y los restantes R4a y R5a son como se describen anteriormente; R6 es independientemente hidrogeno, alquilo, hidroxi-alquilo, cicloalquil-alquilo, arilo, hetero-arilo, heterociclilo o aralquilo; R6a es independientemente hidrogeno, alquilo, cicloalquil-alquilo, o ciano; R7 es hidrogeno, alquilo, trifluoro-metilo, arilo, cicloalquilo, hetero-arilo, heterociclilo, hidroxi-alquilo, cicloalquil-alquilo o aralquilo; y R8 es independientemente un enlace directo, una cadena de alquileno recta o ramificada opcionalmente sustituida, una cadena de alquenileno recta o ramificada opcionalmente sustituida, o una cadena de alquinileno recta o ramificada opcionalmente sustituida; como un estereoisomero, enantiomero, o tautomero de los mismos, una sal farmacéuticamente aceptable de los mismos, o un pro-fármaco del mismo.
ARP090100560A 2008-02-20 2009-02-18 Derivados de 1,3 tiazol como inhibidores de estearoil - coa -desaturasa AR070429A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US3013708P 2008-02-20 2008-02-20

Publications (1)

Publication Number Publication Date
AR070429A1 true AR070429A1 (es) 2010-04-07

Family

ID=40740143

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090100560A AR070429A1 (es) 2008-02-20 2009-02-18 Derivados de 1,3 tiazol como inhibidores de estearoil - coa -desaturasa

Country Status (29)

Country Link
US (2) US8049016B2 (es)
EP (1) EP2245029B1 (es)
JP (2) JP5507474B2 (es)
KR (1) KR101584826B1 (es)
CN (1) CN102007123B (es)
AR (1) AR070429A1 (es)
AU (1) AU2009216769A1 (es)
BR (1) BRPI0907826A2 (es)
CA (1) CA2715947C (es)
CL (1) CL2009000381A1 (es)
CO (1) CO6290655A2 (es)
CR (1) CR11629A (es)
CU (1) CU23890B1 (es)
EA (1) EA022797B1 (es)
EC (1) ECSP10010411A (es)
HK (1) HK1144808A1 (es)
HN (1) HN2010001647A (es)
IL (1) IL207578A (es)
JO (1) JO3014B1 (es)
MA (1) MA32150B1 (es)
MX (1) MX2010009158A (es)
MY (1) MY156317A (es)
NZ (1) NZ587350A (es)
PE (1) PE20091473A1 (es)
SV (1) SV2010003650A (es)
TW (1) TWI457338B (es)
UA (1) UA105000C2 (es)
WO (1) WO2009103739A1 (es)
ZA (1) ZA201005725B (es)

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EA200900820A1 (ru) * 2006-12-20 2010-02-26 Новартис Аг 2-замещенные 5-членные гетероциклы в качестве ингибиторов стеароил-соа-десатуразы (ссд)
EA022797B1 (ru) 2008-02-20 2016-03-31 Новартис Аг ТРИАЗОЛЬНЫЕ ПРОИЗВОДНЫЕ КАК ИНГИБИТОРЫ СТЕАРОИЛ-CoA-ДЕСАТУРАЗЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИХ, И ИХ ПРИМЕНЕНИЕ
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CA3094527A1 (en) 2018-03-23 2019-09-26 Yumanity Therapeutics, Inc. Compounds and uses thereof
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Publication number Publication date
EP2245029A1 (en) 2010-11-03
UA105000C2 (uk) 2014-04-10
HK1144808A1 (en) 2011-03-11
KR101584826B1 (ko) 2016-01-18
BRPI0907826A2 (pt) 2019-12-10
MA32150B1 (fr) 2011-03-01
TW200942534A (en) 2009-10-16
KR20100117677A (ko) 2010-11-03
MX2010009158A (es) 2010-09-24
JP5507474B2 (ja) 2014-05-28
JP2011512384A (ja) 2011-04-21
CO6290655A2 (es) 2011-06-20
ECSP10010411A (es) 2010-09-30
US20120014906A1 (en) 2012-01-19
IL207578A0 (en) 2010-12-30
TWI457338B (zh) 2014-10-21
SV2010003650A (es) 2011-07-05
EA022797B1 (ru) 2016-03-31
US8318949B2 (en) 2012-11-27
EP2245029B1 (en) 2015-04-15
NZ587350A (en) 2012-07-27
IL207578A (en) 2014-11-30
CN102007123A (zh) 2011-04-06
CA2715947A1 (en) 2009-08-27
ZA201005725B (en) 2011-04-28
CN102007123B (zh) 2014-04-30
CR11629A (es) 2010-11-16
US20090264444A1 (en) 2009-10-22
CU20100170A7 (es) 2011-10-31
WO2009103739A1 (en) 2009-08-27
JO3014B1 (ar) 2016-09-05
HN2010001647A (es) 2013-11-11
MY156317A (en) 2016-02-15
CL2009000381A1 (es) 2010-09-10
JP5813162B2 (ja) 2015-11-17
EA201001315A1 (ru) 2011-06-30
AU2009216769A1 (en) 2009-08-27
JP2014132025A (ja) 2014-07-17
PE20091473A1 (es) 2009-10-23
CA2715947C (en) 2016-10-25
CU23890B1 (es) 2013-04-19
US8049016B2 (en) 2011-11-01

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