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BR112012014436A2 - tiazóis bicíclicos como moduladores alostéricos de receptores mglur5 - Google Patents

tiazóis bicíclicos como moduladores alostéricos de receptores mglur5

Info

Publication number
BR112012014436A2
BR112012014436A2 BR112012014436A BR112012014436A BR112012014436A2 BR 112012014436 A2 BR112012014436 A2 BR 112012014436A2 BR 112012014436 A BR112012014436 A BR 112012014436A BR 112012014436 A BR112012014436 A BR 112012014436A BR 112012014436 A2 BR112012014436 A2 BR 112012014436A2
Authority
BR
Brazil
Prior art keywords
mglur5
allosteric
receptor modulators
compounds
bicyclic thiazoles
Prior art date
Application number
BR112012014436A
Other languages
English (en)
Inventor
Avelino Trabanco-Suarez Andrés
John Tresadern Gary
James Macdonald Gregor
Pastor-Fernández Joaquin
Manuel Bartolomé-Nebreda José
Conde-Ceide Susana
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR112012014436A2 publication Critical patent/BR112012014436A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • 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
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Reproductive Health (AREA)
  • Nutrition Science (AREA)
  • Pain & Pain Management (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

tiazóis bicíclicos como moduladores alostéricos de receptores mglur5. a presente invenção refere-se a novos tiazóis bicíclicos os quais são moduladores alostéricos positivos do receptor do glutamato metabotrópico subtipo 5 ("mglur5") e os quais são úteis para o tratamento ou a prevenção de distúrbios associados com disfunção de glutamato e doenças nas quais estão envolvidos os receptores do subtipo mglur5. a invenção também se refere a composições farmacêuticas compreendendo os referidos compostos, a processos para preparar os referidos compostos e composições, e à aplicação dos referidos compostos e composições para a prevenção e o tratamento de distúrbios nos quais mglur5 está envolvido.
BR112012014436A 2009-12-18 2010-12-16 tiazóis bicíclicos como moduladores alostéricos de receptores mglur5 BR112012014436A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09179850 2009-12-18
EP10193019 2010-11-29
PCT/EP2010/069957 WO2011073339A1 (en) 2009-12-18 2010-12-16 Bicyclic thiazoles as allosteric modulators of mglur5 receptors

Publications (1)

Publication Number Publication Date
BR112012014436A2 true BR112012014436A2 (pt) 2019-09-24

Family

ID=43743677

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012014436A BR112012014436A2 (pt) 2009-12-18 2010-12-16 tiazóis bicíclicos como moduladores alostéricos de receptores mglur5

Country Status (19)

Country Link
US (1) US9040707B2 (pt)
EP (1) EP2513117B1 (pt)
JP (1) JP5763672B2 (pt)
KR (1) KR20120097400A (pt)
CN (1) CN102666552B (pt)
AR (1) AR079509A1 (pt)
AU (1) AU2010332811B2 (pt)
BR (1) BR112012014436A2 (pt)
CA (1) CA2782950A1 (pt)
CL (1) CL2012001601A1 (pt)
CO (1) CO6541615A2 (pt)
EA (1) EA019980B1 (pt)
ES (1) ES2431302T3 (pt)
IL (1) IL220360A (pt)
MX (1) MX2012007006A (pt)
NZ (1) NZ600605A (pt)
SG (1) SG181716A1 (pt)
WO (1) WO2011073339A1 (pt)
ZA (1) ZA201204433B (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ600603A (en) 2009-12-18 2013-07-26 Janssen Pharmaceutica Nv Bicyclic thiazoles as allosteric modulators of mglur5 receptors
SG181716A1 (en) 2009-12-18 2012-07-30 Janssen Pharmaceutica Nv Bicyclic thiazoles as allosteric modulators of mglur5 receptors
US9920071B2 (en) * 2014-02-18 2018-03-20 Daiichi Sankyo Company, Limited Method for producing inhibitor of activated blood coagulation factor X (FXa)

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JP2002105085A (ja) * 2000-09-28 2002-04-10 Yamanouchi Pharmaceut Co Ltd 新規イミダゾチアゾール誘導体
WO2004038374A2 (en) 2002-10-24 2004-05-06 Merck & Co., Inc. Alkyne derivatives as tracers for metabotropic glutamate receptor binding
TWI301760B (en) 2004-02-27 2008-10-11 Merz Pharma Gmbh & Co Kgaa Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors
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EP1910350A1 (en) * 2005-07-09 2008-04-16 AstraZeneca AB 2 -heterocyclyloxybenzoyl amino heterocyclyl compounds as modulators of glucokinase for the treatment of type 2 diabetes
WO2007023242A1 (en) 2005-08-24 2007-03-01 Merz Pharma Gmbh & Co. Kgaa Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors
KR20080059635A (ko) 2005-11-07 2008-06-30 아이알엠 엘엘씨 Ｐｐａｒ 조절제로서의 화합물 및 조성물
RU2425834C2 (ru) * 2005-11-08 2011-08-10 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ТИАЗОЛО[4,5-c]ПИРИДИНА В КАЧЕСТВЕ АНТАГОНИСТОВ РЕЦЕПТОРОВ mGluR5
DE102006011574A1 (de) 2006-03-10 2007-10-31 Grünenthal GmbH Substituierte Imidazo[2,1-b]thiazol-Verbindungen und ihre Verwendung zur Herstellung von Arzneimitteln
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SG181716A1 (en) 2009-12-18 2012-07-30 Janssen Pharmaceutica Nv Bicyclic thiazoles as allosteric modulators of mglur5 receptors

Also Published As

Publication number Publication date
AU2010332811B2 (en) 2014-07-24
JP5763672B2 (ja) 2015-08-12
EP2513117B1 (en) 2013-08-28
JP2013514325A (ja) 2013-04-25
ZA201204433B (en) 2014-11-26
EP2513117A1 (en) 2012-10-24
MX2012007006A (es) 2012-07-03
CL2012001601A1 (es) 2012-10-05
AU2010332811A1 (en) 2012-06-21
CO6541615A2 (es) 2012-10-16
CN102666552B (zh) 2014-11-26
NZ600605A (en) 2013-08-30
CN102666552A (zh) 2012-09-12
SG181716A1 (en) 2012-07-30
US9040707B2 (en) 2015-05-26
US20120258955A1 (en) 2012-10-11
IL220360A (en) 2015-03-31
KR20120097400A (ko) 2012-09-03
WO2011073339A1 (en) 2011-06-23
ES2431302T3 (es) 2013-11-25
EA201290532A1 (ru) 2012-11-30
CA2782950A1 (en) 2011-06-23
AR079509A1 (es) 2012-02-01
EA019980B1 (ru) 2014-07-30

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Legal Events

Date Code Title Description
B08F Application fees: application dismissed [chapter 8.6 patent gazette]
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2543 DE 01-10-2019 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.