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

Links

Classifications

    • 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

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
MX2012007006A (es) 2009-12-18 2012-07-03 Janssen Pharmaceutica Nv Tiazoles biciclicos como moduladores alostericos de receptores mglur5.
BR112012014235A2 (pt) 2009-12-18 2016-06-14 Janssen Pharmaceutica Nv tiazóis bicíclicos como moduladores alostéricos de receptores mglur5
ES2815352T3 (es) * 2014-02-18 2021-03-29 Daiichi Sankyo Co Ltd Procedimiento de producción de un inhibidor de factor X de la coagulación sanguínea activado (FXa)

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5753664A (en) 1995-03-16 1998-05-19 Takeda Chemical Industries, Ltd. Heterocyclic compounds, their production and use
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
ES2333243T3 (es) 2004-12-17 2010-02-18 Eli Lilly And Company Derivados de tiazolopiridinona como antagonistas del receptor de mch.
CA2593439C (en) 2005-01-14 2014-02-25 F. Hoffmann-La Roche Ag Thiazole-4-carboxamide derivatives as mglur5 antagonists
JP2009500442A (ja) * 2005-07-09 2009-01-08 アストラゼネカ アクチボラグ ２型糖尿病を処置するためのグルコキナーゼのモジュレーターとしての２−ヘテロシクリルオキシベンゾイルアミノヘテロシクリル化合物
WO2007023242A1 (en) * 2005-08-24 2007-03-01 Merz Pharma Gmbh & Co. Kgaa Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors
RU2008122548A (ru) 2005-11-07 2009-12-20 Айрм Ллк (Bm) Соединения и композиции, как модуляторы арпп (активированных рецепторов пролифератора пероксисом)
BRPI0618636A2 (pt) * 2005-11-08 2011-09-06 Hoffmann La Roche derivados de tiazolo [4,5-c]piridina
DE102006011574A1 (de) 2006-03-10 2007-10-31 Grünenthal GmbH Substituierte Imidazo[2,1-b]thiazol-Verbindungen und ihre Verwendung zur Herstellung von Arzneimitteln
EP2035436B1 (en) 2006-06-26 2011-05-25 UCB Pharma S.A. Fused thiazole derivatives as kinase inhibitors
EP2049548A1 (en) * 2006-07-27 2009-04-22 UCB Pharma, S.A. Fused oxazoles & thiazoles as histamine h3- receptor ligands
GB0622202D0 (en) 2006-11-07 2006-12-20 Addex Pharmaceuticals Sa Novel compounds
EP2094712B1 (en) 2006-11-15 2011-10-12 Vertex Pharmceuticals Incorporated Compounds useful as protein kinase inhibitors
JP4714669B2 (ja) 2006-12-01 2011-06-29 日本化薬株式会社 ヘッダーアッシー、スクイブならびにエアバッグ用ガス発生装置およびシートベルトプリテンショナー用ガス発生装置
EP2089397B1 (en) 2006-12-14 2012-08-29 Eli Lilly & Company 5- [4- (azetidin-3-yl0xy) -phenyl]-2-phenyl-5h-thiaz0l0 [5,4-c]pyridin-4-0ne derivatives and their use as mch receptor antagonists
EP2162136A4 (en) 2007-06-03 2012-02-15 Univ Vanderbilt POSITIVE ALLOSTERIC MGLUR5 BENZAMIDE MODULATORS AND METHOD FOR THEIR PREPARATION AND USE
CA2709784A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
JP5651681B2 (ja) 2009-04-03 2015-01-14 大日本住友製薬株式会社 代謝型グルタミン酸受容体５介在障害の治療のための化合物、およびその使用方法
MX2012007006A (es) 2009-12-18 2012-07-03 Janssen Pharmaceutica Nv Tiazoles biciclicos como moduladores alostericos de receptores mglur5.
CN102753173A (zh) 2009-12-18 2012-10-24 贝林格尔.英格海姆国际有限公司 Hcv组合疗法

Also Published As

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

Similar Documents

Publication Publication Date Title
BR112015031903A2 (pt) composto, sal farmaceuticamente aceitável do composto, composição farmacêutica e utilização de um composto
BR112015022566A2 (pt) composto e composição farmacêutica
MX2011005242A (es) Derivados de indol y benzoxazina como moduladores de los receptores de glutamato metabotropicos.
BR112015016315A2 (pt) fluoro-[1,3]oxazinas como inibidores de bace1
BR112012020273A2 (pt) Compostos de pirazolopiridina, pirazolopirazina, pirazolopirimidina, pirazolotiofeno e pirazolotiazol como pontencializadores alostéricos de mglur4, composições e métodos de tratamento de disfunção neurológica
BRPI1009381B8 (pt) compostos, composição farmacêutica e uso de compostos e de composição farmacêutica
CL2012001072A1 (es) Compuestos derivados de feniletinilo, moduladores alostericos positivos del receptor de glutamato (mglur5); procedimiento de preparacion; composicion farmaceutica; y uso para tratar esquizofrenia o enfermedades cognitivas.
EA201071169A1 (ru) ГИДРОКСИМЕТИЛПИРРОЛИДИНЫ В КАЧЕСТВЕ АГОНИСТОВ АДРЕНЕРГИЧЕСКИХ РЕЦЕПТОРОВ β3
BR112012013431A8 (pt) composto, composição farmacêutica e seu uso
BR112012018386A2 (pt) "inibidores isoindolinona de fosfatidilinositol 3-quinase"
BR112012020271A2 (pt) Benzisoxazóis e azabenzisoxazóis como potencializadores alostéricos de mglur4 composições e métodos de tratamentos de disfunção neurológica
MA32369B1 (fr) Composes de benzene sulfonamide thiazole et oxazole
BRPI0817242A8 (pt) compostos derivados de 1,1,1-trifluoro-2-hidroxi-3-fenilpropano, processo para a sua manufatura e composições farmacêuticas que os contêm
BRPI0919876A8 (pt) Composto, composição farmacêutica, uso de um composto, e, método para intensificar a qualidade do sono, para tratar insônia, e para tratar ou controlar obesidade em um paciente mamífero que necessita do mesmo.
UA111579C2 (uk) ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ
ATE478072T1 (de) Spiroimidazol-derivate als ppar-modulatoren
BR112013031098A2 (pt) halogeno-alquil-1,3 oxazinas como inibidores de bace1 e/ou bace2
EA201390947A1 (ru) Соединения 2-амино-4-арилтиазола в качестве антагонистов trpa1
BRPI0718714B8 (pt) arilamidas substituídas por tiazol e oxazol, seu uso e composição farmacêutica que as compreende
BR112014012056A8 (pt) compostos farmacêuticos
UY30572A1 (es) N-(1-ftalazin-1-il-piperidin-4-il)-amidas como moduladores del receptor ep2
BR112014006763A2 (pt) n-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexa-hidro-ciclopenta[e][1,3]oxazin-4-il)-fenil)-amidas como inibidores de bace1
BRPI0821266B8 (pt) Derivados de arilamida triazol-substituída e seu uso e composição farmacêutica
BR112021006319A2 (pt) compostos de indolinona para uso como inibidores de map4k1
ATE542795T1 (de) Benzylpiperazinderivate als motilin- rezeptorantagonisten

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.