EA201290532A1 - Бициклические тиазолы в качестве аллостерических модуляторов рецепторов mglur5 - Google Patents

Бициклические тиазолы в качестве аллостерических модуляторов рецепторов mglur5

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Publication number
EA201290532A1
EA201290532A1 EA201290532A EA201290532A EA201290532A1 EA 201290532 A1 EA201290532 A1 EA 201290532A1 EA 201290532 A EA201290532 A EA 201290532A EA 201290532 A EA201290532 A EA 201290532A EA 201290532 A1 EA201290532 A1 EA 201290532A1
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EA
Eurasian Patent Office
Prior art keywords
mglur5
modulators
compounds
allysteric
mglur5 receptors
Prior art date
Application number
EA201290532A
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English (en)
Other versions
EA019980B1 (ru
Inventor
Грегор Джеймс Макдональд
Андрес Авелино Трабанко-Суарес
Сусана Конде-Сейде
Гэри Джон Тресадерн
Хосе Мануэль Бартоломе-Небреда
Хоакин Пастор-Фернандес
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Янссен Фармацевтика Нв
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Application filed by Янссен Фармацевтика Нв filed Critical Янссен Фармацевтика Нв
Publication of EA201290532A1 publication Critical patent/EA201290532A1/ru
Publication of EA019980B1 publication Critical patent/EA019980B1/ru

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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
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    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/00—Drugs for disorders of the nervous system
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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)
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  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (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

Настоящее изобретение относится к новым бициклическим тиазолам формулы (I), которые являются позитивными аллостерическими модуляторами метаботропного глутаматного рецептора подтипа 5 ("mGluR5") и пригодны в лечении или предотвращении расстройств, ассоциированных с дисфункцией глутамата, и заболеваний, в патогенезе которых подтип mGluR5 рецепторов принимает участие. Изобретение также направлено на фармацевтические композиции, содержащие такие соединения, на способы получения таких соединений и композиций и на использование таких соединений и композиций с целью лечения расстройств, в патогенезе которых участвует mGluR5.
EA201290532A 2009-12-18 2010-12-16 БИЦИКЛИЧЕСКИЕ ТИАЗОЛЫ В КАЧЕСТВЕ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR5 EA019980B1 (ru)

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 (2)

Publication Number Publication Date
EA201290532A1 true EA201290532A1 (ru) 2012-11-30
EA019980B1 EA019980B1 (ru) 2014-07-30

Family

ID=43743677

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201290532A EA019980B1 (ru) 2009-12-18 2010-12-16 БИЦИКЛИЧЕСКИЕ ТИАЗОЛЫ В КАЧЕСТВЕ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR5

Country Status (19)

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

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG181715A1 (en) 2009-12-18 2012-07-30 Janssen Pharmaceutica Nv Bicyclic thiazoles as allosteric modulators of mglur5 receptors
KR20120097400A (ko) 2009-12-18 2012-09-03 얀센 파마슈티카 엔.브이. Ｍｇｌｕｒ５ 리셉터의 알로스테릭 조절자로서의 비사이클릭 티아졸
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)

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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
JP2006513996A (ja) * 2002-10-24 2006-04-27 メルク　エンド　カムパニー　インコーポレーテッド 代謝調節型グルタミン酸受容体結合用トレーサーとしてのアルキン誘導体
TWI301760B (en) 2004-02-27 2008-10-11 Merz Pharma Gmbh & Co Kgaa Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors
US7902356B2 (en) 2004-12-17 2011-03-08 Eli Lilly And Company Thiazolopyridinone derivates as MCH receptor antagonists
DE602006015607D1 (de) 2005-01-14 2010-09-02 Hoffmann La Roche Thiazol-4-carboxamid-derivate als mglur5-antagonisten
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
JP2009514964A (ja) 2005-11-07 2009-04-09 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｐｐａｒモジュレーターとしての化合物および組成物
CN101291939B (zh) * 2005-11-08 2013-02-13 弗·哈夫曼-拉罗切有限公司 作为mGluR5受体拮抗剂的噻唑并[4,5-C]吡啶衍生物
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
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WO2008151184A1 (en) 2007-06-03 2008-12-11 Vanderbilt University Benzamide mglur5 positive allosteric modulators and methods of making and using same
CA2709784A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
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KR20120097400A (ko) 2009-12-18 2012-09-03 얀센 파마슈티카 엔.브이. Ｍｇｌｕｒ５ 리셉터의 알로스테릭 조절자로서의 비사이클릭 티아졸
US20130029904A1 (en) 2009-12-18 2013-01-31 Boehringer Ingelheim International Gmbh Hcv combination therapy

Also Published As

Publication number Publication date
US20120258955A1 (en) 2012-10-11
CO6541615A2 (es) 2012-10-16
MX2012007006A (es) 2012-07-03
JP5763672B2 (ja) 2015-08-12
JP2013514325A (ja) 2013-04-25
US9040707B2 (en) 2015-05-26
EP2513117B1 (en) 2013-08-28
IL220360A (en) 2015-03-31
WO2011073339A1 (en) 2011-06-23
CA2782950A1 (en) 2011-06-23
CN102666552B (zh) 2014-11-26
AR079509A1 (es) 2012-02-01
SG181716A1 (en) 2012-07-30
NZ600605A (en) 2013-08-30
CL2012001601A1 (es) 2012-10-05
BR112012014436A2 (pt) 2019-09-24
AU2010332811A1 (en) 2012-06-21
CN102666552A (zh) 2012-09-12
AU2010332811B2 (en) 2014-07-24
EP2513117A1 (en) 2012-10-24
ES2431302T3 (es) 2013-11-25
EA019980B1 (ru) 2014-07-30
KR20120097400A (ko) 2012-09-03
ZA201204433B (en) 2014-11-26

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