EA025667B1 - ПРОИЗВОДНЫЕ ЭТИНИЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРА mGluR5 - Google Patents

ПРОИЗВОДНЫЕ ЭТИНИЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРА mGluR5 Download PDF

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Publication number
EA025667B1
EA025667B1 EA201590699A EA201590699A EA025667B1 EA 025667 B1 EA025667 B1 EA 025667B1 EA 201590699 A EA201590699 A EA 201590699A EA 201590699 A EA201590699 A EA 201590699A EA 025667 B1 EA025667 B1 EA 025667B1
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Eurasian Patent Office
Prior art keywords
compound
formula
compounds
methanone
disease
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Application number
EA201590699A
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English (en)
Russian (ru)
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EA201590699A1 (ru
Inventor
Георг ЕШКЕ
Лотар ЛИНДЕМАНН
Антонио РИЧЧИ
Даниэль РЮХЕР
Хайнц Штадлер
Эрик ВИЕЙРА
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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Publication of EA201590699A1 publication Critical patent/EA201590699A1/ru
Publication of EA025667B1 publication Critical patent/EA025667B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/22—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Epidemiology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
EA201590699A 2012-10-18 2013-10-15 ПРОИЗВОДНЫЕ ЭТИНИЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРА mGluR5 EA025667B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12188940 2012-10-18
PCT/EP2013/071500 WO2014060398A1 (en) 2012-10-18 2013-10-15 Ethynyl derivatives as modulators of mglur5 receptor activity

Publications (2)

Publication Number Publication Date
EA201590699A1 EA201590699A1 (ru) 2015-07-30
EA025667B1 true EA025667B1 (ru) 2017-01-30

Family

ID=47049067

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201590699A EA025667B1 (ru) 2012-10-18 2013-10-15 ПРОИЗВОДНЫЕ ЭТИНИЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРА mGluR5

Country Status (26)

Country Link
US (1) US9227959B2 (enExample)
EP (1) EP2909180B1 (enExample)
JP (1) JP5989250B2 (enExample)
KR (1) KR101684816B1 (enExample)
CN (1) CN104718192B (enExample)
AR (1) AR093042A1 (enExample)
AU (1) AU2013333988B2 (enExample)
BR (1) BR112015006454A8 (enExample)
CA (1) CA2882520A1 (enExample)
CL (1) CL2015000891A1 (enExample)
CO (1) CO7200248A2 (enExample)
CR (1) CR20150144A (enExample)
EA (1) EA025667B1 (enExample)
ES (1) ES2599553T3 (enExample)
IL (1) IL237380A (enExample)
MA (1) MA38012B1 (enExample)
MX (1) MX2015004898A (enExample)
MY (1) MY168937A (enExample)
NZ (1) NZ705144A (enExample)
PE (1) PE20150629A1 (enExample)
PH (1) PH12015500398A1 (enExample)
SG (1) SG11201501392TA (enExample)
TW (1) TWI490208B (enExample)
UA (1) UA114529C2 (enExample)
WO (1) WO2014060398A1 (enExample)
ZA (1) ZA201500856B (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA114008C2 (xx) * 2012-10-18 2017-04-10 Похідні етинілу як модулятори активності рецептора mglur5
AU2016273751B2 (en) * 2015-06-03 2020-04-02 F. Hoffmann-La Roche Ag Ethynyl derivatives
EP3353161B1 (en) * 2015-09-25 2021-07-21 The United States of America, as represented by the Secretary, Department of Health and Human Services Triazole derivatives as p2y14 receptor antagonists
RS62517B1 (sr) 2017-12-08 2021-11-30 Boehringer Ingelheim Int Derivati imidazopiridina i njihova upotreba kao leka
EA202191014A1 (ru) * 2018-10-17 2021-11-09 Бёрингер Ингельхайм Интернациональ Гмбх Производные 4-пиразин-2-илметил-морфолина и их применение в качестве лекарственного средства
TW202035396A (zh) 2018-10-17 2020-10-01 德商百靈佳殷格翰國際股份有限公司 4-吡啶基甲基-嗎啉衍生物及其作為藥物之用途
CN112888684B (zh) * 2018-10-17 2023-10-10 勃林格殷格翰国际有限公司 4-嘧啶-5-基甲基-吗啉衍生物及其作为药物的用途
US12398143B2 (en) 2019-06-04 2025-08-26 Boehringer Ingelheim International Gmbh Imidazopyrazine derivatives and the use thereof as medicament
WO2020245136A1 (en) 2019-06-04 2020-12-10 Boehringer Ingelheim International Gmbh Purine derivatives, as nr2b negative modulators and the use thereof as medicament, in particular for treating depressive disorders

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090042855A1 (en) * 2007-06-03 2009-02-12 Conn P Jeffrey BENZAMIDE mGluR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME
WO2011051201A1 (en) * 2009-10-27 2011-05-05 F. Hoffmann-La Roche Ag Positive allosteric modulators (pam)
WO2013049255A1 (en) * 2011-09-26 2013-04-04 Vanderbilt University Substitued 5-(prop-1-yn-1-yl)picolinamide analogs as allosteric modulators of mglur5 receptors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW544448B (en) * 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
UA80888C2 (en) * 2003-06-05 2007-11-12 Hoffmann La Roche Imidazole derivatives as glutmate receptor antagonists
KR20100033981A (ko) * 2007-06-03 2010-03-31 벤더르빌트 유니버시티 벤즈아미드 대사성 글루타민산염 수용체5 양성 알로스테릭 조절자 및 이의 제조 및 사용방법

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090042855A1 (en) * 2007-06-03 2009-02-12 Conn P Jeffrey BENZAMIDE mGluR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME
WO2011051201A1 (en) * 2009-10-27 2011-05-05 F. Hoffmann-La Roche Ag Positive allosteric modulators (pam)
WO2013049255A1 (en) * 2011-09-26 2013-04-04 Vanderbilt University Substitued 5-(prop-1-yn-1-yl)picolinamide analogs as allosteric modulators of mglur5 receptors

Also Published As

Publication number Publication date
MA38012B1 (fr) 2016-12-30
BR112015006454A8 (pt) 2019-08-20
HK1207639A1 (zh) 2016-02-05
EP2909180B1 (en) 2016-10-05
MX2015004898A (es) 2015-07-21
CR20150144A (es) 2015-04-30
KR20150055044A (ko) 2015-05-20
WO2014060398A1 (en) 2014-04-24
AU2013333988A1 (en) 2015-02-26
BR112015006454A2 (pt) 2017-07-04
AR093042A1 (es) 2015-05-13
PE20150629A1 (es) 2015-05-11
US20150225385A1 (en) 2015-08-13
ES2599553T3 (es) 2017-02-02
US9227959B2 (en) 2016-01-05
SG11201501392TA (en) 2015-05-28
IL237380A0 (en) 2015-04-30
JP2015531392A (ja) 2015-11-02
KR101684816B1 (ko) 2016-12-20
CO7200248A2 (es) 2015-02-27
EP2909180A1 (en) 2015-08-26
JP5989250B2 (ja) 2016-09-07
TW201420571A (zh) 2014-06-01
NZ705144A (en) 2018-09-28
TWI490208B (zh) 2015-07-01
AU2013333988B2 (en) 2017-03-09
PH12015500398B1 (en) 2015-04-27
CL2015000891A1 (es) 2015-09-11
UA114529C2 (uk) 2017-06-26
PH12015500398A1 (en) 2015-04-27
MA38012A1 (fr) 2016-05-31
EA201590699A1 (ru) 2015-07-30
MY168937A (en) 2019-01-10
CA2882520A1 (en) 2014-04-24
IL237380A (en) 2017-02-28
CN104718192A (zh) 2015-06-17
CN104718192B (zh) 2016-08-31
ZA201500856B (en) 2016-08-31

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU