UA107002C2 - Етинільні похідні - Google Patents

Етинільні похідні

Info

Publication number
UA107002C2
UA107002C2 UAA201207427A UAA201207427A UA107002C2 UA 107002 C2 UA107002 C2 UA 107002C2 UA A201207427 A UAA201207427 A UA A201207427A UA A201207427 A UAA201207427 A UA A201207427A UA 107002 C2 UA107002 C2 UA 107002C2
Authority
UA
Ukraine
Prior art keywords
lower alkyl
hydrogen
alkoxy
hydroxy
optionally substituted
Prior art date
Application number
UAA201207427A
Other languages
English (en)
Russian (ru)
Inventor
Люк Грін
Вольфганг ГУБА
Гєорг Єшкє
Сініз Жолідон
Лотар Ліндеманн
Хайнц Штадлєр
Ерік Віейра
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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=43446449&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=UA107002(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of UA107002C2 publication Critical patent/UA107002C2/uk

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P25/24—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Даний винахід стосується етинільних похідних формули (І), у якій X позначає N або C-R1; Υ позначає N або C-R2; Ζ позначає СН або N; R4 позначає 6-членний ароматичний замісник, який містить 0, 1 або 2 атоми азоту, необов'язково заміщений 1-3 групами, вибраними з галогену, нижчого алкілу, нижчого алкокси або NRR'; R1 позначає водень, нижчий алкіл, нижчий алкокси, гідрокси, нижчий гідроксіалкіл, нижчий циклоалкіл, або є гетероциклоалкілом, необов'язково заміщеним гідрокси чи алкокси; R2 позначає водень, CN, нижчий алкіл або гетероциклоалкіл; R та R' незалежно один від одного позначають водень або нижчий алкіл; або фармацевтично прийнятної солі чи солі приєднання кислоти, рацемічної суміші або їх відповідних енантіомерів та/або оптичних ізомерів та/або їх стереоізомерів. Несподівано було знайдено, що сполуки загальної формули (І) є позитивними алостеричними модуляторами (РАМ) метаботропного глутаматного рецептора субтипу 5 (mGluR5) і тому вони є придатними для лікування хвороб, пов'язаних з цим рецептором. EMBED ISISServer І
UAA201207427A 2009-12-17 2010-12-14 Етинільні похідні UA107002C2 (uk)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09179719 2009-12-17
PCT/EP2010/069593 WO2011073172A1 (en) 2009-12-17 2010-12-14 Ethynyl derivatives

Publications (1)

Publication Number Publication Date
UA107002C2 true UA107002C2 (uk) 2014-11-10

Family

ID=43446449

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201207427A UA107002C2 (uk) 2009-12-17 2010-12-14 Етинільні похідні

Country Status (27)

Country Link
US (2) US8586581B2 (uk)
EP (1) EP2513102B1 (uk)
JP (1) JP5763094B2 (uk)
KR (1) KR101407856B1 (uk)
CN (1) CN102686589B (uk)
AR (1) AR079467A1 (uk)
AU (1) AU2010332987B2 (uk)
BR (1) BR112012014770A2 (uk)
CA (1) CA2780155A1 (uk)
CL (1) CL2012001596A1 (uk)
CO (1) CO6531478A2 (uk)
CR (1) CR20120269A (uk)
EC (1) ECSP12011977A (uk)
ES (1) ES2551582T3 (uk)
HK (1) HK1171225A1 (uk)
IL (1) IL219371A (uk)
MA (1) MA33802B1 (uk)
MX (1) MX2012006789A (uk)
MY (1) MY162998A (uk)
NZ (1) NZ599553A (uk)
PE (1) PE20121443A1 (uk)
RU (1) RU2553461C2 (uk)
SG (1) SG181779A1 (uk)
TW (1) TWI448465B (uk)
UA (1) UA107002C2 (uk)
WO (1) WO2011073172A1 (uk)
ZA (1) ZA201204429B (uk)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112013010850A8 (pt) * 2010-11-05 2018-06-12 Otsuka Agritechno Co Ltd Composto de etinilfenilamidina ou sal do mesmo, método para produzir o mesmo e fungicida para uso agrícola e em horticultura
PT2702051E (pt) 2011-04-26 2015-05-20 Hoffmann La Roche Derivados de etinilo como reguladores alostéricos positivos de rmglu5
US20130123254A1 (en) 2011-09-30 2013-05-16 Barbara Biemans Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification
UA110862C2 (uk) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
ES2594031T3 (es) * 2012-09-27 2016-12-15 F. Hoffmann-La Roche Ag Derivados de ariletinilo
NZ703537A (en) * 2012-10-18 2018-06-29 Hoffmann La Roche Ethynyl derivatives
EP2916842B1 (en) * 2012-11-07 2016-10-19 F. Hoffmann-La Roche AG Triazolo compounds
PT3303316T (pt) 2015-06-03 2020-04-27 Hoffmann La Roche Derivados de etinilo
MX2018000592A (es) 2015-07-15 2018-04-24 Hoffmann La Roche Derivados de etinilo como moduladores del receptor de glutamato metabotropico.
PE20190382A1 (es) * 2016-07-18 2019-03-08 Hoffmann La Roche Derivados etinilo

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2232017C2 (ru) * 1998-10-02 2004-07-10 Новартис Аг Антагонисты метаботропных глутаматных рецепторов (mglur5) для лечения боли и состояния тревоги
CO5271680A1 (es) * 2000-02-21 2003-04-30 Smithkline Beecham Corp Compuestos
GB0027987D0 (en) * 2000-11-16 2001-01-03 Smithkline Beecham Plc Compounds
US6910976B2 (en) 2001-06-26 2005-06-28 Stx, Llc Multi-component lacrosse stick head
GB0127430D0 (en) * 2001-11-15 2002-01-09 Smithkline Beecham Corp Compounds
GB0127433D0 (en) * 2001-11-15 2002-01-09 Smithkline Beecham Corp Compounds
TWI292318B (en) * 2003-03-10 2008-01-11 Hoffmann La Roche Imidazol-4-yl-ethynyl-pyridine derivatives
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
GB0413605D0 (en) 2004-06-17 2004-07-21 Addex Pharmaceuticals Sa Novel compounds
WO2006048771A1 (en) 2004-11-04 2006-05-11 Addex Pharmaceuticals Sa Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
EP1912966A2 (en) * 2005-06-01 2008-04-23 Ucb, S.A. 2-oxo-1-pyrrolidine derivatives and their therapeutic use on the central nervous system
PT2090575E (pt) 2005-11-15 2011-06-06 Array Biopharma Inc Inibidores de erbb
AU2007263655A1 (en) 2006-06-30 2008-01-03 Astrazeneca Ab Pyrimidine derivatives useful in the treatment of cancer
EP1972628A1 (en) 2007-03-21 2008-09-24 Schwarz Pharma Ag Indolizines and aza-analog derivatives thereof as CNS active compounds
ES2392117T3 (es) * 2007-04-30 2012-12-04 Abbott Laboratories Inhibidores de enzima diacilglicerol O-aciltransferasa de tipo 1
WO2008151184A1 (en) 2007-06-03 2008-12-11 Vanderbilt University Benzamide mglur5 positive allosteric modulators and methods of making and using same
TW201116532A (en) * 2009-08-05 2011-05-16 Merz Pharma Gmbh & Co Kgaa Metabotropic glutamate receptor modulators

Also Published As

Publication number Publication date
CN102686589A (zh) 2012-09-19
MY162998A (en) 2017-07-31
CL2012001596A1 (es) 2013-01-04
KR20120095472A (ko) 2012-08-28
KR101407856B1 (ko) 2014-06-16
TW201144314A (en) 2011-12-16
ES2551582T3 (es) 2015-11-20
RU2012128551A (ru) 2014-01-27
CA2780155A1 (en) 2011-06-23
US20140073638A1 (en) 2014-03-13
BR112012014770A2 (pt) 2016-03-29
US20110152257A1 (en) 2011-06-23
CR20120269A (es) 2012-07-04
EP2513102A1 (en) 2012-10-24
AU2010332987A1 (en) 2012-06-07
CO6531478A2 (es) 2012-09-28
RU2553461C2 (ru) 2015-06-20
AU2010332987B2 (en) 2015-08-13
ECSP12011977A (es) 2012-07-31
TWI448465B (zh) 2014-08-11
EP2513102B1 (en) 2015-08-19
IL219371A (en) 2015-02-26
PE20121443A1 (es) 2012-10-26
US8586581B2 (en) 2013-11-19
ZA201204429B (en) 2013-02-27
CN102686589B (zh) 2014-12-10
JP5763094B2 (ja) 2015-08-12
SG181779A1 (en) 2012-07-30
MX2012006789A (es) 2012-07-10
AR079467A1 (es) 2012-01-25
JP2013514305A (ja) 2013-04-25
IL219371A0 (en) 2012-06-28
WO2011073172A1 (en) 2011-06-23
HK1171225A1 (en) 2013-03-22
NZ599553A (en) 2014-05-30
US8933094B2 (en) 2015-01-13
MA33802B1 (fr) 2012-12-03

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