EA201590252A1 - Арилэтинилпиримидины - Google Patents

Арилэтинилпиримидины

Info

Publication number
EA201590252A1
EA201590252A1 EA201590252A EA201590252A EA201590252A1 EA 201590252 A1 EA201590252 A1 EA 201590252A1 EA 201590252 A EA201590252 A EA 201590252A EA 201590252 A EA201590252 A EA 201590252A EA 201590252 A1 EA201590252 A1 EA 201590252A1
Authority
EA
Eurasian Patent Office
Prior art keywords
formula
mglur5
autism
schizophrenia
stereoisomers
Prior art date
Application number
EA201590252A
Other languages
English (en)
Other versions
EA025165B1 (ru
Inventor
Георг Ешке
Лотар Линдеманн
Хайнц Штадлер
Эрик Виейра
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
Application filed by Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of EA201590252A1 publication Critical patent/EA201590252A1/ru
Publication of EA025165B1 publication Critical patent/EA025165B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61P25/18—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
    • A61P25/28—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

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

Abstract

Настоящее изобретение относится к производным этинила формулы Iгде Rпредставляет собой водород или галоген; Rпредставляет собой С-алкил или -(СН)-О-СН; n означает 2 или 3; m означает 1 или 2; или к их фармацевтически приемлемым солям присоединения кислоты, рацемическим смесям или соответствующим энантиомерам, и/или оптическим изомерам, и/или стереоизомерам. Обнаружено, что соединения общей формулы I представляют собой аллостерические модуляторы подтипа 5 метаботропного глутаматного рецептора (mGluR5) с улучшенными свойствами для лечения шизофрении, когнитивных расстройств, синдрома фрагильной Х-хромосомы или аутизма.
EA201590252A 2012-08-13 2013-08-06 Арилэтинилпиримидины EA025165B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12180209 2012-08-13
PCT/EP2013/066443 WO2014026880A1 (en) 2012-08-13 2013-08-06 Arylethynyl pyrimidines

Publications (2)

Publication Number Publication Date
EA201590252A1 true EA201590252A1 (ru) 2015-06-30
EA025165B1 EA025165B1 (ru) 2016-11-30

Family

ID=46851291

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201590252A EA025165B1 (ru) 2012-08-13 2013-08-06 Арилэтинилпиримидины

Country Status (36)

Country Link
US (1) US9199971B2 (ru)
EP (1) EP2882742B1 (ru)
JP (1) JP5974179B2 (ru)
KR (1) KR101747005B1 (ru)
CN (1) CN104540815B (ru)
AR (1) AR092097A1 (ru)
AU (1) AU2013304212B2 (ru)
BR (1) BR112015002921A2 (ru)
CA (1) CA2880257C (ru)
CL (1) CL2015000290A1 (ru)
CO (1) CO7180198A2 (ru)
CR (1) CR20150028A (ru)
CY (1) CY1118595T1 (ru)
DK (1) DK2882742T3 (ru)
EA (1) EA025165B1 (ru)
ES (1) ES2601511T3 (ru)
HK (1) HK1207378A1 (ru)
HR (1) HRP20161692T1 (ru)
HU (1) HUE030237T2 (ru)
IL (1) IL237015A (ru)
LT (1) LT2882742T (ru)
MA (1) MA37895B1 (ru)
MX (1) MX358011B (ru)
MY (1) MY170255A (ru)
NZ (1) NZ704858A (ru)
PE (1) PE20150685A1 (ru)
PH (1) PH12015500261B1 (ru)
PL (1) PL2882742T3 (ru)
PT (1) PT2882742T (ru)
RS (1) RS55397B1 (ru)
SG (1) SG11201501055SA (ru)
SI (1) SI2882742T1 (ru)
TW (1) TWI501958B (ru)
UA (1) UA113223C2 (ru)
WO (1) WO2014026880A1 (ru)
ZA (1) ZA201500582B (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY174339A (en) 2012-08-13 2020-04-09 Novartis Ag 1,4-disubstituted pyridazine analogs and methods for treating smn-deficiency-related conditions
NZ703537A (en) * 2012-10-18 2018-06-29 Hoffmann La Roche Ethynyl derivatives
PT3303316T (pt) * 2015-06-03 2020-04-27 Hoffmann La Roche Derivados de etinilo

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
RS50603B (sr) * 2004-06-01 2010-05-07 F. Hoffmann-La Roche Ag. Piridin-4-il-etinil-imidazoli i pirazoli kao antagonisti mglu5 receptora
WO2006048771A1 (en) 2004-11-04 2006-05-11 Addex Pharmaceuticals Sa Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
TW200811157A (en) * 2006-05-05 2008-03-01 Astrazeneca Ab mGluR5 modulators I
WO2008151184A1 (en) * 2007-06-03 2008-12-11 Vanderbilt University Benzamide mglur5 positive allosteric modulators and methods of making and using same
KR20100089091A (ko) * 2007-10-26 2010-08-11 아스트라제네카 아베 Ｍｇｌｕｒ5의 조절제로서의 아미노 1,2,4-트리아졸 유도체
US8334287B2 (en) * 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
US8389536B2 (en) * 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
CN103097391B (zh) * 2010-07-09 2015-04-08 雷科尔达蒂爱尔兰有限公司 作为mGlu5拮抗剂的新型螺环杂环化合物
US8642626B2 (en) * 2010-07-29 2014-02-04 Taisho Pharmaceutical Co., Ltd. Ethinyl-pyrazole derivative
MY165141A (en) * 2011-04-26 2018-02-28 Hoffmann La Roche Pyrazolidin-3-one derivatives
US20130123254A1 (en) * 2011-09-30 2013-05-16 Barbara Biemans Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification
UA110995C2 (uk) * 2011-10-07 2016-03-10 Ф. Хоффманн-Ля Рош Аг Етинільні похідні як модулятори метаботропного глутаматного рецептора
UA110862C2 (uk) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
PL2875000T3 (pl) * 2012-07-17 2017-03-31 F.Hoffmann-La Roche Ag Pochodne aryloetynylowe
ES2594031T3 (es) * 2012-09-27 2016-12-15 F. Hoffmann-La Roche Ag Derivados de ariletinilo

Also Published As

Publication number Publication date
PH12015500261A1 (en) 2015-03-30
UA113223C2 (xx) 2016-12-26
HRP20161692T1 (hr) 2017-02-24
MA37895A1 (fr) 2016-12-30
AU2013304212B2 (en) 2017-03-09
IL237015A (en) 2016-11-30
ES2601511T3 (es) 2017-02-15
RS55397B1 (sr) 2017-04-28
US9199971B2 (en) 2015-12-01
JP2015528824A (ja) 2015-10-01
DK2882742T3 (en) 2016-12-12
CN104540815B (zh) 2016-10-19
PL2882742T3 (pl) 2017-03-31
CN104540815A (zh) 2015-04-22
CA2880257A1 (en) 2014-02-20
PT2882742T (pt) 2016-11-16
MX2015001599A (es) 2015-05-11
WO2014026880A1 (en) 2014-02-20
EP2882742A1 (en) 2015-06-17
SI2882742T1 (sl) 2017-01-31
AR092097A1 (es) 2015-03-25
MX358011B (es) 2018-08-02
ZA201500582B (en) 2016-08-31
HUE030237T2 (en) 2017-04-28
CY1118595T1 (el) 2017-07-12
KR20150041132A (ko) 2015-04-15
EA025165B1 (ru) 2016-11-30
PE20150685A1 (es) 2015-05-11
CA2880257C (en) 2020-07-21
NZ704858A (en) 2018-02-23
JP5974179B2 (ja) 2016-08-23
LT2882742T (lt) 2016-12-12
EP2882742B1 (en) 2016-09-21
MA37895B1 (fr) 2017-08-31
CL2015000290A1 (es) 2015-07-03
PH12015500261B1 (en) 2015-03-30
CO7180198A2 (es) 2015-02-09
US20150158848A1 (en) 2015-06-11
AU2013304212A1 (en) 2015-02-12
TW201410671A (zh) 2014-03-16
HK1207378A1 (en) 2016-01-29
KR101747005B1 (ko) 2017-06-27
BR112015002921A2 (pt) 2019-07-30
SG11201501055SA (en) 2015-03-30
TWI501958B (zh) 2015-10-01
CR20150028A (es) 2015-02-27
MY170255A (en) 2019-07-13

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Legal Events

Date Code Title Description
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