MA33802B1 - Dérivés d'éthynyle - Google Patents

Dérivés d'éthynyle

Info

Publication number
MA33802B1
MA33802B1 MA34890A MA34890A MA33802B1 MA 33802 B1 MA33802 B1 MA 33802B1 MA 34890 A MA34890 A MA 34890A MA 34890 A MA34890 A MA 34890A MA 33802 B1 MA33802 B1 MA 33802B1
Authority
MA
Morocco
Prior art keywords
lower alkyl
alkoxy
formula
hydroxy
optionally substituted
Prior art date
Application number
MA34890A
Other languages
Arabic (ar)
English (en)
Inventor
Luke Green
Wolfgang Guba
Georg Jaeschke
Synese Jolidon
Lothar Lindemann
Heinz Stadler
Eric Vieira
Original Assignee
Hoffmann La Roche
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=MA33802(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MA33802B1 publication Critical patent/MA33802B1/fr

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

Abstract

Cette invention concerne des dérivés d'éthynyle de formule (i) ou un sel ou sel d'addition d'acide pharmaceutiquement acceptable de ceux-ci, un mélange racémique, ou l'énantiomère et/ou l'isomère optique et/ou le stéréoisomère lui correspondant. Dans la formule (i), x est n ou c-r1 ; y est n ou c-r2 ; z est ch ou n; r4 est un substituant aromatique à 6 chaînons contenant 0, 1 ou 2 atomes d'azote, éventuellement substitué par de 1 à 3 groupes, choisis parmi un atome d'halogène, un groupe alkyle inférieur, alcoxy inférieur ou nrr'; r1 est un atome d'hydrogène, un groupe alkyle inférieur, alcoxy inférieur, hydroxy, hydroxyalkyle inférieur, cycloalkyle inférieur ou est un groupe hétérocycloalkyle éventuellement substitué par un hydroxy ou un alcoxy; r2 est un atome d'hydrogène, un groupe cn, alkyle inférieur ou hétérocycloalkyle; r et r' sont indépendamment l'un de l'autre un atome d'hydrogène ou un groupe alkyle inférieur. De manière surprenante, on a maintenant découvert que les composés de formule générale i sont des modulateurs allostériques positifs (pam) du récepteur métabotrope du glutamate de sous-type 5 (mglur5) et qu'ils sont, par conséquent, utiles pour traiter les maladies liées à ce récepteur.
MA34890A 2009-12-17 2012-05-24 Dérivés d'éthynyle MA33802B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09179719 2009-12-17
PCT/EP2010/069593 WO2011073172A1 (fr) 2009-12-17 2010-12-14 Dérivés d'éthynyle

Publications (1)

Publication Number Publication Date
MA33802B1 true MA33802B1 (fr) 2012-12-03

Family

ID=43446449

Family Applications (1)

Application Number Title Priority Date Filing Date
MA34890A MA33802B1 (fr) 2009-12-17 2012-05-24 Dérivés d'éthynyle

Country Status (27)

Country Link
US (2) US8586581B2 (fr)
EP (1) EP2513102B1 (fr)
JP (1) JP5763094B2 (fr)
KR (1) KR101407856B1 (fr)
CN (1) CN102686589B (fr)
AR (1) AR079467A1 (fr)
AU (1) AU2010332987B2 (fr)
BR (1) BR112012014770A2 (fr)
CA (1) CA2780155A1 (fr)
CL (1) CL2012001596A1 (fr)
CO (1) CO6531478A2 (fr)
CR (1) CR20120269A (fr)
EC (1) ECSP12011977A (fr)
ES (1) ES2551582T3 (fr)
IL (1) IL219371A (fr)
MA (1) MA33802B1 (fr)
MX (1) MX2012006789A (fr)
MY (1) MY162998A (fr)
NZ (1) NZ599553A (fr)
PE (1) PE20121443A1 (fr)
PH (1) PH12012500867A1 (fr)
RU (1) RU2553461C2 (fr)
SG (1) SG181779A1 (fr)
TW (1) TWI448465B (fr)
UA (1) UA107002C2 (fr)
WO (1) WO2011073172A1 (fr)
ZA (1) ZA201204429B (fr)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3006745C (fr) 2010-11-05 2021-03-30 Oat Agrio Co., Ltd. Ethynylphenylamidine ou l'un de ses sels, son procede de production et fongicide pour applications agricoles et horticoles
EA022019B1 (ru) 2011-04-26 2015-10-30 Ф.Хоффманн-Ля Рош Аг Этинильные производные в качестве положительных аллостерических модуляторов mglur5
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
UA114008C2 (xx) * 2012-10-18 2017-04-10 Похідні етинілу як модулятори активності рецептора mglur5
MX2015005375A (es) * 2012-11-07 2015-07-21 Hoffmann La Roche Compuestos de triazolo.
AU2016273751B2 (en) 2015-06-03 2020-04-02 F. Hoffmann-La Roche Ag Ethynyl derivatives
TR201909160T4 (tr) 2015-07-15 2019-07-22 Hoffmann La Roche Metabotropik glutamat reseptörü modülatörleri olarak etinil türevleri.
WO2018015235A1 (fr) 2016-07-18 2018-01-25 F. Hoffmann-La Roche Ag Dérivés d'éthynyle
WO2026072192A1 (fr) 2024-09-27 2026-04-02 Alto Neuroscience, Inc. Traitement efficace de la dépression chez des patients présentant des troubles cognitifs ou des difficultés d'apprentissage et/ou de mémoire avec un modulateur allostérique positif mglur5

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ID29095A (id) * 1998-10-02 2001-07-26 Novartis Ag Cs Antagonis mglur5 untuk pengobatan rasa sakit dan kegelisahan
AR029803A1 (es) * 2000-02-21 2003-07-16 Smithkline Beecham Plc Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden
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
EP1809620B1 (fr) 2004-11-04 2010-12-29 Addex Pharma SA Nouveaux derives de tetrazole utilises comme modulateurs allosteriques positifs des recepteurs de glutamate metabotropiques
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
US8178533B2 (en) * 2005-06-01 2012-05-15 Ucb Pharma, S.A. 2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses
DE602006021645D1 (de) 2005-11-15 2011-06-09 Array Biopharma Inc Verfahren und Zwischenverbindungen zur Herstellung von N4-Phenyl-Quinazolin-4-Amin Derivaten
TW200817391A (en) 2006-06-30 2008-04-16 Astrazeneca Ab Novel compounds
EP1972628A1 (fr) 2007-03-21 2008-09-24 Schwarz Pharma Ag Indolizines et leurs dérivés aza analogues en tant que composés actifs du SNC
NZ580662A (en) * 2007-04-30 2012-01-12 Abbott Lab Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme used in manufacture of medicament for treatment of diabetes or lipid associated disorders
KR20100033981A (ko) 2007-06-03 2010-03-31 벤더르빌트 유니버시티 벤즈아미드 대사성 글루타민산염 수용체5 양성 알로스테릭 조절자 및 이의 제조 및 사용방법
TW201116532A (en) * 2009-08-05 2011-05-16 Merz Pharma Gmbh & Co Kgaa Metabotropic glutamate receptor modulators

Also Published As

Publication number Publication date
US20110152257A1 (en) 2011-06-23
US8586581B2 (en) 2013-11-19
PH12012500867A1 (en) 2014-10-14
AU2010332987A1 (en) 2012-06-07
CN102686589A (zh) 2012-09-19
BR112012014770A2 (pt) 2016-03-29
MX2012006789A (es) 2012-07-10
AR079467A1 (es) 2012-01-25
TWI448465B (zh) 2014-08-11
CO6531478A2 (es) 2012-09-28
KR20120095472A (ko) 2012-08-28
IL219371A (en) 2015-02-26
HK1171225A1 (en) 2013-03-22
EP2513102B1 (fr) 2015-08-19
CN102686589B (zh) 2014-12-10
US20140073638A1 (en) 2014-03-13
AU2010332987B2 (en) 2015-08-13
WO2011073172A1 (fr) 2011-06-23
RU2553461C2 (ru) 2015-06-20
NZ599553A (en) 2014-05-30
UA107002C2 (uk) 2014-11-10
MY162998A (en) 2017-07-31
TW201144314A (en) 2011-12-16
EP2513102A1 (fr) 2012-10-24
ES2551582T3 (es) 2015-11-20
JP5763094B2 (ja) 2015-08-12
RU2012128551A (ru) 2014-01-27
IL219371A0 (en) 2012-06-28
ZA201204429B (en) 2013-02-27
CR20120269A (es) 2012-07-04
KR101407856B1 (ko) 2014-06-16
ECSP12011977A (es) 2012-07-31
SG181779A1 (en) 2012-07-30
CA2780155A1 (fr) 2011-06-23
PE20121443A1 (es) 2012-10-26
US8933094B2 (en) 2015-01-13
CL2012001596A1 (es) 2013-01-04
JP2013514305A (ja) 2013-04-25

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