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)
  • 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)
  • Addiction (AREA)
  • Hospice & Palliative Care (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

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
ES2689956T3 (es) * 2010-11-05 2018-11-16 Oat Agrio Co., Ltd. Compuesto de etinilfenilamidina o sal del mismo, procedimiento para producir el mismo y fungicida para una utilización agrícola y hortícola
KR101554803B1 (ko) 2011-04-26 2015-09-21 에프. 호프만-라 로슈 아게 Mglur5의 양성 알로스테릭 조절체로서 에틴일 유도체
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
PE20150708A1 (es) * 2012-09-27 2015-05-15 Hoffmann La Roche Derivados de ariletinilo
EA026941B1 (ru) * 2012-10-18 2017-06-30 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ЭТИНИЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРА mGluR5
MX2015005375A (es) * 2012-11-07 2015-07-21 Hoffmann La Roche Compuestos de triazolo.
HRP20200638T1 (hr) 2015-06-03 2020-07-10 F. Hoffmann - La Roche Ag Derivati etinila
ES2733468T3 (es) 2015-07-15 2019-11-29 Hoffmann La Roche Derivados de etinilo como moduladores de los receptores metabotrópicos de glutamato
SI3484889T1 (sl) 2016-07-18 2020-11-30 F. Hoffmann-La Roche Ag Derivati etinila
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
NZ510743A (en) * 1998-10-02 2003-10-31 Novartis Ag mGluR5 antagonists for the treatment of pain and anxiety
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
GB0127433D0 (en) * 2001-11-15 2002-01-09 Smithkline Beecham Corp Compounds
GB0127430D0 (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 (fr) 2004-11-04 2006-05-11 Addex Pharmaceuticals 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
JP2008542323A (ja) * 2005-06-01 2008-11-27 ユセベ ファルマ ソシエテ アノニム ２−オキソ−１−ピロリジン誘導体、その製造方法及びその使用
CA2755268C (fr) 2005-11-15 2013-12-31 Array Biopharma, Inc. Inhibiteurs erbb
MX2008016523A (es) 2006-06-30 2009-01-19 Astrazeneca Ab Derivados de pirimidina utiles en el tratamiento de cancer.
EP1972628A1 (fr) 2007-03-21 2008-09-24 Schwarz Pharma Ag Indolizines et leurs dérivés aza analogues en tant que composés actifs du SNC
CA2685524A1 (fr) * 2007-04-30 2008-11-06 Abbott Laboratories Inhibiteurs d'enzyme diacylglycerol o-acyltransferase de type 1
NZ581817A (en) 2007-06-03 2012-05-25 Univ Vanderbilt 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
KR20120095472A (ko) 2012-08-28
JP5763094B2 (ja) 2015-08-12
AU2010332987B2 (en) 2015-08-13
CL2012001596A1 (es) 2013-01-04
US20140073638A1 (en) 2014-03-13
ZA201204429B (en) 2013-02-27
MX2012006789A (es) 2012-07-10
UA107002C2 (uk) 2014-11-10
BR112012014770A2 (pt) 2016-03-29
ECSP12011977A (es) 2012-07-31
TWI448465B (zh) 2014-08-11
AR079467A1 (es) 2012-01-25
JP2013514305A (ja) 2013-04-25
SG181779A1 (en) 2012-07-30
PH12012500867A1 (en) 2014-10-14
RU2012128551A (ru) 2014-01-27
AU2010332987A1 (en) 2012-06-07
WO2011073172A1 (fr) 2011-06-23
IL219371A0 (en) 2012-06-28
CR20120269A (es) 2012-07-04
CA2780155A1 (fr) 2011-06-23
US8586581B2 (en) 2013-11-19
CN102686589B (zh) 2014-12-10
PE20121443A1 (es) 2012-10-26
ES2551582T3 (es) 2015-11-20
KR101407856B1 (ko) 2014-06-16
MY162998A (en) 2017-07-31
CN102686589A (zh) 2012-09-19
EP2513102B1 (fr) 2015-08-19
NZ599553A (en) 2014-05-30
RU2553461C2 (ru) 2015-06-20
EP2513102A1 (fr) 2012-10-24
US20110152257A1 (en) 2011-06-23
HK1171225A1 (en) 2013-03-22
US8933094B2 (en) 2015-01-13
IL219371A (en) 2015-02-26
TW201144314A (en) 2011-12-16
CO6531478A2 (es) 2012-09-28

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