IN2014CN02478A - - Google Patents

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Publication number
IN2014CN02478A
IN2014CN02478A IN2478CHN2014A IN2014CN02478A IN 2014CN02478 A IN2014CN02478 A IN 2014CN02478A IN 2478CHN2014 A IN2478CHN2014 A IN 2478CHN2014A IN 2014CN02478 A IN2014CN02478 A IN 2014CN02478A
Authority
IN
India
Prior art keywords
lower alkyl
hydrogen
cycloalkyl
attached
form together
Prior art date
Application number
Inventor
Georg Jaeschke
Lothar Lindemann
Antonio Ricci
Daniel Rueher
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of IN2014CN02478A publication Critical patent/IN2014CN02478A/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (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)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

The present invention relates to ethynyl derivatives of formula (I) wherein U is N or CH R is hydrogen halogen lower alkyl or lower alkoxy;Y is N(R) O or C(RR ) ; wherein R4 is hydrogen or lower alkyl and R/R are independently hydrogen hydroxy lower alkyl or lower alkoxy; V is N(R) or C(RR) wherein R6 is hydrogen or lower alkyl and R/R are independently from each other hydrogen lower alkyl CH lower alkoxy or may form together with the carbon atom to which they are attached a C C cycloalkyl; R is phenyl or heteroaryl which are optionally substituted by halogen lower alkyl or lower alkoxy; m is 0 or 1; in case m is 1 R/R are independently from each other hydrogen lower alkyl CH lower alkoxy or may form together with the carbon atom to which they are attached a C C cycloalkyl; n is 0 or 1; in case n is 1 R/R are independently from each other hydrogen lower alkyl CH lower alkoxy or may form together with the carbon atom to which they are attached a C C cycloalkyl; or if m is 1 and n is 0 R and R may form together with the carbon atoms to which they are attached a C cycloalkyl; or if m is 1 and n is 1 R and R or R and R may form together with the carbon atoms to which they are attached a C cycloalkyl; or to a pharmaceutically acceptable acid addition salt to a racemic mixture or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula (I) are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
IN2478CHN2014 2011-10-07 2012-10-04 IN2014CN02478A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11184331 2011-10-07
PCT/EP2012/069599 WO2013050454A1 (en) 2011-10-07 2012-10-04 Ethynyl derivatives as mglur5 allosteric modulators

Publications (1)

Publication Number Publication Date
IN2014CN02478A true IN2014CN02478A (en) 2015-06-19

Family

ID=46968237

Family Applications (1)

Application Number Title Priority Date Filing Date
IN2478CHN2014 IN2014CN02478A (en) 2011-10-07 2012-10-04

Country Status (26)

Country Link
US (1) US8969338B2 (en)
EP (1) EP2763977B1 (en)
JP (1) JP5840793B2 (en)
KR (1) KR101637792B1 (en)
CN (1) CN103857668B (en)
AR (1) AR088246A1 (en)
AU (1) AU2012320598B2 (en)
BR (1) BR112014007898A2 (en)
CA (1) CA2850082C (en)
CL (1) CL2014000819A1 (en)
CO (1) CO6900143A2 (en)
CR (1) CR20140094A (en)
EA (1) EA024973B1 (en)
EC (1) ECSP14013296A (en)
ES (1) ES2564884T3 (en)
HK (1) HK1195298A1 (en)
IL (1) IL231783A (en)
IN (1) IN2014CN02478A (en)
MX (1) MX360667B (en)
MY (1) MY170822A (en)
PE (1) PE20141556A1 (en)
SG (1) SG11201401322UA (en)
TW (1) TWI468401B (en)
UA (1) UA110862C2 (en)
WO (1) WO2013050454A1 (en)
ZA (1) ZA201402069B (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
UA113223C2 (en) * 2012-08-13 2016-12-26 ARYLETINYLPYRIMIDINE
AU2013331782B2 (en) * 2012-10-18 2017-03-09 F. Hoffmann-La Roche Ag Ethynyl derivatives as modulators of mGluR5 receptor activity
UA116023C2 (en) * 2013-07-08 2018-01-25 Ф. Хоффманн-Ля Рош Аг Ethynyl derivatives as metabotropic glutamate receptor antagonists
AU2014327504B2 (en) * 2013-09-25 2018-01-04 F. Hoffmann-La Roche Ag Ethynyl derivatives
CR20170536A (en) 2015-06-03 2018-02-01 Hoffmann La Roche ETHYLENE DERIVATIVES
MA42442B1 (en) 2015-07-15 2019-07-31 Hoffmann La Roche Ethynyl derivatives as modulators of the metabotropic glutamate receptor
CN106632243B (en) * 2015-10-28 2019-03-15 华领医药技术(上海)有限公司 Pyrrolidin derivatives
RU2745068C2 (en) 2016-07-18 2021-03-18 Ф. Хоффманн-Ля Рош Аг Ethinyl derivatives
WO2019034713A1 (en) 2017-08-17 2019-02-21 F. Hoffmann-La Roche Ag Imidazo[1,2-a]imidazol-2-one derivatives for the treatment of diseases such as parkinson's disease
PE20232046A1 (en) 2020-12-17 2023-12-27 Astrazeneca Ab N-(2-(4-CYANOTHIAZOLIDIN-3-IL)-2-OXOETIL)-QUINOLIN-4-CARBOXAMIDES

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3213780B2 (en) 1993-12-21 2001-10-02 キヤノン株式会社 Optically active compound, liquid crystal composition containing the same, liquid crystal element using the liquid crystal composition, display method and display device using the same
JPH09151179A (en) 1995-11-30 1997-06-10 Canon Inc Optically active compound, liquid crystal composition containing the same, liquid crystal element having the composition, liquid crystal apparatus and displaying method using them
US6410728B1 (en) 2000-08-31 2002-06-25 Abbott Laboratories Oxazolidinone chemotherapeutic agents
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
EP1809620B1 (en) 2004-11-04 2010-12-29 Addex Pharma 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
EA200971143A1 (en) * 2007-06-03 2010-06-30 Вандербилт Юниверсити BENZAMIDE MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS FOR THEIR RECEIVING AND APPLICATION
US8389536B2 (en) 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
US8586581B2 (en) * 2009-12-17 2013-11-19 Hoffmann-La Roche Inc Ethynyl compounds useful for treatment of CNS disorders
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
US8772300B2 (en) * 2011-04-19 2014-07-08 Hoffmann-La Roche Inc. Phenyl or pyridinyl-ethynyl derivatives
DK2702051T3 (en) * 2011-04-26 2015-03-16 Hoffmann La Roche Ethynyl derivatives AS POSITIVE allosteric modulators mGluR5
MY165141A (en) * 2011-04-26 2018-02-28 Hoffmann La Roche Pyrazolidin-3-one derivatives

Also Published As

Publication number Publication date
ES2564884T3 (en) 2016-03-29
US20130090332A1 (en) 2013-04-11
BR112014007898A2 (en) 2017-04-04
US8969338B2 (en) 2015-03-03
KR101637792B1 (en) 2016-07-07
KR20140077943A (en) 2014-06-24
CN103857668A (en) 2014-06-11
TW201321365A (en) 2013-06-01
NZ621894A (en) 2016-03-31
ECSP14013296A (en) 2014-05-31
CR20140094A (en) 2014-05-15
CO6900143A2 (en) 2014-03-20
SG11201401322UA (en) 2014-09-26
EA201490722A1 (en) 2014-07-30
EA024973B1 (en) 2016-11-30
CA2850082A1 (en) 2013-04-11
MY170822A (en) 2019-09-01
CA2850082C (en) 2019-05-28
MX360667B (en) 2018-11-13
AR088246A1 (en) 2014-05-21
CL2014000819A1 (en) 2014-09-22
TWI468401B (en) 2015-01-11
UA110862C2 (en) 2016-02-25
MX2014004144A (en) 2014-07-28
HK1195298A1 (en) 2014-11-07
JP2014528435A (en) 2014-10-27
EP2763977A1 (en) 2014-08-13
EP2763977B1 (en) 2016-02-24
IL231783A (en) 2015-09-24
IL231783A0 (en) 2014-05-28
JP5840793B2 (en) 2016-01-06
ZA201402069B (en) 2015-03-25
AU2012320598A1 (en) 2014-03-13
PE20141556A1 (en) 2014-10-30
CN103857668B (en) 2016-04-13
WO2013050454A1 (en) 2013-04-11
AU2012320598B2 (en) 2016-10-13

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