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CL2016000677A1 - Compuestos derivados de etinilo, moduladores alostericos positivos del receptor mglur4; composicion farmaceutica que los comprende; y su uso en enfermedades del snc, cancer y diabetes tipo 2. - Google Patents

Compuestos derivados de etinilo, moduladores alostericos positivos del receptor mglur4; composicion farmaceutica que los comprende; y su uso en enfermedades del snc, cancer y diabetes tipo 2.

Info

Publication number
CL2016000677A1
CL2016000677A1 CL2016000677A CL2016000677A CL2016000677A1 CL 2016000677 A1 CL2016000677 A1 CL 2016000677A1 CL 2016000677 A CL2016000677 A CL 2016000677A CL 2016000677 A CL2016000677 A CL 2016000677A CL 2016000677 A1 CL2016000677 A1 CL 2016000677A1
Authority
CL
Chile
Prior art keywords
diabetes
cancer
type
ethynyl
cns
Prior art date
Application number
CL2016000677A
Other languages
English (en)
Inventor
Georg Jaeschke
Antonio Ricci
Daniel Rueher
Eric Vieira
Wolfgang Guba
Barbara Biemans
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 CL2016000677A1 publication Critical patent/CL2016000677A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C07D239/96Two oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/10Antiepileptics; Anticonvulsants for petit-mal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • C07D239/91Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • 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
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    • 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
    • C07D401/10Heterocyclic 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 linked by a carbon chain containing aromatic rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
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    • C07D475/04Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyridine Compounds (AREA)
  • Epidemiology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Se describen compuestos de fórmula I. Se describen además las composiciones farmacéuticas que los comprenden; y uso de los compuestos para preparar un medicamento útil en el tratamiento de la enfermedad de Parkinson, la ansiedad, la emesis, el trastorno obsesivo-compulsivo, el autismo, la neuroprotección, el cáncer, la depresión y la diabetes de tipo 2.
CL2016000677A 2013-09-25 2016-03-23 Compuestos derivados de etinilo, moduladores alostericos positivos del receptor mglur4; composicion farmaceutica que los comprende; y su uso en enfermedades del snc, cancer y diabetes tipo 2. CL2016000677A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13185856 2013-09-25

Publications (1)

Publication Number Publication Date
CL2016000677A1 true CL2016000677A1 (es) 2016-11-04

Family

ID=49230629

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2016000677A CL2016000677A1 (es) 2013-09-25 2016-03-23 Compuestos derivados de etinilo, moduladores alostericos positivos del receptor mglur4; composicion farmaceutica que los comprende; y su uso en enfermedades del snc, cancer y diabetes tipo 2.

Country Status (27)

Country Link
US (2) US20160207890A1 (es)
EP (1) EP3049409B1 (es)
JP (1) JP6134441B2 (es)
KR (1) KR101757603B1 (es)
CN (1) CN105579447B (es)
AR (1) AR097721A1 (es)
AU (1) AU2014327504B2 (es)
BR (1) BR112016005994A2 (es)
CA (1) CA2924376A1 (es)
CL (1) CL2016000677A1 (es)
CR (1) CR20160075A (es)
DK (1) DK3049409T3 (es)
EA (1) EA029352B1 (es)
ES (1) ES2630319T3 (es)
HU (1) HUE034849T2 (es)
IL (1) IL244039B (es)
MA (1) MA38885B1 (es)
MX (1) MX370341B (es)
MY (1) MY183953A (es)
PE (1) PE20160666A1 (es)
PH (1) PH12016500427A1 (es)
PL (1) PL3049409T3 (es)
SG (1) SG11201602029VA (es)
SI (1) SI3049409T1 (es)
TW (1) TWI527801B (es)
UA (1) UA116277C2 (es)
WO (1) WO2015044075A1 (es)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12006323B2 (en) 2015-07-15 2024-06-11 Hoffmann-La Roche Inc. Ethynyl derivatives

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3110802B1 (en) * 2014-02-25 2018-10-10 F. Hoffmann-La Roche AG Ethynyl derivatives
EP3271353B1 (en) * 2015-03-19 2019-11-27 H. Hoffnabb-La Roche Ag 3-(4-ethynylphenyl)hexahydropyrimidin-2,4-dione derivatives as modulators of mglur4
AR105556A1 (es) * 2015-08-03 2017-10-18 Hoffmann La Roche Derivados de etinilo
US10308656B2 (en) 2015-08-18 2019-06-04 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of Ku70/80 and uses thereof
MA45665B1 (fr) 2016-07-18 2020-11-30 Hoffmann La Roche Dérivés d'éthynyle
JP7633676B2 (ja) 2018-07-26 2025-02-20 ドメイン・セラピューティクス 置換キナゾリノン誘導体、及びmGluR4のポジティブアロステリック調節剤としてのその使用

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Publication number Priority date Publication date Assignee Title
JPH10330359A (ja) * 1997-03-31 1998-12-15 Nippon Bayeragrochem Kk フエニルアセチレン誘導体及び除草剤
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
SG185285A1 (en) * 2007-06-03 2012-11-29 Univ Vanderbilt Benzamide mglur5 positive allosteric modulators and methods of making and using same
CA2773038A1 (en) * 2009-09-04 2011-03-10 P. Jeffrey Conn Mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
KR20120120416A (ko) * 2010-02-11 2012-11-01 벤더르빌트 유니버시티 Mglur4 알로스테릭 강화제로서 벤즈이속사졸 및 아자벤즈이속사졸, 조성물, 및 신경 기능이상을 치료하는 방법
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
JP2013526544A (ja) * 2010-05-12 2013-06-24 ヴァンダービルト ユニバーシティー 複素環スルホンmGluR4アロステリック増強剤、組成物、および神経機能不全を治療する方法
UA110862C2 (uk) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
CN102503888A (zh) * 2011-10-08 2012-06-20 西安交通大学 2-芳基-1,3-异喹啉二酮类抗肿瘤化合物及其合成方法和用途

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12006323B2 (en) 2015-07-15 2024-06-11 Hoffmann-La Roche Inc. Ethynyl derivatives

Also Published As

Publication number Publication date
PE20160666A1 (es) 2016-07-09
MY183953A (en) 2021-03-17
SG11201602029VA (en) 2016-04-28
SI3049409T1 (sl) 2017-08-31
IL244039B (en) 2019-06-30
JP2016531869A (ja) 2016-10-13
KR20160044581A (ko) 2016-04-25
EP3049409B1 (en) 2017-05-03
AR097721A1 (es) 2016-04-13
PL3049409T3 (pl) 2017-09-29
MA38885B1 (fr) 2018-11-30
CR20160075A (es) 2016-05-04
UA116277C2 (uk) 2018-02-26
DK3049409T3 (en) 2017-07-10
BR112016005994A2 (pt) 2017-08-01
EA201690408A1 (ru) 2016-07-29
IL244039A0 (en) 2016-04-21
EP3049409A1 (en) 2016-08-03
EA029352B1 (ru) 2018-03-30
TW201524963A (zh) 2015-07-01
ES2630319T3 (es) 2017-08-21
PH12016500427A1 (en) 2016-05-16
HUE034849T2 (en) 2018-03-28
MX2016002717A (es) 2016-06-08
AU2014327504A1 (en) 2016-02-18
CA2924376A1 (en) 2015-04-02
JP6134441B2 (ja) 2017-05-24
AU2014327504B2 (en) 2018-01-04
HK1220200A1 (zh) 2017-04-28
US20160207890A1 (en) 2016-07-21
TWI527801B (zh) 2016-04-01
CN105579447A (zh) 2016-05-11
KR101757603B1 (ko) 2017-07-12
WO2015044075A1 (en) 2015-04-02
US9676732B2 (en) 2017-06-13
CN105579447B (zh) 2018-11-13
MA38885A1 (fr) 2017-12-29
MX370341B (es) 2019-12-10
US20170114028A1 (en) 2017-04-27

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