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.

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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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    • 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
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    • 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
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    • 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
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    • 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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    • 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
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    • C07D473/00Heterocyclic compounds containing purine ring systems
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    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
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    • 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
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    • 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

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

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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 (28)

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)
HK (1) HK1220200A1 (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)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA029261B1 (ru) * 2014-02-25 2018-02-28 Ф. Хоффманн-Ля Рош Аг Производные этинила
JP6539749B2 (ja) * 2015-03-19 2019-07-03 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft mGluR4のモジュレーターとしての3−(4−エチニルフェニル)ヘキサヒドロピリミジン−2,4−ジオン誘導体
KR20180026438A (ko) 2015-07-15 2018-03-12 에프. 호프만-라 로슈 아게 대사형 글루타메이트 수용체 조절제로서의 에틴일 유도체
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
ES2826389T3 (es) * 2016-07-18 2021-05-18 Hoffmann La Roche Derivados de etinilo
CA3102326A1 (en) 2018-07-26 2020-01-30 Domain Therapeutics Substituted quinazolinone derivatives and their use as positive allosteric modulators of mglur4

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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
MX2009013169A (es) * 2007-06-03 2010-04-30 Univ Vanderbilt Moduladores alostericos positivos del mglur5 benzamida y metodos de elaboracion y uso de los mismos.
US8779157B2 (en) * 2009-09-04 2014-07-15 Vanderbilt University MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
CA2789434A1 (en) * 2010-02-11 2011-08-18 Vanderbilt University Benzisoxazoles and azabenzisoxazoles as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
KR20130079429A (ko) * 2010-05-12 2013-07-10 벤더르빌트 유니버시티 헤테로시클릭 설폰 mglur4 알로스테릭 강화제, 조성물 및 신경 기능이상을 치료하는 방법
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

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

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