PE20160604A1 - Derivados de etinilo como antagonistas del receptor metabotropico de glutamato - Google Patents

Derivados de etinilo como antagonistas del receptor metabotropico de glutamato

Info

Publication number
PE20160604A1
PE20160604A1 PE2015002663A PE2015002663A PE20160604A1 PE 20160604 A1 PE20160604 A1 PE 20160604A1 PE 2015002663 A PE2015002663 A PE 2015002663A PE 2015002663 A PE2015002663 A PE 2015002663A PE 20160604 A1 PE20160604 A1 PE 20160604A1
Authority
PE
Peru
Prior art keywords
antagonists
metabotropic glutamate
glutamate receptor
hydrogen
derivatives
Prior art date
Application number
PE2015002663A
Other languages
English (en)
Inventor
Eric Vieira
Heinz Stadler
Daniel Rueher
Georg Jaeschke
Rainer E Martin
Lothar Lindemann
Antonio Ricci
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 PE20160604A1 publication Critical patent/PE20160604A1/es

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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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La presente invencion se refiere a derivados de etinilo de formula I: en la que: Y es N o CH, R1 es hidrogeno, fluor o cloro, y R2 es hidrogeno o alquilo inferior, o una sal de adicion de acido farmaceuticamente aceptable de los mismos. Ahora se ha encontrado inesperadamente que los compuestos de formula general I son antagonistas de receptores metabotropicos de glutamato (modulares alostericos negativos) para la utilizacion en el tratamiento de la ansiedad y el dolor, la depresion, el sindrome del cromosoma X fragil, los trastornos del espectro autista, la enfermedad de Parkinson y la enfermedad por reflujo gastroesofagico (ERGE)
PE2015002663A 2013-07-08 2014-07-04 Derivados de etinilo como antagonistas del receptor metabotropico de glutamato PE20160604A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13175535 2013-07-08

Publications (1)

Publication Number Publication Date
PE20160604A1 true PE20160604A1 (es) 2016-07-03

Family

ID=48745843

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015002663A PE20160604A1 (es) 2013-07-08 2014-07-04 Derivados de etinilo como antagonistas del receptor metabotropico de glutamato

Country Status (28)

Country Link
US (2) US9682959B2 (es)
EP (1) EP3019486B1 (es)
JP (1) JP6116761B2 (es)
KR (1) KR101767348B1 (es)
CN (1) CN105358543B (es)
AR (1) AR096824A1 (es)
AU (1) AU2014289398B2 (es)
BR (1) BR112015029724A2 (es)
CA (1) CA2914282A1 (es)
CL (1) CL2015003761A1 (es)
CR (1) CR20150650A (es)
DK (1) DK3019486T3 (es)
EA (1) EA027882B1 (es)
ES (1) ES2628206T3 (es)
HK (1) HK1215573A1 (es)
HU (1) HUE033270T2 (es)
IL (1) IL242682B (es)
MA (1) MA38659B1 (es)
MY (1) MY181847A (es)
PE (1) PE20160604A1 (es)
PH (1) PH12015502692A1 (es)
PL (1) PL3019486T3 (es)
SG (1) SG11201510607RA (es)
SI (1) SI3019486T1 (es)
TW (1) TWI527808B (es)
UA (1) UA116023C2 (es)
WO (1) WO2015004007A1 (es)
ZA (1) ZA201508410B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016273751B2 (en) 2015-06-03 2020-04-02 F. Hoffmann-La Roche Ag Ethynyl derivatives
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
SG11202005361RA (en) 2017-12-14 2020-07-29 H Lundbeck As Combination treatments comprising administration of 1h-pyrazolo[4,3-b]pyridines
JP7194738B2 (ja) 2017-12-20 2022-12-22 ハー・ルンドベック・アクチエゼルスカベット PDE1阻害剤としてのピラゾロ[3,4-b]ピリジン及びイミダゾ[1,5-b]ピリダジン

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN153523B (es) * 1980-06-02 1984-07-21 American Cyanamid Co
FI90869C (fi) * 1986-11-14 1994-04-11 Tanabe Seiyaku Co Menetelmä lääkeaineena käyttökelpoisten imidatsolidinonijohdannaisten valmistamiseksi
TW544448B (en) 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
TWI292318B (en) 2003-03-10 2008-01-11 Hoffmann La Roche Imidazol-4-yl-ethynyl-pyridine derivatives
CA2583572C (en) * 2004-10-07 2016-07-12 Merck & Co., Inc. Thiazolyl mglur5 antagonists and methods for their use
US8389536B2 (en) * 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
KR101554803B1 (ko) * 2011-04-26 2015-09-21 에프. 호프만-라 로슈 아게 Mglur5의 양성 알로스테릭 조절체로서 에틴일 유도체
CA2829171C (en) * 2011-04-26 2019-02-26 F. Hoffmann-La Roche Ag Pyrazolidin-3-one derivatives
UA110862C2 (uk) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5

Also Published As

Publication number Publication date
CR20150650A (es) 2016-01-11
JP6116761B2 (ja) 2017-04-19
EA027882B1 (ru) 2017-09-29
US9682959B2 (en) 2017-06-20
SI3019486T1 (sl) 2017-07-31
PH12015502692B1 (en) 2016-03-14
EA201690162A1 (ru) 2016-05-31
UA116023C2 (uk) 2018-01-25
SG11201510607RA (en) 2016-01-28
MY181847A (en) 2021-01-08
DK3019486T3 (en) 2017-06-19
AU2014289398A1 (en) 2015-11-26
PL3019486T3 (pl) 2017-08-31
IL242682B (en) 2018-11-29
US20170217926A1 (en) 2017-08-03
CA2914282A1 (en) 2015-01-15
CL2015003761A1 (es) 2016-07-15
JP2016523939A (ja) 2016-08-12
US20160130255A1 (en) 2016-05-12
ES2628206T3 (es) 2017-08-02
MA38659A1 (fr) 2016-02-29
AU2014289398B2 (en) 2018-02-01
TWI527808B (zh) 2016-04-01
HK1215573A1 (zh) 2016-09-02
KR101767348B1 (ko) 2017-08-10
MA38659B1 (fr) 2016-10-31
US9751856B2 (en) 2017-09-05
PH12015502692A1 (en) 2016-03-14
WO2015004007A1 (en) 2015-01-15
HUE033270T2 (en) 2017-11-28
KR20160017026A (ko) 2016-02-15
AR096824A1 (es) 2016-02-03
BR112015029724A2 (pt) 2017-07-25
TW201506019A (zh) 2015-02-16
ZA201508410B (en) 2017-08-30
EP3019486A1 (en) 2016-05-18
EP3019486B1 (en) 2017-04-12
CN105358543B (zh) 2018-06-12
CN105358543A (zh) 2016-02-24

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