[go: up one dir, main page]

PE20121443A1 - Derivados de etinilo - Google Patents

Derivados de etinilo

Info

Publication number
PE20121443A1
PE20121443A1 PE2012000817A PE2012000817A PE20121443A1 PE 20121443 A1 PE20121443 A1 PE 20121443A1 PE 2012000817 A PE2012000817 A PE 2012000817A PE 2012000817 A PE2012000817 A PE 2012000817A PE 20121443 A1 PE20121443 A1 PE 20121443A1
Authority
PE
Peru
Prior art keywords
phenyletinyl
pyrimidine
compounds
pirazolo
pyrazolo
Prior art date
Application number
PE2012000817A
Other languages
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=PE20121443(A1) "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 PE20121443A1 publication Critical patent/PE20121443A1/es

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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE ETINILO DE FORMULA (I) DONDE X ES N O CR1, EN DONDE R1 ES H, ALQUILO INFERIOR, ALCOXI INFERIOR, HIDROXI, HIDROXIALQUILO INFERIOR, ENTRE OTROS; Y ES N O CR2, EN DONDE R2 ES H, CN, ALQUILO INFERIOR O HETEROCICLOALQUILO; Z ES CH O N; R4 ES UN SUSTITUYENTE AROMATICO DE 6 ESLABONES QUE CONTIENE HASTA 2 N OPCIONALMENTE SUSTITUIDO CON HALOGENO, ALQUILO INFERIOR, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-FENILETINIL-PIRAZOLO[1,5-a]PIRIMIDINA; 2-METIL-6-FENILETINIL-PIRAZOLO[1,5-a]PIRIMIDINA; 6-(2-FLUOR-FENILETINIL)-2-METIL-PIRAZOLO[1,5-a]PIRIMIDINA; 2-TERT-BUTIL-6-(3-FLUOR-FENILETINIL)-PIRAZOLO[1,5-a]-PIRIMIDINA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES ALOSTERICOS POSITIVOS DEL RECEPTOR DE GLUTAMATO METABOTROPICO DEL SUBTIPO 5 (mGluR5) SIENDO UTILES EN EL TRATAMIENTO DE ESQUIZOFRENIA
PE2012000817A 2009-12-17 2010-12-14 Derivados de etinilo PE20121443A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09179719 2009-12-17

Publications (1)

Publication Number Publication Date
PE20121443A1 true PE20121443A1 (es) 2012-10-26

Family

ID=43446449

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012000817A PE20121443A1 (es) 2009-12-17 2010-12-14 Derivados de etinilo

Country Status (27)

Country Link
US (2) US8586581B2 (es)
EP (1) EP2513102B1 (es)
JP (1) JP5763094B2 (es)
KR (1) KR101407856B1 (es)
CN (1) CN102686589B (es)
AR (1) AR079467A1 (es)
AU (1) AU2010332987B2 (es)
BR (1) BR112012014770A2 (es)
CA (1) CA2780155A1 (es)
CL (1) CL2012001596A1 (es)
CO (1) CO6531478A2 (es)
CR (1) CR20120269A (es)
EC (1) ECSP12011977A (es)
ES (1) ES2551582T3 (es)
IL (1) IL219371A (es)
MA (1) MA33802B1 (es)
MX (1) MX2012006789A (es)
MY (1) MY162998A (es)
NZ (1) NZ599553A (es)
PE (1) PE20121443A1 (es)
PH (1) PH12012500867A1 (es)
RU (1) RU2553461C2 (es)
SG (1) SG181779A1 (es)
TW (1) TWI448465B (es)
UA (1) UA107002C2 (es)
WO (1) WO2011073172A1 (es)
ZA (1) ZA201204429B (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2636668B1 (en) * 2010-11-05 2018-08-01 OAT Agrio Co., Ltd. Ethynylphenylamidine compound or salt thereof, method for producing same, and fungicide for agricultural and horticultural use
PL2702051T3 (pl) 2011-04-26 2015-08-31 Hoffmann La Roche Pochodne etynylu jako pozytywne allosteryczne modulatory mglur5
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
WO2014056710A1 (en) * 2012-09-27 2014-04-17 F. Hoffmann-La Roche Ag Arylethynyl derivatives
MY171517A (en) * 2012-10-18 2019-10-16 Hoffmann La Roche Ethynyl derivatives as modulators of mglur5 receptor activity
MX2015005375A (es) * 2012-11-07 2015-07-21 Hoffmann La Roche Compuestos de triazolo.
AU2016273751B2 (en) 2015-06-03 2020-04-02 F. Hoffmann-La Roche Ag Ethynyl derivatives
MA42442B1 (fr) 2015-07-15 2019-07-31 Hoffmann La Roche Dérivés d'éthynyle comme modulateurs du récepteur métabotropique au glutamate
CA3030788A1 (en) 2016-07-18 2018-01-25 F. Hoffmann-La Roche Ag Ethynyl derivatives

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000020001A1 (en) * 1998-10-02 2000-04-13 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
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
ES2441178T3 (es) * 2005-06-01 2014-02-03 Ucb Pharma, S.A. Derivados de 2-oxo-1-pirrolidina, procedimientos para prepararlos y el uso terapéutico de los mismos sobre el sistema nervioso central
CN102887891B (zh) 2005-11-15 2016-03-09 阿雷生物药品公司 N4-苯基-喹唑啉-4-胺衍生物和相关化合物
JP2009541480A (ja) 2006-06-30 2009-11-26 アストラゼネカ アクチボラグ 癌の治療において有用なピリミジン誘導体
EP1972628A1 (en) 2007-03-21 2008-09-24 Schwarz Pharma Ag Indolizines and aza-analog derivatives thereof as CNS active compounds
NZ580662A (en) * 2007-04-30 2012-01-12 Abbott Lab Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme used in manufacture of medicament for treatment of diabetes or lipid associated disorders
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.
TW201116532A (en) * 2009-08-05 2011-05-16 Merz Pharma Gmbh & Co Kgaa Metabotropic glutamate receptor modulators

Also Published As

Publication number Publication date
US20140073638A1 (en) 2014-03-13
CA2780155A1 (en) 2011-06-23
MA33802B1 (fr) 2012-12-03
CO6531478A2 (es) 2012-09-28
MY162998A (en) 2017-07-31
RU2553461C2 (ru) 2015-06-20
AR079467A1 (es) 2012-01-25
HK1171225A1 (en) 2013-03-22
PH12012500867A1 (en) 2014-10-14
KR101407856B1 (ko) 2014-06-16
NZ599553A (en) 2014-05-30
TW201144314A (en) 2011-12-16
KR20120095472A (ko) 2012-08-28
AU2010332987B2 (en) 2015-08-13
JP2013514305A (ja) 2013-04-25
SG181779A1 (en) 2012-07-30
EP2513102A1 (en) 2012-10-24
JP5763094B2 (ja) 2015-08-12
EP2513102B1 (en) 2015-08-19
MX2012006789A (es) 2012-07-10
US20110152257A1 (en) 2011-06-23
US8586581B2 (en) 2013-11-19
CR20120269A (es) 2012-07-04
ECSP12011977A (es) 2012-07-31
AU2010332987A1 (en) 2012-06-07
TWI448465B (zh) 2014-08-11
WO2011073172A1 (en) 2011-06-23
CL2012001596A1 (es) 2013-01-04
CN102686589B (zh) 2014-12-10
US8933094B2 (en) 2015-01-13
ES2551582T3 (es) 2015-11-20
UA107002C2 (uk) 2014-11-10
RU2012128551A (ru) 2014-01-27
IL219371A (en) 2015-02-26
BR112012014770A2 (pt) 2016-03-29
IL219371A0 (en) 2012-06-28
CN102686589A (zh) 2012-09-19
ZA201204429B (en) 2013-02-27

Similar Documents

Publication Publication Date Title
PE20121443A1 (es) Derivados de etinilo
PE20110028A1 (es) Derivados de isoxazol y su uso como potenciadores de los receptores metabotropicos de glutamato
PE20060185A1 (es) ANTAGONISTA DEL RECEPTOR A2A DE LA ADENOSINA CON ESTRUCTURA DE PIRAZOLO--[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA
PE20120031A1 (es) Compuestos aril metil benzoquinazolinona como moduladores alostericos positivos del receptor m1
PE20110834A1 (es) DERIVADOS DE PIRROL[3,4-d]PIRIMIDINA COMO INHIBIDORES DE FOSFODIESTERASA 1 (PDE1)
PE20151249A1 (es) Derivados de pirazolopirimidina como inhibidores de jak quinasas
PE20130184A1 (es) Compuesto heterociclico
PE20090816A1 (es) Derivados de pirrolopirimidinona como agentes ligandos de los receptores p2x3
PE20080948A1 (es) Derivados de imidazol como moduladores de la senda de hedgehog
PE20081845A1 (es) Nuevos derivados de aminopirimidina como inhibidores de plk1
PE20090546A1 (es) Derivados de imidazol como antagonistas de los receptores de quimioquina ccr-2, ccr-3 y ccr-5
PE20070585A1 (es) Derivados de sulfonamida como activadores de glucoquinasa
PE20080527A1 (es) Derivado de pirimidina como inhibidor de la fosfatidilinositol 3-quinasa (pi3k)
MY152805A (en) Benzazepine derivatives useful as vasopressin antagonists
PE20110894A1 (es) Derivados de pirimidin indol para el tratamiento de cancer
PE20070520A1 (es) Compuestos heterociclicos fusionados como moduladores de cinasa
TW200720266A (en) Benzodioxane and benzodioxolan derivatives and uses thereof
PE20090960A1 (es) Derivados de quinazolinadiona, su preparacion y sus aplicaciones terapeuticas
PE20110403A1 (es) Compuestos biciclicos fusionados de pirimidina en el tratamiento del cancer
PE20081887A1 (es) Nuevo compuesto de adenina
PE20141827A1 (es) Inhibidores de proteinas quinasas
PE20141203A1 (es) Benzilindazoles sustituidos para uso como inhibidores de la quinasa bub1 en el tratamiento de enfermedades hiperproliferativas
PE20081800A1 (es) NUEVOS DERIVADOS DE 3-([1,2,4]TRIAZOLO[4,3-a]PIRIDIN-7-IL)BENZAMIDA
SI1838698T1 (sl) Derivati pirimidina kot agonisti gcpr
PE20110296A1 (es) Compuestos heterociclicos fusionados como moduladores del receptor de orexina

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed