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AR055113A1 - Piperazinas acetilenicas como antagonistas de receptores de glutamato metabotropicos - Google Patents

Piperazinas acetilenicas como antagonistas de receptores de glutamato metabotropicos

Info

Publication number
AR055113A1
AR055113A1 ARP060103440A ARP060103440A AR055113A1 AR 055113 A1 AR055113 A1 AR 055113A1 AR P060103440 A ARP060103440 A AR P060103440A AR P060103440 A ARP060103440 A AR P060103440A AR 055113 A1 AR055113 A1 AR 055113A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
alkylhalo
co2r2
so2r2
Prior art date
Application number
ARP060103440A
Other languages
English (en)
Inventor
Louise Edwards
Methvin Isaac
Abdelmalik Slassi
Guang-Ri Sun
Peter Dove
Erwan Arzel
Original Assignee
Astrazeneca Ab
Nps Pharma Inc
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 Astrazeneca Ab, Nps Pharma Inc filed Critical Astrazeneca Ab
Publication of AR055113A1 publication Critical patent/AR055113A1/es

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    • CCHEMISTRY; METALLURGY
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P1/06Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/04Drugs for disorders of the respiratory system for throat disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • 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
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Nutrition Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

También se incluyen composiciones farmacéuticas y usos y procesos para elaborar compuestos, así como métodos para el tratamiento médico de trastornos mediados por mGluR 5. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) en donde: Ar1 es un grupo arilo o heteroarilo opcionalmente sustituido, en donde los sustituyentes se seleccionan del grupo formado por F, Cl, Br, I, OH, nitro, C1-6 alquilo, C1-6 alquilhalo, OC1-6 alquilo, OC1-6 alquilhalo, C2-6 alquenilo, C2-6 alquinilo, -CN, CO2R2, SR2, S(O)R2, SO2R2, arilo, heteroarilo, cicloalquilo y heterocicloalquilo, en donde cualquier grupo cíclico puede ser adicionalmente sustituido con al menos un sustituyente seleccionado del grupo formado por F, Cl, Br, I, OH, nitro, C1-6 alquilo, C1-6 alquilhalo, OC1-6 alquilo, OC1-6 alquilhalo, C2-6 alquenilo, C2-6 alquinilo, -CN, CO2R2, SR2, S(O)R2 y SO2R2; A se selecciona del grupo formado por Ar1, CO2R2, CONR2R3, S(O)R2 y SO2R2; B se selecciona del grupo formado por vinileno y etinileno, en donde el grupo vinileno está opcionalmente sustituido con hasta 2 grupos C1-6 alquilo seleccionados en forma independiente; R1, en cada caso, se selecciona en forma independiente del grupo formado por F, Cl, Br, I, OH, CN, nitro, C1-6 alquilo, C1-6, OC1-6 alquilo, C1-6 alquilhalo, OC1-6 alquilhalo, (CO)R2, O(CO)R2, O(CO)OR2, CO2R2, -CONR2R3, C1-6 alquilenoOR2, OC2-6 alquilenoOR2 y C1-6 alquilenociano; R2 y R3 se seleccionan en forma independiente del grupo formado por H, C1-6 alquilo, C1-6 alquilhalo, C2-6 alquenilo, C2-6 alquinilo y cicloalquilo; m es un entero seleccionado del grupo formado por 0, 1, 2, 3 y 4; y n es un entero seleccionado del grupo formado por 1, 2 y 3; o una sal aceptable para uso farmacéutico, hidrato, solvato, isoforma, tautomero, somero optico, o combinacion de los mismos.
ARP060103440A 2005-08-15 2006-08-08 Piperazinas acetilenicas como antagonistas de receptores de glutamato metabotropicos AR055113A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US70794405P 2005-08-15 2005-08-15

Publications (1)

Publication Number Publication Date
AR055113A1 true AR055113A1 (es) 2007-08-08

Family

ID=37670907

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060103440A AR055113A1 (es) 2005-08-15 2006-08-08 Piperazinas acetilenicas como antagonistas de receptores de glutamato metabotropicos

Country Status (16)

Country Link
US (2) US20080194571A1 (es)
EP (1) EP1919915A2 (es)
JP (1) JP2009504736A (es)
KR (1) KR20080050569A (es)
CN (1) CN101248076A (es)
AR (1) AR055113A1 (es)
AU (1) AU2006280233A1 (es)
BR (1) BRPI0614481A2 (es)
CA (1) CA2616318A1 (es)
IL (1) IL188807A0 (es)
MX (1) MX2008001608A (es)
NO (1) NO20080669L (es)
TW (1) TW200801005A (es)
UY (1) UY29733A1 (es)
WO (1) WO2007021575A2 (es)
ZA (1) ZA200801033B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20090061041A (ko) 2006-09-11 2009-06-15 노파르티스 아게 대사성 글루타메이트 수용체의 조절제로서의 니코틴산 유도체
BRPI0818560A2 (pt) * 2007-10-12 2019-09-24 Novartis Ag compostos orgânicos
WO2009047303A2 (en) * 2007-10-12 2009-04-16 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of pervasive developmental disorder
EP2826478A1 (en) 2008-06-30 2015-01-21 Novartis AG Combinations comprising mglur modulators for the treatment of parkinson's disease
BR112012027816A2 (pt) 2010-04-30 2017-08-08 Novartis Ag marcadores preditivos úteis no tratamento da síndrome do x frágil (fxs).
WO2013131981A1 (en) 2012-03-08 2013-09-12 Novartis Ag Predictive markers useful in the diagnosis and treatment of fragile x syndrome (fxs)
CA3088288A1 (en) * 2018-01-26 2019-08-01 Recordati Industria Chimica E Farmaceutica S.P.A Triazole, imidazole and pyrrole condensed piperazine derivatives and their use as modulators of mglu5 receptors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6231833B1 (en) * 1999-08-05 2001-05-15 Pfizer Inc 2,7-substituted octahydro-1H-pyrido[1,2-A]pyrazine derivatives as ligands for serotonin receptors
CZ192998A3 (cs) * 1995-12-21 1999-05-12 Pfizer Inc. 2,7-Substituované oktahydropyrrolo[1,2-a]pyrazinové deriváty, meziprodukty pro jejich výrobu a farmaceutické prostředky na jejich bázi
EP0982030A3 (en) * 1998-08-17 2000-05-10 Pfizer Products Inc. 2,7-substituted octahydro-pyrrolo 1,2-a]pyrazine derivatives as 5ht 1a ligands
WO2001032660A1 (en) * 1999-11-05 2001-05-10 Nps Allelix Corp. Compounds having 5-ht6 receptor antagonist activity
AU2003229535A1 (en) * 2002-06-06 2003-12-22 Novo Nordisk A/S Substituted hexahydropyrrolo(1,2-a)pyrazines, octahydropyrido(1,2-a)pyrazines and decahydropyrazino(1,2-a)azepines

Also Published As

Publication number Publication date
US20070037817A1 (en) 2007-02-15
UY29733A1 (es) 2007-02-28
US20080194571A1 (en) 2008-08-14
NO20080669L (no) 2008-05-15
BRPI0614481A2 (pt) 2017-06-06
CA2616318A1 (en) 2007-02-22
KR20080050569A (ko) 2008-06-09
EP1919915A2 (en) 2008-05-14
WO2007021575A3 (en) 2007-04-05
WO2007021575A2 (en) 2007-02-22
TW200801005A (en) 2008-01-01
ZA200801033B (en) 2009-01-28
MX2008001608A (es) 2008-04-14
JP2009504736A (ja) 2009-02-05
AU2006280233A1 (en) 2007-02-22
IL188807A0 (en) 2008-08-07
CN101248076A (zh) 2008-08-20

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