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

Piperazinas acetilenicas como antagonistas de receptores de glutamato metabotropicos

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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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    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/16—Central respiratory analeptics
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
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    • A61P25/36—Opioid-abuse
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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

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  • Health & Medical Sciences (AREA)
  • 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)
  • Otolaryngology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Nutrition Science (AREA)
  • Immunology (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

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AR055113A1 true AR055113A1 (es) 2007-08-08

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Country Status (16)

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US (2) US20070037817A1 (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
JP2010502664A (ja) 2006-09-11 2010-01-28 ノバルティス アクチエンゲゼルシャフト 代謝型グルタミン酸受容体の調節剤としてのニコチン酸誘導体
WO2009047303A2 (en) * 2007-10-12 2009-04-16 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of pervasive developmental disorder
BRPI0818560A2 (pt) * 2007-10-12 2019-09-24 Novartis Ag compostos orgânicos
WO2010000763A2 (en) 2008-06-30 2010-01-07 Novartis Ag Combination products
PE20130213A1 (es) 2010-04-30 2013-03-19 Novartis Ag Marcadores predictivos utiles en el tratamiento del sindrome fragil x (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
WO1997023482A1 (en) * 1995-12-21 1997-07-03 Pfizer Inc. 2,7-substituted octahydro-pyrrolo[1,2-a]pyrazine derivatives
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

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

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