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AR032653A1 - Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos. - Google Patents

Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos.

Info

Publication number
AR032653A1
AR032653A1 ARP020100370A ARP020100370A AR032653A1 AR 032653 A1 AR032653 A1 AR 032653A1 AR P020100370 A ARP020100370 A AR P020100370A AR P020100370 A ARP020100370 A AR P020100370A AR 032653 A1 AR032653 A1 AR 032653A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
compounds
aryl
transporter
heteroaryl
Prior art date
Application number
ARP020100370A
Other languages
English (en)
Original Assignee
Telik 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 Telik Inc filed Critical Telik Inc
Publication of AR032653A1 publication Critical patent/AR032653A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/1131,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245Oxadiazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433Thidiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • A61P25/28Drugs 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Provee compuestos, composiciones y métodos para inhibir al transportador de glicina 2 y para afectar la actividad neuronal mediada por el transportador de glicina. Los compuestos utiles comprenden a los compuestos de la formula (1) donde: n es 0, 1, 2 o 3 y R es independientemente, halogeno, hidroxi, alquilo inferior opcionalmente sustituido con halogeno o alcoxi menor opcionalmente sustituido con halogeno; X es O, S o N-R' (donde R' es alquilo inferior, arilo, heteroarilo, arilo-menor alquileno o heteroarilo-menor alquileno); Q puede estar ausente o presente, y cuando está presente, está representado por la formula (2) donde n, R y X son como definimos anteriormente; donde Q está presente, W es un alquileno menor y cuando Q está ausente, W está opcionalmente sustituido con alquilo inferior, opcionalmente sustituido con arilo opcionalmente sustituido con heteroarilo (opcionalmente arilo sustituido)-X-CH2- donde X es como definimos anteriormente; o su sal farmacéuticamente aceptable. Estos compuestos son particularmente utiles para tratar enfermedades nerviosas y musculares, incluyendo a la psicosis, dolor, epilepsia, enfermedades neurodegenerativas, apoplejía, trauma encefálico, esclerosis multiple y similares, y trastornos musculares, incluyendo a las enfermedades o condiciones asociadas con la contraccion aumentada del musculo, como por ejemplo, la espasticidad y mioclonus. Además, se pueden utilizar los compuestos para descubrir otros agentes con una actividad mejorada en los ensayos donde son activos los compuestos de la invencion.
ARP020100370A 2001-02-09 2002-02-04 Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos. AR032653A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26789401P 2001-02-09 2001-02-09

Publications (1)

Publication Number Publication Date
AR032653A1 true AR032653A1 (es) 2003-11-19

Family

ID=23020582

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020100370A AR032653A1 (es) 2001-02-09 2002-02-04 Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos.

Country Status (7)

Country Link
US (1) US6894054B2 (es)
EP (1) EP1357913A1 (es)
JP (1) JP2004522761A (es)
AR (1) AR032653A1 (es)
AU (1) AU2002247098B2 (es)
CA (1) CA2436079A1 (es)
WO (1) WO2002064135A1 (es)

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FR2842804B1 (fr) * 2002-07-29 2004-09-03 Sanofi Synthelabo Derives de n-[phenyl(piperidin-2-yl)methyl]benzamide, leur preparation et leur application en therapeutique
BRPI0409739A (pt) * 2003-04-30 2006-05-09 Lundbeck & Co As H composto, composição farmacêutica, uso de composto, e, método para o tratamento de uma doença ou de um distúrbio
WO2005044810A1 (en) * 2003-10-30 2005-05-19 Janssen Pharmaceutica, N.V. Glyt2 modulators
US7563905B2 (en) * 2004-03-12 2009-07-21 Wyeth Triazole derivatives and method of using the same to treat HIV infections
US7354944B2 (en) * 2004-10-18 2008-04-08 Amgen Inc. Thiadiazole compounds and methods of use
RU2396270C2 (ru) * 2005-01-07 2010-08-10 Ф.Хоффманн-Ля Рош Аг Производные [4-(гетероарил)пиперазин-1-ил]-(2,5-замещенный фенил)метанона в качестве ингибиторов переносчика глицина-1 (glyt-1) для лечения неврологических и психоневрологических заболеваний
EA200801716A1 (ru) * 2006-01-18 2009-04-28 Амген Инк. Тиазольные соединения и их применение
AU2007310897A1 (en) * 2006-10-25 2008-05-02 Neurosearch A/S Oxadiazole and thiadiazole compounds and their use as nicotinic acetylcholine receptor modulators
CA2693473A1 (en) * 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
AU2008276521B2 (en) 2007-07-17 2011-11-03 Amgen Inc. Heterocyclic modulators of PKB
US9345703B2 (en) 2011-09-15 2016-05-24 University Of Kansas Kappa opioid receptor effectors and uses thereof
CN103373993B (zh) * 2012-04-12 2016-03-02 南京大学 一类含吡嗪环的噻二唑衍生物及其制法与用途
CZ305680B6 (cs) * 2013-04-04 2016-02-03 Univerzita Karlova v Praze, Farmaceutická fakulta v Hradci Králové Substituovaný diazol, jeho použití a farmaceutický přípravek ho obsahující
EP3210469A1 (de) 2016-02-23 2017-08-30 Bayer Cropscience AG Verwendung von substituierten thio-1,2,4-triazolen zur steigerung der stresstoleranz in pflanzen

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Also Published As

Publication number Publication date
US6894054B2 (en) 2005-05-17
WO2002064135A1 (en) 2002-08-22
AU2002247098B2 (en) 2006-06-22
JP2004522761A (ja) 2004-07-29
EP1357913A1 (en) 2003-11-05
US20030073726A1 (en) 2003-04-17
CA2436079A1 (en) 2002-08-22

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