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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

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/113—1,3,4-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
    • 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
    • A61K31/41—Heterocyclic 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/28—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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)

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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CA2523585A1 (en) * 2003-04-30 2004-11-11 H. Lundbeck A/S Aromatic oxyphenyl and aromatic sulfanylphenyl derivatives
US7202269B2 (en) 2003-10-30 2007-04-10 Janssen Pharmaceutica N.V. GlyT2 modulators
WO2005090320A2 (en) * 2004-03-12 2005-09-29 Wyeth Triazole derivatives and method of using the same to treat hiv infections
CA2583217C (en) * 2004-10-18 2011-05-31 Amgen Inc. 1,3,4-thiadiazole compounds as protein kinase inhibitors
KR100895752B1 (ko) * 2005-01-07 2009-04-30 에프. 호프만-라 로슈 아게 신경 질환 및 신경정신 질환을 치료하기 위한 글라이신수송자 1(ｇｌｙｔ-1) 저해제로서의[4-(헤테로아릴)피페라진-1-일]-(2,5-치환-페닐)메탄온유도체
US7514566B2 (en) * 2006-01-18 2009-04-07 Amgen, Inc. Thiazole compounds and methods of use
CA2667545A1 (en) * 2006-10-25 2008-05-02 Neurosearch A/S Oxadiazole and thiadiazole compounds and their use as nicotinic acetylcholine receptor modulators
WO2009011880A2 (en) 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
WO2009011871A2 (en) * 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
EP2757881A4 (en) * 2011-09-15 2014-11-12 Univ 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
WO2002064135A1 (en) 2002-08-22
CA2436079A1 (en) 2002-08-22
EP1357913A1 (en) 2003-11-05
JP2004522761A (ja) 2004-07-29
AU2002247098B2 (en) 2006-06-22
US6894054B2 (en) 2005-05-17
US20030073726A1 (en) 2003-04-17

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