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AR041268A1 - Derivados de la 1h -1,2,4- triazol-3-carboxamida que tienen actividad agonista, agonista parcial, agonista inversa o antagonista del receptor cb 1 de cannabinoide y composiciones farmaceuticas que los contienen - Google Patents

Derivados de la 1h -1,2,4- triazol-3-carboxamida que tienen actividad agonista, agonista parcial, agonista inversa o antagonista del receptor cb 1 de cannabinoide y composiciones farmaceuticas que los contienen

Info

Publication number
AR041268A1
AR041268A1 ARP030103347A ARP030103347A AR041268A1 AR 041268 A1 AR041268 A1 AR 041268A1 AR P030103347 A ARP030103347 A AR P030103347A AR P030103347 A ARP030103347 A AR P030103347A AR 041268 A1 AR041268 A1 AR 041268A1
Authority
AR
Argentina
Prior art keywords
group
disorders
whose
substituted
agonist
Prior art date
Application number
ARP030103347A
Other languages
English (en)
Inventor
Stuivenberg Herman H Van
Wilfried Gert Roger Langenaeker
Andrew C Mccreary
Todd M Kruse
Original Assignee
Solvay Pharm Bv
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 Solvay Pharm Bv filed Critical Solvay Pharm Bv
Publication of AR041268A1 publication Critical patent/AR041268A1/es

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    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • 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
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Addiction (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los derivados de 1H-1,2,4-triazol-3-carboxamida son potentes agonistas, agonistas parciales, agonistas inversos o antagonistas del receptor CB1 de cannabinoide, útiles para el tratamiento de desórdenes que involucran neurotransmisión cannabinoide,como depresión, psicosis, dependencia de drogas, ansiedad, Parkinson, dolor, entre otros, composiciones farmacéuticas que los contienen. Reivindicación 1: Un método de tratamiento de desórdenes que involucran neurotransmisión cannabinoide CB1 talescomo psicosis, ansiedad, depresión, deficiencias de atención, desórdenes de memoria, desórdenes cognitivos, desórdenes de apetito, obesidad, adicción, apetencia, dependencia de drogas, desórdenes neurodegenerativos, demencia, distonía, espasticidadmuscular, temblor, epilepsia, esclerosis múltiple, dano cerebral traumático, ataque cerebral, enfermedad de Parkinson, enfermedad de Alzheimer, epilepsia, enfermedad de Huntington, síndrome de Tourette, isquemia cerebral, apoplejía cerebral, traumacraneocerebral, ataque cerebral, dano a la médula espinal, desórdenes neuroinflamatorios, esclerosis de placas, encefalitis viral, desórdenes relacionados con desmielinización, así como para el tratamiento de desórdenes de dolor, incluyendodesórdenes de dolor neuropático, choque séptico, glaucoma, diabetes, cáncer, emesis, náusea, desórdenes gastrointestinales, úlceras gástricas, diarrea y desórdenes cardiovasculares, caracterizado porque para la preparación de una composiciónfarmacéutica para el tratamiento de dichos desórdenes se utiliza un compuesto de fórmula (1) en donde R y R1 independientemente representan un grupo fenilo, naftilo, tienilo, piridilo, pirimidilo, pirazinilo, piridazinilo o triazinilo, cuyos grupospueden estar sustituidos con 1-4 sustituyentes X, los cuales pueden ser iguales o diferentes, del grupo (C1-3)alquilo o alcoxi, ramificados o no ramificados, hidroxi, halógeno, trifluorometilo, trifluorometiltio, trifluorometoxi, nitro, amino, mono-o dialquil (C1-2)-amino, mono- o dialquil (C1-2)-amido, (C1-3)-alcoxicarbonilo, trifluorometilsulfonilo, sulfamoilo, (C1-3)-alquilsulfonilo, carboxilo, ciano, carbamoilo, (C1-3)-dialquilaminosulfonilo, (C1-3)-monoalquilaminosulfonilo y acetilo; R2representa un átomo de H o un grupo C1-8 alquilo, o C1-8 cicloalquil-alquilo ramificados o no ramificados o un grupo fenilo, bencilo o fenetilo cuyos anillos aromáticos pueden estar sustituidos con 1-4 sustituyentes X, en donde X tiene lossignificados como se indicaron anteriormente, o R2 representa un grupo piridilo o tienilo; R3 representa C1-8 alquilo, C1-8 alcoxi, C3-8cicloalquilo, C5-10 bicicloalquilo, C6-10 tricicloalquilo, C3-8 alquenilo, C5-8 cicloalquenilo, ramificados o noramificados, cuyos grupos pueden opcionalmente contener uno o más heteroátomos del grupo (O; N; S), cuyos grupos pueden estar sustituidos con un grupo hidroxi, un grupo etinilo o 1-3 átomos de F; o R3 representa un grupo fenilo, bencilo o fenetilocuyos anillos aromáticos pueden estar sustituidos con 1-4 sustituyentes X, en donde X tiene el significado indicado anteriormente, o R3 representa un grupo piridilo, pirazinilo, piridazinilo, triazinilo o tienilo cuyos anillos heteroaromáticospueden estar sustituidos con 1-2 sustituyentes X, en donde X tiene el significado indicado anteriormente, o R3 representa un grupo NR4R5 en donde R4 y R5, junto con el átomo de N al cual están unidos, forman un grupo molecular heterocíclicomonocíclico o bicíclico, saturado o no saturado, que tiene 4 a 10 átomos de anillo, cuyo grupo heterocíclico contiene uno o dos heteroátomos del grupo N, O, o S, cuyos heteroátomos pueden ser iguales o diferentes, cuyo grupo molecular heterocíclicopuede estar sustituido con un grupo C1-3 alquilo ramificado o no ramificado, hidroxi o trifluorometilo o un átomo de F, o R2 y R3 junto con el átomo de N al cual están unidos, forman un grupo molecular heterocíclico monocíclico o bicíclico, saturadoo no saturado, que tiene 4 a 10 átomos de anillo, cuyo grupo heterocíclico contiene uno o dos heteroátomos del grupo N, O o S, cuyos heteroátomos pueden ser iguales o diferentes, cuyo grupo molecular heterocíclico pueden estar sustituido con ungrupo C1-3 alquilo ramificado o no ramificado, hidroxi, piperidinilo o trifluorometilo o un átomo de F, y prodrogas, estereoisómeros y sales de los mismos.
ARP030103347A 2002-09-19 2003-09-16 Derivados de la 1h -1,2,4- triazol-3-carboxamida que tienen actividad agonista, agonista parcial, agonista inversa o antagonista del receptor cb 1 de cannabinoide y composiciones farmaceuticas que los contienen AR041268A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP02078966 2002-09-19

Publications (1)

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AR041268A1 true AR041268A1 (es) 2005-05-11

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ARP030103347A AR041268A1 (es) 2002-09-19 2003-09-16 Derivados de la 1h -1,2,4- triazol-3-carboxamida que tienen actividad agonista, agonista parcial, agonista inversa o antagonista del receptor cb 1 de cannabinoide y composiciones farmaceuticas que los contienen

Country Status (25)

Country Link
US (1) US7319110B2 (es)
EP (1) EP1542678B1 (es)
JP (1) JP2006501275A (es)
KR (1) KR100996828B1 (es)
CN (1) CN1319529C (es)
AR (1) AR041268A1 (es)
AT (1) ATE458479T1 (es)
AU (1) AU2003299024B2 (es)
BR (1) BR0312020A (es)
CA (1) CA2491394C (es)
DE (1) DE60331444D1 (es)
DK (1) DK1542678T3 (es)
ES (1) ES2341540T3 (es)
HK (1) HK1078796A1 (es)
HR (1) HRP20050053A2 (es)
IL (1) IL165611A (es)
MX (1) MXPA05002862A (es)
NO (1) NO20051870L (es)
PL (1) PL375020A1 (es)
PT (1) PT1542678E (es)
RU (1) RU2325382C2 (es)
SI (1) SI1542678T1 (es)
UA (1) UA80298C2 (es)
WO (1) WO2004026301A1 (es)
ZA (1) ZA200500133B (es)

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