AR045533A1 - USE OF AN ANTAGONIST CB1 RECEIVER COMPOUND, PHARMACEUTICAL COMPOSITION AND TREATMENT METHOD AND / OR PROPHYLAXIS OF DISEASES RELATED TO SUCH CB1 RECEIVER - Google Patents

USE OF AN ANTAGONIST CB1 RECEIVER COMPOUND, PHARMACEUTICAL COMPOSITION AND TREATMENT METHOD AND / OR PROPHYLAXIS OF DISEASES RELATED TO SUCH CB1 RECEIVER

Info

Publication number
AR045533A1
AR045533A1 ARP040103109A ARP040103109A AR045533A1 AR 045533 A1 AR045533 A1 AR 045533A1 AR P040103109 A ARP040103109 A AR P040103109A AR P040103109 A ARP040103109 A AR P040103109A AR 045533 A1 AR045533 A1 AR 045533A1
Authority
AR
Argentina
Prior art keywords
alkyl
prophylaxis
receiver
pyridyl
unbranched
Prior art date
Application number
ARP040103109A
Other languages
Spanish (es)
Inventor
Jochen Antel
Heinz Guenter Krause
Josephus H M Lange
Cornelis G Kruse
Peter-Colin Gregory
Besten Cathaline Den
Original Assignee
Solvay Pharm Gmbh
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 Gmbh filed Critical Solvay Pharm Gmbh
Publication of AR045533A1 publication Critical patent/AR045533A1/en

Links

Classifications

    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/4164—1,3-Diazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • 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
    • A61P25/22—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P9/10—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

Landscapes

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

Abstract

Reivindicación 1: Uso de un compuesto antagonista de receptor de CB1 de la fórmula (1), sus profármacos, tautómeros y sus sales, en la manufactura de medicamentos para el tratamiento y/o profiláxis de enfermedades relacionadas con receptores de CB1 en pacientes juveniles y/o para el tratamiento y/o profiláxis de obesidad inducida por fármacos en pacientes juveniles y adolescentes, en donde R y R1 pueden ser iguales o distintos entre sí y representan fenilo, tienilo o piridilo y pueden tener 1, 2 o 3 sustituyentes y, que pueden ser iguales o distintos entre sí, elegidos del grupo que comprende alquilo C1-3 o alcoxi, hidroxi, halógeno, trifluorometilo, trifluorometiltio, trifluorometoxi, nitro, amino, mono- o dialquil C1-2-amino, mono- o dialquil C1-2-amido, alquil C1-3-sulfonilo, dimetilsulfamido, alcoxicarbonilo C1-5, carboxilo, trifluorometilsulfonilo, ciano, carbamoilo, sulfamoilo y acetilo, o R y/o R1 representan naftilo; R2 representa H, hidroxi, alcoxi C1-3, acetiloxi, o propioniloxi; Aa representa uno e los grupos (i), (ii), (iii), (iv) o (v), en donde R4 y R5 representan independientemente entre sí H o radicales alquilo C1-8 ramificados o no ramificados o cicloalquilo C3-8 o R4 representa acetamido o dimetilamino o 2,2,2-trifluoroetilo o fenilo o piridilo, siempre que R5 represente H; R6 representa H o alquilo C1-3 no ramificado; Bb representa sulfonilo o carbonilo R3 representa bencilo, fenilo, tienilo o piridilo que pueden tener 1, 2 o 3 sustituyentes Y, que pueden ser iguales o distintos entre sí o R3 representa un radical alquilo C1-8 ramificado o no ramificado o cicloalquilo C3-8, o R3 representa naftilo.Claim 1: Use of a CB1 receptor antagonist compound of the formula (1), its prodrugs, tautomers and salts thereof, in the manufacture of medicaments for the treatment and / or prophylaxis of diseases related to CB1 receptors in juvenile patients and / or for the treatment and / or prophylaxis of drug-induced obesity in juvenile and adolescent patients, where R and R1 may be the same or different from each other and represent phenyl, thienyl or pyridyl and may have 1, 2 or 3 substituents and, which may be the same or different from each other, chosen from the group comprising C1-3 alkyl or alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, nitro, amino, mono- or dialkyl C1-2-amino, mono- or dialkyl C1 -2-amido, C1-3 alkyl sulfonyl, dimethylsulfamido, C1-5 alkoxycarbonyl, carboxyl, trifluoromethylsulfonyl, cyano, carbamoyl, sulfamoyl and acetyl, or R and / or R1 represent naphthyl; R2 represents H, hydroxy, C1-3 alkoxy, acetyloxy, or propionyloxy; Aa represents one of the groups (i), (ii), (iii), (iv) or (v), where R4 and R5 independently represent each other H or branched or unbranched C1-8 alkyl radicals or C3- cycloalkyl 8 or R4 represents acetamido or dimethylamino or 2,2,2-trifluoroethyl or phenyl or pyridyl, provided that R5 represents H; R6 represents H or C1-3 unbranched alkyl; Bb represents sulfonyl or carbonyl R3 represents benzyl, phenyl, thienyl or pyridyl which may have 1, 2 or 3 substituents Y, which may be the same or different from each other or R3 represents a branched or unbranched C1-8 alkyl radical or C3- cycloalkyl 8, or R3 represents naphthyl.

ARP040103109A 2003-09-02 2004-08-30 USE OF AN ANTAGONIST CB1 RECEIVER COMPOUND, PHARMACEUTICAL COMPOSITION AND TREATMENT METHOD AND / OR PROPHYLAXIS OF DISEASES RELATED TO SUCH CB1 RECEIVER AR045533A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP03019939 2003-09-02

Publications (1)

Publication Number Publication Date
AR045533A1 true AR045533A1 (en) 2005-11-02

Family

ID=34259159

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040103109A AR045533A1 (en) 2003-09-02 2004-08-30 USE OF AN ANTAGONIST CB1 RECEIVER COMPOUND, PHARMACEUTICAL COMPOSITION AND TREATMENT METHOD AND / OR PROPHYLAXIS OF DISEASES RELATED TO SUCH CB1 RECEIVER

Country Status (11)

Country Link
EP (1) EP1663205A1 (en)
JP (1) JP2007504200A (en)
CN (2) CN1845735A (en)
AR (1) AR045533A1 (en)
AU (1) AU2004268388A1 (en)
BR (1) BRPI0413980A (en)
CA (1) CA2537090A1 (en)
MX (1) MXPA06002365A (en)
RU (1) RU2006110543A (en)
TW (1) TW200511990A (en)
WO (1) WO2005020988A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1575901B1 (en) 2002-12-19 2012-10-10 Merck Sharp & Dohme Corp. Substituted amides
JP5254620B2 (en) 2004-12-03 2013-08-07 メルク・シャープ・アンド・ドーム・コーポレーション Substituted piperazines as CB1 antagonists
WO2009140210A2 (en) * 2008-05-12 2009-11-19 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Radiotracers for imaging cannabinoid sub-type1 (cb1) receptor
WO2010079241A1 (en) 2009-01-12 2010-07-15 Fundacion Hospital Nacional De Paraplejicos Para La Investigacion Y La Integracion Use of antagonists and/or inverse agonists of cb1 receptors for the preparation of drugs that increase motor neuron excitability

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004500401A (en) * 2000-03-23 2004-01-08 ソルベイ・フアーマシユーチカルズ・ベー・ブイ 4,5-Dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
BR0205602A (en) * 2001-03-22 2003-07-08 Solvay Pharm Bv Enantiomer having the 4-position configuration of its pyrazole ring of a compound, pharmaceutical composition, method for preparing pharmaceutical compositions, process for preparing compounds, and methods for treating disorders involving cannabinoid neurotransmission
UA78523C2 (en) * 2001-09-21 2007-04-10 Solvay Pharm Bv 4,5-dihydro-1h-pyrazoie derivatives as cb1 antagonists

Also Published As

Publication number Publication date
EP1663205A1 (en) 2006-06-07
CN1835747A (en) 2006-09-20
JP2007504200A (en) 2007-03-01
CA2537090A1 (en) 2005-03-10
TW200511990A (en) 2005-04-01
AU2004268388A1 (en) 2005-03-10
RU2006110543A (en) 2007-10-10
BRPI0413980A (en) 2006-11-07
MXPA06002365A (en) 2006-06-20
WO2005020988A1 (en) 2005-03-10
CN1845735A (en) 2006-10-11

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