WO2000007542A3 - Empleo de derivados de aril(o heteroaril)azolilcarbinoles en la elaboracion de un medicamento para el tratamiento de los trastornos mediados por un exceso de substancia p - Google Patents

Empleo de derivados de aril(o heteroaril)azolilcarbinoles en la elaboracion de un medicamento para el tratamiento de los trastornos mediados por un exceso de substancia p Download PDF

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Publication number
WO2000007542A3
WO2000007542A3 PCT/ES1999/000255 ES9900255W WO0007542A3 WO 2000007542 A3 WO2000007542 A3 WO 2000007542A3 ES 9900255 W ES9900255 W ES 9900255W WO 0007542 A3 WO0007542 A3 WO 0007542A3
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WO
WIPO (PCT)
Prior art keywords
troubles
group
heteroaryl
mediated
aryl
Prior art date
Application number
PCT/ES1999/000255
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English (en)
French (fr)
Other versions
WO2000007542A2 (es
Inventor
Ramon Merce-Vidal
Jordi Frigola-Constansa
Original Assignee
Esteve Labor Dr
Merce Vidal Ramon
Frigola Constansa Jordi
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
Priority to EP99940199A priority Critical patent/EP1103243B1/en
Priority to JP2000563228A priority patent/JP2002522359A/ja
Application filed by Esteve Labor Dr, Merce Vidal Ramon, Frigola Constansa Jordi filed Critical Esteve Labor Dr
Priority to AU54229/99A priority patent/AU754124B2/en
Priority to DE69914085T priority patent/DE69914085T8/de
Priority to BR9912807-1A priority patent/BR9912807A/pt
Priority to NZ509645A priority patent/NZ509645A/xx
Priority to ES99940199T priority patent/ES2213380T3/es
Priority to CA002339661A priority patent/CA2339661C/en
Priority to AT99940199T priority patent/ATE257379T1/de
Priority to DK99940199T priority patent/DK1103243T3/da
Priority to US09/762,079 priority patent/US6518295B1/en
Priority to PL99346221A priority patent/PL193802B1/pl
Publication of WO2000007542A2 publication Critical patent/WO2000007542A2/es
Publication of WO2000007542A3 publication Critical patent/WO2000007542A3/es
Priority to NO20010634A priority patent/NO20010634L/no
Priority to IL14129501A priority patent/IL141295A0/xx

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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
    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P25/14—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
    • A61P25/18—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Los derivados de aril(o heteroaril)azolilcarbinol (I) donde Ar es fenilo o tienilo opcionalmente sustituidos, R1-C4, R2, es H, dialquilaminoalquilo, alquilazaheterociclilalquilo o azaheterociclilalquilo, y Het es un heterociclo aromático nitrogenado de 5 miembros que contiene de 1 a 3 átomos de nitrógeno, opcionalmente sustituido, son útiles para el tratamiento de los trastornos que vienen mediados por un exceso de substancia P, especialmente, ciertos trastornos de sistema nervioso central tales como ansiedad, depresión, esquizofrenia, psicosis maníaco depresiva, disfunción sexual, drogodependencias, trastornos cognitivos, trastornos locomotores, etc., en mamíferos, incluidos el hombre.
PCT/ES1999/000255 1998-08-07 1999-08-05 Empleo de derivados de aril(o heteroaril)azolilcarbinoles en la elaboracion de un medicamento para el tratamiento de los trastornos mediados por un exceso de substancia p WO2000007542A2 (es)

Priority Applications (14)

Application Number Priority Date Filing Date Title
AT99940199T ATE257379T1 (de) 1998-08-07 1999-08-05 Verwendung von aryl- (oder heteroaryl-) azoylcarbinolderivaten zur behandlung von durch überschuss von substanz p hervorgerufenen beschwerden
CA002339661A CA2339661C (en) 1998-08-07 1999-08-05 Use of derivatives of aryl(or heteroaryl)azolylcarbinols in the manufacture of a medicament for the treatment of disorders mediated by an excess of substance p
AU54229/99A AU754124B2 (en) 1998-08-07 1999-08-05 Utilization of aryl(or heteroaryl)azolylcarbinol derivatives in the preparation of a medicament for the treatment of troubles mediated by an excess of substance P
JP2000563228A JP2002522359A (ja) 1998-08-07 1999-08-05 過剰のサブスタンスｐによって仲介される障害の処置用医薬の製造におけるアリール（またはヘテロアリール）アゾリルカルビノール誘導体の使用
BR9912807-1A BR9912807A (pt) 1998-08-07 1999-08-05 Uso de derivados de arila (ou heteroarila) azolilcarbinol na fabricação de medicamento para tratamento de distúrbios mediados por excesso de substância p
NZ509645A NZ509645A (en) 1998-08-07 1999-08-05 Utilization of phenyl or thienyl subtituted imidazole or pyrazole carbinol derivatives for treating conditions mediated by an excess of substance P
DK99940199T DK1103243T3 (da) 1998-08-07 1999-08-05 Anvendelse af aryl(eller heteroaryl)azolylcarbinol-derivater til behandling af lidelser medieret af et overskud af substans P
EP99940199A EP1103243B1 (en) 1998-08-07 1999-08-05 Utilization of aryl(or heteroaryl)azolylcarbinol derivatives for the treatment of troubles mediated by an excess of substance p
DE69914085T DE69914085T8 (de) 1998-08-07 1999-08-05 Verwendung von aryl- (oder heteroaryl-) azoylcarbinolderivaten zur behandlung von durch überschuss von substanz p hervorgerufenen beschwerden
ES99940199T ES2213380T3 (es) 1998-08-07 1999-08-05 Uso de derivados de aril(o heteroaril)azolilcarbinoles para el tratamiento de los trastornos mediados por un exceso de substancia p.
US09/762,079 US6518295B1 (en) 1998-08-07 1999-08-05 Utilization of aryl(or heteroaryl)azolylcarbinol derivatives in the preparation of a medicament for the treatment of troubles mediated by an excess of substance P
PL99346221A PL193802B1 (pl) 1998-08-07 1999-08-05 Zastosowanie pochodnych arylo (lub heteroarylo) azolilokarbinoli do wytwarzania leku do leczenia zaburzeń wywoływanych nadmiarem substancji P
NO20010634A NO20010634L (no) 1998-08-07 2001-02-06 Anvendelse av derivater av aryl (eller heteroaryl)azolylkarbinol ved fremstilling av et medikament for behandling av forstyrrelser formidlet av et overskudd av substans P
IL14129501A IL141295A0 (en) 1998-08-07 2001-02-07 Use of derivatives of aryl (or heteroaryl) azolycarbinols in the manufacture of a medicament for the treatment of disorders mediated by an excess of substance p

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ESP9801708 1998-08-07
ES009801708A ES2150378B1 (es) 1998-08-07 1998-08-07 Empleo de derivados de aril(o heteroaril)azolilcarbinoles en la elaboracion de un medicamento para el tratamiento de los trastornos mediados por un exceso de substancia p.

Publications (2)

Publication Number Publication Date
WO2000007542A2 WO2000007542A2 (es) 2000-02-17
WO2000007542A3 true WO2000007542A3 (es) 2000-05-11

Family

ID=8304839

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/ES1999/000255 WO2000007542A2 (es) 1998-08-07 1999-08-05 Empleo de derivados de aril(o heteroaril)azolilcarbinoles en la elaboracion de un medicamento para el tratamiento de los trastornos mediados por un exceso de substancia p

Country Status (26)

Country Link
US (1) US6518295B1 (es)
EP (1) EP1103243B1 (es)
JP (1) JP2002522359A (es)
KR (1) KR100558506B1 (es)
CN (1) CN1151789C (es)
AR (1) AR019999A1 (es)
AT (1) ATE257379T1 (es)
AU (1) AU754124B2 (es)
BR (1) BR9912807A (es)
CA (1) CA2339661C (es)
CO (1) CO5080747A1 (es)
CZ (1) CZ292065B6 (es)
DE (1) DE69914085T8 (es)
DK (1) DK1103243T3 (es)
ES (2) ES2150378B1 (es)
HU (1) HUP0105428A3 (es)
IL (1) IL141295A0 (es)
NO (1) NO20010634L (es)
NZ (1) NZ509645A (es)
PL (1) PL193802B1 (es)
PT (1) PT1103243E (es)
RU (1) RU2223116C2 (es)
TR (1) TR200100378T2 (es)
TW (1) TW445259B (es)
WO (1) WO2000007542A2 (es)
ZA (1) ZA200100867B (es)

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ES2174756B2 (es) * 2001-04-06 2003-11-16 Esteve Labor Dr Derivados de aril (o heteroaril) azolilcarbinoles para el tratamiento de enfermedades respiratorias.
ES2180449B1 (es) * 2001-07-06 2004-01-16 Esteve Labor Dr Derivados de aril (o heteroaril) azolilcarbinoles para el tratamiento de la incontinencia urinaria.
US20040142929A1 (en) * 2001-07-06 2004-07-22 Ramon Merce-Vidal Derivatives of aryl (or heteroaryl) azolylcarbinoles for the treatment of urinary incontinence
DE10335566A1 (de) * 2003-07-31 2005-02-24 Grünenthal GmbH Arzneimittel enthaltend Derivate von Aryl( oder Heteroaryl)azolylcarbinolen
EP1584335A3 (en) * 2004-04-05 2006-02-22 Laboratorios Del Dr. Esteve, S.A. Active substance combination comprising a carbinol composition and an opioid
ES2244326B1 (es) * 2004-04-05 2007-02-16 Laboratorios Del Dr. Esteve, S.A. Combinacion de substancias activas.
EP1784178A1 (en) * 2004-07-30 2007-05-16 Laboratorios Del Dr. Esteve, S.A. Aryl (or heteroaryl) azolylcarbinols
US20080045610A1 (en) * 2004-09-23 2008-02-21 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
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CN101557810B (zh) 2006-12-13 2012-11-21 弗·哈夫曼-拉罗切有限公司 作为痕量胺相关受体（taar）的配体的新的2-咪唑类
KR101174191B1 (ko) 2007-02-02 2012-08-14 에프. 호프만-라 로슈 아게 중추 신경계 장애의 치료용 ｔａａｒ1 리간드로서 2-아미노옥사졸린
WO2008098857A1 (en) 2007-02-15 2008-08-21 F. Hoffmann-La Roche Ag 2-aminooxazolines as taar1 ligands
EP2173720A2 (en) 2007-07-02 2010-04-14 F. Hoffmann-Roche AG 2-imidazolines having a good affinity to the trace amine associated receptors (taars)
CA2691704A1 (en) 2007-07-03 2009-01-08 F. Hoffmann-La Roche Ag 4-imidazolines and their use as antidepressants
KR101133862B1 (ko) 2007-07-27 2012-04-06 에프. 호프만-라 로슈 아게 Ｔａａｒ 리간드로서의 2-아제티딘메테인아민 및 2-피롤리딘메테인아민
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US8242153B2 (en) 2008-07-24 2012-08-14 Hoffmann-La Roche Inc. 4,5-dihydro-oxazol-2YL derivatives
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EP0289380A1 (fr) * 1987-04-10 1988-11-02 Laboratorios Del Dr. Esteve, S.A. Dérivés d'aryl-hétéroaryl carbinols avec activité analgésique
EP0699674A1 (en) * 1994-07-22 1996-03-06 Eli Lilly And Company 1-Aryl-2-acetylamidopentanone derivatives for use as tachykinin receptor antagonists
WO1998024439A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating severe anxiety disorders
WO1998024438A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating major depressive disorders
WO1998024445A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating schizophrenic disorders
WO1998024447A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating cognitive disorders

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FR2681322B1 (fr) * 1991-09-12 1993-12-17 Laboratorios Dr Esteve Sa Derives d'aryl-heteroaryl-{n-[2-(3,4-dimethoxyphenyl)-ethyl]-n-methyl-3-aminopropoxy}-methane leur preparation et leur application en tant que medicaments .
ES2150353B1 (es) * 1998-04-15 2001-07-01 Esteve Labor Dr Tienilazolilalcoxietanaminas, su preparacion y su aplicacion como medicamentos.

Patent Citations (6)

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EP0289380A1 (fr) * 1987-04-10 1988-11-02 Laboratorios Del Dr. Esteve, S.A. Dérivés d'aryl-hétéroaryl carbinols avec activité analgésique
EP0699674A1 (en) * 1994-07-22 1996-03-06 Eli Lilly And Company 1-Aryl-2-acetylamidopentanone derivatives for use as tachykinin receptor antagonists
WO1998024439A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating severe anxiety disorders
WO1998024438A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating major depressive disorders
WO1998024445A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating schizophrenic disorders
WO1998024447A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating cognitive disorders

Also Published As

Publication number Publication date
TW445259B (en) 2001-07-11
CZ292065B6 (cs) 2003-07-16
CZ2001412A3 (cs) 2001-08-15
PL193802B1 (pl) 2007-03-30
BR9912807A (pt) 2001-10-16
ATE257379T1 (de) 2004-01-15
ZA200100867B (en) 2001-08-16
PT1103243E (pt) 2004-05-31
NO20010634D0 (no) 2001-02-06
AU754124B2 (en) 2002-11-07
JP2002522359A (ja) 2002-07-23
DE69914085D1 (de) 2004-02-12
PL346221A1 (en) 2002-01-28
US6518295B1 (en) 2003-02-11
DE69914085T8 (de) 2005-04-21
WO2000007542A2 (es) 2000-02-17
ES2213380T3 (es) 2004-08-16
CN1317966A (zh) 2001-10-17
CO5080747A1 (es) 2001-09-25
IL141295A0 (en) 2002-12-01
NO20010634L (no) 2001-04-06
CA2339661A1 (en) 2000-02-17
RU2223116C2 (ru) 2004-02-10
CN1151789C (zh) 2004-06-02
HUP0105428A3 (en) 2003-01-28
TR200100378T2 (tr) 2001-06-21
AR019999A1 (es) 2002-03-27
NZ509645A (en) 2003-01-31
DK1103243T3 (da) 2004-05-03
HUP0105428A2 (hu) 2002-05-29
ES2150378B1 (es) 2001-07-01
KR20010079616A (ko) 2001-08-22
AU5422999A (en) 2000-02-28
ES2150378A1 (es) 2000-11-16
DE69914085T2 (de) 2004-11-25
EP1103243B1 (en) 2004-01-07
EP1103243A2 (en) 2001-05-30
KR100558506B1 (ko) 2006-03-07
CA2339661C (en) 2006-10-17

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