BR0116385A - Composto, composição farmacêutica, embalagem, métodos para alterar a atividade transdutora de sinal de um receptor de gabaa, para tratar ansiedade, depressão, um distúrbio do sono, esquizofrenia, distúrbio do déficit de atenção hiperatividade ou para a memória, para demonstrar a presença de um receptor de gabaa em uma amostra de célula ou tecido e em uma seção de tecido uso de um composto, e, processo para preparar um composto - Google Patents

Composto, composição farmacêutica, embalagem, métodos para alterar a atividade transdutora de sinal de um receptor de gabaa, para tratar ansiedade, depressão, um distúrbio do sono, esquizofrenia, distúrbio do déficit de atenção hiperatividade ou para a memória, para demonstrar a presença de um receptor de gabaa em uma amostra de célula ou tecido e em uma seção de tecido uso de um composto, e, processo para preparar um composto

Info

Publication number
BR0116385A
BR0116385A BR0116385-0A BR0116385A BR0116385A BR 0116385 A BR0116385 A BR 0116385A BR 0116385 A BR0116385 A BR 0116385A BR 0116385 A BR0116385 A BR 0116385A
Authority
BR
Brazil
Prior art keywords
compound
compounds
gaba
depression
demonstrate
Prior art date
Application number
BR0116385-0A
Other languages
English (en)
Inventor
Guiying Li
John M Peterson
Pamela Albaugh
Kevin S Currie
Guolin Cai
Linda M Gustavson
Yyungae Lee
Alan Hutchison
Vinod Singh
George D Maynard
Jun Yuan
Linghong Xie
Manuka Ghosh
Nian Liu
George P Luke
Scott Mitchell
Martin Patrick Allen
Spiro Liras
Original Assignee
Neurogen Corp
Pfizer
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 Neurogen Corp, Pfizer filed Critical Neurogen Corp
Publication of BR0116385A publication Critical patent/BR0116385A/pt

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P25/14—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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • 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
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    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
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    • 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
    • C07D417/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/14—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 three or more hetero rings
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

"COMPOSTO, COMPOSIçãO FARMACêUTICA, EMBALAGEM, MéTODOS PARA ALTERAR A ATIVIDADE TRANSDUTORA DE SINAL DE UM RECEPTOR DE GABA~ A~, PARA TRATAR ANSIEDADE, DEPRESSãO, UM DISTúRBIO DO SONO, ESQUIZOFRENIA, DISTúRBIO DO DéFICIT DE ATENçãO-HIPERATIVIDADE OU PARA REALçAR A MEMóRIA, PARA DEMONSTRAR A PRESENçA DE UM RECEPTOR DE GABA~ A~ EM UMA AMOSTRA DE CéLULA OU TECIDO E EM UMA SEçãO DE TECIDO, USO DE UM COMPOSTO, E, PROCESSO PARA PREPARAR UM COMPOSTO". Esta invenção diz respeito aos benzimidazóis, piridimidazóis e compostos bicíclicos de heteroarila relacionados, todos os quais podem ser descritos pela Fórmula (I). A invenção está particularmente relacionada a tais compostos que se ligam com alta seletividade e alta afinidade ao sítio de benzodiazepina dos receptores de GABA~ A~. Esta invenção também diz respeito às composições farmacêuticas que compreendem tais compostos e ao uso de tais compostos no tratamento de certas doenças do sistema nervoso central (CNS). Novos processos para preparar os compostos da Fórmula I são divulgados. Esta invenção também diz respeito ao uso de benzimidazóis, piridilimidazóis e compostos bicíclicos de heteroarila relacionados da Fórmula I em combinação com um ou mais outros agentes do CNS para potenciar os efeitos dos outros agentes do CNS. Adicionalmente, esta invenção diz respeito ao uso de tais compostos como sondas para a localização dos receptores de GABA~ A~ nas seções de tecido.
BR0116385-0A 2000-12-21 2001-12-21 Composto, composição farmacêutica, embalagem, métodos para alterar a atividade transdutora de sinal de um receptor de gabaa, para tratar ansiedade, depressão, um distúrbio do sono, esquizofrenia, distúrbio do déficit de atenção hiperatividade ou para a memória, para demonstrar a presença de um receptor de gabaa em uma amostra de célula ou tecido e em uma seção de tecido uso de um composto, e, processo para preparar um composto BR0116385A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25749200P 2000-12-21 2000-12-21
PCT/US2001/050038 WO2002050062A2 (en) 2000-12-21 2001-12-21 Benzimidazole and pyridylimidazole derivatives as ligands for gaba receptors

Publications (1)

Publication Number Publication Date
BR0116385A true BR0116385A (pt) 2005-12-13

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BR0116385-0A BR0116385A (pt) 2000-12-21 2001-12-21 Composto, composição farmacêutica, embalagem, métodos para alterar a atividade transdutora de sinal de um receptor de gabaa, para tratar ansiedade, depressão, um distúrbio do sono, esquizofrenia, distúrbio do déficit de atenção hiperatividade ou para a memória, para demonstrar a presença de um receptor de gabaa em uma amostra de célula ou tecido e em uma seção de tecido uso de um composto, e, processo para preparar um composto

Country Status (40)

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US (4) US6916819B2 (pt)
EP (1) EP1368342B3 (pt)
JP (1) JP2004536782A (pt)
KR (1) KR100854174B1 (pt)
CN (1) CN1553909A (pt)
AP (1) AP1503A (pt)
AR (1) AR035774A1 (pt)
AT (1) ATE304008T1 (pt)
AU (2) AU2002232768B2 (pt)
BG (1) BG107899A (pt)
BR (1) BR0116385A (pt)
CA (1) CA2431592A1 (pt)
CO (1) CO5390086A1 (pt)
CZ (1) CZ20031676A3 (pt)
DE (1) DE60113302T2 (pt)
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WO (1) WO2002050062A2 (pt)
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