BRPI0417110A - inibidores de fosfodiesterase 4, incluindo análogos de diarilamina n-substituìdos, composto, composição farmacêutica, método para aumentar a cognição em um paciente no qual tal aumento é desejado, método de tratamento de um paciente que sofre de degeneração ou declìnio da cognição, método para o tratamento de um paciente que tem uma doença que envolve nìveis reduzidos de camp, método de inibição da atividade da enzima pde4 em uma paciente, método de tratamento de um paciente que sofre de degeneração da memória devido a uma doença neurodegenerativa, método de tratamento de um paciente que sofre de degeneração da memória devida a um distúrbio neurodegenerativo agudo, método de tratamento de um paciente que sofre de uma doença alérgica ou inflamatória, método para o tratamento de um paciente que sofre de esquizofrenia, método para o tratamento de um paciente que sofre de psicose caracterizada por nìveis elevados pde4, sendo que a dita psicose é uma forma de depressão - Google Patents

inibidores de fosfodiesterase 4, incluindo análogos de diarilamina n-substituìdos, composto, composição farmacêutica, método para aumentar a cognição em um paciente no qual tal aumento é desejado, método de tratamento de um paciente que sofre de degeneração ou declìnio da cognição, método para o tratamento de um paciente que tem uma doença que envolve nìveis reduzidos de camp, método de inibição da atividade da enzima pde4 em uma paciente, método de tratamento de um paciente que sofre de degeneração da memória devido a uma doença neurodegenerativa, método de tratamento de um paciente que sofre de degeneração da memória devida a um distúrbio neurodegenerativo agudo, método de tratamento de um paciente que sofre de uma doença alérgica ou inflamatória, método para o tratamento de um paciente que sofre de esquizofrenia, método para o tratamento de um paciente que sofre de psicose caracterizada por nìveis elevados pde4, sendo que a dita psicose é uma forma de depressão

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Publication number
BRPI0417110A
BRPI0417110A BRPI0417110-1A BRPI0417110A BRPI0417110A BR PI0417110 A BRPI0417110 A BR PI0417110A BR PI0417110 A BRPI0417110 A BR PI0417110A BR PI0417110 A BRPI0417110 A BR PI0417110A
Authority
BR
Brazil
Prior art keywords
patient
treating
patient suffering
treatment
psychosis
Prior art date
Application number
BRPI0417110-1A
Other languages
English (en)
Inventor
Richard Schumacher
Allen Hopper
Robert Dunn
Erik Kuester
Ashok Tehim
Tomas E Renau
Joan Caroon
Francisco Talamas
Sharada Labadie
Original Assignee
Memory Pharm Corp
Hoffmann La Roche
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 Memory Pharm Corp, Hoffmann La Roche filed Critical Memory Pharm Corp
Publication of BRPI0417110A publication Critical patent/BRPI0417110A/pt

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
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    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • 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
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • C07C229/52—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C229/54—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C229/60—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in meta- or para- positions
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
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    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract

"INIBIDORES DE FOSFODIESTERASE 4, INCLUINDO ANáLOGOS DE DIARILAMINA N-SUBSTITUìDOS, COMPOSTO, COMPOSIçãO FARMACêUTICA, MéTODO PARA AUMENTAR A COGNIçãO EM UM PACIENTE NO QUAL TAL AUMENTO é DESEJADO, MéTODO DE TRATAMENTO DE UM PACIENTE QUE SOFRE DE DEGENERAçãO OU DECLìNIO DA COGNIçãO, MéTODO PARA O TRATAMENTO DE UM PACIENTE QUE TEM UMA DOENçA QUE ENVOLVE NìVEIS REDUZIDOS DE cAMP, MéTODO DE INIBIçãO DA ATIVIDADE DA ENZIMA PDE4 EM UM PACIENTE, MéTODO DE TRATAMENTO DE UM PACIENTE QUE SOFRE DE DEGENERAçãO DA MEMóRIA DEVIDO A UMA DOENçA NEURODEGENERATIVA, MéTODO DE TRATAMENTO DE UM PACIENTE QUE SOFRE DE DEGENERAçãO DA MEMóRIA DEVIDA A UM DISTúRBIO NEURODEGENERATIVO AGUDO, MéTODO DE TRATAMENTO DE UM PACIENTE QUE SOFRE DE UMA DOENçA ALéRGICA OU INFLAMATóRIA, MéTODO PARA O TRATAMENTO DE UM PACIENTE QUE SOFRE DE ESQUIZOFRENIA, MéTODO PARA O TRATAMENTO DE UM PACIENTE QUE SOFRE DE PSICOSE CARACTERIZADA POR NìVEIS ELEVADOS PDE4, SENDO QUE A DITA PSICOSE é UMA FORMA DE DEPRESSãO". A inibição de PDFA é obtida por novos compostos, por exemplo, análogo de diarilamina N-substituídos. Os compostos da presente invenção são da fórmula (I), na qual A, B, D, R¬ 1¬, R¬ 2¬, R¬ 3¬ e R¬ 4¬ são tal como aqui definido.
BRPI0417110-1A 2003-12-11 2004-12-10 inibidores de fosfodiesterase 4, incluindo análogos de diarilamina n-substituìdos, composto, composição farmacêutica, método para aumentar a cognição em um paciente no qual tal aumento é desejado, método de tratamento de um paciente que sofre de degeneração ou declìnio da cognição, método para o tratamento de um paciente que tem uma doença que envolve nìveis reduzidos de camp, método de inibição da atividade da enzima pde4 em uma paciente, método de tratamento de um paciente que sofre de degeneração da memória devido a uma doença neurodegenerativa, método de tratamento de um paciente que sofre de degeneração da memória devida a um distúrbio neurodegenerativo agudo, método de tratamento de um paciente que sofre de uma doença alérgica ou inflamatória, método para o tratamento de um paciente que sofre de esquizofrenia, método para o tratamento de um paciente que sofre de psicose caracterizada por nìveis elevados pde4, sendo que a dita psicose é uma forma de depressão BRPI0417110A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US52848603P 2003-12-11 2003-12-11
PCT/US2004/041068 WO2005061458A2 (en) 2003-12-11 2004-12-10 Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs

Publications (1)

Publication Number Publication Date
BRPI0417110A true BRPI0417110A (pt) 2007-02-06

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BRPI0417110-1A BRPI0417110A (pt) 2003-12-11 2004-12-10 inibidores de fosfodiesterase 4, incluindo análogos de diarilamina n-substituìdos, composto, composição farmacêutica, método para aumentar a cognição em um paciente no qual tal aumento é desejado, método de tratamento de um paciente que sofre de degeneração ou declìnio da cognição, método para o tratamento de um paciente que tem uma doença que envolve nìveis reduzidos de camp, método de inibição da atividade da enzima pde4 em uma paciente, método de tratamento de um paciente que sofre de degeneração da memória devido a uma doença neurodegenerativa, método de tratamento de um paciente que sofre de degeneração da memória devida a um distúrbio neurodegenerativo agudo, método de tratamento de um paciente que sofre de uma doença alérgica ou inflamatória, método para o tratamento de um paciente que sofre de esquizofrenia, método para o tratamento de um paciente que sofre de psicose caracterizada por nìveis elevados pde4, sendo que a dita psicose é uma forma de depressão

Country Status (16)

Country Link
US (1) US20050222207A1 (pt)
EP (1) EP1692109B1 (pt)
JP (1) JP2007513957A (pt)
KR (1) KR20060128909A (pt)
CN (1) CN1922144A (pt)
AR (1) AR046789A1 (pt)
AT (1) ATE478049T1 (pt)
AU (1) AU2004303855A1 (pt)
BR (1) BRPI0417110A (pt)
CA (1) CA2548824A1 (pt)
DE (1) DE602004028754D1 (pt)
MX (1) MXPA06006557A (pt)
MY (1) MY141255A (pt)
RU (1) RU2388750C2 (pt)
TW (1) TW200602322A (pt)
WO (1) WO2005061458A2 (pt)

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US20030149052A1 (en) * 2002-01-22 2003-08-07 Memory Pharmaceuticals Corp. Phosphodiesterase 4 inhibitors
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
HRP20050082A2 (en) * 2002-07-19 2005-06-30 Memory Pharmaceuticals Corporation 6-amino-1h-indazole and 4-aminobenzofuran compounds as phosphodiesterase 4 inhibitors
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
JP4886511B2 (ja) 2003-07-30 2012-02-29 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物による自己免疫疾患の治療または予防方法
CN101115761B (zh) 2005-01-19 2012-07-18 里格尔药品股份有限公司 2,4-嘧啶二胺化合物的前药及其应用
AU2006254840B2 (en) 2005-06-08 2012-08-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
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