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公开(公告)号：SG76623A1
公开(公告)日：2000-11-21
申请号：SG1999002779
申请日：1999-06-09
Applicant: HOFFMANN LA ROCHE
Inventor： ADAM GEO , DAUTZENBERG FRANK , KOLCZEWSKI SABINE , ROVER STEPHAN , WICHMANN JURGEN
IPC: C07D401/14 , A01N43/42 , A61K31/00 , A61K31/395 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61P3/04 , A61P3/12 , A61P9/12 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D471/10 , C07D471/20 , C07D487/20 , C07D498/10 , C07D513/10
Abstract: The present invention relates to compounds of the general formula wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof. The compound of the invention are useful in the treatment of diseases related to the orphanin FQ (OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and leaning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na excretion, arterial blood pressure disorders and metabolic disorders such as obesity.
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公开(公告)号：PE05492000A1
公开(公告)日：2000-07-24
申请号：PE00048599
申请日：1999-06-08
Applicant: HOFFMANN LA ROCHE
Inventor： WICHMANN JURGEN , ADAM GEO , ROVER STEPHAN , DAUTZENBERG FRANK , KOLCZEWSKI SABINE
IPC: C07D401/14 , A01N43/42 , A61K31/00 , A61K31/395 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61P3/04 , A61P3/12 , A61P9/12 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D471/10 , C07D471/20 , C07D487/20 , C07D498/10 , C07D513/10
CPC classification number: C07D471/20
Abstract: SE REFIERE A ESPIRO[PIPERIDIN-4,1`-PIRROLO[3,4-c]PIRROL] DE FORMULA I, DONDE R1 ES CICLOALQUILO C5-C12 OPCIONALMENTE SUSTITUIDO CON ALQUILO, DECAHIDRO-NAFTALEN-1-ILO, INDAN-1-IL, DECAHIDRO-AZULEN-2-ILO, BICICLO[6.2.0]DEC-9-ILO, ACENAFTEN-1-ILO, BICICLO[3.3.1]NON-9-ILO, 2,3-DIHIDRO-1H-FENALEN-1-ILO, ENTRE OTROS; R2 Y R3 SON H, OH, ALQUILO, =O, FENILO OPCIONALMENTE SUSTITUIDO CON ALQUILO, HALOGENO, ALCOXILO; R4 ES H, ALQUILO, (CH2)nCHOHCF3, -(CH2)n-CICLOALQUILO C3-C6, FENILO, BENCILO, TETRAHIDROFURAN-3-ILO, -(CH2)nOCH2C6H5, -(CH2)nMORFOLINILO, 3-METIL-OXETAN-3-IL-METILO, -(CH2)nCH2OH, -SO2-ALQUILO, -CO-ALQUILO, -COCF3, ENTRE OTROS; R5 ES H, HALOGENO, ALQUILO, TRIFLUOROMETILO, ALCOXILO; n ES 0-3. SON COMPUESTOS PREFERIDOS (3'aRS,6'aSR)-1-CICLONONIL-5'-METIL-2'-FENIL-HEXAHIDRO-ESPIRO[PIPERIDIN-4,1'(2'H)-PIRROLO[3,4-c]PIRROL], (3'aRS,6'aSR)-1-CICLODECIL-5'-METIL-2'-FENIL-HEXAHIDRO-ESPIRO[PIPERIDIN-4,1'(2'H)-PIRROLO[3.4-c]PIRROL]-4',6'-DIONA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES UN AGONISTA/ANTAGONISTA DEL RECEPTOR DE LA ORFANINA OFQ POR LO QUE PUEDE SER UTIL EN EL TRATAMIENTO DE TRASTORNOS PSIQUIATRICOS, NEUROLOGICOS Y FISIOLOGICOS COMO TRASTORNOS DE LA ANSIEDAD, ESTRES, DEPRESION, TRAUMAS, PERDIDA DE MEMORIA DEBIDA A LA ENFERMEDAD DE ALZHEIMER, EPILEPSIA, CONVULSIONES
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公开(公告)号：BR9902245A
公开(公告)日：2000-03-21
申请号：BR9902245
申请日：1999-06-11
Applicant: HOFFMANN LA ROCHE
Inventor： ADAM GEO , DAUTZENBERG FRANK , KOLCZEWSKI SABINE , ROEVER STEPHAN , WICHMANN JUERGE
IPC: C07D401/14 , A01N43/42 , A61K31/00 , A61K31/395 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61P3/04 , A61P3/12 , A61P9/12 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D471/10 , C07D471/20 , C07D487/20 , C07D498/10 , C07D513/10
Abstract: The present invention relates to compounds of the general formula wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof. The compound of the invention are useful in the treatment of diseases related to the orphanin FQ (OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and leaning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na excretion, arterial blood pressure disorders and metabolic disorders such as obesity.
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公开(公告)号：HRP990189A2
公开(公告)日：2000-02-29
申请号：HRP990189
申请日：1999-06-11
Applicant: HOFFMANN LA ROCHE
Inventor： GEO ADAM , DAUTZENBERG FRANK , KOLCZEWSKI SABINE , ROEVER STEPHAN , WICHMANN JUERGEN
IPC: C07D401/14 , A01N43/42 , A61K31/00 , A61K31/395 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61P3/04 , A61P3/12 , A61P9/12 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D471/10 , C07D471/20 , C07D487/20 , C07D498/10 , C07D513/10
Abstract: The present invention relates to compounds of the general formula wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof. The compound of the invention are useful in the treatment of diseases related to the orphanin FQ (OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and leaning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na excretion, arterial blood pressure disorders and metabolic disorders such as obesity.
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公开(公告)号：CA2274204A1
公开(公告)日：1999-12-12
申请号：CA2274204
申请日：1999-06-09
Applicant: HOFFMANN LA ROCHE
Inventor： ADAM GEO , ROEVER STEPHAN , WICHMANN JUERGEN , DAUTZENBERG FRANK , KOLCZEWSKI SABINE
IPC: C07D401/14 , A01N43/42 , A61K31/00 , A61K31/395 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61P3/04 , A61P3/12 , A61P9/12 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D471/10 , C07D471/20 , C07D487/20 , C07D498/10 , C07D513/10
Abstract: The present invention relates to compounds of the general formula (see formula I) wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof. The compound of the invention are useful in the treatment of diseases related to the orphanin FQ(OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and learning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na+ excretion, arterial blood pressure disorders and metabolic disorders such as obesity.
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Patent Agency Ranking
公开(公告)号：DE60123458T2
公开(公告)日：2007-08-02
申请号：DE60123458
申请日：2001-11-06
Applicant: HOFFMANN LA ROCHE
Inventor： BREU VOLKER , DAUTZENBERG FRANK , MATTEI PATRIZIO , NEIDHART WERNER , PFLIEGER PHILIPPE
IPC: C07D239/42 , A61K31/337 , A61K31/505 , A61K31/506 , A61P3/04 , A61P3/10 , A61P19/02 , A61P43/00 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06
Abstract: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.
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公开(公告)号：DK1335906T3
公开(公告)日：2007-02-05
申请号：DK01989438
申请日：2001-11-06
Applicant: HOFFMANN LA ROCHE
Inventor： BREU VOLKER , DAUTZENBERG FRANK , MATTEI PATRIZIO , NEIDHART WERNER , PFLIEGER PHILIPPE
IPC: C07D239/42 , A61K31/337 , A61K31/505 , A61K31/506 , A61P3/04 , A61P3/10 , A61P19/02 , A61P43/00 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06
Abstract: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.
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38.发明专利
公开(公告)号：PT1335906E
公开(公告)日：2007-01-31
申请号：PT01989438
申请日：2001-11-06
Applicant: HOFFMANN LA ROCHE
Inventor： WERNER NEIDHART DR , BREU VOLKER , DAUTZENBERG FRANK , MATTEI PATRIZIO , PFLIEGER PHILIPPE
IPC: C07D239/42 , A61K31/337 , A61K31/505 , A61K31/506 , A61P3/04 , A61P3/10 , A61P19/02 , A61P43/00 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06
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公开(公告)号：BR0115045A
公开(公告)日：2004-02-03
申请号：BR0115045
申请日：2001-11-06
Applicant: HOFFMANN LA ROCHE
Inventor： BREU VOLKER , DAUTZENBERG FRANK , NEIDHART WERNER , MATTEI PATRIZIO , PFLIEGER PHILIPPE
IPC: A61K31/337 , A61K31/505 , A61K31/506 , A61P3/04 , A61P3/10 , A61P19/02 , A61P43/00 , C07D239/42 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06
Abstract: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.
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公开(公告)号：DK0963987T3
公开(公告)日：2002-12-30
申请号：DK99110944
申请日：1999-06-07
Applicant: HOFFMANN LA ROCHE
Inventor： ADAM GEO , DAUTZENBERG FRANK , KOLCZEWSKI SABINE , ROEVER STEPHAN , WICHMANN JUERGEN
IPC: C07D401/14 , A01N43/42 , A61K31/00 , A61K31/395 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61P3/04 , A61P3/12 , A61P9/12 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D471/10 , C07D471/20 , C07D487/20 , C07D498/10 , C07D513/10
Abstract: The present invention relates to compounds of the general formula wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof. The compound of the invention are useful in the treatment of diseases related to the orphanin FQ (OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and leaning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na excretion, arterial blood pressure disorders and metabolic disorders such as obesity.
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