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1.发明公开3-SUBSTITUTED AMINO-1H-INDOLE-2-CARBOXYLIC ACID AND 3-SUBSTITUTED AMINO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID DERIVATIVES AS INTERLEUKIN-4 GENE EXPRESSION INHIBITORS 有权3-（氨基SUBSTITUTIERTE）-1H-吲哚-2-羧酸酯和3-（SUBSTITUTIERTE氨基） - 苯并[b]噻吩-2-羧酸酯化合物作为抑制剂的白介素-4基因表达
公开(公告)号：EP1501797A1
公开(公告)日：2005-02-02
申请号：EP03733867.0
申请日：2003-04-23
发明人： ALKAN, Sefik, S. , DINERSTEIN, Robert, J. , SUBRAMANIAM, Arun , HRIB, Nicholas, J. , JURCAK, John, G.
IPC分类号： C07D209/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D401/14 , C07D405/14 , A61K31/40 , A61P11/06 , A61P37/08 , A61P31/04
CPC分类号： C07D401/12 , A61K31/40 , A61K31/405 , C07D209/42 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： This invention discloses and claims substituted 3-amino-2-carboxylic acid indole and benzo(b)thiophene derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. In preferred embodiments of this invention it is also disclosed and claimed that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.
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2.发明授权THIENOISOXAZOLYL AND THIENYLPYRRAZOLYL PHENOXY SUBSTITUTED PROPYL DERIVATIVES USEFUL AS D4 ANTAGONISTS 有权THIENOISOXAZOLYL-和THIENYLPYRAZOLYL，取代的苯氧基PROPYL衍生物作为D4拮抗剂
公开(公告)号：EP1216250B1
公开(公告)日：2003-11-19
申请号：EP00964969.0
申请日：2000-09-13
发明人： FINK, David, M. , FREED, Brian, S. , HRIB, Nicholas, J. , KOSLEY, Raymond, W., Jr. , LEE, George, E. , MERRIMAN, Gregory, H. , RAUCKMAN, Barbara, S.
IPC分类号： C07D498/04 , C07D519/00 , A61K31/40 , A61K31/55 , A61K31/501 , A61K31/42 , A61K31/44 , A61K31/506 , A61P25/18
CPC分类号： C07D498/04 , C07D519/00
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3.发明授权3-(PYRIDINYL-AMINO)-1H-INDOLE-2-CARBOXYLIC ACID DERIVATIVES AS INTERLEUKIN-4 GENE EXPRESSION INHIBITORS 有权3-（吡啶基 - 氨基）-1H-吲哚-2-羧酸化合物AS白细胞介素-4基因表达的抑制剂的
公开(公告)号：EP1501796B1
公开(公告)日：2007-05-09
申请号：EP03721841.9
申请日：2003-04-23
发明人： MERRIMAN, Gregory, H. , WEINTRAUB, Philip, M. , SABOL, Jeffrey, S. , DHARANIPRAGADA, Ramalinga , HRIB, Nicholas, J. , JURCAK, John, G. , GROSS, Alexandre , WHITELEY, Brian , MUSICK, Kwon, Yon , KLEIN, Joseph, T.
IPC分类号： C07D209/42 , C07D401/12 , C07D409/12 , C07D401/14 , C07D405/14 , C07D417/14 , C07D417/12 , C07D403/12 , A61K31/40 , A61P11/06 , A61P37/08 , A61P31/04 , A61P35/00
CPC分类号： C07D401/12 , A61K31/40 , A61K31/405 , C07D209/42 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： This inventions discloses and claims 3-substituted amino-1H-indole-2-carboxylic acid and 3-substituted amino-benzothiophene-2-carboxylic acid derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interieukin-4(IL-4) message, IL-4 release or IL-4 production.
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4.发明公开3-SUBSTITUTED AMINO-1H-INDOLE-2-CARBOXYLIC ACID AND 3-SUBSTITUTED AMINO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID DERIVATIVES AS INTERLEUKIN-4 GENE EXPRESSION INHIBITORS 有权3-（吡啶基 - 氨基）-1H-吲哚-2-羧酸化合物AS白细胞介素-4基因表达的抑制剂的
公开(公告)号：EP1501796A1
公开(公告)日：2005-02-02
申请号：EP03721841.9
申请日：2003-04-23
发明人： MERRIMAN, Gregory, H. , WEINTRAUB, Philip, M. , SABOL, Jeffrey, S. , DHARANIPRAGADA, Ramalinga , HRIB, Nicholas, J. , JURCAK, John, G. , GROSS, Alexandre , WHITELEY, Brian , MUSICK, Kwon, Yon , KLEIN, Joseph, T.
IPC分类号： C07D209/42 , C07D401/12 , C07D409/12 , C07D401/14 , C07D405/14 , C07D417/14 , C07D417/12 , C07D403/12 , A61K31/40 , A61P11/06 , A61P37/08 , A61P31/04 , A61P35/00
CPC分类号： C07D401/12 , A61K31/40 , A61K31/405 , C07D209/42 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： This inventions discloses and claims 3-substituted amino-1H-indole-2-carboxylic acid and 3-substituted amino-benzothiophene-2-carboxylic acid derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interieukin-4(IL-4) message, IL-4 release or IL-4 production.
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5.发明授权3-(SUBSTITUTED AMINO)-1H-INDOLE-2-CARBOXYLIC ACID ESTER AND 3-(SUBSTITUTED AMINO)-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID ESTER DERIVATIVES AS INTERLEUKIN-4 GENE EXPRESSION INHIBITORS 有权3-（氨基SUBSTITUTIERTE）-1H-吲哚-2-羧酸酯和3-（SUBSTITUTIERTE氨基） - 苯并[b]噻吩-2-羧酸酯化合物作为抑制剂的白介素-4基因表达
公开(公告)号：EP1501797B1
公开(公告)日：2009-08-05
申请号：EP03733867.0
申请日：2003-04-23
发明人： ALKAN, Sefik, S. , DINERSTEIN, Robert, J. , SUBRAMANIAM, Arun , HRIB, Nicholas, J. , JURCAK, John, G.
IPC分类号： C07D209/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D401/14 , C07D405/14 , A61K31/40 , A61P11/06 , A61P37/08 , A61P31/04
CPC分类号： C07D401/12 , A61K31/40 , A61K31/405 , C07D209/42 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： This invention discloses and claims substituted 3-amino-2-carboxylic acid indole and benzo(b)thiophene derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. In preferred embodiments of this invention it is also disclosed and claimed that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.
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6.发明授权Benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives useful as D4 antagonists 有权苯并异恶唑，苯并PYRIDOISOXAZOLYL-和基 - 苯氧基衍生物作为D4拮抗剂
公开(公告)号：EP1216244B1
公开(公告)日：2003-08-13
申请号：EP00963370.2
申请日：2000-09-13
发明人： SHUTSKE, Gregory, M. , HENDRIX, James, A. , JURCAK, John, G. , FREED, Brian, S. , HRIB, Nicholas, J. , TOMER, John, D., IV , HANNA, Reda, G.
IPC分类号： C07D413/12 , C07D261/20 , C07D413/14 , C07D471/04 , C07D409/14 , C07D333/56 , C07D409/12 , C07D498/04 , A61K31/42 , A61K31/38 , A61K31/47 , A61K31/44 , C07D213/61 , C07C251/48
CPC分类号： C07D409/12 , C07C251/48 , C07D261/20 , C07D333/56 , C07D413/12 , C07D413/14 , C07D471/04 , C07D491/10
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7.发明公开THIENOISOXAZOLYL AND THIENYLPYRRAZOLYL PHENOXY SUBSTITUTED PROPYL DERIVATIVES USEFUL AS D4 ANTAGONISTS 有权用作D4拮抗剂的噻吩并恶唑和噻吩基吡唑基苯氧取代的丙基衍生物
公开(公告)号：EP1216250A1
公开(公告)日：2002-06-26
申请号：EP00964969.0
申请日：2000-09-13
发明人： FINK, David, M. , FREED, Brian, S. , HRIB, Nicholas, J. , KOSLEY, Raymond, W., Jr. , LEE, George, E. , MERRIMAN, Gregory, H. , RAUCKMAN, Barbara, S.
IPC分类号： C07D498/04 , C07D519/00 , A61K31/40 , A61K31/55 , A61K31/501 , A61K31/42 , A61K31/44 , A61K31/506 , A61P25/18
CPC分类号： C07D498/04 , C07D519/00
摘要： The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
摘要翻译： 这些化合物属于噻吩并异恶唑基 - 和噻吩基吡唑基 - 苯氧基取代的丙基衍生物类，可用作D4拮抗剂。 所述化合物可用于治疗由D4受体抑制介导的医学病症。 这些病症包括例如注意缺陷多动障碍，强迫症，精神病，药物滥用，物质依赖，帕金森病，帕金森综合征，迟发性硬脑膜炎，吉尔斯德拉图雷特综合征，行为障碍和对立违抗性障碍。 本发明的另一方面是提供药物组合物，中间体和制备所述类型的化合物的方法。
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8.发明公开BENZISOXAZOLYL-, PYRIDOISOXAZOLYL- AND BENZTHIENYL-PHENOXY DERIVATIVES USEFUL AS D 4? ANTAGONISTS 有权苯并异恶唑，苯并PYRIDOISOXAZOLYL-和基 - 苯氧基衍生物作为D4拮抗剂
公开(公告)号：EP1216244A1
公开(公告)日：2002-06-26
申请号：EP00963370.2
申请日：2000-09-13
发明人： SHUTSKE, Gregory, M. , HENDRIX, James, A. , JURCAK, John, G. , FREED, Brian, S. , HRIB, Nicholas, J. , TOMER, John, D., IV , HANNA, Reda, G.
IPC分类号： C07D413/12 , C07D261/20 , C07D413/14 , C07D471/04 , C07D409/14 , C07D333/56 , C07D409/12 , C07D498/04 , A61K31/42 , A61K31/38 , A61K31/47 , A61K31/44 , C07D213/61 , C07C251/48
CPC分类号： C07D409/12 , C07C251/48 , C07D261/20 , C07D333/56 , C07D413/12 , C07D413/14 , C07D471/04 , C07D491/10
摘要： The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
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