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公开(公告)号：US5648366A
公开(公告)日：1997-07-15
申请号：US477167
申请日：1995-06-07
IPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10 , A61K31/445
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10
摘要： The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
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公开(公告)号：US5861416A
公开(公告)日：1999-01-19
申请号：US795576
申请日：1997-02-06
IPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10 , A61K31/445 , C07D401/02
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10
摘要： The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
摘要翻译： 本发明涉及取代的吡咯烷基-3-基 - 烷基 - 哌啶，其立体异构体及其药学上可接受的盐及其制备方法。 本发明的化合物可用于其药理活性如速激肽拮抗作用，特别是P物质和神经激肽A拮抗作用等。 表示具有速激肽拮抗作用的化合物用于与神经源性炎症和本文所述的其它疾病相关的病症。
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公开(公告)号：US5661160A
公开(公告)日：1997-08-26
申请号：US487375
申请日：1995-06-07
IPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10 , A61K31/445
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10
摘要： The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
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4.发明授权Substituted 4-(1H-benzimidazol-2-yl-amino)piperidines useful for the treatment of allergic diseases 失效可用于治疗过敏性疾病的4-（1H-苯并咪唑-2-基 - 氨基）哌啶的取代基公开(公告)号：US06211199B1
公开(公告)日：2001-04-03
申请号：US09513846
申请日：1997-12-15
申请人： John M. Kane , George D. Maynard , Timothy P. Burkholder , Larry D. Bratton , Christopher R. Dalton , Braulio Santiago , Elizabeth M. Kudlacz
发明人： John M. Kane , George D. Maynard , Timothy P. Burkholder , Larry D. Bratton , Christopher R. Dalton , Braulio Santiago , Elizabeth M. Kudlacz
IPC分类号： A61K314523
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D405/14 , C07D409/14 , C07D487/04
摘要： The present invention relates to novel substituted piperidine derivatives of formula (1), stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
摘要翻译： 本发明涉及用作组胺受体拮抗剂和速激肽受体拮抗剂的式（1）的取代哌啶衍生物，其立体异构体及其可药用盐。 这种拮抗剂可用于治疗过敏性鼻炎，包括季节性鼻炎和鼻窦炎; 炎性肠病，包括克罗恩病和溃疡性结肠炎; 哮喘; 支气管炎; 和呕吐。
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公开(公告)号：US06316445B1
公开(公告)日：2001-11-13
申请号：US09648005
申请日：1999-05-06
IPC分类号： C07D40114
CPC分类号： C07D401/06 , C07D211/64 , C07D401/12 , C07D401/14 , C07D409/06
摘要： The present invention relates to novel carboxy substituted acyclic carboxamide derivatives of formula (1)): and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.
摘要翻译： 本发明涉及式（1））的新的羧基取代的无环羧酰胺衍生物：及其立体异构体及其药学上可接受的盐及其作为速激肽受体拮抗剂的用途。 这样的拮抗剂可用于治疗速激肽介导的疾病和本文公开的病症，包括：哮喘，咳嗽和支气管炎。
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公开(公告)号：US5977139A
公开(公告)日：1999-11-02
申请号：US971891
申请日：1997-11-17
IPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , A01N43/40
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to novel carboxy substituted cyclic carboxamide derivatives of formula (1), ##STR1## and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, coughs and bronchitis.
摘要翻译： 本发明涉及式（1）的新的羧基取代的环状甲酰胺衍生物及其立体异构体和药学上可接受的盐，以及它们作为速激肽受体拮抗剂的用途。 这样的拮抗剂可用于治疗速激肽介导的疾病和本文公开的病症，包括：哮喘，咳嗽和支气管炎。
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公开(公告)号：US5861417A
公开(公告)日：1999-01-19
申请号：US990672
申请日：1997-12-15
IPC分类号： C07D401/14 , C07D521/00 , A61K31/445
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14
摘要： The present invention relates to novel heterocyclic substituted pyrrolidine amide derivatives of formula (1), ##STR1## and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.
摘要翻译： 本发明涉及式（1），式（1）的新型杂环取代的吡咯烷酰胺衍生物及其立体异构体及其药学上可接受的盐，以及它们作为速激肽受体拮抗剂的用途。 这样的拮抗剂可用于治疗速激肽介导的疾病和本文公开的病症，包括：哮喘，咳嗽和支气管炎。
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公开(公告)号：US5824690A
公开(公告)日：1998-10-20
申请号：US798664
申请日：1997-02-11
IPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10 , C07D409/00
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10
摘要： The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
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公开(公告)号：US5635510A
公开(公告)日：1997-06-03
申请号：US332027
申请日：1994-10-31
IPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10 , A61K31/44 , A61K31/445
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D471/10
摘要： The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
摘要翻译： 本发明涉及取代的吡咯烷基-3-基 - 烷基 - 哌啶，其立体异构体及其药学上可接受的盐及其制备方法。 本发明的化合物可用于其药理活性，如速激肽拮抗作用，特别是P物质和神经激肽A拮抗作用等。 表示具有速激肽拮抗作用的化合物用于与神经源性炎症和本文所述的其它疾病相关的病症。
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![Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic disease](/abs-image/US/2001/02/27/US06194406B1/abs.jpg.150x150.jpg)
10.发明授权Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic disease 失效取代的4-（1H-苯并咪唑-2-基）[1,4]二氮杂环庚烷可用于治疗过敏性疾病公开(公告)号：US06194406B1
公开(公告)日：2001-02-27
申请号：US09513847
申请日：1997-10-29
申请人： John M. Kane , George D. Maynard , Timothy P. Burkholder , Larry D. Bratton , Christopher R. Dalton , Elizabeth M. Kudlacz , Braulio Santiago
发明人： John M. Kane , George D. Maynard , Timothy P. Burkholder , Larry D. Bratton , Christopher R. Dalton , Elizabeth M. Kudlacz , Braulio Santiago
IPC分类号： A61K31551
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
摘要翻译： 本发明涉及可用作组胺受体拮抗剂和速激肽受体拮抗剂的式（1）的新颖的4-（1H-苯并咪唑-2-基）[1,4]二氮杂环庚烷衍生物及其立体异构体及其药学上可接受的盐 。 这种拮抗剂可用于治疗过敏性鼻炎，包括季节性鼻炎和鼻窦炎; 炎性肠病，包括克罗恩病和溃疡性结肠炎; 哮喘; 支气管炎; 和呕吐。
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