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公开(公告)号：US06329392B1
公开(公告)日：2001-12-11
申请号：US09079924
申请日：1998-05-15
申请人： Timothy P. Burkholder , Larry D. Bratton , Elizabeth M. Kudlacz , George P. Maynard , John M. Kane , Braulio Santiago
发明人： Timothy P. Burkholder , Larry D. Bratton , Elizabeth M. Kudlacz , George P. Maynard , John M. Kane , Braulio Santiago
IPC分类号： A61K31445
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to novel substituted piperidine derivatives of the formula 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 diseases including: seasonal rhinitis, allergic rhinitis, and sinusitis.
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新颖的其取代的哌啶衍生物及其药物上可接受的盐。 这些拮抗剂可用于治疗过敏性疾病，包括季节性鼻炎，过敏性鼻炎和鼻窦炎。
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2.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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![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)
3.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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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：US5840726A
公开(公告)日：1998-11-24
申请号：US878695
申请日：1997-06-19
IPC分类号： A61K31/495 , A61P11/00 , A61P43/00 , C07D209/04 , C07D209/08 , C07D209/20 , C07D403/06 , C07D403/14 , C07D209/24
CPC分类号： C07D403/06 , C07D209/20 , C07D403/14
摘要： The present invention relates to substituted piperazinone derivatives (compounds of formula (1)) or stereoisomers, or 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. The present invention also relates to intermediates useful in the preparation of compounds of formula (1).
摘要翻译： 本发明涉及取代的哌嗪酮衍生物（式（1）的化合物）或其立体异构体或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。 本发明还涉及可用于制备式（1）化合物的中间体。
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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：US5597845A
公开(公告)日：1997-01-28
申请号：US262209
申请日：1994-06-20
IPC分类号： C07D309/12 , A61K31/215 , A61K31/35 , A61K31/351 , A61K31/403 , A61K31/404 , A61K31/405 , A61P11/00 , A61P43/00 , C07C211/27 , C07C211/29 , C07C211/30 , C07C223/02 , C07C227/18 , C07C229/36 , C07C233/78 , C07C237/20 , C07C237/52 , C07C271/20 , C07C271/22 , C07D209/14 , C07D209/20 , C07D209/18 , C07D407/06
CPC分类号： C07C271/22 , C07C233/78 , C07C237/20 , C07C237/52 , C07D209/20
摘要： The present invention relates to novel substituted alkyldiamine derivatives and pharmaceutically acceptable salts thereof which are useful tachykinin antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions including asthma, cough, and bronchitis.
摘要翻译： 本发明涉及新的取代烷基二胺衍生物及其药学上可接受的盐，它们是有效的速激肽拮抗剂。 这种拮抗剂可用于治疗速激肽介导的疾病和病症，包括哮喘，咳嗽和支气管炎。
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公开(公告)号：US5864045A
公开(公告)日：1999-01-26
申请号：US67386
申请日：1998-04-27
IPC分类号： A61K31/495 , A61P11/00 , A61P43/00 , C07D209/04 , C07D209/08 , C07D209/20 , C07D403/06 , C07D403/14
CPC分类号： C07D403/06 , C07D209/20 , C07D403/14
摘要： The present invention relates to substituted piperazinone derivatives of formula (1) or stereoisomers, or 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. The present invention also relates to intermediates useful in the preparation of compounds of formula (1).
摘要翻译： 本发明涉及式（1）的取代的哌嗪酮衍生物或其立体异构体或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。 本发明还涉及可用于制备式（1）化合物的中间体。
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公开(公告)号：US5672602A
公开(公告)日：1997-09-30
申请号：US640121
申请日：1996-04-30
IPC分类号： C07D241/04 , A61K31/50 , A61P1/00 , A61P1/08 , A61P11/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P27/02 , A61P27/14 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D241/08 , C07D309/12 , C07D403/06 , A61K31/495 , C07D403/04
CPC分类号： C07D403/06 , C07D241/08 , C07D309/12
摘要： The present invention relates to substituted piperazine derivatives (herein referred to as compounds or compounds of formula (1)) or stereoisomers, or 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： 本发明涉及取代的哌嗪衍生物（本文中称为化合物或式（1）的化合物）或其立体异构体或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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