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公开(公告)号：US5968929A
公开(公告)日：1999-10-19
申请号：US958896
申请日：1997-10-28
申请人： David J. Blythin , Xiao Chen , Richard J. Friary , Kevin D. McCormick , John J. Piwinski , Neng-Yang Shih , Ho-Jane Shue
发明人： David J. Blythin , Xiao Chen , Richard J. Friary , Kevin D. McCormick , John J. Piwinski , Neng-Yang Shih , Ho-Jane Shue
IPC分类号： C07D241/04 , C07D401/12 , C07D403/12 , C07D453/06 , C07D487/08 , A61K31/495 , A61K31/55 , C07D471/08
CPC分类号： C07D401/12 , C07D241/04 , C07D403/12 , C07D453/06 , C07D487/08
摘要： The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', l and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
摘要翻译： 本发明涉及下式化合物其中Z，Rc，y，m，u，Ar2，n，X，Rc'，l和Ar2如本文所述。 这些化合物是神经激肽拮抗剂。 这些化合物可用于治疗慢性气道疾病如哮喘。
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公开(公告)号：US5981520A
公开(公告)日：1999-11-09
申请号：US99221
申请日：1998-06-17
申请人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , Wing C. Tom , John J. Piwinski , Kevin D. McCormick
发明人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , Wing C. Tom , John J. Piwinski , Kevin D. McCormick
IPC分类号： C07D241/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D453/02 , C07D487/04 , C07D487/10 , A61K31/495 , C07D413/14
CPC分类号： C07D241/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D453/02 , C07D487/04 , C07D487/10
摘要： The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
摘要翻译： 本发明涉及式的化合物这些化合物是神经激肽拮抗剂。 这些化合物可用于治疗慢性气道疾病如哮喘。
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公开(公告)号：US5795894A
公开(公告)日：1998-08-18
申请号：US663880
申请日：1996-06-14
申请人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , Wing C. Tom , John J. Piwinski , Kevin D. McCormick
发明人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , Wing C. Tom , John J. Piwinski , Kevin D. McCormick
IPC分类号： C07D241/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D453/02 , C07D487/04 , C07D487/10 , A61K31/495
CPC分类号： C07D241/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D453/02 , C07D487/04 , C07D487/10
摘要： The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
摘要翻译： 本发明涉及下式的化合物这些化合物是神经激肽拮抗剂。 这些化合物可用于治疗慢性气道疾病如哮喘。
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公开(公告)号：US6051575A
公开(公告)日：2000-04-18
申请号：US313150
申请日：1999-05-17
申请人： David J. Blythin , Xiao Chen , Richard J. Friary , Kevin D. McCormick , John J. Piwinski , Neng-Yang Shih , Ho-Jane Shue
发明人： David J. Blythin , Xiao Chen , Richard J. Friary , Kevin D. McCormick , John J. Piwinski , Neng-Yang Shih , Ho-Jane Shue
IPC分类号： C07D241/04 , C07D401/12 , C07D403/12 , C07D453/06 , C07D487/08 , A61K31/496 , C07D409/14 , C07D417/14
CPC分类号： C07D401/12 , C07D241/04 , C07D403/12 , C07D453/06 , C07D487/08
摘要： The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', I and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
摘要翻译： 本发明涉及下式化合物其中Z，Rc，y，m，u，Ar2，n，X，Rc'，I和Ar2如本文所述。 这些化合物是神经激肽拮抗剂。 这些化合物可用于治疗慢性气道疾病如哮喘。
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公开(公告)号：US5892039A
公开(公告)日：1999-04-06
申请号：US706016
申请日：1996-08-30
申请人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , John J. Piwinski , Kevin D. McCormick
发明人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , John J. Piwinski , Kevin D. McCormick
IPC分类号： C07D487/08 , A61K31/40 , A61K31/439 , A61K31/46 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/4995 , A61K31/50 , A61K31/501 , A61K31/505 , A61P1/00 , A61P9/00 , A61P11/00 , A61P11/06 , A61P11/14 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/04 , C07D487/18 , C07D401/02
CPC分类号： C07D401/06 , C07D241/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D453/02 , C07D487/04
摘要： The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
摘要翻译： 本发明涉及下式的化合物这些化合物是神经激肽拮抗剂。 这些化合物可用于治疗慢性气道疾病如哮喘。
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公开(公告)号：US5869488A
公开(公告)日：1999-02-09
申请号：US703154
申请日：1996-08-29
申请人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , John J. Piwinski , Kevin D. McCormick
发明人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , John J. Piwinski , Kevin D. McCormick
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D453/02 , C07D487/04 , A61K31/495 , C07D403/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D453/02 , C07D487/04
摘要： The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', I and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
摘要翻译： 本发明涉及下式化合物其中Z，Rc，y，m，u，Ar2，n，X，Rc'，I和Ar2如本文所述。 这些化合物是神经激肽拮抗剂。 这些化合物可用于治疗慢性气道疾病如哮喘。
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公开(公告)号：US5840725A
公开(公告)日：1998-11-24
申请号：US901028
申请日：1997-07-25
申请人： Gregory A. Reichard , Robert G. Aslanian , Cheryl A. Alaimo , Michael P. Kirkup , Andrew Lupo, Jr. , Pietro Mangiaracina , Kevin D. McCormick , John J. Piwinski , Bandarpalle B. Shankar , Neng-Yang Shih , James M. Spitler , Pauline C. Ting , Ashit Ganguly , Nicholas I. Carruthers
发明人： Gregory A. Reichard , Robert G. Aslanian , Cheryl A. Alaimo , Michael P. Kirkup , Andrew Lupo, Jr. , Pietro Mangiaracina , Kevin D. McCormick , John J. Piwinski , Bandarpalle B. Shankar , Neng-Yang Shih , James M. Spitler , Pauline C. Ting , Ashit Ganguly , Nicholas I. Carruthers
IPC分类号： C07D295/12 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/439 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/45 , A61K31/451 , A61K31/452 , A61K31/4523 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P25/00 , A61P29/00 , A61P43/00 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/14 , C07D211/52 , C07D211/58 , C07D211/76 , C07D295/13 , C07D295/185 , C07D333/22 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D451/04 , C07D403/06
CPC分类号： C07D295/185 , C07D211/52 , C07D211/58 , C07D211/76 , C07D295/13 , C07D333/22 , C07D401/04 , C07D401/06 , C07D409/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Compound represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or3; b, d and e are independently 0, 1 or 2; R is H, C.sub.1-6 alkyl, --OH or C.sub.2 -C.sub.6 hydroxyalkyl; A is an optionally substituted oxime, hydrazone or olefin; X is a bond, --C(O)--, --O--, --NR.sup.6 --, --S(O)e--, --N(R.sup.6)C(O)--, --C(O)N(R.sup.6)-- --OC(O)NR.sup.6 --, --OC(.dbd.S)NR.sup.6 --, --N(R.sup.6)C(.dbd.S)O--, --C(.dbd.NOR.sup.1)--, --S(O).sub.2 N(R.sup.6)--, --N(R.sup.6)S(O).sub.2 --, --N(R.sup.6)C(O)O-- or --OC(O)--;T is H, phthalimidyl, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl; Q is --SR.sup.6, --N(R.sup.6)(R.sup.7), --OR.sup.6, phenyl, naphthyl or heteroaryl; R.sup.6a, R.sup.7a, R.sup.8a, R.sup.9a, R.sup.6 and R.sup.7 are H, C.sub.1-6 alkyl, C.sub.2 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl, phenyl or benzyl; or R.sup.6 and R.sup.7, together with the nitrogen to which they are attached, form a ring; R.sup.9a is R.sup.6 or --OR.sup.6 ; Z is morpholinyl, optionally N-substituted piperazinyl, optionally substituted ##STR2## or substituted ##STR3## g is 0-3 and h is 1-4, provided the sum of h and g is 1-7; wherein aryl, heterocycloalkyl, heteroaryl, cycloalkyl and bridged cycloalkyl groups are optionally substituted; methods of treating asthma, cough, bronchospasm, imflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
摘要翻译： 由结构式I表示的化合物或其药学上可接受的盐，其中：a是0,1,2或3; b，d和e独立地为0,1或2; R为H，C 1-6烷基，-OH或C 2 -C 6羟基烷基; A是任选取代的肟，腙或烯烃; X是键，-C（O） - ， - O - ， - NR 6 - ， - S（O）e - ， - N（R 6）C（O） - ， - OC（O）NR6-， - OC（= S）NR6-，-N（R6）C（= S）O-，-C（= NOR1） - ， - S（O） （R 6）S（O）2 - ， - N（R 6）C（O）O-或-OC（O） - ; T是H，苯偶酰亚氨基，芳基，杂环烷基，杂芳基，环烷基或桥连环烷基; Q是-SR 6，-N（R 6）（R 7），-OR 6，苯基，萘基或杂芳基; R6a，R7a，R8a，R9a，R6和R7是H，C1-6烷基，C2-C6羟基烷基，C1-C6烷氧基-C1-C6烷基，苯基或苄基; 或R 6和R 7与它们所连接的氮一起形成环; R9a为R6或-OR6; Z是吗啉基，任选取代的哌嗪基，任选取代的取代的或取代的，如果h和g之和为1-7，则g是0-3，h是1-4; 其中芳基，杂环烷基，杂芳基，环烷基和桥连环烷基任选被取代; 公开了用所述化合物治疗哮喘，咳嗽，支气管痉挛，炎性疾病和胃肠道疾病的方法，以及包含所述化合物的药物组合物。
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公开(公告)号：US07300941B2
公开(公告)日：2007-11-27
申请号：US10699189
申请日：2003-10-31
申请人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
发明人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
IPC分类号： A61K31/44
CPC分类号： C07D213/73 , A61K31/435 , A61K31/445 , A61K31/495 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.
摘要翻译： 公开的是式的新化合物还公开了包含式I化合物的药物组合物。还公开了治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻 拥塞）。还公开了使用组合式I化合物来治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻塞） 具有H 1受体拮抗剂。
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公开(公告)号：US06720328B2
公开(公告)日：2004-04-13
申请号：US09978267
申请日：2001-10-15
申请人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
发明人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
IPC分类号： C07D40114
CPC分类号： C07D213/73 , A61K31/435 , A61K31/445 , A61K31/495 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： Disclosed are novel compounds of the formula In Formula I, M1 is carbon, M2, M3 and M4 are carbon or nitrogen and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.
摘要翻译： 公开了式I的新化合物，式I中M 1是碳，M 2，M 3和M 4是碳或氮，其余的变量如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了使用式（I）的化合物治疗各种疾病或病症例如过敏，过敏诱发的气道反应和充血（例如，鼻塞）的方法 还公开了使用式I化合物与H1受体拮抗剂组合来治疗各种疾病或病症的方法，例如过敏，过敏诱导的气道反应和充血（例如，鼻塞）。
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公开(公告)号：US20080119487A1
公开(公告)日：2008-05-22
申请号：US11943315
申请日：2007-11-20
申请人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
发明人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
IPC分类号： A61K31/495 , A61K31/445 , A61K31/435 , A61P27/14 , A61P11/02
CPC分类号： C07D213/73 , A61K31/435 , A61K31/445 , A61K31/495 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.
摘要翻译： 公开的是式的新化合物还公开了包含式I化合物的药物组合物。还公开了治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻 拥塞）。还公开了使用组合式I化合物来治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻塞） 具有H 1受体拮抗剂。
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