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1.
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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2.
公开(公告)号:US5696267A
公开(公告)日:1997-12-09
申请号:US641384
申请日:1996-04-30
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 , C07D211/08
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 or 3;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).sub.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为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 - , - NR6 - , - S(O)e - , - N(R6)C(O) - , - (O)NR6-, - OC(= S)NR6-,-N(R6)C(= S)O-,-C(= NOR1) - , - S(O) R6)S(O)2 - , - N(R6)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: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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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:US07220735B2
公开(公告)日:2007-05-22
申请号:US10414943
申请日:2003-04-16
申请人: Pauline C. Ting , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Cao , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom , Qingbei Zeng
发明人: Pauline C. Ting , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Cao , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom , Qingbei Zeng
IPC分类号: A61K31/495
CPC分类号: C07D471/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要: Disclosed are novel compounds of the formula wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally substituted aryl or heteroaryl, and the remaining variables are as defined in the specification, and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.
摘要翻译: 公开了下式的新化合物其中R 1是苯并咪唑酮衍生物,M 1和M 2是任选取代的碳或氮,R SUP > 2 SUP>包括任选取代的芳基或杂芳基,其余变量如说明书中所定义,其余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和使用式I化合物治疗各种疾病或病症如过敏,过敏引起的气道反应和充血(例如,鼻塞)的方法,以及 使用式I化合物与H 1受体拮抗剂组合治疗所述疾病或病症。
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公开(公告)号:US07700592B2
公开(公告)日:2010-04-20
申请号:US11705673
申请日:2007-02-13
申请人: Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert G. Aslanian , Salem Fevrier , Bo Liang , Rong-qiang Liu , Ruiyan Liu , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Lisa Guise-Zawacki , Junying Zheng
发明人: Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert G. Aslanian , Salem Fevrier , Bo Liang , Rong-qiang Liu , Ruiyan Liu , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Lisa Guise-Zawacki , Junying Zheng
IPC分类号: C07D498/04 , A61K31/538
CPC分类号: C07D413/14 , C07D241/36 , C07D279/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D498/04
摘要: In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
摘要翻译: 在其许多实施方案中,本发明涉及可用作α2C肾上腺素能受体激动剂的新一类苯基吗啉和苯硫基吗啉化合物,含有该化合物的药物组合物,以及治疗,预防,抑制或改善一种或多种与 α2C肾上腺素能受体激动剂,使用这些化合物或药物组合物。
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公开(公告)号:US07803828B2
公开(公告)日:2010-09-28
申请号:US11508458
申请日:2006-08-23
申请人: Kevin D. McCormick , Christopher W. Boyce , Robert G. Aslanian , Neng-Yang Shih , Salem Fevrier , Pietro Mangiaracina , Chia-Yu Huang , Bo Liang , Rong-Qiang Liu , Huagang Lu
发明人: Kevin D. McCormick , Christopher W. Boyce , Robert G. Aslanian , Neng-Yang Shih , Salem Fevrier , Pietro Mangiaracina , Chia-Yu Huang , Bo Liang , Rong-Qiang Liu , Huagang Lu
IPC分类号: A01N43/50 , C07D233/00
CPC分类号: C07D403/02 , C07D401/06 , C07D403/06
摘要: In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要翻译: 在其许多实施方案中,本发明提供了作为α2C肾上腺素能受体激动剂抑制剂的新一类中和体,制备此类化合物的方法,含有一种或多种此类化合物的药物组合物,制备包含一种或多种此类化合物的药物制剂的方法,以及 使用这些化合物或药物组合物治疗,预防,抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。
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公开(公告)号:US07105505B2
公开(公告)日:2006-09-12
申请号:US10417391
申请日:2003-04-16
申请人: Qingbei Zeng , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Cao , Joseph A. Kozlowski , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom
发明人: Qingbei Zeng , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Jianhua Cao , Joseph A. Kozlowski , Pietro Mangiaracina , Kevin D. McCormick , Mwangi W. Mutahi , Stuart B. Rosenblum , Neng-Yang Shih , Daniel M. Solomon , Wing C. Tom
IPC分类号: A61K31/495
CPC分类号: C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: Disclosed are novel compounds of the formula wherein R1 is optionally substituted benzimidazolyl or a derivative thereof; R2 is optionally substituted aryl or heteroaryl; M1 and M2 are C(R3) or N; and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.
摘要翻译: 公开了下式的新化合物,其中R 1是任选取代的苯并咪唑基或其衍生物; R 2是任选取代的芳基或杂芳基; M 1和M 2是C(R 3)或N; 剩余的变量如规范中所定义; 还公开了包含式I化合物的药物组合物和使用式I化合物治疗各种疾病或病症如过敏,过敏引起的气道反应和充血(例如,鼻塞)的方法,以及 使用式I化合物与H 1受体拮抗剂组合治疗所述疾病或病症。
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公开(公告)号:US07985748B2
公开(公告)日:2011-07-26
申请号:US12722879
申请日:2010-03-12
申请人: Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Robert G. Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
发明人: Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Robert G. Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
IPC分类号: C07D413/06 , A61K31/538
CPC分类号: C07D413/06 , C07D403/06 , C07D413/04 , C07D413/14 , C07D417/06 , C07D471/04 , C07D487/04 , C07D498/04
摘要: In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
摘要翻译: 在其许多实施方案中,本发明涉及可用作α2C肾上腺素能受体激动剂的新一类苯基吗啉和苯硫基吗啉化合物,含有该化合物的药物组合物,以及治疗,预防,抑制或改善一种或多种与 α2C肾上腺素能受体激动剂,使用这些化合物或药物组合物。
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