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1. 发明授权

US5578616A Phenyl-alkyl-imidazoles 失效
标题翻译：苯基 - 烷基 - 咪唑
公开(公告)号：US5578616A
公开(公告)日：1996-11-26
申请号：US469941
申请日：1995-06-06
申请人： Robert G. Aslanian , Michael J. Green , Neng-Yang Shih
发明人： Robert G. Aslanian , Michael J. Green , Neng-Yang Shih
IPC分类号： C07D233/64 , A61K31/415 , A61P9/00 , A61P25/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D233/54 , C07D401/12 , A61K31/44 , C07D401/10
CPC分类号： C07D233/64 , C07D401/12
摘要： The invention provides novel phenyl-alkyl-imidazoles of the formula ##STR1## wherein A, R.sup.1, R.sup.2, m and n are as defined in the specification, and the group --(CH.sub.2)n--A--R.sup.1 is at the 3- or 4-position, together with their pharmaceutically acceptable salts. These phenyl-alkyl-imidazoles and salts have valuable pharmacological properties, especially CNS activities and activity against inflammatory disease.
摘要翻译：本发明提供了新的式（Ⅰ）所示的苯基 - 烷基 - 咪唑，其中A，R 1，R 2，m和n如说明书中所定义，基团 - （CH 2）n -A-R 1在3-或4- - 位，以及其药学上可接受的盐。这些苯基 - 烷基 - 咪唑和盐具有有价值的药理学性质，特别是CNS活性和抗炎性疾病的活性。

2. 发明授权

US07803828B2 Functionally selective alpha2C adrenoreceptor agonists 有权
标题翻译：功能选择性α2C肾上腺素受体激动剂
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。

3. 发明申请

US20080119487A1 NOVEL NON-IMIDAZOLE COMPOUNDS 审中-公开
标题翻译：新型非咪唑化合物
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。

4. 发明授权

US07220735B2 Benzimidazolone histamine H3 antagonists 失效
标题翻译：苯并咪唑酮组胺H3拮抗剂
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 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。

5. 发明授权

US06849621B2 Piperidine compounds 失效
标题翻译：哌啶化合物
公开(公告)号：US06849621B2
公开(公告)日：2005-02-01
申请号：US10095134
申请日：2002-03-11
申请人： Stuart B. Rosenblum , Qingbei Zeng , Mwangi Wa Mutahi , Robert G. Aslanian , Pauline C. Ting , Neng-Yang Shih , Daniel M. Solomon , Jianhua Cao , Henry A. Vaccaro , Kevin D. McCormick , John J. Baldwin , Ge Li
发明人： Stuart B. Rosenblum , Qingbei Zeng , Mwangi Wa Mutahi , Robert G. Aslanian , Pauline C. Ting , Neng-Yang Shih , Daniel M. Solomon , Jianhua Cao , Henry A. Vaccaro , Kevin D. McCormick , John J. Baldwin , Ge Li
IPC分类号： C07D211/34 , A61K31/496 , A61P1/00 , A61P1/04 , A61P3/04 , A61P9/00 , A61P9/04 , A61P11/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/28 , A61P37/08 , A61P43/00 , C07D211/26 , C07D211/38 , C07D211/62 , C07D211/96 , C07D243/08 , C07D401/06 , C07D401/14 , C07D405/14 , C07D407/12 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D451/02 , C07D487/06 , A61K31/4545 , C07D403/06
CPC分类号： C07D401/14 , C07D211/26 , C07D211/38 , C07D211/62 , C07D211/96 , C07D243/08 , C07D401/06 , C07D407/12 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D451/02 , C07D487/06
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 H. receptor antagonist.
摘要翻译：所公开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，鼻充血）。还公开了使用式I化合物与下列化合物组合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） H.受体拮抗剂。

6. 发明授权

US07700592B2 α2C adrenoreceptor agonists 失效
标题翻译： α2C肾上腺素受体激动剂
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。

7. 发明授权

US07238688B2 Piperidine compounds 失效
标题翻译：哌啶化合物
公开(公告)号：US07238688B2
公开(公告)日：2007-07-03
申请号：US10974329
申请日：2004-10-27
申请人： Stuart B. Rosenblum , Qingbei Zeng , Mwangi Wa Mutahi , Robert G. Aslanian , Pauline C. Ting , Neng-Yang Shih , Daniel M. Solomon , Jianhua Cao , Henry A. Vaccaro , Kevin D. McCormick , John J. Baldwin , Ge Li
发明人： Stuart B. Rosenblum , Qingbei Zeng , Mwangi Wa Mutahi , Robert G. Aslanian , Pauline C. Ting , Neng-Yang Shih , Daniel M. Solomon , Jianhua Cao , Henry A. Vaccaro , Kevin D. McCormick , John J. Baldwin , Ge Li
IPC分类号： A61K31/55 , C07D243/08 , C07D241/02 , C07D401/06 , C07D403/06
CPC分类号： C07D401/14 , C07D211/26 , C07D211/38 , C07D211/62 , C07D211/96 , C07D243/08 , C07D401/06 , C07D407/12 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D451/02 , C07D487/06
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。

8. 发明授权

US5945428A Substituted oximes, hydrazones and olefins as neurokinin antagonists 失效
标题翻译：取代的肟，腙和烯烃作为神经激肽拮抗剂
公开(公告)号：US5945428A
公开(公告)日：1999-08-31
申请号：US960724
申请日：1997-10-30
申请人： Neng-Yang Shih , Gregory A. Reichard , Robert G. Aslanian
发明人： Neng-Yang Shih , Gregory A. Reichard , Robert G. Aslanian
IPC分类号： C07D471/10 , A61K31/44 , C07D221/00
CPC分类号： C07D471/10
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 ; andZ is spiro-substituted piperidinyl or substituted piperazinyl 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 - ， - 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是螺取代的哌啶基或取代的哌嗪基，其中芳基，杂环烷基，杂芳基，环烷基和桥连的环烷基任选被取代; 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。

9. 发明授权

US07105505B2 Benzimidazole derivatives useful as histamine H3 antagonists 失效
标题翻译：可用作组胺H3拮抗剂的苯并咪唑衍生物
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。

10. 发明授权

US06528522B2 Substituted imidazoles as dual histamine H1 and H3 agonists or antagonists 失效
公开(公告)号：US06528522B2
公开(公告)日：2003-03-04
申请号：US09954863
申请日：2001-09-18
申请人： Neng-Yang Shih , Robert G. Aslanian , John J. Piwinski , Andrew T. Lupo, Jr. , Adriano Afonso
发明人： Neng-Yang Shih , Robert G. Aslanian , John J. Piwinski , Andrew T. Lupo, Jr. , Adriano Afonso
IPC分类号： A61K31435
CPC分类号： C07D401/12 , C07D401/14
摘要： The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.

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