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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:US06528522B2
公开(公告)日:2003-03-04
申请号:US09954863
申请日:2001-09-18
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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公开(公告)号:US5990147A
公开(公告)日:1999-11-23
申请号:US186492
申请日:1998-11-05
申请人: Robert G. Aslanian
发明人: Robert G. Aslanian
IPC分类号: A61K31/4174 , C07D233/54 , C07D233/64 , A61K31/415
CPC分类号: C07D233/64 , A61K31/4174
摘要: Disclosed are novel phenyl-alkyl-imidazoles of the formula ##STR1## or pharmaceutically acceptable salts or solvates thereof, wherein A and R, are as defined in the specification.Also disclosed are methods of treating allergy, inflammation, hypotension, glaucoma, sleeping disorders, states of hyper and hypo motility of the gastrointestinal tract, hypo and hyperactivity of the central nervous system, Alzheimer's, schizophrenia, obesity and migraines, comprising administering an effective amount of a compound of formula I (or a salt or solvate thereof) to a patient in need of such treatment.Also disclosed are methods for treatment of upper airway allergic responses comprising administering a compound, or salt or solvate thereof, of formula I in combination or admixture with a histamine H.sub.1 receptor antagonist.
摘要翻译: 公开了下式的新型苯基 - 烷基 - 咪唑或其药学上可接受的盐或溶剂合物,其中A和R如说明书中所定义。 还公开了治疗过敏,炎症,低血压,青光眼,睡眠障碍,胃肠道过度和低运动状态,中枢神经系统的低血压和多动症,阿尔茨海默病,精神分裂症,肥胖症和偏头痛的方法,包括给予有效量 的式I化合物(或其盐或溶剂合物)给予需要这种治疗的患者。 还公开了治疗上呼吸道过敏反应的方法,包括与组胺H1受体拮抗剂组合或混合施用式I化合物或其盐或溶剂合物。
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公开(公告)号:US08283360B2
公开(公告)日:2012-10-09
申请号:US13139656
申请日:2009-12-18
申请人: Anandan Palani , Ashwin U. Rao , Xiao Chen , Ning Shao , Ying R. Huang , Robert G. Aslanian
发明人: Anandan Palani , Ashwin U. Rao , Xiao Chen , Ning Shao , Ying R. Huang , Robert G. Aslanian
IPC分类号: A61K31/437 , C07D498/04
CPC分类号: C07D513/04 , C07D498/04
摘要: The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
摘要翻译: 本发明涉及新型双环杂环衍生物,包含双环杂环衍生物的药物组合物和这些化合物用于治疗或预防治疗过敏,过敏诱发的气道反应,充血,心血管疾病,炎性疾病,胃肠道疾病 糖尿病,糖尿病并发症,葡萄糖耐量降低或空腹血糖受损。
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公开(公告)号:US20120238546A1
公开(公告)日:2012-09-20
申请号:US13378080
申请日:2010-06-15
IPC分类号: A61K31/553 , A61P25/28 , A61K31/551 , C07D498/04 , C07D471/04
CPC分类号: C07D498/04 , C07D471/04 , C07D513/04
摘要: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula (I): Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula (I).
摘要翻译: 本发明提供了作为γ分泌酶调节剂的新型化合物。 化合物具有式(I):还公开了使用式(I)的化合物调节γ-分泌酶活性的方法和治疗阿尔茨海默氏病的方法。
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公开(公告)号:US20120225885A1
公开(公告)日:2012-09-06
申请号:US13505801
申请日:2010-11-12
IPC分类号: A61K31/501 , A61K31/435 , A61K31/437 , C07D471/04 , A61P37/08 , A61P3/10 , A61P29/00 , A61P1/00 , A61P25/00 , A61P3/00 , A61P3/04 , A61K31/506 , A61P9/00
CPC分类号: C07D471/04 , A61K31/4025
摘要: The present invention relates to novel imidazole compounds, pharmaceutical compositions comprising the imidazole compounds and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below:
摘要翻译: 本发明涉及新的咪唑化合物,包含咪唑化合物的药物组合物和这些化合物用于治疗或预防过敏,使用过敏引起的气道反应,充血,心血管疾病,炎性疾病,胃肠道疾病,神经系统疾病 糖尿病,糖尿病并发症,葡萄糖耐量减低或空腹血糖受损。 本发明的说明性化合物如下所示:
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公开(公告)号:US20110182828A1
公开(公告)日:2011-07-28
申请号:US12736063
申请日:2008-12-18
申请人: John C. Anthes , Kevin D. Mccormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Phillippa H. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
发明人: John C. Anthes , Kevin D. Mccormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Phillippa H. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
IPC分类号: A61K31/58 , C07J43/00 , C07J9/00 , C07J41/00 , C07J71/00 , A61K31/573 , A61P17/00 , A61P37/08 , A61P11/10 , A61P11/02 , A61P31/00 , A61P29/00 , A61P37/06 , A61P31/12 , A61P37/02 , A61P17/06 , A61P17/04 , A61P27/02
CPC分类号: C07J43/003
摘要: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
摘要翻译: 本发明提供具有以下通式结构的式(I)化合物及其药学上可接受的盐,溶剂合物,酯,前体药物,互变异构体或异构体):其中L,R1,R2,R3,R4,R5和 R6彼此独立地选择并如本文所定义。 本发明还提供如本文定义的式II,III,IV,V和VI的化合物(和盐,溶剂合物,酯,前药,互变异构体和异构体)。 还提供了药物组合物,制备方法和使用这些化合物在治疗和预防广泛范围的免疫,自身免疫和炎性疾病和病症中的方法。
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公开(公告)号:US20110060006A1
公开(公告)日:2011-03-10
申请号:US12918427
申请日:2009-02-19
申请人: Junying Zheng , Jianhua Chao , Kevin D. McCormick , Robert G. Aslanian , Mwangi W. Muthai , Christopher W. Boyce , Walter S. Won
发明人: Junying Zheng , Jianhua Chao , Kevin D. McCormick , Robert G. Aslanian , Mwangi W. Muthai , Christopher W. Boyce , Walter S. Won
IPC分类号: A61K31/4709 , C07D401/06 , C07D403/08 , A61K31/4178 , A61P29/00 , A61P3/10 , A61P9/00 , A61P25/00 , A61P1/00 , A61P27/06 , A61P11/02 , C12N5/00
CPC分类号: C07D403/06 , C07D403/08
摘要: In its many embodiments, the present invention provides a novel class of heterocyclic derivatives as a2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要翻译: 在其许多实施方案中,本发明提供了一类新颖的杂环衍生物作为α2肾上腺素能受体激动剂,制备此类化合物的方法,含有一种或多种这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,以及方法 使用这些化合物或药物组合物治疗,预防,抑制或改善与α2肾上腺素能受体相关的一种或多种病症。
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公开(公告)号:US20100298372A1
公开(公告)日:2010-11-25
申请号:US12747001
申请日:2008-12-09
IPC分类号: A61K31/4375 , C07D455/02 , A61P25/28
CPC分类号: C07D455/02
摘要: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
摘要翻译: 本发明提供了作为γ分泌酶调节剂的新型化合物。 化合物具有式(I)。 还公开了使用式(I)的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。
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公开(公告)号:US20100249098A1
公开(公告)日:2010-09-30
申请号:US12680282
申请日:2008-09-25
申请人: Jianhua Chao , Robert G. Aslanian
发明人: Jianhua Chao , Robert G. Aslanian
IPC分类号: A61K31/4545 , A61K31/55 , A61K31/506 , A61K31/4725 , A61K31/4709 , C07D401/14 , C07D401/12 , A61P25/00 , C07D417/14 , A61P37/08 , A61P9/00 , A61P1/00 , A61P3/04 , A61P3/00
CPC分类号: C07D417/14 , C07D401/14
摘要: The present invention relates to novel Oxypiperidine Derivatives, pharmaceutical compositions comprising the Oxypiperidine Derivatives and the use of the Oxypiperidine Derivatives for treating or preventing treating allergy, an allergy-induced airway response, congestion, hypotension, a cardiovascular disease, a gastrointestinal disorder, obesity, a sleep disorder, pain, diabetes, a diabetic complication, impaired glucose tolerance, impaired fasting glucose or a central nervous system (CNS) disorder.
摘要翻译: 本发明涉及新的氧哌啶衍生物,包含氧哌啶衍生物的药物组合物和使用氧哌啶衍生物治疗或预防治疗过敏,过敏诱导的气道反应,充血,低血压,心血管疾病,胃肠道疾病,肥胖症, 睡眠障碍,疼痛,糖尿病,糖尿病并发症,葡萄糖耐量降低,空腹血糖受损或中枢神经系统(CNS)障碍。
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