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61. 发明授权

US6103735A Composition and method for treating allergic diseases 有权
标题翻译：用于治疗过敏性疾病的组合物和方法
公开(公告)号：US6103735A
公开(公告)日：2000-08-15
申请号：US412621
申请日：1999-10-06
申请人： Robert G. Aslanian , John J. Piwinski
发明人： Robert G. Aslanian , John J. Piwinski
IPC分类号： A61K45/06 , A61K31/44 , A61K31/415 , A61K31/445
CPC分类号： A61K45/06
摘要： The present invention is directed towards a pharmaceutical composition useful for the treatment of allergic rhinitis, asthma and related disorders. In one embodiment, the composition comprises, in combination, a therapeutically effective amount of at least one neurokinin antagonist, a therapeutically effective amount of at least one H.sub.3 antagonist and a therapeutically effective amount of at least one H.sub.1 antagonist.
摘要翻译：本发明涉及可用于治疗过敏性鼻炎，哮喘和相关疾病的药物组合物。在一个实施方案中，组合物组合包含治疗有效量的至少一种神经激肽拮抗剂，治疗有效量的至少一种H3拮抗剂和治疗有效量的至少一种H1拮抗剂。

62. 发明授权

US06034251A Phenyl-alkyl-imidazoles 失效
标题翻译：苯基 - 烷基 - 咪唑
公开(公告)号：US06034251A
公开(公告)日：2000-03-07
申请号：US185972
申请日：1998-11-05
申请人： Robert G. Aslanian , Kevin D. McCormick , John J. Piwinski
发明人： Robert G. Aslanian , Kevin D. McCormick , John J. Piwinski
IPC分类号： C07D233/54 , C07D233/60 , C07D233/61 , C07D233/90 , A61K31/415
CPC分类号： C07D233/64
摘要： Disclosed are novel phenyl-alkyl-imidazoles of the formula ##STR1## wherein R.sup.1, R.sup.7, m, n, p, q, X, Y, Z, R and R.sup.15 are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Further 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 by administering compounds of formula I.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：其中R1，R7，m，n，p，q，X，Y，Z，R和R15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。进一步公开的是治疗过敏，炎症，低血压，青光眼，睡眠障碍，胃肠道超低运动状态，中枢神经系统低血压和多动症，阿尔茨海默病，精神分裂症，肥胖症和偏头痛。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。

63. 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。

64. 发明授权

US5789422A Substituted arylalkylamines as neurokinin antagonists 失效
标题翻译：取代的芳基烷基胺作为神经激肽拮抗剂
公开(公告)号：US5789422A
公开(公告)日：1998-08-04
申请号：US742606
申请日：1996-10-28
申请人： Gregory A. Reichard , Robert G. Aslanian
发明人： Gregory A. Reichard , Robert G. Aslanian
IPC分类号： C07D211/52 , A61K31/445 , C07D211/22
CPC分类号： C07D211/52
摘要： Compounds represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof are disclosed, wherein: A.sup.1 is --CH.sub.2 R.sup.6, --OR.sup.6, --N(R.sup.6)(R.sup.7), --S(O).sub.e R.sup.13, --(C(R.sup.6)(R.sup.7)).sub.1-6 --OR.sup.6, --(C(R.sup.6)(R.sup.7).sub.1-6 --N(R.sup.6)(R.sup.7) or --(C(R.sup.6) (R.sup.7)).sub.1-6 --S(O).sub.e R.sup.13 and A.sup.2 is H, or A.sup.1 and A.sup.2 together are .dbd.O, .dbd.C(R.sup.6)(R.sup.7), .dbd.NOR.sup.6 or .dbd.S; Q is phenyl, naphthyl, --SR.sup.6, --N(R.sup.6)(R.sup.7), --OR.sup.6 or heteroaryl; T is H, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl; b is 0, 1 or 2; b.sub.1 is 1 or 2; 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.6)--, --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)--; R.sup.6, R.sup.7, R.sup.8a, and R.sup.13 are H, alkyl, hydroxyalkyl, alkoxy 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.9 and R.sup.9a independently are R.sup.6 or --OR.sup.6 ; Z is optionally substituted ##STR2## wherein g is 0-3 and h is 1-4, provided the sum of h and g is 1-7; wherein the aryl, phenyl, benzyl, naphthyl, heterocycloalkyl and heteroaryl 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：公开了由结构式“IMAGE”表示的化合物或其药学上可接受的盐，其中：A1是-CH2R6，-OR6，-N（R6）（R7），-S（O）eR13， - （C（R6）（R 6）（R 7）） - （C（R 6）（R 7））1-6-S（O）e R 13 并且A2是H，或者A1和A2一起是= O，= C（R6）（R7），= NOR6或= S; Q是苯基，萘基，-SR6，-N（R6）（R7）杂芳基; T为H，芳基，杂环烷基，杂芳基，环烷基或桥连环烷基; b为0,1或2; b1为1或2; X为键，-C（O） - ， - O - ，-S（O）e - ， - N（R 6）C（O） - ， - C（O）N（R 6） - ， - OC（O）NR 6 - ， - OC（= S）NR 6 - ， - （R6）C（= S）O-，-C（= NOR6） - ， - S（O）2N（R6） - ， - N（R6））O-或-OC（O） - ; R6，R7，R8a和R13是H，烷基，羟基烷基，烷氧基烷基，苯基或苄基;或R6和R7与它们所连接的氮一起形成 R 9和R 9a独立地是R 6或-OR 6; Z是任选取代的，其中g是0-3且h是1-4，条件是h和g之和是1-7;其中芳基，苯基，苄基，萘羟基，杂环烷基和杂芳基任选被取代。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。

65. 发明授权

US08524697B2 C20-C21 substituted glucocorticoid receptor agonists 失效
标题翻译： C20-C21取代的糖皮质激素受体激动剂
公开(公告)号：US08524697B2
公开(公告)日：2013-09-03
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 , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar , Phillippa H. Solomon
发明人： John C. Anthes , Kevin D. McCormick , John A. Hey , Robert G. Aslanian , Purakkattle J. Biju , Michael Y. Berlin , Daniel M. Solomon , Hongwu Yang , Yeon-Hee Lim , Yoon Joo Lee , Rema Danielle Bitar
IPC分类号： A01N43/00 , A61K31/33 , C07D215/00 , C07D277/62
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。

66. 发明授权

US08470863B2 Derivatives and analogs of chroman as functionally selective ALPHA2C adrenoreceptor agonists 失效
标题翻译：色氨酸的衍生物和类似物作为功能选择性ALPHA2C肾上腺素受体激动剂
公开(公告)号：US08470863B2
公开(公告)日：2013-06-25
申请号：US12525646
申请日：2008-02-11
申请人： Junying Zheng , Kevin D. McCormick , Jianhua Chao , Christopher W. Boyce , Robert G. Aslanian , Younong Yu
发明人： Junying Zheng , Kevin D. McCormick , Jianhua Chao , Christopher W. Boyce , Robert G. Aslanian , Younong Yu
IPC分类号： A61K31/4178 , C07D233/64
CPC分类号： C07D405/06 , C07D405/08 , C07D405/14 , C07D409/06 , C07D417/14 , C07D491/052
摘要： In its many embodiments, the present invention provides a novel class of chroman compounds of formula I as α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of prepaxing 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. wherein J is: Z is —[C(Rc)(Rc)]x—, where x is 1, 2, or 3.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的式I的色满化合物作为α2C肾上腺素能受体激动剂，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，包含一种或多种这类化合物的药物制剂的制备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。其中J为：Z为 - [C（Rc）（Rc）] x-，其中x为1,2或3。

67. 发明授权

US08232274B2 Pyridazinone derivatives useful as glucan synthase inhibitors 有权
标题翻译：用作葡聚糖合酶抑制剂的哒嗪酮衍生物
公开(公告)号：US08232274B2
公开(公告)日：2012-07-31
申请号：US12046755
申请日：2008-03-12
申请人： Pauline C. Ting , Robert G. Aslanian , Jianhua Cao , David Won-Shik Kim , Rongze Kuang , Gang Zhou , Robert Jason Herr , Andrew John Zych , Jinhai Yang , Heping Wu , Nicolas Zorn
发明人： Pauline C. Ting , Robert G. Aslanian , Jianhua Cao , David Won-Shik Kim , Rongze Kuang , Gang Zhou , Robert Jason Herr , Andrew John Zych , Jinhai Yang , Heping Wu , Nicolas Zorn
IPC分类号： A61K31/501 , A61K31/5377 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D413/14 , A61P31/00
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D515/22
摘要： Disclosed is a set of compounds useful as glucan synthase inhibitors having the generic structure of Formula I: wherein the various moieties A, D, R6, etc., are as defined in the specification. These compounds are useful in treating or preventing fungal infections in a patient.
摘要翻译：公开了一组可用作具有式I的通式结构的葡聚糖合酶抑制剂的化合物：其中各个部分A，D，R 6等如说明书中所定义。这些化合物可用于治疗或预防患者的真菌感染。

68. 发明申请

US20120171126A1 NOVEL [3,2-c] HETEROARYL STEROIDS AS GLUCOCORTICOID RECEPTOR AGONISTS COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：新型[3,2-c]异烟肼作为葡萄糖激素受体激动剂组合物及其用途
公开(公告)号：US20120171126A1
公开(公告)日：2012-07-05
申请号：US13378893
申请日：2010-06-15
申请人： Biju J. Purakkattle , Michael Y. Berlin , Yeon-Hee Lim , Rema D. Bitar , Kevin D. McCormick , Robert G. Aslanian , Yoon Joo Lee , Junying Zheng , Ying Huang , Walter Won
发明人： Biju J. Purakkattle , Michael Y. Berlin , Yeon-Hee Lim , Rema D. Bitar , Kevin D. McCormick , Robert G. Aslanian , Yoon Joo Lee , Junying Zheng , Ying Huang , Walter Won
IPC分类号： A61K31/58 , A61K9/12 , A61P37/00 , A61P29/00 , A61P17/00 , A61P17/06 , A61P17/04 , A61P11/06 , A61P11/02 , A61P11/08 , A61P11/00 , A61P1/00 , A61P1/04 , A61P25/00 , A61P27/02 , C07J71/00
CPC分类号： C07J71/0047 , C07J71/0063
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: Formula (I) 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 (H-A), (II-A1), (II-A2), (II-A2.1), (ll-A-2.2), (ll-A-2.3), (II-A4), (H-B), (H-C), (III), (IV), (V), (VI), as described 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 R 5和R 6彼此独立地选择并如本文所定义。本发明还提供式（IIa），（Ⅱ-A1），（Ⅱ-A2），（Ⅱ-A2.1），（Ⅱ-A2）的化合物（和盐，溶剂合物，酯，前体药物，互变异构体和异构体）（II-A-2.3），（II-A4），（HB），（HC），（III），（IV），（V），（VI）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。

69. 发明申请

US20120022057A1 BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYGLYCEROL ACYLTRANSFERASE 审中-公开
标题翻译：双酚化合物作为抑制剂的双环化合物
公开(公告)号：US20120022057A1
公开(公告)日：2012-01-26
申请号：US13256468
申请日：2010-03-16
申请人： Gang Zhou , Grant Wishart , Pauline C. Ting , Robert G. Aslanian , Nicolas Zorn , Jianhua Cao
发明人： Gang Zhou , Grant Wishart , Pauline C. Ting , Robert G. Aslanian , Nicolas Zorn , Jianhua Cao
IPC分类号： A61K31/538 , C07D403/06 , C07D265/36 , C07D241/38 , C07D215/50 , C07D209/42 , C07D401/06 , C07D413/06 , C07D405/12 , C07D401/12 , C07D417/12 , C07D215/233 , A61K31/404 , A61K31/498 , A61K31/47 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/4178 , A61K31/4709 , A61P3/04 , A61P3/00 , A61P3/10 , C07D209/08
CPC分类号： C07D209/08 , C07D215/50 , C07D217/04 , C07D231/54 , C07D239/84 , C07D241/42 , C07D243/14 , C07D265/36 , C07D401/06 , C07D403/06 , C07D403/12 , C07D413/04 , C07D498/04
摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).
摘要翻译：本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖症或肥胖相关障碍的化合物的用途，糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。本发明的说明性化合物如下（I）所示。

70. 发明授权

US07985748B2 ALPHA2C adrenoreceptor agonists 失效
标题翻译： ALPHA2C肾上腺素受体激动剂
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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