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81. 发明授权

US08980889B2 Pyrazole derivative 有权
标题翻译：吡唑衍生物
公开(公告)号：US08980889B2
公开(公告)日：2015-03-17
申请号：US14477683
申请日：2014-09-04
申请人： Mochida Pharmaceutical Co., Ltd.
发明人： Akihiro Okano , Muneyoshi Makabe
IPC分类号： C07D498/02 , A61K31/535 , C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D403/04 , C07D417/04
摘要： It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.
摘要翻译：期望开发一种药物组合物，其用于预防和/或治疗与PDE10相关的各种疾病（例如精神障碍和神经变性障碍）的药剂中。本发明提供：具有PDE10抑制作用的化合物，特别是具有下式（I）表示的4-杂芳基吡唑-5-羧酸酰胺结构的化合物或其药学上可接受的盐或其溶剂合物; 药物组合物包含作为活性成分的化合物或其药学上可接受的盐或其溶剂合物; 化合物或其药学上可接受的盐或其溶剂化物的医疗用途。

82. 发明授权

US08980887B2 2-aryl imidazo[1,2-a]pyridine-3-acetamide derivatives, preparation methods and uses thereof 有权
标题翻译： 2-芳基咪唑并[1,2-a]吡啶-3-乙酰胺衍生物，其制备方法和用途
公开(公告)号：US08980887B2
公开(公告)日：2015-03-17
申请号：US13805967
申请日：2011-06-09
申请人： Rifang Yang , Yunfeng Li , Yongzhen Li , Nan Zhao , Liuhong Yun , Juanjuan Qin , Zhongyao Feng , Youzhi Zhang
发明人： Rifang Yang , Yunfeng Li , Yongzhen Li , Nan Zhao , Liuhong Yun , Juanjuan Qin , Zhongyao Feng , Youzhi Zhang
IPC分类号： A61K31/535 , C07D471/04
CPC分类号： C07D471/04
摘要： Disclosed are 2-arylimidazo[1,2-a]pyridine-3-acetamide derivatives represented by formula I, their tautomer, racemate or optical isomer, their pharmaceutically acceptable salt, or their solvates, wherein R1, R2, R3 and R4 are defined as in the specification. Preparation methods of said compounds and use of said compounds in treating and/or preventing central nervous system disease associated with TSPO functional disorder
摘要翻译：公开了由式I表示的2-芳基咪唑并[1,2-a]吡啶-3-乙酰胺衍生物，其互变异构体，外消旋物或旋光异构体，其药学上可接受的盐或其溶剂合物，其中R1，R2，R3和R4定义如说明书中所述。所述化合物的制备方法和所述化合物在治疗和/或预防与TSPO功能障碍相关的中枢神经系统疾病中的用途

83. 发明授权

US08969343B2 Histone demethylase inhibitors 有权
标题翻译：组蛋白脱甲基酶抑制剂
公开(公告)号：US08969343B2
公开(公告)日：2015-03-03
申请号：US14134989
申请日：2013-12-19
申请人： Quanticel Pharmaceuticals, Inc.
发明人： Toufike Kanouni , Jeffrey Alan Stafford , James Marvin Veal , Michael Brennen Wallace
IPC分类号： A61K31/535 , C07D401/00 , C07D405/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D471/04
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
摘要翻译：本发明一般涉及用于治疗癌症和肿瘤性疾病的组合物和方法。本文提供取代的3-氨基吡啶衍生物化合物，取代的3-氨基哒嗪衍生物化合物和包含所述化合物的药物组合物。主题化合物和组合物可用于抑制组蛋白去甲基化酶。此外，本发明化合物和组合物可用于治疗癌症，例如前列腺癌，乳腺癌，膀胱癌，肺癌和/或黑素瘤等。

84. 发明授权

US08969342B2 Compounds and methods for treating mammalian gastrointestinal microbial infections 有权
标题翻译：用于治疗哺乳动物胃肠道微生物感染的化合物和方法
公开(公告)号：US08969342B2
公开(公告)日：2015-03-03
申请号：US13257418
申请日：2010-03-22
申请人： Lizbeth K. Hedstrom , Gregory D. Cuny , Deviprasad R. Gollapalli , Boris Striepen , Suresh Kumar Gorla , Mandapati Kavitha
发明人： Lizbeth K. Hedstrom , Gregory D. Cuny , Deviprasad R. Gollapalli , Boris Striepen , Suresh Kumar Gorla , Mandapati Kavitha
IPC分类号： A61K31/535
CPC分类号： C07D401/12 , C07C233/15 , C07C235/24 , C07C235/38 , C07C237/20 , C07C255/60 , C07C275/28 , C07C275/30 , C07C275/42 , C07C309/15 , C07D209/08 , C07D209/12 , C07D209/30 , C07D215/38 , C07D235/26 , C07D237/32 , C07D249/06 , C07D263/56 , C07D263/57 , C07D295/192 , C07D401/04 , C07D401/14 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/08 , C07D491/052
摘要： Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
摘要翻译：本文描述了可用作IMPDH抑制剂的化合物及其药学上可接受的盐和前药。在某些实施方案中，本发明的化合物选择性地抑制寄生IMPDH相对于宿主IMPDH。此外，本发明提供包含一种或多种本发明化合物的药物组合物。本发明还涉及治疗哺乳动物中各种寄生虫和细菌感染的方法。此外，化合物可以单独使用或与其它治疗或预防剂如抗病毒剂，抗炎剂，抗微生物剂和免疫抑制剂组合使用。

85. 发明授权

US08962618B2 Inhibitors of diacylglycerol O-acyltransferase 1 (DGAT-1) and uses thereof 有权
标题翻译：二酰基甘油O-酰基转移酶1（DGAT-1）的抑制剂及其用途
公开(公告)号：US08962618B2
公开(公告)日：2015-02-24
申请号：US13458452
申请日：2012-04-27
申请人： K. Raja Reddy , Jeff Stebbins , Serge H. Boyer , Mark D. Erion , Scott J. Hecker , Nicholas Brian Raffaele , Brett C. Bookser , Venkat Reddy Mali
发明人： K. Raja Reddy , Jeff Stebbins , Serge H. Boyer , Mark D. Erion , Scott J. Hecker , Nicholas Brian Raffaele , Brett C. Bookser , Venkat Reddy Mali
IPC分类号： A61K31/54 , A61K31/535 , C07D513/00 , C07D265/36 , C07D498/02 , C07F9/6561 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61K45/06 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6574
CPC分类号： A61K31/675 , A61K31/52 , A61K31/542 , A61K31/662 , A61K31/665 , A61K31/683 , A61K31/688 , A61K45/06 , A61P3/04 , A61P3/10 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/303 , C07F9/3229 , C07F9/40 , C07F9/48 , C07F9/65312 , C07F9/6552 , C07F9/6561 , C07F9/65616 , C07F9/65742 , A61K2300/00
摘要： The invention pertains to the use of fused bicyclo heterocyclic adducts of thiohdroxy pridines or primidines as diacylglycerol O-acyltransferase 1 DGAT-1 inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
摘要翻译：本发明涉及硫代二羟基吡啶或嘧啶的稠合双环杂环加合物作为二酰基甘油O-酰基转移酶1（DGAT-1）抑制剂用于治疗高脂血症和与其相关的各种疾病和病症的用途。其他条件也可以被改善或避免，例如高餐后甘油三酸酯或饮食相关的高甘油三酯血症，与过量甘油三酯相关的心血管风险，以及超重患者，糖尿病患者或其他葡萄糖代谢紊乱如X综合征和胰岛素抵抗/葡萄糖不耐受 /或多囊卵巢疾病。

86. 发明授权

US08962609B2 Pyrimidine compounds as inhibitors of protein kinases IKK epsilon and/or TBK-1, processes for their preparation, and pharmaceutical compositions containing them 有权
标题翻译：嘧啶化合物作为蛋白激酶IKKε和/或TBK-1的抑制剂，其制备方法和含有它们的药物组合物
公开(公告)号：US08962609B2
公开(公告)日：2015-02-24
申请号：US13811164
申请日：2011-07-18
申请人： Trevor Robert Perrior , Gary Karl Newton , Mark Richard Stewart , Rehan Aqil
发明人： Trevor Robert Perrior , Gary Karl Newton , Mark Richard Stewart , Rehan Aqil
IPC分类号： A61K31/5377 , A61K31/535 , A61K31/497 , A61K31/505 , C07D401/12 , C07D401/14 , C07D413/14 , C07D403/10 , C07D417/10 , C07D403/14 , C07D239/42 , C07D403/12 , C07D417/14
CPC分类号： C07D403/10 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D417/14
摘要： C Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKKε and/or TBK-1: in which: R1 represents an aliphatic heterocyclyl group having 4, 5, 6 or 7 ring atoms, bonded to the phenyl group shown in formula I through a ring nitrogen atom, and optionally substituted by one or more substituents defined in the Specification; R2 represents a phenyl or heteroaryl group which is optionally substituted by one or more substituents defined in the Specification; and each of R3 and R4 independently represents a hydrogen atom or a C1-4 alkyl group.
摘要翻译： C通式（I）的化合物及其盐可用于治疗与蛋白激酶IKK＆egr异常活性相关的疾病; 和/或TBK-1：其中：R1表示具有4,5,6或7个环原子的脂族杂环基，其通过环氮原子与式I所示的苯基键合，并且任选地被一个或多个取代基在规范中定义; R 2表示任选被本说明书中定义的一个或多个取代基取代的苯基或杂芳基; R 3和R 4各自独立地表示氢原子或C 1-4烷基。

87. 再颁专利

USRE45323E1 Substituted piperidines as CCR3 antagonists 有权
标题翻译：取代的哌啶作为CCR3拮抗剂
公开(公告)号：USRE45323E1
公开(公告)日：2015-01-06
申请号：US14175082
申请日：2014-02-07
申请人： Marc Grundl , Horst Dollinger , Riccardo Giovannini , Christoph Hoenke , Matthias Hoffmann , Jan Kriegl , Domnic Martyres , Georg Rast , Peter Seither
发明人： Marc Grundl , Horst Dollinger , Riccardo Giovannini , Christoph Hoenke , Matthias Hoffmann , Jan Kriegl , Domnic Martyres , Georg Rast , Peter Seither
IPC分类号： A61K31/535 , A61K31/445 , C07D413/04 , C07D413/14 , C07D401/04 , C07D401/14
CPC分类号： C07D401/04 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/5355 , A61K31/56 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/14
摘要： Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明的目的是新的取代的式1化合物，其中A，R 1，R 2，R 3和R 4如描述中所定义。本发明的另一个目的是提供CCR3的拮抗剂，更具体地说是提供包含药用载体和治疗有效量的至少一种本发明化合物或其药学上可接受的盐的药物组合物。

88. 发明授权

US08927546B2 Therapeutic piperazines 有权
标题翻译：治疗性哌嗪
公开(公告)号：US08927546B2
公开(公告)日：2015-01-06
申请号：US12887920
申请日：2010-09-22
申请人： Alan P. Kaplan , Terence P. Keenan , Michael I. Weinhouse , Mark E. Wilson , Andrew K. Lindstrom , William C. Ripka , Mi Chen
发明人： Alan P. Kaplan , Terence P. Keenan , Michael I. Weinhouse , Mark E. Wilson , Andrew K. Lindstrom , William C. Ripka , Mi Chen
IPC分类号： A61K31/55 , A61K31/4965 , A61K31/497 , A61K31/535 , C07D243/08 , C07D295/092 , C07D413/06 , C07D401/06 , C07D403/06 , A61K45/06 , C07D417/06 , A61K31/5377 , C07D413/14 , C07D241/04 , A61K31/496 , A61K31/495 , A61K31/551
CPC分类号： C07D403/06 , A61K31/495 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D241/04 , C07D243/08 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/06 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , A61K2300/00
摘要： The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
摘要翻译：本发明包括式I化合物：其中R 1，Y，A，n，R 4和Z具有本文所述的任何值，以及这些化合物的盐，包含这些化合物的组合物，以及治疗方法，这样的化合物。这些化合物是PDE4功能的抑制剂，可用于改善认知功能和/或治疗动物，特别是人类的中枢和周围神经系统和/或精神疾病的认知障碍或损伤，创伤性和/或缺血性损伤。

89. 发明授权

US08916552B2 Pharmaceutical combinations 有权
标题翻译：药物组合
公开(公告)号：US08916552B2
公开(公告)日：2014-12-23
申请号：US12445180
申请日：2007-10-12
申请人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
发明人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
IPC分类号： A61K31/535 , A61K31/497 , A01N43/40 , A61K31/435 , A61K31/445 , A01N43/56 , A61K31/415 , A01N43/38 , A61K31/40 , C07D209/44 , A61K45/06 , A61K31/4035 , A61K31/403
CPC分类号： A61K31/403 , A61K31/4035 , A61K45/06 , A61K2300/00
摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase inhibitors.
摘要翻译：本发明提供包含（或基本上由）一种或多种辅助化合物和式（I）化合物或其盐，互变异构体，溶剂合物和N-氧化物的组合; 其中R1是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任意取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。这些组合具有作为Hsp90和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶抑制剂的活性。

90. 发明授权

US08906929B2 Inhibitors of human immunodeficiency virus replication 有权
公开(公告)号：US08906929B2
公开(公告)日：2014-12-09
申请号：US13959268
申请日：2013-08-05
申请人： Bristol-Myers Squibb Company
发明人： B. Narasimhulu Naidu , Manoj Patel , Stanley D'Andrea , Zhizhen Barbara Zheng , Timothy P. Connolly , David R. Langley , Kevin Peese , Zhongyu Wang , Michael A. Walker , John F. Kadow
IPC分类号： C07D471/04 , C07D471/22 , C07D487/04 , A61K31/535 , A01N37/18 , A61K38/00 , A61P31/18 , C07D267/22 , C07D491/22 , A61K31/5383 , A61K31/519 , C07D498/16 , C07D487/16 , A61K45/06 , C07D498/22
CPC分类号： A61K31/5383 , A61K31/519 , A61K45/06 , C07D487/16 , C07D491/22 , C07D498/16 , C07D498/22
摘要： The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

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