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51. 发明授权

US08835420B2 Azaindole derivatives 有权
标题翻译： Azaindole衍生物
公开(公告)号：US08835420B2
公开(公告)日：2014-09-16
申请号：US13937081
申请日：2013-07-08
申请人： Takeda Pharmaceutical Company Limited
发明人： Edcon Chang , Wolfgang Reinhard Ludwig Notz , Michael B. Wallace
IPC分类号： A61K31/395 , A61K31/535 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/505 , C07D413/14 , C07D487/04 , C07D473/02 , C07D403/12 , C07D519/00 , A61K31/5377 , C07D491/107 , A61K45/06 , A61K31/506 , C07D471/04
CPC分类号： C07D491/107 , A61K31/506 , A61K31/519 , A61K31/52 , A61K31/5377 , A61K45/06 , C07D471/04 , C07D473/16 , C07D487/04 , C07D519/00
摘要： Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3Kδ.
摘要翻译：公开了式1的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10在说明书中定义。本公开还涉及制备式1化合物的材料和方法，含有它们的药物组合物及其用于治疗与PI3Kδ相关的免疫学疾病，心血管疾病，癌症和其它疾病，病症或病症的用途。

52. 发明授权

US08697868B2 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions 有权
标题翻译： 8- [3-氨基 - 哌啶-1-基] - 黄嘌呤，它们的制备及其作为药物组合物的用途
公开(公告)号：US08697868B2
公开(公告)日：2014-04-15
申请号：US12360392
申请日：2009-01-27
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Mohammad Tadayyon , Leo Thomas
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Mohammad Tadayyon , Leo Thomas
IPC分类号： C07D473/00 , C07D473/02 , C07D473/04
CPC分类号： C07D473/04
摘要： Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：公开了下式的取代黄嘌呤：其中R如权利要求1所定义，互变异构体，立体异构体，其混合物及其盐具有有价值的药理学性质，特别是对二肽基肽酶-IV酶活性的抑制作用 DPP-IV）。

53. 发明申请

US20110028715A1 NOVEL ADENINE COMPOUND 审中-公开
标题翻译：新颖的化合物
公开(公告)号：US20110028715A1
公开(公告)日：2011-02-03
申请号：US12905012
申请日：2010-10-14
申请人： Yoshiaki ISOBE , Tomoaki NAKAMURA
发明人： Yoshiaki ISOBE , Tomoaki NAKAMURA
IPC分类号： C07D401/14 , C07D473/02 , C07D413/14
CPC分类号： C07D473/24 , C07D473/00 , C07D473/16 , C07D473/18 , C07D473/34
摘要： A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straightened or branched alkylene, etc.; R1 represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R2 and R3 each independently represents hydrogen, or (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted saturated heterocycle, (un)substituted aryl, or (un)substituted heteroaryl, or R2 combines together with L2 or R3 to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO2, NR7, NR7CO wherein R7 is hydrogen or alkyl, or a single bond; provided that X is a single bond when R1 is halogen, or a pharmaceutically acceptable salt thereof. The compound and salt are useful as a medicine.
摘要翻译：由式（1）表示的新型腺嘌呤化合物：其中A表示（un）取代的芳族碳环或（un）取代的芳族杂环; L1和L2各自独立地表示直链或支链亚烷基等; R 1表示卤素，（未）取代的烷基，（未）取代的烯基，（未）取代的炔基，（未）取代的环烷基，（未）取代的芳基或（未）取代的杂芳基; R2和R3各自独立地表示氢，或（未）取代的烷基，（未）取代的烯基，（未）取代的炔基，（未）取代的环烷基，（未）取代的饱和杂环，（未）取代的芳基或（未）或R 2与L 2或R 3一起形成（未）取代的4-至8-元含氮饱和杂环; X是氧，硫，SO，SO 2，NR 7，NR 7 CO，其中R 7是氢或烷基，或单键; 条件是当R 1为卤素时X为单键，或其药学上可接受的盐。化合物和盐可用作药物。

54. 发明申请

US20100016578A1 MACROCYCLIC SERINE PROTEASE INHIBITORS 有权
标题翻译：大肠杆菌丝氨酸蛋白酶抑制剂
公开(公告)号：US20100016578A1
公开(公告)日：2010-01-21
申请号：US12563072
申请日：2009-09-18
申请人： Christophe Claude Parsy , Francois-Rene Alexandre , Dominique Surleraux , Michel Derock , Frederic Leroy
发明人： Christophe Claude Parsy , Francois-Rene Alexandre , Dominique Surleraux , Michel Derock , Frederic Leroy
IPC分类号： C07D487/04 , C07D401/04 , C07D207/16 , C07D471/04 , C07D473/02 , C07D417/14
CPC分类号： C07D487/08
摘要： Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
摘要翻译：本文提供了大环丝氨酸蛋白酶抑制剂化合物，例如式I，包含该化合物的药物组合物及其制备方法。还提供了它们用于在有需要的宿主中治疗HCV感染的方法。

55. 发明授权

US07495006B2 2′ and 3′-substituted cyclobutyl nucleoside analogs for the treatment of viral infections and abnormal cellular proliferation 有权
标题翻译： 2'和3'-取代的环丁基核苷类似物用于治疗病毒感染和异常细胞增殖
公开(公告)号：US07495006B2
公开(公告)日：2009-02-24
申请号：US11301326
申请日：2005-12-08
申请人： Dennis C. Liotta , Shuli Mao , Michael Hager
发明人： Dennis C. Liotta , Shuli Mao , Michael Hager
IPC分类号： A61K31/505 , A61K31/506 , A61K31/513 , A61K31/52 , A61K31/522 , C07F9/113 , C07F9/117 , C07D239/47 , C07D239/48 , C07D473/02 , C07D473/04 , C07D473/18 , C07D473/26 , C07D473/32 , C07D473/34
CPC分类号： C07H19/06 , C07H19/16
摘要： Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.
摘要翻译：提供的环丁基核苷及其用于治疗感染的方法，包括逆转录病毒科（包括HIV），肝炎病毒科（包括HBV）或黄病毒科（包括BVDV和HCV）感染或与异常细胞增殖有关的病症，包括动物，特别是人类。

56. 发明申请

US20080064705A1 Theophylline-based nitophenylpiperazine derivatives for enhancing aortic smooth muscle relaxation 审中-公开
标题翻译：基于茶碱的硝基苯基哌嗪衍生物，用于增强主动脉平滑肌松弛
公开(公告)号：US20080064705A1
公开(公告)日：2008-03-13
申请号：US11520174
申请日：2006-09-12
申请人： Ing-Jun Chen
发明人： Ing-Jun Chen
IPC分类号： A61K31/522 , C07D473/02
CPC分类号： A61K31/522 , C07D473/08
摘要： A substance for enhancing an aortic smooth muscle relaxation is provided. The substance is one selected from the group consisting of a compound of formula (I), a pharmaceutical acceptable therefrom and a solvate therefrom, wherein either of R1 and R2 is one of a hydrogen and a nitro group.
摘要翻译：提供了用于增强主动脉平滑肌松弛的物质。该物质是选自式（I）化合物，其可接受药物和其溶剂化物的化合物，其中R1和R2中的任一个是氢和硝基之一。

57. 发明申请

US20070282104A1 METHOD FOR PRODUCING NUCLEOSIDE DERIVATIVES 失效
标题翻译：生产核苷衍生物的方法
公开(公告)号：US20070282104A1
公开(公告)日：2007-12-06
申请号：US11782695
申请日：2007-07-25
申请人： Satoji TAKAHASHI , Mitsuhiko Kojima , Shouichi Kondou , Tatsuya Ishikawa , Yoshinori Ogawa
发明人： Satoji TAKAHASHI , Mitsuhiko Kojima , Shouichi Kondou , Tatsuya Ishikawa , Yoshinori Ogawa
IPC分类号： C07D473/02 , C07D473/10
CPC分类号： C12P17/182 , C07D473/30 , C07D473/34 , Y02P20/55
摘要： The present invention relates to a method for producing a nucleoside derivative represented by formula (2), comprising the step of reducing a nucleoside of formula (1) in the presence of a noble metal catalyst comprising a carrier and a noble metal supported thereby, selected from the group consisting of (A) a homogeneously supported catalyst where the specific surface area of the noble metal is 95.0 m2/g or more and the particle size of the noble metal is 4.3 nm or less, and (B) a surface-loaded catalyst where the specific surface area of the noble metal is 56.0 m2/g or more and the particle size of the noble metal is 8.0 nm or less, wherein R1 is hydrogen or a protective group, R2 is NH2 or OH, R3 is an acyl group, and X is a chlorine or bromine atom. According to the present invention, the yield can be made equal even when the amount of catalyst is smaller than that used for the conventional products.
摘要翻译：本发明涉及一种制备由式（2）表示的核苷衍生物的方法，包括在贵金属催化剂存在下还原式（1）的核苷的步骤，所述贵金属催化剂包含载体和由其所支持的贵金属，所选择的贵金属被选择来自由（A）贵金属的比表面积为95.0m 2 / g以上的均匀负载的催化剂组成的组，贵金属的粒径为4.3nm以下，和（B）贵金属的比表面积为56.0m 2 / g以上，贵金属的粒径为8.0nm以下的表面负载型催化剂，其中，R' R 1是氢或保护基，R 2是NH 2或OH，R 3是酰基， X是氯或溴原子。根据本发明，即使当催化剂的用量小于常规产品所用量时，产率也可以相等。

58. 发明申请

US20070179297A1 Chemical compounds 审中-公开
公开(公告)号：US20070179297A1
公开(公告)日：2007-08-02
申请号：US11732411
申请日：2007-04-03
申请人： Aaron Rigby , Hitesh Sanganee , Brian Springthorpe , Louise Lawrence
发明人： Aaron Rigby , Hitesh Sanganee , Brian Springthorpe , Louise Lawrence
IPC分类号： A61K31/4545 , C07D471/02 , C07D413/02 , C07D473/02 , A61K31/4743 , A61K31/4745
CPC分类号： C07D401/14 , C07D211/58 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/08 , C07D495/04 , C07D513/04
摘要： The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.

59. 发明申请

US20070066631A1 Pyrazolyl substituted xanthines 失效
标题翻译：吡唑基取代黄嘌呤
公开(公告)号：US20070066631A1
公开(公告)日：2007-03-22
申请号：US11362393
申请日：2006-02-27
申请人： Guoquan Wang , Jayson Rieger , Robert Thompson
发明人： Guoquan Wang , Jayson Rieger , Robert Thompson
IPC分类号： A61K31/522 , C07D473/02
CPC分类号： C07D473/06
摘要： The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
摘要翻译：本发明提供了作为Aβ2A腺苷受体（AR）的选择性拮抗剂的化合物和药物组合物。这些化合物和组合物可用作药剂。

60. 发明申请

US20070065360A1 Nonpolar thymidine analogs 失效
标题翻译：非极性胸苷类似物
公开(公告)号：US20070065360A1
公开(公告)日：2007-03-22
申请号：US11519385
申请日：2006-09-11
申请人： Eric Kool
发明人： Eric Kool
IPC分类号： A61K51/00 , C12Q1/68 , C07D473/02 , C07H21/04
CPC分类号： C07D307/20 , A61K51/0491 , C07H21/04
摘要： Nonpolar thymidine analogs are provided comprising a dihalogenated or trihalogenated base of the structure: where R1 is a sugar moiety; R2 is H or CH3; an imaging moiety or a cytotoxic moiety and X1 and X2 are independently selected from I, Cl, Br, and F, with the proviso that not more than one F will be present at these positions.
摘要翻译：提供非极性胸苷类似物，其包含以下结构的二卤代或三卤代碱：其中R 1是糖部分; R 2是H或CH 3 N; 成像部分或细胞毒素部分，X 1和X 2独立地选自I，Cl，Br和F，条件是不超过一个F将在这些位置出席。

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