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81. 发明授权

US08816095B2 Na channels, disease, and related assays and compositions 有权
标题翻译： Na通道，疾病和相关测定法和组合物
公开(公告)号：US08816095B2
公开(公告)日：2014-08-26
申请号：US13059182
申请日：2009-08-17
申请人： Milton L. Brown , Scott Grindrod , Thomas H. Walls , Todd Hansen , Simeng Suy , Mikell A. Paige
发明人： Milton L. Brown , Scott Grindrod , Thomas H. Walls , Todd Hansen , Simeng Suy , Mikell A. Paige
IPC分类号： C07D233/76 , A61K31/69
CPC分类号： A61K31/4164 , C07D209/14 , C07D233/72 , C07D317/26
摘要： Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [3H]-Batrachotoxin-B ([3H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.
摘要翻译：公开了分子及其合成，用于阻断门控离子通道如电压门控钠通道（VGSC）和前列腺电压钠通道（PVSC）。这些抑制剂具有优异的阻断效能，例如置换与VGSC的位点2结合的放射性配体[3 H] -Batrachotoxin-B（[3 H] -BTX-B）。本发明的分子包含增加前列腺癌细胞（PC）中蛋白质结合位点的分子的结合亲和力的部分，其也是荧光的。在一个实施方案中，本发明分子是可用于在疼痛，癫痫或前列腺癌中选择性地靶向过量或过度活跃的VGSC的抑制系统，从而抑制PC的增殖。荧光部分还有助于药物在体外和体内生物系统中的筛选，跟踪和药效学研究。

82. 发明授权

US08748443B2 Antiviral compounds and uses thereof 有权
公开(公告)号：US08748443B2
公开(公告)日：2014-06-10
申请号：US13260199
申请日：2010-03-25
申请人： David A. Betebenner , John K. Pratt , David A. DeGoey , Pamela L. Donner , Charles A. Flentge , Douglas K. Hutchinson , Warren M. Kati , Allan C. Krueger , Kenton L. Longenecker , Clarence J. Maring , John T. Randolph , Todd W. Rockway , Michael D. Tufano , Rolf Wagner , Dachun Liu
发明人： David A. Betebenner , John K. Pratt , David A. DeGoey , Pamela L. Donner , Charles A. Flentge , Douglas K. Hutchinson , Warren M. Kati , Allan C. Krueger , Kenton L. Longenecker , Clarence J. Maring , John T. Randolph , Todd W. Rockway , Michael D. Tufano , Rolf Wagner , Dachun Liu
IPC分类号： A01N43/54 , A61K31/505 , A61K31/503 , C07D239/54
CPC分类号： C07D409/10 , A61K31/18 , A61K31/27 , A61K31/402 , A61K31/4166 , A61K31/421 , A61K31/425 , A61K31/4418 , A61K31/503 , A61K31/513 , A61K45/06 , C07C311/08 , C07D207/27 , C07D213/64 , C07D233/32 , C07D233/72 , C07D239/10 , C07D239/54 , C07D263/22 , C07D263/24 , C07D275/02 , C07D403/10 , C07D405/10 , Y02P20/55
摘要： This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

83. 发明申请

US20140100224A1 NEUROTROPHIN MIMETICS AND USES THEREOF 审中-公开
标题翻译：神经营养因子及其用途
公开(公告)号：US20140100224A1
公开(公告)日：2014-04-10
申请号：US13927302
申请日：2013-06-26
申请人： The University of North Carolina at Chapel Hill , U.S. Government represented by the Department of Veterans Affairs , The Regents of the University of California
发明人： Frank M. Longo , Stephen M. Massa
IPC分类号： C07D265/30 , C07D233/61 , C07D473/08 , C07D413/06 , C07D413/12
CPC分类号： C07D265/30 , C07D207/16 , C07D233/61 , C07D233/72 , C07D233/76 , C07D241/08 , C07D295/13 , C07D295/135 , C07D295/185 , C07D295/26 , C07D295/32 , C07D413/06 , C07D413/12 , C07D473/08 , C07K5/06034
摘要： The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
摘要翻译：本申请涉及新型神经营养因子模拟物的化合物。本申请还公开了通过施用有效量的这些化合物治疗与p75表达相关的紊乱，例如哺乳动物表达p75的细胞的降解或功能障碍。

84. 发明授权

US08524755B2 Specific diarylhydantoin and diarylthiohydantoin compounds 有权
公开(公告)号：US08524755B2
公开(公告)日：2013-09-03
申请号：US13202970
申请日：2010-02-24
申请人： Rajendra Parasmal Jain , Jacqueline A. Gibbons
发明人： Rajendra Parasmal Jain , Jacqueline A. Gibbons
IPC分类号： A61K31/4166 , C07D233/72
CPC分类号： C07D233/86 , A61K31/4166 , C07D233/72 , C07D233/74 , C07D233/84
摘要： Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others.

85. 发明授权

US08487115B2 Hydantoin derivatives of cyano-substituted chrysanthemic acid esters and their use in pest control 失效
标题翻译：乙腈衍生物氰基取代菊酸酯及其在病虫害防治中的应用
公开(公告)号：US08487115B2
公开(公告)日：2013-07-16
申请号：US13637788
申请日：2011-03-18
申请人： Noritada Matsuo
发明人： Noritada Matsuo
IPC分类号： A01N53/00 , C07D233/72
CPC分类号： C07D233/72 , A01N53/00 , C07D233/78 , C07D249/12
摘要： An ester compound represented by formula (1): wherein R3 represents hydrogen or methyl, R4 represents hydrogen or C1-C4 alkyl, and R5 represents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.
摘要翻译：由式（1）表示的酯化合物：其中R 3表示氢或甲基，R 4表示氢或C 1 -C 4烷基，R 5表示氢或C 1 -C 4烷基; 具有优异的害虫防治效果，因此可用作害虫防治剂的活性成分。

86. 发明申请

US20110130391A1 UREIDO SUBSTITUTED BENZOIC ACID COMPOUNDS AND THEIR USE FOR NONSENSE SUPPRESSION AND THE TREATMENT OF DISEASE 有权
标题翻译： UREIDO替代苯甲酸化合物及其用于非感染抑制和疾病治疗的用途
公开(公告)号：US20110130391A1
公开(公告)日：2011-06-02
申请号：US12980495
申请日：2010-12-29
申请人： Richard G. Wilde , James J. Takasugi , Seongwoo Hwang , Ellen M. Welch , Guangming Chen
发明人： Richard G. Wilde , James J. Takasugi , Seongwoo Hwang , Ellen M. Welch , Guangming Chen
IPC分类号： A61K31/549 , C07D233/38 , C07D401/10 , C07D403/10 , C07D285/16 , C07D285/06 , C07D233/72 , C07C275/42 , A61K31/4172 , A61K31/454 , A61K31/433 , A61K31/195 , A61P31/04 , A61P35/00 , A61P37/02 , A61P3/10 , A61P7/00 , A61P9/00 , A61P25/00 , A61P11/00 , A61P29/00
CPC分类号： C07D285/16 , A61K31/17 , A61K31/4166 , A61K31/4172 , A61K31/4196 , A61K31/421 , A61K31/426 , C07C275/42 , C07D233/32 , C07D233/42 , C07D233/72 , C07D401/04 , C07D401/10 , C07D405/04 , C07D405/06 , C07D409/04
摘要： The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.
摘要翻译：本发明包括脲基取代的苯甲酸化合物，包含该化合物的组合物和通过施用这些化合物或组合物来治疗或预防与无义突变mRNA相关的疾病的方法。

87. 发明申请

US20110046185A1 Arylchalcogenoarylalkyl-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof 审中-公开
标题翻译：芳基硫代芳基烷基取代的咪唑烷-2,4-二酮，其制备方法，包含这些化合物的药物及其用途
公开(公告)号：US20110046185A1
公开(公告)日：2011-02-24
申请号：US12852188
申请日：2010-08-06
申请人： Gerhard JAEHNE , Peter BELOW , Siegfried STENGELIN , Matthias GOSSEL , Thomas KLABUNDE , Irvin WINKLER
发明人： Gerhard JAEHNE , Peter BELOW , Siegfried STENGELIN , Matthias GOSSEL , Thomas KLABUNDE , Irvin WINKLER
IPC分类号： A61K31/4439 , C07D233/72 , A61K31/4166 , A61P3/10 , A61P3/04 , A61P25/32 , A61P25/34 , A61P25/18 , A61P25/28 , C07D401/04 , C07D409/04 , C07D417/10 , A61K31/428
CPC分类号： C07D233/72 , C07D401/04 , C07D405/04 , C07D409/04
摘要： The invention relates to compounds of formula (I) wherein the groups R and R′ A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
摘要翻译：本发明涉及式（I）化合物，其中基团R和R'A，D，E，G，L，p和R 1至R 10具有所述含义及其生理上相容的盐。所述化合物例如适合作为抗肥胖药物。

88. 发明申请

US20110046105A1 Heterocycle-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising them and use thereof 审中-公开
标题翻译：杂环取代的咪唑烷-2,4-二酮，其制备方法，包含它们的药物及其用途
公开(公告)号：US20110046105A1
公开(公告)日：2011-02-24
申请号：US12852233
申请日：2010-08-06
申请人： Gerhard Jaehne , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Irvin Winkler
发明人： Gerhard Jaehne , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Irvin Winkler
IPC分类号： A61K31/4178 , C07D401/12 , A61K31/497 , A61P3/04 , A61P3/10 , A61P25/28 , A61P25/18 , A61P25/32 , A61P25/34 , A61K31/4184 , A61K31/501 , C07D413/14 , A61K31/5355 , A61K31/454
CPC分类号： C07D233/72 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
摘要翻译：本发明涉及式（I）化合物，其中基团R和R'，A，D，E，G，L，p和R 1至R 10具有所述含义及其生理上相容的盐。所述化合物例如适合作为抗肥胖药物。

89. 发明申请

US20110003827A1 HIV protease inhibiting compounds 有权
标题翻译： HIV蛋白酶抑制化合物
公开(公告)号：US20110003827A1
公开(公告)日：2011-01-06
申请号：US11009841
申请日：2004-12-10
申请人： Charles A. Flentge , Hui-Ju Chen , David A. DeGoey , William J. Flosi , David J. Grampovnik , Peggy P. Huang , Dale J. Kempf , Larry L. Klein , Allan C. Krueger , Darold L. Madigan , John T. Randolph , Minghua Sun , Ming C. Yeung , Chen Zhao
发明人： Charles A. Flentge , Hui-Ju Chen , David A. DeGoey , William J. Flosi , David J. Grampovnik , Peggy P. Huang , Dale J. Kempf , Larry L. Klein , Allan C. Krueger , Darold L. Madigan , John T. Randolph , Minghua Sun , Ming C. Yeung , Chen Zhao
IPC分类号： A61K31/501 , C07C317/48 , C07C311/37 , C07D213/46 , C07D307/14 , C07D333/22 , C07D417/12 , C07D409/06 , C07D403/06 , C07D471/04 , A61K31/216 , A61K31/18 , A61K31/4402 , A61K31/341 , A61K31/381 , A61K31/427 , A61K31/4178 , A61K31/4709 , A61K31/437 , A61K31/506 , A61P31/18
CPC分类号： C07D417/12 , C07C311/18 , C07C311/29 , C07C311/41 , C07C311/47 , C07C317/18 , C07D209/14 , C07D213/30 , C07D213/40 , C07D233/36 , C07D233/64 , C07D233/72 , C07D277/24 , C07D277/28 , C07D307/14 , C07D307/20 , C07D307/52 , C07D333/20 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/10 , C07D409/06 , C07D409/10 , C07D417/06 , C07D417/10 , C07D471/04 , C07D493/04
摘要： A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
摘要翻译：公开了式的化合物作为HIV蛋白酶抑制剂。还公开了用于抑制HIV感染的方法和组合物。

90. 发明授权

US07858806B2 Crystal form of 5-hydroxy-1-methylhydantoin 有权
标题翻译：晶体形式的5-羟基-1-甲基乙内酰脲
公开(公告)号：US07858806B2
公开(公告)日：2010-12-28
申请号：US12498967
申请日：2009-07-07
申请人： Kaoru Okamoto , Naoharu Nishimura , Akira Ishii
发明人： Kaoru Okamoto , Naoharu Nishimura , Akira Ishii
IPC分类号： C07D233/80
CPC分类号： C07D233/72
摘要： Conventional I-form crystals of 5-hydroxy-1-methylhydantoin contain, remaining therein in a considerable amount, the organic solvent used in a purification step. In contrast, in II-form crystals, the amount of the organic solvent remaining therein is smaller than the detection limit. Namely, the II-form crystals contain substantially no residual organic solvent. The novel II-form crystals of 5-hydroxy-1-methylhydantoin obtained through recrystallization from water not only contain substantially no residual organic solvent, but also have a high bulk density and are hence advantageous for pharmaceutical preparation. They further have properties advantageous for production, such as low adhesion. The crystals are significantly useful as a material for medicines required to have high safety, such as drugs for renal insufficiency.
摘要翻译：常规的5-羟基-1-甲基乙内酰脲的I型晶体在其中保留相当量的纯化步骤中使用的有机溶剂。相反，在II型晶体中，其中残留的有机溶剂的量小于检测限。即，II型晶体基本上不含残留的有机溶剂。通过从水中重结晶获得的5-羟基-1-甲基乙内酰脲的新型II型晶体不仅基本上不含有残留的有机溶剂，而且还具有高的堆积密度，因此对于药物制剂是有利的。它们还具有有利于生产的性质，例如低粘附性。该晶体作为具有高度安全性的药物的材料，例如用于肾功能不全的药物是显着有用的。

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