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61. 发明申请

US20090163512A1 Spiroindolinone Derivatives 失效
标题翻译：螺吲哚啉酮衍生物
公开(公告)号：US20090163512A1
公开(公告)日：2009-06-25
申请号：US12273035
申请日：2008-11-18
申请人： Li Chen , Xingchun Han , Yun He , Song Yang , Zhuming Zhang
发明人： Li Chen , Xingchun Han , Yun He , Song Yang , Zhuming Zhang
IPC分类号： A61K31/496 , C07D471/10 , A61K31/438
CPC分类号： C07D471/10
摘要： There are provided compounds of the formula and pharmaceutically acceptable salts and esters and enantiomers thereof wherein W, X, X′, Y, V, V′, A, B and R are as described herein.The compounds have utility as antiproliferative agents, especially, as anticancer agents.
摘要翻译：提供下式的化合物及其药学上可接受的盐和酯和对映异构体，其中W，X，X'，Y，V，V'，A，B和R如本文所述。这些化合物具有抗增生剂的作用，特别是作为抗癌剂。

62. 发明授权

US07501408B2 Inhibitors of cathepsin S 失效
标题翻译：组织蛋白酶S抑制剂
公开(公告)号：US07501408B2
公开(公告)日：2009-03-10
申请号：US11932679
申请日：2007-10-31
申请人： Hong Liu , Arnab Chatterjee , David C. Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David H. Woodmansee , Daniel Mutnick , Donald S. Karanewsky , Yun He
发明人： Hong Liu , Arnab Chatterjee , David C. Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David H. Woodmansee , Daniel Mutnick , Donald S. Karanewsky , Yun He
IPC分类号： C07D417/12 , C07D295/10 , A61K31/541
CPC分类号： C07D209/08 , C07D261/14 , C07D295/18 , C07D295/20
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula (I): wherein Q is thiomorpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.
摘要翻译：本发明提供了用于选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。更具体地，本发明提供具有式（I）的化合物：其中Q是硫代吗啉基; A，R5，R6，R7，R8，R9和Ar为取代基。

63. 发明申请

US20080194668A1 Compounds and Compositions as Tpo Mimetics 有权
标题翻译：化合物和组合物作为Tpo模拟物
公开(公告)号：US20080194668A1
公开(公告)日：2008-08-14
申请号：US12063350
申请日：2006-08-15
申请人： Thomas Marsilje , Wenshuo Lu , Phil Alper , Daniel Mutnick , Yun He
发明人： Thomas Marsilje , Wenshuo Lu , Phil Alper , Daniel Mutnick , Yun He
IPC分类号： A61K31/404 , C07D209/04 , A61P7/00
CPC分类号： C07D209/14 , C07D209/18 , C07D235/18
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.
摘要翻译：本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的TPO活性相关的疾病或病症的方法，特别是涉及血小板减少症的疾病或病症。

64. 发明申请

US20080108595A1 INHIBITORS OF CATHEPSIN S 失效
标题翻译： CATHEPSIN的抑制剂
公开(公告)号：US20080108595A1
公开(公告)日：2008-05-08
申请号：US11932679
申请日：2007-10-31
申请人： Hong Liu , Arnab Chatterjee , David Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David Woodmansee , Daniel Mutnick , Donald Karanewsky , Yun He
发明人： Hong Liu , Arnab Chatterjee , David Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David Woodmansee , Daniel Mutnick , Donald Karanewsky , Yun He
IPC分类号： C07D413/00 , A61K31/535 , C07D265/30 , A61K31/5377 , A61K31/54 , C07D279/12 , C07D241/04 , A61K31/495 , A61K31/397 , C07D205/04
CPC分类号： C07D209/08 , C07D261/14 , C07D295/18 , C07D295/20
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
摘要翻译：本发明提供了选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。

65. 发明申请

US20050197326A1 Bicyclic compounds and compostions as PDF inhibitors 失效
标题翻译：双环化合物和组合物作为PDF抑制剂
公开(公告)号：US20050197326A1
公开(公告)日：2005-09-08
申请号：US10903349
申请日：2004-07-30
申请人： Valentina Molteni , Xiaohui He , Yun He , Andreas Kreusch , Juliet Nabakka , Kunyong Yang
发明人： Valentina Molteni , Xiaohui He , Yun He , Andreas Kreusch , Juliet Nabakka , Kunyong Yang
IPC分类号： A61K20060101 , A61K31/438 , A61K31/4706 , A61K31/4985 , A61K31/5415 , A61K31/55 , C07D211/00 , C07D279/00 , C07D401/00 , C07D417/00
CPC分类号： C07D279/16 , C07D215/227 , C07D417/06 , C07D417/12
摘要： This invention is directed to novel bicyclic compounds, to the uses of these compounds in various medicinal applications, including treating disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections, and to pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及新颖的双环化合物，涉及这些化合物在各种药物应用中的用途，包括治疗适合于通过肽基变性酶抑制剂治疗的疾病，例如治疗细菌感染，以及包含这些化合物的药物组合物。

66. 发明申请

US20050113356A1 Inhibitors of cathepsin S 失效
公开(公告)号：US20050113356A1
公开(公告)日：2005-05-26
申请号：US10922515
申请日：2004-08-18
申请人： Hong Liu , Arnab Chatterjee , David Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David Woodmansee , Daniel Mutnick , Donald Karanewsky , Yun He
发明人： Hong Liu , Arnab Chatterjee , David Tully , Phillip Alper , Badry Bursulaya , Jianhua Guo , David Woodmansee , Daniel Mutnick , Donald Karanewsky , Yun He
IPC分类号： A61K20060101 , A61K31/397 , A61K31/401 , A61K31/404 , A61K31/423 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/537 , A61K31/5375 , A61K31/54 , C07D209/04 , C07D209/08 , C07D261/14 , C07D265/30 , C07D295/13 , C07D295/18 , C07D295/20 , C07D411/12 , C07D413/12 , C07D417/12
CPC分类号： C07D209/08 , C07D261/14 , C07D295/18 , C07D295/20
摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

67. 发明授权

US06437138B1 3-pyridyloxymethyl heterocyclic ether compounds useful in controlling chemical synaptic transmission 有权
标题翻译：可用于控制化学突触传播的3-吡啶氧基甲基杂环醚化合物
公开(公告)号：US06437138B1
公开(公告)日：2002-08-20
申请号：US09472399
申请日：2000-03-01
申请人： Nan-Horng Lin , Yun He , Mark W. Holladay , Keith Ryther , Yihong Li , Hao Bai
发明人： Nan-Horng Lin , Yun He , Mark W. Holladay , Keith Ryther , Yihong Li , Hao Bai
IPC分类号： C07D40100
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Novel 3-pyridyloxymethyl heterocyclic ether compounds of the formula: or the pharmaceutically-acceptable salts or prodrugs thereof are selective and potent ligands at neuronal nicotinic cholinergic channel receptors, and are effective in controlling synaptic transmission. Key intermediates and processes using this key intermediates to produce compounds of formula I with the variables defined in the specification are also described.
摘要翻译：下式的新型3-吡啶氧基甲基杂环醚化合物或其药学上可接受的盐或前药是神经元烟碱胆碱能通道受体的选择性和有效配体，并且有效地控制突触传递。还描述了使用该关键中间体产生具有本说明书中定义的变量的式I化合物的关键中间体和方法。

68. 发明授权

US6001849A Furopyridine, thienopyridine pyrrolopyridine useful in controlling chemical synaptic transmission 失效
标题翻译：呋喃吡啶，噻吩并吡啶吡咯并吡啶可用于控制化学突触传播
公开(公告)号：US6001849A
公开(公告)日：1999-12-14
申请号：US834053
申请日：1997-04-11
申请人： Richard L. Elliott , Keith B. Ryther , Mark W. Holladay , James T. Wasicak , Jerome F. Daanen , Nan-Horng Lin , Michael J. Dart , Yun He , Yihong Li
发明人： Richard L. Elliott , Keith B. Ryther , Mark W. Holladay , James T. Wasicak , Jerome F. Daanen , Nan-Horng Lin , Michael J. Dart , Yun He , Yihong Li
IPC分类号： A61K31/00 , A61K31/435 , A61K31/4353 , A61K31/4355 , A61P9/00 , A61P25/00 , A61P25/30 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D495/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/4355 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Novel heterocyclic ether compounds having the formula: ##STR1## wherein A, m, R, X, Y.sup.1, Y.sup.2 and Y.sup.3 are specifically defined, which are useful in selectively controlling chemical synaptic transmission; therapeutically-effective pharmaceutical compositions thereof; and use of said compositions to selectively control synaptic transmission in mammals.
摘要翻译：具有下式的新型杂环醚化合物：其中A，m，R，X，Y 1，Y 2和Y 3具体定义，其可用于选择性地控制化学突触传递; 其治疗有效的药物组合物; 以及使用所述组合物来选择性地控制哺乳动物中的突触传递。

69. 发明授权

US5508418A Intermediates for the preparation of enantiomerically-pure-3-methyl-5-(1-C1-C3-alkyl)-2-pyrrolidinyl)isoxazol e 失效
标题翻译：用于制备对映体纯-3-甲基-5-（1-C 1 -C 3 - 烷基）-2-吡咯烷基）异恶唑的中间体
公开(公告)号：US5508418A
公开(公告)日：1996-04-16
申请号：US477057
申请日：1995-06-07
申请人： Nan-Horng Lin , Yun He , William H. Bunnelle
发明人： Nan-Horng Lin , Yun He , William H. Bunnelle
IPC分类号： C07D413/04 , C07D207/06 , C07D261/04 , C07D261/06
CPC分类号： C07D413/04
摘要： Novel compounds useful in the preparation of enantiomerically-pure 3-methyl-5-(1-(C.sub.1 -C.sub.3 -alkyl)-2-pyrrolidinyl)isoxazole in high yield, namely 5(S)-(3-methyl-5-isoxazolyl)-2-pyrrolidinone, 3-methyl-5-(1-methyl-2-pyrrolidinyl)-5-hydroxy-4,5-dihydro-isoxazole, and 1-(1-methyl-2(S)-pyrrolidinyl)-1,3-butanedione-3-oxime.
摘要翻译：用于以高产率制备对映异构纯的3-甲基-5-（1-（C 1 -C 3 - 烷基）-2-吡咯烷基）异恶唑的新型化合物，即5（S） - （3-甲基-5-异恶唑基）-2-吡咯烷酮，3-甲基-5-（1-甲基-2-吡咯烷基）-5-羟基-4,5-二氢异恶唑和1-（1-甲基-2（S） - 吡咯烷基） - 1,3-丁二酮-3-肟。

70. 发明授权

US09258568B2 Quantization method and apparatus in encoding/decoding 有权
标题翻译：编码/解码中的量化方法和装置
公开(公告)号：US09258568B2
公开(公告)日：2016-02-09
申请号：US12210890
申请日：2008-09-15
申请人： Jianhua Zheng , Jianwen Chen , Yun He , Xinjian Meng
发明人： Jianhua Zheng , Jianwen Chen , Yun He , Xinjian Meng
IPC分类号： H04N7/12 , H04N11/02 , H04N11/04 , H04N19/174 , H04N19/176 , H04N19/70 , H04N19/46 , H04N19/61 , H04N19/126 , H04N19/154 , H04N19/18 , H04N19/177
CPC分类号： H04N19/174 , H04N19/126 , H04N19/154 , H04N19/176 , H04N19/177 , H04N19/18 , H04N19/46 , H04N19/61 , H04N19/70
摘要： A method and apparatus is provided for implementing quantization in encoding/decoding. Firstly, the quantization on the picture transformed coefficient matrix is performed using a quantization parameter model, that is, the coefficient matrix is modeled as a parameter model represented by only several parameters, in which the parameter model includes two sorts of parameters, frequency band distribution parameters and frequency band weighting parameters. Thus, a quantization matrix conforming to the human vision system can be obtained by controlling the model parameters and the subjective quality of the encoded picture can be easily controlled. Secondly, the method does not need to store or transfer the quantization matrix in the bitstream which help to improve the encoding efficiency. Finally, the quantization on picture transformed coefficients using the method is well adapted to the content information of the picture to be encoded. Therefore, the present invention can improve the subjective quality of the encoded picture.
摘要翻译：提供了一种用于在编码/解码中实现量化的方法和装置。首先，使用量化参数模型来执行对图像变换系数矩阵的量化，即，将系数矩阵建模为仅由几个参数表示的参数模型，其中参数模型包括两种参数，频带分布参数和频带加权参数。因此，可以通过控制模型参数来获得符合人类视觉系统的量化矩阵，并且可以容易地控制编码图像的主观质量。其次，该方法不需要存储或传送比特流中的量化矩阵，这有助于提高编码效率。最后，使用该方法的图像变换系数的量化很好地适应于要编码的图像的内容信息。因此，本发明可以提高编码图像的主观质量。

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