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1. 发明申请

US20050054873A1 Process for the preparation of aniline-derived thyroid receptor ligands 审中-公开
标题翻译：制备苯胺衍生甲状腺受体配体的方法
公开(公告)号：US20050054873A1
公开(公告)日：2005-03-10
申请号：US10936062
申请日：2004-09-08
申请人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond Weaver , Jurong Yu , Arun Ghosh
发明人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond Weaver , Jurong Yu , Arun Ghosh
IPC分类号： C07C45/00 , C07C205/11 , C07C205/12 , C07C205/37 , C07C205/38 , C07C205/43 , C07C231/02 , C07C233/25 , C07C309/24 , C07C309/65 , C07C233/73
CPC分类号： C07C309/65 , C07C45/00 , C07C201/12 , C07C205/12 , C07C205/37 , C07C205/38 , C07C205/43 , C07C213/02 , C07C231/02 , C07C233/25 , C07C309/24 , C07C47/575 , C07C217/90
摘要： Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
摘要翻译：提供了合成苯胺衍生物的方法，特别是具有作为甲状腺受体配体活性的某些苯胺衍生物。

2. 发明授权

US06806381B2 Process for the preparation of aniline-derived thyroid receptor ligands 失效
标题翻译：制备苯胺衍生甲状腺受体配体的方法
公开(公告)号：US06806381B2
公开(公告)日：2004-10-19
申请号：US10273268
申请日：2002-10-17
申请人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
发明人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
IPC分类号： C07C22900
CPC分类号： C07C309/65 , C07C45/00 , C07C201/12 , C07C205/12 , C07C205/37 , C07C205/38 , C07C205/43 , C07C213/02 , C07C231/02 , C07C233/25 , C07C309/24 , C07C47/575 , C07C217/90
摘要： Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
摘要翻译：提供了合成苯胺衍生物的方法，特别是具有作为甲状腺受体配体活性的某些苯胺衍生物。

3. 发明申请

US20090326263A1 Process for the preparation of aniline-derived thyroid receptor ligands 失效
标题翻译：制备苯胺衍生甲状腺受体配体的方法
公开(公告)号：US20090326263A1
公开(公告)日：2009-12-31
申请号：US12456313
申请日：2009-06-15
申请人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
发明人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
IPC分类号： C07C309/24 , C07C205/12 , C07C37/04 , C07C47/56
CPC分类号： C07C309/65 , C07C45/00 , C07C201/12 , C07C205/12 , C07C205/37 , C07C205/38 , C07C205/43 , C07C213/02 , C07C231/02 , C07C233/25 , C07C309/24 , C07C47/575 , C07C217/90
摘要： Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
摘要翻译：提供了合成苯胺衍生物的方法，特别是具有作为甲状腺受体配体活性的某些苯胺衍生物。

4. 发明授权

US07956214B2 Process for the preparation of aniline-derived thyroid receptor ligands 失效
标题翻译：制备苯胺衍生甲状腺受体配体的方法
公开(公告)号：US07956214B2
公开(公告)日：2011-06-07
申请号：US12456313
申请日：2009-06-15
申请人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
发明人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
IPC分类号： C07C309/00
CPC分类号： C07C309/65 , C07C45/00 , C07C201/12 , C07C205/12 , C07C205/37 , C07C205/38 , C07C205/43 , C07C213/02 , C07C231/02 , C07C233/25 , C07C309/24 , C07C47/575 , C07C217/90
摘要： Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
摘要翻译：提供了合成苯胺衍生物的方法，特别是具有作为甲状腺受体配体活性的某些苯胺衍生物。

5. 发明申请

US20070049759A1 Methods for Preparing N-Arylated Oxazolidinones Via A Copper Catalyzed Cross Coupling 审中-公开
标题翻译：通过铜催化交联法制备N-甲酰化恶唑烷酮的方法
公开(公告)号：US20070049759A1
公开(公告)日：2007-03-01
申请号：US11461203
申请日：2006-07-31
申请人： Arun Ghosh , Stephane Caron , Janice Sieser
发明人： Arun Ghosh , Stephane Caron , Janice Sieser
IPC分类号： C07D263/00
CPC分类号： C07D291/04 , C07D207/12 , C07D263/22
摘要： Methods for the preparation of N-arylated oxazolidinone compounds via a copper catalyzed cross coupling reaction are disclosed.
摘要翻译：公开了通过铜催化的交叉偶联反应制备N-芳基化恶唑烷酮化合物的方法。

6. 发明申请

US20060234944A1 Beta-secretase inhibitors and methods of use 审中-公开
标题翻译： β-分泌酶抑制剂和使用方法
公开(公告)号：US20060234944A1
公开(公告)日：2006-10-19
申请号：US10493439
申请日：2002-10-23
申请人： Arun Ghosh , Jordan Tang , Geoffrey Bilcer , Wanpin Chang , Lin Hong , Gerald Koelsch , Jeff Loy , Robert Turner III
发明人： Arun Ghosh , Jordan Tang , Geoffrey Bilcer , Wanpin Chang , Lin Hong , Gerald Koelsch , Jeff Loy , Robert Turner III
IPC分类号： A61K38/08 , C07K7/06
CPC分类号： C07K7/06 , C07K5/0207
摘要： Compounds inhibit memapsin 2 β-secretase activity and selectively inhibit memapsin 2 β-secretase activity relative to memapsin 1 β-secretase activity. The compounds are employed in methods to inhibit memapsin 2 β-secretase activity, in the treatment of Alzheimer's disease, in the inhibition of hydrolysis of a β-secretase site of a β-amyloid precursor protein and to decrease β-amyloid protein in in vitro samples and in mammals. Proteins of memapsin 2 associated with compounds of the invention are crystallized.
摘要翻译：化合物抑制复合蛋白2的β-分泌酶活性，并相对于memapsin1β-分泌酶活性选择性地抑制memapsin2β-分泌酶活性。该化合物用于抑制复合体蛋白酶2β-分泌酶活性，治疗阿尔茨海默氏病，抑制β-淀粉样蛋白前体蛋白的β-分泌酶位点的水解并在体外降低β-淀粉样蛋白的方法样品和哺乳动物。与本发明化合物相关的胶原蛋白2的蛋白质结晶。

7. 发明授权

US07223870B2 Methods for preparing N-arylated oxazolidinones via a copper catalyzed cross coupling reaction 失效
标题翻译：通过铜催化交叉偶联反应制备N-芳基化恶唑烷酮的方法
公开(公告)号：US07223870B2
公开(公告)日：2007-05-29
申请号：US10645779
申请日：2003-08-21
申请人： Arun Ghosh , Stephane Caron , Janice E. Sieser
发明人： Arun Ghosh , Stephane Caron , Janice E. Sieser
IPC分类号： C07D263/04
CPC分类号： C07D291/04 , C07D207/12 , C07D263/22
摘要： Methods for the preparation of N-arylated oxazolidinone compounds via a copper catalyzed cross coupling reaction are disclosed.
摘要翻译：公开了通过铜催化的交叉偶联反应制备N-芳基化恶唑烷酮化合物的方法。

8. 发明申请

US20150246888A1 ENOYL REDUCTASE INHIBITORS WITH ANTIBACTERIAL ACTIVITY 审中-公开
标题翻译： ENOYL还原抑制剂具有抗菌活性
公开(公告)号：US20150246888A1
公开(公告)日：2015-09-03
申请号：US14427603
申请日：2013-09-11
申请人： Michael JOHNSON , Shahila CHRISTIE , Arun GHOSH , Kirk HEVENER , The Board of Trustees of the University of Illinois , Purdue Research Foundation
发明人： Michael Johnson , Shahila Christie , Arun Ghosh , Kirk Hevener
IPC分类号： C07D235/06 , C07D491/048 , C07D498/04 , C07D471/14 , C07D487/04 , C07D235/02 , C07D405/06
CPC分类号： C07D235/06 , C07D235/02 , C07D235/04 , C07D405/06 , C07D471/14 , C07D487/04 , C07D491/048 , C07D498/04
摘要： Disclosed are compounds and compositions useful as antibacterials. In particular, disclosed are enoyl reductase (FabI) inhibitors, compositions comprising such compounds, processes for producing such compounds, and methods of using such compounds.
摘要翻译：公开了可用作抗菌剂的化合物和组合物。特别地，公开了烯酰基还原酶（FabI）抑制剂，包含这些化合物的组合物，制备这些化合物的方法，以及使用这些化合物的方法。

9. 发明申请

US20080021196A1 INHIBITORS OF MEMAPSIN 2 AND USE THEREOF 失效
标题翻译： MEMAPSIN 2的抑制剂及其用途
公开(公告)号：US20080021196A1
公开(公告)日：2008-01-24
申请号：US11763342
申请日：2007-06-14
申请人： Jordan TANG , Arun Ghosh
发明人： Jordan TANG , Arun Ghosh
IPC分类号： C07C7/06 , C07C229/24
CPC分类号： C07K5/1021 , A61K38/00 , A61K39/00 , C07K1/1136 , C07K5/06026 , C07K5/06043 , C07K5/0806 , C07K2299/00 , C12N9/6421 , C12N9/6478 , Y02A90/26 , Y10S514/879
摘要： Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1). The inhibition constant of OM99-2 is 1.6×10−9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bound to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.
摘要翻译：已经开发了用于生产纯化的，催化活性的重组突变蛋白2的方法。已经确定了催化活性酶的底物和亚位点特异性。底物和亚位点特异性信息用于设计可以抑制膜蛋白2功能的天然memapsin 2底物的底物类似物。底物类似物基于肽序列，显示与memapsin 2的天然肽底物相关。底物类似物含有至少一个酰胺键的类似物，该类似物不能被膜蛋白2切割。开发了两个底物类似物合成的关键氨基酸残基位点处的等位基因，底物类似物OMR99- 1和OM99-2。 OM99-2基于由过渡态等电位羟基亚乙基取代的Leu-Ala肽键的八肽Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe（SEQ ID NO：28）（图1 ）。 OM99-2的抑制常数相对于重组pro-memapsin为1.6×10 -9 M。使用与该抑制剂结合的胶原蛋白2的结晶学来确定蛋白质的三维结构，以及各种残留物在结合中的重要性。本领域技术人员可以使用本信息来设计新的抑制剂，使用商业上可获得的有机化学和酶学方面熟悉的软件程序和技术来设计新的抑制剂2，可用于诊断和治疗和/或预防阿尔茨海默病。

10. 发明申请

US20070117793A1 Compounds Which Inhibit Beta-Secretase Activity and Methods of Use 有权
标题翻译：抑制β-分泌酶活性的化合物和使用方法
公开(公告)号：US20070117793A1
公开(公告)日：2007-05-24
申请号：US11463558
申请日：2006-08-09
申请人： Arun Ghosh , Nagaswamy Kumaragurubaran , Chunfeng Liu , Thippeswamy Devasamudram , Hui Lei , Lisa Swanson , Sudha Ankala , Jordan Tang , Geoffrey Bilcer
发明人： Arun Ghosh , Nagaswamy Kumaragurubaran , Chunfeng Liu , Thippeswamy Devasamudram , Hui Lei , Lisa Swanson , Sudha Ankala , Jordan Tang , Geoffrey Bilcer
IPC分类号： A61K31/551 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/473 , A61K31/4709 , A61K31/427 , A61K31/422 , A61K31/4178 , A61K31/4184
CPC分类号： C07D213/74 , C07C233/78 , C07C311/08 , C07C311/29 , C07C2601/14 , C07D207/09 , C07D209/14 , C07D211/26 , C07D213/36 , C07D213/40 , C07D213/61 , C07D213/65 , C07D215/12 , C07D233/64 , C07D235/14 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/28 , C07D295/108 , C07D295/13 , C07D295/205 , C07D295/32 , C07D307/52 , C07D307/62 , C07D309/04 , C07D317/58 , C07D417/12 , C07D493/04
摘要： The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
摘要翻译：本发明提供新颖的β-分泌酶抑制剂及其使用方法，包括治疗阿尔茨海默氏病的方法。

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