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21. 发明专利

AU2003287038A8 Method of preparing (3r, 3as, 6ar) -3- hydroxyhexahydrofuro (2, 3-b) furan and related compounds 未知
公开(公告)号：AU2003287038A8
公开(公告)日：2004-05-04
申请号：AU2003287038
申请日：2003-10-08
申请人： UNIV ILLINOIS
发明人： NOETZEL MARCUS W , GHOSH ARUN K , LESHCHENKO SOFIYA
IPC分类号： C07D493/04 , C07D307/00
摘要： A method of synthesizing (3R,3aS,6aR)-3-hydroxyhexahydrofuro[2,3-b]furan (I), and related compounds, in high yield and high enantiomeric selectivity is disclosed. Also disclosed is a method of manufacturing (5S)-5-(benzyloxymethyl)-5H-furan-2-one.

22. 发明专利

ZA200107521B Protease inhibitors that overcome drug resistance. 未知
公开(公告)号：ZA200107521B
公开(公告)日：2003-06-25
申请号：ZA200107521
申请日：2001-09-12
申请人： OKLAHOMA MED RES FOUND , UNIV ILLINOIS
发明人： TANG JORDAN J N , GHOSH ARUN K
IPC分类号： C07D307/20 , A61K , A61P

23. 发明专利

CA2374346A1 INHIBITORS OF MEMAPSIN 2 AND USE THEREOF 未知
公开(公告)号：CA2374346A1
公开(公告)日：2001-01-04
申请号：CA2374346
申请日：2000-06-27
申请人： UNIV ILLINOIS , OKLAHOMA MED RES FOUND
发明人： GHOSH ARUN K , HONG LIN , TANG JORDAN J N
IPC分类号： C12N15/09 , A61K31/164 , A61K38/00 , A61K39/00 , A61P25/28 , A61P43/00 , C07C235/06 , C07C237/12 , C07K1/113 , C07K5/097 , C07K5/113 , C12N9/50 , C12N9/64 , C12N9/99 , C12Q1/37 , C07K14/81 , A61K38/57
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 an d the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is bas ed on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Le u- Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (Figure 1). The inhibition constant of OM99-2 is 1.6 x 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 bythose 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.

24. 发明专利

CA2872424A1 USE OF COMPOUNDS FOR TREATING HIV 未知
公开(公告)号：CA2872424A1
公开(公告)日：1999-12-29
申请号：CA2872424
申请日：1999-06-23
申请人： US OF AMERICA REPRESENTED BY THE SECRETARY , UNIV ILLINOIS
发明人： ERICKSON JOHN W , GULNICK SERGEI V , MITSUYA HIROAKI , GHOSH ARUN K
IPC分类号： A61K31/34 , G01N33/15 , A61K31/4525 , A61P31/18 , A61P37/04 , A61P43/00 , C07D493/04 , C12Q1/02 , C12Q1/37
摘要： Disclosed are compounds of the formula (see above formula) wherein X is oxygen, R5 is isobutyl, and Ar is phenyl substituted with a substituent selected from the group consisting of amino, methoxy, aminomethyl, hydroxy, and hydroxymethyl, or a pharmaceutically acceptable salt thereof, for use in the preparation of a medicament for treating an HIV-infected mammal, in combination with an antiretroviral agent selected from the group consisting of ritonavir, indinavir, and saquinavir.

25. 发明专利

CA2872424C BISFURAN DERIVATIVES USEFUL IN PREVENTING THE EMERGENCE OF MULTIDRUG RESISTANT HIV STRAINS AND TREATMENT OF HIV 未知
公开(公告)号：CA2872424C
公开(公告)日：2017-03-07
申请号：CA2872424
申请日：1999-06-23
申请人： THE UNITED STATES OF AMERICA REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES , UNIV ILLINOIS
发明人： ERICKSON JOHN W , GULNICK SERGEI V , MITSUYA HIROAKI , GHOSH ARUN K
IPC分类号： A61K31/34 , G01N33/15 , A61K31/4525 , A61P31/18 , A61P37/04 , A61P43/00 , C07D493/04 , C12Q1/02 , C12Q1/37
摘要： Disclosed are compounds of the formulas: (see formula IA) and (see formula IB) wherein R1, X, Y, Z, m, n, R3, R5, and R6 are herein defined, or a pharmaceutically acceptable salt thereof, for use in the preparation of a medicament for treating a human immunodeficiency virus (HIV) infection in an antiretroviral treatment-experienced mammal, for inhibiting a mutant retroviral infection in a mammal infected with a mutant retrovirus, and for preventing the development of drug resistance in an HIV-infected mammal.

26. 发明专利

DE60045005D1 INHIBITOREN DES MEMAPSIN 2 UND IHRE VERWENDUNG 未知
公开(公告)号：DE60045005D1
公开(公告)日：2010-11-04
申请号：DE60045005
申请日：2000-06-27
申请人： OKLAHOMA MED RES FOUND , UNIV ILLINOIS
发明人： TANG JORDAN J , HONG LIN , GHOSH ARUN K , LIN XINLI , KOELSCH GERALD
IPC分类号： C07K14/81 , C12N15/09 , A61K31/164 , A61K38/00 , A61K38/57 , A61K39/00 , A61P25/28 , A61P43/00 , C07C235/06 , C07C237/12 , C07F7/18 , C07K1/113 , C07K5/097 , C07K5/113 , C12N9/50 , C12N9/64 , C12N9/99 , C12Q1/37

27. 发明专利

NZ562314A Compounds which inhibit beta-secretase activity and methods of use thereof 未知
公开(公告)号：NZ562314A
公开(公告)日：2010-02-26
申请号：NZ56231406
申请日：2006-04-10
申请人： COMENTIS INC , UNIV ILLINOIS , OKLAHOMA MED RES FOUND , PURDUE RESEARCH FOUNDATION
发明人： GHOSH ARUN K , KUMARAGURUBARAN NAGASWAMY , LIU CHUNFENG , DEVASAMUDRAM THIPPESWAMY , LEI HUI , ANKALA SUDHA V
IPC分类号： C07C233/78 , A61K31/166 , A61K31/18 , A61P25/28 , C07C311/08 , C07C311/29 , C07D207/09 , C07D209/14 , C07D211/26 , C07D213/40 , C07D213/61 , C07D213/65 , C07D213/74 , C07D215/12 , C07D241/12
摘要： Provided are memapsin beta-secretase inhibitors, including N1-(3-hydroxy-4-(4-methoxyphenylsulfonamido)-1-phenylbutan-2-yl)-5-(N-methylmethylsulfonamido)-N3-(1-phenylethyI)isophthalamide and related compounds. The compounds are useful for treating AlzheimerÆs disease and for reducing memapsin 2 catalytic activity.

28. 发明专利

AU2007234506A1 Inhibitors of memapsin 2 and thereof 未知
公开(公告)号：AU2007234506A1
公开(公告)日：2007-12-06
申请号：AU2007234506
申请日：2007-11-16
申请人： OKLAHOMA MED RES FOUND , UNIV ILLINOIS
发明人： GHOSH ARUN K , TANG JORDAN J N
IPC分类号： C07K14/00

29. 发明专利

AU2003216491A1 MICROTUBULE STABILIZING COMPOUNDS 未知
公开(公告)号：AU2003216491A1
公开(公告)日：2003-09-22
申请号：AU2003216491
申请日：2003-03-04
申请人： UNIV ILLINOIS
发明人： GHOSH ARUN K
IPC分类号： A61K31/34 , A61K31/35 , A61K31/395 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D493/08 , C07D493/18 , C07D498/18 , A61K31/439
摘要： Laulimalide and epothilone derivatives useful as microtubule stabilizing agents, and in the treatment of cancers are disclosed. Methods of making the compounds and using the compounds as therapeutic agents in treating cancers also are disclosed.

30. 发明专利

CA2478087A1 MICROTUBULE STABILIZING COMPOUNDS 未知
公开(公告)号：CA2478087A1
公开(公告)日：2003-09-18
申请号：CA2478087
申请日：2003-03-04
申请人： UNIV ILLINOIS
发明人： GHOSH ARUN K
IPC分类号： A61K31/34 , A61K31/35 , A61K31/395 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D493/08 , C07D493/18 , C07D498/18 , A61K31/439
摘要： Laulimalide and epothilone derivatives useful as microtubule stabilizing agents, and in the treatment of cancers are disclosed. Methods of making the compounds and using the compounds as therapeutic agents in treating cancers also are disclosed.

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