The Ghosh Laboratories:
The Home of the Backbone Binding, Bioactive Natural Product Synthesis, and Nature-Inspired Molecular Design for Today's Medicine
List of US Patents (Total of 66)
66. BACE1 inhibitors for the treatment of Alzheimer disease Ghosh, Arun K.; Mesecar, Andres; Brindisi, Margherita; Cardenas, Emilio Leal PCT Int. Appl. (2019), WO 2019075358 A1 20190418.
65. Herboxidiene derivatives and uses thereof in pharmaceutical compositions for treatment of cancer By Ghosh, Arun K.; Jurica, Melissa PCT Int. Appl. (2019), WO 2019023450 A1 20190131.
64. Macrocyclic HIV-1 protease inhibitors and uses thereof By Ghosh, Arun K.; Mitsuya, Hiroaki; Fyvie, Sean; Brindisi, Margherita From PCT Int. Appl. (2019), WO 2019006335 A1 20190103.
63. Preparation of tricyclic p2-ligand derivatives for use as HIV-protease inhibitors By Ghosh, Arun K.; Mitsuya, Hiroaki; Nyalapatla, Prasanth Reddy PCT Int. Appl. (2018), WO 2018089621 A1 20180517.
62. Anti-cancer agents and preparation thereof By Ghosh, Arun K. PCT Int. Appl. (2018), WO 2018057897 A1 20180329.
61. Preparation of callyspongiolide, its analogs and uses thereof By Ghosh, Arun K.; Kassekert, Luke A. PCT Int. Appl. (2017), WO 2017205791 A1 20171130
60. HIV-1 protease inhibitors and uses thereof By Ghosh, Arun K.; Mitsuya, Hiroaki PCT Int. Appl. (2017), WO 2017031220 A1 20170223
59. Compounds and methods for treating AIDS and HIV infections By Ghosh, Arun K. U.S. (2014), US 8921349 B2 20141230.
58. Inhibitors of bace1 and methods for treating alzheimer's disease By Ghosh, Arun K. U.S. Pat. Appl. Publ. (2011), US 20110275619 A1 20111110.
57. C-3 substituted bicyclooctane based HIV protease inhibitors By Ghosh, Arun K.; Mitsuya, Hiroaki; Chapsal, Bruno D. U.S. Pat. Appl. Publ. (2014), US 20140148508 A1 20140529
56. Compounds and methods for treating respiratory diseases By Ghosh, Arun K.; Takayama, Jun; Mesecar, Andrew David; Johnson, Michael E.; Ratia, Kiira M.; Chaudhuri, Rima; Mulhearn, Debbie C. U.S. Pat. Appl. Publ. (2011), US 20110269834 A1 20111103
55. Processes and intermediates for preparing substituted hexahydrofuro [2,3-b] furans By Ghosh, Arun K.; Martyr, Cuthbert D. U.S. (2014), US 8802724 B2 20140812
54. Ccr5 antagonists for treating HIV By Ghosh, Arun K.; Mitsuya, Hiroaki; Kalapala, Venkateswararao; Li, Jianfeng U.S. Pat. Appl. Publ. (2014), US 20140221420 A1 20140807
53. Nonpeptide HIV-1 Protease Inhibitors By Ghosh, Arun K. U.S. (2014), US 8791135 B2 20140729.
52. Synthesis of macrocyclic cancer chemotherapy agents and methods of use By Ghosh, Arun K.; Xu, Xiaoming U.S. (2013), US 8580975 B2 20131112.
51. Fused tricyclic ether carbamates and their use By Ghosh, Arun K.; Xu, Chun-Xiao; Mitsuya, Hiroaki; Parham, Garth U.S. (2013), US 8563597 B2 20131022.
50. Quinazoline Inhibitors of BACE 1 and Methods of Using By Ghosh, Arun K. U.S. (2013), US 8394807 B2 20130312.
49. HIV protease inhibitors and methods for using By Ghosh, Arun K. U.S. (2013), US 8501961 B2 20130806.
48. Compounds for treatment of alzheimer's disease By Ghosh, Arun K. U.S. (2014), US 8703947 B2 20140422.
47. HIV-1 protease inhibitors and uses thereof By Ghosh, Arun K.; Rao, Venkateswara Kalapala; Mitsuya, Hiroaki PCT Int. Appl. (2015), WO 2015175994 A1 20151119.
46. Preparation of FR901464 and spliceostatin A analogs as anti-cancer agents By Ghosh, Arun K. PCT Int. Appl. (2015), WO 2015077370 A1 20150528.
45. Inhibitors of memapsin-1 for the treatment of Alzheimer's disease and diabetes By Ghosh, Arun K. U.S. Pat. Appl. Publ. (2015), US 20150080439 A1 20150319
44. Preparation of gem-difluoro heterobicyclic compounds as HIV-1 protease inhibitors By Ghosh, Arun K.; Mitsuya, Hiroaki; Yashchuk, Sofiya U.S. Pat. Appl. Publ. (2015), US 20150072958 A1 20150312.
43. Preparation of memapsin 2 inhibitors for the treatment of Alzheimer's disease By Tang, Jordan; Kalapala, Venkateswararao; Ghosh, Arun K. PCT Int. Appl. (2014), WO 2014036105 A2 20140306
42. Preparation of bicyclic compounds as HIV-1 protease inhibitors for treating HIV By Ghosh, Arun K.; Chapsal, Bruno D.; Mitsuya, Hiroaki U.S. Pat. Appl. Publ. (2013), US 20130289067 A1 20131031
41. Processes for preparing C-3 substituted bicyclooctane based HIV protease inhibitors By Ghosh, Arun K.; Chapsal, Bruno D.; Mitsuya, Hiroaki PCT Int. Appl. (2013), WO 2013009844 A2 20130117.
40. Fused 6,5 bicyclic ring system p2 ligands, and methods for treating HIV By Ghosh, Arun K. PCT Int. Appl. (2012), WO 2012092168 A1 20120705.
39. Compositions containing HIV protease inhibitors for treatment of HIV infection By Ghosh, Arun K. PCT Int. Appl. (2012), WO 2012092188 A1 20120705
38. A process for the preparation of hexahydrofurofuran derivatives for use as anti-HIV agents By Ghosh, Arun K.; Martyr, Cuthbert D. PCT Int. Appl. (2012), WO 2012075122 A2 20120607
37. Fused tricyclic ether carbamates for treating HIV infected patients By Ghosh, Arun K.; Xu, Chun-Xiao; Mitsuya, Hiroaki; Parham, Garth PCT Int. Appl. (2012), WO 2012031237 A1 20120308.
36. CCR5 modulators for treating human immunodeficiency virus By Ghosh, Arun K.; Mitsuya, Hiroaki PCT Int. Appl. (2011), WO 2011116287 A1 20110922
35. Compounds and methods for treating AIDS and HIV infections By Ghosh, Arun K. PCT Int. Appl. (2010), WO 2010132494 A1 20101118
34. Pyrrolidine compounds as inhibitors of beta-secretase activity and their preparation and use in the treatment of Alzheimer's disease By Bilcer, Geoffrey M.; Devasamudram, Thippeswamy; Ankala, Sudha V.; Lilly, John C.; Liu, Chunfeng; Lei, Hui; Ghosh, Arun K.; Inoue, Makoto PCT Int. Appl. (2010), WO 2010110817 A1 20100930
33. Preparation of aryldicarboxamide derivatives as inhibitors of BACE1 and methods for treating Alzheimer's disease By Ghosh, Arun K. PCT Int. Appl. (2010), WO 2010065861 A2 20100610
32. Quinazoline inhibitors of BACE 1 and methods of using for treatment of Alzheimer's disease By Ghosh, Arun K. PCT Int. Appl. (2010), WO 2010059953 A1 20100527
31. Pyrrolidine compounds which inhibit beta-secretase activity and their preparation and use in the treatment of Alzheimer's disease By Bilcer, Geoffrey M.; Devasamudram, Thippeswamy; Ankala, Sudha V.; Lilly, John C.; Liu, Chunfeng; Lei, Hui; Ghosh, Arun K.; Inoue, Makoto PCT Int. Appl. (2010), WO 2010042892 A1 20100415
30. Preparation of heterocyclylaminoalcohols for treatment of Alzheimer's disease By Ghosh, Arun K. PCT Int. Appl. (2010), WO 2010042796 A1 20100415
29. Compounds and methods for treating respiratory diseases By Ghosh, Arun K.; Takayama, Jun PCT Int. Appl. (2010), WO 2010022355 A1 20100225
28. Lasonolide compounds as reagents for inducing premature chromosome condensation and methods for treating disorders By Pommier, Yves; Zhang, Yongwei; Ghosh, Arun K. U.S. Pat. Appl. Publ. (2010), US 20100041619 A1 20100218
27. Preparation of (polyether) aminohydroxyalkyl urethanes as HIV-1 protease inhibitors By Ghosh, Arun K. PCT Int. Appl. (2010), WO 2010006050 A1 20100114
26. Aryldicarboxamide derivatives as non-peptide HIV-1 protease inhibitors and their preparation, pharmaceutical compositions and use in the treatment of HIV, AIDS and AIDS-related diseases By Ghosh, Arun K. PCT Int. Appl. (2010), WO 2010002994 A1 20100107
25. Small molecule inhibitors of HIV proteases By Ghosh, Arun K. PCT Int. Appl. (2009), WO 2009091941 A1 20090723
24. Asymmetric synthesis of (+)-peloruside A and macrocyclic cancer chemotherapy agents and methods of use By Ghosh, Arun K.; Xu, Xiaoming PCT Int. Appl. (2009), WO 2009089450 A1 20090716.
23. Preparation of (3-hydroxy-4-amino-butan-2-yl)-3-[2-(thiazol-2-yl)pyrrolidine-1-carbonyl] benzamide derivatives and related compounds as selective beta-secretase inhibitors By Ghosh, Arun K.; Liu, Chunfeng; Devasamudram, Thippeswamy; Lei, Hui; Swanson, Lisa M.; Ankala, Sudha V.; Lilly, John C.; Bilcer, Geoffrey M. PCT Int. Appl. (2009), WO 2009042694 A1 20090402
22. Isophthalamide compounds which inhibit beta-secretase activity and their preparation, pharmaceutical compositions and use in the treatment of Alzheimer's disease By Ghosh, Arun K.; Liu, Chunfeng; Devasamudram, Thippeswamy; Lei, Hui; Swanson, Lisa M.; Ankala, Sudha V.; Lilly, John C.; Bilcer, Geoffrey M. PCT Int. Appl. (2009), WO 2009015369 A2 20090129
21. Small molecule inhibitors of HIV protease dimerization for use in treatment of HIV infection and AIDS By Mitsuya, Hiroaki; Koh, Yasuhiro; Ghosh, Arun K. From PCT Int. Appl. (2008), WO 2008133734 A2 20081106
20. β-Secretase inhibitors and methods of use thereof including methods of treating of Alzheimer's disease By Ghosh, Arun K.; Lei, Hui; Devasamudram, Thippeswamy; Liu, Chunfeng; Tang, Jordan J. N.; Bilcer, Geoffrey From U.S. (2008), US 7335632 B2 20080226
19. Design and synthesis of peptidomimetic protease inhibitors containing two or more transition state isosteres, particularly hydroxyethylene and hydroxyethylamine isosteres, that overcome drug resistance By Tang, Jordan J. N.; Ghosh, Arun K. PCT Int. Appl. (2000), WO 2000048466 A2 20000824.
18. Preparation of benzene-1,3-dicarboxamides which inhibit β-secretase activity. By Ghosh, Arun K.; Kumaragurubaran, Nagaswamy; Liu, Chunfeng; Devasamudram, Thippeswamy; Lei, Hui; Swanson, Lisa; Ankala, Sudha; Tang, Jordan; Bilcer, Geoffrey PCT Int. Appl. (2006), WO 2006110668 A1 20061019.
17. Compounds which inhibit beta-secretase activity and methods of use thereof By Ghosh, Arun K.; Tang, Jordan J. N.; Bilcer, Geoffrey; Chang, Wanpin; Hong, Lin; Koelsch, Gerald E.; Loy, Jeffrey A.; Turner, Robert T.; Devasumadram, Thippeswamy U.S. Pat. Appl. Publ. (2004), US 20040121947 A1 20040624.
16. Method of preparing (3R,3aS,6aR)-3-hydroxyhexahydrofuro[2,3-b]furan and related compounds By Ghosh, Arun K.; Leshchenko, Sofiya; Noetzel, Marcus W. PCT Int. Appl. (2004), WO 2004033462 A2 20040422.
15. 2-Oxazolidinones and their use as inhibitors of animal cell motility and growth By Fenteany, Gabriel; Ghosh, Arun K.; McHenry, Kevin; Ankala, Sudha; Anjum, Sarosh; Zhu, Shoutian PCT Int. Appl. (2003), WO 2003106437 A1 20031224.
14. Preparation of carbamates as HIV protease inhibitors By Ghosh, Arun K.; Bilcer, Geoffrey M.; Devasamudram, Thippeswamy PCT Int. Appl. (2003), WO 2003078438 A1 20030925.
13. Preparation of laulimalide and epothilone derivatives as microtubule stabilizing compounds By Ghosh, Arun K. PCT Int. Appl. (2003), WO 2003076445 A2 20030918.
12. Design of β-secretase inhibitors for treatment of Alzheimer's disease based on crystal structures of β-secretase and side chain interactions in inhibitor complexes By Ghosh, Arun K.; Tang, Jordan; Bilcer, Geoffrey; Chang, Wanpin; Hong, Lin; Koelsch, Gerald; Loy, Jeff; Turner, Robert T., III PCT Int. Appl. (2003), WO 2003039454 A2 20030515.
11. Inhibitors of memapsin 2 and their use in Alzheimer's disease treatment By Tang, Jordan J. N.; Koelsch, Gerald; Ghosh, Arun K. PCT Int. Appl. (2002), WO 2002053594 A2 20020711.
10. Inhibitors of memapsin 2 and use thereof By Tang, Jordan J. N.; Hong, Ling; Ghosh, Arun K. PCT Int. Appl. (2001), WO 2001000665 A2 20010104.
9. Multidrug-resistant retroviral protease inhibitors and associated methods By Erickson, John W.; Gulnik, Sergei V.; Ghosh, Arun K.; Hussain, Khaja A. From PCT Int. Appl. (1999), WO 9967254 A2 19991229.
8. Preparation of HIV protease inhibitors By Ghosh, Arun K.; Thompson, Wayne J.; Mckee, Sean P. PCT Int. Appl. (1994), WO 9426749 A1 19941124.
7. Preparation of piperazine derivatives as HIV protease inhibitors By Kim, Byeong Moon; Vacca, Joseph P.; Ghosh, Arun K.; Guare, James P., Jr.; Huff, Joel R.; Hungate, Randall W.; Lee, Hee Yoon; Thompson, Wayne J. PCT Int. Appl. (1994), WO 9418192 A1 19940818.
6. HIV protease inhibitors with an internal lactam ring By Vacca, Joseph P.; Chen, Lin Tsen J.; Hungate, Randall W.; Ghosh, Arun K. From Can. Pat. Appl. (1993), CA 2084800 A1 19930617.
5. Dipeptide isosteres as HIV protease inhibitors useful for the treatment of AIDS By Ghosh, Arun K.; Huff, Joel R.; Thompson, Wayne J.; Lyle, Terry A.; Hungate, Randall W.; McKee, Sean P.; Lee, Hee Y. Can. Pat. Appl. (1993), CA 2075666 A1 19930217.
4. Preparation of decahydroisoquinolinecarboxamides as HIV protease inhibitors By Thompson, Wayne J.; Ghosh, Arun K.; Lee, Hee Yoon; Huff, Joel R. Eur. Pat. Appl. (1993), EP 539192 A1 19930428.
3. HIV protease inhibitors with n-terminal polyether substituents By Graham, Samuel L.; Ghosh, Arun K.; Huff, Joel R.; Scholz, Thomas H. Eur. Pat. Appl. (1993), EP 528661 A2 19930224.
2. Preparation of dipeptide isosters By Thompson, Wayne J.; Vacca, Joseph P.; Huff, Joel R.; Lyle, Terry A.; Young, Steven D.; Hungate, Randall W.; Britcher, Susan F.; Ghosh, Arun K. Eur. Pat. Appl. (1991), EP 434365 A2 19910626.
1. reparation of human immunodeficiency virus (HIV) protease inhibitors for treatment of AIDS By Sigal, Irving S.; Huff, Joel R.; Darke, Paul L.; Vacca, Joseph P.; Young, Steven D.; Desolms, S. Jane; Thompson, Wayne J.; Lyle, Terry A.; Graham, Samuel L.; Ghosh, Arun K. Eur. Pat. Appl. (1989), EP 337714 A2 19891018.