PUBLICATIONS
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Creative scientists at Pharma Inventor Inc. have published a large number of innovative patents covering various phases of medicinal chemistry, process development and synthetic organic methodology developments.
We also have published several peer-reviewed research articles in international journals in the areas of natural product synthesis, organometallic chemistry, carbohydrate, organometallic catalysis, asymmetric synthesis, glycopeptide mimetics
and so on.
Publications | January, 2020
Patents & InternationalÂ
Journal Articles :
1. Optimization of physico-chemical properties of active pharmaceutical ingredients for the treatment of major depressive disorders and methods thereof. McDonald David, Lever Melody, Sadalapure Kashinath, MSI Methylation Sciences Inc. WO/2014 (application in process).
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2. Glycine Transporter-1 Inhibitors, methods of making them and uses thereof. Cioffi Christopher L.; Wolf Mark; Guzzo Peter R.; Liu Shuang; Sadalapure Kashinath; Visweswaran Parthasarathy; Maeng Jun-Ho (Albany Molecular Research Inc.), WO/2011/153359 08-December-2011.
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3. Methods of using piperazine compounds in treating sodium Channel-mediated diseases or conditions. Kamboj, Rajender; Fraser, Robert; Sadalapure, Kashinath; Fu, Jian-Min; (Xenon Pharmaceuticals Inc., Canada). PCT Int. Appl. (May 2007), 60/939, 586
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4. Pyridazine-based SCD-1 inhibitors for use in combination therapy to treat adverse weight gain associated with a drug therapy Abreo, Melwyn; Kondratenko, Mikhail; Harvey, Daniel; Hudson, Cindy; Li, Wenbao; Tu, Chi; Sun, Sengen; Holladay, Mark; Gschwend, Heinz; Kamboj, Rajender; Winther, Michael; Fraser, Robert; Sadalapure, Kashinath; Chafeev, Mikhail; Fu, Jian-Min; Hou, Duanjie; Liu, Shifeng; Raina, Vandna; Seid Bagherzadeh, Mehran. (Xenon Pharmaceuticals Inc., Canada). PCT Int. Appl. (2006)149 pp. WO 2006086445 A2 20060817 Application: WO 2006-US4383 20060208. Priority: US 2005-651584 20050209.
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5. Preparation of piperazinylimidazo[1,2-b]pyridazine-2-carboxamides as inhibitors of Stearoyl-CoA Desaturase, Kamboj, Rajender; Fu, Jian-Min; Kodumuru, Vishnumurthy; Liu, Shifeng; Sadalapure, Kashinath; Chakka, Nagasree; Hou, Duanjie; Sun, Shaoyi. (Xenon Pharmaceuticals Inc., Canada). PCT Int. Appl. (2006), 72 pp. WO 2006034312 A1 20060330. Application: WO 2005-US33738, 20050920. Priority: US 2004-611646, 20040920.
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6. Preparation of pyridazinylpiperazinyl trifluorophenyl methanones as stearoyl-CoA desaturase inhibitors, Kamboj, Rajender; Zhang, Zaihui; Fu, Jian-Min; Kodumuru, Vishnumurthy; Sviridov, Serguei; Sadalapure, Kashinath; Liu, Shifeng; Sun, Shaoyi; Hou, Duanjie; Chakka, Nagasree, (Xenon Pharmaceuticals Inc., Can.). PCT Int. Appl. (2006), 77 pp. WO 2006034440, A2 20060330. Application: WO 2005-US34129 20050920. Priority: US 2004-611644, 20040920.
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7. Preparation of salacinol sulfate-containing alditols as glycosidase inhibitors and antidiabetic agents, Pinto, Brian Mario; Johnston, Blair D.; Ghavami, Ahmad; Szczepina, Monica Gabriela; Liu, Hui; Sadalapure, Kashinath; Jensen, Henrik H.; Kumar, Nag Sharwan; Nasi, Ravindranath, (Simon Fraser University, Canada). U.S. Pat. Appl. Publ. (2006), 121 pp., Application: US 2006-368014, 20060302.
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8. Preparation of salacious sulfate-containing alditols as glycosidase inhibitors and antidiabetic agents, Pinto, Brian Mario; Johnston, Blair D.; Szczepina, Monica Gabriela; Liu, Hui; Sadalapure, Kashinath; Ghavami, Ahmad. U.S. Pat. Appl. Publ. (2005), 62 pp., Cont.-in-part of U.S. Ser. No. 226,657.
9. Methods for the synthesis of substituted tetrahydrofuran compounds Mukund Shankar Chorghade, Mukund Keshao Gurjar, Palakodety Radha Krishna, Sista Venkata Sai Lalitha, Kashinath Sadalapure, Susanta Sekhar Adhikari, Andappan Murugaiah and others. International Patent # WO 00/01683 dated Jan. 13, 2000.
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10. Substituted Oxygen Alicyclic Compounds, Including Methods for Synthesis thereof Mukund Shankar Chorghade, Mukund Keshao Gurjar, Palakodety Radha Krishna, Sista Venkata Sai Lalitha, Kashinath Sadalapure, Susanta Sekhar Adhikari, Vavilala Goverdhan Reddy, Bethi Sridhar Reddy, Hymavathi Lanka, Aminul Islam, Chittineni Hariprasad, Alla Venkata Rama Rao. International Patent # WO 00/01381 dated Jan. 13, 2000.
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11. Substituted oxygen alicyclic compounds, including methods for synthesis thereof Adhikari S. S.; Krishna L. M.; Prasad T. R.; RAO A. V. R.; Rao B. V.; Reddy B. S.; Islam A.; Lanka H.; Sreenivas P.; Gurjar M. K.; Krishna P. R.; Murugaih A. M. S.; Prasad C. H.; Reddy V. G.; Sadalapure K.; Sharma G. V. M.; Lalitha S. V. S.; Chorghade M. S.; Mhaskar S. V. US Patent No. 6566538.
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12. Methods of synthesis of substituted tetrahydrofuran compound Adhikari S. S.; Krishna L. M.; Prasad T. R.; RAO A. V. R.; Rao B. V.; Reddy B. S.; Islam A.; Lanka H.; Sreenivas P.; Gurjar M. K.; Reddy V. G.; Sadalapure K.; Sharma G. V. M.; Lalitha S. V. S.; Chorghade M. S.; Mhaskar S. V. US Patent No. 6541647.
13. Substituted oxygen alicyclic compounds, including methods for synthesis thereof Adhikari S. S.; Krishna L. M.; Prasad T. R.; RAO A. V. R.; Rao B. V.; Reddy B. S.; Islam A.; Lanka H.; Sreenivas P.; Gurjar M. K.; Krishna P. R.; Murugaih A. M. S.; Prasad C. H.; Reddy V. G.; Sadalapure K.; Sharma G. V. M.; Lalitha S. V. S.; Chorghade M. S.; Mhaskar S. V. US Patent No. 6433197.
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14. Methods for synthesis of substituted tetrahydrofuran compound Adhikari S. S.; Krishna L. M.; Prasad T. R.; RAO A. V. R.; Rao B. V.; Reddy B. S.; Islam A.; Lanka H.; Sreenivas P.; Gurjar M. K.; Krishna P. R.; Murugaih A. M. S.; Prasad C. H.; Reddy V. G.; Sadalapure K.; Sharma G. V. M.; Lalitha S. V. S.; Chorghade M. S.; Mhaskar S. V. US Patent No. 6310221.
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15. Substituted oxygen alicyclic compounds, including methods for synthesis thereof Adhikari S. S.; Krishna L. M.; Prasad T. R.; RAO A. V. R.; Rao B. V.; Reddy B. S.; Islam A.; Lanka H.; Sreenivas P.; Gurjar M. K.; Krishna P. R.; Murugaih A. M. S.; Prasad C. H.; Reddy V. G.; Sadalapure K.; Sharma G. V. M.; Lalitha S. V. S.; Chorghade M. S.; Mhaskar S. V. US Patent No. 6306895.
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16. A Novel Synthesis of a Triazolesulfonyl Chloride as a Precursor for GlyT-1 Inhibitors Visweswaran Parthasarathy; Edmund Carulli; Kashinath Sadalapure; Ron Buckle; Christopher L. Cioffi; Karl E. Reineke; Shuang Liu; UK-Singapore Symposium on Contemporary Strategies and Practices in Medicinal Chemistry, 8 September 2011, Biopolis, Singapore.
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17. 2’-Fluoro-4’-thioarabino-modified oligonucleotides: conformational switches linked to siRNA activity Watts Jonathan K., Choubdar Niloufar, Sadalapure Kashinath, Robert Francis, Wahba Alexander S., Pelletier Jerry, Pinto B. Mario and Damha Masad J. Nucleic Acids Research, 35 (5), 2007, 1441-1451.
18. Synthesis and conformational analysis of 2'-fluoro-5-methyl-4'-thioarabinouridine (4'S-FMAU) Watts, Jonathan K.; Sadalapure, Kashinath; Choubdar, Niloufar; Damha, Masad J.; Pinto, B. Mario. Abstracts of Papers, 231st ACS National Meeting, Atlanta, GA, United States, March 26-30, 2006, CARB-003.
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19. Synthesis of functionalized amphiphilic glycoconjugates and glycoclusters Dubber, Michael; Patel, Anupama; Sadalapure, Kashinath; Aumueller, Ingo; Lindhorst, Thisbe K, Eur. J. Org Chem, 23, 2006, 5357-5366.
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20. Synthesis and Conformational Analysis of 2'-Fluoro-5-methyl-4'-thio arabinouridine(4'S- FMAU). J. K. Watts, K. Sadalapure, N. Choubdar, B. Mario Pinto, and M. J. Damha J. Org. Chem., 71 (3), 2006, 921 –925.
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21. Fluorescent Labelled Thiourea-bridged Glycodendrons. Krist Pavel; Vannucci Luca; Kuzma Marek; Man Petr; Sadalapure Kashinath; Patel Anupama Bezouska Karel; Pospisil Milan; Petrus Ladislav; Lindhorst Thisbe K.; Kren Vladimir ChemBioChem., 5 (4), 2004, 445-452.
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22. Effects of N-acetyl-glucosamine-coated glycodendrimers as biological modulators in the B16F10 melanoma model in vivo. Vannucci Luca; Fiserova Anna; Sadalapure Kashinath; Lindhorst Thisbe K; Kuldova Marketa; Rossmann Pavel; Horvath Ondrej; Kren Vladimir; Krist Pavel; Bezouska Karel; Luptovcova Martina; Mosca Franco; Pospisil Miloslav, International J. Oncology, 23 (2), 2003, 285-296.
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23. Glycodendrimeric ligands of C-type lectin receptors as therapeutic agents in experimental cancer. M. Pospisil; L. Vannucci; A. Fiserova; K. Krausova; O. Horvath; V. Kren; F. Mosca; Th. K. Lindhorst; K. S. Sadalapure; K. Bezouska, Adv. Exp. Med. Biol., 495, 2001, 343-347. A general entry in to glycopeptide dendrons, K. S. Sadalapure; Th. K. Lindhorst, Angew. Chem., Int. Ed. 39 (11), 2000, 2010-2013.
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24. Glucose-based AB2-building blocks for the construction of branched glycopeptidomimetics C. Kieburg; K. S. Sadalapure; Th. K. Lindhorst, Eur. J. Org. Chem., 11, 2000, 2035-2040.
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25. A carbohydrate route to CMI-977: a potent 5-lipoxygenase inhibitor. M. S. Chorghade; K. S. Sadalapure; S. Adhikari; SVS. Lalitha; AMS. Murugaiah; P. Radhakrishna; B. S. Reddy; M. K. Gurjar, Carbohydr. Lett., 3 (6), 2000, 405-410.
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26. Synthesis of (2S, 5S)-trans-5-(4-fluorophenoxymethyl)-2- (1-N-hydroxyureidyl)-3-butyn-4-yl)-tetrahydrofuran (CMI-977) M. S. Chorghade; M. K. Gurjar; S. Adhikari; K. S. Sadalapure; SVS. Lalitha; AMS. Murugaiah; P. Radhakrishna, Pure and Appl. Chem., 71 (6), 1999, 1071-1074.
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27. Synthesis and anomeric stability of (16)-thiourea-linked pseudo- oligosaccharides J. M. Benito; C. O. Mellet; K. S. Sadalapure; Th. K. Lindhorst; J. Defaye; J. M. G. Fernández, Carbohydr. Res., 320, 1999, 37-48.
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28. Development of cost-effective syntheses of a potent 5-LO inhibitor M. S. Chorghade; M. K. Gurjar; K. S. Sadalapure; S. V. S. Lalitha; A. M. S. Murugaiah; P. Radhakrishna; S. Adhikari, Book of Abstracts, 216th ACS National Meeting, Boston, 1998, August 23rd –27th.
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29. Kinetic resolution of aryl glycidyl ethers: a practical synthesis of optically pure -blocker, S-metoprolol M. K. Gurjar, K. S. Sadalapure, S. Adhikari, B. V. N. B. S. Sarma, M. S. Chorghade, Heterocycles, 48 (7), 1998, 1471-1476.
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30. A practical synthesis of ® and (S) -benzyl glycidols by hydrolytic kinetic resolution M. K. Gurjar; BVNBS. Sarma; K. S. Sadalapure; S. Adhikari, Synthesis, 10, 1998, 1424-1424.
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31. Zaragozic acid : unusual stereochemical dependence in anhydride formation of carbohydrate templates M. K. Gurjar; S. K. Das; K. S. Sadalapure, Tetrahedron Lett., 36 (11), 1995, 1933-1936.
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32. A Modular Approach for the Synthesis of Oligosaccharide Mimetics, Anupama Patel and Thisbe K. Lindhorst, J. Org. Chem. 2001, 66(8), 2674-2680.
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33. Synthesis of “mixed type” oligosaccharide mimetics based on a carbohydrate scaffold. Anupama Patel and Thisbe K. Lindhorst, Eur. J. Org. Chem. 2002, 1, 79-89.
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34. Efficient Synthesis of Isotopically Pure Isotope-Coded Affinity Tagging Reagents. Anupama Patel and David M. Perrin, Bioconjugate Chem. 2004, 15, 224-230.
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35. Synthesis of functionalized amphiphilic glycoconjugates and glycoclusters. Dubber, Michael; Patel, Anupama; Sadalapure, Kashinath; Aumueller, Ingo; Lindhorst, Thisbe K, Eur. J. Org Chem, 23, 2006, 5357-5366.
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36. Fluorescent Labelled Thiourea-bridged Glycodendrons.
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37. Krist Pavel; Vannucci Luca; Kuzma Marek; Man Petr; Sadalapure Kashinath; Patel Anupama; Bezouska Karel; Pospisil Milan; Petrus Ladislav; Lindhorst Thisbe K.; Kren Vladimir ChemBioChem., 5 (4), 2004, 445-452.
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38. Multivalent glycomimetics: synthesis of nonavalent mannoside clusters with variation of spacer properties. Anupama Patel and Thisbe K. Lindhorst; Carb.Res. 2006, 341(10), 1657-1668.
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39. A mechanism-based proteomic strategy for monitoring cysteine proteases using cathepsin B-targeted ICAT reagents. Anupama Patel, Omid Hekmat, John S. Mort, Stephen G. Withers, and David M. Perrin. Unpublished work.
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40. Synthesis of the C30-C38 fragment of the marine macrolide Altohyrtin, Anupama Patel and Mukund K. Gurjar. Unpublished work.