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Patents and Publications

24 Issued US Patents (Anita Mehta, President and CEO)

1-(4-Arylpiperazin-1-yl)-omega-[n-(alpha,omega-dicarboximido)]-alkanes useful as uro-selective alpha1 -adrenoceptor blockers US Patent 6,083,950 (Issued July 2000, assigned to Ranbaxy), US Patent 6,090,809  (Issued July 2000, assigned to Ranbaxy), US Patent 6,420,366 B1, (Issued July 2002, assigned to Ranbaxy), US patent 6,420,559 B1, US Patent 6,410,735 (Issued June 2002, assigned to Ranbaxy); Oxazolidinone derivatives as antimicrobials US Patent 6,734,307 (issued May, 2004, assigned to Ranbaxy);1-(4-Arylpiperazin-1-yl)-omega-[N-(alpha,omega-dicarboximidoL)]-alkanes useful as uro-selective alpha 1-adrenoceptor blockers, US Patent 6,812,344 (issued November 2004, assigned to Ranbaxy); Oxazolidinone piperazinyl derivatives as potential antimicrobials, US Patent 6,956,040 (issued October 2005, assigned to Ranbaxy); 3,6-Disubstituted azabicyclo derivatives as muscarinic receptor antagonists US Patent 7,232,835 (issued June 2007, assigned to Ranbaxy); 3,6-disubstituted azabicyclo [3.1.0]hexane derivatives useful as muscarinic receptor antagonists, US Patent 7,265,147 (issued September 2007); Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo (3.1.0) hexane derivatives as muscarinic receptor antagonists US Patent 7,288,562 (issued October 2007, assigned to Ranbaxy); 3,6-disubstituted azabicyclo [3.1.0] hexane derivatives useful as muscarinic receptor antagonists US Patent 7,399,779 (issued July15, 2008, assigned to Ranbaxy); 3,6-disubstituted azabicyclo [3.1.0] hexane deriviatives useful as muscarinic receptor antagonists US Patent 7,410,993 (Issued August 2008 ,assigned to Ranbaxy); Azabicyclo derivatives as muscarinic receptor antagonists US Patent 7,446,123 (Issued Nov 2008), 1-substituted-3-pyrrolidine derivatives as muscarinic receptor antagonists US Patent 7,465,751 (issued Dec 2008, assigned to Ranbaxy), US Patent 7,488,748 (issued Feb. 09), Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists US Patent 7,519,905 (issued April 2009, assigned to Ranbaxy), Azabicyclo derivatives as muscarinic receptor antagonists US Patent 7,544,708 Azabicyclo derivatives as muscarinic receptor antagonists (Issued June 2009, assigned to Ranbaxy), Flavaxate derivatives as muscarinic receptor antagonists US Patent 7,501,443 (March 2009, assigned to Ranbaxy); 3,6-Disubstituted azabicyclo hexane derivatives as muscarinic receptor antagonists US Patent 7,560,479 (issued July 2009, assigned to Ranbaxy); Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists US Patent 7,592,359 (issued Sept 2009, assigned to Ranbaxy); Electromuscular incapacitation device and methods US patent 7,736,237 (issued June 2010, assigned to Avocet).


24 Issued US Patents (Mukund Chorghade, CSO)

US Patent 5,424,444 (issued June 13, 1995); European Patent Application # 94931741.6-2101, filed 08-30-1994. German Patent: GR 3036387T  Publication: November 30, 2001, US Patent 5,760,216 (issued June 2, 1998); Canadian Patent Application # 2,195,873, filed September 15, 1994., US Patent 6,255,498 dated July 3, 2001, filed October 16, 1998., U S Patent 6,306,895  dated October 23, 2001 (application # 09/347,113, filed July 2, 1999). European Patent Application # 99933655.5-2112, US Patent 6,310,221 dated October 30, 2001 (application # 09/347,087, filed July 2, 1999). European Patent Application # 99930868.7-2117, US Patent ,403,814 dated June 11, 2002, filed October 16, 1998, U.S.S.N. 09 / 418637.  US Patent 6,255,498 B1, July 3, 2001 Publication: EP: 1121338 August 8, 2001, US Patent 20021289491 dated September 12, 2002, filed October 16, 1998, US Patent 6,433,197  dated August 13, 2002 (application # 969681 filed October 2, 2001). CA 2342156 January 13, 2000, US Patent 6,541,647 dated April 1, 2003, filed October 15, 1999, U. S. S. N. 09 / 418637.  US Patent 6,255,498 B1, July 3, 2001 CA 2342156 January 13, 2000, U S Patent 6,566,538  dated May 20, 2003 (application # 185178 filed June 27, 2002). US Patent 6433197 August 13, 2002, filed October 16, 1998, U.S.S.N. 09 / 419354 European EP 1123095 Publication: August 16, 2001, US Patent 6,878,628, April 12, 2005, US Patent 7,038,073, May 2, 2006, US Patent 6,875,882, April 5, 2005, US Patent 7, 002, 036, February 21, 2006, US Patent 6,903,220 June 7, 2005; US Patent 7,285,676, October 23, 2007, US Patent 6861,532, March 1, 2005, US Patent 6,875,883, April 5, 2005, US Patent 6,846,958 dated Jan 25, 2005 US Patent 6,982,335, January 3, 2006; US Patent 7,285,670, October 23, 2007,  US Patent 7,294,718, November 13, 2007.

Selected Publications (Anita Mehta)

1. Synthesis and biological activity of novel oxazolidinones, Bioorg. Med. Chem. Lett. 200915, 6424-28.
2. Synthesis and antimicrobial activity of potent heterticyclic oxazolidinones and the identification of RBX 7800, Bioorg. Med. Chem. Lett. 200717, 6714-19.
3. Synthesis and optimization of novel and selective muscarinic (M3) receptor antagonistsics, Bioorg. Med. Chem. Lett. 200517, 5256-60.
4. Synthesis and SAR of novel Oxazolididnones: Discovery of Ranbezolid. Bioorg. Med. Chem. Lett. 2005, 15, 4261-67.
5. Synthesis and antimicrobial activity of novel Thiazolidinones, ARKIVOC2005 (ii), 46-5.
​6. Design, synthesis and activity of novel derivatives of Oxybutynin and Tolterodine, Bioorg. Med. Chem. Lett200515, 2093-96.
​7. A general and efficient synthesis of 3,6-diazabicyclo [ 3.2.1.] octanes, Tetrahedron199248 4985.
8. A simple and efficient synthesis of 8- methyl- 3,8-diazabicyclo [3,2,1] octane (azatropane) and 3- substituted azatropanes therefrom using pyroglutamic acid. Tetrahedron Lett. 2007, 48, 545-548.
​9. A Study of the Michael Reaction of 2'- Hydroxychalcones and a Facile Formation of 4H-Pyran Derivatives. Heterocycles 1983, 50, 2369-77.
10. Base Catalysed Isomerisation of 3-Benzylidine-4-chromanones: Formation of 3- Methyl Flavones.  Indian Journal of Chemistry 1983, 22B, 759-61.
​11. Synthesis of 2,2- Dimethyl -2H- Pyran-Fused Flavanols Using the Modified Algar-Flynn-Oyamada Reaction. Bull. Chem. Soc. Jpn. 1983, 56, 1267-68.
​12. A New General Synthesis of polyhydroxyisoflavanones., J. Chem. Soc. Chem. Comm.19856, 338-339.
13. A New Synthesis of homoisoflavonones. Tetrahedron198541, 5933-37.
14. ​A New General Synthesis of hydroxy- and methoxy-isoflavanones, J. Chem. Soc., Perkin Trans. 11986, 215-20.
​15. Improved efficiency and selectivity in peptide synthesis : Use of triethylsilane as a carbocation scavenger in deprotection of t-butyl esters and t-butyloxycarbonyl-protected sites. Tetrahedron Lett1992, 33, 5441-44.
​16. Use of transferred nuclear-Overhauser-effect spectroscopy to measure the bound conformation of a disulphide-replaced analogue of glutathione disulphide as an inhibitor of yeast glutathione reductase. Eur. J. Biochem.1994, 221, 793-99.
​17. Preparation of .beta.-substituted tryptophan derivatives: comparison of the reactivity of N-methylindole toward aziridine-2-lactones and aziridine-2-carboxylic esters and interpretation of results using MNDO calculations. J. Org. Chem., 199459, 434-41. 
​18. Ortho-directed lithiation studies of 3-carboxy-.beta.-carbolines: a direct route to 4-substituted derivatives. J. Org. Chem.199358, 7587-90.

Selected Presentations and Seminars

-The Biochemical Society, 646th Meeting, University of Leeds, UK, March 1993. Title: Novel Inhibitor of Yeast Glutathione Reductase. 
-10th International Conference on Mathematical Modeling and Scientific Computing at Boston, USA, July 1995. Title: Drug Design through Computation and Prediction of Important Organic Reactions using MNDO Calculations. 
-Biosym Incorporation, San Diego, USA, 1995. Title: Proposed Simple Model for Reducing the Number of Analogues to be synthesized for Drug Discovery Process. 
-6th National Organic Synthesis Trust, Pune, India, 1997. Title: Meeting the Challenges of Antibacterial Resistance through Chemical Approaches. 
-ICC Summit at Amsterdam, June 2001, A poster presentation on newly discovered antibacterial NCE-RBx 7644. 
-6th Meeting of the Society of Biologists & Chemists, Baroda, 2002. Cheminformatics, Virtual Screening and Data Mining in New Drug Discovery Research.
-Antibacterial and Antifungal Drug Discovery and Development ICC Summit, Amsterdam, June 2001. Poster presentation - RBx 7644: A novel Oxazolididnone Active against Gram Positive Bacteria.
-223rd American Chemical Society National Meeting, Orlando, Florida, USA April 2002. Paper number 208, Title: Pharmacophore Generation, Development and Use in Drug Design: Accelerated Drug Discovery through Prediction of Chemical Reactivities.
-42nd Interscience Congress of Antimicrobial Agents and Chemotherapy (ICAAC), San Diego, USA September, 2002. Poster presentation: In-vitro Activity of RBx 7644, an extended spectrum investigational oxazolidinone (Abstract F -1288).
-42nd ICAAC, San Diego, September, 2002. Poster presentation: In-vitro susceptibility breakpoint determination for RBx 7644 (Abstract F-1294).
-42nd ICAAC, San Diego, September, 2002. Poster presentation: Subacute toxicity of RBx 7644 by oral route in rats. (Abstract F-1300).
-227th ACS National Meeting, Anaheim, CA, USA, April 2004. Presentation on Novel Derivatives of Tolterodine in hunt for M3 selective Muscarinic Antagonists.
-227th ACS National Meeting, Anaheim, CA, USA, April 2004. Synthesis and SAR of novel Oxazolidinones. 
-Poster Presentation Bio 2006, Chicago, USA


Selected Publications (Mukund Chorghade)

1. Synthesis of Unusual Tricyclic Ring Systems of Biological Interest. Heterocycles2007, 73, 269-74. Issue honoring Ivar Ugi
2. Approaches for Drug Discovery and Development. Current Bioactive Compounds, 20084, 201-12.
3. Practical syntheses of 4-fluoroprolines. J. Fluorine Chem., 2008129, 781-87.
4. A short total synthesis of (+)-cryptocarya diacetate. Heterocycles,  200977, 945-52. Issue honoring Keiichiro Fukumoto.
5. Drug Discovery and Development, Volumes I and II, Mukund S. Chorghade(ed), John Wiley and Sons, 2006 and 2007, Drug Discovery and Development (2007), 2 279-308.
6. Drug Discovery and Development”, Volumes I and II, Mukund S. Chorghade(ed), John Wiley and Sons, 2006 and 2007 Drug Discovery and Development (2007), 2 309-353.
7. Chiral Glycolate Equivalents for the Asymmetric Synthesis of alpha-Hydroxycarbonyl Compounds. Bull. Chem. Soc. Jpn, 200780, 1451-72.
8. Expectations of a chemist from a ‘good’ QSAR Model. QSAR World, June 11 2007.
9. A Short and Efficient Synthetic Strategy for the Total Syntheses of (S)-(+)- and (R)-(–)-Plakolide A. Eur. J. Org. Chem.200730, 5059-63.
10. Mukund S. Chorghade*, Julian White, Brian Warrington, Stephanie Hawkes, Richard Gray, Mark Gilligan, Ian Baxendale and Steven Ley, “Go with the Flow”, Speciality Chemicals Magazine, October 2007, 42-46




Note: None of the patents issued belong to Chicago Discovery Solutions. Chicago Discovery solutions has filed patent applications (not listed here).
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