Dr. Khashayar Karimian

khashayar karimian

22 07 2017 07:01

کد خبر : 10024969

تعداد بازدید : 176

 

                                    
 
 
Khashayar Karimian
Professor 
Ph.D. Bioorganic Chemistry, Louisiana State University, 1976
E-mail: kkarimian@arsato.com
 
 
                                                                                                                                   

                                          

ACADEMIC POSITIONS:

2013-               Invited Member, Chemistry Branch of the Iranian Academy of Science

2010-               Adjunct Professor, Department of Chemical Engineering, College of Engineering, University of Tehran

2002-               Adjunct Professor of Biochemistry, Institute of Biochemistry and Biophysics, University of Tehran

1996-1999       Member, Grant Selection Committee (Chemistry and Biochemistry), National Science and Engineering Research Council (NSRC) of Canada.

1996-1999       Member, Grant Selection Committee for Major Instruments (Chemistry and Biochemistry), National Science and Engineering Research Council (NSERC) of    Canada.

1985-1989       Visiting Professor and Lecturer, Department of Chemistry, University of Toronto

1979-1985       Assistant Professor of Biochemistry, Institute of Biochemistry and Biophysics, University of Tehran

 

INDUSTRIAL POSITIONS:

2015-                  Chairman, Ajand Pharmaceutical Holding Inc.

2014-                  President, Andisheh Pharmaceutical Sciences Research Center Inc.

2011-                  Vice President, Pharmaceutical Active ingredients, Chemicals and Packaging Material Syndicate (Iran)

2002-2012          Chairman and President, Arasto Pharmaceutical Chemicals Inc.

2002-                  Chairman, Avicenna Pharmaceuticals Inc.

1996-2003          Chief Scientific Officer, Medicinal Chemistry, Apotex Research Inc.

1996-1999          Head, Medicinal Chemistry, Apotex Inc.

1995-1996          General Manager, Fine Chemicals Division, Apotex Research Inc.

1994-1995          Director, Fine Chemicals Division, Apotex Research Inc.

1993-1994          Special Advisor, Apotex Inc.

1990-1992          Vice President, Scientific Affairs, ACIC (Canada) Inc.

1988-1990          Vice President, Research and Development, ACIC (Canada) Inc.

1986-1988          Director of Research and Development, ACIC (Canada) Inc.

1980-1984          Member of the Board of Directors, Iran Active Charcoal Company.

1979-1984          Consultant to the Board of Directors, Fine Chemicals Industries (TEMAD), Iranian Ministry of Health.

1979-1984          Consultant to the Board of Directors, Center for Pharmaceutical Research (DP).Iranian Ministry of Health.

 

GRANTS:

2017-2019       Presidential National Grants for Science-Based Companies (Arasto Pharmaceutical Chemicals Inc.) 24 Billion Rials (US $ 686,000),

2017-2019       Presidential National Grants for Science-Based Companies (Avicenna Laboratories Inc.) 14 Billion Rials (US $ 400,000),

2012-2015       Presidential National Major Research Grant 18 Billion Rials (US $ 1.6 Million),

"Industrial Production of 9 Anti-Cancer Active Pharmaceutical Ingredients and the Processes Thereof"

1998-2001       Ontario Research and Development Challenge Fund Grant No. 113-98UI CAN $ 750,000.  Collaborative research with Dept. of Biophysics, University of Toronto, "Rational Design of Human Rhinovirous 3C Protease Inhibitors"

1998-2001       National Science and Engineering Research Council Grant No. CRD 661-104-97 CAN $ 190,000, Collaborative research with Dept. of Chemistry, University of Montreal, "Rational Design of Trans-glutaminase Inhibitors"

1995-1998       National Research Council, Industrial Research Assistance Program Grant No. 25323U CAN $ 1,050,000.  Collaborative research with School of Medicine, McMaster University, "Rational Design of 1,2,4-thiadiazole: A Novel Class of Potential Therapeutics for the Treatment of Ulcer".

1989-1992       National Research Council, Industrial Research Assistance Program Grant No. 90765 CAN $ 80,000.  Collaborative research with Cross Cancer Institute, University of Alberta, "Rational Design of 3'-Cyclocitidines: A Novel Class of Potential Anti-neoplastics".

1982-1985       Iranian Organization for Scientific and Industrial Research Grant CAN $ 30,000. "Economical Synthesis of Ara-C and Related Novel Anti-neoplastics".

1979-1982       University of Tehran Operating Grant No. 36-426 CAN $ 200,000. Institute of Biochemistry and Biophysics, University of Tehran, "Mechanism of Exchange of   C-2 Proton in Thiazolium Salts".

1979-1980       Ministry of Science and Higher Education Grant No. 600-5-36-3 CAN $ 100,000. Institute of Biochemistry and Biophysics, University of Tehran, "Mechanism of Exchange of C-2 Proton in Thiazolium Salts".

 

CV

karimian-pr

21 07 2017 19:47

کد خبر : 10024954

تعداد بازدید : 53

      

      PROFESSIONAL DEGREES:
 
     B.Sc.  Biochemistry, Louisiana State University, 1972
     Ph.D.  Bioorganic Chemistry, Louisiana State University, 1976

karimian-publications

21 07 2017 19:54

کد خبر : 10024939

تعداد بازدید : 96

 

PUBLICATIONS: 
 
1. Fischer, H.H.; Wiley Jr., R.A.; Lin. H-N.; Karimian, K., Politz, S.M., "New Melanpolide Sesquiterpene Lactones from Melanpodiumleucantham", Phytochem. 1975, 14, 2241.
 
2. Karimian, K.; Risinger, G.E., "An Improved Procedure for the Synthesis of 2-Acetyl-3-(2-methyl-4-aminopyridine-5-yl) methyl-3a-methylperhydrofuro [2,3d] thiazole", Org. Prep. Inter. 1978, 10, 45.
 
3. Risinger, G.E.; Karimian, K.; Jungk, S.; Simpson, J., "On the Biosynthesis of Artemisia Ketone and Bakuchiol", Cel. Moll. Life Sci., 1978, 34, 1121.
 
4. Karimian, K.; Ganjian, I.; Askari, M., "Evidence for the Involvement of a Tetrahedral Intermediate in H-D exchange of Thiazolium Ion", Tetrahedron Lett., 1981, 22, 22581.
 
5. Karimian, K.; Askari, M.; Farahani, M., Sachinvala, N.; "Am Improved Procedure for the  Synthesis 2-Alkyldihydrothiamine Ketones", Synthesis, 1981 , 48.
 
6. Karimian, K., Mohtarami, F.; Askari, M., "Mechanism of Base-Catalysed Hydrogen-Deuterium Exchange in Thiazolium Ion: Evidence for the  Involvement of a Tetrahedral Intermediate", J. Chem. Soc. Perkin II, 1981, 1538.
 
7. Gorgani, M. N-; Karimian, K., "Non-ionic Adsorptive Immobilization of Proteins to Palmityl-Sepharose 4-B", Eur. J. Biochem, 1982, 123, 401.
 
8. Askari, M.; Karimian, K., "Conformational Studies of Some Acyclic Tetrasulfides by Molecular Mechanics and MINDO/3 Methods" J. Molecular Structure, 1983, 92, 347.
 
9. Gorgani, M. N-; Karimian, K., "Enzyme Immobilization on Palmityl-Sepharose" Biotech. Bioeng.",  1983, 25, 2617.
 
10. Karimian, K.; Mohanazadeh, F.; Rezai, S.; "Application of Polymer-bound Thiazolium Salts to the Synthesis of Acyloins and Benzoins: Effects of Solvent and Substituents of the Thiazolium Nucleolus" J. Heterocycl. Chem., 1983, 20, 1119.
 
11. Gorgani, M. N-; Karimian., K.; Massih, A.; "Effect of Salt Concentration on Binding of Proteins to a Non-Ionic Adsorbent" Experientia, 1984, 40, 81.
 
12. Gorgani, M. N-; Karimian, K., "Interaction of Proteins With Triton X-100-Substituted Sepharose 4-B" Biotech. Bioeng.,  1984, 26, 565.
 
 
13. Gorgani, M. N-; Karimian, K.; Mohanazadeh, F., "Synthesis, Characterization and Properties of Hexadecyl Silica; A Novel Hydrophobic Matrix for Protein Immobilization" J. Am. Chem. Soc., 1985, 13, 227.
 
14. Kluger, R.; Stergiopoulos, V.; Gish, G.; Karimian. K., "Chiral Intermediates in Thiamine Catalysis: Resolution and Pyrophosphorylation of Hydroxyethylthiamin" Bioorg. Chem., 1985, 13, 227.
 
15. Gorgani, M. N-; Karimian, K., "Use of Hexadecy Fractosil as a Hydrophobic Carrier for Adsorptive Immobilization of Proteins" Biotech. Bioeng. 1986, 28, 1037.
 
16. Karimian, K.; Mohanazadeh, F., "A Convenient Synthesis of 1'-Alkyl- and 1'-Benzylthiazolium Salts", Synthesis, 1986, 1065.
 
17. Karimian, K., "A Very Inexpensive NMR Tube Washer", J. Chem. Education, 1986, 63, 914.
 
18. Kluger, K.; Karimian, K.; Gish, G.; Pangborn, W.A.; DeTitta, G.T., "Chirality of Intermediates in Thiamine Catalysis: Structure of  (+)-2-(1-Hydroxyethy)-3, 4-Dimethyl-5-(2-Hydroxyethyl) thiazolium Iodide, The Absolute Stereochemistry of the Enantiomers of 2-(1-Hydroxyethyl) thiamine, and Enzymatic Reactions of the Diphosphate", J. Am. Chem. Soc., 1987 , 109, 618.
 
19. Kluger, R.; Karimian, K.; Kitumara, K., "Chiral Intermediates in Thiamine Catalysis.  The Stereochemical Course of Decarboxylation Step in the Conversion of Pyruvate to Acetaldehyde", J. Am. Chem. Soc., 1987, 110, 63.
 
20. Bearne, S.L.; Gish, G.; Karimian, K.; Kluger, R., "Direct Selective Phosphorylation of the Primary Hydroxyl Group in Hydroxyethyl Thiamine by Modified Phosphoric Acid-Creosol Solution and Evaluation of the Extension of the Method to Nucleosides", Bioorg. Chem., 1989, 17, 224.
 
21. Mirzayans, R.; Enns, L.; Cubitt, S.; Karimian, K.; Radatus, B.; Paterson, M., "Effect of  DNA Polymerase Inhibitors on Repair of  δ-Ray-Induced DNA Damage in Proliferating (Intact Versus Permeable) Human Fibroblast: Evidence for Probable Differences in the Modes of Action of Aphidicolin and 1-β-D-Arabinofuran Tosylcytosine", Biochem. Biophys. Acta, 1994, 1227, 92.
 
22. Mirzayans, R.; Cubitt, S.; Enns, L. Karimian, K.; Radatus, B.; Hirani-Hojatti, S.; Murthy, K.; Paterson, M., "Comparative Genotoxicity of 2,3--Cyclocytidine and 1--D-Arabinofuranosylcytosine in Human Tumor Cell Lines" Carcinogenesis, 1994, 15, 2319.
 
23. Tam, T.; Leung-Tong, R.; Li, W.; Karimian, K., "Recent Advances in Proton Pump Inhibitors", Invest. Drugs, 2000, 3, 1064.
 
24. Leung-Tong, R.; Li, W.; Tam, T.; Karimian, K., "Thiol-Dependent Enzymes and their inhibitors: A Review", Curr. Med. Chem. 2002, 9, 979. 
 
25. Tam, T.; Leung-Tong, R.; Li, W.; Wang, Y.; Karimian, K.; Spino, M., "Iron Chelation Research: Past Present, and Future", Curr. Med. Chem. 2003, 10, 983.
 
26. Leung-Toung, R.; Tam, T. F. ; Wodzinska, J.; Li, W.; Lowrie, J.;  Kukreja, R.; Desilets, D.; Karimian, K. ; Tam, T.F.,  "1,2,4-Thiadiazole: A Novel Cathepsin B Inhibitor",  Bioorg. Med. Chem., 2003, 11, 5529.  
 
27. Tam, T.F.; Leung-Toung, R.; Li, W.;  Spino, M.;  and Karimian, K. "Medicinal Chemistry and Properties of 1,2,4-Thiadiazoles" Min. Rev. Bio-org.  Chem.  2005, 5, 367.
 
28. Leung-Toung, R.; Tam, T.F.; Wodzinska, J.M.; Zhao; Y.; Lorwrie; J.; Simpson; C. D..;  Karimian, K.; Spino, M "3-Substituted Imidazo[1,2-d][1,2,4]-thiadiazles: A Novel Class of Factor XIIIa Inhibitors, Medicinal", J. Med. Chem.  2005, 48, 2266.
 
29. Leung-Toung,`R.; Tam, T.F.;  Zhao, Y.;  Simpson, C.D.;  Li, W.; Desilets, D.; and  Karimian, K. " Synthesis of 3-Substituted Bicyclic Imidazo[1,2-d][1,2,4]thiadiazoles and Tricyclic Benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazoles", J. Org. Chem., 2005,  70, 6230.
 
30. Regis Leung-Toung, Yanqing Zhao, Wanren Li, Tim F. Tam, Khashayar Karimian and Michael Spino "Thiol Proteases: Inhibitors and Potential Therapeutic Targets" Curr. Med. Chem. 2006, 13, 547.
 
31. Yadegari, H.; Jabbari, A.; Heli, H.; Moosavi-Movahedi, A.A.; Karimian, K.; Khodadadi, A. "Electrocatalytic Oxidation of Deferiprone and its Determination on a Carbon Nanotube Modified Glassy Electrode", Electrochimica Acta, 2008, 53, 2907.
 
32. Hajjizadeh, M.; Jabbari, A.; Heli, H.; Moouavi-Movahedi, A.A.; Shefiee, A.; Karimian, K. "Electrocatalytic Oxidation and Determination of Deferasirox and Deferiprone on Nickel Oxyhydroxide-midified Electrode", Anal. Biochem., 2008, 373,  337.
 
33. Yadegari, H.; Jabbari, A.; Heli, H.; Moosavi-Movahedi, A.A.; Karimian, K. "Electro-oxidation and Determination of Deferiprone on a Glassy Electrode", Chem. Anal. 2008, 53, 33.
 
34. Hajjizadeh M, Jabbari A, Heli H, Moosavi-Movahedi AA, Shafiee A, Karimian K.
"Electrocatalytic oxidation and determination of deferasirox and deferiprone on a nickel oxyhydroxide-modified electrode". Anal. Biochem. 2008 ,373, 337-48
 
 
35. Moosavi-Movahedi, A. A.; Mousavy, S. J.; Divsalar, A.; Babaahmadi, A.; Karimian, K.; Shafiee, A.; Kamarie, M.;  Poursasan. N.; Farzami, B.; Riazi, G. H.; Hakimelahi, G. H.;  Tsai, F.Y.; Ahmad, F.; Amani, M.;  Saboury, A. A. "The Effects of Deferiprone and Deferasirox on the Structure and Function of beta-Thalassemia Hemoglobin", J. Biomolecular Str. Dynamics, 2009, 27, 319-339.
 
36. Karimian, K. "Imidazo[2,1-b]thiazoles and their use as pharmaceuticals" Expert Opinion Therapeutic Patents, 2009, 19, 369-371.
 
37. Karimian, K. "Prerequisites for the Transformation of Science to Technology", Sci. Cultivation, 2011, 1, 6.
 
38. Heli, H.; Mirtorabi, S.; Karimian, K., "Iron Chelation; an Update" Expert Opinion Therapeutic Patents, 2011, 21, 6.
 
39. Heli, H.; Yadegari, H.; Karimian, K., "Nanoflakes of Cobalt Oxide for Highly Sensitive Sensing of two Oral Iron Chelator Drugs Deferasirox and Deferiprone", J. Exp.  Nanoscience, 2011, 6, 488-508.
 
40. Karimian, K. "On the Potential Role of Chemistry on Iran's Social and Economic Structure", Sci. Cultivation, 2013, 1, 19.
 
41. Sattarahmady N, Heli H, Moosavi-Movahedi AA, Karimian K. "Deferiprone: structural and functional modulating agent of hemoglobin fructation", Mol Biol Rep. 2014, 41, 1723-9. 
 
42. R. Dehdari Vais, N. Sattarahmady, K. Karimian, H. Heli "Green electrodeposition of gold hierarchical dendrites of pyramidalnanoparticles and determination of azathioprine" Sensors and Actuators B: Chemical, 2015, 215B, 113-118.
 
43. L. Mahrokh, K. Karimian, A. Moosavi-Movahedi, "Personalized Medicine",  Sci. Cultivation, 2015, 6, 46.
 
44. A. Rahi, K. Karimian, H. Heli, "Nanostructured materials in electroanalysis of pharmaceuticals", Ana. Biochem., 2016, 497, 39-47.
 
45. Noorani, M.,  Azarpira,  N., Karimian, K , Heli, H., "Erlotinib-loaded albumin nanoparticles:  A novel injectable form of erlotinib and its in vivo efficacy against pancreatic adenocarcinoma ASPC-1 and PANC-1 cell lines" to International Journal of Pharmaceutics, Submitted, 2017
 
46. Dehdari Vais, R., Sattarahmady, N.,  Karimian, K.,  Heli, H., "- Electrooxidation and amperometric determination of vorinostat on hierarchical leaf-like gold nanolayers, Microporous and Mesoporous Materials, Submitted 2017
 
47. Nazari-Vanani, R., Azarpira, N. , Heli, H., Karimian, K., Sattarahmady, N., "A novel self-nanoemulsifying formulation for sunitinib: evaluation of anticancer efficacy", Colloids and Surfaces B, Submitted, 2017
 
48. Mokhtrai, J.,  Azarnoosh, S.,  Karimian, K., " Resolution of Racemic Mixtures by Phase Transition of PEGylated Resolving Agents", Nature Chemistry, Submitted, 2017.
 
PAPERS PRESENTED: 
 
1. Bowden, J.A.; Dikeman, R; Helmer, G.; Karimian, K., "Phenylketourea and Maple Syrup Urine Disease: Evidence for a Common Etiology for the Depressed Myeliogenisis Observed", Federation Proceedings, May 23-29, 1973, Atlantic City, New Jersey, Abstract No. 2155.
 
2. Risinger, G.E; Karimian, K., "Stereochemical Aspects of the Michael Addition Between Dibenzalacetone and Cyanoacetamide" American Chemical Society, Division of Organic Chemistry, Oct. 24-29, 1975, Memphis, Tennessee, Abstract No. 463.
 
3. Karimian, K.; Risinger, G.E., "On the Synthesis of 2-Acetyl-3-(2-methyl-4-aminopyridine-5-yl) methyl-3a-methylperhydrofuro [2,3d] thiazole", American Chemical Society, Division of Organic Chemistry, Aug. 29-Sept. 3, 1976, San Francisco, California, Abstract No. 63. 
 
4. Karimian, K.; Azizaldin, M., "Effects of Large and Small Nucleophiles on 2-(1-Hydroxyethyl) thiamine Chloride Hydrochloride", The Sixth International Congress of Heterocyclic Chemistry, July 9-13, 1977, Tehran, Iran.
 
5. Risinger, G.E.; Karimian, K.; Jungk, S., "Irregular Terpene Biosynthesis: Incorporation of 2-(1-Hydroxy-3, 7-dimethyl-1-oct-6-enyl) thiamine Chloride Hydrochloride Into an Artemisia Ketone Analogue", American Chemical Society, Division of Organic Chemistry, Aug. 28 - Sept. 2, 1977, Chicago, Illinois, Abstract No. 140.
 
6. Risinger, G.E.; Jungk, S.; Karimian, K., "Stereochemical Aspects of the Michael Addition Between Dibenzalacetone and Active Methylene Compounds", American Chemical Society,  Division of Organic Chemistry, Aug.29-Sept.2, 1977, New Orleans, Louisiana, Abstract No. 109.
 
7. Gorgani, M.N-., Karimian, K.; Massih, A., "Salt Effect in  Protein Binding to Palmityl Sepharose 4B", The Third International Congress of Biophysics,  Division of Enzymology, Sept. 23-29, 1981, Mexico City, Abstract No. 117.
 
8. Bearne, S.; Karimian, K.; Kluger, R., "Selective Pyrophosphorylation of Primary Hydroxyl Groups", The Third Chemical Congress of North America,  Division of Organic Chemistry, June 10-14, 1988, Toronto, Ontario, Abstract No. 23.
 
9. Azarkeivan A., Karimian K., Mirtorabi Mahabadi S. , Narenjian A. , Eslami M.
Evaluation of gastric side effects of new form of deferiprone, (L1; Enteric coated), 12th International Conference on Thalassemia and Other Hemoglobinopathie, the 14th Thalassemia International Foundation Conference Abstract  350, 11-15 May, 2011, Anatalya, Turkey.
 
UNITED SATES PATENTS:
 
1. Process of making nadolol, US 5,319,141, June 7, 1994.
 
2. Recovery of AZT by guanidine precipitation, US 5,387,677, February 7, 1995.
 
3. Process for preparing 2,3'-O-cyclocytidine, US 5,399,682, March 21, 1995.
 
4. Complex of guanidine and AZT, US 5,519,129, May 21, 1996.
 
5. 5-Halo-2,3'-O-cyclocytidines, US 5,527,782, June 18, 1996.
 
6. Organosulfonyl salts of 2,3'-O-cyclocytidine, US 5,536,824, July 16, 1996.
 
7. Process for preparing halogenated 2,3-O-cyclocytidine derivatives, US 5,596,093, January 21, 1997.
 
8. Process for producing 2,2'-o-cyclonucleosides nucleosides, and analogs thereof, US 5,610,292, March 11, 1997.
 
9. Methods of making ureas and guanidines, including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin, and bunazosin (exemplary of 2- substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefore, US 5,675,006, October 7, 1997.
 
10. Thiadiazole compounds useful as proton pump inhibitors, US 5,677,302, October 14, 1997.
 
11. Methods of making ureas and guanidines, including terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin, and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates thereof, US 5,686,612, November 11, 1997.
 
12. 1,4-Dihydropyridines, N-substituted bicyclic 4-hydropyridines, and bicyclic N-substituted 4,5-dihydropyridines, US 5,723,618, March 3, 1998.
 
13. Methods for the manufacture of terbinafine, US 5,817,875, October 6, 1998.
 
14. Methods for the manufacture of amorphous cefuroxime axetil, US 5,847,118, December 8, 1998.
 
15. Process for the production of the form I of the terazosin monohydrochloride anhydrous US 5,856,482 Octtober 15, 1999.
 
16. Methods for the manufacture of neofazodone, US 5,900,485, May 4, 1999.
 
17. Methods for the manufacture of quinolone carboxylic acids derivatives and intermediates thereof, US 5,914,401, June 22, 1999.
 
18. Process for the manufacture of intermediates suitable to make doxazosin, terazosin, prazosin, tiodazosin,  and related antihypertensive medicines,   US 5,919,931, September 8, 2000.
 
19. Methods for the manufacture of cetirizine, US 6,046,332, April 4, 2000.
 
20. Thiadiazole compounds useful as inhibitors of H+ /K+ ATPase, US 6,060,472, May 9, 2000
 
21. Process for the manufacture of bis-triazole compounds and intermediates useful in the manufacture thereof having antifungal activity, US 6,063,933, May 16, 2000.
 
22. Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, thiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefore, US 6,080,860, June 27, 2000.
 
23. Proton pump inhibitors, US 6,093,738, July 25, 2000.
 
24. Process for scavenging thiols, US 6,114,537, September 5, 2000.
 
25. Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes, US 6,162,791, December 19, 2000.
 
26. Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof, US 6,245,903, June 12, 2001.
 
27 Azithromycin preparation in its noncrystalline and crystalline dehydrate forms, US  6,541,990 August 15, 2001.
 
28. Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes, US 6,468,977, October 22, 2002.
 
29. Process to manufacture simvastatin and intermediates, US 6,506,929, January 14, 2003.
 
30. Sulfonamide derivatives of 3-substituted imidazol[1,2-d]-1,2,4-thiadiazoles and 3-substituted-[1,2,4] thiadiazolo[4,5-a] benzimidazole as inhibitors of fibrin cross-linking and transglutaminases, US 2003225007, December 4, 2003. 
 
31. Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof,   US RE 39,087 E, May 2, 2006.
 
CANADIAN PATENTS:
 
1. Nadolol, CA 1,338,717, November 12, 1996.
 
2. Process for producing 2,2'-cyclocytidine and analogues thereof, CA 2,012,093, December 26, 1995.
 
3. Process for producing cytarabine and analogues thereof, CA 2,012,094, July 23, 1996.
 
4. 3'-Tosylcytidine compounds and process for production thereof, CA 2,012,095, July 23, 1996.
 
5. Cytosine compounds and a process for the production thereof, CA 2,012,096, October 28,
 
6. Methods of making ureas and guanidines, and intermediates therefor, CA 2,077,252, April 10, 2001.
 
7. Anti-viral compounds and processes for production of anti-viral compounds, CA 2,090,026, September 19, 1995.
 
8. Methods for the manufacture of fluconazole and forms thereof, intermediates useful in the manufacture thereof, and combinations comprising fluconazole, CA 2,106,032, November 7, 1995.
 
9. Methods for the manufacture of loratadine, intermediates useful in the manufacture thereof, CA 2,134,128, October 24, 1994.
 
10. Anti-viral compounds and processes for production of anti-viral compounds, CA 2,158,009, June 22, 1992.
 
11. Methods for the manufacture of cetirizine, CA 2,180,993,  July 11, 1996.
 
12. Methods for the manufacture of nefazodone, CA 2,182,241, Septmber 17, 2002.
 
13. Halogenated derivatives of 2,3'-o-cyclocytidine compounds and process for production thereof, CA 2,182,578, April 18, 2000.
 
14. Methods for the manufacture of terbinafine, trans-n-methyl-n-(1-naphthylmethyl)-6,6-dimethylhept-2-en-4 -ynyl-1-amine and pharmaceutically acceptable salt thereof, intermediates useful in the manufacture thereof, novel n-methyl-n-(1-naphthylmethyl)-6,6-dimethyl-2-hydroxyheptan- 4-ynyl-1-amine as potential antimycotic agents, CA 2,185,599, November 30, 1999.
 
15. Process for the manufacture of bis-triazole compounds and intermediates useful in the manufacture thereof having anti-fungal activity, CA 2,185,654, January 18, 1997.
 
16. Methods for the manufacturing of 1,4-dihydropyridines, novel-n-substituted bicyclic 4-hydropyridines, and novel bicyclic n-substituted 4,5-dihydropyridines, intermediates useful in the manufacture thereof, and the compounds the eof which have potential activity as anti-hypertensive agents, CA 2,188,071, October 17, 1996.
 
17. Methods for the manufacture of quinolone carboxylic acids derivatives and intermediates thereof, CA 2,199,645, March 11, 1997.
 
18. Methods for the manufacture of amorphous cefuroxime axetil, CA 2,211,499,  July 25, 1997.
 
19. Process to manufacture simvastatin and intermediates, CA 2,240,983, June 18, 1998.
 
20. Aithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof, CA 2,245,398, January 29, 2002.
 
21. Process for scavenging thiols, CA 2,247,899, September 4, 1997.
 
22. Proton pump inhibitor, CA 2,247,901, September 4, 1997.
 
23. Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes, CA 2,322,838, September 10, 1999.
 
24. Carboxylic acid derivatives of 3-hydroxy-4-oxo-1,4-dihydropyridine as iron chelators, CA 2,379,370, March 28, 2002
 
25. Sulfonamide derivatives of 3-substituted imidazol[1,2-d]-1,2,4-thiadiazoles and 3-substituted-[1,2,4] thiadiazolo[4,5-a] benzimidazole as inhibitors of fibrin cross-linking and transglutaminases, CA 2,379,375, March 28, 2002.
 
SUMMARY OF INTERNATIONAL PATENTS:
 
http://www.freepatentsonline.com/result.html?p=1&sort=relevance&srch=top&query_txt=khashayar+karimian&patents=on
 
 

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WO/1991/004244A1

NADOLOL   
A process for making 5-{d-3-(tert-butylamino)-2-hydroxypropoxy}-1,2,3,4-tetrahydr o-1-cis-2,3 naphthalenediol of formula (I), by reacting formula (II) in an essentially water free environment with...

999

2

WO/1997/003971A1

PROCESS FOR THE MANUFACTURE OF BIS-TRIAZOLE COMPOUNDS AND INTERMEDIATES USEFUL IN THE MANUFACTURE THEREOF HAVING ANTIFUNGAL ACTIVITY   
A process to prepare a compound of formula (I) wherein Y and Z can be identical or different and represent a halogene. The bis-triazole compounds of formula (I) and intermediates have antifungal...

944

3

WO/1995/007895A1

METHODS FOR THE MANUFACTURE OF FLUCONAZOLE AND FORMS THEREOF, INTERMEDIATES USEFUL IN THE MANUFACTURE THEREOF, AND COMBINATIONS COMPRISING FLUCONAZOLE   
A process for making fluconazole comprising the steps shown above.

918

4

WO/2016/110761A1

PROCESS FOR PRODUCING 1-β-D-ARABINOFURANOSYLCYTOSINE AND 2,2'-O-CYCLOCYTIDINE   
An efficient and simple process is provided for producing 1-β-D-arabinofuranosylcytosine or cytarabine wherein cytidine hydrochloride is converted to the corresponding 2,2'-...

873

5

5817875

Methods for the manufacture of terbinafine   
Process for the manufacture of naphthylmethylamine derivatives and among them terbinafine as potential antimycotic agents.

866

6

WO/2016/097989A1

PROCESS FOR THE PREPARATION OF GEMCITABINE HYDROCHLORIDE   
The present invention relates to an improved as well as an industrially viable process for the preparation of 2'-deoxy-2',2'-difluorocytidine and its pharmaceutical acceptable acid salts thereof...

810

7

6046332

Methods for the manufacture of cetirizine   
The present invention relates to a process for the preparation of a [2-[4-[4-(chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]ac etic acid derivative of formula I: and, in particular, for the...

798

8

WO/1994/005628A1

SYNTHESIS OF 2-SUBSTITUTED QUINAZOLINE COMPOUNDS (SUCH AS TERAZOSIN) AND MEOBENTINE AND BETHANIDINE AND INTERMEDIATES THEREFOR   
Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted...

787

9

WO/1991/013900A1

PROCESS FOR PRODUCING 2,2'-O-CYCLONUCLEOSIDES, NUCLEOSIDES, AND ANALOGS THEREOF   
A novel process is provided for producing a nucleoside, such as cytarabine, or a nucleoside analogue, comprising the step of reacting 2,2'-O-cyclonucleoside or an analogue thereof with an amine....

750

10

WO/1998/002425A1

METHODS FOR THE MANUFACTURE OF CETIRIZINE   
A process for the manufacture of [2-[4-[4-(chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]ac etic acid derivatives of formula (I) is provided.

750

11

DE69902212T2

Azithromycinmonohydrat-Isopropanol-Clathrate und Methoden zu deren Herstellung  

721

12

DE69902212D1

Azithromycinmonohydrat-Isopropanol-Clathrate und Methoden zu deren Herstellung  

721

13

6063933

Process for the manufacture of bis-triazole compounds and intermediates useful in the manufacture thereof having antifungal activity   
PCT No. PCT/CA96/00483 Sec. 371 Date Feb. 24, 1998 Sec. 102(e) Date Feb. 24, 1998 PCT Filed Jul. 17, 1996 PCT Pub. No. WO97/03971 PCT Pub. Date Feb. 6, 1997The present invention relates to a...

675

14

WO/1999/065892A1

PROCESS TO MANUFACTURE SIMVASTATIN AND INTERMEDIATES   
A process is disclosed for the preparation of simvastatin which enables highly regio selective C-methylation of the 2'-position group of lovastatin without requiring protection/deprotection of...

675

15

WO/2016/098015A1

NEW EFFICIENT METHODS FOR THE SYNTHESIS OF TAXANE DERIVATIVES SUCH AS DOCETAXEL AND THEIR STRUCTURAL ANALOGOUS, AND A METHOD FOR THE PREPARATION THEREOF   
The present invention relates to a novel process for the preparation of taxanes such as Docetaxel, a very important anticancer drug. Docetaxel 1 is a clinically well-established anti -mitotic...

675

16

WO/2004/083227A1

ISOPROPANOLATE OF AZITHROMYCIN AND METHOD OF MANUFACTURING   
Azithromycin isopropanolate of the empirical formula azithromycin: [H20]x: [isopropanol]y is obtained from the crystallization of azithromycin in isopropanol and water. The x and y values is...

625

17

WO/1991/013901A1

3'-O-TOSYLCYTIDINE AND CYTOSINE COMPOUNDS, AND PROCESS FOR PRODUCTION THEREOF   
Compounds of formula (IV), wherein R?6� is selected from the group comprising a trifluoromethyl group, a C�1?-C�6? alkyl group and a C�6?-C�9? aryl group, and R?1� is selected from the group...

625

18

EP0521923A1

PROCESS FOR PRODUCING NUCLEOSIDES, AND ANALOGS THEROF.   
Abstract not available for EP0521923 Abstract of corresponding document: WO9113900 A novel process is provided for producing a nucleoside, such as cytarabine, or a nucleoside analogue, comprising...

577

19

EP1087958A1

PROCESS TO MANUFACTURE SIMVASTATIN AND INTERMEDIATES  

577

20

EP0840730A1

PROCESS FOR THE MANUFACTURE OF BIS-TRIAZOLE COMPOUNDS AND INTERMEDIATES USEFUL IN THE MANUFACTURE THEREOF HAVING ANTIFUNGAL ACTIVITY   
Abstract not available for EP0840730 Abstract of corresponding document: US6063933 PCT No. PCT/CA96/00483 Sec. 371 Date Feb. 24, 1998 Sec. 102(e) Date Feb. 24, 1998 PCT Filed Jul. 17, 1996 PCT...

577

21

EP1058690A1

THIADIAZOLE COMPOUNDS USEFUL AS INHIBITORS OF CYSTEINE ACTIVITY DEPENDENT ENZYMES  

577

22

EP0984020B1

Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof.   
Abstract of EP0984020 A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of...

577

23

EP0445250A1

Process for preparing nadolol.   
Abstract not available for EP0445250 Abstract of corresponding document: US5319141 PCT No. PCT/CA90/00316 Sec. 371 Date May 20, 1991 Sec. 102(e) Date May 20, 1991 PCT Filed Sep. 25, 1990 PCT Pub....

577

24

EP0523080A1

3'-O-TOSYLCYTIDINE AND CYTOSINE COMPOUNDS, AND PROCESS FOR PRODUCTION THEREOF.   
Abstract not available for EP0523080 Abstract of corresponding document: US5399682 PCT No. PCT/CA91/00078 Sec. 371 Date Oct. 5, 1992 Sec. 102(e) Date Oct. 5, 1992 PCT Filed Mar. 13, 1991 PCT Pub....

577

25

EP0984020A3

Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof.   
Abstract of EP0984020 A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of...

577

26

DE69712608D1

PROTONENPUMPINHIBITOREN  

577

27

DE69015151D1

Verfahren zur Herstellung von Nadolol.  

577

28

DE69712608T2

PROTONENPUMPINHIBITOREN  

577

29

DE69108014T2

VERFAHREN ZUR HERSTELLUNG VON NUCLEOSIDEN UND IHRE ANALOGEN.  

577

30

DE69902788T2

VERFAHREN ZU HERSTELLUNG VON SIMVASTATIN UND ZWISCHENPRODUKTEN  

577

31

DE69015151T2

Verfahren zur Herstellung von Nadolol.  

577

32

DE69111438D1

2,3'-O-CYCLOCYTIDINE UND VERFAHREN ZU DEREN HERSTELLUNG.  

577

33

DE69108014D1

VERFAHREN ZUR HERSTELLUNG VON NUCLEOSIDEN UND IHRE ANALOGEN.  

577

34

DE69111438T2

2,3'-O-CYCLOCYTIDINE UND VERFAHREN ZU DEREN HERSTELLUNG.  

577

35

DE69902788D1

VERFAHREN ZU HERSTELLUNG VON SIMVASTATIN UND ZWISCHENPRODUKTEN  

577

36

WO/2001/090095A1

THIADIAZOLE COMPOUNDS USEFUL AS INHIBITORS OF CYSTEINE ACTIVITY DEPENDENT ENZYMES   
Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in...

540

37

5399682

Process for preparing 2,3'-O-cyclocytidine   
A process for preparing 2,3'-O-cyclocytidine wherein 3'-deoxy-3'-organosulfonyl cytidine is refluxed in the absence of base. 2,3'-cyclocytidine is an intermediate in the preparation of...

530

38

6245903

Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof   
A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of azithromycin monohydrate)...

530

39

6162791

Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes   
Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in...

505

40

6060472

Thiadiazole compounds useful as inhibitors of H+ /K+ atpase   
Novel 3,5-disubstituted 1,2,4-thiadiazole compounds are provided, which are effective in treating peptic ulcers by the inhibition of H+ /K+ -ATPase. The compounds of the present invention are...

505

41

US20060183890

Isopropanolate of azithromycin and method of manufacturing   
Azithromycin isopropanolate of the empirical formula azithromycin:[H20]x:[isopropanol]y is obtained from the crystallization of azithromycin in isopropanol and water. The x and y values is...

505

42

5847118

Methods for the manufacture of amorphous cefuroxime axetil   
A process for preparing pure amorphous cefuroxime axetil comprising the steps of dissolving crystalline cefuroxime axetil in a highly polar organic solvent and adding the resulting solution to...

505

43

EP1087958B1

PROCESS TO MANUFACTURE SIMVASTATIN AND INTERMEDIATES  

505

44

EP0883606A1

PROCESS FOR SCAVENGING THIOLS   
Abstract not available for EP0883606 Abstract of corresponding document: WO9731893 Thiols are trapped, and converted to disulfide compounds, by a process of reacting them with compounds containing...

505

45

EP0521923B1

PROCESS FOR PRODUCING NUCLEOSIDES, AND ANALOGS THEROF   
Abstract not available for EP0521923 Abstract of corresponding document: WO9113900 A novel process is provided for producing a nucleoside, such as cytarabine, or a nucleoside analogue, comprising...

505

46

EP0445250B1

Process for preparing nadolol   
Abstract not available for EP0445250 Abstract of corresponding document: US5319141 PCT No. PCT/CA90/00316 Sec. 371 Date May 20, 1991 Sec. 102(e) Date May 20, 1991 PCT Filed Sep. 25, 1990 PCT Pub....

505

47

EP0984020A2

Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof.   
A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of azithromycin monohydrate)...

505

48

EP0883622A1

PROTON PUMP INHIBITOR   
Abstract not available for EP0883622 Abstract of corresponding document: US5677302 Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating...

505

49

EP0656885A1

SYNTHESIS OF 2-SUBSTITUTED QUINAZOLINE COMPOUNDS (SUCH AS TERAZOSIN) AND MEOBENTINE AND BETHANIDINE AND INTERMEDIATES THEREFOR.   
Abstract not available for EP0656885 Abstract of corresponding document: WO9405628 Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin,...

505

50

6093738

Proton pump inhibitors   
Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H+ /K+ -ATPase. The compounds are...

 

 

500

 

Match

Document

Document Title

Score

51

5610292

Process for producing 2,2'-o-cyclonucleosides nucleosides, and analogs thereof   
A novel process is provided for producing a nucleoside, such as cytarabine, or a nucleoside analogue, comprising the step of reacting 2,2'-O-cyclonucleoside or an analogue thereof with an amine....

484

52

WO/1995/021183A1

HALOGENATED DERIVATIVES OF 2,3'-O-CYCLOCYTIDINE COMPOUNDS AND PROCESS FOR PRODUCTION THEREOF   
In one of its aspects, the present invention provides novel compounds of formula (I) wherein: X is a halide; Y is selected from the group consisting essentially of halide, sulfate, acetate, tosyl,...

435

53

RE39087

Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof   
A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of azithromycin monohydrate)...

433

54

5319141

Process of making nadolol   
A process for making 5-(d-3-(tert-butylamino)-2-hydroxypropoxy)-1,2,3,4-tetrahydr o-1-cis-2,3 naphthalenediol of the formula ##STR1## by reacting ##STR2## in an essentially water free environment...

433

55

5536824

Organosulfonyl salts of 2,3'-O-cyclocytidine   
Compounds of Formula IV: ##STR1## are described. In the compounds of Formula IV, R6 is selected from a trifluoromethyl group, a C1 -C6 alkyl group and a C6 -C9 aryl group, and R1 is selected from...

433

56

6468977

Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes   
Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in...

433

57

EP0523080B1

2,3'-O-CYCLOCYTIDINES, AND PROCESS FOR PRODUCTION THEREOF   
Abstract not available for EP0523080 Abstract of corresponding document: US5399682 PCT No. PCT/CA91/00078 Sec. 371 Date Oct. 5, 1992 Sec. 102(e) Date Oct. 5, 1992 PCT Filed Mar. 13, 1991 PCT Pub....

433

58

WO/1997/031893A1

PROCESS FOR SCAVENGING THIOLS   
Thiols are trapped, and converted to disulfide compounds, by a process of reacting them with compounds containing a 1,2,4-thiadiazole ring structure carrying a substituent at position 3 of the...

433

59

WO/1997/031923A1

PROTON PUMP INHIBITOR   
Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H+/K+-ATPase. The compounds are...

433

60

EP1615941A1

ISOPROPANOLATE OF AZITHROMYCIN AND METHOD OF MANUFACTURING   
Abstract not available

408

61

EP0550714A1

NOVEL ANTI-VIRAL COMPOUNDS AND PROCESSES FOR PRODUCTION OF ANTI-VIRAL COMPOUNDS.   
Abstract not available for EP0550714 Abstract of corresponding document: WO9300351 A process for recovering zidovudine or a derivative thereof from a mixture of chemicals comprising zidovudine or...

408

62

WO/1993/000351A1

NOVEL ANTI-VIRAL COMPOUNDS AND PROCESSES FOR PRODUCTION OF ANTI-VIRAL COMPOUNDS   
A process for recovering zidovudine or a derivative thereof from a mixture of chemicals comprising zidovudine or a derivative thereof. The process comprises the steps of: (i) reacting zidovudine...

408

63

DE550714T1

Antiviralverbindungen und Ihrer Verfahren zur Herstellung.  

408

64

DE69208636D1

VERFAHREN ZUR HERSTELLUNG VON ZIDOVUDINE  

408

65

DE69208636T2

VERFAHREN ZUR HERSTELLUNG VON ZIDOVUDINE  

408

66

5527782

5-halo-2,3'-O-cyclocytidines   
A 5'-halo-2,3'-O-cyclocytidine of Formula I: ##STR1## wherein: X is a bromide, chloride, or iodide;Y is halide, sulfate, acetate, tosyl, mesyl, benzoate, and phosphate;R1 is hydrogen; andR2 is a...

388

67

6506929

Process to manufacture simvastatin and intermediates   
A process is disclosed for the preparation of simvastatin which enables highly regio selective C-methylation of the 2′-position group of lovastatin without requiring protection/deprotection of...

360

68

5686612

Methods of making ureas and guanidines, including terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin, and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates thereof   
Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted...

360

69

EP0883622B1

PROTON PUMP INHIBITOR   
Abstract not available for EP0883622 Abstract of corresponding document: US5677302 Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating...

360

70

WO/1999/045027A1

THIADIAZOLE COMPOUNDS USEFUL AS INHIBITORS OF CYSTEINE ACTIVITY DEPENDENT ENZYMES   
Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in...

360

71

US20030225007

Sulfonamide derivatives of 3-substituted imidazol[1,2-d]-1,2,4-thiadiazoles and 3-substituted-[1,2,4] thiadiazolo[4,5-a] benzimidazole as inhibitors of fibrin cross-linking and transglutaminases   
A method of inhibiting the activity of transglutaminases containing a cysteine residue comprising administering to a mammal an effective amount of a sulfonamide derivative of...

357

72

EP0550714B1

PROCESSES FOR PRODUCTION OF ZIDOVUDINE   
Abstract not available for EP0550714 Abstract of corresponding document: WO9300351 A process for recovering zidovudine or a derivative thereof from a mixture of chemicals comprising zidovudine or...

357

73

EP1348710A1

Sulfonamide derivatives of 3-substituted imidazo[1,2-D]-1,2,4-thiadiazoles and 3-substituted-[1,2,4]thiadiazolo[4,5-A]benzimidazole as inhibitors of fibrin cross-linking and transglutaminases   
A method of inhibiting the activity of transglutaminases containing a cysteine residue comprising administering to a mammal an effective amount of a sulfonamide derivative of...

357

74

5677302

Thiadiazole compounds useful as proton pump inhibitors   
Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H+ /K+ -ATPase. The compounds are...

353

75

5596093

Process for preparing halogenated 2,3-O-cyclocytidine derivatives   
A process from preparing 5-halogenated 2,3-O-cyclocytidine derivatives comprising reacting 2,3-O-cyclocytidine with a halogenating reagent, preferably N-bromosuccinimide, in the presence of an...

333

76

5723618

1,4-dihydropyridines, N-substituted bicyclic 4-hydropyridines, and bicyclic N-substituted 4,5-dihydropyridines   
The invention relates to a novel process to prepare 1,4-dihydropyridines and in particular amlopidine and in novel intermediates obtained during the synthesis of the 1,4-dihydropyridines which...

306

77

5914401

Methods for the manufacture of quinolone carboxylic acids derivatives and intermediates thereof   
Novel process for the preparation of quinolone carboxylic acid derivatives of general formula I, and intermediates thereof as illustrated in Scheme 1 wherein the key intermediate is a compound of...

306

78

5900485

Methods for the manufacture of neofazodone   
Process for the manufacture of triazolone compounds and in particular nefazodone and intermediates useful in the manufacture thereof.

306

79

6114537

Process for scavenging thiols   
Thiols are trapped, and converted to disulfide compounds, by a process of reacting them with compounds containing a 1,2,4-thiadiazole ring structure carrying a substituent at position 3 of the...

288

80

5675006

Methods of making ureas and guanidines, including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin, and bunazosin (exemplary of 2- substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor   
Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted...

288

81

6080860

Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor   
Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted...

288

82

5387677

Recovery of AZT by guanidine precipitation   
A process for recovering 3'-azido-3'-deoxythymidine (AZT) or a salt thereof from a mixture of chemicals involving the reaction of the AZT with guanidine to form a salt precipitate. The salt...

255

83

5519129

Complex of guanidine and AZT   
A composition of a 1:1 molar complex of guanidine and 3'-azido-3'-deoxythymidine (AZT) which is generated at about pH above 9 and disrupted by pH below about 9. This complex is a useful...

255

 
 
 
 
 
 
 
 
 
 
 
RECENT WIPO/PCT APPLCATIONS and SUBMISSIONS 
 
1.    Process for Producing  1-b-D-Arabinofuranosylcytosine and 2,2'-O-CyclocytidineCytarabine WO 2016/110761 A1, July 14, 2016
 
2.    Process for the Preparation of Gemcitabine Hydrochloride, WO 2016097989, June 23, 2016
 
3.    New Efficient Methods for the Synthesis of Taxnane Derivatives Such as   Docetaxel and Their Structural Analogues, and Methods for the Preparation Thereof, WO 2016/098015 A1, June 23, 2016
 
4.    Effervescent Deferiprone Tablet, Submitted August 17, 2016
 
5. Enteric Coated Deferiprone Tablet, Submitted December 23, 2016
 
 
MANUFACTURING  
 
Design and start-up of ACIC Canada Inc. fine chemicals manufacturing plant (1986-1988, USD 20 million). 
 
Design and start-up of Arasto Pharmaceutical Chemicals Inc. fine chemicals manufacturing plant (1991- 1997 USD 5 million).
 
Scientific Consultant for down-stream plant design for commercial production of lovastatin and cyclosporin by fermentation AFI Inc. (1993 – 1997, Winnipeg, Canada USD 90 million).
 
Design of Apotex Fine Chemicals Inc. Research and Development facility (1993–1994, USD 4 million).
 
Design of Arasto Chemotherapy Inc. (HiPo API Production Plant).  API production plant (closed system production of High Potency (HiPo) APIs, including production equipment design and supervision of detailed engineering and fabrication to the required specs, 2015-2017, USD 5 million)
 
Various aspects of fine chemicals production (research and development, pilot and large scale manufacturing, production equipment design and supervision of their fabrication, quality control, quality assurance, regulatory compliance, and DMF preparation in CTD format) of a large number of Active Pharmaceutical Ingredients have been conducted under Dr.  Karimian's supervision in the US, Canada, Europe South America, India and China.  These products include:
 

 

No

Product

No

Product

1

Acyclovir

31

Erlotinib

2

Alendronate Sodium

32

Etidronate Disodium

3

Amitriptyline HCl

33

Fluconazol

4

Amlodipine

34

Fluoxetine HCl

5

Astemizole

35

Gemcytabine

6

Atenolol

36

Imatinib

7

Azathioprine

37

Ketoconozole

8

Azithromycin

38

Lactulose (solution)

9

AZT (Ziduvudine)

39

Lamotrigine

10

Bortezomib

40

Loratidine

11

Buspirone

41

Lovastatin

12

Capecitabine

42

2-Methylmercaptophenothiazine

13

Captopril

43

Methacholine Chloride

14

Carbamazapine

44

Methylphenidate

15

Carbidopa        

45

Montelukast

16

Celecoxib

46

Nadolol

17

2-Chlorophenothiazine

47

Nefazodone

18

Cefuroxime Acxetil

48

Nifedipine

19

Ciprofluxacin

49

Norfluxacin

20

Cimitidine

50

Nortriptyline HCl

21

Citirizine

51

Omeprazole

22

Clomipramine HCl

52

Pantoprazole

23

Cyclosporin

53

Ranitidine

24

Cytarabine        

54

Simvaststin

24

Deferasirox

55 Sunitinib

26

Deferiprone

56

Temzolamide

27 Dipivefrine 57

Terbinafine

28 Docetaxol 58

Terazosin

29 Domperidon 59

Vorinostat

30

Doxazosin

60

Warfarin Na/IPA Clathrate