Abstract: The present disclosure provides novel crystalline sofosbuvir form-M3 and a process for the preparation of sofosbuvir form-M3. The crystalline sofosbuvir form-M3 disclosed herein may be useful in the formulation of pharmaceutical dosage forms.
Abstract: The present disclosure provides amorphous lumacaftor, amorphous solid dispersions of lumacaftor, crystalline lumacaftor acetic acid solvate, crystalline lumacaftor ethyl acetate solvate, and processes for the preparation thereof. The lumacaftor forms disclosed herein may be useful for the preparation of oral dosage forms for treating cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases.
Abstract: The present disclosure provides crystalline carfilzomib form M1 and a process for the preparation thereof. Further disclosed are processes for the preparation of amorphous carfilzomib using crystalline form M1 as a starting material. The present disclosure also relates to an improved process for the preparation of carfilzomib.
Abstract: A process for the preparation of intermediates 9, useful in the synthesis of sofosbuvir, as well as intermediates of formula [12] are disclosed herein.
Abstract: The present disclosure relates to processes for the preparation of sofosbuvir or of its pharmaceutically acceptable salts. The present disclosure also provides intermediates useful in the synthesis of sofosbuvir.
Abstract: The present disclosure provides a process for the preparation of velpatasvir intermediates. The intermediates may be further converted to velpatasvir or pharmaceutically acceptable salts thereof.
Abstract: The present disclosure provides amorphous ixazomib citrate and processes for the preparation thereof. Crystalline form M1, form M2, form M3, and form M4 of ixazomib citrate are also disclosed. The present disclosure also encompasses processes for the preparation of those crystalline forms.
Abstract: Processes for the preparation of dolutegravir and pharmaceutically acceptable salts utilizing alkenylamine are disclosed. Intermediates in those synthetic schemes are also disclosed.
Abstract: The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-Imorpholin-4-yl-pentan-1-one by the reduction of 1-(4-Fluoro-phenyl)-5-morpholin-4-yl-pentane-1,5-dione by using a suitable enzyme or by the resolution of (R, S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-4-yl-pentan-1-one by using an enzyme. The present invention also provides process for the preparation of Ezetimibe comprising the steps of a) protecting the compound (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-4-yl-pentan-1-one with hydroxy protecting group b) hydrolyzing the obtained compound c) condensing with a chiral auxiliary d) reacting with an protected imine compound e) converting to alkyl ester f) cyclizing and g) deprotecting to obtain Ezetimibe.
Type:
Grant
Filed:
June 10, 2016
Date of Patent:
June 12, 2018
Assignee:
Mylan Laboratories Limited
Inventors:
Mofazzal Husain, Srikanth G. S. C., Swapna Thorpunuri, Debashish Datta
Abstract: The present disclosure provides crystalline piperidine sulfamoyl intermediates of formula 8 and 9. The present disclosure also relates to an improved process for the preparation of cobicistat using compounds of formulae 8 and 9.
Abstract: A process for the resolution of racemic 2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine using novel chiral salts is disclosed. An L-phenylalanine p-toluene-sulfonamide salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine and a di-p-toluoyl-L-tartaric acid salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine are also provided.
Abstract: An improved process for the preparation of empagliflozin is disclosed. Novel intermediates of formulas (13) and (14) for the preparation of empagliflozin are also disclosed, wherein R1 and R2 are independently hydrogen or hydroxyl protecting groups.
Abstract: The present disclosure provides novel crystalline forms of cabozantinib (S)-malate, designated as form-M1, M2, M3 and M4 and novel crystalline forms of cabozantinib free base, form-M1, M2 and M3 and methods of their production. The present disclosure also provides processes for the preparation of crystalline cabozantinib (S)-malate form N-1.
Abstract: The present invention relates to novel and stable polymorphic forms of Perindopril (L)-Arginine designated as Form ? and amorphous form and processes for their preparation. The present invention also provides the novel polymorph Form ? with greater stability to heat and humidity and can be prepared on large scale by an efficient, economic and reproducible process.
Abstract: The present disclosure relates to an improved process for the purification of fluticasone propionate by: a) dissolving fluticasone propionate in a ketone solvent to produce a mixture, b) heating the mixture slowly for 1-2 hours to get a clear solution, c) adding water to the step (b) solution at 50-60° C., d) cooling to ?5° C. to 10° C., and e) isolating fluticasone propionate.
Abstract: Described herein are processes for the preparation of nepafenac and related intermediates, particularly wherein 2-aminobenzophenone is treated with a 2-(alkylthio)acetamide in the presence of sulfuryl chloride to afford a 2-(2-amino-3-benzoyl-phenyl)-2-(alkylthio)acetamide, which upon reduction affords nepafenac. Described herein are also processes for the purification of nepafenac, particularly for the removal of structurally similar impurities.