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NOVEL FORMS OF LUMACAFTOR AND PROCESSES FOR THE PREPARATION THEREOF (Fri, 22 Feb 2019)
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.
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NOVEL FORMS OF LUMACAFTOR AND PROCESSES FOR THE PREPARATION THEREOF (Fri, 07 Apr 2017)
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.
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Novel dipeptidyl peptidase IV inhibitors and processes for their preparation and pharmaceutical compositions containing them (Sat, 28 May 2011)
Patent 571319 Disclosed is a compound of formula I, where Y is CN, n is 1 or 2, and wherein the other substituents are as defined in the specification. Also disclosed is a process for the synthesis of the compound. Also disclosed is the use of the compound to treat diabetes, a diabetic complication such as coronary artery disease, stroke, hypertension, nephropathy, peripheral vascular disease, neuropathy, and retinopathy, a metabolic disorder, impaired glucose tolerance, impaired fasting glucose, a diabetic complication, dislipidemia, hypercholesteromia, hypolipidemia, obesity, hyperglycemia, or for lowering blood glucose.
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DIBENZOFURAN DERIVATIVES AS INHIBITORS OF PDE-4 AND PDE-10 (Sat, 31 Mar 2012)
Patent 575389 Disclosed are compounds of formula (I) or any tautomer, stereoisomer, enantiomer, diastereomer, polymorph, pharmaceutically acceptable salt, pharmaceutically acceptable hydrate, pharmaceutically acceptable solvate, or N-oxide thereof, and methods for their preparation. Specific examples of a compound of formula (I) include: 1-(4-Methoxydibenzo[b,d]furan-1-yl)-4-oxocyclohexanecarbonitrile, Ethyl 6-cyano-6-(4-methoxydibenzo[b,d]furan-1-yl)-2-methyl-5,6,7,8-tetrahydroquinoline-3-carboxylate, and Ethyl {[6-cyano-6-(4-methoxydibenzo[b,d]furan-1-yl)-2-methyl-5,6,7,8-tetrahydroquinazolin-4-yl]oxy}acetate. Also disclosed are the use of compounds of formula (I) in treating allergic inflammatory conditions such as bronchial asthma, nephritis and allergic rhinitis, and more broadly, for treating asthma, chronic obstructive pulmonary disorder (COPD), allergic rhinitis, allergic conjunctivitis, respiratory distress syndrome, chronic bronchitis, nephritis, rheumatoid spondylitis, osteoarthritis, atopic dermatitis, eosinophilic granuloma, psoriasis, rheumatoid septic shock, ulcerative colitis, multiple sclerosis, chronic inflammation, Crohn���s syndrome and a central nervous system (CNS) disorder...
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Preparation of cobicistat intermediates (Fri, 14 Oct 2016)
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. embedded image
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Process for the preparation of sofosbuvir (Fri, 04 Nov 2016)
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.
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Process for the preparation of empagliflozin (Fri, 04 Nov 2016)
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. embedded image
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Novel dipeptidyl peptidase IV inhibitors and processes for their preparation and pharmaceutical compositions containing them (Fri, 17 Oct 2008)
The present invention relates to novel compounds representated by formula (I), where R, R1, R2, R3, X, Y, m, n are as defined.The present invention relates to compounds of the general formula I their derivatives, their analogs, their tautomeric forms, their stereoisomers, their diastereomers, their bioisosteres, their polymorphs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them which are predominantly dipeptidyl peptidase IV inhibitors. The present invention also relates to the processes for the preparation of novel compounds of formula (I) and their use in treating type II diabetes and diabetic complications thereof and also for treating dislipidemia, hypercholesterolemia, obesity and hyperglycemia.
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Dibenzofuran derivatives as inhibitors of PDE-4 and PDE-10 (Fri, 03 Apr 2009)
The present invention relates to novel heterocyclic compounds that are useful as phosphodiesterase inhibitors (PDEs) in particular phosphodiesterase type 4 (PDE IV) inhibitors and phosphodiesterase type 10 (PDE 10) inhibitors, processes for their preparation, pharmaceutical compositions containing them and their use in treating allergic and inflammatory diseases as well as for inhibiting the production of Tumor Necrosis Factor(TNF-α).
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DIBENZOFURAN DERIVATIVES AS INHIBITORS OF PDE-4 AND PDE-10 (Fri, 25 Dec 2009)

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Diebenzofuran derivatives as inhibitors of PDE-4 and PDE-10 (Fri, 13 Nov 2009)
The present invention relates to novel heterocyclic compounds that are useful as phosphodiesterase inhibitors (PDEs) in particular phosphodiesterase type 4 (PDE IV) inhibitors and phosphodiesterase type 10 (PDE 10) inhibitors, processes for their preparation, pharmaceutical compositions containing them and their use in treating allergic and inflammatory diseases as well as for inhibiting the production of Tumor Necrosis Factor (TNF-α). embedded image
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Process for the preparation of (3R, 3aS, 6aR)-hexahydrofuro[2,3-b]furan-3-ol (Thu, 03 Oct 2013)
The present invention relates to a novel process for the preparation of (3R, 3aS, 6aR)- hexahydrofuro [2, 3-b] furan-3-ol of formula I by reacting a compound of formula VII with the compound of formula R2-OH in the presence of haloginating agent to obtain a compound of formula VI and treating a compound of formula VI with dehaloginating agent to obtain a compound of formula V by reducing a compound of formula V, followed by cylization to obtain compound of formula IV and separating the enantiomer and diastereomers from compound of formula IV to yield a compound of formula I. Compound of formula I is useful as an intermediate in the preparation of protease inhibitors, in particular broad spectrum HIV protease inhibitors, the present invention also relates to process for the preparation of Darunavir from (3R, 3aS, 6aR)-hexahydrofuro [2, 3-b] furan-3-ol.
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Process for the Preparation of Velpatasvir (Fri, 05 Oct 2018)
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.
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Process for the preparation of sofosbuvir (Fri, 02 Nov 2018)
A process for the preparation of intermediates 9, useful in the synthesis of sofosbuvir, as well as intermediates of formula [12] are disclosed herein. embedded image
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PREPARATION OF COBICISTAT INTERMEDIATES (Thu, 13 Oct 2016)
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.
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Crystalline Darunavir (Fri, 28 Nov 2014)
The present invention relates to a non-solvated crystalline Darunavir, process for its preparation and pharmaceutical composition comprising it. The present invention also relates to a process for the preparation of amorphous Darunavir from a non-solvated crystalline Darunavir.
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Amorphous Ixazomib Citrate (Fri, 05 Oct 2018)
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.
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PROCESS FOR THE PREPARATION OF LAMIVUDINE AND NOVEL SALTS IN THE MANUFACTURE THEREOF (Thu, 23 Aug 2012)
The present invention relates to novel salts of Lamivudine and method for the preparation thereof. The present invention also relates to processes for the preparation of crystalline Lamivudine Form-I and Form-II from novel salts of Lamivudine.
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Process for the preparation of dolutegravir (Fri, 31 Aug 2018)
Processes for the preparation of dolutegravir and pharmaceutically acceptable salts utilizing alkenylamine are disclosed. Intermediates in those synthetic schemes are also disclosed.
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GALLOTANNIC COMPOUNDS FOR LITHOGRAPHIC PRINTING PLATE COATING COMPOSITIONS (Thu, 17 May 2012)
There is provided a gallotannic compound, a method of producing a gallotannic compound, a lithographic printing plate coating composition, a lithographic printing plate, a method of producing a lithographic printing plate and a method of printing.
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