The present invention relates to a lectin for use in the treatment, reduction in progression and curing of inflammation in a subject in need thereof. Pharmaceutical compositions comprising said lectin are also described. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 60% homology to SEQ ID NO: 2.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
2.
AN IMPROVED PROCESS FOR MANUFACTURING OF VALPROIC ACID AND/OR ITS SALT
The present invention provides an improved process for manufacturing of Valproic acid, intermediates, and sodium salt of valproic acid (Divalproex sodium). The present invention provides sequential additions of reactants and/or catalyst or reagents and/or solvent(s) which is most effective to achieve maximum conversion efficiency, less or no impurity formation, which overall results in increased yield as well as purity not less than 99%. Furthermore, it involves use of green solvents (recover and/or recycle easily); mild & cheaper catalyst or reagent; reduced reaction time and steps to be performed. In the present invention, synthesis of valproic acid is carried out without isolating any intermediate compound; and divalproex sodium is synthesised by heating valproic acid without use of solvent at about 60°C to about 110°C. The obtained compound of formula (Divalproex sodium) is substantially free of impurities.
C07C 53/128 - Acids containing more than four carbon atoms the carboxyl group being bound to a carbon atom bound to at least two other carbon atoms, e.g. neo-acids
C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
C07C 51/08 - Preparation of carboxylic acids or their salts, halides, or anhydrides from nitriles
C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
C07C 255/19 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same saturated acyclic carbon skeleton
3.
PROTEIN COMPOSITIONS FOR THE TREATMENT OF INFLAMMATORY DISEASES
The present invention relates to the pharmaceutical compositions of lectin proteins and its use for the prevention, treatment and cure of inflammation, including inflammatory disease. The invention specifically relates to the pharmaceutical compositions for topical application comprising lectin proteins and its use for prevention, treatment and cure of inflammation due to chemotherapy and/or radiotherapy. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 70% homology to SEQ ID NO: 1.
The present invention relates to the protein for treatment of infectious disease caused by Coronaviridae. In particular, the invention relates to a recombinant Sclerotium rolfsii lectin for use in the treatment, reduction in progression and curing of SARS-COV2 disease in a subject in need thereof. Pharmaceutical compositions comprising said recombinant Sclerotium rolfsii lectin are also described. The recombinant Sclerotium rolfsii lectin protein may comprise an amino acid sequence having at least 70% homology to SEQ ID NO: 1.
The present invention relates to the lectin protein for the treatment and prevention of neurodegenerative diseases. The invention further relates to the recombinant lectin protein is derived from Sclerotium rolfsii lectin having sequence 60% homologous to SEQ ID NO: 4 for the treatment and prevention of Neurodegenerative diseases. The invention specifically relates to lectin protein and its variants is derived from Sclerotium rolfsii lectin having sequence 60% homologous to SEQ ID NO: 4 for the treatment of prevention of Parkinson's disease, Alzheimer's disease, Dementia and symptoms of dementia.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07K 14/37 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from fungi
The present disclosure provides a modified protein sequence i.e., recombinantly expressed glycan binding protein. The said glycan binding protein is a variant of Sclerotium Rolfsii Lectin and is modified to include attributes like enhanced molecule stability, reduced N-terminal methionine impurities and aid in conjugation of protein to other biological and chemical agent(s).
C07K 14/37 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from fungi
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
7.
RECOMBINANT PROTEINS, COMPOSITIONS AND METHODS OF STABILIZATION THEREOF
The present invention relates to recombinant proteins, compositions and methods of stabilization thereof. The invention specifically relates to the stable recombinant protein of SEQ ID NO: 1 and composition comprising recombinant protein of SEQ ID NO: 1. The invention further relates to method of preparing, storing and stabilizing recombinant protein of SEQ ID NO: 1 and its composition for longer shelf life.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The present invention provides a binder free an immediate release oral stable pharmaceutical composition and process for preparing the same. Said pharmaceutical composition comprising a crystalline solriamfetol or a pharmaceutically acceptable salt thereof; and one or more pharmaceutically acceptable excipients, wherein pharmaceutically acceptable salt is solriamfetol hydrochloride in anhydrous crystalline Form A.
The present invention relates to a recombinant plasmid, methods and compositions for the expression of recombinant proteins with minimal N-terminal initiator methionine. The present invention also provides strategies for efficient removal of N-terminal initiator methionine in recombinant proteins expressed at industrial scale and provides method for producing proteins with minimal N-terminal initiator methionine.
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein Q is a group of formula Q1 or Q2; wavy bond represents the points of attachment; wherein R1 is —NRaRb; R2 is hydrogen or a C1-C10 alkyl group; Ra and Rb independently represent hydrogen or a C1-C10 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein Q is a group of formula Q1 or Q2; wavy bond represents the points of attachment; wherein R1 is —NRaRb; R2 is hydrogen or a C1-C10 alkyl group; Ra and Rb independently represent hydrogen or a C1-C10 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein Q is a group of formula Q1 or Q2; wavy bond represents the points of attachment; wherein R1 is —NRaRb; R2 is hydrogen or a C1-C10 alkyl group; Ra and Rb independently represent hydrogen or a C1-C10 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
(wavy bond)
A recombinant lectin for use in a method of treatment of cancer by inhibiting angiogenesis in a subject. The treatment comprises administration of a therapeutically effective amount of the recombinant lectin.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
13.
SUBSTITUTED TRICYCLIC COMPOUNDS AND THEIR USE IN COVID-19
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
15.
RECOMBINANT PROTEIN FOR TREATING SARS-COV2 DISEASE
Sclerotium rolfsiiSclerotium rolfsiiSclerotium rolfsiiSclerotium rolfsii lectin protein may comprise an amino acid sequence having at least 70% homology to SEQ ID NO:1.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The present invention relates to the protein for treatment of infectious disease caused by Coronaviridae. In particular, the invention relates to a recombinant Sclerotium rolfsii lectin for use in the treatment, reduction in progression and curing of SARS-COV2disease in a subject in need thereof. Pharmaceutical compositions comprising said recombinant Sclerotium rolfsii lectin are also described. The recombinant Sclerotium rolfsii lectin protein may comprise an amino acid sequence having at least 70% homology to SEQ ID NO:1.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The present disclosure provides a modified protein sequence i.e., recombinantly expressed glycan binding protein. The said glycan binding protein is a variant of Sclerotium Rolfsii Lectin and is modified to include attributes like enhanced molecule stability, reduced N-terminal methionine impurities and aid in conjugation of protein to other biological and chemical agent(s).
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
The present disclosure relates to protein-drug conjugates. The present disclosure specifically relates to the protein-drug conjugates, wherein the protein is a lectin protein having amino acid sequence of SEQ ID NO: 1; or lectin protein having at least 70% sequence identity to SEQ ID NO: 1. The disclosure further relates to process and composition of protein-drug conjugates and method of use thereof.
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
The present disclosure relates to protein-drug conjugates. The present disclosure specifically relates to the protein-drug conjugates, wherein the protein is a lectin protein having amino acid sequence of SEQ ID NO: 1; or lectin protein having at least 70% sequence identity to SEQ ID NO: 1. The disclosure further relates to process and composition of protein-drug conjugates and method of use thereof.
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
The present disclosure provides a modified protein sequence i.e., recombinantly expressed glycan binding protein. The said glycan binding protein is a variant of Sclerotium Rolfsii Lectin and is modified to include attributes like enhanced molecule stability, reduced N-terminal methionine impurities and aid in conjugation of protein to other biological and chemical agent(s).
C07K 14/37 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from fungi
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
The present invention relates to the pharmaceutical compositions of lectin proteins and its use for the prevention, treatment and cure of inflammation, including inflammatory disease. The invention specifically relates to the pharmaceutical compositions for topical application comprising lectin proteins and its use for prevention, treatment and cure of inflammation due to chemotherapy and/or radiotherapy. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 70% homology to SEQ ID NO: 1.
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
22.
PROTEIN COMPOSITIONS FOR THE TREATMENT OF INFLAMMATORY DISEASES
The present invention relates to the pharmaceutical compositions of lectin proteins and its use for the prevention, treatment and cure of inflammation, including inflammatory disease. The invention specifically relates to the pharmaceutical compositions for topical application comprising lectin proteins and its use for prevention, treatment and cure of inflammation due to chemotherapy and/or radiotherapy. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 70% homology to SEQ ID NO: 1.
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
23.
RECOMBINANT PROTEINS, COMPOSITIONS AND METHODS OF STABILIZATION THEREOF
The present invention relates to recombinant proteins, compositions and methods of stabilization thereof. The invention specifically relates to the stable recombinant protein of SEQ ID NO: 1 and composition comprising recombinant protein of SEQ ID NO: 1. The invention further relates to method of preparing, storing and stabilizing recombinant protein of SEQ ID NO: 1 and its composition for longer shelf life.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
24.
RECOMBINANT PROTEINS, COMPOSITIONS AND METHODS OF STABILIZATION THEREOF
The present invention relates to recombinant proteins, compositions and methods of stabilization thereof. The invention specifically relates to the stable recombinant protein of SEQ ID NO: 1 and composition comprising recombinant protein of SEQ ID NO: 1. The invention further relates to method of preparing, storing and stabilizing recombinant protein of SEQ ID NO: 1 and its composition for longer shelf life.
A61J 1/05 - Containers specially adapted for medical or pharmaceutical purposes for collecting, storing or administering blood, plasma or medical fluids
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
A61K 9/19 - Particulate form, e.g. powders lyophilised
The present invention relates to stable formulations of recombinant proteins. The invention specifically relates to the formulations of recombinant lectins derived from Sclerotium rolfsii lectin. The formulation comprises recombinant lectin derived from Sclerotium rolfsii lectin and a pharmaceutically acceptable excipient. The invention also relates to the stable liquid and/or lyophilized formulations comprising recombinant lectins derived from Sclerotium rolfsii lectin.
The present invention relates to the combination chemotherapy with recombinant lectin protein. The invention specifically relates to the cytotoxic effect of recombinant lectin protein having amino acid sequence of SEQ ID NO: 1 in combination with other therapeutic agents, wherein the other therapeutic agents are anti-cancer agents. The combinations are highly synergistic and efficacious against several cancers.
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
The present disclosure provides an extended release composition of tofacitinib for oral administration, and methods of making the composition. The extended release composition employs a matrix drug core comprising tofacitinib or a pharmaceutically acceptable salt thereof and at least one release controlling polymer. The matrix drug core is surrounded by a soluble functional coating comprising at least one coating polymer and at least one pharmaceutically acceptable excipient.
The present invention relates to the lectin protein for the treatment and prevention of neurodegenerative diseases. The invention further relates to the recombinant lectin protein is derived from Sclerotium rolfsii lectin having sequence 60% homologous to SEQ ID NO: 4 for the treatment and prevention of Neurodegenerative diseases. The invention specifically relates to: lectin protein and its variants is derived from Sclerotium rolfsii lectin, having sequence 60% homologous to SEQ ID NO: 4 for the treatment of prevention of Parkinson's disease, Alzheimer's disease, Dementia and symptoms of dementia.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 25/00 - Drugs for disorders of the nervous system
29.
LECTIN PROTEIN FOR TREATMENT AND PREVENTION OF NEURODEGENERATIVE DISEASES
Sclerotium rolfsiiSclerotium rolfsiiSclerotium rolfsii lectin, having sequence 60% homologous to SEQ ID NO: 4 for the treatment of prevention of Parkinson's disease, Alzheimer's disease, Dementia and symptoms of dementia.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 25/00 - Drugs for disorders of the nervous system
30.
Novel Process for the Preparation of Filgotinib and Intermediates Thereof
The present invention relates to a novel process for the preparation of filgotinib or a pharmaceutically acceptable salt and intermediates thereof which avoid Suzuki coupling reaction.
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein Q is a group of formula Q1 or Q2; wavy bond represents the points of attachment; wherein R1 is ?NRaRb; R2 is hydrogen or a C1-C10 alkyl group; Ra and Rb independently represent hydrogen or a C1-C10 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
11 is –NRaRb211010 alkyl group; Raand Rb11010 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
The present invention relates to a lectin for use in the treatment, reduction in progression and curing of inflammation in a subject in need thereof. Pharmaceutical compositions comprising said lectin are also described. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 60% homology to SEQ ID NO: 1.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
34.
Process for the preparation of Rivaroxaban involving novel intermediate
The present invention relates to the novel key intermediate, 4-{4-[(SS)-(Aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, m the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A recombinant lectin for use in a method of treatment of cancer by inhibiting angiogenesis in a subject. The treatment comprises administration of a therapeutically effective amount of the recombinant lectin.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A recombinant lectin for use in a method of treatment of cancer by inhibiting angiogenesis in a subject. The treatment comprises administration of a therapeutically effective amount of the recombinant lectin.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The present invention relates to the process to prepare recombinant lectin having amino acid sequence of SEQ ID NO:1, wherein the process comprises fed-batch fermentation of a clone in a host cell at specific feeding rate with carbon to Nitrogen ratio of 3:1 to 6:1. The invention also relates to the process of purification of recombinant lectin having amino acid sequence of SEQ ID NO: 1.
C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
B01D 15/32 - Bonded phase chromatography, e.g. with normal bonded phase, reversed phase or hydrophobic interaction
B01D 15/36 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving ionic interaction, e.g. ion-exchange, ion-pair, ion-suppression or ion-exclusion
C07K 1/20 - Partition-, reverse-phase or hydrophobic interaction chromatography
C07K 1/34 - ExtractionSeparationPurification by filtration, ultrafiltration or reverse osmosis
C07K 1/36 - ExtractionSeparationPurification by a combination of two or more processes of different types
C07K 14/42 - Lectins, e.g. concanavalin, phytohaemagglutinin
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
A modified lectin protein is provided having at least one amino acid modification in an amino acid sequence of SEQ ID NO. 1 orin an amino acid sequence having at least 60% homology thereto. The amino acid modification is selected from one of more of the following: at least one amino acid modification in a carbohydrate binding site; at least one amino acid modification in the N-terminus; at least one amino acid modification at position 76; or at least one amino acid modification at position 44 or 89. The modified lectin protein does not consist of the amino acid sequence of any of SEQ ID NOs: 2 to 4.
The present invention relates to stable formulations of recombinant proteins. The invention specifically relates to the formulations of recombinant lectins derived from Sclerotium rolfsii lectin. The formulation comprises recombinant lectin derived from Sclerotium rolfsii lectin and a pharmaceutically acceptable excipient. The invention also relates to the stable liquid and/or lyophilized formulations comprising recombinant lectins derived from Sclerotium rolfsii lectin.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The present invention relates to a novel process for the preparation of filgotinib or a pharmaceutically acceptable salt and intermediates thereof which avoid Suzuki coupling reaction. (I)
The present disclosure provides an extended release composition of tofacitinib for oral administration, and methods of making the composition. The extended release composition employs a matrix drug core comprising tofacitinib or a pharmaceutically acceptable salt thereof and at least one release controlling polymer. The matrix drug core is surrounded by a soluble functional coating comprising at least one coating polymer and at least one pharmaceutically acceptable excipient.
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present invention relates to a disintegrant free pharmaceutical composition comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. Particularly the present invention relates to disintegrant free immediate release dosage form comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. It further relates to process of preparing such composition and its use in psoriatic arthritis and psoriasis.
10 equal to or less than 5 μm and one or more and binders in an amount of 0.9% w/w or less, relative to the total weight of composition, where the composition is not free of binder and that the total amount of binder does not exceed 0.9% w/w relative to the total weight of the composition.
The invention relates to vortioxetine hydrobromide having particle size distribution of D98 100-200μ, D50 35-90μ and D5 7-30μ as well as to a stable, reproducible and bioequivalent pharmaceutical composition comprising vortioxetine hydrobromide having particle size distribution of D98 100-200μ, D50 35-90μ and D5 7-30μ and one or more pharmaceutically acceptable excipient. It is produced by wet granulation techniques.
An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.
The present invention relates to the combination chemotherapy with recombinant lectin protein. The invention specifically relates to the cytotoxic effect of recombinant lectin protein having amino acid sequence of SEQ ID NO: 1 in combination with other therapeutic agents, wherein the other therapeutic agents are anti-cancer agents. The combinations are highly synergistic and efficacious against several cancers.
The present invention relates to the combination chemotherapy with recombinant lectin protein. The invention specifically relates to the cytotoxic effect of recombinant lectin protein having amino acid sequence of SEQ ID NO: 1 in combination with other therapeutic agents, wherein the other therapeutic agents are anti-cancer agents. The combinations are highly synergistic and efficacious against several cancers.
The present invention relates to the process to prepare recombinant lectin having amino acid sequence of SEQ ID NO:l, wherein the process comprises fed-batch fermentation of a clone in a host cell at specific feeding rate with carbon to Nitrogen ratio of 3:1 to 6:1. The invention also relates to the process of purification of recombinant lectin having amino acid sequence of SEQ ID NO: 1.
C07K 14/42 - Lectins, e.g. concanavalin, phytohaemagglutinin
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
The present invention relates to a lectin for use in the treatment, reduction in progression and curing of inflammation in a subject in need thereof. Pharmaceutical compositions comprising said lectin are also described. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 60% homology to SEQ ID NO: 1.
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
51.
AN IMPROVED PROCESS FOR THE PREPARATION OF RECOMBINANT LECTIN PROTEIN
The present invention relates to the process to prepare recombinant lectin having amino acid sequence of SEQ ID NO:l, wherein the process comprises fed-batch fermentation of a clone in a host cell at specific feeding rate with carbon to Nitrogen ratio of 3:1 to 6:1. The invention also relates to the process of purification of recombinant lectin having amino acid sequence of SEQ ID NO: 1.
C07K 14/42 - Lectins, e.g. concanavalin, phytohaemagglutinin
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
The present invention relates to a lectin for use in the treatment, reduction in progression and curing of inflammation in a subject in need thereof. Pharmaceutical compositions comprising said lectin are also described. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 60% homology to SEQ ID NO: 1.
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A modified lectin protein is provided having at least one amino acid modification in an amino acid sequence of SEQ ID NO. 1 orin an amino acid sequence having at least 60% homologythereto. The amino acid modification is selected from one of more of the following: at least one amino acid modification in a carbohydrate binding site; at least one amino acid modification in the N-terminus;at least one amino acid modification at position 76; or at least one amino acid modification at position 44 or 89. The modified lectin protein does not consist of the amino acid sequence of any of SEQ ID NOs: 2 to 4.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A modified lectin protein is provided having at least one amino acid modification in an amino acid sequence of SEQ ID NO. 1 orin an amino acid sequence having at least 60% homologythereto. The amino acid modification is selected from one of more of the following: at least one amino acid modification in a carbohydrate binding site; at least one amino acid modification in the N-terminus;at least one amino acid modification at position 76; or at least one amino acid modification at position 44 or 89. The modified lectin protein does not consist of the amino acid sequence of any of SEQ ID NOs: 2 to 4.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
55.
LEADER SEQUENCE FOR HIGHER EXPRESSION OF RECOMBINANT PROTEINS
The present invention relates to the leader sequence for higher expression of recombinant proteins. The invention further relates to the process for preparation of insulin and insulin analogues using leader sequence. The leader peptides significantly increase the expression of pre-proinsulin. The present invention also relates to the protein sequences prepared by fusion of fragments with the leader sequences of the present invention. The invention is demonstrated by preparing and Insulin and its analogues using said leader sequences.
The present invention relates to the novel key intermediate, 4-{4-[(5S)-(Aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, in the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
57.
Process for preparation and purification of vortioxetine hydrobromide
The present invention is related to an improved process for the preparation and purification of crystalline Vortioxetine hydrobromide of Formula-I. The process according to present invention is operationally simple and suitable for industrial application which will avoid hazardous chemicals and eliminate column chromatography to get ICH quality of pharmaceutically acceptable active pharmaceutical ingredient having snow white appearance.
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
90 particle size of more than 100 microns, preferably between 300 and 1000 microns, and more preferably between 350 and 800 microns, and further comprising one or more pharmaceutically acceptable excipients. The present disclosure further provides a process for preparation of a pharmaceutical composition comprising apixaban by wet granulation.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
The present invention relates to an enzymatic process for the preparation of (R)- Sitagliptin. The process involves reductive amination of Pro-Sitagliptin to (R)- Sitagliptin using novel transaminase enzymes. The invention also relates to the Nucleotide sequences encoding novel transaminase enzymes and process to prepare transaminase enzymes.
The present invention relates to nucleotide sequence of SEQ ID 1 and SEQ ID 2 encoding recombinant 3-Quinuclidinone reductase and Glucose Dehydrogenase respectively. The invention further relates to the clone comprising the said nucleotide sequences and process to prepare 3-Quinuclidinone reductase and Glucose Dehydrogenase having amino acid sequence of SEQ ID 3 and SEQ ID 4, respectively.
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to a disintegrant free pharmaceutical composition comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. Particularly the present invention relates to disintegrant free immediate release dosage form comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. It further relates to process of preparing such composition and its use in psoriatic arthritis and psoriasis.
The present invention relates to a disintegrant free pharmaceutical composition comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. Particularly the present invention relates to disintegrant free immediate release dosage form comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. It further relates to process of preparing such composition and its use in psoriatic arthritis and psoriasis.
Rhodotorula rubraRhodotorula rubra. The invention also relates to enzymatically produced (R)-3-quinuclidinol wherein the substrate loading capacity of the enzyme is not less than 100g/L.
The invention relates to a pharmaceutical composition comprising cinacalcet or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipient. The invention also relates to the pharmaceutical composition comprising cinacalcet or pharmaceutically acceptable salts thereof having a particle size distribution D 90 equal to or less than 20 µm, D 50 equal to or less than 10 µm, and D equal to or less than 5 µm and one or more and binders in an amount of 0.9% w/w or less, relative to the total weight of composition, wherein the composition is not free of binder and that the total amount of binder does not exceed 0.9%w/w relative to the total weight of the composition.
An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
67.
AN IMPROVED PROCESS FOR PREPARATION AND PURIFICATION OF VORTIOXETINE HYDROBROMIDE
The present invention is related to an improved process for the preparation and purification of crystalline polymorph of Vortioxetine hydrobromide of Formula-I and Vortioxetine hydrochloride of Formula-Ia. The process according to present invention is operationally simple and suitable for industrial application which will avoid hazardous chemicals and eliminate column chromatography to get ICH quality of pharmaceutically acceptable active pharmaceutical ingredient having snow white appearance.
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 295/096 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
The present disclosure relates to a stable, reproducible and bioequivalent apixaban compositions, wherein the composition comprising apixaban having a D90 particle size of more than 100 microns, preferably between 300 and 1000 microns, and more preferably between 350 and 800 microns, and further comprising one or more pharmaceutically acceptable excipients. The present disclosure further provides a process for preparation of a pharmaceutical composition comprising apixaban by wet granulation.
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 9/00 - Medicinal preparations characterised by special physical form
The invention relates to vortioxetine hydrobromide having particle size distribution of D98 100-200μ, D50 35-90μ and D5 7-30μ as well as to a stable, reproducible and bioequivalent pharmaceutical composition comprising vortioxetine hydrobromide having particle size distribution of D98 100-200μ, D50 35-90μ and D5 7-30μ and one or more pharmaceutically acceptable excipient. It is produced by wet granulation techniques.
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
C07D 211/20 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
C07D 295/033 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic rings
C07D 295/096 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
70.
AN IMPROVED PROCESS FOR THE PREPARATION OF RIVAROXABAN INVOLVING NOVEL INTERMEDIATE
The present invention relates to the novel key intermediate, 4-{4-[(5S)-(Aminomethyl)-2- oxo-l,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, in the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
71.
Process for the preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine
The present disclosure is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises:
(a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4-methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino-4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive amination of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4-methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine. The disclosure is also related to novel intermediates:
wherein R, R′ and X are as described in the specification.
C07D 211/72 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.
The present invention relates to an improved process for the synthesis of (R)- Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.
The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.
The present invention relates to resinates of pharmaceutically acceptable salts of Tofacitinib such as Tofacitinib Citrate, fast disintegrating and or quick release pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions. The resin used to prepare the resinate is selected from copolymers of methacrylic acid and divinylbenzene, cross linked polymer of methacrylic acid and divinylbenzene, sulphonated copolymers of styrene and divinylbenzene. Ion exchange resin is contacted with the solution of Tofacitinib citrate under controlled pH in order to form the resinate. The resinate has versatile use in making of pharmaceutical preparations. Few such pharmaceutical preparations are Tablets, capsules, dry syrups, suspensions, lozenges, films.
The present invention relates to resinates of Tofacitinib. The invention also relates to taste masked, stable and readily dispersible resinates of Tofacitinib, rapidly disintegrating and or quick release taste masked pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions. In order to form the resinate, the resin is selected from copolymers of methacrylic acid and divinylbenzene, cross linked polymer of methacrylic acid and divinylbenzene, sulphonated copolymers of styrene and divinylbenzene. In order to form the resinate, Ion exchange resin is contacted with the solution of Tofacitinib prepared in nonaromatic solvent. The resinate is useful to formulate different pharmaceutical dosage forms such as Tablets, Capsule, drysyrups.
The present invention relates to a process for the preparation of Azilsartan Medoxomil Potassium. The invention further relates to novel highly crystalline polymorph of Azilsartan Medoxomil Potassium and composition comprising it. The invention provides thermostable highly crystalline polymorph of Azilsartan Medoxomil Potassium and process to produce a composition comprising the novel highly crystalline polymorph of Azilsartan Medoxomil Potassium.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
The present invention relates to Orally Disintegrating Tablets (ODT) of Tofacitinib and its pharmaceutically acceptable salts and the process to produce the ODT. The invention further relates to ODTs comprising Tofacitinib and its pharmaceutically acceptable salts, at least one sweetening agent, at least one disintegrant and optionally other excipients. The weight of the Orally Disintegrating tablets is 200 mg or less. The invention further relates to Orally Disintegrating Tablets of Tofacitinib Citrate.
The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.
The present invention relates to a process for the preparation of Azilsartan Medoxomil Potassium. The invention further relates to novel highly crystalline polymorph of Azilsartan Medoxomil Potassium and composition comprising it. The invention provides thermostable highly crystalline polymorph of Azilsartan Medoxomil Potassium and process to produce a composition comprising the novel highly crystalline polymorph of Azilsartan Medoxomil Potassium.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
C07D 413/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
The present invention relates to novel processes for the preparation of Ranolazine (I) and its acid addition salts and the novel process for the preparation of compound of formula (7).
C07D 295/15 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
C07D 303/23 - Oxiranylmethyl ethers of compounds having one hydroxy group bound to a six-membered aromatic ring, the oxiranylmethyl radical not being further substituted, i.e.
82.
AN IMPROVED PROCESS FOR THE PREPARATION OF PHARMACOPOEIAL GRADE INTERFERON ALPHA 2B
The present invention relates to a simple and scalable process for the production of pharmacopoeial grade Interferon alpha 2b by fed-batch fermentation followed by purification using chromatography techniques. The invention also relates to the recombinant expression of interferon alpha 2b in soluble form by fermentation to obtain high yields. The process involves clarification and chromatographic steps for the purification of Interferon alpha 2b.
(a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4-methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino-4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive amination of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4-methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine. The invention is also related to novel intermediates:
wherein R, R′ and X are as described in the specification.
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 211/72 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
84.
AN IMPROVED PROCESS FOR THE PREPARATION OF APIXABAN AND INTERMEDIATES THEREOF
The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.
The present invention is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: (a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4- methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino- 4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive animation of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4- methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1- benzyl-4-methylpiperidin-3-yl)-methylamine. The invention is also related to novel intermediates.
The present invention provides a method for preparing a recombinant lectin expressed in a host cell such as E.coli or yeast, said method comprising the synthesis of a lectin gene based on amino acid sequence derived from the MALDI MS/MS of the Sclerotium rolfsii lectin (SEQ ID.1), a soil borne phytopathogenic fungus, and its cloning in the host cell.
The present invention discloses genes for new variants in E.coli that are more close to the wild type lectin sequence but still differ in surface charges. This recombinant version (exemplified Rec-2 and Rec-3) are cancer cell binding with anti tumor activity show blood group specificity similar to the native lectin but retains the stability and the solubility properties.
Derivatives of anacardic acid having antimicrobial properties and method for preparing said derivatives. The antimicrobial properties include bacteriostatic and bacteriocidal activity.
C07C 237/28 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
C07C 65/01 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
C07C 229/54 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
A01N 37/18 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof
89.
A NOVEL PROCESS FOR THE PREPARATION OF 2-HALO-4-AMINOQUINAZOLINES
2-Halo-4-aminoquinazolines are produced by a one-step process involving intramolecular cyclization of appropriately substituted formamide derivatives in the presence of phosphorous oxyhalides. Exemplary of the process is the intramolecular cyclization of 3,4-dimethoxy-6-cyanoaniline-1-yl formamide in the presence of phosphorous oxychloride to 2-chloro-4-amino-6,7-dimethoxyquinazoline. These chemical compounds are utilized as intermediates in the preparation of some of the important antihypertensive agents e.g. 2-chloro-4-amino-6,7-dimethoxyquinazolines is used for the synthesis of alfuzosin hydrochloride.
Derivatives of anacardic acid having antimicrobial properties and method for preparing said derivatives. The antimicrobial properties include bacteriostatic and bacteriocidal activity.
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group
92.
IMPROVED MANUFACTURING PROCEDURE FOR THE PREPARATION OF POLYMORPHIC FORM II OF CIS-(1S)-N-METHYL-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPTHLENEAMINE HYDROCHLORIDE (SERTRALINE HYDROCHLORIDE)
The present invention relates to the improved, scalable and efficient manufacturing procedure for the preparation of the antidepressant Cis-(1S)-N-Methyl-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1-napthaleneamine hydro chloride, Sertraline Hydrochloride polymorphic form II. The present invention further relates to the improved and modified procedures for preparing, separating and isolating the key intermediates involved in the preparationof Sertraline Hydrochloride polymorphic form II. The present invention also further relates to the use of novel reagents or a combination thereof and new methodologies to prepare some o'f the key intermediates involved in the preparation of Polymorphic Form II of Sertraline Hydrochloride.
C07C 209/26 - Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds by reduction with hydrogen
C07C 209/28 - Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds by reduction with other reducing agents
C07C 211/42 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
93.
AN IMPROVED PROCESS FOR THE MANUFACTURE OF LOSARTAN POTASSIUM
The present invention relates to an improved process for the manufacture of Losartan potassium. The process comprises of condensation of 2-butyl-4-chloro-5-formyl imidazole with 2-cyano-4-bromomethyl biphenyl in a biphasic solvent system under phase transfer catalysis followed by insitu reduction using sodium borohydride. The obtained product is converted to Losartan by treating with sodium azide and an amine salt. Losartan is then converted to its potassium salt by treating it with potassium hydroxide in alcohol.
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
The present invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2, 3-dihydro-1H-pyrrolizin-5-yl acetic acid, in which the key intermediate, 5-Benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole is obtained by the hydrogenation of 2,2-dimethyl-4-oxo-5-phenyl-nitropentane. The invention also relates to the preparation of the intermediates occurring in the above process.
C07C 205/45 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by at least one doubly-bound oxygen atom, not being part of a —CHO group
C07D 207/20 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07C 49/213 - Unsaturated compounds containing keto groups bound to acyclic carbon atoms containing six-membered aromatic rings
C07C 49/203 - Unsaturated compounds containing keto groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
95.
A PROCESS FOR THE PREPARATION OF EZETIMIBE VIA A NOVEL INTERMEDIATE
The present invention relates to a process for the preparation of Ezetimibe via a novel intermediate. Trans-3(R)-(3-⏧2-oxo-4(S)-(4-benzyloxyphenyl)-1-(4-fluorophenyl)-azetidinyl]propanoic acid is converted to trans-N-methoxy-N-methyl-3(R)-3-⏧2-oxo-4(S)-(4-benzyloxyphenyl)-1-(4-fluorophenyl)-azetidinyl]propanamide and the resultant intermediate is subjected to Grignard reaction to obtain trans-1-(4-fluorophenyl)-3(R)-⏧3-oxo-3-(4-fluorophenyl)propyl]-4(S)-(4-benzyloxyphenyl)-2-azetidinone. Reduction of trans-1-(4-JGiuorophenyl)-3(R)-⏧3-oxo-3-(4-fluorophenyl) propyl]-4(S)-(4-benzyloxyphenyl)-2-azetidinone, followed by debenzylation provides Ezetimibe. The invention also relates to the preparation of the intermediate occurring in the above process.
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
96.
A NOVEL PROCESS FOR PREPARATION OF VENLAFAXINE HYDROCHLORIDE AND ITS INTERMEDIATES
A process for the preparation of 1-cyano-⏧(4-methoxyphenyl)methyl] cyclohexanol by reacting cyclohexanone with the carbanion of 4-methoxyphenyl acetonitrile in the presence of polyethylene glycol-400 (PEG-400) or Aliquate-336, as a phase transfer catalyst (PTC). The present invention also relates to an novel process for the preparation of 1-⏧2-amino-1-(4-methoxyphenyl)ethyl]cyclohexanol, using borane-dimethyl sulphide complex (BDMS) or AlCl3-NaBH4, in refluxing tetrahydrofuran. 1-⏧2-Amino-1-(4-methoxyphenyl)ethyl]cyclohexanol thus obtained was subjected to N,N-dimethylation using formic acid-formaldehyde in boiling 1,4-dioxane: water mixture to obtain 1-⏧2-(dimethylamino)-1-(4-methoxyphenyl)ethyl] cyclohexanol in high purity, which was treated with isopropanol saturated with HCl gas to get venlafaxine hydrochloride in high purity and high yield.
C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
C07C 255/37 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by etherified hydroxy groups
C07C 209/28 - Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds by reduction with other reducing agents
C07C 211/27 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains
97.
A NOVEL PROCESS FOR PREPARATION OF ARIPIPRAZOLE AND ITS INTERMEDIATES
A process for the preparation of 7-hydroxy-3,4-dihydro carbostyril (II) by intramolecular Fridel-Craft alkylation of N-(3-methoxyphenyl)-3-chloropropionamide (I) in which an equivalent of N-(3-methoxyphenyl)-3-chloropropionamide (I) is contacted with a Lewis acid (e.g. aluminium chloride) in dimethyl acetamide (DMA), at an elevated temperature of from about 120°C to about 160°C, is provided. The process produces 7-hydroxy-3,4- dihydro carbostyril (II) in high yield and a high state of purity such that it may be used in subsequent .reaction towards the preparation of aripiprazole (IV). Thus 7-hydroxy-3,4- dihydro carbostyril (II) was treated with l-bromo-4-chlorobutane under phase transfer catalyst (PTC) conditions using solvents like acetone or n-butanol at temperature ranging 25°C to 45°C to afford 7-(4-chlorobutoxy)-3,4-dihydro carbostyril (III). The PTC conditions described in this patent afford 7-(4-chlorobutoxy)-3,4-dihydro carbostyril (III) in high purity and high yield with the corresponding dimmer formation is considerably low as compared with the other literature methods of preparing 7-(4-chlorobutoxy)-3,4- dihydro carbostyril (III). Compound (III) was treated with l-(2,3-dichlorophenyl)piperazine, at temperature ranging from 50°C to 100°C, and sodium iodide, potassium carbonate, dimethyl formamide (DMF) as a solvent to afford aripiprazole in high purity and high yield.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
98.
AN IMPROVED PROCESS FOR PREPARATION OF LEFLUNOMIDE
This invention describes a process for the preparation of N-(4-trifluoromethyl)-5-methylisoxazole-4-carboxamide commonly known as leflunomide comprising : (a) reacting ethylaceto acetate, triethylorthoformate, and acetic anhydride with simultaneous distillation to form ethyl ethoxymethyleneacetoacetic ester; (b) reacting the ethyl ethoxymethyleneacetoacetic ester with aqueous hydroxylamine without using any external base and without any distillation to form ethyl-5-methylisoxazole-4-carboxylate; (c) reacting the ethyl-5-methylisoxazole-4-carboxylate with strong acid to form -5-methylisoxazole-4-carboxylic acid; (d) 5-methylisoxazole-4-carboxylic acid is reacted with thionyl chloride in presence of N, N-Dimethylformamide and equimolar of 4-trifluoromethylaniline without any external base to obtain highly pure Leflunomide.
The present invention provides a novel one-pot process for preparation of Pantoprazole sodium sesquihydrate Form-I in the pure form without isolating the pantoprazole base.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
100.
A NOVEL PROCESS FOR THE SYNTHESIS OF LAMOTRIGINE AND ITS INTERMEDIATE
This invention discloses a process for the preparation of 3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of a formula (I), commonly known as Lamotrigine which comprises the step of reacting aminoguanidine bicarbonarte and 2,3- dichlorobenzocynide with a reagent prepared by dissolving phosphorus pentoxide and methane sulfonic acid, to produce a novel intermediate 2-(2,3-dichlorophenyl)-2-(aminoguanidine)-acetonitrile monomesylate which is further cyclized to lamotrigine without basification.
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