The present invention relates to vaccine(s) comprising cancer cells expressing antigen(s), excipients, optionally adjuvant wherein the said antigen(s) is expressed on contacting the said cancer cell with p38 inducer, for use in treatment of Cancer. The vaccine composition induces specific immune response against homologous and heterologus cancer cells of the tissue/organ. The invention also provides method of preparing the same.
The present invention relates to vaccine(s) comprising cancer cells expressing antigen(s), excipients, optionally adjuvant wherein the said antigen(s) is expressed on contacting the said cancer cell with p38 inducer, for use in treatment of Cancer. The vaccine composition induces specific immune response against homologous and heterologus cancer cells of the tissue/organ. The invention also provides method of preparing the same.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for human use namely pharmaceutical preparations for the treatment and prevention of cardiovascular diseases, cardiovascular pharmaceutical preparations, pharmaceutical preparations for the treatment of vascular diseases, pharmaceutical preparations for the treatment of hypertension; Pharmaceutical products and preparations for treatment of cardiovascular diseases; pharmaceutical products and preparations for the treatment of hypertension; pharmaceutical preparations, namely, fixed doses of combination medications containing simvastatin, ramipril, atenolol, hydrochlorothiazide, and acetylsalicylic acid (ASA)
The present invention relates to novel stable indole-3-carbinol derivatives of Formula-I and its pharmaceutical composition and biological activity. The present invention includes compositions and methods for the treatment and prevention of conditions associated with Inflammation.
C07D 209/26 - Radicals 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 an acyl radical attached to the ring nitrogen atom
C07D 209/12 - Radicals substituted by oxygen atoms
Mycobacterium w can also be used along with other therapeutic agent(s)/modalities as per the requirement. The squamous type of non small cell lung cancer is known to be desmocollin-3 expressing cancer. Other cancers also express desmocollin-3.
The present invention relates to novel stable indole-3-carbinol derivatives of Formula-I and its pharmaceutical composition and biological activity. The present invention includes compositions and methods for the treatment and prevention of conditions associated with Inflammation.
The present invention relates to novel stable indole-3-carbinol derivatives of Formula-I and its pharmaceutical composition and biological activity. The present invention includes compositions and methods for the treatment and prevention of conditions associated with Inflammation.
Mycobacterium w or combination there of shows altered protein profile. Thus altered protein profile has at least one protein commonly expressed or over expressed. The commonly expressed or over expressed protein induces immune response specific to cancer cells (homologue and hetrologus) of tissue/organ of origin. The immune response generated by administration of commonly expressed or over expressed antigen not reactive to normal cells and cancer cells or different tissue/organ of origin.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
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
9.
A PROCESS FOR THE PREPARATION OF 6-FLUORO-3,4-DIHYDRO-2H-CHROMENE- 2-CARBALDEHYDE
The present invention relates to a process for ihe preparation of 6-f!uoro-3,4-dihydro- 2H-chromene-2-carbaidehyde which is useful as an Intermediate in the synthesis of Nebivolol or its pharmaceutical acceptable salts.
C07D 311/58 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4
C07D 311/66 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4 with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
The present invention relates to a process for the preparation of Bosentan (Formula 1) or pharmaceutically acceptable salts or hydrates thereof which results the product substantially free of impurities like ethylene glycol bis-sulfonamide dimer and 6-hydroxy sulfonamide. The process according to present invention is also producing Bosentan sodium and Bosentan ammonium which gives Bosentan or pharmaceutically acceptable salts or hydrates thereof in improved yield and quality as compared to prior art processes.
The present invention relates to a stable oral pharmaceutical composition with improved solubility and bioavailability; comprising a taxoid, a solubilizer, a stabilizing agent, a surfactant(s), a solvent(s), and an oil wherein the concentration of taxoid is in the range of 0.1 to 10%.
A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
A01N 43/02 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
The present invention relates to stable liquid pharmaceutical compositions of curcumin or its pharmaceutically acceptable salts or its derivatives with higher curcumin concentration and improved bioavailability without the use of buffer and/or molecular aggregation inhibitor(s). In accordance with present invention the curcumin is in the solubilized form to make a stable liquid pharmaceutical composition.
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A61K 31/21 - Esters, e.g. nitroglycerine, selenocyanates
Cancer cells when treated with cisplatin, paclitaxel, gemcitabine, Mycobacterium w or combination thereof show altered protein profile. Thus altered protein profile has at least one protein commonly expressed or over expressed. The commonly expressed or over expressed protein induces immune response specific to cancer cells (homologous and heterologous) of tissue/organ of origin. An immune response is generated by administration of commonly expressed or over expressed antigen not reactive to normal cells and cancer cells or different tissue/organ of origin.
Cancer cells when treated with cisplatin, paclitaxel, gemcitabine, Mycobacterium w or combination thereof show altered protein profile. Thus altered protein profile has at least one protein commonly expressed or over expressed. The commonly expressed or over expressed protein induces immune response specific to cancer cells (homologous and heterologous) of tissue/organ of origin. An immune response is generated by administration of commonly expressed or over expressed antigen not reactive to normal cells and cancer cells or different tissue/organ of origin.
This invention discloses the process for lyophilization of the treated cells which comprises the use of a solution containing Trehalose along with amphipathic polymer Polyvinylpyrrolidone. Further the invention discloses the process treating cancer cells, freezing, lyophilizing and reconstituting. Immunomodulator treated dead, but intact cancerous cells were recovered, which can subsequently be used for cancer immunotherapy.
The present invention relates to vaccine(s) comprising cancer cells expressing antigen(s), excipients, optionally adjuvant wherein the said antigen(s) is expressed on contacting the said cancer cell with p38 inducer, for use in treatment of Cancer. The vaccine composition induces specific immune response against homologous and heterologus cancer cells of the tissue /organ. The invention also provides method of preparing the same.
The present invention relates to vaccine(s) comprising cancer cells expressing antigen(s), excipients, optionally adjuvant wherein the said antigen(s) is expressed on contacting the said cancer cell with p38 inducer, for use in treatment of Cancer. The vaccine composition induces specific immune response against homologous and heterologus cancer cells of the tissue /organ. The invention also provides method of preparing the same.
The present invention relates to increase in survival of mammals suffering from desmocollin 3 expressing cancers. Mycobacterium w is administered to mammals suffering from desmocollin-3 expressing cancers. The administration of 6 Mycobacterium w results in control of tumor and improvement in survival. Mycobacterium w can also be used along with other therapeutic agent(s) / modalities as per the requirement. The squamous type of non small cell lung cancer is known to 9 be desmocollin-3 expressing cancer. Other cancers also express desmocollin-3.
The present invention relates to increase in survival of mammals suffering from desmocollin 3 expressing cancers. Mycobacterium w is administered to mammals suffering from desmocollin-3 expressing cancers. The administration of 6 Mycobacterium w results in control of tumor and improvement in survival. Mycobacterium w can also be used along with other therapeutic agent(s) / modalities as per the requirement. The squamous type of non small cell lung cancer is known to 9 be desmocollin-3 expressing cancer. Other cancers also express desmocollin-3.
The present invention relates to a process for the removal of t-butyl group from t-butyl methyl 4-(2',3'-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate to provide-1,4-dihydro-2,6-dimethyl-4-(2',3'-dichorophenyl)-5-methoxycarbonyl-3-pyridine- carboxylic acid, which is further converted to to yield clevidipine having HPLC purity over 6 99%.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 405/00 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to a process for the manufacture of N-[2-(7-methoxy-1-naphthalenyl) ethyl]acetamide (Agomelatine) with improved yield and reduced level of N- acetyl-N-[2-(7-methoxy-1-naphthalenyl) ethyl]acetamide impurity.
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 233/21 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings
The present invention relates to the stable oral pharmaceutical composition with improved solubility and bioavailability; comprising of taxoid, solubilizer, stabilizing agent, surfactant(s), solvent(s), and oil wherein the concentration of taxoid is in the range of 0.1 to 10%.
The present invention relates to stable liquid pharmaceutical compositions of curcumin or its pharmaceutically acceptable salts or its derivatives with higher curcumin concentration and improved bioavailability without the use of buffer and/or molecular aggregation inhibitor(s). In accordance with present invention the curcumin is in the solubilized form to make a stable liquid pharmaceutical composition.
The present invention relates to process for preparation of novel compounds which are acting as inhibitors of dipeptidyl peptidase-IV enzyme and is depicted by the structural formula as given below: Formula VI. Which are useful in the treatment or prevention of diseases in which the dipeptidylpeptidase-IV enzyme is involved, such as diabetes and particularly type-2 diabetes.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
C07D 295/00 - 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
25.
Stable pharmaceutical composition for atherosclerosis
The present invention relates to a stable solid oral pharmaceutical multi-component composition comprising combination of blood pressure lowering drugs with lipid lowering agent/s and optionally a platelet aggregation inhibitor in a single dosage form. The blood pressure lowering agents are selected from β-adrenergic receptor blocking agent, ACE inhibitor and diuretic. The lipid lowering agent is selected from HMG Co-enzyme-A reductase inhibitor. The pharmaceutical composition made as per present invention a) overcomes any drug-drug interactions, b) exhibits pharmacokinetic and pharmacodynamic profile of individual therapeutic agent, c) has minimal side effects. The invention provides multi-component composition (MCC) to increase adherences to therapy. The MCC as per present invention provides compositions that maintain activity of all active ingredients without significant increase in adverse event profile. The present invention further relates to a method of preparing the said pharmaceutical composition.
The present invention relates to a novel process for the conversion of (2R)-6-fluoro- 2-[(2S)-oxiran-2-yl]-3,4-dihydro-2H-chromene (formula lll-A) to (2R)-6-fluoro-2-[(2R)-oxiran- 2-yl]-3,4-dihydro-2H-chromene (formula lll-B). The compound of formula lll-A and formula lll-B are key intermediates for preparing Nebivolol.
C07D 311/58 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4
C07D 407/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof. The invention relates to novel amino acid derivatives of the formula (1), wherein, A is amino acid B is peptide bond R-NH- wherein R is defined in the specification
This invention discloses the process for lyophilisation of the treated cells which comprises the use of a solution containing Trehalose along with amphipathic polymer Polyvinylpyrrolidone. Further the invention discloses the process treating cancer cells, freezing, lyophilizing and reconstituting, lmmunomodulator treated dead, but intact cancerous cells were recovered, which can subsequently be used for cancer immunotherapy.
This invention discloses the process for lyophilisation of the treated cells which comprises the use of a solution containing Trehalose along with amphipathic polymer Polyvinylpyrrolidone. Further the invention discloses the process treating cancer cells, freezing, lyophilizing and reconstituting, lmmunomodulator treated dead, but intact cancerous cells were recovered, which can subsequently be used for cancer immunotherapy.
The present invention relates to an improved process for the preparation of pure amorphous atorvastatin calcium comprising reaction of (3R,5R)-2-(4-fluorophenyl)- 3,5-dihydroxy-5-(1 -methylethyl)-3-phenyl-4-[(phenyl amino) carbonyl]-1 H-pyrrole-1 - heptanoic acid t-butyl ester (formula-2) in water immiscible organic solvent with aqueous alkali to give an alkali metal salt of atorvastatin is then converted in-situ to atorvastatin calcium by treatment with calcium source, which is further converted to amorphous atrovastatin calcium by drying and micronization to obtain product having HPLC purity Q 99.5% and free of inorganic impurities.
A01N 43/46 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom rings with more than six members
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
The present invention is directed to novel compounds of formula I and pharmaceutically acceptable salts, enantiomers thereof having inhibiting properties of dipeptidyl peptidase IV enzyme (DP-IV inhibitors). The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds along with its composition in the prevention or treatment of diseases associated with DP-IV enzyme.
2 are as defined in specification.
The present invention relates to pharmaceutical compositions comprising rifampicin, piperine as a bioenhancer for rifampicin and isoniazid is in delayed release form, wherein the said pharmaceutical compositions have maintained bioavailability of rifampicin in presence of isoniazid. The present invention further relates to process for preparing pharmaceutical composition comprising rifampicin, piperine and isoniazid.
C07D 513/00 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or
The present invention relates to a pharmaceutical composition comprising rifampicin and piperine with enhancement in bioavailability of rifampicin by piperine. The present invention further relates to process for preparing pharmaceutical composition comprising rifampicin and piperine.
C12P 17/18 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH (India)
Inventor
Modi, Indravadn, Ambalal
Khamar, Bakulesh, Mafatlal
Gupta, Chhitar, Mal
Puri, Anju
Bhatta, Rabi, Sankar
Pratap, Ram
Jain, Girish, Kumar
Bhadauria, Smrati
Khanna, Ashok, Kumar
Asthana, Omkar, Prasad
Ghatak, Ashim
Abstract
The present invention related to hypolipaemic pharmaceutical compositions comprising lipid lowering agents and BAR antagonist such as 3β-hydroxy pregna-5,16-dien-20-one (Herein known as 16 DP), Guggulsterones, 16 DP is also given a compound number 80/574.
The present invention relates to a stable solid oral pharmaceutical multi-component composition comprising combination of blood pressure lowering drugs with lipid lowering agent/s and optionally a platelet aggregation inhibitor in a single dosage form. The blood pressure lowering agents are selected from β-adrenergic receptor blocking agent, ACE inhibitor and diuretic. The lipid lowering agent is selected from HMG Co-enzyme-A reductase inhibitor. The pharmaceutical composition made as per present invention a) overcomes any drug-drug interactions, b) exhibits pharmacokinetic and pharmacodynamic profile of individual therapeutic agent, c) has minimal side effects. The invention provides multi-component composition (MCC) to increase adherences to therapy. The MCC as per present invention provides compositions that maintain activity of all active ingredients without significant increase in adverse event profile. The present invention further relates to a method of preparing the said pharmaceutical composition.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
36.
AN IMPROVED PROCESS FOR THE PREPARATION OF PALIPERIDONE
The invention relates to an improved process for the preparation of Palϊperidone in high yield and purity. The purity of Paliperidone is ~99.7 % by HPLC, wherein total impurity is less than about 0.3 % and each individual impurity is less than about 0.1 %. The invention also relates to provide the alcohol-water co-solvent for the purification of Paliperidone.
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
37.
NOVEL PROCESS FOR PREPARING PURE 6-FLUORO-3-PIPERIDIN-4-YL-1,2-BENZISOXAZOLE HYDROCHLORIDE AND ITS CONVERSION TO PALIPERIDONE
The invention relates to novel process for providing substantially pure 6-Fluoro-3- piperidin-4-yl-1,2-benzisoxazole hydrochloride and its conversion to Paliperidone having dimer compound of structural formula-1 A is less than 0.2 % and HPLC purity > 99.7%.
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
38.
PREPARATION OF 3-(2-HYDROXY ETHYL)-9-HYDROXY-2-METHYL-4H-PYRIDO-[1,2-A]-PYRIMIDIN-4-ONE OR ITS ACID ADDITION SALT
The invention relates to an improved process for preparation of 3-(2-hydroxy ethyl)-9- hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one or its acid addition salt and its conversion to paliperidone or its acid addition salt without involving the use of an acid catalyst.
C07D 471/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups
The invention relates to an improved process for preparation of 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one, an intermediate used in the synthesis of paliperidone and process for converting the same to Paliperidone.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
The invention provides novel adjuvants and pharmaceutical composition comprising of an adjuvant alone. The invention also provides novel vaccine compositions comprising of an antigen and a novel adjuvant. The novel adjuvant as per present invention is farnesoid-X-receptor (FXR) antagonist. The invention also relates to an adjuvant for variety of antigens. The adjuvant improves antibody production specific to incorporated antigen. The adjuvant also induces cell mediated immune response.
The present invention is directed to novel compounds of formula I and pharmaceutically acceptable salts, enantiomers thereof having inhibiting properties of dipeptidyl peptidase IV enzyme (DP-IV inhibitors). The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds along with its composition in the prevention or treatment of diseases associated with DP-IV enzyme. wherein, A is defined as R3-R4 wherein R3 and R4 are together or independently defined as peptides having amino acids ranging from 1 to 10, B is chemical bond between peptide and substituted amine, R1, and R2 are as defined in specification,
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
The invention relates to an improved process for the preparation of Levothyroxine sodium with reduced levels of impurities. The invention also provides Levothyroxine sodium pentahydrate free from 3,5-Diiodothyronine or d-enantiomer of thyroxine. The invention also provides Levothyroxine sodium pentahydrate having liothyronine below 0.5% wt / wt.
C07C 227/16 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
44.
A PROCESS FOR THE PREPARATION OF CARVEDILOL INVOLVING HALOHYDRIN DERIVATIVE
C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
A61P 9/00 - Drugs for disorders of the cardiovascular system
45.
PROCESS FOR THE PREPARATION OF CARVEDILOL VIA SILYL PROTECTION OF SUBSTITUTED AMINE
The invention provides new process for preparing Carvedilol by reaction of 4-(oxiran-2- yl-methoxy)-9H-carbazole and substituted silyl protected 2-(2-methoxy phenoxy)-ethylamine compound to give silyl protected Carvedilol intermediate. The silyl protected Carvedilol intermediate on desilylation gives Carvedilol. The invention also provides a novel substituted silyl protected 2-(2-methoxy phenoxy)-ethylamine as key intermediate for the preparation of Carvedilol.
C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
C07F 7/10 - Compounds having one or more C—Si linkages containing nitrogen
The present invention relates to a stable pharmaceutical composition comprising soft gelatin capsules containing at least one sparingly soluble active drug (singly or in combination with sparingly soluble and/or soluble drugs) and a solvent system, wherein the solvent system comprises of solvent, co-solvent, solubilizer(s), surfactant, aqueous solution of alkali and crystal growth inhibitor. The present invention further relates to process for preparing a stable pharmaceutical composition of sparingly soluble active drug(s) in soft gelatin capsules.
The present invention provides a novel process for the preparation of O-desmethyl venlafaxine from venlafaxine or its salt. Venlafaxine or its salt is O-demethylated to provide O- desmethylvenlafaxine in high yield and purity by reacting venlafaxine or its salt with trimethyl silyl halide and metal sulfide at elevated temperature, using high boiling ethereal solvent(s). O- desmethylvenlafaxine is isolated by aqueous quenching followed by pH adjustment and isolated at pH ~9.5 to 10. The process avoids formation of high molecular weight sulfur compounds. O- desmethyl venlafaxine is produced in high yield (> 85 %) and purity (> 99.0), wherein each impurity is < 0.1 %.
The present invention describes the method of modulating MAPK pathways. Further more the invention describes the use of Mycobacterium w for modulation of MAPK pathway intermediates for treatment of MAPK mediated conditions.
A Novel device for Intradermal injection referred in figure 1 - 10 comprising bottom surface 'A' and top surface 'S'. It includes Channel /tunnel (1) to guide needle syringe assembly in intradermal space, on surface 'B'. Stoppering mechanism (2) to control penetration of the tip of the needle into intradermal space is provided along channel/tunnel. Holding mechanism (3) with a means to hold the device over injection site is provided at side of device. It also provides a Distal part (4) to control protrusion of skin to facilitate introduction of the tip of needle in intradermal space. The device engages syringe needle assembly to penetrate the skin at a fixed angle so that it only enters intradermal space. The device also provide a method of limiting penetration of needle into intradermal space by controlling protrusion of skin.
A61M 5/46 - Devices for bringing media into the body in a subcutaneous, intra-vascular or intramuscular wayAccessories therefor, e.g. filling or cleaning devices, arm rests having means for controlling depth of insertion
The invention relates to novel p38 MAPK inhibitor which involves Mycobacterium w and/or its constituents in pharmaceutically acceptable carriers and their uses. Mycobacterium w and/or its constituents when administered to mammal results in p38 inhibition The inhibition is found to last more than 28 days. It is also found to induce inhibition of TNF-alfa. it suppresses cytokines in a pattern identical to Glucocorticoids. In transforms cells it also induces apoptosis. P38 mediated conditions include inflammation, cell differentiation, cell proliferation, cell inhibition, cell cycle regulation, anti-inflammatory reactions, immune modulation, vascularization, response to external stimuli and angiogenesis. The use of Mycobacterium w (Mw) and / or constituents of Mycobacterium w for inhibition of p38 protein kinase i.e. (i) to induce apoptosis in transformed cells (ii) for inhibition of TNF-alfa (iii) for inhibition of cytokines.
The present invention relates to an improved method for the preparation of Desloratadine with reduced levels of organic solvents. Further the invention also relates to a process for the preparation of Desloratadine containing reduced level of chloroform and hexane in Desloratadine to meet ICH specifications. The invention also relates to provide Desloratadine in mixture of polymorphic form 1 and form 2.
The present invention relates to solid oral dosage form for the treatment of non-insulin dependant type diabetes (diabetes of type II) using a combination of pharmaceutically acceptable salt of Metformin and Glibenclamide containing essentially surfactant and /or along with other excipients.
The novel stable pharmaceutical composition comprising non-steroidal anti inflammatory drug (NSAIDs), as injectables, which provides a clear and stable pharmaceutical composition without incorporation of any additives.
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
Mycobacterium w or its components are found to have poly TLR antagonistic activity to induced TLRs by varieties of TLR ligands. The induced TLR against which inhibitory effect is seen includes TLR 3, 4, 5, 6, 7, 8, 9. They also display antagonistic activities to effects of TLR ligands. They are also useful in management of diseases wherein TLRs are over expressed, like sepsis, multiple sclerosis, optic neuritis, Chronic obstructive pulmonary diseases multiple myeloma etc.
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
The invention relates to the HMG-CoA reductase inhibitor in particular to Atorvastatin Hemi-calcium. The present invention is directed to novel processes for preparing amorphous form of Atorvastatin hemi calcium and their intermediate in high purity.
C07D 207/00 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
56.
METHOD OF PREPARATION OF AMORPHOUS RABEPRAZOLE SODIUM
The invention relates to preparation of amorphous rabeprazole sodium from rabeprazole using sodium tertiary butoxide in tertiary butyl alcohol. The preparation further avoids the use of halogenated solvents, and freeze drying.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
C07D 403/02 - 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
57.
AN IMPROVED PROCESS FOR THE PREPARATION OF SUBSTANTIALLY PURE ARIPIPRAZOLE
The invention relates to an improved process for preparing substantially pure aripiprazole (HPLC >99.8 %), wherein 7,7'-[tetramethylenebis(oxy)]bis(3,4- dihydroquinolin-2(lH)-one) is present in pure aripiprazole in <0.01 % (w/w).
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
58.
A NOVEL AND IMPROVED PROCESS FRO THE PREPARATION OF NATEGLINIDE AND ITS POLYMORPH FORM-H
Nateglinide is prepared by an improved process comprising reaction of trans-4-isopropyl cyclohexane carbonyl chloride with N,O-bis- trimethylsilyl protected D-phenyl alanine to give after aqueous workup, crude nateglinide which is converted to Nateglinide form- H using a mixture of cyclohexane / ethyl acetate. trans-4-isopropyl cyclohexane carbonyl chloride is prepared from trans-4- isopropyl cyclohexane carboxylic acid using oxalyl chloride.
Rupatadine is synthesized by phase transfer catalysed N-alkylation of Desloratadine in biphasic solvent system using aqueous alkali by reaction of a compound of formula (A), X= leaving group as -OH -OTs, OMs -OAc -OAr -Br -Cl, -l with Desloratadine at temperature up to 50°C , wherein solvent selected is water immiscible organic solvent. Rupatadine is further converted to Rupatadine fumarate by reaction of Rupatadine in ketonic solvent with an alcoholic solution of fumaric acid.
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
