ABSTRACT
Present invention relates to novel heterocyclic compounds as indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) modulators. Compounds of the present invention inhibit tryptophan degradation by modulating IDO and/or TDO.
Formula (I)
The invention further relates to the process o...
The present invention provides a method for purification of 2-alkyl-6-oxo 1,6 dihydro-3,4'-bipyridine-5-carbonitrile derivatives (I) comprising separation of associated impurities at pH 9-10 by addition of an acid and further acidifying the filtrate to provide compound (I), having purity conforming to regulatory spe...
The present invention provides a convenient and industrially viable process for preparation of Zolmitriptan (I) having desired purity. The invention specifically relates to a method for isolating (S)-4-(4-hydrazinobenzyl)-l,3-oxazolidin-2-one hydrochloride (Ilia) of desired purity by separating (lie undesired inorga...
The invention discloses a novel method and apparatus for preparing a controlled release tablet disintegrable in the buccal cavity. The vehicle for the active ingredient is a saccharide matrix granulated in a fluidized bed processor. The matrix along with a suitable lubricant is compressed at low pressures in a die p...
An industrially viable method for the preparation of bicalutamide wherein oxidation of 4-Cyano-3-trifluoromethyl-N-(3-p-fluorophenylsulfanyl-2-hydroxy-2-methyl propionyl )aniline with m-chloroperbenzoic acid (mCPBA) in presence of lower volume of halogenated solvent, followed by addition of ketonic solvent the react...
The present invention relates to a novel synthetic route for the preparation of fingolimod and its pharmaceutically acceptable salts. The method comprises reaction of 2-(4-octylphenyl)-acetaldehyde with nitro acetonide, and subsequent conversions of the resulting acetonide protected nitro-alcohol intermediates of fo...
The present invention relates to a stable ready-to-use injectable pharmaceutical formulation of bortezomib or pharmaceutically acceptable salts thereof. Methods of preparing such formulations are also provided.
The present invention relates to pharmaceutical compositions of Teriflunomide or pharmaceutically acceptable salts thereof and method of preparation of such compositions. Typically, the composition according to present invention comprises about 1% w/w to about 30% w/w Teriflunomide, or a pharmaceutically acceptable ...
The present invention provides a process for preparation of prochlorperazine edisylate (1a) comprising reaction of sub-equimolar quantities of (3-chloropropyl)-4-methylpiperazine (3) and 2-chloro-phenothiazine (2) in presence of mild base followed by treatment with ethanedisulfonic acid to give prochlorperazine edis...
The present invention provides an improved process for the preparation of fosaprepitant dimeglumine (la) free from associated impurities and heavy metals like palladium. The synthetic strategy, which avoids isolation of any of the intermediates, comprises use of resin based metal scavengers and provides pure fosapre...
The present invention relates to pharmaceutical dosage forms comprising dexketoprofen and to
the process for preparation of these dexketoprofen compositions.
The present specification relates to a stable controlled release formulation of zileuton. The present specification is particularly related to a bilayer pharmaceutical composition of zileuton comprising an immediate release portion and a controlled release portion. Further, the present specification also relates to ...
The present invention related to a process for the preparation of dihydropyridine compounds. This invention makes use of chloromethyi ethers in the process of preparation of dihydropyridine compounds. It further used trifluoroacetic acid as specific hydrolyzing media for removal of t-butyl protecting group in the di...
The invention provides a novel process for preparation of neostigmine methylsulfate (I) comprising synthesis of 3-dimethylamino phenol by a process of quateraization of 3-amino phenol with dimethyl sulfate and demethylation with ethanolamine, followed by further reaction with N,N-dimethylcarbamoyl chloride in presen...
ABSTRACT
Present invention relates to novel heterocyclic compounds as indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) modulators. Compounds of the present invention inhibit tryptophan degradation by modulating IDO and/or TDO.
Formula (I)
The invention further relates to the process o...
The present invention provides a cost-effective and industrially viable process for preparation of Eprazinone dihydrochloride. The process involves a novel synthetic route comprising reaction of tertiary butyl piperazine-1-carboxylate (II) with 2-bromo-1-phenylethanone (IV), followed by reduction and subsequent alky...
The present invention provides an improved process for the preparation of prasugrel hydrochloride. More specifically, the invention provides an improved which provides prasugrel hydrochloride of the desired purity with associated impurity conforming to regulatory limits.
The invention relates to an improved 4+4 solution phase synthesis of octreotide acetate (1) comprising coupling of two suitably protected tetrapeptide fragments which on deprotection, oxidation, and treatment with acetic acid provides octreotide acetate (1) having desired purity.
The invention relates to an improved method for 4+4 solution phase synthesis of Lanreotide acetate (1) comprising coupling of two suitably protected tetrapeptide fragments which on deprotection, oxidation, followed by treatment with acetic acid provides Lanreotide acetate (1) having desired purity.
...
The present invention provides a novel and convenient method for preparation of Roflumilast (I). The process involves preparation of imidazol-l-yl-3-(cyclopropylmethoxy-4-(difluoromethoxy)phenylmethanone of formula (IV) in an organic solvent followed by reaction with 4-amino-3,5-dichloro pyridine in a second organic...
The present invention provides a process for preparation of 4-(2,4-difluorobenzoyl)-
piperidine (II), a key intermediate in the preparation of benzisoxazole piperidinyl compounds, with the desired purity and the associated impurities conforming to regulatory limits. The method comprises reacting tert-butyl-4-methox...
The present invention related to a process for the preparation of atosiban acetate using a novel non-linear liquid phase peptide synthesis scheme. This invention makes use of combing precursor peptides synthesised separately in high purity and yield over presently known processes. The disclosed process has several a...
The present invention relates to the preparation of a key Rilpivirine intermediate namely, (E)-4-(2-cyanoethenyl)-2,6-dimethylphenylamine hydrochloride (II) by a process comprising reaction of the tetrafluoroborate salt of the diazonium ion of 2,6-dimethyl-4-aniino-l-carboxybenzyI phenylamine (VI) with acrylonitrile...
The present invention is related to the process for preparation of cidofovir dihydrate comprising reaction of (S)-N1-[(2-hydroxy-3-triphenylmethoxy)propyl]cytosine (Compound II) with diethyl-p-tosyloxymethyl phosphonate using sodium hexamethyldisilazane to give key intermediate phosphonic acid [[(S)-2-(4-amino-2-oxo...
The present invention provides a simple convenient and scalable process for preparation of 2-carboxybenzaldehyde. The process involves reaction of phthalide with sulfuryl chloride in presence of a catalyst to yield the intermediate 3-chlorophthalide, which on aqueous hydrolysis yields 2-carboxybenzaldehyde with puri...
The present invention relates to pharmaceutical compositions of cinacalcet or pharmaceutically acceptable salts thereof and method of preparation of such compositions.
The invention provides a novel process for preparation of Diflunisal of formula (I) involving preparation of 2-bromo-4-(2,4-difluorophenyl)phenol of formula (III) in presence of bromine/acid and its subsequent conversion to 2-bromo-4-(2,4-difiuorophenyl) ethoxybenzene of formula (IV) and carboxylation of (IV) with c...
The present invention provides a stable solid pharmaceutical composition for oral administration of sphingosine-1 phosphate receptor agonist (typically fingolimod) comprising Fingolimod or pharmaceutically acceptable salts thereof and dibasic calcium phosphate. The invention also provides the process of preparation ...
A process for the preparation of 2,6-diisopropylphenoi comprising alkylation of 4-hydroxy benzoic acid with isopropanol in presence of an aqueous acid and isolating by quenching with a mixture of water and toluene at 10-20°C, followed by concentration of the organic layer, dissolving the residue in alcohol and addin...
The present invention provides a stable solid pharmaceutical composition for oral administration of antimuscarnic agents and processes for preparation thereof. Typically, the present invention relates to pharmaceutical compositions of Tolterodine, its pharmaceutically acceptable salt and processes for preparation th...
The present invention provides a novel process for preparation of Raloxifene hydrochloride (Ia) comprising reaction of 2-(4-hydroxyphenyl) benzo [b] thiophene of formula (II) with 4-[2-(l-piperidinyl)-ethoxy]-phenyl] benzoic acid (III) using Eaton's reagent. The resulting compound, 6-methanesulfonyloxy-2-(4-methanes...
The present invention provides an improved process for preparation of midodrine hydrochloride (la). The process comprises reaction of 2-amino-l(2,5-dimethoxyphenyl)-ethanone hydrochloride of formula (Va) with N-BOC-glycine and 1,1'carbonyldiimidazole (CDI) to give novel intermediate, tertiary-butyl-N-({[2-(2,5-dimet...
The present invention provides a pharmaceutical composition comprising Vitamin Kl and the process for preparation of the same. In particular, the present invention relates to stable injectable pharmaceutical compositions comprising a desired diastereomer of phytonadione in quantity not less than 75% of the total wei...
The present invention provides a process for preparation of trientine dihydrochloride (1) comprising reaction of protected triethylene tetramine with hydrochloric acid in an aqueous system to yield the dihydrochloride salt wherein the formation of inorganic impurities and undesired salts is controlled significantly....
The present invention provides a process for preparation of 2-cyano-N-(trifluoro methylphenyl)acetamide) (4) as an intermediate for teriflunomide using boric acid as catalyst and further reaction of (4) with acetic acid in presence of carbonyl diimidazole to obtain teriflunomide (1).
The present invention relates to process for the preparation of Flecainide acetate (I) comprising reaction of 2,5-bis (2,2,2-trifluoroethoxy)benzoic acid with 1,1"-carbonyldrimidazole (CD1) to give (2,5-diethoxy-phenyl)-imidazol-l-yl-methanone, which on coupling with 2-aminomethylpyridine in presence of a base gave ...
The present invention is related to the process for preparation of intermediate of Aprepitant, 2(R)-(1-(R) [3, 5-bis (trifluoromethyl) phenyl] ethoxy-3-(s)-phenyl -4-(2-(n-methylcarboxy-acetamidrazone) morpholine of formula (IV), which after cyclization gives Aprepitant (I) conforming to regulatory specification.
...
The present invention provides a novel process for preparation of Fenspiride hydrochloride (la) comprising preparation of 4-substituted-aminomethyl-1-(2-phenylethyI)-piperidin-4-ol of formula (V) and its further cyclization in presence of a base to give Fenspiride (I), which on subsequent treatment with hydrogen chl...
The invention provides a novel process for preparation of flurbiprofen (1) having desired purity by reaction of Grignard complex of 4-bromo-2-fluorobiphenyl (4) with sodium 2-bromopropionate (3) in presence of a transition metal salt.
The present invention relates to a stable injectable emulsion formulation of Propofol having uniform droplet size, which is obtained at a pH above 8.5 and by avoiding a rotary sterilizer.
A process for preparation of diethyl 2-acetamido-2-(4-octyI phenyl)ethyl malonate (III), a key intermediate of fingolimod hydrochloride comprising reaction of 2-(4-octylphenyl)ethyl iodide (IV) with diethyl acetamido malonate in presence of a base and an iodinating agent and in an organic solvent. The compound of fo...
The present invention relates to an improved process for the preparation of Promethazine hydrochloride. More particularly, the invention relates to a cost-effective process, which provides Promethazine hydrochloride having desired purity, free from its associated impurity
The present invention provides a novel process for the preparation of Darifenacin hydrobromide of desired purity. The process comprises condensation reaction of 3-(S)-(+)-(1-carbamoyl-l,l-diphenylmethyl)pyrrolidine of formula (IX) or its acid addition salt (IXa) with 5-bromoethyl-2)3-dihydrobenzofuran of formula (X)...
A process for the preparation of dronedarone hydrochloride by using a novel protection method in that primary amino moiety of 2-butyl-5-amino benzofuran is protected by a bis-protective group like phthalimido group following by Friedel-Craft acylation of the formed intermediate leading to the formation of dronedaron...
The present invention relates to a stable pharmaceutical composition comprising nicorandil and its pharmaceutically acceptable salts thereof. Particularly, the present invention relates to a prolonged-release pharmaceutical composition in solid form, suitable for oral administration, comprising nicorandil and its ph...
The present invention relates to pharmaceutical compositions comprising aliphatic amine polymer. The formulation, preferably a tablet, contains suitable excipients such as diluents along with the aliphatic amine polymer. The judicious selection of diluent in the pharmaceutical composition of the present invention, r...
The present invention provides a simple and efficient method for synthesis of 4-[bis (2-chloroethyl)-amino]-L-phenylalanine hydrochloride. The process involves the treatment of 4-[bis(2-chloroethyl)-amino]-L-phenylalanine free base with concentrated hydrochloric acid followed by concentration of the reaction mixture...
The present invention provides a convenient and cost-effective process for preparation of
4-carboxyl-5,8,11-tri(carboxymethyl)-l-phenyl-2-oxa-5,8,11-triazatridecan-13-oic acid (BOPTA), which is the key intermediate in the synthesis of Gadobenate dimeglumine. The process comprises reaction of tertiary-butylcarboxyme...
ABSTRACT
The present invention relates to the preparation of stable pyridone disulphide
derivatives and its stereoisomers having general formula (I), which are useful in the treatment of gastrointestinal disorders.
Pyridone disulphide derivatives (I)
wherein,
R], R2 and R3 are independently alkyl, alkoxy, ha...
The present invention provides a novel, simple and convenient method for preparation of Acamprosate calcium. The process involves preparation of 3-aminopropanol mesylate and its reaction with sodium sulfite to yield the key intermediate 3-aminopropane 1-sulfonic acid, which is converted to Acamprosate calcium by tre...
The invention relates to a process for the preparation of formulations of oxaliplatin with improved stability and impurity profile. The invention makes use of carbon dioxide as an acidity and stability agent in the formulations of oxaliplatin. The formulations with improved stability and impurity profile, especially...
This invention discloses a process for manufacture of galanthamine, which involves a stereo-selective reduction step to get the desired isomer of galanthamine. The current embodiment also discusses the method for improving the chiral and chemical purity of galanthamine and galanthamine salts.
A process for the preparation of chirally pure(S)-amlodipine salts,which comprises the steps of (i)adding firstly 0.25 to 0.3 molar equivalent of L-(+)-tartaric acid into the solution of (RS)-amlodipine in an aprotic solvent (ii)filtering the solution obtained of (R)-amlodipine-L-(+)-hemi-tartarate-aprotic solvent-s...
A simple, cost-effective process for improving the yield of Levetiracetam by recycling of the undesired enantiomer of levetiracetam of formula (I) by recycling the mixture of the undesired isomer of levetiracetam of formula (I-B), containing small quantities of the desired (S)- isomer of formula (I). The invention i...
The present invention relates to a palatable pharmaceutical composition of Efavirenz, which is substantially free of hot “jalapeno” test and the process for preparation of said pharmaceutical composition. The Efavirenz composition of the present invention comprise of fumaric acid, citric acid or the mixture thereof,...
The present invention relates to a novel process for preparing 4-[(4-piperidinomethyl) pyridin-2-yl)oxy-] 2-butenamine of formula (III), in high yield and free from associated impurities, comprising reaction of N-{4-[4-(piperidinomethyl) pyridyl-2-oxy]-cis-2-butene} phthalimide of formula (||) with a combination of ...
An improved method for preparation of S-(+)-3-(aminomethyl)-5-methyl hexanoic acid (I) of high purity by treating (S)-mandelic acid salt of S-(+)-3-(aminomethyl)-5-methyl hexanoic acid with a base in an organic solvent.
A pharmaceutical composition comprising a core of decongestant and a piperidinoalkanol mantle coating is provided. Various intermediate coating can be present between the decongestant core and piperidinoalkanol mantle coating. The pharmaceutical composition can provide a controlled release of decongestant for 48 hrs...
The present invention provides an improved and industrially feasible earth metal salts or its hydroxides are reacted with ferrous sulfate to get corresponding ferrous salts, which are reacted with ascorbic acid in an aqueous medium at slightly acidic or neutral condition followed by filtration to get ferrous ascorba...
A process for preparation of optically pure(S)-amlodipine-L-hemitartrate DMF solvate comprising the steps of treating (R,S)amlodipine base with L-tartaric acid in the presence of dimethyl formamide and a co-solvent.
A process for the preparation of rivastigmine of formula (I) comprising a) reacting (S)-3-(1-dimethylaminoethyl) phenol of formula (V-a) with carbonyl diimidazole and performing a step selected from reacting the product of step-a with ethyl methyl amine in an organic solvent to obtain compound (I); or reacting racem...
The present invention relates to an improved and industrial feasible process for the manufacture of copolymer, chemically known as poly(allylamine-co-N,N’-dially1-1,3-diamino-2-hydroxypropane) hydrochloride.
The present invention provides a simple and cost effective method for synthesis of pregabalin. The undesired S-isomer of 3-(carbamoylmethyl)-5-methylhexanoic acid, produced during resolution step in synthesis of pregabalin is racemized to obtain a racemic 3-(carbamoylmethyl)-5-methylhexanoic acid. The said racemic m...
This invention relates to the resolution of anti-inflammatory compounds like 2-substituted alkanoic acid (1a)such as Ibuprofen, Etodolac, flurbiprofen, naproxen, ketoprofen by making use of a chiral amino butanol like (L)-substituted benzyl-2-amino butanol. The process provides single enantiomers of 2-substituted-al...
The present invention provides a simple and cost effective method for synthesis of diarylpyrimidine non-nucleoside reverse transcriptase inhibitor such as etravirine. Typically, etravirine is synthesized by using 2,4,6-trichloropyrimidine and 3,5-dimethyl-4-hydroxybenzonitrile. Further, there are disclosed simple pr...
The present invention provides the procedure for the preparation of optically active albuterol, wherein the reducing agent used is Vitride. Thus use of Vitride as a reducing agent makes the process less hazardous, cost effective, safe, easy and industrial friendly
The present invention relates to an improved cost effective method for preparing amphetamine derivatives, of high purity and in quantitative yield by dehydroxylation of N-tertiary butyloxycarbonyl protected phenylpropanolamines.
The present invention relates to a pharmaceutical composition for oral administration comprising: a first component of ACE inhibitor, with at least one excipients, in the form of blend or pellets; and a second component of a diuretic in the form of tablet, wherein the ACE inhibitor ids present along with lactose, wh...
The invention is directed to preparation of optically active isomer of 6-(5-chloro-2-pyridinyl)-6, 7-dihydro-7-oxo-5H-pyrrolo-[3, 4-b]-pyrazine-5-yl-4-methyl piperazine-1-carboxylate. The current embodiment describes a process which is industrially feasible, cost effective and reduces the time cycle.
...
A unit dosage pharmaceutical preparation is disclosed. Said preparation comprises (a) functional coated composition of galanthamine or its salts; and (b) uncoated/seal coated composition of galanthemine or its salts.
The present invention relates to a process for preparation of isomerically pure trans-4-amino- I -cyclohexanecarboxylic acid derivatives, by epimerization of cis isomer and / or mixture of cis and trans isomer of 4-amino-l-cyclohexanecarboxylic acid derivatives.
The present invention relates to an improved and economical process for the manufacture of copolymer chemically known as poly (allylamine-co-N,N’-diallyl-1,3-diamino-2-hydroxypropane) hydrochloride.
The present invention provides a simple and cost effective method for synthesis of dexmethylphenidate. The undesired l-threo-2-phenyl-2-piperidyl-2-acetamide (II) obtained during the synthesis of dexmethylphenidate is racemized to give a racemic mixture of dl-erythro-threo-2-phenyl-2-piperidyl-2-acetamide (IV) which...
The present invention relates to a pharmaceutically useful composition comprising at least one protease inhibitor and to a process for the preparation of such pharmaceutical compositions, wherein the said pharmaceutical composition is prepared by granulation process.
The invention discloses an improved process for preparation of a chiral propargylic alcohol by asymmetric alkynylation of ketones with a cyclopropyl metal acetylide in the presence of chiral ligands, auxiliaries and base. These chiral alcohols are intermediates for the preparation of a potent HIV reverse transcripta...
The present invention relates to a stable pharmaceutical composition containing amlodipine and S-atenolol, methods of using the composition for treatment of cardiovascular disease such as myocardial infarction and hypertension.
A pharmaceutical composition of metronidazole, comprising a first granular portion which consists of i) about 40 wt% to about 75 wt% of metronidazole ii) a water-insoluble polymer and iii) a hydrophilic polymer; and a second granular portion which comprises about 0 wt% to about 35 wt% of metronidazole; wherein the w...
The present invention provides a novel, simple and cost effective method for synthesis of Donepezil hydrochloride intermediate, l-benzyl-4-(5,6-dimethoxy~l-indanon)-2-ylidenyl methyl piperidine of formula (II) comprising reaction of 5,6-dimethoxy-l-indanone (EH) with l-benzyl-piperidine-4-carboxaldehyde (IV) in an o...
The invention is to provide a simple, cost-effective process for deprotection of phosphonate esters of high purity without the formation of undesired impurities.
The object of the invention is to provide a process for preparation of tenofovir in high yield and purity using an inorganic acid and to utilize reagents ...
The present invention relates to an improved process for the preparation of a cross-linked polyallylamine polymer in a globular form, comprising treatment of polyallylamine hydrochloride with an aqueous solution of an alkali metal hydroxide followed by reaction with a cross-linking agent in presence of a surface ten...
The invention is directed to preparation of non steroidal anti-inflammatory drug 2-[(2,6-dichlorophenyl)amino]phenylacetoxyacetic acid. The current embodiment describes a process, which is industrially feasible, reduces the time cycle and provides high yields.
The present invention provides an improved and economical method for the preparation of 3’-azido-3’ –deoxy-5’ –trityl thymidine of formula (I-A).
The present invention further provides a simple and industrially useful method for the preparation of 3’ –azido-3’ –deoxy-5’ – trityl thymidine of formula (I-A), in a sin...
The present invention relates to a pharmaceutical composition of Efavirenz, which is substantially free of hot “jalapeno” test and the process for process for preparation of said pharmaceutical composition. The Efavirenz composition of the present invention comprises of Natural phospholipids or the mixture thereof, ...
This relates to an improved cost-effective environmental friendly, industrial method for manufacture of Nevirapine. An aspect of the invention relates to a cost-effective method for the preparation of 3-amino-2-chloro-4-methyl pyridine of formula (III), and an alternate method for preparation which comprises reducti...
The present invention is directed towards the presentation of preparation of extended release Alprazolam formulation. The formulation thus obtained provides an efficient mode of delivery of Alprazolam in a continuous manner.
Present invention relates to a novel, improved and cost-effective process for the preparation of Tolmetin (I), comprising reaction of 1-methyl-2-pyrroleacetate (II) with 4-methylbenzoyl chloride (III) in an organic solvent to provide a compound of formula (IV) which on treatment with morpholine followed by a base in...
The present invention relates to a process for the oxidation of the sulphide by making use of an oxaziridine. The invention relates to the oxidation process, which provides the chiral sulphide with less sulfone impurity. Invention further discloses a simple, safe, eco-friendly and cost effective process for the oxid...
A simple, cost-effective process for preparation of efavirenz of formula (1) comprising reacting a solution of 5-chloro-a-(cyclopropylethynyl)-2-amino-a-trifluoromethyl) benzene methanol of formula (1I) in an organic solvent with triphosgene in the presence of an inorganic base at a temperature range -5°C to 25°C, a...
A process for the preparation of dronedarone hydrochloride by using specific ratio of the non-specific P205-methanesulfonic acid reagent for acyiation reaction is disclosed. Dronedarone hydrochloride of formula (3) is prepared by acylating of 2n-butyl-5-sulfonamide benzofuran derivative of formula (1) with benzoic a...
A process for the preparation of febuxostat is disclosed using specific content of phosphorus pentoxide in methanesulfonic acid (Eaton"s reagent). 2-(3-formyl-4-hydroxyphenyl)-4-methyl-5-thiazolecarboxylic acid ethyl ester of formula (3), is a key intermediate for the process of the present invention. An object of t...
The present invention relates to an improved, safe, commercially viable, quick and cost effective process for the preparation of 4,l',6'-trichloro-4,l',6'-trideoxygalactosucrose. The invention is directed towards the convenient synthesis of chlorinated sucrose from 6-acetyl sucrose.
A single tablet dosage form of a synergistic fixed dose composition of stavudine and lamivudine in combination containing 30/40 mg & Lamivudine 150 mg.
The present invention provides a pharmaceutical composition for oral administration comprising p-phenethylamine derivative such as sibutramine, which are useful for treating obesity. An enantiomer of sibutramine, in free base form, is used to prepare the pharmaceutical compositions along with the pharmaceuticaUy acc...
A process for manufacturing an ambroxol core doxycycline shell film coated tablet is disclosed, The granules of the active ambroxol ingredient along with fillers and programmed release agents are first compressed in the core at higher pressures, The tablet so formed is film coated. The tablet has proved effective in...
The present invention related to a process for the preparation of aprepitant, fosaprepitant and similar compounds. This invention makes use of buffering agents as catalysts for the preparation of aprepitant, fosaprepitant, and similar molecules of higher purity and yield over presently known processes.
...
The present invention related to a process for the preparation of atosiban acetate using a novel non-linear liquid phase peptide synthesis scheme. This invention makes use of combing precursor peptides synthesised separately in high purity and yield over presently known processes. The disclosed process has several a...
The present invention provides a novel process for preparation of Fenspiride. The process comprises reaction of N-(2-phenyiethyl)-2-oxo-6-azaspiro[2.5]octane with alkali cyanate such as potassium cyanate to give Fenspiride (I), which on subsequent treatment with hydrogen chloride in presence of methyl isobutyl keton...
The present invention related to a process for the preparation of eptifibatide using a novel non-linear liquid phase peptide synthesis scheme. This invention makes use of combing precursor peptides synthesised separately in high purity and yield over presently known processes. The disclosed process has several advan...
The present invention provides a novel and cost-effective process for preparation of Morniflumate. The process comprises reaction of 2-[[3-(trifluoromethyl)phenyl]amino]-3-pyridinecarboxylic acid with 4-(2-hydroxyethylmorpholine) in presence of l-Ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDAC) hydrochloride and 1...
An effective process for the preparation of crystalline olanzapine form II by using an organic solvent selected from nitro alkane, chlorinated hydrocarbons and alkyl carbonates or mixture thereof, in presence of a base, heating the mixture, optionally adding a second organic solvent and cooling to obtain crystalline...
An industrially viable method for the preparation of fludarabine phosphate; wherein debenzylation of 9-(2,3,5-tri-0-berizyl-|3-D-arabinofuranosyl)-2-fluoroadenine intermediate with palladium-charcoal in presence of transfer hydrogenating agent in an organic solvent and further purification of fuldarabine free base i...
The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).
A process for isolation of cross-linked polymers containing N or amino, ammonium or spirobicyclic ammonium groups, cationic N-containing groups and suitable counter-ions, by filtration of a slurry containing the polymer into a closed vessel equipped with a sintered bottom and a stirrer, which can be raised or lowere...
A method for the preparation of tolvaptan comprising , N-acylation of 7-chloro-5-oxo-2,3,4,5-tetrahydro-lH-l-benzazepine with 2-methyl-4-nitrobenzoyl chloride in an organic solvent and in absence of base; followed by reduction of the nitro group with suitable reducing agent to give 7-chloro-l-(4-amino-2-methylbenzoy...
A process for preparation of bendamustine hydrochloride comprising, chlorination of compound of formula (II) with chlorinating agent in absence of an organic solvent followed by concentration of the reaction mixture, adjusting to neutral pH and isolating bendamustine hydrochloride free from N-alkylated impurities af...
The present invention provides a convenient and cost-effective process for preparation of Treosulfan. The process comprises reduction of dimethyl 2,3-O-isopropylidene-L-tartrate with sodium-bis(2-methoxyethoxy)aluminum hydride to give the alcohol 2,3-O-isopropylidene-L-threitol (III), which on reaction with methanes...
The present invention relates to a novel pharmaceutical composition of amlodipine, or its pharmaceutically acceptable salt and benazepril, or its pharmaceutically acceptable salt and to a process for the preparation thereof.
A process for preparation of trimethobenzamide hydrochloride comprising, coupling of 3,4,5-timethoxy benzoic acid with N,N-carbonyldiimidazole (CDI) in presence of inorganic base in an organic solvent and treatment of N-(3,4,5-trimethoxybenzoyl)imidazole with 4-(dimethylamino ethoxy)-benzylamine in a base and treatm...
This invention relates to a process for the preparation of Sucralose comprising the steps of tritylating Sucrose, acylating tritylated Sucrose, detritylating, isomerizing, chlorinating and deacylating to give Sucralose, the improvement which comprises detritylating TRISPA using the reagents selected from the group ...
The present invention provides the process for the preparation of sodium ferric gluconate complex in sucrose. The iron (III) salt is reacted with water-soluble amine in water followed by filtration to get ferric oxyhydroxide. The isolated ferric oxyhydroxide is suspended in water and reacted with gluconic acid / glu...
The present invention relates to process for the preparation of copolymer, chemically known as poly(allylamine-co-N,N"-diallyl-1,3-diamino-2-hydroxypropane) carbonate (Sevelamer carbonate), wherein sevelamer base is suspended in solvent then treated with carbon dioxide followed by filtration to get sevelamer carbona...
The present invention provides a convenient and cost-effective process for preparation of chiral intermediates through asymmetric reduction of ketones. The process comprises reaction of achiral ketone with the reagent prepared from sodium borohydride, N,N diethylaniline hydrochloride, and optically active α, α-diphe...
The present invention provides a process for preparation of vitamin Kl comprising reaction of 1- acetoxy-4-hydroxy-2-methylnaphthalene (compound II) with 3,7,11,15 tetramethyl hexadecane-2-en-l-ol (Phytol, compound III) in presence of boron trifluoride-acetic acid complex to give 1- acetoxy-4-hydroxy 2-methyl, 3-[(2...
The present invention provides a simple method for preparation of benzphetamine and its acid addition salt comprising reaction of methamphetamine hydrochloride of formula (TTT) with benzyl chloride and treating the isolated benzphetamine of formula (II) with an acid dissolved in an organic solvent to provide benzphe...
The present invention relates to a stable liquid formulation of cabazitaxel. The formulation comprises cabazitaxel, and at least one solubilizer. Typically, formulations are in the form of ready-to-use solutions or concentrates.
The present invention relates to a novel process for the preparation of aryloxy aryl propanamines (I) of desired purity. The process comprises reaction of aryl propanolamines of formula (II) with aryl fluorides of formula (III) in presence of sodium sulfide as a base and dimethyl sulfoxide as solvent to give aryloxy...
The present invention provides a pharmaceutical composition for oral administration comprising dihydropyridine calcium channel blocker, such as nisoldipine and one or more release controlling polymer, which is selected from various hydrophilic polymers or combinations thereof. The said polymer is present at a concen...
The present invention comprises preparation of Fenspiride hydrochloride (Ia) starting from N-(2-phenylethyl)-2-oxo-6-azaspiro[2.5]octane (III) by a novel method. The compound of formula (III) is converted to 4-(aminomethyl)-1-(2-phenyIethyl)piperidin-4-ol of formula (VI) either by treatment with sodium azide/ammoniu...
The present invention provides a process for preparation of {(2E,4E,6E,8E)-9-(4-methoxy-2,3,6-trimethyl)phenyl-3,7-dimethyl-nona-2,4,6,8}tetraenoate, an acitretin intermediate of formula (VI) with trans isomer >97%, comprising of reacting 3-formyl-crotonic acid butyl ester of formula (V), substantially free of impur...
The present invention relates to an improved solid formulation of (2S,3S)-2,3-Dihydroxy-4-methylsulfonyloxybutyl] methanesulfonate. The improved formulations are lyophilized pharmaceutical solid composition containing treosulfan for reconstitution with water to provide a solution for parenteral administration. The p...
The invention relates to improved method of synthesis for Treprostinil comprising condensation reaction of the carbonyl compound having allyl, alkyl, crotyl or MEM-protected phenolic hydroxyl group, compound (4) with a hydroxyl-protected alkynol (5) to give the condensation product, compound (6). Subjecting compound...
The present invention provides a process for preparation of isoproterenol hydrochloride (1a) comprising catalytic hydrogenation of 3",4"-dihydroxy-2-(isopropylamino)-acetophenone hydrochloride (5a) in presence of an ion exchange resin, to provide isoproterenol hydrochloride (1a).
The invention relates to an efficient method for conversion of substrates (II) possessing a steroid skeleton in to a key carbonyl-protected acetal or ketal intermediate (I), during the synthesis of compounds of general formula (III). In cases when the substrates (II) possess chiral structures, the acetalization or ...
A process for preparation of alfuzosin hydrochloride comprising, coupling of Nl-(4-
amino-6,7-dimethoxyquinazol-2-yl)-N 1 -methylpropylenediamine (II) with
tetrahydrofuronic acid in an organic solvent, further, organic layer was treated with aqueous solution of organic acid and followed by concentration of the rea...
The present invention relates to a pre-mixed, ready-to-use, injectable formulation of Carmustine that is stable enough for clinical use, and yet provides a suitable carmustine concentration for immediate use, without dilution, by parenteral administration.
The present invention provides a process for preparation of Isoproterenol hydrochloride (1a) wherein the ketone intermediate (5a) is hydrogenated using Pd/C in presence of a weakly basic anion exchange resin, to minimize associated impurities and provides the final compound (1a) having desired purity in good yield.
...
The present invention relates to pharmaceutical compositions of Apixaban or pharmaceutically acceptable salts thereof and pharmaceutically acceptable excipients and process for its preparation. The compositions were prepared by conventional methods using pharmaceutically acceptable excipients. The impact of particle...
The present invention relates to pharmaceutical compositions of apremilast or pharmaceutically acceptable salts thereof. Methods of preparing such compositions are also provided.
The invention relates to an improved method for a 5+3+2 solution phase syntheses of Icatibant acetate (1) comprising coupling of suitably protected peptide fragments which on deprotection followed by treatment with acetic acid provide Icatibant acetate (1) having desired purity.
The present invention relates to a pharmaceutical lipid composition comprising nitrosoureas and process for its preparation. In particular, the compositions of present invention are useful in the treatment of brain cancers having improved physicochemical and pharmacokinetic characteristics.
The present invention relates to stable paclitaxel and albumin nanosuspension suitable for intravenous administration and method of preparation thereof.
The present invention provides a novel process for preparation of pyridoisoquinolines such as tetrabenazine comprising synthesis of appropriately substituted isoquinoline intermediates, followed by intramolecular cyclization in presence of base to provide pyridoisoquinoline derivatives, which are further converted t...
The present invention provides a convenient and economical process for preparation of tetrabenazine (1) having desired purity, comprising reaction of 3-(dimethylamino)methyl-5-methylhexan-2-one acid addition salt of formula (4) with 6,7-dimethoxy-3,4-dihydroisoquinoline hydrochloride (7) in presence of an organic ac...
“Process for preparation of Lanreotide acetate“
The invention relates to an improved method for the solution phase synthesis of Lanreotide acetate (1) comprising coupling of two suitably protected tetrapeptide fragments wherein the threonine hydroxyl is protected, to give an octapeptide, which on deprotection, oxi...
The present invention provides a liquid pharmaceutical formulation containing carmustine at a high concentration. Typically, the formulation disclosed according to present invention contains from about 20 mg/ml to about 500 mg /ml of carmustine dissolved in a solvent system comprising polyethylene glycol and a solub...
"PROCESS FOR PREPARATION OF VIGABATRIN"
The invention relates to an improved method for the synthesis of vigabatrin starting from amino acids such as methionine or aspartic acid, comprising its reaction with Meldrum’s acid and subsequent conversions to afford 5-vinyl-2-pyrrolidone (8), which, when subjected to hydr...
The present specification relates to use of inert product transfer tubing in the manufacturing of pharmaceutical injectable products. Silicon content in finished drug product was drastically reduced when silicon based product transfer tubing was replaced with fluoropolymer based inert product transfer tubing.
...
The present invention provides a process for fenspiride hydrochloride (1a) having desired purity, comprising treatment of the epoxide 6-(2-phenylethyl)-1-oxa-6-azaspiro[2.5] octane (3) with aqueous ammonia, reaction of resultant 4-(amino methyl)-1-(2-phenylethyl) piperidin-4-ol (4) with di-tertiarybutyl dicarbonate ...
The present invention relates to a composition comprising nitrosourea and pharmaceutically acceptable excipients. In particular, the present invention relates to novel drug delivery systems of carmustine such as nano-suspension and micro-emulsion and its use for the treatment of cancer by intravenous administration....
The present invention relates to a ready-to-use solution of carmustine that does not require dissolution or dilution of the carmustine prior to addition to saline and dextrose parenteral solutions. In particular, the invention relates to a stable liquid pharmaceutical composition containing carmustine in the form of...
The present invention relates to an improved kit for preparing injectable carmustine solutions, methods of preparing and administering such solutions, and methods of treatment with such solutions. The kit includes a product vial containing lyophilised carmustine and a diluent vial containing an ethanol-free non-aqu...
“PROCESS FOR PREPARATION OF 4-FLUORO-2-METHYL BENZONITRILE”
The invention relates to a robust and commercially viable method for the synthesis of 4-Fluoro 2-methyl benzonitrile (1), comprising use of N-Methyl 2-pyrrolidone as a solvent for the reaction of 2-Bromo-5-fluoro toluene with copper cyanide. The process...
1. A process for the preparation of atenolol, comprising the steps of:a) coupling of chloromethyl benzene (XX) with isopropyl amine to give N-benzyl-N-isopropyl amine, b) reacting N-benzyl-N-isopropylamine (XXII) with epichlorohydrin (III-A), c) converting the ...
The invention relates to an improved method for 4+4 solution phase synthesis of Lanreotide acetate (1) comprising coupling of two suitably protected tetrapeptide fragments which on deprotection, oxidation, followed by treatment with acetic acid to provide Lanreotide acetate (1) having desired purity.
...
"PROCESS FOR PREPARATION OF ERIBULIN MESYLATE"
ABSTRACT
The invention relates to a method for preparation of Eribulin mesylate comprising base mediated reduction of the azide intermediate, EBM-N-2, with a trialkyl or triaryl phosphine compound to obtain the amine, Eribulin, followed by treatment with methane sul...
The present invention relates to a ready-to-use solution of carmustine that does not require dissolution or dilution of the carmustine prior to addition to saline and dextrose parenteral solutions. In particular, the invention relates to a stable liquid pharmaceutical composition containing carmustine in the form of...
The present invention relates to a method for rapid infusion of carmustine, for example, in 30 minutes or 1 hour. The present invention relates to an administrable composition of carmustine comprising (i) from about 2.8 to about 3.2 mg/mL carmustine, propylene glycol and an aqueous 0.9% sodium chloride solution or a...
“PROCESS FOR PREPARATION OF EICOSAPENTAENOIC ACID”
The invention relates to a process for the preparation of the Z-isomer of Eicosapentaenoic acid (1) having desired impurity profile and purity by a novel route and by avoiding hazardous reagents and rigorous reaction conditions.
“PROCESS FOR PREPARATION OF A TRELAGLIPTIN INTERMEDIATE”
The invention relates to an improved method for the synthesis of a key intermediate, 2-[(6-chloro-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]-4-fluoro benzonitrile (1), with desired impurity profile, comprising use of a phase transfer catalyst...
" IRON POLYSACCHARIDE COMPLEX "
ABSTRACT
The invention relates to an iron polysaccharide complex of modified icodextrin comprising a modified icodextrin in association with iron salt and having weight average molecular weight between 100 - 250 kilodaltons. A further aspect provides a process for preparing the sa...
ABSTRACT
The invention relates to a continuous flow process for the photochemical synthesis of key intermediates of dydrogesterone, namely, 9ß,10a-pregna-5-7-diene derivatives (I-3). The process comprises photochemical conversion of the corresponding 9a,10ß-pregna-5-7-diene derivatives (I-1) and / or the seco-stero...
DEUTERATED S (-) METOPROLOL SUCCINATE COMPOUNDS, AND A PROCESS FOR ITS PREPARATION
The invention relates to a deuterated S (-) Metoprolol succinate compounds of formulae 1, 2 and 3 and processes for their preparation.
[Class : 5] Pharmaceutical And Medicinal Preparations; Ayurvedic Preparations; Dietary Food Supplements For Medical Use; Dietetic Food Supplements Adapted For Medical Purposes; Health Food Supplements For Persons With Special Dietary Requirements; Medicated Food Supplements.
[Class : 5] Ayurvedic Preparations For Human Beings, Nutraceuticals Preparations For Human Beings, Gummies, Dietary Supplements, Sanitary Preparations For Personal Hygiene, Medicated Cream
[Class : 30] Protein Bars, Food Supplements And Dietary Food Supplements And Other Food Products For Human Consumption In Various Forms, Cereals Prepared For Human Consumption, For Example, Oat Flakes, Corn Chips, Husked Barley, Bulgur, Muesli, Honey
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Citi Bank N.a.
0
01 October 2008
The Bank Of Maharashtra Limited
0
10 October 2017
Hdfc Bank Limited
0
27 September 2016
Axis Bank Limited
0
30 June 2016
Others
0
26 May 2016
Hdfc Bank Limited
0
Documents
Form MGT-7-04042021_signed
Form MGT-14-05102020_signed
Optional Attachment-(1)-30122020
Copy of MGT-8-30122020
List of share holders, debenture holders;-30122020
Form CHG-4-19122020_signed
Letter of the charge holder stating that the amount has been satisfied-18122020
Instrument(s) of creation or modification of charge;-15122020
Form CHG-1-15122020_signed
Optional Attachment-(1)-15122020
CERTIFICATE OF REGISTRATION OF CHARGE-20201215
Form MGT-14-09122020_signed
Optional Attachment-(1)-09122020
Instrument(s) of creation or modification of charge;-09122020
Form CHG-1-09122020_signed
CERTIFICATE OF REGISTRATION OF CHARGE-20201209
Optional Attachment-(1)-08122020
Form DIR-12-08122020_signed
Optional Attachment-(2)-26112020
Form CHG-1-26112020_signed
Instrument(s) of creation or modification of charge;-26112020
Optional Attachment-(1)-26112020
CERTIFICATE OF REGISTRATION FOR MODIFICATION OF CHARGE-20201126
Instrument(s) of creation or modification of charge;-25112020
Form CHG-1-25112020_signed
CERTIFICATE OF REGISTRATION OF CHARGE-20201125
Instrument(s) of creation or modification of charge;-23102020