Abstract: 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. Also provided are methods for preparation of such novel drug delivery systems.

Abstract: 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).

Abstract: 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.

Abstract: 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 (6) to oxidation, reduction, hydroxyl protection and carbonylation, cyclization reactions gave the tricyclic derivative (10). Further reactions comprising reduction, hydrogenation and deprotection of the phenolic and side-chain hydroxyl groups, wherein the sequence and choice of reagents was governed by protecting groups, gave the triol intermediate, compound (14). Cyanoalkylation at phenolic hydroxyl functionality and further hydrolysis yielded the prostacyclin compound, Treprostinil (1) and its pharmaceutically acceptable salts, having desired purity.

Abstract: 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.

Abstract: 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.

Abstract: The present invention relates to bulk sterilized parenteral suspension formulations comprising water insoluble drugs suitable for parenteral use. Further, a process of preparation of such bulk sterilized suspension compositions employing conventional sterilization process under homogenization is also disclosed. The sterilization under homogenization is carried for prolonged period and the finally aseptically filled into suitable container closure systems. The bulk sterilized suspensions prepared by using the current invention exhibited good physical and chemical stability.

Abstract: 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.

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. The invention further relates to the process of their preparation, pharmaceutical composition and their use in modulating the activity of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO). The compounds of the invention can be used alone or in combination for the treatment of conditions that benefits from the inhibition of tryptophan degradation.

Abstract: 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 (6) to oxidation, reduction, hydroxyl protection and carbonylation, cyclization reactions gave the tricyclic derivative (10). Further reactions comprising reduction, hydrogenation and deprotection of the phenolic and side-chain hydroxyl groups, wherein the sequence and choice of reagents was governed by protecting groups, gave the triol intermediate, compound (14). Cyanoalkylation at phenolic hydroxyl functionality and further hydrolysis yielded the prostacyclin compound, Treprostinil (1) and its pharmaceutically acceptable salts, having desired purity.

Abstract: 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 impurities, with 5-(4-methoxy-2,3,6-trimethylphenyl)-3-methyl-penta-2,4-diene-1-triphenyl phosphonium bromide of formula (IV) and isolating resultant compound of formula (VI), treating the filtrate with iodine for isomerization of the undesired cis intermediate and finally obtaining acitretin (I), with desired trans isomer ?97%.

Abstract: A process for preparation of diethyl 2-aetamido-2-(4-octyl 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 formula (III) thus obtained provided fingolimod hydrochloride (Ia) having associated impurities below the regulatory limits.

Abstract: The present invention relates to the preparation of stable pyridone disulphide derivatives having general formula (I) and its stereoisomers, which are useful in the treatment of gastrointestinal disorders. Pyridone disulphide derivatives (I) wherein, R1, R2 and R3 are independently alkyl, alkoxy, halogen, halogenated alkoxy, halogenated alkyl, hydrogen and could be the same or different and X is CH or N. R1 is methyl, methoxy, fluorine, trifluoromethyl, difluoromethoxy and hydrogen, R2 is methyl, methoxy and hydrogen, and R3 is methyl and hydrogen.

Abstract: Controlled release oral dosage formulations containing calcium channel blocker and processes for preparation thereof, are provided for once a day treatment. The active agent is preferably a dihydropyridine calcium channel blocker, such as nisoldipine. In one embodiment, the formulation provides controlled release of micronized nisoldipine with one or more pH independent release controlling polymers. The controlled release matrix formulation is advantageous and can be prepared by a simple, economically viable process as compared to complex core-coat prior-art versions.

Abstract: 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).

Abstract: The present invention relates to the preparation of stable pyridone disulphide derivatives having general formula (I) and its stereoisomers, which are useful in the treatment of gastrointestinal disorders. Pyridone disulphide derivatives (I) wherein, R1, R2 and R3 are independently alkyl, alkoxy, halogen, halogenated alkoxy, halogenated alkyl, hydrogen and could be the same or different and X is CH or N. R1 is methyl, methoxy, fluorine, trifluoromethyl, difluoromethoxy and hydrogen, R2 is methyl, methoxy and hydrogen, and R3 is methyl and hydrogen.

Abstract: 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).

Abstract: 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)-1,3-oxazolidin-2-one hydrochloride (IIIa) of desired purity by separating the undesired inorganic side products such as stannous hydroxide by manipulation of pH at different stages and finally treating with N,N-dimethylamino butyraldehyde diethyl acetal in an acidic medium to provide Zolmitriptan (I) conforming to regulatory specifications.

Abstract: Disclosed is process for 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-amino-1-carboxybenzyl phenylamine (VI) with acrylonitrile in presence of palladium acetate, followed by treatment with an acid and its subsequent conversion to the hydrochloride salt (II), wherein the undesired Z isomer is less than 0.5% and provides Rilpivirine hydrochloride having Z isomer less than 0.1%.

Abstract: Controlled release oral dosage formulations containing calcium channel blocker and processes for preparation thereof, are provided for once a day treatment. The active agent is preferably a dihydropyridine calcium channel blocker, such as nisoldipine. In one embodiment, the formulation provides controlled release of micronized nisoldipine with one or more pH independent release controlling polymers. The controlled release matrix formulation is advantageous and can be prepared by a simple, economically viable process as compared to complex core-coat prior-art versions.