The present invention relates to a process for preparing Lomitapide or its pharmaceutically acceptable salt thereof having high purity with acceptable levels of impurities.
C07C 231/02 - Préparation d'amides d'acides carboxyliques à partir d'acides carboxyliques ou à partir de leurs esters, anhydrides ou halogénures par réaction avec de l'ammoniac ou des amines
C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
C07C 67/293 - Préparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné
C07C 69/157 - Esters d'acide acétique de composés monohydroxylés d'alcools non saturés contenant des cycles aromatiques à six chaînons
C07C 51/367 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par introduction de groupes fonctionnels contenant l'oxygène lié uniquement par une liaison simple
C07C 62/32 - Composés non saturés contenant des groupes hydroxyle ou O-métal
The present invention relates to a process for preparing Lomitapide or its pharmaceutically acceptable salt thereof having high purity with acceptable levels of impurities.
C07C 231/02 - Préparation d'amides d'acides carboxyliques à partir d'acides carboxyliques ou à partir de leurs esters, anhydrides ou halogénures par réaction avec de l'ammoniac ou des amines
C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
C07C 67/293 - Préparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné
C07C 69/157 - Esters d'acide acétique de composés monohydroxylés d'alcools non saturés contenant des cycles aromatiques à six chaînons
C07C 51/367 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par introduction de groupes fonctionnels contenant l'oxygène lié uniquement par une liaison simple
C07C 62/32 - Composés non saturés contenant des groupes hydroxyle ou O-métal
3.
Process for the preparation of intermediate of dolutegravir
The present invention provides a novel processes for preparation of methyl 3-(benzyloxy)-5-(2,4-difluorobenzylcarbamoyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyiridine-2-carboxylate using novel intermediates.
C07D 213/02 - Composés hétérocycliques contenant des cycles à six chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle et avec au moins trois doubles liaisons entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques comportant trois liaisons doubles
C07C 231/02 - Préparation d'amides d'acides carboxyliques à partir d'acides carboxyliques ou à partir de leurs esters, anhydrides ou halogénures par réaction avec de l'ammoniac ou des amines
C07D 213/14 - Préparation à partir de composés contenant de l'oxygène hétérocyclique
C07D 231/46 - Atome d'oxygène en position 3 ou 5 et atome d'azote en position 4
C07C 201/12 - Préparation de composés nitrés par des réactions ne créant pas de groupes nitro
C07D 231/08 - Composés hétérocycliques contenant des cycles diazole-1, 2 ou diazole-1, 2 hydrogéné non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des atomes d'oxygène ou de soufre liés directement aux atomes de carbone du cycle
The present invention provides a novel process for the preparation of pomalidomide crystalline Form I. The present invention also provides a process for the purification of pomalidomide.
C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
The present invention provides novel polymorphs of Lomitapide, process for their preparation and pharmaceutical compositions comprising them. The present invention also provides a novel polymorph of Lomitapide mesylate, process for its preparation and pharmaceutical compositions comprising it.
The present invention provides an improved process for the preparation of 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β,13α-dihydroxy-7β,10β-dimethoxy-9-oxo-11-taxene (7β,10β-dimethoxy-10-deacetoxybaccatin III). The present invention also provides a novel process for the preparation of cabazitaxel.
C07D 305/14 - Composés hétérocycliques contenant des cycles à quatre chaînons comportant un atome d'oxygène comme unique hétéro-atome du cycle condensés avec des carbocycles ou avec des systèmes carbocycliques
The present invention relates to a process for the preparation of Ledipasvir using Bis(triphenylphosphine)palladium(II) dichloride and process for the preparation of intermediates of Ledipasvir.
A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
C07D 403/04 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 403/14 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
The present invention provides processes for the preparation of i) Regorafenib (4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, BAY 73-4506, Stivarga®) and its pharmaceutically acceptable salt thereof; ii) a crystalline solid of Regorafenib tosylate; iii) Regorafenib Polymorph I from Regorafenib tosylate, and iv) a pure 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide from 4-amino-3-fluorophenol and 4-chloro-N-methylpicolinamide in the presence of potassium tert-butoxide.
The present invention relates to compositions of eltrombopag olamine. The present invention also relates to process for preparing compositions comprising eltrombopag olamine.
The present invention relates to a process for preparing Lomitapide or its pharmaceutically acceptable salt thereof having high purity with acceptable levels of impurities.
C07C 31/13 - Alcools monohydroxyliques contenant des cycles saturés
C07C 33/34 - Alcools monohydroxyliques contenant des cycles aromatiques à six chaînons et d'autres cycles
C07C 209/08 - Préparation de composés contenant des groupes amino liés à un squelette carboné par substitution de groupes fonctionnels par des groupes amino par substitution d'atomes d'halogène avec formation de groupes amino liés à des atomes de carbone acycliques ou à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons
C07C 209/74 - Préparation de composés contenant des groupes amino liés à un squelette carboné à partir d'amines, par des réactions n'impliquant pas de groupes amino, p. ex. réduction d'amines non saturées, aromatisation ou substitution du squelette carboné par halogénation, halogénhydratation, déshalogénation ou déshalogénhydratation
C07C 29/09 - Préparation de composés comportant des groupes hydroxyle ou O-métal liés à un atome de carbone ne faisant pas partie d'un cycle aromatique à six chaînons par hydrolyse
C07C 61/29 - Composés non saturés polycycliques comportant un groupe carboxyle lié à un système cyclique condensé
The present invention relates to novel betulinic proline imidazole derivatives and related compounds, compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
A61K 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes contenant des hétérocycles, p. ex. danazol, stanozolol, pancuronium ou digitogénine
C07J 63/00 - Stéroïdes ayant le squelette du cyclopenta[a]hydrophénanthrène modifié par expansion d'un seul cycle par un ou deux atomes
14.
EXTENDED RELEASE COMPOSITIONS OF CARVEDILOL PHOSPHATE
The present invention relates to solid oral dosage forms of carvedilol phosphate. More specifically, the present invention relates to extended release compositions of carvedilol phosphate and process for their preparation.
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/403 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des carbocycles, p. ex. carbazole
15.
NOVEL BETULINIC PROLINE SUBSTITUTED DERIVATIVES AS HIV INHIBITORS
The invention relates to novel betulinic proline substituted derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases. Formula (I)
A61K 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes contenant des hétérocycles, p. ex. danazol, stanozolol, pancuronium ou digitogénine
The present invention provides a novel amorphous solid dispersion of linagliptin in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
The present invention provides a novel process for the purification of alpha-propargylhomoterephthalic acid dimethyl ester substantially free of homoterephthalic acid dimethyl ester. The present invention also provides a novel process for the purification of pralatrexate.
C07C 67/52 - SéparationPurificationStabilisationEmploi d'additifs par modification de l'état physique, p. ex. par cristallisation
C07C 67/343 - Préparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone
C07D 475/08 - Composés hétérocycliques contenant des systèmes cycliques ptéridine avec un atome d'azote lié directement en position 4 avec un atome d'azote lié directement en position 2
The present invention relates to liquid compositions of asenapine with one or more pharmaceutically acceptable excipients. More particularly, the present invention relates to liquid spray compositions comprising asenapine for administration through oral mucosa.
A61K 31/407 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
A61P 25/18 - Antipsychotiques, c.-à-d. neuroleptiquesMédicaments pour le traitement de la manie ou de la schizophrénie
The present invention provides novel polymorphs of Lomitapide, process for their preparation and pharmaceutical compositions comprising them. The present invention also provides a novel polymorph of Lomitapide mesylate, process for its preparation and pharmaceutical compositions comprising it.
The present invention relates to parenteral compositions of bendamustine. More particularly, the present invention relates to parenteral compositions of bendamustine in the form of solution.
The present invention provides a commercially viable process for preparing rilpivirine and its pharmaceutically acceptable acid addition salts thereof in high yields using novel intermediate.
The present invention provides a solid dispersion of rufinamide in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
The present invention provides processes for the preparation of i) Regorafenib (4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl} amino)-3-fluorophenoxy] -N-methylpyridine-2-carboxamide, BAY 73-4506, Stivarga®) and its pharmaceutically acceptable salt thereof; ii) a crystalline solid of Regorafenib tosylate; iii) Regorafenib Polymorph I from Regorafenib tosylate, and iv) a pure 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide from 4-amino-3-fluorophenol and 4-chloro-N-methylpicolinamide in the presence of potassium tert-butoxide.
The present invention provides novel crystalline hydrochloride salt of darunavir, process for its preparation and to pharmaceutical composition comprising it. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it.
C07D 307/93 - Composés hétérocycliques contenant des cycles à cinq chaînons comportant un atome d'oxygène comme unique hétéro-atome du cycle condensés en ortho ou en péri avec des carbocycles ou avec des systèmes carbocycliques condensés avec un cycle autre qu'un cycle à six chaînons
27.
PHARMACEUTICAL COMPOSITIONS OF ROFLUMILAST AND PROCESS FOR PREPARATION THEREOF
The present invention relates to pharmaceutical compositions of roflumilast. More particularly, the present invention relates to pharmaceutical tablet compositions of roflumilast and process for preparing the same.
A61K 31/44 - Pyridines non condenséesLeurs dérivés hydrogénés
C07D 213/75 - Radicaux amino ou imino, acylés par un acide carboxylique, par l'acide carbonique ou par leurs analogues du soufre ou de l'azote, p. ex. des carbamates
The present invention relates to compositions of eltrombopag olamine. The present invention also relates to process for preparing compositions comprising eltrombopag olamine.
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres
A61K 31/4152 - 1,2-Diazoles ayant des groupes oxo liés directement à l'hétérocycle, p. ex. antipyrine, phénylbutazone, sulfinpyrazone
29.
PROCESS FOR THE PREPARATION OF INTERMEDIATE OF DOLUTEGRAVIR
The present invention provides a novel processes for preparation of methyl 3- (benzyloxy)-5-(2,4-difluorobenzylcarbamoyl)-4-oxo-l-(2-oxoethyl)-l,4-dihydropyiridine-2- carboxylate using novel intermediates.
This invention discloses the method of preparation of 4alfa.acetoxy-2alfa-benzoyloxy-5beta,20-epoxy-1beta,13alfa-dihydroxy-7beta, 10beta-dimethoxy-9-oxo-11-taxen (7beta, 10beta-dimethoxy-10-deacetoxybaccatin III) and the preparation of cabazitaxel, which comprises: a. dissolving (2aR,4S,4aS,6R,9S, 11S.I2S, 12aR, 12bS)-12b-acetoxy-9- (( (2R,3 S)-3-amino-2-hydroxy-3-phenylpropanoyl)oxy)-1 I-hydroxy-4,6-dimethoxy-4a,8, 13, 13-tettamethyl-5-oxo-2a, 3,4,4a, 5,6,9, 10, 1 1,12, 12a, 12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[l,2-b]oxet-12-yl benzoate.
The present invention provides a novel crystalline Form of vismodegib, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides a novel amorphous Form of vismodegib, process for its preparation and pharmaceutical compositions comprising it.
C07D 403/02 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles
A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
The present invention provides a novel process for the preparation of rilpivirine. The present invention also provides a novel process for the preparation of rilpivirine hydrochloride. The present invention further provides a rilpivirine hydrochloride monohydrate, process for its preparation and pharmaceutical compositions comprising it.
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
A61P 15/10 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs pour l'impuissance
C07F 9/6512 - Cycles à six chaînons les atomes d'azote étant en positions 1 et 3
The present invention provides a novel process for the preparation of pomalidomide crystalline Form I. The present invention also provides a process for the purification of pomalidomide.
C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 307/89 - Benzo [c] furannesBenzo [c] furannes hydrogénés avec deux atomes d'oxygène liés directement en positions 1 et 3
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
The present invention relates to solid dosage form comprising febuxostat or a pharmaceutically acceptable salt thereof. Particularly, the present invention relates to tablet compositions of febuxostat and process for their preparation.
The present invention provides a novel process for the preparation of 4-(4-hydroxypyrimidin-2-ylamino)benzonitrile. The present invention also provides a novel process for the preparation of 4-iodo-2,6-dimethyl benzenamine. The present invention further provides an improved process for the preparation of rilpivirine. The present invention further provides a tosylate salt of rilpivirine, process for its preparation and pharmaceutical compositions comprising it.
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
C07C 209/74 - Préparation de composés contenant des groupes amino liés à un squelette carboné à partir d'amines, par des réactions n'impliquant pas de groupes amino, p. ex. réduction d'amines non saturées, aromatisation ou substitution du squelette carboné par halogénation, halogénhydratation, déshalogénation ou déshalogénhydratation
The present invention relates to pharmaceutical compositions of saxagliptin. Particularly, the present invention relates to tablet compositions of saxagliptin and process for their preparation.
A61K 31/403 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des carbocycles, p. ex. carbazole
A61P 3/10 - Médicaments pour le traitement des troubles du métabolisme de l'homéostase du glucose de l'hyperglycémie, p. ex. antidiabétiques
The present invention provides a novel amorphous solid dispersion of ticagrelor in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. Specifically, provided is a process for the preparation of amorphous solid dispersion of ticagrelor which comprises: a) preparing a solution comprising a mixture of ticagrelor and one or more pharmaceutically acceptable carriers selected from copovidone, ethyl cellulose, hydroxypropyl methylcellulose, polyethylene glycol or soluplus in a solvent; and b) removing the solvent to obtain amorphous solid dispersion of ticagrelor in the carrier.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
The present invention provides a compound of crizotinib oxalate salt, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides a novel process for the preparation of crizotinib using novel intermediate. The present invention further provides a process for the purification of crizotinib. The present invention further provides a novel amorphous solid dispersion of crizotinib in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
A01N 43/40 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
The present invention provides a novel amorphous solid dispersion of carvedilol phosphate in combination with a pharmaceutically acceptable carrier and, process for its preparation. The present invention also provides pharmaceutical compositions comprising a therapeutically effective amount of amorphous solid dispersion of carvedilol phosphate along with a pharmaceutically acceptable carrier and at least one pharmaceutically acceptable excipient.
The present invention provides novel solvated forms of darunavir and processes for their preparation. The present invention also provides novel processes for the preparation of darunavir amorphous form and pharmaceutical compositions comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form.
A01N 43/08 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un ou plusieurs atomes d'oxygène ou de soufre comme uniques hétéro-atomes du cycle avec un hétéro-atome des cycles à cinq chaînons avec l'oxygène comme hétéro-atome du cycle
A61K 31/34 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide
C07D 493/00 - Composés hétérocycliques contenant des atomes d'oxygène comme uniques hétéro-atomes dans le système condensé
The present invention provides a novel amorphous solid dispersion of saxagliptin hydrochloride in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. The present invention provides pharmaceutical compositions comprising a therapeutically effective amount of amorphous solid dispersion of saxagliptin hydrochloride along with a pharmaceutically acceptable carrier, and at least one pharmaceutically acceptable excipient
A61K 31/403 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des carbocycles, p. ex. carbazole
The present invention provides a novel process for the preparation of abiraterone. The present invention also provides a novel process for the preparation of abiraterone acetate. In one aspect, the present invention provides a novel process for the preparation of abiraterone, which comprises: a) reacting dehydroepiandrosterone-3-acetate in a chlorinated solvent with trifluoromethanesulfonic anhydride in the presence of a base selected from the group consisting of n-methylpyrrolidone, N-methylpiperidine or tetramethylethylenediamine in a chlorinated solvent.
C07J 43/00 - Stéroïdes normaux ayant un hétérocycle contenant de l'azote non condensé ou condensé en spiro avec le squelette du cyclopenta[a]hydrophénanthrène
The present invention provides a novel process for the purification of lurasidone substantially free of isomeric impurity. According to on aspect of the present invention, there is provided a novel process for the purification of lurasidone substantially free of isomeric impurity which comprises crystallizing the lurasidone substantially free of isomeric impurity from a solution of lurasidone containing isomeric impurity in an ester solvent or a chlorinated solvent.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
45.
NOVEL BETULINIC ACID PROLINE DERIVATIVES AS HIV INHIBITORS
The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases. These compounds are esterified in position 3 and are substituted in position 17 of the betulinic acid structure, via a linking group W, by a saturated 5-7 membered nitrogen-heterocycle.
C07J 63/00 - Stéroïdes ayant le squelette du cyclopenta[a]hydrophénanthrène modifié par expansion d'un seul cycle par un ou deux atomes
A61K 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes contenant des hétérocycles, p. ex. danazol, stanozolol, pancuronium ou digitogénine
The present invention provides a novel amorphous solid dispersion of lurasidone hydrochloride in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole
The present invention provides a novel process for the purification of alpha-propargylhomoterephthalic acid dimethyl ester substantially free of homoterephthalic acid dimethyl ester. The present invention also provides a novel process for the purification of pralatrexate.
The disclosure is related to amorphous raltegravir and the solid oral dosage forms of amorphous raltegravir that are of lower dosage than the commercially available reference dosage form. Provided herein are a pharmaceutical solid oral dosage form composed from (a) 300 mg of amorphous raltegravir or an equivalent amount of a pharmaceutically acceptable salt thereof; (b) a polymer; and (c) a pharmaceutically acceptable excipient and a method of reducing adverse effects of raltegravir administration in a human subject, comprising administering to the human subject a solid oral dosage form comprising 300 mg of amorphous raltegravir or an equivalent amount of a pharmaceutically acceptable salt thereof.
C07F 9/6558 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle contenant au moins deux hétérocycles différents ou différemment substitués ni condensés entre eux ni condensés avec un carbocycle commun ou un système carbocyclique commun
The present invention relates to amorphous ritonavir co-precipitated on copovidone, process for its preparation and pharmaceutical compositions comprising it.
A61K 31/427 - Thiazoles non condensés et contenant d'autres hétérocycles
C07D 417/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 277/28 - Radicaux substitués par des atomes d'azote
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
The present invention provides a novel amorphous Form of azilsartan acid, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides novel crystalline Forms of azilsartan medoxomil, processes for their preparations and pharmaceutical compositions comprising them. The present invention further provides a novel amorphous Form of azilsartan medoxomil potassium, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a novel process for the preparation of azilsartan medoxomil potassium crystalline Form II.
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
The present invention relates to pharmaceutical compositions comprising rufinamide premix and one or more pharmaceutically acceptable excipients and methods of preparing the same. Chemically rufinamide is 1-[ (2,6-difluorophenyl)methyl]-IHI,2,3-triazole-4 carboxamide. It has a molecular formula C10H2F2N4) molecular weight of 238.2, and structural Formula I.
A61K 31/41 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec plusieurs hétéro-atomes cycliques, l'un au moins étant l'azote, p. ex. tétrazole
The present invention provides a novel amorphous Form of doxercalciferol, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides a solid dispersion of doxercalciferol in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a novel crystalline Form of doxercalciferol, process for its preparation and pharmaceutical compositions comprising it.
C07C 401/00 - Produits d'irradiation du cholestérol ou de ses dérivésDérivés de vitamine D, séco-9,10 cyclopenta[a]phénanthrène ou leurs analogues obtenus par préparation chimique sans irradiation
The present invention provides a novel amorphous form of vildagliptin, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides a solid dispersion of vildagliptin in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. Vildagliptin (LAF237) is an oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs.
The present invention provides a solid dispersion of rufinamide in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. The present invention provides a solid dispersion of rufinamide in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
A61K 31/41 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec plusieurs hétéro-atomes cycliques, l'un au moins étant l'azote, p. ex. tétrazole
The present invention provides a novel amorphous solid dispersion of linagliptin in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. The present invention provides a novel amorphous solid dispersion of linagliptin in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
C07D 473/04 - Composés hétérocycliques contenant des systèmes cycliques purine avec des atomes d'oxygène, de soufre ou d'azote liés directement en positions 2 et 6 deux atomes d'oxygène
The present invention provides a commercially viable process for preparing rilpivirine and its pharmaceutically acceptable acid addition salts thereof in high yields using novel intermediate. Rilpivirine (TMC278) is an investigational new drug, developed by Tibotec, for the treatment of HIV infection. It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTis.
The present invention provides a novel crystalline form of azilsartan acid, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides a novel crystalline form of azilsartan medoxomil potassium, process for its preparation and pharmaceutical compositions comprising it. Azilsartan medoxomil is chemically (5-methyl-2-oxo-1,3-dioxol-4-yl) methyl-2-ethoxy-1-([2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl)-1 H-benzimidazole-7-carboxylate. Azilsartan is an angiotensin II receptor antagonist used in the treatment of hypertension.
C07D 413/10 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
The present disclosure relates to solid oral compositions of silodosin or its pharmaceutically acceptable salt thereof. More particularly, capsule compositions of silodosin with one or more pharmaceutically acceptable excipients and process for their preparation. In a first embodiment, a solid oral composition is discosed comprising: i) silodosin, ii) sodium stearyl fumarate as lubricant, and iii) one or more pharmaceutically acceptable excipients.
C07D 209/08 - IndolesIndoles hydrogénés avec uniquement des atomes d'hydrogène ou des radicaux ne contenant que des atomes d'hydrogène et de carbone, liés directement aux atomes de carbone de l'hétérocycle
Stable pharmaceutical compositions of fesoterodine or its pharmaceutically acceptable salt thereof and process for preparing the same. In a first embodiment, a stable pharmaceutical composition is provided comprising fesoterodine fumarate, glyceryl behenate and a stabilizer. The stable pharmaceutical tablet composition may further comprise i) fesoterodine fumarate in an 5 amount of 1% to 5% by weight, ii) glyceryl behenate in an amount of 1% to 8% by weight, iii) pregelatinized starch in an amount of 30% to 50% by weight and iv) a stabilizer in an amount of 0.1 % to 10% by weight based on total weight of the composition.
The present invention provides a novel substantially amorphous solid dispersion of ibandronate sodium in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. In a preferred embodiment the process for the preparation of amorphous solid dispersion of ibandronate sodium in combination with a pharmaceutically acceptable carrier comprises: preparing a solution comprising a mixture of ibandronate sodium and one or more pharmaceutically acceptable carriers selected from copovidone, ethyl cellulose, hydroxypropyl methylcellulose, polyethylene glycol, span 20 or soluplus in a solvent, water or mixture thereof; and removing the solvent or water to obtain substantially amorphous solid dispersion of ibandronate sodium in combination with a pharmaceutically acceptable carrier.
The present invention provides a novel amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. In a preferred embodiment the process for the preparation of amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier comprises: preparing a solution comprising a mixture of elvitegravir and one or more pharmaceutically acceptable carriers selected from copovidone, ethyl cellulose, hydroxypropyl methylcellulose, polyethylene glycol, span 20 or soluplus in a solvent; and removing the solvent from the solution obtained; adding hydrocarbon solvent to the residual solid; and isolating amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier.
The present invention provides a novel process for the preparation of sorafenib tosylate polymorph III. The preferred embodiment for the preparation of sorafenib tosylate polymorph III, comprises: providing a solution comprising sorafenib, p-toluenesulfonic acid and a solvent selected from a group consisting of a mixture of dimethyl acetamide and an alcoholic solvent, a mixture of dimethylformamide and an alcoholic solvent and a mixture thereof; adding an alcoholic solvent to the solution obtained; isolating the solid; slurring the solid with an alcoholic solvent; and isolating sorafenib tosylate polymorph III.
C07D 213/78 - Atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile
The present invention provides a novel amorphous solid dispersion of saxagliptin in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. In a preferred embodiment, the process for the preparation of amorphous solid dispersion of saxagliptin in combination with a pharmaceutically acceptable carrier comprises: preparing a solution comprising a mixture of saxagliptin and one or more pharmaceutically acceptable carriers selected from copovidone, ethyl cellulose, hydroxypropyl methylcellulose, polyethylene glycol or soluplus in a solvent; and removing the solvent to obtain amorphous solid dispersion of saxagliptin in combination with a pharmaceutically acceptable carrier.
A61K 31/403 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des carbocycles, p. ex. carbazole
The present invention provides a novel amorphous solid dispersion of desvenlafaxine succinate in combination with soluplus, process for its preparation and pharmaceutical compositions comprising it. In one aspect, the present invention provides amorphous solid dispersion of desvenlafaxine succinate in combination with soluplus. In another aspect, the present invention there is provided a process for the preparation of amorphous solid dispersion of desvenlafaxine succinate in combination with soluplus, which comprises: a) preparing a solution comprising a mixture of desvenlafaxine succinate and soluplus in a solvent; and b) removing the solvent to obtain amorphous solid dispersion of desvenlafaxine succinate in combination with soluplus. Yet in another aspect, the present invention provides pharmaceutical compositions comprising a therapeutically effective amount of amorphous solid dispersion of desvenlafaxine succinate along with soluplus, and at least one pharmaceutically acceptable excipient.
The present invention provides a novel amorphous solid dispersion of sunitinib malate in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. In one aspect, the present invention provides amorphous solid dispersion of sunitinib malate in combination with a pharmaceutically acceptable carrier. In another aspect, the present invention there is provided a process for the preparation of amorphous solid dispersion of sunitinib malate in combination with a pharmaceutically acceptable carrier, which comprises: a) preparing a solution comprising a mixture of sunitinib malate and one or more pharmaceutically acceptable carriers selected form copovidone, span 20, ethyl cellulose, hydroxypropyl methylcellulose, polyethylene glycol or soluplus in water; and b) subjecting the resulting solution to freeze drying to obtain amorphous solid dispersion of sunitinib malate in combination with a pharmaceutically acceptable carrier.
A61K 31/403 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des carbocycles, p. ex. carbazole
68.
NOVEL BETULINIC ACID DERIVATIVES AS HIV INHIBITORS
The present invention provides betulinic acid derivatives and related compounds, which may be used as antiviral particularly as anti-HIV compounds and processes for the synthesis of these compounds. Pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, together with pharmaceutically acceptable carriers, excipients or diluents, which can be used for the treatment of diseases, condition and/or disorders mediated by viral infections, are also provided.
The present invention relates to novel non-hygroscopic anhydrous Form of moxifloxacin hydrochloride, process for its preparation and to pharmaceutical composition containing it.
The present invention provides a compound of 7,8-dimethoxy-3-[3-[[(1S)-(4,5-dimethoxybenzocyclobutan-1-yl)methyl]methylamino]propyl]-1,3-de-hydro-7,8-dimethoxy-2H-3-benzazepin-2-one oxalate (de-hydro ivabradine oxalate salt) and process for its preparation. The present invention also provides a process for the purification of de-hydro ivabradine oxalate salt. The present invention further provides a novel process for the preparation of ivabradine using novel intermediate. The present invention further provides a novel amorphous solid dispersion of ivabradine hydrochloride in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
The present invention provides a solid of pitavastatin tert-butyl ester and process for its preparation. The present invention also provides a novel crystalline form of pitavastatin calcium, process for its preparation and pharmaceutical compositions comprising it.
C07D 215/04 - Composés hétérocycliques contenant les systèmes cycliques de la quinoléine ou de la quinoléine hydrogénée ne comportant pas de liaison entre l'atome d'azote du cycle et un chaînon non cyclique ou ne comportant que des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle avec uniquement des atomes d'hydrogène ou des radicaux ne contenant que des atomes d'hydrogène et de carbone, liés directement aux atomes de carbone du cycle
C07D 215/16 - Composés hétérocycliques contenant les systèmes cycliques de la quinoléine ou de la quinoléine hydrogénée ne comportant pas de liaison entre l'atome d'azote du cycle et un chaînon non cyclique ou ne comportant que des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
The present invention provides a novel amorphous Form of lurasidone hydrochloride, process for its preparation and pharmaceutical compositions comprising it. In one aspect, the present invention provides an amorphous form of lurasidone hydrochloride. In another aspect, the present invention provides a process for the preparation of lurasidone hydrochloride amorphous Form, which comprises: a) dissolving lurasidone hydrochloride in a mixture of alcoholic solvent and water; and b) subjecting the resulting solution to lyophilization to obtain lurasidone hydrochloride amorphous form.
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
The present invention relates to pharmaceutical compositions comprising ritonavir premix, a water soluble polymer and a surfactant and process for preparing the same. The ritonavir premix comprises ritonavir, copovidone, colloidal silicon dioxide and sorbitan monolaurate. More particularly, the present invention relates to hot-melt extrusion process for preparing solid oral compositions of ritonavir premix.
The present invention provides novel crystalline forms of maraviroc phosphate, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides novel process for the preparation of maraviroc amorphous form and pharmaceutical composition comprising it.
C07D 451/04 - Composés hétérocycliques contenant des systèmes cycliques aza-8 bicyclo [3.2.1] octane, aza-9 bicyclo [3.3.1] nonane ou oxa-3 aza-9 tricyclo [3.3.1.02,4] nonane, p. ex. alcaloïdes du tropane ou du granatane, scopolamineLeurs acétals cycliques contenant des systèmes cycliques aza-8 bicyclo [3.2.1] octane ou oxa-3 aza-9 tricyclo [3.3.1.02,4] nonane sans autre condensation, p. ex. tropaneLeurs acétals cycliques avec des hétéro-atomes liés directement en position 3 du système cyclique aza-8 bicyclo [3.2.1] octane ou en position 7 du système cyclique oxa-3 aza-9 tricyclo [3.3.1.02,4] nonane
The present invention is directed to extended release pharmaceutical compositions comprising nevirapine, a release control polymer/ material and one or more pharmaceutically acceptable excipients, process for its preparation and use in the treatment of HIV-1 infection in adults.
CONTROLLED RELEASE SOLID ORAL COMPOSITIONS OF DEXLANSOPRAZOLE ABSTRACT: The present invention relates to controlled release solid oral compositions of dexlansoprazole or its pharmaceutically acceptable salts and process for preparation thereof and its use for healing of erosive esophagitis, maintenance of healed erosive esophagitis and treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease.
The present invention provides a novel process for the preparation of 7-chloro-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one. The present invention also provides an improved process for the preparation of 7-chloro-1-(2-methyl-4-nitrobenzoyl)-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. The present invention further provides an improved process for the preparation of 7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine.
The present invention provides a novel process for the purification of alvimopan. In accordance with the present invention alvimopan was dissolved in dimethylformamide and heated to 120 to 125 deg C, and then added n-butanol at room temperature, the contents were stirred for 15 hours, filtered and then dried to obtain pure alvimopan.
C07D 211/28 - Composés hétérocycliques contenant des cycles pyridiques hydrogénés, non condensés avec d'autres cycles avec uniquement des atomes d'hydrogène et de carbone liés directement à l'atome d'azote du cycle ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone du cycle avec des radicaux hydrocarbonés substitués liés aux atomes de carbone du cycle avec des radicaux hydrocarbonés, substitués par des atomes d'azote auxquels est lié un second hétéro-atome
The present invention is directed to fast release pharmaceutical compositions comprising entecavir or its pharmaceutically acceptable salts, process for preparing the same and use of such compositions for the treatment of Hepatitis B virus infection. In a preferred embodiment, the present invention relates to pharmaceutical composition comprising 0.05-1% by weight of entecavir, 1-6% by weight of acid component, 1-90% by weight of carbonates/ bicarbonates of sodium, magnesium, potassium and calcium and 1-20% by weight of superdisintegrant based on total weight of the composition.
4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile is a key intermediate for the preparation of etravirine. The present invention provides a process for preparation of 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile. The present invention also provides a novel process for the preparation of etravirine crystalline form I. The present invention further provides novel crystalline forms of etravirine, processes for their preparation and pharmaceutical compositions comprising them.
The present invention provides a novel process for the preparation of amorphous alogliptin benzoate. The present invention also provides amorphous alogliptin benzoate co-precipitated on copovidone, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides novel salts of alogliptin, processes for their preparation and pharmaceutical compositions comprising them. The present invention further provides crystalline hydrochloride salt of alogliptin, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides crystalline tartrate salt of alogliptin, process for its preparation and pharmaceutical compositions comprising it.
C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
The present invention provides novel crystalline hydrochloride salt of darunavir, process for its preparation and to pharmaceutical composition comprising it. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it.
C07D 493/02 - Composés hétérocycliques contenant des atomes d'oxygène comme uniques hétéro-atomes dans le système condensé dans lesquels le système condensé contient deux hétérocycles
C07D 307/93 - Composés hétérocycliques contenant des cycles à cinq chaînons comportant un atome d'oxygène comme unique hétéro-atome du cycle condensés en ortho ou en péri avec des carbocycles ou avec des systèmes carbocycliques condensés avec un cycle autre qu'un cycle à six chaînons
A61K 31/34 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide
As used herein the term "room temperature" refers to a temperature of about 25°C to about 35°C. According to one aspect of the present invention, there IS provided a novel process for the preparation of rilpivirine, which comprises: a) condensing the (E)-3-( 4-amino-3,5-dimethylphenyl)acrylonitrile hydrochloride with 4-( 4-chloropyrimidin-2-ylamino )benzonitrile m the presence of Nmethylpyrrolidone; b) heating the contents obtained in step (a) at about 75 to 95°C to obtain a solution; c) cooling the solution obtained in step (b) at below 35°C; d) adding water to the reaction mass; and e) isolating rilpivirine. The reaction in step (b) may preferably be heated to 100 to 110°C. Step (c) may preferably be carried out at room temperature. Rilpivirine may be isolated in step (e) by the methods known such as Filtration or centrifugation.
The present invention relates to amorphous mixture of lopinavir and ritonavir coprecipitated on copovidone, process for its preparation and pharmaceutical compositions comprising it. In one aspect, the present invention provides amorphous mixture of lopinavir and. ritonavir co-precipitated on copovidone. In another aspect, the present invention provides a process for the preparation of amorphous mixture of lopinavir and ritonavir co-precipitated on copovidone, which comprises: i) dissolving a mixture of lopinavir, ritonavir, copovidone, aerosil and span-20 in an alcoholic solvent; and ii) removing the solvent by drying at about 50 to 80°C to obtain amorphous mixture of lopinavir and ritonavir co-precipitated on copovidone.
The present invention provides an improved process for the preparation of 3-(benzyloxycarbonylamino)piperidine-2,6-dione. The present invention also provides an improved process for the preparation of 3-(4-nitro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)piperidine-2,6-dione. The present invention further provides a process for the preparation of lenalidomide crystalline Form H1.
A01N 43/42 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons condensés avec des carbocycles
The present invention provides a process for the preparation of 1H-benzimidazol-1-methyl-5-N,N-di(2-hydroxyethyl)-2-butanoic acid ethyl ester. The present invention also provides a process for the preparation of bendamustine hydrochloride. The present invention further provides a process for the purification of bendamustine hydrochloride.
Crystalline Forms of fosamprenavir calcium are disclosed, processes for its preparation and pharmaceutical compositions therefrom. The process for the preparation of fosamprenavir calcium crystalline Form H1, comprises: a) suspending fosamprenavir calcium in a nitrile solvent; b) heating the suspension obtained in step (a) at reflux; c) optionally adding a solvent to the reaction mass obtained in step (b); d) cooling the reaction mass at below 35 degrees Centigrade; and e) isolating fosamprenavir calcium crystalline Form H1. Another process for the preparation of substantially pure amorphous fosamprenavir calcium, which comprises: a) dissolving fosamprenavir calcium in an ester solvent; b) a portion of solvent from the solution obtained in step (a) until at least separation of fosamprenavir calcium as solid occurs; and c) isolating substantially pure amorphous fosamprenavir calcium. The pharmaceutical composition may comprse substantially pure amorphous fosamprenavir calcium and pharmaceutically acceptable excipients.
C07F 9/655 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle comportant des atomes d'oxygène, avec ou sans atomes de soufre, de sélénium ou de tellure, comme uniques hétéro-atomes du cycle
The present invention provides a process for the preparation of 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention also provides a process for the preparation of 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention further provides novel crystalline Forms of febuxostat, processes for their preparation and pharmaceutical compositions comprising them. The present invention further provides febuxostat crystalline particles having a mean particle size of less than about 25 µm, the methods for the manufacture of said crystalline particles, and pharmaceutical compositions comprising said crystalline particles.
In one aspect, the present invention provides amorphous ritonavir co-precipitated on copovidone. In another aspect, the present invention provides a process for the preparation of amorphous ritonavir co-precipitated on copovidone, which comprises: a) dissolving a mixture of ritonavir and copovidone in an alcoholic solvent; and b) removing the solvent by drying at about 50 to 80°C to obtain amorphous ritonavir co-precipitated on copovidone. Yet in another aspect, the present invention provides a pharmaceutical composition comprising amorphous Form of ritonavir co-precipitated on copovidone and pharmaceutically acceptable excipients.
Pharmaceutical compositions comprise nilotinib or a pharmaceutically acceptable salt thereof and a process for the preparation of the same. Methods of using such compositions treat subjects suffering from Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML). A process for preparing dry-granulated pharmaceutical composition of nilotinib comprising compacting nilotinib hydrochloride alone or mixing with one or more of pharmaceutically acceptable excipient(s) by roller compactor or slugging; sizing the compacts or slugs into granules by milling; mixing the granules with one or more of pharmaceutically acceptable excipients to form the composition.
In one aspect, the present invention provides a novel process for reducing palladium content in fosaprepitant dimeglumine, which comprises: a) providing a solution of fosaprepitant dimeglumine in a solvent; b) adding SiliaBond Metal Scavenger to the solution obtained in step (a); c) maintaining the reaction mass obtained in step (b); d) adding a solvent to the reaction mass; e) isolating the wet solid; f) slurring the wet solid obtained in step (e) with an ester solvent; and g) isolating fosaprepitant dimeglumine.
C07F 9/6558 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle contenant au moins deux hétérocycles différents ou différemment substitués ni condensés entre eux ni condensés avec un carbocycle commun ou un système carbocyclique commun
Described herein is pure amorphous darunavir, methods of making pure amorphous darunavir and pharmaceutical compositions containing amorphous darunavir and a pharmaceutically acceptable excipient.
A01N 43/08 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un ou plusieurs atomes d'oxygène ou de soufre comme uniques hétéro-atomes du cycle avec un hétéro-atome des cycles à cinq chaînons avec l'oxygène comme hétéro-atome du cycle
A61K 31/34 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide
The present invention provides a novel process for the preparation of 4-(4-hydroxypyrimidin-2-ylamino)benzonitrile. The present invention also provides a novel process for the preparation of 4-iodo-2,6-dimethyl benzenamine. The present invention further provides an improved process for the preparation of rilpivirine. The present invention further provides a tosylate salt of rilpivirine, process for its preparation and pharmaceutical compositions comprising it.
Described herein are pharmaceutical compositions of quetiapine, more particularly extended release compositions of quetiapine or its pharmaceutically acceptable salts comprising carboxymethyl ethyl cellulose, a non-gelling, hydrophobic release controlling polymer, and processes for preparing the same.
A01N 43/00 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques
95.
PHARMACEUTICAL COMPOSITIONS OF RALTEGRAVIR, METHODS OF PREPARATION AND USE THEREOF
It has been found that compositions of raltegravir comprising non-gelling polymers are comparable with the marketed raltegravir potassium formulation. In one embodiment, the pharmaceutical composition comprises raltegravir as active ingredient or its pharmaceutically acceptable salt thereof, non-gelling polymer and one or more pharmaceutically acceptable excipients. In anoth embodiment, the pharmaceutical composition comprises raltegravir, non-gelling polymer selected from polymethacrylates and/or polyethylene oxide, and one or more pharmaceutically acceptable excipients, characterized in that said composition is free of anti-nucleating agent.
Disclosed are pharmaceutical compositions comprising HIV integrase strand transfer inhibitor. More particularly, oral pharmaceutical compositions of raltegravir or its pharmaceutically acceptable salts and process for preparing and use of the same are disclosed.
The present invention provides a novel crystalline Form of lenalidomide, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides a novel N-methylpyrrolidone solvate of lenalidomide and process for its preparation.
The present invention relates to a novel amorphous form of lopinavir and ritonavir mixture in the ratio of 3.8:1.2 to 4.2:0.8, process for its preparation and pharmaceutical compositions comprising it.
The present disclosure relates to solid dosage forms comprising the CCR5 co-receptor antagonist maraviroc. More particularly, the present disclosure relates to a solid oral dosage form containing maraviroc which has favorable disintegration properties.
A01N 43/42 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons condensés avec des carbocycles
A61K 31/44 - Pyridines non condenséesLeurs dérivés hydrogénés
The present invention provides a process for the preparation of N-[4-[2-(2-amino-4, 7 -dihydro-4-oxo-1 H-pyrrolo[2,3-d]pyrimidin-5-yl) ethyf]benzoyl]-L-glutamic acid dimethyl ester1 or salts thereof. The present invention also provides a process for the preparation of pemetrexed disodium substantially free of enatiomeric impurity. In another aspect, the present invention provides a process for the preparation of pemetrexed disodium substantially free of enantiomeric impurity, which comprises: a) stirring a solution of N-[4-[2-(2-amino-4,7-dihydro-4-oxo-IH-pyrrolo[2,3- d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid dimethyl ester 4- methylbenzenesulfonic acid with a mixture of sodium hydroxide and water at below 30°C; b) adjusting the pH of the reaction mass to above 7.2 with an acid; c) adding an organic solvent to the solution obtained in step (b) at below 30°C; and d) isolating the pemetrexed disodium substantially free of enantiomeric impurity.
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