The present invention relates to an improved process for the preparation of Avibactam or a pharmaceutically acceptable salt thereof, particularly the present invention relates to process for the preparation of a bridged ester intermediate of Formula I, wherein R1 is a hydroxy protecting group which is a key intermediate for Avibactam or a pharmaceutically acceptable salt thereof. The present invention also relates to the crystalline form of intermediates used for the synthesis of Avibactam or a pharmaceutically acceptable salt thereof. The invention also provides improved processes for the preparation of Avibactam or a pharmaceutically acceptable salt, using the bridged ester compound of formula I prepared by the process of the present invention.
The present invention relates to an improved process for the preparation of CDK inhibiting pyrrolopyrimidine compounds. More particularly the invention provides a process for preparation of high purity 2'-{[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino}-7',8' dihydro- 6'H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one which does not involve the use of expensive chemicals, hazardous reagents or tedious purification techniques. Invention also provides novel intermediate useful for preparation of desired compound in high purity.
C07D 487/12 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains three hetero rings
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
1233 is t-Bu or Bn. The present invention further, relates to a process for the preparation Liraglutide or its pharmaceutically acceptable salts using the tetrapeptide of formula (I).
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
5.
AN IMPROVED PROCESS FOR THE PREPARATION OF SEMAGLUTIDE SIDE CHAIN
The present invention relates to an improved process for the preparation of a compound of Formula (1), The invention also provides improved processes for the preparation of intermediates used in the synthesis of Formula (1). The compound of Formula (1) is used in the synthesis of Semaglutide.
C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07D 207/46 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
The present provides a simple, convenient and time-efficient process for the preparation of propofol. Particularly, the present invention provides an improved process for the preparation of propofol using a heterocyclic base for the decarboxylation reaction. The present invention provides a time-efficient process for the preparation of propofol with high yield and purity.
C07C 37/50 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by reactions decreasing the number of carbon atoms
The present invention relates to a tablet comprising Afatinib or a pharmaceutically acceptable salt thereof, wherein the tablet is obtained by direct compression. The present invention further relates to a process for manufacturing a tablet of the invention as well as the use of the tablet of the invention.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to a process for preparing the Alectinib or a pharmaceutically acceptable salt thereof using lesser reaction steps and also eliminating expensive and time-consuming column chromatography. The invention also relates to novel polymorphic forms of Alectinib and Alectinib hydrochloride.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
B01J 31/04 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides containing carboxylic acids or their salts
B01J 31/12 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides containing organo-metallic compounds or metal hydrides
The present invention relates to an improved process for the preparation of a compound of Formula (1), The invention also provides improved processes for the preparation of intermediates used in the synthesis of Formula (1). The compound of Formula (1) is used in the synthesis of Semaglutide.
A61K 47/52 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an inorganic compound, e.g. an inorganic ion that is complexed with the active ingredient
The present provides a simple, convenient and time-efficient process for the preparation of propofol. Particularly, the present invention provides an improved process for the preparation of propofol using a heterocyclic base for the decarboxylation reaction. The present invention provides a time-efficient process for the preparation of propofol with high yield and purity.
C07C 37/50 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by reactions decreasing the number of carbon atoms
The present invention relates to the polymorphic forms of Belinostat. The invention also relates to the process for the preparation of the polymorphic forms of Belinostat. This invention further relates to pharmaceutical composition of said polymorphic forms of Belinostat and use thereof in the treatment of a patient in need thereof.
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 303/40 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
C07C 311/37 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof.
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The invention relates to a process for the preparation of ribociclib of formula V or its salts. The invention provides novel crystalline forms of ribociclib succinate and ribociclib trifluoroacetate. The present invention also relates to pharmaceutical compositions comprising a crystalline form of ribociclib succinate and at least a pharmaceutically acceptable carrier. It further relates to the use of such compositions in the treatment of cancer.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
14.
Process for preparing alectinib or a pharmaceutically acceptable salt thereof
The present invention relates to a process for preparing the Alectinib or a pharmaceutically acceptable salt thereof using lesser reaction steps and also eliminating expensive and time-consuming column chromatography. The invention also relates to novel polymorphic forms of Alectinib and Alectinib hydrochloride.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
B01J 31/12 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides containing organo-metallic compounds or metal hydrides
B01J 31/04 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides containing carboxylic acids or their salts
The present invention provides an improved and industrially viable process for the preparation of Acalabrutinib and its intermediates in high yield and eliminating the use of time-consuming purification process. The present invention also relates to the purification of (S)-4-(8-Amino-3-(pyrrolidin-2-yl)imidazo[1,5-alpyrazin-1-yl)-N-(pyridin-2-yl) benzamide, a key intermediate for the preparation of Acalabrutinib. Further present invention relates to new polymorphic form of Acalabrutinib.
1 may be independently selected from tert-butyloxycarbonyl (Boc), phthaloyl, 9-fluorenylmethyloxycarbonyl (Fmoc), triphenylmethyl (Trityl), carboxybenzyl (Cbz), trifluoroacetyl, benzyl (Bn), benzylidene, methanesulfonyl (Mesyl), toluene sulfonyl (Tosyl) or acyl; its isolation as solid and use for the preparation of the compound of formula (IV), in particular the compound of formula (IV) i.e. [(1R)-3-methyl-1[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl) amino]propyl]amino]butyl] boronic acid with more than 99.95% chiral purity, as measured by HPLC.
The present invention relates to the polymorphic forms of Belinostat. The invention also relates to the process for the preparation of the polymorphic forms of Belinostat. This invention further relates to pharmaceutical composition of said polymorphic forms of Belinostat and use thereof in the treatment of a patient in need thereof.
C07C 311/37 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 303/40 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
The present invention relates to a process for the purification of compound of formula II, wherein X may be independently selected from trifluoroacetic acid, hydrochloric acid, hydrobromic acid, p-toluene sulfonic acid and phosphoric acid; its isolation as solid and use for the preparation of carfilzomib.
C07K 1/22 - Affinity chromatography or related techniques based upon selective absorption processes
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
The invention relates to a process for the preparation of ribociclib of formula V or its salts. The invention provides novel crystalline forms of ribociclib succinate and ribociclib trifluoroacetate. The present invention also relates to pharmaceutical compositions comprising a crystalline form of ribociclib succinate and at least a pharmaceutically acceptable carrier. It further relates to the use of such compositions in the treatment of cancer.
The present invention relates to a process for the preparation of Treosulfan using sodium borohydride and iodine as reducing agent, which is less hazardous and convenient as compared to the reagents used in the prior art. The invention also relates to a novel intermediate to obtain Treosulfan in high yield and high purity.
C07C 309/68 - Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a carbon skeleton substituted by singly-bound oxygen atoms
C07D 317/18 - Radicals substituted by singly bound oxygen or sulfur atoms
C07D 317/32 - Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
The present invention relates to a stable liquid pharmaceutical composition of pemetrexed for parenteral administration. The invention provides composition comprising pemetrexed diacid, an organic amine and cyclodextrin. The composition may further comprise an inert gas. The composition can be ready to use infusion solution of pemetrexed diacid or liquid concentrate formulation to be diluted before administration to the patient. The present invention further relates to a process for manufacturing the compositions as well as use of the compositions of the invention for the treatment of malignant pleural mesothelioma and non-small cell lung cancer.
The present invention relates to a process for preparing the Alectinib or a pharmaceutically acceptable salt thereof using lesser reaction steps and also eliminating expensive and time- consuming column chromatography. The invention also relates to novel polymorphic forms of Alectinib and Alectinib hydrochloride.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof.
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to a process for the preparation of compound of formula (I), wherein, R1 and R2 are each independently hydroxy, alkoxy, aryloxy, or aralkoxy; or R1 and R2 together form a moiety derived from an alpha-hydroxy carboxylic acid compound or a beta-hydroxy carboxylic acid compound, wherein the atom attached to boron in each case is an oxygen atom; or R1 and R2 together form the boronate esters of boronic acid.
C07D 233/60 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
The present invention relates to an improved process for the preparation of xylene linked cyclam compounds. More particularly the invention provides a process for preparation of high purity plerixafor which does not involve the use of expensive chemicals, hazardous reagents or tedious purification techniques. Invention also provides novel intermediate useful for preparation of desired compound in high purity.
C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
The present invention relates to a tablet comprising Afatinib or a pharmaceutically acceptable salt thereof, wherein the tablet is obtained by direct compression. The present invention further relates to a process for manufacturing a tablet of the invention as well as the use of the tablet of the invention.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to an improved process for the preparation of a compound of formula (I), wherein PG1 may be independently selected from tert-butyloxycarbonyl (Boc), phthaloyl, 9-fluorenylmethyloxycarbonyl (Fmoc), triphenylmethyl (Trityl), carboxybenzyl (Cbz), trifluoroacetyl, benzyl (Bn), benzylidene, methanesulfonyl (Mesyl), toluene sulfonyl (Tosyl) or acyl; its isolation as solid and use for the preparation of the compound of formula (IV), in particular the compound of formula (IV) i.e. [(1R)-3-methyl-1[[(2S)-1-oxo-3-phenyl-2- [(pyrazinylcarbonyl) amino]propyl]amino]butyl] boronic acid with more than 99.95% chiral purity, as measured by HPLC.
The present invention relates to a process for the purification of compound of formula II, wherein X may be independently selected from trifluoroacetic acid, hydrochloric acid, hydrobromic acid, p-toluene sulfonic acid and phosphoric acid; its isolation as solid and use for the preparation of carfilzomib.
C07D 303/32 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention relates to the polymorphic forms of Belinostat. The invention also relates to the process for the preparation of the polymorphic forms of Belinostat. This invention further relates to pharmaceutical composition of said polymorphic forms of Belinostat and use thereof in the treatment of a patient in need thereof.
C07C 311/37 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
The present invention relates to a process for the purification of Carfilzomib of Formula I that reduces the level of an acetamide impurity of Formula II preferably below 0.10 wt %.
The present invention relates to an improved process for the preparation of xylene linked cyclam compounds. More particularly the invention provides a process for preparation of high purity plerixafor which does not involve the use of expensive chemicals, hazardous reagents or tedious purification techniques. Invention also provides novel intermediate useful for preparation of desired compound in high purity.
C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
The present invention relates to a tablet comprising Afatinib or a pharmaceutically acceptable salt thereof, wherein the tablet is obtained by direct compression. The present invention further relates to a process for manufacturing a tablet of the invention as well as the use of the tablet of the invention.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof.
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to a stable ready to use pharmaceutical composition comprising the proteasome inhibitor carfilzomib or pharmaceutically acceptable salt thereof.
A pharmaceutical composition of Pemetrexed represented by formula (I), which is a liquid ready to use solution formulation or a lyophilized pharmaceutical composition for parenteral administration comprising a pharmaceutically acceptable organic amine, an inert gas and optionally containing at least one or more pharmaceutically acceptable excipients. Also provided are processes for preparation of the ready to use solution formulation or lyophilized pharmaceutical composition of the present invention.
The present invention relates to a process for the purification of Carfiizomib of Formula Ϊ that reduces the level of an acetaniide impurity of Formula II preferably below 0.10 wt%. Formula I Formula II.
An improved process for the preparation of Pralatrexate which is less hazardous. The invention further relates to novel intermediates and process thereof useful for the preparation of Pralatrexate. The present invention also relates to a substantially pure Pralatrexate and a process for obtaining the same in high yield.
C07D 475/08 - Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
C07C 67/343 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisationPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by change of size of the carbon skeleton by increase in the number of carbon atoms
39.
Pharmaceutical compositions comprising pemetrexed and tromethamine
A pharmaceutical composition of Pemetrexed represented by formula (I),
which is a liquid ready to use solution formulation or a lyophilized pharmaceutical composition for parenteral administration comprising a pharmaceutically acceptable organic amine, an inert gas and optionally containing at least one or more pharmaceutically acceptable excipients. Also provided are processes for preparation of the ready to use solution formulation or lyophilized pharmaceutical composition of the present invention.
The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ≧99%, which is simple, convenient, economical, does not use hazardous chemicals and is industrially viable.
C07D 235/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
The present invention discloses a process for the preparation of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β,10β-dimethoxy-9-oxotax-11-en-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate Cabazitaxel (I).
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
42.
Process for preparing stable pharmaceutical compositions of compounds susceptible to hydrolysis
The present invention relates to a process of preparing a stable pharmaceutical composition of compounds which are susceptible to hydrolysis comprising a. Addition of required quantity of pharmaceutically acceptable lyophilization excipients optionally in Water for Injection in a formulation vessel; b. Addition of organic solvent to form a appropriate proportion of aqueous and organic solvent; c. Maintaining the temperature of the formulation vessel from the range −5±1° C. to −5±3° C.; d. Addition of required quantity of compound susceptible to hydrolysis to form a solution and lyophilizing the solution.
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ≧99%, which is simple, convenient, economical, does not use hazardous chemicals and is industrially viable.
C07D 235/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
44.
STABLE PHARMACEUTICAL COMPOSITION OF 5-ΑΖΑ-2'ΡΕΟΧΥΟΤΙΡΙΝΕ
The present invention relates to ready to use, non aqueous pharmaceutical compositions comprising 5-aza-2'deoxycitidine and at least one aprotic solvent. The pharmaceutical compositions may further comprise at least one protic solvent. The present invention also relates to process for preparing pharmaceutical compositions and their use for the treatment of patients suffering from myelodysplastic syndromes.
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
The present invention discloses a process for the preparation of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β,10β-dimethoxy-9-oxotax-11-en-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate Cabazitaxel (I).
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
46.
PROCESS FOR THE PREPARATION OF PYRAZOLE SUBSTITUTED AMINOHETEROARYL COMPOUNDS
The present invention relates to an improved process for the preparation of pyrazole substituted aminoheteroaryl compounds. More particularly, the present invention provides highly pure 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4- yl)pyridin-2-amine, its intermediates and preparation thereof. The process of the present invention is simple, convenient, does not use expensive chemicals and avoids use of tedious purification techniques. Invention also provides process intermediates, useful not only in the synthesis, but also useful for providing desired compound with high purity.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
The present invention provides salts of Pralatrexate, in particular, sodium, lithium and potassium salts and their polymorphic forms, process for the preparation thereof, pharmaceutical compositions comprising these salts and at least one pharmaceutically acceptable excipient, and the use of pharmaceutical composition for the treatment of conditions related to human tumors.
C07D 475/08 - Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
An improved process for the preparation of Pralatrexate which is less hazardous. The invention further relates to novel intermediates and process thereof useful for the preparation of Pralatrexate. The present invention also relates to a substantially pure Pralatrexate and a process for obtaining the same in high yield.
C07D 475/08 - Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
A pharmaceutical composition of Pemetrexed represented by formula (I), which is a liquid ready to use solution formulation or a lyophilized pharmaceutical composition for parenteral administration comprising a pharmaceutically acceptable organic amine, an inert gas and optionally containing at least one or more pharmaceutically acceptable excipients. Also provided are processes for preparation of the ready to use solution formulation or lyophilized pharmaceutical composition of the present invention.
A stable ready-to-use pharmaceutical composition comprising pemetrexed or pharmaceutically acceptable salts thereof, wherein the composition is free from antioxidants, amino acids and chelating agents. Also provided is a process for preparing a stable ready-to-use pharmaceutical composition comprising the steps: i) purging inert gas into a parenterally acceptable aqueous solvent until the dissolved oxygen content of the solvent comes to less than 7 mg/L, preferably less than 3 mg/L; ii) adding pemetrexed disodium under stirring; iii) adjusting the pH of the resulting solution to between 4 to 9; iv) optionally adding additional aqueous solvent; wherein the composition is purged with inert gas throughout the entire process.
An improved process, which is simple, convenient, economical and industrially viable, for the preparation of stable, free flowing, non-hygroscopic crystalline alpha form of Imatinib mesylate, free from the beta form. The process comprises a) providing a clear solution of imatinib base in organic solvent; b) optionally, filtering the solution to remove any insoluble impurity; c) adding another organic solvent to the solution of step (b) and heating to obtain a clear solution; d) adding solution of methane sulfonic acid in second organic solvent slowly to the solution of step (c) on heating; e) cooling of the reaction mixture obtained in step (d) followed by seeding of the clear solution with pure alpha crystalline form of Imatinib mesylate on heating; f) slowly cooling of the reaction mixture; g) isolating the imatinib mesylate alpha form; wherein the organic solvent is selected from the group comprising of N, N-dimethyl sulphoxide, Isopropanol and mixtures thereof.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
52.
Crystalline forms of cabazitaxel and process for preparation thereof
The present invention provides Crystalline Forms of 4-acetoxy-2α-benzoyloxy-5β-20-epoxy-1-hydroxy-7β,10β-dimethoxy-9-oxotax-11-en-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate, i.e Cabazitaxel. The present invention also discloses methods for the preparation of Crystalline Forms of Cabazitaxel and pharmaceutical compositions thereof.
C07D 321/00 - Heterocyclic compounds containing rings having two oxygen atoms as the only ring hetero atoms, not provided for by groups
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
53.
PROCESS FOR PREPARING STABLE PHARMACEUTICAL COMPOSITIONS OF COMPOUNDS SUSCEPTIBLE TO HYDROLYSIS
The present invention relates to a process of preparing a stable pharmaceutical composition of compounds which are susceptible to hydrolysis comprising a. Addition of required quantity of pharmaceutically acceptable lyophilization excipients optionally in Water for Injection in a formulation vessel; b. Addition of organic solvent to form a appropriate proportion of aqueous and organic solvent; c. Maintaining the temperature of the formulation vessel from the range -5±1°C to - 5±3°C; d. Addition of required quantity of compound susceptible to hydrolysis to form a solution and lyophilizing the solution.
A61K 9/19 - Particulate form, e.g. powders lyophilised
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
54.
CRYSTALLINE FORMS OF CARBAZITAXEL AND PROCESS FOR PREPARATION THEREOF
The present invention discloses Crystalline Forms of 4-acetoxy-2α-benzoyIoxy- 5β-20-epoxy-1-hydoxy-7β, 10β-dimethoxy-9-oxotan-11-en-13α-y1(2R,3S)-3-tert- butoxycarbony lamino-2-hydoxy-3-phenylpropionate, i.e Cabazitaxel, methods for its preparation and Pharmaceutical compositions thereof.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
C07D 405/02 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
56.
PROCESSES FOR THE PREPARATION OF CABAZITAXEL INVOLVING C(7) -OH AND C(13) -OH SILYLATION OR JUST C(7) -OH SILYLATION
Disclosed are processes towards Cabazitaxel (I) starting from 10-Deacetylbaccatin (III) that involve steps of either 7-OH monosilylation (passing through formula V) or 7,13-disilylation (passing through formulae XI, XII). Isopropanol Solvates of Cabazitaxel and processes to make this are also described.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
57.
AMORPHOUS FORM OF CABAZITAXEL AND PROCESS FOR ITS PREPARATION
An Amorphous Form of Cabazitaxel is disclosed. It is preferably characterized by an X-ray powder diffraction (XRD) pattern as depicted in Fig-1. It is prepared by (a) preparing a solution of Cabazitaxel in a suitable solvent and mixture thereof; and (b) recovering the Amorphous Forms of Cabazitaxel from the solution thereof by removal of the solvent.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
58.
AN IMPROVED PROCESS FOR THE PREPARATION OF BENDAMUSTINE HYDROCHLORIDE
The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1 -Methyl-5-[bis(2-chloroethyl)amino]- 1H-benzimidazol-2-yl]lithium butanoate of formula(V), both having a purity of ≥99%, which is simple, convenient, economical, does not use hazardous chemicals and industrially viable.
C07D 235/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
improved process for the preparation of Pemetrexed of Formula (I) or its salt, the process comprises Reacting 4-(2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)- ethyl) benzoic acid with L-glutamic acid or its ester, or its acid salt, in the presence of acid activating reagent having carbodiimide group, to obtain Pemetrexed Diester; hydrolysis of the same to obtain Pemetrexed; and optionally converting Pemetrexed to Pemetrexed disodium.
A stable pharmaceutical compositions of Rapamycin Esters, in particular Rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid that is free of antioxidants and a process of preparing the same.
A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
61.
PROCESS FOR THE PREPARATION OF TEMSIROLIMUS AND ITS INTERMEDIATES
Intermediates, process for their preparation and their use in the preparation of therapeutically effective antineoplastic agents, in particular Temsirolimus of formula (I).
16 - Paper, cardboard and goods made from these materials
20 - Furniture and decorative products
Goods & Services
Paper, cardboard and goods made from these materials, not included in other classes; Printed matter; book binding material; photographs; Stationery; adhesives for stationery or household purposes; Artists' materials; paint brushes; typewriters and office requisites (except furniture); instructional and teaching material (except apparatus); plastic materials for packaging (not included in other classes); printers' type; Printing blocks; plastic packaging. Containers of plastic (packaging).
63.
AN IMPROVED PROCESS FOR PREPARATION OF LETROZOLE AND ITS INTERMEDIATES
The present invention relates to an improved process for preparation of the non-steroidal aromatase inhibitor drug, Letrozole of formula (I) and its intermediates, 4-[1-(1,2,4-triazolyl) methyl]-benzonitrile of formula (IV) and 4-[1-(1,2,4-triazolyl) methyl]-benzonitrile hydrochloride of formula (VII), all having a purity of ≥99%, which is simple, convenient, economical, does not use hazardous chemicals and industrially viable.
Concentrates or proliposomal compositions of poorly water-soluble drugs and compounds, comprising of one or more membrane forming lipids, a membrane stabilizing agent, in a suitable vehicle, and optionally containing a Polyethylene Glycol (PEG)-coupled phospholipid or a mixture thereof and further, optionally containing pharmaceutically acceptable excipients such as antioxidants, buffering agents, acidifying agents etc. are provided, which have superior long term stability. The concentrates of proliposomal compositions instantly form liposomes of the said poorly water-soluble drugs and compounds on rapid injection to a diluting fluid, the liposomal composition so obtained, characterized by a physical stability more than 24 hours, ≥ 95% drug encapsulation and having a particle size diameter of less than 100 nm. The liposomal compositions so obtained can further be directly administered to patients in need of treatment of the poorly water-soluble drugs and compounds.
A crystalline Temozolomide Monohydrate. A process for preparing the same comprising: i) dissolving Temozolomide, having a purity of 50-70% in acetone at a temperature of about 50-55°C; ii) optionally adding activated carbon to the solution of step i); iii) filtering the activated carbon from the mixture of step ii); iv) evaporating the filtrate of step iii) to obtain a solid substance; v) dissolving the solid substance obtained in step iv) in a mixture of acetone and water in the ratio of 3:1 v/v at a temperature from about 50°C to reflux temperature; vi) optionally adding activated carbon to the solution of step v); vii) cooling the mixture of step vi) to ambient temperature; viii) filtering the activated carbon from the mixture of step vii); ix) cooling the filtrate of step viii) to a temperature of 0-5 °C and collecting the crystals and drying the filtrate of step viii) to give the crystalline Temozolomide Monohydrate.
