The present invention relates to novel pharmaceutical composition comprising meloxicam for the treatment of acute pain, wherein the composition comprises at least a hydrophilic polymer and one or more alkalizing agents or combinations thereof.
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
The present disclosure relates to crystalline forms of mitapivat, amorphous mitapivat mono sulfate, crystalline forms of mitapivat mono sulfate, and crystalline forms of mitapivat hemi sulfate. The present disclosure also relates to process for the preparation of crystalline forms of mitapivat, mitapivat hemi sulfate, mitapivat mono sulfate and amorphous mitapivat mono sulfate.
The present invention provides a crystalline Form M1 of Larotrectinib sulfate and process for the preparation of the same optionally in presence of a coformer.
A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
9.
AN IMPROVED PROCESS FOR THE PREPARATION OF EDOXABAN INTERMEDIATE
The present invention relates to an improved process for the preparation of Edoxaban intermediate and further preparation of Edoxaban or its pharmaceutically acceptable salts.
The present invention provides crystalline polymorphic Form M1, M2, M3, M4, M5 and M6 of Ozanimod hydrochloride. It also provides process for the preparation of the same.
The present invention provides Cocrystal of Roxadustat Nicotinamide Form II and Cocrystal of Roxadustat Nicotinamide Form III, processes for their preparation and pharmaceutical composition thereof.
C07C 235/60 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho- position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
15.
METHODS AND INTERMEDIATES FOR PREPARING HYDROCHLORIDE SALT OF 5-[3-(3-HYDROXYPHENOXY)AZETIDIN-1-YL]-5-METHYL-2,2-DIPHENYLHEXANAMIDE
Methods for providing a carboxamide compound and intermediates used in the preparation of the carboxamide compound are provided. The methods include reacting 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanenitrile benzoate with a reagent and hydrochloric acid to form the carboxamide compound including 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide hydrochloride.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
The present invention provides polymorphic forms namely crystalline Form I, amorphous form and amorphous solid dispersions of Sacubitril-Telmisartan. It also provides process for the preparation of the same.
C07D 235/20 - Two benzimidazolyl-2 radicals linked together directly or via a hydrocarbon or substituted hydrocarbon radical
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
17.
A PROCESS FOR THE PREPARATION OF LAROTRECTINIB OR ITS SALTS
The present invention provides a process for the preparation of Larotrectinib or its pharmaceutically acceptable salts with a key intermediate of Formula IV by using Formula IIa.
A process for the preparation of Abaloparatide or pharmaceutically acceptable salts. Also described is pure Abaloparatide or pharmaceutically acceptable salts thereof obtained from the process for the preparation of Abaloparatide.
The present invention relates to novel pharmaceutical composition comprising meloxicam for the treatment of acute pain, wherein the composition comprises at least a hydrophilic polymer and one or more alkalizing agents or combinations thereof.
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
The present invention relates to novel pharmaceutical composition comprising meloxicam for the treatment of acute pain, wherein the composition comprises at least a hydrophilic polymer and one or more alkalizing agents or combinations thereof.
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61K 31/38 - Heterocyclic compounds having sulfur as a ring hetero atom
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
The present invention provides an improved process for the preparation of upadacitinib of intermediate of formula II by reacting formula B with Grignard reagent in presence of an Iron catalyst.
C07D 207/20 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
Co-crystals of meloxicam co-formers can be prepared by co-crystallization from a polar solvent, such as aqueous dimethyl sulfoxide; or by slurry processes, such as with ethyl acetate. Such co-crystals have improved purities and are physically stable under storage for several months.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur 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
24.
COMBINATION ANTIBACTERIAL COMPOSITION AND METHOD FOR ANTIBACTERIAL THERAPY
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
25.
IMPROVED PROCESS FOR THE PREPARATION OF ROXADUSTAT
A synthetic route for the preparation of Roxadustat, or a pharmaceutically acceptable salt thereof. Each route involves several novel intermediates and avoids the use of column chromatography.
Methods for providing a carboxamide compound and intermediates used in the preparation of the carboxamide compound are provided. The methods include reacting 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanenitrile benzoate with a reagent and hydrochloric acid to form the carboxamide compound including 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide hydrochloride.
The present invention relates to an improved process for the preparation of Valbenazine tosylate. Further the present invention relates to crystalline acid addition salts of Valbenazine and their preparation thereof.
The present invention provides an improved process for the preparation Upadacitinib by using novel intermediates. The present invention also provides processes for the preparation of novel intermediates of Upadacitinib.
"Co-crystal of Roxadustat" The present invention relates to D-proline Co-crystal of Roxadustat having improved stability and suitable for commercial development. The invention also relates to process for the preparation of D- proline Co-crystal of Roxadustat. The invention further relates to pharmaceutical composition comprising of D-proline Co-crystal of Roxadustat. The invention further relates to Roxadustat D-proline is free of photoisomer.
The present disclosure relates to an improved process for the preparation of bedaquiline fumarate, comprising a step of preparing bedaquiline by reaction of 3-benzyl-6-bromo-2-methoxyquinoline 5 with 3-(dimethylamino)-l-(naphthalen-l-yl)propan-l-one 4 in the presence of lithium pyrrolidide.
C07C 233/83 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
42.
POLYMORPHIC FORMS 5-[3-[(1S)-2,3-DIHYDRO-1-[(2-HYDROXYETHYL) AMINO]-1H-INDEN-4-YL]-1,2,4-OXADIAZOL-5-YL]-2-(1-METHYLETHOXY)BENZONITRILE
The present invention provides an amorphous form of (rac)-tramadol.HCl-celecoxib (1:1) and a solid dispersion and processes for the preparation of the same.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07C 217/74 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
A61K 9/00 - Medicinal preparations characterised by special physical form
Co-crystals of meloxicam co-formers can be prepared by co-crystallization from a polar solvent, such as aqueous dimethyl sulfoxide; or by slurry processes, such as with ethyl acetate. Such co-crystals have improved purities and are physically stable under storage for several months.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur 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
Described is a process for the preparation of crystalline Form C of Vadadustat. Also described are Vadadustat co-crystals and processes for the preparation thereof.
C07D 473/12 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1, 3, and 7, e.g. caffeine
The present invention relates generally to pharmaceutically active compounds and more specifically to crystalline Form M1 of Avatrombopag, crystalline Form M2 of Avatrombopag, crystalline Form M3 of Avatrombopag, crystalline Form M4 of Avatrombopag, crystalline Form M5 of Avatrombopag, crystalline Form M1 of Avatrombopag maleate, crystalline Form M2 of Avatrombopag maleate, crystalline Form M3 of Avatrombopag maleate, amorphous Avatrombopag, amorphous Avatrombopag maleate, amorphous solid dispersions of Avatrombopag maleate and processes for the preparation thereof.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
The present invention provides a novel 1:1 co-crystal of (rac)-tramadol hydrobromide-celecoxib and processes for the preparation of the same by reacting (rac)-tramadol with hydrobromic acid and celecoxib. It also provides crystalline form of (rac)-tramadol hydrobromide.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07C 217/74 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
The present invention provides a novel 1:1 co-crystal of (rac)-tramadol hydrobromide-celecoxib and processes for the preparation of the same by reacting (rac)-tramadol with hydrobromic acid and celecoxib. It also provides crystalline form of (rac)-tramadol hydrobromide.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07C 217/74 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
The present disclosure provides methods for purified Plecanatide by a two-step purification method, novel intermediates that may be used in the preparation of Plecanatide, and purified Plecanatide compositions.
The present disclosure provides crystalline forms of bictegravir, amorphous bictegravir sodium, amorphous solid dispersion of bictegravir sodium with pharmaceutically acceptable carrier and processes for the preparation thereof.
A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
The present invention provides, crystalline Form M1, Form M2 and Form M3 of Rucaparib (S)-camsylate salt. It also provides crystalline Form M1, Form M2, Form M3, Form M4 and Form M5 of Rucaparib and processes for the preparation of the same.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present disclosure provides crystalline forms of bictegravir, amorphous bictegravir sodium, amorphous solid dispersion of bictegravir sodium with pharmaceutically acceptable carrier and processes for the preparation thereof.
A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
The present invention relates to process for the preparation of Abametapir. The present 5 invention further relates to Abametapir salts and their preparation thereof.
Sotagliflozin may be prepared using schemes and intermediates disclosed herein. Sotagliflozin may be incorporated into pharmaceutical dosage forms for treatment of diabetes.
Crystalline Form M1 of deutetrabenazine is provided along with methods of its preparation. Deutetrabenazine may be useful in the treatment of a VMAT2-mediated disease and thus crystalline Form M1 of deutetrabenazine may be incorporated into suitable dosage forms for administration to a patient.
C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
The present disclosure relates to crystalline forms of venetoclax and process for their preparation. The present disclosure also relates to process for preparation of amorphous venetoclax.
The present invention relates to crystalline forms of venetoclax and process for their preparation. The present invention also relates to process for preparation of amorphous venetoclax.
A61K 31/437 - 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
The present invention discloses Novel polymorphs of Apalutamide and process for their preparation. The present invention further disclose processes for the preparation of amorphous and amorphous solid dispersion of Apalutamide. Formula (I).
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
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
61.
METHODS AND INTERMEDIATES FOR PREPARING DEUTETRABENAZINE
Disclosed is a process for the preparation of deutetrabenazine and intermediates useful in the preparation thereof. Disclosed are also process for making amorphous deutetrabenazine.
The present invention relates to a process for preparing rucaparib or pharmaceutically acceptable salts thereof. It also provides novel intermediates that may be converted into rucaparib or pharmaceutically acceptable salts thereof.
The present disclosure provides novel polymorphs of abemaciclib, solid dispersions of abemaciclib with pharmaceutical excipients, and processes for the preparation thereof. The disclosure further provides methods for preparing crystalline abemaciclib form I, amorphous abemaciclib, and methods for synthesizing abemaciclib.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present disclosure provides novel crystalline sofosbuvir form-M3 and a process for the preparation of sofosbuvir form-M3. The crystalline sofosbuvir form-M3 disclosed herein may be useful in the formulation of pharmaceutical dosage forms.
C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
A61K 31/7072 - 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 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
C07H 1/00 - Processes for the preparation of sugar derivatives
The present disclosure provides amorphous lumacaftor, amorphous solid dispersions of lumacaftor, crystalline lumacaftor acetic acid solvate, crystalline lumacaftor ethyl acetate solvate, and processes for the preparation thereof. The lumacaftor forms disclosed herein may be useful for the preparation of oral dosage forms for treating cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases.
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
The present disclosure provides crystalline forms of baricitinib (formula (I)), crystalline forms of solvates of baricitinib and processes for the preparation thereof.
Disclosed herein is a process for the preparation of betrixaban hydrochloride and a process for the preparation of betrixaban maleate from betrixaban hydrochloride salt.
The present invention relates to an improved process for the preparation of Iron dextran & Sodium ferric gluconate, which is reproducible, easy to prepare on an industrial scale, and consistent in molecular weight range.
The present disclosure provides a process for the preparation of velpatasvir intermediates. The intermediates may be further converted to velpatasvir or pharmaceutically acceptable salts thereof.
C07C 45/63 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by introduction of halogenPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by substitution of halogen atoms by other halogen atoms
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
C07C 45/45 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by condensation
70.
NOVEL POLYMORPHS OF (5-[3-(3-HYDROXYPHENOXY)AZETIDIN-1-YL]-5-METHYL-2,2-DIPHENYLHEXANAMIDE HYDROCHLORIDE
The present disclosure provides solid forms of the hydrochloride salt of (5-[3-(3-Hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide (Compound-A). In particular, an amorphous form, an ethyl acetate solvate form, a methyl n-butyl ketone solvate form, an anisole solvate form, an isobutyl acetate solvate form, a n-butyl acetate solvate form, a toluene solvate form, a 4-methyl-2-pentanol solvate form, a n-propyl acetate solvate form, a xylene solvate form, Form VIII and Form IX of the salt are disclosed. Processes for the preparation of each of the disclosed forms are also provided.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
A61P 11/00 - Drugs for disorders of the respiratory system
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
71.
IMPROVED PROCESS FOR THE PREPARATION OF CHLORTHALIDONE
The present invention relates to methods for preparing chlorthalidone. In particular, the disclosed processes are feasible on an industrial scale and provide substantially pure chlorthalidone.
A process for the resolution of racemic 2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine using novel chiral salts is disclosed. An L-phenylalanine p-toluene-sulfonamide salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine and a di-p-toluoyl-L-tartaric acid salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine are also provided.
C07C 315/06 - SeparationPurificationStabilisationUse of additives
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
C07C 311/19 - 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 hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07C 69/76 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
C07C 315/04 - Preparation of sulfonesPreparation of sulfoxides by reactions not involving the formation of sulfone or sulfoxide groups
75.
AMORPHOUS OSIMERTINIB MESYLATE, PROCESSES FOR ITS PREPARATION AND SOLID AMORPHOUS DISPERSIONS THEREOF
The present disclosure provides amorphous osimertinib mesylate, amorphous solid dispersions of osimertinib mesylate, and processes for the preparation thereof. Amorphous osimertinib mesylate and solid dispersions thereof may be used to prepare pharmaceutical dosage forms.
An amorphous form of betrixaban maleate and process for the preparation of the same are disclosed. A solid dispersion of amorphous betrixaban maleate with pharmaceutically acceptable excipients and processes for the preparation of the same are also disclosed. Betrixaban base polymorphic forms and processes for preparing the same are also disclosed.
The present disclosure provides solid dispersions of trisodium sacubitril valsartan. Such solid dispersions may be useful in the manufacture of pharmaceutical dosage forms.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
The present disclosure relates to crystalline forms of venetoclax and process for their preparation. The present disclosure also relates to process for preparation of amorphous venetoclax.
The present disclosure provides a novel polymorph of an intermediate useful in the preparation of palbociclib. The polymorph has enhanced properties that influence process ability of the intermediate and synthesis of palbociclib.
The present disclosure provides novel synthetic process for the preparation of venetoclax. The disclosed processes involve the use of novel intermediates. Processes for the preparation of these intermediates are also disclosed as well as methods for the preparation of particularly useful salts thereof.
A61K 31/437 - 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
The invention provides a process for preparing a sterile suspension comprising aripiprazole. More particularly, the invention provides the process for preparing the sterile suspension comprising aripiprazole, wherein said process involves in-process moist-heat sterilization of said suspension comprising aripiprazole. The in-process moist-heat sterilization is particularly efficient and economical process for the sterilization of aripiprazole formulations for parenteral administration, wherein the formulation obtained by said process have comparable physicochemical characteristics with the commercially available Ability Maintena® Injection.
The present disclosure relates to crystalline forms of selexipag and their processes for preparation. The present disclosure also relates to an amorphous solid dispersion of selexipag and its processes for their preparation as well as premix of crystalline selexipag and their process.
Disclosed are compounds and methods for the preparation of Edoxaban. In particular, a camphor sulfonate salt of an amine-protected [(1R,2S,5S)-1,2-amino-5-[(dimethylamino)carbonyl] cyclohexane, an intermediate that may be formed in the synthesis of Edoxaban, is disclosed as well as methods of its preparation.
C07C 271/24 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
The present disclosure provides novel crystalline sofosbuvir form- M3 and a process for the preparation of sofosbuvir form-M3. The crystalline sofosbuvir form-M3 disclosed herein may be useful in the formulation of pharmaceutical dosage forms. Formula (1): Sofosbuvir
C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 1/00 - Processes for the preparation of sugar derivatives
A61K 31/7072 - 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 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
The present disclosure provides anamorphous solid dispersion of palbociclib and a process for the preparation thereof. The solid dispersions disclosed herein may be useful for pharmaceutical compositions or dosage forms.
The present disclosure provides crystalline carfilzomib form M1 and a process for the preparation thereof. Further disclosed are processes for the preparation of amorphous carfilzomib using crystalline form M1 as a starting material. The present disclosure also relates to an improved process for the preparation of carfilzomib.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
The present disclosure relates to amorphous and crystalline forms of 2-butenamide, N-[4- [(3-chloro-4-fluorophenyl)amino]7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-5 (dimethyl amino)-,(2E)-, (2Z)-2-butenedioate (1:2) (afatinib dimaleate). The present disclosure also relates to process for the preparation of amorphous and crystalline forms of afatinib dimaleate. Further, the present disclosure relates to solid dispersion of amorphous afatinib dimaleate and the crystalline form of afatinib.
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
88.
AN AMORPHOUS NINTEDANIB ESYLATE AND SOLID DISPERSION THEREOF
Nintedanib base polymorphic forms and processes for preparing the same. A process for the purification of nintedanib base is disclosed. An amorphous form of nintedanib and process for the preparation of the same are also disclosed. A solid dispersion of amorphous nintedanib with pharmaceutically acceptable excipients and processes for the preparation of the same are also disclosed.
A process for the preparation of intermediates 9, useful in the synthesis of sofosbuvir, as well as intermediates of formula [12] are disclosed herein.
The present disclosure provides a process for the preparation of velpatasvir intermediates of formula 5. The intermediates may be further converted to velpatasvir or pharmaceutically acceptable salts thereof.
C07C 45/63 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by introduction of halogenPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by substitution of halogen atoms by other halogen atoms
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
91.
Polymorphs of cabozantinib (S)-malate and cabozantinib free base
The present disclosure provides amorphous lumacaftor, amorphous solid dispersions of lumacaftor, crystalline lumacaftor acetic acid solvate, crystalline lumacaftor ethyl acetate solvate, and processes for the preparation thereof. The lumacaftor forms disclosed herein may be useful for the preparation of oral dosage forms for treating cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases.
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
93.
POLYMORPHS OF IXAZOMIB CITRATE AND PROCESSES FOR THE PREPARATION THEREOF
The present disclosure provides amorphous ixazomib citrate and processes for the preparation thereof. Crystalline form Ml, form M2, form M3, and form M4 of ixazomib citrate are also disclosed. The present disclosure also encompasses processes for the preparation of those crystalline forms.
The present disclosure provides processes for the preparation of brexpiprazole or pharmaceutically acceptable salts thereof. The present disclosure also provides intermediates useful in the preparation of brexpiprazole.
C07D 215/22 - Oxygen atoms attached in position 2 or 4
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
The present disclosure relates to processes for the preparation of lumacaftor useful for treating a cystic fibrosis transmembrane conductance regulator (CFTR)-mediated disease such as cystic fibrosis. The present disclosure also provides intermediates useful in the preparation of lumacaftor
C07D 317/46 - 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 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
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
The present disclosure provides processes for the preparation of amorphous daclatasvir dihydrochloride. The present disclosure also provides processes for the preparation of amorphous solid dispersion of daclatasvir dihydrochloride in at least one pharmaceutically acceptable carrier. Suitable pharmaceutically acceptable carriers include, but are not limited to, PLASDONETM S-630, polyvinylpyrrolidine K-30, β-cyclodextrin, and hydroxypropyl-β-cyclodextrin (HPBCD).
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
The present disclosure provides a novel process for the preparation of daclatasvir or pharmaceutically acceptable salts thereof using novel intermediates. Formula (I)
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
100.
PROCESS FOR THE ENANTIOMERIC RESOLUTION OF APREMILAST INTERMEDIATES
A process for the resolution of racemic 2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine using novel chiral salts is disclosed. An L-phenylalanine p-toluene-sulfonamide salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine and a di-p-toluoyl-L-tartaric acid salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine are also provided.
