The present invention is directed to Form A of monohydrate of calcium oxybate, a pharmaceutically acceptable composition thereof, its method of making, and use thereof.
C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
C07C 51/47 - SeparationPurificationStabilisationUse of additives by solid-liquid treatmentSeparationPurificationStabilisationUse of additives by chemisorption
A catalytic composition comprising a transition metal catalyst entrapped within a monounsaturated vinyl aromatic/polyunsaturated vinyl aromatic copolymer, such as a styrene-divinyl benzene copolymer, matrix. In addition, processes for decomposing organic materials in a highly alkaline environment, and for conducting organic coupling reactions employing such catalyst compositions are disclosed.
The present disclosure relates to novel co-crystals of savolitinib and processes for the preparation thereof. The present disclosure also relates to pharmaceutical compositions comprising the novel co-crystals of savolitinib and methods for treating disease using the form.
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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 disclosure relates to various crystalline forms of entinostat and to processes for their preparation, particularly Form A of entinostat compound with maleic acid, Form A of entinostat compound with succinic acid, Form B of entinostat compound with succinic acid, and Form C of entinostat compound with succinic acid. The present disclosure also relates to pharmaceutical compositions comprising any of these forms of entinostat and to use of these forms in preparing a medicament or in treating a disease.
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 237/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
6.
POLYMORPHS OF AVAPRITINIB AND METHODS FOR PREPARING THE POLYMORPHS
The present invention relates to crystalline and non-crystalline forms of avapritinib, to processes for their preparation, and to pharmaceutical compositions containing the crystalline or non-crystalline forms.
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
7.
PROCESSES FOR THE PREPARATION AND MANUFACTURE OF RELUGOLIX
Intermediates and processes for the preparation of Relugolix, and to pharmaceutical compositions containing Relugolix manufactured by the invented processes.
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 invention discloses polymorphs of bexagliflozin or hydraates of bexagliflozin, as crystalline solids, processes for the preparation of the polymorphs/hydrates of bexagliflozin as crystalline solids, pharmaceutical compositions comprising the bexagliflozin (hydrtate) polymorphs thereof and to methods of treatment of diabetes using the said compounds.
Anhydrous fruquintinib as amorphous or crystalline (Form 1) solids, co-crystals of fruquintinib and organic acids as crystalline solids and solvates of co-crystals of fruquintinib and organic acids as crystalline solids and processes for preparing thereof are described and characterized herein.
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
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention is directed to a solid-state DMF solvate of relugolix and to solid-state anhydrous forms of relugolix designated as Form A and Form C of anhydrous relugolix. The present invention is further directed to processes for the preparation of the solid-state DMF solvate of relugolix and each of Form A, Form B, and Form C of anhydrous relugolix. The present invention also is directed to pharmaceutical compositions comprising the DMF solvate of relugolix or Form A or Form C of anhydrous relugolix, and to a method for treating disease using the DMF solvate of relugolix or Form A or Form C of anhydrous relugolix.
The present invention provides processes for the preparation of a hydrochloric acid salt of compound of formula (2):
The present invention provides processes for the preparation of a hydrochloric acid salt of compound of formula (2):
The present invention provides processes for the preparation of a hydrochloric acid salt of compound of formula (2):
wherein:
R1 is selected from the group consisting of —H, an unsubstituted straight-chain C1-C20-alkyl, substituted straight-chain C1-C20-alkyl, unsubstituted branched-chain C1-C20-alkyl, substituted branched-chain C1-C20-alkyl, unsubstituted cyclic C3-C20-alkyl, and substituted cyclic C3-C20-alkyl; and
R2 is selected from the group consisting of an unsubstituted straight-chain C1-C20-alkyl, substituted straight-chain C1-C20-alkyl, unsubstituted branched-chain C1-C20-alkyl, substituted branched-chain C1-C20-alkyl, unsubstituted cyclic C3-C20-alkyl, substituted cyclic C3-C20-alkyl, unsubstituted —C1-20-alkyl-C3-20-cycloalkyl, substituted —C1-20-alkyl-C3-20-cycloalkyl, unsubstituted allyl and substituted allyl.
The present invention relates to a process for preparing trientine dihydrochloride as an active pharmaceutical ingredient (API). The present invention relates to a process for the preparation of trientine dihydrochloride with a pharmaceutical grade of purity. The invention also relates to novel intermediates used in the preparation of trientine dihydrochloride.
C07C 209/68 - Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
The present invention is directed to a novel compound, (4R)-1-((S)-1-carboxypropyl)-2-oxo-4-propylpyrrolidine-3-carboxylic acid, which can be used as an intermediate in the preparation of brivaracetam. The invention is also directed to a process of preparing (4R)-1-((S)-1-carboxypropyl)-2-oxo-4-propylpyrrolidine-3-carboxylic acid. Further, the invention is directed to a process of preparing (S)-2-((R)-2-oxo-4-propylpyrrolidin-1-yl)butanoic acid from (4R)-1-((S)-1-carboxypropyl)-2-oxo-4-propylpyrrolidine-3-carboxylic acid. (S)-2-((R)-2-oxo-4-propylpyrrolidin-1-yl)butanoic acid can also be used in a process of preparing brivaracetam.
C07D 207/277 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
The present disclosure relates to various solid-state forms of pracinostat dihydrochloride, including a dimethyl sulfoxide solvate, an amorphous form, a hydrated form and another solid-state form, and several co-crystal forms, and to processes for their preparation. The present disclosure also relates to pharmaceutical compositions comprising any of these forms of pracinostat dihydrochloride and to their use in a method for treating a disease.
The present invention is directed to processes for making an anhydrous form of relugolix, designated herein as Form T of anhydrous relugolix. The processes of making Form T of anhydrous relugolix are from the following: (i) Form A of the DMF solvate of relugolix; (ii) Form B of anhydrous relugolix; or (iii) amorphous relugolix.
The present invention relates to crystalline forms of voxelotor, to processes for their preparation, and to pharmaceutical compositions containing the crystalline forms.
A61K 47/54 - 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 organic compound
The present invention relates to crystalline forms of entrectinib, processes for their preparation, and to pharmaceutical compositions containing the crystalline forms.
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 invention relates to a crystalline molecular complex comprising:
(a) the herbicide pinoxaden, and
(b) a second herbicide selected from the group consisting of fluroxypyr, 2,4-dichlorophenoxyacetic acid, 2-methyl-4-chlorophenoxyacetic acid and 3,6-dichloro-2-methoxybenzoic acid.
The present invention relates to a crystalline molecular complex comprising:
(a) the herbicide pinoxaden, and
(b) a second herbicide selected from the group consisting of fluroxypyr, 2,4-dichlorophenoxyacetic acid, 2-methyl-4-chlorophenoxyacetic acid and 3,6-dichloro-2-methoxybenzoic acid.
The invention also relates to processes for the preparation of the crystalline molecular complex, a herbicidal composition comprising the crystalline molecular complex, and use of the herbicidal composition.
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A01N 37/40 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio-analogue, or a derivative thereof, and a singly bound oxygen or sulfur atom attached to the same carbon skeleton, this oxygen or sulfur atom not being a member of a carboxylic group or of a thio-analogue, or of a derivative thereof, e.g. hydroxy-carboxylic acids having at least one oxygen or sulfur atom attached to an aromatic ring system having at least one carboxylic group or a thio-analogue, or a derivative thereof, and one oxygen or sulfur atom attached to the same aromatic ring system
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
The present disclosure relates to various crystalline forms of entinostat and to processes for their preparation, particularly Form A of entinostat compound with maleic acid, Form A of entinostat compound with succinic acid, Form B of entinostat compound with succinic acid, and Form C of entinostat compound with succinic acid. The present disclosure also relates to pharmaceutical compositions comprising any of these forms of entinostat and to use of these forms in preparing a medicament or in treating a disease.
The present invention relates to a polymorph of venetoclax, to a process for its preparation, and to pharmaceutical compositions containing the polymorph.
The present invention relates to a crystalline molecular complex comprising metazachlor and a carboxylic acid. The invention also relates to a process for the preparation of the crystalline molecular complex, a herbicidal composition comprising the crystalline molecular complex, and use of the herbicidal composition.
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
The present invention relates to a crystalline molecular complex comprising pinoxaden and a carboxylic acid. The invention also relates to a process for the preparation of the crystalline molecular complex, a herbicidal composition comprising the crystalline molecular complex, and use of the herbicidal composition.
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
The present invention relates to additive layer manufacture methods for producing a cured three-dimensional polymerized object, or an object comprising cured polymer on, in and/or around the object, or part thereof. A bittering agent is distributed within the cured polymer.
B29C 64/135 - Processes of additive manufacturing using only liquids or viscous materials, e.g. depositing a continuous bead of viscous material using layers of liquid which are selectively solidified characterised by the energy source therefor, e.g. by global irradiation combined with a mask the energy source being concentrated, e.g. scanning lasers or focused light sources
The present disclosure is directed to amorphous umbralisib monotosylate, and to processes for its preparation; pharmaceutical compositions comprising amorphous umbralisib monotosylate; and to a method for treating a patient using amorphous umbralisib monotosylate.
C07D 211/66 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
The present invention provides a molecular complex of binimetinib, which is binimetinib dimethylsulfoxide (DMSO) solvate. It is also an object of the present invention to provide a molecular complex of binimetinib which is a crystalline molecular complex of binimetinib and citric acid. The present invention also relates to methods for the preparation of these molecular complexes.
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
27.
CRYSTALLINE FORMS OF VOXELOTOR, AND PROCESSES FOR THE PREPARATION THEREOF
The present application relates to crystalline forms of Voxelotor salts and to crystalline forms of a solvate of said compound, to processes for their preparation and to pharmaceutical compositions containing said crystalline forms.
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 disclosure relates to a stabilized anhydrous p-toluenesulfonic acid salt of niraparib, Form A. The present disclosure is also related to processes for the preparation of the stabilized anhydrous p-toluenesulfonic acid salt of niraparib. Further, the present disclosure also relates to pharmaceutical compositions comprising the stabilized anhydrous p-toluenesulfonic acid salt of niraparib and methods for treating disease using the stabilized anhydrous p-toluenesulfonic acid salt of niraparib.
C07D 401/02 - 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
C07D 401/10 - 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 linked by a carbon chain containing aromatic rings
C07C 309/30 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
The present disclosure relates to novel forms of fedratinib dihydrochloride (diHCl) and processes for the preparation of the various forms. The present disclosure also relates to pharmaceutical compositions comprising the novel forms of fedratinib dihydrochloride and methods for treating disease using the forms.
The present disclosure relates to Form Z of acetic acid solvated hydrate of ponatinib hydrochloride. The present disclosure is also related to processes for the preparation of Form Z of acetic acid solvated hydrate of ponatinib hydrochloride. Further, the present disclosure also relates to pharmaceutical compositions comprising Form Z of acetic acid solvated hydrate of ponatinib hydrochloride and methods for treating disease using Form Z of acetic acid solvated hydrate of ponatinib hydrochloride.
The present invention relates to a polymorph of venetoclax, to a process for its preparation, and to pharmaceutical compositions containing the polymorph.
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 disclosure relates to a dasatinib co-crystal form comprising dasatinib and a second compound, also referred to as a co-crystal former, wherein the second compound is selected from butyl paraben, propyl paraben and ethyl vanillin. The present disclosure is also related to an ethyl formate solvate form of dasatinib. The present disclosure is also related to processes for the preparation of the dasatinib co-crystal and solvate forms of dasatinib. Further, the present disclosure also relates to pharmaceutical compositions comprising the dasatinib co-crystal and solvate forms of dasatinib and methods for treating disease using the dasatinib co-crystal and solvate forms of dasatinib.
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
33.
Pyridine or N,N-dimethyl acetamide solvated solid state forms of solvated idelalisib, their use and preparation
The invention relates to a crystalline pyridine or N,N-dimethylacetamide solvated solid-state form of idelalisib (IDB). The invention is also directed to the preparation of the aforesaid solvated solid-state forms of IDB. Furthermore, the invention is directed to the use of the aforesaid solvated solid-state forms of IDB.
The invention relates to a crystalline methanol or dimethyl sulfoxide solvated form of regadenoson and an anhydrous polymorph of regadenoson. The invention is also directed to the preparation of the methanol or dimethyl sulfoxide solvated and anhydrous solid-state forms of regadenoson. In particular, the invention relates to the preparation of the anhydrous polymorph of regadenoson in a stable form from the dimethyl sulfoxide solvated form of regadenoson, which preparation is purifiable and scalable.
The present invention is directed to selinexor co-crystal forms; more particularly to two co-crystal forms with succinic acid as the coformer and a co-crystal form with vanillin as the coformer. The present disclosure is also related to processes for the preparation of selinexor co-crystal forms. Further, the present invention also relates to pharmaceutical compositions comprising a selinexor co-crystal form and method for treating disease using a selinexor co-crystal form.
C07D 403/12 - 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 linked by a chain containing hetero atoms as chain links
36.
Hydrogenation process for preparing oxycodone hydrochloride from 14-hydroxycodeinone
A process for preparing oxycodone hydrochloride, said process comprising hydrogenating 14-hydroxycodeinone in an alcoholic solvent and hydrochloric acid to form oxycodone hydrochloride, wherein (a) the hydrogenation is carried out in the presence of a heterogeneous platinum group metal (PGM) catalyst and hydrogen gas, (b) the hydrogenation is carried out at one or more temperatures greater than ambient temperature in the presence of a hydrogenation catalyst and hydrogen gas, wherein the solution of 14-hydroxycodeinone and hydrochloric acid is heated to temperature before it is exposed to the hydrogen gas, (c) the oxycodone hydrochloride comprises 6a-oxycodol in an amount
The present disclosure is directed to a crystalline, hydrated form of afatinib dimaleate having about 2 to 3 molecules of water, designated as Form Z, a pharmaceutical composition comprising the form, its method of use for treating a patient, and process for its preparation.
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 is directed to novel forms of apremilast and pharmaceutical compositions comprising any of the novel forms of apremilast. Also provided are processes for the preparation of novel forms of apremilast.
Improved processes for making opioid products having low impurity levels including making 14-hydroxycodeinone and 14-hydroxymorphinone from thebaine and oripavine, respectively.
Improved processes for making opioid products having low impurity levels including making 14-hydroxycodeinone and 14-hydroxymorphinone from thebaine and oripavine, respectively.
A process for preparing oxycodone hydrochloride, said process comprising hydrogenating 14- hydroxycodeinone in an alcoholic solvent and hydrochloric acid to form oxycodone hydrochloride, wherein (a) the hydrogenation is carried out in the presence of a heterogeneous platinum group metal (PGM) catalyst and hydrogen gas, (b) the hydrogenation is carried out at one or more temperatures greater than ambient temperature in the presence of a hydrogenation catalyst and hydrogen gas, wherein the solution of 14- hydroxycodeinone and hydrochloric acid is heated to temperature before it is exposed to the hydrogen gas, (c) the oxycodone hydrochloride comprises 6a-oxycodol in an amount < about 0.300 area % as determined by HPLC, characterized in that (d) the pH of the solution of 14-hydroxycodeinone and hydrochloric acid is in the range of about ≥ 2.5 to about ≤4.5; (e) the process is carried out in one pot, and (f) the oxycodone hydrochloride precipitates out of the solution.
An alkyl ester of 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid, such as ethyl 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoate, is obtained by reacting an alkyl ester of 4-(5-amino-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid with 2-hydroxyacetaldehyde under reducing conditions.
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
43.
Processes for making alkylated arylpiperazine and alkylated arylpiperidine compounds including novel intermediates
Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively
5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.
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
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
C07D 215/22 - Oxygen atoms attached in position 2 or 4
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 471/12 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains three hetero rings
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
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
C07C 39/00 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
C07D 417/08 - 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 carbon chain containing alicyclic rings
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
C07D 209/56 - Ring systems containing three or more rings
C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
C07D 401/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 403/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 275/06 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
C07D 311/20 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 hydrogenated in the hetero ring
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 311/06 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
The present disclosure is directed to novel forms of apremilast and pharmaceutical compositions comprising any of the novel forms of apremilast. Also provided are processes for the preparation of novel forms of apremilast.
C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Chemical preparations and substances used to denaturise other chemical substances by rendering them unsuitable for human and animal consumption; fertilisers
(2) All purpose vehicle cleaning preparations, windscreen cleaning preparations
(3) Preparations for destroying vermin; preparations for repelling animals, birds and insects, for use in deterring animals, birds and insects from grazing, eating or damaging plants, trees and the like, manmade structures; pesticides, insecticides and acaricides
The present disclosure is directed to crystalline forms of morphine sulfate and pharmaceutical compositions comprising any of the crystalline forms of morphine sulfate. Also provided are processes for the preparation of crystalline forms of morphine sulfate.
An improved method for the preparation of the low ABUK oxymorphone hydrochloride is provided. The oxymorphone hydrochloride is produced by hydrogenating a starting material comprising oxymorphone base and 14-hydroxymorphinone in a mixture comprising an alcohol, water and an acid, removing some of the water and adding more alcohol to the mixture.
The present invention provides processes for preparing morphinan-6-one compounds, in particular oxymorphone and salts thereof, having improved impurity profiles.
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
A method of preparing purified decitabine comprises mixing crude decitabine with solvent, such as dimethylacetamide, to form a solution or suspension and forming the purified decitabine from the solution or suspension. The forming step comprises adding an anti-solvent, such as ethanol, to the solution or suspension. The forming step may further comprise after adding ethanol to provide a mixture of dimethylacetamide and ethanol: cooling the mixture; isolating the solid decitabine present in the cooled mixture; and evaporating residual dimethylacetamide and ethanol from the solid decitabine to provide the purified decitabine. The mixture of dimethylacetamide and ethanol may be heated. The purification method preferably results in decitabine having a ratio of the β-anomer of decitabine to the α-anomer of decitabine of at least about 99.9:0.1.
Improved processes for making hydrocodone and hydromorphone as well as their 8,14-dihydrothebaine and 8,14-dihydrooripavine derivatives and salts are disclosed.
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
Improved processes for making hydrocodone and hydromorphone as well as their 8,14-dihydrothebaine and 8,14-dihydrooripavine derivatives and salts are disclosed.
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively
5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.
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
C07D 209/56 - Ring systems containing three or more rings
C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
C07D 401/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 403/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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
C07D 417/08 - 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 carbon chain containing alicyclic rings
C07D 275/06 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
C07D 311/20 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 hydrogenated in the hetero ring
C07D 311/06 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
C07D 215/22 - Oxygen atoms attached in position 2 or 4
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 471/12 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains three hetero rings
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
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
C07C 39/00 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
C07D 295/135 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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
Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques.
C07C 211/00 - Compounds containing amino groups bound to a carbon skeleton
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
C07C 229/42 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
C07C 225/22 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
C07C 227/22 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from lactams, cyclic ketones or cyclic oximes, e.g. by reaction involving Beckmann rearrangement
The present disclosure is directed to crystalline forms of morphine sulfate and pharmaceutical compositions comprising any of the crystalline forms of morphine sulfate. Also provided are processes for the preparation of crystalline forms of morphine sulfate.
Improved processes for making hydrocodone and hydromorphone as well as their 8,14-dihydrothebaine and 8,14-dihydrooripavine derivatives and salts are disclosed.
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
The present disclosure is directed to crystalline forms of oxymorphone hydrochloride and compositions comprising any of the crystalline forms of oxymorphone hydrochloride. Also provided are processes for the preparation of crystalline forms of oxymorphone hydrochloride.
A composition comprising a high purity cannabinoid, an acid, and a pharmaceutically-acceptable solvent achieves room temperature stability for over 24 months. The acid improves the stability of the composition and the solvent enhances the solubility of the acid, thereby allowing the acid to have an improved stabilizing effect on the highly pure cannabinoid. Preferably, the solvent is an alcohol and, more preferably, the composition contains an oil. A method for making the composition includes combining the cannabinoid and the solvent and evaporating a portion of the solvent, along with adding an acid to the composition, before, during, or after the evaporating step. A method for making and storing the composition includes storing the composition in a manner adapted to maintain its stability. Pharmaceutical dosage forms include a formulated composition, such as having the oil. A method of treating a subject comprises administering to the subject the dosage form.
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
B67B 3/00 - Closing bottles, jars, or similar containers by applying caps
B67C 3/00 - Bottling liquids or semiliquidsFilling jars or cans with liquids or semiliquids using bottling or like apparatusFilling casks or barrels with liquids or semiliquids
The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.
C07C 69/74 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
C07D 307/937 - Not further condensed cyclopenta [b] furans or hydrogenated cyclopenta [b] furans with hydrocarbon or substituted hydrocarbon radicals directly attached in position 2, e.g. prostacyclins
C07C 69/732 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids
C07C 323/56 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
60.
Process for the preparation of oxymorphone alkaloid and oxymorphone salts
The present invention provides a process for preparing an oxymorphone acid adduct, said process comprising hydrogenating an aqueous solution of 14-hydroxymorphinone and an acid to form a solution of the oxymorphone acid adduct, wherein the hydrogenation is carried out at one or more temperatures greater than 40° C. in the presence of a hydrogenation catalyst and hydrogen gas, wherein the level of 6α-oxymorphol produced is ≦3.00 area % as determined by HPLC.
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
61.
PROCESS FOR THE PREPARATION OF MORPHINAN-6-ONE COMPOUNDS
The present provides a process for preparing a compound of formula (3), the process comprising the steps of: (a) providing an aqueous acidic solution comprising a compound of formula (1) and, as an impurity, a compound of formula (2); and (b) treating the aqueous acidic solution of step (a) such that the compound of formula (2) dehydrates to form a compound of formula (1) and the compound of formula (1) is reduced to form an aqueous acidic solution of the compound of formula (3), wherein: the treating of step (b) is carried out at one or more temperatures greater than ambient in the presence of a hydrogenation catalyst and hydrogen gas; and wherein for the compounds of formulae (1), (2) and (3): i) R1 is -OH, R2 is-OH and R3-H; or ii) R1 is -OCH3, R2 is -H and R3 -CH3; or iii) R1 is-OH, R2 is-H and R3-CH3; or iv) R1, is -OCH3, R2 is -H and R3 -H; or v) R1, is -OH, R2is-H and R3-H; or vi) R1, is -OCH3, R2 is -OH and R3 -H.
Wet bendamustine hydrochloride monohydrate may be dried by a two stage process wherein rapid drying is first carried out to provide a partially dried product, which is then further dried using an inert gas of controlled relative humidity to yield dry bendamustine hydrochloride monohydrate.
C07D 235/12 - Radicals substituted by oxygen atoms
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
63.
Morphine sulfate methanolic solvate, processes for making same and related compositions and methods for treating pain
Processes for reducing the amount of impurities, especially α,β-unsaturated ketones (ABUK), in materials containing morphine. Novel compounds, namely low ABUK morphine sulfate methanolic solvate, and a novel crystal form are also described. The method for making morphine sulfate methanolic solvate comprises mixing a morphine free base composition with methanol to form a solution and adding a liquid comprising sulfuric acid to the solution to form a morphine sulfate methanolic solvate precipitate. A method of making a morphine sulfate compound comprises drying the morphine sulfate methanolic solvate in the presence of water vapor, such that methanol molecules are removed and replaced with water vapor molecules. A composition for treating pain comprises the morphine sulfate compound and at least one pharmaceutically acceptable excipient. A method for treating pain comprises administering to a patient in need thereof the composition comprising the morphine sulfate compound and at least one pharmaceutically acceptable excipient.
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
The present invention provides a process for preparing an oxycodone acid adduct, said process comprising hydrogenating an aqueous solution of 14-hydroxycodeinone and an acid to form a solution of the oxycodone acid adduct, wherein the hydrogenation is carried out at one or more temperatures greater than ambient temperature in the presence of a hydrogenation catalyst and hydrogen gas, wherein the solution of oxycodone acid adduct comprises 6α-oxycodol in an amount ≦about 0.800 area % as determined by HPLC.
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
The present invention provides a process for preparing an oxycodone acid adduct, said process comprising hydrogenating an aqueous solution of 14-hydroxycodeinone and an acid to form a solution of the oxycodone acid adduct, wherein the hydrogenation is carried out at one or more temperatures greater than ambient temperature in the presence of a hydrogenation catalyst and hydrogen gas, wherein the solution of oxycodone acid adduct comprises 6a-oxycodol in an amount = about 0.800 area % as determined by HPLC.
Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques.
C07C 211/00 - Compounds containing amino groups bound to a carbon skeleton
C07C 225/22 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
C07C 229/42 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
68.
Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs
Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques.
C07C 211/00 - Compounds containing amino groups bound to a carbon skeleton
A01N 43/08 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom five-membered rings with oxygen as the ring hetero atom
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
C07C 225/22 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
C07C 229/42 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.
C07C 69/732 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
C07D 307/937 - Not further condensed cyclopenta [b] furans or hydrogenated cyclopenta [b] furans with hydrocarbon or substituted hydrocarbon radicals directly attached in position 2, e.g. prostacyclins
C07C 323/56 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
71.
Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs
Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques.
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
C07C 229/42 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
C07C 225/22 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
C07C 227/22 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from lactams, cyclic ketones or cyclic oximes, e.g. by reaction involving Beckmann rearrangement
C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
74.
Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs
Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques.
A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
76.
Stable cannabinoid compositions and methods for making and storing them
A composition comprising a high purity cannabinoid, an acid, and a pharmaceutically-acceptable solvent achieves room temperature stability for over 24 months. The acid improves the stability of the composition and the solvent enhances the solubility of the acid, thereby allowing the acid to have an improved stabilizing effect on the highly pure cannabinoid. Preferably, the solvent is an alcohol and, more preferably, the composition contains an oil. A method for making the composition includes combining the cannabinoid and the solvent and evaporating a portion of the solvent, along with adding an acid to the composition, before, during, or after the evaporating step. A method for making and storing the composition includes storing the composition in a manner adapted to maintain its stability. Pharmaceutical dosage forms include a formulated composition, such as having the oil. A method of treating a subject comprises administering to the subject the dosage form.
A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A method of preparing oxycodone includes forming 14-hydroxycodeine by reduction of 14-hydroxycodeinone and rearrangement of the 14-hydroxycodeine to form the oxycodone. During the reduction step, the ketone group of an undesirable contaminant precursor, 8,14-dihydroxy-7,8-dihydrocodeinone, is reduced to a hydroxyl group thus forming a triol. This triol is substantially inert with respect to reforming 14-hydroxycodeinone and can be readily separated from oxycodone.
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
A method of preparing a ribofuranose derivative essentially free of pyranose compounds includes a step of contacting a solution of MDR containing MDRP as an impurity in a solvent including methanol and/or tetrahydrofuran with at least one alkali metal periodate under conditions sufficient to oxidize at least a portion of the MDRP. MDR containing at most 5 wt % of MDRP based on the total weight of MDR and MDRP may be produced.
Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques.
C07C 229/00 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton
A01N 37/12 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group , wherein Cn means a carbon skeleton not containing a ringThio-analogues thereof
A01N 37/44 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio-analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio-analogue of a carboxylic group, e.g. amino-carboxylic acids
A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
81.
Preparation of opiate analgesics by reductive alkylation
A process for preparing a compound of formula (A), (B) or (C):
is a single bond or a double bond, is disclosed. The process includes reductive alkylation in the presence of hydrogen and a reductive alkylation catalyst.
C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
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Chemical preparations and substances used to denaturise other chemical substances by rendering them unsuitable for human and animal consumption. Fertilisers; repellents for use in deterring animals and insects from grazing, eating or damaging plants, trees and the like; preparations for destroying vermin; anti-browsing and aversion compositions; preparations for repelling animals, birds and insects; pesticides, insecticides and acaricides.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
31 - Agricultural products; live animals
Goods & Services
(1) Chemicals for use in industry, agriculture, horticulture, silviculture and forestry, namely chemical substances for denaturing other substances to discourage ingestion, chemicals for use as repellents or aversion agents by virtue of their odour or taste, bittering agents for use as additives to discourage accidental ingestion and fertilizers; repellents for use in deterring animals and insects from grazing, eating or damaging plants, trees and the like; chemical preparations being component of repellents and deterrents for domestic and non-domestic animals, livestock and exotic animals; all purpose disinfectants; preparations for destroying vermin; anti-browsing and aversion compositions used to prevent or deter animals and insects from attacking, eating or damaging plants, trees or the like; preparations for application to plants and foliage or ground areas for repelling animals, birds and insects; pesticides and insecticides and acaricides for domestic, commercial and agricultural use.
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
unpleasant tasting flavoring for use as a denaturant in consumer products; namely, disinfectants and household cleaning preparations to render them unpalatable for human consumption
01 - Chemical and biological materials for industrial, scientific and agricultural use
Goods & Services
(1) A chemical substance for use as a denaturant for alcohol.
(2) Chemical preparations and substances used to denature other chemical substances by rendering unsuitable for human consumption; chemical preparations and substances used to render other chemical substances bitter tasting to discourage human consumption and prevent accidental ingestion by humans or animals.
