There are described novel solid forms of ozanimod hydrochloride, having the formula (I). Also described are the processes for the preparation of said solid forms, as well as pharmaceutical compositions comprising them.
An improved preparation of non-steroidal antiandrogen drugs, such as 4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methyl-benzamide and intermediates thereof, is described.
C07D 233/86 - Oxygen and sulfur atoms, e.g. thiohydantoin
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 237/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
3.
A SOLID STATE FORM OF TAFAMIDIS AND A PROCESS FOR ITS PREPARATION
A crystalline form of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid and a method for its preparation are described. The crystalline form is further suitable as intermediate compound to prepare Form 1, Form 4 and Form M with improved stability and purity.
The present invention relates to a crystalline form of darolutamide and to the process for its preparation. Furthermore, the invention relates to the use of said crystalline form for the preparation of a pharmaceutical composition useful for treating prostate cancer.
C07D 231/14 - 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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
A crystalline form of tezacaftor, an industrially viable and advantageous process for its preparation and a method for the preparation of amorphous form of tezacaftor are described.
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
6.
PROCESSES FOR THE PREPARATION OF NON-STEROIDAL ANTIANDROGENS
An improved preparation of non-steroidal antiandrogen drugs, such as 4-[3-[4-cyano-3- (trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methyl- benzamide and intermediates thereof, is described.
C07D 233/86 - Oxygen and sulfur atoms, e.g. thiohydantoin
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 237/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
7.
PROCESSES FOR THE PREPARATION OF NON-STEROIDAL ANTIANDROGENS
An improved preparation of non-steroidal antiandrogen drugs, such as 4-[3-[4-cyano-3- (trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methyl- benzamide and intermediates thereof, is described.
C07D 233/86 - Oxygen and sulfur atoms, e.g. thiohydantoin
C07C 237/00 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 237/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
8.
Process for the preparation of ferric organic compounds
A crystalline form of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid and a method for its preparation are described. The crystalline form is further suitable as intermediate compound to prepare Form 1, Form 4 and Form M with improved stability and purity.
A crystalline form of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid and a method for its preparation are described. The crystalline form is further suitable as intermediate compound to prepare Form 1, Form 4 and Form M with improved stability and purity.
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
11.
Process for the preparation of sphingosine-1-phosphate receptor agonist
Industrially viable and advantageous processes for the preparation of Ozanimod are described. The invention also discloses the intermediates obtained in the process.
C07C 255/58 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
C07D 319/06 - 1,3-DioxanesHydrogenated 1,3-dioxanes not condensed with other rings
C07D 413/10 - 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 carbon chain containing aromatic rings
12.
SOLID FORMS OF TEZACAFTOR AND PROCESSES FOR THE PREPARATION THEREOF
A crystalline form of tezacaftor, an industrially viable and advantageous process for its preparation and a method for the preparation of amorphous form of tezacaftor are described.
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
A crystalline form of tezacaftor, an industrially viable and advantageous process for its preparation and a method for the preparation of amorphous form of tezacaftor are described.
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
A61P 11/00 - Drugs for disorders of the respiratory system
Process for the preparation of a high-purity ferric (III) citrate. The process comprises the following steps: a) bringing into contact ferric acetylacetonate and citric acid in at least one liquid medium so as to obtain a mixture; b) heating the mixture obtained in step a) to a temperature from 35°C to the reflux temperature of the at least one medium used so as to obtain a solution of ferric citrate in said medium; c) bringing into contact the solution of ferric citrate with an antisolvent so as to cause its precipitation; and b) isolating and, optionally, drying it.
It is described an industrially viable and advantageous process for the preparation of (S)-beta-aminosulfone (1) starting from the corresponding racemic compound, said (S)-beta-aminosulfone being a useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
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
17.
PROCESS FOR THE PREPARATION OF SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONIST
Industrially viable and advantageous processes for the preparation of Ozanimod are described. The invention also discloses the intermediates obtained in the process.
C07D 413/10 - 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 carbon chain containing aromatic rings
C07C 255/54 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
C07C 255/58 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
C07C 255/61 - Carboxylic acid nitriles containing cyano groups and nitrogen atoms being part of imino groups bound to the same carbon skeleton
C07C 259/18 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxyamidine groups bound to carbon atoms of six-membered aromatic rings
C07D 319/06 - 1,3-DioxanesHydrogenated 1,3-dioxanes not condensed with other rings
It is described an industrially viable and advantageous process for the preparation of racemic beta-aminosulfone (1), an useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.
C07C 315/04 - Preparation of sulfonesPreparation of sulfoxides by reactions not involving the formation of sulfone or sulfoxide groups
C07C 251/16 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
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
19.
Eluxadoline crystalline forms and processes for their preparation
Novel crystalline forms of Eluxadoline, having the formula (I), are described. Also described are the processes for the preparation of said crystalline forms.
C07D 233/56 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
It is described an industrially viable and advantageous process for the preparation of mixed µOR agonist/δOR antagonists (9). The invention also discloses the intermediates obtained in the process.
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07C 233/65 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
21.
Processes for the preparation of diastereomerically and enantiomerically enriched oxazolines
The invention relates to an industrially viable and advantageous process for the preparation of (2S,3 R)-2-amino-3-(3,4-dihydroxyphenyl)-3-hydroxypropanoic acid, having the following formula (I) generally known as Droxidopa, or of intermediates useful in the synthesis thereof.
C07C 227/32 - Preparation of optical isomers by stereospecific synthesis
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 269/04 - 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 from amines with formation of carbamate groups
C07C 229/36 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
C07C 253/20 - Preparation of carboxylic acid nitriles by dehydratation of carboxylic acid amides
C07C 255/21 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same saturated acyclic carbon skeleton the carbon skeleton being further substituted by doubly-bound oxygen atoms
It is described an industrially viable and advantageous process for the preparation of (S)-beta-aminosulfone (1) starting from the corresponding racemic compound, said (S)-beta-aminosulfone being a useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4.-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.
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
It is described an industrially viable and advantageous process for the preparation of racemic beta-aminosulfone (1), an useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.
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 251/28 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having nitrogen atoms of imino groups acylated
24.
Process for the preparation of (1S,2R)-Milnacipran
The invention relates to a process for the preparation of Levomilnacipran or salts thereof, compounds useful in the treatment of depression, with high yield.
C07C 233/57 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
C07C 231/06 - Preparation of carboxylic acid amides from nitriles by transformation of cyano groups into carboxamide groups
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
25.
PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY ENRICHED DIHYDROBENZOFURANS AND INTERMEDIATE COMPOUNDS OBTAINED IN THE PROCESS
It is described an industrially viable and advantageous process for the preparation of (N- (((1R,2R)-2-(2,3-dihydrobenzofuran-4-yl)cyclopropyl)methyl)propionamide, compound having the formula depicted below and generally known as Tasimelteon, or of intermediates useful in the synthesis thereof: The invention also relates to salts obtained as intermediates of the process.
C07D 307/79 - Benzo [b] furansHydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
A61K 31/343 - 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 condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
26.
ELUXADOLINE CRYSTALLINE FORM AND PROCESS FOR THE PREPARATION THEREOF
It is described a novel crystalline form of Eluxadoline, having the formula (I). It is also described a process for the preparation of said crystalline form.
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
Novel crystalline forms of Eluxadoline, having the formula (I), are described. Also described are the processes for the preparation of said crystalline forms.
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
The invention relates to an industrially viable and advantageous process for the preparation of (2S,3R)-2-amino-3-(3,4-dihydroxyphenyl)-3-hydroxypropanoic acid, having the following formula (I) generally known as Droxidopa, or of intermediates useful in the synthesis thereof.
C07C 227/32 - Preparation of optical isomers by stereospecific synthesis
C07C 229/14 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of carbon skeletons containing rings
C07C 229/34 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
29.
AMORPHOUS POWDER COMPRISING AN ANGIOTENSIN RECEPTOR BLOCKER AND A NEUTRAL ENDOPEPTIDASE INHIBITOR
Several methods for the preparation of an amorphous powder comprising a 1:1 stoichiometric mixture of the trisodium salts of Valsartan and Sacubitril are described, as well as the resulting amorphous powder, pharmaceutical compositions containing it, and their use in the treatment of essential hypertension and/or cardiac failure.
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
30.
NUCLEOSIDE PHOSPHORAMIDATES USEFUL FOR THE TREATMENT OF VIRAL INFECTIONS AND PREPARATION THEREOF
The present invention relates to an industrially applicable process for the preparation of phosphoramidates useful for the treatment of viral infections, such as sofosbuvir, and to intermediates useful for the preparation thereof. Formula (I):
The invention relates to a process for the preparation of Levomilnacipran, a compound useful in the treatment of depression, comprising the following steps: a) directly converting the enantiomerically enriched form of alcohol (D) into the enantiomerically enriched form of the phthalimido derivative (C) by treatment with phthalimide in the presence of a trialkyl or triarylphosphine and of a dialkyl azodicarboxylate, formula (I) wherein the amount of phthalimide is comprised between 1 and 1.3 equivalents with respect to the molar amount of alcohol (D) used, and the amounts of both the phosphine and the azodicarboxylate are comprised, independently from each other, between 1 and 1.5 equivalents with respect to the molar amount of alcohol (D) used; b) deblocking the enantiomerically enriched form of the phthalimido derivative (C) to obtain Levomilnacipran, formula (II).
The present invention relates to a crystalline form of moxifloxacin base, to a process for its preparation, to pharmaceutical compositions containing it, and to its use as an antibacterial agent.
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 relates to a new stable crystalline form of Entacapone, denominated Form F. It also relates to the process for preparing it and to the pharmaceutically acceptable composition that comprises it. The process comprises dissolving by heating the Entacapone product in an organic solvent; adding the solution obtained in the preceding step to a previously heated anti-solvent; cooling the suspension obtained; and isolating the precipitate so obtained by filtration, and then drying the product obtained until constant weight.
C07C 255/41 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by carboxyl groups, other than cyano groups
The present invention refers to a new stable crystalline form of moxifloxacin hydrochloride, to a process of its preparation and to its use in the preparation of pharmaceutical compositions. It is provided a process comprising to dissolve crude moxifloxacin hydrochloride in a mixture of methanol/water by heating at the reflux temperature; to add acetone and to heat the dissolution at a temperature comprised between 40 and 45°C; to cool until a temperature comprised between 15 and 25°C; to separate the crystals formed by filtration; to wash and dry the obtained product until a constant weight is obtained.
The present invention relates to a method for obtaining benzimizadole derivatives and intermediates thereof, preferably, for obtaining Candesartan and Candesartan cilexetil. Said method allows the benzimizadole derivatives to be obtained with a higher yield.
C07D 403/10 - 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 carbon chain containing aromatic rings
The present invention is related to a new process for the preparation of pantoprazole (I) and pharmaceutical acceptable salts thereof, with a good yield and a high purity. In said process, the introduction of the methoxy group is carried over the position 4 of the piridine ring of compound (IV) by substitution of the chlorine atom, by the reaction with an alkaline methoxide in a mixture of methanol and an aprotic polar solvent. Also an aspect of the invention is an isolating process that includes a method for the purification of pantoprazole, and a process for the preparation of compound (IV), which is used as starting product for the preparation of pantoprazole.
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
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
patents
