Abstract

The present invention relates to a process for preparing Semaglutide by solid phase peptide synthesis (SPPS). It describes a convergent synthesis by using different fragments including pseudoprolines in one or more of the fragments bound to a solid support.

IPC Classes  ?

• C07K 14/605 - Glucagons
• C07K 1/04 - General processes for the preparation of peptides on carriers
• C07K 1/06 - General processes for the preparation of peptides using protecting groups or activating agents

Abstract

The present invention relates to a telescoping process for the preparation of brivaracetam. The process according to the present invention is a cost effective process in that it avoids isolation of intermediates at every step (Formula (I)).

IPC Classes  ?

• 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

Abstract

The present invention relates to a process for preparing Liraglutide by solid phase peptide synthesis (SPPS). It describes a convergent synthesis by using different fragments including pseudoprolines in one or more of the fragments bound to a solid support.

IPC Classes  ?

• C07K 14/605 - Glucagons
• C07K 1/04 - General processes for the preparation of peptides on carriers
• C07K 1/06 - General processes for the preparation of peptides using protecting groups or activating agents

Abstract

The present invention provides an improved process for purification and isolation of leuprorelin or pharmaceutically acceptable salt(s) thereof by preparative supercritical fluid chromatography (preparative SFC) method, wherein the said process provides more than 98% purity of leuprorelin or salt(s) thereof.

IPC Classes  ?

• C07K 7/23 - Luteinising hormone-releasing hormone [LHRH]Related peptides
• C07K 1/16 - ExtractionSeparationPurification by chromatography

Abstract

The present invention relates to a process for the preparation Bilastine (1). The process produces Bilastine (1) with greater than or equal to 99.9 % purity.

IPC Classes  ?

• 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

Abstract

The present invention relates to a process for the preparation of Levoketoconazole (1). It further provides a process for the preparation of crystalline anhydrous Levoketoconazole (1).

IPC Classes  ?

• C07D 405/06 - 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 carbon chain containing only aliphatic carbon atoms

Goods & Services

Vitamins for the food industry; vitamins for use in the manufacture of cosmetics; vitamins for use in the manufacture of food supplements; vitamins for use in the manufacture of pharmaceuticals.

Goods & Services

Vitamins for the food industry; vitamins for use in the manufacture of cosmetics; vitamins for use in the manufacture of food supplements; vitamins for use in the manufacture of pharmaceuticals

Abstract

The present invention relates to obtaining single incubation condition for cocktail of probe substrates of 8 major Cytochrome P450 (CYP) isoforms to assess in vitro drug-drug interactions (DDIs) of novel drug candidates using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) method. The present invention provides an improved and reduced substrate concentration and is developed in lower microsomal protein to avoid any non-specific binding of substrates with the microsomal proteins.

IPC Classes  ?

• C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase

Abstract

The present invention relates to a stable, solid composition of Azilsartan or its pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipient(s); optionally, the said composition further comprises a diuretic, preferably a thiazide diuretic such as Chlorthalidone, and processes for its preparation.

IPC Classes  ?

• A61K 31/4245 - Oxadiazoles
• A61K 31/4035 - Isoindoles, e.g. phthalimide
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - DrageesCoated pills or tablets

Abstract

The present invention relates to an industrially feasible and economically viable process for preparation of Anagrelide Hydrochloride Monohydrate of formula (1a).

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems

Abstract

The present invention relates to an industrially feasible and economically viable process for preparation of Edoxaban key intermediate viz. compound of formula (1) which is shown below:

IPC Classes  ?

• 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 271/24 - 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
• C07C 55/10 - Succinic acid

Abstract

The present invention relates to an improved process for 4-(Hydroxymethyl)-5-methyl-1,3-dioxol-2-one (I). The process involves reaction of compound of formula (II) with sodium acetate in presence of catalytic amount of potassium iodide in dimethyl formamide solvent at 25-30° C. to give 5-methyl-2-oxo-1,3-dioxol-4-yl)methyl acetate (IV) which was further Acid hydrolysed by IPA·HCl in Isopropyl alcohol solvent to yield 4-(hydroxymethyl)-5-methyl-1,3-dioxol-2-one (I).

IPC Classes  ?

• C07D 317/36 - Alkylene carbonatesSubstituted alkylene carbonates
• B01J 27/08 - Halides
• C07D 317/40 - Vinylene carbonateSubstituted vinylene carbonates

Abstract

The present invention relates to an improved process for the preparation of N-((1R,2R)-1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl)octanamide (A), which is known as ELIGLUSTAT and its pharmaceutically acceptable salts, comprising the formation of novel intermediate metal complex (III), which on hydrolysis in presence of acid provides amine compound (IV) (as described herein), which is treated with pyrrolidine and subsequently reduced to convert into Eliglustat (A).

IPC Classes  ?

• C07D 319/18 - Ethylenedioxybenzenes, not substituted on the hetero ring
• C07F 1/08 - Copper compounds
• C07F 3/06 - Zinc compounds
• C07F 15/04 - Nickel compounds

Abstract

The present invention relates to an improved process for diastereoselective synthesis of vicinal diamines (1). The process involves highly regio- and diastereoselective addition of 2-azaallyl anions (4) to N-tert-butanesulfinylimines (5) to produce vicinal diamines (1).

IPC Classes  ?

• C07C 303/40 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
• C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical

Abstract

N) respectively.

IPC Classes  ?

• C07D 487/10 - Spiro-condensed systems
• C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
• C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
• C07C 313/06 - Sulfinamides

Abstract

The present invention relates to obtaining single incubation condition for cocktail of probe substrates of 8 major Cytochrome P450 (CYP) isoforms to assess in vitro drug-drug interactions (DDIs) of novel drug candidates using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) method. The present invention provides an improved and reduced substrate concentration and is developed in lower microsomal protein to avoid any non-specific binding of substrates with the microsomal proteins.

IPC Classes  ?

• C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
• C12N 9/06 - Oxidoreductases (1.), e.g. luciferase acting on nitrogen containing compounds as donors (1.4, 1.5, 1.7)
• C12Q 1/00 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions
• C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
• G01N 33/573 - ImmunoassayBiospecific binding assayMaterials therefor for enzymes or isoenzymes

Abstract

The present invention relates to a stable, solid pharmaceutical composition of Azilsartan or its pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipient(s) and processes for its preparation; optionally, the said composition further comprises a diuretic, preferably a thiazide diuretic such as Chlorthalidone. The present invention further relates to a stable, solid pharmaceutical composition comprising Azilsartan kamedoxomil and one or more pharmaceutically acceptable excipient(s).

IPC Classes  ?

• A61K 31/4245 - Oxadiazoles
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/20 - Pills, lozenges or tablets
• A61P 9/12 - Antihypertensives
• A61K 31/4035 - Isoindoles, e.g. phthalimide

Abstract

The present invention provides an improved photochemical rector assembly device, particularly a light emitting diode (LED) based small photochemical reactor and methods for performing the photochemical transformations using the instantly presented device. Accordingly, the present invention relates to an improved photochemical transformation reaction by exposing the reaction mixture to a photochemical rector device as shown in fig. A-G, comprising of (i) light emitting diode (LED) panel (1), (ii) Aluminium based heat sink, and (iii) cooling fan.

IPC Classes  ?

• B01J 19/12 - Processes employing the direct application of electric or wave energy, or particle radiationApparatus therefor employing electromagnetic waves
• B01J 8/08 - Chemical or physical processes in general, conducted in the presence of fluids and solid particlesApparatus for such processes with moving particles
• B01J 8/10 - Chemical or physical processes in general, conducted in the presence of fluids and solid particlesApparatus for such processes with moving particles moved by stirrers or by rotary drums or rotary receptacles
• C07F 5/02 - Boron compounds
• B01J 31/18 - Catalysts comprising hydrides, coordination complexes or organic compounds containing coordination complexes containing nitrogen, phosphorus, arsenic or antimony

Abstract

The present invention relates to an industrially feasible and economically viable process for preparation of SGLT2 inhibitors of formula X in significantly high yield and purity.

IPC Classes  ?

• C07H 7/04 - Carbocyclic radicals
• C07H 1/00 - Processes for the preparation of sugar derivatives
• C07H 1/06 - SeparationPurification
• C07H 7/06 - Heterocyclic radicals

Abstract

The present invention relates to an improved asymmetric synthesis of alpha-branched amines (hereafter referred to as the compound) and relative chiral amines (1″) or its pharmaceutically acceptable salt and derivatives. The process comprises an unusual substrate specific regioselective ortho lithiation of substituted arene compounds, followed by its highly diastereoselective addition to N-tert-butanesulfinylimines resulting in the selective formation of alpha-branched sulfinyl amine and chiral amine; which on subsequently removing the sulfinyl group provides corresponding alpha-branched amines or relative chiral amines (1″).

IPC Classes  ?

• C07C 303/40 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
• C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
• C07B 53/00 - Asymmetric syntheses
• C07C 217/58 - 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 amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
• C07C 217/60 - 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 amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
• C07C 311/13 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings

Abstract

The present invention relates to an improved process for 4-(Hydroxymethyl)-5-methyl-1,3-dioxol-2-one (I). The process involves reaction of compound of formula (II) with sodium acetate in presence of catalytic amount of potassium iodide in dimethyl formamide solvent at 25-30°C to give 5-methyl-2-oxo-1,3-dioxol-4-yl)methyl acetate (IV) which was further Acid hydrolysed by IPA. HCl in Isopropyl alcohol solvent to yield 4-(hydroxymethyl)-5-methyl-1,3-dioxol-2-one (I).

IPC Classes  ?

• C07D 317/40 - Vinylene carbonateSubstituted vinylene carbonates

Abstract

The present invention relates to an improved asymmetric synthesis of alpha-(diarylmethyl) alkyl amines (hereafter referred to as the compound (1)) or its pharmaceutically acceptable salt and derivatives. The process comprises an unusual substrate specific regioselective lithiation of alpha-diarylmethanes. followed by its highly diastereoselective addition to N-tert-butanesulfinylimines resulting in the selective formation of chiral alpha-(diarylmethyl) alkyl amines 4 and chiral amine 5; which on subsequently removing the sulfinyl group provides corresponding alpha-(diarylmethyl) alkyl amines (1) or relative chiral amines (1″).

IPC Classes  ?

• C07C 209/62 - Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds
• C07C 313/06 - Sulfinamides
• C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
• C07C 211/27 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains

Abstract

The present invention provides an improved process for preparation of the L-threo-(2S,3R)-3-(3 4-dihydroxyphenyl)serine (I) or a salt thereof, which is known as Droxidopa; comprising (a) recovery of the by-product compound (V) (as described herein) from the crude compound (I), and (b) recycling and re-use it for the preparation of droxidopa. Accordingly, the present invention relates to an improved economical process for the preparation of L-threo-(2S,3R)-3-(3.4-dihydroxyphenyl)serine (I) or its pharmaceutically acceptable salts; wherein the process relates to recovery and recycling of the by-product compound (V) and also to re-use it for the preparation of droxidopa.

IPC Classes  ?

• C07C 227/40 - SeparationPurification
• C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• 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

Abstract

The present invention provides an improved process for preparation of L-threo-(2S,3R)-3-(3,4-dihydroxyphenyl)serine (I) (Droxidopa) and its salts; comprising (a) reaction of the aldehyde compound (III) (as described herein) with Metal complex (II) (as described herein), and (h) hydrolysis of the compound (IV) obtained from step (a) in presence of acid. The present invention also relates to a novel intermediates metal chiral complex (IV) for the preparation of Droxidopa.

IPC Classes  ?

• 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
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• C07F 15/04 - Nickel compounds

Abstract

The present invention relates to a level meter measuring the quality health of a pharmaceutical manufacturing site and which predicts 24/7 audit readiness for quality outcomes, wherein outcome is interpreted using tangible data; referred to as a Quality Health Barometer. The present invention also relates to a method of evaluating the audit readiness of a pharmaceutical manufacturing site. The present invention further relates to a method of evaluating data integrity (DI) compliance of a pharmaceutical manufacturing site.

IPC Classes  ?

• G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for calculating health indicesICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment
• G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
• G16H 40/20 - ICT specially adapted for the management or administration of healthcare resources or facilitiesICT specially adapted for the management or operation of medical equipment or devices for the management or administration of healthcare resources or facilities, e.g. managing hospital staff or surgery rooms
• G16H 70/20 - ICT specially adapted for the handling or processing of medical references relating to practices or guidelines

Abstract

The present invention relates to an industrially feasible and economically viable process for preparation of Bexagliflozin of formula V in significantly high yield and purity.

IPC Classes  ?

• C07H 7/04 - Carbocyclic radicals
• C07H 1/00 - Processes for the preparation of sugar derivatives
• C07H 1/06 - SeparationPurification
• C07H 7/06 - Heterocyclic radicals

Abstract

The present invention relates to an oral pharmaceutical composition, particularly a tablet, comprising an active ingredient lurasidone or its pharmaceutically acceptable salt(s) or solvate(s) thereof and one or more pharmaceutical excipient(s); and a process for its preparation.

IPC Classes  ?

• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/02 - Inorganic compounds
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• A61K 47/38 - CelluloseDerivatives thereof

Abstract

The present invention relates to a novel process for the preparation of intermediate of fosaprepitant dimeglumine. The present invention particularly relates to a process for the preparation of fosaprepitant dibenzyl ester, an intermediate of fosaprepitant dimeglumine, which is simple, easy to handle on commercial scale and efficient.

IPC Classes  ?

• C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

Goods & Services

PHARMACEUTICALS AND MEDICINAL PREPARATIONS. ADVERTISING; BUSINESS MANAGEMENT; BUSINESS ADMINISTRATION; OFFICE FUNCTIONS; all the aforesaid services relating to pharmaceutical services only. SCIENTIFIC AND TECHNOLOGICAL SERVICES AND RESEARCH AND DESIGN RELATING THERETO; INDUSTRIAL ANALYSIS AND RESEARCH SERVICES; all the aforesaid services relating to pharmaceutical services only.

Goods & Services

PHARMACEUTICALS AND MEDICINAL PREPARATIONS. ADVERTISING; BUSINESS MANAGEMENT; BUSINESS ADMINISTRATION; OFFICE FUNCTIONS; all of the aforesaid services relating to pharmaceutical services only. SCIENTIFIC AND TECHNOLOGICAL SERVICES AND RESEARCH AND DESIGN RELATING THERETO; INDUSTRIAL ANALYSIS AND RESEARCH SERVICES; all of the aforesaid services relating to pharmaceutical services only.

Goods & Services

PHARMACEUTICALS AND MEDICINAL PREPARATIONS. ADVERTISING; BUSINESS MANAGEMENT; BUSINESS ADMINISTRATION; OFFICE FUNCTIONS; all of the aforesaid services relating to pharmaceutical services only. SCIENTIFIC AND TECHNOLOGICAL SERVICES AND RESEARCH AND DESIGN RELATING THERETO; INDUSTRIAL ANALYSIS AND RESEARCH SERVICES; all of the aforesaid services relating to pharmaceutical services only.

Goods & Services

PHARMACEUTICALS AND MEDICINAL PREPARATIONS. ADVERTISING; BUSINESS MANAGEMENT; BUSINESS ADMINISTRATION; OFFICE FUNCTIONS; all of the aforesaid services relating to pharmaceutical services only. SCIENTIFIC AND TECHNOLOGICAL SERVICES AND RESEARCH AND DESIGN RELATING THERETO; INDUSTRIAL ANALYSIS AND RESEARCH SERVICES; all of the aforesaid services relating to pharmaceutical services only.

Goods & Services

PHARMACEUTICALS AND MEDICINAL PREPARATIONS. ADVERTISING; BUSINESS MANAGEMENT; BUSINESS ADMINISTRATION; OFFICE FUNCTIONS; all of the aforesaid services relating to pharmaceutical services only. SCIENTIFIC AND TECHNOLOGICAL SERVICES AND RESEARCH AND DESIGN RELATING THERETO; INDUSTRIAL ANALYSIS AND RESEARCH SERVICES; all of the aforesaid services relating to pharmaceutical services only.

Goods & Services

PHARMACEUTICALS AND MEDICINAL PREPARATIONS. ADVERTISING; BUSINESS MANAGEMENT; BUSINESS ADMINISTRATION; OFFICE FUNCTIONS; all of the aforesaid services relating to pharmaceutical services only. SCIENTIFIC AND TECHNOLOGICAL SERVICES AND RESEARCH AND DESIGN RELATING THERETO; INDUSTRIAL ANALYSIS AND RESEARCH SERVICES; all of the aforesaid services relating to pharmaceutical services only.

Goods & Services

PHARMACEUTICALS AND MEDICINAL PREPARATIONS. ADVERTISING; BUSINESS MANAGEMENT; BUSINESS ADMINISTRATION; OFFICE FUNCTIONS; all of the aforesaid services relating to pharmaceutical services only. SCIENTIFIC AND TECHNOLOGICAL SERVICES AND RESEARCH AND DESIGN RELATING THERETO; INDUSTRIAL ANALYSIS AND RESEARCH SERVICES; all of the aforesaid services relating to pharmaceutical services only.

Goods & Services

PHARMACEUTICALS AND MEDICINAL PREPARATIONS. ADVERTISING; BUSINESS MANAGEMENT; BUSINESS ADMINISTRATION; OFFICE FUNCTIONS; all of the aforesaid services relating to pharmaceutical services only. SCIENTIFIC AND TECHNOLOGICAL SERVICES AND RESEARCH AND DESIGN RELATING THERETO; INDUSTRIAL ANALYSIS AND RESEARCH SERVICES; all of the aforesaid services relating to pharmaceutical services only.

Goods & Services

Scientific and technological services, namely, research and design in the field of contract manufacturing and development of pharmaceuticals for others; Industrial analysis and research services in the field of contract manufacturing and development of pharmaceuticals for others

Goods & Services

Scientific and technological services, namely, research and design in the field of contract manufacturing and development of pharmaceuticals for others; Industrial analysis and research services in the field of contract manufacturing and development of pharmaceuticals for others

Goods & Services

Scientific and technological services, namely, research and design in the field of contract manufacturing and development of pharmaceuticals for others; industrial analysis and research services in the field of contract manufacturing and development of pharmaceuticals for others

Goods & Services

Scientific and technological services, namely, research and design in the field of contract manufacturing and development of pharmaceuticals for others; industrial analysis and research services in the field of contract manufacturing and development of pharmaceuticals for others

Goods & Services

Scientific and technological services, namely, research and design in the field of contract manufacturing and development of pharmaceuticals for others; Industrial analysis and research services in the field of contract manufacturing and development of pharmaceuticals for others

Goods & Services

Scientific and technological services, namely, research and design in the field of contract manufacturing and development of pharmaceuticals for others; Industrial analysis and research services in the field of contract manufacturing and development of pharmaceuticals for others

Goods & Services

Scientific and technological services, namely, research and design in the field of pharmaceuticals for others; Industrial analysis and research services in the field of pharmaceuticals for others

Goods & Services

Scientific and technological services, namely, research and design in the field of contract manufacturing and development of pharmaceuticals for others; industrial analysis and research services in the field of contract manufacturing and development of pharmaceuticals for others

Abstract

The present invention provides an improved process for preparation of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine; commonly known as vortioxetine (referred to as the compound (I)) and pharmaceutically acceptable salts thereof; wherein the process comprises reaction of 2-((2,4-dimethylphenyl)thio)aniline (II) with bis(2-alkyl)amine (IIIa) or its salt in the presence of a cyclic amide solvent.

IPC Classes  ?

• C07D 295/096 - 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 bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• C07B 43/04 - Formation or introduction of functional groups containing nitrogen of amino groups
• C07C 211/46 - Aniline

Abstract

A process for the preparation of 5-(3,4-dimethoxyphenylethyl) methyl-amino-2-(3,4-dimethoxyphenyl)-2-isopropyl valeronitrile, which is known as Verapamil is described. A process for improving the purity of verapamil and therefore of its hydrochloride represented as the compound of formula I, by efficient removal of the impurities formed, affording a product of purity greater than 99% is described.

IPC Classes  ?

• C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
• C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
• C07C 217/60 - 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 amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
• C07C 255/42 - 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 singly-bound nitrogen atoms, not being further bound to other hetero atoms
• B01J 31/02 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
• C07B 63/00 - PurificationSeparation specially adapted for the purpose of recovering organic compoundsStabilisationUse of additives

Abstract

The present invention provides an improved process for the preparation of 8-chloro-1-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione (hereafter referred to as the compound (IV)), which is useful as a key intermediate for the synthesis of Clobazam (referred to as the compound (I)) 7-chloro-1-methyl-5-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione. The process of the present invention further involves transformation of the compound (IV) into Clobazam (I), comprising (a) reacting the compound (II) (as described herein) with monoalkyl malonate in the presence of a coupling agent to obtain the compound (III) (as described herein); followed by the cyclization using a base; (b) reacting the compound-IV (as described herein) obtained from step (a) with methylating agent. The process of the present invention involves formation of novel intermediates methyl 3-((4-chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoate (IIIa) and 3-((4-chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoic acid (V).

IPC Classes  ?

• C07D 243/12 - 1,5-BenzodiazepinesHydrogenated 1,5-benzodiazepines
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• C07C 233/43 - 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 amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
• C07B 37/10 - Cyclisation

Abstract

The present invention provides an improved process for preparation of the substantially pure (3aR,7aR)-4′-(benzo[d]isothiazol-3-yl)octahydrospiro[isoindole-2,1′-piperazin]-1′-ium methanesulfonate (referred to as compound-II), which is useful as a key intermediate for the synthesis of lurasidone ((3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione). The process comprises reaction of the compound-III (as described herein) with the compound-IV (as described herein) in the presence of a solvent mixture selected from an alcohol and water; and a base The improved process for the preparation of compound II provides the product with total amount of unreacted compound-IV as impurity in less than 0.06% and the product with HPLC purity as ≥99.8%. The process further refers purification of Lurasidone hydrochloride, wherein the product contains the residual acetone <5000 ppm.

IPC Classes  ?

• C07D 487/10 - Spiro-condensed systems
• 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
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Goods & Services

Pharmaceutical preparations, especially plasma substitutes.

Goods & Services

Food for babies; Plasters, materials for dressings; Material for stopping teeth, dental wax; Disinfectants; Preparations for destroying vermin; Fungicides, herbicides. Surgical, medical, dental and veterinary apparatus and instruments, artificial limbs, eyes and teeth; Orthopedic articles; Suture materials. Medical services; Veterinary services; Hygienic and beauty care for human beings or animals; Agriculture, horticulture and forestry services.

Goods & Services

Medicines.

Abstract

The present invention provides an improved process for preparation of the substantially pure trazodone and its hydrochloride salt. The process comprises reaction of the compound- ? (as described) with the compound-Ill (as described) optionally in the presence of an inorganic base, and a catalyst; wherein in the said process the trazodone free base and/or its hydrochloride salt are isolated by precipitation at lower temperature. The improved process for the preparation of trazodone hydrochloride (the compound I) provides the product with total amount of alkylating substances (as described herein) as impurity in less than 10 ppm. The improved process for the preparation of trazodone hydrochloride (the compound I) provides the product with total amount of l-(3-chlorophenyl)-4-(3-chloropropyl) piperazine as an impurity in less than 2.5 ppm.

IPC Classes  ?

• C07C 39/06 - Alkylated phenols
• C07C 211/63 - Quaternary ammonium compounds having quaternised nitrogen atoms bound to acyclic carbon atoms
• C07D 295/06 - 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 halogen atoms or nitro radicals
• C07D 471/04 - Ortho-condensed systems

Abstract

The present invention relates to an oral pharmaceutical composition, particularly a tablet, comprising an active ingredient lurasidone or its pharmaceutically acceptable salt(s) or solvate(s) thereof and one or more pharmaceutical excipient(s); and a process for its preparation.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• 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