Synthon BV

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1.

CRYSTALLINE FORM OF ASCIMINIB HYDROCHLORIDE

      
Application Number 19128078
Status Pending
Filing Date 2023-11-09
First Publication Date 2026-08-06
Owner Synthon B.V. (Netherlands)
Inventor
  • Dymácek, Bohumil
  • Hegedus, Michal

Abstract

The application relates to the crystalline Form 1S of Asciminib hydrochloride and processes for the preparation thereof. Also described are solvates of Asciminib with 2-butanol, isobutanol, tert-butanol, 2-methyl tetra hydrofuran and cyclohexanol from which the crystalline Form IS of Asciminib hydrochloride can be prepared. The application relates to the crystalline Form 1S of Asciminib hydrochloride and processes for the preparation thereof. Also described are solvates of Asciminib with 2-butanol, isobutanol, tert-butanol, 2-methyl tetra hydrofuran and cyclohexanol from which the crystalline Form IS of Asciminib hydrochloride can be prepared.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

2.

PHARMACEUTICAL COMPOSITION OF SIPONIMOD

      
Application Number 19137775
Status Pending
Filing Date 2023-12-11
First Publication Date 2026-07-23
Owner Synthon B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to pharmaceutical composition comprising siponimod and processes for preparation thereof.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • A61K 47/02 - Inorganic compounds
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
  • A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
  • A61K 47/38 - CelluloseDerivatives thereof

3.

BUDESONIDE ENTERIC CAPSULE FORMULATION

      
Application Number EP2025088403
Publication Number 2026/132451
Status In Force
Filing Date 2025-12-19
Publication Date 2026-06-25
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to budesonide encapsulated in enterically coated hydroxypropyl methylcellulose capsules with a specific range of enteric coating.

IPC Classes  ?

  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 9/50 - Microcapsules
  • A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
  • A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers

4.

RUXOLITINIB PHOSPHATE CONTROL RELEASE FORMULATION

      
Application Number EP2025082320
Publication Number 2026/099445
Status In Force
Filing Date 2025-11-07
Publication Date 2026-05-15
Owner SYNTHON B.V (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to tablet composition for oral administration of Ruxolitinib phosphate, with a combination of low viscosity HPMC and high viscosity HPMC.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

5.

IMPROVED AZACITIDINE COMPOSITION

      
Application Number EP2025077426
Publication Number 2026/068588
Status In Force
Filing Date 2025-09-25
Publication Date 2026-04-02
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Buchlovic, Marian
  • Sole, Carles

Abstract

The presented invention relates to Azacitidine (compound of formula (1)) particles characterized by bimodal particle size distribution, process for preparation thereof and composition comprising them.

IPC Classes  ?

  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom

6.

PHARMACEUTICAL FORMULATION COMPRISING APALUTAMIDE

      
Application Number EP2025075472
Publication Number 2026/052846
Status In Force
Filing Date 2025-09-08
Publication Date 2026-03-12
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a pharmaceutical composition comprising a solid dispersion of apalutamide and hydroxypropyl methylcellulose phthalate, wherein the solid dispersion is obtained by the spray-drying process. The invention further relates to the use of said pharmaceutical composition as a medicament in the treatment of non-metastatic castration-resistant prostate cancer and hormone-sensitive prostate cancer.

IPC Classes  ?

  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole

7.

CAPILLARY GEL ELECTROPHORESIS SEPARATION OF DIASTEREOMERS OF PHOSPHOROTHIOATED OLIGONUCLEOTIDES

      
Application Number 19124188
Status Pending
Filing Date 2023-10-23
First Publication Date 2026-02-19
Owner Synthon B.V. (Netherlands)
Inventor Durc, Pavol

Abstract

Method of identification and/or characterization of diastereomers mixtures of phosphorothioate oligonucleotides by capillary gel electrophoresis with a background electrolyte that has a pH 6 to 8, comprising the steps of: a) Preparing a gel matrix by dissolving a water soluble polymer containing a side chain having a functional group that interacts with diastereomers mixture to be analysed in a background electrolyte; b) Introducing the gel matrix in the capillary; c) Introducing the sample of diastereomers mixture of phosphorothioate to capillary; d) Applying an electric field greater than 200 volts/cm of capillary across the gel matrix in the capillary; e) Detecting the individual diastereomers and/or the characteristic groups of partially separated diastereomers of phosphorothioate oligonucleotides.

IPC Classes  ?

8.

A PROCESS FOR PREPARATION OF CABOZANTINIB OR TIVOZANIB

      
Application Number 19132542
Status Pending
Filing Date 2023-11-23
First Publication Date 2026-02-19
Owner Synthon B.V. (Netherlands)
Inventor
  • Hylse, Ondrej
  • Partl, Jiri

Abstract

The presented invention relates to a process for preparation of Cabozantinib, compound of formula (1), or Tivozanib, compound of formula (10) or a salr or a solvate thereof: Formula (1); Formula (10). The presented invention relates to a process for preparation of Cabozantinib, compound of formula (1), or Tivozanib, compound of formula (10) or a salr or a solvate thereof: Formula (1); Formula (10).

IPC Classes  ?

  • C07D 215/233 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
  • 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

9.

AMORPHOUS SOLID FORM AND PHARMACEUTICAL COMPOSITIONS OF LENVATINIB BESYLATE

      
Application Number EP2025083606
Publication Number 2026/027799
Status In Force
Filing Date 2025-11-19
Publication Date 2026-02-05
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Sole, Carles
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit
  • Foret, Petr

Abstract

The invention relates to amorphous solid forms and pharmaceutical compositions comprising amorphous lenvatinib besylate (benzene sulfonate), and the processes for their preparation.

IPC Classes  ?

  • C07D 215/48 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
  • A61K 31/47 - QuinolinesIsoquinolines
  • A61P 35/00 - Antineoplastic agents
  • C07C 309/29 - 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

10.

PROCESS FOR PREPARING A SOLID FORM OF ABEMACICLIB

      
Application Number EP2025067237
Publication Number 2025/262206
Status In Force
Filing Date 2025-06-19
Publication Date 2025-12-26
Owner SYNTHON B.V (Netherlands)
Inventor
  • Hegedus, Michal
  • Bednar, Lukas

Abstract

The presented invention relates to processes for preparation of Abemaciclib, compound of formula (1), or a salt or a solvate, preferably and N,N-dimethylformamide hemisolvate, or a cocrystal or solid forms thereof:

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

11.

PROLONGED RELEASE TOFACITINIB COMPOSITIONS WITHOUT FUNCTIONAL COATING

      
Application Number 19106475
Status Pending
Filing Date 2023-08-25
First Publication Date 2025-12-18
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib or a pharmaceutically acceptable salt thereof, without a functional coating.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets

12.

BUDESONIDE TWO LAYERS CAPSULE FORMULATION

      
Application Number 18993276
Status Pending
Filing Date 2023-07-11
First Publication Date 2025-11-20
Owner Synthon B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a Budesonide formulation with one or more layers comprising organic acid and Budesonide in the same layer.

IPC Classes  ?

  • A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/50 - Microcapsules

13.

SOLID FORMS OF ALECTINIB AND ALECTINIB SALTS

      
Application Number 18840429
Status Pending
Filing Date 2023-02-21
First Publication Date 2025-07-24
Owner Synthon B.V. (Netherlands)
Inventor Dymacek, Bohumil

Abstract

The invention relates to Alectinib, compound of formula (1), solid forms thereof, salts thereof, solid forms of the salts and processes for preparation thereof,. The invention relates to Alectinib, compound of formula (1), solid forms thereof, salts thereof, solid forms of the salts and processes for preparation thereof,.

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

14.

PROCESS FOR PREPARING DIROXIMEL FUMARATE

      
Application Number EP2024086054
Publication Number 2025/132026
Status In Force
Filing Date 2024-12-12
Publication Date 2025-06-26
Owner SYNTHON B.V (Netherlands)
Inventor Castulik, Jakub

Abstract

Described is a process for preparing high purity diroximelfumarate in a non- halogenated solvent.

IPC Classes  ?

15.

A PROCESS FOR MAKING TRAMETINIB

      
Application Number EP2024086530
Publication Number 2025/132190
Status In Force
Filing Date 2024-12-16
Publication Date 2025-06-26
Owner SYNTHON B.V. (Netherlands)
Inventor Partl, Jiri

Abstract

The invention relates to a process for preparation of compound of formula (6) and Trametinib, compound of formula (1):

IPC Classes  ?

16.

SOLVATES OF TRAMETINIB

      
Application Number EP2024086872
Publication Number 2025/132408
Status In Force
Filing Date 2024-12-17
Publication Date 2025-06-26
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

The present invention relates to solvates of compound of formula (1) and processes for preparation thereof.

IPC Classes  ?

  • A61P 35/00 - Antineoplastic agents
  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/4353 - 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

17.

SALTS OF AVATROMBOPAG

      
Application Number EP2024087614
Publication Number 2025/132929
Status In Force
Filing Date 2024-12-19
Publication Date 2025-06-26
Owner SYNTHON B.V (Netherlands)
Inventor Hegedus, Michal

Abstract

The invention relates to improved process to prepare avatrombopag hydrogenmaleate form C from the mixture of acetone and water The invention further relates to the novel salts of avatrombopag, their crystalline forms and preparation thereof. The salts are selected from hydrogenmalonate, fumarate, sulphate, besylate and tosylate salts.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
  • A61K 31/435 - 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

18.

A PROCESS FOR MAKING DABRAFENIB

      
Application Number EP2024086844
Publication Number 2025/132388
Status In Force
Filing Date 2024-12-17
Publication Date 2025-06-26
Owner SYNTHON B.V (Netherlands)
Inventor
  • Mitas, Petr
  • Smekal, Oldrich

Abstract

The invention relates to a process for preparation of Dabrafenib, compound of formula (1) or a salt or a solvate thereof:.

IPC Classes  ?

  • C07D 417/04 - 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 directly linked by a ring-member-to-ring- member bond

19.

FORMULATION COMPRISING FORM B OF AVATROMBOPAG MALEATE

      
Application Number EP2024087743
Publication Number 2025/133011
Status In Force
Filing Date 2024-12-19
Publication Date 2025-06-26
Owner SYNTHON B.V (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The invention relates to tablet composition comprising form B of avatrombopag maleate and a surfactant.

IPC Classes  ?

20.

CRYSTALLINE FORMS OF ACALABRUTINIB HYDROGEN MALEATE

      
Application Number EP2024085803
Publication Number 2025/125383
Status In Force
Filing Date 2024-12-11
Publication Date 2025-06-19
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Hegedus, Michal

Abstract

The invention relates to mixed ethanol water solvate and methanol solvate of Acalabrutinib hydrogen maleate, compound of formula (1), solid forms thereof and processes for preparation thereof.

IPC Classes  ?

  • A61P 35/00 - Antineoplastic agents
  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
  • C07D 487/04 - Ortho-condensed systems

21.

A PROCESS FOR MAKING OSIMERTINIB

      
Application Number EP2024084148
Publication Number 2025/124936
Status In Force
Filing Date 2024-11-29
Publication Date 2025-06-19
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Buchlovic, Marian
  • Bednar, Lukas

Abstract

The invention relates to a process for preparation of compounds of formula (6) and (7), key intermediates for preparation of Osimetrtinib, compound of formula (1).

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

22.

CABOZANTINIB SALT WITH L-(+)-TARTARIC ACID AND SOLID FORMS THEREOF

      
Application Number 18842577
Status Pending
Filing Date 2023-02-28
First Publication Date 2025-05-29
Owner Synthon B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Jelinkova, Katerina

Abstract

The invention relates to solid forms of Cabozantinib, compound of formula (1), salt with L-(+)-tartaric acid and processes for preparation thereof, The invention relates to solid forms of Cabozantinib, compound of formula (1), salt with L-(+)-tartaric acid and processes for preparation thereof,

IPC Classes  ?

  • C07D 215/22 - Oxygen atoms attached in position 2 or 4

23.

A PROCESS FOR MAKING OSIMERTINIB

      
Application Number 18686210
Status Pending
Filing Date 2022-09-01
First Publication Date 2025-05-15
Owner Synthon B.V. (Netherlands)
Inventor
  • Vyklicky, Libor
  • Zabadal, Miroslav

Abstract

The invention deals with a novel process for preparation of the pharmaceutically useful product Osimertinib of formula (1). The invention deals with a novel process for preparation of the pharmaceutically useful product Osimertinib of formula (1).

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

24.

PHARMACEUTICAL COMPOSITION COMPRISING IBRUTINIB

      
Application Number 18717130
Status Pending
Filing Date 2022-12-06
First Publication Date 2025-05-08
Owner Synthon B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising Ibrutinib and one ore more pharmaceutically acceptable excipients. The invention further relates to the use of said composition as a medicament, particularly in the treatment of lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL), Waldenström's macroglobulinaemia (WM) and chronic graft versus host disease (cGVHD).

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 9/20 - Pills, lozenges or tablets

25.

PHARMACEUTICAL COMPOSITION OF BEMPEDOIC ACID

      
Application Number 18690975
Status Pending
Filing Date 2022-09-12
First Publication Date 2025-05-01
Owner Synthon B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The presented invention relates to pharmaceutical composition comprising Bempedoic acid and processes for preparation thereof.

IPC Classes  ?

  • A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
  • A61K 9/20 - Pills, lozenges or tablets

26.

PHARMACEUTICAL COMPOSITION COMPRISING ENZALUTAMIDE

      
Application Number 18762066
Status Pending
Filing Date 2024-07-02
First Publication Date 2024-10-24
Owner Synthon B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising a granulate consisting of a co-precipitate on a substrate, wherein the co-precipitate comprises enzalutamide in amorphous form and a cellulosic concentration enhancing polymer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of castration-resistant prostate cancer.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61J 3/00 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
  • A61J 3/10 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin

27.

PROLONGED RELEASE TOFACITINIB COMPOSITIONS

      
Application Number 18566329
Status Pending
Filing Date 2022-06-03
First Publication Date 2024-08-29
Owner Synthon B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets

28.

PROCESS FOR MAKING MELFLUFEN OR A SALT THEREOF

      
Application Number 18565888
Status Pending
Filing Date 2022-06-01
First Publication Date 2024-08-15
Owner Synthon B.V. (Netherlands)
Inventor
  • Bartos, Petr
  • Castulik, Jakub

Abstract

The present invention relates to process for preparing Melflufen, compound of formula (1) or a salt thereof, and to intermediates used in the process and solid forms thereof. The present invention relates to process for preparing Melflufen, compound of formula (1) or a salt thereof, and to intermediates used in the process and solid forms thereof.

IPC Classes  ?

  • C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
  • C07C 237/20 - 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 containing six-membered aromatic rings
  • C07C 237/22 - 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 having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated

29.

PHARMACEUTICAL COMPOSITION COMPRISING PALBOCICLIB

      
Application Number EP2023085226
Publication Number 2024/132652
Status In Force
Filing Date 2023-12-11
Publication Date 2024-06-27
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a pharmaceutical granulate composition comprising Palbociclib free base with a high surface area having improving processability.

IPC Classes  ?

  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

30.

PHARMACEUTICAL COMPOSITION COMPRISING PALBOCICLIB

      
Application Number EP2023087324
Publication Number 2024/133726
Status In Force
Filing Date 2023-12-21
Publication Date 2024-06-27
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a pharmaceutical granulate composition comprising Palbociclib free base with a high surface area having improving processability.

IPC Classes  ?

  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

31.

PHARMACEUTICAL COMPOSITION OF SIPONIMOD

      
Application Number EP2023085195
Publication Number 2024/126409
Status In Force
Filing Date 2023-12-11
Publication Date 2024-06-20
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to pharmaceutical composition comprising siponimod and processes for preparation thereof.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • C07B 63/00 - PurificationSeparation specially adapted for the purpose of recovering organic compoundsStabilisationUse of additives
  • A61K 9/14 - Particulate form, e.g. powders

32.

PHARMACEUTICAL COMPOSITION OF SIPONIMOD

      
Document Number 03275914
Status Pending
Filing Date 2023-12-11
Open to Public Date 2024-06-20
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

IPC Classes  ?

  • A61K 9/14 - Particulate form, e.g. powders
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine

33.

FORMULATION COMPRISING EDOXABAN AND PREPARATION THEREOF

      
Application Number EP2023084960
Publication Number 2024/121413
Status In Force
Filing Date 2023-12-08
Publication Date 2024-06-13
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The invention relates to the tablet composition comprising edoxaban obtained by the direct compression process comprising the step of co-blending edoxaban and first portion of mannitol, wherein the weight ratio of edoxaban and first portion of mannitol is from 1:1 to 1:2.5.

IPC Classes  ?

34.

A PROCESS FOR PREPARATION OF CABOZANTINIB OR TIVOZANIB

      
Application Number EP2023082902
Publication Number 2024/110606
Status In Force
Filing Date 2023-11-23
Publication Date 2024-05-30
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Hylse, Ondrej
  • Partl, Jiri

Abstract

The presented invention relates to a process for preparation of Cabozantinib, compound of formula (1), or Tivozanib, compound of formula (10) or a salr or a solvate thereof: Formula (1); Formula (10).

IPC Classes  ?

  • C07D 215/20 - Oxygen atoms
  • 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
  • C07C 235/74 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of a saturated carbon skeleton

35.

STABLE FORMULATION COMPRISING OBETICHOLIC ACID

      
Application Number EP2023081607
Publication Number 2024/104960
Status In Force
Filing Date 2023-11-13
Publication Date 2024-05-23
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a stable pharmaceutical formulation comprising obeticholic acid in a primary packaging, wherein the primary packaging further comprises adsorbing material. The formulation is preferably in the form of tablets for oral administration.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol

36.

CRYSTALLINE FORM OF ASCIMINIB HYDROCHLORIDE

      
Application Number EP2023081342
Publication Number 2024/100212
Status In Force
Filing Date 2023-11-09
Publication Date 2024-05-16
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Hegedus, Michal

Abstract

The application relates to the crystalline Form 1S of Asciminib hydrochloride and processes for the preparation thereof. Also described are solvates of Asciminib with 2-butanol, isobutanol, tert- butanol, 2-methyl tetra hydrofuran and cyclohexanol from which the crystalline Form 1S of Asciminib hydrochloride can be prepared.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • A61P 35/02 - Antineoplastic agents specific for leukemia
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole

37.

CAPILLARY GEL ELECTROPHORESIS SEPARATION OF DIASTEREOMERS OF PHOSPHOROTHIOATED OLIGONUCLEOTIDES

      
Application Number EP2023079519
Publication Number 2024/088984
Status In Force
Filing Date 2023-10-23
Publication Date 2024-05-02
Owner SYNTHON B.V. (Netherlands)
Inventor Durc, Pavol

Abstract

Method of identification and/or characterization of diastereomers mixtures of phosphorothioate oligonucleotides by capillary gel electrophoresis with a background electrolyte that has a pH 6 to 8, comprising the steps of: a) Preparing a gel matrix by dissolving a water soluble polymer containing a side chain having a functional group that interacts with diastereomers mixture to be analysed in a background electrolyte; b) Introducing the gel matrix in the capillary; c) Introducing the sample of diastereomers mixture of phosphorothioate to capillary; d) Applying an electric field greater than 200 volts/cm of capillary across the gel matrix in the capillary; e) Detecting the individual diastereomers and/or the characteristic groups of partially separated diastereomers of phosphorothioate oligonucleotides.

IPC Classes  ?

38.

PROCESS FOR MAKING IBRUTINIB

      
Application Number 18261896
Status Pending
Filing Date 2022-01-20
First Publication Date 2024-03-21
Owner Synthon B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Vyklicky, Libor
  • Bartl, Jiri
  • Smekal, Oldrich

Abstract

The presented invention relates to a process for preparation of Ibrutinib, comprising: a. Reacting compound of Formula (2) with compound of Formula (3) in a presence of Lewis acid to provide compound of Formula (4); b. Contacting compound of Formula (4) with toluene; c. Isolate a solid form of compound of Formula (4); d. Transforming compound of Formula (4) into Ibrutinib. The presented invention relates to a process for preparation of Ibrutinib, comprising: a. Reacting compound of Formula (2) with compound of Formula (3) in a presence of Lewis acid to provide compound of Formula (4); b. Contacting compound of Formula (4) with toluene; c. Isolate a solid form of compound of Formula (4); d. Transforming compound of Formula (4) into Ibrutinib.

IPC Classes  ?

39.

PROLONGED RELEASE TOFACITINIB COMPOSITIONS WITHOUT FUNCTIONAL COATING

      
Application Number EP2023073382
Publication Number 2024/042218
Status In Force
Filing Date 2023-08-25
Publication Date 2024-02-29
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib or a pharmaceutically acceptable salt thereof, without a functional coating.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

40.

Process for making palbociclib

      
Application Number 18474840
Grant Number 12240847
Status In Force
Filing Date 2023-09-26
First Publication Date 2024-02-01
Grant Date 2025-03-04
Owner Synthon B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Smekal, Oldrich

Abstract

The present invention relates to a process for preparation of palbociclib, compound of formula (1) or a salt thereof, wherein an intermediate, compound (2), is formed by reacting a compound of formula (3) and a compound of formula (4) in a solvent mixture comprising methanol and butanol: The intermediate (2) can be transformed into palbociclib or a salt thereof.

IPC Classes  ?

41.

BUDESONIDE TWO LAYERS CAPSULE FORMULATION

      
Application Number EP2023069160
Publication Number 2024/013154
Status In Force
Filing Date 2023-07-11
Publication Date 2024-01-18
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a Budesonide formulation with one or more layers comprising organic acid and Budesonide in the same layer.

IPC Classes  ?

  • A61K 9/50 - Microcapsules
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin

42.

SIPONIMOD SALTS AND COCRYSTALS

      
Application Number 18246566
Status Pending
Filing Date 2021-09-24
First Publication Date 2024-01-11
Owner Synthon B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Partl, Jiri
  • Tesson, Nicolas
  • Trilla Castano, Montserrat

Abstract

The presented invention relates to solid forms of Siponimod adipic acid salt and cocrystal.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • C07C 55/14 - Adipic acid

43.

SOLID FORMS OF COPANLISIB SALTS

      
Application Number EP2023062757
Publication Number 2023/218032
Status In Force
Filing Date 2023-05-12
Publication Date 2023-11-16
Owner SYNTHON B.V. (Netherlands)
Inventor Dymacek, Bohumil

Abstract

The invention relates to solid forms of Copanlisib hydrogen phosphate salt or Copanlisib fumarate salt or Copanlisib ditosylate salt or Copanlisib hydrogen citrate salt or Copanlisib maleate salt or Copanlisib malate salt or Copanlisib tartrate salt or Copanlisib dilactate salt or Copanlisib diacetate salt or Copanlisib dihydrochloride salt.

IPC Classes  ?

44.

Synthon

      
Application Number 1757730
Status Registered
Filing Date 2023-05-30
Registration Date 2023-05-30
Owner Synthon B.V. (Netherlands)
NICE Classes  ?
  • 05 - Pharmaceutical, veterinary and sanitary products
  • 10 - Medical apparatus and instruments
  • 35 - Advertising and business services
  • 40 - Treatment of materials; recycling, air and water treatment,
  • 42 - Scientific, technological and industrial services, research and design
  • 45 - Legal and security services; personal services for individuals.

Goods & Services

Pharmaceutical preparations, substances and compositions; biological and biochemical drug and cultures for medical use; pharmaceutical active substances; pharmaceutical components and ingredients. Surgical and medical devices, apparatus and instruments; orthopedic articles; injection apparatus for medical purposes. Office functions relating to the registration of pharmaceutical preparations; compiling registration files, for others; procurement of contracts for others; commercial administration of the licensing of goods; advertising, marketing and promotional services for the sale of pharmaceutical drugs, pharmaceutical preparations and medical devices; retail and wholesale services for pharmaceutical drugs, pharmaceutical preparations and medical devices; retail and online sale of pharmaceutical drugs, pharmaceutical preparations and medical devices. Treatment of materials, including on request, for others, for the purpose of manufacturing pharmaceutical and biopharmaceutical preparations; manufacture, for others, of pharmaceutical and biopharmaceutical preparations and raw materials for the pharmaceutical industry. Consulting services in the field of pharmaceutical research; biomedical research services; chemistry and biology laboratories; scientific laboratory services; pharmaceutical research and development in the pharmaceutical field; information relating to medical and scientific research in the field of pharmaceutical preparations; providing information on the results of clinical trials for pharmaceutical preparations; quality control of products for the purpose of certification; laboratory research and laboratory analysis; research and design for the pharmaceutical industry; research and development of new products for others; drug discovery testing in the context of quality control; conducting clinical trials for pharmaceutical preparations; conducting quality control of pharmaceutical preparations; providing information and data relating to medical research and developments; scientific and medical research and development; development of medicines to be sold by and under the trademark of third parties; development of pharmaceutical ingredients for the pharmaceutical industry. Legal services relating to obtaining pharmaceutical registrations and compiling pharmaceutical registration files; management of industrial property and copyright by means of license agreements (legal services); licensing of intellectual property; management of industrial property and copyright by issuing licenses to others (legal services); legal extensions relating to the retention of intellectual property, for others; legal advice in the field of intellectual property.

45.

PHARMACEUTICAL COMPOSITION COMPRISING IBRUTINIB

      
Application Number 18043176
Status Pending
Filing Date 2021-08-23
First Publication Date 2023-10-12
Owner Synthon B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a coated tablet composition comprising ibrutinib and one or more pharmaceutically acceptable excipients, characterized in that: ⋅Ibmtinib is form C, having characteristic peaks in the X-ray powder diffraction pattern at the following 2 theta (±0.2) angles: 6.9°, 18.2°, 19.2°, 19.6° and 23.0°, measured using a Cu Kα radiation; and ⋅The coating is free of plasticizer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of chronic lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL), Waldenström's macroglobulinaemia (WM) and chronic graft-versus-host disease (cGVHD).

IPC Classes  ?

  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

46.

SOLID FORMS OF VISMODEGIB

      
Application Number EP2023058668
Publication Number 2023/194300
Status In Force
Filing Date 2023-04-03
Publication Date 2023-10-12
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

Presented invention relates to solid forms of Vismodegib, compound of formula (1) and processes for preparation thereof.

IPC Classes  ?

47.

Process for preparation of apalutamide

      
Application Number 18043777
Grant Number 12606539
Status In Force
Filing Date 2021-09-03
First Publication Date 2023-10-05
Grant Date 2026-04-21
Owner Synthon B.V. (Netherlands)
Inventor
  • Hylse, Ondrej
  • Chalupa, David
  • Dymacek, Bohumil
  • Buchlovic, Marian

Abstract

The presented invention relates to a process for preparation of Apalutamide, compound (1) or a salt or a solvate thereof: The presented invention further relates to solid forms of Apalutamide, solvates of Apalutamide and to processes for preparation thereof. The presented invention also relates to solid forms of intermediates used in the process for preparing Compound (1).

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
  • C07C 229/48 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring

48.

CABOZANTINIB SALT WITH L-(+)-TARTARIC ACID AND SOLID FORMS THEREOF

      
Document Number 03245315
Status Pending
Filing Date 2023-02-28
Open to Public Date 2023-09-07
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Jelinkova, Katerina

Abstract

The invention relates to solid forms of Cabozantinib, compound of formula (1), salt with L-(+)-tartaric acid and processes for preparation thereof,

IPC Classes  ?

49.

CABOZANTINIB SALT WITH L-(+)-TARTARIC ACID AND SOLID FORMS THEREOF

      
Application Number EP2023054897
Publication Number 2023/165948
Status In Force
Filing Date 2023-02-28
Publication Date 2023-09-07
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Jelinkova, Katerina

Abstract

The invention relates to solid forms of Cabozantinib, compound of formula (1), salt with L-(+)-tartaric acid and processes for preparation thereof,

IPC Classes  ?

50.

SOLID FORMS OF ALECTINIB AND ALECTINIB SALTS

      
Application Number EP2023054326
Publication Number 2023/161233
Status In Force
Filing Date 2023-02-21
Publication Date 2023-08-31
Owner SYNTHON B.V. (Netherlands)
Inventor Dymacek, Bohumil

Abstract

The invention relates to Alectinib, compound of formula (1), solid forms thereof, salts thereof, solid forms of the salts and processes for preparation thereof,.

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
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/04 - Antineoplastic agents specific for metastasis

51.

IMPROVED PROCESS FOR PREPARATION OF COPANLISIB

      
Application Number EP2023051132
Publication Number 2023/139125
Status In Force
Filing Date 2023-01-18
Publication Date 2023-07-27
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dragounova, Kristyna
  • Benovsky, Petr

Abstract

The presented invention relates to a process for preparation of Copanlisib, compound of formula (1), or a salt or a solvate thereof comprising:.

IPC Classes  ?

52.

Crystalline form of ozanimod hydrochloride

      
Application Number 17995180
Grant Number 12398112
Status In Force
Filing Date 2021-03-17
First Publication Date 2023-06-15
Grant Date 2025-08-26
Owner Synthon B.V. (Netherlands)
Inventor Westheim, Raymond

Abstract

The presented invention relates to crystalline form, Form A of Ozanimod hydrochloride, processes for preparation thereof and pharmaceutical compositions comprising the Ozanimod hydrochloride Form A.

IPC Classes  ?

  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles

53.

PHARMACEUTICAL COMPOSITION COMPRISING IBRUTINIB

      
Application Number EP2022084622
Publication Number 2023/104808
Status In Force
Filing Date 2022-12-06
Publication Date 2023-06-15
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising Ibrutinib and one or more pharmaceutically acceptable excipients. The invention further relates to the use of said composition as a medicament, particularly in the treatment of chronic lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL), Waldenstrӧm's macroglobulinaemia (WM) and chronic graft versus host disease (cGVHD).

IPC Classes  ?

54.

PHARMACEUTICAL COMPOSITION OF BEMPEDOIC ACID

      
Document Number 03231425
Status Pending
Filing Date 2022-09-12
Open to Public Date 2023-03-16
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The presented invention relates to pharmaceutical composition comprising Bempedoic acid and processes for preparation thereof.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid

55.

PHARMACEUTICAL COMPOSITION OF BEMPEDOIC ACID

      
Application Number EP2022075272
Publication Number 2023/036980
Status In Force
Filing Date 2022-09-12
Publication Date 2023-03-16
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The presented invention relates to pharmaceutical composition comprising Bempedoic acid and processes for preparation thereof.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid

56.

A PROCESS FOR MAKING OSIMERTINIB

      
Document Number 03229553
Status Pending
Filing Date 2022-09-01
Open to Public Date 2023-03-09
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vyklicky, Libor
  • Zabadal, Miroslav

Abstract

The invention deals with a novel process for preparation of the pharmaceutically useful product Osimertinib of formula (1).

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

57.

A PROCESS FOR MAKING OSIMERTINIB

      
Application Number EP2022074288
Publication Number 2023/031316
Status In Force
Filing Date 2022-09-01
Publication Date 2023-03-09
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vyklicky, Libor
  • Zabadal, Miroslav

Abstract

The invention deals with a novel process for preparation of the pharmaceutically useful product Osimertinib of formula (1).

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

58.

CRYSTALLINE FORMS OF TAFAMIDIS NICOTINAMIDE ADDUCT

      
Application Number EP2022070086
Publication Number 2023/020762
Status In Force
Filing Date 2022-07-18
Publication Date 2023-02-23
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

The presented invention relates to Tafamidis nicotinamide adduct, solid form thereof, crystalline form thereof, processes for preparation thereof and a composition comprising it.

IPC Classes  ?

  • C07D 213/82 - AmidesImides in position 3
  • C07D 263/57 - Aryl or substituted aryl radicals
  • A61P 17/00 - Drugs for dermatological disorders
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 43/00 - Drugs for specific purposes, not provided for in groups
  • A61K 31/423 - Oxazoles condensed with carbocyclic rings

59.

Crystalline forms of sodium salt of Bempedoic acid

      
Application Number 17781915
Grant Number 12516013
Status In Force
Filing Date 2020-12-04
First Publication Date 2023-02-02
Grant Date 2026-01-06
Owner Synthon B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

The presented invention relates to crystalline Forms (I) or (II) or (III) or (IV) of sodium salt of Bempedoic acid, processes for preparation thereof and a composition comprising it.

IPC Classes  ?

  • C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups

60.

Pharmaceutical composition comprising eltrombopag bis(monoethanolamine)

      
Application Number 17782425
Grant Number 12409165
Status In Force
Filing Date 2020-12-04
First Publication Date 2023-01-26
Grant Date 2025-09-09
Owner Synthon B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising calcium silicate as diluent. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia in patients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets

61.

PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG BIS(MONOETHANOLAMINE)

      
Application Number 17782408
Status Pending
Filing Date 2020-12-04
First Publication Date 2023-01-26
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising maltose and isomalt as diluents. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia inpatients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
  • A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers

62.

CONTROLLED RELEASE TOFACITINIB COMPOSITIONS

      
Application Number 17638448
Status Pending
Filing Date 2020-08-27
First Publication Date 2022-12-22
Owner Synthon B.V. (Netherlands)
Inventor
  • Alvarez Fernandez, Lisardo
  • Nogueiras Nieto, Luis
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/50 - Microcapsules
  • A61K 9/20 - Pills, lozenges or tablets

63.

PROCESS FOR MAKING MELFLUFEN OR A SALT THEREOF

      
Application Number EP2022064901
Publication Number 2022/253894
Status In Force
Filing Date 2022-06-01
Publication Date 2022-12-08
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Bartos, Petr
  • Castulik, Jakub

Abstract

The present invention relates to process for preparing Melflufen, compound of formula (1) or a salt thereof, and to intermediates used in the process and solid forms thereof.

IPC Classes  ?

64.

PROLONGED RELEASE TOFACITINIB COMPOSITIONS

      
Application Number EP2022065209
Publication Number 2022/254017
Status In Force
Filing Date 2022-06-03
Publication Date 2022-12-08
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a monolithic tablet composition for oral administration of tofacitinib, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis

65.

PHARMACEUTICAL COMPOSITION COMPRISING ENZALUTAMIDE

      
Application Number 17765934
Status Pending
Filing Date 2020-10-01
First Publication Date 2022-11-03
Owner Synthon B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising a granulate consisting of a co-precipitate on a substrate, wherein the co-precipitate comprises enzalutamide in amorphous form and a cellulosic concentration enhancing polymer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of castration-resistant prostate cancer.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
  • A61J 3/10 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
  • A61J 3/00 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms

66.

Crystalline forms of bempedoic acid

      
Application Number 17765956
Grant Number 12528759
Status In Force
Filing Date 2020-10-02
First Publication Date 2022-11-03
Grant Date 2026-01-20
Owner Synthon B.V. (Netherlands)
Inventor
  • Hegedus, Michal
  • Westheim, Raymond

Abstract

The presented invention relates to crystalline Form A and Form B of Bempedoic acid, a process for preparation thereof and a composition comprising the Form A or Form B.

IPC Classes  ?

  • C07C 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation

67.

SALTS OF OMECAMTIV MECARBIL AND SOLID FORMS THEREOF

      
Application Number 17761900
Status Pending
Filing Date 2020-09-18
First Publication Date 2022-11-03
Owner SYNTHON B.V. (Netherlands)
Inventor Jelinkova, Katerina

Abstract

The presented invention relates to Omecamtiv mecarbil salts with methane sulfonic acid, benzene sulfonic acid and p-toluene sulfonic acid and to processes for preparation thereof.

IPC Classes  ?

  • C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates

68.

SALTS OF OMECAMTIV MECARBIL AND SOLID FORMS THEREOF

      
Application Number 17761944
Status Pending
Filing Date 2020-09-18
First Publication Date 2022-10-27
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Jelinkova, Katerina
  • Hegedus, Michal

Abstract

The presented invention relates to Omecamtiv mecarbil salts, solid forms thereof and to processes for preparation thereof.

IPC Classes  ?

  • 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

69.

LYOPHILIZED COMPOSITION OF COPANLISIB SALT

      
Application Number EP2022058763
Publication Number 2022/214400
Status In Force
Filing Date 2022-04-01
Publication Date 2022-10-13
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Zaludek, Borek
  • Lobl, Jiri

Abstract

The presented invention relates to a lyophilized pharmaceutical formulation comprising copanlisib salt and a bulking agent selected from lactose or trehalose and to a process for preparation thereof.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • 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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

70.

Isavuconazonium salts and process for preparing thereof

      
Application Number 17638102
Grant Number 12570649
Status In Force
Filing Date 2020-08-17
First Publication Date 2022-09-15
Grant Date 2026-03-10
Owner Synthon B.V. (Netherlands)
Inventor Bartos, Petr

Abstract

The present invention relates to the process of preparation of salts of compound of formula (1).

IPC Classes  ?

  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

71.

Process for preparing ozanimod

      
Application Number 17627386
Grant Number 12404256
Status In Force
Filing Date 2020-07-16
First Publication Date 2022-08-18
Grant Date 2025-09-02
Owner Synthon B.V. (Netherlands)
Inventor
  • Chalupova, Lenka
  • Buchlovic, Marian

Abstract

The present invention relates to the process of preparation of compound of formula (I) or a salt thereof. Further it relates to the solid form of compound (I).

IPC Classes  ?

  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles

72.

PROCESS FOR PREPARATION OF ENZALUTAMIDE

      
Application Number 17620314
Status Pending
Filing Date 2020-06-25
First Publication Date 2022-08-04
Owner Synthon B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Smekal, Oldrich

Abstract

The presented invention relates to a process for preparation of Enzalutamide, compound (1) or a salt or a solvate thereof Formula (1). The presented invention also related to 1,4-dioxane solvate of compound (1). The presented invention relates to a process for preparation of Enzalutamide, compound (1) or a salt or a solvate thereof Formula (1). The presented invention also related to 1,4-dioxane solvate of compound (1).

IPC Classes  ?

  • C07D 233/86 - Oxygen and sulfur atoms, e.g. thiohydantoin

73.

PROCESS FOR MAKING IBRUTINIB

      
Application Number EP2022051250
Publication Number 2022/157250
Status In Force
Filing Date 2022-01-20
Publication Date 2022-07-28
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Vyklicky, Libor
  • Bartl, Jiri
  • Smekal, Oldrich

Abstract

The presented invention relates to a process for preparation of Ibrutinib, comprising: a. Reacting compound of Formula (2) with compound of Formula (3) in a presence of Lewis acid to provide compound of Formula (4); b. Contacting compound of Formula (4) with toluene; c. Isolate a solid form of compound of Formula (4); d. Transforming compound of Formula (4) into Ibrutinib.

IPC Classes  ?

74.

Pharmaceutical composition comprising axitinib

      
Application Number 17609545
Grant Number 12290601
Status In Force
Filing Date 2020-05-08
First Publication Date 2022-07-21
Grant Date 2025-05-06
Owner Synthon B.V. (Netherlands)
Inventor
  • Gago Guillan, Manuel
  • Kumar, Rohit
  • Alvarez Fernandez, Lisardo

Abstract

The present invention relates to an immediate release tablet composition comprising axitinib form IV characterized by an XRPD pattern comprising the peaks at about 8.9, 12.0, 14.6, 15.2, 15.7, 17.8, 19.1, 20.6, 21.6, 23.2, 24.2, 24.9, 26.1 and 27.5±0.1 degrees 2θ, when measured with Cu Kα1 radiation and one or more pharmaceutically acceptable excipients, wherein the composition exhibits a dissolution rate between 40% and 70% in 30 minutes when tested in 900 ml 0.01 N hydrochloric acid pH 2.0 at 37° C., 75 rpm in a USP apparatus II.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61P 35/00 - Antineoplastic agents

75.

Process for making Siponimod and intermediate thereof

      
Application Number 17599868
Grant Number 12410126
Status In Force
Filing Date 2020-03-29
First Publication Date 2022-06-30
Grant Date 2025-09-09
Owner Synthon B.V. (Netherlands)
Inventor
  • Keltjens, Rolf
  • Hylse, Ondrej
  • Partl, Jiri

Abstract

The presented invention relates to a process for preparation of compound of formula (I) or a salt or a solvate thereof (i.e.) siponimod. The invention also relates to intermediates used in the process and solid forms of these intermediates.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • C07C 17/16 - Preparation of halogenated hydrocarbons by replacement by halogens of hydroxyl groups
  • C07C 17/18 - Preparation of halogenated hydrocarbons by replacement by halogens of oxygen atoms of carbonyl groups
  • C07C 22/08 - Cyclic compounds containing halogen atoms bound to an acyclic carbon atom having unsaturation in the rings containing six-membered aromatic rings containing fluorine
  • C07C 249/08 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes by reaction of hydroxylamines with carbonyl compounds
  • C07C 249/12 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes by reactions not involving the formation of oxyimino groups
  • C07C 251/48 - Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups bound to a carbon atom of a six-membered aromatic ring
  • C07C 251/52 - Oximes having oxygen atoms of oxyimino groups bound to carbon atoms of substituted hydrocarbon radicals of hydrocarbon radicals substituted by halogen atoms or by nitro or nitroso groups
  • C07C 303/28 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
  • C07C 309/66 - Methanesulfonates

76.

Process for preparation of Axitinib

      
Application Number 17604322
Grant Number 12522581
Status In Force
Filing Date 2020-04-09
First Publication Date 2022-06-23
Grant Date 2026-01-13
Owner Synthon B.V. (Netherlands)
Inventor
  • Castulik, Jakub
  • Skoumal, Radomir

Abstract

In a process of making Axitinib, a palladium catalyst is added to a mixture of 2-vinylpyridine and the protected intermediate of formula (III) to form protected-Axitinib of formula (IV). In the formulas, P is a protective group and X is I, Cl, Br, or trifluoromethanesulfonate. The palladium catalyst is prepared separately, before being added to the reaction mixture, and is made from a mixture of a palladium source, a ligand, and a base in a suitable solvent. By adding the palladium catalyst to this protected intermediate, the process can use lower amounts of palladium and can have faster reaction times.

IPC Classes  ?

  • C07D 401/06 - 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 only aliphatic carbon atoms
  • C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles

77.

SOLID FORMS OF BALOXAVIR, SALTS OF BALOXAVIR AND COCRYSTALS OF BALOXAVIR

      
Application Number EP2021085526
Publication Number 2022/128934
Status In Force
Filing Date 2021-12-13
Publication Date 2022-06-23
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Hegedus, Michal
  • Tesson, Nicolas

Abstract

The presented invention relates to Baloxavir, salts of Baloxavir, cocrystals of Baloxavir, to solid forms of thereof and to processes for preparation thereof.

IPC Classes  ?

  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
  • C07D 498/04 - Ortho-condensed systems
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole

78.

SIPONIMOD SALTS AND COCRYSTALS

      
Document Number 03197026
Status Pending
Filing Date 2021-09-24
Open to Public Date 2022-03-31
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Partl, Jiri
  • Tesson, Nicolas
  • Trilla Castano, Montserrat

Abstract

The presented invention relates to solid forms of Siponimod adipic acid salt and cocrystal.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

79.

SIPONIMOD SALTS AND COCRYSTALS

      
Application Number EP2021076406
Publication Number 2022/064007
Status In Force
Filing Date 2021-09-24
Publication Date 2022-03-31
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Dymacek, Bohumil
  • Partl, Jiri
  • Tesson, Nicolas
  • Trilla Castano, Montserrat

Abstract

The presented invention relates to solid forms of Siponimod adipic acid salt and cocrystal.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • A61P 37/00 - Drugs for immunological or allergic disorders

80.

IMPROVED PROCESS FOR PREPARATION OF APALUTAMIDE

      
Application Number EP2021074415
Publication Number 2022/049265
Status In Force
Filing Date 2021-09-03
Publication Date 2022-03-10
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Hylse, Ondrej
  • Chalupa, David
  • Dymacek, Bohumil
  • Buchlovic, Marian

Abstract

The presented invention relates to a process for preparation of Apalutamide, compound (1) (Formula 1) or a salt or a solvate thereof: The presented invention further relates to solid forms of Apalutamide, solvates of Apalutamide and to processes for preparation thereof. The presented invention also relates to solid forms of intermediates used in the process for preparing Compound (1).

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
  • C07C 229/48 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring

81.

Crystalline forms and processes of lenvatinib besylate

      
Application Number 17282505
Grant Number 12102630
Status In Force
Filing Date 2019-10-01
First Publication Date 2022-03-03
Grant Date 2024-10-01
Owner Synthon B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Westheim, Raymond
  • Jelinkova, Katerina

Abstract

The present invention relates to lenvatinib besylate, its crystalline forms and processes for making them. Furthermore, to a pharmaceutical composition comprising a therapeutically effective dose of lenvatinib besylate.

IPC Classes  ?

  • A61K 31/47 - QuinolinesIsoquinolines
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • C07D 215/48 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

82.

PHARMACEUTICAL COMPOSITION COMPRISING IBRUTINIB

      
Application Number EP2021073253
Publication Number 2022/043251
Status In Force
Filing Date 2021-08-23
Publication Date 2022-03-03
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Vivancos Martinez, Marta
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a coated tablet composition comprising ibrutinib and one or more pharmaceutically acceptable excipients, characterized in that: • Ibrutinib is form C, having characteristic peaks in the X-ray powder diffraction pattern at the following 2 theta (± 0.2) angles: 6.9º, 18.2º, 19.2º, 19.6º and 23.0º, measured using a Cu Kα radiation; and • The coating is free of plasticizer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of chronic lymphocytic leukaemia (CLL), mantle cell lymphoma (MCL), Waldenstrӧm's macroglobulinaemia (WM) and chronic graft-versus-host disease (cGVHD).

IPC Classes  ?

  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 35/00 - Antineoplastic agents
  • A61P 35/02 - Antineoplastic agents specific for leukemia
  • A61K 9/20 - Pills, lozenges or tablets

83.

PHARMACEUTICAL COMPOSITION COMPRISING IVACAFTOR

      
Application Number EP2021069774
Publication Number 2022/013360
Status In Force
Filing Date 2021-07-15
Publication Date 2022-01-20
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to an immediate release tablet composition comprising free particles of ivacaftor a pH dependent polymer and surfactant extragranularly and intragranularly.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

84.

SALTS OF BEMPEDOIC ACID

      
Application Number EP2021066439
Publication Number 2021/255180
Status In Force
Filing Date 2021-06-17
Publication Date 2021-12-23
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

The present invention relates to 2-aminoethanol, piperazine and L- lysine salts of Bempedoic acid and processes for the preparation thereof.

IPC Classes  ?

  • C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups
  • C07D 295/027 - 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
  • C07C 215/08 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
  • C07C 229/26 - 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 more than one amino group bound to the carbon skeleton, e.g. lysine

85.

GRIPMATE

      
Serial Number 97185273
Status Registered
Filing Date 2021-12-22
Registration Date 2025-12-02
Owner Synthon B.V. (Netherlands)
NICE Classes  ? 10 - Medical apparatus and instruments

Goods & Services

Medical apparatus, namely, infusion and injection devices for administering drugs

86.

Process for preparing ozanimod

      
Application Number 17311094
Grant Number 11390593
Status In Force
Filing Date 2019-12-05
First Publication Date 2021-11-25
Grant Date 2022-07-19
Owner Synthon B.V. (Netherlands)
Inventor
  • Buchlovic, Marian
  • Chalupova, Lenka
  • Vyklicky, Libor
  • Bartl, Jiri

Abstract

The presented invention relates to a process for preparation of compound of formula (1) or a salt thereof (i.e.) ozanimod: (1). The invention also relates to intermediates used in the process.

IPC Classes  ?

  • C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
  • C07D 263/22 - Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms

87.

CRYSTALLINE FORM OF OZANIMOD HYDROCHLORIDE

      
Application Number EP2021056821
Publication Number 2021/197852
Status In Force
Filing Date 2021-03-17
Publication Date 2021-10-07
Owner SYNTHON B.V. (Netherlands)
Inventor Westheim, Raymond

Abstract

The presented invention relates to crystalline form, Form A of Ozanimod hydrochloride, processes for preparation thereof and pharmaceutical compositions comprising the Ozanimod hydrochloride Form A.

IPC Classes  ?

88.

PHARMACEUTICAL COMPOSITIONS COMPRISING ELAGOLIX SODIUM

      
Application Number EP2021056219
Publication Number 2021/180862
Status In Force
Filing Date 2021-03-11
Publication Date 2021-09-16
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Garcia Jimenez, Sonia
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to pharmaceutical compositions comprising a therapeutically effective dose of elagolix sodium and pharmaceutically acceptable excipients comprising a super disintegrant. The compositions can further comprise an alkalizer and/or a non-ionic surfactant.

IPC Classes  ?

89.

Process for making palbociclib

      
Application Number 17057425
Grant Number 11858928
Status In Force
Filing Date 2019-05-21
First Publication Date 2021-07-08
Grant Date 2024-01-02
Owner Synthon B.V. (Netherlands)
Inventor
  • Mitas, Petr
  • Smekal, Oldrich

Abstract

The present invention related to a process for preparation of compound of formula (1) or a salt thereof (i.e.) palbociclib: The invention also relates to a solid crystalline form of intermediate of formula (2) used in the process:

IPC Classes  ?

90.

Purification of sugammadex

      
Application Number 17045736
Grant Number 11225565
Status In Force
Filing Date 2019-04-08
First Publication Date 2021-06-17
Grant Date 2022-01-18
Owner Synthon B.V. (Netherlands)
Inventor
  • Buchlovic, Marian
  • Cernova, Lenka

Abstract

The invention deals with a novel process for purification of the pharmaceutically useful product sugammadex of formula (1).

IPC Classes  ?

  • C08L 5/16 - CyclodextrinDerivatives thereof

91.

PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG BIS(MONOETHANOLAMINE)

      
Application Number EP2020084690
Publication Number 2021/110942
Status In Force
Filing Date 2020-12-04
Publication Date 2021-06-10
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising maltose and isomalt as diluents. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia in patients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid

92.

PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG BIS(MONOETHANOLAMINE)

      
Document Number 03160779
Status Pending
Filing Date 2020-12-04
Open to Public Date 2021-06-10
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising calcium silicate as diluent. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia in patients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid

93.

CRYSTALLINE FORMS OF SODIUM SALT OF BEMPEDOIC ACID

      
Application Number EP2020084664
Publication Number 2021/110929
Status In Force
Filing Date 2020-12-04
Publication Date 2021-06-10
Owner SYNTHON B.V. (Netherlands)
Inventor Hegedus, Michal

Abstract

The presented invention relates to crystalline Forms (I) or (II) or (III) or (IV) of sodium salt of Bempedoic acid, processes for preparation thereof and a composition comprising it.

IPC Classes  ?

  • C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups
  • 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

94.

PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG BIS(MONOETHANOLAMINE)

      
Application Number EP2020084723
Publication Number 2021/110959
Status In Force
Filing Date 2020-12-04
Publication Date 2021-06-10
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Nogueiras Nieto, Luis
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a film-coated swallowable tablet comprising eltrombopag bis(monoethanolamine) and pharmaceutically acceptable excipients comprising calcium silicate as diluent. The invention further relates to the use of said tablet as a medicament, particularly in the treatment of immune thrombocytopenia (ITP), thrombocytopenia in patients with chronic hepatitis C virus (HCV) and severe aplastic anaemia (SAA).

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid

95.

PHARMACEUTICAL COMPOSITION COMPRISING ENZALUTAMIDE

      
Document Number 03152909
Status Pending
Filing Date 2020-10-01
Open to Public Date 2021-04-08
Owner SYNTHON BV (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising a granulate consisting of a co-precipitate on a substrate, wherein the co-precipitate comprises enzalutamide in amorphous form and a cellulosic concentration enhancing polymer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of castration-resistant prostate cancer.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

96.

PHARMACEUTICAL COMPOSITION COMPRISING ENZALUTAMIDE

      
Application Number EP2020077565
Publication Number 2021/064123
Status In Force
Filing Date 2020-10-01
Publication Date 2021-04-08
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Fradera Gelabert, Sara
  • Alvarez Fernandez, Lisardo
  • Kumar, Rohit

Abstract

The present invention relates to a tablet composition comprising a granulate consisting of a co-precipitate on a substrate, wherein the co-precipitate comprises enzalutamide in amorphous form and a cellulosic concentration enhancing polymer. The invention further relates to the use of said composition as a medicament, particularly in the treatment of castration-resistant prostate cancer.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

97.

CRYSTALLINE FORMS OF BEMPEDOIC ACID

      
Application Number EP2020077645
Publication Number 2021/064166
Status In Force
Filing Date 2020-10-02
Publication Date 2021-04-08
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Hegedus, Michal
  • Westheim, Raymond

Abstract

The presented invention relates to crystalline Form A and Form B of Bempedoic acid, a process for preparation thereof and a composition comprising the Form A or Form B.

IPC Classes  ?

  • C07C 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation
  • C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups

98.

SALTS OF OMECAMTIV MECARBIL AND SOLID FORMS THEREOF

      
Application Number EP2020076162
Publication Number 2021/053175
Status In Force
Filing Date 2020-09-18
Publication Date 2021-03-25
Owner SYNTHON B.V. (Netherlands)
Inventor Jelinkova, Katerina

Abstract

The presented invention relates to Omecamtiv mecarbil salts with methane sulfonic acid, benzene sulfonic acid and p-toluene sulfonic acid and to processes for preparation thereof.

IPC Classes  ?

  • 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
  • A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins

99.

SALTS OF OMECAMTIV MECARBIL AND SOLID FORMS THEREOF

      
Application Number EP2020076180
Publication Number 2021/053189
Status In Force
Filing Date 2020-09-18
Publication Date 2021-03-25
Owner SYNTHON B.V. (Netherlands)
Inventor
  • Jelinkova, Katerina
  • Hegedus, Michal

Abstract

The presented invention relates to Omecamtiv mecarbil salts, solid forms thereof and to processes for preparation thereof.

IPC Classes  ?

  • 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
  • A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins

100.

ISAVUCONAZONIUM SALTS AND PROCESS FOR PREPARING THEREOF

      
Application Number EP2020072988
Publication Number 2021/037597
Status In Force
Filing Date 2020-08-17
Publication Date 2021-03-04
Owner SYNTHON B.V. (Netherlands)
Inventor Bartos, Petr

Abstract

The present invention relates to the process of preparation of salts of compound of formula (1).

IPC Classes  ?

  • A61P 31/10 - Antimycotics
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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