Actelion Pharmaceuticals Ltd

Switzerland

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Date
2024 December 1
2024 16
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IPC Class
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings 49
A61P 25/00 - Drugs for disorders of the nervous system 47
A61P 9/12 - Antihypertensives 42
C07D 471/04 - Ortho-condensed systems 41
A61K 31/4965 - Non-condensed pyrazines 38
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NICE Class
05 - Pharmaceutical, veterinary and sanitary products 167
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services 47
09 - Scientific and electric apparatus and instruments 30
16 - Paper, cardboard and goods made from these materials 29
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1.

PROCESS FOR MANUFACTURING A DIPHENYLPHRAZINE DERIVATIVE

      
Application Number 18262777
Status Pending
Filing Date 2022-01-28
First Publication Date 2024-12-26
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Vanierschot, Ronny
  • Collas, Alain
  • Leys, Carina
  • Van Mechelen, Kore

Abstract

The present invention relates to a process for the manufacturing of calcium; {4-[(5, 6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate, or a pharmaceutically acceptable hydrate or solvate thereof. Moreover, it relates to calcium; {4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate with high purity, as well as to crystalline forms of calcium; {4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate and hydrates and solvates thereof. Furthermore, the invention relates to the use of calcium; {4-[(5, 6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate for the treatment or prevention of e.g. pulmonary arterial hypertension (PAH) or chronic thromboembolic pulmonary hypertension (CTEPH).

IPC Classes  ?

2.

PYRAZOLOPYRIMIDINES AND THEIR USES AS PDGFR INHIBITORS

      
Application Number 18293023
Status Pending
Filing Date 2022-07-29
First Publication Date 2024-10-31
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Bauman, David
  • Liu, Zhijie
  • Lu, Tianbao

Abstract

The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described. The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

  • C07D 487/04 - Ortho-condensed systems
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
  • A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
  • C07D 471/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

3.

PHARMACEUTICAL COMPOSITION COMPRISING A DIPHENYLPYRAZINE DERIVATIVE

      
Application Number EP2024057700
Publication Number 2024/194449
Status In Force
Filing Date 2024-03-22
Publication Date 2024-09-26
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Axelsen, Lene Nygaard
  • D'Hoore, Peter
  • Fabbrini, Elisa
  • Kimpe, Kristof
  • Remenova, Tatiana
  • Swain, Jabaris
  • Verstraeten, Maxim
  • Verwaest, Kim

Abstract

The present invention relates to a pharmaceutical composition suitable for administration by subcutaneous or intramuscular injection, comprising calcium;{4-[(5,6-diphenylpyrazin- 2-yl)(propan-2-yl)amino]butoxy}acetate or hydrate or solvate thereof in the form of an aqueous suspension. In particular, such suspension is an aqueous suspension comprising microparticles of calcium;{4-[(5,6-diphenylpyrazin-2-yl)(propan-2- yl)amino]butoxy}acetate or hydrate or solvate thereof; and further comprising a surfactant and/or wetting agent, a flocculating agent, and optionally an antioxidant.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/10 - DispersionsEmulsions
  • A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 47/02 - Inorganic compounds
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
  • A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
  • A61P 11/00 - Drugs for disorders of the respiratory system

4.

METHODS FOR TREATING PULMONARY HYPERTENSION IN PATIENTS WITH LEFT VENTRICULAR ASSIST DEVICE IMPLANTATION

      
Application Number 18547959
Status Pending
Filing Date 2022-02-25
First Publication Date 2024-09-12
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Rocco, Mark
  • Selej, Mona
  • Zhao, Carol

Abstract

The present disclosure provides methods for treating pulmonary hypertension in a patient with left ventricular assist device (LVAD) implantation and methods of improving cardiac transplant eligibility in a patient with LVAD implantation. The methods include administering to a patient in need thereof a therapeutically effective amount of macitentan or aprocitentan.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61M 60/90 - Details not provided for in groups , or
  • A61P 9/12 - Antihypertensives

5.

PHARMACEUTICAL COMPOSITION COMPRISING A DIPHENYLPYRAZINE DERIVATIVE

      
Application Number 18435817
Status Pending
Filing Date 2024-02-07
First Publication Date 2024-07-04
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Amssoms, Katie
  • De Proost, Eddy
  • Dong, Wenyu
  • Hartman Kok, Paul
  • Holm, Rene
  • Kimpe, Kristof
  • Meurs, Greet
  • Verstraeten, Maxim

Abstract

The present invention relates to a pharmaceutical composition comprising the calcium; {4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate, in particular to long-acting injectables comprising the same, the use of the pharmaceutical composition for the treatment or prevention of specific diseases, and a process to produce it.

IPC Classes  ?

  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • 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

6.

IN VITRO DISSOLUTION TEST

      
Application Number EP2023087180
Publication Number 2024/133620
Status In Force
Filing Date 2023-12-21
Publication Date 2024-06-27
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Mallants, Michelle
  • Moes, Johannes
  • Peeters, Daisy

Abstract

The present invention relates to testing samples comprising calcium;{4-[(5,6- diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate, or a pharmaceutically acceptable hydrate or solvate thereof, in the form of microparticles and/or nanoparticles, such as suspensions, and measuring the dissolution of the calcium;{4-[(5,6-diphenylpyrazin-2- yl)(propan-2-yl)amino]butoxy}acetate, or a pharmaceutically acceptable hydrate or solvate thereof, in an aqueous medium. The present invention also relates to quality control testing of said samples and to releasing batches comprising said samples for pharmaceutical use. The present invention also relates to a medium for use in dissolution testing.

IPC Classes  ?

  • G01N 33/15 - Medicinal preparations
  • G01N 13/00 - Investigating surface or boundary effects, e.g. wetting powerInvestigating diffusion effectsAnalysing materials by determining surface, boundary, or diffusion effects

7.

PYRAZOLOPYRROLOPYRIDAZINES AND THEIR USES AS PDGFR INHIBITORS

      
Application Number EP2023081630
Publication Number 2024/104968
Status In Force
Filing Date 2023-11-13
Publication Date 2024-05-23
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Lu, Tianbao
  • Liu, Zhijie

Abstract

The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

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
  • 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 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 487/14 - Ortho-condensed systems
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems

8.

EDVANCI

      
Serial Number 98560473
Status Pending
Filing Date 2024-05-21
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Human pharmaceutical preparations for the prevention and treatment of viral diseases, auto-immune and inflammatory diseases, alloimmune diseases, cardiovascular and pulmonary diseases, central nervous system diseases, peripheral neurological system diseases, pain, dermatologic diseases, gastro-intestinal diseases, infectious-related diseases, metabolic diseases, oncologic diseases, ophthalmic diseases, respiratory diseases, hematological diseases, urological diseases, maternal fetal disorders, digital ulcers

9.

COMBINATION OF MACITENTAN AND TADALAFIL FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION

      
Application Number EP2023080821
Publication Number 2024/099953
Status In Force
Filing Date 2023-11-06
Publication Date 2024-05-16
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Morganti, Adele
  • Lassen, Cheryl

Abstract

The present disclosure relates to methods for treating pulmonary arterial hypertension (PAH), comprising administering a fixed dose combination (FDC) comprising macitentan and tadalafil to a human patient in need thereof. The disclosure also provides methods of reducing pulmonary vascular resistance (PVR) and/or increasing six-minute walk distance (6MWD) in a patient having PAH, comprising transitioning said patient to a FDC of macitentan and tadalafil. Prior to administering the FDC, the patient is PAH-specific treatment naive, treated with endothelin receptor antagonist (ERA) monotherapy, or treated with phosphodiesterase type-5 inhibitor (PDE-5) inhibitor monotherapy.

IPC Classes  ?

  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 9/12 - Antihypertensives
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

10.

METHODS AND COMPOSITIONS FOR DETECTING OR AIDING DIAGNOSIS OF PULMONARY HYPERTENSION

      
Application Number IB2023060855
Publication Number 2024/089662
Status In Force
Filing Date 2023-10-27
Publication Date 2024-05-02
Owner
  • ACTELION PHARMACEUTICALS LTD (Switzerland)
  • THE BRIGHAM AND WOMAN'S HOSPITAL, INC. (USA)
Inventor
  • Fong, You-Lian
  • Jatkoe, Timothy Allen
  • Cheng, He
  • Zhuo, Lihan

Abstract

Biomarkers that can be used for the detection and/or aid in the diagnosis of disease states, preferably pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH), to methods of treating PH or PAH in a subject are described. Also described are probes capable of detecting the biomarkers and related methods and kits for detecting or aiding in the diagnosis of PH or PAH.

IPC Classes  ?

  • C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material

11.

METHODS AND COMPOSITIONS FOR DETECTING OR AIDING DIAGNOSIS OF PULMONARY HYPERTENSION

      
Application Number IB2023060918
Publication Number 2024/089673
Status In Force
Filing Date 2023-10-30
Publication Date 2024-05-02
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Fong, Yiu-Lian
  • Jatkoe, Timothy Allen
  • Cheng, He
  • Zhuo, Lihan

Abstract

Biomarkers that can be used for the detection and/or aid in the diagnosis of disease states, preferably pulmonary hypertension (PH), pulmonary arterial hypertension (PAH), chronic thromboembolic pulmonary hypertension (CTEPH), PH in chronic lung disease (PH-CLD), or PH due to left-sided heart disease (PH-LHD), to methods of treating PH, PAH, CTEPH, PH-CLD, or PH-LHD in a subject are described. Also described are probes capable of detecting the biomarkers and related methods and kits for detecting or aiding in the diagnosis of PH, PAH, CTEPH, PH-CLD, or PH-LHD.

IPC Classes  ?

  • C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material

12.

PHARMACEUTICAL COMBINATION COMPRISING A SELECTIVE S1P1 RECEPTOR AGONIST

      
Application Number 18401886
Status Pending
Filing Date 2024-01-02
First Publication Date 2024-04-25
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Clozel, Martine
  • Piali, Luca

Abstract

The present invention relates to a pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z] propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
  • A61K 31/225 - Polycarboxylic acids
  • A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
  • A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide

13.

OCYNTIO

      
Serial Number 98491066
Status Pending
Filing Date 2024-04-09
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Human pharmaceutical preparations for the prevention and treatment of viral diseases, auto-immune and inflammatory diseases, pulmonary diseases, cardiovascular diseases, central nervous system diseases, pain, dermatologic diseases, gastro-intestinal diseases, infection-related diseases, metabolic diseases, oncologic diseases, cerebrovascular diseases, ophthalmic diseases, and respiratory diseases; pharmaceutical anti-allergic preparations and substances; vaccines

14.

PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS

      
Application Number 18258675
Status Pending
Filing Date 2021-12-22
First Publication Date 2024-04-04
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Bauman, David
  • Liu, Zhijie
  • Lu, Tianbao
  • Zhu, Bin
  • Nguyen, Van
  • Cavitt, Marchello
  • Hawkins, Michael J.

Abstract

The disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described. The disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • C07D 513/04 - Ortho-condensed systems

15.

PHARMACEUTICAL COMPOSITION COMPRISING A DIPHENYLPYRAZINE DERIVATIVE

      
Application Number 18261923
Status Pending
Filing Date 2022-01-28
First Publication Date 2024-03-21
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Amssoms, Katie
  • De Proost, Eddy
  • Dong, Wenyu
  • Hartman Kok, Paul
  • Holm, Rene
  • Kimpe, Kristof
  • Meurs, Greet
  • Verstraeten, Maxim

Abstract

The present invention relates to a pharmaceutical composition comprising the calcium; {4-[(5,6-diphenylpyrazin-2-yl) (propan-2-yl)amino]butoxy}acetate, in particular to long-acting injectables comprising the same, the use of the pharmaceutical composition for the treatment or prevention of specific diseases, and a process to produce it.

IPC Classes  ?

  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • 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

16.

INJECTABLE PHARMACEUTICAL COMPOSITION COMPRISING A DIPHENYLPYRAZINE DERIVATIVE

      
Application Number EP2023070064
Publication Number 2024/017964
Status In Force
Filing Date 2023-07-19
Publication Date 2024-01-25
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Amssoms, Katie
  • De Proost, Eddy
  • Dong, Wenyu
  • Hartman Kok, Paul
  • Holm, Rene
  • Kimpe, Kristof
  • Meurs, Greet
  • Verduyckt, Tom
  • Verstraeten, Maxim

Abstract

The present invention relates to a pharmaceutical composition comprising the calcium;{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate, in particular to long-acting injectables comprising the same, the use of the pharmaceutical composition for the treatment or prevention of specific diseases, and a process to produce it.

IPC Classes  ?

  • A61K 31/00 - Medicinal preparations containing organic active ingredients
  • A61K 9/10 - DispersionsEmulsions
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
  • 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

17.

TRIAZOLOPYRIDINE AND BENZOISOXAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS

      
Application Number EP2023066725
Publication Number 2023/247590
Status In Force
Filing Date 2023-06-21
Publication Date 2023-12-28
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Lu, Tianbao
  • Cavitt, Marchello
  • Liu, Zhijie
  • Berry, Angela
  • Reiher, Christopher
  • Wolkenberg, Scott
  • Xu, Guozhang
  • Mulhearn, James

Abstract

The disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 9/12 - Antihypertensives
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/423 - Oxazoles condensed with carbocyclic rings
  • A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
  • 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
  • A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
  • A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
  • C07D 491/08 - Bridged systems
  • C07D 491/10 - Spiro-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 498/04 - Ortho-condensed systems

18.

PYRROLOPYRIDINE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS

      
Application Number EP2023066729
Publication Number 2023/247593
Status In Force
Filing Date 2023-06-21
Publication Date 2023-12-28
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Lu, Tianbao
  • Nguyen, Van
  • Cavitt, Marchello
  • Liu, Zhijie
  • Berry, Angela
  • Zhu, Bin

Abstract

The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 9/12 - Antihypertensives
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 491/08 - Bridged systems
  • C07D 491/10 - Spiro-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
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
  • A61K 31/536 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • 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

19.

PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS

      
Application Number EP2023066734
Publication Number 2023/247596
Status In Force
Filing Date 2023-06-21
Publication Date 2023-12-28
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Lu, Tianbao
  • Nguyen, Van
  • Cavitt, Marchello
  • Zhu, Bin
  • Hawkins, Michael J.
  • Liu, Zhijie
  • Zhang, Wei

Abstract

The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61P 9/12 - Antihypertensives
  • C07D 513/04 - Ortho-condensed systems

20.

PYRAZOLOPYRAZINE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS

      
Application Number EP2023066732
Publication Number 2023/247595
Status In Force
Filing Date 2023-06-21
Publication Date 2023-12-28
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Lu, Tianbao
  • Zhu, Bin
  • Hawkins, Michael J.
  • Liu, Zhijie
  • Xu, Guozhang
  • Guerrero, Carlos A.

Abstract

The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 9/12 - Antihypertensives
  • C07D 487/04 - Ortho-condensed systems
  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

21.

YUVANCI

      
Application Number 018967151
Status Registered
Filing Date 2023-12-21
Registration Date 2024-04-25
Owner Actelion Pharmaceuticals Ltd. (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations, excluding pharmaceutical preparations in relation to blood circulation troubles.

22.

DIPHENYLPYRAZINE COMPOUNDS AS PRODRUGS

      
Application Number EP2023062025
Publication Number 2023/214059
Status In Force
Filing Date 2023-05-05
Publication Date 2023-11-09
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Lu, Tianbao
  • Schips, Tobias
  • Amssoms, Katie
  • Bode, Wilhelmina

Abstract

The present invention relates to a pharmaceutical composition comprising a compound of Formula (I): or a pharmaceutically acceptable salt or solvate thereof; in particular to long-acting injectables comprising the same, the use of the pharmaceutical composition for the treatment or prevention of specific diseases, and a process to produce it.

IPC Classes  ?

  • A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61P 11/00 - Drugs for disorders of the respiratory system

23.

METHODS OF SLOWING AN INCREASE IN BRAIN VENTRICULAR VOLUME

      
Application Number EP2023053304
Publication Number 2023/152290
Status In Force
Filing Date 2023-02-10
Publication Date 2023-08-17
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Ait-Tihyaty, Maria
  • Saad, Ziad Serhal
  • Datta, Ritobrato
  • Dibernardo, Allitia
  • Kolb, Hartmuth
  • Wiegand, Frank

Abstract

The disclosure relates to methods of slowing an increase in brain ventricular volume. In certain aspects, methods of slowing an increase in brain ventricular volume in a patient with multiple sclerosis are disclosed.

IPC Classes  ?

24.

METHODS OF SLOWING AN INCREASE IN BRAIN VENTRICULAR VOLUME

      
Document Number 03220702
Status Pending
Filing Date 2023-02-10
Open to Public Date 2023-08-17
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Ait-Tihyaty, Maria
  • Saad, Ziad Serhal
  • Datta, Ritobrato
  • Dibernardo, Allitia
  • Kolb, Hartmuth
  • Wiegand, Frank

Abstract

The disclosure relates to methods of slowing an increase in brain ventricular volume. In certain aspects, methods of slowing an increase in brain ventricular volume in a patient with multiple sclerosis are disclosed.

IPC Classes  ?

25.

CONTROLLED RELEASE COMPOSITIONS

      
Application Number EP2023050071
Publication Number 2023/131608
Status In Force
Filing Date 2023-01-03
Publication Date 2023-07-13
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Dong, Wenyu
  • Garin, Matthieu
  • Holm, Rene
  • Koerber, Martin

Abstract

The present disclosure related to a pharmaceutical formulation comprising particles comprising 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid (selexipag metabolite), or a pharmaceutically acceptable salt, hydrate, solvate, or combinations thereof (active pharmaceutical ingredient), and poly(lactic-co-glycolic acid) (PLGA); as well as a process for preparing the pharmaceutical formation and uses thereof.

IPC Classes  ?

26.

METHODS FOR TREATING MULTIPLE SCLEROSIS

      
Document Number 03220549
Status Pending
Filing Date 2022-11-04
Open to Public Date 2023-05-11
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Dibernardo, Allitia
  • Ait-Tihyaty, Maria
  • Wiegand, Frank
  • Lair, Lindsey
  • Saad, Ziad Serhal
  • Datta, Ritobrato
  • Kolb, Hartmuth

Abstract

The disclosure relates to methods of preserving myelination of axons in a human subject having a demyelinating disease by administration of an effective amount of a monoselective S1P receptor modulator, such as ponesimod.

IPC Classes  ?

  • A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
  • A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
  • 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 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/4245 - Oxadiazoles
  • A61K 31/426 - 1,3-Thiazoles
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

27.

METHODS FOR TREATING MULTIPLE SCLEROSIS

      
Application Number EP2022080823
Publication Number 2023/079079
Status In Force
Filing Date 2022-11-04
Publication Date 2023-05-11
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Dibernardo, Allitia
  • Ait-Tihyaty, Maria
  • Wiegand, Frank
  • Lair, Lindsey
  • Saad, Ziad Serhal
  • Datta, Ritobrato
  • Kolb, Hartmuth

Abstract

The disclosure relates to methods of preserving myelination of axons in a human subject having a demyelinating disease by administration of an effective amount of a monoselective S1P receptor modulator, such as ponesimod.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
  • A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
  • 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 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/4245 - Oxadiazoles

28.

METHODS OF TREATING MULTIPLE SCLEROSIS

      
Document Number 03220723
Status Pending
Filing Date 2022-10-10
Open to Public Date 2023-04-20
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Dibernardo, Allitia
  • Ait-Tihyaty, Maria

Abstract

The disclosure relates to methods of treating multiple sclerosis. In certain aspects, methods of treating early-stage multiple sclerosis in a patient are disclosed.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

29.

METHODS OF TREATING MULTIPLE SCLEROSIS

      
Application Number IB2022059704
Publication Number 2023/062511
Status In Force
Filing Date 2022-10-10
Publication Date 2023-04-20
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor Dibernardo, Allitia

Abstract

The disclosure relates to methods of treating multiple sclerosis. Also provided are pharmaceutical products containing ponesimod, instructions for use of ponesimod, and methods for reducing clinical management events before or during treatment of multiple sclerosis.

IPC Classes  ?

  • A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
  • A61K 31/426 - 1,3-Thiazoles
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • A61K 9/00 - Medicinal preparations characterised by special physical form

30.

METHODS OF TREATING MULTIPLE SCLEROSIS

      
Application Number EP2022078064
Publication Number 2023/061918
Status In Force
Filing Date 2022-10-10
Publication Date 2023-04-20
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Spiller, Krista
  • Bhattacharya, Anindya
  • Sidorenko, Tatiana
  • Wong, Janice

Abstract

The disclosure relates to methods of treating multiple sclerosis and maintaining or maximizing vaccine effectiveness. In certain aspects, the methods comprise administrating ponesimod, administering a vaccine, and interrupting the administration of the ponesimod.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/00 - Drugs for disorders of the nervous system

31.

METHODS OF TREATING MULTIPLE SCLEROSIS

      
Application Number EP2022078091
Publication Number 2023/061935
Status In Force
Filing Date 2022-10-10
Publication Date 2023-04-20
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor Ait-Tihyaty, Maria

Abstract

The disclosure relates to methods of treating multiple sclerosis. In certain aspects, methods of reducing corticosteroid use in a patient with multiple sclerosis are disclosed.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

32.

METHODS AND COMPOSITIONS FOR PREDICTIVE OUTCOMES FOR PULMONARY ARTERIAL HYPERTENSION TREATMENT

      
Application Number EP2022078317
Publication Number 2023/062046
Status In Force
Filing Date 2022-10-11
Publication Date 2023-04-20
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Jatkoe, Timothy Allen
  • Fong, Yiu-Lian
  • Cheng, He
  • Koon, Yen Ling
  • Yu, Jin
  • Cheruba, Elsie

Abstract

Biomarkers that can be used for the prognosis and disease progression of disease states, preferably pulmonary arterial hypertension (PAH), to the identification of a treatment regimen for PAH, and/or to indicate the responsiveness to the treatment regimen for PAH in a subject are described. Also described are probes capable of detecting the biomarkers and related methods and kits for determining PAH and/or identification of treatment regimens for PAH.

IPC Classes  ?

  • C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material

33.

METHODS OF TREATING MULTIPLE SCLEROSIS

      
Document Number 03220684
Status Pending
Filing Date 2022-10-10
Open to Public Date 2023-04-20
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor Ait-Tihyaty, Maria

Abstract

The disclosure relates to methods of treating multiple sclerosis. In certain aspects, methods of reducing corticosteroid use in a patient with multiple sclerosis are disclosed.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/426 - 1,3-Thiazoles
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

34.

METHODS OF TREATING MULTIPLE SCLEROSIS

      
Document Number 03220715
Status Pending
Filing Date 2022-10-10
Open to Public Date 2023-04-20
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Spiller, Krista
  • Bhattacharya, Anindya
  • Sidorenko, Tatiana
  • Wong, Janice

Abstract

The disclosure relates to methods of treating multiple sclerosis and maintaining or maximizing vaccine effectiveness. In certain aspects, the methods comprise administrating ponesimod, administering a vaccine, and interrupting the administration of the ponesimod.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system

35.

METHODS OF TREATING MULTIPLE SCLEROSIS

      
Document Number 03221343
Status Pending
Filing Date 2022-10-10
Open to Public Date 2023-04-20
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Dibernardo, Allitia
  • Hennessy, Brian Patrick
  • Kracker, Hilke
  • Vaclavkova, Andrea
  • Burcklen, Michel
  • Sidorenko, Tatiana
  • Ouwekerk-Mahadevan, Sivi

Abstract

The disclosure relates to methods of treating multiple sclerosis. Also provided are pharmaceutical products containing ponesimod, instructions for use of ponesimod, and methods for reducing clinical management events before or during treatment of multiple sclerosis.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
  • A61K 31/426 - 1,3-Thiazoles
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

36.

METHODS OF TREATING MULTIPLE SCLEROSIS

      
Application Number EP2022078098
Publication Number 2023/061939
Status In Force
Filing Date 2022-10-10
Publication Date 2023-04-20
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Dibernardo, Allitia
  • Ait-Tihyaty, Maria

Abstract

The disclosure relates to methods of treating multiple sclerosis. In certain aspects, methods of treating early-stage multiple sclerosis in a patient are disclosed.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

37.

CONTROLLED RELEASE SELEXIPAG COMPOSITION

      
Application Number 17759455
Status Pending
Filing Date 2021-01-29
First Publication Date 2023-04-13
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Luyten, Katrien
  • Van Droogenbroeck, Annelien

Abstract

The present invention is concerned with controlled release compositions for oral administration comprising 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N- isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (selexipag, NS-304, ACT- 293987) and its pharmaceutically acceptable salts and/or 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid (metabolite of selexipag, MRE-269, ACT- 333679) and its pharmaceutically acceptable salts; and with processes for preparing such controlled release compositions as well as to uses thereof.

IPC Classes  ?

38.

METHODS OF TREATING AND ASSESSING PULMONARY ARTERIAL HYPERTENSION WITH SELEXIPAG

      
Application Number 17759467
Status Pending
Filing Date 2021-02-02
First Publication Date 2023-03-09
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Cottreel, Emmanuelle
  • Perchenet, Loïc

Abstract

The present disclosure provides methods for treating pulmonary arterial hypertension in a patient in need thereof, comprising (a) performing magnetic resonance imaging (MRI) on the right ventricle of the patient to provide a MRI baseline image; (b) administering a therapeutically effective amount of selexipag; (c) performing MRI on the right ventricle of the patient to provide a MRI test image; and (d) comparing the MRI baseline image with the MRI test image.

IPC Classes  ?

39.

BMP9 VARIANT POLYPEPTIDES AND USES THEREOF

      
Application Number EP2022072038
Publication Number 2023/012318
Status In Force
Filing Date 2022-08-04
Publication Date 2023-02-09
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Luo, Jinquan
  • Kavalkovich, Karl Walter
  • Schips, Tobias Gebhard
  • Winkis, Annmarie
  • Häsler, Julien
  • Jeyaseelan, Jey Raju

Abstract

Isolated BMP9 and pro-BMP9 mutant polypeptides are described. Also described are nucleic acids encoding the isolated BMP9 and pro-BMP9 mutant polypeptides, compositions comprising the isolated BMP9 and pro-BMP9 mutant polypeptides, and methods of producing the BMP9 and pro-BMP9 mutant polypeptides and using the BMP9 and pro-BMP9 mutant polypeptides for treating or preventing vascular diseases and/or respiratory diseases, such as pulmonary arterial hypertension (PAH).

IPC Classes  ?

  • C07K 14/51 - Bone morphogenic factorOsteogeninOsteogenic factorBone-inducing factor

40.

PYRAZOLOPYRIMIDINES AND THEIR USES AS PDGFR INHIBITORS

      
Document Number 03227477
Status Pending
Filing Date 2022-07-29
Open to Public Date 2023-02-02
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Bauman, David
  • Liu, Zhijie
  • Lu, Tianbao

Abstract

The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
  • A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
  • A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
  • A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

41.

METHODS OF TREATING PULMONARY ARTERIAL HYPERTENSION

      
Application Number 17780064
Status Pending
Filing Date 2020-11-27
First Publication Date 2023-02-02
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Maresta, Alessandro
  • Perchenet, Loïc

Abstract

The disclosure relates to methods of reducing the risk of disease progression in a patient with pulmonary arterial hypertension (PAH), comprising administering to a patient in need thereof, an initial triple combination therapy of an endothelin receptor antagonist (ERA), a phosphodiesterase type 5 (PDE-5) inhibitor, and a prostacyclin receptor agonist (IP receptor agonist).

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/4965 - Non-condensed pyrazines
  • A61P 9/12 - Antihypertensives
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61K 9/00 - Medicinal preparations characterised by special physical form

42.

PYRAZOLOPYRIMIDINES AND THEIR USES AS PDGFR INHIBITORS

      
Application Number EP2022071464
Publication Number 2023/007009
Status In Force
Filing Date 2022-07-29
Publication Date 2023-02-02
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Bauman, David
  • Liu, Zhijie
  • Lu, Tianbao

Abstract

The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 487/04 - Ortho-condensed systems
  • A61P 35/00 - Antineoplastic agents

43.

PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF PULMONARY VASCULAR DISEASE AND/OR CARDIAC DYSFUNCTION IN FONTAN-PALLIATED PATIENTS

      
Application Number 17779787
Status Pending
Filing Date 2020-11-25
First Publication Date 2023-01-05
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Csonka, Dénes
  • Fares, Wassim
  • Hoogkamer, Hans
  • Torfs, Koen

Abstract

The present invention relates to high doses of macitentan (INN), i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof for use in the treatment of pulmonary vascular disease and/or cardiac dysfunction in functional single ventricular heart disease patients, especially in Fontan-palliated patients. Moreover, the present invention relates to the use of high doses of macitentan for the manufacture of a medicament as well as to a method for the treatment of said diseases. Further, the present invention relates to a dosage regimen as well as to a combination of macitentan with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Besides, the present invention relates to a pharmaceutical composition for the treatment of pulmonary vascular disease and/or cardiac dysfunction in functional single ventricular heart disease patients, especially in Fontan-palliated patients comprising a high dose of macitentan. Moreover, the present invention relates to the use of high doses aprocitentan for the same purpose.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
  • A61K 9/20 - Pills, lozenges or tablets
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine

44.

PHARMACEUTICAL COMPOSITION COMPRISING SELEXIPAG

      
Application Number 17770155
Status Pending
Filing Date 2020-10-22
First Publication Date 2022-12-22
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Schrader, Iii, Marc Patrik
  • Schlicker-Spain, Alexandra

Abstract

The present invention relates to pharmaceutical compositions comprising 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (selexipag, NS-304, ACT-293987) which are suitable for oral administration (p.o.).

IPC Classes  ?

45.

DISPERSIBLE TABLET FOR ORAL ADMINISTRATION

      
Application Number EP2022065797
Publication Number 2022/258796
Status In Force
Filing Date 2022-06-10
Publication Date 2022-12-15
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Van Hove, Ben
  • Boiy, Annelies

Abstract

The present invention is directed to pharmaceutical compositions or dispersible tablets for oral administration comprising N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (macitentan), the use of said pharmaceutical compositions or dispersible tablets for the treatment of pulmonary hypertension and the process for preparing such dispersible tablets.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 9/12 - Antihypertensives

46.

METHODS OF TREATING PULMONARY HYPERTENSION

      
Application Number EP2022062583
Publication Number 2022/238375
Status In Force
Filing Date 2022-05-10
Publication Date 2022-11-17
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Zhao, Carol
  • Narayan, Veena
  • Sahay, Sandeep
  • El-Kersh, Karim

Abstract

This invention relates to methods of treating pulmonary hypertension, comprising administering to a patient in need thereof a therapeutically effective amount of selexipag, wherein the selexipag is administered at a starting dose and is increased to determine a first individual maximum tolerated dose (iMTD), and the patient undergoes a further titration of selexipag to a second iMTD.

IPC Classes  ?

47.

METHODS FOR TREATING SARCOIDOSIS-ASSOCIATED PULMONARY HYPERTENSION

      
Application Number 17608820
Status Pending
Filing Date 2020-05-06
First Publication Date 2022-10-20
Owner ACTELION PHARMACEUTICALS LTD (China)
Inventor
  • Preiss, Ralph T.
  • Remenova, Tatiana
  • Konourina, Irina
  • Pfister, Thomas
  • Roscher, René
  • Frey, Aline
  • Yannoulis Arceda, Natalia Catalina
  • Zimmermann, Rainer
  • Morrison, Keith John
  • Bruderer, Shirin

Abstract

The present disclosure provides methods for treating sarcoidosis-associated pulmonary hypertension, comprising administering to a patient in need thereof, a therapeutically effective amount of selexipag, wherein the patient is diagnosed with sarcoidosis-associated pulmonary hypertension.

IPC Classes  ?

48.

Pharmaceutical composition comprising macitentan for the treatment of chronic thromboembolic pulmonary hypertension

      
Application Number 17736434
Grant Number 11612600
Status In Force
Filing Date 2022-05-04
First Publication Date 2022-10-20
Grant Date 2023-03-28
Owner Actelion Pharmaceuticals Ltd (Switzerland)
Inventor
  • Csonka, Dénes
  • Fares, Wassim
  • Hoogkamer, Hans
  • Torfs, Koen

Abstract

The present invention relates to high doses of macitentan (INN), i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof, or of aprocitentan, for use in the treatment and/or prevention of chronic thromboembolic pulmonary hypertension (CTEPH). Moreover, the present invention relates to the use of high doses of macitentan or of aprocitentan for the manufacture of a medicament for the treatment and/or prevention of CTEPH, as well as to a method for the treatment and/or prevention of CTEPH comprising administering high doses of macitentan or of aprocitentan to a patient. Further, the present invention relates to a dosage regimen for the treatment and/or prevention of CTEPH as well as to a combination of macitentan, or of aprocitentan, with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Moreover, the present invention relates to a pharmaceutical composition for the treatment of CTEPH comprising a high dose of macitentan or of aprocitentan.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 9/12 - Antihypertensives

49.

METHODS FOR TREATING PULMONARY ARTERIAL HYPERTENSION

      
Application Number 17616313
Status Pending
Filing Date 2020-06-10
First Publication Date 2022-10-13
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Preiss, Ralph T.
  • Bruderer, Shirin
  • Clozel, Martine
  • Yannoulis Arceda, Natalia Catalina

Abstract

The present disclosure provides methods of avoiding treatment interruption in a patient receiving an oral dose of selexipag for treating pulmonary arterial hypertension, wherein the patient is temporarily unable to take oral medication. These methods comprise administering to the patient an intravenous (IV) dose of selexipag, and, subsequently, returning to an oral dose of selexipag.

IPC Classes  ?

50.

PHARMACEUTICAL DOSAGE SYSTEM

      
Document Number 03213818
Status Pending
Filing Date 2022-03-16
Open to Public Date 2022-09-22
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Mayne, Andrew
  • Lutz, Petra
  • Sarkar, Paromita
  • Gouvea, Galina

Abstract

A pharmaceutical dosage system includes a blister pack and a plurality of dosage forms contained by the blister pack. The dosage forms are to be consumed in an up-titration process. Only one single dosage form of the plurality of dosage forms is consumed on a given day throughout the up-titration process whereby dosages increase over the course of a multi-day period of time.

IPC Classes  ?

  • A61J 1/03 - Containers specially adapted for medical or pharmaceutical purposes for pills or tablets
  • A61J 1/16 - Holders for containers
  • A61J 7/04 - Arrangements for time indication or reminder for taking medicine, e.g. programmed dispensers

51.

PHARMACEUTICAL DOSAGE SYSTEM

      
Application Number EP2022056841
Publication Number 2022/194941
Status In Force
Filing Date 2022-03-16
Publication Date 2022-09-22
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Mayne, Andrew
  • Lutz, Petra
  • Sarkar, Paromita
  • Gouvea, Galina

Abstract

A pharmaceutical dosage system includes a blister pack and a plurality of dosage forms contained by the blister pack. The dosage forms are to be consumed in an up-titration process. Only one single dosage form of the plurality of dosage forms is consumed on a given day throughout the up-titration process whereby dosages increase over the course of a multi-day period of time.

IPC Classes  ?

  • A61J 1/03 - Containers specially adapted for medical or pharmaceutical purposes for pills or tablets
  • A61J 7/04 - Arrangements for time indication or reminder for taking medicine, e.g. programmed dispensers
  • A61J 1/16 - Holders for containers

52.

METHODS FOR TREATING PULMONARY HYPERTENSION IN PATIENTS WITH LEFT VENTRICULAR ASSIST DEVICE IMPLANTATION

      
Document Number 03208560
Status Pending
Filing Date 2022-02-25
Open to Public Date 2022-09-01
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Rocco, Mark
  • Selej, Mona
  • Zhao, Carol

Abstract

The present disclosure provides methods for treating pulmonary hypertension in a patient with left ventricular assist device (LVAD) implantation and methods of improving cardiac transplant eligibility in a patient with LVAD implantation. The methods include administering to a patient in need thereof a therapeutically effective amount of macitentan or aprocitentan.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61N 1/362 - Heart stimulators
  • A61P 9/12 - Antihypertensives
  • A61P 11/00 - Drugs for disorders of the respiratory system

53.

METHODS FOR TREATING PULMONARY HYPERTENSION IN PATIENTS WITH LEFT VENTRICULAR ASSIST DEVICE IMPLANTATION

      
Application Number EP2022054742
Publication Number 2022/180194
Status In Force
Filing Date 2022-02-25
Publication Date 2022-09-01
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Rocco, Mark
  • Selej, Mona
  • Zhao, Carol

Abstract

The present disclosure provides methods for treating pulmonary hypertension in a patient with left ventricular assist device (LVAD) implantation and methods of improving cardiac transplant eligibility in a patient with LVAD implantation. The methods include administering to a patient in need thereof a therapeutically effective amount of macitentan or aprocitentan.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61P 9/12 - Antihypertensives
  • A61N 1/362 - Heart stimulators

54.

MACITENTAN FOR USE IN TREATING PORTOPULMONARY HYPERTENSION

      
Application Number 17601123
Status Pending
Filing Date 2020-04-03
First Publication Date 2022-08-18
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Perchenet, Loïc
  • Cottreel, Emmanuelle

Abstract

The present invention provides methods for treating portopulmonary hypertension, comprising administering to a patient in need thereof, a therapeutically effective amount of macitentan. Preferably, the methods are clinically proven safe and/or effective. Also provided are methods of improving liver transplant perioperative mortality risk category, improving MELD exception eligibility, and reducing the risk of removal from a liver transplant waitlist in a patient with portopulmonary hypertension and liver disease, comprising administering to a patient in need thereof a therapeutically effective amount of macitentan.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 9/12 - Antihypertensives
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

55.

TRANSITIONING PATIENTS TREATED FOR PULMONARY ARTERIAL HYPERTENSION TO SELEXIPAG

      
Application Number 17612014
Status Pending
Filing Date 2020-05-20
First Publication Date 2022-08-18
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Zhao, Carol
  • Colvin Riesen, Johanna
  • Palmer, Gary Arnold
  • Keating, Michael
  • Hartline, Brian
  • Benton, Wade
  • Dumitrescu, Camelia
  • Shah, Mehul Bipinchandra

Abstract

The present disclosure provides methods of transitioning a patient being treated for pulmonary arterial hypertension with a non-selexipag prostacyclin pathway agent (PPA) to selexipag.

IPC Classes  ?

  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 9/12 - Antihypertensives

56.

PROCESS FOR MANUFACTURING A DIPHENYLPYRAZINE DERIVATIVE

      
Document Number 03206362
Status Pending
Filing Date 2022-01-28
Open to Public Date 2022-08-04
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Vanierschot, Ronny
  • Collas, Alain
  • Leys, Carina
  • Van Mechelen, Kore

Abstract

The present invention relates to a process for the manufacturing of calcium;{4-[(5, 6- diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate, or a pharmaceutically acceptable hydrate or solvate thereof. Moreover, it relates to calcium;{4-[(5,6-diphenylpyrazin-2- yl)(propan-2-yl)amino]butoxy}acetate with high purity, as well as to crystalline forms of calcium;{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate and hydrates and solvates thereof. Furthermore, the invention relates to the use of calcium;{4-[(5, 6- diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate for the treatment or prevention of e.g. pulmonary arterial hypertension (PAH) or chronic thromboembolic pulmonary hypertension (CTEPH).

IPC Classes  ?

  • A61K 9/08 - Solutions
  • A61K 31/4965 - Non-condensed pyrazines
  • A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
  • A61P 11/08 - Bronchodilators
  • A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
  • A61P 19/04 - Drugs for skeletal disorders for non-specific disorders of the connective tissue
  • C07D 241/20 - Nitrogen atoms

57.

PROCESS FOR MANUFACTURING A DIPHENYLPYRAZINE DERIVATIVE

      
Application Number EP2022052084
Publication Number 2022/162163
Status In Force
Filing Date 2022-01-28
Publication Date 2022-08-04
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Vanierschot, Ronny
  • Collas, Alain
  • Leys, Carina
  • Van Mechelen, Kore

Abstract

The present invention relates to a process for the manufacturing of calcium;{4-[(5, 6- diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate, or a pharmaceutically acceptable hydrate or solvate thereof. Moreover, it relates to calcium;{4-[(5,6-diphenylpyrazin-2- yl)(propan-2-yl)amino]butoxy}acetate with high purity, as well as to crystalline forms of calcium;{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate and hydrates and solvates thereof. Furthermore, the invention relates to the use of calcium;{4-[(5, 6- diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate for the treatment or prevention of e.g. pulmonary arterial hypertension (PAH) or chronic thromboembolic pulmonary hypertension (CTEPH).

IPC Classes  ?

58.

PHARMACEUTICAL COMPOSITION COMPRISING A DIPHENYLPYRAZINE DERIVATIVE

      
Document Number 03206133
Status Pending
Filing Date 2022-01-28
Open to Public Date 2022-08-04
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Amssoms, Katie
  • De Proost, Eddy
  • Dong, Wenyu
  • Hartman Kok, Paul
  • Holm, Rene
  • Kimpe, Kristof
  • Meurs, Greet
  • Verstraeten, Maxim

Abstract

The present invention relates to a pharmaceutical composition comprising the calcium;{4- [(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate, in particular to long-acting injectables comprising the same, the use of the pharmaceutical composition for the treatment or prevention of specific diseases, and a process to produce it.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/10 - DispersionsEmulsions
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system

59.

PHARMACEUTICAL COMPOSITION COMPRISING A DIPHENYLPYRAZINE DERIVATIVE

      
Application Number EP2022052073
Publication Number 2022/162158
Status In Force
Filing Date 2022-01-28
Publication Date 2022-08-04
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Amssoms, Katie
  • De Proost, Eddy
  • Dong, Wenyu
  • Hartman Kok, Paul
  • Holm, Rene
  • Kimpe, Kristof
  • Meurs, Greet
  • Verstraeten, Maxim

Abstract

The present invention relates to a pharmaceutical composition comprising the calcium;{4- [(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}acetate, in particular to long-acting injectables comprising the same, the use of the pharmaceutical composition for the treatment or prevention of specific diseases, and a process to produce it.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/10 - DispersionsEmulsions
  • A61K 9/19 - Particulate form, e.g. powders lyophilised
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system

60.

PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS

      
Document Number 03202944
Status Pending
Filing Date 2021-12-22
Open to Public Date 2022-06-30
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Bauman, David
  • Liu, Zhijie
  • Lu, Tianbao
  • Zhu, Bin
  • Nguyen, Van
  • Cavitt, Marchello
  • Hawkins, Michael J.

Abstract

The disclosure is directed to compounds of formula (I),and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

61.

PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS

      
Application Number EP2021087215
Publication Number 2022/136509
Status In Force
Filing Date 2021-12-22
Publication Date 2022-06-30
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Bauman, David
  • Liu, Zhijie
  • Lu, Tianbao
  • Zhu, Bin
  • Nguyen, Van
  • Cavitt, Marchello
  • Hawkins, Michael J.

Abstract

The disclosure is directed to compounds of formula (I),and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/542 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
  • A61P 35/00 - Antineoplastic agents

62.

SELEXIPAG FOR USE VIA INTRACOLONIC ADMINISTRATION

      
Application Number EP2021082307
Publication Number 2022/106621
Status In Force
Filing Date 2021-11-19
Publication Date 2022-05-27
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Söderlind, Sven Erik
  • Vaes, Elise
  • Van Droogenbroeck, Annelien

Abstract

The present disclosure provides methods for treating pulmonary hypertension, including pulmonary arterial hypertension. The methods comprise administering a therapeutically effective amount of selexipag to a patient in need thereof, wherein at least one dose of selexipag is in an intracolonic form. Also provided are pharmaceutical drug products comprising a therapeutically effective amount of selexipag in an intracolonic form; and instructions for using selexipag via intracolonic administration for the treatment of pulmonary hypertension, including pulmonary arterial hypertension.

IPC Classes  ?

  • A61K 31/4965 - Non-condensed pyrazines
  • A61P 9/12 - Antihypertensives
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61K 9/00 - Medicinal preparations characterised by special physical form

63.

OMLUENNE

      
Application Number 218265200
Status Pending
Filing Date 2022-04-29
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases

64.

BEZYNVI

      
Application Number 218265300
Status Pending
Filing Date 2022-04-29
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases

65.

OPAIRVI

      
Application Number 218265500
Status Pending
Filing Date 2022-04-29
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases

66.

OPZIPULM

      
Application Number 218265400
Status Pending
Filing Date 2022-04-29
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases

67.

PAHDUA

      
Application Number 218265600
Status Pending
Filing Date 2022-04-29
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases

68.

IPSYNVO

      
Application Number 218265700
Status Pending
Filing Date 2022-04-29
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases

69.

EPZYNVO

      
Application Number 218265100
Status Pending
Filing Date 2022-04-29
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

(1) Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases

70.

OPAIRVI

      
Application Number 018690499
Status Registered
Filing Date 2022-04-22
Registration Date 2022-08-13
Owner Actelion Pharmaceuticals Ltd. (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases.

71.

OPZIPULM

      
Application Number 018690500
Status Registered
Filing Date 2022-04-22
Registration Date 2022-08-13
Owner Actelion Pharmaceuticals Ltd. (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases.

72.

EPZYNVO

      
Application Number 018690507
Status Registered
Filing Date 2022-04-22
Registration Date 2022-08-13
Owner Actelion Pharmaceuticals Ltd. (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases.

73.

OMLUENNE

      
Application Number 018690504
Status Registered
Filing Date 2022-04-22
Registration Date 2022-08-13
Owner Actelion Pharmaceuticals Ltd. (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases.

74.

IPSYNVO

      
Application Number 018690506
Status Registered
Filing Date 2022-04-22
Registration Date 2022-08-13
Owner Actelion Pharmaceuticals Ltd. (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases.

75.

BEZYNVI

      
Application Number 018690508
Status Registered
Filing Date 2022-04-22
Registration Date 2022-08-13
Owner Actelion Pharmaceuticals Ltd. (Switzerland)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations; pharmaceuticals preparations for the treatment of cardiovascular and pulmonary diseases.

76.

PHARMACEUTICAL COMPOSITION COMPRISING MACITENTAN FOR THE TREATMENT OF CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION

      
Application Number 17425576
Status Pending
Filing Date 2020-01-24
First Publication Date 2022-03-31
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Csonka, Dénes
  • Fares, Wassim
  • Hoogkamer, Hans
  • Torfs, Koen

Abstract

The present invention relates to high doses of macitentan (INN), i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof, or of aprocitentan, for use in the treatment and/or prevention of chronic thromboembolic pulmonary hypertension (CTEPH). Moreover, the present invention relates to the use of high doses of macitentan or of aprocitentan for the manufacture of a medicament for the treatment and/or prevention of CTEPH, as well as to a method for the treatment and/or prevention of CTEPH comprising administering high doses of macitentan or of aprocitentan to a patient. Further, the present invention relates to a dosage regimen for the treatment and/or prevention of CTEPH as well as to a combination of macitentan, or of aprocitentan, with one or more phosphodiesterase type 5 (PDES) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Moreover, the present invention relates to a pharmaceutical composition for the treatment of CTEPH comprising a high dose of macitentan or of aprocitentan.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 9/12 - Antihypertensives
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

77.

Pharmaceutical composition for the treatment of pulmonary arterial hypertension

      
Application Number 17515132
Grant Number 11464777
Status In Force
Filing Date 2021-10-29
First Publication Date 2022-03-31
Grant Date 2022-10-11
Owner Actelion Pharmaceuticals Ltd (Switzerland)
Inventor
  • Csonka, Dénes
  • Fares, Wassim
  • Hoogkamer, Hans
  • Torfs, Koen

Abstract

The present invention relates to high doses of macitentan, i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof, or of aprocitentan, for use in the treatment and/or prevention of pulmonary arterial hypertension (PAH). Moreover, the present invention relates to the use of high doses of macitentan, or of aprocitentan, for the manufacture of a medicament for the treatment and/or prevention of PAH, as well as to a method for the treatment and/or prevention of PAH comprising high doses of macitentan or of aprocitentan. Further, the present invention relates to a dosage regimen for the treatment and/or prevention of PAH as well as to a combination of macitentan, or of aprocitentan, with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Therein, PAH is preferably mild or moderate PAH. Moreover, the present invention relates to a pharmaceutical composition for the treatment of PAH comprising a high dose of macitentan or of aprocitentan.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 9/12 - Antihypertensives
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems

78.

PHRONTLINE

      
Serial Number 97312218
Status Pending
Filing Date 2022-03-15
Owner Actelion Pharmaceuticals LTD (Switzerland)
NICE Classes  ?
  • 41 - Education, entertainment, sporting and cultural services
  • 44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services

Goods & Services

Educational services, namely, providing podcasts in the field of pulmonary hypertension Providing information in the field of the diagnosis and treatment of pulmonary hypertension via a website

79.

Miscellaneous Design

      
Serial Number 97283994
Status Pending
Filing Date 2022-02-25
Owner Actelion Pharmaceutical LTD (Switzerland)
NICE Classes  ?
  • 05 - Pharmaceutical, veterinary and sanitary products
  • 44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services

Goods & Services

Human pharmaceuticals for treatment of pulmonary arterial hypertension Providing information in the field of pulmonary arterial hypertension

80.

METHODS OF SLOWING BRAIN VOLUME LOSS

      
Document Number 03170688
Status Pending
Filing Date 2021-03-05
Open to Public Date 2021-09-10
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Burcklen, Michel
  • Hennessy, Brian
  • Kracker, Hilke
  • Linscheid, Philippe
  • Sidorenko, Tatiana

Abstract

The disclosure relates to methods of slowing brain volume loss. In certain aspects, methods of slowing brain volume loss in a patient with multiple sclerosis are disclosed.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • 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

81.

METHODS OF SLOWING BRAIN VOLUME LOSS

      
Application Number EP2021055622
Publication Number 2021/176070
Status In Force
Filing Date 2021-03-05
Publication Date 2021-09-10
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Burcklen, Michel
  • Hennessy, Brian
  • Kracker, Hilke
  • Linscheid, Philippe
  • Scherz, Tatiana

Abstract

The disclosure relates to methods of slowing brain volume loss. In certain aspects, methods of slowing brain volume loss in a patient with multiple sclerosis are disclosed.

IPC Classes  ?

  • A61K 31/426 - 1,3-Thiazoles
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • 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

82.

METHODS OF TREATING AND ASSESSING PULMONARY ARTERIAL HYPERTENSION WITH SELEXIPAG

      
Application Number EP2021052374
Publication Number 2021/156227
Status In Force
Filing Date 2021-02-02
Publication Date 2021-08-12
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Cottreel, Emmanuelle
  • Perchenet, Loïc

Abstract

The present disclosure provides methods for treating pulmonary arterial hypertension in a patient in need thereof, comprising (a) performing magnetic resonance imaging (MRI) on the right ventricle of the patient to provide a MRI baseline image; (b) administering a therapeutically effective amount of selexipag; (c) performing MRI on the right ventricle of the patient to provide a MRI test image; and (d) comparing the MRI baseline image with the MRI test image.

IPC Classes  ?

83.

CONTROLLED RELEASE SELEXIPAG COMPOSITION

      
Application Number EP2021052059
Publication Number 2021/152060
Status In Force
Filing Date 2021-01-29
Publication Date 2021-08-05
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Luyten, Katrien
  • Van Droogenbroeck, Annelien

Abstract

The present invention is concerned with controlled release compositions for oral administration comprising 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N- isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (selexipag, NS-304, ACT- 293987) and its pharmaceutically acceptable salts and/or 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid (metabolite of selexipag, MRE-269, ACT- 333679) and its pharmaceutically acceptable salts; and with processes for preparing such controlled release compositions as well as to uses thereof.

IPC Classes  ?

  • A61K 9/50 - Microcapsules
  • A61K 31/4965 - Non-condensed pyrazines
  • A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
  • A61P 9/12 - Antihypertensives
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61P 13/12 - Drugs for disorders of the urinary system of the kidneys

84.

EchoPhast

      
Application Number 211913700
Status Pending
Filing Date 2021-07-07
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ?
  • 41 - Education, entertainment, sporting and cultural services
  • 42 - Scientific, technological and industrial services, research and design
  • 44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services

Goods & Services

(1) Educational services (2) Internet platform (3) Medical services; medical information services

85.

Pharmaceutical composition for the treatment of pulmonary arterial hypertension

      
Application Number 17189881
Grant Number 11234980
Status In Force
Filing Date 2021-03-02
First Publication Date 2021-07-01
Grant Date 2022-02-01
Owner Actelion Pharmaceuticals Ltd (Switzerland)
Inventor
  • Csonka, Dénes
  • Fares, Wassim
  • Hoogkamer, Hans
  • Torfs, Koen

Abstract

The present invention relates to high doses of macitentan, i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof, or of aprocitentan, for use in the treatment and/or prevention of pulmonary arterial hypertension (PAH). Moreover, the present invention relates to the use of high doses of macitentan, or of aprocitentan, for the manufacture of a medicament for the treatment and/or prevention of PAH, as well as to a method for the treatment and/or prevention of PAH comprising high doses of macitentan or of aprocitentan. Further, the present invention relates to a dosage regimen for the treatment and/or prevention of PAH as well as to a combination of macitentan, or of aprocitentan, with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Therein, PAH is preferably mild or moderate PAH. Moreover, the present invention relates to a pharmaceutical composition for the treatment of PAH comprising a high dose of macitentan or of aprocitentan.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 9/12 - Antihypertensives
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems

86.

Stable pharmaceutical compositions comprising a pyrimidine-sulfamide

      
Application Number 17116983
Grant Number 11648249
Status In Force
Filing Date 2020-12-09
First Publication Date 2021-06-24
Grant Date 2023-05-16
Owner Actelion Pharmaceuticals Ltd (Switzerland)
Inventor
  • Adesuyi, Charles Tokunbo
  • Lithgow, Bruce Hamilton
  • Lambert, Olivier
  • Holman, Lovelace

Abstract

The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets

87.

PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF PULMONARY VASCULAR DISEASE AND/OR CARDIAC DYSFUNCTION IN FONTAN-PALLIATED PATIENTS

      
Document Number 03158468
Status Pending
Filing Date 2020-11-25
Open to Public Date 2021-06-03
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Csonka, Denes
  • Fares, Wassim
  • Hoogkamer, Hans
  • Torfs, Koen

Abstract

The present invention relates to high doses of macitentan (INN), i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof for use in the treatment of pulmonary vascular disease and/or cardiac dysfunction in functional single ventricular heart disease patients, especially in Fontan-palliated patients. Moreover, the present invention relates to the use of high doses of macitentan for the manufacture of a medicament as well as to a method for the treatment of said diseases. Further, the present invention relates to a dosage regimen as well as to a combination of macitentan with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Besides, the present invention relates to a pharmaceutical composition for the treatment of pulmonary vascular disease and/or cardiac dysfunction in functional single ventricular heart disease patients, especially in Fontan-palliated patients comprising a high dose of macitentan. Moreover, the present invention relates to the use of high doses aprocitentan for the same purpose.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
  • A61K 31/5578 - Eicosanoids, e.g. leukotrienes having a pentalene ring system, e.g. carbacyclin, iloprost
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

88.

METHODS OF TREATING PULMONARY ARTERIAL HYPERTENSION

      
Document Number 03158292
Status Pending
Filing Date 2020-11-27
Open to Public Date 2021-06-03
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Maresta, Alessandro
  • Perchenet, Loic

Abstract

The disclosure relates to methods of reducing the risk of disease progression in a patient with pulmonary arterial hypertension (PAH), comprising administering to a patient in need thereof, an initial triple combination therapy of an endothelin receptor antagonist (ERA), a phosphodiesterase type 5 (PDE-5) inhibitor, and a prostacyclin receptor agonist (IP receptor agonist).

IPC Classes  ?

  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 9/12 - Antihypertensives

89.

PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF PULMONARY VASCULAR DISEASE AND/OR CARDIAC DYSFUNCTION IN FONTAN-PALLIATED PATIENTS

      
Application Number EP2020083289
Publication Number 2021/105164
Status In Force
Filing Date 2020-11-25
Publication Date 2021-06-03
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Csonka, Dénes
  • Fares, Wassim
  • Hoogkamer, Hans
  • Torfs, Koen

Abstract

The present invention relates to high doses of macitentan (INN), i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof for use in the treatment of pulmonary vascular disease and/or cardiac dysfunction in functional single ventricular heart disease patients, especially in Fontan-palliated patients. Moreover, the present invention relates to the use of high doses of macitentan for the manufacture of a medicament as well as to a method for the treatment of said diseases. Further, the present invention relates to a dosage regimen as well as to a combination of macitentan with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Besides, the present invention relates to a pharmaceutical composition for the treatment of pulmonary vascular disease and/or cardiac dysfunction in functional single ventricular heart disease patients, especially in Fontan-palliated patients comprising a high dose of macitentan. Moreover, the present invention relates to the use of high doses aprocitentan for the same purpose.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
  • A61K 31/5578 - Eicosanoids, e.g. leukotrienes having a pentalene ring system, e.g. carbacyclin, iloprost
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim

90.

METHODS OF TREATING PULMONARY ARTERIAL HYPERTENSION

      
Application Number EP2020083593
Publication Number 2021/105331
Status In Force
Filing Date 2020-11-27
Publication Date 2021-06-03
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Maresta, Alessandro
  • Perchenet, Loïc

Abstract

The disclosure relates to methods of reducing the risk of disease progression in a patient with pulmonary arterial hypertension (PAH), comprising administering to a patient in need thereof, an initial triple combination therapy of an endothelin receptor antagonist (ERA), a phosphodiesterase type 5 (PDE-5) inhibitor, and a prostacyclin receptor agonist (IP receptor agonist).

IPC Classes  ?

  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
  • A61P 9/12 - Antihypertensives
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

91.

PATHWAY TO LIFE

      
Application Number 210580600
Status Registered
Filing Date 2021-05-10
Registration Date 2025-03-03
Owner Actelion Pharmaceuticals Ltd (Switzerland)
NICE Classes  ? 41 - Education, entertainment, sporting and cultural services

Goods & Services

(1) Educational services in the field of healthcare; arranging and conducting seminars, workshops, educational courses, conferences, symposia and events in the field of healthcare

92.

PHARMACEUTICAL COMPOSITION COMPRISING SELEXIPAG

      
Document Number 03154802
Status Pending
Filing Date 2020-10-22
Open to Public Date 2021-04-29
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Schrader, Marc Patrik
  • Schlicker-Spain, Alexandra

Abstract

The present invention relates to pharmaceutical compositions comprising 2-{4-[N-(5,6- diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (selexipag, NS-304, ACT-293987) which are suitable for oral administration (p.o.).

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4965 - Non-condensed pyrazines
  • A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61P 13/12 - Drugs for disorders of the urinary system of the kidneys

93.

PHARMACEUTICAL COMPOSITION COMPRISING SELEXIPAG

      
Application Number EP2020079698
Publication Number 2021/078835
Status In Force
Filing Date 2020-10-22
Publication Date 2021-04-29
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Schrader, Marc, Patrik
  • Schlicker Spain, Alexandra

Abstract

The present invention relates to pharmaceutical compositions comprising 2-{4-[N-(5,6- diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (selexipag, NS-304, ACT-293987) which are suitable for oral administration (p.o.).

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4965 - Non-condensed pyrazines
  • A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61P 13/12 - Drugs for disorders of the urinary system of the kidneys

94.

OPSUMIT

      
Serial Number 90653209
Status Registered
Filing Date 2021-04-18
Registration Date 2022-04-12
Owner Actelion Pharmaceuticals Ltd. (Switzerland)
NICE Classes  ? 44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services

Goods & Services

Providing medical information regarding pharmaceutical products and healthcare to healthcare professionals and patients

95.

USE OF PONESIMOD FOR THE TREATMENT OF MULTIPLE SCLEROSIS

      
Document Number 03145269
Status Pending
Filing Date 2020-07-21
Open to Public Date 2021-01-28
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Burcklen, Michel
  • El Akkad, Tarek
  • Hennessy, Brian
  • Vaclavkova, Andrea
  • Keenan, Alexander

Abstract

The disclosure relates to methods of treating multiple sclerosis. In certain aspects, methods of avoiding worsening of fatigue-related symptoms in a human patient suffering from multiple sclerosis and fatigue, and methods of reducing the number of combined unique active lesions (CUALs) in a patient suffering from multiple sclerosis are disclosed.

IPC Classes  ?

96.

METHODS OF TREATING MULTIPLE SCLEROSIS

      
Application Number EP2020070507
Publication Number 2021/013815
Status In Force
Filing Date 2020-07-21
Publication Date 2021-01-28
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Burcklen, Michel
  • El Akkad, Tarek
  • Hennessy, Brian
  • Vaclavkova, Andrea
  • Keenan, Alexander

Abstract

The disclosure relates to methods of treating multiple sclerosis. In certain aspects, methods of avoiding worsening of fatigue-related symptoms in a human patient suffering from multiple sclerosis and fatigue, and methods of reducing the number of combined unique active lesions (CUALs) in a patient suffering from multiple sclerosis are disclosed.

IPC Classes  ?

97.

METHODS FOR TREATING PULMONARY ARTERIAL HYPERTENSION

      
Application Number EP2020066055
Publication Number 2020/249602
Status In Force
Filing Date 2020-06-10
Publication Date 2020-12-17
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Preiss, Ralph, T.
  • Bruderer, Shirin
  • Clozel, Martine
  • Yannoulis Arceda, Natalia, Catalina

Abstract

The present disclosure provides methods of avoiding treatment interruption in a patient receiving an oral dose of selexipag for treating pulmonary arterial hypertension, wherein the patient is temporarily unable to take oral medication. These methods comprise administering to the patient an intravenous (IV) dose of selexipag, and, subsequently, returning to an oral dose of selexipag.

IPC Classes  ?

98.

TRANSITIONING PATIENTS TREATED FOR PULMONARY ARTERIAL HYPERTENSION TO SELEXIPAG

      
Application Number EP2020064089
Publication Number 2020/234361
Status In Force
Filing Date 2020-05-20
Publication Date 2020-11-26
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Zhao, Carol
  • Colvin Riesen, Johanna
  • Palmer, Gary, Arnold
  • Keating, Michael
  • Hartline, Brian
  • Benton, Wade
  • Dumitrescu, Camelia
  • Shah, Mehul, Bipinchandra

Abstract

The present disclosure provides methods of transitioning a patient being treated for pulmonary arterial hypertension with a non-selexipag prostacyclin pathway agent (PPA) to selexipag.

IPC Classes  ?

  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 9/12 - Antihypertensives

99.

METHODS FOR TREATING SARCOIDOSIS-ASSOCIATED PULMONARY HYPERTENSION

      
Application Number EP2020062568
Publication Number 2020/225297
Status In Force
Filing Date 2020-05-06
Publication Date 2020-11-12
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Preiss, Ralph, T.
  • Remenova, Tatiana
  • Konourina, Irina
  • Pfister, Thomas
  • Roscher, René
  • Frey, Aline
  • Yannoulis Arceda, Natalia, Catalina
  • Zimmermann, Rainer
  • Morrison, Keith, John
  • Bruderer, Shirin

Abstract

The present disclosure provides methods for treating sarcoidosis-associated pulmonary hypertension, comprising administering to a patient in need thereof, a therapeutically effective amount of selexipag, wherein the patient is diagnosed with sarcoidosis-associated pulmonary hypertension.

IPC Classes  ?

  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 9/08 - Vasodilators for multiple indications

100.

MACITENTAN FOR USE IN TREATING PORTOPULMONARY HYPERTENSION

      
Application Number EP2020059499
Publication Number 2020/201479
Status In Force
Filing Date 2020-04-03
Publication Date 2020-10-08
Owner ACTELION PHARMACEUTICALS LTD (Switzerland)
Inventor
  • Perchenet, Loïc
  • Cottreel, Emmanuelle

Abstract

The present invention provides methods for treating portopulmonary hypertension, comprising administering to a patient in need thereof, a therapeutically effective amount of macitentan. Preferably, the methods are clinically proven safe and/or effective. Also provided are methods of improving liver transplant perioperative mortality risk category, improving MELD exception eligibility, and reducing the risk of removal from a liver transplant waitlist in a patient with portopulmonary hypertension and liver disease, comprising administering to a patient in need thereof a therapeutically effective amount of macitentan.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
  • A61K 31/5578 - Eicosanoids, e.g. leukotrienes having a pentalene ring system, e.g. carbacyclin, iloprost
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 11/00 - Drugs for disorders of the respiratory system
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