Patents Assigned to Leo Pharma A/S
  • Patent number: 9908894
    Abstract: The present invention relates to novel methods for the preparation of 1,3-benzodioxole heterocyclic compounds and intermediates for the same. The compounds are useful as PDE4 inhibitors.
    Type: Grant
    Filed: June 22, 2015
    Date of Patent: March 6, 2018
    Assignee: LEO Pharma A/S
    Inventors: Bjorn Metzler, Andre Faldt
  • Patent number: 9855285
    Abstract: The present invention relates to a method of inhibiting the upregulation of the expression of the proinflammatory cytokine interleukin-22 (IL-22) in activated and differentiated human T-cells, said upregulation being induced by administration of a therapeutically effective amount of a phosphodiesterase 4 (PDE4) inhibitor. The method comprises administering, either sequentially to or simultaneously with the administration of the PDE4 inhibitor, a vitamin D receptor agonist in an amount sufficient to inhibit the upregulation of IL-22 expression.
    Type: Grant
    Filed: November 28, 2013
    Date of Patent: January 2, 2018
    Assignee: LEO PHARMA A/S
    Inventor: Paola Lovato
  • Patent number: 9637499
    Abstract: Compounds of the general formula I wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: May 2, 2017
    Assignee: LEO PHARMA A/S
    Inventor: Simon Feldbaek Nielsen
  • Publication number: 20170065618
    Abstract: The present invention relates to a topical spray composition comprising a biologically active vitamin D derivative or analogue and a corticosteroid, and its use in the treatment of dermal diseases and conditions.
    Type: Application
    Filed: October 19, 2016
    Publication date: March 9, 2017
    Applicant: LEO PHARMA A/S
    Inventors: Marianne LIND, Gritt RASMUSSEN, Mette Rydahl SONNE, Jens HANSEN, Karsten PETERSSON
  • Patent number: 9586961
    Abstract: The invention relates to compounds of general formula (I) wherein R1, R2, R3, R4, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immuno-suppression would be desirable for example in organ transplantation.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: March 7, 2017
    Assignee: LEO PHARMA A/S
    Inventors: Simon Felbdæk Nielsen, Daniel R. Greve, Gunnar Grue-Sørensen, Carsten Ryttersgaard, Søren Christian Schou, Anette Graven Sams
  • Patent number: 9566286
    Abstract: The present invention relates to a topical spray composition comprising a biologically active vitamin D derivative or analog and a corticosteroid, and its use in the treatment of dermal diseases and conditions.
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: February 14, 2017
    Assignee: LEO PHARMA A/S
    Inventors: Marianne Lind, Gritt Rasmussen, Mette Rydahl Sonne, Jens Hansen, Karsten Petersson
  • Publication number: 20160324875
    Abstract: A pharmaceutical composition comprising a vitamin D derivative or analogue as the active ingredient dissolved in a three-component surfactant-solvent mixture is useful in the treatment of dermal disorders or conditions.
    Type: Application
    Filed: July 19, 2016
    Publication date: November 10, 2016
    Applicant: LEO PHARMA A/S
    Inventor: Karsten PETERSSON
  • Patent number: 9487494
    Abstract: The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 8, 2016
    Assignee: LEO PHARMA A/S
    Inventors: Jef Fensholdt, Sophie Elisabeth Havez, Bjarne Nørremark
  • Publication number: 20160207930
    Abstract: The invention relates novel NK1 receptor antagonists represented in formula A, wherein R1 and R2 independently are selected from the group consisting of (C1-4)alkyl, (C1-4)haloalkyl, (C1-4)alkoxy, CD3 or halogen; R3 is selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)haloalkyl and (C1-4)hydroxyalkyl; R4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R5 and R6 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4) hydroxyalkyl and (C1-4)haloalkyl and X and Y are independently selected from the group consisting of CH and N. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds.
    Type: Application
    Filed: August 15, 2014
    Publication date: July 21, 2016
    Applicant: LEO PHARMA A/S
    Inventors: Haakan BLADH, Jakob FELDING, Ding ZHOU, Zhen-wei CAI, Morten Dahl SØRENSEN
  • Publication number: 20160206629
    Abstract: A film-forming pharmaceutical composition for dermal application comprises at least one therapeutically active ingredient dissolved in a volatile solvent, the composition further comprising a film-forming polymer, a plasticizer and an oily release-enhancing agent. The composition is capable of forming, after application on skin and evaporation of the solvent, a continuous phase comprising the film-forming polymer and the plasticizer and a dispersed phase comprising droplets of the oily release-enhancing agent.
    Type: Application
    Filed: March 29, 2016
    Publication date: July 21, 2016
    Applicant: LEO Pharma A/S
    Inventors: Karsten PETERSSON, Kit FREDERIKSEN, Diana OMKVIST, Jörgen JANSSON
  • Patent number: 9346809
    Abstract: The invention relates to compounds of general formula (I) wherein A, R1, R2, R3, R4, R5, R9, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.
    Type: Grant
    Filed: July 8, 2010
    Date of Patent: May 24, 2016
    Assignee: LEO PHARMA A/S
    Inventors: Simon Feldbæk Nielsen, Daniel Rodriguez Greve, Carsten Ryttersgaard, Gunnar Grue-Sørensen, Erik Rytter Ottosen, Tina Dahlerup Poulsen, Søren Christian Schou, Anthony Murray
  • Patent number: 9345774
    Abstract: A sprayable film-forming pharmaceutical composition for dermal application comprises at least one therapeutically active ingredient dissolved in a pharmaceutically acceptable propellant selected from the group consisting of dimethyl ether, diethyl ether and methylethylether, and a mixture of dimethyl ether, diethylether and methylethyl ether, and a second propellant selected from C3-5 alkanes, hydrofluoroalkanes, hydrochloroalkanes, fluoroalkanes and chlorofluoroalkanes, the propellant being present in an amount of 50-99.5% w/w of the composition, the composition further comprising a film-forming polymer, a plasticizer and an oily release-enhancing agent.
    Type: Grant
    Filed: July 5, 2013
    Date of Patent: May 24, 2016
    Assignee: LEO PHARMA A/S
    Inventors: Karsten Petersson, Kit Frederiksen, Diana Omkvist, Jörgen Jansson
  • Patent number: 9273064
    Abstract: Compounds of the general formula I wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: March 1, 2016
    Assignee: LEO PHARMA A/S
    Inventor: Simon Feldbaek Nielsen
  • Patent number: 9254296
    Abstract: A topical pharmaceutical composition which is an oil-in-water-oil emulsion comprising a vitamin D derivative or analogue dissolved in a mixture of a non-ionic surfactant and a lower alkanol. The topical pharmaceutical composition may be used in the treatment of dermal conditions, such as psoriasis.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: February 9, 2016
    Assignee: LEO PHARMA A/S
    Inventor: Karsten Petersson
  • Publication number: 20160022657
    Abstract: Compounds of the general formula I wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.
    Type: Application
    Filed: October 1, 2015
    Publication date: January 28, 2016
    Applicant: LEO PHARMA A/S
    Inventor: Simon Feldbaek NIELSEN
  • Patent number: 9238056
    Abstract: A cyclic peptide capable of binding specifically to the ?2 I domain of a collagen binding integrin receptor may be conjugated to a drug containing particle via a linker moiety. The conjugate may be used to target a therapeutic drug to a cell expressing a collagen binding integrin receptor on its surface.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: January 19, 2016
    Assignee: LEO PHARMA A/S
    Inventors: Nina Østergaard Knudsen, Thorsten Thormann
  • Patent number: 9233964
    Abstract: The invention relates to compounds of general Formula (I), Wherein R1, R2, R3, R4, R5, m, n are defined herein, and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: January 12, 2016
    Assignee: LEO PHARMA A/S
    Inventors: Søren Christian Schou, Daniel Rodriguez Greve, Simon Feldbæk Nielsen, Jens Bjørn Jensen, Kevin Neil Dack
  • Publication number: 20150335575
    Abstract: The present invention relates to a topical spray composition comprising a biologically active vitamin D derivative or analogue and a corticosteroid, and its use in the treatment of dermal diseases and conditions.
    Type: Application
    Filed: May 8, 2015
    Publication date: November 26, 2015
    Applicant: LEO PHARMA A/S
    Inventors: Marianne LIND, Gritt RASMUSSEN, Mette Rydahl SONNE, Jens HANSEN, Karsten PETERSSON
  • Patent number: 9181248
    Abstract: The present invention relates to novel [1,2,4]triazolopyridine compounds with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: November 10, 2015
    Assignee: LEO PHARMA A/S
    Inventors: Simon Feldbaek Nielsen, Jens Christian Hojland Larsen
  • Patent number: 9181259
    Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(?O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(?O)R7, C(?O)OR7, C(?O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(?O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ?CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically accep
    Type: Grant
    Filed: February 20, 2013
    Date of Patent: November 10, 2015
    Assignee: LEO PHARMA A/S
    Inventors: Morten Dahl Sørensen, Romano Di Fabio, Alfonso Pozzan, Maria Pia Catalani, Haakon Bladh, Jakob Felding