Patents Assigned to Leo Pharma A/S
  • Process for preparing 7H-pyrrolo[2,3-d]pyrimidine derivatives and synthetic intermediates thereof
    Patent number: 11673900
    Abstract: The present invention provides processes for preparing 7H-pyrrolo[2,3-d]pyrimidine derivatives, which are useful as a Janus kinase (JAK) inhibitor, intermediates thereof, and processes for preparing the intermediates. The present invention provides processes for preparing 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile using salts of (3S,4R)-1-benzyl-3-methyl-1,6-diazaspiro[3.4]octane with organic acids.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: June 13, 2023
    Assignees: Japan Tobacco Inc., LEO Pharma A/S
    Inventors: Hiromu Takiguchi, Akinobu Higashi, Takashi Inaba, Takashi Watanabe, Tsubasa Takeichi, Anders Klarskov Petersen, Per Vedsoe, Kim Lebek Jensen, Jan Bornholdt, Soren Ebdrup
  • Small molecule modulators of IL-17
    Patent number: 11377425
    Abstract: The present invention relates to a compound according to formula I and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: July 5, 2022
    Assignee: Leo Pharma A/S
    Inventors: Kevin Neil Dack, Xifu Liang, Mogens Larsen, Mark Andrews, Alan Stuart Jessiman, Mia Nørreskov Burhardt, Patrick Stephen Johnson, Peter Andersen, Lars Jørgensen
  • Substituted pyrazoloazepin-4-ones and their use as phosphodiesterase inhibitors
    Patent number: 11065257
    Abstract: The present invention relates to novel substituted pyrazoloazepin-4-ones 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 12, 2017
    Date of Patent: July 20, 2021
    Assignee: LEO Pharma A/S
    Inventors: Xifu Liang, Jens Larsen, Simon Feldbaek Nielsen, Peter Andersen
  • Heteroaromatic modulators of the retinoid-related orphan receptor gamma
    Patent number: 10934282
    Abstract: The present invention relates to a compound according to general formula (I) wherein X represents N or CH; R1 is —CN, (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7 membered)heterocycloalkyl, (5-6 membered)heteroaryl, (C3-C7)cycloalkyl(C1-C4)alkyl, (3-7 membered)heterocycloalkyl-(C1-C4)alkyl or (5-6 membered)heteroaryl-(C1-C4)alkyl; R2 is halogen, cyano, (C1-C4)alkyl or (C3-C7)cycloalkyl; R3 is halogen, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl or (C3-C7)cycloalkyl; R4 is (C1-C4)alkyl or (C1-C4)haloalkyl; R5 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-(C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (3-7 membered)heterocycloalkyl, phenyl, (5-6 membered)heteroaryl or —ORa. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds and to intermediates for preparation of said compounds.
    Type: Grant
    Filed: May 15, 2020
    Date of Patent: March 2, 2021
    Assignee: LEO Pharma A/S
    Inventors: Alan Stuart Jessiman, Patrick Stephen Johnson, Kristoffer Maansson, Morten Dahl Sørensen
  • Substituted pyrazoloazepin-4-ones and their use as phosphodiesterase inhibitors
    Patent number: 10906915
    Abstract: The present invention relates to novel substituted pyrazoloazepin-4-ones 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 12, 2016
    Date of Patent: February 2, 2021
    Assignee: LEO Pharma A/S
    Inventors: Xifu Liang, Jens Larsen, Simon Feldbaek Nielsen, Peter Andersen
  • Bicyclic amines as novel JAK kinase inhibitors
    Patent number: 10851116
    Abstract: The present invention relates to a compound according to formula I wherein R1 is alkyl; n is 1 or 2; R2 is selected from the group consisting of hydrogen, cyano, —SO2Ra, —SO2NRbRc, —C(O)Rb, phenyl and 5- and 6-membered heteroaryl or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to pharmaceutical compositions comprising said compounds, and to methods of treating proliferative or inflammatory skin disorders with said compounds.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: December 1, 2020
    Assignee: LEO Pharma A/S
    Inventors: Daniel Rodriguez Greve, Tue Heesgaard Jepsen, Mogens Larsen, Andreas Ritzen
  • SUBSTITUTED PYRAZOLOAZEPIN-4-ONES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
    Publication number: 20200323869
    Abstract: The present invention relates to novel substituted pyrazoloazepin-4-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
    Type: Application
    Filed: December 12, 2017
    Publication date: October 15, 2020
    Applicant: LEO Pharma A/S
    Inventors: Xifu LIANG, Jens LARSEN, Simon Feldbaek NIELSEN, Peter ANDERSEN
  • 5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-5-azaspiro[2.5]octane-8-carboxylic acid derivatives as novel JAK kinase inhibitors
    Patent number: 10799507
    Abstract: The present invention relates to a compound according to formula (I) wherein X represents NH or O; n is an integer selected from 1-3; Y represents a bond, —C(O)O—*, —C(O)OR3—* or —C(O)NHR3—*; W is selected from the group consisting of phenyl, pyridyl, (C3-C7)cycloalkyl and 4-6 membered heterocycloalkyl; or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further 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: February 1, 2018
    Date of Patent: October 13, 2020
    Assignee: Leo Pharma A/S
    Inventors: Mogens Larsen, Andreas Ritzen, Bjarne Nørremark, Daniel Rodriguez Greve
  • Substituted pyrazoloazepin-8-ones and their use as phosphodiesterase inhibitors
    Patent number: 10793580
    Abstract: The present invention relates to novel pyrazoloazepin-8-ones 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 12, 2016
    Date of Patent: October 6, 2020
    Assignee: LEO Pharma A/S
    Inventors: Xifu Liang, Jens Larsen
  • Pharmaceutical spray composition comprising a vitamin D analogue and a corticosteroid
    Patent number: 10716799
    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: Grant
    Filed: August 28, 2019
    Date of Patent: July 21, 2020
    Assignee: LEO Pharma A/S
    Inventors: Marianne Lind, Gritt Rasmussen, Mette Rydahl Sonne, Jens Hansen, Karsten Petersson
  • Amino-imidazopyridine derivatives as Janus kinase inhibitors and pharmaceutical use thereof
    Patent number: 10703751
    Abstract: The present invention relates to a compound according to formula (I) or pharmaceutically acceptable salts, hydrates, or solvates thereof; wherein R1 is C1-alkyl, R2 is C1-alkyl, R3 is C2-alkyl, R4 is hydrogen, R5 is hydrogen. The invention relates further to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to said compounds for use in the treatment autoimmune diseases and to intermediates for the preparation of said compounds.
    Type: Grant
    Filed: January 10, 2018
    Date of Patent: July 7, 2020
    Assignee: Leo Pharma A/S
    Inventors: Jens Larsen, Mogens Larsen, Lars Kyhn Rasmussen, Andreas Ritzen, Tine Marianne Duus
  • Pharmaceutical spray composition comprising a vitamin D analogue and a corticosteroid
    Patent number: 10688108
    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: Grant
    Filed: August 28, 2019
    Date of Patent: June 23, 2020
    Assignee: Leo Pharma A/S
    Inventors: Marianne Lind, Gritt Rasmussen, Mette Rydahl Sonne, Jens Hansen, Karsten Petersson
  • Pharmaceutical spray composition comprising a vitamind D analogue and a corticosteroid
    Patent number: 10682364
    Abstract: A Pharmaceutical Spray Composition Comprising a Vitamin D Analogue and a Corticosteroid 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: Grant
    Filed: August 28, 2019
    Date of Patent: June 16, 2020
    Assignee: LEO Pharma A/S
    Inventors: Marianne Lind, Gritt Rasmussen, Mette Rydahl Sonne, Jens Hansen, Karsten Petersson
  • Pharmaceutical spray composition comprising a vitamin D analogue and a corticosteroid
    Patent number: 10660908
    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: Grant
    Filed: September 19, 2018
    Date of Patent: May 26, 2020
    Assignee: LEO Pharma A/S
    Inventors: Marianne Lind, Gritt Rasmussen, Mette Rydahl Sonne, Jens Hansen, Karsten Petersson
  • Heteroaromatic modulators of the retinoid-related orphan receptor gamma
    Patent number: 10662181
    Abstract: The present invention relates to a compound according to general formula (I) wherein X represents N or CH; R1 is —CN, (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7 membered)heterocycloalkyl, (5-6 membered)heteroaryl, (C3-C7)cycloalkyl(C1-C4)alkyl, (3-7 membered)heterocycloalkyl-(C1-C4)alkyl or (5-6 membered)heteroaryl-(C1-C4)alkyl; R2 is halogen, cyano, (C1-C4)alkyl or (C3-C7)cycloalkyl; R3 is halogen, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl or (C3-C7)cycloalkyl; R4 is (C1-C4)alkyl or (C1-C4)haloalkyl; R5 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-(C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (3-7 membered)heterocycloalkyl, phenyl, (5-6 membered)heteroaryl or —ORa. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds and to intermediates for preparation of said compounds.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: May 26, 2020
    Assignee: LEO Pharma A/S
    Inventors: Alan Stuart Jessiman, Patrick Stephen Johnson, Kristoffer Maansson, Morten Dahl Sørensen
  • Pharmaceutical spray composition comprising a vitamind D analogue and a corticosteroid
    Patent number: 10617698
    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: Grant
    Filed: August 28, 2019
    Date of Patent: April 14, 2020
    Assignee: Leo Pharma A/S
    Inventors: Marianne Lind, Gritt Rasmussen, Mette Rydahl Sonne, Jens Hansen, Karsten Petersson
  • Non-steroidal glucocorticoid receptor modulators for local drug delivery
    Patent number: 10494363
    Abstract: The present invention relates to a compound according to formula (I) wherein R1 is selected from the group consisting of 5- and 6-membered heteroaryl, (C1-C6)alkyl, (C3-C6)cycloalkyl, (4-6)-membered heterocycloalkyl and phenyl; R2 is selected from (C1-C3)alkyl and halo(C1-C3)alkyl; R3 is selected from phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R4 is selected from hydrogen, halogen, (C1-C4)alkyl and halo(C1-C4)alkyl; X1 is selected from CH, C(Rb) and N, X2 is selected from CH and N; Y is selected from —NH— and —O—; m is 0 or 1; n is 0 or 1; L represents a bond, —O—, —NH— or —N(Rc)—; or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to intermediates for the preparation of said compounds, 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: September 13, 2016
    Date of Patent: December 3, 2019
    Assignee: Leo Pharma A/S
    Inventors: Patrick Stephen Johnson, Kevin Neil Dack, Krister Henriksson
  • PHARMACEUTICAL SPRAY COMPOSITION COMPRISING A VITAMIN D ANALOGUE AND A CORTICOSTEROID
    Publication number: 20190015430
    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: September 19, 2018
    Publication date: January 17, 2019
    Applicant: LEO Pharma A/S
    Inventors: Marianne LIND, Gritt RASMUSSEN, Mette Ridahi SONNE, Jens HANSEN, Karsten PETERSSON
  • Pharmaceutical spray composition comprising a vitamin D analogue and a corticosteroid
    Patent number: 10130640
    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: November 20, 2018
    Assignee: Leo Pharma A/S
    Inventors: Marianne Lind, Gritt Rasmussen, Mette Rydahl Sonne, Jens Hansen, Karsten Petersson
  • TREATMENT OF ALOPECIA AREATA
    Publication number: 20180263986
    Abstract: The present invention provides a novel treatment of alopecia areate. The problem to be solved by the invention is to provide a new pharmaceutical use of 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile. A therapeutic or preventive agent for alopecia areata, containing 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile as an active ingredient.
    Type: Application
    Filed: September 22, 2016
    Publication date: September 20, 2018
    Applicants: LEO Pharma A/S, Japan Tobacco Inc.
    Inventors: Michael SIERRA, Tord LABUDA, Atsuo TANIMOTO, Yuichi SHINOZAKI