公开(公告)号：US20240398809A1

公开(公告)日：2024-12-05

申请号：US18405453

申请日：2024-01-05

Applicant: LEO PHARMA A/S ,  Japan Tobacco Inc.

Inventor： Michael SIERRA ,  Tord LABUDA ,  Atsuo TANIMOTO ,  Yuichi SHINOZAKI

IPC: A61K31/519 ,  A61K9/00 ,  A61K9/06 ,  A61K47/06 ,  A61P17/14

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-ox-opropanenitrile. 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.

公开(公告)号：US20240140967A1

公开(公告)日：2024-05-02

申请号：US18136661

申请日：2023-04-19

Applicant: JAPAN TOBACCO INC. ,  LEO Pharma A/S

Inventor： Hiromu Takiguchi ,  Akinobu Higashi ,  Takashi Inaba ,  Takashi Watanabe ,  Tsubasa Takeichi ,  Anders Klarskov Petersen ,  Per Vedsoe ,  Kim Lebek Jensen ,  Jan Bornholdt ,  Soren Ebdrup

IPC: C07D519/00 ,  C07C271/22 ,  C07D487/10

CPC classification number: C07D519/00 ,  C07C271/22 ,  C07D487/10 ,  C07B2200/13

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.

公开(公告)号：US20230250079A1

公开(公告)日：2023-08-10

申请号：US18001464

申请日：2021-06-10

Applicant: LEO PHARMA A/S

Inventor： Mark ANDREWS ,  Morten Dahl SØRENSEN ,  Mogens LARSEN ,  Nicolas DEVAUX ,  Vinicius BARROS RIBEIRO DA SILVA ,  Quentin PERRON ,  Xifu LIANG ,  Jimmi Gerner SEIZBERG

IPC: C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  C07D403/12

CPC classification number: C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  C07D403/12

Abstract: The present disclosure relates to a compound according to formula I




and pharmaceutically acceptable salts, hydrates, or solvates thereof. The disclosure 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.

公开(公告)号：US20230227435A1

公开(公告)日：2023-07-20

申请号：US18002080

申请日：2021-06-17

Applicant: LEO PHARMA A/S

Inventor： Mark ANDREWS ,  Kevin Neil DACK ,  Jimmi Gerner SEITZBERG ,  Peter ANDERSEN

IPC: C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D405/14

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D405/14

Abstract: The present disclosure relates to compounds according to formula I






and pharmaceutically acceptable salts, hydrates, or solvates thereof. The disclosure 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.

公开(公告)号：US11673900B2

公开(公告)日：2023-06-13

申请号：US16470888

申请日：2017-12-20

Applicant: JAPAN TOBACCO INC. ,  LEO Pharma A/S

Inventor： Hiromu Takiguchi ,  Akinobu Higashi ,  Takashi Inaba ,  Takashi Watanabe ,  Tsubasa Takeichi ,  Anders Klarskov Petersen ,  Per Vedsoe ,  Kim Lebek Jensen ,  Jan Bornholdt ,  Soren Ebdrup

IPC: C07D403/06 ,  C07D519/00 ,  C07D487/10 ,  C07D205/08 ,  C07D307/33 ,  C07C271/22 ,  C07C269/00 ,  C07C269/06 ,  C07D491/107 ,  C07D491/10

CPC classification number: C07D519/00 ,  C07C271/22 ,  C07D487/10 ,  C07B2200/13

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.

公开(公告)号：US20220241284A1

公开(公告)日：2022-08-04

申请号：US17610787

申请日：2020-05-14

Applicant: LEO PHARMA A/S

Inventor： Jacob NIELSEN ,  Gitte Pommergaard PEDERSEN ,  Helene MORTENSEN ,  Camilla SANDER ,  Pia Klie REFER

IPC: A61K31/519 ,  A61K9/00 ,  A61K47/06 ,  A61K47/10 ,  A61K47/12 ,  A61K9/10

Abstract: The present invention relates to the treatment of cutaneous lupus erythematosus. 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 cutaneous lupus erythematosus, 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, and a pharmaceutical formulation thereof.

公开(公告)号：US10716799B2

公开(公告)日：2020-07-21

申请号：US16554586

申请日：2019-08-28

Applicant: LEO Pharma A/S

Inventor： Marianne Lind ,  Gritt Rasmussen ,  Mette Rydahl Sonne ,  Jens Hansen ,  Karsten Petersson

IPC: A61K31/593 ,  A61K31/59 ,  A61K47/06 ,  A61K47/08 ,  A61M11/00 ,  A61K9/00 ,  A61K9/12 ,  A61K31/573 ,  A61K31/58 ,  A61M35/00 ,  A61K47/14 ,  A61K47/22 ,  B65D83/20 ,  B65D83/14

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.

公开(公告)号：US20200216470A1

公开(公告)日：2020-07-09

申请号：US16470888

申请日：2017-12-20

Applicant: JAPAN TOBACCO INC. ,  LEO Pharma A/S

Inventor： Hiromu Takiguchi ,  Akinobu Higashi ,  Takashi Inaba ,  Takashi Watanabe ,  Tsubasa Takeichi ,  Anders Klarskov Petersen ,  Per Vedsoe ,  Kim Lebek Jensen ,  Jan Bornholdt ,  Soren Ebdrup

IPC: C07D519/00 ,  C07D487/10 ,  C07C271/22

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.

公开(公告)号：US10688108B2

公开(公告)日：2020-06-23

申请号：US16554539

申请日：2019-08-28

Applicant: LEO Pharma A/S

Inventor： Marianne Lind ,  Gritt Rasmussen ,  Mette Rydahl Sonne ,  Jens Hansen ,  Karsten Petersson

IPC: A61K31/593 ,  A61K31/59 ,  A61K47/06 ,  A61K47/08 ,  A61M11/00 ,  A61K9/00 ,  A61K9/12 ,  A61K31/573 ,  A61K31/58 ,  A61M35/00 ,  A61K47/14 ,  A61K47/22 ,  B65D83/20 ,  B65D83/14

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.

公开(公告)号：US10660908B2

公开(公告)日：2020-05-26

申请号：US16135366

申请日：2018-09-19

Applicant: LEO Pharma A/S

Inventor： Marianne Lind ,  Gritt Rasmussen ,  Mette Rydahl Sonne ,  Jens Hansen ,  Karsten Petersson

IPC: A61K31/593 ,  A61K31/59 ,  A61K47/06 ,  A61K47/08 ,  A61M11/00 ,  A61K9/00 ,  A61K9/12 ,  A61K31/573 ,  A61K31/58 ,  A61M35/00 ,  A61K47/14 ,  A61K47/22 ,  B65D83/20 ,  B65D83/14

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.