公开(公告)号：US20070255066A1

公开(公告)日：2007-11-01

申请号：US11631294

申请日：2005-08-22

Applicant: Hendrik Pedersen ,  Claus Age Bretting ,  Ernst Binderup

Inventor： Hendrik Pedersen ,  Claus Age Bretting ,  Ernst Binderup

IPC: C07C401/00 ,  C07J9/00

CPC classification number: C07J9/00 ,  C07C401/00 ,  C07C2601/02

Abstract: The present invention relates to processes for epimerising alcohols of compounds having a hydroxyl substituent on an asymmetric allylic carbon, such as compounds useful for the synthesis of vitamin D analogues where the epimeric hydroxyl substituent is at the 24 position. The Invention further relates to methods of producing intermediates useful for the synthesis of calcipotriol by said epimerisation processes.

Abstract translation: 本发明涉及在不对称烯丙基碳上具有羟基取代基的化合物的差向异构化方法，例如可用于合成维甲酸类似物的化合物，其中差向异构羟基取代基位于24位。 本发明还涉及通过所述差向异构化方法制备可用于合成卡泊三醇的中间体的方法。

公开(公告)号：US20070249676A1

公开(公告)日：2007-10-25

申请号：US11823571

申请日：2007-06-28

Applicant: Ernst Binderup ,  Tore Duvold

Inventor： Ernst Binderup ,  Tore Duvold

IPC: A61K31/444 ,  A61P35/00

CPC classification number: C07D213/75 ,  A61K31/444

Abstract: Pyridyl cyanoguanidine compounds of the general formula I wherein A, X1, X2, X3, Y1, Y2, Y3, R1, R2, R5, R6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseases such as cancers.

Abstract translation: 通式I的吡啶基氰基胍化合物，其中A，X 1，X 2，X 3，Y 1， Y 2，Y 3，R 1，R 2，R 5， R 6和n如说明书中所示，适合作为增殖性疾病如癌症的人和兽医学治疗中的前药。

公开(公告)号：US20050215588A1

公开(公告)日：2005-09-29

申请号：US10514500

申请日：2003-05-15

Applicant: Ernst Binderup ,  Tore Duvold

Inventor： Ernst Binderup ,  Tore Duvold

IPC: A61K31/44 ,  A61K31/4545 ,  C07D213/75 ,  C07D401/12 ,  C07D41/02

CPC classification number: C04B35/632 ,  C07D213/75 ,  C07D401/12

Abstract: Pyridyl cyanoguanidine compounds of the general formula I wherein A, X1, X2, X3, Y1, Y2, Y3, R1, R2, R5, R6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseases such as cancers.

Abstract translation: 通式I的吡啶基氰基胍化合物，其中A，X 1，X 2，X 3，Y 1， Y 2，Y 3，R 1，R 2，R 5， R 6和n如说明书中所示，适合作为增殖性疾病如癌症的人和兽医学治疗中的前药。

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.