公开(公告)号：US07034015B2

公开(公告)日：2006-04-25

申请号：US10228954

申请日：2002-08-28

Applicant: Erik Rytter Ottosen ,  Anne Marie Horneman ,  Xifu Liang

Inventor： Erik Rytter Ottosen ,  Anne Marie Horneman ,  Xifu Liang

IPC: A61K31/277 ,  A61K31/221 ,  A61K31/165 ,  A61K31/135 ,  A61K31/15

CPC classification number: C07C225/22 ,  C07C229/44 ,  C07C233/40 ,  C07C233/43 ,  C07C235/10 ,  C07C235/20 ,  C07C235/74 ,  C07C271/20 ,  C07C271/22 ,  C07C309/73 ,  C07C311/09 ,  C07C317/48 ,  C07C323/52 ,  C07C2601/14 ,  C07D207/27 ,  C07D207/404 ,  C07D233/74 ,  C07D295/135 ,  C07D307/14 ,  C07D309/12 ,  C07D317/22 ,  C07D317/28 ,  C07D493/04 ,  C07D493/14

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract translation: 本发明涉及新一类氨基二苯甲酮衍生物，包含所述化合物的药物制剂，该制剂的剂量单位，治疗患者的方法，包括施用所述化合物，以及所述化合物在制备药物制剂中的用途。

公开(公告)号：US20250084106A1

公开(公告)日：2025-03-13

申请号：US18960075

申请日：2024-11-26

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

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：US20240208938A1

公开(公告)日：2024-06-27

申请号：US18526149

申请日：2023-12-01

Applicant: LEO Pharma A/S

Inventor： Mark ANDREWS ,  Mogens LARSEN ,  Alan JESSIMAN ,  Patrick JOHNSON ,  Kevin Neil DACK

IPC: C07D401/14

CPC classification number: C07D401/14

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.

公开(公告)号：US20240190977A1

公开(公告)日：2024-06-13

申请号：US18507579

申请日：2023-11-13

Applicant: LEO Pharma A/S

Inventor： Birgitte Ursø ,  Waseem Sajid ,  Paola Lovato ,  Heidi Westh Bagger ,  Christoph Erkel ,  Petra Nussbaumer ,  Simon Schuster

IPC: C07K16/28 ,  A61K39/00

CPC classification number: C07K16/2866 ,  A61K2039/505 ,  C07K2317/21 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/76 ,  C07K2317/92

Abstract: The present disclosure provides novel antibodies and fragments thereof targeting IL-1RAcP (Interleukin-1 receptor accessory protein). Use of IL-1RAcP inhibitors are also provided herein.

公开(公告)号：US20230138114A1

公开(公告)日：2023-05-04

申请号：US17811347

申请日：2022-07-08

Applicant: LEO Pharma A/S

Inventor： Tero WENNBERG ,  Anders Per SØRENSEN

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

Abstract: The present disclosure relates to the treatment of hand eczema. The problem to be solved by the disclosure 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 hand eczema, 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：US20220411517A1

公开(公告)日：2022-12-29

申请号：US17664349

申请日：2022-05-20

Applicant: LEO Pharma A/S

Inventor： Birgitte Ursø ,  Waseem Sajid ,  Paola Lovato ,  Heidi Westh Bagger ,  Christoph Erkel ,  Petra Nussbaumer ,  Simon Schuster

IPC: C07K16/28

Abstract: The present disclosure provides novel antibodies and fragments thereof targeting IL-1RAcP. Use of IL-1RAcP inhibitors are also provided herein.

公开(公告)号：US20210147440A1

公开(公告)日：2021-05-20

申请号：US16624491

申请日：2018-06-19

Applicant: LEO Pharma A/S

Inventor： Allan Carsten DAHL ,  Johan Eriksson BAJTNER ,  Esben Paul Krogh OLSEN ,  Bjørn METZLER

IPC: C07D495/10 ,  B01J21/16

Abstract: The present invention relates to novel methods for the preparation of 1,3-benzodioxole heterocyclic compounds of formula (I). The compounds are useful as PDE4 inhibitors.

公开(公告)号：US20210070769A1

公开(公告)日：2021-03-11

申请号：US16772428

申请日：2018-12-14

Applicant: LEO Pharma A/S

Inventor： Mark ANDREWS ,  Daniel Rodriguez GREVE ,  Jens LARSEN

IPC: C07D495/04

Abstract: The present invention relates to novel substituted azetidine dihydrothienopyrimidines with phosphodiesterase inhibitory activity, and to their use in therapy, and to pharmaceutical compositions comprising the compounds and to methods of treating diseases with the compounds (I).

公开(公告)号：US10851116B2

公开(公告)日：2020-12-01

申请号：US16479375

申请日：2018-01-19

Applicant: LEO Pharma A/S

Inventor： Daniel Rodriguez Greve ,  Tue Heesgaard Jepsen ,  Mogens Larsen ,  Andreas Ritzen

IPC: C07D519/00 ,  A61K31/519

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.

公开(公告)号：US10793580B2

公开(公告)日：2020-10-06

申请号：US16468429

申请日：2016-12-12

Applicant: LEO Pharma A/S

Inventor： Xifu Liang ,  Jens Larsen

IPC: C07D491/20

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.