公开(公告)号：US12110293B2

公开(公告)日：2024-10-08

申请号：US17152930

申请日：2021-01-20

Applicant: GRÜNENTHAL GMBH

Inventor： Florian Jakob ,  Jo Alen ,  Simon Lucas ,  Tobias Craan ,  Ingo Konetzki ,  Achim Kless ,  Stefan Schunk ,  Paul Ratcliffe ,  Sebastian Wachten ,  Simon Cruwys

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to compounds according to general formula (I)




which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.

公开(公告)号：US11981677B2

公开(公告)日：2024-05-14

申请号：US17171520

申请日：2021-02-09

Applicant: Grünenthal GmbH

Inventor： Florian Jakob ,  Jo Alen ,  Simon Lucas ,  Tobias Craan ,  Ingo Konetzki ,  Achim Kless ,  Stefan Schunk ,  Paul Ratcliffe ,  Sebastian Wachten ,  Simon Cruwys

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to compounds according to general formula (I)




which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.

公开(公告)号：US10981918B2

公开(公告)日：2021-04-20

申请号：US16517080

申请日：2019-07-19

Applicant: Grünenthal GmbH

Inventor： Florian Jakob ,  Jo Alen ,  Simon Lucas ,  Tobias Craan ,  Ingo Konetzki ,  Achim Kless ,  Stefan Schunk ,  Paul Ratcliffe ,  Sebastian Wachten ,  Simon Cruwys

IPC: C07D487/04

Abstract: The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.

公开(公告)号：US10391099B2

公开(公告)日：2019-08-27

申请号：US15354424

申请日：2016-11-17

Applicant: Grünenthal GmbH

Inventor： Antonio Nardi ,  Florian Jakob ,  Ingo Konetzki ,  Tobias Craan ,  Christian Hesslinger

IPC: A61K31/5377 ,  A61K31/506 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D401/14

Abstract: The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.

公开(公告)号：US09670189B2

公开(公告)日：2017-06-06

申请号：US14817630

申请日：2015-08-04

Applicant: GRÜNENTHAL GMBH

Inventor： Ingo Konetzki ,  Florian Jakob ,  Tobias Craan ,  Christian Hesslinger ,  Paul Ratcliffe ,  Jason J. Shiers

IPC: A61K31/519 ,  C07D495/04 ,  C07D409/04 ,  C07D417/04 ,  C07D239/70

CPC classification number: C07D409/04 ,  C07D239/70 ,  C07D417/04 ,  C07D495/04

Abstract: The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.

公开(公告)号：US09315490B2

公开(公告)日：2016-04-19

申请号：US14800180

申请日：2015-07-15

Applicant: Grünenthal GmbH

Inventor： Ingo Konetzki ,  Tobias Craan ,  Florian Jakob ,  Antonio Nardi ,  Christian Hesslinger ,  Andre Welbers

IPC: A61K31/506 ,  C07D403/04 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D413/14 ,  C07D491/107 ,  C07D471/10 ,  C07D417/14 ,  C07D487/04 ,  C07D498/08

CPC classification number: C07D403/04 ,  A61K31/506 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107 ,  C07D493/10 ,  C07D498/08

Abstract: The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.

Abstract translation: 本发明涉及通式（I）的新型取代的稠合嘧啶化合物，其中化学基团，取代基和指数如说明书中所定义，以及它们作为药物的用途，特别是作为用于治疗病症和疾病的药物 可以通过PDE4酶的抑制来治疗。

公开(公告)号：US20210179592A1

公开(公告)日：2021-06-17

申请号：US17188743

申请日：2021-03-01

Applicant: Grünenthal GmbH

Inventor： Sven Kuehnert ,  Rene Michael Koenigs ,  Achim Kless ,  Anita Wegert ,  Paul Ratcliffe ,  Ruth Jostock ,  Thomas Koch ,  Klaus Linz ,  Wolfgang Schroeder ,  Klaus Schiene ,  Ingo Konetzki

IPC: C07D405/06 ,  C07D235/02 ,  C07D401/06 ,  C07D403/06

Abstract: The invention relates to 3-((hetero-)aryl)-alkyl-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

公开(公告)号：US10807988B2

公开(公告)日：2020-10-20

申请号：US16450331

申请日：2019-06-24

Applicant: Grünenthal GmbH

Inventor： Sven Kuehnert ,  Rene Koenigs ,  Achim Kless ,  Anita Wegert ,  Ingo Konetzki ,  Paul Ratcliffe ,  Ruth Jostock ,  Thomas Koch ,  Klaus Linz ,  Wolfgang Schroeder

IPC: C07D487/04 ,  C07D409/04 ,  C07D413/02 ,  C07D401/02 ,  C07D405/02 ,  C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D413/14 ,  C07D403/14 ,  C07D405/06 ,  C07D409/14 ,  C07D401/04 ,  C07D235/02 ,  C07D403/04

Abstract: The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

公开(公告)号：US10738015B2

公开(公告)日：2020-08-11

申请号：US16554847

申请日：2019-08-29

Applicant: GRÜNENTHAL GMBH

Inventor： Paul Ratcliffe ,  Ingo Konetzki ,  Nikolay Sitnikov ,  Thomas Koch ,  Ruth Jostock

IPC: C07D235/02 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/06 ,  C07D405/14 ,  A61P25/00 ,  C07D401/06 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06

Abstract: The invention relates to 1,3-diaza-spiro-[3.4]-octane derivatives, their preparation and use in medicine, particularly in various neurological disorders, including but not limited to pain, neurodegenerative disorders, neuroinflammatory disorders, neuropsychiatric disorders, substance abuse/dependence.

公开(公告)号：US09688683B2

公开(公告)日：2017-06-27

申请号：US15018968

申请日：2016-02-09

Applicant: GRÜNENTHAL GMBH

Inventor： Florian Jakob ,  Ingo Konetzki ,  Tobias Craan ,  Antonio Nardi ,  Christian Hesslinger

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: Novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.