公开(公告)号：US12110293B2

公开(公告)日：2024-10-08

申请号：US17152930

申请日：2021-01-20

申请人： GRÜNENTHAL GMBH

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

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： 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

申请人： Grünenthal GmbH

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

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： 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：US11547678B2

公开(公告)日：2023-01-10

申请号：US16662392

申请日：2019-10-24

申请人： GRÜNENTHAL GMBH

发明人： Ulrich Reinhold ,  Marc Schiller ,  Eva Wulsten ,  Sabine Karine Katrien Inghelbrecht ,  Roger Carolus Augusta Embrechts ,  Ulrich Feil

IPC分类号： A61K9/08 ,  A61K31/137 ,  A61K47/12 ,  A61K9/00 ,  A61K47/02

摘要： An aqueous pharmaceutical composition containing tapentadol or a physiologically acceptable salt thereof and being adapted for oral administration. The composition has excellent storage stability without relying on the presence of high amounts of preservatives.

公开(公告)号：US10576047B2

公开(公告)日：2020-03-03

申请号：US15999705

申请日：2018-08-20

申请人： Grünenthal GmbH

发明人： Manoj Maniar

IPC分类号： A61K31/165 ,  A61K31/045 ,  A61K31/16 ,  A61K31/167 ,  A61K31/17 ,  A61K31/18 ,  A61K31/24 ,  A61K31/245 ,  A61K31/325 ,  A61K45/06 ,  A61K9/00

摘要： Formulations and methods are provided for the treatment of pain, and neuropathic pain in particular. The formulations are eutectic mixtures of a capsaicinoid and a local anesthetic agent and/or an anti-pruritic agent.

公开(公告)号：US20200038329A1

公开(公告)日：2020-02-06

申请号：US16653186

申请日：2019-10-15

申请人： GRÜNENTHAL GMBH

发明人： Johannes BARTHOLOMÄUS ,  Anja Geissler ,  Ulrike BERTRAM ,  Kornelia GRIESSMANN ,  Fatima BICANE

IPC分类号： A61K9/20 ,  A61K9/28 ,  A61K31/485

摘要： Thermoformed pharmaceutical dosage form having a breaking strength of at least 300 N, comprising an opioid (A), a free physiologically acceptable acid (B) in an amount of from 0.001 to 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form, and a polyalkylene oxide (C) having a weight average molecular weight Mw of at least 200,000 g/mol.

公开(公告)号：US20200009055A1

公开(公告)日：2020-01-09

申请号：US16516946

申请日：2019-07-19

申请人： GRÜNENTHAL GMBH

发明人： KLAUS WENING ,  ANJA GEISSLER ,  JANA DENKER ,  LUTZ BARNSCHEID

IPC分类号： A61K9/16 ,  A61K31/485 ,  A61K31/137 ,  A61K9/20 ,  A61K9/48

摘要： A tamper-resistant pharmaceutical dosage form comprising a multitude of particles which comprise a pharmacologically active compound, a polyalkylene oxide, and a disintegrant; wherein the pharmacologically active compound is dispersed in a matrix comprising the polyalkylene oxide and the disintegrant; wherein the content of the disintegrant is more than 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; wherein the content of the polyalkylene oxide is at least 25 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; and wherein the dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.

公开(公告)号：US20190375738A1

公开(公告)日：2019-12-12

申请号：US16450259

申请日：2019-06-24

申请人： Grünenthal GmbH

发明人： Sven KUEHNERT ,  Rene Michael KOENIGS ,  Achim KLESS ,  Anita WEGERT ,  Paul RATCLIFFE ,  Ruth JOSTOCK ,  Thomas KOCH ,  Klaus LINZ ,  Wolfgang SCHROEDER

IPC分类号： C07D409/06 ,  C07D235/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04

摘要： The invention relates to 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：US10449547B2

公开(公告)日：2019-10-22

申请号：US15164326

申请日：2016-05-25

申请人： GRÜNENTHAL GMBH

发明人： Alessandro Grassano ,  Anna Perachiotti ,  Matteo Minelli ,  Daniele Volpi

IPC分类号： B02C19/00 ,  B02C19/18 ,  A61K9/14 ,  A61K45/06 ,  B02C7/17 ,  B02C17/18 ,  B02C23/08 ,  B29B7/20 ,  B29B9/10 ,  B29B9/12 ,  B29B9/16 ,  B29K71/00

摘要： A method for the preparation of a powdery pharmaceutical composition composed of a pharmaceutical excipient and a pharmaceutical component, among other possible ingredients, wherein the pharmaceutical excipient is a polyalkylene glycol, the method involving grinding a mixture of the pharmaceutical excipient and the pharmaceutical component at a temperature below ambient temperature.

公开(公告)号：US20190269621A1

公开(公告)日：2019-09-05

申请号：US16416532

申请日：2019-05-20

申请人： Grünenthal GmbH

发明人： Sebastian SCHWIER ,  Marcel Haupts ,  Udo Rüttgers ,  Lutz Barnscheid ,  Jana DENKER

IPC分类号： A61K9/20 ,  A61K31/485 ,  A61K31/138 ,  A61K31/137 ,  A61K31/135 ,  A61K9/28

摘要： The invention relates to a tamper-resistant tablet comprising (i) a matrix material in an amount of more than one third of the total weight of the tablet; and (ii) a plurality of particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a polyalkylene oxide; and form a discontinuous phase within the matrix material; and method of using said tablet to treat pain and other conditions.

公开(公告)号：US10265310B2

公开(公告)日：2019-04-23

申请号：US15710249

申请日：2017-09-20

申请人： GRÜNENTHAL GMBH

发明人： Florian Jakob ,  Sonja Nordhoff ,  David Rider ,  Markus Wagener ,  Gregor Bahrenberg ,  Torsten Dunkern

IPC分类号： A61K31/451 ,  A61K31/17 ,  A61K31/085 ,  A61K31/03 ,  A61K31/445 ,  A61K31/45 ,  A61K31/4545 ,  C07D401/12 ,  C07D211/16 ,  C07D211/56 ,  C07D211/94

摘要： The present invention relates to a compound according to general formula (I) which acts as a modulator of FPR2 and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by FPR2.