公开(公告)号：US20190015343A1

公开(公告)日：2019-01-17

申请号：US16134059

申请日：2018-09-18

申请人： GRÜNENTHAL GMBH

发明人： Carmen STOMBERG ,  Klaus WENING ,  Marcel HAUPTS

IPC分类号： A61K9/20 ,  A61K9/24 ,  A61K31/135

摘要： The invention relates to a three-dimensionally printed pharmaceutical dosage form comprising a first pharmacologically active ingredient and a second pharmacologically active ingredient; wherein the relative weight ratio of the first pharmacologically active ingredient to the second pharmacologically active ingredient in the pharmaceutical dosage form is within the range of from 10,000:1 to 1:1. The invention also relates to a process for the preparation of such pharmaceutical dosage form by three-dimensional printing, preferably by fused deposition modeling.

公开(公告)号：US20180369237A1

公开(公告)日：2018-12-27

申请号：US16116282

申请日：2018-08-29

申请人： Klaus WENING ,  ANJA GEIßLER ,  JANA DENKER ,  LUTZ BARNSCHEID

发明人： Klaus WENING ,  ANJA GEIßLER ,  JANA DENKER ,  LUTZ BARNSCHEID

IPC分类号： A61K31/485 ,  A61K9/16 ,  A61K9/20 ,  A61K31/137 ,  A61K9/50 ,  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：US20180327392A1

公开(公告)日：2018-11-15

申请号：US15984919

申请日：2018-05-21

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 ,  Klaus SCHIENE ,  Ingo KONETZKI

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

CPC分类号： C07D405/06 ,  C07D235/02 ,  C07D401/06 ,  C07D403/06

摘要： 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：US20180147149A1

公开(公告)日：2018-05-31

申请号：US15878524

申请日：2018-01-24

申请人： GRÜNENTHAL GMBH

发明人： Johannes Bartholomäus ,  Heinrich Kugelmann ,  Elisabeth Arkenau-Maric

IPC分类号： A61K9/20 ,  A61K31/485 ,  A61K9/28 ,  A61K9/00

CPC分类号： A61K9/2031 ,  A61K9/0002 ,  A61K9/0053 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2068 ,  A61K9/2095 ,  A61K9/28 ,  A61K9/2893 ,  A61K31/485

摘要： The present invention relates to an abuse-proofed, oral dosage form with controlled opioid-release for once daily administration, characterised in that it comprises at least one opioid with potential for abuse (A), at least one synthetic or natural polymer (C), optionally delayed-release matrix auxiliary substances, physiologically acceptable auxiliary substances (B), optionally a wax (D) and optionally at least one delayed-release coating, component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.

公开(公告)号：US09926302B2

公开(公告)日：2018-03-27

申请号：US15404758

申请日：2017-01-12

申请人： GRÜNENTHAL GMBH

发明人： Stefan Schunk ,  Melanie Reich ,  Florian Jakob ,  Nils Damann ,  Michael Haurand ,  Achim Kless ,  Marc Rogers ,  Kathy Mackenzie

IPC分类号： C07D405/04 ,  A61K31/435 ,  C07D413/04 ,  C07D309/08 ,  C07D405/12

CPC分类号： C07D413/04 ,  C07D309/08 ,  C07D405/04 ,  C07D405/12

摘要： The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

公开(公告)号：US20180078541A1

公开(公告)日：2018-03-22

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

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

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.

公开(公告)号：US20180044347A1

公开(公告)日：2018-02-15

申请号：US15791508

申请日：2017-10-24

申请人： GRÜNENTHAL GMBH

发明人： Klaus WENING ,  Lutz BARNSCHEID ,  Anja GEISSLER ,  Jana DENKER ,  Dagmar LISCHKE

IPC分类号： C07D489/04

CPC分类号： C07D489/04 ,  A61P25/04 ,  A61P29/00 ,  C07B2200/13 ,  C07D489/02

摘要： Crystalline salts of 4,5 α-epoxy-3-methoxy-17-methylmorphinan-6-one tartrate (1:1) (hydrocodone bitartrate) are disclosed and three polymorphic forms of these salts are reported. The invention further relates to a pharmaceutical composition comprising such a salt and such a salt as a medicament and for the treatment and/or prevention of pain.

公开(公告)号：US09855263B2

公开(公告)日：2018-01-02

申请号：US15169778

申请日：2016-06-01

申请人： GRÜNENTHAL GMBH

发明人： Klaus Wening ,  Anja Geiβler ,  Jana Denker ,  Lutz Barnscheid

IPC分类号： A61K9/50 ,  A61K31/485 ,  A61K9/16 ,  A61K9/20 ,  A61K9/48 ,  A61K31/137

CPC分类号： A61K31/485 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1658 ,  A61K9/1694 ,  A61K9/2077 ,  A61K9/4808 ,  A61K9/50 ,  A61K31/137

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：US20170312271A1

公开(公告)日：2017-11-02

申请号：US15649880

申请日：2017-07-14

申请人： Grünenthal GmbH

发明人： Judy ASHWORTH ,  Elisabeth ARKENAU-MARIC ,  Johannes BARTHOLOMÄUS ,  Heinrich KUGELMANN

IPC分类号： A61K31/485 ,  A61J3/10 ,  A61K9/20 ,  B29C43/02 ,  B29B9/12 ,  B29B9/02 ,  B29B7/00 ,  A61K31/554 ,  A61K31/55 ,  A61J3/00 ,  A61K31/4418 ,  A61K31/277 ,  A61K31/135 ,  A61K9/48 ,  A61K9/28 ,  A61K31/4422 ,  B29C35/02 ,  B29C45/00 ,  B29K105/00 ,  B29L31/00

摘要： The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.

公开(公告)号：US09802947B2

公开(公告)日：2017-10-31

申请号：US14693975

申请日：2015-04-23

申请人： GRÜNENTHAL GMBH

发明人： Antonio Nardi ,  Paul Ratcliffe ,  Tobias Craan ,  Torsten Hertrampf ,  Bernhard Lesch ,  Henning Steinhagen

IPC分类号： C07D491/048

CPC分类号： C07D491/048

摘要： The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors exhibiting a pronounced CatK-inhibition, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.