公开(公告)号：US20180085328A1

公开(公告)日：2018-03-29

申请号：US15712812

申请日：2017-09-22

Applicant: Gruenenthal GmbH

Inventor： Angelika ELLERMANN ,  Ulrich REINHOLD ,  Ulrike BERTRAM

IPC: A61K31/137 ,  A61K9/00 ,  A61K47/12

CPC classification number: A61K31/137 ,  A61K9/0019 ,  A61K9/08 ,  A61K47/12 ,  A61K47/14

Abstract: The invention relates to an an aqueous pharmaceutical composition for parenteral administration comprising Tapentadol or a physiologically acceptable salt thereof; wherein the concentration of Tapentadol is greater than 8.00 mg/mL, based on the weight of Tapentadol free base and based on the total volume of the composition; wherein the composition comprises a buffer system; and wherein the pH value of the composition is within the range of from greater than 3.0 to less than 6.7. The invention also relates to a kit comprising the composition according to the invention in a packaging. The pharmaceutical composition according to the invention is particularly useful for treating pain, especially acute pain, preferably in adult patients.

公开(公告)号：US20180008576A1

公开(公告)日：2018-01-11

申请号：US15545553

申请日：2016-01-22

Applicant: Gruenenthal GmbH

Inventor： Elke KLEIDEITER ,  Annette CHRISTOPH ,  Rene FUSSEN ,  Joachim OSSIG ,  Ramesh BOINPALLY

IPC: A61K31/407 ,  A61K9/00

CPC classification number: A61K31/407 ,  A61K9/0053

Abstract: The invention relates to Cebranopadol or a physiologically acceptable salt thereof for use in the treatment or the prevention of pain and/or opioid drug dependence in a subject with impaired hepatic and/or renal function.

公开(公告)号：US09862719B2

公开(公告)日：2018-01-09

申请号：US14804847

申请日：2015-07-21

Applicant: Gruenenthal GmbH

Inventor： Claudia Hinze ,  Otto Aulenbacher ,  Bernd Sundermann ,  Stefan Oberboersch ,  Elmar Friderichs ,  Werner Englberger ,  Babette-Yvonne Koegel ,  Klaus Linz ,  Hans Schick ,  Helmut Sonnenschein ,  Birgitta Henkel ,  Valerie Sarah Rose ,  Michael Jonathan Lipkin

IPC: C07D209/58 ,  C07D471/10 ,  C07C59/265 ,  C07C59/255 ,  C07C309/06 ,  C07C309/04 ,  C07D491/107 ,  C07D491/10 ,  C07D493/10 ,  C07D495/10

CPC classification number: C07D471/10 ,  C07C59/255 ,  C07C59/265 ,  C07C309/04 ,  C07C309/06 ,  C07D491/10 ,  C07D491/107 ,  C07D493/10 ,  C07D495/10

Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.

公开(公告)号：US09850198B2

公开(公告)日：2017-12-26

申请号：US15157216

申请日：2016-05-17

Applicant: GRUENENTHAL GMBH

Inventor： Helmut Heinrich Buschmann ,  Joerg Holenz

IPC: C07C213/08 ,  C07C213/02 ,  C07C231/12 ,  C07C253/30 ,  C07C231/10

CPC classification number: C07C213/08 ,  C07B2200/07 ,  C07C213/02 ,  C07C231/10 ,  C07C231/12 ,  C07C253/30 ,  C07C235/34 ,  C07C215/54 ,  C07C217/62 ,  C07C255/37

Abstract: A process for the preparation of substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds which has advantages over conventional processes with respect to higher conversions and yields, flexibility, a shorter overall route, environmentally acceptable conditions, influence of stereoselectivity such as diastereoselectivity in a targeted manner and at least partial suppression of the formation of undesired side-products and/or undesired stereoisomers, in particular undesired diastereomers.

公开(公告)号：US20170333369A1

公开(公告)日：2017-11-23

申请号：US15674407

申请日：2017-08-10

Applicant: Gruenenthal GmbH

Inventor： Klaus SCHIENE ,  Petra BLOMS-FUNKE

IPC: A61K31/137 ,  A61K31/136 ,  A61K31/13 ,  A61K31/135 ,  A61K45/06 ,  A61K31/192

Abstract: A pharmaceutical combination comprising as components (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and (b) at least one NMDA-antagonist, a pharmaceutical formulation and a dosage form comprising such a combination, and a method of treating pain, e.g. inflammatory pain or neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, with component (a) being administered either before or after component (b), and with components (a) or (b) being administered to the mammal either via the same pathway of administration or via different pathways of administration.

公开(公告)号：US20170216226A1

公开(公告)日：2017-08-03

申请号：US15486543

申请日：2017-04-13

Applicant: Gruenenthal GmbH

Inventor： Klaus SCHIENE ,  Petra BLOMS-FUNKE ,  Thomas CHRISTOPH ,  Wolfgang SCHROEDER

IPC: A61K31/137 ,  A61K9/20 ,  A61K9/00

CPC classification number: A61K31/137 ,  A61K9/0053 ,  A61K9/20 ,  A61K31/135

Abstract: A method of treating irritable bowel syndrome in a patient in need thereof by administering to said patient a pharmaceutically effective amount of tapentadol.

公开(公告)号：US20170216212A1

公开(公告)日：2017-08-03

申请号：US15489046

申请日：2017-04-17

Applicant: GRUENENTHAL GMBH

Inventor： RAMESH SESHA

IPC: A61K9/24 ,  A61K31/137 ,  A61K31/135 ,  A61K31/197 ,  A61K31/192

CPC classification number: A61K9/209 ,  A61K9/284 ,  A61K9/2866 ,  A61K31/135 ,  A61K31/137 ,  A61K31/192 ,  A61K31/195 ,  A61K31/197 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention provides a method of treating pain and pain related conditions by administering to a patient in need thereof, a therapeutically effective amount of a slow release Tapentadol Hydrochloride and therapeutically effective amount of a second analgesic, wherein the second analgesic is gamma-aminobutyric acid (GABA) analogue. The present invention further provides a pharmaceutical composition comprising a therapeutically effective amount of a slow release Tapentadol Hydrochloride and a therapeutically effective amount of a second analgesic, wherein the second analgesic is gamma-aminobutyric acid (GABA) analogue.

公开(公告)号：US20170197949A1

公开(公告)日：2017-07-13

申请号：US15405627

申请日：2017-01-13

Applicant: Gruenenthal GmbH

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

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

CPC classification number: C07D409/06 ,  C07D235/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04

Abstract: 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：US20160346229A1

公开(公告)日：2016-12-01

申请号：US15232841

申请日：2016-08-10

Applicant: Gruenenthal GmbH

Inventor： Ulrich REINHOLD ,  Marc SCHILLER ,  Eva WULSTEN ,  Sabine Karine Katrien INGHELBRECHT ,  Roger Carolus Augusta EMBRECHTS ,  Ulrich FEIL

IPC: A61K31/137 ,  A61K9/06 ,  A61K47/06 ,  A61K47/10 ,  A61K9/00 ,  A61K47/14

CPC classification number: A61K31/137 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/107 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  Y02A50/473 ,  Y02A50/481

Abstract: A semisolid aqueous pharmaceutical composition containing tapentadol or a physiologically acceptable salt thereof.

Abstract translation: 含有他喷他多或其生理上可接受的盐的半固体含水药物组合物。

公开(公告)号：US09388119B2

公开(公告)日：2016-07-12

申请号：US13972253

申请日：2013-08-21

Applicant: Gruenenthal GmbH

Inventor： Helmut Heinrich Buschmann ,  Joerg Holenz

IPC: C07C213/02 ,  C07C213/08 ,  C07C231/12 ,  C07C253/30

CPC classification number: C07C213/08 ,  C07B2200/07 ,  C07C213/02 ,  C07C231/10 ,  C07C231/12 ,  C07C253/30 ,  C07C235/34 ,  C07C215/54 ,  C07C217/62 ,  C07C255/37

Abstract: A process for the preparation of substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds which has advantages over conventional processes with respect to higher conversions and yields, flexibility, a shorter overall route, environmentally acceptable conditions, influence of stereoselectivity such as diastereoselectivity in a targeted manner and at least partial suppression of the formation of undesired side-products and/or undesired stereoisomers, in particular undesired diastereomers.

Abstract translation: 取代的3-（1-氨基-2-甲基戊烷-3-基）苯基化合物的制备方法，相对于较高的转化率和产率，柔韧性，较短的总体路线，环境可接受的条件，影响，具有优于常规方法的优点 的立体选择性，例如以目标方式的非对映选择性，并且至少部分抑制不期望的副产物和/或不期望的立体异构体的形成，特别是不期望的非对映异构体。