公开(公告)号：US09346816B2

公开(公告)日：2016-05-24

申请号：US14072324

申请日：2013-11-05

Applicant: Stephan-Georg Mueller ,  Christopher John Brown ,  Alexander Heifetz ,  Bernd Nosse ,  Juergen Prestle ,  Natacha Prevost ,  Klaus Rudolf ,  Stefan Scheuerer ,  Marcus Schindler ,  Dirk Stenkamp ,  Leo Thomas ,  Heather Tye

Inventor： Stephan-Georg Mueller ,  Christopher John Brown ,  Alexander Heifetz ,  Bernd Nosse ,  Juergen Prestle ,  Natacha Prevost ,  Klaus Rudolf ,  Stefan Scheuerer ,  Marcus Schindler ,  Dirk Stenkamp ,  Leo Thomas ,  Heather Tye

IPC: A61K31/55 ,  C07D487/14

CPC classification number: C07D487/14

Abstract: The present invention relates to compounds defined by formula I wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.

Abstract translation: 本发明涉及由式I定义的化合物，其中基团X，Y，W和R 1至R 4如权利要求1所定义，具有有价值的药理学活性。 特别地，这些化合物是5-HT 2C受体的激动剂，因此适用于治疗和预防可被受体抑制影响的疾病，如代谢和CNS相关疾病。

公开(公告)号：US08952014B2

公开(公告)日：2015-02-10

申请号：US13140607

申请日：2009-12-17

Applicant: Dirk Gottschling ,  Henri Doods ,  Annekatrin Heimann ,  Stephan Georg Mueller ,  Klaus Rudolf ,  Gerhard Schaenzle ,  Dirk Stenkamp

Inventor： Dirk Gottschling ,  Henri Doods ,  Annekatrin Heimann ,  Stephan Georg Mueller ,  Klaus Rudolf ,  Gerhard Schaenzle ,  Dirk Stenkamp

IPC: A01N43/54 ,  C07D239/42 ,  C07D401/04

CPC classification number: C07D413/14 ,  C07D401/14 ,  C07D471/04 ,  C07D498/20

Abstract: The present invention relates to the new compounds of general formula I wherein A, U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers thereof, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.

Abstract translation: 本发明涉及通式I的新化合物，其中A，U，V，X，Y，R 1，R 2和R 3如下文所定义，互变异构体，其异构体，非对映体，对映异构体，水合物， 其混合物和盐以及盐，特别是其生理上可接受的盐与无机或有机酸或碱的水合物，含有这些化合物的药物，其用途和制备方法。

公开(公告)号：US08951999B2

公开(公告)日：2015-02-10

申请号：US12908172

申请日：2010-10-20

Applicant: Henning Priepke ,  Henri Doods ,  Raimund Kuelzer ,  Roland Pfau ,  Dirk Stenkamp ,  Robert Roenn ,  Benjamin Pelcman

Inventor： Henning Priepke ,  Henri Doods ,  Raimund Kuelzer ,  Roland Pfau ,  Dirk Stenkamp ,  Robert Roenn ,  Benjamin Pelcman

IPC: A61K31/445 ,  C07D211/32 ,  C07C311/14 ,  C07D213/82 ,  C07C237/42 ,  C07C237/44 ,  C07C255/23 ,  C07C255/60 ,  C07D205/04 ,  C07D207/10 ,  C07D207/22 ,  C07D207/34 ,  C07D209/08 ,  C07D211/14 ,  C07D211/16 ,  C07D211/18 ,  C07D211/38 ,  C07D213/40 ,  C07D213/75 ,  C07D213/81 ,  C07D215/42 ,  C07D237/30 ,  C07D277/46 ,  C07D277/56 ,  C07D277/60 ,  C07D277/82 ,  C07D295/15 ,  C07D295/155 ,  C07D307/20 ,  C07D307/24 ,  C07D309/12 ,  C07D309/14 ,  C07D333/38 ,  C07D335/02 ,  C07D417/04

CPC classification number: C07D213/82 ,  C07C237/42 ,  C07C237/44 ,  C07C255/23 ,  C07C255/60 ,  C07C311/14 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/10 ,  C07D207/22 ,  C07D207/34 ,  C07D209/08 ,  C07D211/14 ,  C07D211/16 ,  C07D211/18 ,  C07D211/38 ,  C07D213/40 ,  C07D213/75 ,  C07D213/81 ,  C07D215/42 ,  C07D237/30 ,  C07D277/46 ,  C07D277/56 ,  C07D277/60 ,  C07D277/82 ,  C07D295/15 ,  C07D295/155 ,  C07D307/20 ,  C07D307/24 ,  C07D309/12 ,  C07D309/14 ,  C07D333/38 ,  C07D335/02 ,  C07D417/04

Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.

Abstract translation: 本发明涉及式I化合物，它们作为微粒体前列腺素E2合成酶-1（mPGES-1）的抑制剂的用途，含有它们的药物组合物及其用作治疗和/或预防炎性疾病和相关病症的药物 如炎性/伤害性疼痛。 A，M，R 1，R 2，R 7，R a，R b，Q 3，Q 4，Q 6，Z 2，Z 4，Z 5，Z 6和W具有说明书中给出的含义。

公开(公告)号：US20120149676A1

公开(公告)日：2012-06-14

申请号：US13314561

申请日：2011-12-08

Applicant: Henning PRIEPKE ,  Henri DOODS ,  Alexander HEIM-RIETHER ,  Raimund KUELZER ,  Roland PFAU ,  Klaus RUDOLF ,  Dirk STENKAMP

Inventor： Henning PRIEPKE ,  Henri DOODS ,  Alexander HEIM-RIETHER ,  Raimund KUELZER ,  Roland PFAU ,  Klaus RUDOLF ,  Dirk STENKAMP

IPC: A61K31/4184 ,  C07D235/30 ,  C07D403/10 ,  C07D413/10 ,  C07D409/12 ,  C07D413/14 ,  C07D401/14 ,  C07D487/04 ,  C07D513/04 ,  C07D409/14 ,  C07D491/107 ,  C07D491/048 ,  C07D417/10 ,  C07D498/08 ,  C07D403/12 ,  C07D417/14 ,  C07D403/14 ,  A61K31/454 ,  A61K31/429 ,  A61K31/5377 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/4725 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/438 ,  A61K31/541 ,  A61K31/5386 ,  A61K31/4196 ,  A61K31/497 ,  A61P29/00 ,  C07D487/10 ,  C07D491/08 ,  A61K31/439 ,  C07D401/10

CPC classification number: C07D235/30 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D487/04 ,  C07D487/08 ,  C07D491/04 ,  C07D491/08 ,  C07D491/10 ,  C07D498/08 ,  C07D513/04

Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.

Abstract translation: 本发明涉及式I化合物，其用作微粒体前列腺素E2合酶-1（mPGES-1）的抑制剂，含有它们的药物组合物及其作为用于治疗和/或预防炎性疾病及相关病症的药物的用途。 A，L，M，W，R 1，R 2，R 3，R 4，R 6，R 7，R 9，R a，R b具有说明书中给出的含义。

公开(公告)号：US20110172218A1

公开(公告)日：2011-07-14

申请号：US12682853

申请日：2008-10-16

Applicant: Dirk Gottschling ,  Georg Dahmann ,  Henri Doods ,  Annekatrin Heimann ,  Klaus Rudolf ,  Stephan Georg Mueller ,  Gerhard Schaenzle ,  Dirk Stenkamp

Inventor： Dirk Gottschling ,  Georg Dahmann ,  Henri Doods ,  Annekatrin Heimann ,  Klaus Rudolf ,  Stephan Georg Mueller ,  Gerhard Schaenzle ,  Dirk Stenkamp

IPC: A61K31/537 ,  C07D471/10 ,  A61K31/527 ,  C07D403/14 ,  A61K31/506 ,  C07D498/10 ,  C07D498/20 ,  A61P25/06

CPC classification number: C07D471/10 ,  C07D471/04 ,  C07D498/10 ,  C07D498/20

Abstract: The present invention relates to novel CGRP antagonists of the general formula (I) in which U, V, X, Y, R1, R2, R3 are defined as described below, the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof, and the hydrates of the salts, particularly the physiologically compatible salts thereof having inorganic or organic acids or bases, pharmaceuticals comprising said compounds, the use thereof, and the method for the production thereof.

Abstract translation: 本发明涉及通式（I）的新型CGRP拮抗剂，其中U，V，X，Y，R 1，R 2，R 3如下所定义，互变异构体，异构体，非对映异构体，对映异构体，水合物，混合物和盐 以及具有无机或有机酸或碱的盐，特别是其生理上相容的盐的水合物，包含所述化合物的药物，其用途及其制备方法。

公开(公告)号：US20100324028A1

公开(公告)日：2010-12-23

申请号：US12743013

申请日：2008-11-21

Applicant: Dirk Gottschling ,  Georg Dahmann ,  Henri Doods ,  Annekatrin Heimann ,  Stephan Georg Mueller ,  Klaus Rudolf ,  Gerhard Georg Schaenzle ,  Dirk Stenkamp

Inventor： Dirk Gottschling ,  Georg Dahmann ,  Henri Doods ,  Annekatrin Heimann ,  Stephan Georg Mueller ,  Klaus Rudolf ,  Gerhard Georg Schaenzle ,  Dirk Stenkamp

IPC: A61K31/551 ,  A61K31/437 ,  C07D401/14 ,  C07D471/04 ,  A61P25/00 ,  A61P25/06

CPC classification number: C07D401/14 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.

Abstract translation: 本发明涉及通式Ia和Ib的新CGRP拮抗剂，其中R 1，R 2，R 3，R 4和R 5如下所定义，互变异构体，异构体，非对映异构体，对映异构体，水合物，混合物和 其盐以及盐的水合物，特别是其与无机或有机酸或碱的生理上可接受的盐，含有这些化合物的药物组合物，其用途及其制备方法。

公开(公告)号：US20100249114A1

公开(公告)日：2010-09-30

申请号：US12712801

申请日：2010-02-25

Applicant: Stephan Georg MUELLER ,  Klaus RUDOLF ,  Philipp LUSTENBERGER ,  Dirk STENKAMP ,  Alexander DREYER ,  Kirsten ARNDT ,  Henri DOODS ,  Gerhard SCHAENZLE ,  Marco SANTAGOSTINO ,  Fabio PALEARI

Inventor： Stephan Georg MUELLER ,  Klaus RUDOLF ,  Philipp LUSTENBERGER ,  Dirk STENKAMP ,  Alexander DREYER ,  Kirsten ARNDT ,  Henri DOODS ,  Gerhard SCHAENZLE ,  Marco SANTAGOSTINO ,  Fabio PALEARI

IPC: A61K31/551 ,  C07D243/04 ,  C07D401/14 ,  A61K31/497 ,  A61K31/445 ,  C07D471/04 ,  A61K31/4745 ,  C07D239/72 ,  A61K31/517 ,  C07D495/14 ,  A61K31/519 ,  A61P29/00

CPC classification number: C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D495/04

Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.

公开(公告)号：US20100152171A1

公开(公告)日：2010-06-17

申请号：US12706840

申请日：2010-02-17

Applicant: Klaus RUDOLF ,  Stephan Georg MUELLER ,  Dirk STENKAMP ,  Philipp LUSTENBERGER ,  Alexander DREYER ,  Eckhart BAUER ,  Marcus SCHINDLER ,  Kirsten ARNDT ,  Henri DOODS

Inventor： Klaus RUDOLF ,  Stephan Georg MUELLER ,  Dirk STENKAMP ,  Philipp LUSTENBERGER ,  Alexander DREYER ,  Eckhart BAUER ,  Marcus SCHINDLER ,  Kirsten ARNDT ,  Henri DOODS

IPC: A61K31/5513 ,  C07D243/24 ,  C07D239/72 ,  C07D401/14 ,  A61K31/517 ,  A61K31/497 ,  A61P11/06 ,  A61P9/10 ,  A61P3/10 ,  A61P25/06

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D471/08 ,  C07D495/04

Abstract: CGRP antagonists of the formula of which the following are exemplary: (1) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amide, (2) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amide.

Abstract translation: 具有下式的CGRP拮抗剂是示例性的：（1）4-（2-氧代-1,2,4,5-四氢-1,3-苯并二氮杂-3-基） - 哌啶-1-甲酸 - {（R）-1-（3,4-二乙基 - 苄基）-2- [4-（1-甲基 - 哌啶-4-基） - 哌嗪-1-基] -2-氧代 - 乙基} - 酰胺， （2）4-（2-氧代-1,2,4,5-四氢-1,3-苯并二氮杂-3-基） - 哌啶-1-羧酸 - {（R）-1-（3,4- 乙基 - 苄基）-2- [4-（4-甲基 - 哌嗪-1-基） - 哌啶-1-基] -2-氧代 - 乙基} - 酰胺。

公开(公告)号：US07592373B2

公开(公告)日：2009-09-22

申请号：US11021897

申请日：2004-12-23

Applicant: Thorsten Lehmann-Lintz ,  Ralf R. H. Lotz ,  Philipp Lustenberger ,  Stephan Georg Mueller ,  Gerald Juergen Roth ,  Klaus Rudolf ,  Marcus Schindler ,  Dirk Stenkamp ,  Leo Thomas

Inventor： Thorsten Lehmann-Lintz ,  Ralf R. H. Lotz ,  Philipp Lustenberger ,  Stephan Georg Mueller ,  Gerald Juergen Roth ,  Klaus Rudolf ,  Marcus Schindler ,  Dirk Stenkamp ,  Leo Thomas

IPC: C07C233/29 ,  C07C235/24 ,  C07D209/18 ,  A61K31/40 ,  A61K31/167 ,  A61K31/404 ,  A61P3/04

CPC classification number: C07C255/24 ,  C07C233/29 ,  C07C233/44 ,  C07C233/55 ,  C07C237/20 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/12 ,  C07D211/14 ,  C07D211/22 ,  C07D211/44 ,  C07D211/58 ,  C07D213/36 ,  C07D213/56 ,  C07D221/20 ,  C07D231/12 ,  C07D233/60 ,  C07D249/08 ,  C07D263/56 ,  C07D295/155 ,  C07D309/14 ,  C07D401/12

Abstract: Compounds of formula (I) wherein A, B, b, W, X, Y, Z, R1, R2, and R3 have the meanings given in claim 1, pharmaceutical compositions these compounds, and methods of preventing or treating metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes using these compounds.

Abstract translation: 其中A，B，b，W，X，Y，Z，R 1，R 2和R 3具有权利要求1中给出的含义的式（I）化合物，这些化合物的药物组合物，以及预防或治疗代谢紊乱和/ 或进食障碍，特别是肥胖症，食欲过剩，厌食症，食欲过盛和糖尿病。

公开(公告)号：US07528129B2

公开(公告)日：2009-05-05

申请号：US11277177

申请日：2006-03-22

Applicant: Stephan Georg Mueller ,  Klaus Rudolf ,  Philipp Lustenberger ,  Dirk Stenkamp ,  Marco Santagostino ,  Fabio Paleari ,  Gerhard Schaenzle ,  Kirsten Arndt ,  Henri Doods

Inventor： Stephan Georg Mueller ,  Klaus Rudolf ,  Philipp Lustenberger ,  Dirk Stenkamp ,  Marco Santagostino ,  Fabio Paleari ,  Gerhard Schaenzle ,  Kirsten Arndt ,  Henri Doods

IPC: C07D401/14 ,  C07D413/04 ,  A61K31/551 ,  A61P25/06

CPC classification number: C07D405/12 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, mixtures and salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I in which one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.