公开(公告)号：US20140099333A1

公开(公告)日：2014-04-10

申请号：US14048425

申请日：2013-10-08

Applicant: Lothar SCHWINK ,  Martin BOSSART ,  Heiner GLOMBIK ,  Matthias GOSSEL ,  Dieter KADEREIT ,  Thomas KLABUNDE ,  Thomas MAIER ,  Siegfried STENGELIN

Inventor： Lothar SCHWINK ,  Martin BOSSART ,  Heiner GLOMBIK ,  Matthias GOSSEL ,  Dieter KADEREIT ,  Thomas KLABUNDE ,  Thomas MAIER ,  Siegfried STENGELIN

IPC: A61K31/497 ,  A61K31/4015 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/4545 ,  C07D405/14 ,  C07D401/14 ,  A61K31/444 ,  C07D413/14 ,  A61K45/06 ,  C07D207/12 ,  C07D417/14

CPC classification number: A61K31/497 ,  A61K31/4015 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K45/06 ,  A61K48/00 ,  C07D207/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及吡咯烷酮衍生物。 吡咯烷酮衍生物是GPR119调节剂，可用于预防和/或治疗糖尿病，肥胖，血脂异常和相关疾病。 本发明还涉及吡咯烷酮衍生物作为药物中的活性成分的用途，以及包含它们的药物组合物。

公开(公告)号：US08648038B2

公开(公告)日：2014-02-11

申请号：US13176503

申请日：2011-07-05

Applicant: Elisabeth Defossa ,  Stefanie Keil ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Andreas Herling ,  Guido Haschke ,  Thomas Klabunde

Inventor： Elisabeth Defossa ,  Stefanie Keil ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Andreas Herling ,  Guido Haschke ,  Thomas Klabunde

IPC: A61K38/28 ,  A61P5/50

CPC classification number: C07C235/24 ,  C07C255/44

Abstract: The invention relates to substituted (2-aryloxyacetylamino)phenylpropionic acid derivatives, and to the physiologically acceptable salts thereof.The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.

Abstract translation: 本发明涉及取代的（2-芳氧基乙酰基氨基）苯基丙酸衍生物及其生理上可接受的盐。 本发明涉及其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和A各自如上所定义的式Ⅰ化合物及其生理上相容的盐。 该化合物适用于例如治疗糖尿病。

公开(公告)号：US08530413B2

公开(公告)日：2013-09-10

申请号：US13154946

申请日：2011-06-07

Applicant: Stefanie Keil ,  Elisabeth Defossa ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Andreas Herling ,  Guido Haschke ,  Thomas Klabunde

Inventor： Stefanie Keil ,  Elisabeth Defossa ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Andreas Herling ,  Guido Haschke ,  Thomas Klabunde

IPC: A61K38/28 ,  A61P5/50

CPC classification number: C07D209/34 ,  C07D215/227 ,  C07D265/36 ,  C07D277/68 ,  C07D498/04

Abstract: Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicamentsThe invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, and to physiologically compatible salts thereof.The invention relates to compounds of the formula I in which R1, R2, R3, R4, R10, X, n, B1, B2, B3 and B4 are each defined as specified, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.

Abstract translation: 具有氧代基的杂环取代的甲氧基苯基衍生物，其制备方法及其作为药物的用途本发明涉及具有氧代基的杂环取代的甲氧基苯基衍生物及其生理上相容的盐。 本发明涉及其中R 1，R 2，R 3，R 4，R 10，X，n，B 1，B 2，B 3和B 4各自如上所定义的式Ⅰ化合物及其生理上相容的盐。 该化合物适用于例如治疗糖尿病。

公开(公告)号：US08518875B2

公开(公告)日：2013-08-27

申请号：US12724519

申请日：2010-03-16

Applicant: Elisabeth Defossa ,  Thomas Klabunde ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Guido Haschke ,  Andreas Herling ,  Johanna Kuhlmann-Gottke ,  Stefan Bartoschek

Inventor： Elisabeth Defossa ,  Thomas Klabunde ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Guido Haschke ,  Andreas Herling ,  Johanna Kuhlmann-Gottke ,  Stefan Bartoschek

IPC: A61K38/00 ,  C07C255/00

CPC classification number: C07C237/04 ,  C07C235/80

Abstract: The invention relates to (carboxylalkylenephenyl)phenyloxamides and their physiologically tolerated salts, and their use as a medicament.

Abstract translation: 本发明涉及（羧基亚烷基苯基）苯氧基酰胺及其生理上耐受的盐，以及它们作为药物的用途。

公开(公告)号：US20110053947A1

公开(公告)日：2011-03-03

申请号：US12852216

申请日：2010-08-06

Applicant: Gerhard JAEHNE ,  Siegfried STENGELIN ,  Matthias GOSSEL ,  Thomas KLABUNDE ,  Irvin WINKLER

Inventor： Gerhard JAEHNE ,  Siegfried STENGELIN ,  Matthias GOSSEL ,  Thomas KLABUNDE ,  Irvin WINKLER

IPC: A61K31/4985 ,  C07D241/04 ,  C07D233/40 ,  C07D401/04 ,  A61K31/497 ,  A61K31/4166 ,  A61K31/4439 ,  A61P25/18 ,  A61P25/28

CPC classification number: C07D233/74

Abstract: The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.

Abstract translation: 本发明涉及式（I）化合物，其中基团R和R'，A，D，E，G，L，p和R 1至R 10具有所述含义及其生理上相容的盐。 所述化合物例如适合作为抗肥胖药物。

公开(公告)号：US20090149486A1

公开(公告)日：2009-06-11

申请号：US12267925

申请日：2008-11-10

Applicant: Elisabeth Defossa ,  Jochen Goerlitzer ,  Thomas Klabunde ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Guido Haschke ,  Andreas Herling ,  Stefan Bartoschek

Inventor： Elisabeth Defossa ,  Jochen Goerlitzer ,  Thomas Klabunde ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Guido Haschke ,  Andreas Herling ,  Stefan Bartoschek

IPC: A61K31/505 ,  C07D239/34 ,  A61P3/10

CPC classification number: C07D239/34

Abstract: This invention relates to a compound of formula I, wherein R1, R2, m, n, V, W, X and Y are as defined herein, or a physiologically tolerated salt thereof, its pharmaceutical composition and use for lowering blood glucose, treating diabetes, or increasing insulin release.

Abstract translation: 本发明涉及式Ⅰ化合物，其中R1，R2，m，n，V，W，X和Y如本文所定义，或其生理耐受盐，其药物组合物和降血糖用途，治疗糖尿病 ，或增加胰岛素释放。

公开(公告)号：US20090149477A1

公开(公告)日：2009-06-11

申请号：US12267912

申请日：2008-11-10

Applicant: Elisabeth Defossa ,  Jochen Goerlitzer ,  Thomas Klabunde ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Guido Haschke ,  Andreas Herling ,  Stefan Bartoschek

Inventor： Elisabeth Defossa ,  Jochen Goerlitzer ,  Thomas Klabunde ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Guido Haschke ,  Andreas Herling ,  Stefan Bartoschek

IPC: A61K31/505 ,  C07D239/28 ,  A61P3/10

CPC classification number: C07D239/26

Abstract: This invention relates to a compound of formula I, wherein R1, R2, m, n and X are as defined herein, or a physiologically tolerated salt thereof, its pharmaceutical composition and use for lowering blood glucose, treating diabetes, or increasing insulin release.

Abstract translation: 本发明涉及式I化合物，其中R 1，R 2，m，n和X如本文所定义，或其生理学上耐受的盐，其药物组合物和用于降低血糖，治疗糖尿病或增加胰岛素释放的用途。

公开(公告)号：US20080221113A1

公开(公告)日：2008-09-11

申请号：US12124503

申请日：2008-05-21

Applicant: Stefanie Flohr ,  Siegfried Stengelin ,  Matthias Gossel ,  Thomas Klabunde ,  Pavel Safar ,  James Spoonamore ,  Martin Smrcina

Inventor： Stefanie Flohr ,  Siegfried Stengelin ,  Matthias Gossel ,  Thomas Klabunde ,  Pavel Safar ,  James Spoonamore ,  Martin Smrcina

IPC: A61K31/4985 ,  C07D471/04 ,  A61P3/04 ,  A61P3/10 ,  A61P15/00

CPC classification number: C07D487/04

Abstract: Substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicamentsThe invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.

Abstract translation: 取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，其制备方法及其作为药物的用途本发明涉及取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物， 生理上耐受的盐及其生理功能衍生物。 描述了其中基团具有所述含义的式I化合物及其生理上耐受的盐及其制备方法。 该化合物适合于例如厌食剂。

公开(公告)号：US07390814B2

公开(公告)日：2008-06-24

申请号：US10778554

申请日：2004-02-13

Applicant: Stefanie Flohr ,  Siegfried Stengelin ,  Matthias Gossel ,  Thomas Klabunde ,  Pavel Safar ,  James Spoonamore ,  Martin Smrcina

Inventor： Stefanie Flohr ,  Siegfried Stengelin ,  Matthias Gossel ,  Thomas Klabunde ,  Pavel Safar ,  James Spoonamore ,  Martin Smrcina

IPC: A01N43/90 ,  C07D239/70

CPC classification number: C07D487/04

Abstract: Substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicamentsThe invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof.Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.

Abstract translation: 取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物，其制备方法及其作为药物的用途本发明涉及取代的六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物， 生理上耐受的盐及其生理功能衍生物。 描述了其中基团具有所述含义的式I化合物及其生理上耐受的盐及其制备方法。 该化合物适合于例如厌食剂。

公开(公告)号：US20070197539A1

公开(公告)日：2007-08-23

申请号：US11677067

申请日：2007-02-21

Applicant: Petra Lennig ,  Siegfried Stengelin ,  Thomas Klabunde ,  Matthias Gossel ,  Pavel Safar ,  Martin Smrcina ,  James Spoonamore ,  Gregory Merriman ,  Joseph Klein ,  Brian Whiteley ,  Carolina Lanter ,  Kenneth Bordeau ,  Zhaoxia Yang

Inventor： Petra Lennig ,  Siegfried Stengelin ,  Thomas Klabunde ,  Matthias Gossel ,  Pavel Safar ,  Martin Smrcina ,  James Spoonamore ,  Gregory Merriman ,  Joseph Klein ,  Brian Whiteley ,  Carolina Lanter ,  Kenneth Bordeau ,  Zhaoxia Yang

IPC: A61K31/519 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives substituted with amino acids, and to the physiologically tolerated salts thereof, processes for their preparation and their use as medicaments

Abstract translation: 本发明涉及被氨基酸取代的取代六氢吡嗪并[1,2-a]嘧啶-4,7-二酮衍生物及其生理学上可耐受的盐，其制备方法及其用作药物