公开(公告)号：US08853412B2

公开(公告)日：2014-10-07

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: C07D401/00 ,  A61K31/44 ,  A61K31/497 ,  C07D401/12 ,  A61K31/4545 ,  C07D413/14 ,  A61K31/4439 ,  C07D401/14 ,  C07D407/14 ,  C07D417/14 ,  C07D207/12 ,  C07D405/14 ,  A61K31/444 ,  A61K31/4015

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：US20120329765A1

公开(公告)日：2012-12-27

申请号：US13357423

申请日：2012-01-24

Applicant: Peter Boderke ,  Rainer Pooth ,  Juergen Sandow ,  Matthias Gossel ,  Karl-Heinz Nietsch ,  Gerhard Sattler ,  Gerhard Vogel

Inventor： Peter Boderke ,  Rainer Pooth ,  Juergen Sandow ,  Matthias Gossel ,  Karl-Heinz Nietsch ,  Gerhard Sattler ,  Gerhard Vogel

IPC: A61K31/56 ,  A61P35/00

CPC classification number: A61K9/0019 ,  A61K9/127 ,  A61K31/409 ,  A61K31/685 ,  A61K45/06 ,  A61K47/28 ,  A61K2300/00

Abstract: Aqueous phospholipid systems comprising at least one phospholipid, at least one bile acid and water are suitable for producing medicaments for the treatment of adipose tissue disorders and lead to regression of the pathologically proliferated adipose tissue.

Abstract translation: 包含至少一种磷脂，至少一种胆汁酸和水的磷脂体系适用于制备用于治疗脂肪组织病症的药物并导致病理性增殖的脂肪组织消退。

公开(公告)号：US08299104B2

公开(公告)日：2012-10-30

申请号：US11946286

申请日：2007-11-28

Applicant: Lothar Schwink ,  Siegfried Stengelin ,  Thomas Boehme ,  Matthias Gossel ,  Gerhard Hessler ,  Petra Stahl

Inventor： Lothar Schwink ,  Siegfried Stengelin ,  Thomas Boehme ,  Matthias Gossel ,  Gerhard Hessler ,  Petra Stahl

IPC: A61K31/4025 ,  C07D413/10

CPC classification number: A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K45/06 ,  A61K2300/00

Abstract: The invention relates to substituted aryl-substituted heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to process for their preparation and to their use as medicaments.Compounds of the formula I in which the radicals have the stated meanings, the N-oxides thereof, and the physiologically tolerated salts thereof, and process for the preparation thereof are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.

Abstract translation: 本发明涉及取代的芳基取代的杂环及其生理上耐受的盐和生理功能衍生物，用于其制备及其作为药物的用途。 描述了其中基团具有所述含义的式I化合物，其N-氧化物及其生理上耐受的盐及其制备方法。 所述化合物例如引起哺乳动物的体重减轻，并且适合于例如预防和治疗肥胖症和糖尿病。

公开(公告)号：US20110046185A1

公开(公告)日：2011-02-24

申请号：US12852188

申请日：2010-08-06

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

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

IPC: A61K31/4439 ,  C07D233/72 ,  A61K31/4166 ,  A61P3/10 ,  A61P3/04 ,  A61P25/32 ,  A61P25/34 ,  A61P25/18 ,  A61P25/28 ,  C07D401/04 ,  C07D409/04 ,  C07D417/10 ,  A61K31/428

CPC classification number: C07D233/72 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

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：US20110046105A1

公开(公告)日：2011-02-24

申请号：US12852233

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: A61K31/4178 ,  C07D401/12 ,  A61K31/497 ,  A61P3/04 ,  A61P3/10 ,  A61P25/28 ,  A61P25/18 ,  A61P25/32 ,  A61P25/34 ,  A61K31/4184 ,  A61K31/501 ,  C07D413/14 ,  A61K31/5355 ,  A61K31/454

CPC classification number: C07D233/72 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

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：US07223788B2

公开(公告)日：2007-05-29

申请号：US10779853

申请日：2004-02-17

Applicant: Lothar Schwink ,  Siegfried Stengelin ,  Matthias Gossel ,  Thomas Boehme ,  Gerhard Hessler ,  Petra Stahl ,  Dirk Gretzke

Inventor： Lothar Schwink ,  Siegfried Stengelin ,  Matthias Gossel ,  Thomas Boehme ,  Gerhard Hessler ,  Petra Stahl ,  Dirk Gretzke

IPC: A61K31/40 ,  A61K31/4025 ,  C07D207/14 ,  C07D211/56

CPC classification number: C07D207/26 ,  C07D205/04 ,  C07D207/14 ,  C07D207/16 ,  C07D207/34 ,  C07D211/58 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof.Compounds of the formula I in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.

Abstract translation: 本发明涉及取代的N-芳基杂环及其生理上耐受的盐和生理功能衍生物。 描述了其中基团具有所述含义的式I化合物，其N-氧化物及其生理学上可接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：US07015208B2

公开(公告)日：2006-03-21

申请号：US10981045

申请日：2004-11-04

Applicant: Gerhard Jaehne ,  Volker Krone ,  Martin Bickel ,  Matthias Gossel

Inventor： Gerhard Jaehne ,  Volker Krone ,  Martin Bickel ,  Matthias Gossel

IPC: A01N65/00

CPC classification number: C07C323/17 ,  C07C317/20 ,  C07C2602/08

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of embodiments of the invention may include compounds of formula I in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for use as anorectics.

公开(公告)号：US06919380B2

公开(公告)日：2005-07-19

申请号：US10692725

申请日：2003-10-27

Applicant: Gerhard Jaehne ,  Volker Krone ,  Martin Bickel ,  Matthias Gossel

Inventor： Gerhard Jaehne ,  Volker Krone ,  Martin Bickel ,  Matthias Gossel

IPC: A61K31/10 ,  A61K31/137 ,  A61K31/216 ,  A61K31/222 ,  A61K31/365 ,  A61K31/4035 ,  A61K38/22 ,  A61P3/04 ,  C07C317/20 ,  C07C323/17 ,  C07D233/54 ,  A01N41/10 ,  C07C309/00 ,  C07C315/00 ,  C07C321/00

CPC classification number: A61K31/365 ,  A61K31/10 ,  A61K38/2264

Abstract: Derivatives of C2-substituted indan-1-ol compounds of formula I: its physiologically acceptable salts, and its physiologically functional derivatives for the prophylaxis or treatment of obesity are disclosed herein. Compositions comprising the same, methods for preparing the instant compounds, and methods for reducing weight in mammals and for the prophylaxis or treatment of obesity are also described.

Abstract translation: 式I的C2取代茚满-1-醇化合物的衍生物：其生理上可接受的盐及其用于预防或治疗肥胖症的生理功能衍生物。 还描述了包含其的组合物，制备本发明化合物的方法，以及用于减轻哺乳动物体重和预防或治疗肥胖症的方法。

公开(公告)号：US20050143347A1

公开(公告)日：2005-06-30

申请号：US11011333

申请日：2004-12-14

Applicant: Peter Boderke ,  Matthias Gossel ,  Walter Kamm ,  Karl-Heinz Nietsch ,  Rainer Pooth ,  Juergen Sandow ,  Joerg Hager ,  Gerhard Sattler

Inventor： Peter Boderke ,  Matthias Gossel ,  Walter Kamm ,  Karl-Heinz Nietsch ,  Rainer Pooth ,  Juergen Sandow ,  Joerg Hager ,  Gerhard Sattler

IPC: A61K31/195 ,  A61K31/355 ,  A61K31/525 ,  A61K31/56 ,  A61K31/685

CPC classification number: A61K31/525 ,  A61K31/195 ,  A61K31/355 ,  A61K31/56 ,  A61K31/685 ,  A61K2300/00

Abstract: Aqueous preparations comprising at least one phospholipid or at least one bile acid and a component assisting degradation of fat such as riboflavin and water are suitable for producing medicaments for removing subcutaneous accumulations of fat and lead to regression of diet-resistant fat pads.

Abstract translation: 包含至少一种磷脂或至少一种胆汁酸的水性制剂和辅助降解脂肪如核黄素和水的成分适用于制备用于去除皮下脂肪积聚并导致耐饮食脂肪垫消退的药物。

公开(公告)号：US20050113595A1

公开(公告)日：2005-05-26

申请号：US10981045

申请日：2004-11-04

Applicant: Gerhard Jaehne ,  Volker Krone ,  Martin Bickel ,  Matthias Gossel

Inventor： Gerhard Jaehne ,  Volker Krone ,  Martin Bickel ,  Matthias Gossel

IPC: C07D239/38 ,  A61K31/10 ,  A61K31/18 ,  A61K31/423 ,  A61K31/4402 ,  A61K31/505 ,  A61P3/04 ,  A61P3/10 ,  C07C315/02 ,  C07C315/04 ,  C07C317/20 ,  C07C317/48 ,  C07C317/50 ,  C07C319/14 ,  C07C323/17 ,  C07C323/58 ,  C07C323/59 ,  C07D213/71 ,  C07D263/58 ,  C07C323/39

CPC classification number: C07C323/17 ,  C07C317/20 ,  C07C2602/08

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of embodiments of the invention may include compounds of formula I in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for use as anorectics.