公开(公告)号：WO2021028346A1

公开(公告)日：2021-02-18

申请号：PCT/EP2020/072275

申请日：2020-08-07

Applicant: FORSCHUNGSVERBUND BERLIN E.V.

Inventor： KRAUSE, Gerd ,  MARCINKOWSKI, Patrick

IPC: C07K14/72 ,  G01N33/78 ,  G16C20/50

Abstract: The invention relates to one or more regions of the thyroid-stimulating hormone receptor (TSHR), identified herein as a TSHR ligand binding domain. Such a domain is considered a binding pocket for chemical compounds, for example S37 or derivatives thereof, that exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists. Embodiments of the invention relate to proteins and corresponding coding nucleic acids for the proteins of the invention, for example the TSHR ligand binding domain and related proteins. The invention relates to methods of screening for or testing compounds that interact, bind and/or modify the TSHR ligand binding domain of the invention.

公开(公告)号：WO2017186793A1

公开(公告)日：2017-11-02

申请号：PCT/EP2017/059930

申请日：2017-04-26

Applicant: FORSCHUNGSVERBUND BERLIN E.V.

Inventor： KRAUSE, Gerd ,  HOYER, Inna ,  SPECKER, Edgar ,  FURKERT, Jens ,  MARCINKOWSKI, Patrick ,  VON KRIES, Jens-Peter ,  NEUENSCHWANDER, Martin ,  NAZARE, Marc

IPC: A61K31/429 ,  A61K31/495 ,  A61P5/14 ,  A61P35/00

Abstract: The invention relates to chemical compounds that are useful in the treatment of a subject afflicted by a thyroid disease, in particular to compounds that exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and their use in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.

Abstract translation: 本发明涉及用于治疗患有甲状腺疾病的受试者的化合物，特别是涉及表现出作为促甲状腺激素受体（TSHR）拮抗剂的活性的化合物及其在 甲状腺功能亢进症，格雷夫斯病，格雷夫斯眼病和甲状腺癌的治疗。

公开(公告)号：WO2012163925A1

公开(公告)日：2012-12-06

申请号：PCT/EP2012/060066

申请日：2012-05-29

Applicant: MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN ,  FORSCHUNGSVERBUND BERLIN E.V. ,  SCHÄFER, Gesa ,  KRAUSE, Gerd ,  ROSENTHAL, Walter ,  MILIC, Jelena ,  RADEMANN, Jörg ,  SCHILLINGER, Christian ,  KLUSSMANN, Enno

Inventor： SCHÄFER, Gesa ,  KRAUSE, Gerd ,  ROSENTHAL, Walter ,  MILIC, Jelena ,  RADEMANN, Jörg ,  SCHILLINGER, Christian ,  KLUSSMANN, Enno

IPC: A61K31/435 ,  C07D213/81 ,  C07D213/84 ,  C07D401/14 ,  A61P9/04

CPC classification number: C07D401/04 ,  C07D213/81 ,  C07D213/84 ,  C07D401/14

Abstract: The instant invention relates to compounds characterized by a general formula I and use thereof as a medicament, preferably for prevention or treatment of heart failure (I).

Abstract translation: 本发明涉及以通式I为特征的化合物及其作为药物的用途，优选用于预防或治疗心力衰竭（I）。

公开(公告)号：EP3448381A1

公开(公告)日：2019-03-06

申请号：EP17720091.2

申请日：2017-04-26

Applicant: Forschungsverbund Berlin E.V.

Inventor： KRAUSE, Gerd ,  HOYER, Inna ,  SPECKER, Edgar ,  FURKERT, Jens ,  MARCINKOWSKI, Patrick ,  VON KRIES, Jens-Peter ,  NEUENSCHWANDER, Martin ,  NAZARE, Marc

IPC: A61K31/429 ,  A61K31/495 ,  A61P5/14 ,  A61P35/00

公开(公告)号：EP2358684B8

公开(公告)日：2014-10-22

申请号：EP08876356.0

申请日：2008-10-20

Applicant: The Government of the United States of America as represented by the Secretary of the Department of Health and Human Services ,  Forschungsverbund Berlin e.V.

Inventor： GERSHENGORN, Marvin, C. ,  NEUMANN, Susanne ,  RAAKA, Bruce, M. ,  THOMAS, Craig, J. ,  INGLESE, James ,  SOUTHALL, Noel, T. ,  TITUS, Steven ,  ZHENG, Wei ,  HUANG, Wenwei ,  KRAUSE, Gerd ,  KLEINAU, Gunnar

IPC: C07D401/06 ,  C07D405/06 ,  C07D239/91 ,  C07D487/04

CPC classification number: C07D405/06 ,  A61K31/517 ,  A61K49/0004 ,  A61K51/00 ,  C07D239/91 ,  C07D401/06 ,  C07D405/14 ,  C07D487/04

公开(公告)号：EP2018384A2

公开(公告)日：2009-01-28

申请号：EP07777162.4

申请日：2007-05-17

Applicant: The Government of the United States of America as represented by the Secretary of the Department of Health and Human Services ,  Forschungsverbund Berlin E.V.

Inventor： GERSHENGORN, Marvin, C. ,  NEUMANN, Susanne ,  THOMAS, Craig ,  JAESCHKE, Holger ,  MOORE, Susanna ,  KRAUSE, Gerd ,  RAAKA, Bruce ,  PASCHKE, Ralf ,  KLEINAU, Gunnar

IPC: C07D495/04 ,  A61K31/519 ,  A61P5/06 ,  A61P5/08

CPC classification number: A61K31/519 ,  C07D495/04

Abstract: Disclosed herein are small molecule modulators hormone receptors, including agonists and antagonists of luteinizing hormone/choriogonadotropin, follicle stimulating hormone and thyroid stimulating hormone receptors. Exemplary disclosed compounds include those of the formula wherein X is -S(O)nR5; n is 0, 1 or 2; Y is -OR6 or -NR7R8 R1 and R2 independently are selected from optionally substituted lower aliphatic, alkoxy, aralkyl, halogen, H and -OR5, wherein R5 is selected from lower alkyl, H, aralkyl, acyl, alkoxycarbonyl and aminocarbonyl; R3 and R4 independently are selected from acyl, alkoxycarbonyl, aminocarbonyl, aralkyl, H, lower alkyl and cycloalkyl; R5 is selected from lower alkyl, aralkyl, cycloalkyl and haloalkyl; R6 is selected from H, lower alkyl and aralkyl; R7 and R8 independently are selected from H, lower alkyl, aralkyl and cycloalkyl.