公开(公告)号：US20090186881A1

公开(公告)日：2009-07-23

申请号：US12363175

申请日：2009-01-30

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: A61K31/551 ,  C07D243/04 ,  C07D401/14 ,  A61K31/496 ,  C07D239/72 ,  A61K31/517 ,  C07D265/04 ,  A61K31/537 ,  A61P3/00 ,  A61P9/00 ,  A61P29/00

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.

Abstract translation: 本发明涉及通式I的CGRP拮抗剂，其中R 1，R 2，R 3，R 4和X如权利要求1中所定义，互变异构体，异构体，非对映异构体，对映体，水合物，混合物和盐以及 盐，特别是其与无机或有机酸或碱的生理上可接受的盐的水合物，以及其中一个或多个氢原子被氘代替的通式I的那些化合物，含有这些化合物的药物组合物的用途，其用途 及其制备方法。

公开(公告)号：US07538115B2

公开(公告)日：2009-05-26

申请号：US11138868

申请日：2005-05-26

Applicant: Rudolf Hurnaus ,  Klaus Rudolf ,  Stephan Georg Mueller ,  Dirk Stenkamp ,  Philipp Lustenberger ,  Alexander Dreyer ,  Kai Gerlach ,  Marcus Schindler ,  Kirsten Arndt ,  Eckhart Bauer

Inventor： Rudolf Hurnaus ,  Klaus Rudolf ,  Stephan Georg Mueller ,  Dirk Stenkamp ,  Philipp Lustenberger ,  Alexander Dreyer ,  Kai Gerlach ,  Marcus Schindler ,  Kirsten Arndt ,  Eckhart Bauer

IPC: A61K31/517 ,  C07D239/72

CPC classification number: C07D471/04 ,  C07D401/14

Abstract: The present invention relates to substituted piperidines of general formula wherein R, R2 to R5, A, X, Z and n are defined as in claim 1, the tautomers, diastereomers, enantiomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.

Abstract translation: 本发明涉及通式的取代哌啶，其中R，R 2至R 5，A，X，Z和n如权利要求1中所定义，互变异构体，非对映体，对映体，其混合物和盐，特别是其生理上可接受的盐与 具有有价值的药理学性质，特别是CGRP拮抗性的无机或有机酸或碱，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：US20090111797A1

公开(公告)日：2009-04-30

申请号：US12186005

申请日：2008-08-05

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

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

IPC: C07D401/14 ,  A61K31/551 ,  A61P25/00

CPC classification number: C07D401/14

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：US20090069282A1

公开(公告)日：2009-03-12

申请号：US12121251

申请日：2008-05-15

Applicant: Dirk Stenkamp ,  Stephan Georg Mueller ,  Gerald Juergen Roth ,  Thorsten Lehmann-Lintz ,  Klaus Rudolf ,  Philipp Lustenberger ,  Kirsten Arndt ,  Ralf R. H. Lotz ,  Martin Lenter

Inventor： Dirk Stenkamp ,  Stephan Georg Mueller ,  Gerald Juergen Roth ,  Thorsten Lehmann-Lintz ,  Klaus Rudolf ,  Philipp Lustenberger ,  Kirsten Arndt ,  Ralf R. H. Lotz ,  Martin Lenter

IPC: A61K31/397 ,  C07D213/02 ,  A61K31/44 ,  C07D239/24 ,  A61K31/505 ,  A61K31/496 ,  A61K31/47 ,  A61K31/5377 ,  A61K31/50 ,  A61P13/02 ,  A61P3/04 ,  A61K31/55 ,  C07D223/14 ,  C07D215/00 ,  A61K31/551 ,  C07D243/08 ,  C07D237/06 ,  C07D295/00 ,  C07D217/00 ,  C07D401/02 ,  A61K31/4439 ,  C07D221/00 ,  A61K31/4545

CPC classification number: C07D471/10 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/42 ,  C07D213/48 ,  C07D213/53 ,  C07D213/55 ,  C07D213/56 ,  C07D213/57 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/85 ,  C07D215/12 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D333/16 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/06 ,  C07D453/02 ,  C07D471/04 ,  C07D487/08 ,  C07D487/10 ,  C07D495/04

Abstract: The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

Abstract translation: 本发明涉及通式I的炔化合物，其中基团和残基A，B，W，X，Y，Z，R 1和R 2具有权利要求1中给出的含义。本发明还涉及含有至少一种 炔根据本发明。 鉴于其MCH受体拮抗活性，根据本发明的药物组合物适用于治疗代谢紊乱和/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：US07479488B2

公开(公告)日：2009-01-20

申请号：US11093834

申请日：2005-03-29

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

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 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.

Abstract translation: 本发明涉及通式C的CGRP拮抗剂，其中A，X，D，E，G，M，Q和R 1至R 3如权利要求1中所定义，互变异构体，非对映体，对映异构体，其水合物， 其盐及其盐，其盐，特别是其生理上可接受的盐与无机或有机酸的水合物，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：US20070072847A1

公开(公告)日：2007-03-29

申请号：US11533096

申请日：2006-09-19

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

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

IPC: A61K31/5513 ,  A61K31/517 ,  A61K31/454 ,  C07D403/04

CPC classification number: C07D243/10 ,  C07D249/12 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3 and R4 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 thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract translation: 本发明涉及通式I的CGRP拮抗剂，其中R 1，R 2，R 3和R 4， / SUP>如权利要求1中所定义，互变异构体，异构体，非对映异构体，对映异构体，其水合物，其混合物及其盐及其盐的水合物，特别是其生理上可接受的盐与无机或 有机酸或碱，以及其中一个或多个氢原子被氘代替的通式I化合物，其含有这些化合物的药物组合物，其用途和制备方法。

公开(公告)号：US20060142274A1

公开(公告)日：2006-06-29

申请号：US11301446

申请日：2005-12-13

Applicant: Klaus Rudolf ,  Henri Doods ,  Stephan Mueller ,  Annette Zamponi ,  Philipp Lustenberger ,  Kirsten Arndt ,  Gerhard Schaenzle ,  Dirk Stenkamp ,  Rolf-Stefan Brickl

Inventor： Klaus Rudolf ,  Henri Doods ,  Stephan Mueller ,  Annette Zamponi ,  Philipp Lustenberger ,  Kirsten Arndt ,  Gerhard Schaenzle ,  Dirk Stenkamp ,  Rolf-Stefan Brickl

IPC: A61K31/5513 ,  A61K31/517

CPC classification number: A61K31/517

Abstract: The invention relates to the use of selected CGRP antagonists, the physiologically acceptable salts thereof or the hydrates of the hydrates of the salts thereof for combating menopausal hot flushes.

Abstract translation: 本发明涉及选择的CGRP拮抗剂，其生理上可接受的盐或其盐的水合物的水合物用于对抗绝经性潮热的用途。

公开(公告)号：US20050250763A1

公开(公告)日：2005-11-10

申请号：US11107052

申请日：2005-04-15

Applicant: Stephan Mueller ,  Klaus Rudolf ,  Philipp Lustenberger ,  Dirk Stenkamp ,  Kirsten Arndt ,  Henri Doods ,  Gerhard Schaenzle

Inventor： Stephan Mueller ,  Klaus Rudolf ,  Philipp Lustenberger ,  Dirk Stenkamp ,  Kirsten Arndt ,  Henri Doods ,  Gerhard Schaenzle

IPC: A61K31/4184 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/519 ,  A61K31/551 ,  C07D235/26 ,  C07D249/12 ,  C07D401/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08 ,  C07D495/04 ,  C07D519/00 ,  A61K31/5513 ,  A61K31/4545 ,  A61K31/4745

CPC classification number: C07D235/26 ,  C07D249/12 ,  C07D401/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08 ,  C07D495/04

Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X and R1 to R3 are defined as in claim 1, the tautomers, 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：US20050234054A1

公开(公告)日：2005-10-20

申请号：US11107189

申请日：2005-04-15

Applicant: Stephan Mueller ,  Klaus Rudolf ,  Philipp Lustenberger ,  Dirk Stenkamp ,  Kirsten Arndt ,  Henri Doods ,  Gerhard Schaenzle

Inventor： Stephan Mueller ,  Klaus Rudolf ,  Philipp Lustenberger ,  Dirk Stenkamp ,  Kirsten Arndt ,  Henri Doods ,  Gerhard Schaenzle

IPC: A61K31/4747 ,  A61K31/519 ,  A61K31/542

CPC classification number: C07D471/10 ,  C07D498/10 ,  C07D519/00

Abstract: The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, 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.

Abstract translation: 本发明涉及通式C的CGRP拮抗剂，其中A和R 1至R 3定义如权利要求1，互变异构体，非对映异构体，对映异构体， 其水合物，其混合物及其盐以及盐，特别是其生理上可接受的盐与无机或有机酸的水合物，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：US06903337B2

公开(公告)日：2005-06-07

申请号：US10185729

申请日：2002-07-01

Applicant: Oliver Kienzle ,  Dirk Stenkamp ,  Michael Steigerwald ,  Rainer Knippelmeyer ,  Max Haider ,  Heiko Müller ,  Stephan Uhlemann

Inventor： Oliver Kienzle ,  Dirk Stenkamp ,  Michael Steigerwald ,  Rainer Knippelmeyer ,  Max Haider ,  Heiko Müller ,  Stephan Uhlemann

IPC: G03F7/20 ,  H01J31/00 ,  H01J37/09 ,  H01J37/12 ,  H01J37/147 ,  H01J37/244 ,  H01J37/28 ,  H01J37/285

CPC classification number: H01J37/28 ,  H01J2237/082 ,  H01J2237/2446

Abstract: An examining system for imaging an object positionable in an object plane, includes an illumination device for supplying energy to a delimited field of the object such that charged particles emerge from locations of the field, the field being displaceable in the plane of the object, a first deflector for providing a variable deflection field for guiding charged particles emerging from locations of a selectable region of the object through a fixed, predetermined beam cross-section, and a position-sensitive detector disposed in the beam path such that the charged particles, after having passed through the first deflector, impinge on the position-sensitive detector, wherein particles emerging from different locations of the region are imaged on different locations of the position-sensitive detector which are allocated to the locations of emergence.

Abstract translation: 一种用于对物体平面中定位的物体进行成像的检查系统，包括用于向物体的界定场提供能量的照明装置，使得带电粒子从场的位置出现，该场可在物体的平面中移动， 第一偏转器，用于提供可变偏转场，用于引导通过固定的预定光束横截面从物体的可选择区域的位置出射的带电粒子，以及设置在光束路径中的位置敏感检测器，使得带电粒子在 已经穿过第一偏转器，撞击位置敏感检测器，其中从该区域的不同位置出现的颗粒被成像在位置敏感检测器的分配到出现位置的不同位置上。