公开(公告)号：US08536332B2

公开(公告)日：2013-09-17

申请号：US13455187

申请日：2012-04-25

Applicant: Matthias Gerlach ,  Irene Seipelt ,  Eckhard Guenther ,  Emmanuel Polymeropoulos ,  Tilmann Schuster ,  Eckhard Claus

Inventor： Matthias Gerlach ,  Irene Seipelt ,  Eckhard Guenther ,  Emmanuel Polymeropoulos ,  Tilmann Schuster ,  Eckhard Claus

IPC: C07D471/00

CPC classification number: C07D471/04

Abstract: Method of modulating ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and/or SAPK signal transduction pathway with a pyrido[2,3-b]pyrazine of formula (Ia).

Abstract translation: 用式（Ia）的吡啶并[2,3-b]吡嗪调节ras-Raf-Mek-Erk信号转导途径，PI3K-Akt信号转导途径和/或SAPK信号转导途径的方法。

公开(公告)号：US08461178B2

公开(公告)日：2013-06-11

申请号：US12953680

申请日：2010-11-24

Applicant: Tilmann Schuster ,  Matthias Gerlach ,  Irene Seipelt ,  Emmanuel Polymeropoulos ,  Gilbert Mueller ,  Eckhard Guenther ,  Pascal Marchand ,  Julien Defaux

Inventor： Tilmann Schuster ,  Matthias Gerlach ,  Irene Seipelt ,  Emmanuel Polymeropoulos ,  Gilbert Mueller ,  Eckhard Guenther ,  Pascal Marchand ,  Julien Defaux

IPC: A61K31/44 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumors and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.

Abstract translation: 本发明涉及萘啶类型的激酶调节剂以及其作为用于调节错误定向的细胞信号转导过程的药物的制备和用途，特别是用于影响酪氨酸和丝氨酸/苏氨酸激酶的功能以及治疗恶性或 良性肿瘤和基于病理性细胞增殖的其它病症，例如再狭窄，牛皮癣，动脉硬化和肝硬化。

公开(公告)号：US08394801B2

公开(公告)日：2013-03-12

申请号：US12731243

申请日：2010-03-25

Applicant: Matthias Gerlach ,  Irene Seipelt ,  Eckhard Guenther ,  Tilmann Schuster ,  Emmanuel Polymeropoulos ,  Michael Czech ,  Eckhard Claus

Inventor： Matthias Gerlach ,  Irene Seipelt ,  Eckhard Guenther ,  Tilmann Schuster ,  Emmanuel Polymeropoulos ,  Michael Czech ,  Eckhard Claus

IPC: A61K31/495

CPC classification number: C07D241/44 ,  C07D401/12 ,  C07D403/04 ,  C07D409/12 ,  C07D413/12

Abstract: The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders.

Abstract translation: 本发明提供了通式I的喹喔啉，其用作优选用于治疗肿瘤病症的药物，特别是在对其它活性化合物的耐药性和转移性癌症的情况下。 可能的应用不限于肿瘤病症。

公开(公告)号：US20120277219A1

公开(公告)日：2012-11-01

申请号：US13542101

申请日：2012-07-05

Applicant: Matthias Gerlach ,  Irene Seipelt ,  Eckhard Guenther ,  Emmanuel Polymeropoulos ,  Tilmann Schuster ,  Eckhard Claus

Inventor： Matthias Gerlach ,  Irene Seipelt ,  Eckhard Guenther ,  Emmanuel Polymeropoulos ,  Tilmann Schuster ,  Eckhard Claus

IPC: A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P35/00 ,  A61P29/00 ,  A61P19/02 ,  A61P31/18 ,  A61P25/28 ,  A61P17/06 ,  A61P37/02 ,  A61P35/02 ,  A61P3/10 ,  A61P37/06 ,  A61P11/06 ,  A61P1/00 ,  A61P9/10 ,  A61P9/00 ,  A61P13/12 ,  A61P7/02 ,  A61P3/04 ,  A61P9/12 ,  A61K31/538

CPC classification number: C07D471/04

Abstract: The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.

公开(公告)号：US20110150831A1

公开(公告)日：2011-06-23

申请号：US12953680

申请日：2010-11-24

Applicant: Tilmann SCHUSTER ,  Matthias GERLACH ,  Irene SEIPELT ,  Emmanuel POLYMEROPOULOS ,  Gilbert MUELLER ,  Eckhard GUENTHER ,  Pascal MARCHAND ,  Julien DEFAUX

Inventor： Tilmann SCHUSTER ,  Matthias GERLACH ,  Irene SEIPELT ,  Emmanuel POLYMEROPOULOS ,  Gilbert MUELLER ,  Eckhard GUENTHER ,  Pascal MARCHAND ,  Julien DEFAUX

IPC: A61K31/4375 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/444 ,  A61K38/46 ,  A61K38/14 ,  A61K33/24 ,  A61K31/675 ,  A61K31/7068 ,  A61K31/704 ,  A61K31/7048 ,  A61K38/21 ,  A61K39/395 ,  A61K38/12 ,  A61K31/655 ,  A61K31/7076 ,  A61P9/10 ,  A61P1/16 ,  A61P17/06 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumours and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.

Abstract translation: 本发明涉及萘啶类型的激酶调节剂以及其作为用于调节错误定向的细胞信号转导过程的药物的制备和用途，特别是用于影响酪氨酸和丝氨酸/苏氨酸激酶的功能以及治疗恶性或 良性肿瘤和基于病理性细胞增殖的其它病症，例如再狭窄，牛皮癣，动脉硬化和肝硬化。

公开(公告)号：US20080312301A1

公开(公告)日：2008-12-18

申请号：US11916613

申请日：2006-06-06

Applicant: Beatrix Merla ,  Matthias Gerlach ,  Corinna Sundermann ,  Utz-Peter Jagusch ,  Hagen-Heinrich Hennies ,  Stefan Oberborsch ,  Michael Haurand ,  Ruth Jostock ,  Melanie Reich

Inventor： Beatrix Merla ,  Matthias Gerlach ,  Corinna Sundermann ,  Utz-Peter Jagusch ,  Hagen-Heinrich Hennies ,  Stefan Oberborsch ,  Michael Haurand ,  Ruth Jostock ,  Melanie Reich

IPC: A61K31/423 ,  A61P25/00 ,  A61P1/00 ,  C07D261/20 ,  C07D413/12

CPC classification number: C07D413/12 ,  C07D261/20 ,  C07D417/12

Abstract: The invention relates to substituted N-benzo[d]isoxazol-3-yl-amine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are defined as in patent claim 1. The invention also relates to the use of said compounds for producing medicaments.

Abstract translation: 本发明涉及式（I）的取代的N-苯并[d]异恶唑-3-基 - 胺衍生物，其中R 1，R 2，R 3，R 4和R 5如专利权利要求1中所定义。本发明还涉及 所述化合物用于生产药物。

公开(公告)号：US07135568B2

公开(公告)日：2006-11-14

申请号：US10660794

申请日：2003-09-12

Applicant: Matthias Gerlach ,  Corrinna Sundermann ,  Utz-Peter Jagusch ,  Bernd Sundermann ,  Martin Fuhr ,  Adriaan P. Ijzerman ,  Miriam Dissen-De Groote

Inventor： Matthias Gerlach ,  Corrinna Sundermann ,  Utz-Peter Jagusch ,  Bernd Sundermann ,  Martin Fuhr ,  Adriaan P. Ijzerman ,  Miriam Dissen-De Groote

IPC: C07D471/04 ,  C07D513/04 ,  A61K31/519 ,  A61P25/04 ,  A61P25/28

CPC classification number: C07D487/04 ,  C07D513/04

Abstract: Substituted pyrazolopyrimidines and thiazolopyrimidines, specifically, compounds corresponding to the structure (I A), (I B) or (II) processes for their preparation, substance libraries containing them, pharmaceutical formulations containing these compounds, the use of these compounds for the production of medicaments for the treatment and/or prophylaxis of pain and related treatment methods are provided.

Abstract translation: 取代的吡唑并嘧啶和噻唑并嘧啶，具体地，对应于结构（IA），（IB）或（II）的制备方法，含有它们的物质文库，含有这些化合物的药物制剂，使用这些化合物用于制备药物 提供了治疗和/或预防疼痛和相关治疗方法。

公开(公告)号：US20060014818A1

公开(公告)日：2006-01-19

申请号：US11172142

申请日：2005-06-30

Applicant: Klaus Paulini ,  Matthias Gerlach ,  Eckhard Günther ,  Emmanuel Polymeropoulos ,  Silke Baasner ,  Peter Schmidt ,  Ronald Kühne ,  Arvid Soderhall

Inventor： Klaus Paulini ,  Matthias Gerlach ,  Eckhard Günther ,  Emmanuel Polymeropoulos ,  Silke Baasner ,  Peter Schmidt ,  Ronald Kühne ,  Arvid Soderhall

IPC: A61K31/403 ,  C07D209/82

CPC classification number: C07D209/88 ,  C07D209/82

Abstract: The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.

Abstract translation: 本发明提供具有改进性质的新型四氢咔唑衍生物，其可用作GPCR的抑制剂。 这导致使用新化合物治疗其严重程度取决于GPCR的病理生化作用的病理状况的可能性。 本发明的化合物特别是通过拮抗LHRH受体的抑制作用。 本发明进一步提供了包含一种或多种新化合物作为活性成分的药物。 药物特别适用于哺乳动物，特别是人的口服剂型。