公开(公告)号：US08975265B2

公开(公告)日：2015-03-10

申请号：US13808430

申请日：2011-07-07

Applicant: Stuart Ince ,  Andrea Hägebarth ,  Oliver Politz ,  Roland Neuhaus ,  Ulf Bömer ,  William Scott

Inventor： Stuart Ince ,  Andrea Hägebarth ,  Oliver Politz ,  Roland Neuhaus ,  Ulf Bömer ,  William Scott

IPC: A01N43/90 ,  A61K31/519 ,  A61K31/437 ,  C07D471/04 ,  C07D487/04 ,  A61K45/06 ,  C07F5/04

CPC classification number: A61K31/437 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07F5/04

Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.

Abstract translation: 作为Pi3K / Akt途径的有效抑制剂的式（I）化合物，其制备方法及其作为药物的用途。

公开(公告)号：US20130190332A1

公开(公告)日：2013-07-25

申请号：US13808430

申请日：2011-07-07

Applicant: Stuart Ince ,  Andrea Hägebarth ,  Oliver Politz ,  Roland Neuhaus ,  Ulf Bömer ,  William Scott

Inventor： Stuart Ince ,  Andrea Hägebarth ,  Oliver Politz ,  Roland Neuhaus ,  Ulf Bömer ,  William Scott

IPC: A61K31/437 ,  A61K45/06 ,  C07D471/04 ,  C07F5/04 ,  C07D487/04 ,  A61K31/519

CPC classification number: A61K31/437 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07F5/04

Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.

Abstract translation: 作为Pi3K / Akt途径的有效抑制剂的式（I）化合物，其制备方法及其作为药物的用途。

公开(公告)号：US20060116380A1

公开(公告)日：2006-06-01

申请号：US11265517

申请日：2005-11-03

Applicant: Rolf Bohlmann ,  Martin Haberey ,  Andreas Huth ,  Stuart Ince ,  Martin Krueger ,  Karl-Heinz Thierauch ,  Holger Hess-Stumpp ,  Andreas Reichel

Inventor： Rolf Bohlmann ,  Martin Haberey ,  Andreas Huth ,  Stuart Ince ,  Martin Krueger ,  Karl-Heinz Thierauch ,  Holger Hess-Stumpp ,  Andreas Reichel

IPC: A61K31/506 ,  A61K31/501 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/444 ,  C07D403/14 ,  C07D401/14

CPC classification number: C07D401/12

Abstract: The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis.

公开(公告)号：US20050054654A1

公开(公告)日：2005-03-10

申请号：US10870491

申请日：2004-06-18

Applicant: Andreas Huth ,  Ludwig Zorn ,  Martin Krueger ,  Stuart Ince ,  Karl Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

Inventor： Andreas Huth ,  Ludwig Zorn ,  Martin Krueger ,  Stuart Ince ,  Karl Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

IPC: C07D213/61 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D43/02 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07D41/02

CPC classification number: C07D213/61 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver; mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.

Abstract translation: 描述了VEGFR-2和VEGFR-3抑制性邻氨基苯酰胺吡啶酰胺，其作为用于治疗由持续血管发生引起的疾病的药物的制备和用途，以及用于制备化合物的中间产物。 根据本发明的化合物可用于或在肿瘤或转移生长的情况下，牛皮癣，卡波西肉瘤，再狭窄，例如支架诱导的再狭窄，子宫内膜异位，克罗恩病，霍奇金病，白血病; 关节炎，如类风湿关节炎，血管瘤，血管纤维瘤; 眼睛疾病如糖尿病性视网膜病变，新生血管性青光眼; 肾脏疾病如肾小球性肾炎，糖尿病肾病，恶性肾硬化，血栓性微血管病综合征，移植排斥反应和肾小球病; 纤维化疾病，如肝硬化; 肾小球膜细胞增生性疾病，动脉硬化，神经组织损伤，以及球囊导管治疗后血管假体中或使用机械装置用于保持血管开放（例如，支架）作为免疫抑制剂的抑制，作为免疫抑制剂 无疤痕愈合，老年角化病和接触性皮炎的支持。 在淋巴管生成的情况下，根据本发明的化合物也可以用作VEGFR-3抑制剂。

公开(公告)号：US08957064B2

公开(公告)日：2015-02-17

申请号：US13201277

申请日：2010-02-02

Applicant: Matthias Vennemann ,  Thomas Bär ,  Thomas Maier ,  Swen Hölder ,  Gerrit Beneke ,  Florian Dehmel ,  Armin Zülch ,  Andreas Strub ,  Stuart Ince ,  Hartmut Rehwinkel ,  Ningshu Liu ,  Ulf Bömer ,  Barbara Beckers

Inventor： Matthias Vennemann ,  Thomas Bär ,  Thomas Maier ,  Swen Hölder ,  Gerrit Beneke ,  Florian Dehmel ,  Armin Zülch ,  Andreas Strub ,  Thomas Beckers ,  Stuart Ince ,  Hartmut Rehwinkel ,  Ningshu Liu ,  Ulf Bömer

IPC: A61K31/495 ,  A61K31/519 ,  A61K31/505 ,  C07D401/12 ,  C07D487/04 ,  A61K45/06 ,  C07D471/04

CPC classification number: A61K31/519 ,  A61K31/495 ,  A61K31/505 ,  A61K45/06 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of formula (I) or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6, R7, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.

Abstract translation: 式（I）化合物或所述化合物的N-氧化物，盐，互变异构体或立体异构体，或所述N-氧化物，互变异构体或立体异构体的盐，其中环B和与其稠合的嘧啶，R4 R5，R6，R7，m和n具有在描述和权利要求中给出的含义，它们是Pi3K / Akt途径的有效抑制剂，其生产方法及其作为药物的用途。

公开(公告)号：US07846928B2

公开(公告)日：2010-12-07

申请号：US11761672

申请日：2007-06-12

Applicant: Ingo Hartung ,  Stuart Ince ,  Georg Kettschau ,  Karl-Heinz Thierauch ,  Hans Briem ,  Ulf Boemer

Inventor： Ingo Hartung ,  Stuart Ince ,  Georg Kettschau ,  Karl-Heinz Thierauch ,  Hans Briem ,  Ulf Boemer

IPC: A61K31/44 ,  A61K31/501 ,  A61K31/535 ,  A61P43/00 ,  C07D401/00 ,  C07D413/00 ,  C07D471/02

CPC classification number: C07D213/85 ,  C07D471/04

Abstract: The invention relates to substituted pyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted pyrazolopyridine compounds, to methods of preparing said substituted pyrazolopyridines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.

Abstract translation: 本发明涉及根据通式（I）的取代吡唑并吡啶：其中A，B，D，E，Ra，R1，R2，R3，R4，R5和q如权利要求中所定义， 包含所述取代的吡唑并吡啶化合物的药物组合物，制备所述取代的吡唑并吡啶的方法，以及其用于制备用于治疗失调的血管生长的疾病的药物组合物或伴有血管生长失调的疾病的用途，其中所述化合物 有效干扰Tie2信号。

公开(公告)号：US20080039455A1

公开(公告)日：2008-02-14

申请号：US11765647

申请日：2007-06-20

Applicant: Stuart Ince ,  Olaf Prien ,  Shoufu Lu ,  Hongyi Yu ,  Manfred Husemann ,  Karina Schuck

Inventor： Stuart Ince ,  Olaf Prien ,  Shoufu Lu ,  Hongyi Yu ,  Manfred Husemann ,  Karina Schuck

IPC: A61K31/519 ,  A61K31/5377 ,  A61P29/00 ,  A61P35/00 ,  A61P9/00 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The invention relates to pyrazolopyrimidines according to the general formula (I): and salts thereof, to pharmaceutical compositions comprising said pyrazolopyrimidines and to a method of preparing said pyrazolopyrimidines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment or prophylaxis of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth

Abstract translation: 本发明涉及根据通式（I）的吡唑并嘧啶及其盐，其包含所述吡唑并嘧啶的药物组合物和制备所述吡唑并嘧啶的方法及其用于制备用于治疗或预防疾病的药物组合物的用途 的血管生长失调或伴随血管生长失调的疾病

公开(公告)号：US09340528B2

公开(公告)日：2016-05-17

申请号：US13393583

申请日：2010-08-24

Applicant: Benjamin Bader ,  Ulf Bömer ,  Stuart Ince ,  Marcus Koppitz ,  Philip Lienau ,  Tobias Marquardt ,  Duy Nguyen ,  Stefan Prechtl ,  Gerhard Siemeister ,  Christof Wegscheid-Gerlach

Inventor： Benjamin Bader ,  Ulf Bömer ,  Stuart Ince ,  Marcus Koppitz ,  Philip Lienau ,  Tobias Marquardt ,  Duy Nguyen ,  Stefan Prechtl ,  Gerhard Siemeister ,  Christof Wegscheid-Gerlach

IPC: A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D487/04

CPC classification number: C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D487/04

Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract translation: 本发明涉及通式（I）的取代氨基喹喔啉化合物，其中（II），R2，R3，R4，R6，R7，n和m如说明书和权利要求书中所给出，涉及制备所述化合物的方法 涉及包含所述化合物的药物组合物和组合，用于制备用于治疗或预防疾病的药物组合物的所述化合物的用途，以及可用于制备所述化合物的中间体化合物。

公开(公告)号：US09206185B2

公开(公告)日：2015-12-08

申请号：US14007427

申请日：2012-04-05

Applicant: Lars Bärfacker ,  William Scott ,  Andrea Hägebarth ,  Stuart Ince ,  Hartmut Rehwinkel ,  Oliver Politz ,  Roland Neuhaus ,  Hans Briem ,  Ulf Bömer

Inventor： Lars Bärfacker ,  William Scott ,  Andrea Hägebarth ,  Stuart Ince ,  Hartmut Rehwinkel ,  Oliver Politz ,  Roland Neuhaus ,  Hans Briem ,  Ulf Bömer

IPC: C07D487/04 ,  A61K31/5025 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K45/06

Abstract: The application relates to imidazopyridazines of formula (I) which are useful as Akt inhibitors suitable for the treatment of cancer, and processes for their production and the use thereof.

Abstract translation: 本申请涉及可用作适于治疗癌症的Akt抑制剂及其制备方法及其用途的式（I）咪唑并哒嗪。

公开(公告)号：US20120263708A1

公开(公告)日：2012-10-18

申请号：US13393583

申请日：2010-08-24

Applicant: Benjamin Bader ,  Ulf Bömer ,  Stuart Ince ,  Marcus Koppitz ,  Philip Lienau ,  Tobias Marquardt ,  Duy Nguyen ,  Stefan Prechtl ,  Gerhard Siemeister ,  Christof Wegscheid-Gerlach

Inventor： Benjamin Bader ,  Ulf Bömer ,  Stuart Ince ,  Marcus Koppitz ,  Philip Lienau ,  Tobias Marquardt ,  Duy Nguyen ,  Stefan Prechtl ,  Gerhard Siemeister ,  Christof Wegscheid-Gerlach

IPC: A61K31/498 ,  A61K31/5377 ,  C07D413/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  A61K31/551 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/573 ,  A61K31/565 ,  A61K31/704 ,  A61K38/14 ,  A61K31/7048 ,  A61K31/675 ,  A61K31/7068 ,  A61K31/7076 ,  A61K31/69 ,  A61K33/24 ,  A61K39/395 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00 ,  A61P35/02 ,  A61P35/04 ,  A61K31/513 ,  A61K31/501 ,  C07D413/04

CPC classification number: C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D487/04

Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract translation: 本发明涉及通式（I）的取代氨基喹喔啉化合物，其中（II），R2，R3，R4，R6，R7，n和m如说明书和权利要求书中所给出，涉及制备所述化合物的方法 涉及包含所述化合物的药物组合物和组合，用于制备用于治疗或预防疾病的药物组合物的所述化合物的用途，以及可用于制备所述化合物的中间体化合物。