公开(公告)号：US09730929B2

公开(公告)日：2017-08-15

申请号：US14123511

申请日：2012-05-30

申请人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

发明人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

IPC分类号： C07D487/04 ,  A61K31/5025 ,  C07D519/00 ,  A61K45/06

CPC分类号： A61K31/5025 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

摘要： The present invention relates to substituted aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

公开(公告)号：US09284319B2

公开(公告)日：2016-03-15

申请号：US14129043

申请日：2012-06-21

申请人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

发明人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

IPC分类号： A61K31/5025 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to heterocyclyl aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

摘要翻译： 本发明涉及通式（I）的杂环基氨基咪唑并哒嗪化合物：其中A，R1，R2，R3和R4如权利要求中所定义，涉及制备所述化合物的方法，药物组合物和包含所述化合物的组合， 所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的用途。

公开(公告)号：US20140288069A1

公开(公告)日：2014-09-25

申请号：US14118519

申请日：2012-05-14

申请人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

发明人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

IPC分类号： C07D487/04 ,  A61K31/5377 ,  A61K31/5025

CPC分类号： C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  C07D519/00

摘要： The present invention relates to amino imidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said 10 compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

摘要翻译： 本发明涉及通式（I）的氨基咪唑并哒嗪化合物：其中A，R 1，R 2，R 3和R 4如权利要求中所定义，涉及制备所述化合物的方法，药物组合物和包含所述10种化合物和 涉及用于制造用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的用途。

公开(公告)号：US20150038485A1

公开(公告)日：2015-02-05

申请号：US14129043

申请日：2012-06-21

申请人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

发明人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to heterocyclyl aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

摘要翻译： 本发明涉及通式（I）的杂环基氨基咪唑并哒嗪化合物：其中A，R1，R2，R3和R4如权利要求中所定义，涉及制备所述化合物的方法，药物组合物和包含所述化合物的组合， 所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的用途。

公开(公告)号：US20140194430A1

公开(公告)日：2014-07-10

申请号：US14123511

申请日：2012-05-30

申请人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

发明人： Knut Eis ,  Florian Pühler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Jörg Fanghänel ,  Daniel Korr

IPC分类号： A61K31/5025 ,  C07D487/04 ,  C07D519/00 ,  A61K45/06

CPC分类号： A61K31/5025 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

摘要： The present invention relates to substituted aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

摘要翻译： 本发明涉及通式（I）的取代的氨基咪唑并哒嗪化合物：其中A，R 1，R 2，R 3和R 4如权利要求中所定义，涉及制备所述化合物的方法，药物组合物和包含所述化合物的组合， 所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的用途。

公开(公告)号：US09499547B2

公开(公告)日：2016-11-22

申请号：US14342977

申请日：2012-09-05

申请人： Knut Eis ,  Florian Puehler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Marion Hitchcock

发明人： Knut Eis ,  Florian Puehler ,  Ludwig Zorn ,  Arne Scholz ,  Philip Lienau ,  Mark Jean Gnoth ,  Ulf Bömer ,  Judith Günther ,  Marion Hitchcock

IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K45/06

CPC分类号： C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K45/06

摘要： The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I): in which A, R1, R3 and n are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20130252890A1

公开(公告)日：2013-09-26

申请号：US13806845

申请日：2011-06-21

申请人： Tim Wintermantel ,  Carsten Möller ,  Ulrich Bothe ,  Reinhard Nubbemeyer ,  Ludwig Zorn ,  Dirk Kosemund ,  Antonius Ter Laak ,  Rolf Bohlmann ,  Lars Wortmann ,  Donald Bierer

发明人： Tim Wintermantel ,  Carsten Möller ,  Ulrich Bothe ,  Reinhard Nubbemeyer ,  Ludwig Zorn ,  Dirk Kosemund ,  Antonius Ter Laak ,  Rolf Bohlmann ,  Lars Wortmann ,  Donald Bierer

IPC分类号： C07C317/28 ,  A61K38/22 ,  A61K31/18 ,  A61K31/216 ,  A61K31/165 ,  A61K31/277 ,  C07C323/25 ,  A61K31/145

CPC分类号： C07C317/28 ,  A61K31/145 ,  A61K31/165 ,  A61K31/18 ,  A61K31/216 ,  A61K31/277 ,  A61K38/22 ,  C07B59/001 ,  C07B2200/05 ,  C07C323/25 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/12

摘要： The invention relates to selective oestrogen receptor modulators (SERM) and methods of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception.

摘要翻译： 本发明涉及选择性雌激素受体调节剂（SERM）及其生产方法，其用于治疗和/或预防疾病的用途及其用于生产用于治疗和/或预防疾病的药物的用途，特别是 出血性疾病，骨质疏松症，子宫内膜异位症，肌瘤，激素依赖性肿瘤，用于激素替代疗法和避孕。

公开(公告)号：US07202260B2

公开(公告)日：2007-04-10

申请号：US10866078

申请日：2004-06-14

申请人： Andreas Huth ,  Martin Krueger ,  Ludwig Zorn ,  Stuart Ince ,  Rolf Bohlmann ,  Karl Heinz Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

发明人： Andreas Huth ,  Martin Krueger ,  Ludwig Zorn ,  Stuart Ince ,  Rolf Bohlmann ,  Karl Heinz Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

IPC分类号： C07D401/01 ,  C07D213/02 ,  A61K31/44

CPC分类号： C07D213/64

摘要： Novel VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridones and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are selected.

摘要翻译： 选择新型VEGFR-2和VEGFR-3抑制性邻氨基苯甲酰胺吡啶酮及其作为用于治疗由持续性血管生成引发的疾病的药物的用途。

公开(公告)号：US07148357B2

公开(公告)日：2006-12-12

申请号：US10631018

申请日：2003-07-31

申请人： Andreas Huth ,  Ludwig Zorn ,  Martin Kruger ,  Stuat Ince ,  Karl-Heinz Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

发明人： Andreas Huth ,  Ludwig Zorn ,  Martin Kruger ,  Stuat Ince ,  Karl-Heinz Thierauch ,  Andreas Menrad ,  Martin Haberey ,  Holger Hess-Stumpp

IPC分类号： C07D401/10

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

摘要： 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.

公开(公告)号：US20050090477A1

公开(公告)日：2005-04-28

申请号：US10625559

申请日：2003-07-24

申请人： Ludwig Zorn ,  Rolf Bohlmann ,  Norbert Gallus ,  Hermann Kuenzer ,  Hans-Peter Muhn ,  Reinhard Nubbemeyer

发明人： Ludwig Zorn ,  Rolf Bohlmann ,  Norbert Gallus ,  Hermann Kuenzer ,  Hans-Peter Muhn ,  Reinhard Nubbemeyer

IPC分类号： C07J1/00 ,  C07J3/00 ,  C07J5/00 ,  C07J7/00 ,  C07J9/00 ,  C07J11/00 ,  C07J31/00 ,  C07J41/00 ,  C12P33/10 ,  C12P33/16

CPC分类号： C07J1/00 ,  C07J1/0051 ,  C07J3/00 ,  C07J5/00 ,  C07J7/00 ,  C07J9/00 ,  C07J11/00 ,  C07J31/00 ,  C07J41/00 ,  C12P33/10 ,  C12P33/16

摘要： A novel method of synthesis for the manufacture of upstream products for the production of compounds with general formulas 8, 10, and 12 is described. In this synthesis, compounds with general formula 4,B are produced in a microbiological reaction. The meanings of R7, R10, R11, R13, R17 and R17′ as well as of the grouping U-V-W-X-Y-Z are indicated in the claims.

摘要翻译： 描述了用于制备用于生产具有通式8,10和12的化合物的上游产物的合成新方法。 在该合成中，通式4的化合物B在微生物反应中产生。 R 7，R 10，R 11，R 13，R 17，R 17，R 17， SUP＆gt;和R＆lt; 17＆gt;以及分组UVWXYZ在权利要求中表示。