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1. 发明申请

US20080312244A1 Squaric Acid Derivatives as Protein Kinase Inhibitors 审中-公开
标题翻译：方酸衍生物作为蛋白激酶抑制剂
公开(公告)号：US20080312244A1
公开(公告)日：2008-12-18
申请号：US11997036
申请日：2006-06-30
申请人： Werner Mederski , Ulrich Emde , Gerhard Barnickel , Frank Zenke , Hartmut Greiner , Frank Stieber
发明人： Werner Mederski , Ulrich Emde , Gerhard Barnickel , Frank Zenke , Hartmut Greiner , Frank Stieber
IPC分类号： A61K31/4965 , A61K31/4402 , C07D241/10 , A61P35/00 , A61P3/10 , C07D213/38
CPC分类号： C07D213/38 , C07C225/20 , C07C2601/04 , C07D207/323 , C07D207/325 , C07D213/61 , C07D213/85 , C07D215/12 , C07D217/12 , C07D231/12 , C07D233/54 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12
摘要： Compounds of the formula I, in which R, X, R1, R2, R3, R4 and R5 have the meanings indicated in Claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be employed, inter alia, for the treatment of cancer.
摘要翻译：其中R，X，R 1，R 2，R 3，R 4和R 5具有权利要求1所示含义的式I化合物是CHK1 CHK2和SGK激酶的抑制剂，并且可以用于治疗癌症。

2. 发明申请

US20080234266A1 Squaric Acid Derivatives II 审中-公开
标题翻译：方酸衍生物II
公开(公告)号：US20080234266A1
公开(公告)日：2008-09-25
申请号：US11997073
申请日：2006-06-30
申请人： Werner Mederski , Ulrich Emde , Gerhard Barnickel , Frank Zenke , Hartmut Greiner , Frank Stieber
发明人： Werner Mederski , Ulrich Emde , Gerhard Barnickel , Frank Zenke , Hartmut Greiner , Frank Stieber
IPC分类号： A61K31/4184 , C07D235/14 , C07D231/56 , C07D513/04 , C07D471/04 , C07D217/12 , A61K31/429 , A61K31/4725 , A61K31/454 , A61P13/00 , A61P9/00 , A61P27/02 , A61P29/00 , A61P3/00 , A61P35/00 , A61K31/496 , A61K31/437 , A61K31/416 , C07D401/14 , C07D413/12 , C07D403/12 , A61K31/5377
CPC分类号： C07D209/80 , C07D231/56 , C07D235/04 , C07D235/06 , C07D249/18 , C07D277/62 , C07D277/64 , C07D307/82 , C07D471/04 , C07D513/04
摘要： Compounds of the formula (I), in which R, X, X′ and R2, R2′, R2″, R3″, R2″″ and R7 have the meanings indicated in claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be employed, inter alia, for the treatment of cancer.
摘要翻译：其中R，X，X'和R“2，R”2“，R”2“，或” R“3”，R 2“”“和”R“具有权利要求1所示的含义，是CHK1 CHK2和SGK的抑制剂激酶，并且可以用于治疗癌症。

3. 发明申请

US20070191353A1 Use of thiadiazoleurea derivatives 审中-公开
标题翻译：噻二唑衍生物的使用
公开(公告)号：US20070191353A1
公开(公告)日：2007-08-16
申请号：US10590729
申请日：2005-01-31
申请人： Lars Burgdorf , Frank Stieber , Hans-Peter Buchstaller , Soheila Anzali , Christiane Amendt , Hartmut Greiner , Matthias Grell , Christian Sirrenberg , Frank Zenke
发明人： Lars Burgdorf , Frank Stieber , Hans-Peter Buchstaller , Soheila Anzali , Christiane Amendt , Hartmut Greiner , Matthias Grell , Christian Sirrenberg , Frank Zenke
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/433 , C07D417/02
CPC分类号： C07D285/135 , C07D417/06 , C07D417/12
摘要： Use of compounds of the formula (I), in which Ar1, Ar2 and Z have the meanings indicated in Patent Claim 1, for the prophylaxis and/or treatment of diseases in which the inhibition, regulation and/or modulation of signal transduction by kinases, in particular RAF kinases, plays a role.
摘要翻译：使用式（I）化合物，其中Ar 1，Ar 2和Z具有专利权利要求1中所示的含义，用于预防和/或治疗其中通过激酶，特别是RAF激酶的信号转导的抑制，调节和/或调节起作用的疾病。

4. 发明申请

US20070142440A1 Pyridinamide derivatives as kinase inhibitors 审中-公开
标题翻译：吡啶酰胺衍生物作为激酶抑制剂
公开(公告)号：US20070142440A1
公开(公告)日：2007-06-21
申请号：US10590724
申请日：2005-01-13
申请人： Lars Burgdorf , Hans-Peter Buchstaller , Frank Stieber , Christiane Amendt , Hartmut Greiner , Matthias Grell , Christ8an Sirrenberg , Frank Zenke
发明人： Lars Burgdorf , Hans-Peter Buchstaller , Frank Stieber , Christiane Amendt , Hartmut Greiner , Matthias Grell , Christ8an Sirrenberg , Frank Zenke
IPC分类号： C07D211/84 , A61K31/4412
CPC分类号： C07D213/81 , C07D401/12
摘要： The invention relates to substituted arylamide derivatives of the formula I, the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases that are caused, mediated and/or propagated by angiogenesis. Compounds of the formula I are effective inhibitors of tyrosine kinases, in particular TIE-2 and VEGFR, and of Raf kinases.
摘要翻译：本发明涉及式I的取代的芳基酰胺衍生物，其制备和用途，用于制备用于治疗由血管发生引起，介导和/或传播的疾病，特别是肿瘤和/或疾病的药物。式I化合物是酪氨酸激酶，特别是TIE-2和VEGFR以及Raf激酶的有效抑制剂。

5. 发明授权

US06441013B1 Sulphonyloxazolamines as therapeutic active ingredients 失效
标题翻译：磺酰氯唑胺作为治疗活性成分
公开(公告)号：US06441013B1
公开(公告)日：2002-08-27
申请号：US09868097
申请日：2001-06-14
申请人： Hartmut Greiner , Gerd Bartoszyk , Henning Böttcher , Gerhard Barnickel , Bertram Cezanne
发明人： Hartmut Greiner , Gerd Bartoszyk , Henning Böttcher , Gerhard Barnickel , Bertram Cezanne
IPC分类号： A61K3142
CPC分类号： C07D263/48
摘要： The present invention relates to sulphonylexazolamines of general formula (I), wherein R1, R2 represent independently from each other H, A, —(CH2)n—Ar or alkenyl with 2-6 C atoms, R1 and R2 together also represent a mononuclear saturated heterocycle with 1-2 N, O and/or S atoms, Z is H, A, CF3, NO2, Hal, OH, OA, NH2, NHA or NH2. A represents alkyl with 1-6 C atoms, Ar is Z-monosubstituted or Z-disubstituted phenyl, Hal is F, Cl, Br, or L n is 1 or 2 of the physiologically acceptable salts or solvates thereof. Said sulphonyloxazolamines are used as therapeutic active ingredients. The invention also relates to the use of sulphonyloxazolamines as therapeutic active ingredients and/or to the production of pharmaceutical preparations to combat diseases of the central nervous system. The invention further relates to a pharmaceutical preparation and the production thereof.
摘要翻译：本发明涉及通式（I）的磺酰基唑胺，其中R 1，R 2彼此独立地表示H，A， - （CH 2）n -Ar或具有2-6个C原子的烯基，R 1和R 2一起也表示单核具有1-2个N，O和/或S原子的饱和杂环，Z是H，A，CF 3，NO 2，Hal，OH，OA，NH 2，NHA或NH 2。 A表示具有1-6个C原子的烷基，Ar是Z-单取代或Z-二取代的苯基，Hal是F，Cl，Br或L n是其生理上可接受的盐或溶剂化物的1或2。所述磺酰基恶唑胺用作治疗活性成分。本发明还涉及磺酰氯唑胺作为治疗活性成分和/或用于制备用于对抗中枢神经系统疾病的药物制剂的用途。本发明还涉及药物制剂及其制备。

6. 发明申请

US20070299065A1 Tetrahydropyran Derivatives as Antidiabetics 审中-公开
标题翻译：四氢吡喃衍生物作为抗糖尿病药
公开(公告)号：US20070299065A1
公开(公告)日：2007-12-27
申请号：US11792133
申请日：2005-11-07
申请人： Werner Mederski , Christoph Van Amsterdam , Christa Burger , Hartmut Greiner
发明人： Werner Mederski , Christoph Van Amsterdam , Christa Burger , Hartmut Greiner
IPC分类号： A61K31/5355 , A61K31/351 , A61K31/4433 , A61K31/453 , A61P3/10 , C07D315/00 , C07D413/12 , C07D405/12 , C07D239/36 , A61K31/497 , A61K31/501 , A61K31/506
CPC分类号： C07H15/203
摘要： Novel compounds of the formula (I), in which T, E, R, R′, R″, R1, R2 and R2′ have the meanings indicated in patent Claim 1, are suitable as antidiabetics.
摘要翻译：式（I）的新型化合物，其中T，E，R，R'，R“，R”，R“2和R”2“ 具有专利权利要求1中所示的含义，适合作为抗糖尿病药。

7. 发明申请

US20120101095A1 ALKOXY-THIENOPYRIMIDINES AS TGF-BETA RECEPTOR KINASE MODULATORS 审中-公开
标题翻译：作为TGF-β受体激酶调节剂的ALKOXY-THIENOPYRIMININES
公开(公告)号：US20120101095A1
公开(公告)日：2012-04-26
申请号：US13379773
申请日：2010-05-27
申请人： Guenter Hoelzemann , Dieter Dorsch , Hartmut Greiner , Christiane Amendt , Frank Zenke
发明人： Guenter Hoelzemann , Dieter Dorsch , Hartmut Greiner , Christiane Amendt , Frank Zenke
IPC分类号： A61K31/5377 , A61K31/519 , A61P35/00 , A61P35/04 , A61P9/00 , A61P25/28 , A61P9/10 , C12N9/99 , A61P43/00 , C07D495/04 , A61P31/18
CPC分类号： C07D495/04
摘要： Novel alkoxy-thienopyrimidine derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.
摘要翻译：式（I）的新型烷氧基 - 噻吩并嘧啶衍生物，其中R 1和R 2具有权利要求1的含义，是TGF-β受体I激酶的抑制剂，并且可以用于治疗肿瘤。

8. 发明申请

US20090131506A1 Oxindoles as Kinase Inhibitors 有权
标题翻译： Oxindoles作为激酶抑制剂
公开(公告)号：US20090131506A1
公开(公告)日：2009-05-21
申请号：US11916902
申请日：2006-05-11
申请人： Lars Thore Burgdorf , David Bruge , Hartmut Greiner , Maria Kordowicz , Christian Sirrenberg , Frank Zenke
发明人： Lars Thore Burgdorf , David Bruge , Hartmut Greiner , Maria Kordowicz , Christian Sirrenberg , Frank Zenke
IPC分类号： A61K31/404 , C07D209/34 , A61P35/00
CPC分类号： C07D209/34
摘要： The present invention relates to oxindoles of the formula I, their use as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases and their use for the manufacture of a pharmaceutical composition.
摘要翻译：本发明涉及式I的羟吲哚，其用作蛋白激酶激活剂或抑制剂，其制备方法，其用于制备用于治疗疾病的药物及其用于制备药物组合物的用途。

9. 发明授权

US07781475B2 Oxindoles as kinase inhibitors 有权
标题翻译： Oxindoles作为激酶抑制剂
公开(公告)号：US07781475B2
公开(公告)日：2010-08-24
申请号：US11916902
申请日：2006-05-11
申请人： Lars Thore Burgdorf , David Bruge , Hartmut Greiner , Maria Kordowicz , Christian Sirrenberg , Frank Zenke
发明人： Lars Thore Burgdorf , David Bruge , Hartmut Greiner , Maria Kordowicz , Christian Sirrenberg , Frank Zenke
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D209/34
摘要： The present invention relates to oxindoles of the formula I, their use as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases and their use for the manufacture of a pharmaceutical composition.
摘要翻译：本发明涉及式I的羟吲哚，其用作蛋白激酶激活剂或抑制剂，其制备方法，其用于制备用于治疗疾病的药物及其用于制备药物组合物的用途。

10. 发明申请

US20100197757A1 OXINDOLES AS KINASE INHIBITORS 审中-公开
标题翻译：氧化物作为激酶抑制剂
公开(公告)号：US20100197757A1
公开(公告)日：2010-08-05
申请号：US12761021
申请日：2010-04-15
申请人： Lars Thore BURGDORF , David Bruge , Hartmut Greiner , Maria Kordowicz , Christian Sirrenberg , Frank Zenke
发明人： Lars Thore BURGDORF , David Bruge , Hartmut Greiner , Maria Kordowicz , Christian Sirrenberg , Frank Zenke
IPC分类号： A61K31/404 , A61P35/00 , A61P35/02
CPC分类号： C07D209/34
摘要： The present invention relates to oxindoles of the formula I, their use as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases and their use for the manufacture of a pharmaceutical composition.
摘要翻译：本发明涉及式I的羟吲哚，其用作蛋白激酶激活剂或抑制剂，其制备方法，其用于制备用于治疗疾病的药物及其用于制备药物组合物的用途。

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