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1. 发明授权

US08232283B2 Raf inhibitors 有权
标题翻译： Raf抑制剂
公开(公告)号：US08232283B2
公开(公告)日：2012-07-31
申请号：US13105957
申请日：2011-05-12
申请人： Andreas Schoop , Alexander Backes , Joachim Vogt , Lars Neumann , Jan Eickhoff , Stefan Hannus , Kerrin Hansen , Peter Amon , Igor Ivanov , Matthias Borgmann , Chase Smith , Arthur F. Kluge , Krishan Murthi , Rebecca Casaubon
发明人： Andreas Schoop , Alexander Backes , Joachim Vogt , Lars Neumann , Jan Eickhoff , Stefan Hannus , Kerrin Hansen , Peter Amon , Igor Ivanov , Matthias Borgmann , Chase Smith , Arthur F. Kluge , Krishan Murthi , Rebecca Casaubon
IPC分类号： C07D471/04 , A61K31/505 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are inhibitors or kinases such as Raf, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
摘要翻译：本发明提供吡啶并[2,3-d]嘧啶-7-酮的衍生物。这些化合物是抑制剂或激酶如Raf，包括显示抗增殖活性的化合物，包括抗肿瘤细胞，并且可用于治疗包括癌症在内的疾病。

2. 发明授权

US06589972B2 &bgr;-phenylalanine derivatives as integrin antagonists 失效
标题翻译： β-苯丙氨酸衍生物作为整联蛋白拮抗剂
公开(公告)号：US06589972B2
公开(公告)日：2003-07-08
申请号：US09867835
申请日：2001-05-30
申请人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
发明人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
IPC分类号： A01N4350
CPC分类号： C07C311/19 , C07C311/47
摘要： The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4′, —COOR4″, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.
摘要翻译：本发明涉及通式（1）的化合物，其中R 4是-SO 2 R 4'，-COOR 4“，-COR 4'， - CONR 4'2或-CSNR 4'2; R 4'是氢，取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺，酰胺，醚，酯，酮，脲，硫醚，亚砜或砜单元; X为N，O或S; 及其生理上可接受的盐和立体异构体。本发明还涉及制备式（1）化合物的方法，含有这些化合物中的至少一种的药物组合物，以及式（1）化合物在制备药物组合物中的用途具有整合素拮抗作用，特别是用于治疗和预防癌症，溶骨性疾病如骨质疏松症，动脉硬化，再狭窄和眼科疾病。

3. 发明授权

US06420393B1 Cyclopentabenzofuran derivatives and their use 失效
标题翻译：环戊苯并呋喃衍生物及其用途
公开(公告)号：US06420393B1
公开(公告)日：2002-07-16
申请号：US09762417
申请日：2001-03-26
申请人： Walter Guarnieri , Thomas Jaetsch , Andreas Schoop , Jörg Baumgarten , Axel Kretschmer , Horst-Peter Antonicek
发明人： Walter Guarnieri , Thomas Jaetsch , Andreas Schoop , Jörg Baumgarten , Axel Kretschmer , Horst-Peter Antonicek
IPC分类号： A61K31443
CPC分类号： C07D307/93
摘要： The invention relates to cyclopentabenzofuran derivatives, processes for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-&kgr;B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.
摘要翻译：本发明涉及环戊烷并苯并呋喃衍生物，其制备方法，使用环戊二酸苯并呋喃衍生物用于制备用于治疗NF-κB依赖性疾病的药物和含有环戊二酸苯并呋喃衍生物的药物。

4. 发明授权

US06291503B1 &bgr;-phenylalanine derivatives as integrin antagonists 失效
标题翻译： β-苯丙氨酸衍生物作为整联蛋白拮抗剂
公开(公告)号：US06291503B1
公开(公告)日：2001-09-18
申请号：US09232738
申请日：1999-01-15
申请人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
发明人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
IPC分类号： A01N4356
CPC分类号： C07C311/19 , C07C311/47
摘要： The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4, —COOR4′, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.
摘要翻译：本发明涉及通式（1）的化合物，其中R4是-SO2R4，-COOR4'，-COR4'，-CONR4'2或-CSNR4'2; R 4'是氢，取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺，酰胺，醚，酯，酮，脲，硫醚，亚砜或砜单元; X为N，O或S; 及其生理上可接受的盐和立体异构体。本发明还涉及制备式（1）化合物的方法，含有这些化合物中的至少一种的药物组合物，以及式（1）化合物在制备药物组合物中的用途具有整合素拮抗作用，特别是用于治疗和预防癌症，溶骨性疾病如骨质疏松症，动脉硬化，再狭窄和眼科疾病。

5. 发明授权

US09243000B2 Thia-triaza-indacenes 有权
公开(公告)号：US09243000B2
公开(公告)日：2016-01-26
申请号：US13265241
申请日：2010-04-22
申请人： Lars Van Der Veen , Darryl McConnell , Siegfried Schneider , Matthias Grauert , Andreas Schoop , Tobias Wunberg
发明人： Lars Van Der Veen , Darryl McConnell , Siegfried Schneider , Matthias Grauert , Andreas Schoop , Tobias Wunberg
IPC分类号： C07D513/04 , A61K31/381 , C07D513/14
CPC分类号： C07D513/04 , C07D513/14
摘要： The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
摘要翻译：本发明包括通式（1）的化合物，其中R 1至R 3和X如权利要求1中所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，以及其用于制备具有上述属性。

6. 发明申请

US20090163467A1 New compounds 有权
标题翻译：新化合物
公开(公告)号：US20090163467A1
公开(公告)日：2009-06-25
申请号：US11747337
申请日：2007-05-11
申请人： Stephan Karl Zahn , Bojan Bister , Guido Boehmelt , Ulrich Guertler , Andreas Mantoulidis , Ulrich Reiser , Andreas Schoop , Flavio Solca , Ulrike Tontsch-Grunt , Matthias Treu
发明人： Stephan Karl Zahn , Bojan Bister , Guido Boehmelt , Ulrich Guertler , Andreas Mantoulidis , Ulrich Reiser , Andreas Schoop , Flavio Solca , Ulrike Tontsch-Grunt , Matthias Treu
IPC分类号： A61K31/397 , C07D401/12 , A61K31/506 , C07D403/12 , C07D401/14 , C07D413/14 , A61K31/5377 , A61K31/496 , C07D417/14 , A61K31/541 , A61P35/00 , A61P29/00 , A61P31/00 , A61P37/00
CPC分类号： C07D405/12 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention encompasses compounds of general formula (1) wherein R1, R2, R4, X, m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
摘要翻译：本发明包括通式（1）的化合物，其中R 1，R 2，R 4，X，m，n和p如权利要求1中所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，用于制备具有上述性质的药物组合物。

7. 发明授权

US07220824B1 Integrin-mediated drug targeting 有权
标题翻译：整合素介导的药物靶向
公开(公告)号：US07220824B1
公开(公告)日：2007-05-22
申请号：US10070208
申请日：2000-08-28
申请人： Hans-Georg Lerchen , Jörg Baumgarten , Ulf Brüggemeier , Markus Albers , Andreas Schoop , Thomas-J. Schulze
发明人： Hans-Georg Lerchen , Jörg Baumgarten , Ulf Brüggemeier , Markus Albers , Andreas Schoop , Thomas-J. Schulze
IPC分类号： A61K38/14
CPC分类号： C07D491/22
摘要： The present invention relates to cytostatics which have a tumour-specific action as a result of linkage to αvβ3 integrin antagonists via preferred linking units. The preferred linking units guarantee serum stability of the conjugate of cytostatic and αvβ3 integrin antagonist and at the same time the desired intracellular action in tumour cells as a result of their enzymatic or hydrolytic cleavability with release of the cytostatic.
摘要翻译：本发明涉及通过优选连接单元与α-β3整联蛋白拮抗剂连接而具有肿瘤特异性作用的细胞抑制剂。优选的连接单元保证细胞生长抑制和α3β3整联蛋白拮抗剂的缀合物的血清稳定性，同时由于它们的结合，肿瘤细胞中期望的细胞内作用酶促或水解裂解性，释放细胞抑制作用。

8. 发明授权

US07173028B2 Pyrimidine derivatives 有权
标题翻译：嘧啶衍生物
公开(公告)号：US07173028B2
公开(公告)日：2007-02-06
申请号：US10271763
申请日：2002-10-16
申请人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schnapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
发明人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schnapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
IPC分类号： C07D417/10 , C07D239/48 , A61K31/506
CPC分类号： C07D239/48 , C07D231/12 , C07D233/56 , C07D239/50 , C07D239/80 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D451/04 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
摘要： The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
摘要翻译：本发明涉及如权利要求1所定义的式（I）的三取代嘧啶，其中R 1和R 2定义如权利要求1所述，其适用于治疗以过量为特征的疾病或异常细胞增殖，其用于制备具有上述性质的药物组合物的用途及其制备方法。

9. 发明授权

US08207349B2 Thiazolyl-dihydro-indazoles 有权
标题翻译：噻唑基 - 二氢 - 吲唑
公开(公告)号：US08207349B2
公开(公告)日：2012-06-26
申请号：US12685213
申请日：2010-01-11
申请人： Bodo Betzemeier , Trixi Brandl , Steffen Breitfelder , Ralph Brueckner , Thomas Gerstberger , Michael Gmachl , Matthias Grauert , Frank Hilberg , Christoph Hoenke , Matthias Hoffmann , Maria Impagnatiello , Dirk Kessler , Christian Klein , Bernd Krist , Udo Maier , Darryl McConnell , Charlotte Reither , Stefan Scheuerer , Andreas Schoop , Norbert Schweifer , Oliver Simon , Martin Steegmaier , Steffen Steurer , Irene Waizenegger , Ulrike Weyer-Czernilofsky , Andreas Zoephel
发明人： Bodo Betzemeier , Trixi Brandl , Steffen Breitfelder , Ralph Brueckner , Thomas Gerstberger , Michael Gmachl , Matthias Grauert , Frank Hilberg , Christoph Hoenke , Matthias Hoffmann , Maria Impagnatiello , Dirk Kessler , Christian Klein , Bernd Krist , Udo Maier , Darryl McConnell , Charlotte Reither , Stefan Scheuerer , Andreas Schoop , Norbert Schweifer , Oliver Simon , Martin Steegmaier , Steffen Steurer , Irene Waizenegger , Ulrike Weyer-Czernilofsky , Andreas Zoephel
IPC分类号： C07D277/60
CPC分类号： C07D513/04 , C07D277/84
摘要： The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.
摘要翻译：本发明包括通式（1）的化合物，其中R 1至R 3如权利要求1中所定义，其适用于治疗特征为过度或异常细胞增殖的疾病，以及其用于制备具有上述属性。

10. 发明授权

US07709480B2 Pyrimidine derivatives 有权
标题翻译：嘧啶衍生物
公开(公告)号：US07709480B2
公开(公告)日：2010-05-04
申请号：US11313380
申请日：2005-12-21
申请人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
发明人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
IPC分类号： C07D417/00 , C07D239/48 , A61K31/506
CPC分类号： C07D239/48 , C07D231/12 , C07D233/56 , C07D239/50 , C07D239/80 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D451/04 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
摘要： The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
摘要翻译：本发明涉及式（I）的三取代嘧啶，其中0Ra至Re如权利要求1所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，其用于制备具有上述药物组合物的用途性质及其制备方法。

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