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91. 发明申请

US20070293667A1 4-Amino-quinazolines 有权
标题翻译： 4-氨基 - 喹唑啉
公开(公告)号：US20070293667A1
公开(公告)日：2007-12-20
申请号：US11300626
申请日：2005-12-14
申请人： Werner Mederski , Ralf Devant , Gerhard Barnickel , Sabine Bernotat-Danielowski , James Vickers , Bertram Cezanne , Daljit Dhanoa , Bao-Ping Zhao , James Rinker , Mark Player , Edward Jaeger , Richard Soll
发明人： Werner Mederski , Ralf Devant , Gerhard Barnickel , Sabine Bernotat-Danielowski , James Vickers , Bertram Cezanne , Daljit Dhanoa , Bao-Ping Zhao , James Rinker , Mark Player , Edward Jaeger , Richard Soll
IPC分类号： C07D239/72 , C07D403/02 , C07D413/02
CPC分类号： C07D239/94 , C07D403/12 , C07D405/12 , C07D409/10 , C07D409/14 , C07D413/12
摘要： Quinazolines of the formula I in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent Claim 1, and their salts or solvates as glycoprotein IbIX antagonists.
摘要翻译：其中R 1，R 2，R 2，R 3，R 4和Y 4的式I的喹唑啉具有专利权利要求1中所示的含义，并且其盐或溶剂合物作为糖蛋白IbIX拮抗剂。

92. 发明申请

US20060019974A1 4-Amino-quinazolines 有权
标题翻译： 4-氨基 - 喹唑啉
公开(公告)号：US20060019974A1
公开(公告)日：2006-01-26
申请号：US10380908
申请日：2001-09-17
申请人： Werner Mederski , Ralf Devant , Maria Devant , Gerhard Barnickel , Sabine Bernotat-Danielowski , James Vickers , Bertram Cezanne , Daljit Dhanoa , Bao-Ping Zhao , James Rinker , Mark Player , Edward Jaeger , Richard Soll
发明人： Werner Mederski , Ralf Devant , Maria Devant , Gerhard Barnickel , Sabine Bernotat-Danielowski , James Vickers , Bertram Cezanne , Daljit Dhanoa , Bao-Ping Zhao , James Rinker , Mark Player , Edward Jaeger , Richard Soll
IPC分类号： A61K31/517 , C07D403/02 , C07D239/94
CPC分类号： C07D239/94 , C07D239/95 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/14
摘要： Quinazolines of the formula (I) in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists.
摘要翻译：式（I）的喹唑啉其中R 1，R 2，R 2，R 3，R 4，并且Y具有专利权利要求1中所示的含义，并且其盐或溶剂合物作为糖蛋白IbIX拮抗剂。

93. 发明授权

US5798364A Imidazopyridines 失效
标题翻译：咪唑并吡啶
公开(公告)号：US5798364A
公开(公告)日：1998-08-25
申请号：US725242
申请日：1996-10-04
申请人： Werner Mederski , Johannes Sombroek , Pierre Schelling , Norbert Beier , Ingeborg Lues , Klaus-Otto Minck
发明人： Werner Mederski , Johannes Sombroek , Pierre Schelling , Norbert Beier , Ingeborg Lues , Klaus-Otto Minck
IPC分类号： C07D471/04 , A61K31/415 , C07D471/06
CPC分类号： C07D471/04
摘要： Imidazopyridine derivatives and pharmacologically acceptable salts having antagonistic properties towards angiotensin II can be used for the treatment of hypertension, aldosteronism and cardiac insufficiency.
摘要翻译：对血管紧张素II有拮抗作用的咪唑并吡啶衍生物和药理学上可接受的盐可用于治疗高血压，醛固酮增多和心功能不全。

94. 发明授权

US5321137A Process for the preparation of imidazopyridines 失效
标题翻译：咪唑并吡啶的制备方法
公开(公告)号：US5321137A
公开(公告)日：1994-06-14
申请号：US102175
申请日：1993-08-04
申请人： Werner Mederski , Heinz-Hermann Bokel
发明人： Werner Mederski , Heinz-Hermann Bokel
IPC分类号： A61K31/435 , A61K31/44 , A61P9/12 , A61P43/00 , C07D471/04 , C07D213/75
CPC分类号： C07D471/04
摘要： The invention relates to a novel process for the preparation of imidazopyridines of formula I: ##STR1## in which R is an alkyl having 1-6 C atoms, characterized in that 3,4-diamino-2-chloropyridine (II) is reacted with an acid anhydride of the formula RCO--O--COR 40 (III), in which R is as defined and R' is R or can be another aliphatic or aromatic radical, to give a 4-amino-2-chloro-3-R-CO-aminopyridine (IV), this is converted with 4'-bromomethyl-2-cyanobiphenyl (V), in the presence of an alkali metal alcoholate in an inert solvent, to a 4-amino-2-chloro-3-R-CO-[N-(2'-cyano-biphenyl-4-ylmethyl)-amino]pyridine (VI) and this is treated with a strong acid, a 2-R-4-chloro-3-(2'-cyano-biphenyl-4-ylmethyl)-3H-imidazo[4,5-c]pyridine (VII) being formed as an intermediate.
摘要翻译：本发明涉及制备式I的咪唑并吡啶的新方法：其中R是具有1-6个C原子的烷基，其特征在于3,4-二氨基-2-氯吡啶（II）反应与式RCO-O-COR 40（III）的酸酐反应，其中R如上所定义，R'是R或可以是其它脂族或芳族基团，得到4-氨基-2-氯-3- 将R-CO-氨基吡啶（Ⅳ）在惰性溶剂中，在碱金属醇盐存在下，用4-溴甲基-2-氰基联苯（Ⅴ）转化成4-氨基-2-氯-3- R-CO- [N-（2'-氰基 - 联苯-4-基甲基） - 氨基]吡啶（Ⅵ），用强酸，2-R-4-氯-3-（2'- 氰基 - 联苯-4-基甲基）-3H-咪唑并[4,5-c]吡啶（VII）。

95. 发明申请

US20130172337A1 Imidazo[4,5-c]quinolines as DNA-PK inhibitors 有权
标题翻译：咪唑并[4,5-c]喹啉作为DNA-PK抑制剂
公开(公告)号：US20130172337A1
公开(公告)日：2013-07-04
申请号：US13819488
申请日：2011-07-26
申请人： Thomas Fuchss , Werner Mederski , Frank Zenke
发明人： Thomas Fuchss , Werner Mederski , Frank Zenke
IPC分类号： C07D471/04 , A61K31/5377 , A61K31/4745 , C07D215/46 , A61K45/06
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4745 , A61K31/5377 , A61K45/06 , C07D215/42 , C07D215/44 , C07D215/46 , C12N9/12 , C12Y207/11001 , A61K2300/00
摘要： The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).
摘要翻译：本发明涉及式（I）和（II）的化合物，其中R 1，R 2，R 3，R 4，R 5，R 8，X和m具有权利要求中所示的含义，和/或生理上可接受的盐，互变异构体和立体异构体包括其所有比例的混合物。式（I）的化合物可用于抑制丝氨酸/苏氨酸蛋白激酶和癌细胞对抗癌剂和/或电离辐射的敏化。本发明还涉及结合放射治疗和/或抗癌剂的式（I）化合物在癌症，肿瘤，转移或血管生成障碍的预防，治疗或进展控制中的用途。本发明还涉及制备式（I）化合物的方法。

96. 发明申请

US20130150359A1 PYRAZOLOQUINOLINES 有权
标题翻译：吡唑啉醇
公开(公告)号：US20130150359A1
公开(公告)日：2013-06-13
申请号：US13807954
申请日：2011-06-24
申请人： Thomas Fuchss , Werner Mederski , Frank Zenke
发明人： Thomas Fuchss , Werner Mederski , Frank Zenke
IPC分类号： C07D471/04 , C07D519/00 , C07D215/18 , A61K31/496 , A61K45/06 , A61K31/4745 , A61K31/5377 , C12N9/99 , C07D215/38
CPC分类号： C07D471/04 , A61K31/4745 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D215/18 , C07D215/38 , C07D519/00 , C12N9/99 , A61K2300/00
摘要： The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formula (II) or (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of its salts
摘要翻译：本发明涉及式（I），（II）和（III）的化合物，和/或其生理上可接受的盐，互变异构体和立体异构体，包括其所有比例的混合物。式（I）的化合物可用于抑制丝氨酸/苏氨酸蛋白激酶和癌细胞对抗癌剂和/或电离辐射的敏化。本发明还涉及结合放射治疗和/或抗癌剂的式（I）化合物在癌症，肿瘤，转移或血管生成障碍的预防，治疗或进展控制中的用途。本发明还涉及通过式（II）或（III）化合物与式（I）化合物的碱或酸的任意转化来制备式（I）化合物的方法，成为其中一种盐

97. 发明申请

US20130012489A1 Morpholinylquinazolines 有权
标题翻译：吗啉基喹唑啉
公开(公告)号：US20130012489A1
公开(公告)日：2013-01-10
申请号：US13581699
申请日：2011-02-17
申请人： Werner Mederski , Thomas Fuchss , Frank Zenke
发明人： Werner Mederski , Thomas Fuchss , Frank Zenke
IPC分类号： A61K31/5377 , C07D417/06 , C12N9/99 , C12N5/09 , A61P35/04 , C07D417/14 , C07D413/14 , A61K31/55 , A61K35/00 , C07D413/10 , C07D409/06
CPC分类号： C07D239/94 , C07D239/86 , C07D295/155 , C07D401/04 , C07D401/14 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/06 , C07D417/14
摘要： The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in claim 1, and/or physiologically acceptable salts, tautomers and stereo-isomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.
摘要翻译：本发明涉及其中R1，R2，R3，R4，Y，W1，W2，L，A，Alk，Cyc，Ar，Het1，Het2，Hal等式（I），（II）和（III）和n具有权利要求1所述的含义，和/或其生理上可接受的盐，互变异构体和立体异构体，包括其所有比例的混合物。式（I）的化合物可用于抑制丝氨酸/苏氨酸蛋白激酶和癌细胞对抗癌剂和/或电离辐射的敏化。本发明还涉及结合放射治疗和/或抗癌剂的式（I）化合物在癌症，肿瘤，转移或血管生成障碍的预防，治疗或进展控制中的用途。本发明还涉及通过式（II）和（III）化合物的反应制备式（I）化合物的方法，并且任选地转化式（I）化合物的碱或酸，成为他们的一种盐。

98. 发明授权

US07776920B2 Mandelic hydrazides 失效
标题翻译：扁豆酰肼
公开(公告)号：US07776920B2
公开(公告)日：2010-08-17
申请号：US12279227
申请日：2007-01-18
申请人： Rolf Gericke , Markus Klein , Werner Mederski , Norbert Beier , Florian Lang
发明人： Rolf Gericke , Markus Klein , Werner Mederski , Norbert Beier , Florian Lang
IPC分类号： C07C243/38 , A61K31/166
CPC分类号： C07C243/38
摘要： Novel mandelic hydrazides of the formula (I), in which R1-R11 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.
摘要翻译：式（I）的新型扁桃酸酰肼，其中R 1 -R 11具有权利要求1所述的含义，是SGK抑制剂，可用于治疗SGK诱发的疾病和投诉，例如糖尿病，肥胖症，代谢综合征血脂异常），全身和肺高血压，心血管疾病和肾脏疾病，通常在任何类型的纤维和炎症过程中。

99. 发明申请

US20090221712A1 MANDELIC HYDRAZIDES 失效
公开(公告)号：US20090221712A1
公开(公告)日：2009-09-03
申请号：US12279227
申请日：2007-01-18
申请人： Rolf Gericke , Markus Klein , Werner Mederski , Norbert Beier , Florian Lang
发明人： Rolf Gericke , Markus Klein , Werner Mederski , Norbert Beier , Florian Lang
IPC分类号： A61K31/166 , C07C243/38 , C07C241/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P25/28 , A61P11/00 , A61P29/00
CPC分类号： C07C243/38
摘要： Novel mandelic hydrazides of the formula (I), in which R1-R11 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.
摘要翻译：式（I）的新型扁桃酸酰肼，其中R 1 -R 11具有权利要求1所述的含义，是SGK抑制剂，可用于治疗SGK诱发的疾病和投诉，例如糖尿病，肥胖症，代谢综合征血脂异常），全身和肺高血压，心血管疾病和肾脏疾病，通常在任何类型的纤维和炎症过程中。

100. 发明申请

US20080234348A1 3-Oxoindazolesquaric Acid Derivatives 审中-公开
标题翻译： 3-氧代吲唑啉酸衍生物
公开(公告)号：US20080234348A1
公开(公告)日：2008-09-25
申请号：US12064395
申请日：2006-08-02
申请人： Werner Mederski , Rolf Gericke , Markus Klein , Norbert Beier , Florian Lang
发明人： Werner Mederski , Rolf Gericke , Markus Klein , Norbert Beier , Florian Lang
IPC分类号： A61K31/416 , C07D231/54 , A61P3/10 , A61P3/04 , A61P35/00
CPC分类号： C07D231/56
摘要： Novel squaric acid compounds of the formula (I), in which R1, R2, R2′, R2″ and X have the meanings indicated in claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be used for the treatment of diseases and complaints such as cancer, diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.
摘要翻译：式（I）的新型方酸化合物，其中R 1，R 2，R 2，R 2， / SUP>“，X具有权利要求1所述的含义，是CHK1 CHK2和SGK激酶的抑制剂，可用于治疗疾病和投诉，例如癌症，糖尿病，肥胖症，代谢综合征（血脂异常），全身和肺高血压，心血管疾病和肾脏疾病，通常在任何类型的纤维和炎症过程中。

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