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公开(公告)号:US20070021446A1
公开(公告)日:2007-01-25
申请号:US11434658
申请日:2006-05-16
申请人: Jan Ehlert , Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Wael Saeb , Christoph Schaechtele , Stefan Tasler , Frank Totzke , Ute Zirrgiebel
发明人: Jan Ehlert , Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Wael Saeb , Christoph Schaechtele , Stefan Tasler , Frank Totzke , Ute Zirrgiebel
IPC分类号: A61K31/517 , A61K31/4709 , A61K31/506 , A61K31/4439 , C07D403/02
CPC分类号: C07D417/12 , C07D417/14 , C07D473/34 , C07D487/04 , C07D495/04
摘要: The present invention relates to compounds of the general formula (I) and salts, prodrugs, and stereoisomers thereof, wherein Y independently represents S, O, NR2, SO, SO2; A independently represents a fife- or six-membered aromatic carbocycle or heterocycle and wherein R1 to R20 in formula (I) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties.
摘要翻译: 本发明涉及通式(I)的化合物及其盐,前体药物和立体异构体,其中Y独立地表示S,O,NR 2,SO,SO 2, >; A独立地表示芳族或六元芳族碳环或杂环,并且其中式(I)中的R 1至R 20彼此独立地表示各种不同的取代基 包括烷基,芳基,芳烷基,烷基芳基,杂芳基和单官能部分。
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公开(公告)号:US20060142570A1
公开(公告)日:2006-06-29
申请号:US11317909
申请日:2005-12-22
申请人: Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
发明人: Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
IPC分类号: C07D473/14 , C07D487/02 , C07D417/02
CPC分类号: C07D417/12 , C07D413/12 , C07D417/14 , C07D473/34
摘要: The present invention relates to compounds of the general formulas (I), (Ia) and (II) and salts and physiologically functional derivatives thereof, wherein the substituents —Y are attached to the 5- or 6-position of the benzazole.
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公开(公告)号:US07514460B2
公开(公告)日:2009-04-07
申请号:US11303854
申请日:2005-12-15
申请人: Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
发明人: Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
IPC分类号: A61K31/428 , A61K31/517 , A61K31/496 , C07D417/02 , C07D403/02 , C07D403/14 , C07D401/02 , C07D401/14
CPC分类号: C07D417/12 , C07D473/34
摘要: The present invention relates to N2-heteroaryl-benzazole-2,(5 or 6)-diamine derivatives and compositions thereof as protein kinase inhibitors for the treatment of e.g. cancer.
摘要翻译: 本发明涉及作为蛋白激酶抑制剂的N 2 - 杂芳基 - 苯并噻唑-2(5或6) - 二胺衍生物及其组合物。 癌症。
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公开(公告)号:US07576090B2
公开(公告)日:2009-08-18
申请号:US11317909
申请日:2005-12-22
申请人: Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
发明人: Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
IPC分类号: A61K31/517 , A61K31/519 , A61K31/52 , C07D487/00 , C07D239/70
CPC分类号: C07D417/12 , C07D413/12 , C07D417/14 , C07D473/34
摘要: The present invention relates to compounds of the general formulas (I), (Ia) and (II) and salts and physiologically functional derivatives thereof, wherein the substituents —Y are attached to the 5- or 6-position of the benzazole.
摘要翻译: 本发明涉及通式(I),(Ia)和(II)的化合物及其盐和生理功能衍生物,其中取代基-Y连接于苯并唑的5-或6-位。
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公开(公告)号:US20060135782A1
公开(公告)日:2006-06-22
申请号:US11303854
申请日:2005-12-15
申请人: Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
发明人: Thomas Herz , Rolf Krauss , Michael Kubbutat , Martin Lang , Christoph Schaechtele , Stefan Tasler , Frank Totzke
IPC分类号: C07D277/62 , C07D263/60
CPC分类号: C07D417/12 , C07D473/34
摘要: The present invention relates to N2-heteroaryl-benzazole-2,(5 or 6)-diamine derivatives and compositions thereof as protein kinase inhibitors for the treatment of e.g. cancer.
摘要翻译: 本发明涉及作为蛋白激酶抑制剂的N 2 - 杂芳基 - 苯并噻唑-2(5或6) - 二胺衍生物及其组合物。 癌症。
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公开(公告)号:US20070149523A1
公开(公告)日:2007-06-28
申请号:US11559662
申请日:2006-11-14
申请人: Jan Ehlert , Thomas Herz , Rolf Krauss , Micheal Kubbutat , Martin Lang , Stefano Pegoraro , Christoph Schachtele , Frank Totzke , Ute Zirrgiebel
发明人: Jan Ehlert , Thomas Herz , Rolf Krauss , Micheal Kubbutat , Martin Lang , Stefano Pegoraro , Christoph Schachtele , Frank Totzke , Ute Zirrgiebel
IPC分类号: A61K31/5377 , A61K31/53 , A61K31/52 , A61K31/519 , A61K31/506 , A61K31/4745 , A61K31/4439 , C07D473/02 , C07D487/02 , C07D417/02
CPC分类号: C07D417/12
摘要: Compounds of formula (I) and salts and physiologically functional derivatives thereof, wherein R2 is attached at the 4- or 5-position of the thiazole ring and is hydrogen, alkyl, halogen, cyano, alkoxy, haloalkoxy, or alkylamino; X independently represents a divalent linkage group selected from S, O, NR4, SO, or SO2; R4 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, or heterocyclyl; R1 is attached at the 4- or 5-position of the thiazole ring and independently represents a group of formula (II): wherein the dotted line represents a single or double bond; * indicates the point of attachment to the thiazole ring; and n is 1, 2, or 3. Also disclosed are pharmaceutical compositions comprising the above compounds and method of treatments for cancer and other diseases.
摘要翻译: 式(I)化合物及其盐和生理功能衍生物,其中R 2连接在噻唑环的4-或5-位,并且是氢,烷基,卤素,氰基,烷氧基, 卤代烷氧基或烷基氨基; X独立地表示选自S,O,NR 4,SO或SO 2的二价键合基团。 R 4是氢,烷基,环烷基,环烷基烷基或杂环基; R 1连接在噻唑环的4-或5-位,独立地表示式(II)的基团:其中虚线表示单键或双键; *表示与噻唑环的连接点; 并且n为1,2或3.还公开了包含上述化合物的药物组合物和用于癌症和其它疾病的治疗方法。
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公开(公告)号:US20050143382A1
公开(公告)日:2005-06-30
申请号:US10978353
申请日:2004-11-02
申请人: Katharina Aulinger-Fuchs , Thomas Herz , Rolf Krauss , Michael Kubbatat , Martin Lang , Christoph Schachtele , Frank Totzke
发明人: Katharina Aulinger-Fuchs , Thomas Herz , Rolf Krauss , Michael Kubbatat , Martin Lang , Christoph Schachtele , Frank Totzke
IPC分类号: A61K31/495 , A61K31/498 , C07D491/02 , C07D498/04
CPC分类号: C07D498/04
摘要: The present invention relates to furazanopyrazine derivatives of the general formula (I): wherein: R′ represents —NR1R2 or —OR9 R″ represents —NR5—NR3R4, —NR5—ORb, —O—NR3R4; wherein R1 to R9 in formula (I) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties.
摘要翻译: 本发明涉及通式(I)的呋喃并吡嗪衍生物:其中:R'表示-NR 1 R 2或-OR 9, R“表示-NR 5 -NR 3 R 4,-NR 5 -OR B, -O-NR 3 R 4; 其中式(I)中的R 1至R 9彼此独立地表示包含烷基,芳基,芳烷基,烷基芳基,杂芳基和单官能部分的多种不同取代基。
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公开(公告)号:US06949567B2
公开(公告)日:2005-09-27
申请号:US10083008
申请日:2002-02-26
申请人: Andrea Aschenbrenner , Katharina Aulinger Fuchs , Matthias Dormeyer , Gabriel Garcia , Bernd Kramer , Jürgen Kraus , Rolf Krauss , Johan Leban , Stefano Pegoraro , Wael Saeb , Kristina Wolf
发明人: Andrea Aschenbrenner , Katharina Aulinger Fuchs , Matthias Dormeyer , Gabriel Garcia , Bernd Kramer , Jürgen Kraus , Rolf Krauss , Johan Leban , Stefano Pegoraro , Wael Saeb , Kristina Wolf
IPC分类号: A61P33/02 , A61P35/00 , C07C275/40 , C07C275/42 , C07C311/21 , C07C311/37 , C07C311/38 , C07C311/46 , C07C311/47 , C07C317/50 , C07C323/44 , C07C335/22 , C07D209/48 , C07D213/75 , C07D215/38 , C07D217/06 , C07D233/24 , C07D261/18 , C07D277/82 , C07D295/13 , C07D307/14 , C07D333/38 , C07D333/54 , C07D413/12 , A61K31/17 , C07C275/28 , C07C275/30
CPC分类号: C07D209/48 , C07C275/40 , C07C275/42 , C07C311/21 , C07C311/37 , C07C311/38 , C07C311/46 , C07C311/47 , C07C317/50 , C07C323/44 , C07C335/22 , C07C2603/74 , C07D213/75 , C07D215/38 , C07D217/06 , C07D233/24 , C07D261/18 , C07D277/82 , C07D295/13 , C07D307/14 , C07D333/38 , C07D333/54
摘要: The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C═O, C═S, C═NH, (C═O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.
摘要翻译: 本发明涉及具有式(I)的新的二苯脲或其盐,其中Y是C-O,C-S,C-NH,(C-O)2或SO 2。 以及这些化合物的制备方法及其在治疗原生动物疾病中的用途以及细胞内蛋白质降解途径的抑制是有益的疾病。
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公开(公告)号:US08227516B2
公开(公告)日:2012-07-24
申请号:US11778297
申请日:2007-07-16
申请人: Alexander B. Maurer , Sascha Hoevelmann , Elke Martin , Bernd Hentsch , Michael Gassen , Juergen Kraus , Rolf Krauss , Adam-Spencer Vincek
发明人: Alexander B. Maurer , Sascha Hoevelmann , Elke Martin , Bernd Hentsch , Michael Gassen , Juergen Kraus , Rolf Krauss , Adam-Spencer Vincek
IPC分类号: A61K31/16
CPC分类号: C07C259/04 , C07C2601/08 , C07C2601/14
摘要: The present invention relates to compounds as inhibitors of enzymes having histone deacetylase activity, to the processes for the preparation of those compounds, and to their use for the treatment of diseases which are associated with hypoacetylation of histones and/or other molecules, or in which induction of hyperacetylation has a beneficial effect for example by inhibition of proliferation and/or induction of differentiation and/or induction of apoptosis in transformed cells, such as cancer. Furthermore, the compounds are useful for the treatment of other proliferative diseases, for therapy or prophylaxis of conditions associated with abnormal gene expression.
摘要翻译: 本发明涉及作为具有组蛋白脱乙酰酶活性的酶的抑制剂的化合物,这些化合物的制备方法及其用于治疗与组蛋白和/或其他分子的低乙酰化相关的疾病的用途,或其中 超乙酰化的诱导例如通过抑制转化细胞(例如癌症)的增殖和/或诱导分化和/或诱导细胞凋亡具有有益的作用。 此外,该化合物可用于治疗其他增殖性疾病,用于治疗或预防与异常基因表达相关的病症。
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公开(公告)号:US20050176686A1
公开(公告)日:2005-08-11
申请号:US10624571
申请日:2003-07-23
申请人: Alexander Maurer , Sascha Hoevelmann , Elke Martin , Bernd Hentsch , Michael Gassen , Juergen Kraus , Rolf Krauss , Adam-Spencer Vincek
发明人: Alexander Maurer , Sascha Hoevelmann , Elke Martin , Bernd Hentsch , Michael Gassen , Juergen Kraus , Rolf Krauss , Adam-Spencer Vincek
IPC分类号: A61K31/19 , A61K31/66 , C07C259/04
CPC分类号: C07C259/04 , C07C2601/08 , C07C2601/14
摘要: The present invention is directed to compounds of the general formula (I) or pharmaceutical acceptable salts or physiologically functional derivatives thereof wherein: n is a non-aromatic ring system containing two to seven carbon atoms, wherein the ring system can contain one ore two double bonds; X is C, CH or CH2; Y is selected from C, CH, CH2, S, NR, CH2-CH2, H2C—CH, HC—CH2, C—CH2, H2C—C, or C—C; one or more of the hydrogen atoms can optionally be substituted by one or more substituents R′; each of the dotted lines means a single, a double or triple bond with the exclusion of a combination of a triple with triple bond and a double with a triple bond; R′ is independently H, —CN, alkyl, cycloalkyl, aminoalkyl, alkylamino, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, hydroxyalkylamino, halogene, haloalkyl, haloalkyloxy; R is H, an alkyl or cycloalkyl group; Z is CH, C, or P; p is 0 or 1.
摘要翻译: 本发明涉及通式(I)的化合物或其药学上可接受的盐或生理功能衍生物,其中:n是含有2至7个碳原子的非芳族环系统,其中所述环体系可以包含一个二价双 债券 X是C,CH或CH 2; Y选自C,CH,CH 2,S,NR,CH 2 -CH 2,H 2, C-CH,HC-CH 2,C-CH 2,H 2 CC或CC; 一个或多个氢原子可以任选被一个或多个取代基R'取代; 每个虚线意味着单,双或三键,排除三元组与三键的组合和具有三键的双键; R'独立地是H,-CN,烷基,环烷基,氨基烷基,烷基氨基,烷氧基,-OH,-SH,烷硫基,羟基烷基,羟烷基氨基,卤素基,卤代烷基,卤代烷氧基。 R是H,烷基或环烷基; Z是CH,C或P; p为0或1。
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