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1. 发明申请

WO2005120513A1 PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：蛋白激酶抑制剂
公开(公告)号：WO2005120513A1
公开(公告)日：2005-12-22
申请号：PCT/CH2005/000321
申请日：2005-06-09
申请人： ESBATECH AG , BERSET, Catherine , AUDETAT, Stephan , TIETZ, Julia , GUNDE, Tea , BARBERIS, Alcide , SCHUMACHER, Andreas , TRAXLER, Peter
发明人： BERSET, Catherine , AUDETAT, Stephan , TIETZ, Julia , GUNDE, Tea , BARBERIS, Alcide , SCHUMACHER, Andreas , TRAXLER, Peter
IPC分类号： A61K31/519
CPC分类号： A61K31/519 , A61K31/695
摘要： The present invention relates to the use of compounds for the treatment of disorders involving a protein kinase, preferably a tyrosine kinase. The compounds e.g. have the general formula (I) wherein R 1 , R 2 and R 4 are independently selected from hydrogen, optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, NR 6 R 7 , OR 6 , SR 6 , (CH) m R 6 R 7 , wherein R 6 and R 7 are independently selected from hydrogen, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted aryl, optionally substituted 5- or 6- membered heterocycle, (CH 2 ) n CO(O)R 8 , (CH 2 ) m R' where n = 0, 1, 2, 3, 4 and wherein R 8 is hydrogen, C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted aryl and wherein R' is selected from hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, optionally substituted aryl, halogen, hydroxyl, NO 2 , NH 2 , SO 2 NH 2 , cyano and m is 0, 1, 2, 3, 4; R 3 is hydroxyl, halogen, NH 2 , NO 2 , cyano, SH, optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted aryl, optionally substituted 5- or 6-membered heterocycle, R 5 is selected from C 1 -C 6 alkyl, hydrogen, alkoxy, NH 2 , halogen, cyano, alkine, COOR'' wherein R'' is selected from hydrogen, C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl.
摘要翻译：本发明涉及化合物用于治疗涉及蛋白激酶，优选酪氨酸激酶的病症的用途。化合物例如具有通式（I）其中R 1，R 2和R 4独立地选自氢，任选取代的C 1 -C 6烷基，任选取代的C 3 -C 8环烷基，NR 6 R 7，OR 6，SR 6，（CH）m R 6 R 7，其中R 6和R 7独立地选自氢，任选取代的C 3 -C 8环烷基，任选取代的芳基，任选取代的5-或6-元杂环，（CH 2）n CO（O）R 8，（CH 2）m R'，其中n = 0,1,2,3， 4，并且其中R 8是氢，C 1 -C 6烷基，任选取代的C 3 -C 8环烷基，任选取代的芳基，并且其中R'选自氢，C 1 -C 6烷基，C 1 -C 6烷氧基，任选取代的芳基，卤素，羟基，NO 2 ，NH2，SO2NH2，氰基和m是0,1,2,3,4; R3是羟基，卤素，NH2，NO2，氰基，SH，任选取代的C 1 -C 6烷基，任选取代的C 3 -C 8环烷基，任选取代的芳基，任选取代的5-或6-元杂环，R 5选自C 1 -C 6烷基，氢，烷氧基，NH 2，卤素，氰基，烷基，COOR“，其中R”选自氢，C 1 -C 6烷基，C 3 -C 8环烷基。

2. 发明申请

WO2006111035A1 METHOD FOR THE IDENTIFICATION OF POSSIBLY HARMFUL RECEPTOR TYROSINE KINASE (RTK) MUTATIONS AND OF INHIBITORS OR MEDICATION DIRECTED AGAINST RTK MUTANTSTITLE 审中-公开
标题翻译：识别有效受体酪氨酸激酶（RTK）突变体的方法和针对RTK突变的抑制剂或药物的方法
公开(公告)号：WO2006111035A1
公开(公告)日：2006-10-26
申请号：PCT/CH2006/000212
申请日：2006-04-19
申请人： ESBATECH AG , GUNDE, Tea , BARBERIS, Alcide , BERSET, Catherine
发明人： GUNDE, Tea , BARBERIS, Alcide , BERSET, Catherine
IPC分类号： C12Q1/48 , G01N33/50
CPC分类号： C12Q1/485 , G01N2500/04
摘要： Described is a method for the identification of mutations in a receptor tyrosine kinase leading to a change in activity, said method comprises the steps of providing a host cell comprising a nucleic acid sequence derived from tissue, in particular cancerous tissue, of a particular individual said nucleic acid sequence encoding a polypeptide which comprises an active part of a receptor tyrosine kinase under the control of an inducible promoter, and determining the activity level of said RTK or rather the deviation of the activity from a standard form of the respective RTK, e.g. the wild-type (wt) RTK. Host cells prepared and characterized in the scope of the above defined method may then be used to determine the responsiveness to specific RTK inhibitors and/or to find new RTK inhibitors.
摘要翻译：描述了用于鉴定导致活性变化的受体酪氨酸激酶中的突变的方法，所述方法包括以下步骤：提供宿主细胞，其包含衍生自特定个体的组织，特别是癌组织的核酸序列，编码多肽的核酸序列，其包含在诱导型启动子控制下的受体酪氨酸激酶的活性部分，并确定所述RTK的活性水平，或者确定活性与相应RTK的标准形式的偏差，例如野生型（wt）RTK。然后可以使用在上述定义的方法的范围内制备和表征的宿主细胞来确定对特异性RTK抑制剂的反应性和/或找到新的RTK抑制剂。

3. 发明申请

WO2005040413A1 METHOD FOR THE IDENTIFICATION AND/OR VALIDATION OF RECEPTOR TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：受体酪氨酸激酶抑制剂的鉴定和/或验证方法
公开(公告)号：WO2005040413A1
公开(公告)日：2005-05-06
申请号：PCT/CH2003/000694
申请日：2003-10-24
申请人： ESBATECH AG , GUNDE, Tea , BERSET, Catherine , BARBERIS, Alcide
发明人： GUNDE, Tea , BERSET, Catherine , BARBERIS, Alcide
IPC分类号： C12Q1/48
CPC分类号： C12Q1/485 , G01N2500/00
摘要： An in vivo method for the identification and/or validation of receptor tyrosine kinase inhibitors is described. Said method is characterised by the following steps: a) providing host cells comprising a nucleic acid construct encoding a peptide which comprises a tyrosine kinase domain of a receptor tyrosine kinase wherein said peptide lacks a transmembrane domain or a functional fragment thereof and said tyrosine kinase activity in the cytoplasma leads to proliferation arrest, b) contacting said host cells with a candidate compound and c) identification of inhibitors of said tyrosine kinase activity by cultivation of said host cells under suitable conditions such that the modulation of the tyrosine kinase activity by the candidate compound leads to cell growth.
摘要翻译：描述了用于鉴定和/或验证受体酪氨酸激酶抑制剂的体内方法。所述方法的特征在于以下步骤：a）提供宿主细胞，其包含编码肽的核酸构建体，所述肽包含受体酪氨酸激酶的酪氨酸激酶结构域，其中所述肽缺少跨膜结构域或其功能片段，并且所述酪氨酸激酶活性在细胞质中导致增殖停滞，b）使所述宿主细胞与候选化合物接触，和c）通过在合适的条件下培养所述宿主细胞来鉴定所述酪氨酸激酶活性的抑制剂，使得候选物调节酪氨酸激酶活性化合物导致细胞生长。

4. 发明申请

WO2006131003A1 ANGIOGENESIS INHIBITORS 审中-公开
标题翻译：血管生成抑制剂
公开(公告)号：WO2006131003A1
公开(公告)日：2006-12-14
申请号：PCT/CH2005/000736
申请日：2005-12-09
申请人： ESBATECH AG , BERSET, Catherine , AUDETAT, Stephan , TIETZ, Julia , GUNDE, Tea , BARBERIS, Alcide , SCHUMACHER, Andreas , TRAXLER, Peter
发明人： BERSET, Catherine , AUDETAT, Stephan , TIETZ, Julia , GUNDE, Tea , BARBERIS, Alcide , SCHUMACHER, Andreas , TRAXLER, Peter
IPC分类号： A61K31/519 , A61K31/695 , A61P35/00
CPC分类号： A61K31/519 , A61K31/695
摘要： The present invention relates to the use of compounds for the treatment of angiogenesis related disorders involving a protein kinase as a medicament. The compounds e.g. have the general formula I. In preferred embodiments Rl and R5 are independently selected from hydrogen, halogen, cyano, nitro, CF3 and methyl, R2 and R4 are independently selected from hydrogen, alkyl and NHR7, wherein R7 is optionally substituted aryl, and R3 is optionally substituted C 1 -C 6 alkyl, optionally substituted aryl or optionally substituted 5-or 6-membered heterocycle.
摘要翻译：本发明涉及化合物用于治疗涉及蛋白激酶作为药物的血管生成相关病症的用途。化合物例如具有通式I.在优选实施方案中，R 1和R 5独立地选自氢，卤素，氰基，硝基，CF 3和甲基，R 2和R 4独立地选自氢，烷基和NHR 7，其中R 7是任选取代的芳基，任选取代的C 1 -C 6烷基，任选取代的芳基或任选取代的5-或6-元杂环。

5. 发明申请

WO2009023978A1 PYRAZOLO [3,4 -D] PYRIMIDINE COMPOUNDS AND THEIR USE AS MODULATORS OF PROTEIN KINASE 审中-公开
标题翻译：吡咯并[3,4-D]吡嗪化合物及其作为蛋白激酶调节剂的用途
公开(公告)号：WO2009023978A1
公开(公告)日：2009-02-26
申请号：PCT/CH2008/000348
申请日：2008-08-14
申请人： ONCALIS AG , LÜTHI, Urs , BERSET, Catherine , SCHMID, Gerhard , CAPRARO, Hans-Georg , TRAXLER, Peter Martin
发明人： LÜTHI, Urs , BERSET, Catherine , SCHMID, Gerhard , CAPRARO, Hans-Georg , TRAXLER, Peter Martin
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to pyrazolo[3,4-d]pyrimidine compounds of formula (I) and its salts wherein the substitents are as defined in the specification, their use for the treatment of protein kinase modulation responsive diseases or in the manufacture of pharmaceutical preparations useful in the treatment of said diseases, pharmaceutical preparations, especially useful against said diseases, comprising said compounds and a pharmaceutically acceptable carrier, said compounds for use in the treatment of the animal or human body, especially against said diseases, methods of treatment of the animal or human body comprising administering said compounds to an animal or human, and processes for the manufacture of said compounds.
摘要翻译：本发明涉及式（I）的吡唑并[3,4-d]嘧啶化合物及其盐，其中取代基如本说明书中所定义，其用于治疗蛋白激酶调节反应性疾病或用于制备药物制剂可用于治疗所述疾病，特别可用于所述疾病的药物制剂，其包含所述化合物和药学上可接受的载体，所述化合物用于治疗动物或人体，特别是针对所述疾病，治疗所述疾病的方法动物或人体，包括向动物或人施用所述化合物，以及制备所述化合物的方法。

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