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1. 发明申请

WO2002094796A2 BENZO[G]QUINOXALINE DERIVATIVES AS EFFECTIVE COMPOUNDS AGAINST INFECTIOUS DISEASES 审中-公开
标题翻译：苯并[G]喹啉衍生物作为有效的化合物对抗感染性疾病
公开(公告)号：WO2002094796A2
公开(公告)日：2002-11-28
申请号：PCT/EP2002/005573
申请日：2002-05-21
申请人： AXXIMA PHARMACEUTICALS AG , PATÓ, János , KÉRI, György , ÖRFI, László , WÁCZEK, Frigyes , HORVÁTH, Zoltán , BÁNHEGYI, Péter , SZABADKAI, István , MAROSFALVI, Jenö , HEGYMEGI-BARAKONYI, Bálint , SZÉKELYHIDI, Zsolt , GREFF, Zoltán , CHOIDAS, Axel , BACHER, Gerald , DAUB, Henrik , OBERT, Sabine , KURTENBACH, Alexander , HABENBERGER, Peter
发明人： PATÓ, János , KÉRI, György , ÖRFI, László , WÁCZEK, Frigyes , HORVÁTH, Zoltán , BÁNHEGYI, Péter , SZABADKAI, István , MAROSFALVI, Jenö , HEGYMEGI-BARAKONYI, Bálint , SZÉKELYHIDI, Zsolt , GREFF, Zoltán , CHOIDAS, Axel , BACHER, Gerald , DAUB, Henrik , OBERT, Sabine , KURTENBACH, Alexander , HABENBERGER, Peter
IPC分类号： C07D241/00
CPC分类号： C07D241/38 , C07D231/12 , C07D233/56 , C07D241/52 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D513/14
摘要： The present invention relates to benzo[g]quinoxaline derivatives of the general formula (I), processes for manufacturing said benzo[g]quinoxaline derivatives, the use of the benzo[g]quinoxaline derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases and opportunistic infections, diabetes, cancer, inflammation, as well as compositions containing at least one benzo[g]quinoxaline derivative and/or pharmaceutically acceptable salt thereof. Further, the present invention is directed to methods for preventing and/or treating of infectious diseases, diabetes, cancer, and inflammation using the inventive benzo[g]quinoxaline derivatives.
摘要翻译：本发明涉及通式（I）的苯并[g]喹喔啉衍生物，制备所述苯并[g]喹喔啉衍生物的方法，使用苯并[g]喹喔啉衍生物作为药物活性剂，特别是用于预防和 /或治疗感染性疾病和机会性感染，糖尿病，癌症，炎症，以及含有至少一种苯并[g]喹喔啉衍生物和/或其药学上可接受的盐的组合物。此外，本发明涉及使用本发明的苯并[g]喹喔啉衍生物预防和/或治疗感染性疾病，糖尿病，癌症和炎症的方法。

2. 发明申请

WO2005105097A3 PYRIDOPYRIMIDINES FOR TREATING INFLAMMATORY AND OTHER DISEASES 审中-公开
公开(公告)号：WO2005105097A3
公开(公告)日：2005-11-10
申请号：PCT/EP2005/051892
申请日：2005-04-27
申请人： GPC BIOTECH AG , DAUB, Henrik , WISSING, Josef , MISSIO, Andrea , KLEBL, Bert
发明人： DAUB, Henrik , WISSING, Josef , MISSIO, Andrea , KLEBL, Bert
IPC分类号： A61K31/513 , A61P29/00 , A61P37/00
摘要： The present invention relates to the use of pyridopyrimidine derivatives having the general formula (I) wherein X represents =NH, =N-Acyl, =O, or =S; R 1 represents -NR 3 R 4 , -SR 3 , -SO-R 3 , -SO 2 -R 3 , -OR 3 ; R 2 , R 3 , and R 4 are independently of each other hydrogen, -(CH 2 ) n Ph*, heteroaryl, C 3 -C 7 -cycloalkyl, C 1 -C 6 -alkyl, C 1 -C 6 -alkanoyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR 5 R 6 , phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R 5 and R 6 are independently of each other hydrogen, (CH 2 ) n Ph*, heteroaryl, C 3 -C 7 -cycloalkyl, C 1 -C 6 -alkyl, C 1 -C 6 -alkanoyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl; R 5 and R 6 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ph* represents phenyl or substituted phenyl; n is 0, 1, 2, or 3; R 4 can optionally be -CO-R 3 , -CO-OR 3 , -SO 2 -R 3 , -SO 2 -NR 5 R 6 , -CO-NR 5 R 6 , -CS-NR 5 R 6 , -C(=NH)-R 3 , -C(=NH)-NR 5 R 6 ; R 3 and R 4 can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ar represents phenyl, substituted phenyl, or heteroaryl; and pharmaceutically acceptable salts thereof for prophylaxis and/or treatment of inflammatory diseases, neurodegenerative disorders, immunological diseases, neuroimmunological diseases, autoimmune diseases, diabetes, transplant rejection, infective diseases, prion diseases, cardiovascular diseases and disorders.

3. 发明申请

WO2005105097A2 PYRIDOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡啶衍生物衍生物
公开(公告)号：WO2005105097A2
公开(公告)日：2005-11-10
申请号：PCT/EP2005051892
申请日：2005-04-27
申请人： GPC BIOTECH AG , DAUB HENRIK , WISSING JOSEF , MISSIO ANDREA , KLEBL BERT
发明人： DAUB HENRIK , WISSING JOSEF , MISSIO ANDREA , KLEBL BERT
IPC分类号： A61K31/513 , A61P29/00 , A61P37/00
CPC分类号： A61K31/513
摘要： The present invention relates to the use of pyridopyrimidine derivatives having the general formula (I) wherein X represents =NH, =N-Acyl, =O, or =S; R represents -NR R , -SR , -SO-R , -SO2-R , -OR ; R , R , and R are independently of each other hydrogen, -(CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR R , phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R and R are independently of each other hydrogen, (CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; R and R can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ph* represents phenyl or substituted phenyl; n is 0, 1, 2, or 3; R can optionally be -CO-R , -CO-OR , -SO2-R , -SO2-NR R , -CO-NR R , -CS-NR R , -C(=NH)-R , -C(=NH)-NR R ; R and R can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ar represents phenyl, substituted phenyl, or heteroaryl; and pharmaceutically acceptable salts thereof for prophylaxis and/or treatment of inflammatory diseases, neurodegenerative disorders, immunological diseases, neuroimmunological diseases, autoimmune diseases, diabetes, transplant rejection, infective diseases, prion diseases, cardiovascular diseases and disorders.
摘要翻译：本发明涉及具有通式（I）的吡啶并嘧啶衍生物的用途，其中X表示= NH，= N-酰基，= O或= S; R 1表示-NR 3 R 4，-SR 3，-SO-R 3，-SO 2 -R 3，-OR 3; R 2，R 3和R 4彼此独立地为氢， - （CH 2）n Ph *，杂芳基，C 3 -C 7 - 环烷基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷酰基，C 2 C 1-6 - 烯基，C 2 -C 6 - 炔基; 其中环烷基，烷基，烷酰基，烯基，炔基残基可以任选被一个或多个下列基团取代：-NR 5 R 6，苯基，取代的苯基，硫代烷基，烷氧基，羟基，羧基，卤素，环烷基 ; R 5和R 6彼此独立地为氢，（CH 2）n Ph *，杂芳基，C 3 -C 7 - 环烷基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷酰基，C 2 -C 6 - 烯基， C6炔基; R 5和R 6可以与它们所连接的氮一起连接，以形成具有3至7个碳原子的环，任选地含有1,2或3个选自氮，氧和硫的杂原子; Ph *表示苯基或取代的苯基; n为0,1,2或3; R 4可以任选地是-CO-R 3，-CO-OR 3，-SO 2 -R 3，-SO 2 -NR 5 R 6，-CO-NR 5， R 6，-C 6 -NR 5 R 6，-C（= NH）-R 3，-C（= NH）-NR 5 R 6; R 3和R 4可以与它们所连接的氮一起连接，以形成具有3-7个碳原子的环，任选地含有1,2或3个选自氮，氧和硫的杂原子; Ar表示苯基，取代的苯基或杂芳基; 用于预防和/或治疗炎性疾病，神经变性疾病，免疫疾病，神经免疫疾病，自身免疫疾病，糖尿病，移植排斥，感染性疾病，朊病毒疾病，心血管疾病和病症的药学上可接受的盐。

4. 发明申请

WO2004005264A2 IMIDAZOLE COMPOUNDS AND HUMAN CELLULAR PROTEINS CASEIN KINASE I ALPHA, DELTA AND EPSILON AS TARGETS FOR MEDICAL INTERVENTION AGAINST HEPATITIS C VIRUS INFECTIONS 审中-公开
标题翻译：用于治疗丙型肝炎病毒感染的咪唑化合物
公开(公告)号：WO2004005264A2
公开(公告)日：2004-01-15
申请号：PCT/EP2003/007286
申请日：2003-07-07
申请人： AXXIMA PHARMACEUTICALS AG , SALASSIDIS, Konstadinos , KURTENBACH, Alexander , DAUB, Henrik , OBERT, Sabine
发明人： SALASSIDIS, Konstadinos , KURTENBACH, Alexander , DAUB, Henrik , OBERT, Sabine
IPC分类号： C07D233/64
CPC分类号： C07D233/64 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention describes novel imidazole compounds, which are particularly useful against Hepatitis C Virus infections and diseases associated therewith. Furthermore, the invention relates to the human cellular proteins casein kinase I alpha (α), delta (δ), and epsilon (ε) as targets for medical intervention against Hepatitis C Virus (HCV) infections and diseases. In addition, the present invention refers to a method for the identification of compounds which are useful for the prophylaxis and/or treatment of infections and diseases caused by Hepatitis C Virus, methods for treating Hepatitis C Virus infections and diseases, as well as pharmaceutical compositions useful for the prophylaxis and/or treatment of Hepatitis C Virus infections and diseases. Moreover, disclosed are antibodies, oligonucleotides and specific compounds which are effective for the detection, prophylaxis and/or treatment of infections and diseases caused by Hepatitis C Virus. In addition, the present invention describes solid supports useful for the identification of compounds suitable for preventing and/or treating infections and diseases caused by said Hepatitis C Virus.
摘要翻译：本发明描述了新颖的咪唑化合物，其特别适用于丙型肝炎病毒感染和与之相关的疾病。此外，本发明涉及作为针对丙型肝炎病毒（HCV）感染和疾病的医学干预的靶标的人细胞蛋白酪蛋白激酶Iα（α），δ（delta）和ε（ε）。此外，本发明涉及用于鉴定可用于预防和/或治疗由丙型肝炎病毒引起的感染和疾病的化合物的方法，用于治疗丙型肝炎病毒感染和疾病的方法以及药物组合物可用于预防和/或治疗丙型肝炎病毒感染和疾病。此外，公开了对丙型肝炎病毒引起的感染和疾病的检测，预防和/或治疗有效的抗体，寡核苷酸和特异性化合物。此外，本发明描述了可用于鉴定适合于预防和/或治疗由所述丙型肝炎病毒引起的感染和疾病的化合物的固体支持物。

5. 发明申请

WO2009043829A1 PROTEOME-WIDE QUANTIFICATION OF SMALL MOLECULE BINDING TO CELLULAR TARGET PROTEINS 审中-公开
标题翻译：小分子结合细胞靶向蛋白的广泛定量
公开(公告)号：WO2009043829A1
公开(公告)日：2009-04-09
申请号：PCT/EP2008/062979
申请日：2008-09-26
申请人： MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V. , DAUB, Henrik , BAIRLEIN, Michaela , SHARMA, Kirti , GODL, Klaus , TEBBE, Andreas , WEBER, Christoph
发明人： DAUB, Henrik , BAIRLEIN, Michaela , SHARMA, Kirti , GODL, Klaus , TEBBE, Andreas , WEBER, Christoph
IPC分类号： C12Q1/48 , G01N33/543 , G01N33/68
CPC分类号： G01N33/54306 , C12Q1/485 , G01N30/6043 , G01N30/7233 , G01N30/8675 , G01N33/6851
摘要： This invention relates to methods for the evaluation and/or quantification of the binding affinity of small molecules or other compounds to target components contained within an analyte, such as target proteins contained within the proteome of a cell or tissue.
摘要翻译：本发明涉及用于评估和/或定量小分子或其它化合物对分析物中所含的靶组分（例如包含在细胞或组织的蛋白质组中的靶蛋白）的结合亲和力的方法。

6. 发明申请

WO2004013633A2 MEDIUM AND METHOD FOR ENRICHING, PURIFYING OR DEPLETING ATP BINDING PROTEINS FROM A POOL OF PROTEINS 审中-公开
标题翻译：从蛋白质池中增殖，净化或减少ATP结合蛋白的培养基和方法
公开(公告)号：WO2004013633A2
公开(公告)日：2004-02-12
申请号：PCT/EP2003/008375
申请日：2003-07-29
申请人： AXXIMA PHARMACEUTICALS AG , GODL, Klaus , MISSIO, Andrea , DAUB, Henrik , STEIN-GERLACH, Matthias , GREFF, Zoltan
发明人： GODL, Klaus , MISSIO, Andrea , DAUB, Henrik , STEIN-GERLACH, Matthias , GREFF, Zoltan
IPC分类号： G01N33/68
CPC分类号： G01N33/573 , A61K38/00 , C07D401/04 , C07D401/14 , C07K1/22 , G01N33/6803 , G01N2333/91205
摘要： The present invention relates to a medium and a method for enriching ATP binding proteins, e.g. proteinkinases, from a pool of proteins, like a proteome. The medium of the present invention comprises specific inhibitors, e.g. at least one of the compounds 4-[4-(4-fluoro-phenyl)-5-pyridine-4-yl-l H -imidazole-2-yl]-benzylamine, 2-[4-(2-Amino-ethoxy)- phenylamino]-6-(2,6-dichloro-phenyl)-8-methyl-8 H -pyrido[2,3-d]pyrimidine-7-one, 2-[1-(3-aminopropyl)-1 H -indole-3-yl)maleimide, 3-[1-(3-Aminopropyl)-1 H -indol-3-yl]-3-(1 H -indol 3-yl)-maleinmide, 3-[1-(3-Aminopropyl)-1 H -indol-3-yl]-4-(1-methyl-l H -indol-3-yl) maleinimide, 3-(8-Aminomethyl-6,7,8,9-tetrahydropyrido-[1,2- a ]-indol-10-yl)-4-(1-methyl-l H -indol -3-y1)-maleinmide, [6-(3-Amino-propoxy)-methoxy-quinazolin-4-yl]-(3-chloro-phenyl)-amine, 6-(3-Amino-propoxy)-7-methoxy-quinazolin-4-yl-(3-chloro-4-fluoro-phenyl)-amine, 6-(3Amino-propoxy)-7-methoxy-quinazolin-4-yl]-(3-bromo-phenyl)-amine and 4-[4-(4-Amino-butyl)-piperazin-l-yl-methyl]- N -[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide immobilized on a support material. According to the method of the present invention the above-mentioned immobilized compounds are used to selectively bind protein kinases from a pool of heterogeneous proteins.
摘要翻译：本发明涉及一种培养基和一种富含ATP结合蛋白的方法，蛋白质蛋白酶，来自蛋白质库，如蛋白质组。本发明的培养基包含特异性抑制剂，例如， 4- [4-（4-氟 - 苯基）-5-吡啶-4-基-1H-咪唑-2-基] - 苄胺中的至少一种化合物，2- [4-（2-氨基 - 乙氧基） - 苯基氨基] -6-（2,6-二氯 - 苯基）-8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮，2- [1-（3-氨基丙基）-1H-吲哚 -3-基）马来酰亚胺，3- [1-（3-氨基丙基）-1H-吲哚-3-基] -3-（1H-吲哚-3-基） - 马来酰亚胺，3- [1-（3-氨基丙基） -1H-吲哚-3-基] -4-（1-甲基-1H-吲哚-3-基）马来酰亚胺，3-（8-氨基甲基-6,7,8,9-四氢吡啶并[1,2-a ] - （1-甲基-1H-吲哚-3-基） - 马来酰胺，[6-（3-氨基 - 丙氧基） - 甲氧基 - 喹唑啉-4-基] - （3- 苯基） - 胺，6-（3-氨基 - 丙氧基）-7-甲氧基 - 喹唑啉-4-基 - （3-氯-4-氟 - 苯基） - 胺，6-（3Amino-丙氧基） - -7-甲氧基 - 喹唑啉-4-基] - （3-溴 - 苯基） - 胺和4- [4-（4-氨基 - 丁基） - 哌嗪-1-基 - 甲基] -N- [4-甲基 - 3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺固定在载体材料上。根据本发明的方法，上述固定化化合物用于选择性地结合来自异质蛋白库的蛋白激酶。

7. 发明申请

WO2006021458A3 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO2006021458A3
公开(公告)日：2007-04-12
申请号：PCT/EP2005009291
申请日：2005-08-29
申请人： GPC BIOTECH AG , KLEBL BERT , BAUMANN MATTHIAS , HOPPE EDMUND , BREHMER DIRK , DAUB HENRIK , KERI GYOERGY , VARGA ZOLTAN , MAROSFALVI JENOE , OERFI LASZLO
发明人： KLEBL BERT , BAUMANN MATTHIAS , HOPPE EDMUND , BREHMER DIRK , DAUB HENRIK , KERI GYOERGY , VARGA ZOLTAN , MAROSFALVI JENOE , OERFI LASZLO
IPC分类号： C07D239/42 , A61K31/506 , A61P37/08 , C07D401/04 , C07D401/10 , C07D401/14
CPC分类号： C07D239/42 , C07D401/04 , C07D401/10 , C07D401/14
摘要： The present invention relates to pyrimidine derivatives, methods for their synthesis, and the use of said pyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferation disorders, cancer, leukemia, erectile dysfunction, cardiovascular diseases and disorders, inflammatory diseases, transplant rejection, immunological diseases, neuroimmunological diseases, autoimmune diseases, infective diseases including opportunistic infections, prion diseases and/or neuro-degeneration. Furthermore, the present invention relates to pharmaceutical compositions containing at least one pyrimidine derivative and/or pharmaceutically acceptable salts thereof as an active ingredient together with at least one pharmaceutically acceptable carrier, excipient or diluents as well as to methods for prophylaxis and/or treatment of the above-mentioned diseases and disorders.
摘要翻译：本发明涉及嘧啶衍生物，其合成方法和所述嘧啶衍生物作为药物活性剂的用途，特别是用于预防和/或治疗细胞增殖障碍，癌症，白血病，勃起功能障碍，心血管疾病和病症，炎症性疾病，移植排斥反应，免疫疾病，神经免疫疾病，自身免疫疾病，感染性疾病，包括机会性感染，朊病毒疾病和/或神经变性。此外，本发明涉及含有至少一种嘧啶衍生物和/或其药学上可接受的盐作为活性成分以及至少一种药学上可接受的载体，赋形剂或稀释剂的药物组合物，以及用于预防和/或治疗上述疾病和障碍。

8. 发明申请

WO2006021458A2 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO2006021458A2
公开(公告)日：2006-03-02
申请号：PCT/EP2005/009291
申请日：2005-08-29
申请人： GPC BIOTECH AG , KLEBL, Bert , BAUMANN, Matthias , HOPPE, Edmund , BREHMER, Dirk , DAUB, Henrik , KÉRI, György , VARGA, Zoltán , MAROSFALVI, Jenö , ÖRFI, László
发明人： KLEBL, Bert , BAUMANN, Matthias , HOPPE, Edmund , BREHMER, Dirk , DAUB, Henrik , KÉRI, György , VARGA, Zoltán , MAROSFALVI, Jenö , ÖRFI, László
CPC分类号： C07D239/42 , C07D401/04 , C07D401/10 , C07D401/14
摘要： The present invention relates to pyrimidine derivatives, methods for their synthesis, and the use of said pyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferation disorders, cancer, leukemia, erectile dysfunction, cardiovascular diseases and disorders, inflammatory diseases, transplant rejection, immunological diseases, neuroimmunological diseases, autoimmune diseases, infective diseases including opportunistic infections, prion diseases and/or neuro-degeneration. Furthermore, the present invention relates to pharmaceutical compositions containing at least one pyrimidine derivative and/or pharmaceutically acceptable salts thereof as an active ingredient together with at least one pharmaceutically acceptable carrier, excipient or diluents as well as to methods for prophylaxis and/or treatment of the above-mentioned diseases and disorders.
摘要翻译：本发明涉及嘧啶衍生物，其合成方法和所述嘧啶衍生物作为药物活性剂的用途，特别是用于预防和/或治疗细胞增殖障碍，癌症，白血病，勃起功能障碍，心血管疾病和病症，炎症性疾病，移植排斥反应，免疫疾病，神经免疫疾病，自身免疫疾病，感染性疾病，包括机会性感染，朊病毒疾病和/或神经变性。此外，本发明涉及含有至少一种嘧啶衍生物和/或其药学上可接受的盐作为活性成分以及至少一种药学上可接受的载体，赋形剂或稀释剂的药物组合物，以及用于预防和/或治疗上述疾病和障碍。

9. 发明申请

WO2004013633A3 METHOD FOR ISOLATING ATP BINDING PROTEINS BY MEANS OF IMMOBOLIZED PROTEIN INHIBITORS 审中-公开
标题翻译：通过免疫蛋白抑制剂分离ATP结合蛋白的方法
公开(公告)号：WO2004013633A3
公开(公告)日：2004-10-28
申请号：PCT/EP0308375
申请日：2003-07-29
申请人： AXXIMA PHARMACEUTICALS AG , GODL KLAUS , MISSIO ANDREA , DAUB HENRIK , STEIN-GERLACH MATTHIAS , GREFF ZOLTAN , KLEBL BERT , ORFI LASZLO , KERI GYOERGY , VARGA ZOLTAN
发明人： GODL KLAUS , MISSIO ANDREA , DAUB HENRIK , STEIN-GERLACH MATTHIAS , GREFF ZOLTAN , KLEBL BERT , ORFI LASZLO , KERI GYOERGY , VARGA ZOLTAN
IPC分类号： A61K38/00 , C07D239/72 , C07D401/04 , C07D401/14 , C07K1/22 , G01N33/573 , G01N33/68
CPC分类号： G01N33/573 , A61K38/00 , C07D401/04 , C07D401/14 , C07K1/22 , G01N33/6803 , G01N2333/91205
摘要： The present invention relates to a medium and a method for enriching ATP binding proteins, e.g. proteinkinases, from a pool of proteins, like a proteome. The medium of the present invention comprises specific inhibitors, e.g. at least one of the compounds 4-[4-(4-fluoro-phenyl)-5-pyridine-4-yl-lH-imidazole-2-yl]-benzylamine, 2-[4-(2-Amino-ethoxy)- phenylamino]-6-(2,6-dichloro-phenyl)-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one, 2-[1-(3-aminopropyl)-1H-indole-3-yl)maleimide, 3-[1-(3-Aminopropyl)-1H-indol-3-yl]-3-(1H-indol 3-yl)-maleinmide, 3-[1-(3-Aminopropyl)-1H-indol-3-yl]-4-(1-methyl-lH-indol-3-yl) maleinimide, 3-(8-Aminomethyl-6,7,8,9-tetrahydropyrido-[1,2-a]-indol-10-yl)-4-(1-methyl-lH-indol -3-y1)-maleinmide, [6-(3-Amino-propoxy)-methoxy-quinazolin-4-yl]-(3-chloro-phenyl)-amine, 6-(3-Amino-propoxy)-7-methoxy-quinazolin-4-yl-(3-chloro-4-fluoro-phenyl)-amine, 6-(3Amino-propoxy)-7-methoxy-quinazolin-4-yl]-(3-bromo-phenyl)-amine and 4-[4-(4-Amino-butyl)-piperazin-l-yl-methyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide immobilized on a support material. According to the method of the present invention the above-mentioned immobilized compounds are used to selectively bind protein kinases (e.g. p38, JNK1, JNK2, CK18, RICK, GAK) from a pool of heterogeneous proteins.
摘要翻译：本发明涉及一种培养基和一种富含ATP结合蛋白的方法，蛋白质蛋白酶，来自蛋白质库，如蛋白质组。本发明的培养基包含特异性抑制剂，例如， 4- [4-（4-氟 - 苯基）-5-吡啶-4-基-1H-咪唑-2-基] - 苄胺中的至少一种化合物，2- [4-（2-氨基 - 乙氧基） - 苯基氨基] -6-（2,6-二氯 - 苯基）-8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮，2- [1-（3-氨基丙基）-1H-吲哚 -3-基）马来酰亚胺，3- [1-（3-氨基丙基）-1H-吲哚-3-基] -3-（1H-吲哚-3-基） - 马来酰亚胺，3- [1-（3-氨基丙基） -1H-吲哚-3-基] -4-（1-甲基-1H-吲哚-3-基）马来酰亚胺，3-（8-氨基甲基-6,7,8,9-四氢吡啶并[1,2-a ] - （1-甲基-1H-吲哚-3-基） - 马来酰胺，[6-（3-氨基 - 丙氧基） - 甲氧基 - 喹唑啉-4-基] - （3- 苯基） - 胺，6-（3-氨基 - 丙氧基）-7-甲氧基 - 喹唑啉-4-基 - （3-氯-4-氟 - 苯基） - 胺，6-（3Amino-丙氧基） - -7-甲氧基 - 喹唑啉-4-基] - （3-溴 - 苯基） - 胺和4- [4-（4-氨基 - 丁基） - 哌嗪-1-基 - 甲基] -N- [4-甲基 - 3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺固定在载体材料上。根据本发明的方法，上述固定化化合物用于选择性地结合蛋白激酶（例如p38，JNK1，JNK2，CK18，RICK，GAK）从异源蛋白质库中。

10. 发明申请

WO2004005264A3 IMIDAZOLE COMPOUNDS FOR THE TREATMENT OF HEPATITIS C VIRUS INFECTIONS 审中-公开
标题翻译：咪唑类化合物治疗丙型肝炎病毒感染
公开(公告)号：WO2004005264A3
公开(公告)日：2004-03-04
申请号：PCT/EP0307286
申请日：2003-07-07
申请人： AXXIMA PHARMACEUTICALS AG , SALASSIDIS KONSTADINOS , KURTENBACH ALEXANDER , DAUB HENRIK , OBERT SABINE , GREFF ZOLTAN , KERI GYOERGY , OERFI LASZLO , WACZEK FRIGYES
发明人： SALASSIDIS KONSTADINOS , KURTENBACH ALEXANDER , DAUB HENRIK , OBERT SABINE , GREFF ZOLTAN , KERI GYOERGY , OERFI LASZLO , WACZEK FRIGYES
IPC分类号： A61K31/4178 , A61P31/20 , C07D233/54 , C07D233/64 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
CPC分类号： C07D233/64 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention describes novel imidazole compounds, which are particularly useful against Hepatitis C Virus infections and diseases associated therewith. Furthermore, the invention relates to the human cellular proteins casein kinase I alpha (alpha), delta (delta), and epsilon (ϵ) as targets for medical intervention against Hepatitis C Virus (HCV) infections and diseases. In addition, the present invention refers to a method for the identification of compounds which are useful for the prophylaxis and/or treatment of infections and diseases caused by Hepatitis C Virus, methods for treating Hepatitis C Virus infections and diseases, as well as pharmaceutical compositions useful for the prophylaxis and/or treatment of Hepatitis C Virus infections and diseases. Moreover, disclosed are antibodies, oligonucleotides and specific compounds which are effective for the detection, prophylaxis and/or treatment of infections and diseases caused by Hepatitis C Virus. In addition, the present invention describes solid supports useful for the identification of compounds suitable for preventing and/or treating infections and diseases caused by said Hepatitis C Virus.
摘要翻译：本发明描述了新的咪唑化合物，其特别可用于抗丙型肝炎病毒感染和与之相关的疾病。此外，本发明涉及作为针对丙型肝炎病毒（HCV）感染和疾病的医学干预的靶标的人细胞蛋白质酪蛋白激酶Iα（α），δ（δ）和ε（ε）。此外，本发明涉及鉴定可用于预防和/或治疗由丙型肝炎病毒引起的感染和疾病的化合物的方法，治疗丙型肝炎病毒感染和疾病的方法，以及药物组合物用于预防和/或治疗丙型肝炎病毒感染和疾病。此外，公开了对检测，预防和/或治疗由丙型肝炎病毒引起的感染和疾病有效的抗体，寡核苷酸和特定化合物。此外，本发明描述了用于鉴定适合于预防和/或治疗由所述丙型肝炎病毒引起的感染和疾病的化合物的固体支持物。

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