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1. 发明申请

WO2002082329A2 METHOD FOR GENERATING A QUANTITATIVE STRUCTURE PROPERTY ACTIVITY RELATIONSHIP 审中-公开
标题翻译：产生定量结构属性活动关系的方法
公开(公告)号：WO2002082329A2
公开(公告)日：2002-10-17
申请号：PCT/EP2002/003622
申请日：2002-04-02
申请人： AXXIMA PHARMACEUTICALS AG , KÖVESDI, István , KÉRI, György , ÖRFI, László
发明人： KÖVESDI, István , KÉRI, György , ÖRFI, László
IPC分类号： G06F17/50
CPC分类号： G06F19/704 , G06F19/707
摘要： The present invention relates to a method for generating a quantitative structure property activity relationship (QSPAR) between the structure of chemical compounds and their pharmacological activity. Said method comprises the steps of establishing at least one database containing molecular descriptors especially 2D and/or 3D biological/physical/chemical data; selecting significant descriptors according to their influence to said structure property activity relationship; providing at least a model for generating a quantitative structure property activity relationship; verifying said model by the use of at least one quality parameter; and repeating steps b, c, and d until said quality parameter reaches a predetermined value. The method is especially useful for the correlation of chemical compounds with large differences in structure. Furthermore, a system for generating a quantitative structure property activity relationship (QSPAR) between the structure of chemical compounds and their pharmacological activity is disclosed.
摘要翻译：本发明涉及化学化合物结构与其药理活性之间产生定量结构性质活性关系（QSPAR）的方法。所述方法包括以下步骤：建立包含分子描述符，特别是2D和/或3D生物/物理/化学数据的至少一个数据库; 根据其对所述结构性能活动关系的影响选择重要描述符; 提供至少一个用于产生定量结构性质活动关系的模型; 通过使用至少一个质量参数验证所述模型; 并重复步骤b，c和d直到所述质量参数达到预定值。该方法对结构差异较大的化合物的相关性特别有用。此外，公开了一种用于在化学结构结构与其药理活性之间产生定量结构性质活性关系（QSPAR）的系统。

2. 发明申请

WO2002082329A3 METHOD FOR GENERATING A QUANTITATIVE STRUCTURE PROPERTY ACTIVITY RELATIONSHIP 审中-公开
公开(公告)号：WO2002082329A3
公开(公告)日：2002-10-17
申请号：PCT/EP2002/003622
申请日：2002-04-02
申请人： AXXIMA PHARMACEUTICALS AG , KÖVESDI, István , KÉRI, György , ÖRFI, László
发明人： KÖVESDI, István , KÉRI, György , ÖRFI, László
IPC分类号： G06F19/00
摘要： The present invention relates to a method for generating a quantitative structure property activity relationship (QSPAR) between the structure of chemical compounds and their pharmacological activity. Said method comprises the steps of establishing at least one database containing molecular descriptors especially 2D and/or 3D biological/physical/chemical data; selecting significant descriptors according to their influence to said structure property activity relationship; providing at least a model for generating a quantitative structure property activity relationship; verifying said model by the use of at least one quality parameter; and repeating steps b, c, and d until said quality parameter reaches a predetermined value. The method is especially useful for the correlation of chemical compounds with large differences in structure. Furthermore, a system for generating a quantitative structure property activity relationship (QSPAR) between the structure of chemical compounds and their pharmacological activity is disclosed.

3. 发明申请

WO2002094796A3 BENZO[G]QUINOXALINE DERIVATIVES AS EFFECTIVE COMPOUNDS AGAINST INFECTIOUS DISEASES 审中-公开
公开(公告)号：WO2002094796A3
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： C07D241/38
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.

4. 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。

5. 发明申请

WO2010100515A2 FRACTIONS OF WHEAT GERM FERMENT 审中-公开
标题翻译：小麦胚芽发酵的部分
公开(公告)号：WO2010100515A2
公开(公告)日：2010-09-10
申请号：PCT/HU2010/000026
申请日：2010-03-05
申请人： HIDVÉGI, Máté , BENCZE, Gyula , KÉRI, György , ÖRFI, László
发明人： HIDVÉGI, Máté , BENCZE, Gyula , KÉRI, György , ÖRFI, László
IPC分类号： A61K36/899 , A61P37/02 , A61P37/04 , A61P35/00
CPC分类号： A61K36/899
摘要： The invention concerns wheat germ ferment, its biologically active fractions, the process for their production, the pharmaceutical preparations containing them and their uses.
摘要翻译：本发明涉及小麦胚芽发酵，其生物活性级分，其生产方法，含有它们的药物制剂及其用途。

6. 发明申请

WO2011077171A1 4-PHENYLAMINO-PYRIMIDINE DERIVATIVES HAVING PROTEIN KINASE INHIBITOR ACTIVITY 审中-公开
标题翻译：具有蛋白激酶抑制剂活性的4-苯基氨基吡啶衍生物
公开(公告)号：WO2011077171A1
公开(公告)日：2011-06-30
申请号：PCT/HU2010/000145
申请日：2010-12-17
申请人： VICHEM CHEMIE KUTATÓ KFT. , GREFF, Zoltán , VARGA, Zoltán , KÉRI, György , NÉMETH, Gábor , ÖRFI, László , SZÁNTAI KIS, Csaba
发明人： GREFF, Zoltán , VARGA, Zoltán , KÉRI, György , NÉMETH, Gábor , ÖRFI, László , SZÁNTAI KIS, Csaba
IPC分类号： C07D239/42 , C07D401/04 , C07D403/04 , C07D403/14 , C07D409/14 , A61K31/505 , A61K31/506 , A61P9/00 , A61P29/00 , A61P31/00 , A61P35/00
CPC分类号： C07D239/42 , C07D401/04 , C07D403/04 , C07D403/14 , C07D409/14
摘要： The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1 is halogen, vinylene-aryl, substituted aryl, heteroaryl or a benzo[1,3]dioxolil group, W is a group of formula -NH-SO2-R2 or heteroaryl group or NHR3 group where R3 is hydrogen or heteroaryl; and n is 1, 2, 3 or 4. Furthermore, the present invention is directed to pharmaceutical composition containing at least one compound of general formula (I) and/or pharmaceutically acceptable salts or solvates thereof and for the use of them for the preparation of pharmaceutical compositions for the prophylaxis and/or the treatment of protein kinase related, especially CDK9-related diseases e.g. cell proliferative disease, infectious disease, pain, cardiovascular disease and inflammation.
摘要翻译：本发明涉及通式（I）的化合物及其药学上可接受的盐和溶剂化物，其中R 1是卤素，亚乙烯基 - 芳基，取代的芳基，杂芳基或苯并[1,3]二氧杂环戊烷基，W是式-NH- SO 2 -R 2或杂芳基或NHR 3基团，其中R 3是氢或杂芳基; 此外，本发明涉及含有至少一种通式（I）的化合物和/或其药学上可接受的盐或溶剂化物的药物组合物，并且用于制备它们用于预防和/或治疗蛋白激酶相关的药物组合物，特别是CDK9相关疾病，例如细胞增殖性疾病，感染性疾病，疼痛，心血管疾病和炎症。

7. 发明申请

WO2006089874A1 BENZO[2,3]AZEPINO[4,5-B]INDOL-6-ONES 审中-公开
标题翻译：苯并[2,3]氮杂并[4,5-b]吲哚-6-酮
公开(公告)号：WO2006089874A1
公开(公告)日：2006-08-31
申请号：PCT/EP2006/060100
申请日：2006-02-20
申请人： GPC BIOTECH AG , KLEBL, Bert , NEUMANN, Lars , HAFENBRADL, Doris , GREFF, Zoltán , KÉRI, György , ÖRFI, László
发明人： KLEBL, Bert , NEUMANN, Lars , HAFENBRADL, Doris , GREFF, Zoltán , KÉRI, György , ÖRFI, László
IPC分类号： C07D487/04 , A61K31/55 , A61P25/00 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to benzo[2,3]azepino[4,5-b]indol-6-ones of the general formula (I): and pharmaceutically acceptable salts thereof, the use of these compounds as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke. Furthermore, the present invention is directed towards pharmaceutical composition containing at least one of the benzo[2,3]azepino[4,5-b]indol-6-ones and/or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及通式（I）的苯并[2,3]氮杂环庚烯并[4,5-b]吲哚-6-酮及其药学上可接受的盐，这些化合物作为药物活性剂的用途，特别是传染病，包括机会性疾病，朊病毒疾病，免疫疾病，自身免疫疾病，双相和临床病症，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经退行性疾病和中风的预防和/或治疗。此外，本发明涉及含有至少一种苯并[2,3]氮杂环庚烷并[4,5-b]吲哚-6-酮和/或其药学上可接受的盐的药物组合物。

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

WO2011045084A1 QUINOLINYLOXYPHENYLSULFONAMIDES 审中-公开
公开(公告)号：WO2011045084A1
公开(公告)日：2011-04-21
申请号：PCT/EP2010/006525
申请日：2010-10-16
申请人： MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V. , ULLRICH, Axel , TORKA, Robert , ZHANG, Yixiang , KÉRI, György , ÖRFI, László , SZABADKAI, István
发明人： ULLRICH, Axel , TORKA, Robert , ZHANG, Yixiang , KÉRI, György , ÖRFI, László , SZABADKAI, István
IPC分类号： C07D215/20 , C07D409/12 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/14 , A61K31/47 , A61K31/4709 , A61P35/00 , A61P35/04
CPC分类号： C07D417/12 , C07D215/20 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.
摘要翻译：本发明涉及这些喹啉氧基苯基磺酰胺化合物的喹啉氧基苯磺酰胺和立体异构形式，溶剂合物，水合物和/或药学上可接受的盐，以及含有至少一种这些化合物以及至少一种药学上可接受的载体，赋形剂和/或稀释剂的药物组合物。所述喹啉氧基苯基磺酰胺可用于预防，治疗和/或治疗过度增殖性疾病，如癌症，肿瘤，特别是癌症转移。

10. 发明申请

WO2009104027A1 THERAPEUTIC APPLICATION OF TRICICLIC AROMATIC AND SATURATED BENZO(4,5)THIENO-(2,3-D)PYRIMIDINE DERIVATES, AS WELL AS THEIR THERAPEUTICALLY ACCEPTABLE SALTS 审中-公开
标题翻译： TRICICLIC AROMATIC AND SATURATED BENZO（4,5）THIENO-（2,3-D）PYRIMININE DERIVATES的治疗应用，作为其治疗方案可接受的口服
公开(公告)号：WO2009104027A1
公开(公告)日：2009-08-27
申请号：PCT/HU2008/000017
申请日：2008-02-19
申请人： VICHEM CHEMIE KUTATÓ KFT , BÁNHEGYI, Péter , KÉRI, György , ÖRFI, László , SZÉKELYHIDI, Zsolt , WÁCZEK, Frigyes
发明人： BÁNHEGYI, Péter , KÉRI, György , ÖRFI, László , SZÉKELYHIDI, Zsolt , WÁCZEK, Frigyes
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D495/04
摘要： The subject of the invention is therapeutic application of tricyclic aromatic and saturated benzo[4,5]thieno[2,3-d]pyrimidine derivatives and their therapeutically acceptable salts. The compounds according to the invention is used particularly as active agent of therapeutic preparations of tyrosine-kinase inhibiting action.
摘要翻译：本发明的主题是三环芳族和饱和的苯并[4,5]噻吩并[2,3-d]嘧啶衍生物及其治疗上可接受的盐的治疗应用。根据本发明的化合物特别用作酪氨酸激酶抑制作用的治疗制剂的活性剂。

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