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1. 发明申请

WO1995019169A2 TREATMENT OF PLATELET DERIVED GROWTH FACTOR RELATED DISORDERS SUCH AS CANCERS USING INHIBITORS OF PLATELET DERIVED GROWTH RECEPTOR 审中-公开
标题翻译：治疗板片衍生生长因子相关疾病如使用平板衍生生长受体的抑制剂
公开(公告)号：WO1995019169A2
公开(公告)日：1995-07-20
申请号：PCT/US1995000363
申请日：1995-01-06
申请人： SUGEN, INC. , BIOSIGNAL LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WISSENSCHAFTEN E.V. , REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： SUGEN, INC. , BIOSIGNAL LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WISSENSCHAFTEN E.V. , REGENTS OF THE UNIVERSITY OF CALIFORNIA , HIRTH, Klaus, Peter , SCHWARTZ, Donna, Pruess , MANN, Elaina , SHAWVER, Laura, Kay , KERI, Gyorgy , SZEKELY, Istvan , BAJOR, Tamas , HAIMICHAEL, Janis , ORFI, Laszlo , LEVITZKI, Alex , GAZIT, Aviv , ULLRICH, Axel , LAMMERS, Reiner , KABBINAVAR, Fairooz, F. , SLAMON, Dennis, J. , TANG, Cho, Peng
IPC分类号： A61K31/42
CPC分类号： C07D231/38 , A61K9/0019 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/70 , A61K33/24 , A61K45/06 , A61K47/10 , A61K47/26 , C07C255/23 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , G01N33/5011 , Y10S977/904 , Y10S977/911 , Y10S977/912 , Y10S977/915
摘要： The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity of other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see Figure 1A), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
摘要翻译：本发明涉及可以抑制血小板衍生生长因子受体（PDGF-R）活性的化合物，优选地，这些化合物也抑制PDGF-R超家族的其他成员的活性，并且对PDGF-R超家族的成员是选择性的。 PDGF-R超家族包括PDGF-R和PDGF-R相关的激酶Flt和KDR。特征化合物在细胞培养物中是有活性的，以降低PDGF-R，优选一种或多种PDGF-R相关激酶的活性。以下描述特征化合物A10（参见图1A）及其抑制体内肿瘤细胞生长的能力的实例。使用本申请作为指导，可以获得能够抑制PDGF-R，优选Flt和/或KDR的其它化合物。这些化合物优选用于治疗患有以不适当的PDGF-R活性为特征的细胞增殖性疾病的患者。

2. 发明申请

WO1995021613A1 COMPOUNDS FOR THE TREATMENT OF DISORDERS RELATED TO VASCULOGENESIS AND/OR ANGIOGENESIS 审中-公开
标题翻译：用于治疗与血液发生和/或血管生成有关的疾病的化合物
公开(公告)号：WO1995021613A1
公开(公告)日：1995-08-17
申请号：PCT/US1995001751
申请日：1995-02-09
申请人： SUGEN, INC. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY IN JERUSALEM
发明人： SUGEN, INC. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY IN JERUSALEM , GAZIT, Aviv , LEVITZKI, Alexander , APP, Harald , TANG, Cho, Peng , MCMAHON, Gerald, M.
IPC分类号： A61K31/24
CPC分类号： C07D487/04 , A61K31/235 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/495 , A61K31/502 , A61K31/505 , A61K31/517 , A61K31/535 , A61K38/00 , C07C229/60 , C07C255/36 , C07C255/40 , C07C255/41 , C07C255/66 , C07C317/46 , C07C327/44 , C07D209/18 , C07D239/93 , C07D239/94 , C07D241/42 , C07D241/44 , C07K14/71 , C07K16/2863 , C07K2319/32 , G01N33/5008 , G01N33/5011 , G01N33/502 , G01N33/5064 , G01N33/5091 , G01N33/6893 , G01N2333/71 , G01N2500/04
摘要： The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described. The invention also relates to the use of the disclosed compounds in the treatment of disorders, including cancer, diabetes, hemangioma and Kaposi's sarcoma, which are related to vasculogenesis and angiogenesis.
摘要翻译：本发明涉及能够调节酪氨酸激酶信号转导的有机分子，特别是涉及调节和/或调节血管发生和血管生成的KDR / FLK-1受体信号转导。本发明部分基于KDR / FLK-1酪氨酸激酶受体表达与内皮细胞相关的证据，以及作为FLK-1的高亲和力配体的血管内皮生长因子（VEGF）的鉴定。这些结果表明KDR / FLK-1在血管发生和血管发生过程中在信号系统中的主要作用。还描述了表达FLK-1的宿主细胞的工程和表达FLK-1用于通过激动剂或拮抗剂活性评估和筛选参与FLK-1调节的VEGF的类似物的用途。本发明还涉及所公开的化合物在治疗与血管发生和血管发生相关的疾病（包括癌症，糖尿病，血管瘤和卡波西氏肉瘤）中的应用。

3. 发明申请

WO1995024190A2 RECEPTOR TYROSINE KINASE INHIBITORS FOR INHIBITING CELL PROLIFERATIVE DISORDERS AND COMPOSITIONS THEREOF 审中-公开
标题翻译：用于抑制细胞增殖性疾病的受体酪氨酸激酶抑制剂及其组合物
公开(公告)号：WO1995024190A2
公开(公告)日：1995-09-14
申请号：PCT/US1995002826
申请日：1995-03-06
申请人： SUGEN, INC. , YISSUM RESEARCH DEVELOPMENT COMPANY
发明人： SUGEN, INC. , YISSUM RESEARCH DEVELOPMENT COMPANY , CHEN, Hui , GAZIT, Aviv , HIRTH, Klaus, Peter , LEVITZKI, Alex , MANN, Elaina , SHAWVER, Laura, K. , TSAI, Jianming , TANG, Peng, Cho
IPC分类号： A61K31/275
CPC分类号： C07D241/52 , A61K31/245 , A61K31/277 , A61K31/415 , A61K31/4184 , A61K31/4402 , A61K31/498 , A61K31/517 , C07C229/60 , C07C255/36 , C07C255/37 , C07C255/41 , C07C255/42 , C07C255/66 , C07C311/27 , C07C317/46 , C07C327/44
摘要： The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.
摘要翻译：本发明涉及化合物及其抑制受体酪氨酸激酶活性的用途。本发明优选用于治疗细胞增殖性疾病，例如以过度活动或不适当活性HER2或EGFR为特征的癌症。

4. 发明申请

WO2004013091A2 4-ANILIDO SUBSTITUTED QUINAZOLINES AND USE THEREOF AS INHIBITORS OF EPIDERMAL GROWTH FACTOR RECEPTOR KINASES 审中-公开
标题翻译： 4-ANILIDO取代喹啉腈及其作为抗生殖因子受体激动剂的抑制剂
公开(公告)号：WO2004013091A2
公开(公告)日：2004-02-12
申请号：PCT/IL2003/000632
申请日：2003-07-31
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , GAZIT, Aviv , LEVITZKI, Alexander
发明人： GAZIT, Aviv , LEVITZKI, Alexander
IPC分类号： C07D
CPC分类号： C07D401/12 , A61K31/517 , C07D239/86 , C07D239/88 , C07D239/94 , C07D239/95 , C07D403/04 , C07D403/12 , C07D417/12 , C07D417/14
摘要： The present invention provides 4-anilido substituted quinazoline compounds which are potent inhibitors of protein tyrosine (PTK) kinase activity, particularly epidermal growth factor receptor (EGFR) kinase activity, and pharmaceutical compositions comprising these compounds. The present invention further provides methods of inhibiting the activity of a protein tyrosine kinase (PTK), for example an EGFR kinase, comprising the step of contacting the PTK with an effective inhibitory amount of any of the quinazoline compounds defined herein. The present invention further provides a method of inhibiting the activity of a protein tyrosine kinase (PTK) in a subject, for example an EGFR kinase, comprising the step of administering to the subject a therapeutically effective amount of any of the quinazoline compounds defined herein. The present invention further provides a method of treating or preventing a protein tyrosine kinase (PTK) related disorder in a subject, for example an EGFR related disorder, comprising the step of administering to the subject a therapeutically effective amount of any of the quinazoline compounds defined herein. The quinazoline compounds are useful in treating a variety of PTK related disorders such as cell proliferative disorders, fibrotic disorders, metabolic disorders and cancer.
摘要翻译：本发明提供了作为蛋白酪氨酸（PTK）激酶活性，特别是表皮生长因子受体（EGFR）激酶活性的有效抑制剂的4-苯胺基取代的喹唑啉化合物，以及包含这些化合物的药物组合物。本发明进一步提供了抑制蛋白酪氨酸激酶（PTK），例如EGFR激酶的活性的方法，其包括使PTK与有效抑制量的本文定义的任何喹唑啉化合物接触的步骤。本发明进一步提供了抑制受试者例如EGFR激酶中蛋白质酪氨酸激酶（PTK）的活性的方法，包括向受试者施用治疗有效量的本文定义的任何喹唑啉化合物的步骤。本发明还提供了治疗或预防受试者中的蛋白酪氨酸激酶（PTK）相关病症的方法，例如EGFR相关病症，其包括向受试者施用治疗有效量的任何定义的喹唑啉化合物于此。喹唑啉化合物可用于治疗各种PTK相关疾病，例如细胞增殖性疾病，纤维化病症，代谢紊乱和癌症。

5. 发明申请

WO2003066608A1 CATECHOL BIOISOSTERES 审中-公开
公开(公告)号：WO2003066608A1
公开(公告)日：2003-08-14
申请号：PCT/IL2003/000094
申请日：2003-02-05
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , GAZIT, Aviv , LEVITZKI, Alexander , BLUM, Galia
发明人： GAZIT, Aviv , LEVITZKI, Alexander , BLUM, Galia
IPC分类号： C07D263/54
CPC分类号： C07D263/58
摘要： The present invention provides catechol bioisostere compounds which are potent inhibitors of protein tyrosine kinases (PTKs). The present invention further provides methods of inhibiting PTKs, for example receptor protein tyrosine kinases (RTKs), comprising administering the catechol bioisosteres. The catechol bioisostere compounds are useful in treating or preventing PTK-related disease states, particularly protein tyrosine kinase related disorders which are associated with defects in signaling pathways mediated by PTKs.
摘要翻译：本发明提供了作为蛋白酪氨酸激酶（PTK）的有效抑制剂的儿茶酚生物电子等排化合物。本发明还提供了抑制PTK的方法，例如受体蛋白酪氨酸激酶（RTK），其包括施用儿茶酚生物电子等排体。邻苯二酚生物电子等离子体化合物可用于治疗或预防PTK相关疾病状态，特别是与由PTK介导的信号传导途径缺陷相关的蛋白酪氨酸激酶相关病症。

6. 发明申请

WO2003065971A3 NON-MYELOABLATIVE TOLEROGENIC TREATMENT WITH TYRPHOSTINS 审中-公开
公开(公告)号：WO2003065971A3
公开(公告)日：2003-08-14
申请号：PCT/IL2002/000467
申请日：2002-06-16
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , HADASIT MEDICAL RESEARCH SERVICES AND DEVELOPMENT LTD. , SLAVIN, Shimon , LEVITZKI, Alexander , GAZIT, Aviv , MORECKI, Shoshana
发明人： SLAVIN, Shimon , LEVITZKI, Alexander , GAZIT, Aviv , MORECKI, Shoshana
IPC分类号： A61K48/00
摘要： A method of inducing immune tolerance in a first mammal to antigens of a second, non-syngeneic, mammal, is disclosed. The method is utilized to minimize graft rejection and/or reduce graft-versus-host diseases in transplantation procedures and to produce hematopoietic mixed chimeras. Methods of determining the activity of tyrphostins and the optimal concentration thereof in this method are also disclosed.

7. 发明申请

WO2006087718A1 EXTENSION OF LIFESPAN WITH DRUGS 审中-公开
标题翻译：延长寿命与药物
公开(公告)号：WO2006087718A1
公开(公告)日：2006-08-24
申请号：PCT/IL2006/000205
申请日：2006-02-16
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , SLAVIN, Shimon , GAZIT, Aviv
发明人： SLAVIN, Shimon , GAZIT, Aviv
IPC分类号： A61K31/277 , C07C255/40 , C07C255/41 , C07C255/42 , C07C317/46 , C07C327/44 , A61P43/00
CPC分类号： C07C255/40 , C07C255/37 , C07C317/46 , C07C323/60 , C07C327/44
摘要： New compounds, inhibiting protein tyrosine kinases (PTKs) or steroid-related enzymes (SREs), which affect apoptosis in malignant tissues, and can be used in the preparation of medicaments for treating various disorders, and for elongating the lifespan of a subject while sustaining that subject in good health. Further, a method and antiaging compositions are provided for extending the lifespan.
摘要翻译：新化合物，抑制蛋白酪氨酸激酶（PTK）或类固醇相关酶（SREs），其影响恶性组织中的细胞凋亡，并且可用于制备用于治疗各种疾病的药物并延长受试者的寿命，同时维持那个问题身体健康。此外，提供了延长使用寿命的方法和抗衰老组合物。

8. 发明申请

WO2003065971A2 NON-MYELOABLATIVE TOLEROGENIC TREATMENT WITH TYRPHOSTINS 审中-公开
标题翻译：具有类型性的非骨髓性多发性骨髓瘤治疗
公开(公告)号：WO2003065971A2
公开(公告)日：2003-08-14
申请号：PCT/IL2002/000467
申请日：2002-06-16
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , HADASIT MEDICAL RESEARCH SERVICES AND DEVELOPMENT LTD. , SLAVIN, Shimon , MORECKI, Shoshana , LEVITZKI, Alexander , GAZIT, Aviv
发明人： SLAVIN, Shimon , MORECKI, Shoshana , LEVITZKI, Alexander , GAZIT, Aviv
IPC分类号： A61K
CPC分类号： A61K49/0004 , A61K31/277 , A61K31/404 , A61K31/50 , A61K31/517 , A61K31/519 , A61K39/00 , A61K39/001 , A61K39/39 , A61K41/00 , A61K2039/55511 , A61K2300/00
摘要： A method of inducing immune tolerance in a first mammal to antigens of a second, non-syngeneic, mammal, is disclosed. The method is utilized to minimize graft rejection and/or reduce graft-versus-host diseases in transplantation procedures and to produce hematopoietic mixed chimeras. Methods of determining the activity of tyrphostins and the optimal concentration thereof in this method are also disclosed.
摘要翻译：公开了一种在第一种哺乳动物中诱导免疫耐受的方法，该方法是第二种非同系哺乳动物的抗原。该方法用于在移植过程中最小化移植物排斥和/或减少移植物抗宿主病，并产生造血混合嵌合体。还公开了确定酪氨酸磷酸酶活性的方法及其在该方法中的最佳浓度。

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