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1. 发明申请

WO1995009365A1 METHODS AND COMPOSITIONS FOR TREATMENT OF BCR-ABL ASSOCIATED LEUKEMIAS AND OTHER CELL PROLIFERATIVE DISORDERS 审中-公开
标题翻译：用于治疗BCR-ABL相关性白血病和其他细胞增殖性疾病的方法和组合物
公开(公告)号：WO1995009365A1
公开(公告)日：1995-04-06
申请号：PCT/US1994011067
申请日：1994-09-28
申请人： NEW YORK UNIVERSITY MEDICAL CENTER , SUGEN, INC. , DUKE UNIVERSITY MEDICAL CENTER , SCHLESSINGER, Joseph , GISHIZKY, Mikhail, L. , PENDERGAST, Ann, M. , APP, Harald
发明人： NEW YORK UNIVERSITY MEDICAL CENTER , SUGEN, INC. , DUKE UNIVERSITY MEDICAL CENTER
IPC分类号： G01N33/574
CPC分类号： G01N33/5005 , A61K38/00 , C07K14/4705 , C07K14/82 , G01N33/5008 , G01N33/5011 , G01N33/5041 , G01N33/573 , G01N33/68
摘要： The present invention relates to compositions and methods for the prevention and treatment of cell proliferative disorders wherein a protein tyrosine kinase or protein tyrosine phosphatase capable of complexing with a member of the SH2- and/or SH3 domain-containing family of adaptor proteins is involved. This invention is based, in part, on the surprising discovery that the adaptor protein, GRB-2, binds the intracellular BCR-ABL tyrosine kinase product in vivo and is necessary for the activation of the oncogenic potential of the BCR/ABL product. The present invention further relates to protein tyrosine kinase/adaptor protein complexes and the uses of these complexes for the identification of agents capable of decreasing or inhibiting the interaction between the members of such complexes.
摘要翻译：本发明涉及用于预防和治疗细胞增殖性疾病的组合物和方法，其中涉及能够与适配蛋白的SH2-和/或SH3结构域的家族成员络合的蛋白质酪氨酸激酶或蛋白质酪氨酸磷酸酶。本发明部分基于令人惊奇的发现，即接头蛋白GRB-2在体内结合细胞内BCR-ABL酪氨酸激酶产物，并且是激活BCR / ABL产物的致癌潜力所必需的。本发明还涉及蛋白质酪氨酸激酶/衔接蛋白复合物以及这些复合物用于鉴定能够降低或抑制这些复合物成员之间相互作用的试剂的用途。

2. 发明申请

WO1998024902A1 ADAPTOR PROTEIN FRS2 AND RELATED PRODUCTS AND METHODS 审中-公开
标题翻译：适应蛋白FRS2及相关产品及方法
公开(公告)号：WO1998024902A1
公开(公告)日：1998-06-11
申请号：PCT/US1997021851
申请日：1997-12-01
申请人： SUGEN, INC. , NEW YORK UNIVERSITY MEDICAL CENTER , KOUHARA, Haruhiku , SPIVAK-KROIZMAN, Taly , LAX, Irit , SCHLESSINGER, Joseph
发明人： SUGEN, INC. , NEW YORK UNIVERSITY MEDICAL CENTER
IPC分类号： C12N15/12
CPC分类号： C07K14/4705 , C07K2319/00
摘要： The present invention relates generally to a newly identified adaptor protein FRS2 and related products and methods. FRS2 links protein kinases to activating partners in cells. The invention also relates to nucleic acid molecules encoding portions of FRS2, nucleic acid vectors containing FRS2 related nucleic acid molecules, recombinant cells containing such nucleic acid vectors, polypeptides purified from such recombinant cells, antibodies to such polypeptides, and methods of identifying compounds that enhance or block FRS2 interactions with natural binding partners. Also disclosed are methods for diagnosing abnormal conditions in an organism with FRS2 related molecules or compounds.
摘要翻译：本发明一般涉及新鉴定的衔接蛋白FRS2及其相关产品和方法。 FRS2将蛋白激酶与细胞中的激活配偶体连接。本发明还涉及编码部分FRS2的核酸分子，含有FRS2相关核酸分子的核酸载体，含有此类核酸载体的重组细胞，从这些重组细胞纯化的多肽，对这些多肽的抗体，以及鉴定增强的化合物的方法或阻断与天然结合配偶体的FRS2相互作用。还公开了用于诊断具有FRS2相关分子或化合物的生物体中的异常状况的方法。

3. 发明申请

WO1998026054A2 PYK2 RELATED PRODUCTS AND METHODS 审中-公开
标题翻译： PYK2相关产品及方法
公开(公告)号：WO1998026054A2
公开(公告)日：1998-06-18
申请号：PCT/US1997022565
申请日：1997-12-09
申请人： SUGEN, INC. , NEW YORK UNIVERSITY MEDICAL CENTER , LEV, Simma , SCHLESSINGER, Joseph
发明人： SUGEN, INC. , NEW YORK UNIVERSITY MEDICAL CENTER
IPC分类号： C12N09/12
CPC分类号： C12N9/1205 , G01N33/566 , G01N2500/00
摘要： The present invention features a method for treatment of an organism having a disease or condition characterized by an abnormality in a signal transduction pathway, wherein the signal transduction pathway includes a PYK2 protein. The invention also features methods for diagnosing such diseases and for screening for agents that will be useful in treating such diseases. The invention also features purified and/or isolated nucleic acid encoding a PYK2 protein.
摘要翻译：本发明的特征在于一种具有特征在于信号转导途径异常的疾病或病症的生物体的方法，其中所述信号转导途径包括PYK2蛋白。本发明还具有用于诊断这些疾病和筛选可用于治疗这些疾病的药剂的方法。本发明还具有编码PYK2蛋白质的纯化和/或分离的核酸。

4. 发明申请

WO1998016639A1 RDGB-PROTEINS 审中-公开
标题翻译： RDGB蛋白
公开(公告)号：WO1998016639A1
公开(公告)日：1998-04-23
申请号：PCT/US1997017374
申请日：1997-09-26
申请人： SUGEN, INC. , NEW YORK UNIVERSITY MEDICAL CENTER , LEV, Sima , PLOWMAN, Gregory, D. , SCHLESSINGER, Joseph
发明人： SUGEN, INC. , NEW YORK UNIVERSITY MEDICAL CENTER
IPC分类号： C12N15/12
CPC分类号： C07K14/47 , C07K14/43545 , C07K14/43581 , C07K16/18
摘要： The present invention features a method for treatment of an organism having a disease or condition characterized by an abnormality in a signal transduction pathway, wherein the signal transduction pathway includes a rdgB protein. The invention also features methods for diagnosing such diseases and for screening for agents that will be useful in treating such diseases. The invention also features purified and/or isolated nucleic acid encoding a rdgB protein.
摘要翻译：本发明的特征在于一种用于治疗具有以信号转导途径异常为特征的疾病或病症的生物体的方法，其中所述信号转导途径包括rdgB蛋白。本发明还具有用于诊断这些疾病和筛选可用于治疗这些疾病的药剂的方法。本发明还具有编码rdgB蛋白质的纯化和/或分离的核酸。

5. 发明申请

WO1998007835A2 CRYSTAL STRUCTURES OF A PROTEIN TYROSINE KINASE 审中-公开
标题翻译：蛋白酪氨酸激酶的晶体结构
公开(公告)号：WO1998007835A2
公开(公告)日：1998-02-26
申请号：PCT/US1997014885
申请日：1997-08-21
申请人： SUGEN, INC. , MOHAMMADI, Moosa , LI, Sun , LIANG, Congxin , SCHLESSINGER, Joseph , HUBBARD, Stevan, R. , McMAHON, Gerald , TANG, Peng, C.
发明人： SUGEN, INC.
IPC分类号： C12N09/00
CPC分类号： G01N33/6842 , C07K14/71 , C12N9/1205 , G01N33/68
摘要： The present invention relates to the three-dimensional structures of a protein tyrosine kinase optionally complexed with one or more compounds. The atomic coordinates that define the structures of the protein tyrosine kinase and any of the compounds bound to it are pertinent to methods for determining the three-dimensional structures of protein tyrosine kinases with unknown structure and to methods that identify modulators of protein tyrosine kinase functions.
摘要翻译：本发明涉及任选与一种或多种化合物配合的蛋白质酪氨酸激酶的三维结构。定义蛋白酪氨酸激酶和任何与其结合的化合物的结构的原子坐标与确定具有未知结构的蛋白质酪氨酸激酶的三维结构的方法以及鉴定蛋白酪氨酸激酶功能调节剂的方法是相关的。

6. 发明申请

WO1996040629A1 TYRPHOSTIN-LIKE COMPOUNDS FOR THE TREATMENT OF CELL PROLIFERATIVE DISORDERS OR CELL DIFFERENTIATION DISORDERS 审中-公开
标题翻译：用于治疗细胞增殖性疾病或细胞分化障碍的类似类似物的化合物
公开(公告)号：WO1996040629A1
公开(公告)日：1996-12-19
申请号：PCT/US1996010213
申请日：1996-06-04
申请人： SUGEN, INC.
发明人： SUGEN, INC. , TANG, Peng, Cho , SUN, Li , NEMATALLA, Asaad, S. , McMAHON, Gerald
IPC分类号： C07C317/46
CPC分类号： C07D333/34 , C07C311/27 , C07C317/46 , C07D213/71
摘要： The present invention relates to compounds to formula (1), wherein: X is selected from the group consisting of NH, -C(CN)=C, and CH2CN; m is 0 or 1; n is 0, 1, 2, or 3; Q is an optionally substituted aryl or heteroaryl; and R1-4 are selected from the group consisting of halo, trihalo, methyl, alkyl, alkoxy, hydroxy, H, nitro, cyano, amide, sulphonyl, sulphonamide, carboxy, carboxamide, and amino; capable of modulating tyrosine signal transduction to prevent or treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.
摘要翻译：本发明涉及式（1）化合物，其中：X选自NH，-C（CN）= C和CH 2 CN; m为0或1; n为0,1,2或3; Q是任选取代的芳基或杂芳基; 卤素，三卤代，甲基，烷基，烷氧基，羟基，H，硝基，氰基，酰胺，磺酰基，磺酰胺，羧基，甲酰胺和氨基; 能够调节酪氨酸信号转导以通过抑制一种或多种异常酪氨酸激酶活性来预防或治疗与特定酪氨酸激酶相关的细胞增殖性疾病或细胞分化障碍。

7. 发明申请

WO1996033179A1 THIOAMIDES DERIVATES AND THEIR USE AS INHIBITORS OF HYPER-PROLIFERATIVE CELL GROWTH 审中-公开
标题翻译：噻唑衍生物及其作为高增殖细胞生长抑制剂的用途
公开(公告)号：WO1996033179A1
公开(公告)日：1996-10-24
申请号：PCT/US1996005470
申请日：1996-04-19
申请人： SUGEN, INC. , TANG, Peng, Cho
发明人： SUGEN, INC.
IPC分类号： C07D261/18
CPC分类号： C07D213/75 , C07C327/44 , C07D213/85 , C07D261/10 , C07D261/18 , C07D413/12
摘要： The present invention features compounds and methods for inhibiting hyper-proliferative cell growth. The compounds and method are preferably used to treat patients having a hyper-proliferative cell disorder. The compounds are preferably of formulas (I.A) and (I.B) wherein T is carbon or nitrogen; if T is carbon m is either 0, 1, 2, 3, 4 or 5; and if T is nitrogen m is either 0, 1, 2, 3 or 4; each X is independently selected from the group consisting of: SH, OH, lower alkyl, lower alkenyl, lower alkoxy, haloalkoxy, halogen, haloalkyl, cyano, sulfonyl-aryl, amino, aminosulfonyl, and NO2; R1 is hydrogen or lower alkyl; R3 is selected from the group consisting of: hydrogen, carboxy, alkoxy, and carbalkoxy; R4 is selected from the group consisting of: alkyl, alkenyl, alkyl-aryl, alkenyl-aryl, and alkynyl-aryl; R5 is hydrogen or a group which is cleavable in vivo; and pharmaceutically acceptable salts thereof.
摘要翻译：本发明的特征在于抑制高增殖细胞生长的化合物和方法。化合物和方法优选用于治疗患有高增殖性细胞病症的患者。所述化合物优选为式（ⅠA）和（ⅠB），其中T为碳或氮; 如果T是碳，则m为0，1，2，3，4或5; 如果T是氮，则m为0,1,2,3或4; 每个X独立地选自：SH，OH，低级烷基，低级烯基，低级烷氧基，卤代烷氧基，卤素，卤代烷基，氰基，磺酰基 - 芳基，氨基，氨基磺酰基和NO 2; R1是氢或低级烷基; R3选自：氢，羧基，烷氧基和烷氧羰基; R 4选自：烷基，烯基，烷基 - 芳基，烯基 - 芳基和炔基 - 芳基; R5是氢或体内可切割的基团; 及其药学上可接受的盐。

8. 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。

9. 发明申请

WO1998027092A1 THIAZOLE COMPOUNDS AND METHODS OF MODULATING SIGNAL TRANSDUCTION 审中-公开
标题翻译：噻唑化合物和调节信号传递的方法
公开(公告)号：WO1998027092A1
公开(公告)日：1998-06-25
申请号：PCT/US1997023521
申请日：1997-12-17
申请人： SUGEN, INC.
发明人： SUGEN, INC. , TANG, Peng, C. , RAMPHAL, John, Y. , HARRIS, G., Davis, Jr. , NEMATALLA, Asaad, S.
IPC分类号： C07D417/12
CPC分类号： C07D417/06 , C07D277/58 , C07D417/12 , C07D417/14 , C07D487/04
摘要： The present invention relates to thiazole containing compounds capable of inhibiting protein tyrosine phosphatase activity. The invention further relates to the use of such compounds to modulate or regulate signal transduction by inhibiting protein tyrosine phosphatase activity. Finally, the invention relates to the use of such compounds to treat various disease states including diabetes mellitus.
摘要翻译：本发明涉及能够抑制蛋白酪氨酸磷酸酶活性的含噻唑化合物。本发明还涉及这种化合物通过抑制蛋白酪氨酸磷酸酶活性来调节或调节信号转导的用途。最后，本发明涉及这些化合物用于治疗各种疾病状态（包括糖尿病）的用途。

10. 发明申请

WO1996040113A2 PHOSPHATASE INHIBITORS 审中-公开
标题翻译：磷酸酶抑制剂
公开(公告)号：WO1996040113A2
公开(公告)日：1996-12-19
申请号：PCT/US1996009960
申请日：1996-06-07
申请人： SUGEN, INC.
发明人： SUGEN, INC. , MCMAHON, Gerald , HIRTH, Klaus, P. , TANG, Peng, Cho
IPC分类号： A61K31/38
CPC分类号： A61K31/381 , A61K31/00 , A61K31/135 , A61K31/137 , A61K31/215 , A61K31/22 , A61K31/222 , A61K31/341 , A61K31/352 , A61K31/42 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/53 , A61K31/55
摘要： The present invention relates to organic molecules capable of inhibiting protein tyrosine phosphatase activity. The invention further relates to the use of such molecules to modulate or regulate signal transduction by inhibiting protein tyrosine phosphatase activity. Finally, the invention relates to the use of such molecules to treat various disease states including diabetes mellitus.
摘要翻译：本发明涉及能抑制蛋白酪氨酸磷酸酶活性的有机分子。本发明还涉及通过抑制蛋白酪氨酸磷酸酶活性来调节或调节信号转导的这种分子的用途。最后，本发明涉及这种分子用于治疗包括糖尿病在内的各种疾病状态的用途。

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