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1. 发明申请

WO2012071469A2 HISTONE DEMETHYLASE INHIBITORS AND USES THEREOF FOR TREATMENT O F CANCER 审中-公开
标题翻译： HISTONE DEMETHYLASE抑制剂及其用于治疗的用途
公开(公告)号：WO2012071469A2
公开(公告)日：2012-05-31
申请号：PCT/US2011061954
申请日：2011-11-22
申请人： NEVADA CANCER INST , SHENZHEN GRADUATE SCHOOL OF PEKING UNIVERSITY , ZHANG HUI , YE TAO , QUAN JUNMIN , WANG JING
发明人： ZHANG HUI , YE TAO , QUAN JUNMIN , WANG JING
IPC分类号： C07D403/02 , A61K31/496
CPC分类号： C07D295/215 , A61K31/496 , C07D211/46 , C07D211/58 , C07D211/62
摘要： A compound of formula I: or a pharmaceutically acceptable salt, Ri is an optionally substituted heterocyclic group; R and R' are independently H, CH3, NO2, SO2N(CH3)2, SO2N((CH3)SO2), COOH, COOCH3, CO(N(CH3)), alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, heteroaryl, heterocycloalkyl, alkoxy, alkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aryloxycarbonyloxy, carboxylate, alkylcarbonyl, alkylaminocarbonyl, aralkylaminocarbonyl, alkenylaminocarbonyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkenylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylthiocarbonyl, trifluoromethyl, pentafluoroethyl, halogen, cyano, thio, amido, ether, ester, hydroxyl, hydroxyalkyl, saturated or unsaturated fatty acids, azido, phosphonamido, sulfonamido, lactam, phosphate, phosphonato, phosphinato, amino, acylamino, amidino, imino, guanidino, sulfhydryl, alkylthio, arylthio, thiocarboxylate, sulfates, alkylsulfinyl, sulfonato, sulfamoyl, sulfonamido, nitro, cyano, or azido; m and n are independently integers from 1 to 4; T, U, V, and Z are independently CH, N, or CR; L is NH, CH2, O, S, or SO2; X is N or CH; Y and Y' are independently O or S; and R3 is an optionally substituted aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group.
摘要翻译：式I化合物或其药学上可接受的盐，R 1是任选取代的杂环基; R和R'独立地是H，CH 3，NO 2，SO 2 N（CH 3）2，SO 2 N（（CH 3）SO 2），COOH，COOCH 3，CO（N（CH 3）），烷基，烯基，炔基，芳基，芳烷基，环烷基，杂芳基，杂环烷基，烷氧基，烷基羰基氧基，芳基羰基氧基，烷氧基羰基氧基，芳氧基羰基氧基，羧酸酯，烷基羰基，烷基氨基羰基，芳烷基氨基羰基，烯基氨基羰基，烷基羰基，芳基羰基，芳烷基羰基，烯基羰基，烷氧羰基，氨基羰基，烷硫基羰基，三氟甲基，五氟乙基，卤素，氰基，醚，酯，羟基，羟基烷基，饱和或不饱和脂肪酸，叠氮基，酰基氨基，亚磺酰氨基，内酰胺，磷酸酯，膦酰基，次膦酸酯基，氨基，酰氨基，脒基，亚氨基，胍基，巯基，烷硫基，芳硫基，硫代羧酸酯，硫酸酯，烷基亚磺酰基，磺酸基，氨磺酰基，亚磺酰氨基，硝基，氰基或叠氮基; m和n独立地为1至4的整数; T，U，V和Z独立地为CH，N或CR; L是NH，CH 2，O，S或SO 2; X为N或CH; Y和Y'独立地为O或S; 并且R 3是任选取代的芳基，杂芳基，环烷基或杂环烷基。

2. 发明申请

WO2007064696A3 TARGETING OF SALL4 FOR THE TREATMENT AND DIAGNOSIS OF PROLIFERATIVE DISORDERS ASSOCIATED WITH MYELODYSPLASTIC SYNDROME (MDS) 审中-公开
标题翻译：针对SALL4的治疗与诊断与MYELODYSPLASTIC SYNDROME（MDS）相关的增生性疾病的诊断
公开(公告)号：WO2007064696A3
公开(公告)日：2008-07-03
申请号：PCT/US2006045672
申请日：2006-11-29
申请人： NEVADA CANCER INST , MA YUPO
发明人： MA YUPO
IPC分类号： A01K67/027 , C12Q1/00
CPC分类号： C07K16/18 , A01K67/0275 , A01K2217/05 , A01K2227/105 , A01K2267/0331 , A01K2267/0381 , C07K14/4705 , C12N15/8509 , G01N33/5011 , G01N33/57426 , G01N33/57492
摘要： The present invention discloses nucleic acids, proteins, and antibodies for SALL4 (including isoforms SALL4A, SALL4B, and SALL4C), a zinc finger transcriptional factor. Further, methods are disclosed which demonstrate that constitutive expression of SALL4 increases leukemogenic potential in cells of model animal systems. Moreover, constitutive expression of select isoforms (e.g., SALL4B) in transgenic mice demonstrate that these animals develop myelodysplastic syndrome (MDS)-like signs and symptoms, including subsequent acute myeloid leukemia (AML), which is transplantable. The disclosure also provides methods for identifying and purifying embryonic stem cells, adult stem cells, cancer stem cells, including leukemia stem cells, methods for identifying substances which bind to and/or modulate SALL4, methods for diagnosing MDS in a subject, and methods of treating a subject presenting MDS.
摘要翻译：本发明公开了用于SALL4（包括同种型SALL4A，SALL4B和SALL4C）的核酸，蛋白质和抗体，锌指转录因子。此外，公开了表明SALL4的组成型表达增加模型动物系统的细胞中的白血病潜力的方法。此外，转基因小鼠中选择性同种型（例如SALL4B）的组成型表达证明这些动物发生骨髓增生异常综合征（MDS）样迹象和症状，包括可移植的随后的急性骨髓性白血病（AML）。本公开还提供了用于鉴定和纯化胚胎干细胞，成体干细胞，包括白血病干细胞在内的癌症干细胞的方法，用于鉴定结合和/或调节SALL4的物质的方法，用于诊断受试者的MDS的方法和方法治疗呈现MDS的受试者。

3. 发明申请

WO2008151035A3 TARGETING OF SALL4 FOR THE TREATMENT AND DIAGNOSIS OF PROLIFERATIVE DISORDERS ASSOCIATED WITH MYELODYSPLASTIC SYNDROME (MDS) 审中-公开
标题翻译：用于治疗和诊断与MYELODYSPLASTIC SYNDROME（MDS）相关的增生性疾病的SALL4的目标
公开(公告)号：WO2008151035A3
公开(公告)日：2009-01-29
申请号：PCT/US2008065349
申请日：2008-05-30
申请人： NEVADA CANCER INST , MA YUPO
发明人： MA YUPO
IPC分类号： C12Q1/00
CPC分类号： A01K67/0275 , A01K2217/05 , A01K2227/105 , A01K2267/0331 , A01K2267/0381 , C07K14/4705 , C07K16/18 , C07K16/3061 , C12N15/8509 , C12N2800/30 , C12N2830/008 , C12Q1/6886 , C12Q2600/106 , C12Q2600/118 , C12Q2600/178 , G01N33/5011 , G01N33/57426 , G01N33/57492
摘要： The present invention discloses nucleic acids, proteins, and antibodies for SALL4 (including isoforms SALL4A, SALL4B, and SALL4C), a zinc finger transcriptional factor. Further, methods are disclosed which demonstrate that constitutive expression of SALL4 increases leukemogenic potential in cells of model animal systems. Moreover, constitutive expression of select isoforms (e.g., SALL4B) in transgenic mice demonstrate that these animals develop myelodysplastic syndrome (MDS)-like signs and symptoms, including subsequent acute myeloid leukemia (AML), which is transplantable. The disclosure also provides methods for identifying and purifying embryonic stem cells, adult stem cells, cancer stem cells, including leukemia stem cells, methods for identifying substances which bind to and/or modulate SALL4, methods for diagnosing MDS in a subject, and methods of treating a subject presenting MDS, AML and other forms of leukemia.
摘要翻译：本发明公开了用于SALL4（包括同工型SALL4A，SALL4B和SALL4C）（锌指转录因子）的核酸，蛋白质和抗体。此外，公开了表明SALL4的组成型表达增加模型动物系统的细胞中的白血病发生潜力的方法。此外，转基因小鼠中选择性异构体（例如SALL4B）的组成型表达证明这些动物发生骨髓增生异常综合征（MDS）样迹象和症状，包括可移植的随后的急性骨髓性白血病（AML）。本公开还提供了用于鉴定和纯化胚胎干细胞，成体干细胞，癌症干细胞（包括白血病干细胞）的方法，用于鉴定结合和/或调节SALL4的物质的方法，用于诊断受试者的MDS的方法和方法治疗呈现MDS，AML和其他形式的白血病的受试者。

4. 发明申请

WO2008112297A3 METHODS OF TREATING CANCER BY INTERFERING WITH IGF-I RECEPTOR SIGNALING 审中-公开
标题翻译：通过干扰IGF-I受体信号治疗癌症的方法
公开(公告)号：WO2008112297A3
公开(公告)日：2008-10-30
申请号：PCT/US2008003393
申请日：2008-03-13
申请人： UNIV YALE , NEVADA CANCER INST , SUN HONG , GHOSH PAPIA , KIM YONGSOON
发明人： SUN HONG , GHOSH PAPIA , KIM YONGSOON
IPC分类号： C12N5/16 , C12N15/113
CPC分类号： C07K16/18 , A01K2227/105 , A01K2267/0331 , C07K16/40 , C07K2317/76 , C12N15/1137 , C12N2310/14 , C12Y301/04012
摘要： The invention includes methods of reducing proliferation, causing apoptosis and treating cancer through the inhibition of ASM, the disruption of lipid rafts and the interference with IGF-IR and Racl signaling using a variety of compounds including siRNA, anti-ASM antibodies, anti-ceramide antibodies, short- chain ceramide derivatives, desipramine, clomipramine, mangostin and/or sphingomyelin substrate analogues.
摘要翻译：本发明包括通过抑制ASM减少增殖，引起细胞凋亡和治疗癌症的方法，使用各种化合物（包括siRNA，抗ASM抗体，抗神经酰胺）来抑制脂筏和干扰IGF-1R和Rac1信号传导抗体，短链神经酰胺衍生物，地昔帕明，氯米帕明，芒果苷和/或鞘磷脂底物类似物。

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