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1. 发明申请

WO2005012482B1 ASSAY FOR IDENTIFICATION OF BIOACTIVE COMPOUNDS THAT INTERACT WITH HEAT SHOCK PROTEIN 90 审中-公开
标题翻译：用于识别与热冲击蛋白质相互作用的生物化合物的测定90
公开(公告)号：WO2005012482B1
公开(公告)日：2005-12-22
申请号：PCT/US2004021297
申请日：2004-06-30
申请人： SLOAN KETTERING INST CANCER , CHIOSIS GABRIELA , ROSEN NEAL , HUEZO HENRI
发明人： CHIOSIS GABRIELA , ROSEN NEAL , HUEZO HENRI
IPC分类号： C12N20060101 , G01N21/21 , G01N33/52 , G01N33/53 , G01N33/566 , G01N33/567
CPC分类号： G01N33/542 , C07D405/12 , G01N33/5008 , G01N33/5011 , G01N33/582 , G01N33/68 , G01N33/6845 , G01N2500/00 , G01N2500/02
摘要： A method for evaluation of molecules to identify those that can act as therapeutic inhibitors of Hsp90 makes use of a fluorescence polarization (FP) assay and a cell based assay, either individually or in combination. The FP assay uses a fluorescently-labeled Hsp90 binding agent and measure the degree of fluorescence polarization relative to the standard. A decrease in the degree of polarization indicates that fluorescently-labeled Hsp90 binding agent has been wholly or partially displaced by a candidate molecule, and identifies the molecule as having activity as an inhibitor of Hsp90. The cell based assay tests for decrease is an Hsp90-dependent activity of normal or tumor cells.
摘要翻译：用于评估分子以鉴定可以作为Hsp90的治疗性抑制剂的分子的方法使用单独或组合的荧光偏振（FP）测定和基于细胞的测定。 FP测定使用荧光标记的Hsp90结合剂，并测量相对于标准品的荧光偏振度。极化程度的降低表明荧光标记的Hsp90结合剂已经被候选分子完全或部分置换，并且将该分子鉴定为具有作为Hsp90抑制剂的活性。基于细胞的测定减少的测定是正常或肿瘤细胞的Hsp90依赖性活性。

2. 发明申请

WO2005012482A3 ASSAY FOR IDENTIFICATION OF BIOACTIVE COMPOUNDS THAT INTERACT WITH HEAT SHOCK PROTEIN 90 审中-公开
标题翻译：测定与热休克蛋白相互作用的生物活性化合物90
公开(公告)号：WO2005012482A3
公开(公告)日：2005-09-15
申请号：PCT/US2004021297
申请日：2004-06-30
申请人： SLOAN KETTERING INST CANCER , CHIOSIS GABRIELA , ROSEN NEAL , HUEZO HENRI
发明人： CHIOSIS GABRIELA , ROSEN NEAL , HUEZO HENRI
IPC分类号： C12N20060101 , G01N21/21 , G01N33/52 , G01N33/53 , G01N33/566 , G01N33/567
CPC分类号： G01N33/542 , C07D405/12 , G01N33/5008 , G01N33/5011 , G01N33/582 , G01N33/68 , G01N33/6845 , G01N2500/00 , G01N2500/02
摘要： A method for evaluation of molecules to identify those that can act as therapeutic inhibitors of Hsp90 makes use of a fluorescence polarization (FP) assay and a cell based assay, either individually or in combination. The FP assay uses a fluorescently-labeled Hsp90 binding agent and measure the degree of fluorescence polarization relative to the standard. A decrease in the degree of polarization indicates that fluorescently-labeled Hsp90 binding agent has been wholly or partially displaced by a candidate molecule, and identifies the molecule as having activity as an inhibitor of Hsp90. The cell based assay tests for decrease is an Hsp90-dependent activity of normal or tumor cells.
摘要翻译：评估分子以鉴定那些可以充当Hsp90的治疗性抑制剂的方法使用荧光偏振（FP）测定法和基于细胞的测定法，单独或组合使用。 FP测定使用荧光标记的Hsp90结合剂并测量相对于标准的荧光偏振度。极化程度的降低表明荧光标记的Hsp90结合剂已经被候选分子全部或部分置换，并将该分子鉴定为具有作为Hsp90抑制剂的活性。基于细胞的测定测试降低是正常或肿瘤细胞的Hsp90依赖性活性。

3. 发明申请

WO2002094196A2 METHOD OF TREATMENT FOR CANCERS ASSOCIATED WITH ELEVATED 审中-公开
标题翻译：治疗与高血压相关的癌症的方法
公开(公告)号：WO2002094196A2
公开(公告)日：2002-11-28
申请号：PCT/US2002/016287
申请日：2002-05-23
申请人： SLOAN KETTERING INSTITUTE FOR CANCER RESEARCH , ROSEN, Neal , MUNSTER, Pamela
发明人： ROSEN, Neal , MUNSTER, Pamela
IPC分类号： A61K
CPC分类号： A61K31/395 , A61K31/336
摘要： Novel methods of treating proliferative disorders characterized by elevated Her-2, and the patient is then administered an effective amount of an HSP90 inhibitor.
摘要翻译：治疗以Her-2升高为特征的增殖性疾病的新方法，然后向患者施用有效量的HSP90抑制剂。

4. 发明申请

WO0236171A9 METHODS FOR ENHANCING THE EFFICACY OF CYTOTOXIC AGENTS THROUGH THE USE OF HSP90 INHIBITORS 审中-公开
标题翻译：通过使用HSP90抑制剂增强细胞毒性因子效力的方法
公开(公告)号：WO0236171A9
公开(公告)日：2002-11-21
申请号：PCT/US0146304
申请日：2001-11-01
申请人： SLOAN KETTERING INST CANCER , ROSEN NEAL , MUNSTER PAMELA
发明人： ROSEN NEAL , MUNSTER PAMELA
IPC分类号： A61K45/06 , A61K31/282 , A61K31/337 , A61K31/365 , A61K31/395 , A61K31/505 , A61K31/704 , A61K33/24 , A61K38/00 , A61K38/43 , A61P11/00 , A61P15/00 , A61P35/00 , A61P43/00 , A61K48/00 , A61P , G01N33/535
CPC分类号： A61K33/24 , A61K31/282 , A61K31/337 , A61K31/365 , A61K31/395 , A61K31/505 , A61K31/704 , A61K2300/00
摘要： The administration of cytotoxic agents followed by the administration of heat shock protein 90 inhibitors, such as ansamycins, has a synergistic effect on the growth inhibition of cells. This synergy occurs at doses of each cytotoxic agent that normally only causes minimal growth inhibition of cells. Such combination therapy thus allows one to use lower doses of cytotoxic agents to avoid or reduce their respective toxicity to patients without compromising their growth inhibitory effects. Thus, these combinations can be used for the treatment of an animal, preferably a mammal, that has a cell proliferative disorder, whether the cells have wild-type Rb or are Rb deficient or Rb negative. One such method, directed to treating cell proliferative disorders includes the step of administering a therapeutic effective amount of a cytotoxic agent followed by administering a therapeutic effective amount of a heat shock protein 90 inhibitor. The cytotoxic agent may be a microtubule-affecting agent, topoisomerase II inhibitor, a platinum complex, paclitaxel, or a paclitaxel derivative. The HSP90 inhibitor may be an ansamycin, radicicol or a synthetic compound that binds to the ATP-binding site of HSP90.
摘要翻译：细胞毒性剂的施用，然后施用热休克蛋白90抑制剂，例如安莎霉素，对细胞的生长抑制具有协同作用。这种协同作用发生在通常仅引起细胞生长抑制最小的各细胞毒剂剂量。因此，这样的组合疗法允许使用较低剂量的细胞毒剂以避免或降低其对患者的相应毒性而不损害其生长抑制作用。因此，这些组合可用于治疗具有细胞增殖性疾病的动物，优选哺乳动物，细胞是否具有野生型Rb或Rb缺陷或Rb阴性。针对治疗细胞增殖性疾病的一种这样的方法包括施用治疗有效量的细胞毒性剂的步骤，然后施用治疗有效量的热休克蛋白90抑制剂。细胞毒性剂可以是微管影响剂，拓扑异构酶II抑制剂，铂络合物，紫杉醇或紫杉醇衍生物。 HSP90抑制剂可以是结合HSP90的ATP结合位点的安莎霉素，根霉素或合成化合物。

5. 发明申请

WO0236075A3 SMALL MOLECULE COMPOSITIONS FOR BINDING TO HSP90 审中-公开
标题翻译：用于绑定到HSP90的小分子组合物
公开(公告)号：WO0236075A3
公开(公告)日：2003-06-05
申请号：PCT/US0146303
申请日：2001-11-01
申请人： SLOAN KETTERING INST CANCER , CHIOSIS GABRIELA , ROSEN NEAL
发明人： CHIOSIS GABRIELA , ROSEN NEAL
IPC分类号： G01N33/53 , A61K31/52 , A61K45/00 , A61P35/00 , A61P43/00 , C07D209/36 , C07D473/00 , C07D473/34 , C07D473/40 , C07K14/47 , G01N33/15 , G01N33/566 , C07D487/04 , A61K31/404 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/519 , A61K31/522 , C07D209/08 , C07D209/12 , C07D209/18 , C07D209/22 , C07D235/08 , C07D235/12 , C07D235/16 , C07D235/18 , C07D235/26 , C07D263/56 , C07D263/57 , C07D277/64 , C07D277/66 , C07D471/04 , C07D473/02 , C07D473/18 , C07D473/22 , C07D473/24 , C07D473/28 , C07D473/30 , C07D473/36 , C07D498/04 , C07D513/04 , G01N33/543
CPC分类号： C07D473/00 , A61K31/52 , C07D209/36 , C07D473/34 , C07D473/40
摘要： Structural differences in binding pockets of members of the HSP90 family are exploited to achieve differential degradation of k nases and other signaling proteins by using small molecules which interact with the N-terminal binding pocket with an affinity greater than ADP and different from ansamycin antibiotics for at least one HSP90 family species (Figure 5). These small molecules are soluble in aqueous media, providing a further advantage over ansamycins. Pharmaceutical compositions contain a carrier and a molecule that includes a moiety which binds to the N-terminal pocket of at least one member of the HSP90 family. Such binding moieties have anti proliferative activity against tumor cells which depend on proteins requiring chaperones of the HSP90 family. Different chemical species have different activity, allowing the selection of Her2 degradation without degradation of Raf kinase. Thus, the binding moieties possess inherent targeting capacity. The small molecules can be linked to targeting moieties to target the activity to specific classes of cells. The invention includes treatment of diseases, including cancers. Dimeric forms of the binding moieties may be employed.
摘要翻译：利用HSP90家族成员结合口袋的结构差异，通过使用与N-末端结合口袋相互作用的小分子，以比ADP更大的亲和力和不同于安莎霉素抗生素的小分子来实现k蛋白和其他信号蛋白的差异降解至少有一个HSP90家族（图5）。这些小分子可溶于含水介质，提供了比安莎霉素更优越的优点。药物组合物含有载体和分子，其包括结合HSP90家族的至少一个成员的N末端口袋的部分。这种结合部分具有抗肿瘤细胞的抗增殖活性，其依赖于需要HSP90家族伴侣蛋白质的蛋白质。不同的化学物种具有不同的活性，允许选择Her2降解而不降解Raf激酶。因此，结合部分具有固有的靶向能力。小分子可以连接到靶向部分以将活性靶向特定类别的细胞。本发明包括治疗疾病，包括癌症。可以使用结合部分的二聚体形式。

6. 发明申请

WO2005061481A1 NOVEL MA CROCYCLES AND USES THEREOF 审中-公开
标题翻译：新加坡制造商及其用途
公开(公告)号：WO2005061481A1
公开(公告)日：2005-07-07
申请号：PCT/US2004/042887
申请日：2004-12-17
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , YANG, Zhi-Qiang , GENG, Xudong , CHOU, Ting-Chao , ROSEN, Neal
发明人： DANISHEFSKY, Samuel, J. , YANG, Zhi-Qiang , GENG, Xudong , CHOU, Ting-Chao , ROSEN, Neal
IPC分类号： C07D315/00
CPC分类号： C07D313/00
摘要： The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) (I) wherein R,,-R4, Z, X, A-B, D-E, G-J, and K-L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.
摘要翻译：本发明涉及其结构（及其药学上可接受的衍生物）（I）的化合物，其中R 1 -R 4，Z，X，AB，DE，GJ和KL如本文所定义，其合成和使用这些化合物作为治疗剂。

7. 发明申请

WO2005012482A2 ASSAY FOR IDENTIFICATION OF BIOACTIVE COMPOUNDS THAT INTERACT WITH HEAT SHOCK PROTEIN 90 审中-公开
标题翻译：测定与热休克蛋白相互作用的生物活性化合物90
公开(公告)号：WO2005012482A2
公开(公告)日：2005-02-10
申请号：PCT/US2004/021297
申请日：2004-06-30
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , CHIOSIS, Gabriela , ROSEN, Neal , HUEZO, Henri
发明人： CHIOSIS, Gabriela , ROSEN, Neal , HUEZO, Henri
IPC分类号： C12N
CPC分类号： G01N33/542 , C07D405/12 , G01N33/5008 , G01N33/5011 , G01N33/582 , G01N33/68 , G01N33/6845 , G01N2500/00 , G01N2500/02
摘要： A method for evaluation of molecules to identify those that can act as therapeutic inhibitors of Hsp90 makes use of a fluorescence polarization (FP) assay and a cell based assay, either individually or in combination. The FP assay uses a fluorescently-labeled Hsp90 binding agent and measure the degree of fluorescence polarization relative to the standard. A decrease in the degree of polarization indicates that fluorescently-labeled Hsp90 binding agent has been wholly or partially displaced by a candidate molecule, and identifies the molecule as having activity as an inhibitor of Hsp90. The cell based assay tests for decrease is an Hsp90-dependent activity of normal or tumor cells.
摘要翻译：用于评估分子以鉴定可以充当Hsp90的治疗性抑制剂的分子的方法使用荧光偏振（FP）测定法和基于细胞的测定法，单独或组合使用。 FP测定使用荧光标记的Hsp90结合剂并测量相对于标准的荧光偏振度。极化程度的降低表明荧光标记的Hsp90结合剂已经被候选分子全部或部分置换，并将该分子鉴定为具有作为Hsp90抑制剂的活性。基于细胞的分析检测降低是正常细胞或肿瘤细胞的Hsp90依赖性活性。

8. 发明申请

WO2002094196A3 METHOD OF TREATMENT FOR CANCERS ASSOCIATED WITH ELEVATED 审中-公开
公开(公告)号：WO2002094196A3
公开(公告)日：2002-11-28
申请号：PCT/US2002/016287
申请日：2002-05-23
申请人： SLOAN KETTERING INSTITUTE FOR CANCER RESEARCH , ROSEN, Neal , MUNSTER, Pamela
发明人： ROSEN, Neal , MUNSTER, Pamela
IPC分类号： C12Q1/68
摘要： Novel methods of treating proliferative disorders characterized by elevated Her-2, and the patient is then administered an effective amount of an HSP90 inhibitor.

9. 发明申请

WO0216369A3 NOVEL MACROCYCLES AND USES THEREOF 审中-公开
标题翻译：新的MACROCYCLES及其用途
公开(公告)号：WO0216369A3
公开(公告)日：2002-08-29
申请号：PCT/US0126577
申请日：2001-08-24
申请人： SLOAN KETTERING INST CANCER , DANISHEFSKY SAMUEL J , GARBACCIO ROBERT M , BAESCHLIN DANIEL K , STACHEL SHAWN J , SOLIT DAVID , SHTIL ALEXANDER , ROSEN NEAL
发明人： DANISHEFSKY SAMUEL J , GARBACCIO ROBERT M , BAESCHLIN DANIEL K , STACHEL SHAWN J , SOLIT DAVID , SHTIL ALEXANDER , ROSEN NEAL
IPC分类号： A61P43/00 , C07D225/06 , C07D313/00 , C07D491/04 , C07D493/04 , A61K31/335 , A61K31/395 , C07D495/20
CPC分类号： C07D491/04 , C07D225/06 , C07D313/00 , C07D493/04
摘要： The present invention relates to compounds having the structure (1) (and pharmaceutically acceptable derivatives thereof), wherein R1-R4, Z, X, A-B, D-E, G-J, and K-L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.
摘要翻译：（1）（及其药学上可接受的衍生物）的化合物，其中R 1 -R 4，Z，X，化合物作为治疗剂。

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