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1. 发明申请

WO2008005572A2 SUBSTITUTED 4-ARYL-CHROMENE AS ACTIVATOR OF CASPASES AND INDUCER OF APOPTOSIS AND AS ANTIVASCULAR AGENT AND THE USE THEREOF 审中-公开
标题翻译：取代的4-ARYL-CHROMENE作为CASPASES的激活剂和疫苗诱导剂和抗微生物剂及其用途
公开(公告)号：WO2008005572A2
公开(公告)日：2008-01-10
申请号：PCT/US2007015676
申请日：2007-07-06
申请人： CYTOVIA INC , CAI SUI XIONG , DREWE JOHN A , KASIBHATLA SHAILAJA , KEMNITZER WILLIAM E , TSENG BEN Y , BLAIS CHARLES , GOURDEAU HENRIETTE , LABRECQUE DENIS
发明人： CAI SUI XIONG , DREWE JOHN A , KASIBHATLA SHAILAJA , KEMNITZER WILLIAM E , TSENG BEN Y , BLAIS CHARLES , GOURDEAU HENRIETTE , LABRECQUE DENIS
IPC分类号： A61K31/353
CPC分类号： C07D405/12 , C07D311/58
摘要： The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth, and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.
摘要翻译：本发明涉及基本上不含相应（S） - 立体异构体的由式1R表示的取代的4H-色烯。本发明还涉及发现基本上不含相应的（S） - 立体异构体的化合物1R 是胱天蛋白酶和凋亡诱导剂的激活剂，以及抗血管性药剂。因此，可以使用基本上不含相应（S） - 立体异构体的化合物1R在多种临床条件下诱导细胞死亡，其中发生不受控制的生长和异常细胞的扩散。基本上不含相应（S） - 立体异构体的化合物1R也可用于治疗由于脉管系统过度生长（如实体瘤和眼新生血管形成）引起的疾病。

2. 发明申请

WO2004002428A2 DERIVATIVES OF GAMBOGIC ACID AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS 审中-公开
标题翻译：作为杀虫剂和杀虫剂的激活剂的游离酸和类似物的衍生物
公开(公告)号：WO2004002428A2
公开(公告)日：2004-01-08
申请号：PCT/US0320668
申请日：2003-07-01
申请人： CYTOVIA INC , TSENG BEN , SIRISOMA NILANTHA SUDATH
发明人： TSENG BEN , SIRISOMA NILANTHA SUDATH , CAI SUI XIONG , ZHANG HAN-ZHONG , KASIBHATLA SHAILAJA , OLLIS KRISTIN P , DREWE JOHN A
IPC分类号： C07D493/20 , C12N5/02 , A61K
CPC分类号： A61K31/00 , C07D493/20
摘要： The present invention is directed to derivatives of gambogic acid and analogs thereof. Exemplary gambogic acid derivatives of the present invention include, among others, derivatives substituted in the C10 and C28 positions of gambogic acid. The present invention also relates to the discovery that certain preferred compounds of the present invention are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：本发明涉及吡啶酸及其类似物的衍生物。本发明的示例性的吡咯烷酸衍生物包括其中取代为吡咯烷酸的C10和C28位置的衍生物。本发明还涉及本发明的某些优选化合物是胱天蛋白酶的活化剂和凋亡诱导剂的发现。因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于诱导异常细胞发生不受控制的生长和扩散的各种临床病症中的细胞死亡。

3. 发明申请

WO2004094648A2 METHODS OF TREATING DISEASES RESPONSIVE TO INDUCTION OF APOPTOSIS AND SCREENING ASSAYS 审中-公开
标题翻译：治疗反应性感染和筛查测定的方法
公开(公告)号：WO2004094648A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/011916
申请日：2004-04-19
申请人： CYTOVIA, INC. ET AL. , KASIBHATLA, Shailaja , CAI, Sui, Xiong , TSENG, Ben , JESSEN, Katayoun, Alavi , MALIARTCHOUK, Serguei , ENGLISH, Nicole, Marion , KUEMMERLE, Jared , KEMNITZER, William, E. , ZHANG, Han-Zhong
发明人： KASIBHATLA, Shailaja , CAI, Sui, Xiong , TSENG, Ben , JESSEN, Katayoun, Alavi , MALIARTCHOUK, Serguei , ENGLISH, Nicole, Marion , KUEMMERLE, Jared , KEMNITZER, William, E. , ZHANG, Han-Zhong
IPC分类号： C12Q
CPC分类号： G01N33/5011 , A61K31/729
摘要： The present invention pertains to a method of treating, preventing or ameliorating a disease responsive to induction of the caspase cascade in an animal, comprising administering to the animal a compound which binds specifically to a Tail Interacting Protein Related Apoptosis Inducing Protein (TIPRAIP). The present invention also relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using TIPRAIP as a target for the discovery of apoptosis activators useful as anticancer agents. The screening methods of the present invention can employ homogenous or heterogenous binding assays using purified or partially purified TIPRAIP; or whole cell assays using cells with altered levels of TIPRAIP. The invention also contemplates use of 3-(4azidophenyl)-5-(3-chloro-thiophen-2-yl)-[1,2,4]-oxadiazole or a substituted 3aryl-5-aryl-[1,2,4]-oxadiazole which bind TIPRAIP and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled 3-(4azidophenyl)-5-(3-chloro-thiophen-2-yl)-[1,2,4]-oxadiazole (or a labeled substituted 3-aryl-5-aryl-[1,2,4]-oxadiazole) is used for competitive binding assays for drug discovery. Such assays afford high throughput screening of chemical libraries for apoptosis activators.
摘要翻译：本发明涉及治疗，预防或改善对动物中胱天蛋白酶级联诱导有反应的疾病的方法，包括向动物施用与尾部相互作用蛋白相关的细胞凋亡诱导蛋白（TIPRAIP）特异性结合的化合物。本发明还涉及可用于药物发现凋亡诱导化合物的筛选方法。特别地，筛选方法涉及使用TIPRAIP作为发现可用作抗癌剂的凋亡激活剂的靶标。本发明的筛选方法可以使用纯化或部分纯化的TIPRAIP的均质或异源结合测定; 或使用具有改变水平的TIPRAIP的细胞的全细胞测定。本发明还考虑使用3-（4-氮杂苯基）-5-（3-氯 - 噻吩-2-基） - [1,2,4] - 恶二唑或取代的3-芳基-5-芳基 - [1,2 ，4] - 恶二唑，其结合TIPRAIP，因此可用于产生用于药物发现的抗体。或者，标记3-（4-氮杂苯基）-5-（3-氯 - 噻吩-2-基） - [1,2,4] - 恶二唑（或标记的取代的3-芳基-5-芳基 - [1,2 ，4] - 恶二唑）用于药物发现的竞争性结合测定。这样的测定提供用于凋亡激活剂的化学文库的高通量筛选。

4. 发明申请

WO2004094647A3 METHODS OF TREATING DISEASES RESPONSIVE TO INDUCTION OF APOPTOSIS AND SCREENING ASSAYS 审中-公开
公开(公告)号：WO2004094647A3
公开(公告)日：2004-11-04
申请号：PCT/US2004/011915
申请日：2004-04-19
申请人： CYTOVIA, INC. , KASIBHATLA, Shailaja , CAI, Sui Xiong , TSENG, Ben , JESSEN, Katayoun Alavi , MALIARTCHOUK, Serguei , ENGLISH, Nicole, Marion , JIANG, Songchun , SIRISOMA, Nilantha Sudath , ZHANG, Han-Zhong , KUEMMERLE, Jared
发明人： KASIBHATLA, Shailaja , CAI, Sui Xiong , TSENG, Ben , JESSEN, Katayoun Alavi , MALIARTCHOUK, Serguei , ENGLISH, Nicole, Marion , JIANG, Songchun , SIRISOMA, Nilantha Sudath , ZHANG, Han-Zhong , KUEMMERLE, Jared
IPC分类号： A61K49/00
摘要： The present invention pertains to a method of treating, preventing or ameliorating a disease responsive to induction of the caspase cascade in an animal, comprising administering to the animal a compound which binds specifically to one or more Apoptosis Inducing Proteins (AIPs). AIPs include Transferrin Receptor Related Apoptosis Inducing Proteins (TRRAIPs), Clathrin Heavy Chain Related Apoptosis Inducing Proteins (CHCRAIPs), IQ motif containing GTPase Activating Protein Related Apoptosis Inducing Proteins (IQGAPRAIPs), and Heat Shock Protein Related Apoptosis Inducing Proteins (HSPRAIPs). The present invention also relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using AIPs as a target for the discovery of apoptosis activators useful as anticancer agents. The screening methods of the present invention can employ homogenous or heterogenous binding assays using purified or partially purified AIPs; or whole cell assays using cells with altered levels of one or more AIPs. The invention also contemplates use of gambogic acid or GA-related compounds which bind AIPs and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled GA is used for competitive binding assays for drug discovery. Such assays afford high throughput screening of chemical libraries for apoptosis activators.

5. 发明申请

WO2008005572A3 SUBSTITUTED 4-ARYL-CHROMENE AS ACTIVATOR OF CASPASES AND INDUCER OF APOPTOSIS AND AS ANTIVASCULAR AGENT AND THE USE THEREOF 审中-公开
公开(公告)号：WO2008005572A3
公开(公告)日：2008-01-10
申请号：PCT/US2007/015676
申请日：2007-07-06
申请人： CYTOVIA, INC. , CAI, Sui, Xiong , DREWE, John, A. , KASIBHATLA, Shailaja , KEMNITZER, William, E. , TSENG, Ben, Y. , BLAIS, Charles , GOURDEAU, Henriette , LABRECQUE, Denis
发明人： CAI, Sui, Xiong , DREWE, John, A. , KASIBHATLA, Shailaja , KEMNITZER, William, E. , TSENG, Ben, Y. , BLAIS, Charles , GOURDEAU, Henriette , LABRECQUE, Denis
IPC分类号： A61K31/353 , C07D311/58
摘要： The present invention is directed to a substituted 4H-chromene represented by the Formula (1R), substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth, and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.

6. 发明申请

WO2004002401A2 CASPASE INHIBITORS FOR THE TREATMENT OF DISEASES AND CONDITIONS CAUSED BY EXPOSURE TO RADIONUCLIDES, BIOLOGICAL AGENTS, OR CHEMICAL AGENTS 审中-公开
标题翻译：用于治疗由放射性核素，生物制剂或化学试剂接触引起的疾病和病症的CASPASE抑制剂
公开(公告)号：WO2004002401A2
公开(公告)日：2004-01-08
申请号：PCT/US2003/010645
申请日：2003-04-07
申请人： CYTOVIA, INC. , CAI, Sui, Xiong , TSENG, Ben, Y.
发明人： CAI, Sui, Xiong , TSENG, Ben, Y.
IPC分类号： A61K
CPC分类号： A61K31/16 , A61K31/19 , A61K31/195 , A61K31/198 , A61K31/27 , A61K31/35 , A61K31/44 , A61K31/535 , A61K38/05 , A61K38/55 , A61K51/12 , Y02A50/406 , Y02A50/471
摘要： The use of caspase inhibitors for treating cell death induced by radionuclides, biological agents, or chemical agents is disclosed. In particular, treatment of diseases or conditions caused by exposure to radionuclides, biological agents, or chemical agents, spread of radionuclides, biological agents, or chemical agents, explosion of radionuclides, biological agents, or chemical agents by terrorists or accidental exposure to radionuclides, biological agents, or chemical agents from a nuclear power plant, manufacturing or processing plant, research facility, or hospital is disclosed.
摘要翻译：公开了使用半胱天冬酶抑制剂来治疗由放射性核素，生物制剂或化学试剂引起的细胞死亡。特别是治疗暴露于放射性核素，生物制剂或化学药剂，放射性核素，生物制剂或化学药剂的扩散，恐怖分子的爆炸性放射性核素，生物制剂或化学试剂引起的疾病或病症或意外暴露于放射性核素，公开了来自核电站，制造或加工厂，研究设施或医院的生物制剂或化学试剂。

7. 发明申请

WO2004094648A3 METHODS OF TREATING DISEASES RESPONSIVE TO INDUCTION OF APOPTOSIS AND SCREENING ASSAYS 审中-公开
标题翻译：治疗反应性感染和筛查测定的方法
公开(公告)号：WO2004094648A3
公开(公告)日：2006-03-23
申请号：PCT/US2004011916
申请日：2004-04-19
申请人： CYTOVIA INC , KASIBHATLA SHAILAJA , CAI SUI XIONG , TSENG BEN , JESSEN KATAYOUN ALAVI , MALIARTCHOUK SERGUEI , ENGLISH NICOLE MARION , KUEMMERLE JARED , KEMNITZER WILLIAM E , ZHANG HAN-ZHONG
发明人： KASIBHATLA SHAILAJA , CAI SUI XIONG , TSENG BEN , JESSEN KATAYOUN ALAVI , MALIARTCHOUK SERGUEI , ENGLISH NICOLE MARION , KUEMMERLE JARED , KEMNITZER WILLIAM E , ZHANG HAN-ZHONG
IPC分类号： A61K31/47 , A61K38/00 , C12Q20060101 , A61K48/00 , A61K39/395 , C12Q1/68
CPC分类号： G01N33/5011 , A61K31/729
摘要： The present invention pertains to a method of treating, preventing or ameliorating a disease responsive to induction of the caspase cascade in an animal, comprising administering to the animal a compound which binds specifically to a Tail Interacting Protein Related Apoptosis Inducing Protein (TIPRAIP). The present invention also relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using TIPRAIP as a target for the discovery of apoptosis activators useful as anticancer agents. The screening methods of the present invention can employ homogenous or heterogenous binding assays using purified or partially purified TIPRAIP; or whole cell assays using cells with altered levels of TIPRAIP. The invention also contemplates use of 3-(4azidophenyl)-5-(3-chloro-thiophen-2-yl)-[1,2,4]-oxadiazole or a substituted 3aryl-5-aryl-[1,2,4]-oxadiazole which bind TIPRAIP and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled 3-(4azidophenyl)-5-(3-chloro-thiophen-2-yl)-[1,2,4]-oxadiazole (or a labeled substituted 3-aryl-5-aryl-[1,2,4]-oxadiazole) is used for competitive binding assays for drug discovery. Such assays afford high throughput screening of chemical libraries for apoptosis activators.
摘要翻译：本发明涉及治疗，预防或改善对动物中胱天蛋白酶级联诱导有反应的疾病的方法，包括向动物施用与尾部相互作用蛋白相关的细胞凋亡诱导蛋白（TIPRAIP）特异性结合的化合物。本发明还涉及可用于药物发现凋亡诱导化合物的筛选方法。特别地，筛选方法涉及使用TIPRAIP作为发现可用作抗癌剂的凋亡激活剂的靶标。本发明的筛选方法可以使用纯化或部分纯化的TIPRAIP的均一或异源结合测定; 或使用具有改变的TIPRAIP水平的细胞的全细胞测定。本发明还考虑使用3-（4-氮杂苯基）-5-（3-氯 - 噻吩-2-基） - [1,2,4] - 恶二唑或取代的3-芳基-5-芳基 - [1,2 ，4] - 恶二唑，其结合TIPRAIP，因此可用于引发可用于药物发现的抗体。或者，标记3-（4-氮杂苯基）-5-（3-氯 - 噻吩-2-基） - [1,2,4] - 恶二唑（或标记的取代的3-芳基-5-芳基 - [1,2 ，4] - 恶二唑）用于药物发现的竞争性结合测定。这样的测定提供用于凋亡激活剂的化学文库的高通量筛选。

8. 发明申请

WO2004094647A2 METHODS OF TREATING DISEASES RESPONSIVE TO INDUCTION OF APOPTOSIS AND SCREENING ASSAYS 审中-公开
标题翻译：治疗反应性感染和筛查测定的方法
公开(公告)号：WO2004094647A2
公开(公告)日：2004-11-04
申请号：PCT/US2004011915
申请日：2004-04-19
申请人： CYTOVIA INC , KASIBHATLA SHAILAJA , CAI SUI XIONG , TSENG BEN , JESSEN KATAYOUN ALAVI , MALIARTCHOUK SERGUEI , ENGLISH NICOLE MARION , JIANG SONGCHUN , SIRISOMA NILANTHA SUDATH , ZHANG HAN-ZHONG , KUEMMERLE JARED
发明人： KASIBHATLA SHAILAJA , CAI SUI XIONG , TSENG BEN , JESSEN KATAYOUN ALAVI , MALIARTCHOUK SERGUEI , ENGLISH NICOLE MARION , JIANG SONGCHUN , SIRISOMA NILANTHA SUDATH , ZHANG HAN-ZHONG , KUEMMERLE JARED
IPC分类号： A61K31/352 , A61K38/17 , A61K49/00 , C07D493/20 , C07D519/00 , C12Q20060101 , C12Q
CPC分类号： A61K49/0052 , A61K31/352 , A61K49/0043 , A61K51/0412 , A61K51/0419 , A61K51/0421 , A61K51/0453 , A61K51/0495
摘要： The present invention pertains to a method of treating, preventing or ameliorating a disease responsive to induction of the caspase cascade in an animal, comprising administering to the animal a compound which binds specifically to one or more Apoptosis Inducing Proteins (AIPs). AIPs include Transferrin Receptor Related Apoptosis Inducing Proteins (TRRAIPs), Clathrin Heavy Chain Related Apoptosis Inducing Proteins (CHCRAIPs), IQ motif containing GTPase Activating Protein Related Apoptosis Inducing Proteins (IQGAPRAIPs), and Heat Shock Protein Related Apoptosis Inducing Proteins (HSPRAIPs). The present invention also relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using AIPs as a target for the discovery of apoptosis activators useful as anticancer agents. The screening methods of the present invention can employ homogenous or heterogenous binding assays using purified or partially purified AIPs; or whole cell assays using cells with altered levels of one or more AIPs. The invention also contemplates use of gambogic acid or GA-related compounds which bind AIPs and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled GA is used for competitive binding assays for drug discovery. Such assays afford high throughput screening of chemical libraries for apoptosis activators.
摘要翻译：本发明涉及一种治疗，预防或改善对动物中胱天蛋白酶级联诱导起反应的疾病的方法，包括向动物施用与一种或多种凋亡诱导蛋白（AIP）特异性结合的化合物。 AIPs包括转铁蛋白受体相关凋亡诱导蛋白（TRRAIP），网格蛋白重链相关凋亡诱导蛋白（CHCRAIPs），包含GTPase激活蛋白相关凋亡诱导蛋白（IQGAPRAIPs）和热休克蛋白相关凋亡诱导蛋白（HSPRAIPs）的IQ基序。本发明还涉及可用于药物发现凋亡诱导化合物的筛选方法。特别地，筛选方法涉及使用AIP作为发现用作抗癌剂的凋亡激活剂的靶标。本发明的筛选方法可以使用纯化或部分纯化的AIPs进行均一或异源结合测定; 或使用具有改变水平的一种或多种AIP的细胞的全细胞测定。本发明还考虑使用结合AIP的葡萄糖酸或GA相关化合物，因此可以用于产生可用于药物发现的抗体。或者，标记的GA用于药物发现的竞争性结合测定。这样的测定提供用于凋亡激活剂的化学文库的高通量筛选。

9. 发明申请

WO2004002401A3 CASPASE INHIBITORS FOR THE TREATMENT OF DISEASES AND CONDITIONS CAUSED BY EXPOSURE TO RADIONUCLIDES, BIOLOGICAL AGENTS, OR CHEMICAL AGENTS 审中-公开
标题翻译： CASPASE抑制剂用于治疗由放射性核素，生物剂或化学药剂引起的疾病和病症
公开(公告)号：WO2004002401A3
公开(公告)日：2004-04-01
申请号：PCT/US0310645
申请日：2003-04-07
申请人： CYTOVIA INC , CAI SUI XIONG , TSENG BEN Y
发明人： CAI SUI XIONG , TSENG BEN Y
IPC分类号： A61K31/16 , A61K31/19 , A61K31/195 , A61K31/198 , A61K31/27 , A61K31/35 , A61K31/44 , A61K31/535 , A61K38/05 , A61K38/55 , A61K51/12 , A61K38/00
CPC分类号： A61K31/16 , A61K31/19 , A61K31/195 , A61K31/198 , A61K31/27 , A61K31/35 , A61K31/44 , A61K31/535 , A61K38/05 , A61K38/55 , A61K51/12
摘要： The use of caspase inhibitors for treating cell death induced by radionuclides, biological agents, or chemical agents is disclosed. In particular, treatment of diseases or conditions caused by exposure to radionuclides, biological agents, or chemical agents, spread of radionuclides, biological agents, or chemical agents, explosion of radionuclides, biological agents, or chemical agents by terrorists or accidental exposure to radionuclides, biological agents, or chemical agents from a nuclear power plant, manufacturing or processing plant, research facility, or hospital is disclosed.
摘要翻译：公开了使用半胱天冬酶抑制剂来治疗由放射性核素，生物剂或化学试剂诱导的细胞死亡。具体而言，治疗由放射性核素，生物制剂或化学制剂接触引起的疾病或病症，放射性核素，生物制剂或化学制剂的扩散，恐怖分子爆炸放射性核素，生物制剂或化学制剂或意外暴露于放射性核素，生物制剂或来自核电厂，制造或加工厂，研究机构或医院的化学制剂。

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