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71. 发明授权

US09290460B2 1-(Arylmethyl)quinazoline-2,4(1H,3H)-diones as PARP inhibitors and the use thereof 有权
标题翻译： 1-（芳基甲基）喹唑啉-2,4（1H，3H） - 二酮作为PARP抑制剂及其用途
公开(公告)号：US09290460B2
公开(公告)日：2016-03-22
申请号：US14006722
申请日：2012-03-31
申请人： Sui Xiong Cai , Ye Edward Tian , Xiuhua Hu
发明人： Sui Xiong Cai , Ye Edward Tian , Xiuhua Hu
IPC分类号： C07D403/12 , A61K31/517 , C07D239/96 , C07D401/06 , A61K45/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
CPC分类号： C07D409/12 , A61K31/517 , A61K45/06 , C07D239/96 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.
摘要翻译：公开了由式（I）表示的1-（芳基甲基）喹唑啉-2,4（1H，3H） - 二酮，其中Ar，R 1 -R 6在本文中定义。具有式（I）的化合物是PARP抑制剂。因此，本发明的化合物可用于治疗对抑制PARP活性有反应的临床病症。

72. 发明授权

US08258145B2 Method of treating brain cancer 有权
标题翻译：治疗脑癌的方法
公开(公告)号：US08258145B2
公开(公告)日：2012-09-04
申请号：US11773285
申请日：2007-07-03
申请人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma
发明人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma
IPC分类号： A61K31/517 , A61K31/535 , A61K31/47
CPC分类号： A61K31/4709 , A61K31/517 , A61K31/5377
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer.
摘要翻译：公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。本发明的化合物可用于治疗发生异常细胞的不受控制的生长和扩散的各种临床病症，特别是这些化合物在治疗脑癌中的用途。

73. 发明授权

US07989462B2 4-arylamin-or-4-heteroarylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译： 4-芳基氨基 - 或 - 4-杂芳基氨基 - 喹唑啉及其类似物作为胱天蛋白酶的活化剂和凋亡诱导剂及其用途
公开(公告)号：US07989462B2
公开(公告)日：2011-08-02
申请号：US11773303
申请日：2007-07-03
申请人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma , Hong Zhang , Kazuyuki Suzuki
发明人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma , Hong Zhang , Kazuyuki Suzuki
IPC分类号： A01N43/90 , A61K31/519 , C07D401/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D239/02
CPC分类号： C07D239/94 , C07D239/72 , C07D403/12
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症。

74. 发明授权

US07842805B2 Pharmaceutical compounds as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：药物化合物作为胱天蛋白酶的活化剂和凋亡诱导剂及其用途
公开(公告)号：US07842805B2
公开(公告)日：2010-11-30
申请号：US11773293
申请日：2007-07-03
申请人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Songchun Jiang , Robert J. Halter , Rachel Slade , Yevgeniya Klimova
发明人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Songchun Jiang , Robert J. Halter , Rachel Slade , Yevgeniya Klimova
IPC分类号： C07D403/12 , C07D253/08 , A61K31/53 , A61P35/00
CPC分类号： C07D237/34 , C07D253/08
摘要： Disclosed are 1-arylamino-phthalazines, 4-arylamino-benzo[d][1,2,3]triazines, and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：公开了1-芳基氨基 - 酞嗪，4-芳基氨基 - 苯并[d] [1,2,3]三嗪及其类似物作为胱天蛋白酶的活化剂和凋亡诱导剂。本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症。

75. 发明授权

US07592143B2 Methods of treating diseases responsive to induction of apoptosis and screening assays 失效
标题翻译：治疗对凋亡诱导作用的疾病的筛选方法和筛选试验
公开(公告)号：US07592143B2
公开(公告)日：2009-09-22
申请号：US10826909
申请日：2004-04-19
申请人： Shailaja Kasibhatla , Sui Xiong Cai , Ben Tseng , Katayoun Alavi Jessen , Nicole Marion English , Serguei Maliartchouk , Songchun Jiang , Nilantha Sudath Sirisoma , Han-Zhong Zhang , Jared Kuemmerle
发明人： Shailaja Kasibhatla , Sui Xiong Cai , Ben Tseng , Katayoun Alavi Jessen , Nicole Marion English , Serguei Maliartchouk , Songchun Jiang , Nilantha Sudath Sirisoma , Han-Zhong Zhang , Jared Kuemmerle
IPC分类号： G01N33/53
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 relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using Apoptosis Inducing Proteins (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 heterogeneous 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，筛选方法涉及使用细胞凋亡诱导蛋白（AIPs）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进行均一或异质结合测定; 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。

76. 发明申请

US20080051398A1 METHOD OF TREATING BRAIN CANCER 有权
标题翻译：治疗脑癌的方法
公开(公告)号：US20080051398A1
公开(公告)日：2008-02-28
申请号：US11773285
申请日：2007-07-03
申请人： Sui Xiong Cai , Mark Anderson , Adam Willardsen , Nilantha Sirisoma
发明人： Sui Xiong Cai , Mark Anderson , Adam Willardsen , Nilantha Sirisoma
IPC分类号： A61K31/5377 , A61K31/4709 , A61P25/00 , A61P35/00 , A61K31/517
CPC分类号： A61K31/4709 , A61K31/517 , A61K31/5377
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer.
摘要翻译：公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症，特别是这些化合物在治疗脑癌中的用途。

77. 发明授权

US07176234B2 Derivatives of gambogic acid and analogs as activators of caspases and inducers of apoptosis 失效
标题翻译：葡萄糖酸和类似物的衍生物作为胱天蛋白酶的活化剂和凋亡诱导剂
公开(公告)号：US07176234B2
公开(公告)日：2007-02-13
申请号：US10609670
申请日：2003-07-01
申请人： Sui Xiong Cai , Shailaja Kasibhatla , Kristin P. Ollis , Han-Zhong Zhang , John A. Drewe , Ben Tseng , Nilantha Sudath Sirisoma
发明人： Sui Xiong Cai , Shailaja Kasibhatla , Kristin P. Ollis , Han-Zhong Zhang , John A. Drewe , Ben Tseng , Nilantha Sudath Sirisoma
IPC分类号： A61K31/352 , C07D313/06
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。

78. 发明授权

US06984718B2 Fluorescence dyes and their applications for whole-cell fluorescence screening assays for caspases, peptidases, proteases and other enzymes and the use thereof 失效
标题翻译：荧光染料及其在半胱氨酸蛋白酶，肽酶，蛋白酶和其他酶的全细胞荧光筛选测定中的应用及其用途
公开(公告)号：US06984718B2
公开(公告)日：2006-01-10
申请号：US10138375
申请日：2002-05-06
申请人： Han-Zhong Zhang , Sui Xiong Cai , John A. Drewe , Wu Yang
发明人： Han-Zhong Zhang , Sui Xiong Cai , John A. Drewe , Wu Yang
IPC分类号： C07K5/00 , G01N33/573
CPC分类号： C07D493/10 , C07D311/82 , C07K5/06191 , C07K5/0827 , C07K5/1027 , C07K7/06 , Y10T436/142222
摘要： The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
摘要翻译：本发明涉及新的荧光染料，新的荧光和荧光报道分子和新的酶测定方法，其可用于检测来自任何活生物体的全细胞，细胞系和组织样品中参与细胞凋亡的半胱天冬酶和其它酶的活性或器官。报告分子和测定方法可以用于药物筛选程序中，以鉴定在整个细胞或组织中作为半胱天冬酶级联的抑制剂或诱导剂的化合物。本文所述的试剂和测定法也可用于确定人类癌细胞对用化学治疗药物治疗的化学敏感性。本发明还涉及可用于检测2型甲硫氨酸氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶，HCMV蛋白酶和HCV蛋白酶的活性的新的荧光和荧光报道分子和新的酶测定方法。

79. 发明授权

US06613762B2 Gambogic acid, analogs and derivatives as activators of caspases and inducers of apoptosis 失效
标题翻译：甘草酸，类似物和衍生物作为胱天蛋白酶的活化剂和凋亡诱导剂
公开(公告)号：US06613762B2
公开(公告)日：2003-09-02
申请号：US10066805
申请日：2002-02-06
申请人： Sui Xiong Cai , Han-Zhong Zhang , Shailaja Kasibhatla , Federico C. Gaeta
发明人： Sui Xiong Cai , Han-Zhong Zhang , Shailaja Kasibhatla , Federico C. Gaeta
IPC分类号： A61K31352
CPC分类号： C07D493/20 , A61K31/352 , A61K31/4025 , A61K31/4178 , A61K31/4188 , A61K31/4433 , A61K31/45 , A61K31/453 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/5513 , C07D493/22 , C07D519/00
摘要： The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined in the specification.
摘要翻译：本发明涉及由通式I-III表示的吡啶酸，类似物及其衍生物：其中R1-R5在说明书中定义。

80. 发明授权

US06335429B1 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof 有权
标题翻译：荧光或荧光报告分子及其在半胱氨酸蛋白酶和其他酶的全细胞荧光筛选测定中的应用及其用途
公开(公告)号：US06335429B1
公开(公告)日：2002-01-01
申请号：US09521650
申请日：2000-03-08
申请人： Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： C07K1702
CPC分类号： G01N15/1456 , C12Q1/68 , G01N33/533 , G01N2015/1006 , G01N2015/1488 , Y10S436/80
摘要： The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
摘要翻译：本发明涉及新的荧光染料，新的荧光和荧光报道分子和新的酶测定方法，其可用于检测来自任何活生物体的全细胞，细胞系和组织样品中参与细胞凋亡的半胱天冬酶和其它酶的活性或器官。报告分子和测定方法可以用于药物筛选程序中，以鉴定在整个细胞或组织中作为半胱天冬酶级联的抑制剂或诱导剂的化合物。本文所述的试剂和测定法也可用于确定人类癌细胞对用化学治疗药物治疗的化学敏感性。本发明还涉及可用于检测2型甲硫氨酸氨基肽酶，二肽基肽酶IV，钙蛋白酶，氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶的活性的新型荧光和荧光报告分子和新的酶测定方法， HCMV蛋白酶和HCV蛋白酶。

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