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1. 发明授权

US07270801B2 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof 失效
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：US07270801B2
公开(公告)日：2007-09-18
申请号：US10829381
申请日：2004-04-22
申请人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： A61N49/00
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。

2. 发明授权

US06342611B1 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for capsases and other enzymes and the use thereof 失效
标题翻译：荧光或荧光报道分子及其在全酶抑制剂中的应用及其用途
公开(公告)号：US06342611B1
公开(公告)日：2002-01-29
申请号：US09168888
申请日：1998-10-09
申请人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： C07D31188
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。

3. 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。

4. 发明授权

US06759207B2 Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof 失效
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：US06759207B2
公开(公告)日：2004-07-06
申请号：US09947387
申请日：2001-09-07
申请人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
发明人： Eckard Weber , Sui Xiong Cai , John F. W. Keana , John A. Drewe , Han-Zhong Zhang
IPC分类号： G01N33573
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。

5. 发明授权

US06949516B2 Dipeptide apoptosis inhibitors and the use thereof 失效
公开(公告)号：US06949516B2
公开(公告)日：2005-09-27
申请号：US10429095
申请日：2003-05-05
申请人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
发明人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
IPC分类号： A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D233/54 , C07D277/16 , C07K5/06 , A61K38/04 , C07C233/45 , C07K5/04
CPC分类号： C07D233/64 , A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D277/16 , C07K5/06191 , C12N2810/40 , Y10S514/885
摘要： The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

6. 发明授权

US06184210B2 Dipeptide apoptosis inhibitors and the use thereof 有权
标题翻译：二肽凋亡抑制剂及其用途
公开(公告)号：US06184210B2
公开(公告)日：2001-02-06
申请号：US09270736
申请日：1999-03-16
申请人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe
发明人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe
IPC分类号： A61K3805
CPC分类号： C07D233/64 , A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D277/16 , C07K5/06191 , C12N2810/40 , Y10S514/885
摘要： The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
摘要翻译：本发明涉及其由通式I表示的新型二肽：其中R1-R3和AA在本文中定义。本发明涉及发现具有式I的化合物是凋亡性细胞死亡的有效抑制剂。因此，本发明的抑制剂可以在发生细胞，组织或整个器官的损失的各种临床病症中阻滞或阻断细胞死亡。

7. 发明授权

US06596693B1 Dipeptide apoptosis inhibitors and the thereof 失效
标题翻译：二肽凋亡抑制剂及其
公开(公告)号：US06596693B1
公开(公告)日：2003-07-22
申请号：US09653279
申请日：2000-08-31
申请人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
发明人： John F. W. Keana , Sui Xiong Cai , John Guastella , Wu Yang , John A. Drewe , Eckard Weber
IPC分类号： A61K3805
CPC分类号： C07D233/64 , A61K38/00 , C07C237/22 , C07C271/22 , C07C323/60 , C07D277/16 , C07K5/06191 , C12N2810/40 , Y10S514/885
摘要： The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
摘要翻译：本发明涉及其由通式I表示的新型二肽：其中R1-R3和AA在本文中定义。本发明涉及发现具有式I的化合物是凋亡性细胞死亡的有效抑制剂。因此，本发明的抑制剂可以在发生细胞，组织或整个器官的损失的各种临床病症中阻滞或阻断细胞死亡。

8. 发明授权

US07435750B2 Method of using substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：使用取代的3-芳基-5-芳基 - [1,2,4] - 恶二唑和类似物作为胱天蛋白酶的活化剂和凋亡诱导剂的方法及其用途
公开(公告)号：US07435750B2
公开(公告)日：2008-10-14
申请号：US11074077
申请日：2005-03-08
申请人： Sui Xiong Cai , Han-Zhong Zhang , John A. Drewe , P. Sanjeeva Reddy , Shailaja Kasibhatla , Jared Daniel Kuemmerle , Kristin P. Ollis
发明人： Sui Xiong Cai , Han-Zhong Zhang , John A. Drewe , P. Sanjeeva Reddy , Shailaja Kasibhatla , Jared Daniel Kuemmerle , Kristin P. Ollis
IPC分类号： A61K31/422 , A61K31/4245 , A61K31/443 , A61K31/4709 , A61K31/4155 , A61K31/4178 , A61K31/4025 , A61K31/381 , A61K31/341 , A61K31/519 , A61K31/4725
CPC分类号： C07D413/14 , A61K31/335 , A61K31/38 , A61K31/395 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/14 , C07D471/04
摘要： The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may 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：本发明涉及由式I表示的取代的3-芳基-5-芳基 - [1,2,4] - 恶二唑及其类似物：其中Ar 1，Ar 3 A，B和D在本文中定义。本发明还涉及发现具有式I的化合物是胱天蛋白酶的活化剂和凋亡诱导剂。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在异常细胞发生不受控制的生长和扩散的各种临床病症中诱导细胞死亡。

9. 发明授权

US07041685B2 Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：取代的3-芳基-5-芳基 - [1,2,4] - 恶二唑和类似物作为胱天蛋白酶的激活剂和凋亡诱导剂及其用途
公开(公告)号：US07041685B2
公开(公告)日：2006-05-09
申请号：US10164705
申请日：2002-06-10
申请人： Sui Xiong Cai , Han-Zhong Zhang , John A. Drewe , P. Sanjeeva Reddy , Shailaja Kasibhatla , Jared Daniel Kuemmerle , Kristin P. Ollis
发明人： Sui Xiong Cai , Han-Zhong Zhang , John A. Drewe , P. Sanjeeva Reddy , Shailaja Kasibhatla , Jared Daniel Kuemmerle , Kristin P. Ollis
IPC分类号： A61K31/44 , C07D413/14
CPC分类号： C07D413/14 , A61K31/335 , A61K31/38 , A61K31/395 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/14 , C07D471/04
摘要： The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may 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：本发明涉及由式I表示的取代的3-芳基-5-芳基 - [1,2,4] - 恶二唑及其类似物：其中Ar 1，Ar 3 A，B和D在本文中定义。本发明还涉及发现具有式I的化合物是胱天蛋白酶的活化剂和凋亡诱导剂。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在异常细胞发生不受控制的生长和扩散的各种临床病症中诱导细胞死亡。

10. 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。

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