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1. 发明申请

US20110152281A1 COMPOUNDS AND METHOD FOR TREATMENT OF CANCER 有权
标题翻译：化合物和治疗癌症的方法
公开(公告)号：US20110152281A1
公开(公告)日：2011-06-23
申请号：US12810722
申请日：2008-12-24
申请人： Wayne R. Danter , Cheuk Kun Lau
发明人： Wayne R. Danter , Cheuk Kun Lau
IPC分类号： C07D403/12 , C07D401/12 , A61K31/501 , A61K31/496 , A61P35/04 , A61P35/02
CPC分类号： C07D237/08 , C07D401/14 , C07D403/12
摘要： The invention relates to a compound of Formula (I) and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof, wherein X is selected from S or O; R5 is selected from a substituted or unsubstituted aromatic group, a substituted or unsubstituted heteroaromatic group, or (Formula II) and the remaining substituents are described herein; and a composition comprising the thiosemicarbazone and/or the semicarbazone. The invention also relates to a method of administration of a thiocarbazone and/or a semicarbazone; and use thereof to treat a cancer.
摘要翻译：本发明涉及式（I）化合物和/或其药学上可接受的盐，水合物，溶剂化物，互变异构体，旋光异构体，E-异构体，Z-异构体或其组合，其中X选自S或O; R5选自取代或未取代的芳族基团，取代或未取代的杂芳族基团或（式II），其余取代基在本文中描述; 和包含缩氨基硫脲和/或缩氨基脲的组合物。本发明还涉及施用硫卡巴腙和/或缩氨基脲的方法; 及其用途来治疗癌症。

2. 发明申请

US20120195887A1 Inhibitor Compounds and Cancer Treatment Methods 有权
标题翻译：抑制剂化合物和癌症治疗方法
公开(公告)号：US20120195887A1
公开(公告)日：2012-08-02
申请号：US13363558
申请日：2012-02-01
申请人： Wayne R. Danter
发明人： Wayne R. Danter
IPC分类号： A61K31/496 , A61K39/395 , A61K31/7068 , C07D471/04 , A61P35/00 , A61K33/24 , C07D401/14
CPC分类号： C07D215/40 , A61K31/337 , A61K31/439 , A61K31/496 , A61K31/555 , A61K31/704 , A61K33/24 , A61K39/3955 , A61K45/06 , C07D401/12 , C07D471/04 , C07D471/14
摘要： A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.
摘要翻译：用于治疗癌症的抗癌剂和治疗化合物如mTOR-Rictor复合抑制剂，丝氨酸473磷酸化抑制剂，AKT2抑制剂或其组合的协同有效组合，以及方法和其用途。还包括缩氨基硫脲用于治疗有需要的哺乳动物的癌症的方法和用途，其特征在于RAS过度表达，EGFR突变和/或AKT2的过度表达。

3. 发明申请

US20090298855A1 Protein Tyrosine Kinase Inhibitors 有权
标题翻译：蛋白酪氨酸激酶抑制剂
公开(公告)号：US20090298855A1
公开(公告)日：2009-12-03
申请号：US12510862
申请日：2009-07-28
申请人： Wayne R. Danter , Martyn Brown , George Ma , Ghenadie Rusu , Jianhua Zhong , Natalie Lazarowych , Stephen Houldsworth
发明人： Wayne R. Danter , Martyn Brown , George Ma , Ghenadie Rusu , Jianhua Zhong , Natalie Lazarowych , Stephen Houldsworth
IPC分类号： A61K31/506 , C07D401/12 , A61K31/4545 , A61P35/00
CPC分类号： C07D401/14
摘要： The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions in mammals: wherein n is an integer, preferably n is 1; wherein R1 and R2 are independently selected from the group consisting of:
摘要翻译：本发明涉及抑制，调节和/或调节酪氨酸激酶信号转导的式I化合物及其药学上可接受的盐和立体异构体，以及使用它们治疗酪氨酸激酶依赖性疾病的方法和哺乳动物的条件：其中n为整数，优选n为1; 其中R1和R2独立地选自：

4. 发明授权

US08420643B2 Compounds and method for treatment of cancer 有权
标题翻译：化合物和治疗癌症的方法
公开(公告)号：US08420643B2
公开(公告)日：2013-04-16
申请号：US13310506
申请日：2011-12-02
申请人： Wayne R. Danter , Martyn Brown , Franck LePifre
发明人： Wayne R. Danter , Martyn Brown , Franck LePifre
IPC分类号： A61K31/535 , A61K31/497 , C07D403/12 , C07D417/12 , C07D401/12
CPC分类号： C07D401/12 , C07D471/04
摘要： The present invention is directed to methods of use of a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.
摘要翻译：本发明涉及使用式I化合物和/或其药学上可接受的盐，水合物，溶剂化物，互变异构体，旋光异构体或其组合的方法，包含缩氨基硫脲的组合物，其施用方法，及其用途来治疗癌症。

5. 发明授权

US07629347B2 Protein tyrosine kinase inhibitors 有权
标题翻译：蛋白酪氨酸激酶抑制剂
公开(公告)号：US07629347B2
公开(公告)日：2009-12-08
申请号：US10531107
申请日：2003-10-09
申请人： Wayne R. Danter , George Ma , Natalie Lazarowych , Stephen Houldsworth , Martyn Brown , Ghenadie Rusu , Jianhua Zhong
发明人： Wayne R. Danter , George Ma , Natalie Lazarowych , Stephen Houldsworth , Martyn Brown , Ghenadie Rusu , Jianhua Zhong
IPC分类号： C07D401/14 , A61K31/506
CPC分类号： C07D401/14 , A61K31/506
摘要： The present invention relates to uses of the compounds of Formula I as well as pharmaceutically acceptable salts and stereoisomers thereof in methods to treat a variety of tumors in mammals involving abnormal tyrosine kinase signaling, the compounds represented as: wherein R1 and R2 are independently selected from the group consisting of H; alkyl; alkenyl; alkynyl; halogen; aryl; heteroaryl containing N, O, or S; the aryl and heteroaryl may be further substituted with halogen, an alkyl, alkenyl, and alkynyl; NZ1Z2, wherein Z1 and Z2 are independently selected from the group consisting of H and alkyl; and (CO)Y wherein Y is selected from the group consisting of H, alkyl, alkenyl, alkynyl, aryl, heteroaryl containing N, O, or S, and the aryl and heteroaryl may be further substituted with halogen, alkyl, alkenyl, and alkynyl; with the proviso that when R1 is hydrogen, R2 is a group other than hydrogen.
摘要翻译：本发明涉及式I化合物及其药学上可接受的盐和立体异构体在治疗涉及异常酪氨酸激酶信号传导的哺乳动物中的各种肿瘤的方法中的用途，所述化合物表示为：其中R1和R2独立地选自由H组成的组; 烷基; 烯基; 炔基; 卤素; 芳基; 含有N，O或S的杂芳基; 芳基和杂芳基可以进一步被卤素，烷基，烯基和炔基取代; NZ1Z2，其中Z1和Z2独立地选自H和烷基; 和（CO）Y，其中Y选自H，烷基，烯基，炔基，芳基，含有N，O或S的杂芳基，芳基和杂芳基可以进一步被卤素，烷基，烯基和炔基; 条件是当R 1是氢时，R 2是不同于氢的基团。

6. 发明申请

US20110281887A1 COMPOUNDS AND METHOD FOR TREATMENT OF CANCER 有权
标题翻译：化合物和治疗癌症的方法
公开(公告)号：US20110281887A1
公开(公告)日：2011-11-17
申请号：US13190230
申请日：2011-07-25
申请人： Wayne R. Danter , Martyn Brown , Franck LePifre
发明人： Wayne R. Danter , Martyn Brown , Franck LePifre
IPC分类号： A61K31/497 , A61P35/00 , A61P35/02 , A61K31/496
CPC分类号： C07D401/12 , C07D471/04
摘要： The present invention is directed to methods of use of a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.
摘要翻译：本发明涉及使用式I化合物和/或其药学上可接受的盐，水合物，溶剂化物，互变异构体，旋光异构体或其组合的方法，包含缩氨基硫脲的组合物，其施用方法，及其用途来治疗癌症。

7. 发明申请

US20100015140A1 Inhibitor Compounds and Cancer Treatment Methods 有权
标题翻译：抑制剂化合物和癌症治疗方法
公开(公告)号：US20100015140A1
公开(公告)日：2010-01-21
申请号：US12505295
申请日：2009-07-17
申请人： Wayne R. Danter
发明人： Wayne R. Danter
IPC分类号： A61K39/395 , A61K31/497
CPC分类号： C07D215/40 , A61K31/337 , A61K31/439 , A61K31/496 , A61K31/555 , A61K31/704 , A61K33/24 , A61K39/3955 , A61K45/06 , C07D401/12 , C07D471/04 , C07D471/14
摘要： A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.
摘要翻译：用于治疗癌症的抗癌剂和治疗化合物如mTOR-Rictor复合抑制剂，丝氨酸473磷酸化抑制剂，AKT2抑制剂或其组合的协同有效组合，以及方法和其用途。还包括缩氨基硫脲用于治疗有需要的哺乳动物的癌症的方法和用途，其特征在于RAS过度表达，EGFR突变和/或AKT2的过度表达。

8. 发明授权

US08367675B2 Compounds and method for treatment of cancer 有权
公开(公告)号：US08367675B2
公开(公告)日：2013-02-05
申请号：US13190230
申请日：2011-07-25
申请人： Wayne R. Danter , Martyn Brown , Franck LePifre
发明人： Wayne R. Danter , Martyn Brown , Franck LePifre
IPC分类号： A61K31/497 , A61K31/535
CPC分类号： C07D401/12 , C07D471/04
摘要： The present invention is directed to methods of use of a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.

9. 发明申请

US20120077820A1 COMPOUNDS AND METHOD FOR TREATMENT OF CANCER 有权
标题翻译：化合物和治疗癌症的方法
公开(公告)号：US20120077820A1
公开(公告)日：2012-03-29
申请号：US13310506
申请日：2011-12-02
申请人： Wayne R. Danter , Martyn Brown , Franck LePifre
发明人： Wayne R. Danter , Martyn Brown , Franck LePifre
IPC分类号： A61K31/496 , A61P35/00 , A61P35/02 , C07D401/14
CPC分类号： C07D401/12 , C07D471/04
摘要： The present invention is directed to methods of use of a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.
摘要翻译：本发明涉及使用式I化合物和/或其药学上可接受的盐，水合物，溶剂化物，互变异构体，旋光异构体或其组合的方法，包含缩氨基硫脲的组合物，其施用方法，及其用途来治疗癌症。

10. 发明申请

US20080171744A1 COMPOUNDS AND METHOD FOR TREATMENT OF CANCER 有权
标题翻译：化合物和治疗癌症的方法
公开(公告)号：US20080171744A1
公开(公告)日：2008-07-17
申请号：US12013079
申请日：2008-01-11
申请人： Wayne R. Danter , Martyn Brown , Franck LePifre
发明人： Wayne R. Danter , Martyn Brown , Franck LePifre
IPC分类号： A61K31/5375 , A61P35/00 , C07D401/14 , C07D415/00 , A61K31/497
CPC分类号： C07D401/12 , C07D471/04
摘要： The present invention is directed to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.
摘要翻译：本发明涉及式I化合物：和/或药学上可接受的盐，水合物，溶剂化物，互变异构体，旋光异构体或其组合，包含缩氨基硫脲的组合物，其施用方法及其用途治疗癌症。

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