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1. 发明授权

US09006247B2 Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases 有权
公开(公告)号：US09006247B2
公开(公告)日：2015-04-14
申请号：US13115376
申请日：2011-05-25
申请人： Zhi-Fu Tao , Xilu Wang , Andrew J. Souers , Nathaniel D. Catron , Gerard M. Sullivan
发明人： Zhi-Fu Tao , Xilu Wang , Andrew J. Souers , Nathaniel D. Catron , Gerard M. Sullivan
IPC分类号： A61K31/497 , C07D401/00 , C07F9/02 , A61K31/44 , A61K31/18 , C07D471/04
CPC分类号： C07D471/04 , A61K31/18 , A61K31/44 , A61K31/496 , A61P35/00 , C07F9/65616 , Y02A50/385 , Y02A50/401 , Y02A50/411 , Y02A50/463
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

2. 发明授权

US08853209B2 1-oxyalkyl-2-carboxy-7-nonsubstituted indole derivatives 有权
标题翻译： 1-氧代烷基-2-羧基-7-非取代的吲哚衍生物
公开(公告)号：US08853209B2
公开(公告)日：2014-10-07
申请号：US13088206
申请日：2011-04-15
申请人： Xiaohong Song , Hong Ding , Steven W. Elmore , Milan Bruncko , David J. Madar , Andrew J. Souers , Cheol-Min Park , Zhi-Fu Tao , Xilu Wang , Aaron R. Kunzer
发明人： Xiaohong Song , Hong Ding , Steven W. Elmore , Milan Bruncko , David J. Madar , Andrew J. Souers , Cheol-Min Park , Zhi-Fu Tao , Xilu Wang , Aaron R. Kunzer
IPC分类号： C07D209/42 , C07D403/04
CPC分类号： C07D209/42 , C07D403/04
摘要： Compounds of Formula I wherein A1, B1, C1, D1, E1, F1 and L1 are as defined herein, which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mdl-1 protein, such as leukemia and lymphoma, are disclosed.
摘要翻译：其中A1，B1，C1，D1，E1，F1和L1如本文所定义的式I化合物，其抑制抗细胞凋亡Mcl-1蛋白的活性，含有该化合物的组合物，以及治疗涉及过表达或未调节的疾病的方法公开了诸如白血病和淋巴瘤的Md1-1蛋白。

3. 发明授权

US08557983B2 Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases 有权
公开(公告)号：US08557983B2
公开(公告)日：2013-10-15
申请号：US12793413
申请日：2010-06-03
申请人： George A. Doherty , Laura A. Hexamer , Robert A. Mantei , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Todd M. Hansen
发明人： George A. Doherty , Laura A. Hexamer , Robert A. Mantei , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Todd M. Hansen
IPC分类号： C07D403/14 , C07D413/14
CPC分类号： C07D213/76 , A61K31/495 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D209/08 , C07D211/06 , C07D211/58 , C07D213/74 , C07D213/84 , C07D231/56 , C07D235/06 , C07D277/24 , C07D295/14 , C07D295/30 , C07D309/04 , C07D309/32 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

4. 发明授权

US07981888B2 1-oxyalkyl-2-carboxyl-7-nonsubstituted indole derivatives 有权
标题翻译： 1-烷氧基-2-羧基-7-非取代的吲哚衍生物
公开(公告)号：US07981888B2
公开(公告)日：2011-07-19
申请号：US12104319
申请日：2008-04-16
申请人： Xiaohong Song , Hong Ding , Steven W. Elmore , Milan Bruncko , David J. Madar , Andrew J. Souers , Cheol-Min Park , Zhi-Fu Tao , Xilu Wang , Aaron R. Kunzer
发明人： Xiaohong Song , Hong Ding , Steven W. Elmore , Milan Bruncko , David J. Madar , Andrew J. Souers , Cheol-Min Park , Zhi-Fu Tao , Xilu Wang , Aaron R. Kunzer
IPC分类号： A61K31/535
CPC分类号： C07D209/42 , C07D403/04
摘要： Compounds of Formula I wherein A1, B1, C1, D1, E1, F1 and L1 are as defined herein, which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein, such as leukemia and lymphoma, are disclosed.
摘要翻译：其中A1，B1，C1，D1，E1，F1和L1如本文所定义的式I化合物，其抑制抗细胞凋亡Mcl-1蛋白的活性，含有该化合物的组合物，以及治疗涉及过表达或未调节的疾病的方法公开了Mcl-1蛋白，如白血病和淋巴瘤。

5. 发明授权

US07956185B2 Cyclobut-3-ene-1,2,-dione inhibitors of polo-like kinases 有权
标题翻译：马球状激酶的环丁-3-烯-1,2， - 二酮抑制剂
公开(公告)号：US07956185B2
公开(公告)日：2011-06-07
申请号：US11753279
申请日：2007-05-24
申请人： Robert B. Diebold , Stevan W. Djuric , Vincent L. Giranda , Laura A. Hexamer , Nan-Horng Lin , Julie M. Miyashiro , Thomas D. Penning , Magdalena Przytulinska , Thomas J. Sowin , Gerard M. Sullivan , Zhi-Fu Tao , Yunsong Tong , Anil Vasudevan , Le Wang , Keith W. Woods , Zhiren Xia , Henry Q. Zhang
发明人： Robert B. Diebold , Stevan W. Djuric , Vincent L. Giranda , Laura A. Hexamer , Nan-Horng Lin , Julie M. Miyashiro , Thomas D. Penning , Magdalena Przytulinska , Thomas J. Sowin , Gerard M. Sullivan , Zhi-Fu Tao , Yunsong Tong , Anil Vasudevan , Le Wang , Keith W. Woods , Zhiren Xia , Henry Q. Zhang
IPC分类号： C07D239/02
CPC分类号： C07D249/14 , C07C225/20 , C07C2601/02 , C07C2601/04 , C07D277/64 , C07D285/06 , C07D333/20
摘要： Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.
摘要翻译：其中X1，C1和D1在本文中定义的式（I）化合物是polo样激酶的抑制剂。式（I）化合物可用于治疗细胞增殖疾病，例如癌症。

6. 发明申请

US20090030196A1 PIM KINASE INHIBITORS AS CANCER CHEMOTHERAPEUTICS 审中-公开
标题翻译： PIM激酶抑制剂作为癌症化学疗法
公开(公告)号：US20090030196A1
公开(公告)日：2009-01-29
申请号：US12133985
申请日：2008-06-05
申请人： Le Wang , Lisa A. Hasvold , Zhi-Fu Tao , Laura Hexamer , Thomas D. Penning
发明人： Le Wang , Lisa A. Hasvold , Zhi-Fu Tao , Laura Hexamer , Thomas D. Penning
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Inhibitors of Pim kinases, ways to make them and methods of treating patients using them are disclosed.
摘要翻译：披露了Pim激酶的抑制剂，制备方法以及使用它们治疗患者的方法。

7. 发明授权

US06713633B1 Compounds capable of cleaving double-stranded DNA and method of utilization of the same 失效
标题翻译：能切割双链DNA的化合物及其利用方法
公开(公告)号：US06713633B1
公开(公告)日：2004-03-30
申请号：US09701264
申请日：2001-08-08
申请人： Hiroshi Sugiyama , Zhi-Fu Tao , Isao Saito
发明人： Hiroshi Sugiyama , Zhi-Fu Tao , Isao Saito
IPC分类号： A61K314164
CPC分类号： A61K31/407 , C07D487/04
摘要： Novel chemical species capable of simultaneously alkylating double-stranded DNA and cleaving the same; methods for alkylating and cleaving DNA by using these species; and anticancer agents with the use of these compounds. Compounds represented by the following general formula (I) which are capable of simultaneously alkylating double-stranded DNA and cleaving the same; a method for alkylating DNA and a method for cleaving double stranded DNA by using these compounds; and medicinal compositions with the use of these compounds: B—L—A(I) wherein B represents a chemical structure capable of recognizing the base sequence of DNA, for example, optionally substituted pyrrole-imidazole polyamide; A represents a chemical structure capable of binding to one base of DNA, for example, the alkylation moiety of duocarmycin A; and L represents a linker capable of binding the chemical structures A and B, for example, vinyl.
摘要翻译：能够同时烷化双链DNA并切割相同的新型化学物质; 通过使用这些物质烷基化和切割DNA的方法; 和使用这些化合物的抗癌剂。由以下通式（I）表示的化合物，其能够同时烷基化双链DNA并将其切割; 用于烷基化DNA的方法和通过使用这些化合物切割双链DNA的方法; 和使用这些化合物的药物组合物：B-L-A（I）其中B表示能够识别DNA碱基序列的化学结构，例如任选取代的吡咯 - 咪唑聚酰胺; A表示能够结合DNA的一个碱基的化学结构，例如二焦耳霉素A的烷基化部分; L表示能够结合化学结构A和B的接头，例如乙烯基。

8. 发明授权

US08546399B2 Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases 有权
标题翻译：凋亡诱导剂用于治疗癌症和免疫和自身免疫性疾病
公开(公告)号：US08546399B2
公开(公告)日：2013-10-01
申请号：US12787682
申请日：2010-05-26
申请人： Milan Bruncko , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa A. Hasvold , Laura Hexamer , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Robert Mantei , Todd M. Hansen
发明人： Milan Bruncko , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa A. Hasvold , Laura Hexamer , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Robert Mantei , Todd M. Hansen
IPC分类号： A61K31/407 , C07D401/12
CPC分类号： C07D401/12 , A61K31/496 , C07D209/82 , C07D401/14 , C07D403/12 , C07D471/04 , C07D519/00 , Y02A50/463
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
摘要翻译：公开了抑制抗凋亡Bcl-2蛋白活性的化合物，含有化合物的组合物和治疗疾病的方法，其中表达抗凋亡Bcl-2蛋白。

9. 发明授权

US08426422B2 Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases 有权
公开(公告)号：US08426422B2
公开(公告)日：2013-04-23
申请号：US12689106
申请日：2010-01-18
申请人： Laura A. Hexamer , Hong Ding , Steven W. Elmore , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Michael D. Wendt
发明人： Laura A. Hexamer , Hong Ding , Steven W. Elmore , Aaron R. Kunzer , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Michael D. Wendt
IPC分类号： A61K31/496 , C07D209/08 , C07D213/71 , C07D231/56 , C07D235/04 , C07D265/02 , C07D285/14 , C07D311/14 , C07D295/155
CPC分类号： C07D295/155 , C07D209/08 , C07D213/71 , C07D231/56 , C07D235/04 , C07D265/02 , C07D285/14 , C07D311/14
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

10. 发明授权

US08232273B2 Heterocyclic compounds and methods of use 有权
标题翻译：杂环化合物和使用方法
公开(公告)号：US08232273B2
公开(公告)日：2012-07-31
申请号：US12641141
申请日：2009-12-17
申请人： Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Peter Czabotar , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Lisa A. Hasvold , Andrew M. Petros , Andrew J. Souers , Zhi-Fu Tao , Le Wang , Xilu Wang , Kurt Deshayes
发明人： Jonathan Bayldon Baell , Chinh Thien Bui , Peter Colman , Peter Czabotar , Danette A. Dudley , Wayne J. Fairbrother , John A. Flygare , Guillaume Laurent Lessene , Chudi Ndubaku , George Nikolakopoulos , Brad Edmund Sleebs , Brian John Smith , Keith Geoffrey Watson , Steven W. Elmore , Lisa A. Hasvold , Andrew M. Petros , Andrew J. Souers , Zhi-Fu Tao , Le Wang , Xilu Wang , Kurt Deshayes
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D417/14 , C07D471/06 , C07D473/00 , C07D487/04 , C07D495/04 , C07D513/04 , C07D513/06
摘要： In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
摘要翻译：一方面，本发明提供了其中变量X1a，X1b，X1c，X1d，Q，A，R1，B，L，E和下标m和n具有如本文所述的含义的式I化合物。另一方面，本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症（例如，癌症，血小板增多症等）的方法的Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。

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