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1. 发明专利

AU2916601A Inhibition of cell motility and angiogenesis 未知
公开(公告)号：AU2916601A
公开(公告)日：2001-04-30
申请号：AU2916601
申请日：2000-10-20
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR
发明人： BOTTARO DONALD P , ATABEY SAFIYE N , SORIANO JESUS V , BRECKENRIDGE DIANE E , YAO ZHU-JUN , GAO YANG
IPC分类号： C12Q1/02 , A61K38/00 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07K5/08 , C07K5/093 , C12Q1/48
摘要： Disclosed are methods of inhibiting cell motility, for example, by inhibiting the binding between an intracellular transducer and a receptor protein tyrosine kinase, and more particularly by inhibiting hepatocyte growth factor (HGF) induced cell motility. The present invention also provides a method of inhibiting angiogenesis. The methods of the present invention employ peptides such as phosphotyrosyl mimetics. The present invention further provides methods of preventing and/or treating diseases, disorders, states, or conditions such as cancer, particularly metastatic cancer comprising administering to a mammal of interest one or more peptides of the present invention. Also disclosed are methods of blocking HGF, VEGF, or bFGF-stimulated migration, cell proliferation, and formation of capillary-like structures

2. 发明申请

WO2013016441A1 HIV INTEGRASE INHIBITORY OXOISOINDOLINE SULFONAMIDES 审中-公开
标题翻译：艾滋病病毒综合抑制氧化硫丹磺胺
公开(公告)号：WO2013016441A1
公开(公告)日：2013-01-31
申请号：PCT/US2012/048169
申请日：2012-07-25
申请人： THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH & HUMAN SERVICES , ZHAO, Xue, Zhi , HUGHES, Stephen, H. , VU, Bao-Han, Christie , SMITH, Steven , JOHNSON, Barry , POMMIER, Yves , BURKE, Terrence, R., Jr.
发明人： ZHAO, Xue, Zhi , HUGHES, Stephen, H. , VU, Bao-Han, Christie , SMITH, Steven , JOHNSON, Barry , POMMIER, Yves , BURKE, Terrence, R., Jr.
IPC分类号： C07D209/46 , C07D401/12 , C07D403/14 , C07D515/04 , A61K31/4035 , A61P31/18
CPC分类号： C07D209/46 , C07D401/12 , C07D403/12 , C07D403/14 , C07D515/04
摘要： Novel oxoisoindoline sulfonamide integrase inhibitors are useful to inhibit HIV activity, and are therefore suitable for treatment or prophylaxis of HIV infection, for example in the treatment or prevention of AIDS. In particular embodiments, the inhibitors are oxoisoindoline-4- sulfonamides, such as 6,7- dihydroxy- 1 -oxoisomdolirie-4-sulfonamides.
摘要翻译：新的氧代异二氢吲哚磺酰胺整合酶抑制剂可用于抑制HIV活性，因此适用于治疗或预防HIV感染，例如用于治疗或预防艾滋病。在具体实施方案中，抑制剂是氧代异二氢吲哚-4-磺酰胺，例如6,7-二羟基-1-氧代异恶唑烷-4-磺酰胺。

3. 发明申请

WO2012142245A2 PEPTIDE MIMETIC LIGANDS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE 审中-公开
标题翻译： POLO-like激素的肽类化合物1 POLO BOX域及其使用方法
公开(公告)号：WO2012142245A2
公开(公告)日：2012-10-18
申请号：PCT/US2012033259
申请日：2012-04-12
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R , QIAN WENJIAN , LIU FA , LEE KYUNG S , PARK JUNG-EUN
发明人： BURKE TERRENCE R , QIAN WENJIAN , LIU FA , LEE KYUNG S , PARK JUNG-EUN
IPC分类号： C07K14/435 , A61K47/48 , A61P35/00 , C12N9/12
CPC分类号： C07K7/06 , A61K38/00 , A61K47/60 , C07K1/006 , C07K5/0827 , C12N9/12 , C12Y207/11021
摘要： Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
摘要翻译：提供了通过polo-box结构域结合polo样激酶的新型化合物。在某些实施方案中，新化合物是PEG化肽。根据本发明的聚乙二醇化肽表现出高PBD结合亲和力。在某些实施方案中，聚乙二醇化肽还在整个细胞系统中获得活性。本发明还提供通过马球结构域结合polo样激酶并具有减少的阴离子电荷的化合物。还提供了聚乙二醇化肽的设计和/或合成方法及其使用方法。本发明提供了化合物的使用方法和化合物的合成方法。

4. 发明申请

WO2010132869A2 PEPTIDE MIMETIC LIGANDS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE 审中-公开
标题翻译： POLO-like激素的肽类化合物1 POLO BOX域及其使用方法
公开(公告)号：WO2010132869A2
公开(公告)日：2010-11-18
申请号：PCT/US2010/035069
申请日：2010-05-17
申请人： GOVERNMENT OF THE U.S.A., AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , BURKE, Terrence, R. , LIU, Fa , LEE, Kyung, S. , PARK, Jung-eun
发明人： BURKE, Terrence, R. , LIU, Fa , LEE, Kyung, S. , PARK, Jung-eun
IPC分类号： C07K7/06
CPC分类号： C07K7/06 , A61K38/00
摘要： Found in various eukaryotic organisms, polo-like kinases (collectively, Plks) are a conserved subfamily of Ser/Thr protein kinases that play critical roles in cell proliferation. Provided herein are compounds that specifically inhibit the activity of Plks, specifically Plkl. Further provided herein are methods for use of the compounds for the treatment of hyperprolif erative disorders, particularly cancer. Also provided are uses of the compounds for the preparation of a medicament.
摘要翻译：在各种真核生物中发现，polo样激酶（统称为Plks）是Ser / Thr蛋白激酶的保守亚家族，在细胞增殖中起关键作用。本文提供了特异性抑制Plks，特别是Plk1活性的化合物。本文进一步提供的是使用该化合物治疗过度扩张性疾病，特别是癌症的方法。还提供了化合物用于制备药物的用途。

5. 发明申请

WO2004003005A3 SH2 DOMAIN BINDING INHIBITORS 审中-公开
标题翻译： SH2域绑定抑制剂
公开(公告)号：WO2004003005A3
公开(公告)日：2007-02-01
申请号：PCT/US0319987
申请日：2003-06-26
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , SHI ZHEN-DAN , GAO YANG
发明人： BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , SHI ZHEN-DAN , GAO YANG
IPC分类号： A61K38/12 , A61K38/00 , A61K38/02 , A61K38/05 , A61K38/06 , A61K38/08 , A61P35/00 , C07C211/30 , C07F9/40 , C07K1/00 , C07K1/04 , C07K1/06 , C07K1/14 , C07K5/06 , C07K5/08 , C07K5/12 , C07K7/04 , C07K7/56 , G01N33/68
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827 , C07K5/123 , C07K5/126 , C07K7/56
摘要： Disclosed are compounds for SH2 domain binding inhibition, for example, a compound of formula (I), wherein R 1 is a lipophile; R 2 , in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R 3 is hydrogen, azido, amino, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, or alkylcarbonylamino, wherein the alkyl portion of R 3 may be optionally substituted with a substituent selected from the group consisting of halo, hydroxy, carboxyl, amino, aminoalkyl, alkyl, alkoxy, and keto; R 6 is a linker; AA is an amino acid; and n is 1 to 6; or a salt thereof. The conformationally compounds provide enhanced binding affinity with SH2 domain protein. Also disclosed are a pharmaceutical compositions and a method for inhibiting an SH2 domain from binding with a phosphoprotein.
摘要翻译：公开了用于SH2结构域结合抑制的化合物，例如式（I）的化合物，其中R 1是亲脂体; R 2与苯环组合是苯基磷酸酯模拟基团或被保护的苯基磷酸酯模拟基团; R 3是氢，叠氮基，氨基，羧基烷基，烷氧基羰基烷基，氨基羰基烷基或烷基羰基氨基，其中R 3的烷基部分可以任选地被选自由卤素，羟基，羧基，氨基，氨基烷基，烷基，烷氧基和酮基组成; R 6是连接体; AA是氨基酸; n为1〜6; 或其盐。构象化合物提供与SH2结构域蛋白质增强的结合亲和力。还公开了用于抑制SH2结构域与磷蛋白结合的药物组合物和方法。

6. 发明申请

WO2004065411A3 PEPTIDES 审中-公开
标题翻译：肽
公开(公告)号：WO2004065411A3
公开(公告)日：2005-01-27
申请号：PCT/US2004000669
申请日：2004-01-12
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR , LEE KYEONG , GAO YANG , PHAN JASON , WAUGH DAVID S
发明人： BURKE TERRENCE R JR , LEE KYEONG , GAO YANG , PHAN JASON , WAUGH DAVID S
IPC分类号： A61K38/00 , C07K5/093 , C07K38/00
CPC分类号： C07K5/0819 , A61K38/00 , Y02P20/55
摘要： Disclosed are compounds which are tripeptides of the formula P-A-B-C or prodrugs thereof, wherein A is an amino acid having a carboxy alkyl group (e.g., carboxy C1-C6 alkyl group), B is tyrosine, phenylalanine, or a substituted tyrosine or phenylalanine, C is a hydrophobic amino acid, and P is an amine protecting group protecting the amine end of A. Also disclosed are pharmaceutical compositions comprising such a compound and a pharmaceutically acceptable carrier, and a method of treating an animal, e.g., a human, exposed to or infected by Yersihia pestis. The compounds find use as anti-bioterrorism agents.
摘要翻译：公开了作为式PABC或其前药的三肽的化合物，其中A是具有羧基烷基的氨基酸（例如羧基C 1 -C 6烷基），B是酪氨酸，苯丙氨酸或取代的酪氨酸或苯丙氨酸，C 是疏水性氨基酸，P是保护A的胺末端的胺保护基。还公开了包含这种化合物和药学上可接受的载体的药物组合物，以及治疗动物（例如人）暴露于或感染鼠疫耶尔氏酵母。该化合物可用作抗生物恐怖剂。

7. 发明申请

WO0216407A3 SH2 DOMAIN BINDING INHIBITORS 审中-公开
标题翻译： SH2域绑定抑制剂
公开(公告)号：WO0216407A3
公开(公告)日：2003-11-20
申请号：PCT/US0126078
申请日：2001-08-22
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , GAO YANG
发明人： BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , GAO YANG
IPC分类号： A61K38/00 , A61P35/00 , C07K5/06 , C07K5/065 , C07K5/08 , A61K38/05 , A61K38/06 , C07C211/30 , C07F9/40 , C07K5/087 , G01N33/68
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06191 , C07K5/0827
摘要： Disclosed are compounds for SH2 domain binding inhibition. For example, disclosed is a compound of formula (I) wherein R1 is a lipophile; R2, in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R3 is hydrogen, azido, amino, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, or alkylcarbonylamino, wherein the alkyl portion of R3 may be optionally substituted with a substituent selected from the group consisting of halo, hydroxy, carboxyl, amino, aminoalkyl, alkyl, alkoxy, and keto; R6 is a linker; AA is an amino acid; and n is 1 to 6; or a salt thereof. The compounds of the present invention have the advantage that their conformation is constrained to provide enhanced binding affinity with SH2 domain protein. Also disclosed are a pharmaceutical composition comprising a pharmaceutically or pharmacologically acceptable carrier and a compound of the present invention, a method for inhibiting an SH2 domain from binding with a phosphoprotein comprising contacting an SH2 domain with a compound of the present invention, a method of preventing or treating a disease, state, or condition by the use of one or more of these compounds, and a method for preparing the compounds of the present invention. The present invention further provides intermediates useful in the preparation of the compounds.
摘要翻译：公开了用于SH2结构域结合抑制的化合物。例如，公开了式（I）的化合物，其中R 1是亲油体; R2与苯环组合是苯基磷酸酯模拟基团或被保护的苯基磷酸酯模拟基团; R 3是氢，叠氮基，氨基，羧基烷基，烷氧基羰基烷基，氨基羰基烷基或烷基羰基氨基，其中R3的烷基部分可以任选地被选自卤素，羟基，羧基，氨基，氨基烷基，烷基，烷氧基，和酮 R6是连接体; AA是氨基酸; n为1〜6; 或其盐。本发明的化合物具有这样的优点：它们的构象被限制以提供与SH2结构域蛋白质的增强的结合亲和力。还公开了包含药学上可接受的载体和本发明化合物的药物组合物，一种抑制SH2结构域与磷蛋白结合的方法，包括使SH2结构域与本发明的化合物接触，一种预防或通过使用一种或多种这些化合物治疗疾病，状态或病症，以及制备本发明化合物的方法。本发明还提供可用于制备化合物的中间体。

8. 发明申请

WO2010132869A3 PEPTIDE MIMETIC LIGANDS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE 审中-公开
标题翻译： POLO-like激素的肽类化合物1 POLO BOX域及其使用方法
公开(公告)号：WO2010132869A3
公开(公告)日：2011-04-07
申请号：PCT/US2010035069
申请日：2010-05-17
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R , LIU FA , LEE KYUNG S , PARK JUNG-EUN
发明人： BURKE TERRENCE R , LIU FA , LEE KYUNG S , PARK JUNG-EUN
IPC分类号： C07K7/06 , C12N9/12
CPC分类号： C07K7/06 , A61K38/00
摘要： Found in various eukaryotic organisms, polo-like kinases (collectively, Plks) are a conserved subfamily of Ser/Thr protein kinases that play critical roles in cell proliferation. Provided herein are compounds that specifically inhibit the activity of Plks, specifically Plkl. Further provided herein are methods for use of the compounds for the treatment of hyperprolif erative disorders, particularly cancer. Also provided are uses of the compounds for the preparation of a medicament.
摘要翻译：在各种真核生物中发现，polo样激酶（统称为Plks）是Ser / Thr蛋白激酶的保守亚家族，在细胞增殖中起关键作用。本文提供了特异性抑制Plks，特别是Plk1活性的化合物。本文进一步提供的是使用该化合物治疗过度扩张性疾病，特别是癌症的方法。还提供了化合物用于制备药物的用途。

9. 发明申请

WO2009026248A2 HYDRAZIDE, AMIDE, PHTHALIMIDE AND PHTHALHYDRAZIDE ANALOGS AS INHIBITORS OF RETROVIRAL INTEGRASE 审中-公开
标题翻译：酰肼，酰胺，邻苯二甲酰亚胺和邻苯二甲酰肼类似物作为逆转录病毒整合酶的抑制剂
公开(公告)号：WO2009026248A2
公开(公告)日：2009-02-26
申请号：PCT/US2008/073511
申请日：2008-08-18
申请人： THE GOVERNMENT OF THE UNITED STATES, AS REPRESENTED BY THE SECRETARY OF HEALTH AND HUMAN SERVICES, NATIONAL INSTITUTES OF HEALTH, OFFICE OF TECHNOLOGY TRANSFER , BURKE, Terrence R., Jr. , ZHAO, Xue Zhi , SEMENOVA, Elena A. , MADDALI, Kasthuraiah , POMMIER, Yves
发明人： BURKE, Terrence R., Jr. , ZHAO, Xue Zhi , SEMENOVA, Elena A. , MADDALI, Kasthuraiah , POMMIER, Yves
IPC分类号： C07D207/36 , C07D209/46 , C07D209/48 , C07D213/69
CPC分类号： C07D213/81 , C07D207/416 , C07D209/46 , C07D209/48 , C07D213/82 , C07D401/06 , C07D403/10 , C07D417/04
摘要： The present invention provides catechol-containing hydrazides, amides, phthalimide and phthalhydrazide analogs. These compounds are inhibitors of retroviral integrase, an essential enzyme for the proliferation of retroviruses such as HIV-1. Also provided are pharmaceutical compositions comprising at least one of the catechol-containing hydrazides, amides, phthalimide or phthalhydrazide analogs and a method of using the hydrazide, amide, phthalimide and phthalhydrazide analogs to inhibit retroviral proliferation and as therapeutics for the treatment of AIDS.
摘要翻译：本发明提供了含有儿茶酚的酰肼，酰胺，邻苯二甲酰亚胺和酞酰肼类似物。这些化合物是逆转录病毒整合酶的抑制剂，逆转录病毒整合酶是逆转录病毒如HIV-1增殖的必需酶。还提供了包含含儿茶酚的酰肼，酰胺，邻苯二甲酰亚胺或酞酰肼类似物中的至少一种的药物组合物，以及使用酰肼，酰胺，邻苯二甲酰亚胺和酞酰肼类似物抑制逆转录病毒增殖并作为治疗AIDS的方法。 / p>

10. 发明申请

WO2008036565A1 TRIPEPTIDES FOR TREATING CANCER METASTASIS, PROSTATE CANCER AND MELANOMA 审中-公开
标题翻译：治疗癌症METASTASIS，前列腺癌和MELANOMA的TRIPEPTIDES
公开(公告)号：WO2008036565A1
公开(公告)日：2008-03-27
申请号：PCT/US2007/078494
申请日：2007-09-14
申请人： GOVERNMENT OF THE UNITED STATES, REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , BOTTARO, Donald P. , GIUBELLINO, Alessio , ATABEY, Safiye N. , SORIANO, Jesus V. , BRECKENRIDGE, Diane E. , BURKE, Terrence R.
发明人： BOTTARO, Donald P. , GIUBELLINO, Alessio , ATABEY, Safiye N. , SORIANO, Jesus V. , BRECKENRIDGE, Diane E. , BURKE, Terrence R.
IPC分类号： A61K38/06 , A61P35/00 , A61P35/04
CPC分类号： C07K5/0819 , A61K38/05 , A61K38/06 , A61K38/07 , C07K5/0827
摘要： Disclosed are methods of inhibiting cell motility, for example, by inhibiting the binding between an intracellular transducer and a receptor protein tyrosine kinase, and more particularly by inhibiting hepatocyte growth factor (HGF) induced cell motility. The present invention also provides a method of inhibiting angiogenesis. The methods of the present invention employ peptides such as phosphotyrosyl mimetics. Also disclosed are methods of preventing and/or treating diseases, disorders, states, or conditions such as cancer, particularly metastatic cancer, for example, melanoma or prostate cancer, comprising administering to a mammal of interest one or more peptides of the present invention. Also disclosed are methods of blocking blocks HGF, VEGF, or bFGF-stimulated migration, cell proliferation, and formation of capillary-like structures.
摘要翻译：公开了抑制细胞运动性的方法，例如通过抑制细胞内换能器和受体蛋白酪氨酸激酶之间的结合，更具体地通过抑制肝细胞生长因子（HGF）诱导的细胞运动性。本发明还提供抑制血管发生的方法。本发明的方法使用诸如磷酸二甲酰基模拟物之类的肽。还公开了预防和/或治疗诸如癌症，特别是转移性癌症，例如黑素瘤或前列腺癌的疾病，病症，状态或病症的方法，其包括给感兴趣的哺乳动物施用本发明的一种或多种肽。还公开了阻断HGF，VEGF或bFGF刺激的迁移，细胞增殖和毛细血管样结构的形成的方法。

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