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1. 发明授权

US07767645B2 SH2 domain binding inhibitors 有权
标题翻译： SH2结构域结合抑制剂
公开(公告)号：US07767645B2
公开(公告)日：2010-08-03
申请号：US11932424
申请日：2007-10-31
申请人： Terrence R. Burke, Jr. , Zhen-Dan Shi , Sang-Uk Kang
发明人： Terrence R. Burke, Jr. , Zhen-Dan Shi , Sang-Uk Kang
IPC分类号： A61K38/12
CPC分类号： C07K5/021 , A61K38/00 , C07K5/06078
摘要： Disclosed are compounds represented by the formula: or a pharmaceutically acceptable salt or isomer thereof, wherein R1-R6 are as defined in the specification. These compounds are targeted for use as inhibitors of SH2 domain binding with a phosphoprotein, and are contemplated for use in a number of diseases including cancer. Also disclosed are pharmaceutical compositions comprising a compound of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了由下式表示的化合物或其药学上可接受的盐或异构体，其中R 1 -R 6如说明书中所定义。这些化合物被靶向用作与磷蛋白SH2结构域结合的抑制剂，并且被预期用于许多疾病，包括癌症。还公开了包含本发明化合物和药学上可接受的载体的药物组合物。

2. 发明授权

US06977241B2 SH2 domain binding inhibitors 失效
标题翻译： SH2结构域结合抑制剂
公开(公告)号：US06977241B2
公开(公告)日：2005-12-20
申请号：US10362231
申请日：2001-08-22
申请人： Terrence R. Burke, Jr. , Chang-Qing Wei , Johannes H. Voigt , Yang Gao
发明人： Terrence R. Burke, Jr. , Chang-Qing Wei , Johannes H. Voigt , Yang Gao
IPC分类号： A61K38/00 , A61P35/00 , C07K5/06 , C07K5/065 , C07K5/08 , A61K38/02 , C07K2/00
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, forms 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. Also disclosed are a pharmaceutical composition, a method for inhibiting an SH2 domain from binding with a phosphoprotein and a method of treating breast cancer.
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是亲脂体; R 2与苯环组合形成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。还公开了药物组合物，抑制SH2结构域与磷蛋白结合的方法和治疗乳腺癌的方法。

3. 发明授权

US5475129A Phosphonoalkyl phenylalanine compounds suitably protected for use in peptide synthesis 失效
标题翻译：适合保护用于肽合成的膦酰烷基苯丙氨酸化合物
公开(公告)号：US5475129A
公开(公告)日：1995-12-12
申请号：US73088
申请日：1993-06-08
申请人： Terrence R. Burke, Jr. , Mark S. Smyth , Benjamin B. Lim
发明人： Terrence R. Burke, Jr. , Mark S. Smyth , Benjamin B. Lim
IPC分类号： C07F9/40
CPC分类号： C07F9/4056 , C07F9/4065
摘要： The disclosure is concerned with providing phosphonic acid-containing derivatives of phenylalanine and optically active isomers thereof, which are functionalized in a manner which makes them suitable for facile incorporation into peptides using standard solid-phase or solution-phase techniques.
摘要翻译：本公开涉及提供苯丙氨酸及其光学活性异构体的含膦酸衍生物，其以使得它们适合于使用标准固相或溶液相技术容易地掺入肽的方式官能化。

4. 发明授权

US07226991B1 Phenylalanine derivatives 有权
标题翻译：苯丙氨酸衍生物
公开(公告)号：US07226991B1
公开(公告)日：2007-06-05
申请号：US09937150
申请日：2000-03-23
申请人： Terrence R. Burke, Jr. , Yang Gao , Zhu-jun Yao , Dajun Yang
发明人： Terrence R. Burke, Jr. , Yang Gao , Zhu-jun Yao , Dajun Yang
IPC分类号： C07K5/08
CPC分类号： C07K5/0812 , A61K38/00 , C07K7/06
摘要： Disclosed herein are phenylalanine derivative compounds of the following formula W—Y—(AA)n—Z wherein Y is a phenylalanyl radical, AA is an amino acid, n is an integer of 1 to 15, and substituent variables W and Z are as described herein. The compounds can be used to inhibit SH2 binding with phosphoproteins, and to inhibit proliferation of tumor cells.
摘要翻译：本文公开的是下式的苯丙氨酸衍生物化合物：α-in-line-formula description =“In-line formula”end =“lead”？> WY-（AA）n -Z < -line-formula description =“In-line Formulas”end =“tail”？>其中Y是苯丙氨酰基，AA是氨基酸，n是1到15的整数，取代基变量W和Z如上所述这里。该化合物可用于抑制与磷蛋白结合的SH2，并抑制肿瘤细胞的增殖。

5. 发明授权

US5200546A Phosphonoalkyl phenylalanine compounds suitably protected for use in peptide synthesis 失效
标题翻译：适用于肽合成的适合保护的磷酰基苯基亚胺化合物
公开(公告)号：US5200546A
公开(公告)日：1993-04-06
申请号：US767621
申请日：1991-09-30
申请人： Terrence R. Burke, Jr. , Benjamin B. Lim
发明人： Terrence R. Burke, Jr. , Benjamin B. Lim
IPC分类号： C07K1/06 , C07F9/40
CPC分类号： C07F9/4056 , C07F9/4065
摘要： There are disclosed novel compounds of the formula: ##STR1## wherein, x is --CH.sub.2 --, --CHF--, --CF.sub.2, --CHOH-- or --C(O)--;R.sup.6 is hydrogen, benzyl, pentafluorophenyl, nitrophenyl, 1-benzotriazolyl or 1-succinimidoyl;Fmoc is 9-fluorenylmethyloxycarbonyl; and* indicates a chiral carbon atom.The Formula (I) compounds are useful in synthesizing peptides. There are also disclosed novel synthesis methods which include the step of hydrogenating a compound of the Formula ##STR2## wherein R.sup.4 and R.sup.5 are C.sub.1-8 lower alkyl, to give a compound of the formula ##STR3## wherein R.sup.4 and R.sup.5 are as defined above. The compounds of formula (II) are useful as intermediates in preparing certain formula (I) compounds.
摘要翻译：公开了下式的新化合物：其中x是-CH 2 - ， - CHF - ， - C 2 F 2，-CHOH - 或-C（O） - ; R6是氢，苄基，五氟苯基，硝基苯基，1-苯并三唑基或1-琥珀酰亚氨基; Fmoc是9-芴基甲氧基羰基; 和*表示手性碳原子。式（I）化合物可用于合成肽。还公开了新的合成方法，其包括氢化其中R 4和R 5为C 1-8低级烷基的式（III）化合物的步骤，得到下式化合物其中R 4 和R5如上所定义。式（II）化合物可用作制备某些式（I）化合物的中间体。

6. 发明授权

US07825216B2 Phenylanine derivatives 有权
标题翻译：苯胺衍生物
公开(公告)号：US07825216B2
公开(公告)日：2010-11-02
申请号：US11749499
申请日：2007-05-16
申请人： Terrence R. Burke, Jr. , Yang Gao , Zhu-jun Yao , Dajun Yang
发明人： Terrence R. Burke, Jr. , Yang Gao , Zhu-jun Yao , Dajun Yang
IPC分类号： C07K2/00
CPC分类号： C07K5/0819 , A61K38/00 , C07C271/22 , C07D265/32 , C07K5/0812 , C07K5/0827
摘要： The present invention provides phenylalanine derivatives that inhibit SH2 domain binding with a phosphoprotein. These derivatives include compounds of the formula: W—Y-(AA)n-Z wherein n is 0 to 15; Y is a phenylalanyl radical having a phenyl ring, an amine end, and a carboxyl end, the phenyl ring having one or more substituents, e.g., hydroxyl, carboxyl, formyl, carboxyalkyl, carboxyalkyloxy, dicarboxyalkyl, dicarboxyalkyloxy, dicarboxyhaloalkyl, dicarboxyhaloalkyloxy, and phosphonoalkyl, or phosphonohaloalkyl; W is a moiety attached to the nitrogen of Y and is, e.g., alkylcarbonyl, oxalyl, alkylaminooxalyl, arylaminooxalyl, arylalkylaminooxalyl, or alkoxyoxalyl; AA is an amino acid, the amine end of which is attached to the carboxyl end of Y; and Z is an arylalkylamino or arylheterocyclyl alkylamino; or a salt thereof; with the proviso that W is not arylalkylamino when the phenyl ring of phenylalanyl contains a phosphonoalkyl or phosphonohaloalkyl substituent at a position para to the alkylamido group and the ortho and meta positions are unsubstituted. The present invention further provides precursors suitable for preparing the phenylalanine derivatives and a method for the preparation of the precursors. The present invention further provides conjugates comprising a precursor and a conjugant that are covalently linked. These conjugates have biological and/or pharmacological properties.
摘要翻译：本发明提供抑制与磷蛋白结合的SH2结构域的苯丙氨酸衍生物。这些衍生物包括下式的化合物：其中n为0至15的W-Y-（AA）n-Z; Y是具有苯环，胺末端和羧基端的苯丙氨酰基，苯环具有一个或多个取代基，例如羟基，羧基，甲酰基，羧基烷基，羧基烷氧基，二羧基烷基，二羧基烷氧基，二羧基卤代烷基，二羧基卤代烷氧基和膦酰基烷基，或膦酰卤代烷基; W是连接到Y的氮的部分，例如烷基羰基，草酰基，烷基氨基草酰基，芳基氨基草酰基，芳基烷基氨基草酰基或烷氧基草酰基; AA是氨基酸，其末端连接到Y的羧基末端; Z是芳基烷基氨基或芳基杂环基烷基氨基; 或其盐; 条件是当苯丙氨酰基的苯环在烷基酰氨基的对位位置含有膦酰基烷基或膦酰卤代烷基取代基时，W不是芳烷基氨基，邻位和间位是未取代的。本发明还提供适用于制备苯丙氨酸衍生物的前体和前体的制备方法。本发明进一步提供包含共价连接的前体和共轭物的缀合物。这些缀合物具有生物学和/或药理学性质。

7. 发明授权

US5688992A O-malonyltryrosyl compounds, O-malonyltryrosyl compound-containing peptides, and use thereof 失效
标题翻译： O-丙二酰基酪酰基化合物，含有O-丙二酰基特异性基化合物的肽及其用途
公开(公告)号：US5688992A
公开(公告)日：1997-11-18
申请号：US414520
申请日：1995-03-31
申请人： Terrence R. Burke, Jr. , Bin Ye , Miki Akamatsu , Hemanta K. Kole , Xinjian Yan , Peter R. Roller
发明人： Terrence R. Burke, Jr. , Bin Ye , Miki Akamatsu , Hemanta K. Kole , Xinjian Yan , Peter R. Roller
IPC分类号： A61K38/00 , A61K31/195 , A61K31/215 , A61P3/08 , A61P3/10 , A61P35/00 , A61P37/04 , A61P43/00 , C07C229/36 , C07C237/20 , C07C271/22 , C07K5/065 , C07K7/06 , C07K14/47 , C07K14/705 , C07C57/145 , A61K31/19
CPC分类号： C07C271/22 , C07C229/36 , C07C237/20 , C07K14/705 , C07K5/06078 , A61K38/00 , C07C2103/18
摘要： The present invention relates to non-phosphorus containing O-malonyltryrosyl compounds, derivatives thereof, uses of the O-malonyltryrosyl compounds in the synthesis of peptides, and O-malonyltryrosyl compound-containing peptides. The O-malonyltyrosyl malonyltyrosyl compounds and O-malonyltryrosyl compound-containing peptides of the present invention are uniquely stable to phosphotases, capable of crossing cell membranes, suitable for application to peptide synthesis of O-malonyltryrosyl compound-containing peptides, and amenable to prodrag defivatization for delivery into cells. The present invention also provides for O-malonyltryrosyl compound-containing peptides which exhibit inhibitory potency against binding interactions of receptor domains with phosphotyrosyl-containing peptide ligands.
摘要翻译：本发明涉及不含磷的O-壬二酰基特异性基团的化合物，其衍生物，O-丙二酰基二辛基化合物在肽的合成中的应用，以及含有O-丙二酰基二酰基化合物的肽。本发明的O-丙二酰基特异酰基丙二酰基酪氨酸化合物和含O-丙二酰基酪酰基化合物的肽对于能够与细胞膜交叉的磷酸酶是独特稳定的，适用于肽合成含有O-丙二酰基二酰基化合物的肽，并且适于产生衍生化用于送入细胞。本发明还提供了对具有含磷酰基的肽配体的受体结构域的结合相互作用具有抑制效力的含有O-丙二酰基二酰基化合物的肽。

8. 发明授权

US09175038B2 Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 有权
标题翻译： polo样激酶1 polo box结构域的肽模拟配体和使用方法
公开(公告)号：US09175038B2
公开(公告)日：2015-11-03
申请号：US13320726
申请日：2010-05-17
申请人： Terrence R. Burke, Jr. , Fa Liu , Kyung S. Lee , Jung-Eun Park
发明人： Terrence R. Burke, Jr. , Fa Liu , Kyung S. Lee , Jung-Eun Park
IPC分类号： A61K38/08 , A01K61/00 , C07K7/06 , A61K38/00
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 Plk1. Further provided herein are methods for use of the compounds for the treatment of hyperproliferative 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。本文提供特异性抑制Plks活性的化合物，特别是Plk1。本文还提供了用于治疗过度增殖性疾病，特别是癌症的化合物的方法。还提供了化合物用于制备药物的用途。

9. 发明授权

US10266565B2 Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 有权
公开(公告)号：US10266565B2
公开(公告)日：2019-04-23
申请号：US14111540
申请日：2012-04-12
申请人： Terrence R. Burke, Jr. , Fa Liu , Kyung S. Lee , Jung-Eun Park
发明人： Terrence R. Burke, Jr. , Fa Liu , Kyung S. Lee , Jung-Eun Park
IPC分类号： C07K7/06 , C07K1/00 , C07K5/08 , C12N9/12 , A61K47/60 , A61K38/00
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.

10. 发明授权

US07132392B1 Inhibition of cell motility and angiogenesis by inhibitors of Grb2-SH2-domain 有权
标题翻译：通过Grb2-SH2结构域抑制剂抑制细胞运动和血管发生
公开(公告)号：US07132392B1
公开(公告)日：2006-11-07
申请号：US10111192
申请日：2000-10-20
申请人： Donald P. Bottaro , Safiye N. Atabey , Jesus V. Soriano , Diane E. Breckenridge , Zhu-Jun Yao , Yang Gao , Terrence R. Burke, Jr.
发明人： Donald P. Bottaro , Safiye N. Atabey , Jesus V. Soriano , Diane E. Breckenridge , Zhu-Jun Yao , Yang Gao , Terrence R. Burke, Jr.
IPC分类号： A61K38/08 , A61K38/07 , A61K38/06 , C07K7/04 , C07K5/10 , C07K5/08
CPC分类号： A61K38/07 , A61K38/05 , A61K38/06 , C07K5/0819 , 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. 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
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。本发明还提供了预防和/或治疗诸如癌症，特别是转移性癌症的疾病，病症，状态或病症的方法，其包括向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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