专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US07342095B2 Peptidomimetic inhibitors of STAT activity and uses thereof 有权
标题翻译： STAT活性的拟肽抑制剂及其用途
公开(公告)号：US07342095B2
公开(公告)日：2008-03-11
申请号：US10784309
申请日：2004-02-20
申请人： James Turkson , Richard Jove , Said M. Sebti , Andrew D. Hamilton
发明人： James Turkson , Richard Jove , Said M. Sebti , Andrew D. Hamilton
IPC分类号： A61K38/06 , A61K38/00 , A61K38/16
CPC分类号： C07K7/06 , A61K38/00 , C07K5/06191 , C07K5/0827
摘要： The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention include compounds of the formula RY*L (where Y* represents phosphotyrosine), with the R group at the Y-1 position. Peptidomimetics of the invention disrupt Stat3 activation and function. Peptidomimetics of the invention significantly inhibit tumor cell growth and induce tumor cell death.
摘要翻译：本发明涉及用于阻断癌细胞生长或增殖和/或诱导癌细胞死亡的组合物和方法。本发明的组合物是抑制STAT功能的肽模拟物。本发明的肽模拟物包括式RY * L（其中Y *表示磷酸酪氨酸）的化合物，其中R基团在Y-1位。本发明的肽模拟物破坏Stat3的活化和功能。本发明的肽模拟物显着抑制肿瘤细胞生长并诱导肿瘤细胞死亡。

2. 发明申请

US20090318367A1 Use of SH2 STAT3/STAT1 Peptidomimetics as Anticancer Drugs 有权
标题翻译：使用SH2 STAT3 / STAT1肽模拟物作为抗癌药物
公开(公告)号：US20090318367A1
公开(公告)日：2009-12-24
申请号：US12480376
申请日：2009-06-08
申请人： Said M. Sebti , Andrew D. Hamilton , James Turkson , Richard Jove
发明人： Said M. Sebti , Andrew D. Hamilton , James Turkson , Richard Jove
IPC分类号： A61K38/06 , C07K5/08 , C12N5/00 , A61P35/00
CPC分类号： C07K5/06078 , A61K38/00
摘要： The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention display selective inhibition of specific STAT isoform homo-dimerization. The peptidomimetic probes of STAT1 function, described herein, provide the means to preferentially inhibit STAT1 over STAT3 through the exploration of the C-terminus.
摘要翻译：本发明涉及用于阻断癌细胞生长或增殖和/或诱导癌细胞死亡的组合物和方法。本发明的组合物是抑制STAT功能的肽模拟物。本发明的肽模拟物显示特异性STAT同种型同二聚化的选择性抑制。本文所述的STAT1功能的拟肽探针提供了通过探索C末端优先抑制STAT3的方法。

3. 发明授权

US08153596B2 Use of SH2 STAT3/STAT1 peptidomimetics as anticancer drugs 有权
标题翻译：使用SH2 STAT3 / STAT1肽模拟物作为抗癌药物
公开(公告)号：US08153596B2
公开(公告)日：2012-04-10
申请号：US12480376
申请日：2009-06-08
申请人： Said M. Sebti , Andrew D. Hamilton , James Turkson , Richard Jove
发明人： Said M. Sebti , Andrew D. Hamilton , James Turkson , Richard Jove
IPC分类号： A61K38/06 , C07K5/08 , C12N5/00
CPC分类号： C07K5/06078 , A61K38/00
摘要： The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention display selective inhibition of specific STAT isoform homo-dimerization. The peptidomimetic probes of STAT1 function, described herein, provide the means to preferentially inhibit STAT1 over STAT3 through the exploration of the C-terminus.
摘要翻译：本发明涉及用于阻断癌细胞生长或增殖和/或诱导癌细胞死亡的组合物和方法。本发明的组合物是抑制STAT功能的肽模拟物。本发明的肽模拟物显示特异性STAT同种型同二聚化的选择性抑制。本文所述的STAT1功能的拟肽探针提供了通过探索C末端优先抑制STAT1的STAT1功能的方法。

4. 发明授权

US07842671B1 Peptidomimetic inhibitors of STAT activity and uses thereof 有权
标题翻译： STAT活性的拟肽抑制剂及其用途
公开(公告)号：US07842671B1
公开(公告)日：2010-11-30
申请号：US11986237
申请日：2007-11-19
申请人： James Turkson , Richard Jove , Said M. Sebti , Andrew D. Hamilton
发明人： James Turkson , Richard Jove , Said M. Sebti , Andrew D. Hamilton
IPC分类号： A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/06191 , C07K5/0827
摘要： The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention include compounds of the formula RY*L (where Y* represents phosphotyrosine), with the R group at the Y-1 position. Peptidomimetics of the invention disrupt Stat3 activation and function. Peptidomimetics of the invention significantly inhibit tumor cell growth and induce tumor cell death.
摘要翻译：本发明涉及用于阻断癌细胞生长或增殖和/或诱导癌细胞死亡的组合物和方法。本发明的组合物是抑制STAT功能的肽模拟物。本发明的肽模拟物包括式RY * L（其中Y *表示磷酸酪氨酸）的化合物，其中R基团在Y-1位。本发明的肽模拟物破坏Stat3的活化和功能。本发明的肽模拟物显着抑制肿瘤细胞生长并诱导肿瘤细胞死亡。

5. 发明授权

US08609639B2 Stat3 inhibitor having anti-cancer activity and methods 有权
标题翻译： Stat3抑制剂具有抗癌活性和方法
公开(公告)号：US08609639B2
公开(公告)日：2013-12-17
申请号：US12517453
申请日：2007-12-05
申请人： James Turkson , Said Sebti , Richard Jove , Andrew D. Hamilton
发明人： James Turkson , Said Sebti , Richard Jove , Andrew D. Hamilton
IPC分类号： A61K31/675 , C07F9/653 , C12N5/071
CPC分类号： C07F9/653
摘要： A small-molecule Stat3 dimerization inhibitor, S3I-M2001, is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers.
摘要翻译：描述了一种小分子Stat3二聚体抑制剂S3I-M2001，阐明了Stat3化学探针抑制剂生物化学和生物学效应背景下激活的Stat3的细胞内加工动力学。 S3I-M2001是Stat3 Src同源性（SH）2结构域结合磷酸酪氨酸肽的新鉴定的基于恶唑的拟肽，其选择性地破坏活性Stat3：Stat3二聚体。 S3I-M2001抑制Stat3依赖性恶性转化，存活，迁移和入侵持续激活Stat3的小鼠和人类癌细胞。 S3I-M2001抑制Stat3依赖的转录调控肿瘤生存基因，如Bcl-xL。所公开的化合物可用作某些癌症的新的潜在治疗。

6. 发明申请

US20110124602A1 Stat3 Inhibitor Having Anti-Cancer Activity and Methods 有权
标题翻译： Stat3抑制剂具有抗癌活性和方法
公开(公告)号：US20110124602A1
公开(公告)日：2011-05-26
申请号：US12517453
申请日：2007-12-05
申请人： James Turkson , Said Sebti , Richard Jove , Andrew D. Hamilton
发明人： James Turkson , Said Sebti , Richard Jove , Andrew D. Hamilton
IPC分类号： A61K31/675 , C07F9/653 , C12N5/071 , C12N5/09 , A61P35/00 , A61P35/04
CPC分类号： C07F9/653
摘要： A small-molecule Stat3 dimerization inhibitor, S3I-M2001, is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers.
摘要翻译：描述了一种小分子Stat3二聚体抑制剂S3I-M2001，阐明了Stat3化学探针抑制剂生物化学和生物学效应背景下激活的Stat3的细胞内加工动力学。 S3I-M2001是Stat3 Src同源性（SH）2结构域结合磷酸酪氨酸肽的新鉴定的基于恶唑的拟肽，其选择性地破坏活性Stat3：Stat3二聚体。 S3I-M2001抑制Stat3依赖性恶性转化，存活，迁移和入侵持续激活Stat3的小鼠和人类癌细胞。 S3I-M2001抑制Stat3依赖的转录调控肿瘤生存基因，如Bcl-xL。所公开的化合物可用作某些癌症的新的潜在治疗。

7. 发明授权

US09453049B2 Substrate-mimetic Akt inhibitor 有权
标题翻译：底物模拟Akt抑制剂
公开(公告)号：US09453049B2
公开(公告)日：2016-09-27
申请号：US14472966
申请日：2014-08-29
申请人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
发明人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
IPC分类号： A61K31/404 , A61K31/132 , C07D209/04 , C07C255/50 , C07C255/51 , C07K7/06 , C07K5/02 , C12N9/12 , C07C255/60 , C07C279/12 , C07D209/14 , C07K5/06 , C07K5/08 , C07K5/10 , A61K38/00
CPC分类号： C12N9/12 , A61K31/132 , A61K31/404 , A61K38/00 , C07C255/50 , C07C255/51 , C07C255/60 , C07C279/12 , C07C2601/16 , C07D209/04 , C07D209/14 , C07K5/02 , C07K5/0207 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/02 , C07K7/06 , C12N9/1205 , C12Y207/11001
摘要： Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.
摘要翻译：本文公开了Akt的一种肽和非肽抑制剂，其是致癌蛋白。从Akt靶基质GSK-3的残基开始，对GSK-3残基的功能结构域进行了表征。功能同源的非肽基团被GSK-3的氨基酸取代，产生能结合Akt的杂合肽 - 非肽和非肽化合物。与肽对应物相比，非肽化合物显示出增加的稳定性和刚性，并且不易降解。结合的非肽化合物对Akt具有抑制作用，类似于基于肽的Akt抑制剂。

8. 发明授权

US07482483B2 Growth factor-binding compounds and methods of use 有权
标题翻译：生长因子结合化合物和使用方法
公开(公告)号：US07482483B2
公开(公告)日：2009-01-27
申请号：US11044980
申请日：2005-01-27
申请人： Said M. Sebti , Andrew D. Hamilton , Rishi Jain
发明人： Said M. Sebti , Andrew D. Hamilton , Rishi Jain
IPC分类号： C07C229/00 , A61K31/195
CPC分类号： B82Y5/00 , A61K47/54 , A61K47/6949
摘要： Growth factor binding compounds having a plurality of acyclic isophthalic acid groups attached to a non-peptide organic scaffold and pharmaceutical compositions of the same are disclosed. Methods of administering and using the growth factor binding compounds or the growth factor binding compositions are also taught. These novel growth factor binding compounds are useful for treating angiogenesis, excessive cellular proliferation, tumor growth, and a combination thereof as well as inhibiting growth factor binding to cells and phosphorylation.
摘要翻译：公开了具有连接到非肽有机支架上的多个无环间苯二甲酸基团和其药物组合物的生长因子结合化合物。还教导了施用和使用生长因子结合化合物或生长因子结合组合物的方法。这些新的生长因子结合化合物可用于治疗血管发生，过度的细胞增殖，肿瘤生长及其组合以及抑制生长因子结合细胞和磷酸化。

9. 发明授权

US06221865B1 Inhibitors of protein isoprenyl transferases 失效
标题翻译：蛋白质异戊二烯转移酶抑制剂
公开(公告)号：US06221865B1
公开(公告)日：2001-04-24
申请号：US09073795
申请日：1998-05-07
申请人： Said M. Sebti , Andrew D. Hamilton , Kenneth J. Barr , Stephen A. Fakhoury , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Bryan K. Sorensen , Gerard M. Sullivan , James T. Wasicak , Kenneth J. Henry , Le Wang
发明人： Said M. Sebti , Andrew D. Hamilton , Kenneth J. Barr , Stephen A. Fakhoury , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Bryan K. Sorensen , Gerard M. Sullivan , James T. Wasicak , Kenneth J. Henry , Le Wang
IPC分类号： A61K315377
CPC分类号： C07C237/36 , C07B2200/07 , C07C239/20 , C07C271/22 , C07C317/50 , C07C323/59 , C07C323/60 , C07C327/42 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07C2603/24 , C07C2603/74 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/267 , C07D209/48 , C07D211/14 , C07D211/42 , C07D211/52 , C07D211/58 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/36 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D213/89 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/90 , C07D235/06 , C07D237/14 , C07D239/26 , C07D239/42 , C07D241/04 , C07D241/12 , C07D241/18 , C07D249/08 , C07D253/06 , C07D257/04 , C07D261/02 , C07D263/22 , C07D263/32 , C07D265/30 , C07D277/30 , C07D277/36 , C07D277/48 , C07D277/50 , C07D277/587 , C07D279/12 , C07D295/084 , C07D295/13 , C07D295/155 , C07D295/185 , C07D307/54 , C07D307/81 , C07D317/30 , C07D317/60 , C07D333/18 , C07D333/20 , C07D333/24 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/08 , C07F9/5333
摘要： Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (a) (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, and —P(W)RR3RR3′; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5—(d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5—, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene (k) a covalent bond, (l) and (m) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要翻译：具有式的化合物或其药学上可接受的盐，其中R 1是（a）氢，（b）低级烷基，（c）烯基，（d）烷氧基，（e）硫代烷氧基，（f）卤素，（g）卤代烷基，（h）芳基-L2-和（i）杂环-L2-; R 2选自（a）（b）-C（O）NH-CH（R 14）-C（O）OR 15，（d）-C（O）NH-CH（R 14）-C（O）NHSO 2 R 16 e）-C（O）NH-CH（R14） - 四唑基，（f）-C（O）NH-杂环基和（g）-C（O）NH-CH（R14）-C（O）NR17R18; R 3是取代或未取代的杂环或芳基，取代或未取代的环烷基或环烯基，和-P（W）RR 3 R R 3'; R4是氢，低级烷基，卤代烷基，卤素，芳基，芳基烷基，杂环或（杂环）烷基; （a）-L4-N（R5）-L5-，（b）-L4-O-L5-，（c）-L4-S（O）n-L5-（d） - L4-L6-C（W）-N（R5）-L5-，（e）-L4-L6-S（O）mN（R5）-L5-，（f）-L4-N（R5）-C W）-L7-L5-，（g）-L4-N（R5）-S（O）p-L7-L5-，（h）任选取代的亚烷基，（i）任选取代的亚烯基，（j）任选取代的亚炔基（k）共价键，（1）和（m）是蛋白质异戊二烯基转移酶的抑制剂。还公开了蛋白质异戊二烯转移酶抑制组合物和抑制蛋白质异戊二烯转移酶的方法。

10. 发明申请

US20150004698A1 SUBSTRATE-MIMETIC AKT INHIBITOR 有权
标题翻译：基质 - 酮化酮抑制剂
公开(公告)号：US20150004698A1
公开(公告)日：2015-01-01
申请号：US14472966
申请日：2014-08-29
申请人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
发明人： Said M. Sebti , Jin Q. Cheng , Andrew D. Hamilton , Katherine Kayser-Bricker
IPC分类号： C07K7/06 , C07K5/10 , C12N9/12 , C07C279/12 , C07C255/60 , C07D209/14 , C07K5/08 , C07K5/06
CPC分类号： C12N9/12 , A61K31/132 , A61K31/404 , A61K38/00 , C07C255/50 , C07C255/51 , C07C255/60 , C07C279/12 , C07C2601/16 , C07D209/04 , C07D209/14 , C07K5/02 , C07K5/0207 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/02 , C07K7/06 , C12N9/1205 , C12Y207/11001
摘要： Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.
摘要翻译：本文公开了Akt的一种肽和非肽抑制剂，其是致癌蛋白。从Akt靶基质GSK-3的残基开始，对GSK-3残基的功能结构域进行了表征。功能同源的非肽基团被GSK-3的氨基酸取代，产生能结合Akt的杂合肽 - 非肽和非肽化合物。与肽对应物相比，非肽化合物显示出增加的稳定性和刚性，并且不易降解。结合的非肽化合物对Akt具有抑制作用，类似于基于肽的Akt抑制剂。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式