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1. 发明授权

US6143740A Heregulin antagonists and methods for their use 失效
标题翻译：促胰岛素拮抗剂及其使用方法
公开(公告)号：US6143740A
公开(公告)日：2000-11-07
申请号：US308396
申请日：1999-08-16
申请人： Dajun Yang , Shaomeng Wang , Alan P. Kozikowski , Marc E. Lippman
发明人： Dajun Yang , Shaomeng Wang , Alan P. Kozikowski , Marc E. Lippman
IPC分类号： C07D498/18 , A61K31/34 , A61K31/395 , A61K31/495 , A61K31/496 , A61K31/551 , A61K31/655 , A61P35/00 , A61P43/00 , C07D498/08 , A61K31/33 , C07K1/00 , C07K16/00
CPC分类号： A61K31/708 , A61K31/395 , A61K31/495 , A61K31/496 , A61K31/551 , A61K31/655 , A61K31/704 , A61K31/7076 , C07D498/08
摘要： The invention provides a method of inhibiting cancer cell growth, and thereby of treating cancer comprising administering to a mammal afflicted with cancer an effective amount of the compound of formula (I), wherein the variables of R.sub.1, and R.sub.2 have the meanings defined in the specification. The present invention also provides novel compounds of formula (I) as well as novel pharmaceutical compositions and intermediates useful for preparing compounds of formula (I). The figure illustrates the structure and binding activity of compounds of the invention and some of the rifamycin analogs.______________________________________ ##STR1## ______________________________________ Compounds R.sub.1 = ______________________________________ A1 --OH A2 --OH A3 --OH A4 --OH A5 --OH A6 --OH A7 --OH - A8 ##STR2## ______________________________________ Compounds R.sub.2 = ______________________________________ A1 #STR3## - A2 #STR4## - A3 #STR5## - A4 #STR6## - A5 #STR7## - A6 #STR8## - A7 #STR9## - A8 --H ______________________________________ Compounds IC.sub.50 (1) IC.sub.50 (2) ______________________________________ A1 10 uM 1 uM A2 10 uM 3 uM A3 10 uM 3 uM A4 50 uM 5 uM A5 >500 uM >50 uM A6 >500 uM >50 uM A7 >200 uM >50 uM A8 >500 M >50 uM ______________________________________
摘要翻译： PCT No.PCT / US97 / 21474 Sec。 371日期1999年8月16日 102（e）1999年8月16日PCT 1997年11月19日PCT公布。第WO98 / 21956号公报日期1998年5月28日本发明提供抑制癌细胞生长，从而治疗癌症的方法，包括向患有癌症的哺乳动物施用有效量的式（I）化合物，其中R1和R2的变量具有在本说明书中定义的含义。本发明还提供新的式（I）化合物以及可用于制备式（I）化合物的新型药物组合物和中间体。该图示出了本发明化合物和一些利福霉素类似物的结构和结合活性。 - 化合物R1 = -Al-OH-A2-OH-A3-OH-A4-OH-A5-OH-A6-OH-A7 -OH - - A8化合物R2 = 图像 - - A2 - - A3 - - A4 GE> - - A7 - - A8 -H - 化合物IC50（1）IC50（2） - A1 10 uM 1 uM - A2 10 uM 3 uM - A3 10 uM 3 uM - A4 50 uM 5 uM - A5> 500 uM> 50 uM - A6> 500 uM> 50 uM - A7> 200 uM> 50 uM - A8> 500 M> 50 uM -

2. 发明授权

US06420572B1 Synthetic methods for preparation of protected proanthocyanidin(s) 失效
标题翻译：用于制备被保护的原花色素的合成方法
公开(公告)号：US06420572B1
公开(公告)日：2002-07-16
申请号：US09169554
申请日：1998-10-09
申请人： Leo J. Romanczyk, Jr. , Alan P. Kozikowski , Werner Tueckmantel , Marc E. Lippman
发明人： Leo J. Romanczyk, Jr. , Alan P. Kozikowski , Werner Tueckmantel , Marc E. Lippman
IPC分类号： C07D31160
CPC分类号： C07H17/06 , A61K31/35 , C07D311/32 , C07D311/60 , C07D311/62
摘要： A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.
摘要翻译：公开了用于生产具有多酚单体单元的多酚低聚物的方法，n为2-18的整数。该方法包括将被保护的酚羟基的被保护的多酚与C-4官能化的多酚单体的偶联。受保护的多酚可以是受保护的多酚单体或具有2-17单体单元的被保护的多酚低聚物。有利地，形成多酚低聚物的多酚单体单元可以是相同或不同的类黄酮化合物。

3. 发明授权

US06849746B2 Synthetic methods for polyphenols 失效
标题翻译：多酚的合成方法
公开(公告)号：US06849746B2
公开(公告)日：2005-02-01
申请号：US10355606
申请日：2003-01-31
申请人： Leo J. Romanczyk, Jr. , Alan P. Kozikowski , Werner Tueckmantel , Marc E. Lippman
发明人： Leo J. Romanczyk, Jr. , Alan P. Kozikowski , Werner Tueckmantel , Marc E. Lippman
IPC分类号： A61K31/35 , A61K31/352 , A61K31/353 , A61P35/00 , C07D311/32 , C07D311/60 , C07D311/62 , C07H17/06 , C07D321/10
CPC分类号： C07H17/06 , A61K31/35 , C07D311/32 , C07D311/60 , C07D311/62
摘要： A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.
摘要翻译：公开了用于生产具有多酚单体单元的多酚低聚物的方法，n为2-18的整数。该方法包括将被保护的酚羟基的被保护的多酚与C-4官能化的多酚单体的偶联。受保护的多酚可以是受保护的多酚单体或具有2-17单体单元的被保护的多酚低聚物。有利地，形成多酚低聚物的多酚单体单元可以是相同或不同的类黄酮化合物。

4. 发明授权

US06528664B2 Synthetic methods for polyphenols 失效
公开(公告)号：US06528664B2
公开(公告)日：2003-03-04
申请号：US10017812
申请日：2001-12-14
申请人： Leo J. Romanczyk, Jr. , Alan P. Kozikowski , Werner Tueckmantel , Marc E. Lippman
发明人： Leo J. Romanczyk, Jr. , Alan P. Kozikowski , Werner Tueckmantel , Marc E. Lippman
IPC分类号： C07D31160
CPC分类号： C07H17/06 , A61K31/35 , C07D311/32 , C07D311/60 , C07D311/62
摘要： A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.

5. 发明授权

US07268240B2 Synthetic methods for polyphenols 失效
标题翻译：多酚的合成方法
公开(公告)号：US07268240B2
公开(公告)日：2007-09-11
申请号：US10858449
申请日：2004-05-28
申请人： Leo J. Romanczyk, Jr. , Alan P. Kozikowski , Werner Tueckmantel , Marc E. Lippman
发明人： Leo J. Romanczyk, Jr. , Alan P. Kozikowski , Werner Tueckmantel , Marc E. Lippman
IPC分类号： C07D311/62
CPC分类号： C07H17/06 , A61K31/35 , C07D311/32 , C07D311/60 , C07D311/62
摘要： A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.
摘要翻译：公开了用于生产具有多酚单体单元的多酚低聚物的方法，n为2-18的整数。该方法包括将被保护的酚羟基的被保护的多酚与C-4官能化的多酚单体的偶联。受保护的多酚可以是受保护的多酚单体或具有2-17单体单元的被保护的多酚低聚物。有利地，形成多酚低聚物的多酚单体单元可以是相同或不同的类黄酮化合物。

6. 发明申请

US20110123441A1 NOVEL GREB1A MONOCLONAL ANTIBODY 审中-公开
标题翻译：新GREB1A单克隆抗体
公开(公告)号：US20110123441A1
公开(公告)日：2011-05-26
申请号：US12908348
申请日：2010-10-20
申请人： Marc E. Lippman , Harry James Hnatyszyn , Mingli Liu , James M. Rae
发明人： Marc E. Lippman , Harry James Hnatyszyn , Mingli Liu , James M. Rae
IPC分类号： A61K51/00 , A61K39/395 , A61K39/00 , C07K14/00 , A61P35/00 , C07K16/18 , C07H21/04
CPC分类号： C07K16/3015 , C07K2317/34 , G01N33/57484
摘要： The generation and validation of a novel monoclonal GREB1 antibody (GREB1ab). Methods for the prognosis, diagnosis, assessment of disease progression, severity and outcome utilize GREB1 molecules as biomarkers. The GREB1 antibody is also a useful tool for investigations focused on the expression, distribution and function of GREB1 in normal and cancer tissues.
摘要翻译：新型单克隆GREB1抗体（GREB1ab）的产生和验证。预后，诊断，疾病进展评估，严重程度和结局的方法利用GREB1分子作为生物标志物。 GREB1抗体也是一个有用的工具，用于研究重点在正常和癌组织中GREB1的表达，分布和功能。

7. 发明授权

US6040290A Ligand growth factor gp30 that binds to the erbB-2 receptor protein and induces cellular responses 失效
标题翻译：配体生长因子gp30结合erbB-2受体蛋白并诱导细胞反应
公开(公告)号：US6040290A
公开(公告)日：2000-03-21
申请号：US703089
申请日：1996-08-26
申请人： Marc E. Lippman , Ruth Lupu
发明人： Marc E. Lippman , Ruth Lupu
IPC分类号： A61K38/00 , A61K51/08 , C07K14/475 , C07K14/495 , C07K14/705 , C07K14/71 , C07K16/22 , C07K19/00 , G01N33/566 , G01N33/574 , G01N33/68 , G01N33/74 , A61K38/18 , C07K17/02
CPC分类号： A61K51/08 , C07K14/4756 , C07K14/495 , C07K14/705 , C07K14/71 , C07K16/22 , C07K19/00 , G01N33/566 , G01N33/57492 , G01N33/6872 , G01N33/74 , A61K38/00 , C07K2317/73 , G01N2333/485 , G01N2333/71 , G01N2500/00
摘要： The present invention relates to erbB-2 ligands and functional derivatives thereof which are capable of binding to the erbB-2 oncogene product. The present invention further pertains to anti-ligand molecules capable of recognizing and binding to the erbB-2 ligand molecule and to screening assays for such ligands. The present invention additionally relates to uses for the erbB-2 ligand, the anti-ligand molecules and the screening assays. The present invention also pertains to a method for inhibiting the growth of adenocarcinoma cells.
摘要翻译：本发明涉及能够结合erbB-2致癌基因产物的erbB-2配体及其功能衍生物。本发明还涉及能够识别和结合erbB-2配体分子并筛选这些配体的测定的抗配体分子。本发明还涉及erbB-2配体，抗配体分子和筛选测定的用途。本发明还涉及抑制腺癌细胞生长的方法。

8. 发明授权

US06566104B1 ERbB-4 targeted ribozymes 失效
标题翻译： ERbB-4靶向核酶
公开(公告)号：US06566104B1
公开(公告)日：2003-05-20
申请号：US09530224
申请日：2000-06-23
申请人： Careen K. Tang , Marc E. Lippman
发明人： Careen K. Tang , Marc E. Lippman
IPC分类号： C12P1934
CPC分类号： C12N15/1138 , A61K38/00 , C12N2310/111 , C12N2310/121
摘要： Enzymatic RNA molecules which cleave ErbB-4 mRNA and uses thereof.
摘要翻译：切割ErbB-4 mRNA的酶RNA分子及其用途

9. 发明授权

US5578482A Ligand growth factors that bind to the erbB-2 receptor protein and induce cellular responses 失效
标题翻译：结合erbB-2受体蛋白并诱导细胞反应的配体生长因子
公开(公告)号：US5578482A
公开(公告)日：1996-11-26
申请号：US96277
申请日：1993-07-26
申请人： Marc E. Lippman , Ruth Lupu
发明人： Marc E. Lippman , Ruth Lupu
IPC分类号： A61K38/00 , A61K51/08 , C07K14/475 , C07K14/495 , C07K14/705 , C07K14/71 , C07K16/22 , C07K19/00 , G01N33/566 , G01N33/574 , G01N33/68 , G01N33/74 , C12N1/38 , C12N5/26
CPC分类号： A61K51/08 , C07K14/4756 , C07K14/495 , C07K14/705 , C07K14/71 , C07K16/22 , C07K19/00 , G01N33/566 , G01N33/57492 , G01N33/6872 , G01N33/74 , A61K38/00 , C07K2317/73 , G01N2333/485 , G01N2333/71 , G01N2500/00
摘要： The present invention relates to erbB-2 ligands and functional derivatives thereof which are capable of binding to the erbB-2 oncogene product. The present invention further pertains to anti-ligand molecules capable of recognizing and binding to the erbB-2 ligand molecule and to screening assays for such ligands. The present invention additionally relates to uses for the erbB-2 ligand, the anti-ligand molecules and the screening assays.A method for inhibiting the growth of adenocarcinoma cells in a human, which cells overexpress the oncogene erbB-2, which entails administering to said human an amount of a 30 kDa glycoprotein effective to inhibit the growth of said cells.
摘要翻译：本发明涉及能够结合erbB-2致癌基因产物的erbB-2配体及其功能衍生物。本发明还涉及能够识别和结合erbB-2配体分子并筛选这些配体的测定的抗配体分子。本发明还涉及erbB-2配体，抗配体分子和筛选测定的用途。一种抑制人类腺癌细胞生长的方法，该细胞过表达癌基因erbB-2，所述方法需要向所述人施用一定量的有效抑制所述细胞生长的30kDa糖蛋白。

10. 发明授权

US5874528A Binding peptides which interact with ligand growth factors of the epidermal growth factor receptor and erbB-2 receptor 失效
标题翻译：与表皮生长因子受体和erbB-2受体的配体生长因子相互作用的结合肽
公开(公告)号：US5874528A
公开(公告)日：1999-02-23
申请号：US117187
申请日：1994-10-27
申请人： Ruth Lupu , Marc E. Lippman
发明人： Ruth Lupu , Marc E. Lippman
IPC分类号： A61K38/00 , A61K51/08 , C07K14/475 , C07K14/495 , C07K14/705 , C07K14/71 , C07K16/22 , C07K19/00 , G01N33/566 , G01N33/574 , G01N33/68 , G01N33/74 , C07K7/52 , C07K7/00
CPC分类号： G01N33/74 , C07K14/4756 , C07K14/495 , C07K14/705 , C07K14/71 , C07K16/22 , C07K19/00 , G01N33/566 , G01N33/57492 , G01N33/6872 , A61K38/00 , G01N2333/485 , G01N2333/71 , G01N2500/00
摘要： The present invention relates to blocking peptides which are capable of binding to ligands for the erbB-2 receptor or the epidermal growth factor receptor (EGFR). The blocking peptides of the invention are used to detect the presence of such ligand molecules. In addition, the blocking peptides are useful in inhibiting or preventing the growth of adenocarcinoma cells which express the erbB-2 receptor or the EGFR.
摘要翻译： PCT No.PCT / US93 / 04055 Sec。 371日期：1994年10月27日 102（e）日期1994年10月27日PCT 1993年4月29日提交PCT本发明涉及能够结合erbB-2受体或表皮生长因子受体（EGFR）的配体的肽。本发明的阻断肽用于检测这种配体分子的存在。此外，阻断肽可用于抑制或预防表达erbB-2受体或EGFR的腺癌细胞的生长。

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