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1. 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。

2. 发明申请

WO2009066822A1 A METHOD OF PRODUCING SEDOHEPTULOSE USING THERMOSTABLE ENZYMES 审中-公开
标题翻译：使用可热固化酶生产皂苷的方法
公开(公告)号：WO2009066822A1
公开(公告)日：2009-05-28
申请号：PCT/KR2007/005966
申请日：2007-11-23
申请人： KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY , LEE, Dae-sil , BAE, Jungdon , PARK, Miri , PARK, Jung Eun , KIM, Dooil
发明人： LEE, Dae-sil , BAE, Jungdon , PARK, Miri , PARK, Jung Eun , KIM, Dooil
IPC分类号： C12P19/04
CPC分类号： C12P19/02
摘要： The present invention relates to a method for producing sedoheptulose-7-phosphate from alpha-glucan or from intermediate products obtained during the production process using thermostable enzymes which are derived from Thermus sp., and to transaldolase and transketolase represented by SEQ ID NO.1 and 3, which are isolated from Thermus sp. Since the enzymes derived from Thermus sp. of the present invention are thermostable, sedoheptulose-7-phosphate can be produced from alpha-glucan or from intermediate products using the enzymes by a continuous reaction process in one reactor, in which the production process is performed at a high temperature, thereby preventing contamination during the overall process.
摘要翻译：本发明涉及一种由α-葡聚糖或在生产过程中使用来自嗜热栖热菌属的热稳定酶得到的中间产物和由SEQ ID NO.1表示的转醛醇酶和转酮酶制备景深庚酮糖-7-磷酸酯的方法和3，它们与栖热菌属由于源自Thermus sp。本发明的热稳定性，可以在一个反应器中通过连续反应方法使用酶从α-葡聚糖或中间产物生产表皮葡聚糖-7-磷酸酯，其中在高温下进行生产过程，从而防止污染在整个过程中。

3. 发明申请

WO2012142245A8 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：WO2012142245A8
公开(公告)日：2013-11-21
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. The compounds of the invention have potential therapeutic activity in view of their binding and inhibitory activities towards Plkl. They are based on the amino acid sequence PLHSpT (phosphorylated Thr). The PEG moiety, when present, is covalently attached at the N- terminus. The invention also encompasses derivatives having substituents on the Pro and/or the His side chains, substituents on the phosphate group, the replacement of His with Gln, the replacement of Pro with a N-substituted Gly, the replacement of Ser with Ala, as well as HS-pT fragments with N-terminal alkoxycarbonyl group and PLHS fragments with a C-terminal glyco-imino-alkylxyalkylamide group.
摘要翻译：提供了新的化合物，其通过polo-box结构域结合polo样激酶。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盒结构域结合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。考虑到它们对Plk1的结合和抑制活性，本发明的化合物具有潜在的治疗活性。它们基于氨基酸序列PLHSpT（磷酸化的Thr）。存在时，PEG部分在N末端共价连接。本发明还包括在Pro和/或His侧链上具有取代基的衍生物，磷酸基团上的取代基，用Gln取代His，用N-取代的Gly取代Pro，用Ala取代Ser，作为以及具有N-末端烷氧基羰基的HS-pT片段和具有C-末端糖 - 亚氨基 - 烷基烷基酰胺基团的PLHS片段。

4. 发明申请

WO2010140835A3 NOVEL PYRIDONE COMPOUNDS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, METHOD FOR PRODUCING THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME FOR TREATING CANCER 审中-公开
标题翻译：新颖的吡咯烷酮化合物或其药学上可接受的盐，其生产方法和含有其的药物组合物用于治疗癌症
公开(公告)号：WO2010140835A3
公开(公告)日：2011-03-24
申请号：PCT/KR2010003539
申请日：2010-06-01
申请人： UNIV YONSEI IACF , KOREA RES INST OF BIOSCIENCE , BIORUNX , HAN GYOONHEE , CHOI EUNHYUN , LEE CHULHO , PARK JUNG EUN , CHO MISUN , SEO JEONGJEA , KIM HWAN MOOK , PARK SONG KYU , LEE KIHO , LEE CHANG WOO , LEE KI HOON , KIM HYUN-JUNG
发明人： HAN GYOONHEE , CHOI EUNHYUN , LEE CHULHO , PARK JUNG EUN , CHO MISUN , SEO JEONGJEA , KIM HWAN MOOK , PARK SONG KYU , LEE KIHO , LEE CHANG WOO , LEE KI HOON , KIM HYUN-JUNG
IPC分类号： C07D211/34 , C07D211/74
CPC分类号： C07D213/64 , C07D401/06 , C07D405/06 , C07D409/06
摘要： The present invention relates to novel pyridone compounds or pharmaceutically acceptable salts thereof, a method for producing the same and a pharmaceutical composition containing the same for treating cancer. The compounds according to the present invention utilize the superior effects of the RUNX activity found in the HDAC inhibitor for inhibiting tumor cell growth, and are thus useful for treating cancer.
摘要翻译：本发明涉及新颖的吡啶酮化合物或其药学上可接受的盐，其制备方法和含有其的治疗癌症的药物组合物。根据本发明的化合物利用HDAC抑制剂中发现的RUNX活性的优异效果来抑制肿瘤细胞生长，因此可用于治疗癌症。

5. 发明申请

WO2009096615A1 COMPOSITION FOR PREVENTING OR TREATING BRAIN CANCERS 审中-公开
标题翻译：用于预防或治疗脑癌的组合物
公开(公告)号：WO2009096615A1
公开(公告)日：2009-08-06
申请号：PCT/KR2008/000602
申请日：2008-01-31
申请人： KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY , LEE, Changjoon Justin , ROH, Eun-Joo , CHOI, Jin-Kyu , HAN, Kyung-Suk , PARK, Jung-Eun , KANG, Sang-Soo
发明人： LEE, Changjoon Justin , ROH, Eun-Joo , CHOI, Jin-Kyu , HAN, Kyung-Suk , PARK, Jung-Eun , KANG, Sang-Soo
IPC分类号： A61K31/522
CPC分类号： A61K31/522
摘要： A composition for preventing and/or treating brain tumor, containing caffeine and/or its analog, and/or their pharmaceutically acceptable salt, as an active ingredient, is provided. The composition for preventing or treating brain tumor has an activity to inhibit invasion, migration, and proliferation of brain tumor cells, and thereby very effective for the prevention and treatment of brain tumor.
摘要翻译：提供了用于预防和/或治疗含有咖啡因和/或其类似物的脑肿瘤和/或其药学上可接受的盐作为活性成分的组合物。用于预防或治疗脑肿瘤的组合物具有抑制脑肿瘤细胞的侵袭，迁移和增殖的活性，因此对预防和治疗脑肿瘤非常有效。

6. 发明申请

WO2008060112A1 COMPOSITION COMPRISING ARALIAE CORDATAE RADIX EXTRACT OR COMPOUNDS ISOLATED FROM THE SAME FOR PREVENTING OR TREATING PERIODONTITIS 审中-公开
标题翻译：包含ARALIAE CORDATAE RADIX提取物或其化合物的组合物从其分离用于预防或治疗周期性
公开(公告)号：WO2008060112A1
公开(公告)日：2008-05-22
申请号：PCT/KR2007/005741
申请日：2007-11-15
申请人： KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY , LEE, Dae-sil , KOH, Sukhoon , KIM, Joong Su , BAE, Jungdon , KIM, Dooil , PARK, Jung Eun , PARK, Miri , CHOI, Yongseok , PARK, Bo Hyun , KIM, Jin Sook , JANG, Dae Sik , KOOK, Joong-ki , SONG, Gyu Yong
发明人： LEE, Dae-sil , KOH, Sukhoon , KIM, Joong Su , BAE, Jungdon , KIM, Dooil , PARK, Jung Eun , PARK, Miri , CHOI, Yongseok , PARK, Bo Hyun , KIM, Jin Sook , JANG, Dae Sik , KOOK, Joong-ki , SONG, Gyu Yong
IPC分类号： A61K36/25 , A61K31/19 , A23L1/29 , A61P1/02
CPC分类号： A61K31/19 , A23L33/105 , A61K36/25
摘要： The present invention relates to a composition comprising an Araliae Cordatae Radix extract or compounds isolated from the same for preventing or treating periodontitis. The Araliae Cordatae Radix extract or compounds isolated from the extract according to the present invention has/have excellent antimicrobial and bactericidal activities against Porphyromonas endodontalis, Porphyromonas gingivalis and Prevotella intermedia, which are periodontal pathogens, thereby being used to prevent or treat periodontitis.
摘要翻译：本发明涉及包含Araliae Cordatae Radix提取物或从其分离的用于预防或治疗牙周炎的化合物的组合物。根据本发明的提取物中分离出的Araliae Cordatae Radix提取物或化合物对牙龈卟啉单胞菌属牙龈卟啉单胞菌和牙周膜间质瘤具有优异的抗菌和杀菌活性，它们是牙周病原体，因此用于预防或治疗牙周炎。

7. 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。

8. 发明申请

WO2009140632A1 METHOD FOR DETECTION AND QUANTIFICATION OF PLK1 EXPRESSION AND ACTIVITY 审中-公开
标题翻译： PLK1表达和活性的检测和定量方法
公开(公告)号：WO2009140632A1
公开(公告)日：2009-11-19
申请号：PCT/US2009/044202
申请日：2009-05-15
申请人： THE GOV. OF THE U.S.A AS REPRESENTED BY THE SECRETARY OF THE DEPT. OF HEALTH AND HUMAN SERVICES , LEE, Kyung, S. , PARK, Jung-Eun
发明人： LEE, Kyung, S. , PARK, Jung-Eun
IPC分类号： C12N9/00
CPC分类号： C07K14/00 , C07K17/00 , C12N9/1229 , C12Q1/485 , G01N33/57484 , G01N2500/04 , G01N2800/56
摘要： Isolated peptide substrates of Plk1 and nucleic acids encoding these peptides are disclosed. The peptides include two to ten repeats of the amino acid sequence set forth as X 1 X 2 AX 3 X 4 X 5 PLHSTX 6 X 7 X 8 X 9 X 10 X 11 X 12 (SEQ ID NO: 1), in which within each repeat X 1 , X 2 , X 6 , X 7 , X 8 , X 9 , X 10 , X 11 , and X 12 are each independently any amino acid or no amino acid, and X3 and X4 are each independently any amino acid. Methods of using these peptides to detect Plk1 activity in a sample are also disclosed. In some examples, the method includes contacting a sample with a disclosed peptide substrate of Plk1 in the presence of adenosine triphosphate, or an analog thereof, for a period of time sufficient for Plk1 to phosphorylate the PBIPtide. The presence and/or amount of the phosphorylated and/or the unphosphorylated peptide is detected, thereby detecting and/or quatitating Plk1kinase activity in the sample.
摘要翻译：公开了Plk1的分离的肽底物和编码这些肽的核酸。肽包括X1X2AX3X4X5PLHSTX6X7X8X9X10X11X12（SEQ ID NO：1）所示的氨基酸序列的2至10个重复，其中每个重复X1，X2，X6，X7，X8，X9，X10，X11和X12各自独立地任何氨基酸或不含氨基酸，X3和X4各自独立地为任何氨基酸。还公开了使用这些肽检测样品中Plk1活性的方法。在一些实例中，该方法包括在三磷酸腺苷或其类似物的存在下将样品与公开的Plk1肽底物接触足以使Plk1磷酸化PBIPtide的时间。检测磷酸化和/或未磷酸化的肽的存在和/或量，从而检测和/或测定样品中的Plk1激酶活性。

9. 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。

10. 发明申请

WO2009066934A3 METHODS FOR IMPROVEMENT OF BIRTH RATES IN CANIDAE ON SOMATIC CELL NUCLEAR TRANSFER 审中-公开
标题翻译：改善角膜细胞核转移中生殖系统发生率的方法
公开(公告)号：WO2009066934A3
公开(公告)日：2009-08-27
申请号：PCT/KR2008006821
申请日：2008-11-19
申请人： SEOUL NAT UNIV IND FOUNDATION , LEE BYEONG CHUN , KIM MIN KYU , JANG GOO , OH HYUN JU , HONG SO GUN , PARK JUNG EUN , KANG JUNG TAEK
发明人： LEE BYEONG CHUN , KIM MIN KYU , JANG GOO , OH HYUN JU , HONG SO GUN , PARK JUNG EUN , KANG JUNG TAEK
IPC分类号： C12N15/877
CPC分类号： C12N5/16 , A01K67/0273 , A01K2227/10 , C12N15/877 , C12N2501/405 , C12N2517/10
摘要： The present invention relates to a method for increasing the efficiency of offspring production in producing animals belonging to the family Canidae (canines) by somatic cell nuclear transfer. More specifically, relates to a method for increasing the efficiency of production of cloned canines by a method for cloning canines comprising enucleating the oocyte of a canine to prepare an enucleated oocyte, fusing a nuclear donor cell with the enucleated oocyte to prepare a nuclear transfer embryo and transferring the nuclear transfer embryo into the oviduct of a surrogate mother, wherein the nuclear donor cell is cultured in a medium containing a specific cell cycle synchronization-inducing substance such as roscovitine in the preparation thereof. The method enables to clone canines with high efficiency, and thus can contribute to the development of studies in the fields of veterinary medicine, anthropology and medical science such as the propagation of superior canines, the conservation of rare or nearly extinct canines, xenotransplantation and disease animal models.
摘要翻译：本发明涉及通过体细胞核转移提高属于犬科（犬科）的动物的后代生产效率的方法。更具体地，涉及通过克隆犬的方法来提高克隆犬的生产效率的方法，包括将犬的卵母细胞去核以制备去核卵母细胞，将核供体细胞与去核卵母细胞融合以制备核转移胚并将核转移胚转移到替代母体的输卵管中，其中在其制备中，在含有特定细胞周期同步诱导物质如roscovitine的培养基中培养核供体细胞。该方法能够高效地克隆犬科动物，从而有助于兽医，人类学，医学等领域的研究开发，如高等犬传播，保护罕见或几乎灭绝的犬，异种移植和疾病动物模型。

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