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1. 发明授权

US5426194A Isolation and structure of Halistatin 1 失效
标题翻译： Halistatin的分离和结构1
公开(公告)号：US5426194A
公开(公告)日：1995-06-20
申请号：US4851
申请日：1993-01-19
申请人： George R. Pettit , Rui Tan , Feng Gao
发明人： George R. Pettit , Rui Tan , Feng Gao
IPC分类号： A61K31/365 , A61K35/00 , A61K35/02 , A61K35/56 , A61P35/00 , A61P35/02 , C07D493/22 , C07H9/02 , C12P17/18 , C12P19/44 , C07D323/00
CPC分类号： C07H9/02 , C07D493/22 , C12P17/181 , C12P19/445
摘要： An intensive long-term investigation of marine organisms as sources of new anticancer drugs has led to the isolation and structural elucidation (primarily by high field NMR and mass spectrometry) of halistatin 1, a new polyether macrolide of the halipyran-type, from the Western Indian Ocean sponge Phakellia carteri. Halistatin 1 (8.8.times.10.sup.-7 % yield) caused the accumulation of cells arrested in mitosis, inhibited tubulin polymerization, and inhibited the binding of radiolabeled vinblastine and GTP to tubulin.
摘要翻译：对海洋生物进行深入的长期调查，作为新的抗癌药物的来源，导致了halistatin 1（Halipyran型的新型聚醚大环内酯类）的隔离和结构解释（主要是通过高场NMR和质谱），来自西方印度洋海绵Phakellia carteri。 Halistatin 1（8.8×10-7％产率）引起细胞中有丝分裂停滞的积累，抑制微管蛋白聚合，并抑制放射性标记的长春花碱和GTP与微管蛋白的结合。

2. 发明申请

US20100197570A1 Cyclodepsipeptides with Antineoplastic Activity and Methods of Using to Inhibit Cancer and Microbial Growth 有权
标题翻译：具有抗肿瘤活性的Cyclopepsipeptide和使用抑制癌症和微生物生长的方法
公开(公告)号：US20100197570A1
公开(公告)日：2010-08-05
申请号：US12598943
申请日：2008-06-05
申请人： George R. Pettit , Rui Tan , Robin K. Pettit
发明人： George R. Pettit , Rui Tan , Robin K. Pettit
IPC分类号： A61K38/15 , C07K7/50 , A61P35/00 , A61P31/00
CPC分类号： C07K11/02 , A61K38/15 , Y02A50/473
摘要： The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.
摘要翻译：本发明涉及具有抗肿瘤和/或抗微生物活性的环糊肽化合物，优选为益母斯特汀1。本发明还涉及通过向所施用的环糊精肽化合物来抑制其引起的宿主中的癌细胞生长和/或微生物生长的方法主办。

3. 发明申请

US20130184201A1 Cyclodepsipeptides with Antineoplastic Activity and Methods of Using to Inhibit Cancer and Microbial Growth 有权
标题翻译：具有抗肿瘤活性的Cyclopepsipeptide和使用抑制癌症和微生物生长的方法
公开(公告)号：US20130184201A1
公开(公告)日：2013-07-18
申请号：US13786731
申请日：2013-03-06
申请人： George R. Pettit , Rui Tan , Robin K. Pettit
发明人： George R. Pettit , Rui Tan , Robin K. Pettit
IPC分类号： C07K11/02
CPC分类号： C07K11/02 , A61K38/15 , Y02A50/473
摘要： The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.
摘要翻译：本发明涉及具有抗肿瘤和/或抗微生物活性的环糊肽化合物，优选为益母斯特汀1。本发明还涉及通过向所施用的环糊精肽化合物来抑制其引起的宿主中的癌细胞生长和/或微生物生长的方法主办。

4. 发明授权

US08415294B2 Cyclodepsipeptides with antineoplastic activity and methods of using to inhibit cancer and microbial growth 有权
标题翻译：具有抗肿瘤活性的Cyclopepsipeptide和用于抑制癌症和微生物生长的方法
公开(公告)号：US08415294B2
公开(公告)日：2013-04-09
申请号：US12598943
申请日：2008-06-05
申请人： George R. Pettit , Rui Tan , Robin K. Pettit
发明人： George R. Pettit , Rui Tan , Robin K. Pettit
IPC分类号： A61K38/15 , A61K38/04 , A61K38/12 , C07K7/50
CPC分类号： C07K11/02 , A61K38/15 , Y02A50/473
摘要： The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.
摘要翻译：本发明涉及具有抗肿瘤和/或抗微生物活性的环糊肽化合物，优选为益母斯特汀1。本发明还涉及通过向所施用的环糊精肽化合物来抑制其引起的宿主中的癌细胞生长和/或微生物生长的方法主办。

5. 发明授权

US5801222A Isolation and structure of the human cancer cell growth inhibitory cyclic octapeptides phakellistatin 10 and 11 失效
标题翻译：人类癌细胞生长抑制性环状八肽phakellistatin 10和11的分离和结构
公开(公告)号：US5801222A
公开(公告)日：1998-09-01
申请号：US360239
申请日：1994-12-20
申请人： George R. Pettit , Rui Tan
发明人： George R. Pettit , Rui Tan
IPC分类号： A61K38/00 , C07K7/64 , A61K38/12
CPC分类号： C07K7/64 , A61K38/00
摘要： Two new compounds which may be useful in the treatment of one or more neoplastic diseases through chemotherapy have been isolated from the Western Pacific Ocean marine sponge Phakellia sp. The cyclic octapeptides phakellistatin 10 and phakellistatin 11 are disclosed herein. As the included data demonstrate, phakellistatin 10 attained an LC.sub.50 of less than 10.sup.-5 M per milliliter against the MDA-MB-435 breast cancer cell line. It also achieved total growth inhibition for two breast cancers and two CNS cancer cell lines at a concentration of less than 10.sup.-6 M per milliliter. The included data for phakellistatin 11 shows a moderately higher level of in vitro activity as shown by an LC.sub.50 of less than 10.sup.-5 M per milliliter against the MDA-MB-435 breast cancer cell line and five other cell lines. It also achieved total growth inhibition for two breast cancers, one CNS cancer, one Ovarian cancer, and one non-small cell lung cancer cell lines at a concentration of less than 10.sup.-7 M per milliliter.
摘要翻译：两种可用于通过化疗治疗一种或多种肿瘤疾病的新化合物已从西太平洋海洋海绵Phakellia sp。本文公开了环状八肽phakellistatin 10和phakellistatin 11。如附图所示，phakellistatin 10对MDA-MB-435乳腺癌细胞株的LC50值低于10-5M / ml。它还实现了两种乳腺癌和两种浓度小于10-6M / ml的两种CNS癌细胞系的总生长抑制。包含phakellistatin 11的数据显示了较高水平的体外活性，如相对MDA-MB-435乳腺癌细胞系和其他五种细胞系小于10-5M / ml的LC50所示。它还实现了两种乳腺癌，一种CNS癌症，一种卵巢癌和一种浓度低于10-7M /毫升的非小细胞肺癌细胞系的总生长抑制。

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