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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. 发明授权

US5196447A Neristatin 1 失效
标题翻译： NERISTATIN 1
公开(公告)号：US5196447A
公开(公告)日：1993-03-23
申请号：US742609
申请日：1991-08-08
申请人： George R. Pettit , Feng Gao
发明人： George R. Pettit , Feng Gao
IPC分类号： A61K31/365 , A61K35/56 , A61P35/02 , A61P43/00 , C07D493/22
CPC分类号： C07D493/22
摘要： The marine bryozoan Bugula neritina has been found to contain a novel 22-membered macrocyclic lactone which is an inhibitor of lymphocytic leukemia as measured by the US National Cancer Institute's P 388 and in vitro evaluation system. The novel lactone is herein denominated "neristatin 1" and is elucidated.

3. 发明授权

US5352804A Isolation and structure of Halistatin 2 失效
标题翻译： Halistatin 2的分离和结构
公开(公告)号：US5352804A
公开(公告)日：1994-10-04
申请号：US4852
申请日：1993-01-19
申请人： George R. Pettit , Feng Gao
发明人： George R. Pettit , Feng Gao
IPC分类号： A61K31/365 , A61K35/56 , A61P35/00 , A61P35/02 , C07D493/22 , C07H9/02 , C12P17/18 , C12P19/44 , C07D323/00
CPC分类号： C07D493/22 , C07H9/02 , 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 2, a new polyether macrolide of the halipyran-type, from the Western Indian Ocean sponge Axinella cf. carteri (Dendy). Halistatin 2 (1.4.times.10.sup.-6 % yield) caused the accumulation of cells arrested in mitosis, inhibited tubulin polymerization, and inhibited the binding of radiolabeled vinblastine and GTP to tubulino. Further, Halistatin 2 displayed significant activity against selected human tumor cell lines.
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 2（Halipyran型新型聚醚大环内酯类）的隔离和结构阐释（主要是通过高场NMR和质谱），从西方印度洋海绵Axinella参考卡特里（Dendy）。 Halistatin 2（1.4×10-6％产率）引起细胞在有丝分裂中的积累，抑制微管蛋白聚合，并抑制放射性标记的长春碱和GTP与tubulin的结合。此外，Halistatin 2对选定的人肿瘤细胞系显示出显着的活性。

4. 发明授权

US08053416B2 Isolation and structure of turbostatins 1-4 有权
标题翻译：涡轮增压剂的隔离和结构1-4
公开(公告)号：US08053416B2
公开(公告)日：2011-11-08
申请号：US11913169
申请日：2006-05-11
申请人： George R. Pettit , Yuping Tang
发明人： George R. Pettit , Yuping Tang
IPC分类号： A61K31/7028 , C07H15/02
CPC分类号： C07H15/00
摘要： Described herein are novel cerebroside compounds, designated as Turbostatin 1, Turbostatin 2, Turbostatin 3, and Turbostatin 4. These compounds were extracted and isolated from the marine mollusk Turbo stenogyrus, and their structures elucidated. The new compounds exhibit significant cancer cell growth inhibition activity against a variety of murine and human cancer cell lines, and as such appear will be useful in the treatment of various forms of neoplastic disease.
摘要翻译：本文描述的是命名为Turbostatin1，Turbostatin2，Turbostatin3和Turbostatin4的新型脑苷脂化合物。这些化合物从海洋软体动物Turbo stenogyrus中提取和分离，并且阐明其结构。这些新化合物对多种鼠和人类癌细胞株表现出显着的癌细胞生长抑制活性，并且如此出现可用于治疗各种形式的肿瘤性疾病。

5. 发明授权

US07705188B2 Structural modification of resveratrol: sodium resverastatin phosphate 失效
标题翻译：白藜芦醇的结构修饰：磷酸白藜芦醇钠
公开(公告)号：US07705188B2
公开(公告)日：2010-04-27
申请号：US10510675
申请日：2003-04-10
申请人： George R. Pettit , Matthew P. Grealish
发明人： George R. Pettit , Matthew P. Grealish
IPC分类号： C07C43/20 , C07F9/09
CPC分类号： C07C43/23 , A61K31/66 , C07C41/26 , C07C41/30 , C07F9/12 , C07C43/215
摘要： Described herein are novel compounds having antineoplastic and antimicrobial activity, obtained via structural modifications of resveratrol and combretastatin A-4, methods for synthesis of these compounds, and their use in pharmaceutical composition and for use in the treatment of mammals having cancer. Examples of the novel compounds are: (Z)- and (E)-3,4′,5-trimethoxystilbene (4a, 4b); (Z)- and (E)-3,5-dimethoxy-4′-hydroxystilbene (14c, 14d); (Z)- and (E)-3-hydroxy-4′,5-dimethoxystilbene (14g, 14h); (Z)- and (E)-3,5-dihydroxy-4′-methoxy-stilbene (14k, 14l); sodium resverastatin dibenzyl phosphate ((Z)-3,5-dimethoxy-4-[O-bis(benzyl)phosphoryl]-stilbene) (14m); and sodium resverastatin phosphate (14n).
摘要翻译：本文描述了通过白藜芦醇和考布他汀A-4的结构修饰获得的具有抗肿瘤和抗微生物活性的新化合物，它们用于合成这些化合物的方法，以及它们在药物组合物中的用途以及用于治疗具有癌症的哺乳动物。新化合物的实例是：（Z） - 和（E）-3,4'，5-三甲氧基茋（4a，4b）; （Z） - 和（E）-3,5-二甲氧基-4'-羟基茋（14c，14d）; （Z） - 和（E）-3-羟基-4'，5-二甲氧基茋（14g，14h）; （Z） - 和（E）-3,5-二羟基-4'-甲氧基 - 二苯乙烯（14k，14l）; （（Z）-3,5-二甲氧基-4- [O-双（苄基）磷酰基] - 二苯乙烯钠（14m）; 和雷铂霉素磷酸钠（14n）。

6. 发明授权

US07462609B2 Narcistatin prodrugs 失效
标题翻译： Narcistatin前药
公开(公告)号：US07462609B2
公开(公告)日：2008-12-09
申请号：US10537968
申请日：2003-12-09
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： A61K31/675 , C07F9/06
CPC分类号： C07F9/65744
摘要： The present invention provides prodrugs derived from the sparingly soluble anticancer isocarbostyril narciclasine, a component of various Narcissus species, said prodrugs having potential for use against animal and human cancers. Also disclosed is an efficient procedure for the synthetic conversion of narciclasine to several more soluble cyclic phosphate compounds, including “narcistatin”.
摘要翻译：本发明提供衍生自微溶性抗癌异卡波斯特尔亚硝酸钠（各种水仙物种的组分）的所述前药，所述前药具有用于对动物和人类癌症的潜力。还公开了将亚硝酸钠合成转化为几种更易溶的环状磷酸酯化合物（包括“非肌抑素”）的有效方法。

7. 发明授权

US06686445B1 Synthetic antineoplastic agents derived from dolastatin 15 and methods of making same 有权
标题翻译：衍生自多拉司他坦15的合成抗肿瘤剂及其制备方法
公开(公告)号：US06686445B1
公开(公告)日：2004-02-03
申请号：US09509066
申请日：2000-03-21
申请人： George R. Pettit , Erik J. Flahive
发明人： George R. Pettit , Erik J. Flahive
IPC分类号： C07K700
CPC分类号： C07K7/02 , A61K38/00 , C07K11/00
摘要： A composition of matter, denominated herein as 12a-r, having the structural formula set forth below: wherein R is selected from the group consisting of: a) R=NHPh; b) R=NHCH2Ph; c) R=NH(CH2)2Ph; d) R=NH(CH2)2‘-4-F-Ph; e) R=NH(CH2)2-4-Cl-Ph; f) R=NH(CH2)2-3-Cl-Ph; g) R=NH(CH2)2-2-Cl-Ph; h) R=NH(CH2)2-4-Br-Ph; i) R=NH(CH2)2-4-NO2-Ph; j) R=NH(CH2)2-3,4-(CH3O)2Ph; k) R=NH(CH2)2-2-pyridine; l) R=NH(CH2)3Ph; m) R=L-Phe-OCH3; n) R=L-Met-OCH3; o) R=L-Pro-OCH3; p) R=NH-2-thiazolyl; q) R=NH-2-benzothiazolyl; r) R=NH-3-quinolyl; and methods of making these compounds 12a-r.
摘要翻译：其中R选自：a）R = NHPh; b）R = NHCH 2 Ph; c）R = NH（CH 2）2， 2 Ph; d）R = NH（CH 2）2 -4 -F-Ph; e）R = NH（CH 2）2-4-Cl-Ph; f）R = NH（CH 2）2-3-Cl-Ph ; g）R = NH（CH 2）2-2-Cl-Ph; h）R = NH（CH 2）2-4-Br-Ph; i）R = NH（CH 2）2-4 -NO 2-Ph; j ）R = NH（CH 2）2-3,4-（CH 3 O）2 Ph; k）R = NH（CH 2）2-2 - 吡啶; l）R = NH（CH 2）3 Ph; m）R = OCH 3; n）R = L-Met-OCH 3; o）R = L-Pro-OCH 3; p）R = NH-2-噻唑基; q）R = NH-2-苯并噻唑基; r）R = 喹啉基;以及制备这些化合物12a-r的方法。

8. 发明授权

US06569834B1 Elucidation and synthesis of antineoplastic tetrapeptide w-aminoalkyl-amides 失效
标题翻译：抗肿瘤四肽w-氨基烷基酰胺的阐释和合成
公开(公告)号：US06569834B1
公开(公告)日：2003-05-27
申请号：US07985697
申请日：1992-12-03
申请人： George R. Pettit , Jozsef Barkoczy
发明人： George R. Pettit , Jozsef Barkoczy
IPC分类号： A61K3800
CPC分类号： C07K7/06 , A61K38/07 , C07K5/101
摘要： Dolastatin 10, a linear pentapeptide, has shown potent antineoplastic activity profiles against various experimental cancer systems. The synthesis of structural modifications of dolastatin 10 having significant antineoplastic activity against human cancer cell lines has been accomplished; namely antineoplastic tetrapeptide w-amino alkyl amides related to dolastatin 10, which have been found to demonstrate effective antineoplastic activity against various human cancer cell lines. Members of this have demonstrated significant antineoplastic activity against human cancer cell lines. The human cancer cell lines against which the substances of the present invention have yielded the significant antineoplastic activity are: Ovarian OVCAR-3; Central Nervous System (“CNS”) SF295; Renal A498; Lung NCI460; Colon KM20L2 and Melanoma SK-MEL-3.
摘要翻译：线性五肽Dolastatin 10已经显示出针对各种实验性癌症系统的有效的抗肿瘤活性。已经完成了对人癌细胞系具有显着抗肿瘤活性的多拉司他汀10的结构修饰的合成; 即与多拉司他汀10相关的抗肿瘤四肽w-氨基烷基酰胺，已被发现证明对各种人类癌细胞系具有有效的抗肿瘤活性。其成员已经证明对人类癌细胞系具有显着的抗肿瘤活性。本发明的物质产生显着的抗肿瘤活性的人类癌细胞系是：卵巢OVCAR-3; 中枢神经系统（“CNS”）SF295; 肾A498; 肺NCI460; 结肠KM20L2和黑色素瘤SK-MEL-3。

9. 发明授权

US6060505A Method of treating cancer using C-26 modified bryostatin 有权
标题翻译：使用C-26改良的苔藓抑素治疗癌症的方法
公开(公告)号：US6060505A
公开(公告)日：2000-05-09
申请号：US142945
申请日：1999-02-16
申请人： Peter M. Blumberg , Zoltan Szallasi , George R. Pettit
发明人： Peter M. Blumberg , Zoltan Szallasi , George R. Pettit
IPC分类号： A61K31/365 , A01N43/02
CPC分类号： A61K31/365 , Y10S514/883 , Y10S514/885 , Y10S514/908 , Y10S514/95
摘要： Disclosed are modified bryostatins and their use as anticancer drugs.
摘要翻译： PCT No.PCT / US97 / 04515 Sec。 371日期1999年2月16日 102（e）1999年2月16日PCT 1997年3月20日PCT公布。出版物WO97 / 34598 日期1997年9月25日被公开是修饰的降冰片碱及其作为抗癌药物的用途。

10. 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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