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1. 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。

2. 发明授权

US07994320B2 Narcistatin prodrugs 有权
标题翻译： Narcistatin前药
公开(公告)号：US07994320B2
公开(公告)日：2011-08-09
申请号：US12208191
申请日：2008-09-10
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： 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。

3. 发明授权

US07541346B2 Pancratistatin cyclic phosphate prodrugs and phenpanstatin cyclic phosphate prodrugs 有权
标题翻译： Pancratistatin环磷酸酯前药和phenpanstatin环磷酸酯前药
公开(公告)号：US07541346B2
公开(公告)日：2009-06-02
申请号：US12025525
申请日：2008-02-04
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： A61K31/675 , A61K31/4741
CPC分类号： A61K31/675 , C07F9/6561 , C07F9/65744
摘要： Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexylcarbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient route to a new series (3b-3d) of promising 3,4-O-cyclic phosphate prodrugs designated phenpanstatin phosphates. Application of analogous reaction conditions to pancratistatin (1a) led to a mixture of monophosphate derivatives where sodium pancratistatin 4-O-phosphate (4a) was isolated and the structure confirmed by x-ray crystallography. Modification of the reaction conditions allowed direct phosphorylation of pancratistatin followed by cation exchange chromatography to afford sodium pancratistatin 3,4-O-cyclic phosphate (5b) which was selected for preclinical development.
摘要翻译：发现使用四丁基二磷酸二氢铵和二环己基碳二亚胺在吡啶中进行选择性磷酸化，然后进行阳离子交换色谱法，提供了一种有前途的有前途的3,4-O-环磷酸酯前体药物（3b-3d）的有效途径，其命名为phenpanstatin 磷酸盐。将类似的反应条件应用于pancratistatin（1a）导致单磷酸酯衍生物的混合物，其中分离出pancratistatin 4-O-磷酸钠（4a），并通过x射线晶体学证实结构。反应条件的改变允许pancratistatin直接磷酸化，然后进行阳离子交换层析，得到选择用于临床前发展的pancratistatin 3,4-O-环磷酸钠（5b）。

4. 发明申请

US20080139509A1 PANCRATISTATIN CYCLIC PHOSPHATE PRODRUGS AND PHENPANSTATIN CYCLIC PHOSPHATE PRODRUGS 有权
标题翻译：泛酸环磷酸盐和磷酸钙环磷酸盐
公开(公告)号：US20080139509A1
公开(公告)日：2008-06-12
申请号：US12025525
申请日：2008-02-04
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： A61K31/675 , A61P35/00
CPC分类号： A61K31/675 , C07F9/6561 , C07F9/65744
摘要： Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexylcarbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient route to a new series (3b-3d) of promising 3,4-O-cyclic phosphate prodrugs designated phenpanstatin phosphates. Application of analogous reaction conditions to pancratistatin (1a) led to a mixture of monophosphate derivatives where sodium pancratistatin 4-O-phosphate (4a) was isolated and the structure confirmed by x-ray crystallography. Modification of the reaction conditions allowed direct phosphorylation of pancratistatin followed by cation exchange chromatography to afford sodium pancratistatin 3,4-O-cyclic phosphate (5b) which was selected for preclinical development.
摘要翻译：发现使用四丁基二磷酸二氢铵和二环己基碳二亚胺在吡啶中进行选择性磷酸化，然后进行阳离子交换色谱法，提供了一种有前途的有前途的3,4-O-环磷酸酯前体药物（3b-3d）的有效途径，其命名为phenpanstatin 磷酸盐。将类似的反应条件应用于pancratistatin（1a）导致单磷酸酯衍生物的混合物，其中分离出pancratistatin 4-O-磷酸钠（4a），并通过x射线晶体学证实结构。反应条件的改变允许pancratistatin直接磷酸化，然后进行阳离子交换层析，得到选择用于临床前发展的pancratistatin 3,4-O-环磷酸钠（5b）。

5. 发明授权

US06949647B2 Synthesis of pancratistatin 有权
标题翻译： pancratistatin的合成
公开(公告)号：US06949647B2
公开(公告)日：2005-09-27
申请号：US10450917
申请日：2001-12-20
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： A61P35/00 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04
摘要： (+)-Narciclasine (2), available in quantity from certain Amaryllidaceae species or by total synthesis, is employed in for a ten step synthetic conversion (3.6% overall yield) to natural (+)-pancratistatin (1a). The key procedures involve the epoxidation of natural (+)-narciclasine (2) to an epoxide (6), reduction of the epoxide (6) to diol (8), formation of cyclic sulfate (12) and its ring opening with cesium benzoate followed by saponification of the benzoate to afford (+)-pancratistatin (1a).
摘要翻译：（+） - 亚硝酸钠（2），可从某些芳樟科物种或全合成得到的数量用于十天合成转化（3.6％总产率）至天然（+） - 泛酸盐（1a）。关键方法是将天然（+） - 亚硝酸（2）环氧化成环氧化物（6），将环氧化物（6）还原成二醇（8），形成环硫酸酯（12），并用苯甲酸铯开环然后将苯甲酸酯皂化，得到（+） - 泛酸盐（1a）。

6. 发明申请

US20210206798A1 BETULASTATIN COMPOUNDS 有权
公开(公告)号：US20210206798A1
公开(公告)日：2021-07-08
申请号：US16762781
申请日：2018-11-09
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： C07J63/00 , C07J71/00
摘要： The present disclosure relates to Betulastatin compounds, pharmaceutical compositions and kits comprising such compounds, and methods for using such compounds or pharmaceutical compositions.

7. 发明申请

US20090131672A1 SYNTHESIS OF SODIUM NARCISTATIN AND RELATED COMPOUNDS 失效
标题翻译：复方丹参及其相关化合物的合成
公开(公告)号：US20090131672A1
公开(公告)日：2009-05-21
申请号：US11813657
申请日：2006-01-17
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： C07F9/6574 , C07D491/056
CPC分类号： C07D491/04 , C07F9/65744
摘要： The present invention involves use of the compounds narciclasine (2a) and 7-deoxy-narciclasine (2c), which are obtained via isolation from the medicinal plant species Narcissus (Amaryllidaceae), as precursors in a novel synthesis method in which each of these compounds are selectively hydrogenated to produce trans-dihydronarciclasine (1a) and 7-deoxy-trans-dihydronarciclasine (1c). Also described herein is a novel synthesis method for producing sodium narcistatin (11) from narciclasine (2a). Further described herein are certain novel 3,4-cyclic phosphate prodrugs, including sodium-7-deoxynarcistatin (8), sodium-7-deoxy-transdihydronarcistatin (9), and sodium transdihydronarcistatin (10).
摘要翻译：本发明涉及通过从药用植物种水仙（Amaryllidaceae）中分离获得的化合物亚硝酸（2a）和7-脱氧 - 亚硝酰胺（2c）的用途，作为其中每种化合物的新型合成方法中的前体被选择性氢化以产生反式 - 二氢亚肼基卡那霉素（1a）和7-脱氧 - 反式 - 二氢氢化亚胺（1c）。本文还描述了一种从亚硝酸（2a）生产钠盐（11）的新型合成方法。本文进一步描述了一些新的3,4-环磷酸酯前药，包括7-脱氧丝氨酸激素（8），7-脱氧 - 二氢氯沙坦钠（9）和十二氢肌苷钠（10）。

8. 发明申请

US20090082569A1 NARCISTATIN PRODRUGS 有权
公开(公告)号：US20090082569A1
公开(公告)日：2009-03-26
申请号：US12208191
申请日：2008-09-10
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： C07F9/6561 , C07F9/6568
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。

9. 发明授权

US07351830B2 Pancratistatin cyclic phosphate prodrugs and phenpanstatin cyclic phosphate prodrugs 有权
标题翻译： Pancratistatin环磷酸酯前药和phenpanstatin环磷酸酯前药
公开(公告)号：US07351830B2
公开(公告)日：2008-04-01
申请号：US10561338
申请日：2004-06-18
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： C07F9/59 , C07D491/12
CPC分类号： A61K31/675 , C07F9/6561 , C07F9/65744
摘要： Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexyl-carbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient mute to a new series (3b-3d) of promising 3,4-O-cyclic phosphate prodrugs designated phenpanstatin phosphates. Application of analogous reaction conditions to pancratistatin (1a) led to a mixture of monophosphate derivatives where sodium paancratistatin 4-O-phosphate (4a) was isolated and the structure confirmed by x-ray craxtallography. Modification of the reaction conditions allowed direct phosphorylation of pancratistatin followed by cation exchange chromatography to afford sodium pancratistatin 3,4-O-cyclic phosphate (5b) which was selected for preclinical development.
摘要翻译：发现使用四丁基二氢磷酸二氢铵和二环己基碳二亚胺在吡啶中进行的选择性磷酸化，然后进行阳离子交换色谱法，为新的3,4-O- 环磷酸酯前药指定为苯巴毒素磷酸盐。将类似的反应条件应用于pancratistatin（1a）导致单分散磷酸盐衍生物的混合物，其中分离出钠盐钠（4 a），并通过x射线照相术证实结构。反应条件的改变允许pancratistatin直接磷酸化，然后进行阳离子交换层析，得到选择用于临床前发展的pancratistatin 3,4-O-环磷酸钠（5b）。

10. 发明申请

US20210101900A1 EMETINE AURISTATIN COMPOUNDS 有权
公开(公告)号：US20210101900A1
公开(公告)日：2021-04-08
申请号：US17062295
申请日：2020-10-02
申请人： George R. Pettit , Noeleen Melody
发明人： George R. Pettit , Noeleen Melody
IPC分类号： C07D471/04 , A61P35/04
摘要： The present disclosure relates to Emetine Auristatin compounds, pharmaceutical compositions and kits comprising such compounds, and methods for using such compounds or pharmaceutical compositions.

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