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1. 发明申请

US20220089606A1 Biologically Active Taxane Analogs and Methods of Treatment by Oral Administration 有权
公开(公告)号：US20220089606A1
公开(公告)日：2022-03-24
申请号：US17539578
申请日：2021-12-01
申请人： Tapestry Pharmaceuticals, Inc.
发明人： James D. McChesney , Gilles H. Tapolsky , David Lloyd Emerson , John Marshall , Michael Kurman , Manuel R. Modiano
IPC分类号： C07D493/06 , A61K31/357 , A61K31/495 , A61K39/395 , A61K45/06
摘要： The present invention relates to a novel chemical compound for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.

2. 发明申请

US20130022668A1 Biologically Active Taxane Analogs And Methods Of Treatment By Oral Administration 有权
标题翻译：生物活性紫杉烷类似物和口服治疗方法
公开(公告)号：US20130022668A1
公开(公告)日：2013-01-24
申请号：US13620852
申请日：2012-09-15
申请人： James D. McChesney , Gilles TAPOLSKY , David L. EMERSON , John MARSHALL , Tauseef AHMED , Allen COHN , Michael KURMAN , Manuel MODIANO
发明人： James D. McChesney , Gilles TAPOLSKY , David L. EMERSON , John MARSHALL , Tauseef AHMED , Allen COHN , Michael KURMAN , Manuel MODIANO
IPC分类号： A61K31/357 , A61P31/10 , A61K9/48 , A61K9/00 , A61K9/127
CPC分类号： C07D493/06 , A61K31/357 , A61K31/495 , A61K39/3955 , A61K45/06
摘要： The present invention relates to a novel chemical compound of formula S-(1): for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.
摘要翻译：本发明涉及式S-（1）的新型化合物：用于治疗癌症的组合物，含有所述化合物的组合物，制备方法和与其它治疗剂的组合。

3. 发明授权

US07879904B2 9, 10-α,α-OH-taxane analogs and methods for production thereof 有权
标题翻译： 9,10-α，α-OH-紫杉烷类似物及其制备方法
公开(公告)号：US07879904B2
公开(公告)日：2011-02-01
申请号：US12792427
申请日：2010-06-02
申请人： Jan Zygmunt , James Ferrara , James D. McChesney
发明人： Jan Zygmunt , James Ferrara , James D. McChesney
IPC分类号： A61K31/337 , A61K31/427
CPC分类号： A61K31/337 , A61K31/357 , C07D305/14 , C07D409/12 , C07D493/08 , Y02P20/55
摘要： The present invention relates to a method for the treatment of cancer in a cancer patient. In particular, the invention provides a method for the treatment comprising administering a taxane compound to a cancer patient, wherein the taxane compound is made by a process comprising treating a first compound represented by either Formula G′ or Formula M′: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
摘要翻译：本发明涉及癌症患者的癌症治疗方法。特别地，本发明提供了一种治疗方法，其包括向癌症患者施用紫杉烷化合物，其中所述紫杉烷化合物通过包括用式G'或式M'表示的第一化合物与第二化合物的通式R8R9C（OCH3）2和选自樟脑磺酸（CSA），对甲苯磺酸（PTSA），盐酸（HCl）和乙酸（AcOH）的酸的酸，其中R1和R2是各自选自H，烷基，烯烃基，芳族基，O-烷基，O-烯烃基或O-芳族基; R7是烷基，烯基或芳基; P1是羟基保护基; P5是7位的H或酸不稳定保护基; R8是H，烷基，烯属或芳基; 并且R 9为：H，烷基，烯属或芳族或如说明书中所定义。

4. 发明申请

US20210401797A1 Taxane Analogs for the Treatment of Brain Cancer 有权
公开(公告)号：US20210401797A1
公开(公告)日：2021-12-30
申请号：US17470891
申请日：2021-09-09
申请人： TAPESTRY PHARMACEUTICALS, INC.
发明人： James D. MCCHESNEY , Gilles H. TAPOLSKY , David L. EMERSON , John MARSHALL , Michael KURMAN , Manuel MODIANO
IPC分类号： A61K31/357 , A61K31/495 , A61K39/395 , A61K31/337 , A61K45/06 , C07D493/04 , A61K31/4188
摘要： Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.

5. 发明申请

US20170273942A1 Taxane Analogs for the Treatment of Brain Cancer 审中-公开
公开(公告)号：US20170273942A1
公开(公告)日：2017-09-28
申请号：US15483551
申请日：2017-04-10
申请人： Tapestry Pharmaceuticals, Inc.
发明人： James D. McChesney , Gilles H. Tapolsky , David L. Emerson , John Marshall , Michael Kurman , Manuel Modiano
IPC分类号： A61K31/357 , A61K39/395 , A61K31/4188 , A61K31/495 , C07D493/04 , A61K31/337 , A61K45/06
CPC分类号： A61K31/357 , A61K31/337 , A61K31/4188 , A61K31/495 , A61K39/3955 , A61K45/06 , C07D493/04 , A61K2300/00
摘要： Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.

6. 发明申请

US20150133536A1 9, 10-Alpha, Alpha-OH-Taxane Analogs and Methods for Production Thereof 有权
标题翻译： 9，10-α，α-OH-紫杉烷类似物及其生产方法
公开(公告)号：US20150133536A1
公开(公告)日：2015-05-14
申请号：US14604147
申请日：2015-01-23
申请人： Tapestry Pharmaceuticals, Inc.
发明人： Jan ZYGMUNT , James FERRARA , James D. MCCHESNEY
IPC分类号： A61K31/357 , A61K31/337
CPC分类号： A61K31/337 , A61K31/357 , C07D305/14 , C07D409/12 , C07D493/08 , Y02P20/55
摘要： Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G′ or Formula M′: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
摘要翻译：本文提供了化合物，含有该化合物的组合物，以及在癌症患者中治疗癌症的方法。特别地，所述化合物通过以下方法制备，所述方法包括用式G'或式M'表示的第一化合物与通式为R 8 R 9 C（OCH 3）2的第二化合物和选自樟脑磺酸（CSA），对甲苯磺酸（PTSA），盐酸（HCl）和乙酸（AcOH），其中R1和R2各自选自H，烷基，烯基，芳族基团，烷基，O-烯烃基或O-芳族基; R7是烷基，烯基或芳基; P1是羟基保护基; P5是7位的H或酸不稳定保护基; R8是H，烷基，烯属或芳基; 并且R 9为：H，烷基，烯属或芳族或如说明书中所定义。

7. 发明申请

US20090156828A1 Novel Compounds and Methods for Forming Taxanes and Using the Same 审中-公开
标题翻译：新型化合物和形成紫杉烷并使用它的方法
公开(公告)号：US20090156828A1
公开(公告)日：2009-06-18
申请号：US12097900
申请日：2005-12-21
申请人： John T. Henri , James D. McChesney , Sylesh Venkataraman , Christian Sumner , George Petros Yiannikouros , Aaron Michael Stemphoski , Donald G. Walker
发明人： John T. Henri , James D. McChesney , Sylesh Venkataraman , Christian Sumner , George Petros Yiannikouros , Aaron Michael Stemphoski , Donald G. Walker
IPC分类号： C07D263/02 , C07D305/14
CPC分类号： C07D305/14 , C07C271/22 , C07D263/06
摘要： The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds. More particularly, the present embodiments disclosed herein relate to novel side chains, that when coupled to a taxane, are useful for the synthesis of pharmaceutically useful taxanes. Methods of forming the novel side chains and coupling them to hindered alcohols, namely taxanes resulting in useful esters are also disclosed. Various taxanes compounds are known to exhibit anti-tumor activity.
摘要翻译：本发明广泛地涉及可用于合成生物活性化合物的新化合物。更具体地，本文公开的本实施方案涉及新颖的侧链，当与紫杉烷结合时可用于合成药学上有用的紫杉烷。还公开了形成新型侧链并将其偶联到受阻醇（即得到有用酯的紫杉烷）的方法。已知各种紫杉烷类化合物具有抗肿瘤活性。

8. 发明申请

US20080269319A1 Biologically active taxane analogs and methods of treatment 审中-公开
公开(公告)号：US20080269319A1
公开(公告)日：2008-10-30
申请号：US12215563
申请日：2008-06-26
申请人： James D. McChesney , Rodger Lamb , Stanley Kahler
发明人： James D. McChesney , Rodger Lamb , Stanley Kahler
IPC分类号： A61K31/337 , C07D305/14 , A61P35/00
CPC分类号： C07D493/06
摘要： The present application relates to new taxane analogs, pharmaceutical compositions comprising such analogs and methods of treating cancer comprising such compositions. The compounds according to the present application have the general formula: wherein R1 and R2 are each selected from H, alkyl, alkenyl or aryl; R3 is hydroxyl or OP1; R4 is OH or R7COO; R7 is alkyl, alkenyl or aryl, R8 and R9 are each independently selected from H, alkyl or alkenyl. The compounds of the present application may particularly be 9,10-α,α-OH taxane analogs that are formed by a process starting with a standard taxane as the starting compound.

9. 发明申请

US20060281807A1 Quassinoid compositions for the treatment of cancer and other proliferative diseases 审中-公开
标题翻译：用于治疗癌症和其他增殖性疾病的类软组合物
公开(公告)号：US20060281807A1
公开(公告)日：2006-12-14
申请号：US11151625
申请日：2005-06-13
申请人： James McChesney , Piotr Bartyzel , Jonathan Foster
发明人： James McChesney , Piotr Bartyzel , Jonathan Foster
IPC分类号： A61K31/366 , C07D493/14
CPC分类号： C07D493/08
摘要： The invention provides quassinoid compounds that are useful in treating cancer. The invention further provides a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of killing a cancer cell, and a method of treating cancer in a mammal.
摘要翻译：本发明提供了可用于治疗癌症的类喹诺酮类化合物。本发明还提供了包含药学上合适的载体和本发明的至少一种化合物，杀死癌细胞的方法和在哺乳动物中治疗癌症的方法的组合物。

10. 发明授权

US10143677B2 Taxane analogs for the treatment of brain cancer 有权
公开(公告)号：US10143677B2
公开(公告)日：2018-12-04
申请号：US15483551
申请日：2017-04-10
申请人： Tapestry Pharmaceuticals, Inc.
发明人： James D. McChesney , Gilles H. Tapolsky , David L. Emerson , John Marshall , Michael Kurman , Manuel Modiano
IPC分类号： A61K31/357 , C07D493/04 , A61K45/06 , A61K31/495 , A61K31/4188 , A61K39/395 , A61K31/337
摘要： Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.

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