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1. 发明授权

US09937139B2 β-substituted γ-amino acids and analogs as chemotherapeutic agents 有权
公开(公告)号：US09937139B2
公开(公告)日：2018-04-10
申请号：US15594904
申请日：2017-05-15
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： Bernd Jandeleit , Wolf-Nicolas Fischer , Kerry J. Koller
IPC分类号： C07C229/08 , A61K31/197 , C07C271/46 , C07C309/69 , C07D257/04 , A61K31/41 , A61K31/662 , C07C229/42 , C07C237/30 , C07C239/20 , C07F9/48 , C07C239/18 , C07F9/32 , A61K47/54 , A61K47/48
CPC分类号： A61K31/197 , A61K31/41 , A61K31/662 , A61K47/542 , C07C229/08 , C07C229/42 , C07C237/30 , C07C239/18 , C07C239/20 , C07C271/46 , C07C309/69 , C07D257/04 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

2. 发明申请

US20180078517A1 BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS 审中-公开
公开(公告)号：US20180078517A1
公开(公告)日：2018-03-22
申请号：US15826042
申请日：2017-11-29
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： BERND JANDELEIT , WOLF-NICOLAS FISCHER , KERRY J. KOLLER
IPC分类号： A61K31/197 , C07F9/30 , C07C233/35 , C07C237/20 , C07C229/42 , A61K31/27 , A61K31/255 , C07C229/08 , C07F9/32 , C07C239/20 , C07C237/30 , C07C229/34 , C07C229/22 , C07F9/48 , A61K31/662 , C07C309/69 , C07C271/46 , C07C237/04 , C07C309/66
CPC分类号： A61K31/197 , A61K31/255 , A61K31/27 , A61K31/662 , C07C229/08 , C07C229/22 , C07C229/34 , C07C229/42 , C07C233/35 , C07C237/04 , C07C237/20 , C07C237/30 , C07C239/20 , C07C271/46 , C07C309/66 , C07C309/69 , C07F9/306 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

3. 发明申请

US20160296484A1 BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS 审中-公开
标题翻译：作为化学治疗剂的β-取代的氨基酸和类似物
公开(公告)号：US20160296484A1
公开(公告)日：2016-10-13
申请号：US15181817
申请日：2016-06-14
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： BERND JANDELEIT , WOLF-NICOLAS FISCHER , KERRY J. KOLLER
IPC分类号： A61K31/197 , A61K31/255 , A61K31/27 , A61K31/662
CPC分类号： A61K31/197 , A61K31/255 , A61K31/27 , A61K31/662 , C07C229/08 , C07C229/22 , C07C229/34 , C07C229/42 , C07C233/35 , C07C237/04 , C07C237/20 , C07C237/30 , C07C239/20 , C07C271/46 , C07C309/66 , C07C309/69 , C07F9/306 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
摘要翻译： β取代的β-氨基酸，β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物和（生物）等电点及其作为化学治疗剂的用途。 β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物和（生物）等分子体是选择性LAT1 / 4F2hc底物，并且在表达LAT1 / 4F2hc转运蛋白的肿瘤中表现出快速吸收和保留。还公开了合成β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物的方法和使用该化合物治疗癌症的方法。 β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物在表达LAT1 / 4F2hc转运蛋白的肿瘤细胞中表现出选择性摄取，并且当在体内施用于受试者时，其积累在癌细胞中。 β取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物和（生物）等体积体对几种肿瘤类型表现出细胞毒性。

4. 发明申请

US20150218085A1 BETA-SUBSTITUTED GAMMA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS 有权
标题翻译：经取代的氨基酸氨基酸和类似物作为化学治疗剂
公开(公告)号：US20150218085A1
公开(公告)日：2015-08-06
申请号：US14613130
申请日：2015-02-03
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： BERND JANDELEIT , WOLF-NICOLAS FISCHER , KERRY J. KOLLER
IPC分类号： C07C229/08 , C07C271/46 , C07D257/04 , C07C309/69 , C07F9/48
CPC分类号： A61K31/197 , A61K31/41 , A61K31/662 , A61K47/542 , C07C229/08 , C07C229/42 , C07C237/30 , C07C239/18 , C07C239/20 , C07C271/46 , C07C309/69 , C07D257/04 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.
摘要翻译：＆bgr; - 取代的γ-氨基酸，＆被取代的γ-氨基酸衍生物和＆gt;取代的γ-氨基酸类似物和（生物）等电点及其作为化学治疗剂的用途。取代的γ-氨基酸衍生物和取代的γ-氨基酸类似物和（生物）等分子体是选择性LAT1 / 4F2hc底物，能够通过血脑屏障，并且在肿瘤中表现出快速的摄取和保留表达LAT1 / 4F2hc转运蛋白。还公开了合成取代的γ-氨基酸衍生物和取代的γ-氨基酸类似物和（生物）等离子体的方法和使用该化合物治疗肿瘤的方法。取代的γ-氨基酸衍生物和取代的γ-氨基酸类似物和（生物）等分子体对于表达LAT1 / 4F2hc转运蛋白的肿瘤细胞表现出改善的选择性，并且当在体内施用于受试者时积累在癌细胞中。取代的γ-氨基酸衍生物和取代的γ-氨基酸类似物和（生物）等分子体对各种肿瘤类型表现出增加的功效。

5. 发明申请

US20140045794A1 Phosphonate Compounds 有权
标题翻译：膦酸酯化合物
公开(公告)号：US20140045794A1
公开(公告)日：2014-02-13
申请号：US14059365
申请日：2013-10-21
申请人： The Regents of the University of California
发明人： Karl Y. Hostetler , James R. Beadle
IPC分类号： C07F9/48 , C07F9/6512 , C07F9/6561 , C07F9/572
CPC分类号： A61K31/675 , A61K9/0053 , A61K9/20 , A61K9/48 , C07F9/3873 , C07F9/404 , C07F9/405 , C07F9/48 , C07F9/5728 , C07F9/6512 , C07F9/65583 , C07F9/65616 , C07H19/04 , C07H19/10
摘要： The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
摘要翻译：本发明涉及膦酸酯化合物，含有它们的组合物，获得它们的方法及其用于治疗各种医学病症，例如骨质疏松症和其他骨代谢疾病，癌症，病毒感染等的用途。

6. 发明申请

US20130122213A1 METHOD OF COATING AN INORGANIC SUBSTRATE WITH A STABLE ORGANIC LAYER 有权
标题翻译：用稳定的有机层涂覆无机基材的方法
公开(公告)号：US20130122213A1
公开(公告)日：2013-05-16
申请号：US13811526
申请日：2010-07-21
申请人： Fabien Bellenger , Floryan De Campo , Camille Jourde , Tao Zhang
发明人： Fabien Bellenger , Floryan De Campo , Camille Jourde , Tao Zhang
IPC分类号： C09D4/00
CPC分类号： C09D4/00 , C03C17/324 , C07F9/3826 , C07F9/48 , C08F230/02
摘要： A method for coating a metallic or inorganic substrate is described, such as metal or glass supports, with an organic layer comprising conjugated diene phosphinate or phosphonate compounds.
摘要翻译：描述了金属或无机基材的涂覆方法，例如金属或玻璃载体，其中有机层包含共轭二烯次膦酸酯或膦酸酯化合物。

7. 发明授权

US08008308B2 Phosphonate compounds 有权
标题翻译：膦酸酯化合物
公开(公告)号：US08008308B2
公开(公告)日：2011-08-30
申请号：US12701410
申请日：2010-02-05
申请人： Karl Y. Hostetler , James R. Beadle , Ganesh D. Kini
发明人： Karl Y. Hostetler , James R. Beadle , Ganesh D. Kini
IPC分类号： A61K31/52 , C07C9/02
CPC分类号： A61K31/675 , A61K9/0053 , A61K9/20 , A61K9/48 , C07F9/3873 , C07F9/404 , C07F9/405 , C07F9/48 , C07F9/5728 , C07F9/6512 , C07F9/65583 , C07F9/65616 , C07H19/04 , C07H19/10
摘要： The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
摘要翻译：本发明涉及膦酸酯化合物，含有它们的组合物，获得它们的方法及其用于治疗多种医学病症，例如骨质疏松症和其他骨代谢疾病，癌症，病毒感染等的用途。

8. 发明申请

US20080103115A1 PHOSPHONATE COMPOUNDS 有权
标题翻译：磷酸盐化合物
公开(公告)号：US20080103115A1
公开(公告)日：2008-05-01
申请号：US11925309
申请日：2007-10-26
申请人： Karl Hostetler , James Beadle , Ganesh Kini
发明人： Karl Hostetler , James Beadle , Ganesh Kini
IPC分类号： A61K31/675 , A61P31/16 , A61P31/18 , A61P31/22 , C07F9/6561
CPC分类号： A61K31/675 , A61K9/0053 , A61K9/20 , A61K9/48 , C07F9/3873 , C07F9/404 , C07F9/405 , C07F9/48 , C07F9/5728 , C07F9/6512 , C07F9/65583 , C07F9/65616 , C07H19/04 , C07H19/10
摘要： The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
摘要翻译：本发明涉及膦酸酯化合物，含有它们的组合物，获得它们的方法及其用于治疗多种医学病症，例如骨质疏松症和其他骨代谢疾病，癌症，病毒感染等的用途。

9. 发明授权

US07094772B2 Phosphonate compounds 有权
标题翻译：膦酸酯化合物
公开(公告)号：US07094772B2
公开(公告)日：2006-08-22
申请号：US11100882
申请日：2005-04-06
申请人： Karl Y. Hostetler , James R. Beadle , Ganesh D. Kini
发明人： Karl Y. Hostetler , James R. Beadle , Ganesh D. Kini
IPC分类号： A61K31/662 , C07D239/02 , C07D473/00
CPC分类号： A61K31/675 , A61K9/0053 , A61K9/20 , A61K9/48 , C07F9/3873 , C07F9/404 , C07F9/405 , C07F9/48 , C07F9/5728 , C07F9/6512 , C07F9/65583 , C07F9/65616 , C07H19/04 , C07H19/10
摘要： The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
摘要翻译：本发明涉及膦酸酯化合物，含有它们的组合物，获得它们的方法及其用于治疗各种医学病症，例如骨质疏松症和其他骨代谢疾病，癌症，病毒感染等的用途。

10. 发明授权

US06806383B1 Process for preparing (metal) alkylphosphonites I 失效
标题翻译：制备（金属）烷基亚膦酸盐的方法I
公开(公告)号：US06806383B1
公开(公告)日：2004-10-19
申请号：US09578421
申请日：2000-05-25
申请人： Norbert Weferling , Martin Sicken
发明人： Norbert Weferling , Martin Sicken
IPC分类号： C07F928
CPC分类号： C07F9/48
摘要： The invention relates to a process for the preparation of (metal) salts of alkylphosphonous acids, which comprises reacting elemental yellow phosphorus with halogen-free alkylating agents in the presence of at least one base. The invention also relates to the use of the (metal) salts of alkylphosphonous acids prepared by this process.
摘要翻译：本发明涉及一种制备烷基亚磷酸（金属）盐的方法，其包括在至少一种碱的存在下使元素黄磷与无卤素烷基化剂反应。本发明还涉及（金属）通过该方法制备的烷基磷酸的盐。

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