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1. 发明申请

US20180141965A1 AUTOTAXIN INHIBITORS AND USES THEREOF 审中-公开
公开(公告)号：US20180141965A1
公开(公告)日：2018-05-24
申请号：US15575035
申请日：2016-05-18
申请人： NATIONAL AND KAPODISTRIAN UNIVERSITY OF ATHENS
发明人： GEORGE KOKOTOS
IPC分类号： C07F9/48 , C07C335/08 , C07C327/42 , C07C259/06 , C07C237/22 , C07F9/40 , A61P35/00 , A61P3/04 , A61P29/00 , A61P37/00
CPC分类号： C07F9/4816 , A61P3/04 , A61P29/00 , A61P35/00 , A61P37/00 , C07C237/22 , C07C259/06 , C07C327/42 , C07C335/08 , C07F9/4006
摘要： Novel inhibitors of the enzyme autotaxin are described. The inhibitors contain one or two zinc-binding groups at the appropriate distance, Also described are uses thereof, such as for the inhibition of autotaxin activity and the treatment of various conditions (e.g., inflammatory conditions, cancer, obesity, autoimmune diseases).

2. 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.

3. 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.

4. 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。

5. 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。

6. 发明授权

US08987489B2 Method for producing mono-carboxy-functionalized dialkylphosphinic acids, esters and salts using a vinyl ether and the use thereof 有权
标题翻译：使用乙烯基醚制备单羧基官能化二烷基次膦酸，酯和盐的方法及其用途
公开(公告)号：US08987489B2
公开(公告)日：2015-03-24
申请号：US13132196
申请日：2009-10-06
申请人： Michael Hill , Mathias Dietz , Werner Krause , Martin Sicken
发明人： Michael Hill , Mathias Dietz , Werner Krause , Martin Sicken
IPC分类号： C07F9/32 , C07F9/30 , C07F9/48 , C08K5/5313 , C09K21/12 , C08L21/00
CPC分类号： C07F9/30 , C07F9/301 , C07F9/32 , C07F9/4816 , C07F9/4866 , C08K5/5313 , C08L21/00 , C09K21/12
摘要： A method for producing mono-carboxy-functionalized dialkylphosphinic acids, esters and salts using a vinyl ether. The method is characterized by the following steps: a) reacting a phosphinic acid source (I) with olefins (IV) in the presence of a catalyst A to give an alkylphosphonous acid, the salt or the ester (II) thereof, b) reacting the alkylphosphonous acid so obtained, the salt or the ester (II) thereof with a vinyl ether of formula (V) in the presence of a catalyst B to give a mono-functionalized dialkylphosphinic acid derivative (VI) and c) reacting this derivative (VI) with an oxidant or in the presence of a catalyst C to give a mono-carboxy-functionalized dialkylphosphinic acid derivative (III), wherein the catalysts A and C are transition metals and/or transition metal compounds, and the catalyst B is a peroxide-forming compound and/or a peroxo compound and/or an azo compound.
摘要翻译：使用乙烯基醚制备单羧基官能化的二烷基次膦酸，酯和盐的方法。该方法的特征在于以下步骤：a）在催化剂A存在下使次膦酸源（I）与烯烃（IV）反应，得到烷基亚磷酸，其盐或其酯（II），b）使所得的烷基亚磷酸，其盐或其酯（II）与式（V）的乙烯基醚在催化剂B的存在下反应，得到单官能化的二烷基次膦酸衍生物（VI），和c）使该衍生物 VI）与氧化剂或催化剂C的存在下反应，得到单羧基官能化的二烷基次膦酸衍生物（III），其中催化剂A和C为过渡金属和/或过渡金属化合物，催化剂B为过氧化物形成化合物和/或过氧化合物和/或偶氮化合物。

7. 发明授权

US08916729B2 Compounds with (perfluoroalkyl) fluorohydrogenphosphate anions 有权
标题翻译：具有（全氟烷基）氟代磷酸氢根阴离子的化合物
公开(公告)号：US08916729B2
公开(公告)日：2014-12-23
申请号：US13516029
申请日：2010-12-06
申请人： Nikolai (Mykola) Ignatyev , Michael Schulte , Anne Julia Bader , Berthhold Theo Hoge
发明人： Nikolai (Mykola) Ignatyev , Michael Schulte , Anne Julia Bader , Berthhold Theo Hoge
IPC分类号： C07F9/535 , C07F9/30 , C07F9/38 , C07F9/48 , C07F9/54
CPC分类号： C07F9/535 , C07F9/301 , C07F9/3808 , C07F9/4816 , C07F9/5442
摘要： The present invention relates to a process for the preparation of compounds with (perfluoroalkyl)fluorohydrogenphosphate anion, and to compounds containing (perfluoroalkyl)fluorohydrogenphosphate anion and to the use thereof.
摘要翻译：本发明涉及一种制备具有（全氟烷基）氟代磷酸氢根阴离子的化合物和含有（全氟烷基）氟代磷酸氢根阴离子的化合物的方法及其用途。

8. 发明授权

US08735476B2 Method for producing mono-carboxy-functionalized dialkylphosphinic acids, esters and salts using a vinyl ester of a carboxylic acid and the use thereof 有权
标题翻译：使用羧酸的乙烯基酯制备单羧基官能化的二烷基次膦酸，酯和盐的方法及其用途
公开(公告)号：US08735476B2
公开(公告)日：2014-05-27
申请号：US13132153
申请日：2009-10-06
申请人： Michael Hill , Mathias Dietz , Werner Krause , Martin Sicken
发明人： Michael Hill , Mathias Dietz , Werner Krause , Martin Sicken
IPC分类号： C08K5/5313
CPC分类号： C09K21/12 , C07F9/301 , C07F9/4816 , C07F9/4866 , C08K5/5313
摘要： The invention relates to a method for producing mono-carboxy-functionalized dialkylphosphinic acids, esters and salts using a vinyl ester of a carboxylic acid. The method is characterized by the following steps: a) reacting a phosphinic acid source (I) with olefins (IV) in the presence of a catalyst A to give an alkylphosphinic acid, the salt or the ester (II) thereof, b) reacting the alkylphosphinic acid so obtained, the salt or the ester (II) thereof with a vinyl ester of a carboxylic acid of formula (V) in the presence of a catalyst B to give a mono-functionalized dialkylphosphinic acid derivative (VI) and c) reacting the mono-functionalized dialkylphosphinic acid derivative (VI) so obtained in the presence of a catalyst C to give a mono-functionalized dialkylphosphinic acid derivative (VII) and d) reacting the mono-functionalized dialkylphosphinic acid derivative (VII); with an oxidant or in the presence of a catalyst D to give a mono-carboxy-functionalized dialkylphosphinic acid derivative (III).
摘要翻译：本发明涉及使用羧酸的乙烯基酯制备单羧基官能化的二烷基次膦酸，酯和盐的方法。该方法的特征在于以下步骤：a）在催化剂A存在下使次膦酸源（I）与烯烃（IV）反应，得到烷基次膦酸，其盐或其酯（II），b）使如此获得的烷基次膦酸，其盐或其酯（II）与式（V）的羧酸的乙烯基酯在催化剂B的存在下反应，得到单官能化的二烷基次膦酸衍生物（Ⅵ）和c）使在催化剂C存在下得到的单官能化二烷基次膦酸衍生物（Ⅵ）反应，得到单官能化二烷基次膦酸衍生物（Ⅶ），和d）使单官能化二烷基次膦酸衍生物（Ⅶ）反应; 与氧化剂或在催化剂D存在下反应，得到单羧基官能化的二烷基次膦酸衍生物（III）。

9. 发明授权

US08293938B2 Alkylphosphonous acids, salts and esters, methods for the production thereof, and use of the same 有权
标题翻译：烷基亚磷酸，盐和酯，其制备方法及其用途
公开(公告)号：US08293938B2
公开(公告)日：2012-10-23
申请号：US12668814
申请日：2008-07-02
申请人： Michael Hill , Harald Bauer , Werner Krause
发明人： Michael Hill , Harald Bauer , Werner Krause
IPC分类号： C07F9/28
CPC分类号： C07F9/4866 , C07F9/4816 , C07F9/485 , C08K5/5393
摘要： The invention relates to alkylphosphonous acids, salts and esters of formula (I) A-P(═O)(OX)—H (I) wherein A is C2-C20alkyl, C2-C20alkylene, and C8-C20 alkaryl are optionally substituted, and X is H, alkyl, aryl, alkylaryl, alkenyl, substituted alkyl, aryl, alkaryl, alkenyl, ammonium, primary, secondary, tertiary, quaternary alkyl and/or aryl ammonium, an alkali metal, an alkaline earth metal, a metal of the third and fourth main group and the second, fourth and eight sub-group or a metal of the lanthanoid group. The invention also relates to methods for producing same and to the uses of said compounds.
摘要翻译：本发明涉及烷基亚磷酸，其中A是C 2 -C 20烷基，C 2 -C 20亚烷基和C 8 -C 20烷芳基的式（I）AP（= O）（OX）-H（I）的烷基亚磷酸，盐和酯，是烷基，芳基，烷基芳基，烯基，取代的烷基，芳基，烷芳基，烯基，铵，伯，仲，叔，季烷基和/或芳基铵，碱金属，碱土金属，第三和第四主要组和第二，第四和第八子组或镧系元素的金属。本发明还涉及其生产方法和所述化合物的用途。

10. 发明申请

US20110213078A1 Method for Producing Mono-Aminofunctionalized Dialkylphosphinic Acids and Esters and Salts Thereof by Means of Acrylnitriles and Use Thereof 有权
标题翻译：通过丙烯腈生产单氨基官能化二烷基膦酸及其酯及其盐的方法及用途
公开(公告)号：US20110213078A1
公开(公告)日：2011-09-01
申请号：US13127072
申请日：2009-10-06
申请人： Michael Hill , Werner Krause , Martin Sicken
发明人： Michael Hill , Werner Krause , Martin Sicken
IPC分类号： C08L67/02 , C07F9/30 , C07F9/32 , C07F5/06 , C07F7/28 , C08G63/183 , C08L77/06 , C08G69/26
CPC分类号： C07F9/3211 , C07F9/301 , C07F9/3264 , C07F9/4816 , C07F9/4866 , C08K5/5313 , C09K21/12
摘要： The invention relates to a method for producing mono-aminofunctionalized dialkylphosphinic acids and esters and salts thereof by means of acrylnitriles, characterized in that a) a phosphinic acid source (I) is reacted with olefins (IV) to yield an alkylphosphonic acid, salt or ester (II) thereof in the presence of a catalyst A, b) the thus obtained alkylphosphonic acid, salt or ester (II) thereof is reacted with an acrylnitrile of formula (V) to yield a mono-functionalized dialkylphosphinic acid derivative (VI) in the presence of a catalyst B, and c) the thus obtained mono-functionalized dialkylphosphinic acid derivative (VI) is reacted to yield a mono-aminofunctionalized dialkylphosphinic acid derivative (III) in the presence of a catalyst C or a reduction agent, wherein R1, R2, R3, R4, R5, R6, R7 are the same or different and stand independently of each other, among other things, for H, C1-C18 alkyl, C6-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl and X stands for H, C1-C18 alkyl, C6-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl, Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K and/or a protonized nitrogen base, and Y stands for a mineral acid, a carboxylic acid, a Lewis acid or an organic acid, n=an integer or fractional number of 0 to 4 and the catalysts A and C are formed by transition metals, transition metal compounds and/or catalyst systems composed of a transition metal and/or a transition metal compound and at least one ligand, and catalyst B is formed by compounds forming peroxides, peroxo compounds, azo compounds, alkali metals, alkaline earth metals, alkali hydrides, alkaline earth hydrides and/or alkali alcoholates and alkaline earth alcoholates.
摘要翻译：本发明涉及一种通过丙烯腈生产单氨基官能化二烷基次膦酸及其酯及其盐的方法，其特征在于a）将次膦酸源（I）与烯烃（Ⅳ）反应，得到烷基膦酸盐或盐酯（II），b）将由此得到的烷基膦酸，其盐或酯（II）与式（V）的丙烯腈反应，得到单官能化二烷基次膦酸衍生物（Ⅵ）在催化剂B存在下，和c）将由此得到的单官能化二烷基次膦酸衍生物（Ⅵ）反应，得到单氨基官能化二烷基次膦酸衍生物（Ⅲ），其中催化剂C或还原剂存在下，其中对于H，C 1 -C 18烷基，C 6 -C 18芳基，C 6 -C 18芳烷基，C 6 -C 18烷基，R 1，R 2，R 3，R 4，R 5，R 6，R 7相同或不同，彼此独立烷基芳基，X代表H，C1-C18烷基，C6-C 18芳基，C 6 -C 18芳烷基，C 6 -C 18烷基芳基，Mg，Ca，Al，Sb，Sn，Ge，Ti，Fe，Zr，Zn，Ce，Bi，Sr，Mn，Cu，Ni，Li，Na，K 和/或质子化的氮碱，Y表示无机酸，羧酸，路易斯酸或有机酸，n = 0至4的整数或分数，催化剂A和C由过渡金属形成由过渡金属和/或过渡金属化合物和至少一种配体组成的过渡金属化合物和/或催化剂体系和催化剂B通过形成过氧化物，过氧化合物，偶氮化合物，碱金属，碱土金属，碱金属氢化物，碱土金属氢化物和/或碱金属醇盐和碱土金属盐。

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