公开(公告)号：US06211382B1

公开(公告)日：2001-04-03

申请号：US09463357

申请日：2000-04-13

申请人： Csaba Huszár ,  Attila Kis-Tamás ,  Attila Németh ,  Zsuzsanna Nád ,  Zoltán Makovi ,  Antal Gajáry ,  Endre Kollár ,  Péter Aranyosi ,  Károly Gyüre ,  István Mészáros ,  Zsuzsanna Csetriné Hári ,  Attila Supic ,  Ilona Dervalicsne Zrinyi ,  Katalin Dubovszki ,  Lajosné Páli ,  Ágnes Kunsztné Kárász ,  Erzsébet Bognár

发明人： Csaba Huszár ,  Attila Kis-Tamás ,  Attila Németh ,  Zsuzsanna Nád ,  Zoltán Makovi ,  Antal Gajáry ,  Endre Kollár ,  Péter Aranyosi ,  Károly Gyüre ,  István Mészáros ,  Zsuzsanna Csetriné Hári ,  Attila Supic ,  Ilona Dervalicsne Zrinyi ,  Katalin Dubovszki ,  Lajosné Páli ,  Ágnes Kunsztné Kárász ,  Erzsébet Bognár

IPC分类号： C07D23502

CPC分类号： C07D235/02 ,  C07C255/46 ,  C07C2601/08

摘要： Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C1-6 alkyl group, or C7-12 aralkyl group or phenyl group, characterised in that a) the compound of formula (III) is reacted with a compound of formula (IV) wherein X means halogen atom or C1-5 alkoxy group or hydroxyl group, and the resulting compound of formula (II) is transformed, in a reaction medium with pH above 7, into the compound of formula (I) or b) the compound of formula (III) is reacted with an anhydride of general formula (V) and the resulting compound of formula (II) transformed, in a reaction medium with pH above 7, into the compound of formula (I), or c) a compound of formula (II) is transformed, in a reaction medium with pH above 7, into the compound of formula (I), and if desired, the resulting compounds of formula (I), before or after isolation, are transformed into acid addition salts, or the compounds of formula (I) are liberated from their acid addition salts. Thus a process for the preparation of intermediates useful in synthesis of angiotensin II antagonists is disclosed.

摘要翻译： 制备其中R表示氢原子或C 1-6烷基或C 7-12芳烷基或苯基的式（I）化合物的方法，其特征在于a）式（III）化合物与 其中X表示卤素原子或C 1-5烷氧基或羟基的式（Ⅳ）化合物，将所得式（Ⅱ）化合物在pH高于7的反应介质中转化为式（I）化合物， 或b）将式（III）化合物与通式（V）的酸酐反应，并将所得的式（II）化合物在pH高于7的反应介质中转化为式（I）化合物， 或c）将式（II）化合物在pH高于7的反应介质中转化为式（I）化合物，如果需要，所得到的式（I）化合物在分离前或分离后为 转化成酸加成盐，或式（I）化合物从其酸加成盐中释放出来。 因此，公开了制备可用于合成血管紧张素II拮抗剂的中间体的方法。

公开(公告)号：US06239286B1

公开(公告)日：2001-05-29

申请号：US09463434

申请日：2000-05-15

申请人： Attila Kis-Tamás ,  Csaba Huszár ,  Bertrand Castro ,  Attila Németh ,  Péter Aranyosi ,  Károly Gyüre ,  István Mészáros ,  Ilona Dervalicsné Zrínyi ,  Katalin Dubovszki ,  Lajosné Páli ,  Antal Gajáry ,  Attila Supic ,  Zsuzsanna Nád ,  Zoltán Makovi ,  Endre Kollár ,  Zsuzsanna Csetriné Hári ,  Ágnes Kunsztné Kárász ,  Erzsébet Bognár

发明人： Attila Kis-Tamás ,  Csaba Huszár ,  Bertrand Castro ,  Attila Németh ,  Péter Aranyosi ,  Károly Gyüre ,  István Mészáros ,  Ilona Dervalicsné Zrínyi ,  Katalin Dubovszki ,  Lajosné Páli ,  Antal Gajáry ,  Attila Supic ,  Zsuzsanna Nád ,  Zoltán Makovi ,  Endre Kollár ,  Zsuzsanna Csetriné Hári ,  Ágnes Kunsztné Kárász ,  Erzsébet Bognár

IPC分类号： C07D23502

CPC分类号： C07D235/02 ,  C07C255/46 ,  C07C2601/08

摘要： Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C1-6 alkyl group, or C7-12 aralkyl group or phenyl group, characterised in that: a) the compound of formula (III) is reacted with a compound of formula (IV) wherein X means halogen atom or C1-5 alkoxy group or hydroxyl group and the resulting compound of formula (II) is transformed in the presence of an oxidising agent in a reaction medium with pH above 7, into the compound of formula (I), or b) the compound of formula (III) is reacted with an anhydride of general formula (V) and the resulting compound of formula (II) transformed in the presence of an oxidising agent, in a reaction medium with pH above 7, into the compound of formula (I), or c) a compound of formula (II) is transformed in the presence of an oxidising agent, in a reaction medium with pH above 7, into the compound of formula (I), and if desired, the resulting compounds of formula (I), before or after isolation, are transformed into acid addition salts, or the compounds of formula (I) are liberated from their acid addition salts. Thus a process for the preparation of intermediates useful in synthesis of angiotensin II antagonists is disclosed.

摘要翻译： 制备其中R表示氢原子或C 1-6烷基或C 7-12芳烷基或苯基的式（I）化合物的方法，其特征在于：a）将式（III）化合物与 式（Ⅳ）化合物，其中X表示卤素原子或C 1-5烷氧基或羟基，所得式（II）化合物在氧化剂存在下，在pH高于7的反应介质中转化为 式（I）化合物或b）使式（III）化合物与通式（V）的酸酐和所得的式（II）化合物在氧化剂存在下在反应介质中反应 （II）的化合物转化成式（I）的化合物，或c）将式（II）化合物在氧化剂存在下，在pH高于7的反应介质中转化成式（I ），如果需要，所得到的式（I）化合物在分离之前或之后被转化为 酸加成盐或式（I）化合物从其酸加成盐中释放出来。 因此，公开了制备可用于合成血管紧张素II拮抗剂的中间体的方法。

公开(公告)号：US08129197B2

公开(公告)日：2012-03-06

申请号：US12300479

申请日：2007-05-14

申请人： György Báthori ,  Dóra Méhn ,  Pál Ákos ,  Péter Krajcsi ,  Lajos Szente ,  Éva Fenyvesi ,  Ágnes Telbisz ,  Balázs Sarkadi ,  András Váradi ,  Szilvia Gedey ,  Hristos Glavinas ,  Emese Kis ,  Tünde Nagy ,  Attila Németh ,  Éva Molnár

发明人： György Báthori ,  Dóra Méhn ,  Pál Ákos ,  Péter Krajcsi ,  Lajos Szente ,  Éva Fenyvesi ,  Ágnes Telbisz ,  Balázs Sarkadi ,  András Váradi ,  Szilvia Gedey ,  Hristos Glavinas ,  Emese Kis ,  Tünde Nagy ,  Attila Németh ,  Éva Molnár

IPC分类号： G01N33/567 ,  G01N33/53 ,  C12P1/00 ,  C12P21/06 ,  C12N5/07 ,  C12N5/00

CPC分类号： G01N33/6872 ,  G01N33/92

摘要： The invention provides for a novel cholesterol loaded insect cell membrane preparation having an increased cholesterol level as compared to physiological cholesterol levels of insect cell membranes or to control insect cell membrane preparations without cholesterol loading, wherein said cholesterol loaded membrane preparation comprises an ABC transporter protein having an increased substrate transport activity due to increased cholesterol level of the membrane. The invention also relates to reagent kits comprising the preparations of the invention. The invention also relates to methods for manufacturing said preparations and methods for measuring any type of activity of the ABC transporters present in the cholesterol loaded membranes as well as studying or testing compounds and interaction of compounds and ABC transporters, in this assay systems. The invention also provides for a test system useful for testing whether ABC transporter proteins can be activated by cholesterol in an insect cell membrane.

摘要翻译： 本发明提供了与昆虫细胞膜的生理胆固醇水平相比具有增加的胆固醇水平或控制没有胆固醇负荷的昆虫细胞膜制剂的新型胆固醇负载的昆虫细胞膜制剂，其中所述胆固醇负载的膜制剂包含具有 由于膜的胆固醇水平升高导致的底物转运活性增加。 本发明还涉及包含本发明制剂的试剂盒。 本发明还涉及用于制备所述制剂的方法和用于测量存在于胆固醇负载膜中的ABC转运蛋白的任何类型的活性的方法，以及在该测定系统中研究或测试化合物和化合物和ABC转运蛋白的相互作用。 本发明还提供了一种用于测试ABC转运蛋白是否可以在昆虫细胞膜中被胆固醇激活的测试系统。

公开(公告)号：US20100021927A1

公开(公告)日：2010-01-28

申请号：US12300479

申请日：2007-05-14

申请人： György Báthori ,  Dóra Méhn ,  Pál Ákos ,  Péter Krajcsi ,  Lajos Szente ,  Éva Fenyvesi ,  Ágnes Telbisz ,  Balázs Sarkadi ,  András Váradi ,  Szilvia Gedey ,  Hristos Glavinas ,  Emese Kis ,  Tünde Nagy ,  Attila Németh ,  Éva Molnár

发明人： György Báthori ,  Dóra Méhn ,  Pál Ákos ,  Péter Krajcsi ,  Lajos Szente ,  Éva Fenyvesi ,  Ágnes Telbisz ,  Balázs Sarkadi ,  András Váradi ,  Szilvia Gedey ,  Hristos Glavinas ,  Emese Kis ,  Tünde Nagy ,  Attila Németh ,  Éva Molnár

IPC分类号： G01N33/53 ,  C12N5/10 ,  C12N1/00 ,  C12Q1/60 ,  G01N33/48 ,  C12Q1/02

CPC分类号： G01N33/6872 ,  G01N33/92

摘要： The invention provides for a novel cholesterol loaded insect cell membrane preparation having an increased cholesterol level as compared to physiological cholesterol levels of insect cell membranes or to control insect cell membrane preparations without cholesterol loading, wherein said cholesterol loaded membrane preparation comprises an ABC transporter protein having an increased substrate transport activity due to increased cholesterol level of the membrane. The invention also relates to reagent kits comprising the preparations of the invention. The invention also relates to methods for manufacturing said preparations and methods for measuring any type of activity of the ABC transporters present in the cholesterol loaded membranes as well as studying or testing compounds and interaction of compounds and ABC transporters, in this assay systems. The invention also provides for a test system useful for testing whether ABC transporter proteins can be activated by cholesterol in an insect cell membrane.

摘要翻译： 本发明提供了与昆虫细胞膜的生理胆固醇水平相比具有增加的胆固醇水平或控制没有胆固醇负荷的昆虫细胞膜制剂的新型胆固醇负载的昆虫细胞膜制剂，其中所述胆固醇负载的膜制剂包含具有 由于膜的胆固醇水平升高导致的底物转运活性增加。 本发明还涉及包含本发明制剂的试剂盒。 本发明还涉及用于制备所述制剂的方法和用于测量存在于胆固醇负载膜中的ABC转运蛋白的任何类型的活性的方法，以及在该测定系统中研究或测试化合物和化合物和ABC转运蛋白的相互作用。 本发明还提供了一种用于测试ABC转运蛋白是否可以在昆虫细胞膜中被胆固醇激活的测试系统。