公开(公告)号：US5157038A

公开(公告)日：1992-10-20

申请号：US566274

申请日：1990-08-10

申请人： Edit Toth ,  Jozsef Torley ,  Bela Hegedus ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

发明人： Edit Toth ,  Jozsef Torley ,  Bela Hegedus ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

IPC分类号： A61K31/42 ,  A61K31/445 ,  A61K31/4465 ,  A61P3/00 ,  A61P25/00 ,  A61P43/00 ,  C07D211/48 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113 ,  C07D493/10 ,  C07D498/10

CPC分类号： C07D491/10

摘要： The invention relates to novel 2-oxo-1-oxa-8-azaspiro[4,5]decane derivatives of the formula (I), ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen; a C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.1-4 alkyl group, the two latter two substituents optionally substituted on their aromatic moiety by one or more, same or different halogen, one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl group; or a tosyl group;R.sup.1 and R.sup.2 together represent a methylene group or, when X stands for an >NR group wherein R is as defined above, one of R.sup.1 and R.sup.2 m may represent a hydroxyl group and the other one is a methyl group; andR.sup.3 means hydrogen, benzyl, (C.sub.1-4 alkoxy)carbonyl, phenoxycarbonyl, benzyloxycarbonyl, formyl, piperidin-1-ylcarbonyl, morpholin-4-ylcarbonyl, 4-methylpiperazin-1-ylcarbonyl, 4-(2-hydroxethyl)piperazin-1-ylcarbonyl, 2-chloro-3-nicotinoylcarbamoyl or C.sub.1-6 alkylcarbamoyl group,as well as their acid addition and quaternary ammonium salts.

公开(公告)号：US20070043117A1

公开(公告)日：2007-02-22

申请号：US10564017

申请日：2004-07-08

申请人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Torley ,  Monika Babjak

发明人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Torley ,  Monika Babjak

IPC分类号： A61K31/198 ,  C07C237/20

CPC分类号： C07C233/63 ,  C07C231/12 ,  C07C231/24

摘要： The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester thereof with a base to yield an alkali salt and liberating the product from said salt by proper addition of an acid, is also provided. Still another aspect of the invention is a process for the preparation of nateglinide in the crystalline form “H” from other crystalline modifications of nateglinide.

摘要翻译： 本发明涉及新型晶型“G”中的N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（那格列奈）及其制备方法。 还提供了通过用碱处理其低级烷基酯以产生碱金属盐并通过适当添加酸从所述盐释放产物来制备手性纯奈格列奈的方法。 本发明的另一方面是从那格列奈的其他结晶修饰物制备结晶形式“H”的那格列奈的方法。

公开(公告)号：US20100256414A1

公开(公告)日：2010-10-07

申请号：US12755572

申请日：2010-04-07

申请人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Törley ,  Monika Babjak

发明人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Törley ,  Monika Babjak

IPC分类号： C07C229/36

CPC分类号： C07C233/63 ,  C07C231/12 ,  C07C231/24

摘要： The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester thereof with a base to yield an alkali salt and liberating the product from said salt by proper addition of an acid, is also provided. Still another aspect of the invention is a process for the preparation of nateglinide in the crystalline form “H” from other crystalline modifications of nateglinide.

摘要翻译： 本发明涉及新型晶型“G”中的N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（那格列奈）及其制备方法。 还提供了通过用碱处理其低级烷基酯以产生碱金属盐并通过适当添加酸从所述盐释放产物来制备手性纯奈格列奈的方法。 本发明的另一方面是从那格列奈的其他结晶修饰物制备结晶形式“H”的那格列奈的方法。

公开(公告)号：US07767847B2

公开(公告)日：2010-08-03

申请号：US10564017

申请日：2004-07-08

申请人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Törley ,  Monika Babjak

发明人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Törley ,  Monika Babjak

IPC分类号： C07C229/00

CPC分类号： C07C233/63 ,  C07C231/12 ,  C07C231/24

摘要： The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester thereof with a base to yield an alkali salt and liberating the product from said salt by proper addition of an acid, is also provided. Still another aspect of the invention is a process for the preparation of nateglinide in the crystalline form “H” from other crystalline modifications of nateglinide.

摘要翻译： 本发明涉及新型晶型“G”中的N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（那格列奈）及其制备方法。 还提供了通过用碱处理其低级烷基酯以产生碱金属盐并通过适当添加酸从所述盐释放产物来制备手性纯奈格列奈的方法。 本发明的另一方面是从那格列奈的其他结晶修饰物制备结晶形式“H”的那格列奈的方法。

公开(公告)号：US4555858A

公开(公告)日：1985-12-03

申请号：US513116

申请日：1983-06-14

申请人： Bela Hegedus ,  Sandor Balint ,  Janos Hudak ,  Gyorgy Barta ,  Jozsef Aszlanyi

发明人： Bela Hegedus ,  Sandor Balint ,  Janos Hudak ,  Gyorgy Barta ,  Jozsef Aszlanyi

IPC分类号： F26B17/12 ,  F26B25/22 ,  F26B21/10

CPC分类号： F26B25/22 ,  F26B17/122 ,  Y02P70/40

摘要： A hot drying agent discharged from the section for material transport of the bound moisture, having a low moisture content, is recirculated to the front part of the drying area; the moisture content of both of the fed and discharged material is measured and by means of the differential-analogue signal thus obtained the stream of the material to be dried and in a given case the heating of the drying agent is controlled. An apparatus for performing the drying operation is also provided.

摘要翻译： PCT No.PCT / HU82 / 00053 Sec。 371日期1983年6月14日第 102（e）日期1983年6月14日PCT申请日1982年10月18日PCT公开号 公开号WO83 / 01502 日期：1983年4月28日。从部分排出的热干燥剂再循环到干燥区域的前部，用于物料输送具有低含水量的结合水分的结合水分。 测量进料和排料两者的含水量，并通过所得到的差示模拟信号得到被干燥材料的流，在给定的情况下控制干燥剂的加热。 还提供了一种用于进行干燥操作的设备。