公开(公告)号：US5118687A

公开(公告)日：1992-06-02

申请号：US566275

申请日：1990-08-10

申请人： Edit Toth ,  Jozsef Torley ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Katalin Csomor ,  Mihaly Bodo ,  Judit Laszy ,  Zsolt Szentirmay

发明人： Edit Toth ,  Jozsef Torley ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Katalin Csomor ,  Mihaly Bodo ,  Judit Laszy ,  Zsolt Szentirmay

IPC分类号： A61K31/33 ,  A61K31/335 ,  A61K31/42 ,  A61K31/435 ,  A61K31/445 ,  A61P3/00 ,  A61P9/00 ,  A61P9/10 ,  A61P25/28 ,  C07D221/00 ,  C07D263/00 ,  C07D317/00 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113 ,  C07D493/10 ,  C07D498/10

CPC分类号： C07D491/10

摘要： The invention relates to novel compounds 1-oxa-2-oxo-8- 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.10-4 alkyl group, the latter two groups are optionally substituted on their aromatic moiety by one or more, same or different halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy group(s);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 may represent a hydroxyl group whereas the other is a methyl group;R.sup.3 stands for hydrogen or a phenyl group optionally substituted by one or more halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy or hydroxyl group(s);R.sup.4 means hydrogen, one or more halogen(s), C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl or trihalomethyl group(s); andn is 1, 2 or 3as well as their acid addition and quaternary ammonium salts.

公开(公告)号：US5096902A

公开(公告)日：1992-03-17

申请号：US509473

申请日：1990-04-12

申请人： Karoly Nador ,  Pal Scheiber ,  nee Szelecsenyi; Erzsebet Andrasi ,  Bela Molnar ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Mihaly Bodo ,  Katalin Csomor ,  Judit Laszy ,  Zsolt Szentirmay

发明人： Karoly Nador ,  Pal Scheiber ,  nee Szelecsenyi; Erzsebet Andrasi ,  Bela Molnar ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Mihaly Bodo ,  Katalin Csomor ,  Judit Laszy ,  Zsolt Szentirmay

IPC分类号： A61K31/425 ,  A61K31/426 ,  A61K31/445 ,  A61K31/54 ,  A61P9/10 ,  A61P25/28 ,  C07D277/04 ,  C07D277/06 ,  C07D279/06 ,  C07D283/02 ,  C07D417/06

CPC分类号： C07D417/06 ,  C07D277/04 ,  C07D277/06 ,  C07D279/06

摘要： The invention relates to novel nitrogen- and sulfur-containing heterocyclic compounds of the formula (I), acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## Ar stands for an optionally mono- or polysubstituted aryl or heteroaryl group;R.sup.1 means a carbonyl or (C.sub.2-6 alkenyl)carbonyl group;R.sup.2 stands for hydrogen C.sub.1-6 alkyl, phenyl or phenyl (C.sub.1-4 alkyl) group;R.sup.3 means hydrogen or (C.sub.1-6 alkoxy)carbonyl group;R.sup.4 and R.sup.5 stand, independently from each other, for hydrogen or C.sub.1-6 alkyl group;R.sub.6 ogen, C.sub.1-6 alkyl group or halophenyl group;m is 0 or 1; andn is 1 or 2,with the proviso that R.sup.2 means hydrogen when m is 0.The compounds of formula (I) show a significant cerebral antihypoxic action and thus, they can be used for the treatment of diseases caused by hypoxic brain damages such as e.g. the senile dementia, Alzheimer's disease or disturbances of the cognitive function.

公开(公告)号：US5589486A

公开(公告)日：1996-12-31

申请号：US244867

申请日：1995-01-17

申请人： Kalman Harsanyi ,  Tibor Gizur ,  Eva Agai-Csongor ,  Anna Kallai-Sohonyai ,  Marta Kapolnas-Pap ,  Eva Csizer ,  Bela Heged us ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Mihaly Bodo ,  Katalin Csomor ,  Judit Laszy ,  Zsolt Szentirmai ,  Erzsebet Lapis ,  Sandor Szabo ,  Peter Bod ,  Attila Csehi

发明人： Kalman Harsanyi ,  Tibor Gizur ,  Eva Agai-Csongor ,  Anna Kallai-Sohonyai ,  Marta Kapolnas-Pap ,  Eva Csizer ,  Bela Heged us ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Mihaly Bodo ,  Katalin Csomor ,  Judit Laszy ,  Zsolt Szentirmai ,  Erzsebet Lapis ,  Sandor Szabo ,  Peter Bod ,  Attila Csehi

IPC分类号： A61K31/44 ,  A61K31/445 ,  A61K31/451 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P25/28 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/52 ,  C07D211/70

CPC分类号： C07D211/52 ,  C07D211/14 ,  C07D211/70

摘要： The invention relates to novel N-hydroxy-substituted 1,2,3,6-tetrahydropyridine and piperidine derivatives of the formula ##STR1## wherein A, B, D, E, G, I and R are as defined in the specification, m is 0, 1 or 2, with the proviso that:m is 0 or 2, or both G and I are hydrogen, when A is benzyl or halogen-monosubstituted benzyl group; andm is 1, when A is 2-picolyl, as well as their pharmaceutically acceptable acid addition salts. The compounds of formula (I) are useful for enhancing the tolerance of mammals (including man) against hypoxic and/or ischaemic states as well as for treating the degenerative and functional disturbances arising from hypoxic and/or ischaemic results.

摘要翻译： PCT No.PCT / HU92 / 00050 Sec。 371日期1995年1月17日 102（e）日期1995年1月17日PCT提交1992年12月1日PCT公布。 公开号WO93 / 11107 日期：1993年6月10日本发明涉及式（I）的新型N-羟基取代的1,2,3,6-四氢吡啶和哌啶衍生物，其中A，B，D，E，G，I和R m为0,1或2，条件是：当A为苄基或卤素 - 单取代的苄基时，m为0或2，或G和I均为氢。 当A为2-吡啶甲基时，m为1，以及其药学上可接受的酸加成盐。 式（I）化合物可用于增强哺乳动物（包括人）对缺氧和/或缺血状态的耐受性，以及用于治疗由缺氧和/或缺血结果引起的退行性和功能障碍。

公开(公告)号：US5494909A

公开(公告)日：1996-02-27

申请号：US244736

申请日：1994-07-20

申请人： Jen Kobor ,  Laszlo Lazar ,  Imre Huber ,  Judit Arva ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Mihaly Bodo ,  Katalin Csomor ,  Judit Laszy ,  Zsolt Szentirmai ,  Erzsebet Lapis ,  Sandor Szabo ,  Gabor Bernath ,  Ferenc Fulop

发明人： Jen Kobor ,  Laszlo Lazar ,  Imre Huber ,  Judit Arva ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Mihaly Bodo ,  Katalin Csomor ,  Judit Laszy ,  Zsolt Szentirmai ,  Erzsebet Lapis ,  Sandor Szabo ,  Gabor Bernath ,  Ferenc Fulop

IPC分类号： A61K31/535 ,  A61P3/00 ,  A61P9/08 ,  A61P9/10 ,  A61P25/28 ,  C07D217/06 ,  C07D498/04 ,  A61K31/47 ,  C07D265/14

CPC分类号： C07D498/04

摘要： New compounds with the ability to inhibit calcium uptake in the brains of mammals are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.4 alkyl;one of R.sup.2 and R.sup.3 is C.sub.1 to C.sub.4 alkoxy and the other one is phenyl-C.sub.1 to C.sub.4 alkoxy optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus; andR.sup.4 is phenyl optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus, or their solvates, individual optically active and geometric isomers, mixtures of such isomers, as well as pharmaceutically acceptable acid addition salts thereof. The compounds of the Formula (I) are capable of inhibiting calcium uptake to brain cells and have a protective effect on hypobaric hypoxia.

摘要翻译： PCT No.PCT / HU92 / 00053 Sec。 371日期：1994年7月20日 102（e）日期1994年7月20日PCT提交1992年12月11日PCT公布。 公开号WO93 / 12118 （I）其中R 1是氢，C 1至C 4烷基，苯基或苯基的式（I）公开了具有抑制哺乳动物脑中钙摄取的能力的新化合物。 C1至C4烷基; R2和R3中的一个是C1-C4烷氧基，另一个是在芳核中被C1-C4烷基任选取代的苯基-C 1至C 4烷氧基; 并且R 4是任选地被芳族核中的C 1 -C 4烷基取代的苯基，或它们的溶剂化物，单独的光学活性和几何异构体，这些异构体的混合物，以及其药学上可接受的酸加成盐。 式（I）的化合物能够抑制钙对脑细胞的吸收并对低压缺氧具有保护作用。

公开(公告)号：US5225416A

公开(公告)日：1993-07-06

申请号：US805861

申请日：1991-12-10

申请人： Tibor Gizur ,  Kalman Harsanyi ,  Attila Csehi ,  Aniko Demeter nee Szabo ,  Ferenc Trischler ,  Eva Vajda ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Mihaly Bodo ,  Katalin Csomor ,  Judit Laszy ,  Zsolt Szentirmai ,  Erzsebet Lapis ,  Sandor Szabo

发明人： Tibor Gizur ,  Kalman Harsanyi ,  Attila Csehi ,  Aniko Demeter nee Szabo ,  Ferenc Trischler ,  Eva Vajda ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Mihaly Bodo ,  Katalin Csomor ,  Judit Laszy ,  Zsolt Szentirmai ,  Erzsebet Lapis ,  Sandor Szabo

IPC分类号： A61K31/435 ,  A61P9/00 ,  C07D211/70

CPC分类号： C07D211/70

摘要： The present invention relates to novel 1,2,3,6-tetrahydropyridine derivatives of the general formula (I) ##STR1## wherein R stands for hydrogen or an alkyl group,X stands for an unsubstituted phenyl or benzyl group or for a phenyl or benzyl group substituted with a halogen atom,Y stands for hydrogen or halogen or a trifluoro-methyl groupas well as enantiomers acid addition salts thereof.The invention further extends to pharmaceutical compositions containing said compounds as active ingredient mainly for improving cerebral blood circulation and antihypoxic activity. The 1,2,3,6-tetrahydropyridine derivatives of the general formula (I) are prepared by treating an oxo derivative of the general formula (II) ##STR2## wherein R, X and Y are as given above in an organic solvent by a reducing agent and reacting the obtained 1,2,3,6-tetrahydropyridine derivative of the general formula (I), wherein R, X and Y are as given above, with a mineral or organic acid and converting the same, if desired, to an acid addition salt.

公开(公告)号：US5584297A

公开(公告)日：1996-12-17

申请号：US313218

申请日：1994-11-28

申请人： Mihaly Bodo ,  Istvan Nagy ,  Janos Peredi ,  Gyorgy Thuroczy ,  Laszlo Ozsvald

发明人： Mihaly Bodo ,  Istvan Nagy ,  Janos Peredi ,  Gyorgy Thuroczy ,  Laszlo Ozsvald

IPC分类号： A61B5/00 ,  A61B5/0205 ,  A61B5/02

CPC分类号： A61B5/4884 ,  A61B5/0002 ,  A61B5/0205

摘要： A method and apparatus diagnose a circulation disorder in a patient, and in particular, predict whether a patient is likely to suffer a stroke. The diagnosis is made based on a patient's responses to questions regarding whether the patient has experienced symptoms of a neurological disorder, and based on sensed electrical brain activity and sensed blood pulse activity. The pulse measurements may be taken at the patient's head, and/or at the patient's arms and/or legs. The diagnosis may be based upon a comparison of the patient's electrical brain activity on the right and left sides of the patient's brain, and on a comparison of the pulse activity on the right and left sides of the patient's head, arms and legs. The diagnosis may also be based on the patient's electrical heart activity. The diagnosis may further be based on the results of a stress test that measures the patient's blood pressure, pulse rate and anxiety level. Such a stress test may be performed before and/or after the patient's electrical brain activity, blood pulse activity and electrical heart activity have been measured. The diagnosis may also be based on whether the patient exhibits one or more arteriosclerosis risk factors and based on patient data such as age, weight, height, sex, blood cholesterol level and blood sugar level.

摘要翻译： PCT No.PCT / HU93 / 00006 Sec。 371日期：1994年11月28日 102（e）日期1994年11月28日PCT提交1993年2月8日PCT公布。 公开号WO93 / 19665 日期：1993年10月14日一种诊断患者循环障碍的方法和装置，特别是预测患者是否可能患有中风。 诊断是基于患者对关于患者是否经历神经障碍症状的问题以及基于感测的电脑活动和感测的血液脉冲活动的回答进行的。 可以在患者的头部和/或患者的手臂和/或腿部进行脉搏测量。 该诊断可以基于患者的大脑右侧和左侧的电脑大脑活动的比较，以及患者头部，手臂和腿部的左侧和右侧的脉搏活动的比较。 诊断也可以基于患者的电心脏活动。 诊断可以进一步基于测量患者血压，脉搏率和焦虑程度的压力测试的结果。 这样的压力测试可以在患者的电脑活动，血液脉冲活动和电心脏活动被测量之前和/或之后进行。 诊断还可以基于患者是否表现出一种或多种动脉硬化危险因素，并且基于患者数据，例如年龄，体重，身高，性别，血液胆固醇水平和血糖水平。