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32 条记录 (耗时 0.036 秒)

    2-(substituted imino)-thiazolidines and process for the preparation thereof
    24.
    发明授权
    2-(substituted imino)-thiazolidines and process for the preparation thereof 失效
    2-（取代的亚氨基） - 噻唑啉及其制备方法

    公开(公告)号：US5240918A

    公开(公告)日：1993-08-31

    申请号：US857067

    申请日：1992-03-24

    申请人： Karoly Lempert ,  Gyula Hornyak ,  Jozsef Fetter ,  Antal Feller ,  Klara Gaso ,  Gabor Gigler ,  Laszlo Kapolnai ,  Lujza Petocz ,  Katalin Szemeredi ,  Marton Fekete

    发明人： Karoly Lempert ,  Gyula Hornyak ,  Jozsef Fetter ,  Antal Feller ,  Klara Gaso ,  Gabor Gigler ,  Laszlo Kapolnai ,  Lujza Petocz ,  Katalin Szemeredi ,  Marton Fekete

    IPC分类号： C07D277/18

    CPC分类号： C07D277/18

    摘要： The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.1-6 alkenyl optionally carrying a halogen or a di-(C.sub.1-4 alkyl)-amino substituent; orZ and R.sup.5 together stand for a trivalent nitrogen atom, with the proviso that if Z denotes a substituted imino group, R.sup.5 stands for C.sub.1-4 alkylthio, and if R.sup.5 is C.sub.1-4 alkylthio, Z represents a substituted imino, and with the further proviso that if Z denotes sulfur, R.sup.5 is other than hydrogen or C.sub.1-4 alkyl,and possess valuable antianginal and analgesic properties.

    摘要翻译： 本发明涉及新的2-（取代的亚氨基） - 噻唑烷，其制备方法，包含该方法的药物组合物，所述2-（取代的亚氨基）噻唑烷用于治疗疾病和用于制备药物 适用于治疗疾病的组合物。 本发明提供的新的2-（取代亚氨基） - 噻唑烷衍生物对应于通式（I），其中R 1和R 2各自表示卤素，硝基，C 1-4烷氧基或C 1-4烷基 ，其可以任选地带有一个或多个卤素取代基，R 3和R 4各自表示氢或C 1-4烷基，Z表示氧，硫或亚氨基，后者被C 1-6烷基或C 1-6 烯基，R5代表氢，C1-4烷基，C1-4烷硫基或基团-NH-R，其中R表示C1-6烷基，芳基，芳烷基或任选携带卤素或 二（C 1-4烷基） - 氨基取代基; 或Z和R5一起代表三价氮原子，条件是如果Z表示取代的亚氨基，则R5表示C1-4烷硫基，如果R5是C1-4烷硫基，则Z表示取代的亚氨基，并且与 进一步的条件是，如果Z表示硫，R5不是氢或C1-4烷基，并且具有有价值的抗心绞痛和止痛特性。

    5-(substituted amino)-1,2,4-triazolo (1,5-A) pyrimidine derivatives
    26.
    发明授权
    5-(substituted amino)-1,2,4-triazolo (1,5-A) pyrimidine derivatives 失效
    5-（取代氨基）-1,2,4-三唑并（1,5-A）嘧啶衍生物

    公开(公告)号：US5478825A

    公开(公告)日：1995-12-26

    申请号：US261214

    申请日：1994-06-15

    申请人： Jozsef Reiter ,  Gabor Berecz ,  Gizella Zsila ,  Lujza Pet cz ,  Gabor Gigler ,  Marton Fekete ,  Maria Szecsey nee Heged s ,  Enik Szirt nee Kiszelly ,  Ludmila Rohacs nee Zamkovaja ,  Frigyes Gorgenyi ,  Margit Csorg

    发明人： Jozsef Reiter ,  Gabor Berecz ,  Gizella Zsila ,  Lujza Pet cz ,  Gabor Gigler ,  Marton Fekete ,  Maria Szecsey nee Heged s ,  Enik Szirt nee Kiszelly ,  Ludmila Rohacs nee Zamkovaja ,  Frigyes Gorgenyi ,  Margit Csorg

    IPC分类号： C07D471/14 ,  C07D487/04 ,  C07D495/14 ,  A61K31/535 ,  A61K31/505

    CPC分类号： C07D471/14 ,  C07D487/04 ,  C07D495/14

    摘要： The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.9 is alkyl substituted by alkoxy-carbonyl and possess inotropic and antianginal effects, complemented by antiinflammatory, ulcus, and gastric acid secretion inhibiting, and by weaker tranquillant, spasmolytic, and analgesic properties.

    摘要翻译： 所公开的化合物具有式“IMAGE”，其中Q为6元饱和杂环基团或S（O）pR 3基团，其中p为0,1或2，R 3为烷基，烯基或苯基，其中 可以具有卤素或硝基取代基，或任选取代的苯基; 或NR4R5，其中R4和R5是氢，烷基，烯基，苯基 - 烷基或二 - 烷基 - 氨基 - 烷基; 或者一起形成基团（CH 2）n -Y-（CH 2）m，其中Y是CH 2或NR 6，其中R 6是苯基 - 烷基，n和m是0或1至5; Z是NR7R8，其中R7和R8各自是氢，烯基，环烷基，金刚烷基或苯基 - 烷基，其可以具有一个或多个取代基或一起形成（CH 2）j W-（CH 2）k的基团，其中j和k 各自为1至3，W为氧，CH 2，CHOH或NR 10，其中R 10为氢，烷氧基羰基或烷基，后者可以被取代。 - 或SR9，其中R9是被烷氧基 - 羰基取代的烷基，并且具有各向同性和抗心绞痛作用，由抗炎，溃疡和胃酸分泌抑制以及较弱的镇静剂，解痉药和镇痛药物补充。

    Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same
    28.
    发明授权
    Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same 失效
    氨基丙醇衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：US5234934A

    公开(公告)日：1993-08-10

    申请号：US876091

    申请日：1992-04-30

    申请人： Zoltan Budai ,  Klara Reiter nee Esses ,  Eniko Sziri nee Kiszelly ,  Gizella Zsila ,  Gabor Gigler ,  Lujza Petocz ,  Maria Szecsey nee Hegedus ,  Marton Fekete ,  Valeria Hoffmann ,  Laszlo Kapolnai

    发明人： Zoltan Budai ,  Klara Reiter nee Esses ,  Eniko Sziri nee Kiszelly ,  Gizella Zsila ,  Gabor Gigler ,  Lujza Petocz ,  Maria Szecsey nee Hegedus ,  Marton Fekete ,  Valeria Hoffmann ,  Laszlo Kapolnai

    IPC分类号： C07C251/58 ,  C07D213/16 ,  C07D295/088

    CPC分类号： C07D213/16 ,  C07C251/58 ,  C07D295/088 ,  C07C2101/02 ,  C07C2101/08 ,  C07C2101/14 ,  C07C2101/18

    摘要： The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6,acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.

    摘要翻译： 本发明涉及式I的新型外消旋或光学活性氨基丙醇衍生物其中R和R 1独立地为氢原子，卤素原子，低级烷氧基或一起代表亚甲基二氧基，R2和R3一起表示化学键或 独立地代表氢原子，R4和R5独立地是氢原子，C3-7环烷基或任选被一个或多个二烷基氨基烷基，二甲氧基苯基或苯基取代的直链或支链，饱和或不饱和的C 1-12烷基，或R 4 和R5与相邻的氮原子一起形成任选地包含氧，硫或另外的氮原子的4至7元环，该环任选被苯基，苄基或C 1-3烷基取代，所述取代基可以携带 羟基，一个或两个甲氧基，卤素原子或三氟甲基，或R4和R5与相邻的氮原子一起形成哌啶环，其任选地是 由苯基或苄基构成，如果需要，它包含双键，R6代表氢原子或苯甲酰基，n代表3-6的整数，其酸加成盐和季铵衍生物。 本发明还涉及制备这些化合物的方法。 本发明的化合物发挥心脏循环控制和/或改善，中枢神经系统镇定和/或消化系统不调节改善作用。

    Condensed quinolinium and isoquinolinium derivatives
    29.
    发明授权
    Condensed quinolinium and isoquinolinium derivatives 失效
    浓缩的喹啉和异喹啉衍生物

    公开(公告)号：US4994448A

    公开(公告)日：1991-02-19

    申请号：US251445

    申请日：1988-09-30

    申请人： Andras Messmer ,  Gyorgy Hajos ,  Zsuzsa Juhasz nee Riedl ,  Pal Benko ,  Laszlo Pallos ,  Lujza Petocz ,  Eniko Szirt nee Kiszelly ,  Gabor Gigler ,  Istvan Gyertyan ,  Maria Hegedus

    发明人： Andras Messmer ,  Gyorgy Hajos ,  Zsuzsa Juhasz nee Riedl ,  Pal Benko ,  Laszlo Pallos ,  Lujza Petocz ,  Eniko Szirt nee Kiszelly ,  Gabor Gigler ,  Istvan Gyertyan ,  Maria Hegedus

    IPC分类号： A61K31/53 ,  A61P25/02 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-4 alkyl or aralkyl; andR.sub.2 represents hydroxy; orR.sub.1 and R.sub.2 together form a valency bond;R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl, amino, alkylthio or a group of the Formula --NR.sub.7 R.sub.8 in which R.sub.7 and R.sub.8 may be the same or different and stand for hydrogen, C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl or di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl or together with the nitrogen atom they are attached to form a 6-membered heterocyclic ring which may optionally contain a further nitrogen, oxygen or sulfur atom; orR.sub.2 and R.sub.3 together form an oxo (.dbd.O) or thixo (.dbd.S) group;R.sub.4 represents hydrogen, C.sub.1-4 alkyl or phenyl which may optionally bear one or two halogen or nitro substituent(s);Z is a group of the Formula (a) or (b) ##STR2## A.sup.- represents an anion) and isomers thereof possess useful local anaesthetic, antidepressant, tranquillo-sedative and smooth muscle relaxant properties accompanied by a weaker analgesic effect and are useful in therapy.

    摘要翻译： 通式I的新化合物Ⅰ（其中R1代表C1-4烷基或芳烷基，R2代表羟基;或R1和R2一起形成价键; R3是氢，C1-4烷基，C1- 烷氧基，苯基，氨基，烷硫基或式-NR7R8的基团，其中R 7和R 8可以相同或不同，代表氢，C 1-4烷基，苯基-C 1-4烷基，羟基-C 1-4烷基 或二 - （C 1-4烷基） - 氨基-C 1-4烷基或与它们连接的氮原子一起形成可任选地含有另外的氮，氧或硫原子的6元杂环;或R 2和R 3 一起形成氧代（= O）或触变（= S）基团; R4代表氢，C1-4烷基或苯基，其可任选地带有一个或两个卤素或硝基取代基; Z是式（a ）或（b）和A-表示阴离子）及其异构体具有有用的局部麻醉剂，抗抑郁药，镇痛镇痛和平滑肌松弛剂性质，伴随较弱的镇痛剂 c效应，可用于治疗。

    Optically active 2-chloro-12-(3-dimethylamino-2-methyl-propyl)-12H-dibenzo[d.g] [1,3,6] dioxazocines and a process for the preparation thereof
    30.
    发明授权
    Optically active 2-chloro-12-(3-dimethylamino-2-methyl-propyl)-12H-dibenzo[d.g] [1,3,6] dioxazocines and a process for the preparation thereof 失效
    光学活性的2-氯-12-（3-二甲基氨基-2-甲基 - 丙基）-12H-二苯并[d] [1,3,6]二氧杂吖庚因及其制备方法

    公开(公告)号：US4906622A

    公开(公告)日：1990-03-06

    申请号：US195691

    申请日：1988-05-18

    申请人： Laszlo Rozsa ,  Lujza Petocz ,  Eniko Szirt nee Kiszelly ,  Peter Tompe ,  Gabor Gigler

    发明人： Laszlo Rozsa ,  Lujza Petocz ,  Eniko Szirt nee Kiszelly ,  Peter Tompe ,  Gabor Gigler

    IPC分类号： A61K31/395 ,  A61P25/00 ,  A61P25/16 ,  C07D273/00 ,  C07D273/01

    CPC分类号： C07D273/00

    摘要： The invention relates to optically active 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]dioxazocine of the Formula ##STR1## and pharmaceutically acceptable acid additional salts thereof. The enantiomers are especially active against Parkinsion's disease.The optically active enantiomers are prepared by(a) resolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine with a optically active organic acid and separating the enantiomers; or(b) dissolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine in an organic solvent, crystallizing and isolating one of the enantiomers, optionally dissolving additional racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine in the mother liquor obtained and crystallizing and isolating the other enantiomer, and, if desired, repeating the whole process.

    摘要翻译： 本发明涉及式（I）的光学活性2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6]二恶唑辛嗪和药学上 其可接受的酸性附加盐。 对映异构体对帕金森氏病特别活跃。 旋光对映异构体通过以下步骤制备：（a）用光学拆分外消旋的2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] 活性有机酸并分离对映异构体; 或（b）将外消旋的2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] - 二氧杂吖嗪在有机溶剂中溶解， 的对映异构体，任选地将另外的外消旋的2-氯-12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] - 二氧杂吖嗪应用于所获得和结晶的母液中， 分离另一个对映体，如果需要，重复整个过程。