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61. 发明授权

US4866062A 1,4-disubstituted piperazines, pharmaceutical compositions thereof and method of use 失效
标题翻译： 1,4-二取代哌嗪，其药物组合物和使用方法
公开(公告)号：US4866062A
公开(公告)日：1989-09-12
申请号：US41234
申请日：1987-04-22
申请人： Edit Toth , Bela Kiss , Jozsef Turley , Eva Palosi , Istvan Hajdu , Laszlo Szporny , Dora Groo , Erzsebet Lapis , Istvan Laszlovszky
发明人： Edit Toth , Bela Kiss , Jozsef Turley , Eva Palosi , Istvan Hajdu , Laszlo Szporny , Dora Groo , Erzsebet Lapis , Istvan Laszlovszky
IPC分类号： C07D295/08 , A61K31/495 , A61P25/00 , A61P25/24 , A61P25/26 , A61P43/00 , C07D295/088
CPC分类号： C07D295/088
摘要： The invention relates to novel 1,4-disubstituted piperazine derivatives of the general formula (I), pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation.In the general formula (I) ##STR1## R.sub.1 and R.sub.2 are the same or different and stand for hydrogen or halogen or a lower alkyl, trihalomethyl or lower alkoxy group.The compounds of the general formula (I) are therapeutically useful for the treatment of diseases arising from a hypofunction of the dopaminergic system.
摘要翻译：本发明涉及通式（I）的新的1,4-二取代哌嗪衍生物，其药学上可接受的酸加成盐，含有它们的药物组合物及其制备方法。在通式（I）中，R 1和R 2相同或不同，代表氢或卤素或低级烷基，三卤代甲基或低级烷氧基。通式（I）的化合物可用于治疗由多巴胺能系统功能低下引起的疾病。

62. 发明授权

US4810709A Nintrovincaminic acid derivatives having pharmaceutical utility 失效
标题翻译：具有药用效用的新一代氨基酸衍生物
公开(公告)号：US4810709A
公开(公告)日：1989-03-07
申请号：US105959
申请日：1987-10-07
申请人： Andras Vedres , Csaba Szantay , Istvan Moldvai , Bela Stefko , Dora Groo , Egon Karpati , Bela Kiss , Eva Palosi , Miklos Riesz , Zsolt Szombathelyi , Laszlo Szporny , Maria Zajer nee Balazs
发明人： Andras Vedres , Csaba Szantay , Istvan Moldvai , Bela Stefko , Dora Groo , Egon Karpati , Bela Kiss , Eva Palosi , Miklos Riesz , Zsolt Szombathelyi , Laszlo Szporny , Maria Zajer nee Balazs
IPC分类号： A61K31/435 , A61P9/00 , A61P9/08 , A61P25/08 , C07D461/00 , A61K31/475
CPC分类号： C07D461/00
摘要： The invention relates to a new process for preparing novel racemic and optically active 9- or 11-nitroapovincaminic acid derivatives of the general formula (I) ##STR1## wherein R stands for a --CO--X group, wherein X means a halogen atom; orfor a --CO--OR.sup.1 group, wherein R.sup.1 means an optionally mono- or polysubstituted C.sub.1-10 aliphatic group, a C.sub.3-8 alicyclic group or an aromatic C.sub.6-14 hydrocarbyl group; orfor a --CO--NR.sup.2 R.sup.3 group, wherein R.sup.2 and R.sup.3 are the same or different and stand for a hydrogen atom or a C.sub.1-8 alkyl group optionally forming a saturated heterocycle together with the adjacent nitrogen atom and optionally with one or more further nitrogen atoms or other heteroatoms, and R.sup.3 may also represent an amino group when R.sup.2 stands for a hydrogen atom; orfor a cyano group,as well as their salts and pharmaceutical preparations containing these compounds. Furthermore the invention relates to a process for preparing these compounds and preparations.The racemic and optically active substances of the general formula (I) as well as their pharmaceutically acceptable acid addition and quaternary salts have valuable therapeutic properties, namely vasodilating, spasmolytic, antihypoxic and anticonvulsive effects.
摘要翻译：本发明涉及制备通式（I）的新型外消旋和光学活性的9-或11-硝基
氨基嘌呤酸衍生物的新方法，其中R代表-CO-X基团，其中X表示卤素原子; 或-CO-OR 1基团，其中R 1表示任选的单取代或多取代的C 1-10脂族基团，C 3-8脂环族基团或芳族C 6-14烃基; 或-CO-NR 2 R 3基团，其中R 2和R 3相同或不同，代表氢原子或任选地与相邻的氮原子一起形成饱和杂环的C 1-8烷基，并且任选地与一个或多个另外的氮原子或其它杂原子，当R 2代表氢原子时，R 3也可以表示氨基; 或氰基，以及它们的含有这些化合物的盐和药物制剂。此外，本发明涉及一种制备这些化合物和制剂的方法。通式（I）的外消旋和光学活性物质及其药学上可接受的酸加成盐和季盐具有有价值的治疗性质，即血管舒张，解痉，抗缺氧和抗惊厥作用。

63. 发明授权

US4753949A 2-chloronicergoline having antihypoxic activity 失效
标题翻译：具有抗低氧活性的2-氯麦角林
公开(公告)号：US4753949A
公开(公告)日：1988-06-28
申请号：US877294
申请日：1986-06-23
申请人： Gabor Megyeri , Tibor Keve , Bala Stefko , Erik Bogsch , Janos Galambos , Anna Kassi nee Zieger , Ferenc Trischler , Eva Palosi , Dora Groo , Egon Karpati , Zsolt Szombathelyi , Laszlo Szporny , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis
发明人： Gabor Megyeri , Tibor Keve , Bala Stefko , Erik Bogsch , Janos Galambos , Anna Kassi nee Zieger , Ferenc Trischler , Eva Palosi , Dora Groo , Egon Karpati , Zsolt Szombathelyi , Laszlo Szporny , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis
IPC分类号： A61K31/48 , A61P3/00 , A61P3/14 , A61P9/00 , A61P25/02 , A61P25/28 , C07D457/02
CPC分类号： C07D457/02
摘要： The invention relates to a novel process for the preparation of partially new 2-halonicergoline derivatives of the formula (I), ##STR1## wherein X stands for chlorine, bromine or iodine atom, as well as their acid addition salts.The process of the invention comprises esterifying a novel 2-halo-1-methyllumilysergol of the formula (II), ##STR2## wherein X is the same as defined above, or an acid addition salt thereof and, if desired, converting the thus-obtained 2-halonicergoline derivative of the formula (I) to an acid addition salt.The compounds of the invention improve the cognitive function of the brain and show an antihypoxic as well as a strong .alpha.-adrenerg blocking and calcium-antagonistic action.
摘要翻译：本发明涉及制备式（I）的部分新的2-卤代麦角灵衍生物的新方法，其中X代表氯，溴或碘原子，以及它们的酸加成盐。本发明的方法包括酯化式（II）的新的2-卤代-1-甲基烯丙基谷维素，其中X与上述定义相同，或其酸加成盐，如果需要，转化将由此获得的式（I）的2-卤代麦角灵衍生物与酸加成盐反应。本发明的化合物改善了脑的认知功能，并且显示出抗低氧以及强的α-肾上腺素能阻断和钙拮抗作用。

64. 发明授权

US4598080A Certain-2-methyl-6-{4-[1-phenyl-1-hydroxypropyl]-phenoxymethyl}pyridines which inhibit microsonal monoxygenase systems in liver 失效
标题翻译：在肝脏中抑制微血管单加氧酶系统的某些2-甲基-6- {4- [1-苯基-1-羟丙基] - 苯氧基甲基}吡啶
公开(公告)号：US4598080A
公开(公告)日：1986-07-01
申请号：US565831
申请日：1983-12-27
申请人： Edit Toth , Jozsef Torley , Eva Palosi , Szabolcs Szebereneyi , Laszlo Szporny , Sandor Gorog , Istvan Hajdu
发明人： Edit Toth , Jozsef Torley , Eva Palosi , Szabolcs Szebereneyi , Laszlo Szporny , Sandor Gorog , Istvan Hajdu
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4418 , A61P1/16 , A61P39/02 , A61P43/00 , C07D213/30
CPC分类号： C07D213/30
摘要： The invention relates to new pyridine derivatives of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. In particular, they inhibit the microsomal monooxigenase enzyme system of the liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
摘要翻译：本发明涉及式（I）的新的吡啶衍生物：其中R 1和R 2独立地表示氢，卤素，三卤代甲基，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基，以及酸加成物和季铵盐。根据本发明的另一方面，提供了这些化合物的制备方法。式（I）的化合物具有药理活性。特别地，它们抑制肝脏的微粒体单致原子酶系统。含有它们作为活性成分的药物组合物也在本发明的范围内。

65. 发明授权

US4508926A 4-Hydroxy-benzhydrols, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译： 4-羟基 - 二苯甲醛，其制备方法和含有它们的药物组合物
公开(公告)号：US4508926A
公开(公告)日：1985-04-02
申请号：US565840
申请日：1983-12-27
申请人： Edit Toth , Jozsef Torley , Gyorgy Fekete , Laszlo Szporny , Laszlo Vereczkey , Eva Palosi , Imre Klebovich , Pal Vittay , Sandor Gorog , Istvan Hajdu
发明人： Edit Toth , Jozsef Torley , Gyorgy Fekete , Laszlo Szporny , Laszlo Vereczkey , Eva Palosi , Imre Klebovich , Pal Vittay , Sandor Gorog , Istvan Hajdu
IPC分类号： C07C43/23 , A61K31/047 , A61K31/05 , A61K31/075 , A61P25/30 , C07C27/00 , C07C29/143 , C07C29/149 , C07C37/055 , C07C37/20 , C07C39/12 , C07C39/367 , C07C41/00 , C07C41/30 , C07C67/00 , C07C39/11
CPC分类号： C07C43/23 , C07C37/055 , C07C37/20 , C07C39/367
摘要： The invention relates to new 4-hydroxy-benzhydrols of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms, with the proviso that if R.sub.1 is hydrogen, R.sub.2 is other than hydrogen or a 3-trifluoromethyl group, or if R.sub.1 is a 2-methyl group, R.sub.2 is other than a 5-methyl group.According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. In particular, they are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them as active ingredients are also within the scope of the invention.
摘要翻译：本发明涉及式（I）的新的4-羟基 - 二苯甲醇：其中R 1和R 2独立地表示氢，卤素，三卤代甲基，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基原子，条件是如果R1是氢，R2不是氢或3-三氟甲基，或者如果R1是2-甲基，则R2不是5-甲基。根据本发明的另一方面，提供了这些化合物的制备方法。式（I）的化合物具有药理活性。特别地，它们适用于治疗急性乙醇中毒。含有它们作为活性成分的药物组合物也在本发明的范围内。

66. 发明授权

US4179467A Dopamine hydroxylase inhibiting 2-amino-cyclopent-1-ene-1-thiocarboxylic acid-disulfides 失效
标题翻译：多巴胺羟化酶抑制2-氨基 - 环戊-1-烯-1-硫代羧酸二硫化物
公开(公告)号：US4179467A
公开(公告)日：1979-12-18
申请号：US865429
申请日：1977-12-29
申请人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bella Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bella Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/13 , C07C87/02
CPC分类号： C10M1/08
摘要： New 2-amino-cyclopent-1-ene-thiocarboxylic acid-disulfides of the formula, ##STR1## wherein R is a C.sub.1-6 alkyl group having optionally a C.sub.1-4 alkoxy, hydroxy, carboxy and/or amino substituent, a C.sub.2-4 alkenyl group, or a C.sub.3-8 cycloalkyl group, are prepared by oxidizing the respective 2-amino-cyclopent-1-ene-dithiocarboxylic acids of the formula, ##STR2## wherein R is as defined above. The compounds of the formula (I) exert dopamine-.beta.-hydroxylase inhibiting effects and can be applied in therapy.
摘要翻译：新的2-氨基 - 环戊-1-烯 - 硫代羧酸 - 二硫化物，其中R是具有任选C 1-4烷氧基的C 1-6烷基，羟基，羧基和/或氨基取代基，C 2-4链烯基或C 3-8环烷基，是通过将下式所示的2-氨基环戊-1-烯二硫代羧酸，其中R如上定义。式（I）化合物发挥多巴胺-β-羟化酶抑制作用，可用于治疗。

67. 发明授权

US4094908A Alpha-substituted benzhydrol derivatives 失效
标题翻译： α-取代的二苯甲醇衍生物
公开(公告)号：US4094908A
公开(公告)日：1978-06-13
申请号：US722063
申请日：1976-09-09
申请人： Edit Toth , Jozsef Torley , Szabolcs Szeberenyi , Eva Palosi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
发明人： Edit Toth , Jozsef Torley , Szabolcs Szeberenyi , Eva Palosi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
IPC分类号： C07C33/34 , C07C39/21 , C07C65/01 , C07D295/135 , C07C93/08
CPC分类号： C07D295/135 , C07C255/00 , C07C33/34 , C07C39/21 , C07C65/01
摘要： The invention relates to new .alpha.-substituted benzhydrols and pharmaceutically acceptable acid addition salts or quaternary ammonium salts thereof with enzyme promoting or inhibiting effects;
摘要翻译：本发明涉及新的α-取代二苯甲醇及其药学上可接受的酸加成盐或季铵盐，具有促进或抑制酶的作用;

68. 发明授权

US4017507A 2,3-Dihydro-7-chlorothiazolo[3,2-a]benzimidazole and salt 失效
标题翻译： 2,3-二氢-7-氯噻唑并[8 3,2-a {9苯并咪唑和盐
公开(公告)号：US4017507A
公开(公告)日：1977-04-12
申请号：US637978
申请日：1975-12-05
申请人： Kalman Hideg , Olga Hankovszky , Eva Palosi , Gyorgy Hajos , Laszlo Szporny
发明人： Kalman Hideg , Olga Hankovszky , Eva Palosi , Gyorgy Hajos , Laszlo Szporny
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： New tricyclic fused imidazole derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##STR2## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a=C-- group, orA stands for a group of the general formula (III), ##STR3## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##STR4## wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##STR5## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(ch.sub.2).sub.m --X VI.in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen. The reaction is carried out optionally in the presence of a base. The compounds of the general formula (I) can be converted into their acid addition salts.The compounds of the general formula (I) as well as their acid addition salts exert antipyretic and antiphlogistic activities, inhibit the reproduction of viruses, and exert a protecting effect against albumine shock.
摘要翻译：通式（I）的新型三环稠合咪唑衍生物，其中R1代表氢或羟基，N等于零或一，M等于零，一或二，A代表一个基团的通式（II），其中R 2表示氢或羟基，R 3表示氢或氨基，或Q和Z各自代表氮或a = C-基团，或A表示一个通式（III），其中R 4和R 5各自代表氢，甲基，氯或硝基，通过反应通用化合物（IV）化合物（IV）制备其中A和n各自具有与上述定义相同的含有通式（Ⅴ）的化合物，其中X代表卤素，R6代表氢，R7代表通式（Ⅵ）的基团，（CH2）mX VI。

69. 发明授权

US3989701A Diamine-benzophenones and a process for the preparation thereof 失效
标题翻译：二胺 - 二苯甲酮及其制备方法
公开(公告)号：US3989701A
公开(公告)日：1976-11-02
申请号：US485744
申请日：1974-07-03
申请人： Edit Toth , Jozsef Torley , Eva Palosi , Szaboles Szeberenyi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
发明人： Edit Toth , Jozsef Torley , Eva Palosi , Szaboles Szeberenyi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
IPC分类号： C07D295/10 , A61K31/135 , A61K31/165 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P25/24 , A61P25/26 , C07C67/00 , C07C213/00 , C07C225/22 , C07C231/00 , C07C231/02 , C07C233/43 , C07D207/06 , C07D233/56 , C07D233/61 , C07D295/135 , C07D295/00
CPC分类号： C07D295/135 , Y10S514/916
摘要： New compounds of the general formula (I) ##SPC1##whereinR.sub.1 and R.sub.2 each is a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form substituted or unsubstituted heterocyclic group with or without a further oxygen or nitrogen heteroatom, andR.sub.3 is hydrogen or an acyl group derived from a C.sub.1.sub.-18 carboxylic acid.The compounds are prepared by reducing the corresponding nitro compounds of the general formula (II) ##SPC2##and optionally acylating the obtained product.The compounds of the general formula (I) and their acid addition salts and quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess valuable antipyretic activity and a yohimbine lethality increasing effect characteristic of antidepressants.
摘要翻译：通式（I）的新化合物，其中R 1和R 2各自为饱和或不饱和的直链或支链烷基，芳烷基，饱和或不饱和环烷基或芳基，或者R1和R2与相邻的氮原子可以形成具有或不具有另外的氧或氮杂原子的取代或未取代的杂环基，并且R 3是氢或衍生自C 1-18羧酸的酰基。

70. 发明授权

US3932395A Tricyclic imidazole derivatives 失效
标题翻译：三环咪唑衍生物
公开(公告)号：US3932395A
公开(公告)日：1976-01-13
申请号：US473184
申请日：1974-05-24
申请人： Kalman Hideg , Olga Hankovszky , Eva Palosi , Gyorgy Hajos , Laszlo Szporny
发明人： Kalman Hideg , Olga Hankovszky , Eva Palosi , Gyorgy Hajos , Laszlo Szporny
IPC分类号： C07D513/16 , C07D513/04 , C07D513/14 , C07D279/08 , C07D279/14
CPC分类号： C07D513/04 , C07D513/14 , Y10S514/916
摘要： New tricyclic fused imidazole derivatives of the general formula (I), ##SPC1##whereinR.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##EQU1## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a =C-- group, orA stands for a group of the general formula (III), ##EQU2## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##SPC2##wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##EQU3## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(CH.sub.2).sub.m --X (VI)in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen. The reaction is carried out optionally in the presence of a base. The compounds of the general formula (I) can be converted into their acid addition salts.The compounds of the general formula (I) as well as their acid addition salts exert antipyretic and antiphlogistic activities, inhibit the reproduction of viruses, and exert a protecting effect against albumine shock.
摘要翻译：新的通式（I）的三环稠合咪唑衍生物，其中R1代表氢或羟基，N等于零或一，M等于零，一或二，A代表通式（II ），-C = QC = Z- |（II）R2R3其中R2表示氢或羟基，R3表示氢或氨基，或Q和Z各自代表氮或a = C-基团，或A表示通式（III）-CH = C-C = CH- |（III）R4R5其中R4和R5各自表示氢，甲基，氯或硝基，通过反应通用化合物（IV）的化合物制备，其中A和n各自具有与上述相同的含义，与通式（V）的化合物，X-CH 2 -CH-CH 2 ||（V）R 6 R 7，其中X代表卤素，R6代表氢，R7 代表通式（VI）， - （CH 2）m X（VI）的基团，其中m和X各自具有与上述相同的含义，或者R6和R7一起代表氧。任选地在碱的存在下进行反应。通式（I）的化合物可以转化成它们的酸加成盐。

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