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71. 发明授权

US4806545A (-)-1.beta.-ethyl-1.alpha.-hydroxymethyl-1,2,3,4,6,7,12, 12B.alpha.-octahydroindolo(2,3-A)quinolizine, process for its preparation and pharmaceutical compositions containing same 失效
标题翻译：（ - ） - 1β-乙基-1α-羟甲基-1,2,3,4,6,7,12,12aαα-八氢吲哚（2,3-A）喹嗪，其制备方法和含有它们的药物组合物
公开(公告)号：US4806545A
公开(公告)日：1989-02-21
申请号：US851327
申请日：1986-04-14
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Istvan Laszlovszky , Erzsebet Lapis , Laszlo Szporny , Lilla Forgacs , Csaba Kuthi , Aniko Gere
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Istvan Laszlovszky , Erzsebet Lapis , Laszlo Szporny , Lilla Forgacs , Csaba Kuthi , Aniko Gere
IPC分类号： A61K31/435 , A61P9/00 , A61P9/08 , C07D471/14 , C07D455/00
CPC分类号： C07D471/14
摘要： The invention relates to the new (-)-1.beta.-ethyl-1.alpha.-hydroxymethyl-1,2, 3,4,6,7,12,12b.alpha.-octa-hydroindolo[2,3-a] quinolizine of the formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of the compound of formula (I) and acid addition salts thereof by resolution of the corresponding racemic compound and optionally by subsequent hydrolysis and/or salt formation.The compound of formula (I) shows a remarkable peripheral vasodilating and antihypoxial activity. Pharmaceutical compositions comprising it as active ingredient are also within the scope of the invention.
摘要翻译：本发明涉及新的（ - ） - 1β-乙基-1α-羟基甲基-1,2,3,4,6,7,12,12bα-正 - 氢吲哚并[2,3-a]喹嗪式（I）化合物（I）及其酸加成盐。根据本发明的另一方面，提供了通过拆分相应的外消旋化合物和任选地随后的水解和/或盐形成来制备式（I）化合物及其酸加成盐的方法。式（I）化合物显示出显着的外周血管扩张和抗低氧活性。包含其作为活性成分的药物组合物也在本发明的范围内。

72. 发明授权

US4769373A Anti-arrhythmic azabicyclic compounds 失效
标题翻译：抗心律不齐的氮杂双环化合物
公开(公告)号：US4769373A
公开(公告)日：1988-09-06
申请号：US674773
申请日：1984-11-26
申请人： Karoly Nador , Gabor Kraiss , Margit Paroczay , Egon Karpati , Laszlo Szporny
发明人： Karoly Nador , Gabor Kraiss , Margit Paroczay , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/435 , A61P9/06 , A61P25/02 , C07D211/72 , C07D221/22 , C07D405/12 , C07D409/12 , A61K31/44
CPC分类号： C07D221/22 , C07D211/72 , C07D405/12 , C07D409/12
摘要： The invention relates to new anti-arrythmic azabicyclo[3.3.1]nonanes of the general formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are C.sub.1-4 alkyl groups which are the same or different, or one of them is a benzyl group and the others are C.sub.1-4 alkyl groups, andR.sup.4 is a hydroxy group, or an etherified hydroxy group of the formula --OR.sup.5, or an esterified hydroxy group of the formula --OOCR.sup.6, in which the esterifying groupR.sup.5 is a phenyl or benzyl group which optionally each can have a trihalomethyl substituent or one or more halogen or C.sub.1-4 substituents, or is a diphenyl or benzhydryl group, and the esterifying groupR.sup.6 is a C.sub.1-8 alkyl or a C.sub.3-6 cycloalkyl group, or a phenyl or benzyl group which optionally each can have a halo-substituent or one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro or phenyl substituents, or is an optionally halogenated or hydrogenated naphthyl group, or a cinnamyl group optionally substituted by a halogen atom or C.sub.1-4 alkoxy groups, or is a benzhydryl or 1,1-diphenyl-hydroxymethyl group, or is a heterocyclic substituent selected from the group consisting of thenyl, 9-xanthenyl or 3-indolyl-(C.sub.1-3 alkyl) groups,as well as the stereoisomers and pharmaceutically acceptable acid addition salts thereof.The invention also provides a process for the preparation of the new compounds of the general formula (I), in which new intermediates of the general formula (IV), ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, are utilized.
摘要翻译：本发明涉及通式（I）的新的抗焦虑氮杂二氮杂双环[3.3.1]壬烷，其中R1，R2和R3是相同或不同的C1-4烷基，或其中之一它们是苄基，其它是C 1-4烷基，R4是羟基，或式-OR5的醚化羟基或式-OOCR6的酯化羟基，其中酯化基团R5 是任选地可以具有三卤代甲基取代基或一个或多个卤素或C 1-4取代基的苯基或苄基，或者是二苯基或二苯甲基，酯化基团R6是C 1-8烷基或C 3-6环烷基基团或苯基或苄基，其任选地各自可以具有卤素取代基或一个或多个C 1-4烷基，C 1-4烷氧基，硝基或苯基取代基，或者是任选卤代或氢化的萘基或肉桂基任选被卤素原子或C 1-4烷氧基取代，或者是二苯甲基或1,1-二苯基 - 氢或者是选自草酰基，9-呫吨基或3-吲哚基 - （C 1-3烷基）基团的杂环取代基，以及它们的立体异构体和药学上可接受的酸加成盐。本发明还提供了制备通式（I）的新化合物的方法，其中通式（IV）的新中间体，其中R 1，R 2和R 3如上所定义，被利用。

73. 发明授权

US4481204A E-Homo-eburnane derivatives, process for their preparation, and pharmaceutical compositions containing these compounds 失效
标题翻译： E-Homo-eburnane衍生物，其制备方法和含有这些化合物的药物组合物
公开(公告)号：US4481204A
公开(公告)日：1984-11-06
申请号：US509150
申请日：1983-06-29
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/22 , A61K31/395 , C07D459/00 , C07D461/00
CPC分类号： C07D471/22
摘要： The invention relates to racemic or optically active E-homo-eburnane derivatives of the formula /I/, ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and acid addition salts thereof.The new compounds are pharmaceutically active, for example their certain representatives, in particular from the cis-series, show antidepressive activity, while others, especially the compounds of the trans-series, are potent anthypoxial agents. The compounds of the formula /I/ and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions.
摘要翻译：本发明涉及式/ I /，其中R 1和R 2独立地表示具有1至6个碳原子的烷基的式/ I /，/ IMAGE / I / C的外消旋或光学活性的E-均 - burn烷衍生物及其酸加成盐。新化合物是药学上活性的，例如它们的特定代表，特别是顺式的化合物显示出抗抑郁活性，而其它代表，特别是反式系列的化合物是有效的抗氧化剂。因此，式/ I /的化合物及其药学上可接受的酸加成盐可用作药物组合物的活性成分。

74. 发明授权

US4428877A Cis-10-bromo-E-homoeburnanes 失效
标题翻译：顺式-10-溴-E-高乙炔二醇
公开(公告)号：US4428877A
公开(公告)日：1984-01-31
申请号：US234577
申请日：1981-02-13
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
IPC分类号： C07D209/16 , C07D209/42 , C07D461/00 , C07D471/14 , C07D471/22 , C07D459/00
CPC分类号： C07D471/14 , C07D209/16 , C07D209/42 , C07D461/00
摘要： A novel process for preparing 10-bromo-vincaminic acid esters and homologous compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group is disclosed.All the intermediate products are new and exhibit valuable therapeutical effect on the blood circulation.
摘要翻译：公开了一种制备10-溴 - 长春胺酸酯和通式为“IMAGE”的同系化合物的新方法，其中R1和R2各自代表C1-6烷基。所有的中间产品都是新的，对血液循环具有宝贵的治疗作用。

75. 发明授权

US4386073A Tripeptides acting on the central nervous system and a process for the preparation thereof 失效
标题翻译：作用于中枢神经系统的三肽及其制备方法
公开(公告)号：US4386073A
公开(公告)日：1983-05-31
申请号：US163830
申请日：1980-06-27
申请人： Lajos Kisfaludy , Tamas Szirtes , Lajos Balaspiri , Eva Palosi , Laszlo Szporny , Adam Sarkadi
发明人： Lajos Kisfaludy , Tamas Szirtes , Lajos Balaspiri , Eva Palosi , Laszlo Szporny , Adam Sarkadi
IPC分类号： C07K5/08 , A61K38/00 , A61K38/04 , A61K38/06 , A61P5/12 , A61P25/00 , A61P25/26 , C07K1/02 , C07K1/06 , C07K1/08 , C07K1/113 , C07K5/06 , C07K5/078 , C07K5/087 , C07K5/097 , C07K14/575 , A61K37/00 , C07C103/52
CPC分类号： C07K5/0825 , C07K5/06043 , C07K5/06052 , C07K5/06147 , C07K5/06173 , C07K5/0821 , A61K38/00
摘要： The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),X--Y--W--NH.sub.2 (I)whereinX is L-pyroglutamyl, D-pyroglutamyl, L-2-keto-imidazolidine-4-carbonyl, L-6-keto-pipecolyl, L-thiazolidine-4-carbonyl, L-prolyl or orotyl group,Y is L-leucyl, L-norvalyl or L-histidyl group, andW is L-prolyl, D-prolyl, L-thiazolidine-4-carbonyl, L-pipecolyl, L-homoprolyl, L-leucyl, L-isoleucyl, L-methionyl or D-pipecolyl group, orthe W-NH.sub.2 group stands for pyrrolidyl or piperidyl group, with the proviso that if X is L-pyroglutamyl and Y is L-histidyl group, W is other than L-prolyl group, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.
摘要翻译：本发明涉及作用于中枢神经系统并对应于通式（I）的XYW-NH 2（I）的新肽衍生物，其中X是L-焦谷氨酰基，D-焦谷氨酰基，L-2-酮 - 咪唑烷-4 羰基，L-6-酮基哌啶基，L-噻唑烷-4-羰基，L-脯氨酰基或正十二烷基，Y是L-亮氨酰，L-缬氨酰或L-组氨酰基，W是L-脯氨酰基，D- 脯氨酰基，L-噻唑烷-4-羰基，L-哌啶基，L-高辛基，L-亮氨酰基，L-异亮氨酰基，L-甲硫氨酰基或D-哌啶基，或W-NH 2基团代表吡咯烷基或哌啶基，条件是，如果X是L-焦谷氨酰基，Y是L-组氨酰基，则W不是L-脯氨酰基，和其药学上可接受的复合物。这些化合物通过肽化学中常用的方法制备。

76. 发明授权

US4200636A 3-Amino-17a-aza-D-homoandrostane compounds, and pharmaceutical compositions containing them 失效
标题翻译： 3-氨基-17α-氮杂-D-高雄甾烷化合物和含有它们的药物组合物
公开(公告)号：US4200636A
公开(公告)日：1980-04-29
申请号：US934799
申请日：1978-08-17
申请人： Zoltan Tuba , Maria Marsai , Sandor Gorog , Katalin Biro , Egon Karpati , Laszlo Szporny
发明人： Zoltan Tuba , Maria Marsai , Sandor Gorog , Katalin Biro , Egon Karpati , Laszlo Szporny
IPC分类号： C07D221/18 , A61K31/395 , A61P21/02 , C07J73/00 , C07D401/04 , A61K31/47 , A61K31/495 , C07D401/10
CPC分类号： C07J73/005 , Y10S514/906
摘要： The invention relates to new 3-amino-17a-aza-D-homo-5.alpha.-androstane derivatives of the general formula I ##STR1## wherein R.sub.1 represents a methylene or an >N--CH.sub.3 group, and n stands for 1 or 2, and the acid addition salts and the quaternary salts of the general formula ##STR2## thereof, wherein R.sub.2 stands for an alkyl or alkenyl group having from 1 to 4 carbon atoms, and A represents a halogen atom, provided that if R.sub.1 stands for an >N--CH.sub.3 group, R.sub.2 is attached to the nitrogen of that >N--CH.sub.3 group. The new compound possess a non-polarizing neuromuscular blocking activity and have a short activity period.
摘要翻译：本发明涉及通式I的新的3-氨基-17a-氮杂-D-高-5α-雄甾烷衍生物，其中R1代表亚甲基或> N-CH3基团，n代表1或 2及其酸加成盐和通式Ⅰ（a）的季盐，其中R2代表具有1至4个碳原子的烷基或烯基，A代表卤素原子，条件是如果R1表示> N-CH3基团，则R2连接到> N-CH 3基团的氮。新化合物具有非极化的神经肌肉阻滞活性，活性较短。

77. 发明授权

US4199598A Method of treating noradrenaline dysfunction or for dopamine-.beta.-hydroxylase inhibition 失效
标题翻译：治疗去甲肾上腺素功能障碍或多巴胺-β-羟化酶抑制的方法
公开(公告)号：US4199598A
公开(公告)日：1980-04-22
申请号：US29475
申请日：1979-04-12
申请人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bela Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bela Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/185
CPC分类号： A61K31/185
摘要： A method of treating mammalian noradrenaline malfunctions or dysfunction or effecting dopamine-.beta.-hydroxylase inhibition comprises administering an effective dose of an acid derivative of the formula (I), ##STR1## wherein R is C.sub.2-4 alkenyl, C.sub.3-8 cycloalkyl, benzyl or C.sub.1-6 alkyl which has a C.sub.1-4 alkoxy or a hydroxy substituent, or C.sub.2-6 alkyl with a carboxy and/or amino substituent, or C.sub.5 - or C.sub.6 -unsubtituted alkyl.
摘要翻译：治疗哺乳动物去甲肾上腺素功能障碍或功能障碍或影响多巴胺-β-羟化酶抑制的方法包括施用有效剂量的式（I）的酸衍生物，其中R是C 2-4链烯基，C 3-8 环烷基，苄基或具有C1-4烷氧基或羟基取代基的C1-6烷基，或具有羧基和/或氨基取代基的C2-6烷基或C5-或C6-未取代的烷基。

78. 发明授权

US4184040A Hydroxymethyl-pyridine esters and a process for the preparation thereof 失效
标题翻译：羟甲基 - 吡啶酯及其制备方法
公开(公告)号：US4184040A
公开(公告)日：1980-01-15
申请号：US839605
申请日：1977-10-05
申请人： Ferenc Noteisz , Mihaly Bartok , Karoly Felfoldi , Egon Karpati , Laszlo Szporny
发明人： Ferenc Noteisz , Mihaly Bartok , Karoly Felfoldi , Egon Karpati , Laszlo Szporny
IPC分类号： C07D213/16 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61P9/06 , C07D213/30 , C07D405/12 , C07D213/55
CPC分类号： C07D213/30
摘要： New hydroxymethyl-pyridine esters of the formula (I) ##STR1## wherein R represents a 9-xanthenyl group or a phenyl group substituted by a halogen atom or a trifluoromethyl group or by an alkyl or alkoxy group, either having 1 to 4 carbon atoms, and pharmaceutically acceptable acid addition salts and quaternary salts thereof are prepared by acylating the corresponding hydroxymethyl pyridines with a carboxylic acid of the formula R--COOH, or with a reactive derivative thereof, and, if desired, converting the obtained product of the formula I into a pharmaceutically acceptable acid addition salt or quaternary salt thereof. The new compounds exert beneficial effects on functional disorders of the heart.
摘要翻译：式（I）的新羟甲基 - 吡啶酯其中R表示9-呫吨基或被卤素原子或三氟甲基取代的苯基或被烷基或烷氧基取代的苯基，其具有1至 4个碳原子及其药学上可接受的酸加成盐和季盐通过用式R-COOH的羧酸或其反应性衍生物酰化相应的羟甲基吡啶来制备，如果需要，将所得产物式I化合成其药学上可接受的酸加成盐或其季盐。新化合物对心脏功能障碍有益。

79. 发明授权

US4120858A 14-Substituted vincanes 失效
标题翻译： 14取代的维根素
公开(公告)号：US4120858A
公开(公告)日：1978-10-17
申请号：US719066
申请日：1976-08-30
申请人： Otto Clauder , Jozsef Kokosi , Laszlo Szporny , Egon Karpati
发明人： Otto Clauder , Jozsef Kokosi , Laszlo Szporny , Egon Karpati
IPC分类号： A61K31/435 , A61P9/08 , A61P9/12 , A61P25/02 , A61P43/00 , C07D461/00 , C07D519/04
CPC分类号： C07D461/00 , Y10S514/824
摘要： A compound of the formula (I) ##STR1## wherein X stands for a hydrogen atom, an optionally substituted aliphatic or aromatic sulfonyloxy group, a thiocyanato group, an azido group or an amino group optionally mono- or disubstituted by aliphatic, cycloaliphatic, aromatic or araliphatic hydrocarbon groups, acyl, alkyloxycarbonyl, cycloalkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl, aminocarboimido groups or the substituents of the said amino group may form with the nitrogen atom thereof a five-, six- or seven-membered saturated or unsaturated heterocyclic ring optionally containing a further nitrogen, oxygen or sulfur hetero atom, and a quaternary salt or acid addition salt thereof. The compounds are useful in the treatment of arteriosclerosis and high blood pressure.
摘要翻译：式（I）的化合物其中X代表氢原子，任选取代的脂族或芳族磺酰氧基，硫氰酸酯基，叠氮基或氨基，任选被脂族，脂环族，芳族或芳脂族烃基，酰基，烷氧基羰基，环烷氧基羰基，芳氧基羰基，芳烷氧基羰基，氨基羧基亚氨基或所述氨基的取代基可以与其氮原子一起形成五元，六元或七元饱和或不饱和杂环，任选地含有进一步的氮，氧或硫杂原子，及其季盐或酸加成盐。该化合物可用于治疗动脉硬化和高血压。

80. 发明授权

US4082813A 3-Ioda-.alpha.-ethynyl benzhydrol 失效
标题翻译： 3-IODA-“ - 乙基苯甲醛
公开(公告)号：US4082813A
公开(公告)日：1978-04-04
申请号：US630512
申请日：1975-11-10
申请人： Edit Toth , Jozsef Torley , Sandor Gorog , Laszlo Szporny , Eva Palosi , Szabolcz Szeberenyi
发明人： Edit Toth , Jozsef Torley , Sandor Gorog , Laszlo Szporny , Eva Palosi , Szabolcz Szeberenyi
IPC分类号： C07C29/42 , C07C33/06
CPC分类号： C07C33/486 , C07C29/42
摘要： The invention is directed to a new substituted derivative of .alpha.-ethylnyl-benzophenone, namely, the 3-iodo-.alpha.-ethynyl-benzhydrol which has high antifungal activity.

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