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1. 发明授权

US4438132A 4-Oxo-PGI.sub.2 compounds, their use in inhibition of thrombii and their production 失效
标题翻译： 4-Oxo-PGI2化合物，它们用于抑制血栓形成及其产生
公开(公告)号：US4438132A
公开(公告)日：1984-03-20
申请号：US368013
申请日：1982-04-13
申请人： Gaza Galambos , Vilmos Simonidesz , Istvan Szekely , Jozsef Ivanics , Krisztina Kekesi , Gabor Kovacs , Istvan Stadler , Peter Kormoczy , Karoly Horvath
发明人： Gaza Galambos , Vilmos Simonidesz , Istvan Szekely , Jozsef Ivanics , Krisztina Kekesi , Gabor Kovacs , Istvan Stadler , Peter Kormoczy , Karoly Horvath
IPC分类号： C07D307/935 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/08 , C07C405/00 , C07D307/937
CPC分类号： C07D307/937 , C07C317/00 , Y02P20/55 , Y10S514/824 , Y10S514/926 , Y10S514/927
摘要： The invention relates to a process for the preparation of novel 4-oxo-PGI.sub.2 derivatives of formula I ##STR1## where (a) compounds of formula III ##STR2## are oxidized, then the obtained 5-substituted-4-oxo-PGI.sub.1 derivatives of general formula II ##STR3## are eliminated by the splitting off of the W-H-molecule, or (b) the compounds of formula IV ##STR4## are reacted in a solvent in the presence of a catalyst with compounds of general formula V ##STR5## then the obtained compounds of formula I are transformed if desired by saponification, hydrolysis, salt formation, insertion of a protection group to another compound which belongs to the compounds of formula I, too.The pharmaceutical products of the invention can be used for the treatment of circulatory diseases, they inhibit the aggregation of blood plaques, dilate the bronchi and inhibit the secretion of gastric acid.
摘要翻译：本发明涉及一种制备式I（I）的新型4-氧代-GII 2衍生物的方法，其中（a）式III的化合物（XIIIX）被氧化，然后得到5-取代的通过分解WH分子来消除通式II（XIIX）的4-氧代-PGI1衍生物，或（b）式IV化合物（XIVX）在溶剂中在然后如果需要，通过皂化，水解，形成盐，将保护基团插入另一种属于式（I）化合物的化合物的化合物，转化所得到的式I化合物，我也。本发明的药物可用于治疗循环系统疾病，抑制血斑聚集，扩张支气管，抑制胃酸分泌。

2. 发明授权

US4451483A 2,3,4-Trinor-m-inter-phenylene-prostaglandin derivatives and compositions and method for inhibiting blood platelet aggregation 失效
标题翻译： 2,3,4-三硝基间亚苯基前列腺素衍生物及其抑制血小板聚集的组合物和方法
公开(公告)号：US4451483A
公开(公告)日：1984-05-29
申请号：US367068
申请日：1982-04-09
申请人： Istvan Szekely , Krisztina Kekesi , Mariann Lovasz nee Gaspar , Sandor Botar , Pal Hadhazy , Istvan Rakoczi , Laszlo Muszbek , Judit Skopal , Istvan Stadler , Karoly Horvath , Gabor Kovacs , Peter Kormoczy
发明人： Istvan Szekely , Krisztina Kekesi , Mariann Lovasz nee Gaspar , Sandor Botar , Pal Hadhazy , Istvan Rakoczi , Laszlo Muszbek , Judit Skopal , Istvan Stadler , Karoly Horvath , Gabor Kovacs , Peter Kormoczy
IPC分类号： A61K31/5575 , C07C405/00 , C07D307/937 , A61K31/34 , C07D307/935
CPC分类号： C07D307/937 , C07C405/00 , C07C405/0041 , Y10S514/822
摘要： 2,3,4-trinor-1,5-inter-m-phenylene-prostacycline derivatives of the formula (I), ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1-4 alkyl group, an alkali metal cation or a primary, secondary, tertiary or quaternary ammonium cation,R.sup.2 and R.sup.3 each represent hydrogen or a C.sub.1-4 alkanoyl, benzoyl, substituted benzoyl, tetrahydropyranyl, ethoxyethyl or tri-(C.sub.1-4 alkyl)-silyl group,R.sup.4 is hydrogen or a C.sub.1-4 alkyl group, andR.sup.5 is a hexyl, heptyl, phenoxymethyl or m-trifluoromethylphenoxymethyl group, orR.sup.5 represents a group of the general formula ##STR2## and in this latter formula Z is an amino group or an optionally halo-substituted C.sub.1-4 alkanoylamino, benzoylamino or tosylamino group, andR.sup.6 is a C.sub.4-6 alkyl, phenyl or benzyl group,are prepared by reacting a bicyclic lactol of the formula (II), ##STR3## with a reactive phosphorane prepared from a triphenyl-m-carbobenzylphosphonium halide and a strong base, optionally esterifying the resulting prostaglandin derivative and, whenever it contains a free amino group, protecting this amino group by acylation, reacting then the prostaglandin derivative with an electrophilic reagent of the formula E-X, wherein X is halogen atom and E is halogen atom or an acetyl, trifluoroacetyl or N-succinimido group, and subjecting the resulting halogenated PGI.sub.1 derivative to hydrogen halide elimination. The compounds of the formula (I) possess valuable biological effects and can be applied in therapy primarily as blood platelet aggregation inhibiting agents.
摘要翻译：式（I）的2,3,4-三硝基-1,5-间 - 间 - 亚苯基 - 前列环素衍生物，其中R 1是氢，C 1-4烷基，碱金属阳离子或伯，仲，叔或季铵阳离子，R2和R3各自表示氢或C1-4烷酰基，苯甲酰基，取代的苯甲酰基，四氢吡喃基，乙氧基乙基或三（C1-4烷基） - 甲硅烷基，R4是氢或 C 1-4烷基，R 5为己基，庚基，苯氧基甲基或间三氟甲基苯氧基甲基，或R 5表示通式“IMAGE”的基团，在后一式中Z为氨基或任意卤素取代的C1 -4烷酰基氨基，苯甲酰氨基或甲苯磺酰氨基，R6是C4-6烷基，苯基或苄基，是通过使式（II）的双环内酰醇与式（II）的双环内酰醇与由三苯基-m-苄基苄基卤化鏻和强碱，任选地酯化所得的前列腺素衍生物，并且每当其含有时游离氨基，通过酰化保护该氨基，然后将前列腺素衍生物与式EX的亲电试剂反应，其中X是卤素原子，E是卤素原子或乙酰基，三氟乙酰基或N-琥珀酰亚胺基，并使得到的卤化PGI1衍生物消除卤化氢。式（I）化合物具有有价值的生物学效应，可用作主要作为血小板聚集抑制剂的治疗。

3. 发明授权

US4565827A 7-Substituted PGI.sub.2 -derivatives and pharmaceutical compositions containing them 失效
标题翻译： 7-取代的PGI2-衍生物和含有它们的药物组合物
公开(公告)号：US4565827A
公开(公告)日：1986-01-21
申请号：US315408
申请日：1981-10-27
申请人： Istvan Szekely , Marianna Lovasz nee Gaspar , Gabor Kovacs , Krisztina Kekesi , Sandor Botar , Karoly Horvath , Peter Kormoczy , Pal Hadhazy , Istvan Rakoczy , Laszlo Fesus
发明人： Istvan Szekely , Marianna Lovasz nee Gaspar , Gabor Kovacs , Krisztina Kekesi , Sandor Botar , Karoly Horvath , Peter Kormoczy , Pal Hadhazy , Istvan Rakoczy , Laszlo Fesus
IPC分类号： C07C405/00 , C07D307/937 , C07D307/935 , A61K31/34 , A61K31/557
CPC分类号： C07D307/937 , C07C405/00
摘要： The invention relates to new, 7-substituted PGI.sub.2 -derivatives of formula (I) ##STR1## The new compounds have valuable therapeutical properties, and in particular show prostacyclin-like effects.
摘要翻译：本发明涉及式（I）的新的7-取代的PGI 2衍生物。（I）新化合物具有有价值的治疗特性，特别是显示前列环素样效应。

4. 发明授权

US4425358A 13-Thia-prostacycline derivatives 失效
标题翻译： 13-前列环素衍生物
公开(公告)号：US4425358A
公开(公告)日：1984-01-10
申请号：US370503
申请日：1982-04-21
申请人： Csaba Szantay , Lajos Novak , Jozsef Aszodi , Vilmos Simonidesz , Geza Galambos , Gabor Kovacs , Sandor Virag , Istvan Stadler , Peter Kormoczy
发明人： Csaba Szantay , Lajos Novak , Jozsef Aszodi , Vilmos Simonidesz , Geza Galambos , Gabor Kovacs , Sandor Virag , Istvan Stadler , Peter Kormoczy
IPC分类号： C07D307/935 , A61K31/557 , A61P7/02 , A61P9/12 , C07C405/00 , C07D307/937 , C07D407/12
CPC分类号： C07D307/937 , C07C405/0033 , C07D407/12 , Y10S514/822
摘要： The invention relates to new optically active or racemic 13-thia-prostacycline derivatives of the Formula I ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation or a straight or branched chain alkyl group having 1-5 carbon atoms;R.sup.2 is straight or branched chain alkyl having 4-9 carbon atoms or monosubstituted phenoxymethyl;--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- of Z-- or E-- configuration or --C.tbd.C--;one of the symbols X and Y is hydrogen, methyl or ethyl and the other is hydroxy, tetrahydropyranyoxy, 1-ethoxy-ethoxy or trialkylsilyloxy; orX and Y together form a --O--CH.sub.2 --CH.sub.2 --O-- group;Z is a sulfur atom or a --SO-- group.The compounds of the Formula I can be prepared by reacting a 13-thia-prostaglandine of the Formula III ##STR2## if desired after oxidation into the corresponding 13-oxide derivative--with a halogenating agent; and treating the 5-halogeno-13-thia-prostacycline of the Formula II ##STR3## thus obtained wherein E is halogen with an organic or inorganic base; and thereafter if desired removing the protecting groups X and/or Y and if desired converting a compound of the Formula I obtained into a salt or setting free the same from a salt. The new compounds of the Formula I possess anti-coagulant and hypotensive properties and can be used in therapy.
摘要翻译：本发明涉及式I的新的光学活性或外消旋的13-前列环素衍生物，其中R1是氢，可药用阳离子或具有1-5个碳原子的直链或支链烷基; R2是具有4-9个碳原子的直链或支链烷基或单取代的苯氧基甲基; -A-B-是Z-或E-构型的-CH 2 -CH 2 - ， - CH = CH-或-C 3 D C-; 符号X和Y之一是氢，甲基或乙基，另一个是羟基，四氢吡喃基氧基，1-乙氧基 - 乙氧基或三烷基甲硅烷氧基; 或X和Y一起形成-O-CH 2 -CH 2 -O-基团; Z是硫原子或-SO-基。式I的化合物可以通过使式III的13-前 - 前列腺素（III）反应来制备。

5. 发明授权

US4379164A Vasodilative 4-thia-PGI.sub.1 and 4-sulfinyl-PGI.sub.1 and derivatives thereof 失效
标题翻译：血管扩张型4-thia-PGI1和4-亚磺酰基-PGI1及其衍生物
公开(公告)号：US4379164A
公开(公告)日：1983-04-05
申请号：US314433
申请日：1981-10-23
申请人： Istvan Tomoskozi , Peter Gyory , Gabor Kovacs , Sandor Virag , Peter Kormoczy , Istvan Stadler
发明人： Istvan Tomoskozi , Peter Gyory , Gabor Kovacs , Sandor Virag , Peter Kormoczy , Istvan Stadler
IPC分类号： C07D307/935 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P9/08 , A61P11/08 , C07C405/00 , C07D307/937 , A61K31/335
CPC分类号： C07D307/937
摘要： A compound having vasodilative, bronchodilative, stomach-mucosa-protective and platelet-aggregation-inhibiting activity has the formulaA 4-thia- or 4-sulfinyl-PGI.sub.1 -compound of the formula I ##STR1## wherein Q stands for --S-- or --SO--,A stands for C.sub.1-6 straight or branched chain alkylene,B stands for ethylene, vinylene or ethinylene,R.sup.1 represents hydrogen or C.sub.1-4 alkyl,R.sup.2 represents C.sub.1-8 straight or branched chain alkyl or mono-substituted aryl-oxy-methyl,R.sup.3 stands for hydrogen or acetyl, andZ represents --COOH, --CN, --CH.sub.2 OH or --COOW, wherein W stands for an equivalent of a pharmacologically acceptable cation or C.sub.1-4 alkyl.
摘要翻译：具有血管扩张性，支气管扩张性，胃粘膜保护性和血小板聚集抑制活性的化合物具有式I的4-硫杂或4-亚磺酰基-GlyI化合物，其中Q代表 - S-或-SO-，A代表C 1-6直链或支链亚烷基，B代表亚乙基，亚乙烯基或亚乙烯基，R 1代表氢或C 1-4烷基，R 2代表C1-8直链或支链烷基或单 - 取代的芳氧基 - 甲基，R3代表氢或乙酰基，Z代表-COOH，-CN，-CH2OH或-COOW，其中W代表药理学上可接受的阳离子或C 1-4烷基的当量。

6. 发明授权

US4735965A 7-oxo-PGI.sub.2 -ephedrine salts and their pharmaceutical compositions and methods 失效
标题翻译： 7-氧代-PGI2-麻黄碱盐及其药物组合物和方法
公开(公告)号：US4735965A
公开(公告)日：1988-04-05
申请号：US868772
申请日：1986-05-28
申请人： Gabor Kovacs , Geza Galambos , Istvan Tomoskozi , Karoly Kanai , Peter Gyory , Peter Kormoczy , Istvan Stadler , Laszlo Szekeres , Gyula Papp , Eva Udvary , Pal Hadhazy , Jeno Marton , Gyorgy Dorman
发明人： Gabor Kovacs , Geza Galambos , Istvan Tomoskozi , Karoly Kanai , Peter Gyory , Peter Kormoczy , Istvan Stadler , Laszlo Szekeres , Gyula Papp , Eva Udvary , Pal Hadhazy , Jeno Marton , Gyorgy Dorman
IPC分类号： C07C59/90 , A61K31/135 , A61K31/19 , A61K31/34 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P1/16 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P35/00 , A61P43/00 , C07C51/00 , C07C51/41 , C07C67/00 , C07C213/00 , C07C215/40 , C07C405/00 , C07D307/935 , C07D307/937 , C07D521/00
CPC分类号： C07D307/937
摘要： The invention relates to new 7-oxo-PGI.sub.2 -ephedrine salt analogues of the Formula I ##STR1## wherein A stands for --(CH.sub.2).sub.2 --, cis or trans --CH.dbd.CH-- or --C.tbd.C--;R.sup.1 is lower alkyl or hydrogen;B represents a chemical bond, --CH.sub.2 -- or --CR.sup.2 R.sup.3 ;R.sup.2 stands for lower alkyl or hydrogen;R.sup.3 represents lower alkyl or hydrogen;X is a chemical bond, --O-- or --CH.sub.2 --;R.sup.4 stands for C.sub.1-6 alkyl, C.sub.4-7 cycloalkyl, C.sub.1-6 fluoroalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenyl, substituted phenyl or heteroaryl.The salts of the Formula I show the same pharmacological profile as the sodium salt of PGI.sub.2, they inhibit blood aggregation and the secretion of gastric acid, are useful in the prevention of anginal attacks. Accordingly the salts of the present invention are useful in the prevention of peripheral vascular diseases, in improving circulation of extremities, in relieving the seriousness of cardiac infarction and also in the treatment and prevention of gastrointestinal ulcer and acute or chronical liver injury.
摘要翻译：本发明涉及式I的新的7-氧代-PGI-麻黄碱盐类似物，其中A代表 - （CH 2）2 - ，顺式或反式-CH = CH-或-C 3位C; R1是低级烷基或氢; B表示化学键，-CH 2 - 或-CR 2 R 3; R2代表低级烷基或氢; R3表示低级烷基或氢; X是化学键，-O-或-CH2-; R4代表C 1-6烷基，C 4-7环烷基，C 1-6氟代烷基，C 2-6烯基，C 2-6炔基，苯基，取代的苯基或杂芳基。式I的盐显示与PGI2的钠盐相同的药理学特征，它们抑制血液聚集和胃酸分泌，可用于预防心绞痛发作。因此，本发明的盐可用于预防周围血管疾病，改善四肢的循环，缓解心肌梗死的严重性，以及治疗和预防胃肠溃疡和急性或慢性肝损伤。

7. 发明授权

US4840949A Oxadiazole-alkyl-purine derivatives useful as antitussive agents 失效
标题翻译：用作镇咳剂的恶二唑 - 烷基嘌呤衍生物
公开(公告)号：US4840949A
公开(公告)日：1989-06-20
申请号：US107693
申请日：1987-10-09
申请人： Dezso Korbonits , Emil Minker , Zoltan Vargai , Gergely Heja , Gabor Kovacs , Agnes Gottsegen , Sandor Antus , Sandor Virag , Andrea Bolehovszky , Jeno Marton , Katalin Marmarosi nee Kellner , Lorand Debreczeni , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Gabor Horvath
发明人： Dezso Korbonits , Emil Minker , Zoltan Vargai , Gergely Heja , Gabor Kovacs , Agnes Gottsegen , Sandor Antus , Sandor Virag , Andrea Bolehovszky , Jeno Marton , Katalin Marmarosi nee Kellner , Lorand Debreczeni , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Gabor Horvath
IPC分类号： C07D473/04 , A61K31/52 , A61K31/522 , A61P11/04 , A61P11/14 , C07D271/06 , C07D273/02 , C07D473/06
CPC分类号： C07D473/06
摘要： The invention relates to new oxidiazole-alkyl-purine-derivatives of the Formula I ##STR1## and pharmaceutically acceptable salts thereof wherein A stands for C.sub.1-4 alkylene andR.sup.1 represents C.sub.1-6 alkyl, hydroxyalkyl, halogenoalkyl, carboxyalkyl, C.sub.5-6 cycloalkyl or aminoalkyl of the Formula --(CH.sub.2).sub.n --NR.sup.2 R.sup.3 in which group n is an integer 1-3; R.sup.2 and R.sup.3 each stand for hydrogen or C.sub.1-4 alkyl or together with the adjacent nitrogen atom they are attached to form a 5- or 6-membered nitrogen containing heterocyclic ring which may optionally comprise a further nitrogen atom or an oxygen atom as heteroatom; orR.sup.1 stands for phenyl, hydroxyphenyl, carboxyphenyl, benzyl or dimethoxybenzylThe compounds of the Formula I can be prepared by methods known per se and can be used in therapy as antitussive agents.
摘要翻译：本发明涉及式I的新型氧化噻唑烷基嘌呤衍生物及其药学上可接受的盐，其中A代表C1-4亚烷基，R1代表C1-6烷基，羟基烷基，卤代烷基，羧基烷基，C5-6环烷基或其中基团n为整数1-3的式 - （CH 2）n -NR 2 R 3的氨基烷基; R 2和R 3各自代表氢或C 1-4烷基或与它们相连的相邻氮原子一起形成5-或6-元含氮杂环，其可以任选地包含另外的氮原子或氧原子作为杂原子; 或R 1代表苯基，羟基苯基，羧基苯基，苄基或二甲氧基苄基。式I化合物可以通过本身已知的方法制备，并且可用于作为止咳剂的治疗。

8. 发明授权

US4988730A Diphenkylpropylamines for the therapy of heart disease 失效
标题翻译：用于治疗心脏病的二苯基丙胺
公开(公告)号：US4988730A
公开(公告)日：1991-01-29
申请号：US385539
申请日：1989-07-21
申请人： Dezso Korbonits , Pal Kiss , Laszlo Szekeres , Gyula Papp , Gabor Kovacs , Andrea Santane Csutor , Sandor Virag , Eva Udvari , Imre Bata , Katalin Marmarosi nee Kellner , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Zoltan Vargai
发明人： Dezso Korbonits , Pal Kiss , Laszlo Szekeres , Gyula Papp , Gabor Kovacs , Andrea Santane Csutor , Sandor Virag , Eva Udvari , Imre Bata , Katalin Marmarosi nee Kellner , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Zoltan Vargai
IPC分类号： C07C215/50 , A61K31/13 , A61K31/135 , A61K31/137 , A61K31/16 , A61K31/165 , A61K31/335 , A61K31/36 , A61P3/00 , A61P9/06 , A61P9/08 , A61P9/10 , C07C20060101 , C07C27/00 , C07C67/00 , C07C209/00 , C07C209/08 , C07C209/24 , C07C209/26 , C07C209/62 , C07C209/68 , C07C211/00 , C07C211/03 , C07C211/16 , C07C211/26 , C07C211/27 , C07C211/29 , C07C211/43 , C07C213/00 , C07C217/10 , C07C217/54 , C07C217/56 , C07C217/58 , C07C227/10 , C07C227/16 , C07C229/34 , C07C229/38 , C07C231/00 , C07C231/12 , C07C233/42 , C07C233/43 , C07C233/67 , C07D311/48 , C07D317/00 , C07D317/48 , C07D317/58
CPC分类号： C07D317/58 , C07C211/27 , C07C211/29 , C07C217/58 , C07C233/43
摘要： The invention relates to novel diphenylpropylamine derivatives of the general formula (I). ##STR1## R.sup.1 stands for hydrogen or a methyl group; R.sup.2 stands for hydrogen, a methyl or n-decyl group;Z means a phenyl group substituted by R.sup.3, R.sup.4 and R.sup.5, whereinR.sup.3 means hydrogen, fluorine, chlorine or bromine, or a nitro, C.sub.1-12 alkyl, C.sub.1-4 alkoxy, phenoxy or benzyloxy group;R.sup.4 and R.sup.5 represent hydrogen, chlorine or a hydroxy, alkoxy, benzyloxy, acetamino or carboxy group; orR.sup.4 and R.sup.5 together form a methylendioxy group; orZ may stand for a 4-methoxynaphtyl or 4-ethoxy-naphthyl group; andR.sup.6 stands for hydrogen or fluorine, with the proviso that each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 cannot simultaneously stand for hydrogen, as well as their physiologically acceptable acid addition salts.The invention also relates to a process for the preparation of these compounds and to the pharmaceutical compositions containing these compounds.The compounds of the general formula (I) can preferably be used for the treatment of cardiovascular diseases.
摘要翻译：本发明涉及通式（I）的新型二苯基丙胺衍生物。（I）R1代表氢或甲基; R2代表氢，甲基或正癸基; Z表示被R 3，R 4和R 5取代的苯基，其中R 3表示氢，氟，氯或溴，或硝基，C 1-12烷基，C 1-4烷氧基，苯氧基或苄氧基; R4和R5代表氢，氯或羟基，烷氧基，苄氧基，乙酰氨基或羧基; 或R4和R5一起形成甲基二氧基; 或Z可以代表4-甲氧基萘基或4-乙氧基 - 萘基; 并且R6代表氢或氟，条件是R1，R2，R3，R4和R6各自不能同时代表氢，以及它们的生理上可接受的酸加成盐。本发明还涉及制备这些化合物的方法和含有这些化合物的药物组合物。通式（I）的化合物可优选用于治疗心血管疾病。

9. 发明授权

US5589513A Pharmaceutical composition and process for the preparation thereof 失效
标题翻译：药物组合物及其制备方法
公开(公告)号：US5589513A
公开(公告)日：1996-12-31
申请号：US256128
申请日：1994-06-17
申请人： Kalman Magyar , Jozsef Gaal , Istvan Sziraki , Jozsef Lengyel , Anna Z. Szabo , Katalin Marmarosi , Istvan Hermecz , Istvan Szatmari , Zoltan Torok , Peter Kormoczy
发明人： Kalman Magyar , Jozsef Gaal , Istvan Sziraki , Jozsef Lengyel , Anna Z. Szabo , Katalin Marmarosi , Istvan Hermecz , Istvan Szatmari , Zoltan Torok , Peter Kormoczy
IPC分类号： A61K45/00 , A61K20060101 , A61K31/135 , A61K31/137 , A61K45/06 , A61P25/24 , A61P25/26 , A61P25/28 , C07C43/00 , C07C205/00 , C07C217/00 , A01N33/02
CPC分类号： A61K31/135
摘要： The invention relates to two phase pharmaceutical compositions comprising as active ingredient a MAO inhibitor and an uptake inhibitor together with usual pharmaceutical auxiliaries. The compositions can be used for the treatment of neurodegenerative diseases. As active ingredient optionally N-(1-phenyl-isopropyl)-N-methyl-propinylamine or N-(4-fluoro-phenyl)-isoprop-1-yl-N-methyl-propinylamine or their salts, optically active isomers or metabolites are used both as MAO inhibitor and as uptake inhibitor.
摘要翻译： PCT No.PCT / HU92 / 00060 Sec。 371日期：1994年6月17日 102（e）日期1994年6月17日PCT提交1992年12月18日PCT公布。公开号WO93 / 12775 PCT 日期：1993年7月8日本发明涉及包含作为活性成分的MAO抑制剂和吸收抑制剂以及通常的药物助剂的两相药物组合物。该组合物可用于治疗神经变性疾病。作为活性成分，任选地N-（1-苯基 - 异丙基）-N-甲基 - 丙烯胺或N-（4-氟 - 苯基） - 异丙基-1-基-N-甲基 - 丙基胺或其盐，旋光异构体或代谢物被用作MAO抑制剂和摄取抑制剂。

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