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56 条记录 (耗时 0.191 秒)

    Derivatives of bicyclic lactols
    1.
    发明授权
    Derivatives of bicyclic lactols 失效
    双环乳糖的衍生物

    公开(公告)号：US4257962A

    公开(公告)日：1981-03-24

    申请号：US942819

    申请日：1978-09-15

    申请人： Tibor Szabo ,  Laszlo Institoris ,  Gabor Kovacs ,  Gyula Dalmadi ,  Bela Koszegi ,  Istvan Stadler

    发明人： Tibor Szabo ,  Laszlo Institoris ,  Gabor Kovacs ,  Gyula Dalmadi ,  Bela Koszegi ,  Istvan Stadler

    IPC分类号： C07C405/00 ,  A61K31/34 ,  A61K31/343 ,  A61P7/02 ,  A61P25/02 ,  A61P35/00 ,  C07D307/935

    CPC分类号： C07D307/935

    摘要： Racemic or optically active compounds with antitumor activity of the formula: ##STR1## wherein X is oxygen or sulfur;R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkanoyl, benzoyl or phenyl-substituted benzoyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkanoyl;R.sup.3 is C.sub.2 to C.sub.40 straight or branched chain alkyl substituted by hydroxy, epoxy, amino, C.sub.1 to C.sub.6 alkylamino, C.sub.1 to C.sub.6 dialkylamino, C.sub.1 to C.sub.6 alkanoyloxy or, C.sub.1 to C.sub.4 alkoxycarbonyl; cyclohexyl, phenyl unsubstituted or substituted by halogen, amino, C.sub.1 to C.sub.4 alkyl-substituted amino, C.sub.1 to C.sub.4 alkoxy, nitro, or hydroxy; C.sub.1 to C.sub.6 alkanoyl; allyl or phenyl-C.sub.1 to C.sub.4 alkyl unsubstituted or substituted by a C.sub.2 to C.sub.6 alkene group; or where X is sulfur R.sup.3 is as defined above or is C.sub.1 to C.sub.40 straight or branched chain alkyl; and.about. represents the exo- or endo-steric position in the ring and indicates an .alpha.- or .beta.-steric position in the side chain are disclosed.

    摘要翻译： 具有下式的抗肿瘤活性的外消旋或光学活性化合物：其中X是氧或硫; R1是氢，C1至C4烷酰基，苯甲酰基或苯基取代的苯甲酰基; R2是氢或C1-C4烷酰基; R3为C2至C40被羟基，环氧基，氨基，C1至C6烷基氨基，C1至C6二烷基氨基，C1至C6烷酰氧基或C1至C4烷氧基羰基取代的直链或支链烷基; 环己基，未取代或被卤素取代的苯基，氨基，C1至C4烷基取代的氨基，C1至C4烷氧基，硝基或羟基; C1至C6烷酰基; 烯丙基或未被取代或被C2至C6烯基取代的苯基-C1至C4烷基; 或其中X为硫的R 3如上所定义或为C 1至C 40直链或支链烷基; 而DIFFERENCE表示环中的外 - 或内 - 立体位置，并且表示侧链中的α或β-甾族位置。

    2,3,4-Trinor-m-inter-phenylene-prostaglandin derivatives and compositions and method for inhibiting blood platelet aggregation
    6.
    发明授权
    2,3,4-Trinor-m-inter-phenylene-prostaglandin derivatives and compositions and method for inhibiting blood platelet aggregation 失效
    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。

    13-Thia-prostacycline derivatives
    7.
    发明授权
    13-Thia-prostacycline derivatives 失效
    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。

    Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use
    8.
    发明授权
    Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use 失效
    含硫异喹啉衍生物在药物组合物和使用方法中的应用

    公开(公告)号：US4425349A

    公开(公告)日：1984-01-10

    申请号：US381775

    申请日：1982-05-25

    申请人： Kalman Takacs ,  Maria H. Papp ,  Gabor Kovacs ,  Ilona K. Ajzert ,  Antal Simay ,  Peter Literati Nagy ,  Marian E. Puskas ,  Gyula Sebestyen ,  Istvan Stadler ,  Zoltan Sumeghy

    发明人： Kalman Takacs ,  Maria H. Papp ,  Gabor Kovacs ,  Ilona K. Ajzert ,  Antal Simay ,  Peter Literati Nagy ,  Marian E. Puskas ,  Gyula Sebestyen ,  Istvan Stadler ,  Zoltan Sumeghy

    IPC分类号： C07D217/14 ,  C07D513/04 ,  A61K31/47

    CPC分类号： C07D513/04 ,  C07D217/14 ,  Y10S514/826 ,  Y10S514/869

    摘要： The invention concerns new sulfur-containing isoquinoline derivatives. More particularly, the invention relates to isoquinoline derivatives of the general formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbamoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.2 is a straight or branched chained alkylene group having 1 to 6 carbon atoms, andthe dotted line stands for a further carbon-carbon bond or hydrogen atoms in the 3- and 4-positions of the ring,and salts and cyclic amides thereof.The new compounds possess valuable pharmaceutical activities, more particularly, are potent diuretic, antiasthmatic, hypotensive and antiinflammatory agents. Thus another aspect of the invention is a pharmaceutical composition which comprises as active ingredient a pharmaceutically effective amount of at least one compound of the general formula (I) with at least one pharmaceutically inert carrier or diluent. The invention also relates to a process for preparing these compounds.

    摘要翻译： 本发明涉及新的含硫异喹啉衍生物。 更具体地说，本发明涉及通式（I）的异喹啉衍生物，其中R独立地表示氢，羟基或具有1至4个碳原子的烷氧基，R 1是氢，具有1至4个碳原子的烷基和 任选地被苯基取代，任选被一个或多个卤素或烷氧基取代的苯基，氰基或氨基甲酰基，R 2是任选被一个或多个卤素，烷氧基或羧基取代的苯基或通式A的基团，其中R 3是 氢，具有1至4个碳原子的直链或支链烷基或苯基，m和n独立地表示0,1或2，条件是m + n至少为1，R4为氢，苯基，羟基，酰氧基， 羧基，具有1至6个碳原子的烷氧基羰基，在烷基部分含有1至6个碳原子的氨基甲酰基，咔唑基或二烷基氨基，或者是具有1至6个碳原子的直链或支链的亚烷基，虚线代表 进一步c 环的3-和4-位的碳 - 碳键或氢原子，及其盐和环状酰胺。 新化合物具有有价值的药物活性，特别是有效的利尿，止喘，降压和抗炎药。 因此，本发明的另一方面是药物组合物，其包含作为活性成分的药学有效量的至少一种通式（I）的化合物与至少一种药学上惰性的载体或稀释剂。 本发明还涉及制备这些化合物的方法。