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    • 2. 发明授权
    • Antiphlogistic and anticoagulant condensed pyrimidine derivatives
    • 消炎和抗凝血嘧啶衍生物
    • US4460771A
    • 1984-07-17
    • US742464
    • 1976-11-17
    • Zoltan MeszarosJozsef KnollPeter SzentmiklosiIstvan HermesAgnes HorvathSandor ViragLelle Vasvari nee DebreczyAgoston David
    • Zoltan MeszarosJozsef KnollPeter SzentmiklosiIstvan HermesAgnes HorvathSandor ViragLelle Vasvari nee DebreczyAgoston David
    • A61K31/505A61K31/519A61P7/02A61P25/04A61P29/00A61P43/00C07D471/04
    • C07D471/04
    • New optionally racemic or optically active pyrimido(1,2a) heterocyclic compounds of the formula ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is an alkyl group containing one to six carbon atoms,R.sup.1 is hydrogen, alkyl containing one to six carbon atoms,R.sup.2 is hydrogen, alkyl containing one to six carbon atoms, optionally substituted amino, optionally substituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sup.1 and R.sup.2 together form a --(CH.dbd.CH).sub.2 -- group attached to the two adjacent carbon atoms of the ring A and the broken line represents a chemical bond,R.sup.3 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl or optionally substituted hydroxy,R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl orR.sup.3 and R.sup.4 together with the nitrogen can form an optionally substituted five-, six- or seven-membered ring, which can contain a further heteroatom or heteroatoms,R.sup.5 is oxygen or an optionally substituted imino group are disclosed as well as a process for the preparation thereof.
    • 新的任选的外消旋或光学活性嘧啶(1,2a)杂环化合物,其中m为0,1或2,n为0,1或2,R为含有1至6个碳原子的烷基,R 1为 是氢,含有1至6个碳原子的烷基,R 2是氢,含1至6个碳原子的烷基,任选取代的氨基,任选取代的羟基,羧基或衍生自羧酸的基团或R 1和R 2一起形成 - (CH = CH)连接到环A的两个相邻碳原子上的2-基团,虚线表示化学键,R 3是氢,任选取代的烷基,任选取代的芳基,任选取代的芳烷基,任选取代的杂环,任选取代的环烷基, 任选取代的酰基或任选取代的羟基,R 4是氢,任选取代的烷基,任选取代的芳基,任选取代的芳烷基,任选取代的杂环,任选取代的环烷基,选择 可以将氮取代的酰基或R3和R4与氮一起形成任选取代的五元,六元或七元环,其可以含有另外的杂原子或杂原子,R5是氧或任选取代的亚氨基, 其制备方法。
    • 3. 发明授权
    • Synergistic antimicrobial compositions
    • 协同抗菌组合物
    • US4404189A
    • 1983-09-13
    • US226615
    • 1981-01-21
    • Gabor KulcsarGyula SebestyenAgoston DavidTibor Zilahi
    • Gabor KulcsarGyula SebestyenAgoston DavidTibor Zilahi
    • A61K31/65A61K35/00
    • A61K31/70A61K31/65
    • A synergistic antimicrobial active ingredient for a pharmaceutical or veterinary composition comprises 5 to 50 percent by weight of a primycin component which consists of a primycin fermentation product of Thermonospora galeriensis and 95 to 50 percent by weight of at least one other component selected from the group which consists of doxycyline compounds and sisomicin compounds. The doxycycline compounds are selected from the group which consists of doxycycline, salts thereof with mineral acids, and doxycycline tryclate. The sisomicin compounds are selected from the group which consists of sisomicin, substituted sisomicins with substitution at the N atom by lower alkyl, hydroxyl lower alkyl, lower aminoalkyl and lower alkanoyl, and sisomicin acid salts.
    • 用于药物或兽医组合物的协同抗微生物活性成分包含5-50重量%的伯霉素组分,所述伯霉素组分由热霉菌属(Thermomonospora galeriensis)的伯霉素发酵产物和95至50重量%的至少一种选自以下的组中 由多西环素化合物和西索米星化合物组成。 多西环素化合物选自由多西环素,其与无机酸的盐和多西环素三环酸组成的组。 西索米星化合物选自西索霉素,在N原子被低级烷基取代的取代的西索米星,羟基低级烷基,低级氨基烷基和低级烷酰基以及西索米星酸盐组成的组。
    • 5. 发明授权
    • Process for the preparation of benzo(a)quinolizidine derivatives
    • 苯并(a)喹嗪衍生物的制备方法
    • US4102886A
    • 1978-07-25
    • US624470
    • 1975-10-21
    • Csaba SzantayLajos SzaboLaszlo TokeIstvan TothSandor ViragErzsebet KanyoAgoston David
    • Csaba SzantayLajos SzaboLaszlo TokeIstvan TothSandor ViragErzsebet KanyoAgoston David
    • C07D455/06C07D491/056C07D491/14
    • C07D491/14C07D455/06
    • A process for the preparation of a compound of the formula I or a salt thereof ##STR1## wherein R.sup.1 and R.sup.2 each represent hydrogen or a C.sub.1-4 alkoxy group, or together form a methylenedioxy group;R.sup.3, r.sup.4, r.sup.5 and R.sup.6 are the same or different and are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n --R.sup.7 with the proviso that at least one of the members R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen; R.sup.7 is carboxyl or a carboxylic acid derivative group;N = 0.1 or 2 which comprises reacting a compound of the formula II ##STR2## with an organic secondary amine and reacting the N-amine of the formula III ##STR3## thus obtained wherein R.sup.8 and R.sup.9 each represent a C.sub.1-5 alkyl group, or together with the adjacent nitrogen atom form a 5- or 6-membered heterocyclic ring which can contain a further heteroatom, with a compound of the formula IVch.sub.2 .dbd. ch -- (ch.sub.2).sub.n -- R.sup.10 (IV)wherein R.sup.10 is a cyano or alkoxycarbonyl group.
    • 一种制备式I化合物或其盐的方法,其中R 1和R 2各自代表氢或C 1-4烷氧基,或一起形成亚甲二氧基; R 3,R 4,R 5和R 6相同或不同,为氢或式-CH 2 - (CH 2)n -R 7的基团,条件是至少有一个R 3,R 4,R 5和R 6不是 氢; R7是羧基或羧酸衍生物基团; N = 0.1或2,其包含用有机仲胺反应式II化合物,并使由此得到的式III的N-胺反应,其中R 8和R 9各自表示C 1-5烷基, 或者与相邻的氮原子一起形成可以含有另外的杂原子的5或6元杂环与式IV的化合物CH2 = CH-(CH2)n-R10(IV),其中R10是氰基或 烷氧基羰基。