Schistosomicidal acridanone hydrazones
    1.
    发明授权
    Schistosomicidal acridanone hydrazones 失效
    血吸虫吖啶酮腙

    公开(公告)号:US4544659A

    公开(公告)日:1985-10-01

    申请号:US551816

    申请日:1983-11-15

    摘要: Acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro, R.sup.2 is hydrogen or lower alkyl, one of the substituents R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond and R.sup.5 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower alkyl substituted by halogen or lower alkoxy,and pharmaceutically acceptable acid addition salts thereof, processes for their preparation and pharmaceutical compositions based thereon, are described. The compounds of formula I are useful as schistosomicidal agents.

    摘要翻译: 式Ⅰ的吖啶酮衍生物,其中虚线是任选键,R 1是氢,卤素或硝基,R 2是氢或低级烷基,取代基R 3和R 4之一是氢或低级烷基,另一个与 R是另外的键,R5是氢,低级烷基,低级烯基,低级炔基或被卤素或低级烷氧基取代的低级烷基,及其药学上可接受的酸加成盐,其制备方法和基于此的药物组合物。 式I的化合物可用作血吸虫病剂。

    Schistosomicidal acridanone hydrazones
    2.
    发明授权
    Schistosomicidal acridanone hydrazones 失效
    血吸虫吖啶酮腙

    公开(公告)号:US4711889A

    公开(公告)日:1987-12-08

    申请号:US887580

    申请日:1986-07-18

    CPC分类号: C07D417/12 C07D417/14

    摘要: The invention relates to acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro,R.sup.2 is hydrogen or lower alkyl,one of R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond,A is lower alkylene,R.sup.5 is a 5-membered nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or the group ##STR2## the symbol is a 5- or 6-membered, optionally lower alkyl-substituted saturated heterocycle which can contain as a ring member oxygen or sulfur or the group >NH or >N(B).sub.n --A.sup.1 --R.sup.6, B is the group --CO--, --COO-- or --SO.sub.2 --, n is the number 0 or 1, A.sup.1 is lower alkylene, R.sup.6 is hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R.sup.7 is hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts thereof, their preparation and pharmaceutical compositions based thereon.

    摘要翻译: 本发明涉及下式吖啶酮衍生物,其中虚线是任选的键,R 1是氢,卤素或硝基,R 2是氢或低级烷基,R 3和R 4之一是氢或低级烷基,而另一个 与R一起是另外的键,A是低级亚烷基,R5是5元含氮的,任选的低级烷基取代的芳族杂环,氨基或基团是5-或6- 可以包含作为环成员的氧或硫或NH>> N(B)n-Al-R 6的基团的任选的低级烷基取代的饱和杂环,B是基团-CO - , - COO-或-SO 2 - ,n为0或1,A1为低级亚烷基,R6为氢,氨基,低级烷基氨基或二(低级烷基)氨基,R7为氢或低级烷基,及其药学上可接受的酸加成盐, 基于此的组合物。

    Cephalosporin derivatives
    5.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号:US4292428A

    公开(公告)日:1981-09-29

    申请号:US51669

    申请日:1979-06-25

    CPC分类号: C07D501/36

    摘要: There is presented cephalosporin derivatives which are the readily hydrolysable esters and ethers of compounds of the general formula ##STR1## wherein R represents furyl, thienyl or phenyl optionally substituted by halogen, hydroxy, lower alkoxy or lower alkyl, R.sub.1 represents lower alkyl or aminocarbonylmethyl and X represents a group of the formula ##STR2## in which one of the two symbols R.sub.2 and R.sub.3 represents hydrogen and the other represents lower alkyl and R.sub.4 represents lower alkyl,as well as salts of said esters and ethers and hydrates of said esters, ethers and salts.

    摘要翻译: 提出了头孢菌素衍生物,它们是通式(I)化合物的易水解的酯和醚,其中R表示呋喃基,噻吩基或任选被卤素,羟基,低级烷氧基或低级烷基取代的苯基,R 1表示低级烷基 或氨基羰基甲基,X表示下式的基团:其中两个符号R2和R3之一表示氢,另一个表示低级烷基,R4表示低级烷基,以及所述酯的盐 所述酯,醚和盐的醚和水合物。

    Imidazole derivatives
    7.
    发明授权
    Imidazole derivatives 失效
    咪唑衍生物

    公开(公告)号:US4908363A

    公开(公告)日:1990-03-13

    申请号:US169207

    申请日:1988-03-15

    摘要: Imidazole derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2 each is lower alkyl, X is a residue of the formula ##STR2## R.sup.3 is hydrogen and R.sup.4 is hydrogen or lower alkyl or R.sup.3 and R.sup.4 taken together are an additional carbon-nitrogen bond; R.sup.5 is hydrogen or lower alkyl; R.sup.6 is hydrogen, lower alkyl, lower alkylthio or a residue of the formula --NR.sup.7 R.sup.8 ; and R.sup.7 and R.sup.8 each is lower alkyl or taken together with the nitrogen atom are a 5- or 6-membered saturated heterocycle; and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I possess valuable pharmacodynamic properties, especially inflammation-inhibiting and edema-inhibiting properties, so that they can be used for the control or prevention of illnesses, especially for the control or prevention of inflammations and edemas.

    摘要翻译: 式I的咪唑衍生物其中R 1和R 2各自为低级烷基,X为下式的残基R 3为氢,R 4为氢或低级烷基,或者R 3和R 4一起为另外的碳氮 键; R5是氢或低级烷基; R6是氢,低级烷基,低级烷硫基或式-NR7R8的残基; 并且R 7和R 8各自为低级烷基或与氮原子一起为5-或6-元饱和杂环; 及其药学上可接受的酸加成盐。 式I化合物具有有价值的药效学特性,特别是炎症抑制和水肿抑制性质,因此它们可用于控制或预防疾病,特别是用于控制或预防炎症和水肿。

    Cephalosporin derivatives
    9.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号:US4349672A

    公开(公告)日:1982-09-14

    申请号:US207163

    申请日:1980-11-17

    CPC分类号: C07D277/587

    摘要: There are presented cephalosporin derivatives of the formula ##STR1## wherein X is the group ##STR2## R is hydrogen or a readily hydrolyzable ester or ether group and n stands for 1 or 2,as well as salts of these compounds and hydrates of these compounds and salts.

    摘要翻译: 呈现下式的头孢菌素衍生物,其中X是基团R是氢或易水解的酯或醚基,n代表1或2,以及这些化合物和这些化合物的水合物的盐 化合物和盐。

    Thiazolylacelamide cephalosporins
    10.
    发明授权
    Thiazolylacelamide cephalosporins 失效
    噻唑立酰胺头孢菌素

    公开(公告)号:US4327210A

    公开(公告)日:1982-04-27

    申请号:US963255

    申请日:1978-11-24

    CPC分类号: C07D501/36 Y02P20/55

    摘要: Acyl derivatives of the formula ##STR1## wherein R signifies hydrogen or a protective group which can be split off, R.sup.1 signifies lower alkyl and X signifies the group ##STR2## wherein one of the residues R.sup.2 and R.sup.3 represents hydrogen and the other represents alkyl and R.sup.4 represents lower alkylthe easily hydrolyzable esters and ethers thereof, the salts and hydrates of the above compounds, esters, ethers and salts.

    摘要翻译: 其中R表示氢或可被分离的保护基团的酰基衍生物,R 1表示低级烷基,X表示基团R 2和R 3表示氢和 另一个代表烷基,R4代表低级烷基易易水解的酯和醚,上述化合物的盐和水合物,酯,醚和盐。