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    • 3. 发明授权
    • New acyl-1H-1,2,4-triazole derivatives
    • 新的酰基-1H-1,2,4-三唑衍生物
    • US4888350A
    • 1989-12-19
    • US915119
    • 1986-10-03
    • Amedeo Omodei-Sale'Pietro ConsonniGiulio Galliani
    • Amedeo Omodei-Sale'Pietro ConsonniGiulio Galliani
    • C07D233/54C07D249/08
    • C07D233/64C07D233/54C07D249/08
    • New acyl -1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylendioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy; a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenactyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluormethyl, phenyl, halo and dimethylamino;R.sub.2 may represent the group ##STR2## wherein R.sub.7 is hydrogen or methyl and R.sub.8 is a (C.sub.1-4)alkyl radical, the group R.sub.5.sup.--CO or the group R.sub.6.sup.-- SO.sub.2 in which R.sub.5 and R.sub.6 are defined as above, or R.sub.7 and R.sub.8 taken together may represent a further bond between the carbon and oxygen atom;R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R.sub.1 and R.sub.4 taken together may also repesent a methylenedioxy group; with the provison that, when R represents hydrogen, R.sub.2 must be the group ##STR3## in which R.sub.8 must be the group R.sub.6.sup.--SO.sub.2 wherein R.sub.6 is as above defined; and salts therewith of pharmaceutically acceptable acids. The compounds possess antireproductive utility.
    • 式Ⅰ的新的酰基-1H-1,2,4-三唑衍生物,其中R可以位于两个相邻的氮原子之一上并且可以代表氢; 其中R 5选自(C 1-4)烷基,(C 2-4)烯基,(C 2-4)炔基,苯基,被一至三个独立地选自卤素,(C 1-4) 烷基,(C 1-4)烷氧基,三氟甲基,氰基,硝基,氨基,二 - (C 1-4)烷基氨基,(C 2-4)酰氨基和亚甲二氧基,苄基,肉桂基,氨基,(C 1-4)烷基氨基, (C 1 -C 4)烷基氨基,苯基氨基,苯基氨基,其中苯环可以被一至三个独立地选自卤素,(C 1-4)烷基,(C 1-4)烷氧基,三氟甲基,氰基,硝基,氨基,二 - (C 1-4)烷基氨基,(C 2-4)酰氨基和甲基二氧基,卤代(C 1-4)烷基,(C 1-4)烷氧基和苄氧基; 基团R6-SO2,其中R6可以表示(C1-4)烷基,苯基,被选自(C1-4)烷基和(C1-4)烷氧基的基团取代的苯基或苯甲酰基; R 1选自氢,(C 1-4)烷基,(C 1-4)烷氧基,烯丙氧基,炔丙氧基,三氟甲基,苯基,卤素和二甲基氨基; R 2可以表示基团,其中R 7是氢或甲基,R 8是(C 1-4)烷基,R 5 -CO或其中R 5和R 6如上所定义的基团R 6 -SO 2,或R 7和 一起可以代表碳和氧原子之间的另一个键; R 3和R 4独立地选自氢,卤素,(C 1-4)烷基和(C 1-4)烷氧基; R 1和R 4一起也可以代替亚甲二氧基; 当R表示氢时,R2必须是其中R8必须是R6-SO2的基团,其中R6如上所定义; 以及其与药学上可接受的酸的盐。 该化合物具有抗生素效用。
    • 4. 发明授权
    • Acyl-1H-1,2,4-triazole derivatives
    • US4459302A
    • 1984-07-10
    • US87375
    • 1979-10-23
    • Amedeo Omodei-Sale Pietro ConsonniGiulio Galliani
    • Amedeo Omodei-Sale Pietro ConsonniGiulio Galliani
    • A61K31/41C07D233/54C07D249/08C07D249/12C07D405/04
    • C07D233/64C07D233/54C07D249/08Y10S514/841
    • New acyl-1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy;a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenacyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, halo and dimethylamino;R.sub.2 may represent a (C.sub.1-4)alkyl radical or the group ##STR2## wherein R.sub.7 is hydrogen or methyl and R.sub.8 is a (C.sub.1-4)alkyl radical, the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 in which R.sub.5 and R.sub.6 are defined as above, or R.sub.7 and R.sub.8 taken together may represent a further bond between the carbon and oxygen atom;R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R.sub.1 and R.sub.4 taken together may also represent a methylenedioxy group; with the proviso that, when R represents hydrogen, R.sub.2 must be the group ##STR3## in which R.sub.8 must be the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 wherein R.sub.5 and R.sub.6 are as above defined;and salts therewith of pharmaceutically acceptable acids. The compounds possess antireproductive utility.
    • 5. 发明授权
    • 3,5-Disubstituted-1H-1,2,4-triazole derivatives as antifertility agents
    • 3,5-二取代-1H-1,2,4-三唑衍生物作为抗菌剂
    • US4370336A
    • 1983-01-25
    • US254729
    • 1981-04-16
    • Amedeo Omodei-SalePietro ConsonniGiulio GallianiLeonard Lerner
    • Amedeo Omodei-SalePietro ConsonniGiulio GallianiLeonard Lerner
    • C07D249/08A61K31/41
    • C07D249/08
    • New 3,5-disubstituted-1H-1,2,4-triazoles of formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, fluoro, chloro and dimethylamino;R.sub.1 represents a (C.sub.1-4)alkyl group;R.sub.2 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl, methoxy and ethoxy;R.sub.3 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R and R.sub.3 taken together represent a methylenedioxy group; with the proviso that, when simultaneously R, R.sub.2 and R.sub.3 represent hydrogen,cannot be methyl;with the further proviso that, when simultaneously R.sub.2 and one of R and R.sub.3 represent hydrogen, R.sub.1 and the other of R and R.sub.3 cannot simultaneously represent methyl;and salts therewith of pharmaceutically acceptable acids.The compounds possess anti-reproductive utility.
    • 新的式(I)的3,5-二取代-1H-1,2,4-三唑其中:R选自氢,(C 1-4)烷基,(C 1-4)烷氧基,烯丙氧基,炔丙氧基,三氟甲基, 苯基,氟,氯和二甲基氨基; R1表示(C1-4)烷基; R 2选自氢,氟,氯,(C 1-4)烷基,甲氧基和乙氧基; R3选自氢,氟,氯,(C1-4)烷基和(C1-4)烷氧基; R和R3一起代表亚甲二氧基; 条件是当同时R,R 2和R 3表示氢时,不能是甲基; 进一步的条件是当R 2和R 3中的一个表示氢时,R 1和R 3和R 3中的另一个不能同时表示甲基; 以及其与药学上可接受的酸的盐。 这些化合物具有抗生殖效用。
    • 7. 发明授权
    • 1,2,4-Triazole derivatives, and their use as antifertility agents
    • 1,2,4-三唑衍生物及其作为抗生育剂的用途
    • US4409388A
    • 1983-10-11
    • US87376
    • 1979-10-23
    • Amedeo Omodei-Sale'Pietro ConsonniGiulio Galliani
    • Amedeo Omodei-Sale'Pietro ConsonniGiulio Galliani
    • A61K31/41C07D249/08
    • C07D249/08
    • Novel 1,2,4-triazole derivatives are described having the following formula ##STR1## wherein R represents hydrogen or methyl, R.sub.1 stands for hydrogen or (C.sub.1 -C.sub.4)alkyl, or R and R.sub.1 taken together may represent a further bond between the carbon atom and the oxygen atom, R.sub.2 and R.sub.4, each independently, represent hydrogen, chloro, fluoro, bromo, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, R.sub.3 stands for (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, chloro, fluoro, bromo or dimethylamino or R.sub.3 and R.sub.4 taken together may represent a methylenedioxy group.Also described is a process for their manufacture.Use of the novel compounds as antireproductive agents and pharmaceutical compositions containing them as active ingredients are also claimed.
    • 描述了具有下列结构式的新的1,2,4-三唑衍生物:其中R代表氢或甲基,R1代表氢或(C1-C4)烷基,或者R和R1一起代表在 碳原子和氧原子,R2和R4各自独立地代表氢,氯,氟,溴,(C1-C4)烷基或(C1-C4)烷氧基,R3代表(C1-C4)烷基,(C1- C4)烷氧基,烯丙氧基,炔丙氧基,三氟甲基,苯基,氯,氟,溴或二甲基氨基或R3和R4一起表示亚甲二氧基。 还描述了其制造方法。 还要求保护使用新化合物作为抗生素剂和含有它们作为活性成分的药物组合物。
    • 8. 发明授权
    • 3,5-Disubstituted-1H-1,2,4-triazole derivatives
    • 3,5-二取代-1H-1,2,4-三唑衍生物
    • US4379155A
    • 1983-04-05
    • US284033
    • 1981-07-17
    • Amedeo Omodei-SalePietro ConsonniGiulio GallianiLeonard J. Lerner
    • Amedeo Omodei-SalePietro ConsonniGiulio GallianiLeonard J. Lerner
    • C07D249/08A61K31/41
    • C07D249/08
    • New 3,5-disubstituted 1H-1,2,4-triazoles of formula I ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, fluoro, chloro and dimethylamino;R.sub.1 represents a (C.sub.1-4)alkyl group;R.sub.2 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl, methoxy and ethoxy;R.sub.3 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R and R.sub.3 taken together represent a methylenedioxy group; with the proviso that, when R, R.sub.2 and R.sub.3 simultaneously represent hydrogen, R.sub.1 cannot be methyl;with the further proviso that, when R.sub.2 and one of R and R.sub.3 simultaneously represent hydrogen, R.sub.1 and the other of R and R.sub.3 cannot simultaneously represent methyl; and with the still further proviso that compounds of formula I are excluded wherein R.sub.2 is hydrogen and one of R and R.sub.3 is simultaneously a 2-positioned alkyl group and the other of R and R.sub.3 is hydrogen; and salts thereof with pharmaceutically acceptable acids. The compounds possess anti-reproductive utility.
    • 新的式I的3,5-二取代的1H-1,2,4-三唑其中:R选自氢,(C 1-4)烷基,(C 1-4)烷氧基,烯丙氧基,炔丙氧基,三氟甲基, 苯基,氟,氯和二甲基氨基; R1表示(C1-4)烷基; R 2选自氢,氟,氯,(C 1-4)烷基,甲氧基和乙氧基; R3选自氢,氟,氯,(C1-4)烷基和(C1-4)烷氧基; R和R3一起代表亚甲二氧基; 条件是当R,R 2和R 3同时表示氢时,R 1不能是甲基; 进一步的条件是当R 2和R 3中的一个同时表示氢时,R 1和R 3和R 3中的另一个不能同时代表甲基; 并且另外的条件是排除式I化合物,其中R 2是氢,R 3和R 3之一同时是2-位烷基,R和R 3中的另一个是氢; 和其盐与药学上可接受的酸。 这些化合物具有抗生殖效用。
    • 9. 发明授权
    • 1,2,4-Triazole derivatives as antifertility agents and pharmaceutical
compositions containing them
    • 1,2,4-三唑衍生物作为抗生育剂和含有它们的药物组合物
    • US4370337A
    • 1983-01-25
    • US283715
    • 1980-07-16
    • Amedeo Omodei-Sale'Pietro ConsonniGiulio Galliani
    • Amedeo Omodei-Sale'Pietro ConsonniGiulio Galliani
    • C07D249/08A61K31/41
    • C07D249/08
    • Novel 1,2,4-triazole derivatives are described having the following formula ##STR1## wherein R represents hydrogen or methyl, R.sub.1 stands for hydrogen or (C.sub.1 -C.sub.4)alkyl, or R and R.sub.1 taken together may represent a further bond between the carbon atom and the oxygen atom, R.sub.2 and R.sub.4, each independently, represent hydrogen, chloro, fluoro, bromo, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, R.sub.3 stands for (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, chloro, fluoro, bromo or dimethylamino or R.sub.3 and R.sub.4 taken together may represent a methylenedioxy group.Also described is a process for their manufacture. Use of the novel compounds as antireproductive agents and pharmaceutical compositions containing them as active ingredient are also claimed.
    • 描述了具有下列结构式的新的1,2,4-三唑衍生物:其中R代表氢或甲基,R1代表氢或(C1-C4)烷基,或者R和R1一起代表在 碳原子和氧原子,R2和R4各自独立地代表氢,氯,氟,溴,(C1-C4)烷基或(C1-C4)烷氧基,R3代表(C1-C4)烷基,(C1- C4)烷氧基,烯丙氧基,炔丙氧基,三氟甲基,苯基,氯,氟,溴或二甲基氨基或R3和R4一起表示亚甲二氧基。 还描述了其制造方法。 还要求保护使用新化合物作为抗再生剂和含有它们作为活性成分的药物组合物。