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    • 3. 发明授权
    • 1-azabicycloalkane derivatives, their preparation process and their use
as medicaments
    • 1-氮杂双环链烷烃衍生物,其制备方法及其作为药物的用途
    • US5015655A
    • 1991-05-14
    • US426778
    • 1989-10-26
    • Giulio GallianiFernando BarzaghiCarla BonettiEmilio Toja
    • Giulio GallianiFernando BarzaghiCarla BonettiEmilio Toja
    • A61K31/40A61K31/435A61K31/55A61P25/02A61P25/28C07D453/02C07D471/08C07D487/08
    • C07D487/08C07D453/02
    • Compounds useful in the treatment of Alzheimers's disease, senile dementia or memory disorders of the aged of the formula ##STR1## in which n represents the number 1, 2 or 3,R.sub.1 and R.sub.2, identical or different, represent hydrogen, a linear, branched or cyclic alkyl, alkenyl, or alkynyl which contain up to 6 carbon atoms, R.sub.1 and R.sub.2 optionally substituted by hydroxy, alkoxy containing up to 6 carbon atoms, aralkyl containing up to 14 carbon atoms, a COOalk.sub.1 radical in which alk.sub.1 represents alkyl containing up to 6 carbon atoms, a --CON(alk.sub.2).sub.2 radical in which alk.sub.2 represents alkyl containing up to 6 carbon the radical --C(R.sub.1).dbd.NOR.sub.2 being in position 2, 3 or 4, in all their isomer forms and their mixture, as well as their addition salts with pharmaceutically acceptable organic or mineral acids. Also therapeutic compositions containing the compounds, method of treatment and method of preparation.
    • 用于治疗阿尔茨海默病,老年痴呆或老年化记忆障碍的化合物,其中n表示数字1,2或3,R 1和R 2相同或不同,表示氢,a 含有至多6个碳原子的直链,支链或环状烷基,烯基或炔基,任选被羟基取代的R 1和R 2,含有至多6个碳原子的烷氧基,含有至多14个碳原子的芳烷基,其中alk1代表 含有至多6个碳原子的烷基,-CON(alk2)2基团,其中alk2表示含有至多6个碳的烷基,基团-C(R 1)= NOR 2位于2,3或4位,全部为其异构体形式, 它们的混合物,以及它们与药学上可接受的有机或无机酸的加成盐。 还含有该化合物的治疗组合物,治疗方法和制备方法。
    • 4. 发明授权
    • Derivatives of 1-arylsulphonyl-2-pyrrolidinone and their use as
medicaments
    • 1-芳基磺酰基-2-吡咯烷酮的衍生物及其作为药物的用途
    • US4990531A
    • 1991-02-05
    • US315170
    • 1989-02-24
    • Giulio GallianiFernando BarzaghiMichel FortinCarlo GoriniEmilio Toja
    • Giulio GallianiFernando BarzaghiMichel FortinCarlo GoriniEmilio Toja
    • C07D207/263A61K31/40A61K31/4015A61K31/4427A61K31/445A61K31/495A61K31/535A61P25/02C07D207/27C07D207/48C07D401/12
    • C07D207/48
    • Compounds useful for the treatment of patients suffering from muscle spasms of the formula (I) ##STR1## in which R represents the radical ##STR2## in which R.sub.1, in any position on the phenyl nucleus, represents a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, identical or different each represents a hydrogen atom, a linear alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or form together with the nitrogen atom to which they are joined, a heterocyclic radical optionally containing another heteroatom, or NO.sub.2, or OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, or aryl containing up to 14 carbon atoms, or an SR.sub.4 or S(O)R.sub.5 radical, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or R represents naphthyl, optionally substituted by an R.sub.1 radical, as defined above; also therapeutic compositions containing the same and method of use.
    • 可用于治疗患有式(I)的肌肉痉挛的患者的化合物(I)其中R表示基团“IMAGE”,其中在苯基核上任何位置的R 1表示直链,支链或 含有至多8个碳原子的环烷基,烯基或炔基,或其中R 2和R 3相同或不同各自表示氢原子,直链烷基,烯基或炔基,其含有至多8个碳原子的基团, 或与其连接的氮原子一起形成任选地含有另外的杂原子的杂环基团,或代表氢的NO 2或OR',R',含有至多8个碳原子的直链,支链或环状烷基,或含有 至多14个碳原子,或SR4或S(O)R5基团,R4和R5代表含有至多8个碳原子的直链,支链或环状烷基,烯基或炔基,或R代表萘基,任选被R1 如上所述; 还含有相同的治疗组合物和使用方法。
    • 5. 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.
    • 8. 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。