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    3-Hydrazonomethyl rifamycins
    1.
    发明授权
    3-Hydrazonomethyl rifamycins 失效
    3-肼基甲基利福霉素

    公开(公告)号：US3862934A

    公开(公告)日：1975-01-28

    申请号：US33311173

    申请日：1973-02-16

    申请人： LEPETIT SPA

    发明人： CRICCHIO RENATO ,  LANCINI GIANCARLO

    IPC分类号： C07D231/00 ,  C07D498/08 ,  C07D99/02 ,  C07D99/04

    CPC分类号： C07D498/08

    摘要： WHEREIN R is hydrogen or phenyl, R1 is phenyl or pcarboxyphenyl, and R and R1 taken together with the adjacent carbon atom may represent a 5 to 10 carbon atom cycloalkylidene group. The compounds are prepared by reacting 3-formylrifamycin SV or its 25-desacetyl or hexahydro derivative with a hydrazine of the formula

    3-Hydrazonomethyl rifamycin compounds of the following formula and their 25-desacetyl and 16, 17; 18, 19; 28, 29-hexahydro derivatives:

    摘要翻译： 3-肼基甲基利福平化合物及其25-去乙酰基和16,17; 18，19; 28,29-六氢衍生物：

    3-Acylhydrazonomethyl rifamycins
    3.
    发明授权
    3-Acylhydrazonomethyl rifamycins 失效
    3-酰基肼基甲基利福霉素

    公开(公告)号：US3865812A

    公开(公告)日：1975-02-11

    申请号：US34204773

    申请日：1973-03-16

    申请人： LEPETIT SPA

    发明人： CRICCHIO RENATO ,  LANCINI GIANCARLO

    IPC分类号： G01F1/68 ,  A61K31/485 ,  A61P11/14 ,  A61P25/04 ,  C07D489/02 ,  C07D489/12 ,  C07D498/08 ,  C07D87/54

    CPC分类号： A61K31/485 ,  C07D489/02 ,  C07D489/12

    摘要： WHEREIN R and X have the same meaning as before, and R5 may be the same as R1 under (a), (b) or (c) as given above or it may further represent a -CO-NH-NH2 or a -(R4)-CO-NH-NH2 group wherein R4 has the same meaning as before; or R and R5 taken together may also represent a carbocyclic chain forming with the adjacent -NX-group a 5- to 7-membered heterocyclic ring fused with a benzene nucleus. The compounds have antimicrobial activity.

    The compounds are prepared by reacting at a water-liberating temperature 3-formylrifamycin SV or its 25-desacetyl or the corresponding hexahydro derivative in a suitable organic solvent with a substantially equimolar amount of a substituted hydrazine of the formula

    and 25-desacetyl and 16, 17; 18, 19; 28, 29-hexahydro derivatives thereof in which X is a -CO-, -CS-, -C(:NH)- or -SO2group, Me is a methyl group, R is hydrogen, R1 is a member of the group consisting of (a) alkyl, alkoxy, aryl and aralkyl groups; (b) an -NR2R3 group wherein R2 and R3 are independently selected from the group of hydrogen, C1-C6 lower alkyl, C3-C6 lower alkenyl, nitro and anilino groups; (c) a -CO-NH-N CH-A or a -(R4)-CO-NH-N CH-A group, wherein R4 is a divalent aliphatic, cycloaliphatic, aromatic or heterocyclic group and A represents the rifamycin SV group:

    3-Acylhydrazonomethyl rifamycin SV derivatives, of formula (I)

    摘要翻译： 3-酰基肼基甲基利福霉素SV衍生物，式（I）和25-脱乙酰基和16,17; 18，19; 28，29-六氢衍生物，其中X是-CO - ， - CS-， -​​ C（：NH） - 或-SO 2 - 基，Me是甲基，R是氢，R 1是基团的成员 由（a）烷基，烷氧基，芳基和芳烷基组成; （b）-NR2R3基团，其中R2和R3独立地选自氢，C1-C6低级烷基，C3-C6低级烯基，硝基和苯胺基; （c）-CO-NH-N = CH-A或 - （R4）-CO-NH-N = CH-A基团，其中R4是二价脂族，脂环族，芳族或杂环基团，A代表利福霉素 SV组：或相应的25-去乙酰基或16,17; 18，19; 28,29-六氢衍生物; 并且R和R 1与相邻的-N-X基团一起可以表示与苯核稠合的5-至7-元杂环。

    Antiviral compositions containing piperazine derivatives and method of use
    5.
    发明授权
    Antiviral compositions containing piperazine derivatives and method of use 失效
    含有哌嗪衍生物的抗病毒组合物及其使用方法

    公开(公告)号：US3928593A

    公开(公告)日：1975-12-23

    申请号：US13655871

    申请日：1971-04-22

    申请人： LEPETIT SPA

    发明人： LANCINI GIANCARLO ,  THIRY LISE

    IPC分类号： C07D295/30 ,  C07D487/08 ,  A61K31/495

    CPC分类号： C07D295/30 ,  C07D487/08

    摘要： Compositions and methods for controlling viral infections comprising a piperazine compound corresponding to the formula

    WHEREIN R represents hydrogen, lower alkyl, lower acyl or phenyl-lower-alkyl; R1, R2, R3 and R4 each represents hydrogen or lower alkyl; each of the pairs R1 and R2 or R3 and R4 may also represent a lower alkylene group bridging the piperazine ring; X is selected from H2, benzylidene and (H, lower acyl); and pharmaceutically acceptable acid addition salts of such compounds.

    摘要翻译： 用于控制病毒感染的组合物和方法，包括对应于式WHEREIN R的哌嗪化合物代表氢，低级烷基，低级酰基或苯基 - 低级 - 烷基; R1，R2，R3和R4各自表示氢或低级烷基; 对R1和R2或R3和R4中的每一个也可以代表桥接哌嗪环的低级亚烷基; X选自H 2，亚苄基和（H，低级酰基）; 和这些化合物的药学上可接受的酸加成盐。

    3-formylrifamycin azines
    10.
    发明授权
    3-formylrifamycin azines 失效
    3-FORMYLRIFAMYCIN AZINES

    公开(公告)号：US3900465A

    公开(公告)日：1975-08-19

    申请号：US34836473

    申请日：1973-04-05

    申请人： LEPETIT SPA

    发明人： CRICCHIO RENATO ,  LANCINI GIANCARLO

    IPC分类号： A61K38/45 ,  C07D519/00 ,  C07D41/00 ,  C07D41/06 ,  C07D87/54

    CPC分类号： C07D519/00 ,  A61K38/45

    摘要： Azine and bis-azine derivatives of 3-formylrifamycin SV of formula (I)

    and the corresponding 25-desacetyl and 16, 17; 18, 19; 28, 29hexahydro derivatives wherein Me is methyl; A is (1) a direct bond connecting the 2 nitrogen atoms, or (2) an

    wherein y is a -CO-, -CNH-, -CS-, -SO2a divalent aliphatic, cycloaliphatic, aromatic, araliphatic or heterocyclic group, and R2 and R3 independently are hydrogen, lower alkyl or taken together form an aliphatic divalent chain of 1 to 4 carbon atoms connecting the two terminal nitrogen atoms or (3) a divalent

    wherein X is a direct bond between the 2 carbon atoms, a divalent aliphatic, cycloaliphatic, aromatic or a heterocyclic group; and R and R1 may independently be hydrogen, alkyl, cycloalkyl, aryl, heterocyclic or, taken together, form an aliphatic chain of 1 to 8 carbon atoms connecting the 2 terminal carbon atoms.