Antibacterial compounds, and use
    1.
    发明授权
    Antibacterial compounds, and use 失效
    抗菌化合物及用途

    公开(公告)号:US4839351A

    公开(公告)日:1989-06-13

    申请号:US941069

    申请日:1986-12-12

    摘要: A compound of the general formula: ##STR1## wherein R.sup.0 is hydrogen, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; A is S, S.fwdarw.O, O or CH.sub.2 ; R.sup.4 is hydrogen, methoxy group or formamido group; R.sup.13 is hydrogen, methyl, hydroxyl or a halogen; and A is an optionally substituted condensed cyclic group formed by combining an imidazole or pyrazole ring with 5- or 6-membered nitrogen-containing aromatic heterocyclic ring to share a C-N bond with each other,or a salt or ester thereof.and a process for preparing the same and a pharmaceutical composition thereof are disclosed.

    摘要翻译: 通式为:其中R 0为氢,含氮杂环基,酰基或氨基保护基的化合物。 A是S,S-> O,O或CH 2; R4是氢,甲氧基或甲酰氨基; R 13是氢,甲基,羟基或卤素; A是通过将咪唑或吡唑环与5-或6-元含氮芳族杂环相结合而形成的任选取代的稠合环状基团,以共价C-N键或其盐或酯。 并公开了其制备方法及其药物组合物。

    Cephem compounds, their production and use
    2.
    发明授权
    Cephem compounds, their production and use 失效
    头孢烯化合物,其生产和使用

    公开(公告)号:US4921851A

    公开(公告)日:1990-05-01

    申请号:US396758

    申请日:1989-08-22

    摘要: This invention relates to a compound of the formula: ##STR1## wherein Q is nitrogen or CH; R.sup.1 is hydrogen or a lower alkyl group which may be substituted; and ring A is a pyridine or pyridazine ring which is substituted at the ring-constituting carbon atom by a group of the formula:--E--(CH.sub.2).sub.n --R.sup.2in which E is sulfur or NH; R.sup.2 is an amino, carbamoylamino, formylamino, acetylamino, N-formimidoylamino, N-acetimidoylamino, lower alkylamino, hydroxyl or carbamoyloxy group; and n is an integer of 2 to 4, or a pharmaceutically acceptable salt thereof. The compound (I) or a pharmaceutically acceptable sale thereof has excellent antibacterial activity and is used as antibiotics.

    摘要翻译: 本发明涉及下式的化合物:其中Q是氮或CH; R1是氢或可被取代的低级烷基; 环A为吡啶或哒嗪环,其在环的构成碳原子上被下列基团取代:其中E为硫或NH的-E-(CH2)n-R2; R2是氨基,氨基甲酰基氨基,甲酰氨基,乙酰氨基,N-甲脒基氨基,N-亚氨代乙酰氨基,低级烷基氨基,羟基或氨基甲酰氧基; n为2〜4的整数,或其药学上可接受的盐。 化合物(I)或其药学上可接受的销售具有优异的抗菌活性并用作抗生素。

    1-Acyloxyalkyl esters of cephalosporin
    3.
    发明授权
    1-Acyloxyalkyl esters of cephalosporin 失效
    头孢菌素的1-芳氧基烷基酯

    公开(公告)号:US4797395A

    公开(公告)日:1989-01-10

    申请号:US886814

    申请日:1986-07-18

    CPC分类号: C07D501/36

    摘要: A compound of the formula ##STR1## wherein (1) R.sub.1 is a lower alkyl group of 2 to 6 carbon atoms or a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a cycloalkyl group of 5 to 7 carbon atoms or a lower alkyl group of 1 to 3 carbon atoms which is substituted by a cycloalkyl group of 5 to 7 carbon atoms or by a phenyl group, or (2) R.sub.1 is a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a lower alkyl group of 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.

    摘要翻译: 式(Ⅰ)化合物其中(1)R 1为2〜6个碳原子的低级烷基或5〜7个碳原子的环烷基,R 2为5〜7个碳原子的环烷基 原子或碳原子数为5〜7的环烷基取代的1〜3个碳原子的低级烷基或苯基,或(2)R 1为5〜7个碳原子的环烷基,R 2为 提供1〜5个碳原子的低级烷基或其药学上可接受的盐,其制备方法及其药物组合物。 该化合物可口服施用,具有改善生物利用度的抗生素。

    Imidazopyridazines, their production and use
    5.
    发明授权
    Imidazopyridazines, their production and use 失效
    咪达唑德他们的生产和使用

    公开(公告)号:US5145850A

    公开(公告)日:1992-09-08

    申请号:US659704

    申请日:1991-02-25

    CPC分类号: C07D487/04

    摘要: An imidazo [1,2-b]pyridazine compound of the formula (I): ##STR1## wherein R.sub.1 is a halogen atom or a lower alkyl group optionally having substituent(s), R.sub.2 and R.sub.3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R.sub.2 and R.sub.3 together with the adjacent nitrogen atom to which they bond may form a heterolcyclic ring optionally having substituent(s), X is an oxygen atom or S(O).sub.k (k is zero to two), a group --.circle.A-- is a bivalent three to seven membered homocyclic or heterocyclic group optionally having substituent(s), m.sup.1 and m.sup.2 each is an integer of 0 to 4 and n is an integer of 0 or 1; or its salt, which is useful as antiasthmatics.

    Cephem compounds, their production and use
    7.
    发明授权
    Cephem compounds, their production and use 失效
    头孢烯化合物,其生产和使用

    公开(公告)号:US5948774A

    公开(公告)日:1999-09-07

    申请号:US836424

    申请日:1997-07-29

    CPC分类号: C07D501/00

    摘要: Cephem compounds of the formula: ##STR1## wherein R.sup.1 is an optionally protected amino group; R.sup.2 is a fluoro-lower alkyl group; and the ring A may have further substituent(s), or their esters or salts, show broad and excellent antibacterial activities and are useful as antibacterial agents.

    摘要翻译: PCT No.PCT / JP96 / 01436 Sec。 371日期1997年7月29日第 102(e)日期1997年7月29日PCT提交1996年5月28日PCT公布。 WO96 / 34851 PCT出版物 日期:1996年12月5日化学式:其中R1为任选保护的氨基; R2是氟代低级烷基; 并且环A可以具有其它取代基或其酯或盐,显示出广泛和优异的抗菌活性并且可用作抗菌剂。

    Triazolopyridazine derivatives, their production and use
    8.
    发明授权
    Triazolopyridazine derivatives, their production and use 失效
    三唑并哒嗪衍生物,其生产和使用

    公开(公告)号:US5492909A

    公开(公告)日:1996-02-20

    申请号:US225981

    申请日:1994-04-12

    CPC分类号: C07D487/04

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 are a hydrogen atom, a lower alkyl group or a 5- to 7-membered cyclic group formed together with the adjacent --C.dbd.C--; X is an oxygen atom, a sulfur atom or a methylene group; Y is an optionally substituted methylene group, a divalent 3- to 7-membered homo- or heterocyclic group; R.sup.6 and R.sup.7 are a hydrogen atom, a lower alkyl group, a cycloalkyl group, an aryl group, or a nitrogen-containing heterocyclic group formed together With the adjacent nitrogen atom; m is an integer of 0 to 4; and n is an integer of 0 to 4, or a salt thereof. Said compound has an excellent anti-PAF activity, antiallergic action, etc., thus is useful as an antiasthmatic agent.

    摘要翻译: 下式的化合物:其中R 1是氢原子,低级烷基或卤素原子; R2和R3是与相邻的-C = C-一起形成的氢原子,低级烷基或5-至7-元环基; X是氧原子,硫原子或亚甲基; Y是任选取代的亚甲基,二价3-至7-元同 - 或杂环基; R6和R7是与相邻的氮原子一起形成的氢原子,低级烷基,环烷基,芳基或含氮杂环基; m为0〜4的整数。 n为0〜4的整数,或其盐。 所述化合物具有优异的抗PAF活性,抗过敏作用等,因此可用作抗哮喘药。

    1-Acyloxyalkyl esters of cephalosporin
    10.
    发明授权
    1-Acyloxyalkyl esters of cephalosporin 失效
    头孢菌素的1-芳氧基烷基酯

    公开(公告)号:US4725592A

    公开(公告)日:1988-02-16

    申请号:US637138

    申请日:1984-08-03

    CPC分类号: C07D501/36

    摘要: A compound of the formula: ##STR1## wherein R.sub.1 stands for n-propyl or isopropyl; and R.sub.2 stands for n-butyl, isobutyl, n-pentyl, n-hexyl or 2-ethylbutyl, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.

    摘要翻译: 下式的化合物:其中R 1代表正丙基或异丙​​基; R2代表正丁基,异丁基,正戊基,正己基或2-乙基丁基,或其药学上可接受的盐,其制备方法及其药物组合物。 该化合物可口服施用,具有改善生物利用度的抗生素。