Crystalline cephalosporin compounds
    2.
    发明授权
    Crystalline cephalosporin compounds 失效
    结晶头孢菌素化合物

    公开(公告)号:US4959469A

    公开(公告)日:1990-09-25

    申请号:US315917

    申请日:1989-02-27

    IPC分类号: A61K31/545 C07D501/46

    摘要: The present invention relates to stable cyrstalline (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)-3-cephem-4-carboxylate sulfate or its hydrate, a process for production of the compound and (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxyl-1-methylethoxyimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carboxylate hydrochloride or its hydrate which is a starting material useful for the production of the desired compound of the present invention.

    摘要翻译: 本发明涉及稳定的cyrstalline(6R,7R)-7 - [(Z)-2-(2-氨基噻唑-4-基)-2-(1-羧基-1-甲基乙氧基亚氨基)乙酰氨基] -3-( 5,6-二羟基-2-甲基-2-异二氢吲哚鎓)-3-头孢烯-4-羧酸甲酯硫酸盐或其水合物,该化合物的制备方法和(6R,7R)-7 - [(Z)-2 - (2-氨基噻唑-4-基)-2-(1-羧基-1-甲基乙氧基亚胺)乙酰胺基] -3-(5,6-二羟基-2-甲基-2-异二氢吲哚鎓)甲基-3-环丙基 - 4-羧酸盐酸盐或其水合物,其为可用于制备本发明所需化合物的原料。

    2-(2-cyclopropylpyrrolidin-4-ylthio)carbapenhem derivatives
    8.
    发明授权
    2-(2-cyclopropylpyrrolidin-4-ylthio)carbapenhem derivatives 失效
    2-(2-环丙基吡咯烷-4-基)乙酰胺衍生物

    公开(公告)号:US5112818A

    公开(公告)日:1992-05-12

    申请号:US635218

    申请日:1990-12-28

    IPC分类号: C07D477/20

    CPC分类号: C07D477/20

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 form together with the adjacent nitrogen atom a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group, a piperidino group, a piperazinyl group and a morpholino group, A is a carbonyl group or a single bond, and n is an integer of from 0 to 3; or a pharmaceutically acceptable salt or ester thereof.

    Carbapenem derivatives
    9.
    发明授权
    Carbapenem derivatives 失效
    卡巴培南衍生物

    公开(公告)号:US5707987A

    公开(公告)日:1998-01-13

    申请号:US696910

    申请日:1996-08-23

    CPC分类号: C07D477/20

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group, R.sup.2 is a hydrogen atom or a negative charge, R.sup.3 is a hydrogen atom or a lower alkyl group, Ar is a phenyl group, a naphthyl group or a group of: ##STR2## (wherein each of A.sub.4 and A.sub.5 is a single bond, --NHSO.sub.2 -- or the like, and Het is a pyrrolinyl group, a 1,4-diazabicyclo�2.2.2!octanyl group or the like which may be substituted with a hydroxyl group, a carbamoyl lower alkyl group or the like) which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfonyl group or the like; a hydroxyl group; a di-lower alkylsulfamoyl group or the like, each of A.sub.1, A.sub.2 and A.sub.3 is a single bond or a lower alkylene group which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfamoyl group or the like; a pyridyl group or a pyridino group; and W is a sulfur atom, a single bond; or a pharmaceutically acceptable salt or ester; a process for its production and an antibacterial agent containing it as an active ingredient.

    摘要翻译: PCT No.PCT / JP95 / 00280 Sec。 371日期:1996年8月23日 102(e)日期1996年8月23日PCT提交1995年2月24日PCT公布。 公开号WO95 / 23150 PCT 日期:1995年8月31日具有下式的化合物:其中R 1为氢原子或低级烷基,R 2为氢原子或负电荷,R 3为氢原子或低级烷基, Ar是苯基,萘基或基团,-NHSO 2 - 等,Het是可被取代的吡咯啉基,1,4-二氮杂双环[2.2.2]辛烷基等 可以被可被羟基,二低级烷基磺酰基等取代的低级烷基,低级烷基氨磺酰基等取代的羟基,氨基甲酰基低级烷基等)。 羟基; 二低级烷基氨磺酰基等,A1,A2和A3各自为可以被羟基取代的低级烷基,低级烷基氨磺酰基等取代的单键或低级亚烷基 基,二低级烷基氨磺酰基等; 吡啶基或吡啶基; W是硫原子,单键; 或药学上可接受的盐或酯; 其生产方法和含有它作为活性成分的抗菌剂。

    2-(substituted pyrrolidinylthio)carbapenem derivatives
    10.
    发明授权
    2-(substituted pyrrolidinylthio)carbapenem derivatives 失效
    2-(取代的吡咯烷硫基)碳青霉烯衍生物

    公开(公告)号:US5374720A

    公开(公告)日:1994-12-20

    申请号:US780142

    申请日:1991-10-21

    CPC分类号: C07D477/20

    摘要: A compound of the formula: ##STR1## wherein R is a hydrogen atom or a methyl group, R.sup.1 is a hydrogen atom or a negative charge, each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group, a formimidoyl group, an acetoimidoyl group, --COOR.sup.4, --CON(R.sup.5)R.sup.6, --N(R.sup.5)R.sup.6, --CH.sub.2 COOR.sup.4, --CH.sub.2 N(R.sup.5)R.sup.6 or --CH.sub.2 CON(R.sup.5)R.sup.6 (wherein R.sup.4 is a hydrogen atom or a lower alkyl group, each of R.sup.5 and R.sup.6 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.5 and R.sup.6 form together with the adjacent nitrogen atom a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group and a piperidyl group), A is .dbd.NR.sup.7, .dbd.N.sup.+ (R.sup.7)R.sup.8, wherein each of R.sup.7 and R.sup.8 which may be the same or different, is a hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group, a formimidoyl group, an acetoimidoyl group, --COOR.sup.4, --CON(R.sup.5)R.sup.6, --N(R.sup.5)R.sup.6, --CH.sub.2 COOR.sup.4, --CH.sub.2 N(R.sup.5)R.sup.6 or --CH.sub.2 CON(R.sup.5)R.sup.6 (wherein R.sup.4, R.sup.5 and R.sup.6 are as defined above), p is an integer of from 0 to 3, and q is an integer of from 1 to 3; or a pharmaceutically acceptable salt or ester thereof.

    摘要翻译: 下式的化合物:其中R是氢原子或甲基,R 1是氢原子或负电荷,R 2和R 3可以相同或不同,为氢原子 ,低级烷基,羟基低级烷基,亚氨基,亚氨酰基,-COOR4,-CON(R5)R6,-N(R5)R6,-CH2COOR4,-CH2N(R5)R6或-CH2CON( R5)R6(其中R4是氢原子或低级烷基,R5和R6各自可以相同或不同,是氢原子或低级烷基,或R5和R6与相邻的氮原子一起形成) 选自氮丙啶基,氮杂环丁烷基,吡咯烷基和哌啶基的杂环基),A为= NR 7 = N +(R 7)R 8,其中R 7和R 8可以相同或不同, 不同的是氢原子,低级烷基,羟基低级烷基,亚氨基,亚氨代乙酰基,-COOR4,-CON(R5)R6,-N(R5)R6,-CH2COOR4,-CH2N(R5 )R6或-CH2CON(R5)R6(其中 在R4中,R5和R6如上所定义),p是0-3的整数,q是1至3的整数; 或其药学上可接受的盐或酯。