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    Process for preparing 2-carbamoyloxyalkyl-1,4-dihydropyridine derivatives
    1.
    发明授权
    Process for preparing 2-carbamoyloxyalkyl-1,4-dihydropyridine derivatives 失效
    2-氨基甲酰氧基烷基-1,4-二氢吡啶衍生物的制备方法

    公开(公告)号：US4958024A

    公开(公告)日：1990-09-18

    申请号：US230418

    申请日：1988-08-10

    申请人： Tetsuji Miyano ,  Kunio Suzuki ,  Ryosuke Ushijima ,  Susumu Nakagawa

    发明人： Tetsuji Miyano ,  Kunio Suzuki ,  Ryosuke Ushijima ,  Susumu Nakagawa

    IPC分类号： C07D211/90 ,  C07D295/205

    CPC分类号： C07D295/205 ,  C07D211/90

    摘要： A process for preparing a 2-carbamoylocxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

    Certain intermediate 3-carbamoyloxyalkyl propiolic acid derivatives
    2.
    发明授权
    Certain intermediate 3-carbamoyloxyalkyl propiolic acid derivatives 失效
    某些中间体3-氨基甲酰氧基烷基丙炔酸衍生物

    公开(公告)号：US4914227A

    公开(公告)日：1990-04-03

    申请号：US863984

    申请日：1986-05-16

    申请人： Tetsuji Miyano ,  Kunio Suzuki ,  Ryosuke Ushijima ,  Susumu Nakagawa

    发明人： Tetsuji Miyano ,  Kunio Suzuki ,  Ryosuke Ushijima ,  Susumu Nakagawa

    IPC分类号： C07D211/90 ,  C07D295/205

    CPC分类号： C07D295/205 ,  C07D211/90

    摘要： A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

    Carbapenem derivatives
    3.
    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

    申请人： Susumu Nakagawa ,  Hiroshi Fukatsu ,  Ryosuke Ushijima

    发明人： Susumu Nakagawa ,  Hiroshi Fukatsu ,  Ryosuke Ushijima

    IPC分类号： A61K31/407 ,  A61K31/695 ,  A61P31/04 ,  C07D477/20 ,  C07D519/06 ,  C07F7/10 ,  A61K31/40 ,  C07D487/04

    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。

    Crystalline cephalosporin compounds
    4.
    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

    申请人： Susumu Nakagawa ,  Ryosuke Ushijima ,  Fumio Nakano ,  Koji Yamada ,  Eiichi Mano

    发明人： Susumu Nakagawa ,  Ryosuke Ushijima ,  Fumio Nakano ,  Koji Yamada ,  Eiichi Mano

    IPC分类号： A61K31/545 ,  C07D501/46

    CPC分类号： C07D501/46 ,  A61K31/545 ,  C07D501/18 ,  C07D501/38

    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
    6.
    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

    申请人： Susumu Nakagawa ,  Koji Yamada ,  Ryosuke Ushijima

    发明人： Susumu Nakagawa ,  Koji Yamada ,  Ryosuke Ushijima

    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.