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    • 15. 发明授权
    • Carbapenem derivatives
    • 卡巴培南衍生物
    • US5707987A
    • 1998-01-13
    • US696910
    • 1996-08-23
    • Susumu NakagawaHiroshi FukatsuRyosuke Ushijima
    • Susumu NakagawaHiroshi FukatsuRyosuke Ushijima
    • A61K31/407A61K31/695A61P31/04C07D477/20C07D519/06C07F7/10A61K31/40C07D487/04
    • C07D477/20
    • 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.
    • 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。
    • 18. 发明授权
    • Process for producing halogenated heteroaryl compounds
    • 卤化杂芳基化合物的制备方法
    • US6114524A
    • 2000-09-05
    • US319642
    • 1999-06-08
    • Shigemitsu OkadaRyosuke UshijimaKiyofumi Ishikawa
    • Shigemitsu OkadaRyosuke UshijimaKiyofumi Ishikawa
    • C07D213/61C07D213/79C07D213/85C07D215/48C07D241/44C07D213/02C07D215/18C07D215/20C07D237/12C07D237/14
    • C07D213/79C07D213/61C07D213/85C07D215/48C07D241/44
    • The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group. The compound is prepared by reacting a compound represented by the formula (I): ##STR2## with a quaternary ammonium halide in the presence of phosphorus pentoxide.
    • PCT No.PCT / JP97 / 04508 Sec。 371 1999年6月8日第 102(e)日期1999年6月8日PCT 1997年12月9日PCT公布。 第WO98 / 25906号公报 日期:1998年6月18日本发明涉及式(II)表示的化合物的制造方法:其中,X为卤素原子,A1,A2和A3各自相同或不同,选自碳原子数 或氮原子,条件是至少A1,A2或A3为氮原子。 R 1,R 2,R 3和R 4各自相同或不同,选自氢原子,低级烷基,氰基,羧基,低级烷氧基羰基,卤素原子和硝基。 还提供其中R 1和R 2彼此相邻,R 1和R 2可以彼此组合以形成5-或6-元环,其可以在其环上带有一个选自以下的取代基: 低级烷基,腈基,羧基,低级烷氧基羰基,氨基甲酰基,卤素原子,硝基和氨基 - (低级烷基)基。 该化合物通过在五氧化二磷存在下使式(I)表示的化合物与季铵卤化物反应来制备。