公开(公告)号：US3951954A

公开(公告)日：1976-04-20

申请号：US550457

申请日：1975-02-18

申请人： Masuo Murakami ,  Ichiro Isaka ,  Teruya Kashiwagi ,  Hidefumi Matsui ,  Kohzi Nakano ,  Kozo Takahashi ,  Hiroshi Horiguchi ,  Akio Koda

发明人： Masuo Murakami ,  Ichiro Isaka ,  Teruya Kashiwagi ,  Hidefumi Matsui ,  Kohzi Nakano ,  Kozo Takahashi ,  Hiroshi Horiguchi ,  Akio Koda

IPC分类号： C07D499/00 ,  C07D499/32 ,  C07D499/68 ,  C07D501/20 ,  C07D501/22 ,  C07D501/32

CPC分类号： C07D499/00

摘要： The oxofuryl ester derivatives of 6-(.alpha.-amino-phenylacetamido)penicillanic acid, 7-(.alpha.-aminophenylacetamido)-cephalosporanic acid, or 7-(.alpha. -aminophenylacetamide)desacetoxycephalosporanic acid represented by the general formula ##SPC1##Wherein A represents ##SPC2##Wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a lower alkyl group, said R.sup.1 and R.sup.2 may form together a 1,3-butadienylene group, R.sup.3 represents a hydrogen atom or an acetoxy group, andMeans a single bond or a double bond, and acid addition salts of them. When those compounds are orally administered, they are readily absorbed by the intestines and show antibacterial activity by splitting their ester bonds. The rate of absorption of the compounds by the intestines are higher and the toxic property of them is less than those of known compounds similar to the above compounds.

摘要翻译： 6-（α-氨基 - 苯乙酰氨基）青霉烷酸，7-（α-氨基苯基乙酰氨基） - 头孢烷酸或由通式为WHEREIN A表示的7-（α-氨基苯基乙酰胺）脱乙酰氧基头孢烷酸的氧代氟代酯衍生物代表其中R1和R2 可以相同或不同，各自表示氢原子或低级烷基，所述R 1和R 2可以一起形成1,3-丁二烯基，R 3表示氢原子或乙酰氧基，和单个键 或双重债券及其酸加法销售。 当口服这些化合物时，它们容易被肠子吸收，并通过分裂其酯键显示抗菌活性。 肠中化合物的吸收速率较高，其毒性低于与上述化合物相似的已知化合物。

公开(公告)号：US3939150A

公开(公告)日：1976-02-17

申请号：US514363

申请日：1974-10-15

申请人： Masuo Murakami ,  Ichiro Isaka ,  Khozi Nakano ,  Isao Souzu ,  Akio Koda ,  Teruaki Ozasa ,  Teruya Kashiwagi ,  Yukiyasu Murakami

发明人： Masuo Murakami ,  Ichiro Isaka ,  Khozi Nakano ,  Isao Souzu ,  Akio Koda ,  Teruaki Ozasa ,  Teruya Kashiwagi ,  Yukiyasu Murakami

IPC分类号： C07D213/78 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68

CPC分类号： C07D213/78 ,  C07D499/00

摘要： The penicillin derivatives represented by the formula ##SPC1##Wherein ring A represents a 5- or 6-membered single or fused ring which may contain one or more nitrogen atoms, an oxygen atom, or a sulfur atom; R.sup.1, R.sup.2, and R.sup.3, which may be the same or different, each represents a hydrogen atom, a hydroxy group, a lower alkyl group, a nitro group, a halogen atom, or an oxo group; and B represents a p-hydroxyphenyl group or a 1,4-cyclohexadien -1-yl group, and their nontoxic pharmaceutically acceptable salts.The compounds are antibiotics having excellent antibacterial activity in particular with respect to the Pseudomonas genus.

摘要翻译： 由式WHEREIN RING A表示的青霉素衍生物代表可含有一个或多个氮原子，氧原子或硫原子的5-或6-元单或稠环; R 1，R 2和R 3可以相同或不同，表示氢原子，羟基，低级烷基，硝基，卤原子或氧代基; B表示对羟基苯基或1,4-环己二烯-1-基及其无毒的药学上可接受的盐。

公开(公告)号：US3935198A

公开(公告)日：1976-01-27

申请号：US426108

申请日：1973-12-19

申请人： Masuo Murakami ,  Kozo Takahashi ,  Ichiro Isaka ,  Teruaki Ozasa ,  Teruya Kashiwagi

发明人： Masuo Murakami ,  Kozo Takahashi ,  Ichiro Isaka ,  Teruaki Ozasa ,  Teruya Kashiwagi

IPC分类号： C07D20060101 ,  C07D499/04 ,  C07D501/10

CPC分类号： C07D501/10

摘要： A process for the preparation of cephalosporanic acid derivatives represented by the formula ##SPC1##Wherein R.sub.1 and R.sub.2, which may be the same or different, each represents a univalent group other than a hydrogen atom, said R.sub.1 and R.sub.2 may be combined to form a divalent group and A represents a divalent group represented by the formulae ##SPC2##Wherein R.sub.3 represents a hydrogen atom or a group which does not contribute to the reaction, which comprises heating a penicillin sulfoxide derivative represented by the formula ##SPC3##Wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above.The cephalosporanic acid derivatives prepared by the process of this invention are useful as a starting material for the preparation of antibacterials.

摘要翻译： 制备由式WHEREIN R1和R2表示的头孢烷酸衍生物的方法可以相同或不同，分别表示氢原子以外的一价基团，所述R 1和R 2可以组合形成二价基团， A表示由下式表示的二价基团，其中R 3表示氢原子或对反应无贡献的基团，其包括加热由式WHEREIN R1表示的青霉素亚砜衍生物，R2和R3如上所定义。

公开(公告)号：US4051126A

公开(公告)日：1977-09-27

申请号：US704770

申请日：1976-07-13

申请人： Masuo Murakami ,  Ichiro Isaka ,  Teruya Kashiwagi

发明人： Masuo Murakami ,  Ichiro Isaka ,  Teruya Kashiwagi

IPC分类号： C07D499/00 ,  C07D499/21 ,  C07D499/44 ,  C07D499/58

CPC分类号： C07D499/00

摘要： An improved process of preparing a 6-alkoxy-substituted penicillin or penicillin sulfoxide is disclosed. This process comprises adding a halogenating agent to penicillin or penicillin sulfoxide while cooling, and then adding an alkali metal alcoholate to the hydrogenation product in the presence of an alcohol corresponding to the alcoholate.

摘要翻译： 公开了制备6-烷氧基取代的青霉素或青霉素亚砜的改进方法。 该方法包括在冷却的同时向青霉素或青霉素亚砜中加入卤化剂，然后在对应于醇化物的醇的存在下向加氢产物中加入碱金属醇化物。

公开(公告)号：US4376200A

公开(公告)日：1983-03-08

申请号：US137632

申请日：1980-04-07

申请人： Teruaki Ozasa ,  Teruya Kashiwagi

发明人： Teruaki Ozasa ,  Teruya Kashiwagi

IPC分类号： C07D501/04 ,  C07D501/18 ,  C07D501/36

CPC分类号： C07D501/04

摘要： An improved process for the displacement of the acetoxy group of a 7-aminocephalosporanic acid by a heterocyclic thiol in the presence of sulfuric acid.

摘要翻译： 在硫酸存在下通过杂环硫醇置换7-氨基头孢烷酸的乙酰氧基的改进方法。