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：US3953428A

公开(公告)日：1976-04-27

申请号：US356120

申请日：1973-05-01

申请人： Masuo Murakami ,  Ichiro Isaka ,  Akio Koda ,  Norio Kawahara ,  Teruya Ashiwagi ,  Yukiyasu Murakami ,  Kuniichiro Yano ,  Kohzi Nakano ,  Isao Souzo

发明人： Masuo Murakami ,  Ichiro Isaka ,  Akio Koda ,  Norio Kawahara ,  Teruya Ashiwagi ,  Yukiyasu Murakami ,  Kuniichiro Yano ,  Kohzi Nakano ,  Isao Souzo

IPC分类号： A61K31/43 ,  C07D20060101 ,  C07D499/12 ,  C07D499/44 ,  C07D499/68 ,  C07D499/70 ,  C07D499/72

CPC分类号： C07D499/68

摘要： The ampicillin derivatives represented by the general formula ##SPC1##Wherein R represents ##SPC2##Wherein R' represents a hydrogen atom, a methyl group, or an ethyl group and A and B each represents a hydrogen atom, a hydroxyl group, a methyl group, a methoxy group, a nitro group, or a halogen atom and further said B may combine with A on the carbon atom at the position to form ##SPC3##Group (where in Z represents --CH=N-- or --CH=CH-- and an R.sup.2 represents a hydrogen atom, a hydroxyl group, a phenyl group, a methyl group, an ethyl group, a methoxy group, an ethoxyl group, a methylthio group, a trifluoromethyl group, a halogen atom, a nitro group, an acetyl group, an acetamido group, a ethoxycarbonyloxy group, or a methylsulfonyl group and further R.sub.2 and ##SPC4##May form a thiazole, isothiazolo, pyrrolo, furo, or benzo fused ring which may be substituted by an oxo group, a methyl group, or an acetyl group) and the dotted line means an arbitrary double bond, ##SPC5##Wherein R.sup.3 and R.sup.4 each represents a hydrogen atom or a methyl group, ##SPC6##Wherein R.sup.5 represents a halogen atom, a methoxy group, a nitro group, or a hydroxyl group and R.sup.6 represents a hydrogen atom, a methoxy group, a halogen atom, a nitro group, or a hydroxyl group, or ##SPC7##Wherein R.sup.7 represents a hydrogen atom or a hydroxyl group, Y represents O or S, and the dotted line means an arbitrary double bond, said substituent group, being bonded to the ampicillin molecule through --CO-- at the 2-position, 3-position, 5-position or 6-position when the oxo group (+0) is at the 4-portion and being bonded to the ampicillin molecule through the --CO-- group at the 2-position, 4-position, or 5-position when the oxy group is at the 6-position, and salts of the ampicillin derivatives.Those compounds are valuable as antibacterial agents.

摘要翻译： 由通式WHEREIN R表示的氨苄青霉素衍生物代表WHEREIN R'表示氢原子，甲基或乙基，A和B各自表示氢原子，羟基，甲基，甲氧基， 硝基或卤素原子，并且所述B可以与碳原子上的A结合形成基团（其中Z表示-CH = N-或-CH = CH-，R2表示氢原子， 羟基，苯基，甲基，乙基，甲氧基，乙氧基，甲硫基，三氟甲基，卤素原子，硝基，乙酰基，乙酰氨基，乙氧基羰基氧基 或甲基磺酰基，并且还可以是OXO基团，甲基或乙酰基团可以取代的噻唑，异噻唑，吡咯，呋喃，或苯并呋喃环），并且被引导的线表示仲胺双 BOND，其中R 3和R 4各自表示氢原子或甲基 其中，R5表示卤素原子，甲氧基，硝基或羟基，R6表示氢原子，甲氧基，卤素原子，硝基或羟基，或者WHEREIN R7表示 氢原子或羟基，Y表示O或S，虚线表示任意双键，所述取代基通过2-位，3-位，5-位上的-CO-键合到氨苄青霉素分子上 当氧基团（+0）为4-部分时，或6-位，当氧基团为氧基团时，2-位，4-位或5-位通过-CO-基团连接于氨苄青霉素分子 在6位，和氨苄青霉素衍生物的盐。