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1. 发明授权

US4051126A Process for the preparation of 6-alkoxy-substituted penicillins 失效
标题翻译：制备6-烷氧基取代的青霉素的方法
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。

2. 发明授权

US3951954A Novel oxofuryl ester derivatives of penicillin and cephalosporin 失效
标题翻译：新型青霉素和头孢菌素的氧氟草醚衍生物
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。

3. 发明授权

US3939150A Penicillin derivatives 失效
标题翻译：青霉素衍生物
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。

4. 发明授权

US3935198A Process for the preparation of the cephalosporanic acid derivative 失效
标题翻译：制备头孢菌酸衍生物的方法
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。

5. 发明授权

US4036834A Derivatives of 7-(.alpha.-hydroxy-substituted pyridyl carboxamido-.alpha. p h .DELTA..sup.3 -cephem-4-carboxylic acid 失效
标题翻译： 7 - （{6-羟基 - 取代的吡啶基甲酰氨基 - {60 {0苯基 - 乙酰氨基-3-取代的硫代甲基{66 {hu 3 {b-头孢烯-4-羧酸
公开(公告)号：US4036834A
公开(公告)日：1977-07-19
申请号：US620552
申请日：1975-10-08
申请人： Masuo Murakami , Masaru Iwanami , Ichiro Isaka , Yoshinobu Nagano , Masaharu Fujimoto , Tetsuya Maeda
发明人： Masuo Murakami , Masaru Iwanami , Ichiro Isaka , Yoshinobu Nagano , Masaharu Fujimoto , Tetsuya Maeda
IPC分类号： A61K20060101 , A61K31/545 , C07D20060101 , C07D501/04 , C07D501/36
CPC分类号： C07D501/36
摘要： Novel 7-(.alpha.-hydroxy-substituted pyridylcarboxamido-.alpha.-phenylacetamido)-3-substituted thiomethyl-.DELTA..sup.3 -cephem-4-carboxylic acid derivatives are disclosed. The compounds of this invention have high water solubility and show excellent antibacterial activities against various strains of Pseudomonas and Proteus.
摘要翻译：公开了新的7-（α-羟基取代的吡啶基甲酰氨基-α-苯基乙酰胺基）-3-取代的硫代甲基-D-TA-头孢烯-4-羧酸衍生物。本发明化合物具有高水溶性，对各种假单胞菌和变形菌菌株均具有优异的抗菌活性。

6. 发明授权

US4068074A Cephalosporin derivatives having at the 3-position of the cephem ring a heterocyclic thiomethyl group with a carboxy or sulfo group and at the 7-position of the cephem ring an .alpha.-heterocylic acylaminophenyl-acetamide group 失效
标题翻译：头孢菌素衍生物在头孢烯的3位具有羧基或磺基的杂环硫代甲基，并且在头孢烯环的7-位具有{60-环己基酰氨基苯基 - 乙酰胺基
公开(公告)号：US4068074A
公开(公告)日：1978-01-10
申请号：US695085
申请日：1976-06-11
申请人： Masuo Murakami , Ichiro Isaka , Norio Kawahara , Masaru Iwanami , Masaharu Fujimoto , Tetsuya Maeda , Tadao Shibanuma , Yoshinobu Nagano
发明人： Masuo Murakami , Ichiro Isaka , Norio Kawahara , Masaru Iwanami , Masaharu Fujimoto , Tetsuya Maeda , Tadao Shibanuma , Yoshinobu Nagano
IPC分类号： C07D501/36
CPC分类号： C07D501/36
摘要： A novel cephalosporin derivative having at the 3-position of the cephem ring a heterocyclic thiomethyl group having a carboxy group or a sulfo group and at the 7-position of the cephem ring, an .alpha.-heterocyclic acylaminophenylacetamide group. The compounds of this invention have excellent antibacterial activity against Pseudomonas and Proteus strains of bacteria.
摘要翻译：在头孢烯环的3位具有羧基或磺基的杂环硫甲基和头孢烯环的7-位的新型头孢菌素衍生物为α-杂环酰氨基苯基乙酰胺基。本发明的化合物对细菌的假单胞菌和变形菌菌株具有优异的抗菌活性。

7. 发明授权

US3953428A Ampicillin derivatives substituted by heterocyclic acyl group 失效
标题翻译：由杂环酰基取代的氨苄青霉素衍生物
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。

8. 发明授权

US4311842A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US4311842A
公开(公告)日：1982-01-19
申请号：US53852
申请日：1979-07-02
申请人： Akio Koda , Ichiro Isaka , Yukiyasu Murakami
发明人： Akio Koda , Ichiro Isaka , Yukiyasu Murakami
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/57 , C07D501/56
CPC分类号： C07D501/20 , A61K31/545 , C07D501/24
摘要： Cephalosporin compounds shown by the general formula ##STR1## wherein R.sub.1 represents hydrogen atom or an amino group; R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen atom, a hydroxy group, an oxo group, a lower alkyl group, or a lower alkoxy group; R.sub.4 represents a hydrogen atom or a lower alkoxy group; R.sub.5 represents an acetoxy group or --S--R.sub.6 (wherein R.sub.6 represents a 5- or 6-membered nitrogen-containing heterocyclic group which can be substituted by a lower alkyl group or lower alkoxy group); and A represents a monocyclic or bicyclic heterocyclic ring containing one or two atoms selected from the group consisting of nitrogen, oxygen and a sulfur atom; and pharmaceutically acceptable nontoxic salts thereof.These compounds have excellent antimicrobial activity against various microorganisms including resistant bacteria and are used for the treatment of bacterial infections of animals including human beings.
摘要翻译：由通式表示的头孢菌素化合物，其中R1表示氢原子或氨基; R 2和R 3可以相同或不同，各自表示氢原子，羟基，氧代基，低级烷基或低级烷氧基; R4代表氢原子或低级烷氧基; R5表示乙酰氧基或-S-R6（其中R6表示可被低级烷基或低级烷氧基取代的5-或6-元含氮杂环基）。 A表示含有一个或两个选自氮，氧和硫原子的原子的单环或双环杂环; 及其药学上可接受的无毒盐。这些化合物对包括抗性细菌在内的各种微生物具有优异的抗微生物活性，并用于治疗包括人在内的动物的细菌感染。

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