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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US4845211A Amino-3-substituted-methyl-3-cephem-4-carboxylic acid and lower alkylsilyl derivatives thereof 失效
标题翻译：氨基-3-取代甲基-3-头孢烯-4-羧酸及其低级烷基甲硅烷基衍生物
公开(公告)号：US4845211A
公开(公告)日：1989-07-04
申请号：US46661
申请日：1987-05-04
申请人： Tadao Shibanuma , Kohji Nakano , Noriaki Nagano , Yukiyasu Murakami , Ryuichiro Hara , Akio Koda , Atsuki Yamazaki
发明人： Tadao Shibanuma , Kohji Nakano , Noriaki Nagano , Yukiyasu Murakami , Ryuichiro Hara , Akio Koda , Atsuki Yamazaki
IPC分类号： C07D501/04 , A61K31/545 , C07D215/06 , C07D231/06 , C07D501/16 , C07D501/18 , C07D501/20 , C07D501/38 , C07D501/46 , C07D501/58
CPC分类号： C07D501/18 , Y02P20/55
摘要： Various 7-amino-3-substituted-methyl-3-cephem-4-carboxylic acids and lower alkylsily derivatives such as 7-amino-3-(2,3-cyclopenteno-1-pyridiniomethyl)-3-cephem-4 -carboxylic acid iodide and trimethylsilyl 7-trimethylsilylamino-3 -(5,6,7,8-tetrahydro-2-isoquinoliniomethyl)-3-cephem-4 -carboxylate iodide are valuable intermediates in the preparation of new and novel antibacterial agents. A new process for the preparation of these acids and the derivatives has been devised.

6. 发明授权

US4699980A Process for preparing 3-substituted-methyl-3-cephem derivatives 失效
标题翻译： 3-取代甲基-3-头孢烯衍生物的制备方法
公开(公告)号：US4699980A
公开(公告)日：1987-10-13
申请号：US699584
申请日：1985-02-08
申请人： Tadao Shibanuma , Kohji Nakano , Noriaki Nagano , Yukiyasu Murakami , Ryuichiro Hara , Akio Koda , Atsuki Yamazaki
发明人： Tadao Shibanuma , Kohji Nakano , Noriaki Nagano , Yukiyasu Murakami , Ryuichiro Hara , Akio Koda , Atsuki Yamazaki
IPC分类号： C07D501/04 , A61K31/545 , C07D215/06 , C07D231/06 , C07D501/16 , C07D501/18 , C07D501/20 , C07D501/38 , C07D501/46 , C07D501/58
CPC分类号： C07D501/18 , Y02P20/55
摘要： Various 7-amino-3-substituted-methyl-3-cephem-4-carboxylic acids and lower alkylsilyl derivatives such as 7-amino-3-(2,3-cyclopenteno-1-pyridiniomethyl)-3-cephem-4-carboxylic acid iodide and trimethylsilyl 7-trimethyl-silylamino-3-(5,6,7,8-tetrahydro-2-isoquinoliniomethyl)-3-cephem-4-carboxylate iodide are valuable intermediates in the preparation of new and novel antibacterial agents. A new process for the preparation of these acids and the derivatives has been devised.
摘要翻译：各种7-氨基-3-取代的甲基-3-头孢烯-4-羧酸和低级烷基甲硅烷基衍生物如7-氨基-3-（2,3-环戊烯-1-吡啶基甲基）-3-头孢烯-4-羧酸碘化三甲基甲硅烷基和三甲基甲硅烷基7-三甲基甲硅烷基氨基-3-（5,6,7,8-四氢-2-异喹啉甲基）-3-头孢烯-4-羧酸酯碘化物是制备新型和新型抗菌剂的有价值的中间体。已经设计出了制备这些酸和衍生物的新方法。

7. 发明授权

US4690921A Cephalosporin compounds and salts thereof 失效
标题翻译：头孢菌素化合物及其盐
公开(公告)号：US4690921A
公开(公告)日：1987-09-01
申请号：US656162
申请日：1984-09-28
申请人： Tadao Shibanuma , Noriaki Nagano , Ryuichiro Hara , Kohji Nakano , Akio Koda , Atsuki Yamazaki , Yukiyasu Murakami
发明人： Tadao Shibanuma , Noriaki Nagano , Ryuichiro Hara , Kohji Nakano , Akio Koda , Atsuki Yamazaki , Yukiyasu Murakami
IPC分类号： C07D277/20 , C07D277/42 , C07D417/12 , C07D501/34 , C07D501/46 , A61K31/545
CPC分类号： C07D277/587 , C07D277/42 , C07D417/12
摘要： Novel cephalosporin compounds of the formula ##STR1## wherein the wavy line means syn-form and anti-form bonds, R.sup.1 represents a cyanomethyl group, a thiocarbamoylmethyl group or an aminothiazolylmethyl group, and A represents a unsubstituted or substituted pyridinio group; and salts thereof. These compounds have excellent antibacterial activities.
摘要翻译：新颖的具有式（IMAGE）的头孢菌素化合物，其中波浪线表示顺式和反式键，R 1表示氰基甲基，硫代氨基甲酰基甲基或氨基噻唑基甲基，A表示未取代或取代的吡啶并基; 及其盐。这些化合物具有优良的抗菌活性。

8. 发明授权

US4581353A Cephalosporin derivative and pharmaceutical composition 失效
标题翻译：头孢菌素衍生物和药物组合物
公开(公告)号：US4581353A
公开(公告)日：1986-04-08
申请号：US628971
申请日：1984-07-11
申请人： Masaru Iwanami , Akio Koda , Yukiyasu Murakami
发明人： Masaru Iwanami , Akio Koda , Yukiyasu Murakami
IPC分类号： C07D277/20 , C07D501/20 , C07D501/36 , A61K31/545
CPC分类号： C07D277/587 , Y02P20/55
摘要： A cephalosporin derivative of the formula ##STR1## wherein R is a hydrogen atom, a lower alkyl group which may have been substituted or a carbamoyl group which may have been substituted; R.sub.1 is hydrogen atom or a methoxy group; R.sub.2 is a hydrogen atom, an acyloxy group, or a nitrogen-containing 5-membered heterocyclic thio group which may have been substituted; R.sub.3 is a free amino group or an amino group having a protective group; and R.sub.4 is a free carboxy group or a carboxy group having a protective group or the salts thereof.The compound of this invention has an excellent antibacterial activity against gram negative bacteria and gram positive bacteria.
摘要翻译：其中R为氢原子，可被取代的低级烷基或可被取代的氨基甲酰基的式IMAMA的头孢菌素衍生物; R1是氢原子或甲氧基; R2是氢原子，酰氧基或可以被取代的含氮5元杂环硫基; R3是游离氨基或具有保护基的氨基; R4为游离羧基或具有保护基的羧基或其盐。本发明化合物对革兰氏阴性细菌和革兰氏阳性细菌具有优异的抗菌活性。

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