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1. 发明专利

JPS5839688A 7ALPHA-METHOXY-3-CEPHEM DERIVATIVE 失效
公开(公告)号：JPS5839688A
公开(公告)日：1983-03-08
申请号：JP13915781
申请日：1981-09-03
申请人： EISAI CO LTD
发明人： MACHIDA YOSHIMASA , SAITOU ISAO , NOMOTO SEIICHIROU , NEGI SHIGETO , IKUTA HIRONORI , KITOU KIYOUSUKE
IPC分类号： C07D501/57 , A61K31/545 , A61K31/546 , A61P31/04
摘要： NEW MATERIAL:A compound (salt) of formulaI. EXAMPLE:7beta-[D-2-(6,7-Dihydroxychromone-3-carboxamido)-2-phenylaceta mido]- 7alpha-methoxy-3-(1-carboxymethyl-5-tetrazolyl)thiomethyl-3-cephem-4-c arboxylic acid. USE:An antimicrobial agent for Gram-positive and Gram-negative bacteria, e.g. Pseudomonas aeruginosa, Serratia marcescens or Proteus morganii, and microorganisms producing beta-lactamases. PROCESS:A 7beta-(D-2-amino-2-phenylacetamido)-7alpha-methoxy-3-(1-carboxymethyl-5- tetrazolyl)thiomethyl-3-cephem-4-carboxylic acid (salt), e.g. trifluoroacetate, is reacted with a 6,7-dihydroxychromone-3-carboxylic acid (reactive derivative), e.g. acid chloride, to give the compound of formulaI.

2. 发明专利

JPS5839687A PREPARATION OF 3-(1-CARBOXYMETHYL-5-TETRAZOLYL) THIOMETHYL-3-CEPHEM DERIVATIVE 失效
公开(公告)号：JPS5839687A
公开(公告)日：1983-03-08
申请号：JP13708581
申请日：1981-09-02
申请人： EISAI CO LTD
发明人： NOMOTO SEIICHIROU , IKUTA HIRONORI , KAMIYA TAKU , YAMAUCHI HIROSHI , MACHIDA YOSHIMASA , SAITOU ISAO
IPC分类号： C07D501/04 , C07D501/36
摘要： PURPOSE:To obtain the titled compound of high purity, by hydrolyzing a reaction product between a specific 3-acetoxymethyl-3-cephem-4-carboxylic acid and 5-mercapto-1-tetrazolylacetic acid. CONSTITUTION:A compound of formulaI[R1 is H or OH; R2 and R3 are (Cl-substituted) lower alkoxy or acyloxy], e.g. 7beta-{D-2-[6,7-bis(ethoxycarbonyloxy)chromone-3-carboxamido]-2-(4-hyd roxyphenyl)acetamido}-3-acetoxymethyl-3-cephem-4-carboxylic acid, is reacted with a 5-mercapto-1-tetrazolylacetic acid of formula II to give a compound of formula III, which is then hydrolyzed to afford the aimed compound of formula IV, e.g. disodium 7beta-[D-2-(6,7-dihydroxychromone-3-carboxamido)]-3-(1-carboxymethyl-5 -tetrazolyl)thiomethyl-3- cephem-4-carboxylate.

3. 发明专利

JPS56122384A 7ALPHAAMETHOXYCEPHALOSPORIN DERIVATIVE* ITS PREPARATION AND ANTIFUNGAL AGENT COMPRISING IT 失效
公开(公告)号：JPS56122384A
公开(公告)日：1981-09-25
申请号：JP2611280
申请日：1980-03-04
申请人： EISAI CO LTD
发明人： MACHIDA YOSHIMASA , SAITOU ISAO , NOMOTO SEIICHIROU , NEGI SHIGETO , IKUTA HIRONORI , KITOU KIYOUSUKE
IPC分类号： C07D501/57 , A61K31/545 , A61K31/546 , A61P31/04 , C07D311/22
摘要： NEW MATERIAL:A 7alpha-methoxycephalosporin derivative shown by the formula I (R1 is acyloxy, a group shown by the formula II or formula III; R2 is H or OH; R3, R4, R5, and R6 are H, OH, acyloxy, aralkyloxy, NO2, etc.). EXAMPLE:7beta-[ D-2-( chromone-3-carboxamide )-2-(4-hydroxyphenyl)acetamide ]- 7alpha-methoxy-3-[ 5-( 1-methyl-1,2,3,4-tetrazolyl )thiomethyl ]-DELTA -cephem-4-carboxylic acid. USE:An antibacterial agent. Having improved antibacterial action on Gram-positive and Gram-negative bacteria. Especially effective slightly curable bacteria, e.g., against Pseudomonas aeruginosa, Proteus morganii, beta-lactamase producing bacteria. PROCESS:A compound shown by the formula IV is reacted with a compound shown by the formula V or its reactive derivative, to give a compound shown by the formula I.

4. 发明专利

JPS55136292A CEPHALOSPORIN DERIVATIVE* ITS PREPARATION* AND ANTIBACTERIAL COMPRISING IT 失效
公开(公告)号：JPS55136292A
公开(公告)日：1980-10-23
申请号：JP4202379
申请日：1979-04-09
申请人： EISAI CO LTD
发明人： MACHIDA YOSHIMASA , SAITOU ISAO , YAMANAKA MOTOSUKE , NOMOTO SEIICHIROU , NEGI SHIGETO , KITOU KIYOUSUKE , KATSU KAMAMASA , OOYA YUKIO , SUZUKI TAKESHI , KOIZUMI KIYOUKO
IPC分类号： C07D501/22 , A61K31/545 , A61K31/546 , A61P31/04 , C07D311/22 , C07D501/34
摘要： NEW MATERIAL:A cephalosporin derivative of formula I (R1 is H or acyloxy group; R2-R5 are H, halogen, alkyl, cycloalkyl groups, etc.), and its nontoxic salt. EXAMPLE:7beta-[ D-2-( 6-n-Propylchromone-3-carboxyamido )-2-phenylacetamido ]- -3-acetoxymethyl-DELTA cephem-4-carboxylic acid. USE:An antibacterial effective against Gram-positive and Gram-negative bacteria, having remarkable effects, particularly on pseudomonas aeruginosa. PROCESS:A compound of formula II, its salt, or hydrate, is reacted with a compound of formula II or its reactive derivative in a solvent, e.g. acetone, if necessary in the presence of a dehydration condensation agent, base, or silylating agent, to give the compound of formula I.

5. 发明专利

JPS5540629A PREPARATION OF CISSPROPENYLPHOSPHONIC ACID 失效
公开(公告)号：JPS5540629A
公开(公告)日：1980-03-22
申请号：JP11363778
申请日：1978-09-18
申请人： EISAI CO LTD
发明人： MACHIDA YOSHIMASA , YAMANAKA MOTOSUKE , NOMOTO SEIICHIROU , SAITOU ISAO
IPC分类号： C07F9/38 , C07F9/40
摘要： PURPOSE:To prepare the title compound useful as an intermediate of an antibacterial substance effective to a wide variety of pathogenic bacteria, in a short time, under mild conditions, in high yield, by treating cis-propenylphosphonic acid di- lower alkyl ester with specific two compounds. CONSTITUTION:cis-Propenylphosphonic acid II is prepared by treating (1mole of) cis-propenylphosphonic acid di-lower alkyl ester I (R is lower alkyl) with trimethylsilyl chloride (pref. 2-20moles) and an alkali iodide, pref. lithium iodide (pref. 2-5moles) at a temperature between room temperature and 50 deg.C, for 0.5-1hour. The compound II is converted to an antibiotic substance III having a broad antibacterial spectrum, by reacting with an oxidizing agent.

6. 发明专利

JPS5867695A PREPARATION OF 3-(1-CARBOXYMETHYL-5-TETRAZOLYL) THIOMETHYLCEPHEM DERIVATIVE 失效
公开(公告)号：JPS5867695A
公开(公告)日：1983-04-22
申请号：JP16567081
申请日：1981-10-19
申请人： EISAI CO LTD
发明人： IKUTA HIRONORI , NOMOTO SEIICHIROU , TAKAYANAGI KEIZOU , MACHIDA YOSHIMASA , YAMAUCHI HIROSHI , KANAI TAKEO , SAITOU ISAO
IPC分类号： C07D501/04 , C07D501/36
摘要： PURPOSE:To prepare the titled derivative having antibacterial activity, or its non-toxic salt, in high purity, by the substitution reaction of a specific cephem derivative at 3-position. CONSTITUTION:The objective 7beta-[D-2-(6,7-dihydroxychromone-3-carboxamido)- 2-(4-hydroxyphenyl)acetamido]-3-(1-carboxymethyl-5-tetrazolyl)thiometh yl-3-cephem-4-carboxylic acid of formula V can be prepared by (1) reacting thecompound of formulaIwith the compound of formula II at 50-80 deg.C in the presence of a base such as sodium bicarbonate, etc. to obtain 7beta-[D-2-(6,7-dihydroxychromone- 3-carboxamido )-2-( 4-hydroxyphenyl )-acetamido]-3-(2-benzimidazolyl)thiomethyl- 3-cephem-4-carboxylic acid of formula III, and (2) reacting the product with 5- mercapto-1-tetrazolylacetic acid of formula IV in a solvent such as dimethylformamide at 10-100 deg.C.

7. 发明专利

JPS57165389A NOVEL PENICILLIN AND CEPHALOSPORIN COMPOUND 失效
公开(公告)号：JPS57165389A
公开(公告)日：1982-10-12
申请号：JP4843781
申请日：1981-04-02
申请人： EISAI CO LTD
发明人： MACHIDA YOSHIMASA , SAITOU ISAO , SUGIYAMA ISAO , NEGI SHIGETO , NOMOTO SEIICHIROU , IKUTA HIRONORI , YAMAUCHI HIROSHI , KITOU KIYOUSUKE
IPC分类号： C07D499/68 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D499/64 , C07D501/34 , C07D501/36
摘要： NEW MATERIAL:The compound of formulaI[R1 is H or methoxy; R2 is H or OH; R3 and R4 are OH or acyloxy; x is group of formula II or formula III (R5 is acyloxy or N-containing heterocyclic-thio which may have substituent group); Y is S or >N-R6 (R6 is H or lower alkyl)], its non-toxic salt, and its carboxylic acid ester. EXAMPLE:7beta-[ D-2-( 6,7-Diacetoxy-1,4-dihydro-4-oxoquinoline-3-carboxamindo )- 2-( 4-hydroxyphenyl )acetamido ]-3-( 1-carboxymethyl-5-tetrazolyl )thiomethyl-3- cephem-4-carboxylic acid. USE:Antibacterial agent hvaing extremely strong antibacterial activity especially against Pseudomonas aeruginosa and Klebsiella pneumoniae. PROCESS:The compound of formulaIis prepared by reacting the compound of formula IV, its salt or its hydrate with the compound of formula V or its reactive derivative.

8. 发明专利

JPS5799591A 7ALPHA-METHOXY-3-CEPHEM DERIVATIVE, ITS PREPARATION AND ANTIBACTERIAL AGENT COMPRISING IT 失效
公开(公告)号：JPS5799591A
公开(公告)日：1982-06-21
申请号：JP17386580
申请日：1980-12-11
申请人： EISAI CO LTD
发明人： MACHIDA YOSHIMASA , SAITOU ISAO , NOMOTO SEIICHIROU , NEGI SHIGETO , IKUTA HIRONORI , KITOU KIYOUSUKE
IPC分类号： C07D501/57 , A61K31/545 , A61K31/546 , A61P31/04
摘要： NEW MATERIAL:A 7alpha-methoxy-3-cephem derivative shown by the formula I(R1 is H, OH; R2 is a group shown by the formula II, etc.) and its nontoxic salt. EXAMPLE:7beta-[D-2-(6,7-Dihydroxychromone-3-carboxamide)-2-(4-hydroxyp henyl) acetamido]-7alpha-methoxy-3-[5-carboxymethyl-2-(1,3,4-thiadiazolyl)]th iomethyl-3- cephem-4-carboxylic acid. USE:An antibacterial agent. Effective against Gram-positive and Gram-negative bacteria, especially against slightly curable bacteria such as Pseudomonas aeruginosa and bacteria capable of producing beta-lactamase. PROCESS:A compound shown by the formula III or its salt is reacted with a compound shown by the formula IV or its reactive derivative (e.g., acid chloride) in an inert solvent in the presence or absence of a basic reagent or a silylating agent, to give the desired compound shown by the formula I.

9. 发明专利

JPS5735584A N-(substituted chromone-3-carbonyl)phenylglycine derivative 失效
标题翻译： N-（取代的CHROMONE-3-CARBONYL）苯乙烯衍生物
公开(公告)号：JPS5735584A
公开(公告)日：1982-02-26
申请号：JP10916180
申请日：1980-08-11
申请人： Eisai Co Ltd
发明人： NOMOTO SEIICHIROU , IKUTA HIRONORI , MACHIDA YOSHIMASA , NEGI SHIGETO , SUGIYAMA ISAO , YAMAUCHI HIROSHI , KANAI TAKEO , SAITOU ISAO
IPC分类号： C07D311/22 , C07D501/36
CPC分类号： C07D311/22
摘要： NEW MATERIAL:The titled derivatives of formula I [R
1 is H, hydroxyl; R
2 is H, acyl, alkoxycarbonyl, chlorine-substituted alkoxycarbonyl].
EXAMPLE: D-2-(6,7-Diacetoxychromone-3-carboxamide)-2-phenylacetic acid.
USE: Synthetic intermediate of novel compound of formula II or its salt, which are used as an antibiotic.
PREPARATION: The reaction of a compound of formula III such as D(-)-α-phenylglycine with another compound of formula IV such as 6,7-diacetoxychromone-3- carbonyl chloride is conducted in an inert solvent such as dichloromethane, when necessary, using a silylating agent at a temperature lower than room one, e.g. at 0°C, to produce the compound of formula I. The novel compound of formula II is obtained by reaction of a compound of formula I with another compound of formula V.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：式I的标题衍生物[R1是H，羟基; R2是H，酰基，烷氧基羰基，氯取代的烷氧羰基]。实施例：D-2-（6,7-二乙酰氧基色酮-3-甲酰胺）-2-苯基乙酸。用途：用作抗生素的式Ⅱ化合物或其盐的合成中间体。制备：式III化合物如D（ - ） - α-苯基甘氨酸与其它式Ⅳ化合物如6,7-二乙酰氧基色酮-3-碳酰氯的反应在惰性溶剂如二氯甲烷中进行，必要时，在低于室温的温度下使用甲硅烷化剂，例如在0℃下制备式I化合物。式II的新化合物通过式I化合物与另一种式V化合物的反应得到。

10. 发明专利

JPS5598200A PREPARATION OF 24XI* 255DIHYDROXYCHOLESTAA1*4*66TRIENN33ONE 失效
公开(公告)号：JPS5598200A
公开(公告)日：1980-07-25
申请号：JP292079
申请日：1979-01-17
申请人： EISAI CO LTD
发明人： SAIGA AKISUKE , SUGIYAMA KUNISHIGE , NOMOTO SEIICHIROU
IPC分类号： C07J9/00 , C07J17/00 , C07J21/00
摘要： PURPOSE:To obtain the title compound which is an intermediate for the active vitamin D3 analogs advantageously, by using inexpensive lithocholic acid easily available in a large quantity as a starting material. CONSTITUTION:Easily available lithocholic acid of formula I is esterified with a lower alkanol, oxidized with Jone's reagent to give a compound of formula II, which is reacted with 2-methyl-2-ethyl-1,3-dioxolan, hydrogenated with LiAlH4, and oxidized to form a compound of formula III. The resulting compound is reacted with (C6H5)3P=C (CH3)2, oxidized with an organic peracid, and hydrolyzed with an acid to form a compound of formula IV, which is diacylated, and dehydrogenated to have a double bond introduced. The protecting groups are eliminated to give 24xsi, 25-dihydroxy-cholesta-1,4,6-trien-3-one (D) of formula V in an overall yield >= about 5.5%. 1, 24xsi, 25-Trihydroxycholecaciferol can be derived from D.

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