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1. 发明专利

JPS6425783A NOVEL CEPHALOSPORIN COMPOUND AND ANTIBACTERIAL MATERIAL 失效
公开(公告)号：JPS6425783A
公开(公告)日：1989-01-27
申请号：JP10726288
申请日：1988-04-28
申请人： MEIJI SEIKA KAISHA , MICROBIAL CHEM RES FOUND
发明人： TSURUOKA TAKASHI , IWAMATSU KATSUYOSHI , KATANO KIYOAKI , NAKABAYASHI AKIRA , OGINO HIROKO , YOSHIDA TAKASHI , SEZAKI MASAJI , KONDO SHINICHI
IPC分类号： C07D501/20 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46
摘要： NEW MATERIAL:The compound (salt) of formula I [R and R are H, 1-5C lower alkyl or (substituted)phenyl; A is H or nucleophilic compound residue]. EXAMPLE:(6R, 7R)-7-[(Z)-2-( 2-aminothiazol-4-yl )-2-(1, 5-dihydroxy-4-pyridon-2-yl)methoxyiminoacetamido]-3-(1-methylpyridiniu m-4-yl)-thiomethyl-ceph-3-em-4-carbox ylate. USE:An antibacterial agent. PREPARATION:The compound of formula I can be produced e.g. by reacting a carboxylic acid derivative of formula II (R is H or amino-protecting group; R and R are benzyl, p-nitrobenzyl, etc.) with a compound of formula III (R is H or carboxyl-protecting group) and removing the protecting group from the reaction product.

2. 发明专利

JPH0782291A WATER-SOLUBLE ANTHRACYCLINE DERIVATIVE 失效
公开(公告)号：JPH0782291A
公开(公告)日：1995-03-28
申请号：JP24967293
申请日：1993-09-13
申请人： MICROBIAL CHEM RES FOUND , MEIJI SEIKA KAISHA
发明人： NAKABAYASHI AKIRA , TANIGUCHI MAKOTO , UDAGAWA SHIYUUKO , HORINAGA NORIKO , MIYAZAWA TAKEO , OUCHI TATSURO , TSUCHIYA OSAMU , TAKAGI YASUSHI
IPC分类号： C07H15/252 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61K31/71
摘要： PURPOSE:To provide the subject novel derivative having an excellent antitumor effect, improved in solubility in water, releasing an anthracycline compound main body having a cell-killing activity by an enzymatic hydrolysis reaction, and useful as a therapeutic agent for cancers. CONSTITUTION:A water-soluble anthracycline derivative of formula I [n is 1-100; R is hydroxyl group, lower alkoxy, amino, mono-lower alkylamino, etc.; R is spacer group of formula II, formula II, formula III or formula III' (m is 1-8)]. For example, 14-0-(2 monomethoxypolyoxyethylenecarbamoyl- acetyl)-7-0-(2,6-dideoxy-2-fluoro-alpha-L-talopyranosyl)adriamycin. The compound of formula I is obtained e.g. by reacting an anthracycline compound of formula IV (X is Cl, Br, I atom) with an alkali metal salt of polyoxyethylenecarboxylic acid of formula V in an inactive polar solvent.

3. 发明专利

JPS6466191A NOVEL CEPHALOSPORIN DERIVATIVE AND ANTIBACTERIAL 失效
公开(公告)号：JPS6466191A
公开(公告)日：1989-03-13
申请号：JP22326187
申请日：1987-09-07
申请人： MEIJI SEIKA KAISHA
发明人： TSURUOKA TAKASHI , OGINO HIROKO , KATANO KIYOAKI , IWAMATSU KATSUYOSHI , NAKABAYASHI AKIRA , YOSHIDA TAKASHI , KONDO SHINICHI
IPC分类号： C07D501/36 , A61K31/545 , A61K31/546 , A61P31/04
摘要： NEW MATERIAL:A compound of formula I (R is H, 1-4C acyclic alkyl which may be substituted with halogen; R is 1-5C alkyl which may be substituted with halogen, phenyl) and its salts. EXAMPLE:(6R,7R)-[(Z)-2-(2-Aminothiazol-4-yl)-2-methoxyiminoaceto-amide ]-3-(3,4- dihydro-4-methyl-1,1,3-trioxo-2H-1, 2, 4, 6-thia-triazin-5-yl)thiomethyl-ceph-3-em-4- carboxylic acid. USE:Antibacterial. It has high antibacterial activity with high durability in serum concentration. PREPARATION:A compound of formula II (X is acetoxy, halogen; R is H, carboxyl-protecting group; R is H, amino group-protecting group is allowed to react with 3,4,5,6-tetrahydro-4-substituted-1,1,3-trioxo-2H-1,2,4,6-th-iatriazine-5- thione.

4. 发明专利

JPS6117589A Novel cephalosporin derivative and its preparation 失效
标题翻译：新CEPHALOSPORIN衍生物及其制备
公开(公告)号：JPS6117589A
公开(公告)日：1986-01-25
申请号：JP13820684
申请日：1984-07-03
申请人： Meiji Seika Kaisha Ltd
发明人： INOUE SHIGEHARU , TSURUOKA TAKASHI , NAKABAYASHI AKIRA , KATANO KIYOAKI , IWAMATSU KATSUYOSHI , OGINO HIROKO , YOSHIDA TAKASHI , KONDOU SHINICHI
IPC分类号： C07D501/36 , A61K31/545 , A61K31/546 , A61P31/04
摘要： NEW MATERIAL:The compound of formula I {R
1 is 1W5C alkyl, 3W6C cycloalkanomethyl (the above groups may be substituted with halogen), or group of formula II [m is 0W3; A is -COR
6 (R
6 is 1W5C alkyl, alkenyl, O, or -(CH
2 )
p B (p is 0W3; B is amino, alkyl-substituted amino, OH, COOH, CN, etc.); n is 3W5}.
EXAMPLE: Syn-7-[2-( 2-aminothiazol-4-yl )2-methoxyiminoacetamido]-3-( 2,3-cyclopenteno-1-carboxymethylpyridinium-4-yl )thiomethyl-3-cephem-4-carboxylic acid sodium salt.
USE: Antibacterial agent effective to Gram-negative and Gram-positive bacteria.
PREPARATION: The objective compound can be prepared by reacting the compound of formula IV with the 2-(2aminothiazol-4-yl) 2-syn-substituted-oxyiminoacetatic acid of formula V (R
9 is H or aminoprotecting group; R
10 is same as R
1 ), etc.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：新物质：式I的化合物{R 1是1-5C烷基，3-6C环烷基甲基（上述基团可以被卤素取代）或式II的基团[m是0-3; A是-COR 6（R 6是1-5C烷基，烯基，O或 - （CH 2）pB（p是0-3; B是氨基，烷基取代的氨基，OH，COOH，CN，等等）; n为3-5}实施例：Syn-7- [2-（2-氨基噻唑-4-基）-2-甲氧基亚氨基乙酰氨基] -3-（2,3-环戊烯-1-羧甲基吡啶鎓-4-基）硫代甲基-3-头孢烯-4-羧酸钠盐用途：对革兰氏阴性菌和革兰氏阳性菌有效的抗菌剂制备：目标化合物可以通过使式IV化合物与2-（2-氨基噻唑）（R 9为H或氨基保护基; R 10与R 1相同）等）的2-顺式取代的羟基亚氨基乙酸

5. 发明专利

JPH1180022A LYOPHILIZED PREPARATION OF VANCOMYCIN 失效
公开(公告)号：JPH1180022A
公开(公告)日：1999-03-23
申请号：JP5647698
申请日：1998-03-09
申请人： MEIJI SEIKA KAISHA
发明人： WATANABE TOMIO , HAMANO RIEKO , NAKABAYASHI AKIRA
IPC分类号： A61K9/14 , A61K9/19 , A61K38/00 , A61K47/18 , A61P31/04
摘要： PROBLEM TO BE SOLVED: To obtain the subject stable preparation suppressed in the chemical decomposition of vancomycin. SOLUTION: This lyophilized preparation comprises vancomycin or a pharmaceutically acceptable salt thereof and amino acid(s); wherein the amino acid(s) is pref. at least one kind selected from the group consisting of arginine, alanine, aspartic acid, histidine and glycine, the amount thereof to be formulated being pref. 8-100 pts.wt. based on 100 pts.wt. of the vancomycin or the salt thereof.

6. 发明专利

JPH07309758A CANCEROUS CELL METASTASIS INHIBITOR 失效
公开(公告)号：JPH07309758A
公开(公告)日：1995-11-28
申请号：JP31533594
申请日：1994-12-19
申请人： MEIJI SEIKA KAISHA
发明人： NAKABAYASHI AKIRA , TSURUOKA TAKASHI , ISHII YUKO , TSURUOKA TSUTOMU , FUKUYASU SHUNKAI , YAMAMOTO HARUO , INOUE SHIGEHARU , KONDO SHINICHI
IPC分类号： C07D211/76 , A61K31/445 , A61P35/00
摘要： PURPOSE:To obtain a medicine extremely inhibiting formation of metastatic focus of cancerous cell and having extremely slight cytotoxicity, comprising 6-O-triphenyl-D-glyco-delta-lactam as an active ingredient. CONSTITUTION:This cancerous cell metastasis inhibitor comprises 6-O- triphenylmethyl-D-glyco-delta-lactam as an active ingredient. The inhibitor is made into an oral or parenteral preparation and is administered intravenouslv, via artery or skin, subcutaneously, intracutaneously, rectally, intramuscularly or orally. Strong effect is shown by administering the inhibitor directly to a tumor. A daily dose is 100-3,000mg and administered once to several times dividedly. Carcinostatic effect can be raised by use in surgical operation therapy or radiation therapy even by simultaneous administration with an existing carcinostatic agent.

7. 发明专利

JPH01172321A ANTIVIRAL AGENT CONTAINING 6-0-SUBSTITUTED-D-GLUCO-DELTA-LACTAM 失效
公开(公告)号：JPH01172321A
公开(公告)日：1989-07-07
申请号：JP32838787
申请日：1987-12-26
申请人： MEIJI SEIKA KAISHA
发明人： TSURUOKA TAKASHI , NAKABAYASHI AKIRA , MATSUHASHI YUJI , YAMAMOTO HARUO , INOUE SHIGEHARU , KONDO SHINICHI
IPC分类号： C07D211/74 , A61K31/445 , A61P31/12 , A61P31/18
摘要： PURPOSE:To obtain an antiviral agent having low toxicity and high safety and effective in preventing and remedying the infectious diseases of retrovirus including the virus of acquired immune deficiency syndrome (AIDS), by using a 6-0-substituted-D-gluco-delta-lactam as an active component. CONSTITUTION:The objective agent contains a 6-0-substituted-D-gluco-delta-lactam of formula (n is 2 or 3; A is methyl when n is 2 and is quaternary carbon when n is 3) as an active component. Concrete examples of the active component are 6-0-triphenylmethyl-D-gluco-delta-lactam and 6-0-diphenylmethyl-D-gluco-delta-lactam. It can be used in the form of capsule, tablet, granule, etc. D-gluco-delta-lactam which is a synthetic raw material for the compound of formula can be produced by oxidizing the 1-hydroxyl group of nojirimycin which is a fermentation metabolic product of actinomycete.

8. 发明专利

JPS59116264A Novel 2-oxoazetidine derivative and its preparation 失效
标题翻译：新二氧化氮衍生物及其制备
公开(公告)号：JPS59116264A
公开(公告)日：1984-07-05
申请号：JP22390882
申请日：1982-12-22
申请人： Meiji Seika Kaisha Ltd
发明人： TSURUOKA TAKASHI , IWAMATSU KATSUYOSHI , OGINO HIROKO , NAKABAYASHI AKIRA , KAI FUMIO , INOUE SHIGEHARU
IPC分类号： C07D205/08 , A61K31/395 , A61K31/397 , A61P31/04 , C07D205/085
CPC分类号： Y02P20/55
摘要： NEW MATERIAL:The compound of formula I [X is lower alkylene chain which may be interrupted with O or S; Y is O or S; n is 0 or 1; Z is phenyl, aminopyridyl, thienyl, furyl, aminothiazolyl, aminothiadiazolyl or aminopyrimidinyl which may have OH group; R
1 is H or CH
2 R
3 (R
3 is H, halogen or OH); R
2 is SO
3 H or OSO
3 H] or its pharmacologically permissible salt.
EXAMPLE: 3S-3-{[(2R, S)-2-(((2R, S)-2-Amino-2-carboxy)ethylthioacetamido)-2-(2- amino-4-thiazolyl)]acetamido}-2-oxo-1-azetidinesulfonic acid sodium salt.
USE: Antibacterial agent.
PROCESS: The compound of formula I can be prepared by acylating the compound of formula II or its salt with the compound of formula III (R
4 and R
5 are protecting group), and eliminating the protecting groups from the product.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新物质：式I化合物[X是可被O或S中断的低级亚烷基链; Y为O或S; n为0或1; Z是可以具有OH基团的苯基，氨基吡啶基，噻吩基，呋喃基，氨基噻唑基，氨基噻二唑基或氨基嘧啶基; R1是H或CH2R3（R3是H，卤素或OH）; R2是SO3H或OSO3H]或其药理学上允许的盐。实施例：3S-3 - {[（2R，S）-2 - （（（2R，S）-2-氨基-2-羧基）乙硫基乙酰氨基）-2-（2-氨基-4-噻唑基）]乙酰氨基} - 2-氧代-1-氮杂环丁烷磺酸钠盐。用途：抗菌剂。方法：式I化合物可以通过将式II化合物或其盐与式III化合物（R4和R5是保护基）进行酰化，并从产物中除去保护基团来制备。

9. 发明专利

JPH08217787A FAT-SOLUBLE ANTHRACYCLINE DERIVATIVE 失效
公开(公告)号：JPH08217787A
公开(公告)日：1996-08-27
申请号：JP2637095
申请日：1995-02-15
申请人： MEIJI SEIKA KAISHA
发明人： UDAGAWA SHIYUUKO , ANDO TAKASHI , FUKUYASU SHUNKAI , AZEDAKA MASAYUKI , NAKABAYASHI AKIRA
IPC分类号： C07H15/252 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P43/00
摘要： PURPOSE: To obtain the subject new derivative comprising a fat-soluble prodrug derivative, which is a specific anthracycline derivative having a fat-soluble group, having a stronger carcinostatic action and slight side effect, and useful as a chemotherapeutant, etc., for cancer diseases. CONSTITUTION: This new fat-soluble derivative is represented by formula I [R is a C12-21 . aliphatic acyl; R is a group of formula II, formula III (R is a C2-21 . aliphatic acyl; R is H or a methyl) or formula IV (R is a C2-24 aliphatic acyl; X is O or S); R is H, tetrahydropyranyl or a C2-24 aliphatic acyl; Me is a methyl] and has stronger carcinostatic action and slight side effect, and is useful as a chemotherapeutant, etc., for cancer diseases. The compound is obtained by reacting 4'-O-tetrahydropyranyl-adriamycin with salicylaldehyde etc., in a solvent at room temperature to prepare 3'-N-salicylidene-4'-O- tetrahydropyranyl-adriamycin, thereafter, reacting the prepared compound with palmitic acid, etc., in a solvent in the presence of 4-dimethylaminopyridine.

10. 发明专利

JPH0643306B2 失效
公开(公告)号：JPH0643306B2
公开(公告)日：1994-06-08
申请号：JP3109588
申请日：1988-02-12
申请人： MEIJI SEIKA KAISHA
发明人： TSURUOKA TSUTOMU , FUKUYASU SHUNKAI , YAMAMOTO HARUO , NAKABAYASHI AKIRA , TSURUOKA TAKASHI , INOUE SHIGEHARU , KONDO SHINICHI
IPC分类号： C07D211/46 , A61K31/445 , A61P35/00

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