| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 121 | Azetidinode disulfide derivative | JP9427286 | 1986-04-22 | JPS62249983A | 1987-10-30 | TORII SHIGERU; TANAKA HIDEO; TANAKA MOTOAKI; YAMADA SHOZO; NAKAI AKIRA; OBAYASHI HISASHI |
| NEW MATERIAL:A compound expressed by formula I [R 1 is (1W4C alkyl- substituted) benzothiazole, tetrazole, thiadiazole, pyridyl or pyrimidyl; R 2 is carboxy-protecting group]. EXAMPLE: Benzhydryl 3,3-dibromo-4-(benzothiazol-2-yl)dithio-2-oxazetidine-1-(2- isopropenyl)acetate. USE: An intermediate for producing compounds having β-lactamase inhibitory action. PREPARATION: A penilcillanic acid sulfoxide derivative expressed by formula II, e.g. benzhydryl 6,6-dibromopenicillanic acid-1-oxide, etc., is reacted with a mercapto derivative expressed by the formula R 1-SH, e.g. 2- mercaptobenzothiazole, etc., in a molar amount of about normally about 1W1.5 times based on the compound expressed by formula II in a solvent, e.g. toluene, etc., normally at 50W150°C for 0.5W10hr. COPYRIGHT: (C)1987,JPO&Japio | ||||||
| 122 | Azetidin-2-one derivative and production thereof | JP26941785 | 1985-12-02 | JPS62129281A | 1987-06-11 | NAGAO YOSHIMITSU; KUMAGAI TOSHIO; SHIMIZU HISASHI |
| NEW MATERIAL:A compound shown by formula I [R 1 is lower alkyloxy, aralkyloxy, lower alkylthio, aralkylthio or protected amino; R 2 is H, lower alkyl, aryl or aralkyl; R 3 is H or group shown by formula II (R 4 is OH- protecting)]. EXAMPLE: 4S-[R-( 4S-Isopropyl-1, 3-thiazolidine-2-thion-3-ylcarbonyl)-methoxyme thyl]-azetidin-2-one. USE: A novel synthetic raw material for drugs such as carbapenem antibiotic substance, monocyclic β-lactam antibiotic, etc. PREPARATION: A compound shown by formula III (racemic modification or optical active substance is included) is reacted with tin(II)triflate in an inert solvent in the presence of a base and then alkylated with a compound shown by formula IV (L is lower alkanoyloxy, lower alkylsulfonyl or arylsulfonyl) to give a compound shown by formula I. COPYRIGHT: (C)1987,JPO&Japio | ||||||
| 123 | Manufacture of 2-(1-oxo-3-thiolanyl)-2-penem antibiotic | JP24727286 | 1986-10-17 | JPS6299379A | 1987-05-08 | KAYE ROBERT L; LINDNER DAVID L; VOLKMANN ROBERT A |
| 124 | Azetidinone derivative | JP22727985 | 1985-10-12 | JPS6287562A | 1987-04-22 | KAWASHIMA YUTAKA; SHIBUYA AKIRA; SATO MASAKAZU; HATADA YUICHI; HASATO IKUKO; NAKAJIMA YOSHIMOTO; SODA KAORU |
| NEW MATERIAL:The derivative of formula I (R<1> is lower alkyl or phenyl; R<2> is H or methyl; R<3> is H, lower alkyl, cycloalkyl, phenyl, benzyl, etc.; the wavy line represents E- or Z-configuration), EXAMPLE:(E)-4-methyl-3-(2-oxopropylidene)-1-phenyl-2-azetidinone. USE:Platelet coagulation inhibitor. PREPARATION:The objective compound of formula I can be produced by (1) condensing the compound of formula II with the compound of formula III in an inert solvent in the presence of a base (e.g. lithium isopropylamide), (2) selectively reducing the resultant compound of formula IV in an organic solvent with an alkali metal borohydride, etc., to form an alcohol of formula V, (3) converting the alcohol to the compound of formula VI with an acylation agent (e.g. acetyl chloride) or a halogenation agent (e.g. phosphorus trichloride) is the presence or absence of a base, (4) subjecting the product to elimination reaction and (5) removing the protecting group from the resultant compound of formula VII with an oxidizing agent (e.g. methyl iodide). | ||||||
| 125 | Azetidin-2-one derivative and production thereof | JP21612785 | 1985-10-01 | JPS6277384A | 1987-04-09 | NAGAO YOSHIMITSU; KUMAGAI TOSHIO; KURAMOTO YASUHIRO |
| NEW MATERIAL:The azetidin-2-one derivative of formula I R 1 is H, alkyl or aralkyl; R 2 is lower alkyl, aryl or aralkyl; R 3 is H or hydroxyl-protecting group). EXAMPLE: 3S-(1R-tert-butyldimethylsiloxyethyl)-4R[4S-ethyl-1, 3-thiazolidine-2-thi on-3-yl)carbonylmethyl]azetidin-2-one. USE: Useful as a synthetic intermediate for carbapenem antibiotic substance having a specific steric configuration (e.g. thienamycin). PREPARATION: The optically active compound of formula II is treated with tin(II) triflate in the presence of a base, the resultant enol compound is made to react with the racemic compound of formula III (L is lower alkanoyloxy, lower alkylsulfonyl or arylsulfonyl) and the obtained compound of formula I is resolved to obtain its isomer. COPYRIGHT: (C)1987,JPO&Japio | ||||||
| 126 | Optically active azetidin-2-one derivative and production thereof | JP19290585 | 1985-08-31 | JPS6253986A | 1987-03-09 | NAGAO YOSHIMITSU; KUMAGAI TOSHIO; TAMAI SEI |
| NEW MATERIAL:A compound shown by the formula I (R 1 is H, alkyl, aryl or aralkyl; R 2 is R, lower alkyl or S configuration, aryl or aralkyl). EXAMPLE: 4S-[(4S-Ethyl-1, 3-thiazolidine-2-thion-3-yl)carbonylmethyl] azetidin-2-one. USE: An intermediate for synthesizing carbapenum antibiotics, monocyclic β-lactam antibiotics, etc. PREPARATION: An optically active compound of a compound shown by the formula II is reacted with tin (II) triflate in the presence of a base. Then, the reaction product is reacted with a compound shown by the formula III (L is lower alkanoyl, lower alkylsulfonyl or arylsulfonyl). COPYRIGHT: (C)1987,JPO&Japio | ||||||
| 127 | Novel beta-lactam compound | JP12311785 | 1985-06-06 | JPS61280469A | 1986-12-11 | SUNAKAWA JUN; MATSUMURA HARUKI; SETA AKINORI; SASAKI AKIRA |
| NEW MATERIAL:The compound of formula I [R1 is vinyl, hydroxymethyl, formyl, aryl or group of formula II (X is O, S or NH); R2 is H or carboxyl- protecting group; R3 is H or hydroxyl-protecting group]. EXAMPLE:4-Carboxy-3-(1-hydroxyethyl)-1-allyl-2-azetidinone. USE:Useful as an intermediate for various carbapenem derivative having antibacterial activity. PREPARATION:The compound of formula I can be produced by reacting the Schiff base of formula II with a diketene in the presence of imidazole in an inert solvent, reducing the acetyl group of the resultant 3-acetyl-2-azetidinone-4- carboxylic acid ester derivative of formula III and, if necessary, removing the carboxyl-protecting group R2 or protecting the hydroxyl group. | ||||||
| 128 | Novel thiazole derivative | JP9648185 | 1985-05-07 | JPS61254584A | 1986-11-12 | NAKANISHI EIJI; OGASAWARA YOSHIAKI; NAKAZAWA MASAKAZU; YASUDA NAOHIKO; ONUKI TAKASHI; KATO NOBUAKI |
| NEW MATERIAL:The compound of formula I {R<1> is protectable amino; R is C(W)(Y)-Z [Z is CO2R<3> (R<3> is H, alkali metal, etc.), CO2<->, etc.; W is R<4> (R<4> is H, 1-6C lower alkyl, etc.), F, OR<4>, etc.; Y is F, OR<4>, etc.]; A is group of formula II (B is H or nucleophilic compound residue), etc.} or the compound of formula III {R<5> is group of formula CH2C(T)U)-Z [T is R<4>, F, OR<4>, etc.]}. EXAMPLE:2-( 2-Triphenylmethylamino-1, 3-thiazol-4-yl )-2-[1-t-butyloxy-carbon ylethenyl)oxyimino]acetic acid. USE:Antibacterial agent and its intermediate. PREPARATION:The compound of formula Ie can be produced by acylating the compound of formula XI(R<10> is same as R<2> and R<5>) or its reactive derivative at the carboxyl group or its salt and the compound of formula XXIV or its reactive derivative at the amino group. | ||||||
| 129 | Benzo-heterocyclic compound | JP9429585 | 1985-04-30 | JPS61251667A | 1986-11-08 | TONE HITOSHI; MIYAMOTO HISASHI; NAKAGAWA KAZUYUKI |
| NEW MATERIAL:The compound of formula I [R<1> is halogen, group of formula II (R<3> is H or alkyl) or 1-pyrrolidyl; R<2> is thienyl, thiazolyl, pyridyl, pyrrolyl, furylalkyl, pyridylalkyl or morpholino; X is halogen)] or its salt. EXAMPLE:6,7-Difluoro-1-(2-thienyl)-1,4-dihydro-4-oxoquinoline--3-carbox ylic acid. USE:An antibacterial agent having remarkable antibacterial activity against Gram-negative bacteria and Gram-positive bacteria. Useful also as a remedy for urethral infection, intestinal infection, etc. PREPARATION:The compound of formula I can be produced by halogenating the compound of formula III (X<1> is X), reacting with the compound of formula IV [R<4> is COR<9> (R<9> is alkyl), etc.; R<5> is alkyl], removing R<4> group from the resultant compound of formula V, reacting successively with the compound of formula VI and the compound of formula R<2>.NH2 and cyclizing and hydrolyz ing the produced compound of formula VII. | ||||||
| 130 | Antispasmodic and antiepileptic 3-aryloxyazetidinecarboxamide | JP4390586 | 1986-02-28 | JPS61210031A | 1986-09-18 | CHIYANDORAA ROI TEIRAA JIYUNIA; ARUBAATO DANKAN KEERU JIYUNIAA; HARORUDO FUITSUSHIYAA SUTOUFUA |
| 131 | Radiation sensitizer | JP3449985 | 1985-02-25 | JPS61194019A | 1986-08-28 | KAGITANI TSUTOMU; MINAGAWA MOTONOBU; NAKAHARA YUTAKA; KIMURA RIYOUJI; TSUBAKIMOTO TSUNEO; OSHIUMI RYOICHI; SAKANO KOICHI |
| PURPOSE:A radiation sensitizer promoting deactivation of invetrate low-oxygen cell existing in a malignant tumor by radiation, containing a specific nitrotriazole compound. CONSTITUTION:A radiation sensitizer containing a compound such as 2-(3'- nitro-1'-triazolyl)acetic acid shown by the formula I [R is (R1-O)nX1, R2-CO-X2, formula II, CH2-CO-CH2-X2, saccharide residue, etc.; R1 is alkylene; X1 is H, or acyl; n is 1-5; R2 is alkylene, hydroxyalkylene, or arylene; X2 is O-R3 (R3 is H, alkyl, etc.), N(R4)R5 (R4 is R; R5 is R3, etc.); X3 is halogen, acyloxy, or X2] as an active ingredient. The compound increases extremely sensitivity of low-oxygen cell to radiation, and enlarges the effect of actiotherapeutics. A dose is generally 20-10,000mg in an oral drug, 0.5-10,000mg in injection, and 20-10,000mg in suppository. | ||||||
| 132 | Novel 4-oxo-2-azetidinecarboxylic acid derivative | JP19982784 | 1984-09-25 | JPS6178785A | 1986-04-22 | TSUKAMOTO SHINICHI; TAMURA TOSHIYA; YOSHIDA MAKOTO; IWAMOTO HIDENORI; YAMAMOTO MINORU; KAGAMI SOICHI |
| NEW MATERIAL:A compound shown by the formula I [R<1> is azido, amino, etc.; R<2> is imidazoyl shown by the formula II or formula III (R<3> is H, or loweralkyl); Y is OH, lower alkoxy, etc.] and its salt. EXAMPLE:N<alpha>-[(2S,3R)-3-Azido-4-oxo-2-azetidinylcarbonyl]-L--h-ist idyl-L-prolin amide. USE:An improver for disturbance of consciousness in schizophrenia, depression, etc., an improver for hypobulia, etc. PREPARATION:For example, a compound shown by the formula IV and a compound shown by the formula V as starting raw materials are reacted, the prepared intermediate and a compound shown by the formula VI are subjected to peptide synthesis reaction preferably by a method wherein dicylohyxyl carbodiimide is used as a condensation agent. | ||||||
| 133 | Optically active 3-azido-azetidin-2-on-1-ylacetic acid derivative | JP19005984 | 1984-09-10 | JPS6168465A | 1986-04-08 | HATANAKA MINORU; NITTA TAKESHI; ISHIMARU HISAYASU |
| NEW MATERIAL:A compound shown by the formula I [X is OH, halogen, alkylsulfonyloxy, etc.; Y is O or NH; R 1 is H, 1W6C alkyl, phenyl, trityl, nitrobenzyl, etc.; R 2 is (esterified or amidated)carboxyl or its salt, 1W10C alkyl, cycloalkyl, phenyl, etc.]. EXAMPLE: (3S,4S)-3-Azido-1-[(R,S)-2,2-diethoxy-1-p-nitrobenzyl-carbamoylethyl]-4- hydroxymethyl-acetidin-2-one. USE: An intermediate for synthesizing a β-lactam compound showing antibacterial activity. PREPARATION: A compound shown by the formula II is reacted with an aromatic sulfonylazide to give a compound shown by the formula III, the N- protecting group of the compound is eliminated under acidic condition to give a compound shown by the formula IV, which is reacted with an equimolar mixture of an aldehyde shown by the formula R 1-CHO and an isonitrile shown by the formula R 2-NC, to give a compound shown by the formula I wherein X is OH and Y is NH. COPYRIGHT: (C)1986,JPO&Japio | ||||||
| 134 | JPS612671B2 - | JP3340176 | 1976-03-25 | JPS612671B2 | 1986-01-27 | NARISADA MASAYUKI; NAGATA WATARU |
| 135 | Bisazetidinone disulfide derivative | JP13401584 | 1984-06-27 | JPS6112686A | 1986-01-21 | RONARUDO JIYOOJI MIKETEITSUSHI; TANAKA MOTOAKI; YAMAZAKI TOMIO; NAKAI AKIRA; OGAWA KAZUO |
| NEW MATERIAL:A compound shown by the formula I (X is O or S; R 1 is carboxy-protecting group). EXAMPLE: 2,5-Bis[[ 1-{2-methyl-1-( p-nitrobenzyloxycarbonyl )-2-propen-1-yl}-2-oxoazetidin-4-yl]dithio]-1,3,4-thiadiazole. USE: An intermediate for synthesizing a β-lactamase inhibitor. PREPARATION: For example, penicillanic acid sulfoxide derivative such as 2,2- dimethylpenem-3-α-carboxylic acid 1-oxide, etc. shown by the formula II is reacted with a mercapto derivative such as 2,5-dimercapto-1,3,4-thiadiazole, etc. shown by the formula III in a solvent such as THF, etc. at 50W150°C for 0.5W 10hr. COPYRIGHT: (C)1986,JPO&Japio | ||||||
| 136 | Azetidinone derivative | JP23695383 | 1983-12-15 | JPS60130566A | 1985-07-12 | KATOU TOSHIHISA; YASUDA NAOHIKO; NAKANISHI EIJI; SASAKI YUKIO |
| NEW MATERIAL:The azetidinone derivative of formula I (R 1 is acyl, H or amino-protecting group; X is H, alkyloxy, aralkyloxy, aryloxy, OH, OSO 3H or SO 3H). EXAMPLE: 3-[D(-)-α-( 4-Ethyl-2,3-dioxy-1-piperazinecarboxamido )-α-phenylacetamido]-4-trifluoromethyl-2-azetidinone-1-sulfonic acid tetrabutylammonium salt. USE: A derivative wherein R 1 is acyl is useful as an antibiotic having broad antibacterial spectrum against Gram-negative and Gram-positive bacteria including Pseudomonas aeruginosa, and a derivative wherein R 1 is H or amino-protecting group is expected to be useful as an intermediate of the above antibiotic. PREPARATION: The compound of formula I wherein R 1 is amino-protecting group and X is H can be produced by reacting the compound of formula II with titanium trichloride in a mixture of water and alcohol or in an aqueous solution at 0W30°C for 1W2hr. COPYRIGHT: (C)1985,JPO&Japio | ||||||
| 137 | 2-azetidinone-4-substitution product | JP22146983 | 1983-11-25 | JPS60115577A | 1985-06-22 | TAMURA TOSHIYA; IWAMOTO HIDENORI; YOSHIDA MAKOTO; YAMAMOTO MINORU |
| NEW MATERIAL:A compound of formula I [R 1 is a group of formula II (R 2 is H or lower alkyl), etc.; X is methylene, ethylene, O or S; Y is amino which may be substituted; R 3 and R 4 are H or lower alkyl; n is 0 or an integer 1W3] and a salt thereof. EXAMPLE: N α-[ ( S )-2-Azetidinone-4-carbonyl ]-L-histidyl-dL-( 3,3-dimethyl )prolinamide. USE: A central nervous system acting agent. PREPARATION: A compound of formula III is reacted with a compound of formula IV to give a reaction product, which is then reacted with a compound of formula V. Alternatively, the compound of formula IV is reacted with the compound of formula V to give a reaction product, which is then reacted with the compound of formula III to afford the aimed compound of formula I . COPYRIGHT: (C)1985,JPO&Japio | ||||||
| 138 | 3-acylamino-4-methyl-2-azetidinone-1-sulfonic acid derivative, its production and drug containing said derivative | JP20460583 | 1983-10-31 | JPS6097978A | 1985-05-31 | MATSUMURA KIYOTOSHI; KIYOKAWA HIROSHI; SUZUKI DAISUKE; SHIMABAYASHI AKIHIRO; YONEMOTO YOSHIMASA |
| NEW MATERIAL:The compound of formula I (R 1 is amino or protected amino; R 2 is lower alkenyl or lower alkynyl). EXAMPLE: 3-[2-( 2-Aminothiazol-4-yl )-2-(2-propenyloxyimino)acetamido]-4-methyl- 2-azetidinone-1-sulfonic acid. USE: An antibacterial agent useful for the prevention and remedy of bacterial infectious diseases. PREPARATION: The compound of formula I can be produced by reacting the compound of formula II or its reactive derivative at the amino group or their salt with the compound of formula III or its reactive derivative at the carboxyl group or their salt, in a solvent, in the presence of a base such as trialkylamine under cooling or heating, preferably at 0W40°C. COPYRIGHT: (C)1985,JPO&Japio | ||||||
| 139 | Azetidinones | JP20900984 | 1984-10-03 | JPS6094958A | 1985-05-28 | ROBAATO ZAARAA; UIRIAMU EICHI KOSUTAA; UIRIAMU EI SURUSAACHIKU |
| 140 | Manufacture of beta-lactam compounds | JP6050584 | 1984-03-27 | JPS6045560A | 1985-03-12 | MARUBIN JIEI MIRAA |
QQ群二维码
意见反馈
意见反馈