| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 181 | JPH05500218A - | JP51302390 | 1990-09-04 | JPH05500218A | 1993-01-21 | |
| 182 | JPH0450313B2 - | JP19774383 | 1983-10-21 | JPH0450313B2 | 1992-08-13 | MATSUMOTO JUNICHI; MYAMOTO KOSHI; UNO JUN; NAKAMURA SHINICHI |
| 183 | Intermediate useful for preparation of nitrogen-containing polycyclic compound | JP5358791 | 1991-02-27 | JPH04210961A | 1992-08-03 | TAUNREE PII KARUBAATOSON; JIYON EMU DOOMAGARA; TOMASU EFU MITSUKU; JIEFURII BII NIKORUSU |
| PURPOSE: To provide an intermediate useful for the production of a nitrogen- containing polycyclic compound used for treating bacterial infections. CONSTITUTION: (A) 3-Pyrrolidinemethanamines of formula I [R 3 is 1-4C alkyl, 3-6C cycloalkyl; R 4 is H, 1-4C alkyl, 2-4C hydroxyalkyl or R 7CO-C (R 7 is 1-4C alkyl or 1-4C alkoxy]. (B) 2,7-Diazaspiro[4,4]nonane of formula II. (C) Ethyl[(3- pyrolidinyl)methyl] carbamate. (D) A compound of formula III (R 1 is H, 1-6C alkyl or cation; R 2 is 1-4C alkyl, vinyl, 2-4C haloalkyl or 2-4C hydroxyalkyl; X is CH, CCl, CF, C-OH, CO-1-3C alkyl, CNH-1-3C alkyl-N; and Y is H, F, Cl or Br) or IV (R 8 and R 9 are H or 1-3C alkyl). COPYRIGHT: (C)1992,JPO | ||||||
| 184 | JPH0414676B2 - | JP26844384 | 1984-12-21 | JPH0414676B2 | 1992-03-13 | HASEGAWA YOSHIHIRO; KURYAMA TAKASHI; SHIMOMURA HATSUSHI; SUGAI SABURO; OKAZAKI TOKUJI; KAJIWARA YOSHIO; KIMURA TOMONORI; KAWADA TOMIE; KANBARA TOSHIBUMI; NAITO YASUO; YOSHIDA SEIICHIRO; AKABOSHI MITSUYA; IKEGAMI |
| 185 | JPH041747B2 - | JP26543686 | 1986-11-07 | JPH041747B2 | 1992-01-14 | BANAUARA RAKUSHUMANA MIRARI; ERITSUKU ROBAATO RAASON; UIRIAMU JEI ZEMUBUROSUKII |
| 186 | Azabicycloquinolonecarboxylic acid | JP21646190 | 1990-08-16 | JPH0386875A | 1991-04-11 | KIYASARIN ERIZABESU BURAITEI |
| NEW MATERIAL: A compd. of formula I, [where R 1 is H, a cation or an alkyl; Y is ethyl, t-butyl, vinyl or cyclopropyl; W is H, F, Cl, Br, an alkyl or amino; A is CH, CF, C-CN or N; A is C which composes a five- or six-membered ring together with Y and C and N, which are combined with Y; R 2 is formula II or III, (where R 3 to R 7, R 9, R 10 and R 25 are each H, CH 3, CH 2NH 2 or CH 2 NHCH 3, and in add., R 5 to R 7 and R 9 are each NH 2, NHCH 3 or NHC 2H 5, on the condition that up to three of them are groups other than H)]. EXAMPLE: 7-(1-Amino-3-azabicyclo[3. 1. 0] hex-3-yl)-6-fluoro-1-(2,4- difluorophenyl)-1,4-dihydro-4oxo-1,8-naphthylidine-3-carboxylic acid. USE: As an antibactericide useful for the medical treatment of gram-positive infection. PROCESS: The compd. of formula I is obtd. by allowing a compd. of formula IV, (where X is an elimination group), to react with a compd. of the formula (R 2H). COPYRIGHT: (C)1991,JPO | ||||||
| 187 | JPH0130823B2 - | JP12302480 | 1980-09-05 | JPH0130823B2 | 1989-06-22 | IRIKURA TSUTOMU; SHIBA TOSHE; MATSUKUBO HIROSHI |
| 188 | Quinoline based compound, production thereof and anticancer agent containing said compound as active ingredient | JP6976687 | 1987-03-24 | JPS63238079A | 1988-10-04 | YAMATO MASATOSHI |
| NEW MATERIAL:A compound expressed by formula I (X is O or S). EXAMPLE:N-{4-[ (Benzoflo[3,2-b]quinoline-11yl)amino ]-3-methoxyphenyl}metha nesulfoneamide. USE:An anticancer agent. PREPARATION:A compound expressed by formula II is reacted with N-(4- amino-3-methoxyphenyl)methanesulfoneamide while stirring under heat and reflux to provide the aimed compound expressed by formula I. | ||||||
| 189 | Production of n-alkylquinolonecarboxylic acid derivative | JP2749787 | 1987-02-09 | JPS63196589A | 1988-08-15 | NISHIDA HIROSHI; MAGARA OSAMU; UMEMURA TAKEAKI |
| PURPOSE: To industrially and advantageously obtain a precursor for N- alkylquinolonecarboxylic acids useful as agricultural germicides, etc., by thermally rearranging a specific 4-alkoxyquinolinecarboxylic acid ester in the presence of a specific onium salt. CONSTITUTION: A 4-alkoxyquinolinecarboxylic acid ester expressed by formula I [R 1 and R 2 are lower alkyl; R 3 is H or lower alkyl; A is H, halogen, lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, -OCH 2O- (at the 6,7- positions) or formula II (at the 5,6-positions; R 4 is lower alkyl)] is thermally rearranged in the presence of an onium salt expressed by the formula R 3(R 4) 3NX or (R 5) 3SX (R 3 and R 4 are lower alkyl or benzyl; R 5 is lower alkyl; X is halogen) in a molar amount of preferably 0.02W0.1 based on the ester expressed by formula I, preferably at 120W150°C to afford the aimed compound expressed by formula III. COPYRIGHT: (C)1988,JPO&Japio | ||||||
| 190 | 2-amino-1,3,4-thiadiazole derivative and antiulcer agent containing said derivative as active component | JP17184686 | 1986-07-23 | JPS63190886A | 1988-08-08 | HASEGAWA YOSHIHIRO; HOSAKA KUNIO; TAKEDA SHIGEFUMI; MIHASHI HIROSHI |
| NEW MATERIAL:The compound of formula (R is pyridylmethylthio, pyridylmethylsulfinyl, pyridylthiomethyl or quinolylmethylthio). EXAMPLE:2-Amino-5-(2-pyridylmethylthio)-1,3,4-thiadiazole. USE:an antitumor agent. PREPARATION:The objective compound can be produced by reacting 2-amino-5- mercapto-1,3,4-thiadiazole with a compound of formula ClCH2-X (X is pyridyl or 4-quinolyl) (e.g. 2-picolyl chloride hydrochloride) in the presence of a base (e.g. sodium hydroxide) using a phase-transfer catalyst (e.g. tetra-n- butylammonium bromide). The reaction solvent is preferably a mixture of water and a water-insoluble organic solvent such as benzene. | ||||||
| 191 | JPS6256151B2 - | JP17127183 | 1983-09-19 | JPS6256151B2 | 1987-11-24 | ITO YASUO; KATO HIDEO; OGAWA NOBUO; ETSUCHU EIICHI; SUZUKI TOMIO; YAGI NORYUKI |
| 192 | Quinolone derivative | JP10668486 | 1986-05-12 | JPS62263157A | 1987-11-16 | SHIMIZU SHIGEO; YAGIHASHI FUJIO; TAKANO HIROYUKI |
| NEW MATERIAL:The compound of formula I [R<1> is halogen, (substituted) cyclic amino or imidazolyl; R<2> is alkyl which may be substituted with halogen or OH; R<3> is lower alkyl) and its salt. EXAMPLE:1-Ethyl-3-carboxy-6,7-difluoro-8-methoxy-4-quinolone. USE:An antibacterial agent. PREPARATION:The objective compound of formula I can be produced by (1) reacting the compound of formula II with R<3>ONa, (2) reducing the reaction product, (3) reacting with diethyl ethoxymethylenemalonate of formula C2H5OCH =C(COOC2H5)2, (4) contacting the resultant compound of formula III with NaH in a solvent such as DMF, (5) adding a compound of formula R<2>-X to the system after ceasing the generation of hydrogen, thereby introducing a substituent group R<2> to N atom, (6) treating the product at 60-120 deg.C in a polyphosphoric acid ester to effect cyclization and (7) subjecting the obtained compound of formula IV to hydrolysis, etc. | ||||||
| 193 | Novel quinolone derivative, ester and salt thereof | JP7166786 | 1986-03-28 | JPS62226962A | 1987-10-05 | MIYAMOTO KOSHI; KATAOKA MASAHIRO; NAKANO JUNJI; MATSUMOTO JUNICHI; NAKAMURA SHINICHI |
| NEW MATERIAL:A quinolone derivative of formula I [X1 and X2 are H or halogen; Y is O or S; R1 is H, lower alkyl or benzyl; R2 is halogen, lower mono- or dialkylamino, group of formula II or formula III (Z is O, S or R8-N; R4-R6 and R8 are H or lower alkyl; R7 is H, hydroxyl, amino, lower mono- or dialkylamino, etc.); R3 is lower alkyl, lower alkenyl etc.; n is 3-5], its ester and salt. EXAMPLE:5-Benzyloxy-1-cyclopropyl-6, 7, 8-trifluoro-1,4-dihydro-4- oxoquinoline-3- carboxylic acid ethyl ester. USE:Useful as an antibacterial agent. Also useful as a drug for man and animal, drug for fish disease, agricultural chemical, food preservative, etc. PREPARATION:The compound of formula I can be produced e.g. by reacting a novel compound of formula IV (X3 is halogen) with a compound of formula V in the presence of a base. | ||||||
| 194 | Quinoline-3-carboxylic acid derivative | JP1675886 | 1986-01-30 | JPS62178586A | 1987-08-05 | ITO YASUO; KATO HIDEO; ETSUCHU EIICHI; OGAWA NOBUO; YAGI NORIYUKI |
| NEW MATERIAL:A compound expressed by formula I (R1 is lower alkyl; R2 is H or lower alkanoyl; R3 is lower alkyl) and salt thereof. EXAMPLE:7-( 4-Acetyl-3-methyl-1-piperazinyl )-8-chloro-1-ethyl-6-fluoro-1, 4,-dihydro-4- quinoline-3-carboxylic acid. USE:An antimicrobial agent. PREPARATION:The 8-position of a quinoline-3-carboxylic acid derivative expressed by formula III, e.g. 7-(4-acetyl-3-methyl-1-piperazinyl)-1-ethyl-6- fluoro-1,4-di-hydro-4-oxoquinoline-3-carboxylic acid, etc., is directly chlorinated with a chlorinating agent, e.g. chlorine, sulfuryl chloride, etc. | ||||||
| 195 | Heterocyclic ring-containing polymeric compound and its production | JP29460185 | 1985-12-27 | JPS62153321A | 1987-07-08 | NIWA TAKAKAZU; KUROHARA TAKAYUKI; MOTOYAMA YUKIO |
| PURPOSE:To obtain a heterocyclic ring-containing polymeric compound having high physical strength, high heat resistance and good moldability, by condensing a specified heterocyclic ring-containing tetracarboxylic acid dianhydride with a specified diamine. CONSTITUTION:A heterocyclic ring-containing tetracarboxylic acid dianhydride of formula I is condensed with a diamine of the formula: H2N-R'-NH2 to obtain a heterocyclic ring-containing polymeric compound of formula II. In the formu lae, R is a 4-21C tetravalent organic residue, R1 and R2 are each H, methyl or phenyl, A is a pyridine, dipyridine, imidazole or quinoline ring which may have a substituent, R' is a 2 C or higher bivalent organic residue and n >=1. The compound of formula II can be obtained by condensing the heterocyclic compound of formula III with the tetracarboxylic acid dianhydride of formula III in the presence of a catalyst. | ||||||
| 196 | Selective herbicide | JP28970185 | 1985-12-23 | JPS62148470A | 1987-07-02 | ONODERA NOBUO; SOMEYA SHINZO |
| NEW MATERIAL:The ketoxime derivative of formula I [R 1 is lower alkyl; R 2 is lower alkyl or lower alkoxycarbonylalkyl; R 1 and R 2 may together form -(CH 2) 4- or -(CH 2) 5- which may be substituted with methyl group and one of the -CH 2- groups may be substituted with S]. EXAMPLE: 3,7-Dichloroquinoline-8-carboxylic acid acetoxime ester. USE: Useful as a herbicide. It can be safely applied to rice plant (grown in dry field or paddy field) which is a gramineous crop. It is effective in controlling gramineous weeds such as cockspur-grass, green foxtail, etc. Especially, cockspur-grass can be completely exterminated with said herbicide. PREPARATION: The compound of formula I can be produced by reacting an active compound of 3,7-dichloroquinoline-8-carboxylic acid with a ketoxime derivative of formula II. COPYRIGHT: (C)1987,JPO&Japio | ||||||
| 197 | Heterocyclic compound and manufacture | JP24330486 | 1986-10-15 | JPS62135462A | 1987-06-18 | DEIBITSUDO KOTSUKUSU; DEIBITSUDO EDOWAADO HOORU; ANTONII HAWAADO INGOORU; JIYON RUISU SASUCHITSUKII |
| 198 | Tetrahydroquinoline derivative | JP25248985 | 1985-11-11 | JPS62103080A | 1987-05-13 | UCHIDA MINORU; MORITA SEIJI; CHIHIRO MASATOSHI; NAKAGAWA KAZUYUKI |
| NEW MATERIAL:A compound shown by the formula I[R<1> and R<2> are H, alkyl, alkoxy, halogen, OH, alkenyloxy, alkynyloxy or alkoxyalkoxy; R<3> and R<4> are H, halogen, (halogen-substituted)alkyl, alkoxy, NO2 or alkanoyl; A and B are alkylene; l, m and n are 0 or 1] and its salt. EXAMPLE:5-(5-Methoxy-2-benzimidazolyl)-sulfinyl-5,6,7,8-tetrahydroquin oline. USE:Having antiulcer action, useful as a remedy for ulcers of digestive organ such as gastric ulcer, duodenal ulcer, etc. PREPARATION:For example, a compound shown by the formula II is reacted with a compound shown by the formula III(one of X1 and X2 is mercapto and the other is halogen, alkanesulfonyloxy, etc.,) in a proper solvent in the presence of a basic compound, to give a compound shown by the formula I where lis 0. | ||||||
| 199 | Quinophthalone dye | JP21286086 | 1986-09-11 | JPS6296571A | 1987-05-06 | UORUFUGANGU ROTSUCHIYU; PEETAA NOIMAN; HAINRITSUHI KOBUARUSHIYU |
| 200 | Quinazoline derivative and pharmaceutical | JP20446385 | 1985-09-18 | JPS6267077A | 1987-03-26 | YOKOYAMA KEIICHI; ONO HIROYASU; KATOU KOUJI; KITAHARA TAKUMI; NISHINA TAKASHI; WATANABE KAZUYUKI; SARUTA SAKAE; KUMAKURA MIKIO; AWAYA AKIRA; NAKANO TAKUO |
| NEW MATERIAL:The compound of formula I [Het is group of formula II (R<1> is alkyl, cycloalkyl, OH-substituted lower alkyl, aralkyl, etc.), formula III (R<3> and R<4> are lower lakoxy, OH, lower alkylamino, etc.), formula IV, formula V, etc.] or its pharmacologically permissible salt. EXAMPLE:4-Amino-6, 7-dimethoxy-2-[ 4-( 2-methyl-3-oxo-2, 3-dihydro-1 H-pyrazolo[3,4- d]pyrimidin-6-yl) piperazino] quinazoline hydrochloride. USE:Medicine. Hypotensor. It has strong and long-acting hypotensive effect. The orthostatic hypotension which is an undesirable side effect caused by rapid lowering of blood tension is alleviated or suppressed almost completely in the present hypotensor. the agent is expected to have a remedying effect to cardiac insufficiency. PREPARATION:The objective compound of formula I can be produced by reacting the compound of formula IV with the compound of formula VII in a solvent such as isoamyl alcohol at 100-150 deg.C for 1-6 hr under refluxing. | ||||||
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