161 |
JPH0552306B2 - |
JP623586 |
1986-01-17 |
JPH0552306B2 |
1993-08-05 |
MITO KUNIO |
|
162 |
JPH0546339B2 - |
JP15830785 |
1985-07-19 |
JPH0546339B2 |
1993-07-13 |
KAIHO TATSUO; OOTSUKA KENGO; ITO TOSHIHIKO; KITANO TAKASHI; MARUYAMA MASAHIKO; HIRAYAMA MAKOTO |
|
163 |
JPH0546337B2 - |
JP7118285 |
1985-04-05 |
JPH0546337B2 |
1993-07-13 |
ITO TOSHIHIKO; SUZUKI TSUNESHI; MITO KUNIO; MARUYAMA MASAHIKO; HIRAYAMA MAKOTO; KITANO TAKASHI |
|
164 |
JPH05500218A - |
JP51302390 |
1990-09-04 |
JPH05500218A |
1993-01-21 |
|
|
165 |
1-arylsulfonylpiperazines and their acid addition salt permissible as medicine |
JP14566491 |
1991-05-20 |
JPH04342579A |
1992-11-30 |
HIDAKA HIROYOSHI; ISHIKAWA TOMOHIKO; ARAKAWA EITARO; KATO TETSUO; TAKAMURA TSUKASA |
PURPOSE: To obtain the subject compounds, having vascular smooth muscle relaxing action and action on biological enzyme systems and useful as ameliorants of cerebral circulation, vasolidators hypotensive agents, etc.
CONSTITUTION: Compounds expressed by formula I [Ar is phenyl, 2-pyridyl, etc.; R
1 and R
2 are H, lower alkyl, etc., or both the groups together form imino, oxy, etc.; R
3 is halogen, nitro, etc.; (n) is 0-5; X is vinylene, CH
2 or O] and an acid addition salt permissible as a medicine, e.g. 1-(3-phenyl-trans-2- propenyl)-4-(8-quinolinylsulfonyl)piperazine. The compounds expressed by formula I are obtained by reacting, e.g. a piperazine compound expressed by formula II (R
4 and R
5 are H, lower alkyl, etc., or R
4 and R
5 together form oxy) with a compound (e.g. benzenesulfonyl chloride) expressed by formula III in a molar amount of preferably 1-3 times in the presence of an acid acceptor (e.g. sodium hydrogencarbonate) in a solvent such as ethanol, preferably at 0-80°C and, as necessary, deprotecting and hydrolyzing the resultant compound.
COPYRIGHT: (C)1992,JPO&Japio |
166 |
JPH0359071B2 - |
JP20754386 |
1986-09-02 |
JPH0359071B2 |
1991-09-09 |
KAMURO YASUO; TANIGUCHI EIJI; WATANABE KATSUJI |
|
167 |
JPH0143740B2 - |
JP7615781 |
1981-05-18 |
JPH0143740B2 |
1989-09-22 |
TAWARA YOSHUKI; KOMATSU YASUHIRO; KOYAMA HIROYASU; KUBOTA REIKO; YAMAGUCHI TERUTO; TAKAHASHI TOSHIHIRO |
|
168 |
JPH0131502B2 - |
JP8928180 |
1980-07-02 |
JPH0131502B2 |
1989-06-26 |
KAARUMAAN TAKAACHU; MAARIA HAA PAPU; GAABORU KOBAACHU; IRONA KAA AIYUZERUTO; ANTARU SHIMAI; PEETERU RITERAATEI NAJII; MARIAN EE PUSUKAASHU; JURA SHEBESHUTEIEEN; ISHUTOAAN SHITADORERU; ZORUTAAN SHUUMEGII |
|
169 |
JPH0118899B2 - |
JP8683281 |
1981-06-08 |
JPH0118899B2 |
1989-04-07 |
SUZUKI YASUSHI; TSUKAMOTO KUNIO; MINAMI NOBUYOSHI; HASEGAWA YUKIO; SATO MICHITAKA; YAMAMOTO NORIO; MYASAKA KATSUHIKO; KENJO TAKASHI; FUNAKOSHI SATOSHI |
|
170 |
Isatin derivative |
JP13844386 |
1986-06-13 |
JPS62294654A |
1987-12-22 |
KOBAYASHI MICHIHIRO; KITAZAWA MAKIO; AKAHA MASUO; TSUKAMOTO TSUTOMU; YAMAMOTO RYOJI; NAKANO YASUSHI |
NEW MATERIAL:The compound of formula I (R is halogen, alkyl, alkoxy, amino, acylamino or alkoxycarbonyl; n is 0 or 1; R<1> is H, alkyl, aryl, aralkyl or cycloalkyl; Y is 2-4C alkylene; R<2> and R<3> are H, 1-5C alkyl, alkenyl, aralkyl or cycloalkyl; R<2> and R<3> may together with N form pyrrolidinyl, piperidino, piperazinyl or tetrahydroisoquinolyl) and its acid addition salt. EXAMPLE:(E)-5-bromo-1-[2-(2,2,6,6-tetramethylpiperidino)ethyl]isatin-3 -semicarba zone. USE:A remedy for gastric and duodenal ulcer free from strong central suppressing activity. PREPARATION:The compound of formula I can be produced by reacting the compound of formula II with a semicarbazide derivative of formula III. The starting compound of formula II is obtained e.g. by the reaction of the compound of formula IV with an aminoalkyl derivative of formula V (X is acid residue). |
171 |
Cyclic amine derivative |
JP2815386 |
1986-02-12 |
JPS62187452A |
1987-08-15 |
UNO JUN; KUROKAWA MIKIO; SATO FUMINORI; NARUTO SHUNSUKE; HOSOKI KAZU; TAKEYAMA KUNIHIKO |
NEW MATERIAL:A compound expressed by formula I (R1 is formula II or III; ring A and ring B are benzene ring or cyclohexane ring; both Y and Z and H or together form single bond, O, S, CH=CH, etc.; R2 is H, R or OR; R is lower alkyl; W is CO or SO2; X is alkylene; R3 is formula IV-VIII; R4 and R5 are H, halogen, R, etc.; R6 is H, R, OH, etc.; R7 is H, halogen, OH, etc.; R8 is H or OH; R9 is COOR', phenyl, etc.; R' is R or aralkyl; a and b are integers of 1-4; d and f are 1, 2 or 3; e is 0 or 1). EXAMPLE:11-[4-(1,2,3,4-Tetrahydroisoquinolin-2-yl)butyrylamino]-6,11-d ihydroben zo[b,e]thiepin. USE:A calcium antagonistic agent. PREPARATION:A compound corresponding to formula I (R3 is substituted by reactive residue of alcohol) is reacted with a compound expressed by the formu la R3'H (R3' is formula IV or V) to afford the aimed compound expressed by formula I (R3 is R3'). |
172 |
Pyrazoloisoquinoline derivative, production thereof and agricultural chemical |
JP20754386 |
1986-09-02 |
JPS62149676A |
1987-07-03 |
KAMURO YASUO; TANIGUCHI EIJI; WATANABE KATSUJI |
NEW MATERIAL:The pyrazoloisoquinoline derivative of formula I [R
1 and R
2 are H, halogen, nitro, lower alkyl, halogen-substituted (lower) alkyl, lower alkoxy, lower alkylthio or aryloxy].
EXAMPLE: 2-Phenyl-5,6-dihydropyrazolo[5,1-a]isoquinolin-5-one.
USE: It has strong auxin transport inhibiting activity and is useful as a plant- growth regulator. It can be used for suppressing the growth of plant height and succulent shoot of e.g. tomato, eggplant, green pepper, etc., suppressing the growth of plant height of flowers such as chrysanthemum, cosmos, etc., suppressing the growth of succulent shoot of fruit trees such as apple, ear, etc., and increasing the yield of gramineous crops, etc.
PREPARATION: The compound of formula I can be produced by reacting an ortho-substituted phenylacetic acid derivative of formula II with hydrazine in a solvent such as tetrahydrofuran.
COPYRIGHT: (C)1987,JPO&Japio |
173 |
Isoquinoline derivative and remedying composition containing same as active ingredient |
JP15830785 |
1985-07-19 |
JPS6219570A |
1987-01-28 |
KAIHO TATSUO; OOTSUKA KENGO; ITO TOSHIHIKO; KITANO TAKASHI; MARUYAMA MASAHIKO; HIRAYAMA MAKOTO |
NEW MATERIAL:A compound shown by the formula I (X is ethoxycarbonyl CN, acetyl, NO2, pyridinocarbonyl, dimethylcarbamoyl, pyridylcarbonyl, morpholinocarbonyl, benzyl, etc.). EXAMPLE:4-Cyano-7-ethoxycarbonyl-2,3,5,6,7,8-hexahydro-1-methy-l-3-oxo isoquino line. USE:A cardiac, an agent for alleviating cardiac incompetence and a remedy for circulatory diseases having excellent cardiac action. PREPARATION:A compound shown by the formula III is reacted with a silylating agent in the presence of a base to give a compound shown by the formula IV, which is subjected to Diels-Alder reaction with a compond shown by the formula V to give a compound shown by the formula VI. Then, this compound is reacted with acetyl chloride in the presence of a Lewis acid to give a compound shown by the formula VII, which is subjected to ring closure through condensation with cyanoacetamide in the presence of an organic solvent to give a compound shown by the formula I. |
174 |
Novel thiazoles, its production and drug |
JP14597986 |
1986-06-20 |
JPS6212768A |
1987-01-21 |
DEIITAA ZORUKU |
|
175 |
Isoquinoline derivative |
JP13194085 |
1985-06-19 |
JPS61291570A |
1986-12-22 |
SUZUKI TSUNESHI; MITO KUNIO; ITO TOSHIHIKO; KITANO TAKASHI; MARUYAMA MASAHIKO; HIRAYAMA MAKOTO; KAMIYA JOJI; AWAYA AKIRA |
NEW MATERIAL:A compound shown by the formula I (R1 is CH3 or methoxymethyl; R2 and R3 are H, lower alkyl, lower alkoxy, cyclohexyl, phenyl, pyridyl, etc.) and its salt. EXAMPLE:4-Cyano-2,3,5,6,7,8-hexahydro-1-methyl-3-oxo-7-(4-pyridyl) isoquinoline. USE:A cardiac. PREPARATION:A compound shown by the formula II is condensed with bromopyridine in the presence of n-butyllithium, etc. to give a compound shown by the formula III, which is dehydrated, then reduced with hydrogen in a mineral acid to give a compound shown by the formula IV, which is acylated and condensed with a cyanoacetamide in the presence of piperidine, etc., in an alcohol to give a compound shown by the formula I wherein one of R<2> and R<3> is pyridyl. |
176 |
2-acyl-4-(4-pyridyl)cyclohexanone and production thereof |
JP29242685 |
1985-12-27 |
JPS61291568A |
1986-12-22 |
MITO KUNIO |
NEW MATERIAL:A 2-acyl-4-(4-pyridyl)cyclohexanone shown by the formula (R1 is methyl or methoxy). EXAMPLE:2-Acetyl-4-(4-pyridyl)cyclohexanone. USE:An intermediate or raw material for producing a novel isoquinoline derivative useful as a cardiac having pharmacological action. PREPARATION:4-(4-Pyridyl)cyclohexanone is acylated to give a 2-acyl-4-(4- pyridyl)cyclohexanone shown by the formula. |
177 |
Isoquinoline derivative bearing sulfone group |
JP6851285 |
1985-04-02 |
JPS61227581A |
1986-10-09 |
HIDAKA HIROYOSHI; SONE TAKANORI |
NEW MATERIAL:An isoquinoline derivative of formula I (A is ethylene unsubstituted or substituted in H atoms bonding to carbon atoms with alkyl of 1-6 carbon atoms, phenyl or benzyl; B is propylene unsubstituted or substituted with 1-6 carbon atoms, phenyl, benzyl; R is H, 1-6C alkyl) and its acid adduct. EXAMPLE:1-(5-Isoquinolinesulfonyl)homopiperazine. USE:It acts on smooth muscles of blood vessels in mammarians and is used as a vasodilator, cerebral circulation improver, remedy for heart attack and as a preventive for cerebral thrombosis and hypertension. PREPARATION:The reaction of 5-isoquinolinesulfonyl chloride of formula VII with a homopiperazine derivative of formula VIII in the presence of an acid acceptor gives the compound of formula I. |
178 |
Direct introduction of trifluoromethyl group to aromatic compound by photo-reaction |
JP14596584 |
1984-07-16 |
JPS6127927A |
1986-02-07 |
SUGIMORI AKIRA; KATO KOJI; AKIYAMA TAKEO |
PURPOSE: To obtain the objective compound directly in one step, using an easily available inexpensive reagent, by irradiating acetonitrile solution of an aromatic compound with light in the presence of trifluoromethyl bromide.
CONSTITUTION: An acetonitrile solution of an aromatic compound selected from naphthalene, anisole, isoquinoline and ferrocence (preferably 6×10
-3W8×10
-3mol/ dm
3 concentration) is irradiated with a high-pressure mercury lamp for about 6hr while introducing trifluoromethyl bromide vapor into the solution to obtain an aromatic compound having trifluoromethyl group. The trifluoromethylation is carried out selectively at the 1-position in the case of naphthalene, and 4-position in the case of anisole.
COPYRIGHT: (C)1986,JPO&Japio |
179 |
JPS6043351B2 - |
JP982674 |
1974-01-24 |
JPS6043351B2 |
1985-09-27 |
PEETERU SENTOMIKUROOSHI; ZORUTAAN MEESAAROSHU; RAASUROO TARUDOSHU; ISHUTOBAAN HERUMETSUTSU; IRONA ERUDEERYUI; AAGOSHUTON DAAUIDO; AARUPAADONEE UASHUBAARI; AAGUNESHU HORUAATO |
|
180 |
JPS6023100B2 - |
JP12880475 |
1975-10-25 |
JPS6023100B2 |
1985-06-05 |
KAARU DARUTON RANSUFUOODO; IN HOO CHEN |
|