序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
81 Quinone derivative JP23705190 1990-09-10 JPH03188042A 1991-08-16 ABE SHINYA; OKAMOTO YASUSHI; TAGAMI KATSUYA; HIBI SHIGEKI; NAGAGAWA JUNICHI; HIROTA KAZUO; HISHINUMA TAKAHARU; MIYAMOTO KANAME; YAMANAKA TEIJI; YOKOHAMA HIROMITSU; YOSHIMURA TSUTOMU; HORIE TORU; AKITA HASHINORI; KATAYAMA KOICHI; YAMATSU ISAO
NEW MATERIAL:A compound expressed by formula I {A is formula II, formula III [R 3 to R 5 are H, alkyl or alkoxy; X and Y are OH or formula IV (n is 0 or 1; R 6 is alkyl)]; R 1 is alkyl, cycloalkyl, alkenyl, alkynyl, arylalkyl, (CH 2) 1-10-CN, etc.; R2 is O-R 8 (R 8 is H or alkyl), NR 9R 10 (R 9 and R 10 are H, alkyl, heteroaryl, etc.)} or salt thereof. EXAMPLE: (E)-3-[5-(6-Methyl-1-methoxymethyloxy-2, 3, 4-trimethoxy) phenyl]-2- nonyl-2-propenoic acid. USE: A remedy for lever disease. PREPARATION: For example, an aldehyde derivative expressed by formula V is subjected to Wittig reaction with a posphonate expressed by formula Vl in the presence of a base to provide the compound expressed by formula I (A is formula III). COPYRIGHT: (C)1991,JPO&Japio
82 JPH0335306B2 - JP2379884 1984-02-10 JPH0335306B2 1991-05-27 HASHIMOTO KINJI; GOTO KYOTO; TSUDA YOSHIAKI
83 Cyclocondensation quinone derivative JP2186388 1988-02-03 JPH01197453A 1989-08-09 TATSUOKA TOSHIO; SUZUKI KENJI; SATO FUMIO; MIYANO SEIJI; SUMOTO KUNIHIRO
NEW MATERIAL:A cyclocondensation quinone derivative shown by formula I (R 1, R 2 and R 3 are H, methyl or methoxy; R 4 is hydroxymethyl or carboxyl which may be amidated or esterified; X is H, halogen, lower alkyl or methoxy; Y is CH 2 or O) or a hydroquinone derivative thereof. EXAMPLE: 1,2,3,4-Tetrahydro-4-(3,4-dimethoxy-6-methyl-2,5-benzoquinonyl)-2- naphthoic acid. USE: A drug useful for improving and treating diseases based on organic disorder in the brain. A small of the drug is orally administered. Low toxicity. PREPARATION: For example, a substituted benzaldehyde is reacted with succinic anhydride to give a butyrolactonecarboxylic acid derivative shown by formula II, which is esterified, reduced and then subjected to ring closure to give a tetralone derivative shown by formula IV. This derivative is reduced and treated with a dehydrating condensation agent to give a lactone shown by formula VI, which is condensed with a hydroquinone derivative shown by formula VII to give a compound shown by formula I wherein Y=CH 2. COPYRIGHT: (C)1989,JPO&Japio
84 JPH0120126B2 - JP1462887 1987-01-23 JPH0120126B2 1989-04-14 IMADA ISUKE; TERAO SHINJI; KAWADA MITSURU; SHIRAISHI MITSURU
85 Remedy for hepatic disease JP1936587 1987-01-28 JPS63185921A 1988-08-01 MIZOGUCHI YASUHIRO; MAKI YOSHITAKA
PURPOSE: To obtain a remedy for hepatic diseases, by using a quinone derivative or its hydroquinone compound as an active component. CONSTITUTION: The objective remedy for hepatic diseases contains a compound of formula (R 1 and R 2 are methyl, methoxy or together form -CH=CH-CH=CH-; R 3 is methyl, hydroxymethyl or (esterified) carboxyl; Z is -C≡C- or -CH=CH-; m and n are 0W10; k is 1W5; when n is 2 or 3, Z and k may be arbitrarily varied in the recurring unit in the parentheses [ ]) or its hydroquinone compound as an active component. Since the compound of formula has strong 5- lipoxygenase-inhibiting and antioxidation effects and low toxicity, it is useful for the prevention and remedy of chronic heptatitis, fulminant hepatitis, hepatofibrosis, hepatocirrhosis, alcoholic hepatitis, etc. It is administered by oral or parenteral administration preferably at a rate of 0.2W20mg/kg per dose and 1W3 doses daily. COPYRIGHT: (C)1988,JPO&Japio
86 Thromboxane a2 receptor antagonist JP24790086 1986-10-17 JPS63101322A 1988-05-06 TERAO SHINJI; NISHIKAWA KOHEI
PURPOSE: To provide the titled antagonist containing a quinone derivative having bulky group on the α-carbon of a side chain or its hydroquinone compound as an active component, resistant to inactivation by metabolism in living body and capable of keeping effective drug concentration in blood over a long period. CONSTITUTION: The objective agent contains a quinone derivative of formula [R 1 and R 2 are methyl, methoxy or together form -CH=CH-CH=CH-; R 3 is (substituted) phenyl, naphthyl or thienyl; R 4 is carboxyl or a group which can be converted to carboxyl group in living body; n is 3W15] or its hydroquinone compound, e.g. 7-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-7-phenylheptanoic acid, as an active component. The agent is useful as a remedy and preventive for diseases caused by the insulfficiency or disorder of the function of circulation system or peripheral circulation system. It is convenient to administer 0.1W20mg/kg weight of the active component once or twice a day in the case of oral administration to an adult patient. COPYRIGHT: (C)1988,JPO&Japio
87 JPS6247176B2 - JP11777179 1979-09-12 JPS6247176B2 1987-10-06 TERAO SHINJI; SHIRAISHI MITSURU; KATO KANEYOSHI
88 Medicine containing quinone compound as active component JP1462887 1987-01-23 JPS62174010A 1987-07-30 IMADA ISUKE; TERAO SHINJI; KAWADA MITSURU; SHIRAISHI MITSURU
PURPOSE: To provide a medicine containing a specific quinone compound as an active component, having excellent characteristics such as low toxicity and fat-solubility and high absorbability and useful as a hypotensor, remedy for cardiopathy, bronchodilator, cerebul circulation improver, etc. CONSTITUTION: The objective medicine contains, as an active component, the compound of formula I [the α-β bond is a) saturated bond or b) double bond; R is CH 3, OCH 3 or two R groups together form CH=CHCH=CH; n is integer of 0W9; R 2 is H or OH when the bond α-β is a) and is H when the bond is b); R 1 is COOH, (CH 2) mOH or group of formula II when the α-β bond is b) or R 2 is OH or R 1 is CH 2OH or group of formula II when the bond α-β is a) and R 2 is H; m is 1, 2 or 3]. The compound has various pharmacological activities such as bio-membrane stabilizing action, electron-transfer action, hypotensive action, cardiomegalyinhibiting action, bronchial muscule relaxing action, cerebral circulation improving action, cerebral ischemia preventive action, etc., and is useful as the above medicines for the prevention and remedy of hypertension, cardiac insufficiency, asthma, cerebral apoplexy, etc. COPYRIGHT: (C)1987,JPO&Japio
89 JPS61501388A - JP50393084 1984-10-19 JPS61501388A 1986-07-10
90 Quinone derivative JP17052085 1985-07-31 JPS6144840A 1986-03-04 TERAO SHINJI; MAKI YOSHITAKA
NEW MATERIAL:The quinone derivative or hydroquinone compound of formula I (R<1> and R<2> are H, methyl or methoxy, or R<1> and R<2> together form -CH= CH-CH=CH-; R<3> is H or methyl; R<4> is (substituted) aliphatic group, aromatic group or heterocyclic group; R<5> is methyl, methoxy, hydroxymethyl or carboxy; Z is C=C, CH=CH, group of formula II, formula III, etc.; n is 0-10; m is 0-3; k is 0-5). EXAMPLE:6-(3,5,6-Trimethyl-1,4-benzoquinon-2-yl)-6-(2-thienyl)hexanoic acid ethyl ester. USE:Antiasthmic agent, antiallergic agent or cerebral cardio-vascular system improver. PREPARATION:The compound of formula I can be prepared by reacting the compound of formula II (R<6> is H, methyl, methoxymethyl, benzyl, etc.; R<7> is H, OH, methoxy, methoxymethyloxy, etc.) with an oxidizing agent.
91 Quinone compound JP10137083 1983-06-06 JPS59225138A 1984-12-18 TERAO SHINJI; MAKI YOSHITAKA
NEW MATERIAL:A quinone compound shown by the formula I (R is methyl, or methoxy; Y is formyl, carboxyl, 2W5C alkoxycarbonyl, carbamoyl, mono- or di- 1W4C alkylcarbamoyl, or carbamoyloxymethyl group) or its hydroquinone derivative. EXAMPLE: 2,3,5-Trimethyl-6-(11-carboxyundecane-5,10-diynyl)-1,4-hydroquinone. USE: Having inhibitory action on production of particularly fatty acid peroxide, inhibitory action on production of SRS-A (slow reacting substance of anaphylaxis), useful as a drug such as antiasthmatic, antiallergic, hypotensor, antiulcer, diuretic, etc. PREPARATION: For example, a compound shown by the formula II (R 1 is lower alkyl, benzyl group, etc.) is deprotected, to give a compound shown by the formula I . COPYRIGHT: (C)1984,JPO&Japio
92 Novel 1,4-benzoquinones JP7415583 1983-04-28 JPS58203935A 1983-11-28 FUREDERITSUKU HARORUDO HAUERU
93 Benzoquinone derivative JP6222482 1982-04-13 JPS58177934A 1983-10-18 TERAO SHINJI; OKAZAKI NAOYOSHI; IMADA ISUKE
NEW MATERIAL:The benzoquinone derivative of formula I [R 1 and R 2 are methyl or methoxy; n is 0W21; m is 0 or 1; Z is CH 2N(R 3)R 4 [R 3 and R 4 are H, alkyl or morpholino of N(R 3)R 4], COR 5 (R 5 is α-amino acid residue or glucosamine residue), group of formula II (R 6 is residue of bivalent hydrocarbon), formula III or formula IV (l is 1W4; R 7 is OH, methoxy or methyl]. EXAMPLE: 3-(2,4-Dimethoxy-5-methyl-1,4-benzoquinon-6-yl)propionylglycine. USE: Pharmaceuticals having protocollagen-proline hydrolase-inhibiting and collagen biosynthesis-suppressing activities, etc. Remedy for arteriosclerosis, hepatocirrhosis, scleroderma, keroid, nodose rheumatism, etc. PROCESS: The compound of formula I can be prepared e.g. by oxidizing the compound of formula V [X is H or (protected) OH; Y is (protected) OH] if necessary after removing the protecting group. COPYRIGHT: (C)1983,JPO&Japio
94 Quinones and their preparation JP4995680 1980-04-15 JPS56147746A 1981-11-16 IMADA ISUKE; OKUYA TETSUYA; WATANABE MASAZUMI
NEW MATERIAL:A compound shown by the formula I (n is 10W21; R is H or lower alkyl). EXAMPLE: 2, 3-Dimethoxy-6-( 12-methoxycarbonyldodecyl )-5-methyl-1, 4-bezoquinone. USE: Having hypotensive actions, tissue metabolism activating actions, immune adjusting actions, lysosome membrane stabilizing actions, and SRS-A actions, useful as a remedy for cardiac incompetence, remedy for cerebral circulation disorder, immune adjusting agent, and antiallergic agent. PROCESS: A compound shown by the formula II is reacted with a peroxide of a compound shown by the formula III or its anhydride in an inert solvent, e.g., n-hexane, etc. at 80W100°C, to give a compound shown by the formula I. Forms of drugs are capsules, granules, powder, tablets, etc., and the antiallergic agent is an ointment, aerosol, inhalant, etc. A dose per adult a day is 5W500mg. COPYRIGHT: (C)1981,JPO&Japio
95 1,4-naphthoquinone derivative, its preparation, and its use JP2967580 1980-03-06 JPS56125335A 1981-10-01 IKUSHIMA KOUICHI; TANAKA HIROKAZU; OOE OSAMU; IGUCHI HIDEKO; MUKOUZAKA MASANOBU; AOKI HATSUO; ARAKAWA HIROSHI; IMANAKA HIROSHI
NEW MATERIAL:A 1,4-naphthoquinone derivative of formula I [R<1> is H, OH, lower alkoxy, or arylthio; R<2> is carboxy, esterified carboxy, or amidated carboxy; or R<1> and R<2> together form -O-C(=O)-; R<3> is H or lower alkyl; R<4> is lower alkyl; R<5> is H or halogen; R<6> is H, lower alkyl, or lower alkanoyl], or its salt at the carboxyl group. EXAMPLE:8-Hydroxy-1-methoxy-3-methyl-7,12-dihydro-5H-benzo[d]naphtho [2,3-b] pyran-5,7,12-trione. USE:Preventive and remedy for coccidiosis. PROCESS:The compound of formula I' (R<1> and R<2> particular groups defined in the formula I) is separated from the cultured product obtained by culturing bacteria belonging to Streptomyces genus and capable of producing the compound of formula I', e.g. Streptomyces auranticolor No.5995, in a culturing medium.
96 Quinone compound and its preparation JP11777179 1979-09-12 JPS5640651A 1981-04-16 TERAO SHINJI; SHIRAISHI MITSURU; KATOU KANEYOSHI
NEW MATERIAL:A compound of formula I (n is an integer 1W10; R 1 is methyl, methoxy, or two R 1s form -CH=CH-CH=CH-; R 2 is amino) or a hydroquinone form thereof. EXAMPLE: The compound of formula II (n is 1; R 2 is a group of formula III). USE: A hypotensive agent, an analgesic agent, an antitumor agent, an anti-inflammatory agent, a diuretic agent and an immune regulator having a regulating action on biosynthesis of prostaglandin, an inhibitory action on SRS-A (a slow-reacting substance of anaphylaxis) and an adrenergic blocking action. PROCESS: A carboxylic acid of formula IV or V or a reactive derivative at the carboxyl group thereof is reacted with a compound of the formula R 2-H in the presence of an active condensing agent, e.g. N,N'-dicyclohexylcarbodiimide, in an organic solvent, e.g. dichloromethane, at -20W150°C to give the compound of formula I. COPYRIGHT: (C)1981,JPO&Japio
97 JPS50148325A - JP5000374 1974-05-02 JPS50148325A 1975-11-27
98 JPS5026529B1 - JP8762270 1970-10-06 JPS5026529B1 1975-09-01
99 JPS5095244A - JP151974 1973-12-25 JPS5095244A 1975-07-29
100 JPS5010574B1 - JP6693870 1970-07-30 JPS5010574B1 1975-04-22
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