| 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 | Method for resolution of benzazepine derivative | JP30304689 | 1989-11-20 | JPH02193970A | 1990-07-31 | JIYON KEI SOTSUTASHIRU |
| PURPOSE: To obtain a cis(+)enantiomer and to effectively reuse the residue by a method wherein a racemic modification of cis and trans enantiomers is reacted with an anhydride and then, is treated with a resolution agent and a new cis body obtd. is crystallized and then, it is treated with a base in the presence of a solvent. CONSTITUTION: A mixture of racemic bodies of cis and trans enantiomers of formula I (R 1 and R 2 are each H, a halogen, an alkyl, an alkoxy, etc.), is treated with an anhydride (e.g. phthalic anhydride, etc.), of formula II (R' and R'' are each H, a benzene ring by both groups) to obtain a new racemic intermediate of formula III and then, it is treated with a resolution agent such as a S-(-)-α- methylbenzylamine to obtain a cis(+)enantiomer of formula I. The resolution agent is returned to the starting material from the filtrate after the product is taken out and a new compd. of formula V from the mother liquor after the racemic bodies are resoluted is returned to the starting material through compd. of formulas VI and VII to effectively reuse them respectively. COPYRIGHT: (C)1990,JPO | ||||||
| 182 | Benzopyranole derivative and pharmaceutical composition | JP20490589 | 1989-08-09 | JPH0283379A | 1990-03-23 | ARUMIN BUARUSERU |
| NEW MATERIAL: A henzopyrazole derivative represented by formula I [wherein A is -C=C-R 6, -CH 2CH 2-R 7(R 6 and R 7 are each heteroaromatic, phenyl, naphthyl or phenanthryl) or a group represented by formula II (R 8-R 10 are each OH, alkyl, alkoxy, hydroxyalkyl or the like and Y is Cl or N), R 1 is H or alkanoyl: R 2-R 4 are each H or alkyl; and R 5 is alkyl] and its salts. EXAMPLE: R(-)-[2-benzo[b]thien-3-yl)ethynyl]-3,4-dihydro-2,5,7,8-tetramethyl-2H- benzo-pyran-6-ol. USE: This new material is a 5-riboxygenase inhibitor, a lipid peroxidation inhibitor and a treatment agent of inflammation, arthrits, allergy, asthma, psoriasis or the like. PROCESS: For example, a compd. represented by formula III and a compd. represented by the formula: R 6X (X is Br, I, etc.), are reacted to obtain a compd. represented by formula I. COPYRIGHT: (C)1990,JPO | ||||||
| 183 | Imidazole derivative | JP15033189 | 1989-06-13 | JPH0242077A | 1990-02-13 | HANSUUJIIDAA SHIYUNAIDAA |
| NEW MATERIAL: 5,6-Dihydrocyclopentathiophenyl-imidazole deriv. of formula I (wherein X is formula II, formula III, etc.; R 1 is H and SH; L is CN, COOH, COOR 8, COSR 8, etc.; R 2 and R 3 are each H, an alkyl, an alkenyl, etc., R 4 and R 5 are each H and an alkyl; R 6 is H, CN, a halogen, an alkyl, NO 2, etc.; R 7 is H, a halogen and an alkyl; R 8 is an alkyl, a cycloalkyl, benzyl, etc.), their stereoisomers and their salts. EXAMPLE: 1-(5,6-Dihydro-5,5-dimethyl-4H-cyclopenta[b]thiopshen-4-yl)-5-imidazole carboxylic acid methyl ester. USE: Selective herbicides. PROCESS: N-cyanoformamidine of formula IV is alkylated with a haloacetate in the presence of a base and the obtd. intermediate product of formula IV is cyclized to obtain a compd. of formula VII and then, diazotization and removal of nitrogen are performed to obtain the compd. of the formula I wherein R 1 is H. COPYRIGHT: (C)1990,JPO | ||||||
| 184 | 3,4-dihydroxy2-pyrrolidinone derivatives and production thereof | JP9901489 | 1989-04-20 | JPH01311060A | 1989-12-15 | GEERUHARUTO KURETSUCHIYUMARU; FURANTSU HOTSUKU |
| NEW MATERIAL: Compds. of formula I [wherein R 1 represents H, 1-8C alkylcarbonyl or the like, R 2 represents H, 1-7C (substituted) alkylaryl, (substituted) heteroaryl or the like (the substituent is CF 3, F or the like); and R 3 represents H, 1-7C alkyl or the like] and salts thereof. EXAMPLE: 1-Benzyl(3R,4R)-3,4-dihydroxy2-pyrrolidinone. USE: Useful in the treatment of Alzheimer's disease and cognition dysfunction caused by senile dementia. PREPARATION: An amine of formula II is reacted with a compd. of formula III to obtain a new amide of formula IV, which is converted into a new compd. of formula V (wherein Z represents a leaving group). This compd. is then, for example, converted into a protected pyrrolidinone derivative of formula VI to obtain the compound of formula I. COPYRIGHT: (C)1989,JPO | ||||||
| 185 | Tricyclic compound | JP29935088 | 1988-11-25 | JPH01308274A | 1989-12-12 | OSHIMA ETSUO; OBASE HIROYUKI; KARASAWA HIROSHI; KUBO KAZUHIRO; MIKI ICHIRO; ISHII AKIO; ISHII HIDEE; OOMORI TAKEMORI |
| NEW MATERIAL:A compound expressed by formula I {X 1-X 2 are CH 2-O, formu la II (l is 0-2), CH 2-CH 2 or CH=CH; W is S or CH; n is 1-4; either of RA and RB is H and the other is Y-M [Y is single bond, CR 1R 2-(CH 2) m (R 1 and R 2 are H or alkyl; m is 0-4), etc.; M is COOR 3 (R 3 is H or alkyl), tetrazolyl, etc.]; GA and GB are alkyl, halogen OH, etc.; gA and gB are 0-3; Z is N-E 1Q (E 1 is single bond, CO, SO 2, etc.; Q is aryl, aralkyl, etc.), etc.; p is 1-3} and salt thereof. EXAMPLE: Methyl 11-[2-(4-phenyl-1-piperazinyl)ethyl]thio-6,11-dihydrodibenz-o[b, e]oxepin-2-carboxylate. USE: A medicinal composition having thromboxane A 2 (TXA 2) antagonistic action with antiallergic or antihistaminic activity in combination. PREPARATION: For example, a compound expressed by formula III (formula IV is formula V) is reacted with a compound expressed by formula VI to afford the compound expressed by formula I (W is S). COPYRIGHT: (C)1989,JPO&Japio | ||||||
| 186 | N-substituted imidazole, its preparation and remedy containing the same and used against estrogen-induced disease | JP7874889 | 1989-03-31 | JPH01290670A | 1989-11-22 | PEETAA SHIYUTOREERUKE; RORUFU BOORUMAN; DEBUITSUTO HENDAASON; NISHINO YUKISHIGE |
| NEW MATERIAL: A compound represented by formula I (wherein R 1 is H, a 1-10C saturated or unsaturated linear or branched hydrocarbon group, a 3-9C cyclohydrocarbon group, a 4-12C cycloalkylalkyl or a 7-10C arylalkyl; R 2 is H, a halogen, CN, methyl which may be substituted, carboxyl which may be in the form of a derivative, a 2-10C alkanoyl which may be substituted or benzoyl which may be substituted; R 3 is H or benzyloxy which may be substituted; and X is CN=N, formula II or S). EXAMPLE: 2-[1-(1-Imidazolyl) butyl]-5bromothiophene. USE: An estrogen biosynthesis inhibitor (aromatase inhibitor). PREPARATION: A compound of formula III (wherein Z is an eliminable group) is reacted with a compound of formula IV (wherein M is H or an alkali metal) to obtain a compound of formula I. COPYRIGHT: (C)1989,JPO | ||||||
| 187 | N-substituted imidazole, its production and remedy containing the same and used against estrogen-induced disease | JP7874989 | 1989-03-31 | JPH01290663A | 1989-11-22 | PEETAA SHIYUTOREERUKE; RORUFU BOORUMAN; DEBUITSUDO HENDAASON; NISHINO YUKISHIGE |
| NEW MATERIAL: A compound of formula I (wherein R 1 is H, a 1-10C hydrocarbon group, a 3-9C cyclohydrocarbon group, a 4-12C cycloalkylalkyl or a 7-12C arylalkyl; R 2 is benzyloxy or the like; and R 3 is CN, a 2-12C alkanoyl, benzoyl, carboxyl or the like) and a salt thereof. EXAMPLE: 4-(2,4-Dichlorobenzyloxy)3-[1-(imidazolyl)butyl] benzonitrile. USE: A remedy against estrogen-induced diseases. PREPARATION: A compound of formula II (wherein Z is an eliminable group) is reacted with a compound of formula III (wherein M is H or an alkali metal atom) in an inert organic solvent such as DMF. to obtain a compound of formula I, which is optionally treated with a carboxyl compound to convert it into the form of an ester, an acid halide, an acid amide or the like. COPYRIGHT: (C)1989,JPO | ||||||
| 188 | N-substituted imidazole, its preparation and remedy against estrogen-induced disease | JP7874789 | 1989-03-31 | JPH01287074A | 1989-11-17 | PEETAA SHIYUTOREERUKE; RORUFU BOORUMAN; DEBUITSUDO HENDAASON; NISHINO YUKISHIGE |
| NEW MATERIAL: An N-substituted imidazole of formula I (wherein R 1 is H, a 1-10C saturated or unsaturated linear or branched hydrocarbon group, a 3-9C cyclohydrocarbon group, a 4-12C cycloalkylalkyl or a 7-10C arylalkyl; R 2 is a 1-10C substituted linear or branched saturated or unsaturated hydrocarbon group, formyl which may be in the form of a derivative, a 2-10C substituted or unsubstituted alkanoyl, benzoyl or carboxyl) and a salt thereof. EXAMPLE: 4-[1-(1Imidazolyl)butyl] benzoic acid methyl ester. USE: Useful as an inhibitor for the biosynthesis of estrogen. For example used for the treatment of breast cancers, prostatauxe, etc., used to inhibit ovulation and also used to treat male sterility. PREPARATION: A compound of formula II (wherein Z is an eliminable group) is reacted with a compound of formula III (wherein M is H or the like) to obtain a compound of formula I. COPYRIGHT: (C)1989,JPO | ||||||
| 189 | JPH01501935A - | JP50230387 | 1987-04-03 | JPH01501935A | 1989-07-06 | |
| 190 | JPH01500433A - | JP50469687 | 1987-07-27 | JPH01500433A | 1989-02-16 | |
| 191 | Anhydrous crystal sodium salt of 5-chloro-3-(2-thenoyl)-2-oxyindole-1-carboxamide and manufacture | JP2267588 | 1988-02-02 | JPS63201184A | 1988-08-19 | DAGURASU JIYON MERUDORAMU AREN; BURAIAN TOOMASU ONIIRU |
| 192 | JPS63501941A - | JP50029687 | 1986-12-12 | JPS63501941A | 1988-08-04 | |
| 193 | JPS62501709A - | JP50076886 | 1986-01-23 | JPS62501709A | 1987-07-09 | |
| 194 | JPS6220167B2 - | JP7459875 | 1975-06-20 | JPS6220167B2 | 1987-05-06 | KAARU HAINTSU BYUTSUHERU; MANFURETSUTO PURENPERU |
| 195 | JPS62501004A - | JP50501485 | 1985-10-25 | JPS62501004A | 1987-04-23 | |
| 196 | JPS61501991A - | JP50493585 | 1985-10-21 | JPS61501991A | 1986-09-11 | |
| 197 | Optically active ketal compound, manufacture and synthesis of alpha-aryl saturated fatty carboxylic acid therewith | JP7127185 | 1985-04-05 | JPS60228440A | 1985-11-13 | KURAUDEIO GIORUDANO; GURAJIANO KASUTARUDEI; FURUBIO UGERI; SHIRUBIA KABITSUCHIORI |
| 198 | JPS6039677B2 - | JP11572275 | 1975-09-26 | JPS6039677B2 | 1985-09-06 | MERUBIN HARISU ROZEN |
| 199 | JPS58502216A - | JP50034083 | 1982-12-30 | JPS58502216A | 1983-12-22 | |
| 200 | JPS57502215A - | JP50034082 | 1982-01-21 | JPS57502215A | 1982-12-16 | |
QQ群二维码
意见反馈
意见反馈