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1. 发明专利

JPH11228570A 5-(SUBSTITUTED PHENYL)-4-(3-INDOLYL)IMIDAZOLE DERIVATIVE 失效
公开(公告)号：JPH11228570A
公开(公告)日：1999-08-24
申请号：JP3945998
申请日：1998-02-20
申请人： TAISHO PHARMA CO LTD , SAGAMI CHEM RES
发明人： OTA TOMOKI , NAKANISHI MISA , TOMIZAWA KAZUYUKI , KOBORI TAKEO , HATANAKA YURIKO
IPC分类号： C07D403/04 , A61K31/415 , A61P9/00 , A61P25/00 , A61P25/28 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To provide a new compound that selectively inhibits Ca-calmodulin- dependent phsphoesterase and is useful for improvement of cerebral circulation and central main function for the diseases such as central hypofunction after cerebral blood vessel occlusion, cerebral blood vessel dementia and senile dementia. SOLUTION: This compound is represented by formula I [R is a group of formula II (R is an alkyl, OH or the like) or the like], typically 5-[4-(cyclohexylmethoxy)phenyl]-4-(3-indolyl)-2-phenylimidazole. The compound of formula I is prepared, for example, by condensation reaction between indole-3- glyoxylyl chloride and a compound of the formula: R H [R is a group of formula III (R is an alkyl or the like) and the like] such as (cyclohexylmethoxy) phenyl ether or the like in the presence of a Lewis acid as anhydrous aluminum chloride in a solvent, preferably at 0 deg.C to the refluxing temperature and by reaction of the product with benzaldehyde in the presence of an excessive amount of ammonia or ammonium salt in a solvent, preferably at room temperature to the refluxing temperature.

2. 发明专利

JPH10265460A PHENOXYPYRIDINE DERIVATIVE 失效
公开(公告)号：JPH10265460A
公开(公告)日：1998-10-06
申请号：JP6933097
申请日：1997-03-24
申请人： TAISHO PHARMA CO LTD
发明人： OTA TOMOKI , YOSHIMURA MISA , TAGUCHI MINORU , TOMIZAWA KAZUYUKI
IPC分类号： C07D213/64 , A61K31/44 , A61P9/00 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P43/00 , C07D213/73
摘要： PROBLEM TO BE SOLVED: To obtain a new compound having a specific phenoxypyridine skeleton, further having inhibiting activities against Na /Ca exchange system and useful for treatment and prophylosis of ischemic heart disease such as myocardial infraction. SOLUTION: The objective compound is represented by formula I (X is amino or nitro; R is a lower alkyl, a lower alkoxy, a halogen, etc.; R and R are each H, a lower alkyl, a lower alkoxy, etc.) and exemplified by 2-[4-(4- chlorobenzyloxy) phenoxy]-3-nitropyridine. The objective compound is obtained, for example, by reacting hydroquinone with a compound of formula II (Y is F or Cl) in the presence of a base (e.g. triethylamine) in a reaction solvent (e.g. acetone) at a temperature of 0 deg.C to the reflux temperature to provide a compound of formula III and further reacting the compound of formula III to provide the objective compound.

3. 发明专利

JPH09227555A THIENYLPYRAZOLE DERIVATIVE 失效
公开(公告)号：JPH09227555A
公开(公告)日：1997-09-02
申请号：JP2922296
申请日：1996-02-16
申请人： TAISHO PHARMA CO LTD
发明人： TAGUCHI MINORU , OKUBO TAKETOSHI , YOSHIMURA MISA , HATADA YUICHI , OTA TOMOKI , TOMIZAWA KAZUYUKI
IPC分类号： C07D409/04 , A61K31/495 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D409/14
摘要： PROBLEM TO BE SOLVED: To obtain a thienylpyrazole derivative useful as an antihypertensive medicine, a therapeutic agent for urinary disturbance, etc., having antihypertensive action or improving action on urinary disturbance, by blocking an α 1-adrenaline receptor. SOLUTION: This thienylpyrazole derivative (salt) is shown by formula I [R is H, an alkyl, a group of the formula, (CH2 )m CO2 R (R is H or an alkyl; (m) is an integer of 0-3), a group of the formula, (CH2 )n CONH2 ((n) is an integer of 0-3), a group of the formula, (CH2 )p CN ((p) is an integer of 0-3), a group of formula II ((q) is an integer of 0-3), a (substituted)phenyl or a (substituted) pyridyl; R is a (substituted)phenyl; (1) is an integer of 1-3]. The derivative has antihypertensive action and improving action on urinary disturbance and is useful as an antihypertensive medicine, a therapeutic agent for urinary disturbance, etc. The compound is obtained by reacting a thienone compound of formula III (X1 is a halogen, etc.) with a piperazine, then reacting the reaction product with an aminoacetal to give a compound of formula IV (R and R are each a lower alkyl, etc.) and subjecting the compound to a ring formation reaction.

4. 发明专利

JPH09227524A PHENYLPYRAZOLE DERIVATIVE 失效
公开(公告)号：JPH09227524A
公开(公告)日：1997-09-02
申请号：JP4229596
申请日：1996-02-29
申请人： TAISHO PHARMA CO LTD
发明人： TAGUCHI MINORU , OKUBO TAKETOSHI , HATADA YUICHI , OTA TOMOKI , TOMIZAWA KAZUYUKI
IPC分类号： C07D231/12 , A61K31/415 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To obtain a new phenylpyrazole derivative, having suppressing actions on the contraction of smooth muscles of blood vessels, prostate glands, urethras, etc., due to the blocking of an α1-adrenergic receptor and useful as a hypotensive agent or an improver for dysuria. SOLUTION: This phenylpyrazole derivative is represented by formula I [R is H, a lower alkyl, a lower hydroxyalkyl or phenyl (substitutable with a halogen); R is phenyl (substitutable with a halogen, an alkyl or OH); R is phenyl (substitutable with a halogen, an alkyl or an alkoxy); (m) is 1-3] or its pharmaceutically permissible acid addition salt, e.g. 4-[2-[4-(2- methoxyphenyl)piperazino]ethyl]-1-methyl-5-phenylpyrazole. The compound represented by formula I is obtained by reacting, e.g. a compound represented by formula II with a compound represented by formula III, providing a compound represented by formula I, then reacting the resultant compound represented by formula IV with a compound represented by the formula, (R ) R NCH(OR )2 (R and R are each an alkyl, etc.; R is an alkyl), affording a compound represented by formula V and finally reacting the prepared compound represented by formula V with a compound represented by the formula, R HNNH2 .

5. 发明专利

JPH02167262A 1,4-DIHYDROPYRIDINE DERIVATIVE 失效
公开(公告)号：JPH02167262A
公开(公告)日：1990-06-27
申请号：JP19870089
申请日：1989-07-31
申请人： TAISHO PHARMA CO LTD
发明人： OGAWA TOSHIHISA , OTA TOMOKI , SUNAGA TAKEMI , WATANABE YOSHIAKI , HATAYAMA KATSUO , SATO SHUICHI
IPC分类号： C07D211/90 , A61K31/445 , A61K31/451 , A61P9/12
摘要： NEW MATERIAL:1,4-dihydropyridine derivative expressed by formula I (R is H, alkoxy, mercapto, alkylcarbonylthio or benzoylthio; R is mercapto, alkylcarbonylthio, benzoylthio or 2-cyanoethylthio; A and B are same or different alkylene; X is H, nitro, halogen or trifluoromethyl). EXAMPLE:2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarbo xylic acid 3-methoxymethylester 5-(2acetylthioethyl)ester. USE:The compound has excellent anti-resistance cancer activity and useful as a medicine with small side effect. PREPARATION:For instance, benzaldehyde derivative expressed by formula II, acetoacetate ester expressed by formula III and 3-aminocrotonate expressed by formula IV are heated in an organic solvent to afford the compound expressed by formula I.

6. 发明专利

JPH0283372A CYCLOHEXYLIMIDAZOLE DERIVATIVE 失效
公开(公告)号：JPH0283372A
公开(公告)日：1990-03-23
申请号：JP23396788
申请日：1988-09-19
申请人： TAISHO PHARMA CO LTD
发明人： YOSHIKAWA YOSHINARI , OUCHI YUTAKA , SAITO HIDEJI , OTA TOMOKI , HATAYAMA KATSUO
IPC分类号： C07D233/58 , A61K31/415 , A61P25/04 , A61P29/00 , C07D233/64 , C07D233/84 , C07D409/04
摘要： NEW MATERIAL:A compound shown by formula I [R is cyclohexyl or phenyl; R is butyl, halogenated lower alkyl, thienyl, mercapto, group shown by formula II (R is lower alkyl; n is 0-2), lower alkoxy or nitro- or halogen-substituted phenyl] and a tautomer thereof. EXAMPLE:4(5)-Cyclohexyl-5(4)-phenyl-2-(t-butyl)imidazole. USE:A drug. A compound having high safety and a little side effects such as digestive tract disorder useful as antiphlogistic, antipyretic and analgesic. PREPARATION:A diketone shown by formula IV is reacted with an aldehyde shown by formula IV or an equivalent thereof (hemiacetal) in the presence of excess ammonia or ammonium salt in an organic solvent such as acetic acid at room temperature-the boiling point of the solvent for 30 minutes-3 hours under heating to give a compound shown by formula I wherein R is R mercapto and R is not group shown by formula II.

7. 发明专利

JP2000355537A SODIUM ION/CALCIUM ION EXCHANGE SYSTEM INHIBITOR 失效
公开(公告)号：JP2000355537A
公开(公告)日：2000-12-26
申请号：JP2000115750
申请日：2000-04-17
申请人： TAISHO PHARMA CO LTD
发明人： OTA TOMOKI , NAKANISHI MISA , AIBE IZUMI , TAGUCHI MINORU , TOMIZAWA KAZUYUKI
IPC分类号： A61K31/136 , A61P9/10 , A61P43/00 , C07C217/90
摘要： PROBLEM TO BE SOLVED: To obtain a 2-phenoxyaniline derivative having Na+/Ca2+ exchange system inhibitory effect, and useful for the therapy, prophylactic or the like of ischemic heart diseases, brain diseases, and renal diseases. SOLUTION: This medicinal composition is obtained by including a 2- phenoxyaniline derivative of formula I (R1 is H or a lower alkoxy; R2 and R3 are each a halogen) e.g. 2-[4-(3,4-difluorobenzyloxy)phenoxy]aniline hydrochloride} as an active ingredient. The above-mentioned derivative is obtained by, for example, the following steps: reacting a compound of formula II with 4-hydroxyacetophenone in the presence of a base; reacting the thus produced compound with a peracid followed by deacetylation in the presence of a base, reacting the thus obtained compound with a compound of formula III in the presence of a base, and thereafter reducing the resultant compound of formula IV. The above-mentioned derivative is prepared in the form of tablets, capsules or the like, to make the derivative applicable to oral use or parenteral use. The daily dose thereof is 0.1-1,000 mg.

8. 发明专利

JPH11193263A 2-PHENOXYANILINE DERIVATIVE 失效
公开(公告)号：JPH11193263A
公开(公告)日：1999-07-21
申请号：JP29895098
申请日：1998-10-20
申请人： TAISHO PHARMA CO LTD
发明人： OTA TOMOKI , NAKANISHI MISA , AIBE IZUMI , TAGUCHI MINORU , TOMIZAWA KAZUYUKI
IPC分类号： A61K31/00 , A61K31/135 , A61K31/136 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P43/00 , C07C217/90
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound having a phenoxyaniline skeleton, inhibiting actions on an Na /Ca exchange system and useful for the treatment or prophylaxis of ischemic cardiac diseases such as myocardial infarction, ischemic cerebral diseases such as cerebral infarction or ischemic renal diseases or the cytoprotection at the time of surgical treatment such as angioplasty. SOLUTION: This compound is represented by formula I (R is hydrogen or a lower alkoxy; R is a halogen or nitro; R is hydrogen or a halogen), e.g. 2-[4-(3,4-difluorobenzyloxy)phenoxy]aniline hydrochloride. The compound is obtained by reacting a compound represented by formula II with 4- hydroxyacetophenone in the presence of a base, then reacting the resultant compound with a peracid such as peracetic acid, deacetylating the prepared product in the presence of a base, subsequently reacting the resultant compound represented by formula III with a compound represented by formula IV in the presence of a base and further reducing the obtained product with palladium carbon-hydrogen, etc. The compound represented by formula I is usually administered in a daily dose of 0.1-1,000 mg for an adult.

9. 发明专利

JPH07242628A N-SUBSTITUTED INDOLE DERIVATIVE 失效
公开(公告)号：JPH07242628A
公开(公告)日：1995-09-19
申请号：JP43195
申请日：1995-01-06
申请人： TAISHO PHARMA CO LTD
发明人： KAWASHIMA YUTAKA , OTA TOMOKI , TAGUCHI MINORU , HORIGUCHI AKIYO , HATAYAMA KATSUO
IPC分类号： C07D401/12 , A61K31/495 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D209/14
摘要： PURPOSE:To obtain an N-substituted indole derivative capable of blocking alpha -adrenalin receptor and strongly and continuously exhibiting an antihypertensive effect or a dysuria-improving effect thereby. CONSTITUTION:A compound is expressed by formula I {R and R are H, an alkyl, formula II [R and R are each a lower alkyl; (n') is 1 to 3]; R is a phenyl which may be substituted with one or two halogens, lower alkyls, lower alkoxys or piperidinos or a 2-pyridyl which may be substituted with one or two halogens, lower alkyls or lower alkoxys; R is H or a lower alkyl; R is H or a lower alkoxy; (n) is 1 to 5} and its acid adduct salt, e.g. 1-(2-N,N- diethylamino-2-oxoethyl)-3-{2-[4-(2-methoxyphenyl)piperazinyl]ethyl}in dole dihydrochloric acid salt. This compound can be synthesized by reacting a compound of formula III (X is a halogen or methanesulfonyloxy) with a compound of formula IV (Y is a halogen) in the presence of a base and reacting the resultant compound of formula V with a compound of formula VI in the presence of a base.

10. 发明专利

JPH05139936A HAIR PRODUCING AGENT 失效
公开(公告)号：JPH05139936A
公开(公告)日：1993-06-08
申请号：JP30143491
申请日：1991-11-18
申请人： TAISHO PHARMA CO LTD
发明人： YOKOMORI SADAKAZU , TAKAHASHI TAKEKI , OTA TOMOKI , HASEGAWA MASAHIRO , HATAYAMA KATSUO
IPC分类号： A61K8/00 , A61K8/40 , A61Q5/00 , A61Q7/00 , C07C233/38
摘要： PURPOSE:To obtain a hair producing agent of new type having an excellently trichogenic effects. CONSTITUTION:A hair producing agent having excellently high trichogenic effects blended with 0.05-30wt.%, preferably 0.5-5wt.% based on the whole amount of a preparation of a compound of formula I (R is 6-25C unsaturated hydrocarbon group; R and R are 1-4C alkyl; A is 1-5C alkylene; n is 2, 3 or 4) such as N-{3-[(E)-9-octadeceneamido]propyl}-N,N-dimethylammonio acetato of formula II. The hair producing gent is made into a dosage form such as lotion, milky lotion, cream, gel or aerosol and a proper amount of the agent is applied to scalp several times daily. The hair producing agent can be mixed with substances useful in common hair tonics in a range not to damage the above-mentioned effects besides the above-mentioned essential component.

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