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公开(公告)号:JPH08269056A
公开(公告)日:1996-10-15
申请号:JP10893495
申请日:1995-03-29
Applicant: CHUGAI PHARMACEUTICAL CO LTD
Inventor: KOBAYASHI TAKAMITSU , ISHIKAWA AKIRA , TAMURA KUNIO
IPC: C07D453/02 , A61K31/435 , A61K31/44 , A61P3/06 , A61P43/00
Abstract: PURPOSE: To obtain a new quinuclidine derivative suppressing the biosynthesis of cholesterol by inhibiting squalene formation. CONSTITUTION: This derivative (salt) is shown by formula I [R1 is a (substituted) phenyl or a (substituted) pyridyl; R2 is a 5-9C alkylene, a 5-9C alkenylene or a 5-9C alkynylene; R3 to R5 are: (R3 , R4 , R5 )=(O, H, H), (O-CH2 , H, H) or R4 and R5 are bonded to form a double bond] such as 3- 5-[4-(3-methylphenoxy) phenyl]-2-pentenyloxy}-1-azabicyclo[2,2,2]octane. The derivative, for example, is obtained by reacting a compound of the formula R1 -R2 -X (X is a halogen, an alkylsulfonic acid ester, etc.) with a compound of formula II in an inert solvent in the presence of a base at 0-100 deg.C (preferably 0-25 deg.C) for 1-48 hours (preferably 12-24 hours) to give a compound of formula III and removing the amino-protecting group, borane.
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公开(公告)号:JPH07330759A
公开(公告)日:1995-12-19
申请号:JP12033795
申请日:1995-04-10
Applicant: CHUGAI PHARMACEUTICAL CO LTD
Inventor: KATO YOSHIAKI , ISHIKAWA AKIRA , TAMURA KUNIO
IPC: C07D333/52 , A61K31/38 , A61K31/381 , A61P3/06 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P43/00 , C07D333/56 , C07D333/58 , C09K15/14
Abstract: PURPOSE:To obtain the subject new compound excellent in antioxidation effect and lipid peroxidation inhibitory effect and useful as a therapeutic agent for ischemic organopathy such as arterial sclerosis or cardiac infarction. CONSTITUTION:A compound of formula I [R1 is H, a lower alkyl or an acyl; R2 and R3 are each H, a (substituted) alkyl or a (substituted) alkenyl; R4 is R3, etc.; (n) is 0 to 2] and its salts, e.g. 4,6-ditert-butyl-5-hydroxy-2, 2-dipentyl-2, 3-dihydrobenzothiophene. The compound of formula I is synthesized by converting a compound of formula II as the starting substance into a compound of formula III (R6 and R7 are each a lower alkyl; R8 is R4; R9 is R3), reacting the resultant compound in the presence of a Lewis acid such as boron trifluoride etherate in a solvent such as chloroform at room temperatures to synthesize a compound of formula IV and deprotecting it.
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公开(公告)号:JPH1135568A
公开(公告)日:1999-02-09
申请号:JP14085598
申请日:1998-05-22
Applicant: CHUGAI PHARMACEUTICAL CO LTD
Inventor: ISHIKAWA AKIRA , KATO YOSHIAKI , TAMURA KUNIO , TAKASHIMA YOSHIAKI , SHINSHI OSAMU
IPC: C07D307/79 , A01N1/02 , A01N43/12 , A61K31/34 , A61K31/343 , A61P13/02 , A61P15/00 , C07D307/94
Abstract: PROBLEM TO BE SOLVED: To obtain the subject novel compound that manifests strong cell- protecting action against the cytotoxicity caused by oxidized LDL in the kidney- originating cells and is useful for treatment or prevention of chronic renal failure and diabetic nephropathy and as an internal organ preservative. SOLUTION: This compound is represented by the formula (R1 is H, an acyl which may be substituted; R2 -R4 are each H, a lower alkyl, a lower alkenyl where both of them are not t-butyl, simultaneously; R and R are each H, an alkyl which may be substituted), typically 4,7-di -t-butyl-5 -hydroxy-2, 3- dihydrobenzofuran. This compound is prepared by adding dropwise methanesulfonic acid to a solution of 4-t -butyl-5 -hydroxy-2, 3-dihydrobenzofuran in a mixture of t-butyl alcohol with chloroform followed by extraction, washing and concentration of the product.
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公开(公告)号:JPH1072458A
公开(公告)日:1998-03-17
申请号:JP13376197
申请日:1997-05-23
Applicant: CHUGAI PHARMACEUTICAL CO LTD
Inventor: SHINSHI OSAMU , TAKASHIMA YOSHIAKI , TAMURA KUNIO , ISHIKAWA AKIRA , KATO YOSHIAKI
IPC: C07D333/50 , A01N1/02 , A61K31/085 , A61K31/10 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/38 , A61K31/381 , A61K31/40 , A61P13/02 , A61P15/00 , C07C69/16 , C07C69/712 , C07C323/20 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/94 , C07D333/54 , C07D333/58 , C07D491/107 , C07D493/10 , C07D495/10
Abstract: PROBLEM TO BE SOLVED: To obtain the subject medicine containing a specific 2,6-di-t-butylphenol derivative as an active ingredient, and expressing a strong cell-protecting action on kidney-originated cells and a strong renal function-improving effect in puromycin nephropathy, etc. SOLUTION: This renal disease medicine contains a compound of formula I X is O, a group of formula II [(n) is 0-2]; R1 is H, an acyl; R3 is a lower alkyl; R2 is H, R3 , a lower alkenyl; R4 , R5 are each H, a (substituted)alkyl, a (substituted)aryl, etc.; R6 is R4 , formyl, carboxyl, etc.; R3 and R4 may be combined with each other to form a five-membered ring; when the five- membered ring and the benzene ring in the formula form benzofuran, benzo[b]thiophene, etc., R6 does not exit; R5 and R6 may be combined with each other to form a cycloalkyl group, etc.}, its optical active isomer or salt as an active ingredient. The medicine is preferably administered at a daily active ingredient dose of 1-1000mg once to twice a day for an adult by a (non) oral administration method, a sustained release administration method, etc.
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