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公开(公告)号：JPH06206842A
公开(公告)日：1994-07-26
申请号：JP28971593
申请日：1993-10-14
发明人： TAMURA KUNIO , KATO YOSHIAKI , YOSHIDA MITSUTAKA , SHINSHI OSAMU , OBA YASUHIRO
IPC分类号： A61K31/05 , A61K31/085 , A61K31/22 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/351 , A61K31/352 , A61K31/38 , A61K31/382 , A61K31/435 , A61P3/06 , A61P9/08 , A61P9/10 , C07C43/23 , C07C47/277 , C07C69/157 , C07D307/82 , C07D309/06 , C07D335/02
摘要： PURPOSE:To provide a 4-alkoxy-2,6-di-t-butylphenol derivative having selective high antioxidizing activity, useful as a medicine for arteriosclerosis and cardiac infarction, etc. CONSTITUTION:The compound of formula I [R is H or acyl; R is lower alkyl; R is H or lower alkyl; R to R are each H, (substituted) alkyl, alkenyl, alkynyl or aryl; R and R may be combined into five-membered ring; R and R may be combined into cycloalkyl or heterocyclic group where at least one CH2 group on the cycloalkyl ring has been substituted by O, S or alkyl-substituted N; however, in case the above five-membered ring is benzofuran ring, R is absent], e.g. 2,4,6-tri-t-butyl-5-hydroxybenzofuran. The compound of the formula I can be synthesized from a new intermediate of formula II (A is protecting group; R is H or lower alkyl; m is 0 or 1).
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公开(公告)号：JPH09188619A
公开(公告)日：1997-07-22
申请号：JP29608196
申请日：1996-11-08
发明人： SHINSHI OSAMU , SEKIMORI REIKO , KATO YOSHIAKI
IPC分类号： C07D333/54 , A61K31/085 , A61K31/215 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61P9/00 , A61P43/00 , C07D307/80 , C07D307/94 , C07D333/62 , C07D493/10
摘要： PROBLEM TO BE SOLVED: To obtain a vascular inner membrane hypertrophy depressor manifesting strong propagation-depfessing action against cell propagation induced by a blood serum, etc., in a cultured cell derived from vascular smooth muscle and effective for curing of arctation in a vascular inner membrane hypertrophy after PTCA (percutaneous transluminal coronary angioplasty) containing a 2,6-di-t-butylphenol derivative as an active component. SOLUTION: This vascular inner membrane hypertrophy depressor contains a compound expressed by formula I [X is O or expressed by formula II ((n) is 0, 1 or 2); R1 is H or an acyl; R2 is H or a lower alkyl, etc.; R3 is a lower alkyl; R4 , R5 and R6 are each independently H or an alkyl, etc.; when a ring formed by R3 and R4 together is benzofuran, benzo [b]thiophene, benzo[b]thiophene-1-oxide or benzo[b]thiophene-1,1-dioxide, R6 is not exist], e.g. 4,6-di-t-butyl-2,2-di-n-pentyl-5-hydroxy-2,3-dihydrobenzofuran as an active component.
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公开(公告)号：JP2002275063A
公开(公告)日：2002-09-25
申请号：JP2002036769
申请日：2002-02-14
发明人： SHINSHI OSAMU , SEKIMORI REIKO , KATO YOSHIAKI
IPC分类号： C07D333/54 , A61K31/05 , A61K31/343 , A61K31/351 , A61K31/381 , A61P9/00 , A61P9/10 , C07D307/80 , C07D493/10
摘要： PROBLEM TO BE SOLVED: To obtain a hyperplasia inhibitor for capillary endothelium, especially a medicine useful for treatment and prevention of restenosis detected after coronary angioplasty. SOLUTION: Disclosed is a hyperplasia inhibitor for capillary endothelium featured by containing as an active component a compound represented by formula (1) [wherein, X is oxygen atom or a general formula (2) (wherein, (n) is an integer from 0 to 2); R1 is hydrogen atom or an acyl group; R2 is hydrogen atom, a lower alkyl group or a lower alkenyl group; R3 is a lower alkyl group; R4 , R5 and R6 are each allowable to be same or different and each hydrogen atom or an alkyl group which may have a substituent; and R5 and R6 may also jointly form a cycloalkyl group].
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公开(公告)号：JP2002234839A
公开(公告)日：2002-08-23
申请号：JP2001400184
申请日：2001-12-28
发明人： SHINSHI OSAMU
IPC分类号： C07D307/79 , A61K31/343 , A61P9/10 , A61P35/00
摘要： PROBLEM TO BE SOLVED: To obtain a new prophylactic or a new therapeutic agent for arteriosclerosis having clinically sufficient effects. SOLUTION: This prophylactic or therapeutic agent for the arteriosclerosis comprises a compound represented by general formula (I) (wherein, R1 denotes hydrogen atom, an acyl group or an arylalkoxycarbonyl group; R2 and R4, together with oxygen atom, form a dihydrofuran ring; R3 denotes hydrogen atom; and R5 and R6 may each be the same or different and denote each a linear or a branched chain pentyl group, hexyl group, heptyl group or octyl group, except that R1 and R6 are simultaneously n-pentyl group), its possible optically active substance or a pharmaceutically acceptable salt as an active ingredient.
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公开(公告)号：JPH0296535A
公开(公告)日：1990-04-09
申请号：JP19063788
申请日：1988-08-01
摘要： PURPOSE:To obtain the subject safe remedy, containing a human erythropoietin as an active ingredient and having excellent treating effects. CONSTITUTION:A remedy containing a human erythropoietin(EPO), e.g., human urine EPO obtained by extraction from normal urine or urine or blood plasma of patients suffering from hypoplastic anemia, human gammaEPO prepared by expressing character of a gene capable of coding the amino acid sequence of the human EPO in a host cell or the human EPO obtained from lymphoblastic cells, derived from humans and having the ability to produce the human EPO, as an active ingredient. The dose of the above-mentioned compound is 500-100000U/day for an adult and administered every day or once in at least two weeks. The human EPO is effective in relieving bone marrow dysfunction caused by side effects of a carcinostatic agent (e.g., cisplatin or 5-fluorouracil).
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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
IPC分类号： C07D307/79 , A01N1/02 , A01N43/12 , A61K31/34 , A61K31/343 , A61P13/02 , A61P15/00 , C07D307/94
摘要： 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：JPH1121238A
公开(公告)日：1999-01-26
申请号：JP11297398
申请日：1998-04-23
发明人： SHINSHI OSAMU
IPC分类号： C07D307/79 , A61K31/34 , A61K31/343 , A61P3/00 , A61P3/06 , A61P9/10 , A61P25/00 , A61P27/02 , A61P27/12 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To obtain the subject new preventive and therapeutic agent having clinically sufficient effect by formulating a 2,6-di-t-butylphenol derivative as an active ingredient. SOLUTION: The objective preventive and therapeutic agent is obtained by formulating a 2,6-di-t-butylphenol derivative (e.g. 4,6-di-t-butyl-2,2-di-n-pentyl-5- hydroxy-2,3-dihydrobenzofuran and the like) of the formula [R is H, an acyl and an arylalkoxycarbonyl; R is a lower alkyl; R is H and a lower alkyl; R -R are each H, an alkyl, an alkenyl, an alkinyl, an aryl, etc., or R -R are incorporated together with O to form a furan ring and the like and R and R are together incorporated to form a cycloalkyl or a heterocyclic group] as an active ingredient. The dose of the compound of the formula is generally e.g. 1-1000 mg, preferable 100-300 mg, a day per an adult.
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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
IPC分类号： 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
摘要： 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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公开(公告)号：JPS6232A
公开(公告)日：1987-01-06
申请号：JP2293086
申请日：1986-02-06
发明人： SHINSHI OSAMU , MIZUNO KOJI
IPC分类号： A61K35/22 , A61K35/12 , A61K35/14 , A61K38/00 , A61K38/22 , A61P7/06 , A61P29/00 , C07K14/505
摘要： PURPOSE:An agent containing human erythropoietin as an active constituent and useful as a remedy for chronic rheumarthritis anemia. CONSTITUTION:A remedy containing human erythropoietin as an active constituent. The erythropoietin (hereinafter abbreviated to EPO) is a glycoprotein mainly produced in the kidney and a humoral hematopoietic factor having action of affecting erythroblastic stem cells present in marrow to promote differentiation to erythrocytic cells, but is effective for anemia which is a complication in chronic patients with chronic rheumarthritis. The human EPO can be obtained by various means. Examples thereof include methods of purification from human urine, gene expression of a gene coding amino acid sequence of the human EPO in a host cell, e.g. Escherichia coli, yeast, Chinese hamster, ovarian cell, COS cell, etc. The remedy is normally administered by a method for administering the human EPO pharmaceutical containing 0.1-500mug EPO per adult 1-7times/week.
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