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1. 发明专利

JPH02129169A QUINOLINE COMPOUND AND PHARMACEUTICAL USE THEREOF 失效
公开(公告)号：JPH02129169A
公开(公告)日：1990-05-17
申请号：JP28183088
申请日：1988-11-08
申请人： UBE INDUSTRIES , YOSHITOMI PHARMACEUTICAL
发明人： KUROKI YOSHIAKI , ASADA HIDEKI , ODA HIROYUKI , CHIHARA YASUAKI , IZUMI NORIYOSHI , SHIMADA SHUJI
IPC分类号： C07D215/24 , A61K31/47 , A61K31/495 , A61P3/06 , A61P7/02 , C07D215/38 , C07D215/42 , C07D215/50 , C07D215/52 , C07D401/00
摘要： NEW MATERIAL:The compound of formula I [R is H, carboxyl, 1-22C alkoxycarbonyl, alkylcarbamoyl, alkoxy, amino, group of formula II (R is phenyl or aralkyl), etc.; R is H, lower alkoxy, amino, etc.; R is alkyl, aralkenyl, pyridyl, (substituted) phenyl, etc.], the compound of formula III and their pharmacologically permissible acid addition salts. EXAMPLE:2-Phenyl-4-(4-phenylpyrazin-1-ylmethyl)-5-methoxy-7,8-dihydro- 7,8- dioxoquinoline. USE:An agent for preventing peroxidation of lipid and a platelet coagulation inhibiting agent. PREPARATION:A compound of formula III wherein R is H can be produced by demethylating a compound of formula IV e.g., by treating the compound with boron tribromide in an inert solvent at -78 deg.C to room temperature. The compound of formula I is obtained by the oxidative demethylation of the compound of formula IV with cerium ammonium nitrate, etc.

2. 发明专利

JPH05208948A CYCLOALKYLUREA COMPOUND 失效
公开(公告)号：JPH05208948A
公开(公告)日：1993-08-20
申请号：JP10886892
申请日：1992-04-01
申请人： YOSHITOMI PHARMACEUTICAL
发明人： MISHINA TADASHI , HARADA KYO , YASUOKA JOJI , KUSUHARA HIDENOBU , IZUMI NORIYOSHI
IPC分类号： A61K31/17 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P3/06 , A61P9/10 , C07C275/26 , C07C275/28 , C07C275/30 , C07D213/36 , C07D295/12
摘要： PURPOSE:To obtain a new cycloalkylurea compound having ACAT inhibiting action and useful as a therapeutic agent for hyperlipemia and arteriosclerosis. CONSTITUTION:A compound of formula I [R is formula II (R to R are H or alkyl, with the proviso that two or more groups thereof are not simultaneously H), haloalkyl, alkoxy, phenyl, etc.; R is H or phenyl; R is H, alkyl, cycloalkyl, aralkyl, aralkyloxyalkyl, heteroarylalkyl, a group of formula III or formula IV [(m) is l or 2; R is H or alkyl; R is R or aralkyl], etc.; R4 substituent group is phenyl having alkyl, alkoxy, halogen, amino, etc.; (n) is l-3] or its pharmaceutically permissible salt, e.g. N-(2,6-diisopropylphenyl) N'-(2-phenylcyclohexyl)urea. The compound is obtained by reacting a cycloalkylamine of formula V or its salt with an isocyanic acid ester of formula VI.

3. 发明专利

CA2065086A1 CYCLOALKYLUREA COMPOUNDS 未知
公开(公告)号：CA2065086A1
公开(公告)日：1992-10-05
申请号：CA2065086
申请日：1992-04-03
申请人： YOSHITOMI PHARMACEUTICAL
发明人： MISHINA TADASHI , HARADA KANOU , YASUOKA JOJI , KUSUHARA HIDENOBU , IZUMI NORIYOSHI
IPC分类号： C07C275/28 , C07C275/30 , C07C275/32 , C07C275/40 , C07C323/44 , C07D213/40 , C07D265/30 , C07D295/13 , C07D307/52 , C07D333/22 , C07D333/36 , C07D295/15 , A61K31/17 , C07D319/18 , C07D333/24 , C07D239/26 , A61K31/33 , C07D211/34 , C07D307/54 , C07D213/56 , C07D317/60
摘要： A cycloalkylurea compound of the formula (I): (I) wherein Rl is a group of the formula (a): (a) (wherein R6, R7 and R8 are the same or different and each is hydrogen or alkyl having 1 to 8 carbon atoms, with the proviso that compounds wherein two or three of R6, R7 and R8 are hydrogens are excluded), haloalkyl, cycloalkyl, alkoxy having 1 to 5 carbon atoms, phenyl, aralkyl or heteroaryl, or phenyl, aralkyl or heteroaryl each substituted on the aromatic ring by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 8 carbon atoms, cycloalkyl, cycloalkyloxy, haloalkyl, haloalkoxyl halogen, nitro, amino and substituted amino; R2 is hydrogen, phenyl or phenyl substituted by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, haloalkyl and halogen, whererin R1 and R2 may be substituted on the same carbon atom of cycloalkyl ring; R1 and R2 together may form a substituted or unsubstituted cyclic hydrocarbon having 3 to 7 carbon atoms or a substituted or unsubstituted spiran; R3 is hydrogen, alkyl having 1 to 8 carbon atoms, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, aralkyl substituted by alkylenedioxy, aralkyl, aralkyloxyalkyl, aralkyl or aralkyloxyalkyl each substituted on the aromatic ring by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 5 carbon atoms, halogen, nitro, hydroxy, amino, substituted amino, haloalkyl, alkylthio, benzyloxy and benzylthio, heteroarylalkyl, phenoxyalkyl, or heteroarylalkyl or phenoxyalkyl each substituted on the aromatic ring by 1 to 3 substituents selected from halogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, nitro, amino and haloalkyl, or a group of the formula (c) or (d): (c) (d) wherein m is 1 or 2, R11 is hydrogen or alkyl having 1 to 4 carbon atoms, R12 is hydrogen, alkyl having 1 to 4 carbon atoms or aralkyl; R4 is phenyl substituted by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, haloalkyl, halogen, amino and substituted amino; n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof, which compound inhibits ACAT and is useful as hypolipidemic and antiatherosclerotic medicine.

4. 发明专利

HUT61724A PROCESS FOR PRODUCING CYCLOALKYLUREA COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH ACTIVE INGREDIENT 未知
公开(公告)号：HUT61724A
公开(公告)日：1993-03-01
申请号：HU9201138
申请日：1992-04-03
申请人： YOSHITOMI PHARMACEUTICAL
发明人： MISHINA TADASHI , HARADA KANOU , YASUOKA JOJI , IZUMI NORIYOSHI , KUSUHARA HIDENOBU
IPC分类号： C07C275/28 , C07C275/30 , C07C275/32 , C07C275/40 , C07C323/44 , C07D213/40 , C07D265/30 , C07D295/13 , C07D307/52 , C07D333/22 , C07D333/36 , C07C275/26 , C07D211/06 , A61K31/17 , A61K31/395
摘要： A cycloalkylurea compound of the formula (I): wherein R is a group of the formula (a): (wherein R , R and R are the same or different and each is hydrogen or alkyl having 1 to 8 carbon atoms, with the proviso that compounds wherein two or three of R , R and R are hydrogens are excluded), haloalkyl, cycloalkyl, alkoxy having 1 to 5 carbon atoms, phenyl, aralkyl or heteroaryl, or phenyl, aralkyl or heteroaryl each substituted on the aromatic ring by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 8 carbon atoms, cycloalkyl, cycloalkyloxy, haloalkyl, haloalkoxy, halogen, nitro, amino and substituted amino; R is hydrogen, phenyl or phenyl substituted by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, haloalkyl and halogen, whererin R and R may be substituted on the same carbon atom of cycloalkyl ring; R and R together may form a substituted or unsubstituted cyclic hydrocarbon having 3 to 7 carbon atoms or a substituted or unsubstituted spiran; R is hydrogen, alkyl having 1 to 8 carbon atoms, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, aralkyl substituted by alkylenedioxy, aralkyl, aralkyloxyalkyl, aralkyl or aralkyloxyalkyl each substituted on the aromatic ring by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 5 carbon atoms, halogen, nitro, hydroxy, amino, substituted amino, haloalkyl, alkylthio, benzyloxy and benzylthio, heteroarylalkyl, phenoxyalkyl, or heteroarylalkyl or phenoxyalkyl each substituted on the aromatic ring by 1 to 3 substituents selected from halogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, nitro, amino and haloalkyl, or a group of the formula (c) or (d): wherein m is 1 or 2, R is hydrogen or alkyl having 1 to 4 carbon atoms, R is hydrogen, alkyl having 1 to 4 carbon atoms or aralkyl; R is phenyl substituted by 1 to 3 substituents selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, haloalkyl, halogen, amino and substituted amino; n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof, which compound inhibits ACAT and is useful as hypolipidemic and anti-atherosclerotic medicine.

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