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41. 发明专利

JPH089617B2 失效
公开(公告)号：JPH089617B2
公开(公告)日：1996-01-31
申请号：JP50186891
申请日：1990-12-27
IPC分类号： A61K31/52 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/48 , A61K31/522 , A61P9/04 , A61P9/08 , A61P11/08 , A61P37/08 , C07D239/54 , C07D473/04 , C07D473/06
摘要： Xanthines of the general formula: wherein R represents a straight or branched chain alkyl, alkenyl or alkynyl group of 3-6 carbon atoms, and R and R , which may be the same or different, each represent hydrogen or halogen or a methyl, methoxy, nitro or trifluoromethyl group or R and R together form a methylenedioxy or ethylenedioxy group; with the proviso that R and R are not both hydrogen; and pharmacologically acceptable salts thereof with an alkali metal base or a nitrogen base containing organic base, are bronchodilators making them of value in treating asthma and vasodilators making them of interest in treating angina, hypertension, congestive heart failure and multi-infarct dementia. The compounds are also of use in combatting other conditions where inhibition of PDE type IV is thought to be beneficial. The compounds can be prepared by treating the corresponding 6-amino uracil with sodium nitrite and formic acid in an excess of formamide and adding sodium dithionate to reduce the resulting 6-amino-5-nitroso compound to give the 5,6-diamino compound that ring closes with the excess of formamide.

43. 发明专利

JPH07107063B2 失效
公开(公告)号：JPH07107063B2
公开(公告)日：1995-11-15
申请号：JP41802990
申请日：1990-12-21
IPC分类号： A61K31/52 , A61K31/522 , A61P9/08 , C07D473/04 , C07D473/06 , C12P17/18 , C12P41/00 , C12R1/865

44. 发明专利

JPH0788382B2 失效
公开(公告)号：JPH0788382B2
公开(公告)日：1995-09-27
申请号：JP50411386
申请日：1986-07-08
IPC分类号： C07D473/00 , A61K31/52 , A61K31/522 , A61P3/00 , A61P9/00 , A61P9/08 , A61P25/28 , C07D473/04 , C07D473/06 , C07D473/08

45. 发明专利

JPH0788381B2 失效
公开(公告)号：JPH0788381B2
公开(公告)日：1995-09-27
申请号：JP9495786
申请日：1986-04-25
IPC分类号： C07D473/04 , A61K31/52 , A61K31/522 , A61P9/00 , A61P11/00 , A61P43/00 , C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22

46. 发明专利

JPH07188231A CYCLOPROPANE DERIVATIVE AND ANTIVIRAL AGENT CONTAINING THE DERIVATIVE 失效
公开(公告)号：JPH07188231A
公开(公告)日：1995-07-25
申请号：JP28464794
申请日：1994-11-18
申请人： AJINOMOTO KK
发明人： SEKIYAMA TAKAAKI , IKEMURA OSAMU , ONISHI TOMOYUKI , TSUJI HISASHI , IWAYAMA SATOSHI , SUZUKI KATSUYA , OMURA HIROKO , OKUNISHI MASAHIKO
IPC分类号： C07D473/04 , A61K31/52 , A61K31/522 , A61P31/12 , C07D473/16 , C07D473/18 , C07D473/28 , C07D473/32 , C07D473/34 , C07D473/40
摘要： PURPOSE:To obtain a new cyclopropane derivative useful as an antiviral agent having excellent solubility in water, oral absorbability and therapeutic effect. CONSTITUTION:This cyclopropane derivative is a compound of formula I [R and R each is H or a group of formula II (R is a 1-6C alkyl); R and R are not H at the same time; X is H, OH, NH2 or a halogen; Y is H, OH or NH2] or its pharmacologically permissible salt, e.g. 9-[1'S,2'R-bis(O-L-alanyloxymethyl) cyclopropan-1'beta-yl]methylguanine. The compound of formula I wherein both R and R are group of formula II can be produced by carrying out dehydrative condensation of a cyclopropane derivative of formula III with an N-protected amino acid of formula IV (Z is amino-protecting group) in a polar solvent using a condensation agent and deprotecting the protecting group of the amino group of the obtained ester.

48. 发明专利

JPH05294965A 失效
公开(公告)号：JPH05294965A
公开(公告)日：1993-11-09
申请号：JP12134892
申请日：1992-04-15
申请人： JAPAN ENERGY CORP
发明人： HIROTA KOSAKU , ISOBE YOSHIAKI , CHIBA SHINSUKE , YAMAMOTO SHIGEKO
IPC分类号： A61K31/505 , A61P11/00 , A61P13/02 , A61P15/00 , C07D473/04
摘要： PURPOSE:To provide a new compound effective in removing active oxygen formed in the body, having excellent bronchodilating action and diuretic action and useful for the treatment of asthma, nephritis, etc. CONSTITUTION:The compound of formula I (R and R are H, lower alkyl, lower alkoxy, substituted phenyl or cyclohexyl; R is 1-4C lower alkyl or lower alkoxy), e.g. 8-(3,5-di-t-butyl-4-hydroxyphenyl)-1,3-dimethylxanthine. The compound of formula I can be produced by reacting a compound of formula II with a compound of formula III.

50. 发明专利

JPH05105631A ANTIDEMENTIAL AGENT 失效
公开(公告)号：JPH05105631A
公开(公告)日：1993-04-27
申请号：JP26774891
申请日：1991-10-16
申请人： KYOWA HAKKO KOGYO KK
发明人： SUZUKI FUMIO , KATO HIROMASA , SHIMADA JUNICHI , ISHII AKIO , SHIOZAKI SHIZUO
IPC分类号： A61K31/52 , A61K31/522 , A61P25/28 , C07D473/04
摘要： PURPOSE:To obtain an antidemential agent containing a xanthine derivative or its pharmacologically permissible salt as an active component. CONSTITUTION:The objective agent contains, as an active component, the compound of formula I (R is lower alkyl; R is substituted or unsubstituted cycloalkyl) or its pharmacologically permissible salt, e.g. 3-(4-aminophenetyl)-1- propyl-8-cyclopentylxanthine. The compound of formula I can be produced by reacting a compound of formula II (P is protecting group) with a compound of the formula R CO2H, cyclizing the obtained compound of formula III by treating with a dehydration agent or by heating and deprotecting the reactional product.

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