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61. 发明专利

JPH0687738A ANTIFUNGAL AGENT 失效
公开(公告)号：JPH0687738A
公开(公告)日：1994-03-29
申请号：JP26564492
申请日：1992-09-09
申请人： NIPPON KAYAKU KK
发明人： AOYANAGI KAYO , ABE FUMINORI , TOMIYOSHI TSUGIO
IPC分类号： A61K31/16 , A61K31/165 , A61K38/00 , A61P31/04 , A61P31/10 , C07C237/12 , C07C279/12 , C07C279/18 , C07K5/06 , C07K14/195 , C07K14/41 , A61K37/02
摘要： PURPOSE:To obtain an antifungal agent having high stability by containing a spergualin related compound as an active ingredient. CONSTITUTION:The objective antifungal agent contains a compound of formula I {Gu is quanidino; X0 is (CH2)0-5 or phenylene which may be substituted; X1 is (CH2)0-2, CH(R00)-(CH2)0-2 (R00 is H, OH or CH2OH); X2 is NHR2 [R2 is (CH2)1-3COOH], NH(CH2)4N(R01)-(CH2)3-NH-R02 (R01 and R02 are H, amino acid or residue after removing OH from carboxyl of peptide)} and its pharmacologically permissible salt or a compound of formula II [X is (CH2)0-3 or phenylene which may be substituted; m is 0-2; n is 1 or 2; R1 is OH, NH (CH2)1-4COOH] and its pharmacologically permissible salt, e.g. 18-amino-7-(RS)- hydroxy-5,10-dioxo-4,9-diazaoctadecanoic acid as active ingredients. As compounds belonging to the compound of formula I, further compounds of formula III and formula IV are exemplified.

63. 发明专利

JPH0613549B2 失效
公开(公告)号：JPH0613549B2
公开(公告)日：1994-02-23
申请号：JP9541390
申请日：1990-04-10
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： KURODA YOSHIO , IGUCHI HIDEKO , KOSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI , KITAURA YOSHIHIKO , NAKAGUCHI OSAMU , HENMI KEIJI , ARAYA MATSUHIKO , TAKENO SHUICHI , OKADA TATSU , TANAKA HIROKAZU , HASHIMOTO SHINJI
IPC分类号： A61K38/00 , A61K31/195 , A61K31/22 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/455 , A61K39/00 , A61K39/39 , A61P5/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/04 , C07C67/00 , C07C237/12 , C07C237/22 , C07C239/00 , C07C271/22 , C07D207/28 , C07D213/82 , C07D333/24 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/10 , C07K9/00
摘要： This invention relates to the new peptides of the general formula: More particularly, this invention relates to this new peptide and the pharmaceutically acceptable salt thereof, which have pharmacological activities, to processes for the preparation thereof and to a new intermediate for preparing the active peptide, and to the pharmaceutical composition comprising the same and a method of use thereof.

64. 发明专利

JPH0649004A ALKANOYL-L-CARNITINAMIDE DERIVATIVE AND DRUG COMPOSITION 失效
公开(公告)号：JPH0649004A
公开(公告)日：1994-02-22
申请号：JP12372592
申请日：1992-05-15
申请人： SIGMA TAU IND FARMACEUTI
发明人： JIYURIO TARIARATERA , NIKORA FUANTO , MOSE SANTANIERO , KURAUJIO KABAZA
IPC分类号： C07C229/26 , C07C237/12 , C07C237/22 , C07C275/16 , C07C279/14
摘要： Amides of alkanoyl L-carnitines of general formula (1). wherein R is a straight or branched alkanoyl group having from 2 to 8 carbon atoms selected from acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, hexanoyl, 1-methylbutyryl, t-butylacetyl, 2-ethylbutyryl, 3-methylvaleryl, 4-methylvaleryl, 2-ethylhexanoyl and 2-propylpentanoyl; R' is the monovalent residue of a naturally occurring aminoacid selected from: and X is the anion of a pharmacologically acceptable acid are active in regenerating the nervous tissue, inhibiting neuronal degeneration, enhancing the processes of learning and memory and for the treatment of coma. Orally or parenterally administrable compositions in unit dosage form comprise between about 50 and about 500 mg of an amide of formula (1).

65. 发明专利

JPH06500315A 失效
公开(公告)号：JPH06500315A
公开(公告)日：1994-01-13
申请号：JP51367191
申请日：1991-08-13
IPC分类号： A61K31/165 , A61K31/19 , A61K31/245 , A61K31/40 , A61K31/415 , A61P3/06 , A61P9/10 , C07C59/125 , C07C233/47 , C07C233/49 , C07C233/54 , C07C237/12 , C07C237/42 , C07C237/44 , C07C319/20 , C07C323/42 , C07C323/60 , C07C323/63 , C07D207/06 , C07D233/61

66. 发明专利

JPH05310667A 失效
公开(公告)号：JPH05310667A
公开(公告)日：1993-11-22
申请号：JP11033992
申请日：1992-04-28
申请人： MITSUBISHI PETROCHEMICAL CO
发明人： SASAKI NORIO , TAKEHARA JUN , TAKAYAMA YOSHIHIRO , SAWAI NOBUMITSU
IPC分类号： A01N37/44 , C07C237/12 , C07C255/24 , C07C255/46
摘要： PURPOSE:To obtain a new compound used as a germicide for agriculture, especially exhibiting excellent control effects on rice blast and entirely exhibiting no phytotoxicity to rice. CONSTITUTION:A compound of formula I [X is halogen or alkyl; n is 0-3; R and R are H or lower alkyl; R and R are lower alkyl or cycloalkyl; R and R together are -(CH2)m-; m is 4-6; Y is cyano or COOR ; R is lower alkyl], e.g. 2-(2,4-dichloro-3-methylanilino)-N-(1-cyano-1,2-dimethylpropyl)propionic amide. This compound of formula I is obtained by reacting a carboxyl active derivative of formula II with an amino compound of formula III, as necessary, in the presence of a deacidifying agent (e.g. triethylamine) in a solvent (e.g. THF) at -20 deg.C to a reflux temperature of the solvent.

68. 发明专利

JPH04330046A PRODUCTION OF POLYFLUOROALKYL COMPOUND 失效
公开(公告)号：JPH04330046A
公开(公告)日：1992-11-18
申请号：JP10372891
申请日：1991-03-28
申请人： JAPAN RES DEV CORP , TAKEDA YOSHIYUKI
发明人： TAKEDA YOSHIYUKI , WATANABE KYOKO
IPC分类号： C07C235/34 , C07C235/52 , C07C237/12
摘要： PURPOSE:To produce the subject compound having high purity under the perfect inhibition of side-reactions by reacting an alcohol with L-glutamic acid in the presence of a salt-forming agent under azeotropical dehydration, and subsequently subjecting the reactional product to a salt-forming agent-removing reaction, an acylation reaction and a quaternization reaction under a constant temperature in a high pressure atmosphere. CONSTITUTION:A compound of formula: R-X-OH [R is CF3(CF2)n ((n) is 7-13); X is 6-11C hydrocarbon which may contain a double bond, a triple bond or an ether bond at an arbitrary position)] is allowed to react with L-glutamic acid in the presence of a salt-forming agent of formula: QH (Q is p-toluene sulfonium ion, sulfate ion, etc.) (e.g. p-toluene sulfonic acid) under azeotropical dehydration. The obtained compound of formula I is brought into contact with an alkali carbonate aqueous solution in a hydrophobic solvent such as toluene for the removal of the salt-forming agent, and subsequently reacted with a tertiary amine and an omega-halocarboxylic acid active derivative to produce the acylated amide compound of formula II. The compound of formula II is made to react with a tertiary amine such as trimethyl amine at 40-90 deg.C in a high pressure atmosphere to provide a highly pure compound of formula III (e.g. a compound of formula IV).

69. 发明专利

JPH03236318A ANTIDEPRESSANT 失效
公开(公告)号：JPH03236318A
公开(公告)日：1991-10-22
申请号：JP26750390
申请日：1990-10-03
申请人： SIGMA TAU IND FARMACEUTI
发明人： KURAUJIO KABAZA
IPC分类号： A61K31/16 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/255 , A61K31/44 , A61P9/00 , A61P9/04 , A61P25/24 , A61P25/26 , C07C67/00 , C07C227/16 , C07C229/22 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/18 , C07C233/89 , C07C237/06 , C07C237/12 , C07C273/10 , C07C311/46
摘要： PURPOSE: To obtain an antidepressant that contains an acyl-carnitine as an active ingredient, has cerebral neurochemical effect comprising the change in central serotonergic activity and is useful for improving the depression due to sleep disturbance in particular. CONSTITUTION: This antidepressant agent contains, as active ingredient, a new ester of the compound of the formula [R' is acetyl, propionyl, butyryl, isobutyryl, acetoacetyl; R" is methoxy, isopropyloxy, isobutyloxy, trichloroethyloxy, 1- methuyl-2-carbethoxyethyloxy; X is a halogenide ion. The ester of the formula is formulated to pharmaceutical preparations such as tablets, capsules, or solutions and can be administered orally or parenterally.

70. 发明专利

JPH03170399A PRODUCTION OF THIN FILM 失效
公开(公告)号：JPH03170399A
公开(公告)日：1991-07-23
申请号：JP30992389
申请日：1989-11-29
申请人： JAPAN RES DEV CORP , SHIMIZU RYUICHI , ITAMI YASUO
发明人： SHIMIZU RYUICHI , ITAMI YASUO , KUNITAKE TOYOKI
IPC分类号： B05D1/20 , C07C235/12 , C07C237/12 , C09K3/00 , C30B29/54
摘要： PURPOSE:To readily obtain a thin film extended kinds of usable solvents, provided with various kinds of functions and having a regular molecular orientation by dispersing a specific lipid having fluoroalkyl chain as a hydrophobic group in a solvent and then casting the developing solvent. CONSTITUTION:A lipid having fluoroalkyl chain as a hydrophobic group and having a synthetic bimolecular film-forming ability or a regular associated body-forming ability is prepared. Concrete examples of the lipid include a compound expressed by formula I ((n) is 8 and (m) is 2; X is Cl), compound expressed by formula II ((n) is 10 and (m) is 11), etc. Then, by casting a developing solvent (e.g. tetrahydrofuran) dispersing the liquid, a thin film having a regular molecular orientation is obtained. Thereby, according to the purpose it becomes possible to use selectively various kinds of organic solvents in addition to water for dispersing the liquid, because a liquid having hydrophobic properties due to the possession of fluoroalkyl chain as a hydrophobic group is used.

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