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91. 发明专利

JPS6310768A PYRAZINE DERIVATIVE AND INHIBITOR OF BLOOD PLATELET AGGREGATION CONTAINING SAME 失效
公开(公告)号：JPS6310768A
公开(公告)日：1988-01-18
申请号：JP27987286
申请日：1986-11-26
申请人： TERUMO CORP
发明人： WAKABAYASHI TOSHIO , HASEGAWA HIROKAZU , OOTA AKIHIRO
IPC分类号： C07D405/06 , A61K31/495 , A61P7/02 , C07D241/12 , C07D409/06
摘要： NEW MATERIAL:A pyrazine derivative shown by formula I [X is H, halogen, lower alkyl, lower alkoxy or di- lower alkylamino; R is H or lower alkyl; R is lower alkyl, benzyl which may be replaced with (lower alkyl, lower alkoxy or methylenedioxy) or thienyl which may be replaced with (lower alkyl, lower alkoxy or methlenedioxy); a case wherein R is H and R is methyl is omitted]. EXAMPLE:2,3-Bis(p-chlorophenyl)-5-ethylpyrazine. USE:Useful as an inhibitor of blood platelet aggregation and an anti-inflammatory drug having inhibitory action on blood platelet aggregation and inhibitory action on cyclooxygenase, capable of being orally administered and intravenously injected. PREPARATION:A compound shown by formula II and a compound shown by formula III are heated in an organic solvent and the prepared compound shown by formula IV is heated in the presence of S at 100-180 deg.C to give a compound shown by formula I.

92. 发明专利

JPS62228059A AMIDE DERIVATIVE AND ANTIALLERGIC AGENT CONTAINING SAME 失效
公开(公告)号：JPS62228059A
公开(公告)日：1987-10-06
申请号：JP9663886
申请日：1986-04-28
申请人： TERUMO CORP
发明人： TAKAI MAKOTO , OMORI KAZUHIRO , HATTORI MAKOTO , KUMONAKA YASUHIRO , OZAWA SHINJI , WAKABAYASHI TOSHIO
IPC分类号： C07D295/12 , A61K31/443 , A61K31/445 , A61K31/495 , A61P37/08 , C07D211/14 , C07D211/26 , C07D211/44 , C07D211/46 , C07D211/58 , C07D295/13 , C07D405/12
摘要： NEW MATERIAL:The amide derivative of formula I [R and R are lower alkyl benzyl, tetrahydrofuranyl, lower alkoxy-lower alkyl or lower alkoxycarbonyl; R is H or lower alkoxy; n is 1 or 2; Y is group of formula II, III or IV (X and X are H, halogen or lower alkoxy; n, p and q are 1-4)]. EXAMPLE:1-{1-[5-( 3-Methoxy-4-ethoxycarbonyloxyphenyl )-2,4-pentadienoyl]am inoethyl}-4-benzhydroxypiperidine. USE:Useful as an antiallergic agent effective against allergic symptoms such as allergic asthma, allergic rhinitis, etc. PREPARATION:The compound of formula I can be produced e.g. by reacting the carboxylic acid derivative of formula V with the amine derivative of formula VI in the presence of a condensation agent at room temperature.

93. 发明专利

JPS62221621A COMPLEX TRANSFUSION SOLUTION 失效
公开(公告)号：JPS62221621A
公开(公告)日：1987-09-29
申请号：JP6649686
申请日：1986-03-24
申请人： TANABE SEIYAKU CO , TERUMO CORP
发明人： SAMEJIMA MASAYOSHI , MATSUDA SABURO , WAKABAYASHI TOSHIO , HAYAKAWA NAOKI
IPC分类号： A61K31/165 , A61K9/08 , A61K31/195 , A61K31/198 , A61K31/40 , A61K31/405 , A61K31/415 , A61K38/00 , A61P3/00 , A61P3/12
摘要： PURPOSE:A complex transfusion solution, containing a reducing sugar, physiological amino acids and electrolytes at composition ratios balanced within specific ranges and capable of exhibiting nutritionally improved effect and suppressing the browning phenomenon by the Maillard reaction. CONSTITUTION:A complex transfusion solution obtained by blending a reducing sugar, preferably glucose or maltose which is a physiological caloric source with an amino acid mixture which is a nitrogen source and electrolytes in amounts blended shown in the table. Cysteine and/or cystine in the amino acid mixture may be partially or wholly replaced by methionine and tyrosine may be partially or wholly replaced by phenylalanine. The concentration of the reducing sugar is preferably within the range of 6-8wt/vol% and the concentration of the total amino acids is preferably within the range of 2.5-3.5wt/vol%. From the viewpoint of the stabilization of the pharmaceutical, the respective concentrations are preferably adjusted to give 7-25, particularly 17-23 product of the concentrations of both the reducing sugar and total amino acid.

94. 发明专利

JPS62205052A NITRIC ACID ESTER DERIVATIVE AND VASODILATOR CONTAINING SAME 失效
公开(公告)号：JPS62205052A
公开(公告)日：1987-09-09
申请号：JP4815886
申请日：1986-03-05
申请人： TERUMO CORP
发明人： KUMONAKA YASUHIRO , SUWABE YASUSHI , TAGUCHI SHIGERU , WAKABAYASHI TOSHIO
IPC分类号： C07C233/57 , A61K31/21 , A61P9/08 , A61P9/10 , C07C67/00 , C07C231/00 , C07C233/12 , C07C235/28
摘要： NEW MATERIAL:The compound of formula I (R is H or 1-5C alkyl; m is 1 or 2; n is 2-5). EXAMPLE:N-(beta-hydroxyethyl)-5-(3,4,5-trimethoxyphenyl)-2,4-pentadienoic acid amide nitric acid ester. USE:A vasodilator for the remedy of coronary vessel disorder, cerebral vessel disorder and peripheral vessel disorder, etc., to which increase of blood flow rate is effective. PREPARATION:The compound of formula I can be produced by reacting 5-(3,4,5- trimethoxyphenyl)-2,4-pentadienoic acid thiazolidinethionamide with the compound of formula II.

95. 发明专利

JPS62195370A 5-FLUOROURACIL DERIVATIVE AND DRUG PREPARATION CONTAINING SAME 失效
公开(公告)号：JPS62195370A
公开(公告)日：1987-08-28
申请号：JP3622486
申请日：1986-02-20
申请人： TERUMO CORP
发明人： WAKABAYASHI TOSHIO , SHIMIZU MASAKI , INOUE KAZUHITO , KANEKO KIMIYOSHI , KATAYAMA HAJIME
IPC分类号： C07D239/553 , A61K31/505 , A61P7/02 , A61P35/00 , C07D239/54
摘要： NEW MATERIAL:A 5-fluorouracil derivative shown by formula I (R is H or 1-3C alkyl; R is acyl derived from linoleic acid, triene higher fatty acid or pentaene higher fatty acid). EXAMPLE:1-[2-(9,12,15-Octadecatrienoylamino)ethoxy]methyl-5-fluorouracil. USE:A carcinostatic agent, and an inhibitor of blood platelet aggregation and further a preventive against thrombosis, cancer metastasis, etc. PREPARATION:2,4-Ditrimethylsilyloxy-5-fluoro-pyrimidine is condensed with a compound shown by formula II, the subjected to azide formation reaction with sodium azide and further subjected to reaction using both the above- mentioned higher fatty acid and triphenylphosphine to give a compound shown by formula I.

96. 发明专利

JPS62106019A ANTI-HYPERLIPEMIC AGENT 失效
公开(公告)号：JPS62106019A
公开(公告)日：1987-05-16
申请号：JP24579485
申请日：1985-11-01
申请人： TERUMO CORP
发明人： TAKAHASHI KEIKO , WAKABAYASHI TOSHIO
IPC分类号： C07D213/80 , A61K31/4406 , A61K31/455 , A61P3/06 , A61P9/10
摘要： PURPOSE:To provide an anti-hyperlipemic agent containing a specific ethanolamine derivative as an active component, having remarkable effect to lower serum lipid level, useful for the prevention of diseases caused by high lipid level in serum, especially arteriosclerosis, myocardial infarction, etc., and having high safety. CONSTITUTION:The objective anti-hyperlipemic agent contains the ethanolamine derivative of formula (R is H or acyl derived from triene higher fatty acid or eicosapentaene higher fatty acid). The triene higher fatty acid is preferably alpha-linolenic acid or gamma-linolenic acid. The compound of formula can be produced by condensing a triene higher fatty acid, a pentaene higher fatty acid or their reactive derivative with ethanolamine. The compound of formula exhibits remarkable activity to lower the lipid level in serum. It is used especially as a preventive for arteriosclerosis, myocardial infarction and cerebral infarction. Dose: preferably 300-2,000mg daily.

97. 发明专利

JPS61122270A Amide derivative and inhibitor of 5-lipoxygenase-action containing same 失效
标题翻译：含有5-LIPOXYGENASE作用的酰胺衍生物和抑制剂
公开(公告)号：JPS61122270A
公开(公告)日：1986-06-10
申请号：JP24569584
申请日：1984-11-20
申请人： Terumo Corp
发明人： WAKABAYASHI TOSHIO , TAKAI MAKOTO , ICHIKAWA HIDEJI , ARAI JUNICHIRO , MUROTA SEIITSU
IPC分类号： C07D211/46 , A61K31/445 , A61K31/495 , A61K31/52 , A61K31/522 , A61P37/08 , A61P43/00 , C07D209/00 , C07D211/00 , C07D295/18 , C07D401/06 , C07D473/08 , C12N9/99
CPC分类号： Y02P20/55
摘要： NEW MATERIAL:A compound expressed by formula I [(R) represents 3,4- dihydroxy, 3-methoxy-4-hydroxy, 3,4-dimethoxy, 3,5-dimethoxy-4-hydroxy, 3,4- dimethoxy-4-toluoyloxy or 3,4,5-trimethoxy; n is 1 or 2 which means the number of double bond in trans configuration; Y represents formula II or formula III (n is 3 or 4 in both formulae)]. EXAMPLE:7-{4-{-[3-(3,4-Dihydroxyphenyl-2-propenoyl]piperaz-in-1-yl}but hyl}theo phylline. USE:An inhibitor of 5-lipoxygenase-action useful as an antiallergic agent controlling biosynthesis of an allergy pathopoietic factor of leukotrienes such as leukotrienes C4 and D4. PREPARATION:A compound expressed by formula IV or V is reacted with piperidine, and the resultant compound is condensed with a theophylline derivative, followed by eliminating reaction of protecting groups to obtain the compound expressed by formula I.
摘要翻译：新材料：由式I [（R）m表示的化合物表示3,4-二羟基，3-甲氧基-4-羟基，3,4-二甲氧基，3,5-二甲氧基-4-羟基，3,4 - 二甲氧基-4-甲苯酰氧基或3,4,5-三甲氧基; n为1或2，表示反式构型中的双键数; Y表示式II或式III（两式中n为3或4）]。实施例：7- {4 - { - [3-（3,4-二羟基苯基-2-丙烯酰基）哌嗪-1-基}但是羟基线。使用：5-脂氧合酶作用抑制剂可用作控制白三烯C4和D4等白三烯过敏药物生物合成的抗过敏药。制剂：将式IV或V表示的化合物与哌啶反应，将所得化合物与茶碱衍生物缩合，然后除去保护的反应以获得由式I表示的化合物。

98. 发明专利

JPS61106564A Unsaturated fatty acid amide derivative and inhibitor of blood platelet aggregation containing same 失效
标题翻译：不饱和脂肪酸酰胺衍生物和血液平滑肌细胞抑制剂
公开(公告)号：JPS61106564A
公开(公告)日：1986-05-24
申请号：JP22827284
申请日：1984-10-30
申请人： Terumo Corp
发明人： HOTODA KATSUMI , TAKAHASHI KEIKO , WAKABAYASHI TOSHIO
IPC分类号： C07D295/18 , A61K31/495 , A61P7/02
CPC分类号： Y02P20/55
摘要： NEW MATERIAL:An unsaturated fatty acid amide derivative shown by the formula I [R
1 is H, or methyl; R
2 is H, or methyl, and when R
1 is H, R
2 is also H; m is number of double bonds in trans configuration, 1 or 2; Y is group shown by the formula II (n is 2, 4, or 4; X is acyl derived from either triene higher fatty acid or pentaene higher fatty acid), or group shown by the formula III]. E X A M P L E : 1 - [ N - [ 3 - ( 3 - Methoxy-4-hydroxy)phenyl]-2-propenoyl]-β-aminoethyl]-4-(5,8,11,14,17-eicosapentaenoyl)piperazine.
USE: An inhibitor of blood platelet aggregation.
PREPARATION: For example, a carboxylic acid derivative shown by the formula IV (R
1 is methyl, or methoxyethoxymethyl; R
2 is R
1 ) or a reactive derivative shown by the formula V is subjected to a condensation reaction and a protecting group removing reaction, to give a compound shown by the formula I.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：新材料：式I所示的不饱和脂肪酸酰胺衍生物[R 1]为H或甲基; R 2是H或甲基，当R 1是H时，R 2也是H; m是反式构型中的双键数，1或2; Y为式II所示的基团（n为2,4或4; X为衍生自三烯高级脂肪酸或五烯基高级脂肪酸的酰基）或式III所示的基团。 E X A M P L E：1- [N- [3-（3-甲氧基-4-羟基）苯基] -2-丙烯酰基] - 氨基乙基] -4-（5,8,11,14,17-二十碳五烯酰基）哌嗪。用途：血小板聚集抑制剂。制备例如式IV所示的羧酸衍生物（R 1为甲基或甲氧基乙氧基甲基; R 2为R 1）或式V所示的反应性衍生物进行缩合反应和保护基除去反应，得到式I所示的化合物。

99. 发明专利

JPS60222419A FAT TRANSFUSION SOLUTION 失效
公开(公告)号：JPS60222419A
公开(公告)日：1985-11-07
申请号：JP7718784
申请日：1984-04-17
申请人： TERUMO CORP
发明人： WAKABAYASHI TOSHIO , OKAMOTO KAZUO , KUNIMASA MEGUMI
IPC分类号： A61K31/23 , A61P3/06 , A61P9/00 , A61P9/10 , C07C69/587
摘要： PURPOSE:A fat transfusion solution, containing an ester of gamma-linolenic acid, having better lowering action on blood cholesterol than the commercially available fat transfusion solution, and useful as a transfusion solution for conditions of diseases capable of treating or preventing asteriosclerosis. CONSTITUTION:A fat transfusion solution containing an ester of gamma-linolenic acid, preferably triglyceride containing gamma-linolenic acid as a component or ethyl linolenate. Evening primrose oil may be cited as the fat containing mainly the triglyceride containing the gamma-linolenic acid as a component. The transfusion solution has lowering action on blood cholesterol, and can be used as a preventing and treating agent for arteriosclerosis, i.e. hardening of the main artery or coronary artery, cardiac infarction, cerebral thrombosis, hyperlipemia, etc.

100. 发明专利

JPS60152454A AMIDE DERIVATIVE AND 5-LIPOXIGENASE INHIBITOR CONTAINING SAID DERIVATIVE AS ACTIVE COMPONENT 失效
公开(公告)号：JPS60152454A
公开(公告)日：1985-08-10
申请号：JP657684
申请日：1984-01-18
申请人： TERUMO CORP
发明人： WAKABAYASHI TOSHIO , KUMONAKA YASUHIRO , ICHIKAWA HIDEJI , MUROTA SEIITSU
IPC分类号： C07D295/18 , A61K31/165 , A61K31/195 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P11/00 , A61P37/08 , A61P43/00 , C07C235/34 , C07D211/74 , C12N9/99
摘要： NEW MATERIAL:The compound of formula I (when R is H, R is piperidyl, morpholyl, 4-oxopiperidyl, etc.; when R is methyl, R is morpholyl, 2-hydroxycarbonylanilino, 4-oxopiperidyl, etc.). EXAMPLE:N-Caffeoyl piperidine. USE:Useful as an inhibitor for 5-lipoxigenase activity, i.e. an antiallerigic agent (e.g. remedy for allergic asthma, allertic rhinitis, etc.). It suppresses the production of leucotrienes which are critical factors of allergy. PREPARATION:The compound of formula I can be prepared by reacting the compound of formula II (R is methoxyethoxymethyl or methyl) with an amine such as piperidine, and eliminating the methoxyethoxymethyl group with hydrous acetic acid, trifluoroacetic acid, etc.

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