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1. 发明专利

JPH07165573A ANTITHROMBOTIC AGENT 失效
公开(公告)号：JPH07165573A
公开(公告)日：1995-06-27
申请号：JP22385494
申请日：1994-09-20
申请人： TANABE SEIYAKU CO
发明人： IWASAKI TAMEO , NISHITANI TAKASHI , OTANI AKIO , INAMASU MASANORI
IPC分类号： A61K31/215 , A61P7/02 , A61P9/00 , A61P9/10 , C07C235/34
摘要： PURPOSE:To obtain an antithrombotic agent, containing a 3-butenoic acid derivative or its salt as an active ingredient, having excellent antithrombotic actions and useful for preventing and treating cardiac infarction, etc. CONSTITUTION:This antithrombotic agent contains a compound expressed by the formula (ring A is a tri-lower alkoxyphenyl; either of R and R is a lower alkoxy and the other is amino) or its salt as an active ingredient. The compound expressed by the formula has excellent promoting actions on the activity of plasminogen activators and inhibiting actions on the activity of plasminogen inhibitor-1 and is capable of manifesting excellent antithrombotic actions by either of the oral and parenteral administrations. Methyl (E)-2-[ (E)-3,4,5- trimethoxybenzyl idene]-3-carbamoyl-4-phenyl-3-butenoate is exemplified as the compound expressed by the formula. The daily dose thereof is 0.1-100mg/kg in the case of the oral administration and 0.01-10mg/kg in the case of the parenteral administration. The agent is useful for preventing and treating cardiac infarction, cerebral apoplexy, pulmonary embolism, deep venous thrombosis, peripheral arterial obstruction, angina pectoris, disseminated intravascular coagulation, venous occlusion, diabetic complications, etc.

2. 发明专利

JPS6138198B2 失效
公开(公告)号：JPS6138198B2
公开(公告)日：1986-08-28
申请号：JP9526179
申请日：1979-07-25
申请人： TANABE SEIYAKU CO
发明人： INOE KAZUMI , IWASAKI TAMEO , NISHITANI TAKASHI
IPC分类号： A61K31/32 , A61P7/00 , A61P9/08 , A61P9/10 , C07F7/22

3. 发明专利

JPS55130975A 55FLUOROURACIL DERIVATIVE AND ITS PRODUCTION 失效
公开(公告)号：JPS55130975A
公开(公告)日：1980-10-11
申请号：JP3894279
申请日：1979-03-30
申请人： TANABE SEIYAKU CO
发明人： INOUE KAZUMI , ARAI YOSHIHISA , IWASAKI TAMEO , NISHITANI TAKASHI
IPC分类号： C07D411/04 , A61K31/505 , A61K31/535 , A61P35/00 , C07D405/04 , C07D413/04
摘要： NEW MATERIAL:5-Fluorouracil derivatives of formula I [X is O, NR (R is lower aliphatic acyl, aroyl, lower alkyloxycarbonyl); Y is O, S, NR , when X is O (R is H, benzyloxycarbonyl), when X is NR , Y is O; A is lower alkylene] and their pharmacologically permissible salts. EXAMPLE:1-(1,4-Dioxacyclohexan-2-yl)-5-fluorouracil. USE:Antitumorigenic agent. PREPARATION:The reaction of a compound of formula II with another compound of formula III (Y' is O, S, benzyloxycarbonylimino; R is lower alkyl) or formula IV (R is lower alkyl) is conducted in the presence of a Lewis acid, preferably stannic tetrachloride or boron trifluoride etherate, when necessary, further a compound of formula V is reduced to give the objective compounds of formula I corresponding to each reaction.

4. 发明专利

JPS54125685A URACIL DERIVATIVE AND ITS PREPARATION 失效
公开(公告)号：JPS54125685A
公开(公告)日：1979-09-29
申请号：JP3120378
申请日：1978-03-17
申请人： TANABE SEIYAKU CO
发明人： INOUE KAZUMI , IWASAKI TAMEO , NISHITANI TAKASHI , HORIKAWA HIROSHI , ARAI YOSHIHISA
IPC分类号： C07D401/04 , A61K31/505 , A61P35/00 , C07D403/04
摘要： NEW MATERIAL:5-Fluorouracil derivative of formula I (R is H, alkyl, aryl, aralkyloxy, aminoalkyl, aralkyloxycarbamoylalkyl; A is lower alkylene), and its salt. EXAMPLE:1-(1-Formylpyrrolidin-2-yl)-5-fluorouracil. USE:Carcinostatic agent. PROCESS:The compound I-A is prepared by reacting a compound II with a compound III (R is H, alkyl, aryl, etc.; X is halogen, lower alkoxy, etc.) in a solvent such as methylene chloride, acetonitrile, etc., in the presence or absence of tin tetrachloride, under cooling or at room temperature.

5. 发明专利

JPH07149642A ANTITHROMBOTIC MEDICINE 失效
公开(公告)号：JPH07149642A
公开(公告)日：1995-06-13
申请号：JP22385394
申请日：1994-09-20
申请人： TANABE SEIYAKU CO
发明人： IWASAKI TAMEO , NISHITANI TAKASHI , OTANI AKIO , INAMASU MASANORI
IPC分类号： C07D207/02 , A61K31/40 , A61P7/02 , A61P9/00 , A61P9/10
摘要： PURPOSE:To obtain an antithrombotic medicine exhibiting excellent antithrombotic action and capable of using as a medicine for preventing and treating a vascular disease such as cardiac infarction and diabetic complication. CONSTITUTION:This antithrombotic medicine contains a 2,5-pyrrolidine-dione derivative of the formula (ring A is a tri-lower-alkoxyphenyl) or its pharmacologically permissible salt, preferably 3-[(E)-benzylidene]-4-[(E)-3,4,5- trimethoxy-benzylidene]-2,5-pyrrolidinedione as an active ingredient. The compound has excellent PA activity-promoting action and PAI-1 activity-inhibiting action and exhibits excellent antithrombotic action in either of oral administration and parental administration unlike a conventional well-known enzyme preparation. The dose of the compound is preferably 0.5-50mg/kg.day in oral administration and preferably 0.05-5mg/kg.day in parental administration. The antithrombotic medicine can be used also as a medicine for preventing re- obstruction after percutaneous coronary artery forming operation or after thrombolytic therapy or a medicine for preventing and treating arteriosclerosis.

6. 发明专利

JPH045264A ETHANOLAMINE DERIVATIVE AND PRODUCTION THEREOF 失效
公开(公告)号：JPH045264A
公开(公告)日：1992-01-09
申请号：JP10707690
申请日：1990-04-23
申请人： TANABE SEIYAKU CO
发明人： SATO TADASHI , IWASAKI TAMEO , NISHITANI TAKASHI , MASAKI YUJI
IPC分类号： C07C213/00 , C07C215/42 , C07C233/23
摘要： NEW MATERIAL:An ethanolamine derivative expressed by formula I or salt of said derivative (ring A is crosslinked cyclic hydrocarbon substitutable with cycloalkane or hydroxy methyl; R is alkyl, alkenyl, saturated aliphatic acyl or unsaturated fatty acyl). EXAMPLE:1-(palitoylamino)cyclopentyl methanol. USE:Useful as preventive and remedy of various diseases having high selectivity and strong inhibiting activity against protein kinase C. For instance, useful as an anti-cancer agent, anti-inflammation agent, platelet aggregation-inhibitor, antihypertensive agent, immunomodulation agent and further as cerebral activator. PREPARATION:For instance, a compound expressed by formula II(ring B is cycloalkane; R is ester residue) is reduced by using a reducing agent, or a compound expressed by formula II (ring C is crosslinked cyclic hydrocarbon; R is H, etc.) is reduced to afford the aimed compound expressed by formula I.

7. 发明专利

JPS58216169A 5-fluorouracil derivative and its preparation 失效
标题翻译： 5-氟尿嘧啶衍生物及其制备
公开(公告)号：JPS58216169A
公开(公告)日：1983-12-15
申请号：JP10097182
申请日：1982-06-11
申请人： Tanabe Seiyaku Co Ltd
发明人： INOUE KAZUMI , IWASAKI TAMEO , NISHITANI TAKASHI , KONDOU KAZUHIKO , ARAI YOSHIHISA
IPC分类号： C07D239/553 , A61K31/505 , A61P35/00 , C07D239/54
摘要： NEW MATERIAL:5-Fluorouracil derivative of formula I (R
1 is H, 1W15C alkyl, lower alkyl substituted with lower alkoxy; R
2 is formyl, lower alkanoyl, halogen-substituted lower alkanoyl; R
3 is lower alkyl, lower alkyl substituted with phenyl-lower-alkoxy; R
4 is lower alkyl, lower alkyl substituted with phenyl- lower-alkoxy) or its salt.
EXAMPLE: N-Acetyl-N-methyl-2-(5-fluorouracil-1-yl)glycine ethyl ester.
USE: Since it has antitumor activity, it is used as a medicine.
PREPARATION: The reaction between 2,4-bis(trimethylsilyl)-5-fluorouracil and a compound of formula II (R
5 is H, 1W5C alkyl; R
6 is formyl; R
7 is lower alkyl; R
8 is lower alkyl; Z is lower alkanoyloxy) in the presence of a Lewis acid gives the compound of formula I .
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：式I的5-氟尿嘧啶衍生物（R 1是H，1-15C烷基，被低级烷氧基取代的低级烷基; R 2是甲酰基，低级烷酰基，卤素取代的低级烷酰基; R 3，是低级烷基，被苯基 - 低级烷氧基取代的低级烷基; R 4是低级烷基，被苯基 - 低级烷氧基取代的低级烷基）或其盐。实施例：N-乙酰基-N-甲基-2-（5-氟尿嘧啶-1-基）甘氨酸乙酯。用途：由于具有抗肿瘤活性，用作药物。制备：2,4-双（三甲基甲硅烷基）-5-氟尿嘧啶与式II化合物（R 5）之间的反应是H，1-5C烷基; R 6是甲酰基; R 7是低级烷基 ; R 8为低级烷基; Z为低级烷酰氧基），在路易斯酸存在下，得到式I化合物。

8. 发明专利

JP2541421B2 失效
公开(公告)号：JP2541421B2
公开(公告)日：1996-10-09
申请号：JP11948192
申请日：1992-03-26
申请人： TANABE SEIYAKU CO
发明人： IWASAKI TAMEO , NISHITANI TAKASHI , OOTANI AKIO , INAMASU MASANORI
IPC分类号： A61K31/215 , A61P7/02 , C07C231/02 , C07C235/34

9. 发明专利

JPH07149643A ANTITHROMBOTIC MEDICINE 失效
公开(公告)号：JPH07149643A
公开(公告)日：1995-06-13
申请号：JP22385594
申请日：1994-09-20
申请人： TANABE SEIYAKU CO
发明人： IWASAKI TAMEO , NISHITANI TAKASHI , OTANI AKIO , INAMASU MASANORI
IPC分类号： C07D401/06 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/535 , A61P7/02 , A61P9/00 , A61P9/10 , C07D207/02 , C07D207/46 , C07D207/50
摘要： PURPOSE:To obtain an antithrombotic medicine exhibiting excellent antithrombotic action and capable of using as a medicine for preventing and treating vascular diseases such as cardiac infarction and diabetic complication. CONSTITUTION:This antithrombotic medicine contains a 2,5-pyrrolidine-dione derivative of the formula (ring A is a trialkoxyphenyl; R is a substitutive alkyl, a substitutive alkoxy, a substitutive amino or pyridinylcarbonyl) or its pharmacologically permissible salt, e.g. (3E,4E)-1-methyl-3-benzylidene-4-(3,4,5- trimethoxybenzylidene)-2,5-pyrrolidinedione as an active ingredient. The compound has excellent PA activity promoting action and PAT-1 activity inhibiting action and exhibits excellent antithrombotic action even in either of oral administration and parental administration. The dose of the compound is preferably 0.5-50mg/kg.day in oral administration and preferably 0.05-5mg/kg.day in parental administration. The antithrombotic medicine can be used also as a medicine for preventing reobstruction after percutaneous coronary artery forming operation or after thrombolytic therapy or a medicine for preventing and treating arteriosclerosis.

10. 发明专利

JP2541420B2 失效
公开(公告)号：JP2541420B2
公开(公告)日：1996-10-09
申请号：JP11948092
申请日：1992-03-26
申请人： TANABE SEIYAKU CO
发明人： IWASAKI TAMEO , NISHITANI TAKASHI , OOTANI AKIO , INAMASU MASANORI
IPC分类号： A61K31/215 , A61P7/02 , C07C231/02 , C07C235/34 , C07C243/32 , C07C259/06

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