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公开(公告)号：US4985428A
公开(公告)日：1991-01-15
申请号：US302747
申请日：1989-03-20
IPC分类号： A61K31/42 , A61K31/495 , A61K31/496 , A61P25/28 , C07D20060101 , C07D261/18 , C07D413/12
CPC分类号： C07D261/18 , C07D413/12
摘要： Nootropically active isoxazoles which are certain specified derivatives of N-(5-isoxazolecarbonyl)-4 aminobutyric acid.
摘要翻译： PCT No.PCT / EP88 / 00445 Sec。 371日期1989年3月20日 102（e）日期1989年3月20日PCT提交1988年5月19日PCT公布。 公开号WO88 / 09330 日期为1988年12月1日。作为N-（5-异恶唑羰基）-4-氨基丁酸的某些特定衍生物的精氨酸活性异恶唑。
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公开(公告)号：US4840936A
公开(公告)日：1989-06-20
申请号：US72569
申请日：1987-07-13
IPC分类号： A61K31/425 , A61K31/426 , A61P9/08 , A61P9/10 , A61P11/00 , A61P25/04 , A61P29/00 , C07D277/06 , C07D417/06 , C07K5/078
CPC分类号： C07D417/06 , C07D277/06 , C07K5/06139
摘要： Compounds of formula ##STR1## in which R, R.sub.1 and Y have the meanings shown in the description, their preparation by condensing an aldehyde or a ketone with cysteine or a derivative thereof and their use in the pharmaceutical field.The compounds of formula I possess antipyretic, anti-inflammatory, mucolytic and analgesic activity together with a low capacity to cause gastric injuries.The compounds of formula I, furthermore, are particularly useful in the treatment of ischemia and reperfusion syndromes.
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公开(公告)号：US5028626A
公开(公告)日：1991-07-02
申请号：US322890
申请日：1989-03-15
IPC分类号： A61K38/55 , A61P35/00 , A61P37/00 , A61P43/00 , C07C317/48 , C07C323/32 , C07C323/41 , C07C323/59 , C07C323/63 , C07K1/113 , C07K5/02 , C07K14/575 , C07K14/655
CPC分类号： C07C323/32 , C07C317/48
摘要： Compounds of formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and n have the meanings reported in the specification, processes for their preparation and pharmaceutical compositions containing them as active ingredient are described. The compounds of formula I are inhibitors of enzymatic systems and they are useful in pharmaceutical field.
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4.发明授权
公开(公告)号：US4766137A
公开(公告)日：1988-08-23
申请号：US845694
申请日：1986-03-13
IPC分类号： C07D417/00 , C07D261/08 , C07D261/10 , C07D261/12 , C07D261/18 , C07D417/04 , A61K31/425
CPC分类号： C07D261/10 , C07D261/08 , C07D261/12 , C07D261/18 , C07D417/04
摘要： 4-(isoxazolyl)-thiazole-2-oxamic acids, esters and salts thereof; method for preparing them and intermediate compounds useful for their preparation.Said compounds possess antiallergic and antianaphylactic activity and may be used in the pharmaceutical field.Compositions for pharmaceutical use containing said compounds as the active ingredients are also described.
摘要翻译： PCT No.PCT / EP85 / 00381 Sec。 371日期：1986年3月13日 102（e）日期1986年3月13日PCT提交1985年7月30日PCT公布。 第WO86 / 00900号公报 日期2月13日，1986.4-（异恶唑基） - 噻唑-2-氧杂恶唑酸，其酯和盐; 制备它们的方法和用于其制备的中间体化合物。 所述化合物具有抗过敏和抗过敏活性，可用于制药领域。 还描述了含有所述化合物作为活性成分的药物用组合物。
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5.发明授权N-substituted 1-(4'-alkylsulfonylphenyl)-2-amino-1,3-propanediols, pharmaceutical compositions containing them, having local anesthetic activity 失效N-取代的1-（4'-烷基磺酰基苯基）-2-氨基-1,3-丙二醇，含有它们的药物组合物，具有局部麻醉活性
公开(公告)号：US4632940A
公开(公告)日：1986-12-30
申请号：US637575
申请日：1984-08-03
IPC分类号： A61K31/135 , A61K20060101 , A61K31/095 , A61K31/13 , A61K31/395 , A61K31/495 , A61P25/02 , C07C20060101 , C07C67/00 , C07C313/00 , C07C315/02 , C07C315/04 , C07C317/32 , C07C323/32 , C07D20060101 , C07D241/04 , C07D295/08 , C07D295/10 , C07D295/12
CPC分类号： C07C317/32
摘要： N-substituted derivatives of 1-(4'-alkylsulfonylphenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with local anesthetic activity.
摘要翻译： 1-（4'-烷基磺酰基苯基）-2-氨基-1,3-丙二醇的N-取代衍生物，它们与药学上可接受的有机酸和无机酸的盐，其制备方法，含有它们的药物组合物和可用于其制备的中间体 。 根据本发明的新型衍生物具有局部麻醉活性。
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公开(公告)号：US5145872A
公开(公告)日：1992-09-08
申请号：US323814
申请日：1989-03-15
IPC分类号： A61K38/55 , A61P35/00 , A61P37/00 , A61P43/00 , C07C231/02 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C317/48 , C07C323/41 , C07C323/58 , C07C323/59 , C07K1/113 , C07K5/00 , C07K5/02 , C07K14/575 , C07K14/655
CPC分类号： C07C317/48 , C07K5/0202 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Compounds of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and n have the meanings reported in the specification, processes for their preparation and pharmaceutical compositions containing them as active ingredient are described.The compounds of formula I are inhibitor of enzymatic systems and they are useful in pharmaceutical field.
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7.发明授权1-(4-alkylthiophenyl)-2-(substituted or unsubstituted piperazine-1-yl)-1,3-propanediol, pharmaceutical compositions containing them useful as antiarrhythmic and vasodilating agents 失效1-（4-烷硫基苯基）-2-（取代或未取代的哌嗪-1-基）-1,3-丙二醇，含有它们的药物组合物可用作抗心律不齐和血管舒张剂
公开(公告)号：US4638003A
公开(公告)日：1987-01-20
申请号：US636714
申请日：1984-08-01
IPC分类号： C07D295/10 , A61K31/135 , A61K31/495 , A61P9/06 , A61P9/08 , C07C67/00 , C07C313/00 , C07C323/32 , C07D295/084 , C07D295/12 , C07D241/04
CPC分类号： C07D295/092
摘要： N-substituted derivatives of 1-(4'-alkylthiophenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with calcium antagonist activity and are useful as antiarrhythmic and vasodilating agents.
摘要翻译： 1-（4'-烷硫基苯基）-2-氨基-1,3-丙二醇的N-取代衍生物，它们与药学上可接受的有机酸和无机酸的盐，其制备方法，含有它们的药物组合物和可用于其制备的中间体 。 本发明的新型衍生物具有钙拮抗剂活性，可用作抗心律失常药和血管舒张剂。
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8.发明授权
公开(公告)号：US4960788A
公开(公告)日：1990-10-02
申请号：US354361
申请日：1989-05-19
IPC分类号： C07D207/12 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P23/00 , A61P25/04 , C07D207/26 , C07D211/76 , C07D405/00 , C07D409/00 , C07D409/06 , C07D413/06
CPC分类号： C07D207/26 , C07D211/76 , C07D409/06 , C07D413/06
摘要： Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3 and n have the meanings reported in the specification), their salts with pharmaceutically acceptable acids, process for their preparation and pharmaceutical compositions containing them are described.The compounds of formula I have a remarkable analgesic activity.
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9.发明授权Derivatives of thiazolidine-4-carboxylic acid having pharmacological activity 失效具有药理活性的噻唑烷-4-羧酸的衍生物
公开(公告)号：US4952596A
公开(公告)日：1990-08-28
申请号：US287042
申请日：1988-12-21
IPC分类号： A61K31/425 , A61K31/426 , A61P9/00 , A61P9/10 , A61P11/10 , A61P25/04 , A61P29/00 , C07D277/06 , C07D417/06 , C07D417/10 , C07K5/078
CPC分类号： C07D417/06 , C07D277/06 , C07K5/06139
摘要： Compounds of the formula ##STR1## wherien R, R.sub.1, R.sub.2 and Y have the meanings mentioned in the description, processes for their preparation and their use in the pharmaceutical field are described.The compounds of formula I are endowed with antipyretic, anti-inflammatory, mucolitic and analgesic activity together with good gastric tolerability.In addition, the compounds of formula I are active in the treatment of ischemic or reperfusion syndromes.
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公开(公告)号：US4766138A
公开(公告)日：1988-08-23
申请号：US849458
申请日：1986-03-13
IPC分类号： C07D417/00 , C07D261/08 , C07D261/10 , C07D261/12 , C07D261/18 , C07D417/04 , A61K31/425
CPC分类号： C07D261/10 , C07D261/08 , C07D261/12 , C07D261/18 , C07D417/04
摘要： Use of 4-(isoxazolyl)-thiazole-2-oxamic acid derivatives; method for preparing them and intermediate compounds useful for their preparation.Said compounds possess antiarthritic activity; compositions for pharmaceutical use containing said compounds as the active ingredients are also described.
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