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1.发明授权Dipeptide compounds having pharmaceutical activity and compositions containing them 失效具有药物活性的二肽化合物和含有它们的组合物
公开(公告)号：US4761399A
公开(公告)日：1988-08-02
申请号：US874179
申请日：1986-08-11
IPC分类号： C07D277/06 , A61K38/00 , C07K5/06 , C07K5/078 , A61K31/41
CPC分类号： C07K5/06139
摘要： The compounds of formula ##STR1## wherein the group ##STR2## represents the residue of a natural amino acid selected from the group consisting of glycine, alanine, beta-alanine, phenylalanine, isoleucine, methionine, proline, aspartic acid and arginine; R represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl; and their acid-addition salts with pharmaceutically acceptable organic or inorganic acids; are useful in the preventive and curative treatment of pathologic syndromes due to the lowering of glutathione (GSH) levels.
摘要翻译： PCT No.PCT / EP85 / 00543 Sec。 371日期：1986年8月11日 102（e）日期1986年8月11日PCT提交1985年10月16日PCT公布。 公开号WO86 / 02353 1986年4月24日。式IMA的化合物（I）其中基团IMAGE表示天然氨基酸的残基，其选自甘氨酸，丙氨酸，β-丙氨酸，苯丙氨酸，异亮氨酸，甲硫氨酸 ，脯氨酸，天冬氨酸和精氨酸; R表示氢原子或C1-C4烷基; 和它们与药学上可接受的有机酸或无机酸的酸加成盐; 可用于预防和治疗由于谷胱甘肽（GSH）水平降低导致的病理综合征。
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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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3.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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4.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：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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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：US4806567A
公开(公告)日：1989-02-21
申请号：US72714
申请日：1987-07-13
IPC分类号： C07C319/20 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/22 , A61K31/265 , A61P9/00 , A61P9/08 , A61P9/10 , C07C67/00 , C07C313/00 , C07C323/59 , C07C325/00 , C07C327/34 , C07C153/11
CPC分类号： A61K31/215 , A61K31/265
摘要： A method for the treatment of ischemia and reperfusion syndromes, which consists in administering to a patient in need thereof a therapeutically effective amount of a compound of the formula: ##STR1## in which R is hydrogen or a C.sub.1 -C.sub.6 alkyl group, or of a salt thereof, when R.dbd.H, with a pharmaeutically acceptable base.New compounds and pharmaceutical compositions useful in the method of this invention.
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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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