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公开(公告)号:US4342760A
公开(公告)日:1982-08-03
申请号:US196830
申请日:1980-10-14
IPC分类号: A61K31/535 , A61K31/545 , A61K31/546 , A61P31/04 , C07D205/085 , C07D205/095 , C07D498/04 , C07D501/14 , C07D501/18 , C07D501/20 , C07D505/00 , C07F9/40 , C07F9/568
CPC分类号: C07F9/5683 , C07D205/085 , C07D205/095 , C07D505/00 , C07F9/568 , Y02P20/55
摘要: The invention deals with Cephalosporin Analogues of the formula: ##STR1## wherein R.sup.1 is amino or amino substituted with a pharmaceutically acceptable carboxylic acyl protective group for the amino substituents in cephalosporin compounds or with benzyl, phenethyl or trityl, andR.sup.2 is carboxy or a pharmaceutically acceptable ester of said carboxy group employed in cephalosporin compounds, and pharmaceutically acceptable salts thereof, and their use as antimicrobial agents.
摘要翻译: 本发明涉及下列化学式的头孢菌素类似物:其中R 1是氨基或氨基被药学上可接受的羧基酰基保护基取代,用于头孢菌素化合物中的氨基取代基或与苄基,苯乙基或三苯甲基,R2是羧基或药学上 用于头孢菌素化合物的所述羧基的可接受的酯及其药学上可接受的盐及其作为抗微生物剂的用途。
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公开(公告)号:US4497801A
公开(公告)日:1985-02-05
申请号:US529646
申请日:1983-09-06
申请人: Masashi Hashimoto , Keiji Hemmi , Daijiro Hagiwara
发明人: Masashi Hashimoto , Keiji Hemmi , Daijiro Hagiwara
IPC分类号: A61K38/00 , C07K7/06 , C07K14/42 , C07K14/575 , C07K14/66 , A61K37/00 , C07C103/52
CPC分类号: C07K7/062 , C07K14/42 , C07K14/57581 , C07K14/66 , A61K38/00
摘要: Peptides of the following formulae:H-THR-LYS-GLU-LYS-LEU-LYS-SER-GLU-LEU-VAL-ALA-ASN-OH, H-GLU-LEU-LYS-SER-GLU-LEU-VAL-ALA-ASN-OH, H-LYS-LEU-LYS-SER-GLU-OH,are effective in the treatment of bacteria viral infection.
摘要翻译: 下式的肽:H-THR-LYS-GLU-LYS-LEU-LYS-SER-GLU-LEU-VAL-ALA-ASN-OH,H-GLU-LEU-LYS-SER-GLU-LEU-VAL- ALA-ASN-OH,H-LYS-LEU-LYS-SER-GLU-OH可有效治疗细菌病毒感染。
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公开(公告)号:US4264597A
公开(公告)日:1981-04-28
申请号:US43706
申请日:1979-05-30
IPC分类号: A61K31/535 , A61K31/545 , A61K31/546 , A61P31/04 , C07D205/085 , C07D205/095 , C07D498/04 , C07D501/14 , C07D501/18 , C07D501/20 , C07D505/00 , C07F9/40 , C07F9/568
CPC分类号: C07F9/5683 , C07D205/085 , C07D205/095 , C07D505/00 , C07F9/568 , Y02P20/55
摘要: Compounds of the formula ##STR1## wherein X is --O--or --S--;R.sup.1 is amino or a substituted amino group;R.sup.2 is carboxy or a protected carboxy group; and the heavy solid line means single or double bond; the compounds are useful in the treatment of infectious diseases particularly fungal infection, in human beings and animals.
摘要翻译: 其中X是-O - 或 - S-的式IMAMA的化合物; R1是氨基或取代的氨基; R2是羧基或被保护的羧基; 重实线表示单键或双键; 该化合物可用于治疗人类和动物中的感染性疾病,特别是真菌感染。
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公开(公告)号:US4234724A
公开(公告)日:1980-11-18
申请号:US972382
申请日:1978-12-22
IPC分类号: C07D205/08 , A61K31/397 , A61K31/535 , A61P31/04 , C07D205/085 , C07D277/20 , C07D277/40 , C07D505/00 , C07F9/6561 , C07D498/04
CPC分类号: C07D505/00
摘要: Cephalosporin analogues represented by the formula ##STR1## wherein R.sup.1 is amino or a substituted amino,R.sup.2 is carboxy or a protected carboxy, andR.sup.3 is hydrogen or lower alkoxy, processes for making the same, azetidinone intermediates and pharmaceutical compositions comprising said cephalosporin analogues as active ingredients.
摘要翻译: 由式(I)表示的头孢菌素类似物,其中R 1是氨基或取代的氨基,R 2是羧基或保护的羧基,R 3是氢或低级烷氧基,制备其的方法,氮杂环丁酮中间体和药物组合物, 头孢菌素类似物作为活性成分。
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公开(公告)号:US4350694A
公开(公告)日:1982-09-21
申请号:US134346
申请日:1980-03-27
IPC分类号: C07D205/08 , A61K31/397 , A61K31/535 , A61P31/04 , C07D205/085 , C07D277/20 , C07D277/40 , C07D505/00 , C07F9/6561 , C07D265/12
CPC分类号: C07D505/00
摘要: This invention relates to cephalosporin analogues and pharmaceutically acceptable salts thereof, of high antimicrobial activity.
摘要翻译: 本发明涉及高抗微生物活性的头孢菌素类似物及其药学上可接受的盐。
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公开(公告)号:US4369312A
公开(公告)日:1983-01-18
申请号:US279546
申请日:1981-07-01
IPC分类号: C07D499/00 , C07D501/04 , C07D503/00 , C07D505/00
CPC分类号: C07D505/00 , C07D499/00 , C07D503/00 , Y02P20/55
摘要: This invention relates to a novel method of producing oxo-containing azetidinone compounds, or salts thereof, or hydrates thereof, said compounds having utility as antimicrobial agents and as intermediates for the synthesis of other azetidinone compounds having antimicrobial activity.
摘要翻译: 本发明涉及一种生产含氧的氮杂环丁酮化合物或其盐或其水合物的新方法,所述化合物具有作为抗微生物剂的作用,以及用于合成具有抗微生物活性的其它氮杂环丁酮化合物的中间体。
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公开(公告)号:US5633232A
公开(公告)日:1997-05-27
申请号:US258456
申请日:1994-06-10
申请人: Masaaki Matsuo , Daijiro Hagiwara , Hiroshi Miyake
发明人: Masaaki Matsuo , Daijiro Hagiwara , Hiroshi Miyake
IPC分类号: A61K38/00 , A61K38/06 , A61P11/00 , A61P25/04 , A61P27/02 , A61P29/00 , A61P43/00 , C07K1/02 , C07K5/02 , C07K5/078 , C07K5/097 , A61K38/05
CPC分类号: C07K5/06165 , C07K5/0202 , C07K5/06139 , A61K38/00
摘要: Disclosed herein are compounds of the following formula: ##STR1## wherein R.sup.1 is a group of the formula ##STR2## "X" is CH.sub.2 or N, "Z" is O, S, or N--R.sup.6, "A" is an amino acid residue, and Y, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are substituent variables as defined herein.The compounds are antagonists of tachykinin, and as such are useful for alleviation of pain and for treatment of disorders including asthma, bronchitis, rhinitis, conjunctivitis, dermatitis, arthritis, and urticaria.
摘要翻译: 本文公开的是下式的化合物:其中R 1是下式的基团:X是CH 2或N,“Z”是O,S或N-R 6,“A”是氨基 酸残基,Y,R2,R3,R4,R5,R6和R7是本文定义的取代基变量。 这些化合物是速激肽的拮抗剂,因此可用于缓解疼痛和用于治疗包括哮喘,支气管炎,鼻炎,结膜炎,皮炎,关节炎和荨麻疹的疾病。
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公开(公告)号:US4010178A
公开(公告)日:1977-03-01
申请号:US607759
申请日:1975-08-26
申请人: Takashi Kamiya , Masumi Itoh , Daijiro Hagiwara
发明人: Takashi Kamiya , Masumi Itoh , Daijiro Hagiwara
IPC分类号: C07D207/16 , C07D249/18 , C07K1/06
CPC分类号: C07D249/18 , C07D207/16 , C07K1/06
摘要: Carbonic acid esters of the formula substituent(s) substituents(s)R'.sub.1 OCOOR'.sub.2wherein R'.sub.1 is lower alkyl which may have substituent)s) selected from the group of halogen, lower alkoxy and aryloxy, or ar(lower)-alkyl which may have substituents)s) selected from the group of lower alkoxy, halogen, nitro and cyano, andR'.sub.2 is benzotriazolyl which may have halogen; or a group represented by the formula: ##STR1## wherein Y' and Z' are each cyano, nitro, carbamoyl, esterified carboxy, lower alkanoyl, aroyl or disubstituted carbamoyl; provided that whenR'.sub.2 is a group represented by the formula: ##STR2## wherein Y' and Z' are each cyano, nitro, carbamoyl or esterified carboxy, R'.sub.1 is ar(lower) alkyl having substituent(s) selected from the group of lower alkoxy, halogen, nitro and cyano.A process for the protection of amino and/or imino groups in compounds containing them by reacting them with the aforementioned esters is also disclosed.
摘要翻译: 式(1)的碳酸酯取代基R'1OCOOR'2其中R'1是可以具有取代基的低级烷基,s)选自卤素,低级烷氧基和芳氧基,或Ar(低级) 可以具有选自低级烷氧基,卤素,硝基和氰基的取代基的烷基),R'2是可具有卤素的苯并三唑基; 或由下式表示的基团:其中Y'和Z'各自为氰基,硝基,氨基甲酰基,酯化羧基,低级烷酰基,芳酰基或二取代的氨基甲酰基; 条件是当R'2是由下式表示的基团时:其中Y'和Z'各自为氰基,硝基,氨基甲酰基或酯化羧基,R'是具有选自以下的取代基的芳基(低级)烷基: 低级烷氧基,卤素,硝基和氰基。
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公开(公告)号:US5883098A
公开(公告)日:1999-03-16
申请号:US884039
申请日:1997-06-27
申请人: Masaaki Matsuo , Daijiro Hagiwara , Takashi Manabe , Nobukiyo Konishi , Shinji Shigenaga , Kenji Murano , Hiroshi Matsuda , Hiroshi Miyake
发明人: Masaaki Matsuo , Daijiro Hagiwara , Takashi Manabe , Nobukiyo Konishi , Shinji Shigenaga , Kenji Murano , Hiroshi Matsuda , Hiroshi Miyake
IPC分类号: C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D417/06 , C07D417/14 , A61K31/495
CPC分类号: C07D401/06 , C07D241/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D417/06 , C07D417/14
摘要: A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl;Y is a direct bond or lower alkylene; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.
摘要翻译: 下式的哌嗪化合物:其中:X为羰基或磺酰基; Y是直接键或低级亚烷基; 并且R 1,R 2,R 3,R 4如本文所定义。 该化合物例如有利地用作速激肽拮抗剂用于治疗呼吸系统疾病,眼科疾病和炎性疾病。
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公开(公告)号:US5321032A
公开(公告)日:1994-06-14
申请号:US916853
申请日:1992-08-12
申请人: Masaaki Matsuo , Daijiro Hagiwara , Hiroshi Miyake
发明人: Masaaki Matsuo , Daijiro Hagiwara , Hiroshi Miyake
IPC分类号: A61K38/00 , C07K5/078 , C07K5/083 , C07K5/093 , A61K37/00 , A61K31/405 , A61K31/415 , A61K31/45 , C07D209/20 , C07D401/12 , C07D403/12 , C07K5/00
CPC分类号: C07K5/06156 , C07K5/081 , C07K5/0819 , A61K38/00 , Y02P20/55
摘要: A tachykinin-antagonistic compound of the following general formula:R.sup.1 --A.sup.1 --D--Trp(R.sup.2)--A.sup.2 --R.sup.3[whereinR.sup.1 is hydrogen or amino-protective groupR.sup.2 is amino-protective groupR.sup.3 is ar(lower)alkoxy or N-(lower)alkyl or N-ar(lower)alkylaminoA.sup.1 is single bond or one amino acid residueA.sup.2 is one amino acid residue other than Phe.]or the salt thereof.
摘要翻译: PCT No.PCT / JP91 / 00167 Sec。 371日期:1992年8月12日 102(e)日期1992年8月12日PCT 1991年2月12日提交PCT公布。 公开号WO91 / 12266 1991年8月22日,下列通式的速激肽拮抗剂R1-A1-D-Trp(R2)-A2-R3 [其中R1为氢或氨基保护基R2为氨基保护基R3为 芳基(低级)烷氧基或N-(低级)烷基或N-芳(低级)烷基氨基A1为单键或一个氨基酸残基A2为Phe之外的一个氨基酸残基]或其盐。
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