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452 条记录 (耗时 0.02 秒)

    Manufacture of antibiotics
    61.
    发明授权
    Manufacture of antibiotics 失效
    制造抗生素

    公开(公告)号：US4510312A

    公开(公告)日：1985-04-09

    申请号：US441249

    申请日：1982-11-12

    申请人： William S. Strachan ,  Alastair C. Brodie

    发明人： William S. Strachan ,  Alastair C. Brodie

    IPC分类号： C07D277/20 ,  C07D277/40 ,  C07D277/42 ,  C07D277/38

    CPC分类号： C07D277/587

    摘要： The invention provides crystalline ethyl (Z)-2-hydroxyimino-2-(2-triphenylmethylaminothiazol-4-yl)acetate hydrochloride N,N-dimethylformamide solvate which is of value as an intermediate in the preparation of .beta.-lactam antibiotics such as ceftazidime, azthreonam, cefmenoxime, cefotaxime, ceftriaxon, ceftizoxime and cefodizime.

    摘要翻译： 本发明提供了结晶乙基（Z）-2-羟基亚氨基-2-（2-三苯基甲基氨基噻唑-4-基）乙酸盐酸盐N，N-二甲基甲酰胺溶剂化物，其作为制备β-内酰胺类抗生素如头孢他啶的中间体 ，氨曲南，头孢匹肟，头孢噻肟，头孢曲松，头孢唑肟和头孢地嗪。

    Alkyloximes of 7-amino-thiazolyl-acetamido-cephalosporanic acids
    62.
    发明授权
    Alkyloximes of 7-amino-thiazolyl-acetamido-cephalosporanic acids 失效
    7-氨基 - 噻唑基 - 乙酰氨基 - 头孢烷酸的肟基

    公开(公告)号：US4396618A

    公开(公告)日：1983-08-02

    申请号：US94196

    申请日：1979-11-14

    申请人： Rene Heymes ,  Andre Lutz

    发明人： Rene Heymes ,  Andre Lutz

    IPC分类号： C07D501/06 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/20 ,  C07D277/38 ,  C07D501/04 ,  C07D501/20 ,  C07D501/22 ,  C07D501/36

    CPC分类号： C07D277/20 ,  C07D277/38 ,  C07D277/587

    摘要： Novel alkyloximes of 7-amino-thiazolyl-acetamide-cephalosporanic acids of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms and --CH.sub.2 --SR', R' is selected from the group consisting of acyl of an alkanoic acid of 2 to 4 carbon atoms, 1-methyl-tetrazolyl and 2-methyl-1,3,4-thiadiazolyl, R.sub.1 is selected from the group consisting of hydrogen and a group easily removeable by acid hydrolysis or hydrogenolysis, R.sub.2 is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, A is selected from the group consisting of hydrogen, an alkali metal cation, an equivalent of an alkaline earth metal or magnesium, an organic amine base cation and an ester group easily removeable by acid hydrolysis or hydrogenolysis with the proviso that when R.sub.1 is hydrogen, A is not an ester group easily removeable by hydrogenolysis or acid hydrolysis and the wavy line means that OR.sub.2 is in one or the other of the two possible syn or anti isomeric positions having a very good antibiotic activity and novel processes and intermediates for their preparation.

    摘要翻译： 具有下式的其中R选自1至5个碳原子的烷基，3至5个碳原子的环烷基和-CH 2 -SR'的7-氨基 - 噻唑基 - 乙酰胺 - 头孢菌酸的新型烷基肟， R'选自2至4个碳原子的链烷酸的酰基，1-甲基 - 四唑基和2-甲基-1,3,4-噻二唑基，R 1选自氢和 可通过酸解或氢解容易除去的基团，R 2选自1至4个碳原子的烷基和2至4个碳原子的烯基和炔基，A选自氢，碱金属阳离子 相当于碱土金属或镁，有机胺碱阳离子和酯基可以通过酸解或氢解容易除去，条件是当R1是氢时，A不是通过氢解或酸解可容易地除去的酯基， 波浪线意味着O R2具有非常好的抗生素活性的两种可能的顺式或反式异构体位置中的一种或另一种，以及用于其制备的新方法和中间体。

    Thiazole derivatives
    68.
    发明授权
    Thiazole derivatives 失效
    噻唑衍生物

    公开(公告)号：US4200578A

    公开(公告)日：1980-04-29

    申请号：US970517

    申请日：1978-12-18

    申请人： Aldo A. Algieri ,  Ronnie R. Crenshaw

    发明人： Aldo A. Algieri ,  Ronnie R. Crenshaw

    IPC分类号： A61K31/425 ,  A61K31/426 ,  A61P1/04 ,  A61P43/00 ,  C07D277/20 ,  C07D277/26 ,  C07D277/28 ,  C07D277/38 ,  C07D277/42 ,  C07D277/48

    CPC分类号： C07D277/28 ,  C07D277/38 ,  Y10S514/927

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 and R.sup.3 each are independently hydrogen, (lower)alkyl, guanidino or --(CH.sub.2).sub.p NR.sup.4 R.sup.5 ; R.sup.4 and R.sup.5 each are independently hydrogen, (lower)alkyl or phenyl; n is 2 or 3; p is 1, 2 or 3; X is NR.sup.6 or CHR.sup.6 ; R.sup.6 is cyano, nitro, SO.sub.2 Ar or SO.sub.2 (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.

    摘要翻译： 式Ⅰ的化合物，其中R 1是含有3至9个碳原子的直链或支链炔基，包括端值; （低级）烷基，胍基或 - （CH 2）pNR 4 R 5; R4和R5各自独立地为氢，（低级）烷基或苯基; n为2或3; p为1,2或3; X为NR6或CHR6; R6是氰基，硝基，SO2Ar或SO2（低级）烷基; 和Ar是苯基或含有1或2个选自卤素和（低级）烷基的取代基的苯基; 和无毒的药学上可接受的盐是有效的抗溃疡剂。

    Process for the production of urea derivatives
    69.
    发明授权
    Process for the production of urea derivatives 失效
    尿素衍生物生产工艺

    公开(公告)号：US4183856A

    公开(公告)日：1980-01-15

    申请号：US895105

    申请日：1978-04-10

    申请人： Yasuo Makisumi ,  Takashi Sasatani ,  Akira Murabayashi

    发明人： Yasuo Makisumi ,  Takashi Sasatani ,  Akira Murabayashi

    IPC分类号： C07D275/02 ,  C07D213/75 ,  C07D261/14 ,  C07D263/48 ,  C07D275/03 ,  C07D277/20 ,  C07D277/38 ,  C07D277/46 ,  C07D277/48 ,  C07D277/82

    CPC分类号： C07D213/75 ,  C07D261/14 ,  C07D275/03 ,  C07D277/48 ,  C07D277/82

    摘要： Urea derivatives of the formula ##STR1## (wherein Ar represents a residue of 5- or 6-membered heteroaromatic ring; R represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group; and R.sup.2 represents a C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxy group) are produced by reacting an amine of the formulaAr--NH--R(wherein Ar and R have the significance given above) with a carbamoyl halogenide of the formula ##STR2## (wherein X represents a halogen atom, and R.sup.1 and R.sup.2 have the significance given above) in the presence of a Lewis acid in an inert solvent.

    摘要翻译： 下式的脲衍生物（其中Ar表示5或6元杂芳环的残基; R表示氢原子或C1-C6烷基; R1表示C1-C6烷基; R2表示 C 1 -C 6烷基，C 2 -C 6烯基或C 1 -C 6烷氧基）通过使式Ar-NH-R（其中Ar和R具有上述含义）具有下式的氨基甲酰卤化物： 图像（其中X表示卤原子，R1和R2具有上述含义）在路易斯酸存在下在惰性溶剂中反应。

    Guanidino imidazoles and thiazoles
    70.
    发明授权
    Guanidino imidazoles and thiazoles 失效
    胍基咪唑和噻唑

    公开(公告)号：US4165377A

    公开(公告)日：1979-08-21

    申请号：US897910

    申请日：1978-04-19

    申请人： Derrick F. Jones ,  Tobias O. Yellin

    发明人： Derrick F. Jones ,  Tobias O. Yellin

    IPC分类号： A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61P1/04 ,  A61P43/00 ,  C07C277/08 ,  C07D209/48 ,  C07D233/88 ,  C07D277/20 ,  C07D277/38 ,  C07D277/42 ,  C07D277/48

    CPC分类号： C07D209/48 ,  C07D233/88 ,  C07D277/48

    摘要： The invention relates to guanidine derivatives of imidazoles and thiazoles which are histamine H-2 antagonists and which inhibit the secretion of gastric acid, to methods for their manufacture, to pharmaceutical compositions containing them and to methods of using such guanidine derivatives and compositions. The guanidine derivatives are of the general formula I: ##STR1## in which X is S or NH, Y is CH.sub.2, a direct bond or a vinylene radical, m is 0 to 4 and n is 1 to 4, R.sup.1 is hydrogen, halogen or alkyl, R.sup.2 is hydrogen, alkyl, alkanoyl or aroyl, A is a 3,4-dioxocyclobuten-1,2-diyl radical or C.dbd.Z in which Z is O, S, NCN, NNO.sub.2, CHNO.sub.2, NCONH.sub.2, C(CN).sub.2, NCOR.sup.3, NCO.sub.2 R.sup.3, NSO.sub.2 R.sup.3 or NR.sup.4 in which R.sup.3 is alkyl or aryl and R.sup.4 is hydrogen or alkyl, B is alkoxy or alkylthio or NR.sup.5 R.sup.6 in which R.sup.5 and R.sup.6 are independently hydrogen, alkyl, alkenyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, alkylaminoalkyl or dialkylaminoalkyl; and the salts thereof.

    摘要翻译： 本发明涉及作为组胺H-2拮抗剂的咪唑和噻唑的胍衍生物，其抑制胃酸的分泌，其制备方法，含有它们的药物组合物以及使用这种胍衍生物和组合物的方法。 胍衍生物具有通式I：其中X为S或NH，Y为CH 2，直接键或亚乙烯基，m为0至4，n为1至4，R 1为氢， 卤素或烷基，R 2是氢，烷基，烷酰基或芳酰基，A是3,4-二氧杂环丁烯-1,2-二基或C = Z，其中Z是O，S，NCN，NNO 2，CHNO 2，NCONH 2，C （CN）2，NCOR3，NCO2R3，NSO2R3或NR4，其中R3是烷基或芳基，R4是氢或烷基，B是烷氧基或烷硫基或NR5R6，其中R5和R6独立地是氢，烷基，烯基，环烷基，羟基烷基， 烷氧基烷基，烷基氨基烷基或二烷基氨基烷基; 及其盐。