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19 条记录 (耗时 0.019 秒)

    Processes for making cephems from allenylazetidinone derivatives
    1.
    发明授权
    Processes for making cephems from allenylazetidinone derivatives 失效
    从烯丙基氮杂环丁酮衍生物制备头孢烯的方法

    公开(公告)号：US5162521A

    公开(公告)日：1992-11-10

    申请号：US711250

    申请日：1991-06-06

    申请人： Vittorio Farina ,  Stephen R. Baker

    发明人： Vittorio Farina ,  Stephen R. Baker

    IPC分类号： C07D501/00 ,  C07D501/10

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： This invention relates to a novel process for making a cephem of formula II from 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate of formula I. In another aspect, this invention is concerned with a process of further converting a compound of formula II into an antibacterial cephem of formula III. ##STR1## In formulae I, II and III, R.sup.1 is hydrogen, a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.

    摘要翻译： 本发明涉及由式I的2-（3-氨基-2-氧代 - 氮杂环丁烷-1-基）-2,3-丁二烯酸制备式II的头孢烯的新方法。另一方面，本发明涉及 其具有将式II化合物进一步转化成式III的抗菌头孢烯的方法。 在式I，II和III中，R 1是氢，常规的氨基保护基或酰基; R2是芳族杂环或芳基; R3是常规的羧基保护基或-CO 2 R 3一起形成生理上可水解的酯; 并且R 4是选自C 1-6烷基，C 2-6烯基，C 2-6炔基，环C 3-6烷基和芳基的基团。 n为0或2。

    Sulfur containing alkenylenyl substituted benzoic acids and phenyl tetrazoles and their use as anti-allergic agents
    5.
    发明授权
    Sulfur containing alkenylenyl substituted benzoic acids and phenyl tetrazoles and their use as anti-allergic agents 失效
    含硫烯基取代的苯甲酸和苯基四唑及其作为抗过敏剂的用途

    公开(公告)号：US4675335A

    公开(公告)日：1987-06-23

    申请号：US822703

    申请日：1986-01-27

    申请人： Stephen R. Baker ,  William J. Ross

    发明人： Stephen R. Baker ,  William J. Ross

    IPC分类号： A61K31/41 ,  A61P11/00 ,  A61P17/00 ,  A61P37/08 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07C323/52 ,  C07D257/04 ,  C07C63/06

    CPC分类号： C07D257/04 ,  Y02P20/55

    摘要： Pharmaceutical compounds are described of the formula ##STR1## in which R.sup.1 is (i) R.sup.4 O(CH.sub.2 CH.sub.2 O).sub.n (CH.sub.2).sub.m --, where R.sup.4 is hydrogen or C.sub.1-5 alkyl, n is 0 or 1 to 5 and m is 1 to 7, or (ii) R.sup.5 --X-- where R.sup.5 is a polar group and X is a C.sub.6-20 alkylene or a C.sub.6-20 alkenylene radical containing from 1 to 3 double bonds, R.sup.2 is a group of the formula A--B-- where A is --COOH or ##STR2## where R.sup.6 is hydrogen or a protecting group, and B is C.sub.1-6 alkylene, and R.sup.3 is --COOH or ##STR3## where R.sup.7 is hydrogen or a protecting group; or a salt or ester thereof.

    摘要翻译： 药物化合物描述于其中R 1为（ⅰ）R 4 O（CH 2 CH 2 O）n（CH 2）m - ，其中R 4为氢或C 1-5烷基，n为0或1至5并且m为1至 7，或（ii）R 5 -X-，其中R 5是极性基团，X是含有1至3个双键的C 6-20亚烷基或C 6-20亚烯基，R 2是式AB-的基团，其中A 是-COOH或，其中R 6是氢或保护基，B是C 1-6亚烷基，R 3是-COOH或者R 7是氢或保护基; 或其盐或酯。

    Aurone derivatives
    6.
    再颁专利
    Aurone derivatives 失效
    Aurone衍生物

    公开(公告)号：USRE32196E

    公开(公告)日：1986-07-01

    申请号：US379793

    申请日：1982-05-19

    申请人： Stephen R. Baker ,  William B. Jamieson ,  William J. Ross

    发明人： Stephen R. Baker ,  William B. Jamieson ,  William J. Ross

    IPC分类号： C07D307/88 ,  A61K31/34 ,  A61K31/343 ,  A61P11/00 ,  C07C45/63 ,  C07C65/40 ,  C07D257/04 ,  C07D307/83 ,  C07D307/92 ,  C07D317/30 ,  C07D405/10

    CPC分类号： C07D257/04 ,  C07C45/63 ,  C07C65/40 ,  C07D307/83 ,  C07D307/92 ,  C07D317/30

    摘要： Substituted aurones of formula (I): ##STR1## wherein R.sup.1, R.sup.2 R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and can each represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.3-8 cycloalkyl, optionally substituted phenyl, C.sub.1-6 haloalkyl, amido, amino, cyano, hydroxy, nitro, C.sub.2-4 alkenyl, carboxyl, tetrazol-5-yl and --CH.dbd.CHCOOH; orwherein R.sup.1 and R.sup.2 taken together can represent a group of formula --CH.dbd.CH--CH.dbd.CH-- provided that at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is carboxyl, tetrazol-5-yl or --CH.dbd.CHCOOH;or a pharmaceutically-acceptable salt or ester thereof, are effective in the prophylactic chemotherapy of allergic conditions such as bronchial asthma.

    摘要翻译： AURONE DERIVAT IVES式（I）的取代的噢：其中R 1，R 2，R 3，R 4，R 5和R 6相同或不同并且各自表示氢，卤素，C 1-6烷基，C 1-6 烷氧基，C 3-8环烷基，任选取代的苯基，C 1-6卤代烷基，酰氨基，氨基，氰基，羟基，硝基，C 2-4烯基，羧基，四唑-5-基和-CH_CHCOOH; 或者其中R 1和R 2一起可以表示式-CH-CH-CH-CH-基团，条件是R 17，R 3，R 4，R 5和R 6中的至少一个是羧基，四唑-5-基或-CH = CICOOH; 或其药学上可接受的盐或酯在过敏性疾病例如支气管哮喘的预防性化学疗法中是有效的。

    SRS-A antagonists
    8.
    发明授权
    SRS-A antagonists 失效
    SRS-A拮抗剂

    公开(公告)号：US4513005A

    公开(公告)日：1985-04-23

    申请号：US386570

    申请日：1982-06-09

    申请人： Stephen R. Baker ,  William B. Jamieson ,  William J. Ross ,  Alec Todd

    发明人： Stephen R. Baker ,  William B. Jamieson ,  William J. Ross ,  Alec Todd

    IPC分类号： C07B45/04 ,  C07C317/46 ,  C07C323/22 ,  C07C323/56 ,  C07C323/58 ,  C07D303/40 ,  C07D303/42 ,  C07D307/38 ,  C07D309/12 ,  C07D309/30 ,  C07D313/04 ,  C07F9/53 ,  C07K5/06 ,  C07C149/20 ,  A61K31/23 ,  A61K31/335

    CPC分类号： C07D307/38 ,  C07B45/04 ,  C07C317/46 ,  C07C323/22 ,  C07C323/56 ,  C07C323/58 ,  C07D303/40 ,  C07D303/42 ,  C07D309/12 ,  C07D309/30 ,  C07D313/04 ,  C07F9/5304 ,  C07F9/5325 ,  C07K5/06034

    摘要： There are described pharmacologically active compounds, useful in the treatment of allergic/inflammatory disorders involving SRS-A as causal mediator and which, in free acid form, are of formula I, ##STR1## in which R.sub.1 is (i) an aliphatic, saturated or unsaturated hydrocarbyl radical of up to 20 carbon atoms, unsubstituted or substituted by at least one substituent selected from halogen, hydroxy, C.sub.3-6 alkoxy, C.sub.3-6 cycloalkyl, aryl or heteroaryl, the cycloalkyl, aryl or heteroaryl being unsubstituted or substituted by at least one substituent selected from hydroxy, halogen and alkyl, alkenyl or alkynyl of up to 10 carbon atoms,(ii) cycloalkyl of 3 to 8 carbon atoms unsubstituted or substituted by alkyl, alkenyl or alkynyl of up to 16 carbon atoms, or(iii) aryl or heteroaryl, unsubstituted or substituted by hydroxyl, C.sub.1-4 alkoxy, halogen or alkyl, alkenyl or alkynyl of up to 16 carbon atoms; and R.sub.2 is(i) alkyl, cycloalkyl or alkenyl of up to 10 carbon atoms, unsubstituted or substituted by one or more substituents selected from aryl, cycloalkyl, halogen, hydroxy, NHR.sub.3 and COX, where R.sub.3 is H, C.sub.1-4 alkyl, aryl or an amino acid residue or COX, and X is OH, C.sub.1-4 alkyl, NH.sub.2 or an amino acid residue, or(ii) aryl or heteroaryl, unsubstituted or substituted by one or more substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 acyl, halogen, hydroxy, carboxy, nitro, trihalomethyl, phenyl, C.sub.1-4 acylamino and NHR.sub.4, where R.sub.4 is hydrogen or C.sub.1-4 alkyl; and Y is --S--, --SO-- or --SO.sub.2 --,with the proviso that when --YR.sub.2 is glutathionyl, cysteinyl or cysteinylglycinyl, then R.sub.1 is other than an unsubstituted alkatetraenyl or alkapentaenyl radical of 12 to 16 carbon atoms.

    摘要翻译： 描述了用于治疗涉及SRS-A作为因果介质的过敏性/炎症性疾病，其游离酸形式为式I的化学活性化合物，其中R 1是（i）脂族， 至少20个碳原子的饱和或不饱和烃基，未被取代或被至少一个选自卤素，羟基，C 3-6烷氧基，C 3-6环烷基，芳基或杂芳基的取代基取代，环烷基，芳基或杂芳基是未取代或取代的 至少一个选自羟基，卤素和至多10个碳原子的烷基，烯基或炔基的取代基，（ii）未被取代或被至多16个碳原子的烷基，烯基或炔基取代的3至8个碳原子的环烷基，或 （iii）未被取代或被羟基，C 1-4烷氧基，卤素或至多16个碳原子的烷基，链烯基或炔基取代的芳基或杂芳基; 并且R 2是（i）至少10个碳原子的烷基，环烷基或链烯基，未被取代或被一个或多个选自芳基，环烷基，卤素，羟基，NHR 3和COX的取代基取代，其中R 3是H，C 1-4烷基， 芳基或氨基酸残基或COX，X为OH，C 1-4烷基，NH 2或氨基酸残基，或（ii）未被取代或被一个或多个选自C 1-4烷基，C 1 -4-烷氧基，C 2-5酰基，卤素，羟基，羧基，硝基，三卤甲基，苯基，C 1-4酰基氨基和NHR 4，其中R 4是氢或C 1-4烷基; 并且Y是-S-，-SO-或-SO 2 - ，条件是当-YR 2是谷胱甘肽基，半胱氨酰基或半胱氨酰甘氨酰基时，则R 1不同于未被取代的具有12至16个碳原子的烷基四烯基或烷基五烯基。