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    Caphalosporin compounds having at position-7 an .alpha.-etherified hydroxyiminoarylacetamido group
    3.
    发明授权
    Caphalosporin compounds having at position-7 an .alpha.-etherified hydroxyiminoarylacetamido group 失效
    在位置-7处具有α-乙酰化羟基亚氨基芳基乙酰胺基的咖啡糊精化合物

    公开(公告)号：US4208517A

    公开(公告)日：1980-06-17

    申请号：US855080

    申请日：1977-11-28

    申请人： Michael W. Foxton ,  Gordon I. Gregory ,  David M. Rogers

    发明人： Michael W. Foxton ,  Gordon I. Gregory ,  David M. Rogers

    IPC分类号： C07D307/54 ,  C07D501/32 ,  C07D501/34 ,  A61K31/545

    CPC分类号： C07D307/54

    摘要： Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R.sup.a and R.sup.b, which may be the same or different, are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, or R.sup.a and R.sup.b together wth the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; R.sup.c and R.sup.d, which may be the same or different, each represents a hydrogen atom or a substituting group e.g. an alkyl group or substituted alkyl group; or R.sup.c and R.sup.d together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring which contains 5-7 ring members and which may contain additional hetero atoms, and may be substituted by lower alkyl; R.sup.e represents hydrogen or C.sub.1-4 alkyl; m and n are each 0 or 1 such that the sum of m and n is 0 or 1 and Y is selected from various oxygen and sulphur nucleophiles] and non-toxic derivatives thereof.

    摘要翻译： 通式（I）的抗生素化合物[其中R是苯基，噻吩基或呋喃基; R a和R b可以相同或不同，各自选自氢，C 1-4烷基，C 2-4烯基，C 3-7环烷基，苯基，萘基，噻吩基，呋喃基，羧基，C 2-5烷氧基羰基和氰基， 或者R a和R b一起与它们所连接的碳原子一起形成C 3-7亚环烷基或亚环烯基; R c和R d可以相同或不同，表示氢原子或取代基团。 烷基或取代的烷基; 或Rc和Rd与它们所连接的氮原子一起形成饱和或不饱和的杂环，其含有5-7个环成员并且可以含有另外的杂原子，并且可以被低级烷基取代; Re表示氢或C 1-4烷基; m和n各自为0或1，使得m和n的和为0或1，Y选自各种氧和硫亲核试剂]及其无毒的衍生物。

    Heterocyclic compounds which inhibit aromatase
    4.
    发明授权
    Heterocyclic compounds which inhibit aromatase 失效
    抑制芳香酶的杂环化合物

    公开(公告)号：US5578630A

    公开(公告)日：1996-11-26

    申请号：US338510

    申请日：1994-11-25

    申请人： Peter C. Cherry ,  Michael W. Foxton ,  Andrew T. Merritt

    发明人： Peter C. Cherry ,  Michael W. Foxton ,  Andrew T. Merritt

    IPC分类号： C07D405/06 ,  A61K31/41 ,  C07D521/00

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

    摘要： This invention relates to heterocyclic compounds which are inhibitors of the enzyme aromatase, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.Particular compounds of the invention are compounds of formula (I) ##STR1## wherein R.sup.1 represents a cyano or nitro group; R.sup.2 represents hydrogen or one or more halogen atoms;R.sup.3 represents a C.sub.1-6 alkyl group and R.sup.4 represents hydrogen or aC.sub.1-6 alkyl group or R.sup.3 and R.sup.4 together represent a C.sub.3-6 cycloalkyl group; andR.sup.5 represents hydrogen or one or more halogen atoms or C.sub.1-6 alkoxy groups and pharmaceutically acceptable salts and solvates thereof.

    摘要翻译： PCT No.PCT / EP93 / 01520 Sec。 371日期：1994年11月25日 102（e）日期1994年11月25日PCT提交1993年6月14日PCT公布。 出版物WO93 / 25548 日期1993年12月23日本发明涉及作为芳香酶酶的抑制剂，其制备方法的杂环化合物，含有它们的药物组合物及其在药物中的用途。 本发明的具体化合物是式（I）化合物其中R 1表示氰基或硝基; R2表示氢或一个或多个卤素原子; R3表示C1-6烷基，R4表示氢或C1-6烷基，R3和R4表示C3-6环烷基; 并且R 5表示氢或一个或多个卤素原子或C 1-6烷氧基及其药学上可接受的盐和溶剂化物。

    3-(Optionally substituted-but-1-en-3-ynyl) cephalosporins
    5.
    发明授权
    3-(Optionally substituted-but-1-en-3-ynyl) cephalosporins 失效
    3-（任选取代的，1-en-3-炔基）头孢菌素

    公开(公告)号：US4666899A

    公开(公告)日：1987-05-19

    申请号：US732094

    申请日：1985-05-09

    申请人： Richard Bell ,  Paul D. Hallam ,  Michael W. Foxton

    发明人： Richard Bell ,  Paul D. Hallam ,  Michael W. Foxton

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/20 ,  C07D501/06 ,  C07D501/14 ,  C07D501/16 ,  C07D501/18 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/60 ,  C07F7/18

    CPC分类号： C07D277/587 ,  C07F7/1852

    摘要： Compounds of general formula I ##STR1## (wherein R represents NH.sub.2 -- or an acylated or silylated amino group;R.sup.2 represents a hydrogen, halogen, alkyl, aryl, carboxyl or lower alkoxycarbonyl group;R.sup.3 is hydrogen or a carboxyl blocking group;B is >Sor>S.fwdarw.O (.alpha.- or .beta.-); and the dotted line represents .DELTA..sup.2 or .DELTA..sup.3 unsaturation) and salts, solvates and esters thereof are described.Compounds where R.sup.3 is hydrogen, the dotted line represents .DELTA..sup.3 unsaturation and R is a group of formula ##STR2## (where R.sup.a is an optionally substituted heterocyclic aryl group having one or more hetero atoms selected from S, N and O in the ring, R.sup.b is an optionally substituted aryl group, R.sup.c is hydrogen, acyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.d is as defined for R.sup.a or is an optionally substituted group and X is amino, hydroxyl, acylated hydroxyl, carboxyl or esterified carboxyl)and especially the compounds in which B is >S, have valuable antibiotic activities.Compounds in which the --CH.dbd.CH--C.tbd.C--R.sup.2 group is in the trans configuration have been found to have good oral absorption.The remaining compounds of formula (I) are valuable as intermediates in processes for the preparation of the above active antibiotics, which processes are also described.

    摘要翻译： 通式I的化合物（I）（其中R表示NH 2 - 或酰化或甲硅烷基化的氨基; R 2表示氢，卤素，烷基，芳基，羧基或低级烷氧基羰基; R 3是氢或羧基封端基 ; B是> Sor> S-> O（α-或β-）;虚线代表DELTA 2或DELTA 3不饱和键）及其盐，溶剂合物和酯。 其中R 3为氢的化合物，虚线表示DELTA 3不饱和度，R为式R a R 2 CONH（R a）的基团，其中R a为具有一个或多个选自S，N和O的杂原子的任选取代的杂环芳基 在环中，R b是任选取代的芳基，R c是氢，酰基，烷基，烯基，炔基，环烷基，环烷基烷基，芳基或芳烷基，Rd如对Ra定义或是任选取代的基团，X是氨基，羟基 ，酰化羟基，羧基或酯化羧基），特别是其中B> S的化合物具有有价值的抗生素活性。 已经发现其中-CH = CH-C 3 D C-R 2基团处于反式构型的化合物具有良好的口服吸收。 剩余的式（I）化合物在制备上述活性抗生素的方法中作为中间体是有价值的，该方法也被描述。

    Cephalosporin antibiotics
    6.
    发明授权
    Cephalosporin antibiotics 失效
    头孢菌素类抗生素

    公开(公告)号：US5043334A

    公开(公告)日：1991-08-27

    申请号：US441612

    申请日：1989-11-27

    申请人： Richard Bell ,  Michael W. Foxton ,  Brian E. Looker

    发明人： Richard Bell ,  Michael W. Foxton ,  Brian E. Looker

    IPC分类号： A61K31/545 ,  A61P31/04 ,  C07D277/20 ,  C07D501/20 ,  C07D501/24

    CPC分类号： C07D277/587 ,  Y02P20/55

    摘要： Compounds of general formula (I) ##STR1## (where R.sup.1 is a carboxyl group, a group COO.sup..crclbar. or a blocked carboxyl group;R.sup.2 is an amino or protected amino group; andR is hydrogen or a group of the formula CH.sub.2 X, where X represents a halogen atom, a hydroxyl group, an acetoxy group; a group of the formula O.CO.NHR.sup.3, where R.sup.3 is hydrogen, a C.sub.1-4 alkyl group optionally substituted by 1 to 3 halogen atoms or an N-protecting group; a group of the formula OR.sup.4, where R.sup.4 is a C.sub.1-4 alkyl group optionally substituted by halogen or a C.sub.1-4 alkoxy group; or a pyridinium, 3-carbamoyl-pyridinium or 4-carbamoyl-pyridinium group;B is --S-- or --SO-- (.alpha.- or .beta.-); and the dotted line bridging the 2-, 3- and 4- positions indicates that the compound is a ceph-2-em or ceph-3-em compound) and salts thereof, the compounds of formula (I) being associated with an anion when X represents a pyridinium, 3-carbamoylpyridinium group or a 4-carbamoylpyridinium group and R.sup.1 is other than COO.sup..crclbar.) are disclosed.Processes for their preparation and pharmaceutical compositions containing them are also disclosed.

    摘要翻译： 通式（I）的化合物（Ⅰ）（其中R1是羧基，COO（ - ）或封端羧基; R2是氨基或被保护的氨基; R是氢或一个 式CH 2 X，其中X表示卤素原子，羟基，乙酰氧基;式O.CO.NHR 3的基团，其中R 3是氢，任选被1至3个卤素原子取代的C 1-4烷基或 N-保护基;式OR4的基团，其中R4是任选被卤素或C 1-4烷氧基取代的C 1-4烷基;或吡啶鎓，3-氨基甲酰基 - 吡啶鎓或4-氨基甲酰基 - 吡啶鎓基 ; B是-S-或-SO-（α-或β-）;桥接2-，3-和4-位的虚线表示该化合物是ceph-2-em或ceph-3-em 化合物）及其盐，当X表示吡啶鎓，3-氨基甲酰基吡啶鎓基或4-氨基甲酰基吡啶基且R 1不同于COO（ - ）时，式（I）的化合物与阴离子缔合。 还公开了其制备方法和含有它们的药物组合物。

    Cephalosporins having a carbamoylalkoxyiminoarylacetamido group at 7-position
    7.
    发明授权
    Cephalosporins having a carbamoylalkoxyiminoarylacetamido group at 7-position 失效
    在7位具有氨基甲酰基烷氧基亚氨基乙酰胺基的头孢菌素

    公开(公告)号：US4385177A

    公开(公告)日：1983-05-24

    申请号：US124109

    申请日：1980-02-25

    申请人： Michael W. Foxton ,  Gordon I. Gregory ,  David M. Rogers

    发明人： Michael W. Foxton ,  Gordon I. Gregory ,  David M. Rogers

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D307/54 ,  C07D333/24 ,  C07D501/20 ,  C07D501/34 ,  C07D501/56

    CPC分类号： C07D307/54 ,  C07D333/24

    摘要： Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R.sup.a and R.sup.b, which may be the same or different, are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, or R.sup.a and R.sup.b together with the carbon atom to which they are attached from a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; R.sup.c is hydrogen or lower alkyl; R.sup.d is hydroxy, lower alkoxy, aralkoxy or aryloxy; m and n are each 0 or 1 such that the sum of m and n is 0 or 1; and P is selected from a hydrogen atom, a halogen atom and various organic groups] and non-toxic derivatives thereof.

    摘要翻译： 通式（I）的抗生素化合物[其中R是苯基，噻吩基或呋喃基; R a和R b可以相同或不同，各自选自氢，C 1-4烷基，C 2-4烯基C 3-7环烷基，苯基，萘基，噻吩基，呋喃基，羧基，C 2-5烷氧基羰基和氰基，或 R a和R b与它们所连接的碳原子一起为C3-7亚环烷基或环亚烯基; Rc是氢或低级烷基; Rd为羟基，低级烷氧基，芳烷氧基或芳氧基; m和n各自为0或1，使得m和n的和为0或1; 和P选自氢原子，卤素原子和各种有机基团]及其无毒的衍生物。

    7 2-(Aminocarbonylalkoxyimino)acetamido! derivatives of cephalosporin
    8.
    发明授权
    7 2-(Aminocarbonylalkoxyimino)acetamido! derivatives of cephalosporin 失效
    7 {8 2-（氨基羰基烷氧基亚氨基）乙酰氨基{9 {头孢菌素衍生物

    公开(公告)号：US4074047A

    公开(公告)日：1978-02-14

    申请号：US694465

    申请日：1976-06-09

    申请人： Michael W. Foxton ,  Gordon I. Gregory ,  David M. Rogers

    发明人： Michael W. Foxton ,  Gordon I. Gregory ,  David M. Rogers

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D307/54 ,  C07D333/24 ,  C07D501/20 ,  C07D501/26 ,  C07D501/32 ,  C07D501/34

    CPC分类号： C07D501/20 ,  C07D307/54 ,  C07D333/24

    摘要： Cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## (WHERE R is phenyl, thienyl or furyl; R.sup.a and R.sup.b are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl, aminocarbonyl, N-substituted aminocarbonyl and cyano, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; R.sup.c is hydrogen or C.sub.1-4 alkyl; and m and n are each 0 or 1 such that the sum of m and n is 0 or 1) exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly good activity against Proteus organisms including indole positive strains and, especially when both R.sup.a and R.sup.b are other than hydrogen, against Pseudomonas organisms.

    摘要翻译： 头孢菌素抗生素，其中7β-酰胺基具有结构（其中R是苯基，噻吩基或呋喃基; R a和R b各自选自氢，C 1-4烷基，C 2-4链烯基，C 3-7环烷基， 苯基，萘基，噻吩基，呋喃基，羧基，C 2-5烷氧基羰基，氨基羰基，N-取代的氨基羰基和氰基，或者R a和R b与它们所连接的碳原子一起形成C 3-7亚环烷基或亚环烯基; R c是 氢或C 1-4烷基; m和n各自为0或1，使得m和n的和为0或1）表现出广谱抗生素活性，其特征在于对革兰氏阴性微生物特别高的活性，包括产生β- 内酰胺酶 作为syn异构体的化合物或含有至少90％的顺式异构体的合成和反异构体的混合物的化合物对包括吲哚阳性菌株在内的变形杆菌生物具有特别好的活性，特别是当Ra和Rb都不是氢时， 针对假单胞菌生物。