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    Carbapenem derivatives having antibiotic activity, their preparation and their use
    3.
    发明授权
    Carbapenem derivatives having antibiotic activity, their preparation and their use 失效
    具有抗生素活性的碳青霉烯类衍生物及其制备及其应用

    公开(公告)号：US5420119A

    公开(公告)日：1995-05-30

    申请号：US143996

    申请日：1993-10-27

    申请人： Isao Kawamoto ,  Masao Miyauchi ,  Eiji Nakayama ,  Rokuro Endo ,  Satoshi Ohya ,  Yukio Utsui

    发明人： Isao Kawamoto ,  Masao Miyauchi ,  Eiji Nakayama ,  Rokuro Endo ,  Satoshi Ohya ,  Yukio Utsui

    IPC分类号： C07D487/04 ,  A61K31/40 ,  A61K31/435 ,  A61K31/44 ,  A61K31/495 ,  A61K31/55 ,  C07D477/00 ,  C07D477/10 ,  C07D477/12 ,  C07D477/20 ,  A01N43/00 ,  A61K31/395

    CPC分类号： C07D477/20

    摘要： Carbapenem compounds of formula (I): ##STR1## [in which: A is a fully saturated heterocyclic group, of which at least one ring atom is nitrogen; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or a negative ion; Q is: (i) --B--N.sup.+ R.sup.8 R.sup.9 R.sup.10, where R.sup.8, R.sup.9 and R.sup.10 are alkenyl, alkynyl or optionally substituted alkyl, and B is alkylene or alkylidene; (ii) a heterocyclic group of which one ring atom is a >N.sup.+ R.sup.11 R.sup.12, where R.sup.11 and R.sup.12 are alkenyl, alkynyl or optionally substituted alkyl; (iii) alkyl substituted by a heterocyclic group as defined in (ii) above; or (iv) alkyl substituted by an aromatic heterocyclic group, of which one ring atom is ##STR2## or R.sup.2 and Q, and the nitrogen to which they are attached, form a group of formula (II): ##STR3## where m and n are 1, 2 or 3; R.sup.6 is optionally substituted alkyl; and R.sup.7 is alkenyl, alkynyl or optionally substituted alkyl] and pharmaceutically acceptable salts and esters thereof have valuable antibacterial activity with enhanced resistance to dehydropeptidase I and .beta.-lactamase. Methods of preparing and using the compounds are also provided.

    摘要翻译： （I）的碳青霉烯化合物：其中：A是完全饱和的杂环基团，其中至少一个环原子是氮; R1是氢或甲基; R2是氢或烷基; R3是氢或负离子; Q为：（i）-B-N + R8R9R10，其中R8，R9和R10为烯基，炔基或任选取代的烷基，B为亚烷基或亚烷基; （ii）一个环原子是> N + R11R12的杂环基，其中R11和R12是烯基，炔基或任选取代的烷基; （iii）被上述（ii）中定义的杂环基取代的烷基; 或（iv）被芳族杂环基取代的烷基，其中一个环原子是R 1和R 2和Q，并且与它们相连的氮形成式（II）的基团： 其中m和n为1,2或3; R6是任选取代的烷基; 并且R 7是烯基，炔基或任选取代的烷基]及其药学上可接受的盐和酯具有有利于抗脱水肽酶I和β-内酰胺酶的抗菌活性。 还提供了制备和使用化合物的方法。

    2-(heterocyclylthio) carbapenem derivatives, their preparation and their use as antibiotics
    4.
    发明授权
    2-(heterocyclylthio) carbapenem derivatives, their preparation and their use as antibiotics 失效
    2-（杂环硫基）碳青霉烯衍生物，其制备及其作为抗生素的用途

    公开(公告)号：US5242914A

    公开(公告)日：1993-09-07

    申请号：US831070

    申请日：1992-02-04

    申请人： Isao Kawamoto ,  Teruo Tanaka ,  Rokuro Endo ,  Masayuki Iwata ,  Masao Miyauchi

    发明人： Isao Kawamoto ,  Teruo Tanaka ,  Rokuro Endo ,  Masayuki Iwata ,  Masao Miyauchi

    IPC分类号： C07D477/20

    CPC分类号： C07D477/20

    摘要： Compounds of formula (I): ##STR1## in which R.sup.a is a group of formula (II): ##STR2## where one of R' is a bond to the remainder of the compound, one more of R' is R.sup.2 and the others of R' are all hydrogen, R.sup.1 is hydrogen or methyl, R.sup.2 is hydrogen, optionally substituted alkyl, halogen, hydroxy, alkoxy, amino, alkanoylamino, alkanoyloxy, alkanoyl, carboxy, alkoxycarbonyl, cyano, --S(O).sub.j R.sup.9 where j is 0, 1 or 2 and R.sup.9 is alkyl, or --CONR.sup.6 R.sup.7 which is optionally substituted carbamoyl or heterocyclyl-carbonyl, --NR.sup.3 R.sup.4 is optionally substituted amino or heterocyclic, and --COOR.sup.5 is carboxy, --COO.sup.-, --COOM.sub.x, where M is a cation and x is the reciprocal of the valence of the cation M or protected carboxy and, where --COOR.sup.5 is carboxy, --COOM.sub.x or protected carboxy, the compound of formula (I) also contains an anion; l, m and n are independently 0, 1, 2 or 3, provided that (m+n) is an integer from 2 to 6; p is 0, 1 or 2; Y is a single bond, oxygen, sulfur or ##STR3## wherein R.sup.8 is hydrogen, alkyl or alkanoyl, and pharmaceutically acceptable salts and esters thereof. Such compounds are useful as antibiotics.

    摘要翻译： 式（I）的化合物：其中R a是式（II）的基团：其中R'中的一个与化合物的其余部分键合，R 1是R '是R 2，其余的R'都是氢，R 1是氢或甲基，R 2是氢，任选取代的烷基，卤素，羟基，烷氧基，氨基，烷酰基氨基，烷酰氧基，烷酰基，羧基，烷氧基羰基，氰基，-S O）j R 9其中j为0,1或2，R 9为烷基或-CONR 6 R 7，其为任选取代的氨基甲酰基或杂环基 - 羰基，-NR 3 R 4为任选取代的氨基或杂环，-COOR 5为羧基，-COO - ， - COOMx 其中M是阳离子，x是阳离子M或保护的羧基的价数的倒数，并且其中-COOR 5是羧基，-COOM x或被保护的羧基，式（I）化合物还含有阴离子; l，m和n分别为0,1,2或3，条件是（m + n）为2至6的整数; p为0,1或2; Y是单键，氧，硫或其中R8是氢，烷基或烷酰基，及其药学上可接受的盐和酯。 这些化合物可用作抗生素。

    Carbapenem derivatives, their preparation and their use as antibiotics
    5.
    发明授权
    Carbapenem derivatives, their preparation and their use as antibiotics 失效
    碳青霉烯类衍生物，其制备及其作为抗生素的用途

    公开(公告)号：US5866564A

    公开(公告)日：1999-02-02

    申请号：US889542

    申请日：1997-07-08

    申请人： Isao Kawamoto ,  Rokuro Endo ,  Masao Miyauchi ,  Katsuya Ishikawa ,  Eiji Nakayama ,  Hiroshi Yasuda ,  Satoshi Ohya ,  Yukio Utsui ,  Katsuhiko Watanabe

    发明人： Isao Kawamoto ,  Rokuro Endo ,  Masao Miyauchi ,  Katsuya Ishikawa ,  Eiji Nakayama ,  Hiroshi Yasuda ,  Satoshi Ohya ,  Yukio Utsui ,  Katsuhiko Watanabe

    IPC分类号： C07D477/20 ,  C07D487/04 ,  A61K31/40

    CPC分类号： C07D477/20

    摘要： Compound of formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or --C(.dbd.NH)R.sup.0 where R.sup.0 is hydrogen or C.sub.1 -C.sub.6 alkyl;A is ##STR2## R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or --C(.dbd.NH)R.sup.6 where R.sup.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.7 cycloalkyl; R.sup.3 and R.sup.4 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, carboxy, cyano, --CO.NR.sup.a R.sup.b, --OCO.NR.sup.a R.sup.b or --NR.sup.a R.sup.b, where R.sup.a and R.sup.b are independently hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.20", R.sup.21', and R.sup.22" are independently hydrogen or C.sub.1 -C.sub.6 alkyl or R.sup.20" and R.sup.21" or R.sup.20" and R.sup.22" together form a heterocyclic group; R.sup.23" and R.sup.24" are independently hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; n is 1, 2 or 3; and n.sup.3" is 1, 2 or 3. The compounds are antibiotics which are resistant to dehydropeptidase I, and are useful for the treatment of microbial infections.

    摘要翻译： 式（I）化合物：其中R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或-C（= NH）R 0）其中R 0是氢或C 1 -C 6烷基; （C 1 -C 6）烷基，C 2 -C 6烯基，C 2 -C 6炔基或-C（= NH）R 6，其中R 6是氢，C 1 -C6烷基或C3-C7环烷基; R 3和R 4独立地是氢，C 1 -C 6烷基，卤素，羟基，羧基，氰基，-CO.RRRRb，-OCO，NR a R b或-NR a R b，其中R a和R b独立地是氢或C 1 -C 6烷基; R 20“，R 21'和R 22”独立地是氢或C 1 -C 6烷基或R 20“，R 21”或R 20“和R 22”一起形成杂环基; R 23“和R 24”独立地是氢，卤素或C 1 -C 6烷基; n为1,2或3; 和n3“是1,2或3.化合物是抗脱水肽酶I的抗生素，并且可用于治疗微生物感染。

    2-(heterocyclylthio)carbapenem derivatives, their preparation and their use as antibiotics
    7.
    发明授权
    2-(heterocyclylthio)carbapenem derivatives, their preparation and their use as antibiotics 失效
    2-（间苯二酚）碳水化合物衍生物，其制备及其作为抗生素的用途

    公开(公告)号：US5104867A

    公开(公告)日：1992-04-14

    申请号：US540878

    申请日：1990-06-20

    申请人： Isao Kawamoto ,  Teruo Tanaka ,  Rokuro Endo ,  Masayuki Iwata ,  Masao Miyauchi

    发明人： Isao Kawamoto ,  Teruo Tanaka ,  Rokuro Endo ,  Masayuki Iwata ,  Masao Miyauchi

    IPC分类号： C07D477/20

    CPC分类号： C07D477/20

    摘要： Compounds of formula (I): ##STR1## in which R.sup.a is a group of formula (II): ##STR2## or a group of formula (III): ##STR3## (where one of R' is a bond to the remainder of the compound, one more of R' is R.sup.2 and the others of R' are all hydrogen), R.sup.1 is hydrogen or methyl, R.sup.2 is hydrogen, optionally substiuted alkyl, halogen, hydroxy, alkoxy, amino, alkanoylamino, alkanoyloxy, alkanoyl, carboxy, alkoxycarbonyl, cyano, --S(O).sub.j R.sup.9 (where j is 0, 1 or 2 and R.sup.9 is alkyl), or --CONR.sup.6 R.sup.7 (which is optionally substituted carbamoyl or heterocyclyl-carbonyl), R.sup.2a is hydrogen, alkyl or alkanoyl, --NR.sup.3 R.sup.4 is optionally substituted amino or heterocyclic, and --COOR.sup.5 is carboxy, --COO.sup.-, --COOM.sub.x (where M is a cation and x is the reciprocal of the valence of the cation M) or protected carboxy and, where --COOR.sup.5 is carboxy, --COOM.sub.x or protected carboxy, the compound of formula (I) also contains an anion; l, m and n are independently 0, 1, 2 or 3, provided that (m+n) is an integer from 2 to 6; p is 0, 1 or 2; Y is a single bond, oxygen, sulfur or R.sup.8 N

    Carbapenem derivatives
    8.
    发明授权
    Carbapenem derivatives 失效
    卡巴培南衍生物

    公开(公告)号：US4771046A

    公开(公告)日：1988-09-13

    申请号：US856696

    申请日：1986-04-25

    申请人： Isao Kawamoto ,  Rokuro Endo ,  Masayuki Iwata

    发明人： Isao Kawamoto ,  Rokuro Endo ,  Masayuki Iwata

    IPC分类号： C07D477/00 ,  A61K31/397 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/425 ,  A61K31/43 ,  A61K31/445 ,  A61K31/495 ,  A61K31/54 ,  A61K31/55 ,  A61P31/04 ,  C07D477/20 ,  C07D499/00 ,  C07D499/88 ,  C07D499/897 ,  C07D487/04

    CPC分类号： C07D477/20 ,  Y02P20/55

    摘要： Carbapenem derivatives useful as antibacterial agents have the formula ##STR1## wherein: X represents a hydrogen atom or a methyl group; andY represents a group of the formula: ##STR2## in which: Z represents an oxygen atom or two hydrogen atoms;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a C.sub.1-4 alkanoyl group, or a C.sub.1-4 alkanesulfonyl group;R.sup.2 represents a hydrogen atom or a hydroxy group, and R.sup.3 represents a carbamoyl group; orR.sup.2 represents a carbamoyloxy group, and R.sup.3 represents a hydrogen atom or a carbamoyl group;R.sup.4 represents a hydrogen atom or a C.sub.1-4 alkyl group; and ##STR3## represents a 4-6 membered saturated heterocyclic group in which the indicated nitrogen atom is the only hetero-atom;or a pharmaceutically acceptable salt or ester thereof.

    摘要翻译： 可用作抗菌剂的碳青霉烯类衍生物具有下式（I）其中：X表示氢原子或甲基; Y表示下式的基团：其中：Z表示氧原子或两个氢原子; R1表示氢原子，C1-4烷基，C1-4烷酰基或C1-4烷基磺酰基; R2表示氢原子或羟基，R3表示氨基甲酰基; 或R 2表示氨基甲酰氧基，R 3表示氢原子或氨基甲酰基; R4表示氢原子或C1-4烷基; 而“IMAGE”表示4-6元饱和杂环基，其中指定的氮原子是唯一的杂原子; 或其药学上可接受的盐或酯。