Substituted 4-thio pyridones
    21.
    发明授权
    Substituted 4-thio pyridones 失效
    取代的4-硫代吡啶酮

    公开(公告)号:US5668290A

    公开(公告)日:1997-09-16

    申请号:US697384

    申请日:1996-08-23

    CPC分类号: C07D501/00

    摘要: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).

    摘要翻译: 由通式表示的新型头孢烯衍生物,其中酰基取代基是下式的基团:其中Ar是亲脂性任选取代的苯基,萘基或吡啶基; R1表示杂环氨基酸的残基或被羧基和式-NR9R10或基团取代的C2-C10烷基,其中R9和R10各自独立地为氢或C1-C6烷基, 所述C 2 -C 10烷基任选被一个或多个氮原子或羰基中断,并且R 2和R 3各自独立地为氢,烷基或氨基烷基为革兰氏阳性抗菌剂,特别可用于治疗由甲氧西林抗性引起的疾病 金黄色葡萄球菌(以下也称为MRSA或耐甲氧西林金黄色葡萄球菌)。

    Use of chiral 2-(phosphonomethoxy)propyl guanines as antiviral agents
    23.
    发明授权
    Use of chiral 2-(phosphonomethoxy)propyl guanines as antiviral agents 失效
    使用手性2-(膦酰乙氧基)丙基鸟嘌呤作为抗病毒剂

    公开(公告)号:US5302585A

    公开(公告)日:1994-04-12

    申请号:US918507

    申请日:1992-07-22

    IPC分类号: C07F9/6561 A61K31/675

    CPC分类号: C07F9/65616

    摘要: The present invention provides chiral nucleotide analogs having the Formulas I and II ##STR1## and pharmaceutically acceptable salts and solvates thereof, and their pharmaceutical compositions for use in the treatment of viral infections, especially those caused by human immunodeficiency virus (HIV).

    摘要翻译: 本发明提供具有式I和II II及其药学上可接受的盐和溶剂合物的手性核苷酸类似物及其用于治疗病毒感染的药物组合物,特别是由人类免疫缺陷病毒引起的病毒感染 艾滋病毒)。

    Antiviral acyclic phosphonomethoxyalkylsubstituted alkenyl and alkynyl
purine and pyrimidine derivatives
    26.
    发明授权
    Antiviral acyclic phosphonomethoxyalkylsubstituted alkenyl and alkynyl purine and pyrimidine derivatives 失效
    抗病毒非环磷酰氧基烷基取代的烯基和炔基嘌呤和嘧啶衍生物

    公开(公告)号:US5696263A

    公开(公告)日:1997-12-09

    申请号:US350851

    申请日:1994-12-06

    CPC分类号: C07F9/65616 C07F9/65121

    摘要: Compounds are provided that generally have the structure BCH.sub.2 CH(R)OCH.sub.2 P(O)(OH).sub.2, wherein B is a purinyl or pyrimidinyl base and R is C.sub.1-2 alkyl substituted with azido or amino, straight or branched alkenyl of 2-6 carbon atoms or alkynyl of 2-6 carbon atoms, together with the monester and diesters of such compounds with a C.sub.1-5 alkanol, and the corresponding salts, hydrates, solvates, the (R) or (S) isomers and the racemic (RS) mixtures thereof. The compounds have desirable antiviral activity.

    摘要翻译: 提供的化合物通常具有结构BCH 2 CH(OCH 2 P(O)(OH)2),其中B是嘌呤基或嘧啶基,R是被叠氮基或氨基取代的C 1-2烷基,直链或支链的2-6位的链烯基 碳原子或2-6个碳原子的炔基以及这些化合物与C1-5链烷醇的单酯和二酯,以及相应的盐,水合物,溶剂合物,(R)或(S)异构体和外消旋(RS )混合物。 该化合物具有所需的抗病毒活性。

    Cephalosporin derviatives
    29.
    发明授权
    Cephalosporin derviatives 失效
    头孢菌素衍生物

    公开(公告)号:US5620969A

    公开(公告)日:1997-04-15

    申请号:US427778

    申请日:1995-04-25

    CPC分类号: C07D501/00

    摘要: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).

    摘要翻译: 由通式表示的新型头孢烯衍生物,其中酰基取代基是下式的基团:其中Ar是亲脂性任选取代的苯基,萘基或吡啶基; R1表示杂环氨基酸的残基或被羧基和式-NR9R10或基团取代的C2-C10烷基,其中R9和R10各自独立地为氢或C1-C6烷基, 所述C 2 -C 10烷基任选被一个或多个氮原子或羰基中断,并且R 2和R 3各自独立地为氢,烷基或氨基烷基为革兰氏阳性抗菌剂,特别可用于治疗由甲氧西林抗性引起的疾病 金黄色葡萄球菌(以下也称为MRSA或耐甲氧西林金黄色葡萄球菌)。