利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

39 条记录 (耗时 0.023 秒)

    Morpholin- and thiomorpholin-4-ylamides
    21.
    发明授权
    Morpholin- and thiomorpholin-4-ylamides 失效
    吗啉和硫代吗啉-4-基酰胺

    公开(公告)号：US5409927A

    公开(公告)日：1995-04-25

    申请号：US36748

    申请日：1993-03-25

    申请人： Guido Bold ,  Alexander Fassler ,  Marc Lang ,  Peter Schneider

    发明人： Guido Bold ,  Alexander Fassler ,  Marc Lang ,  Peter Schneider

    IPC分类号： A61K38/00 ,  A61P31/12 ,  A61P31/18 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81 ,  A61K31/535 ,  C07D265/30

    CPC分类号： C07K5/0207 ,  A61K38/00

    摘要： There are described compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or lower alkyl,R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl, phenyl- or naphthyl-lower alkoxycarbonyl, heterocyclylcarbonyl wherein heterocyclyl contains 5 or 6 ring atoms, is saturated and is bonded to the carbonyl group via a ring nitrogen atom and, in addition to the bonding nitrogen atom, contains as ring member one or more further hetero atoms selected from unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted NH, O, S, S.dbd.O and SO.sub.2, or is lower alkanoyl, phenyl- or naphthyl-lower alkanoyl or lower alkanesulfonyl,R.sub.3 is morpholino, thiomorpholino, S-oxothiomorpholino or S,S-dioxothiomorpholino, the heterocyclyl radical in heterocyclylcarbonyl R.sub.2 having the same definition as R.sub.3 or having a definition other than R.sub.3, andR.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, cyano, trifluoromethyl or fluorine, and salts of those compounds where salt-forming groups are present. These compounds are inhibitors of HIV-protease and are used in the treatment of ADS.

    摘要翻译： 描述了式I的化合物其中R 1是氢或低级烷基，R 2是氢，低级烷基，低级烷氧基羰基，苯基或萘基 - 低级烷氧基羰基，其中杂环基含有5或6个环原子的杂环基羰基是 并且通过环氮原子与羰基键合，并且除了键合氮原子外，还含有一个或多个选自未取代的或C 1 -C 4烷基取代的NH，O，S，S = O和SO 2，或者是低级烷酰基，苯基或萘基 - 低级烷酰基或低级链烷磺酰基，R3是吗啉代，硫代吗啉代，S-氧硫代吗啉代或S，S-二氧代硫代吗啉代，杂环基羰基R2中的杂环基与R3具有相同的定义或具有 除R3以外的定义，R4为氢，羟基，C1-C4烷氧基，氰基，三氟甲基或氟，以及存在成盐基团的那些化合物的盐。 这些化合物是HIV-蛋白酶的抑制剂，用于治疗ADS。

    Bicyclic beta-lactam carboxylic acids
    25.
    发明授权
    Bicyclic beta-lactam carboxylic acids 失效
    双环β-内酰胺羧酸

    公开(公告)号：US4965260A

    公开(公告)日：1990-10-23

    申请号：US153377

    申请日：1988-02-08

    申请人： Marc Lang

    发明人： Marc Lang

    IPC分类号： C07D499/88

    CPC分类号： C07D499/88

    摘要： Compounds of the formula ##STR1## in which R.sub.1 is lower alkyl substituted by hydroxy or by protected hydroxy, R.sub.2 represents carboxy or functionally modified carboxy, R.sub.3 is hydrogen, amino, mono- or di-substituted amino, carbamoyl, hydroxy, protected hydroxy, carbamoyloxy, lower alkoxy, halogen, lower alkanoyl, sulphamoyl or heteroarylthio, each of R.sub.4 and R.sub.5, independently of the other, represents hydrogen, lower alkyl, hydroxy, protected hydroxy, lower alkoxy, halogen, amino, protected amino, lower alkanoylamino or carbamoyl, or R.sub.4 and R.sub.5 together represent methylenedioxy, Y represents a group of the formula --O--, --S-- or --NR.sub.6 --, R.sub.6 is hydrogen or lower alkyl, A.sub.1 represents lower alkylene or unsubstituted or substituted phenylene and A.sub.2 represents a direct bond or lower alkylene, and salts of such compounds, have antibacterial activity. The compounds of the formula I are manufactured by processes that are known per se.

    摘要翻译： 式（I）化合物，其中R 1是被羟基或保护的羟基取代的低级烷基，R 2表示羧基或官能改性的羧基，R 3是氢，氨基，一取代或二取代的氨基，氨基甲酰基，羟基， 保护的羟基，氨基甲酰氧基，低级烷氧基，卤素，低级烷酰基，氨磺酰基或杂芳硫基，R4和R5各自独立地代表氢，低级烷基，羟基，保护的羟基，低级烷氧基，卤素，氨基，被保护的氨基，低级 烷酰基氨基或氨基甲酰基，或者R4和R5一起代表亚甲二氧基，Y代表式为-O - ， - S-或-NR6-的基团，R6为氢或低级烷基，A1为低级亚烷基或未取代或取代的亚苯基，A2为 直接键合或低级亚烷基，以及这些化合物的盐具有抗菌活性。 式I的化合物通过本身已知的方法制备。

    Penen compounds
    28.
    发明授权
    Penen compounds 失效
    Penen化合物

    公开(公告)号：US4826832A

    公开(公告)日：1989-05-02

    申请号：US42768

    申请日：1987-04-27

    申请人： Marc Lang

    发明人： Marc Lang

    IPC分类号： C07D499/897 ,  A61K31/43 ,  A61P31/04 ,  C07D499/06 ,  C07D499/88 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/88

    摘要： Compounds of the formula ##STR1## in which R.sub.1 represents lower alkyl substituted by hydroxy or by protected hydroxy, R.sub.2 represents carboxy or functionally modified carboxy, and R.sub.3 represents optionally substituted 3-pyridyl or optionally substituted 4-pyridyl, and pharmaceutically acceptable salts of such compounds, have antibacterial activity. The compounds of the formula I can be manufactured according to processes known per se.

    摘要翻译： 式（I）的化合物，其中R 1表示被羟基或保护的羟基取代的低级烷基，R 2表示羧基或官能改性的羧基，R 3表示任选取代的3-吡啶基或任选取代的4-吡啶基， 这些化合物的盐具有抗菌活性。 式I的化合物可以根据本身已知的方法制备。

    6-substituted penem compounds
    29.
    发明授权
    6-substituted penem compounds 失效
    6-取代的penem化合物

    公开(公告)号：US4692442A

    公开(公告)日：1987-09-08

    申请号：US208105

    申请日：1980-11-18

    申请人： Jacques Gosteli ,  Ivan Ernest ,  Marc Lang ,  Robert B. Woodward

    发明人： Jacques Gosteli ,  Ivan Ernest ,  Marc Lang ,  Robert B. Woodward

    IPC分类号： A61K31/397 ,  A61K31/43 ,  A61P31/04 ,  C07D205/08 ,  C07D205/09 ,  C07D417/12 ,  C07D499/04 ,  C07D499/06 ,  C07D499/86 ,  C07D499/861 ,  C07D499/87 ,  C07D499/88 ,  C07D499/881 ,  C07D499/883 ,  C07D499/887 ,  C07D499/897 ,  C07F9/568 ,  C07D499/00

    CPC分类号： C07D499/88 ,  C07D205/08 ,  C07D205/09 ,  C07F9/5683

    摘要： The invention relates to 2-penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.a represents an organic radical bonded by a carbon atom to the ring carbon atom, a free, etherified or esterified hydroxy or mercapto group or a halogen atom, R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom, or an etherified mercapto group, and R.sub.2 represents a hydroxy group or an R.sub.2.sup.A radical that together with the carbonyl grouping --C(.dbd.O)-- forms a protected carboxyl group, and to salts of such compounds with salt-forming groups, processes for the manufacture of such compounds, pharmaceutical preparations containing compounds of the formula I with pharmacological properties, and their use. The compounds have antibiotic activity.

    摘要翻译： 本发明涉及式（Ⅰ）的2-青霉烯-3-羧酸化合物，其中Ra表示通过碳原子与环碳原子键合的有机基团，游离醚化或酯化的羟基或巯基 或卤素原子，R1表示氢，由碳原子键合至环碳原子的有机基团或醚化巯基，R 2表示与羰基-C（= O）一起形成的羟基或R2A基团 ）形成保护的羧基，以及这些化合物与成盐基团的盐，制备这些化合物的方法，含有药理学性质的式I化合物的药物制剂及其用途。 这些化合物具有抗生素活性。