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    4,5-dihydro pyrazole compounds
    1.
    发明授权
    4,5-dihydro pyrazole compounds 失效
    4,5-二氢吡唑化合物

    公开(公告)号：US4956378A

    公开(公告)日：1990-09-11

    申请号：US286268

    申请日：1989-02-10

    申请人： Sidney C. Burford ,  David N. Hardern

    发明人： Sidney C. Burford ,  David N. Hardern

    IPC分类号： C07D231/06 ,  C07D401/04 ,  C07D401/12

    CPC分类号： C07D231/06 ,  C07D401/04 ,  C07D401/12

    摘要： There are described compounds of formula I, ##STR1## in which Ar.sub.1 and Ar.sub.2, which may be the same or different, each independently represent phenyl or pyridinyl, the phenyl or the pyridinyl each optionally being substituted by one or more of halogen; hydroxy; --COOR.sub.12 ; trihalomethyl; alkoxy C1 to 6; alkyl C1 to 6; --NR.sub.1 R.sub.2 ; alkoxy C1 to 6 substituted by --NR.sub.1 R.sub.2 or by phenyl; or alkyl C1 to 6 substituted by --NR.sub.1 R.sub.2 or by --COOR.sub.12 ;R.sub.1 and R.sub.2, which may be the same or different, each independently represent hydrogen or alkyl C1 to 6,R.sub.3 represents hydrogen, alkyl C1 to 6, alkanoyl C1 to 6, benzoyl, --COOR.sub.8, or --CONHR.sub.11,R.sub.4, R.sub.5, R.sub.6 and R.sub.7, which may be the same or different each independently represent hydrogen, alkyl C1 to 6 or phenyl;R.sub.8 represents alkyl C1 to 6 or aryl,R.sub.11 represents alkyl C1 to 6 or aryl,R.sub.12 represents hydrogen or alkyl C1 to 6, and pharmaceutically acceptable derivatives thereof.There are also described compositions containing the compounds and methods for their preparation. The compounds are indicated for use as pharmaceutical, e.g. antiinflammatory agents.

    Pyrazoline compounds compositions and use
    2.
    发明授权
    Pyrazoline compounds compositions and use 失效
    吡唑啉化合物组合物和用途

    公开(公告)号：US4824859A

    公开(公告)日：1989-04-25

    申请号：US606867

    申请日：1984-05-03

    申请人： Sidney C. Burford ,  David N. Hardern

    发明人： Sidney C. Burford ,  David N. Hardern

    IPC分类号： C07D231/06 ,  C07D401/04 ,  C07D401/12 ,  A61K31/415

    CPC分类号： C07D231/06 ,  C07D401/04 ,  C07D401/12

    摘要： There are described compounds of formula I, ##STR1## in which Ar.sub.1 and Ar.sub.2, which may be the same or different, each independently represent phenyl or pyridinyl, the phenyl or the pyridinyl each optionally being substituted by one or more of halogen; hydroxy; --COOR.sub.12 ; trihalomethyl; alkoxy C1 to 6; alkyl C1 to 6; --NR.sub.1 R.sub.2 ; alkoxy C1 to 6 substituted by --NR.sub.1 R.sub.2 or by phenyl; or alkyl C1 to 6 substituted by --NR.sub.1 R.sub.2 or by --COOR.sub.12 ;R.sub.1 and R.sub.2, which may be the same or different, each independently represent hydrogen or alkyl C1 to 6,R.sub.3 represents hydrogen, alkyl C1 to 6, alkanoyl C1 to 6, benzoyl, --COOR.sub.8, or --CONHR.sub.11,R.sub.4, R.sub.5, R.sub.6 and R.sub.7, which may be the same or different each independently represent hydrogen, alkyl C1 to 6 or phenyl,R.sub.8 represents alkyl C1 to 6 or aryl,R.sub.11 represents alkyl C1 to 6 or aryl,R.sub.12 represents hydrogen or alkyl C1 to 6, and pharmaceutically acceptable derivatives thereof.There are also described compositions containing the compounds and methods for their preparation.The compounds are indicated for use as pharmaceutical, eg antiinflammatory agents.

    摘要翻译： 描述了式I的化合物，其中Ar 1和Ar 2可以相同或不同，各自独立地表示苯基或吡啶基，苯基或吡啶基各自任选被一个或多个卤素取代; 羟基; -COOR12; 三卤甲基 烷氧基C1至6; 烷基C1至6; -NR1R2; 被-NR 1 R 2取代的C 1-6烷氧基或苯基取代; 或被-NR 1 R 2或-COOR 12取代的C 1-6的烷基; R1和R2可以相同或不同，各自独立地表示氢或C1至6的烷基，R3表示氢，C1至6的烷基，C1至6的烷酰基，苯甲酰基，-COOR8或-CONHR11，R4，R5，R6 和R 7可以相同或不同，各自独立地表示氢，烷基C1至6或苯基，R8表示烷基C1至6或芳基，R11表示烷基C1至6或芳基，R12表示氢或C1-6烷基，和 药学上可接受的衍生物 还描述了含有这些化合物的组合物及其制备方法。 化合物被指示用作药物，例如抗炎剂。

    Anti-inflammator 1,n-diarylpyrazol-3-amines
    3.
    发明授权
    Anti-inflammator 1,n-diarylpyrazol-3-amines 失效
    抗炎剂1，正二芳基吡唑-3-胺

    公开(公告)号：US4810719A

    公开(公告)日：1989-03-07

    申请号：US733591

    申请日：1985-05-10

    申请人： Richard A. Appleton ,  Sidney C. Burford ,  David N. Hardern ,  David Wilkinson

    发明人： Richard A. Appleton ,  Sidney C. Burford ,  David N. Hardern ,  David Wilkinson

    IPC分类号： A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/47 ,  A61K31/505 ,  A61P29/00 ,  C07D213/57 ,  C07D231/06 ,  C07D231/38 ,  C07D333/00 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/00 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D417/12

    CPC分类号： C07D231/06 ,  C07C255/00 ,  C07D213/57 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D417/12

    摘要： There are described compounds of formula I, ##STR1## in which either R.sub.2 represents hydrogen, alkyl or Ar.sub.2, andR.sub.3 represents hydrogen, alkyl or alkyl substituted by Ar.sub.3 ;or R.sub.2 and R.sub.3 together form the chain --(CH.sub.2).sub.m --;R.sub.4 and R.sub.5, which may be the same or different, each independently represent hydrogen, halogen, Ar, alkyl, or alkyl substituted by Ar,Ar.sub.1, Ar.sub.2 and Ar, which may be the same or different each independently represent aryl or aryl substituted by one or more ofhalogen, hydroxy, --CN, --COR.sub.6, trihalomethyl, alkoxy, alkoxy substituted by --COR.sub.6, alkoxy substituted by --NR.sub.7 R.sub.8, alkyl, alkyl substituted by --COR.sub.6, alkyl substituted by NR.sub.7 R.sub.8, alkoxy substituted by Ar.sub.3, S(O).sub.n R.sub.9, --NR.sub.7 R.sub.8 or OAr.sub.3 ;R.sub.6 represents --OR.sub.10, --NR.sub.7 R.sub.8, hydrogen or alkyl;R.sub.7 and R.sub.8, which may be the same or different, each independently represent hydrogen, alkyl, alkanoyl or Ar.sub.3 ;R.sub.9 represents alkyl or Ar.sub.3 ;R.sub.10 represents hydrogen, alkyl or Ar.sub.3 ;m represents an integer from 3 to 6 inclusive;n represents 0, 1 or 2; andAr.sub.3 represents unsubstituted aryl;or a pharmaceutically acceptable derivative thereof.There are also described compositions containing the compounds and methods for their preparation.The compounds are indicated for use as pharmaceutical, e.g. anti-inflammatory, agents.

    摘要翻译： 描述式I化合物，其中R 2表示氢，烷基或Ar 2，R 3表示氢，被Ar 3取代的烷基或烷基; 或R 2和R 3一起形成链 - （CH 2）m - ; R 4和R 5可以相同或不同，各自独立地表示氢，卤素，Ar，烷基或被Ar，Ar1，Ar2和Ar取代的烷基，它们可以相同或不同，各自独立地表示被 一个或多个卤素，羟基，-CN，-COR 6，三卤代甲基，烷氧基，被-COR 6取代的烷氧基，被-NR 7 R 8取代的烷氧基，被-COR 6取代的烷基，被NR 7 R 8取代的烷基，被Ar 3取代的烷氧基，S（ O）n R 9，-NR 7 R 8或OAr 3; R6表示-OR10，-NR7R8，氢或烷基; R 7和R 8可以相同或不同，各自独立地表示氢，烷基，烷酰基或Ar 3; R9代表烷基或Ar3; R 10表示氢，烷基或Ar 3; m表示3〜6的整数， n表示0,1或2; 和Ar 3表示未取代的芳基; 或其药学上可接受的衍生物。 还描述了含有这些化合物的组合物及其制备方法。 化合物指示用作药物，例如， 抗炎，药剂。

    Macrocyclic compounds
    6.
    发明授权
    Macrocyclic compounds 失效
    大环化合物

    公开(公告)号：US5376663A

    公开(公告)日：1994-12-27

    申请号：US391538

    申请日：1989-07-25

    申请人： Martin E. Cooper ,  David K. Donald ,  David N. Hardern

    发明人： Martin E. Cooper ,  David K. Donald ,  David N. Hardern

    IPC分类号： C07D498/18 ,  C07D498/22 ,  C07H19/01 ,  A61K31/395 ,  A61K31/445 ,  C07D498/16

    CPC分类号： C07D498/18 ,  C07D498/22 ,  C07H19/01

    摘要： Compounds of formula (I), in which [R.sup.1 and R.sup.2 ], [R.sup.3 and R.sup.4 ] and [R.sup.5 and R.sup.6 ] represent a carbon-carbon bond or two hydrogen atoms; R.sup.2 additionally represents alkyl; R.sup.7, R.sup.8 and R.sup.9 represent groups including H or OH, R.sup.10 has various significances including alkyl and alkenyl; X and Y represent groups including O and (H, OH); R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.22 and R.sup.23 represent H or alkyl; R.sup.20 and R.sup.21 represent groups including O, (H, OH) and (H, O-alkyl), n is 1, 2 or 3, and in addition, Y, R.sup.10 and R.sup.23, together with the carbon atoms to which they are attached, may represent a heterocyclic ring, (with certain provisos) are described. Processes for making the compounds and pharmaceutical formulations containing them, e.g. for use as immunosuppressive agents, are also described. ##STR1##

    摘要翻译： PCT No.PCT / GB88 / 01093 Sec。 371日期：1989年7月25日 102（e）日期1989年7月25日PCT提交1988年12月2日PCT公布。 出版物WO89 / 05304 （I）化合物，其中[R 1和R 2]，[R 3和R 4]和[R 5和R 6]表示碳 - 碳键或两个氢原子; R2另外表示烷基; R7，R8和R9表示包括H或OH的基团，R10具有各种含义，包括烷基和烯基; X和Y表示包括O和（H，OH）的基团; R14，R15，R16，R17，R18，R19，R22和R23表示H或烷基; R 20和R 21表示包括O，（H，OH）和（H，O-烷基），n为1,2或3的基团，此外，Y，R 10和R 23与它们所连接的碳原子一起 可以表示杂环（具有一定条件）。 制备化合物和含有它们的药物制剂的方法，例如 也用作免疫抑制剂。

    Macrocyclic compounds
    8.
    发明授权
    Macrocyclic compounds 失效
    大环化合物

    公开(公告)号：US5179087A

    公开(公告)日：1993-01-12

    申请号：US568855

    申请日：1990-08-17

    申请人： David K. Donald ,  David N. Hardern ,  Martin E. Cooper ,  Mark Furber

    发明人： David K. Donald ,  David N. Hardern ,  Martin E. Cooper ,  Mark Furber

    IPC分类号： C07D498/18 ,  A61K31/445 ,  A61P37/06 ,  C07H19/01

    CPC分类号： C07H19/01

    摘要： There are described compounds of formula I, ##STR1## wherein R.sup.1 represents H or OH; R.sup.2 represents H; in addition, R.sup.1 and R.sup.2 may together represent a second carbon-carbon bond between the carbon atoms to which they are attached; R.sup.3 represents OH or OCH.sub.3 ; X represents O or (H,OH); and Y represents O or N--OR.sup.4, in which R.sup.4 represents H or alkyl C.sub.1-6 ; provided that when R.sup.1 is OH, R.sup.2 is H and X is O, then Y does not represent O.Processes for their production and compositions containing them, eg. for use as immunosuppressive agents, are also described.