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30 条记录 (耗时 0.013 秒)

    New 2,5-diaryl tetrahydrofurans and analogs thereof as paf-antagonists
    1.
    发明公开
    New 2,5-diaryl tetrahydrofurans and analogs thereof as paf-antagonists 失效
    新的2,5-DIARYL四氢呋喃和其类似物作为PAF拮抗剂

    公开(公告)号：EP0144804A3

    公开(公告)日：1986-01-08

    申请号：EP84113600

    申请日：1984-11-12

    申请人： MERCK & CO. INC.

    发明人： Biftu, Tesfaye ,  Hwang, San-Bao ,  Doebber, Thomas W. ,  Beattie, Thomas R. ,  Shen, Tsung-Ying

    IPC分类号： C07D307/12 ,  C07D307/18 ,  C07D307/20 ,  A61K31/34

    CPC分类号： C07D307/18 ,  C07C45/00 ,  C07C45/72 ,  C07D307/12 ,  C07D307/14 ,  C07D307/20 ,  C07C49/84

    摘要： Compounds of formula:
    are disclosed wherein R and R' independently are
    (a) hydrogen; (b) haloloweralkyl; (c) halo; (d) CONR 2 R 3 wherein R 2 and R 3 independently represent C 1-6 alkyl and hydrogen; (e) loweralkenyl; (f) -COR 2 (g) -CH 2 OR 2 ; (h) loweralkynyl; (i) -CH 2 -NR 2 R 3 ; (j) -CH 2 SR 2 ; (k) =0; or (I) -OR 2 ; Ar and Ar' are the same or different from each other and are (a) phenyl or substituted phenyl of formula
    where R 4 -R 8 independently represent H, RO-, R 2 S-, R 2 SO 2 -,CF 3 O-, CF 3 S-, R 2 R 3 N-, -OCH 2 CO 2 R 2 , -SO 2 NR 2 R 3 , -C0 2 R 2 , -NR 2 SO 2 R 3 , COR 2 , N0 2 , or CN or R 4 -R 5 , R 5 -R 6 , R 6 -R 7 and R 7 -R 8 are joined together forming a bridge;
    (b) pyrryl or substituted pyrryl; (c) furyl or substituted furyl; (d) pyridyl or substituted pyridyl; or (e) thiophene or substituted thiophene. These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby are useful in the treatment of varous diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.

    Tricyclic derivatives of substituted pyrrole acids as analgesic and anti-inflammatory agents
    3.
    发明公开
    Tricyclic derivatives of substituted pyrrole acids as analgesic and anti-inflammatory agents 失效
    Tricyclische衍生取代器Pyrrolsäurenals analgetische undentzündungshemmendeMittel。

    公开(公告)号：EP0068460A1

    公开(公告)日：1983-01-05

    申请号：EP82105637.1

    申请日：1982-06-25

    申请人： Merck & Co., Inc.

    发明人： Doherty, James B. ,  Dorn, Conrad P. ,  Witzel, Bruce E. ,  Allison, Debra L. ,  Shen, Tsung-Ying ,  Finke, Paul E.

    IPC分类号： C07D491/044 ,  C07D495/04 ,  C07D487/04 ,  C07D209/70 ,  A61K31/55 ,  A61K31/38 ,  A61K31/365 ,  A61K31/385

    CPC分类号： C07D487/04 ,  C07D207/34 ,  C07D209/70 ,  C07D313/08 ,  C07D491/04 ,  C07D495/04

    摘要： Compounds having the structural formula:
    are disclosed wherein
    there are 0-4 R groups and

    R is e.g. hydrogen, lower alkyl, halo-loweralkyl, hydroxy, lower alkoxy, halo, lower alkylthio or lower alkylsulfinyl;
    R 1 is e.g. hydrogen or lower alkyl;


    Z is (a) -(CH 2 ) o-n , n being 0-10;
    (b) -CO(CH 2 ) 1-n -;
    (c) -(CH 2 ) 1-n -CO-; or
    (d)

    R 2 is e.g. hydrogen or lower alkyl;
    R 3 is hydrogen, lower alkyl, hydroxy, loveralkoxy or halo; and
    X-Y is e.g. -O-CH 2 - or -S-CH 2 -.

    Those compounds have been prepared via hydrolysis of a precursor or decarboxylation of a precursor-diacid. These tricyclic compounds are found to have high analgesic and anti-inflammatory activities but low ulcerogenic side effects.

    摘要翻译： 公开了具有结构式：的化合物，其中存在0-4个R基团，并且R为例如。 氢，低级烷基，卤代低级烷基，羟基，低级烷氧基，卤素，低级烷硫基或低级烷基亚磺酰基; R 1是例如。 氢或低级烷基; Z是（a） - （CH 2）0-n，n是0-10; （b）-CO（CH 2）1-n; （c） - （CH 2）1-n -CO-; 或（d） - @@ - （CH 2）0-n; R 2是例如。 氢或低级烷基; R 3是氢，低级烷基，羟基，卤代烷氧基或卤素; 而X-Y是例如。 -O-CH 2 - 或-S-CH 2 - 。 这些化合物是通过前体的水解或前体二酸的脱羧制备的。 发现这些三环化合物具有高的止痛和抗炎活性，但是具有低的溃疡性副作用。

    New 2,5-diaryl tetrahydrofurans and analogs thereof as paf-antagonists
    7.
    发明公开
    New 2,5-diaryl tetrahydrofurans and analogs thereof as paf-antagonists 失效
    2,5-二芳基四氢呋喃及其类似物作为血小板活化因子拮抗剂。

    公开(公告)号：EP0144804A2

    公开(公告)日：1985-06-19

    申请号：EP84113600.5

    申请日：1984-11-12

    申请人： Merck & Co., Inc.

    发明人： Biftu, Tesfaye ,  Hwang, San-Bao ,  Doebber, Thomas W. ,  Beattie, Thomas R. ,  Shen, Tsung-Ying

    IPC分类号： C07D307/12 ,  C07D307/18 ,  C07D307/20 ,  A61K31/34

    CPC分类号： C07D307/18 ,  C07C45/00 ,  C07C45/72 ,  C07D307/12 ,  C07D307/14 ,  C07D307/20 ,  C07C49/84

    摘要： Compounds of formula:
    are disclosed wherein R and R' independently are

    (a) hydrogen;
    (b) haloloweralkyl;
    (c) halo;
    (d) CONR 2 R 3 wherein R 2 and R 3 independently represent C 1-6 alkyl and hydrogen;
    (e) loweralkenyl;
    (f) -COR 2
    (g) -CH 2 OR 2 ;
    (h) loweralkynyl;
    (i) -CH 2 -NR 2 R 3 ;
    (j) -CH 2 SR 2 ;
    (k) =0; or
    (I) -OR 2 ;

    Ar and Ar' are the same or different from each other and are (a) phenyl or substituted phenyl of formula
    where R 4 -R 8 independently represent H, RO-, R 2 S-, R 2 SO 2 -,CF 3 O-, CF 3 S-, R 2 R 3 N-, -OCH 2 CO 2 R 2 , -SO 2 NR 2 R 3 , -C0 2 R 2 , -NR 2 SO 2 R 3 , COR 2 , N0 2 , or CN or R 4 -R 5 , R 5 -R 6 , R 6 -R 7 and R 7 -R 8 are joined together forming a bridge;

    (b) pyrryl or substituted pyrryl;
    (c) furyl or substituted furyl;
    (d) pyridyl or substituted pyridyl; or
    (e) thiophene or substituted thiophene.

    These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby are useful in the treatment of varous diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.

    摘要翻译： 式的化合物：... ...被盘游离缺失worin R和R <1>独立地是...（a）氢; ...（B）卤代低级烷基; ...（C）卤素; ...（D）CONR <2> [R <3> worinř<2>和R <3>独立地表示C 1-6烷基和氢; ...（E）低级链烯基; ...（F）-COR <2> ...（G）-CH 2 OR <2>，...（H）loweralkynyl; （I）-CH2-NR <2> [R <3>; ...（J） - CH 2 SR <2>; ...（K）= 0; 或...（L）-O-R <2>; ... Ar和Ar <1>是相同的或彼此不同的并且是...的（a）苯基或式的取代的苯基...... ...其中R <4> -R <8>独立地表示H，RO-，R <2> S-，R <2> SO 2，CF 3 O-，CF3S-，R <2> [R <3> N-，-OCH2CO2R <2>，-SO 2 NR < 2> [R <3>，-CO 2 R <2>，-NR <2> SO 2 <3>，COR <2>，NO 2，或CN或R <4> -R <5>，R <5> -R < 6>，R <6> -R <7>和R <7> -R <8>连接在一起形成一个桥; ...（b）吡咯基或吡咯基substituiertem; ...（C）呋喃基或呋喃基substituiertem; ...（D ）吡啶基或取代的吡啶基; 或者......（五）噻吩或噻吩substituiertem。 ... 被发现这些化合物具有强而特异性的PAF（血小板活化因子）拮抗活性和从而处于varous疾病或病症由PAF介导的治疗中有用，例如，炎症，心血管疾病，哮喘，肺 水肿，成人呼吸窘迫综合征，疼痛，血小板聚集。

    Immunologically active dipeptidyl saccharides and methods of preparation
    9.
    发明公开
    Immunologically active dipeptidyl saccharides and methods of preparation 失效
    免疫活性的二肽的糖类及其制备方法。

    公开(公告)号：EP0014159A1

    公开(公告)日：1980-08-06

    申请号：EP80400130.3

    申请日：1980-01-28

    申请人： Merck & Co., Inc.

    发明人： Durette, Philippe L. ,  Shen, Tsung-Ying

    IPC分类号： C07H15/04 ,  C07H15/12 ,  C07H15/18 ,  C07H15/20 ,  A61K31/70

    CPC分类号： C07K9/005

    摘要： 2-Amino-2-deoxy-glycoses of the general structural formula:

    wherein

    R 1 is hydrogen, alkyl (1-7C), substituted alkyl (1-7C), phenyl, substituted phenyl, benzyl, or substituted benzyl;
    R 2 is alkyl, substituted alkyl, phenyl, or substituted phenyl;
    R 3 is H or lower alkyl (1-10C) with the proviso that when the aminoglycose has the 2-amino-2-deoxy-D-glucose configuration, R 3 cannot be H;
    R 4 and R 5 are same or different and are H, aliphatic or aromatic acyl (2-21 C) or substituted acyl (2-21 C);
    R 6 is H, or R 6 -R 7 together is -CH 2 -CH 2 -CH 2 -,
    R 7 is H, alkyl (1-7C), hydroxymethyl, mercaptomethyl, benzyl, or substituted benzyl;
    R 8 and Rg each is carboxyl, esterified carboxyl (1-7C), amidated carboxyl, or mono- or di-alkyl-(1-3C)-amidated carboxyl;
    provided that when R 3 is lower alkyl, the stereochemistry at asymmetric center I can be either D or L, but that when the caminoglycose has the 2-amino-2-deoxy-D-glucose configuration, the stereochemistry at I cannot be D;
    when R 7 is not H, the stereochemistry at asymmetric center II is either L or D; and
    the stereochemistry at asymmetric center III is D.

    These compounds possess immunostimulatory properties.