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30 条记录 (耗时 0.017 秒)

    Improved anti-inflammatory combinations having reduced ulcerogenicity
    21.
    发明公开
    Improved anti-inflammatory combinations having reduced ulcerogenicity 失效
    具有降低的抗炎化合物溃疡效果。

    公开(公告)号：EP0017169A1

    公开(公告)日：1980-10-15

    申请号：EP80101633.8

    申请日：1980-03-27

    申请人： Merck & Co., Inc.

    发明人： Shen, Tsung-Ying

    IPC分类号： A61K31/62 ,  A61K31/61 ,  A61K31/615

    CPC分类号： A61K31/621 ,  A61K31/60 ,  A61K2300/00

    摘要： A novel drug combination for more effective treatment of pain, fever, and inflammation with reduced ulcerogenicity comprising either 1-(p-chlorobenzoyl)-5-methoxy-2-methylindo|e-3-acetic acid (indomethacin), and (b) a member selected from phenyl benzoic acid compounds, especially 2-hydroxy-5-(2',4'-difluorophenyl)benzoic acid (diflunisal), wherein the molar ratio of (b) to (a) is from 0.5 to 1.0 to 15.0 to 1.0; or a member selected from (b) and one or more members selected from ibuprofen, ketoprofen, naproxen, diclofenac sodium, tolmetin, flurbiprofen, indoprofen, benozaprofen, piroxicam.

    New 2,5-diaryl tetryhydrofurans and analogs thereof as paf antagonists
    22.
    发明公开
    New 2,5-diaryl tetryhydrofurans and analogs thereof as paf antagonists 失效
    新的2,5-DIARYL四氢呋喃和其模拟物作为PAF拮抗剂

    公开(公告)号：EP0199324A3

    公开(公告)日：1988-02-10

    申请号：EP86105471

    申请日：1986-04-21

    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： C07D307/10 ,  C07D307/18 ,  C07D405/04 ,  C07D405/14 ,  C07D417/04 ,  A61K31/34

    CPC分类号： C07D307/18 ,  C07D307/12 ,  C07D307/14 ,  C07D307/16 ,  C07D307/20 ,  C07D307/24 ,  C07D307/34 ,  C07D405/04 ,  C07D405/14 ,  C07D407/12 ,  C07D409/14 ,  C07D417/04

    摘要： Compounds of formula:
    are disclosed wherein R and R' are
    (a) hydrogen; (b) haloloweralkyl; (c) halo; (d) CONR 2 R 3 wherein R 2 and R 3 independently represent hydrogen, C 1-8 alkyl, or C 3-8 cycloalkyl; (e) loweralkenyl; (f) -COR 2 ; (g) -CH 2 OR 2 ; (h) loweralkynyl; (i) -CH 2 NR 2 R 2 ; (j) -CH 2 SR 2 ; (k) = O; or (l) -OR 2 ; (m) -R 2 ; Ar and Ar 1 are (a) phenyl or substituted phenyl of formula where R 4 -R 8 independently where R 4 -R 8 independently represent H; R 2 ; YO-wherein Y is loweralkenyl, loweralkynyl, - CH 2 -, -CH 2 C(O)OR 2 , -CH 2 OR 2 , -CH 2 C 3- 8 cycloalkyl, -CH 2 Ar 2 wherein Ar 2 is phenyl or substituted phenyl, -CH 2 -CH(OH)CH 2 OH; R 2 S-(O) n wherein R 2 can only be C 3-8 cycloalkyl and n is 0 to 2; CF 3 SO, CF 3 SO 2 ; - CONR 2 R 3 ; -NR 2 COR 3 ; -OCONH 2 -CR 2 R 3 R 9 wherein R 9 is the same as or different from R Z ; -CH 2 OR 2 ; -CH 2 CO 2 R 2 ; -CH 2 OCOR 3 ; -GH 2 O-CO-OR 2 ; -NHCH 2 COOR 2 ; halo; or N + R 2 R 3 R 9 X- wherein X- is an anion;
    (b) monoheteroaryl, di-or polyheteroaryl or fused heteroaryl containing 1 to 3 of any one or more of the heteroatoms N, S or O; (c) heteroarylalkyl; (d) heterocycloalkyl; or (e) heterocycloalkenyl. These compounds are found to have potent and specific PAF - (Platelet Activating Factor) antagonistic activities.

    Cell-specific glycopeptide ligands
    27.
    发明公开
    Cell-specific glycopeptide ligands 失效
    细胞特异性糖肽配体

    公开(公告)号：EP0063373A1

    公开(公告)日：1982-10-27

    申请号：EP82103247.1

    申请日：1982-04-19

    申请人： Merck & Co., Inc.

    发明人： Ponpipom, Mitree M. ,  Bugianesi, Robert L. ,  Robbins, James C. ,  Shen, Tsung-Ying

    IPC分类号： C07H15/00 ,  C07K9/00

    CPC分类号： C07H15/14 ,  A61K47/549 ,  C07H15/04 ,  C07J31/006 ,  C07J41/005

    摘要： Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides include e.g. N 2 -{N 2 , N 6 -bis[3-(a-D-mannopyranosylthio)propionyl]-L-lysyl} -N 6- [3-(a-D-mannopyranosylthiolpropionyl]-L-lysine (5). Those compounds are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release.

    摘要翻译： 包含糖和氨基酸或肽的缀合物的细胞特异性配体由氨基酸如鸟氨酸，赖氨酸，肽如二赖氨酸，二鸟氨酸或寡聚赖氨酸和具有被合适的封闭基团保护的反应性官能团的选定糖合成。 这种糖肽包括例如 N2- {N2，N6-双[3-（α-D-吡喃甘露糖基硫基）丙酰基] -L-赖氨酰} -N6- [3-（α-D-吡喃甘露糖基硫代丙酰基）-L-赖氨酸（5）这些化合物可用作组织特异性物质 ，当它们通过可代谢或可水解的连接与生物活性材料结合时，将这些生物活性材料输送到选定的部位。这样，抗炎药如地塞米松通过可代谢或可水解的键连接，并且在给予患有炎性疾病的动物 药物到细胞内释放的炎症部位。

    Immunologically active dipeptidyl 4-0-, 6-0-acyl-2-amino-2-deoxy-D-glucose derivatives and methods for their preparation
    28.
    发明公开
    Immunologically active dipeptidyl 4-0-, 6-0-acyl-2-amino-2-deoxy-D-glucose derivatives and methods for their preparation 失效
    4-0，6-0酰基-2-胺-2-脱氧-D-葡萄糖的二肽衍生物具有用于它们的制备的免疫活性和过程。

    公开(公告)号：EP0038750A1

    公开(公告)日：1981-10-28

    申请号：EP81400608.6

    申请日：1981-04-15

    申请人： Merck & Co., Inc.

    发明人： Shen, Tsung-Ying ,  Durette, Philippe L. ,  Dorn, Conrad P, Jr. ,  Doherty, James B. ,  Dean, Richard T.

    IPC分类号： C07H15/04 ,  A61K31/70

    CPC分类号： C07K9/005

    摘要： Immunologically active compounds of the formula:
    wherein:

    R 1 is C 1-7 alkyl; substituted C 1-7 alkyl; phenyl; or substituted phenyl;
    R 2 is hydrogen; C 1-7 alkyl; substituted C 1-7 alkyl; phenyl; substituted phenyl; phenyl C 1-4 alkyl; or substituted phenyl C 1-4 alkyl;
    R 3 and R 4 may be the same or different and are each independently hydrogen, provided that R 3 and R 4 may not both be hydrogen; or
    where
    X is -O-; -S-; or

    R 10 is hydrogen; C 1-30 alkyl; C 2 - 30 alkenyl; C 1-30 alkoxy; phenyl; C 1-20 alkylsulfonyl; or cholesteryl;
    R 11 , R 12 , R 13 , R 14 and R 15 may be the same or different and are each independently hydrogen; C 1-20 alkyl; C 1-20 alkylcarbonyloxy; amino; benzyl; C 1-20 alkoxymethyl; C 1-20 alkylamido; or
    r is 0 or 1; s is 0 or 1; and t is 0 to 20; provided that s may only be 0 when both rand tare greater than 0 or when r is 0 and R 10 is amino; phenyl; substituted phenyl; 1-adamantyl; or heterocycle selected from the group consisting of 2- or 3-furyl, 2- or 3- thienyl, 2- or 3- pyrrolidinyl, 2-, 3- or 4- pyridyl, and 1-tetrazolyl, said heterocycle optionally substituted with C 1-20 alkylcarbonyl; and where R 3 or R 4 is other than hydrogen, the other of R 3 or R 4 may additionally be Ci-4 alkylcarbonyl;
    R 5 is hydrogen or C 1-10 alkyl;
    R 6 is hydrogen or R 6 and R 7 taken together are -(CH 2 ) 3 -;
    R 7 is hydrogen; C 1-7 alkyl; hydroxymethyl; mercaptomethyl; benzyl; or substituted benzyl;
    Rs and R 9 may be the same or different and are each independently COOR, or CONR'R", where R is hydrogen or Ci-7 alkyl, and R' and R" are hydrogen or C 1-3 alkyl;
    when R 5 is C 1-10 alkyl, the stereochemistry at asymmetric . center I is D or L;
    when R 7 is other than hydrogen, the stereochemistry at asymmetric centre II is L; and

    the stereochemistry at asymmetric center III is D; and acid addition and quaternary salts thereof.