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    ATRIAL PEPTIDE DERIVATIVES
    123.
    发明申请
    ATRIAL PEPTIDE DERIVATIVES 审中-公开
    ATRIAL肽衍生物

    公开(公告)号：WO1990014362A1

    公开(公告)日：1990-11-29

    申请号：PCT/US1990002917

    申请日：1990-05-23

    Applicant: ABBOTT LABORATORIES ,  LUCAS, Scott, D. ,  ROCKWAY, Todd, W. ,  DAVIDSEN, Steven, K. ,  THOMAS, A., Mitchell ,  VON GELDERN, Thomas, W.

    Inventor： ABBOTT LABORATORIES

    IPC: C07K07/08

    CPC classification number: C07K14/58 ,  A61K38/00

    Abstract: The present invention provides novel peptides which exhibit useful hypotensive, natriuretic, diuretic, renovasodilating, reno-protective, smooth muscle relaxant, and vasorelaxant activities. The novel atrial peptides of the instant invention are encompassed by formula (I) or a pharmaceutically acceptable salt, ester or amide thereof, wherein R is selected from hydrogen, AcetylArg, Aha, Arg, Cit, His, Lys, Orn and Ser-Ser; R is a sulfur-containing group; R is a hydrophobic amino acid or dipeptide; R is a dipeptide spacer or a tripeptide of the formula X-Y, where X is a dipeptide spacer and Y is a basic amino acid; R is a hydrophobic amino acid; R is a peptide of up to three amino acids; R is selected from Cha, Phe, Cha-Arg, Phe-Arg, (D)Phe-Arg, Phe-(D)Arg, Phe Arg, Leu-Arg, Ala-Arg, Arg and Gly-Ala; and R is a sulfur-containing group.

    Abstract translation: 本发明提供了具有有用的低血压，利尿钠，利尿剂，改善释放，肾保护，平滑肌松弛剂和血管舒张活性的新型肽。 本发明的新型心房肽包括式（I）或其药学上可接受的盐，酯或酰胺，其中R 1选自氢，乙酰基氨基，氨基，Arg，Cit，His，Lys，Orn和 丝氨酸 - 丝氨酸; R 2是含硫基团; R 3是疏水性氨基酸或二肽; R 4是二肽间隔物或式X-Y的三肽，其中X是二肽间隔物，Y是碱性氨基酸; R 5是疏水性氨基酸; R 6是多至三个氨基酸的肽; R 7选自Cha，Phe，Cha-Arg，Phe-Arg，（D）Phe-Arg，Phe-（D）Arg，Phe> Arg，Leu-Arg，Ala-Arg，Arg和Gly -翼; R 8为含硫基团。

    4-HYDROXYTHIAZOLES AS 5-LIPOXYGENASE INHIBITORS
    124.
    发明申请
    4-HYDROXYTHIAZOLES AS 5-LIPOXYGENASE INHIBITORS 审中-公开
    4-羟基噻唑作为5-LIPOXYGENASE抑制剂

    公开(公告)号：WO1990009381A1

    公开(公告)日：1990-08-23

    申请号：PCT/US1990000653

    申请日：1990-02-02

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  BROOKS, Dee, W. ,  KERDESKY, Francis, A., J. ,  HOLMS, James, H.

    IPC: C07D417/04

    CPC classification number: C07D417/04 ,  C07D277/34 ,  C07D277/54 ,  C07D277/64

    Abstract: A composition for the inhibition of lipoxygenase enzymes comprising a pharmaceutically acceptable carrier and a compound of formula (I), wherein R1 and R2 are independently selected from the group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, arylalkenyl, reduced heteroaryl, and reduced heteroarylalkyl and substituted derivatives thereof having one or more substituents independently selected from the group consisting of halogen, alkyl, halosubstituted alkyl, aryl, arylalkyl, reduced heteroaryl, arylalkoxy, cyano, nitro, COR4, SO2R4, NR5R6, OR6, COCX1X2NR6R7, CON(OH)R6, NR6COR4, CR5(NH2)CO2R5, NHCX1X2CO2R5, N(OH)CONR5R6, N(OH)COR4, NHCONR5R6, C(NOH)NHOH and CONHNR5R6; R3 is selected from the group consisting of hydrogen, a pharmaceutically acceptable salt, COR4, COCX1X2NR6R7, CR8R9OR10, CH2CR8(OR10)CH2OR11 and SiR12R13R14; R4 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced heteroaryl, reduced heteroarylalkyl, OR5, NHCX1X2CO2R5 and NR6R7; R5 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl, and reduced heteroarylalkyl; R6 and R7 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl;, reduced heteroarylalkyl and (CH2)nOR5 where n is 2-4 and R5 is as defined above; R8, R9, R10 and R11 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl and (CH2)nOR5 or at least two of R8, R9, R10 and R11 together form a ring system containing 5-10 atoms wherein said ring system is carbocyclic, heterocyclic or reduced heterocyclic and R5 and n are as defined above; R12, R13 and R14 are independently selected from the group consisting of alkyl and aryl; and X1 and X2 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, and arylalkyl; and the acid addition salts thereof.

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