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    PHARMACEUTICAL COMPOSITIONS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-IV (DPP-IV)
    3.
    发明专利
    PHARMACEUTICAL COMPOSITIONS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-IV (DPP-IV) 未知

    公开(公告)号：NZ591609A

    公开(公告)日：2012-10-26

    申请号：NZ59160906

    申请日：2006-08-25

    Applicant: ABBOTT LAB

    Inventor： PEI ZHONGHAU ,  VON GELDERN THOMAS ,  MADAR DAVID J ,  LI XIAOFENG ,  BASHA FATIMA ,  YONG HONG ,  LONGENECKER KENTON L ,  BACKES

    IPC: C07D317/64 ,  A61K31/135 ,  A61K31/137 ,  C07C211/40 ,  C07C211/54 ,  C07C211/62 ,  C07D213/38 ,  C07D213/68 ,  C07D487/04

    Abstract: Disclosed are trans-6-(phenyl)cyclohex-3-en-1-amine / trans-2-(phenyl)cyclohex-4-enyl-amine derivatives as represented by the general formula (I), wherein the substituents are as disclosed herein. Representative compounds include trans-6-(2-chlorophenyl)cyclohex-3-en-1-amine, trans-6-(2,4-dichlorophenyl)cyclohex-3-enyl-amine, 4-{ [trans-5-amino-4-(2,4-dichlorophenyl)-2-pyridin-3-ylcyclohex-1 -en-1-yl]methoxy} benzonitrile, trans-methyl 3-{ { 5-amino-4-(2,4-dichlorophenyl)-2-pyridin-3-ylcyclohex-1-en-1-yl]methoxy} benzoate, trans-3-(phenoxymethyl)-6-(2,4,5-trifluorophenyl)cyclohex-3-en-1-amine, trans-3-{ [4-(methylsulfonyI)phenoxy] methyl} -6-(2,4,5-trifluorophenyl)cyclohex-3-en-1-amine, N-(3-{ [trans-5-amino-4-(2,4,5-trifluorophenyl)cyclohex-1-en-1-yl)methoxy } phenyl)acetamide, 3-{ [trans-5-amino-4-(2,4,5-trifluorophenyl)cyclohex-1-en-1-yl]methoxy} -4-fluorobenzoic acid, trans-3-{ [3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]methyl} -6-(2,4,5-trifluorophenyl)cyclohex-3-en-1-amine and trans-3-[(4-acetylpiperazin-1-yI)methyl]-6-(2,4,5-trifluorophenyl)cyclohex -3-en-1-amine. Further disclosed is a pharmaceutical composition which comprises a therapeutically effective amount of a compound as defined above, in combination with a pharmaceutically suitable carrier for the treatment of diseases selected from the group consisting of cardiovascular disease, atherosclerosis, cerebrovascular diseases, diseases and disorders of the central nervous system, schizophrenia, anxiety, bipolar disease, depression, insomnia, cognitive disorders, gastrointestinal diseases and disorders, cancer, inflammation and inflammatory diseases, respiratory diseases and disorders, musculo-skeletal disorders, osteoporosis, menopausal symptoms, periodontal diseases, gingivitis, and various immunomodulatory diseases.

    ATRIAL PEPTIDE DERIVATIVES
    4.
    发明专利
    ATRIAL PEPTIDE DERIVATIVES 未知

    公开(公告)号：CA2033198A1

    公开(公告)日：1990-11-25

    申请号：CA2033198

    申请日：1990-05-23

    Applicant: ABBOTT LAB

    Inventor： LUCAS SCOTT D ,  ROCKWAY TODD W ,  DAVIDSEN STEVEN K ,  THOMAS MITCHELL A ,  VON GELDERN THOMAS

    IPC: A61K38/00 ,  A61K38/22 ,  A61P7/10 ,  A61P9/12 ,  C07K7/08 ,  C07K14/575 ,  C07K14/58 ,  A61K38/10

    Abstract: Novel atrial peptides of the formula are disclosed which have useful hypotensive, natriuretic and diuretic activity and in which R1 is selected from hydrogen, AcetylArg, Aha, Arg, Cit, His, Lys, Orn and Ser-Ser; R2 is a sulfur-containing group; R3 is a hydrophobic amino acid or dipeptide; R4 is a dipeptide spacer, or a tripeptide containing a dipeptide spacer plus a basic amino acid residue; R5 is a hydrophobic amino acid; R6 is a peptide of up to three amino acids; R7 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 R8 is a sulfur-containing group, as well as pharmaceutically acceptable salts, esters and amides thereof.

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