1-aminoalkyl-2 2-disubstituted indolin-3-ones and a process for the production therefor
    43.
    发明授权
    1-aminoalkyl-2 2-disubstituted indolin-3-ones and a process for the production therefor 失效
    1-氨基-2-乙基-2-取代的吲哚啉-3-酮及其生产方法

    公开(公告)号:US3631063A

    公开(公告)日:1971-12-28

    申请号:US3631063D

    申请日:1969-05-28

    申请人: UPJOHN CO

    发明人: LEDNICER DANIEL

    IPC分类号: C07D209/36 C07D27/40

    CPC分类号: C07D209/36

    摘要: COMPOUNDS OF THE FORMULA:

    1-((R2-)2-N-(CH2)N-),2-R1,2-R2,3-(O=),X-INDOLINE

    WHEREIN X IS HYDROGEN, LOWER-ALKYL, HALOGEN OR -CF3; WHEREIN R1 AND R2 ARE LOWER-ALKYL OR -C6H4X'' IN WHICH X'' IS HYDROGEN, LOWER-ALKYL, HALOGEN, LOWER-ALKOXY OR -CF3; WHEREIN R3 IS LOWER-ALKYL OR TOGETHER -N(R3)2 IS 1-PYRROLIDINYL, 1-PIPERIDINYL OR 4-MORPHOLINYL; AND WHEREIN N IS AN INTEGER FROM 2 TO 4, INCLUSIVE, ARE MADE FROM 3H-INDOL-3-OLS. THE PRODUCTS AS WELL AS THEIR PHARMACOLGICALLY ACCEPTABLE ACID ADDITION SALTS HAVE SEDATIVE ACTIVITY AND CAN BE ADMINISTERED TO TRANQUILIZE MAMMALS.

    Small Molecule Inhibitors of G(alpha)i2 Protein and Uses Thereof

    公开(公告)号:US20220340526A1

    公开(公告)日:2022-10-27

    申请号:US17556820

    申请日:2021-12-20

    摘要: The disclosure relates to novel compounds and methods of use of the compounds to maintain the Gαi2 protein in its inactive GDP-bound state. The disclosure describes the knockdown or inhibition of Gαi2 negatively regulated migration of breast and ovarian cancer cell lines. The novel compounds inhibit the migratory behavior of PC3, DU145 and E006AA prostate cancer cell lines. Specifically, the novel compounds block the activation of Gαi2 in oxytocin-stimulated prostate cancer PC3 cells and inhibits the migratory capability of DU145 cells overexpressing constitutively active form of Gαi2, under basal and EGF-stimulated conditions.