SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR
申请人:Baumann Andrew Christian
公开号:US20060281788A1
公开(公告)日:2006-12-14
The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′:
Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention:
or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
Synthesis and Structure–Activity Relationship Studies of C2-Modified Analogs of the Antimycobacterial Natural Product Pyridomycin
作者:Maryline Kienle、Patrick Eisenring、Barbara Stoessel、Oliver P. Horlacher、Samuel Hasler、Gwénaëlle van Colen、Ruben C. Hartkoorn、Anthony Vocat、Stewart T. Cole、Karl-Heinz Altmann
DOI:10.1021/acs.jmedchem.9b01457
日期:2020.2.13
A series of derivatives of the antimycobacterial naturalproduct pyridomycin have been prepared with the C2 side chain attached to the macrocyclic core structure by a C-C single bond, in place of the synthetically more demanding enol ester double bond found in the naturalproduct. Hydrophobic C2 substituents of sufficient size generally provide for potent anti-Mtb activity of these dihydropyridomycins
[EN] HETEROCYCLIC AMIDE DERIVATIVES WHICH POSSESS GLYCOGEN PHOSPHORYLASE INHIBITORY ACTIVITY<br/>[FR] DERIVES AMIDES HETEROCYCLIQUES POSSEDANT UNE ACTIVITE INHIBITRICE DE GLYCOGENE PHOSPHORYLASE
申请人:ASTRAZENECA AB
公开号:WO2005018637A1
公开(公告)日:2005-03-03
A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; (1) wherein, for example: R4 and R5 together are either -S-C(R6=C(R7)- or -C(R7)=C(R6)-S- ; R6 and R7 are independently selected from hydrogen and halo; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is halo, cyano or carboxy; R2 is for example methyl; R3 is for example selected from halo(1-4C)alkyl, dihalo(1-4C)alkyl, trifluoromethyl, hydroxy(1-4C)alkyl, dihydroxy(2-4C)alkyl, trihydroxy(3-4C)alkyl, cyano(1-4C)alkyl (optionally substituted on alkyl with hydroxy), (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkoxy(1-4C)alkyl, di[(1-4C)alkoxy](1-4C)alkyl, (hydroxy)[(1-4C)alkoxy](1-4C)alkyl; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
Synthesis of (S)-(+)-methyl .BETA.,.GAMMA.-dihydroxy-.ALPHA.-methylenebutyrate and (S)-(-)-tulipalin B.
作者:Akira TANAKA、Kyohei YAMASHITA
DOI:10.1271/bbb1961.44.199
日期:——
The synthesis of (S)-(+)-methyl β, γ-dihydroxy-α-methylenebutyrate and (S)-(-)-tulipalin B, antibacterial substances isolated from Spiraea thunliergii Sieb. has been accomplished starting from isopropylidene-D-glyceraldehyde.