摘要:
Novel derivatives of compound (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one and the use thereof for the preparation of medicaments for the treatment of tumors in which the tyrosine kinase activity proteins Met, PDGF-R, FGF-R1, FGF-R3, Kit and the oncoproteins of the Ret family are involved.
摘要:
The use of an arylidene 2-indolinone derivative for treating tumors involving Met, PDGF-R, FGF-RI, FGF-R3 and Kit tyrosine kinases, or the oncoproteins of Ret family is disclosed. The invention also provides pharmaceutical compositions comprising laid arylidene 2-indolinone derivative as well as a kit comprising, in separate containers, said derivative and an anti-cancer or anti-tumor agent.
摘要:
The use of an arylidene 2-indolinone derivative for treating tumors involving Met, PDGF-R, FGF-RI, FGF-R3 or Kit tyrosine kinases, or a Ret oncoprotein which includes a MEN2-associated mutation is disclosed.
摘要:
The invention relates to the use of diketodithiopiperazine antibiotics, in particular chaetocin and gliotoxin, for the preparation of pharmaceutical compositions for antitumor therapy.
摘要:
A compound of general formula (I): in which: R is selected from the group consisting of (C1-C25)alkyl, (C2-C25)alkenyl, aryl, (C7-C10)aralkyl; n and m are each independently an integer of two to eight; p is one or two; A is selected from the group consisting of —B—, —B—(CH2)r—B—, —B—(CH2)r—B—(CH2)z—B—, wherein r and z are an integer from 2 to 8, B is a —NR1— or —N(R2)2+1/pQ−p group, in which R1 is selected from hydrogen, (C1-C4)alkyl, (C1-C4)acyl, tert-butoxycarbonyl, and R2 is selected from hydrogen and (C1-C4)alkyl; Q−p is an anion selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R3COO− wherein R3 has the same meanings as R, independently from one another and R4—O—SO3− wherein R4 is (C2-C14)alkyl with the proviso that, when Q−p is selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R is not (C1-C4)alkyl.
摘要:
A compound of general formula (I): in which: R is selected from the group consisting of (C1-C25)alkyl, (C2-C25)alkenyl, aryl, (C7-C10)aralkyl; n and m are each independently an integer of two to eight; p is one or two; A is selected from the group consisting of —B—, —B—(CH2)r—B—, —B—(CH2)r—B—(CH2)z—B—, wherein r and z are an integer from 2 to 8, B is a —NR1— or —N(R2)2+ 1/pQ−p group, in which R1 is selected from hydrogen, (C1-C4)alkyl, (C1-C4)acyl, tert-butoxycarbonyl, and R2 is selected from hydrogen and (C1-C4)alkyl; Q−p is an anion selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R3COO− wherein R3 has the same meanings as R, independently from one another and R4—O—SO3− wherein R4 is (C2-C14)alkyl with the proviso that, when Q−p is selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R is not (C1-C4)alkyl.
摘要:
The compounds of formula (I) wherein A and R1-R5 are as defined in the description, are inhibitors of Vascular Endothelial Growth Factor and are useful as angiogenesis inhibitors and antiproliferative agents.
摘要:
The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity.
摘要:
The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.
摘要:
Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2, that can be the same or different, are hydrogen, alkyl, aryl, aralkyl groups or, if taken together, cycloalkyl groups;A is a carbon atom, a residue of 2,3-dioxybutandioic-2,4-dioxyphtalic acid or disubstituted malonic acid derivatives;n.sub.1 and n.sub.2 are selected in such a manner that the result of their addition is from 2 to 40;T.sub.1 and T.sub.2 that can be the same or different, are hydrogen, alkyl, benzyl, phenyl, acyl or cycloalkyl or a residue of formulae ##STR2## Compounds I are useful as anti-tumor agents in human therapy.