摘要:
The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)- T wherein - STxB is the Shiga Toxin B subunit or a functional equivalent thereof, - Z(n) wehrein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoidof sulfydryl group, or is a polypeptide, - Cys is the amino-acid residue for Cysteine, - T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: . agents for in vivo diagnosis, . cytotoxic agents, . prodrugs, or . enzymes for the conversion of a prodrug to a drug, - Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.
摘要:
The present invention concerns novel dibenzo[c,h] [1, 5]naphthyridine of formula (I) and their use as DNA probes, as well as the methods for marking DNA using the same .
摘要:
The present invention relates to novel compounds selected from 2-aminoaryloxazoles of formula I that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors.
摘要:
The present invention relates to specific compounds; pharmaceutical composition comprising at least one of said compounds; and the use of at least one of said compounds in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.
摘要:
The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.
摘要:
The present invention is concerned among others with compounds of formula (1), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein Q is halo, C1-6 alkyl or C2-6 alkenyl; X is (a-2) with q and r being O and Z being O, S or SO; R1 is aryl; R2 is selected from formyl; C1-6alkyloxycarbonylalkyl; Het?2; Het2C¿1-6alkyl, C1-6alkylthio; C1-6alkyl optionally substituted with one or two substituents each independently selected from hydroxy, and halo; R3 is selected from formyl; C1-6alkyl optionally substituted with one or two C1-6alkyloxy; R4 is hydrogen, with HIV inhibiting properties.
摘要:
The present invention relates to Penta- hexa-, hepta-, octa-, nona- and, deca-heteroaryl derivatives, comprising a combination of heterocycle 1 (Het-1) a and/or heterocycie 2 (Het-2) b and/ or heterocycle 3 (Het-3) c and/or heterocycle 4 (Het-4) d of formulae I, II, III and IV respectively, the N-oxides, the pharmaceutically acceptable addition salts. The compounds claimed are suitable for the treatment of cancer.