摘要:
The present invention concerns a new assay which allows the identification of compounds which inhibit the formation of complexes between a product of the double minute 2 gene ('dm2') and p53 but not between p53 and DNA. Both the complex formation of labeled DNA, C-terminally truncated p53 and dm2 and disruption of dm2 from the labeled DNA-p53 complex by an inhibitor of an p53-dm2 interaction can be detected by a gel shift assay procedure. This assay permits the selection of compounds which, besides their inhibitory property, do not alter p53 specific DNA binding and do not disturb p53 conformation required for DNA binding or formation of active tetramer.
摘要:
The use of 5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide or a tautomer thereof or a pharmaceutically acceptable salt or a hydrate or a solvate for the treatment of cancer of the bladder, the colon, the liver, the lung,the breast, the ovaries, the pancreas, the kidney, the stomach, the gastrointestinal tract, the prostate, the head and neck, the brain, and/or the blood
摘要:
The present invention relates to novel radicicol derivatives of the formula (I), in which R is R', (CH3)nCOOR' or (CH2)nCONHR, wherein R' is 11CH3, [3H]3C, [3H]2HC, [3H]H2C or (CH2)nHal, wherein Hal is 123I, 125I, 131I, I, 75Br, 76Br, 77Br, 82Br, Br, 18F or F, or R' is (CH2)n-1[3H]HCHal or (CH2)n-1[3H]2CHaI, wherein Hal is I, Br or F, and n is, each independently, 1 , 2, 3 or 4, in free form or in salt form, to their preparation, to their use as radiotracers/markers and to compositions containing them.
摘要:
The invention relates to the use of 9H-purine-2,6-diamine compounds and salts thereof in the treatment of proliferative diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, pharmaceutical preparations comprising 9Hpurine-2,6-diamine compounds, novel 9H-purine-2,6-diamine compounds, and a process for the preparation of the novel 9H-purine-2,6-diamine compounds.
摘要:
The invention relates to the use of benzoimidazolone compounds and salts thereof in the treatment of proliferative diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, pharmaceutical preparations comprising benzoimidazolone compounds, novel benzoimidazolone compounds, and a process for the preparation of the novel benzoimidazolone compounds.
摘要:
The invention relates to the use of 1H-indazol-6-ol compounds and salts thereof in the treatment of proliferative diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, pharmaceutical preparations comprising 1H-indazol-6-ol compounds, novel 1H-indazol-6-ol compounds, and a process for the preparation of the novel 1H-indazol-6-ol compounds.
摘要:
The present invention relates to compounds capable of binding to the oncogene protein MDM2, processes for the preparation of such compounds, pharmaceutical preparations comprising such compounds, and uses of said compounds, e.g. in the therapeutic (including prophylactic) treatment of an animal or especially of the human body. The present further relates to methods of and compounds for inhibiting the growth of tumor cells which comprise the wild type p53 suppressor by interfering with the interaction between human p53 and human MDM2.