C07D255/02

2-Pyrazole Anilines and Related Analogs for Inhibiting YAP/TAZ-TEAD

The present disclosure relates to novel compounds, to said compounds for use as a medicine, more in particular for the prevention or treatment of diseases mediated by activity of YAP/TAZ-TEAD transcription, yet more in particular for the prevention or treatment of cancer or fibrosis. The present disclosure also relates to a method for the prevention or treatment of said diseases comprising the use of the novel compounds.

PSMA-TARGETING COMPOUNDS AND USES THEREOF
20230348405 · 2023-11-02 ·

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

PSMA-TARGETING COMPOUNDS AND USES THEREOF
20230348405 · 2023-11-02 ·

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

USE OF TRIAZOLE COMPOUND AS GHRELIN RECEPTOR AGONIST
20230339869 · 2023-10-26 ·

The present invention relates to a use of a triazole compound as a ghrelin receptor agonist and, more specifically, to a composition for preventing or treating diseases mediated by the ghrelin receptor, the composition being of a triazole compound which strongly binds to the ghrelin receptor with very high specificity. The compound provided by the present invention exhibits a strong binding force to the ghrelin receptor with very high specificity, and thus may be very usefully employed for preventing or developing a therapeutic agent for diseases mediated by the ghrelin receptor.

USE OF TRIAZOLE COMPOUND AS GHRELIN RECEPTOR AGONIST
20230339869 · 2023-10-26 ·

The present invention relates to a use of a triazole compound as a ghrelin receptor agonist and, more specifically, to a composition for preventing or treating diseases mediated by the ghrelin receptor, the composition being of a triazole compound which strongly binds to the ghrelin receptor with very high specificity. The compound provided by the present invention exhibits a strong binding force to the ghrelin receptor with very high specificity, and thus may be very usefully employed for preventing or developing a therapeutic agent for diseases mediated by the ghrelin receptor.

PSMA-TARGETING COMPOUNDS AND USES THEREOF
20220259161 · 2022-08-18 ·

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

PSMA-TARGETING COMPOUNDS AND USES THEREOF
20220259161 · 2022-08-18 ·

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

Methods for low temperature fluorine-18 radiolabeling of biomolecules

New chelators such as H.sub.3L1, H.sub.3L2, H.sub.3L3, H.sub.3L26 and derivatives were synthesized for the complexation of {Al.sup.18F}.sup.2+. These new chelators are able to complex {AI.sup.18F}.sup.2+ with good radiochemical yields using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and AI.sup.18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and Al.sup.18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and derivatives have been synthesized. We have explored the complexation of {AI.sup.18F}.sup.2+ with new chelators and obtained very favourable radiochemical yields (>85%) using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum at 37° C., where AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and Al.sup.18F-L26 showed high stability, since only very limited bone uptake—which would be an indication of release of fluorine-18 in the form of fluoride—was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestines due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and H.sub.3L26 demonstrated to be good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and several derivatives have been synthesized.

Methods for low temperature fluorine-18 radiolabeling of biomolecules

New chelators such as H.sub.3L1, H.sub.3L2, H.sub.3L3, H.sub.3L26 and derivatives were synthesized for the complexation of {Al.sup.18F}.sup.2+. These new chelators are able to complex {AI.sup.18F}.sup.2+ with good radiochemical yields using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and AI.sup.18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and Al.sup.18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and derivatives have been synthesized. We have explored the complexation of {AI.sup.18F}.sup.2+ with new chelators and obtained very favourable radiochemical yields (>85%) using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum at 37° C., where AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and Al.sup.18F-L26 showed high stability, since only very limited bone uptake—which would be an indication of release of fluorine-18 in the form of fluoride—was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestines due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and H.sub.3L26 demonstrated to be good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and several derivatives have been synthesized.

COMPOUNDS FOR USE AS IRON(III) MRI CONTRAST AGENTS
20220259244 · 2022-08-18 ·

Provided are macrocyclic compounds and compounds with two or more macrocyclic groups, iron coordinated macrocyclic compounds, and iron coordinated compounds with two or more macrocyclic groups. The iron is high-spin iron(III). The iron coordinated compounds may exhibit a negative redox potential (e.g., relative to a normal hydrogen electrode at a biologically relevant pH, for example, a pH of 6.5-7.5). The compounds can be used as MRI contrast agents.