C07D233/32

Chemical crosslinkers and compositions thereof
09695189 · 2017-07-04 · ·

Cleavable crosslinkers of Formula (I) useful reagents in biochemical drug research and development such as antibody drug conjugates are disclosed. ##STR00001##

Antiviral compounds and uses thereof

This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

SUBSTITUTED PYRIDINES AS P2X3 AND P2X2/3 ANTAGONISTS

Methods of treating diseases associated with P2X.sub.3 and/or a P2X.sub.2/ with compounds

##STR00001##

formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined herein.

Process for manufacturing a cyclic urea adduct of an ethyleneamine compound

A process is provided for manufacturing a cyclic urea adduct of an ethyleneamine compound, the ethyleneamine compound having a linear NHCH.sub.2CH.sub.2NH group. The process includes, in an absorption step, contacting a liquid medium comprising an ethyleneamine compound having a linear NHCH.sub.2CH.sub.2NH group with a CO.sub.2-containing gas stream at a pressure of from about 1 to about 20 bara, resulting in the formation of a liquid medium into which CO.sub.2 has been absorbed. The process further includes bringing the liquid medium to cyclic urea formation conditions, and, in an urea formation step, forming cyclic urea adduct of the ethyleneamine compound, urea formation conditions including a temperature of at least about 120 C., wherein the total pressure at the end of the urea formation step is at most about 20 bara, and wherein the temperature in the absorption step is lower than the temperature in the urea formation step.

Process for manufacturing a cyclic urea adduct of an ethyleneamine compound

A process is provided for manufacturing a cyclic urea adduct of an ethyleneamine compound, the ethyleneamine compound having a linear NHCH.sub.2CH.sub.2NH group. The process includes, in an absorption step, contacting a liquid medium comprising an ethyleneamine compound having a linear NHCH.sub.2CH.sub.2NH group with a CO.sub.2-containing gas stream at a pressure of from about 1 to about 20 bara, resulting in the formation of a liquid medium into which CO.sub.2 has been absorbed. The process further includes bringing the liquid medium to cyclic urea formation conditions, and, in an urea formation step, forming cyclic urea adduct of the ethyleneamine compound, urea formation conditions including a temperature of at least about 120 C., wherein the total pressure at the end of the urea formation step is at most about 20 bara, and wherein the temperature in the absorption step is lower than the temperature in the urea formation step.

PHENOLIC COMPOUNDS SUBSTITUTED WITH NON-RADIOACTIVE ISOTOPES AND USES THEREOF

The present invention relates to phenolic compounds substituted with non-radioactive isotopes and the uses thereof, and more specifically to phenolic compounds in which some elements of biotin-phenol or desthiobiotin-phenol are substituted with non-radioactive isotopes and the uses thereof as probes for APEX family enzymes used in proximity molecular labeling. According to the present invention, proteins that are present in spaces that are not separated by membranes (e.g., mitochondrial cristae lumen), which previously could not be analyzed, can be identified, and the quantitative comparative analysis of protein expression in cells in different environments is possible, and it has the advantage of being able to quantitatively compare and analyze protein ratios in different adjacent spaces, and particularly, it has the advantage of being able to label proteins economically compared to the conventional technique of labeling proteins using heavy-carbon labeled amino acids.

Substituted 2-imidazolidinones and 2-imidazolones and their use in the treatment of cancer

Compounds of formula (I) wherein R.sub.1, R.sub.4, R.sub.8, X and Y as defined herein are provided as useful for the inhibition of certain types of cancer cells, amongst others, breast cancer cells, or for the manufacture of anti-cancer agents. ##STR00001##

Substituted 2-imidazolidinones and 2-imidazolones and their use in the treatment of cancer

Compounds of formula (I) wherein R.sub.1, R.sub.4, R.sub.8, X and Y as defined herein are provided as useful for the inhibition of certain types of cancer cells, amongst others, breast cancer cells, or for the manufacture of anti-cancer agents. ##STR00001##

Compound as PPAR agonist and application thereof
12545653 · 2026-02-10 · ·

The present invention provides compounds as PPAR agonists and their application, involving a new class of peroxisome proliferator-activated receptor (PPAR) gamma receptor agonist, which can inhibit the production of mitochondrial reactive oxygen species, and most of which can readily cross the blood-brain barrier. The present invention also includes pharmaceutical uses of the compounds.