C07D239/54

Pyrimidine cyclohexenyl glucocorticoid receptor modulators

The present invention provides a class of pyrimidinedione cyclohexenyl compounds and methods of using these compounds as glucocorticoid receptor modulators.

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
20220409536 · 2022-12-29 ·

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
20220409536 · 2022-12-29 ·

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

PYRIMIDINEDIONE DERIVATIVES

The present invention covers pyrimidinedione derivatives of general formula (I): (I), in which R.sup.1, R.sup.2, R.sup.4, R.sup.5 and X are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer, as a sole agent or in combination with other active ingredients.

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PYRIMIDINEDIONE DERIVATIVES

The present invention covers pyrimidinedione derivatives of general formula (I): (I), in which R.sup.1, R.sup.2, R.sup.4, R.sup.5 and X are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer, as a sole agent or in combination with other active ingredients.

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3-((R)-2-(AMINO-2-PHENYLETHYL)-1-(2-FLUORO-6 TRIFLUOROMETHYL BENZYL)-5-IODO-6-METHYL-1H-PYRIMIDINE-2,4-DIONE OR A SALT THEREOF, PROCESS FOR ITS PREPARATION, AND ITS USE IN THE SYNTHESIS OF ELAGOLIX

A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

CRBN ligands and uses thereof

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.

TARGETED PROTEIN DEGRADATION

This invention provides pharmaceutical protein degraders and E3 ubiquitin ligase binders for therapeutic applications as described further herein.

Substituted thiophenyl uracils, salts thereof and the use thereof as herbicidal agents

The invention relates to substituted thiophenyl uracils of general formula (I) or the salts (I) thereof, wherein the groups in general formula (I) are as defined in the description, and to the use thereof as herbicides, in particular for controlling weeds and/or weed grasses in crops of cultivated plants and/or as plant growth regulators for influencing the growth of crops of cultivated plants. ##STR00001##

COMPOUNDS AND THEIR USE FOR THE TREATMENT OF ALPHA1-ANTITRYPSIN DEFICIENCY

The invention relates to specified benzamide compounds of formula (1), and pharmaceutical compositions containing the compounds. The compounds may be inducers of α.sub.1-antitrypsin (A1AT), and may be used in the treatment of a disease or disorder such as α.sub.1-antitrypsin deficiency (A1AD or AATD).