C07D213/64

Labile esters of agrochemicals for controlled release and reduction of off-site movement
11465960 · 2022-10-11 · ·

The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.

Labile esters of agrochemicals for controlled release and reduction of off-site movement
11465960 · 2022-10-11 · ·

The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.

Complexation of Pirfenidone with Polyphenolic Calixarene or Resorcin[4]arenes

A cocrystal complex of pirfenidone with a polyphenolic macrocycle host is disclosed. The composition is useful, in some embodiments, as an acne treatment. In one embodiment, the macrocycle is calixarene or a calixarene derivative. In another embodiment, the macrocycle is resorcin[4]arene. In one embodiment, the macrocycle is C-methylresorcin[4]arene (RsC1). In another embodiment, the macrocycle is C-butylresorcin[4]arene (RsC4).

Complexation of Pirfenidone with Polyphenolic Calixarene or Resorcin[4]arenes

A cocrystal complex of pirfenidone with a polyphenolic macrocycle host is disclosed. The composition is useful, in some embodiments, as an acne treatment. In one embodiment, the macrocycle is calixarene or a calixarene derivative. In another embodiment, the macrocycle is resorcin[4]arene. In one embodiment, the macrocycle is C-methylresorcin[4]arene (RsC1). In another embodiment, the macrocycle is C-butylresorcin[4]arene (RsC4).

SUBSTITUTED PYRIDINE AND PYRAZINE COMPOUNDS AS PDE4 INHIBITORS

The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating treating peripheral disorders, including inflammatory and renal disorders.

SUBSTITUTED PYRIDINE AND PYRAZINE COMPOUNDS AS PDE4 INHIBITORS

The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating treating peripheral disorders, including inflammatory and renal disorders.

SIGMA-1 RECEPTOR LIGANDS AND THERAPEUTIC USES THEREOF

The present invention relates to the field of medicine. More specifically, the present invention relates to compounds that are sigma-1 receptor agonists and their use for the treatment of central nervous system disorders, including cognitive or neurodegenerative disorders, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, Amyotrophic lateral sclerosis, and multiple sclerosis.

BROMODOMAIN INHIBITORS
20220315601 · 2022-10-06 · ·

The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.

BROMODOMAIN INHIBITORS
20220315601 · 2022-10-06 · ·

The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.

CYCLIC PEPTIDE COMPOUND HAVING KRAS INHIBITORY ACTION

The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.