C07D207/323

Viral replication inhibitors

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds. ##STR00001##

Viral replication inhibitors

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds. ##STR00001##

Two-step synthesis of pyrrole compounds from furan compounds

Pyrrole compounds are produced by contacting a furan compound, a solid acid catalyst, and water to form a reaction mixture containing a γ-dicarbonyl compound, and then contacting the γ-dicarbonyl compound with ammonia or an ammonium salt to form a reaction product mixture containing the pyrrole compound. A representative pyrrole compound that can be synthesized using these processes is 2,5-dimethylpyrrole.

Two-step synthesis of pyrrole compounds from furan compounds

Pyrrole compounds are produced by contacting a furan compound, a solid acid catalyst, and water to form a reaction mixture containing a γ-dicarbonyl compound, and then contacting the γ-dicarbonyl compound with ammonia or an ammonium salt to form a reaction product mixture containing the pyrrole compound. A representative pyrrole compound that can be synthesized using these processes is 2,5-dimethylpyrrole.

SMALL MOLECULE AGONISTS OF MUCOLIPIN 1 AND USES THEREOF

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a phenyl-sulfonic amide (or similar) structure which function as agonists of mucolipin 1 (ML1), and their use as therapeutics for the treatment of Duchenne muscular dystrophy (DMD) and related disorders.

SMALL MOLECULE AGONISTS OF MUCOLIPIN 1 AND USES THEREOF

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a phenyl-sulfonic amide (or similar) structure which function as agonists of mucolipin 1 (ML1), and their use as therapeutics for the treatment of Duchenne muscular dystrophy (DMD) and related disorders.

BENZENESULFONAMIDE DERIVATIVES AS TRAP1 MODULATORS AND USES THEREOF
20230174523 · 2023-06-08 · ·

The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as α-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof).

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BENZENESULFONAMIDE DERIVATIVES AS TRAP1 MODULATORS AND USES THEREOF
20230174523 · 2023-06-08 · ·

The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as α-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof).

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Method for labeling of aldehyde containing target molecules

The present description relates to a method for binding to a target molecule having an aldehyde compound derived from N-(2-aminoethyl)pyrrole, which compound also has a moiety of interest, to compounds (conjugates) obtained by this method, having both the target molecule and the moiety of interest and to novel substances derived from N-(2-aminoethyl)pyrrole. In one embodiment, the compound has the formula of Formula II ##STR00001##
wherein R1, R2 and R3 independently are H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein R4, R5, R6, R7 and R8 independently are H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or -LM, wherein L is absent or is a linker and M is a moiety of interest selected from a nucleotide, an oligonucleotide, a peptide, a label, a cytotoxic agent, a partner of a binding pair and a functional group, wherein two of R4, R5, R6, R7, and R8 optionally are linked to form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted heterocycloalkyl, and T is a target molecule selected from the group consisting of a solid phase, a polypeptide, a protein, a carbohydrate, a nucleotide and a nucleic acid, with the proviso that at least one of R4, R5, R6, R7 or R8 is -LM.

CYCLOPROPANECARBOXYLIC ACID GPR120 MODULATORS

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein coupled receptor modulators which may be used as medicaments

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