C07C2601/02

Antibacterial agents: arylalkylcarboxamido phloroglucinols

The invention provides compounds of formula (I) or (II) and tautomers and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula (I) or (II) or a tautomer or salt thereof, methods of making a compound of formula (I) or (II) or a tautomer or salt thereof, and methods of using a compound of formula (I) or (II) or a tautomer or salt thereof as, e.g., inhibitors of bacterial RNA polymerase or as antibacterial agents. ##STR00001##

FLOW CHEMISTRY SYNTHESIS OF ISOCYANATES
20230095750 · 2023-03-30 ·

The disclosure provides, inter alia, safe and environmentally-friendly methods, such as flow chemistry, to synthesize isocyanates, such as methylene diphenyl diisocyanate, toluene diisocyanate, hexamethylene diisocyanate, isophorone diisocyanate, and tetramethylxylene diisocyanate.

NOVEL SUBTITUTED SULFONYLUREA AND SULFOXIMINEUREA DERIVATIVES
20230096220 · 2023-03-30 ·

The present invention relates to novel compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as the compounds of the invention belong to the family of NOD-like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators as well as to the use of the novel inhibitor compounds in the treatment of diseases or conditions in which interleukin 1β activity is implicated.

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Compositions and methods for differential release of 1-methylcyclopropene

A clathrate of 1-methylcyclopropene with α-cyclodextrin, obtained as a solid particulate product, is modified by comminuting, classifying, or both to obtain a modified particulate. When subjected to identical atmospheric disgorgement conditions of humidity and temperature, identical masses of the modified and unmodified particulates exhibit different rates of 1-methylcyclopropene disgorgement. Specifically, we have found that a smaller mean particle size is inversely related to a greater rate of 1-methylcyclopropene release.

Insect repellent compounds and compositions, and methods thereof

The present invention relates to monoterpenoid and phenylpropanoid containing derivative compounds, methods of making the compounds, compositions comprising the compounds, and methods of repelling pests using the compounds and/or compositions.

Improved process for preparing cyclopropyl compounds from alkenes
20220348526 · 2022-11-03 · ·

The invention relates to an improved process for preparing cyclopropyl compounds from alkenes through reaction of the alkene in the presence of bromochloromethane, elemental zinc, and elemental copper or copper compounds (cyclopropanation reaction).

PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
20220347176 · 2022-11-03 ·

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).

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CANNABINOID DERIVATIVES

This disclosure relates to cannabinoid derivatives of Formula (I), wherein R4 or R7 is a carboxamide group, pharmaceutical compositions comprising these compounds and methods of using the cannabinoid derivatives. These compounds are potential cannabinoid receptor inhibitors, including CB1 and CB2 receptors.

CALPAIN-2 INHIBITOR COMPOUNDS AND METHODS OF TREATMENT
20230091121 · 2023-03-23 ·

Compounds of Formula (I) or (X) are provided including for treatment of disorders such as a disorder or symptom associated with neuronal cell death. In one aspect, compounds which are selective inhibitors of calpain-2 are provided. Preferred compounds can be useful to treat acute neurodegeneration.

MESCALINE DERIVATIVES WITH MODIFIED ACTION

A composition for use in substance-assisted therapy, wherein: R is hydrogen, methyl, or ethyl, and R′ is C.sub.1-C.sub.5 branched or unbranched alkyl with the alkyl optionally substituted with F.sub.1-F.sub.5 fluorine substituents up to a fully fluorinated alkyl, C.sub.3-C.sub.6 cycloalkyl optionally and independently substituted with one or more substituents such as F.sub.1-F.sub.5 fluorine and/or C.sub.1-C.sub.2 alkyl, (C.sub.3-C.sub.6 cycloalkyl)-C.sub.1-C.sub.2 branched or unbranched alkyl optionally substituted with one or more substituents such as F.sub.1-F.sub.5 fluorine and/or C.sub.1-C.sub.2 alkyl, or C.sub.2-C.sub.5 branched or unbranched alkenyl with E or Z vinylic, cis or trans allylic, E or Z allylic or other double bond position in relation to the attached ether function, where any of the carbons of the branched or unbranched alkenyl substituent is optionally substituted independently with one or more C.sub.1-C.sub.2 alkyl, with F.sub.1-F.sub.5 fluorine or with D.sub.1-D.sub.5 deuteron substituents.