C07C235/64

Carboxamides as modulators of sodium channels

Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

Carboxamides as modulators of sodium channels

Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

COMPOUND WITH BROAD-SPECTRUM ANTIBACTERIAL ACTIVITY AND ITS ANTIBACTERIAL COMPOSITION

A compound with broad-spectrum antibacterial activity and its antibacterial composition are provided. The compound with broad-spectrum antibacterial activity has formula (I), which are antibacterial drug source compounds with a broad antibacterial spectrum, good antibacterial activity, suitable in vivo pharmacokinetics, and significant in vivo therapeutic effects. Preferred compound BAB159 has good antibacterial activity against Staphylococcus, Clostridium perfringens, Enterococcus, Bacillus, Streptococcus, Haemophilus, Candida krusei, Aspergillus niger, and Trichophyton, which is comparable or better than the listed drugs. The combination of preferred compound BAB159 and polymyxin E exhibits significantly enhanced synergistic antibacterial activity, especially against multidrug-resistant strains.

COMPOUND WITH BROAD-SPECTRUM ANTIBACTERIAL ACTIVITY AND ITS ANTIBACTERIAL COMPOSITION

A compound with broad-spectrum antibacterial activity and its antibacterial composition are provided. The compound with broad-spectrum antibacterial activity has formula (I), which are antibacterial drug source compounds with a broad antibacterial spectrum, good antibacterial activity, suitable in vivo pharmacokinetics, and significant in vivo therapeutic effects. Preferred compound BAB159 has good antibacterial activity against Staphylococcus, Clostridium perfringens, Enterococcus, Bacillus, Streptococcus, Haemophilus, Candida krusei, Aspergillus niger, and Trichophyton, which is comparable or better than the listed drugs. The combination of preferred compound BAB159 and polymyxin E exhibits significantly enhanced synergistic antibacterial activity, especially against multidrug-resistant strains.

COMPOUNDS AND COMPOSITIONS FOR USE AS MODULATORS OF TAU AGGREGATION AND ALLEVIATION OF TAUOPATHIES
20170008838 · 2017-01-12 ·

This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.

COMPOUNDS AND COMPOSITIONS FOR USE AS MODULATORS OF TAU AGGREGATION AND ALLEVIATION OF TAUOPATHIES
20170008838 · 2017-01-12 ·

This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.

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.

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.

Stable heavy isotopes in amide functional groups and uses thereof

There are provided isotope-enriched compounds containing stable heavy isotope-enriched amide functional groups for modulating the pharmacokinetic profile, metabolic profile, and/or delivery efficiency of a drug or prodrug, as well as its therapeutic or prophylactic efficacy and/or adverse effects. Use of the isotope-enriched amide-containing drugs and prodrugs for the treatment or prevention of disease states and conditions is also provided. ##STR00001##

N,N'-DIPHENYL-4,4'-BIPHENYLDICARBOXAMIDE ANALOGS AND THEIR USE IN CANCER TREATMENT
20250289780 · 2025-09-18 ·

In one aspect, the disclosure relates to a for -helix mimetics that can replicate the -helices found at protein protein interaction (PPI) interfaces and can selectively discriminate cognate proteins in PPIs. In one aspect, the scaffolds have Formula I

##STR00001## wherein each of X.sub.1-X.sub.8 is individually selected from H, OR.sub.1, NR.sub.1R.sub.2, SR.sub.1, or PR.sub.1R.sub.2; wherein each of Y.sub.1-Y.sub.2 is individually selected from H, CO.sub.2R.sub.1, C(O)NR.sub.1R.sub.2, C(O)R.sub.1, OR.sub.1, NR.sub.1R.sub.2, SR.sub.1, or PR.sub.1R.sub.2; and wherein each of R.sub.1 and R.sub.2 is individually selected from H, or optionally substituted linear or branched C1-C20 alkyl, C3-C20 aryl, linear or branched C2-C20 alkenyl, linear or branched C2-C20 alkynyl, or C3-C20 arylalkyl.

Also disclosed are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating cancer using the compounds.