A61K31/7056

Aryl hydrocarbon receptor modulators
11547698 · 2023-01-10 · ·

The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, ##STR00001## R′ is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3, ##STR00002##
two R.sub.a is independently H, or two R.sub.a together form ═O or ═N—W.sub.3—R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.

Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection

The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections. ##STR00001## X is selected from the group consisting of O and H; R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl, and R.sup.2 is selected from (C.sub.1 to C.sub.10) alkyl, (C.sub.1 to C.sub.10) alkenyl, (C.sub.1 to C.sub.10) alkynyl, (C.sub.3 to C.sub.10) cycloalkyl, and (C.sub.5 to C.sub.10) cycloalkenyl, and NR.sup.3aR.sup.3b is defined in the specification. These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.

Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection

The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections. ##STR00001## X is selected from the group consisting of O and H; R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl, and R.sup.2 is selected from (C.sub.1 to C.sub.10) alkyl, (C.sub.1 to C.sub.10) alkenyl, (C.sub.1 to C.sub.10) alkynyl, (C.sub.3 to C.sub.10) cycloalkyl, and (C.sub.5 to C.sub.10) cycloalkenyl, and NR.sup.3aR.sup.3b is defined in the specification. These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.

Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection

The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections. ##STR00001## X is selected from the group consisting of O and H; R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl, and R.sup.2 is selected from (C.sub.1 to C.sub.10) alkyl, (C.sub.1 to C.sub.10) alkenyl, (C.sub.1 to C.sub.10) alkynyl, (C.sub.3 to C.sub.10) cycloalkyl, and (C.sub.5 to C.sub.10) cycloalkenyl, and NR.sup.3aR.sup.3b is defined in the specification. These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.

Benzalkonium-embedded mesostructured silica compositions and uses of same

The present invention relates in one aspect to the discovery of novel mesoporous silica nanoparticles (MSNs) templated around and comprising benzalkonium chloride (BAC). In certain embodiments, the BAC-SiO.sub.2 mesoporous nanoparticles are capable of sustained release of BAC under acidic conditions, thereby acting as a long release antimicrobial agent. In other embodiments, the BAC-SiO.sub.2 mesoporous nanoparticles can be incorporated into a variety of consumer products as an antimicrobial agent additive, including for example, but not limited to, surgical dressings, bandages, deodorants, soaps, facial cleansers and industrial cleaners.

Benzalkonium-embedded mesostructured silica compositions and uses of same

The present invention relates in one aspect to the discovery of novel mesoporous silica nanoparticles (MSNs) templated around and comprising benzalkonium chloride (BAC). In certain embodiments, the BAC-SiO.sub.2 mesoporous nanoparticles are capable of sustained release of BAC under acidic conditions, thereby acting as a long release antimicrobial agent. In other embodiments, the BAC-SiO.sub.2 mesoporous nanoparticles can be incorporated into a variety of consumer products as an antimicrobial agent additive, including for example, but not limited to, surgical dressings, bandages, deodorants, soaps, facial cleansers and industrial cleaners.

PHARMACEUTICAL COMBINATION HAVING POTENT ANTIVIRAL ACTIVITY AGAINST SINGLE-STRANDED RNA VIRUSES INCLUDING CORONAVIRUSES AND MONKEYPOX
20230210844 · 2023-07-06 · ·

A pharmaceutical composition for treating viral infections, including treatments for treatments for viral and non-viral infections, such as Monkeypox virus (MPV, MPXV, or hMPXV)) and SARS-CoV-2 infections, and illnesses due to the viral infections, such as COVID-19 is provided herein. Also provided are methods for treating viral and non viral infections as well as illnesses due to viral and non-viral infections, such as COVID-19 and Monkeypox virus (MPV, MPXV, or hMPXV)).

Substituted pyrazole compound, preparation method therefor, pharmaceutical composition and medical use thereof

The invention discloses a substituted pyrazole compound of formula (I), preparation method therefor, a pharmaceutical composition and a medical use thereof. The said compound features excellent stability, solubility, and low cytotoxicity, which is significantly beneficial for neurological protection, effectively preventing and treating nerve cell injuries. It is an ideal pharmaceutical compound for preventing or treating stroke, cerebral embolism, stroke sequelae, stroke-related motor dysfunction, mitochondrial encephalomyopathy, and amyotrophic lateral sclerosis. ##STR00001##

Novel Immunodulating Small Molecules
20230000887 · 2023-01-05 ·

The present invention includes novel compositions and methods for treating comprising a compound with the Formula I:

##STR00001##

wherein n=0, 1, 2, 3, 4, or 5; X=NH or O or S; Y=phenyl, or a phenyl group substituted with at least one methyl, a phenyl group substituted with at least one nitro, a phenyl group substituted with at least one nitrogen, a phenyl group substituted with at least one boron, aryl, substituted aryl, heteroaryl, four to six membered cycloalkyl, four to six membered heterocycloalkyl; R=H, C(O)R.sub.2, SO.sub.2R.sub.2; R.sub.1=H, C(O)R.sub.2, SO.sub.2R.sub.2; R.sub.2=Ethyl, methyl, isopropyl, n-propyl, t-butyl, n-butyl, NH.sub.2, NR.sub.3R.sub.4; R.sub.3, R.sub.4=Ethyl, methyl, isopropyl, n-propyl, t-butyl, n-butyl, three to six membered cycloalkyl, and Z=NH, or O, or none, and optionally wherein both X and Z are not both S, and wherein the amount of the compound is selected to either inhibit or activate the immune response.

Novel Immunodulating Small Molecules
20230000887 · 2023-01-05 ·

The present invention includes novel compositions and methods for treating comprising a compound with the Formula I:

##STR00001##

wherein n=0, 1, 2, 3, 4, or 5; X=NH or O or S; Y=phenyl, or a phenyl group substituted with at least one methyl, a phenyl group substituted with at least one nitro, a phenyl group substituted with at least one nitrogen, a phenyl group substituted with at least one boron, aryl, substituted aryl, heteroaryl, four to six membered cycloalkyl, four to six membered heterocycloalkyl; R=H, C(O)R.sub.2, SO.sub.2R.sub.2; R.sub.1=H, C(O)R.sub.2, SO.sub.2R.sub.2; R.sub.2=Ethyl, methyl, isopropyl, n-propyl, t-butyl, n-butyl, NH.sub.2, NR.sub.3R.sub.4; R.sub.3, R.sub.4=Ethyl, methyl, isopropyl, n-propyl, t-butyl, n-butyl, three to six membered cycloalkyl, and Z=NH, or O, or none, and optionally wherein both X and Z are not both S, and wherein the amount of the compound is selected to either inhibit or activate the immune response.