C07D249/08

Heteroaromatic inhibitors of astacin proteinases

The present invention relates to novel hydroxamic acid derivatives useful as inhibitors of astacin metalloproteinases, in particular procollagen C-proteinase (PCP) enzymes, meprins, ovastacin and/or nematode astacins; more particularly human or mammalian meprin α, meprin β, BMP-1, ovastacin and/or DPY-31 from nematodes; pharmaceutical compositions comprising such compounds; methods for treatment or prophylaxis of diseases or conditions, especially such that are related to said metalloproteinases; and compounds and pharmaceutical compositions for use in such methods.

LIPOXYGENASE INHIBITORS
20230117592 · 2023-04-20 · ·

Various embodiments of the present disclosure are directed to compounds having Formula I, Formula II, Formula IIA, Formula III, Formula IIIA, Formula IIIB, and/or pharmaceutically acceptable salts thereof. The compounds can be suitable for inhibiting lipoxygenases and/or treating associated diseases. In some embodiments, subject compounds are used to prepare a composition that is effective in treating neurodegenerative diseases.

LIPOXYGENASE INHIBITORS
20230117592 · 2023-04-20 · ·

Various embodiments of the present disclosure are directed to compounds having Formula I, Formula II, Formula IIA, Formula III, Formula IIIA, Formula IIIB, and/or pharmaceutically acceptable salts thereof. The compounds can be suitable for inhibiting lipoxygenases and/or treating associated diseases. In some embodiments, subject compounds are used to prepare a composition that is effective in treating neurodegenerative diseases.

METHOD FOR PRODUCING AZOLE DERIVATIVE, BROMOHYDRIN DERIVATIVE AND METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING 1-CHLORO-3-(4-CHLOROPHENOXY)BENZENE

A novel method of producing an azole derivative represented by General Formula (I) includes: reacting an organometallic reagent formed from 1-bromo-2-chloro-4-(4-chlorophenoxy)benzene by transmetalation reaction with a bromopyruvic acid derivative to obtain a bromohydrin derivative; and reacting the bromohydrin derivative with imidazole, 1,2,4-triazole, or an alkali metal salt thereof to obtain the azole derivative.

METHOD FOR PRODUCING AZOLE DERIVATIVE, BROMOHYDRIN DERIVATIVE AND METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING 1-CHLORO-3-(4-CHLOROPHENOXY)BENZENE

A novel method of producing an azole derivative represented by General Formula (I) includes: reacting an organometallic reagent formed from 1-bromo-2-chloro-4-(4-chlorophenoxy)benzene by transmetalation reaction with a bromopyruvic acid derivative to obtain a bromohydrin derivative; and reacting the bromohydrin derivative with imidazole, 1,2,4-triazole, or an alkali metal salt thereof to obtain the azole derivative.

AROMATIC SULFONAMIDE DERIVATIVES

Substituted aromatic sulfonamides of formula (I)

##STR00001##

pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.

AROMATIC SULFONAMIDE DERIVATIVES

Substituted aromatic sulfonamides of formula (I)

##STR00001##

pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.

CANNABINOID DERIVATIVES
20220324806 · 2022-10-13 ·

The current application relates to cannabinoid derivatives of formula (I) and pharmaceutical compositions comprising the same. The cannabinoid derivative can be used for the treatment of diseases associated with cannabinoid receptor such as pain, ADHD/ADD, alcohol use disorder, anxiety disorder, and dementias.

CANNABINOID DERIVATIVES
20220324806 · 2022-10-13 ·

The current application relates to cannabinoid derivatives of formula (I) and pharmaceutical compositions comprising the same. The cannabinoid derivative can be used for the treatment of diseases associated with cannabinoid receptor such as pain, ADHD/ADD, alcohol use disorder, anxiety disorder, and dementias.

Small molecule inhibitors of Ebola and Lassa fever viruses and methods of use

Disclosed herein are compounds having a structure of formula (I), compositions and methods useful for the treatment of a disease or infection, such as a viral infection (e.g., Ebola), cancer and obesity: ##STR00001##
wherein A is N or CR.sup.8; Z is ##STR00002## E is selected from optionally substituted alkyl, cycloalkyl, arylalkyl, cycloalkylalkyl, amino, alkoxy, cycloalkyloxy, and cycloalkylamino; R.sup.1 is selected from optionally substituted aryl and heteroaryl, R.sup.2 and R.sup.3 are independently selected from H, deutero, optionally substituted alkyl, haloalkyl, or R.sup.2 and R.sup.3, together with the carbon to which they are bound, combine to form a carbonyl; and R.sup.8 is selected from H, deutero, halo, hydroxyl, cyano, amino, alkyl, alkoxy, carboxy, alkoxycarbonyl, and aminocarbonyl,
provided that E is not ##STR00003##