Patent classifications
C07D277/62
Histone deacetylase inhibitors and compositions and methods of use thereof
Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. ##STR00001##
Histone deacetylase inhibitors and compositions and methods of use thereof
Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. ##STR00001##
THERAPEUTIC COMPOUNDS
The invention provides compounds of formula I:
##STR00001##
or a salt thereof as described herein. The invention also provided pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.
Highly selective sigma receptor radioligands
Compounds having the general formula III, or IV ##STR00001##
wherein R.sub.1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R.sub.2,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y is S; Z can be either H, O, S, SR or NR where R groups can be either H, aryls, alkyls, or cycloalkyls; n can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R.sub.1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C.sub.3-C.sub.5 cycloalkyl group, aromatic, and heterocyclic group; and wherein X is C.sub.1-C.sub.4 radiohaloalkyl.
INHIBITORS OF SARS-COV-2
Described herein are compounds and methods for the treatment of coronavirus infection. The compounds can function as an inhibitor of the main protease (Mpro) of coronaviruses. The compounds can include diphenylmethyl piperazine derivatives, diphenylmethyl piperidine derivatives, diphenylmethylidene piperidine derivatives, tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen derivatives, tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaen derivatives, 6,11-dihydrobenzo[c][1]benzoxepin derivatives, 6,11-dihydrobenzo[c][1]benzothiepin derivatives, 5,5-dioxo-6,11-dihydrobenzo[c][1]benzothiepin derivatives, and 6-oxo-5,11-dihydrobenzo[c][1]benzazepin derivatives, as well as pharmaceutically acceptable salts, hydrates, and prodrugs thereof.
ANTIBACTERIAL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF TREATING BACTERIAL INFECTIONS
Compounds disclosed herein may exhibit antibacterial and anti-inflammatory properties. Pharmaceutical compositions containing the compound(s) may be used to treat bacterial infections, such as urinary tract infections, and/or disorders associated with chronic inflammation.
ANTIBACTERIAL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF TREATING BACTERIAL INFECTIONS
Compounds disclosed herein may exhibit antibacterial and anti-inflammatory properties. Pharmaceutical compositions containing the compound(s) may be used to treat bacterial infections, such as urinary tract infections, and/or disorders associated with chronic inflammation.
Halogenated compounds for photodynamic therapy
Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
Halogenated compounds for photodynamic therapy
Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
Fused heterocyclic compound and pest control applications thereof
A fused heterocyclic compound represented by formula (1) or an N-oxide thereof has an excellent control effect on pests: ##STR00001##
wherein A.sup.1 represents N or the like, A.sup.2 represents NR.sup.6 or the like, A.sup.3 represents CR.sup.12 or the like, R.sup.1 represents a C1 to C6 chain hydrocarbon group or the like, R.sup.2, R.sup.4 and R.sup.5 are the same or different and represent a C1 to C3 alkyl group optionally having one or more halogen atoms or the like, R.sup.3 represents a C1 to C6 chain hydrocarbon group or the like, R.sup.6 represents a C1 to C6 chain hydrocarbon group or the like, any one set of R.sup.9 and R.sup.10, R.sup.10 and R.sup.11, and R.sup.11 and R.sup.12 in R.sup.9, R.sup.10, R.sup.11 and R.sup.12, together with the carbon atoms to which they are bound, forms a ring, and n represents 0, 1 or 2.