Patent classifications
C07D239/56
DACOS Type NNRTIS Amino Acid Ester Derivative, Preparation Method Thereof, Pharmaceutical Composition, and Application Thereof
Disclosed is a DACOs-type NNRTIs amino acid ester derivative, a preparation method thereof, a pharmaceutical composition, and an application thereof. The structure of the DACOs-type NNRTIs amino acid ester derivative is represented by formula (I). The DACOs-type NNRTIs amino acid ester derivative represented by formula (I) can be used as HIV-1 inhibitors and for the preparation of a drug for treating and/or preventing immunodeficiency viruses.
##STR00001##
PTGR2 inhibitors and their use
Disclosed are compounds of formula (I) as follows: ##STR00001## in which each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, L.sub.1, W, and Het is defined herein. Also provides are a method of inhibiting prostaglandin reductase 2 (PTGR2) using such a compound and a pharmaceutical composition containing same.
PTGR2 inhibitors and their use
Disclosed are compounds of formula (I) as follows: ##STR00001## in which each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, L.sub.1, W, and Het is defined herein. Also provides are a method of inhibiting prostaglandin reductase 2 (PTGR2) using such a compound and a pharmaceutical composition containing same.
Pyrimidone compounds used as Lp-PLA.SUB.2 .inhibitors and pharmaceutical compositions thereof
The present invention relates to pyrimidone compounds used as Lp-PLA.sub.2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R.sub.1, R.sub.2, R.sub.3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA.sub.2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA.sub.2 enzyme. ##STR00001##
Pyrimidone compounds used as Lp-PLA.SUB.2 .inhibitors and pharmaceutical compositions thereof
The present invention relates to pyrimidone compounds used as Lp-PLA.sub.2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R.sub.1, R.sub.2, R.sub.3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA.sub.2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA.sub.2 enzyme. ##STR00001##
Heat shock protein binding compounds, compositions, and methods for making and using same
The present subject matter relates to a compound represented by the general formula (I) or (I) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
Heat shock protein binding compounds, compositions, and methods for making and using same
The present subject matter relates to a compound represented by the general formula (I) or (I) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
SULFONYLUREAS AND SULFONYLTHIOUREAS AS NLRP3 INHIBITORS
The present invention relates to compounds of formula (I):
##STR00001##
wherein Q is O or S, R.sup.1 is a 6-membered heteroaryl group containing at least one nitrogen atom in the 6-membered ring structure, wherein R.sup.1 may optionally be substituted, and R.sup.2 is a cyclic group substituted at the -position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
COMPOSITIONS AND METHODS FOR INHIBITING N-SMASE2
Provided herein are compounds of Formula (I) and (II) and their salts, and compositions comprising such compounds that are useful for useful for modulating neutral sphingomyelinase 2 (n-SMase2) in cells. Also disclosed herein are methods of using the disclosed compounds and compositions for inhibiting the spread of Tau seeds from donor cells to recipient cells. Moreover, disclosed herein are methods of using the disclosed compounds and compositions for treating or preventing a neurodegenerative disorder, such as a tauopathy, Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), Lewy body dementia, frontotemporal dementia, and amyotrophic lateral sclerosis (ALS).
COMPOSITIONS AND METHODS FOR INHIBITING N-SMASE2
Provided herein are compounds of Formula (I) and (II) and their salts, and compositions comprising such compounds that are useful for useful for modulating neutral sphingomyelinase 2 (n-SMase2) in cells. Also disclosed herein are methods of using the disclosed compounds and compositions for inhibiting the spread of Tau seeds from donor cells to recipient cells. Moreover, disclosed herein are methods of using the disclosed compounds and compositions for treating or preventing a neurodegenerative disorder, such as a tauopathy, Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), Lewy body dementia, frontotemporal dementia, and amyotrophic lateral sclerosis (ALS).