Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.

This invention relates to a field of pharmaceuticals, in particular to desidustat particles having specific particle size distribution and pharmaceutical compositions thereof.

A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of:

##STR00001##

wherein X is N, C(OH), or CH;
Y is H or OH;
each of Z.sup.1-Z.sup.5 is independently H or halogen;
R.sup.4 is H, OH, NH.sub.2, NHR.sup.8, NR.sup.8R.sup.9 or R.sup.8;
R.sup.5, R.sup.6, and R.sup.7 is each independently H, halogen, OR.sup.8, R.sup.8, NHR.sup.8, NR.sup.8R.sup.9, CO.sub.2R.sup.8, CONR.sup.8R.sup.9, SO.sub.2NR.sup.8R.sup.9, or R.sup.5 and R.sup.6 together with the carbon atoms to which R.sup.5 and R.sup.6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and
R.sup.8 and R.sup.9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R.sup.8 and R.sup.9 together with the nitrogen to which R.sup.8 and R.sup.9 are attached form an optionally-substituted heterocycle.

A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of:

##STR00001##

wherein X is N, C(OH), or CH;
Y is H or OH;
each of Z.sup.1-Z.sup.5 is independently H or halogen;
R.sup.4 is H, OH, NH.sub.2, NHR.sup.8, NR.sup.8R.sup.9 or R.sup.8;
R.sup.5, R.sup.6, and R.sup.7 is each independently H, halogen, OR.sup.8, R.sup.8, NHR.sup.8, NR.sup.8R.sup.9, CO.sub.2R.sup.8, CONR.sup.8R.sup.9, SO.sub.2NR.sup.8R.sup.9, or R.sup.5 and R.sup.6 together with the carbon atoms to which R.sup.5 and R.sup.6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and
R.sup.8 and R.sup.9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R.sup.8 and R.sup.9 together with the nitrogen to which R.sup.8 and R.sup.9 are attached form an optionally-substituted heterocycle.

This invention relates to fluorinating agents and, more particularly, to chiral non-racemic fluorinating agents useful for enantioselective fluorination, as well as to their synthesis and use and other subject matter. The fluorinating agents are based on a substituted 1,4-diazabicyclo[2.2.2]octane (DABCO) skeleton and provide electrophillic fluorine enantioselectively.

This invention relates to fluorinating agents and, more particularly, to chiral non-racemic fluorinating agents useful for enantioselective fluorination, as well as to their synthesis and use and other subject matter. The fluorinating agents are based on a substituted 1,4-diazabicyclo[2.2.2]octane (DABCO) skeleton and provide electrophillic fluorine enantioselectively.

The invention provides tetrahydroquinoline sulfonamide compounds, tetrahydronaphthalene sulfonyl compounds, and related compounds, pharmaceutical compositions, methods of promoting RORy activity, methods of increasing the amount of IL-17 in a subject, and methods of treating cancer and other medical disorders using such compounds.

The invention provides tetrahydroquinoline sulfonamide compounds, tetrahydronaphthalene sulfonyl compounds, and related compounds, pharmaceutical compositions, methods of promoting RORy activity, methods of increasing the amount of IL-17 in a subject, and methods of treating cancer and other medical disorders using such compounds.

A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: ##STR00001##
wherein X is N, C(OH), or CH;
Y is H or OH;
each of Z.sup.1-Z.sup.5 is independently H or halogen;
R.sup.4 is H, OH, NH.sub.2, NHR.sup.8, NR.sup.8R.sup.9 or R.sup.8;
R.sup.5, R.sup.6, and R.sup.7 is each independently H, halogen, OR.sup.8, R.sup.8, NHR.sup.8, NR.sup.8R.sup.9, CO.sub.2R.sup.8, CONR.sup.8R.sup.9, SO.sub.2NR.sup.8R.sup.9, or R.sup.5 and R.sup.6 together with the carbon atoms to which R.sup.5 and R.sup.6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and
R.sup.8 and R.sup.9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R.sup.8 and R.sup.9 together with the nitrogen to which R.sup.8 and R.sup.9 are attached form an optionally-substituted heterocycle.

A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: ##STR00001##
wherein X is N, C(OH), or CH;
Y is H or OH;
each of Z.sup.1-Z.sup.5 is independently H or halogen;
R.sup.4 is H, OH, NH.sub.2, NHR.sup.8, NR.sup.8R.sup.9 or R.sup.8;
R.sup.5, R.sup.6, and R.sup.7 is each independently H, halogen, OR.sup.8, R.sup.8, NHR.sup.8, NR.sup.8R.sup.9, CO.sub.2R.sup.8, CONR.sup.8R.sup.9, SO.sub.2NR.sup.8R.sup.9, or R.sup.5 and R.sup.6 together with the carbon atoms to which R.sup.5 and R.sup.6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and
R.sup.8 and R.sup.9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R.sup.8 and R.sup.9 together with the nitrogen to which R.sup.8 and R.sup.9 are attached form an optionally-substituted heterocycle.