A compound of formula (I) ##STR00001##
wherein X is 0, C=0 or S; Y is N or CH; R.sub.2 and R.sub.4 are each independently H, —(CH.sub.2).sub.pCOOH, —(CH.sub.2).sub.pCON(R.sup.5).sub.2 or —(CH.sub.2).sub.pCOOC.sub.1-6alkyl; or R.sub.2 and R.sub.4 together form a 6-membered phenyl ring fused to the five membered ring; each R.sub.1 is independently selected from H, halo (e.g. fluoro or chloro), C.sub.6-10aryl, C.sub.7-12arylalkyl, C.sub.2-12 alkenyl; OC.sub.1-12 alkyl, OC.sub.2-12 alkenyl or a C.sub.1-12 alkyl group; each R.sup.5 is H or C.sub.1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof.

A compound of formula (I) ##STR00001##
wherein X is 0, C=0 or S; Y is N or CH; R.sub.2 and R.sub.4 are each independently H, —(CH.sub.2).sub.pCOOH, —(CH.sub.2).sub.pCON(R.sup.5).sub.2 or —(CH.sub.2).sub.pCOOC.sub.1-6alkyl; or R.sub.2 and R.sub.4 together form a 6-membered phenyl ring fused to the five membered ring; each R.sub.1 is independently selected from H, halo (e.g. fluoro or chloro), C.sub.6-10aryl, C.sub.7-12arylalkyl, C.sub.2-12 alkenyl; OC.sub.1-12 alkyl, OC.sub.2-12 alkenyl or a C.sub.1-12 alkyl group; each R.sup.5 is H or C.sub.1-6 alkyl; each p is 0 to 3; n is 1 to 4; or a salt, ester, solvate, N-oxide, or prodrug thereof, e.g. a salt thereof.

High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

The present invention relates to pharmaceutical formulations to treat gout by managing uric acid content in human body by control of making of uric acid in the body and/or removing uric acid from the body. Further, such formulations for treatment of gout are fast available for pharmacological action. Pharmaceutical formulation of the present invention is orally disintegrating solid pharmaceutical dosage form of febuxostat for treating hyperuricemia.

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

The present invention relates to novel linkers containing a 2,3-disubstituted succinic group, or 2-monosubstituted, or 2,3-disubstituted fumaric or maleic (trans (E)- or cis (Z)-butenedioic), or acetylenedicarboxyl group for conjugation of a cytotoxic agent, and/or one or more different functional molecules per linker to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule specifically. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.

The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.