The invention provides a compound according to formula (I) or a tautomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, W.sub.1, W.sub.2, W.sub.3, A, X and Y are as defined in the specification. The compounds are potent inhibitors of the serine/threonine kinase, TAK1. The present invention further provides: a pharmaceutical composition comprising a compound of formula (I) and at least one pharmaceutically acceptable excipient; a compound of formula (I) for use as a medicament (for example for the treatment or prophylaxis of a condition selected from cancer, inflammatory diseases, autoinflammatory diseases and autoimmune diseases); and a method of treating or preventing a disease or disorder comprising administering a pharmaceutically effective amount of a compound of formula (I) to a subject in need thereof.

##STR00001##

The present invention discloses a 1,4-sulfur-bridged polycyclic compound containing dihydrobenzofuran structure which has a structural formula (I). A preparation method is also disclosed which includes the steps of: dissolving 2-nitrobenzofuran (II) and 5H-thiazolone (III) in an organic solvent; then adding molecular sieve and chiral catalyst, stirring and allowing reaction at room temperature under argon protection until the reaction is completed; and carrying out separation and purification to obtain a 1,4-sulfur-bridged polycyclic compound (I) containing dihydrobenzofuran structure. The polycyclic compounds of the present invention have a substructure of dihydrobenzofuran and 1,4-thiopiperidinone. The application of the compound for the preparation of antitumor drugs is also disclosed, which has a good potential value in antitumor drug research. The preparation method has the advantages of novelty, simplicity, simple operation, mild reaction conditions, high yield and high stereoselectivity, and etc.

The present invention discloses a 1,4-sulfur-bridged polycyclic compound containing dihydrobenzofuran structure which has a structural formula (I). A preparation method is also disclosed which includes the steps of: dissolving 2-nitrobenzofuran (II) and 5H-thiazolone (III) in an organic solvent; then adding molecular sieve and chiral catalyst, stirring and allowing reaction at room temperature under argon protection until the reaction is completed; and carrying out separation and purification to obtain a 1,4-sulfur-bridged polycyclic compound (I) containing dihydrobenzofuran structure. The polycyclic compounds of the present invention have a substructure of dihydrobenzofuran and 1,4-thiopiperidinone. The application of the compound for the preparation of antitumor drugs is also disclosed, which has a good potential value in antitumor drug research. The preparation method has the advantages of novelty, simplicity, simple operation, mild reaction conditions, high yield and high stereoselectivity, and etc.

An isolated compound of Formula I and salts thereof are provided:

##STR00001##

wherein X is Cl or Br. A compound isolated from Actinomadura and having a chemical formula of C.sub.43H.sub.69ClN.sub.4O.sub.10S.sub.2 or C.sub.43H.sub.69BrN.sub.4O.sub.10S.sub.2 is also provided. Compositions including the compounds and methods of using the compounds to treat fungal infections including those such as Candida are also disclosed.

An isolated compound of Formula I and salts thereof are provided:

##STR00001##

wherein X is Cl or Br. A compound isolated from Actinomadura and having a chemical formula of C.sub.43H.sub.69ClN.sub.4O.sub.10S.sub.2 or C.sub.43H.sub.69BrN.sub.4O.sub.10S.sub.2 is also provided. Compositions including the compounds and methods of using the compounds to treat fungal infections including those such as Candida are also disclosed.

Use of H3K9me3 modulation for enhancing cognitive function and treating anxiety related disorders is presented. A composition is administered to the subject comprising a therapeutically effective amount of a SUV39H1 inhibitor comprising analogs of ETP69. The therapeutically effective amount is effective in treating cognitive dysfunction in aging and age-related disorders.

Provided herein, inter alia, is the synthesis of ETP derivatives. The uses of the ETP derivatives described herein include treatment of cancer.

Provided herein, inter alia, is the synthesis of ETP derivatives. The uses of the ETP derivatives described herein include treatment of cancer.

The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as -lactamase inhibitors and/or as antibacterial agents.

The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as -lactamase inhibitors and/or as antibacterial agents.