Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.

Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.

The present invention provides a compound represented by following formula (1), ##STR00001##
wherein R.sup.1 represents a 2n-valent group having 1 to 30 carbon atoms, each of R.sup.2 to R.sup.5 independently represents a straight, branched or cyclic alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkoxy group having 1 to 30 carbon atoms, a halogen atom, a thiol group or a hydroxyl group, provided that at least one selected from R.sup.1 to R.sup.5 represents a group including an iodine atom and at least one R.sup.4 and/or at least one R.sup.5 represent/represents one or more selected from the group consisting of a hydroxyl group and a thiol group, each of m.sup.2 and m.sup.3 independently represents an integer of 0 to 8, each of m.sup.4 and m.sup.5 independently represents an integer of 0 to 9, provided that m.sup.4 and m.sup.5 do not represent 0 at the same time, n represents an integer of 1 to 4, and each of p.sup.2 to p.sup.5 independently represents an integer of 0 to 2.

The present invention provides a compound represented by following formula (1), ##STR00001##
wherein R.sup.1 represents a 2n-valent group having 1 to 30 carbon atoms, each of R.sup.2 to R.sup.5 independently represents a straight, branched or cyclic alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkoxy group having 1 to 30 carbon atoms, a halogen atom, a thiol group or a hydroxyl group, provided that at least one selected from R.sup.1 to R.sup.5 represents a group including an iodine atom and at least one R.sup.4 and/or at least one R.sup.5 represent/represents one or more selected from the group consisting of a hydroxyl group and a thiol group, each of m.sup.2 and m.sup.3 independently represents an integer of 0 to 8, each of m.sup.4 and m.sup.5 independently represents an integer of 0 to 9, provided that m.sup.4 and m.sup.5 do not represent 0 at the same time, n represents an integer of 1 to 4, and each of p.sup.2 to p.sup.5 independently represents an integer of 0 to 2.

The present invention provides a compound represented by following formula (1), ##STR00001##
wherein R.sup.1 represents a 2n-valent group having 1 to 30 carbon atoms, each of R.sup.2 to R.sup.5 independently represents a straight, branched or cyclic alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkoxy group having 1 to 30 carbon atoms, a halogen atom, a thiol group or a hydroxyl group, provided that at least one selected from R.sup.1 to R.sup.5 represents a group including an iodine atom and at least one R.sup.4 and/or at least one R.sup.5 represent/represents one or more selected from the group consisting of a hydroxyl group and a thiol group, each of m.sup.2 and m.sup.3 independently represents an integer of 0 to 8, each of m.sup.4 and m.sup.5 independently represents an integer of 0 to 9, provided that m.sup.4 and m.sup.5 do not represent 0 at the same time, n represents an integer of 1 to 4, and each of p.sup.2 to p.sup.5 independently represents an integer of 0 to 2.

The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compoundsdiarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compoundsdiarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

Compounds that inhibit or reduce glucose transport and methods of using the compounds to treat cancer are provided herein.

The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compoundsdiarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compoundsdiarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.