The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, for use as a drug, especially as an antibiotic. The present invention also relates to a pharmaceutical composition comprising said compound of formula (I) and at least one pharmaceutically acceptable excipient. The present invention further concerns a method of preparation of a compound of formula (I).

##STR00001##

Disclosed herein are methods for preparing [(2S,3R)N[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound G): ##STR00001##
and precursors thereof.

Disclosed herein are methods for preparing [(2S,3R)N[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound G): ##STR00001##
and precursors thereof.

Disclosed herein are methods for preparing [(2S,3R)N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound G): and precursors thereof.

##STR00001##

The invention generally relates to methods of treating a patient having, and/or at risk of, oxidative distress disorders and/or age-related disorders. The disclosure also generally relates to methods of treating memory impairment or enhancing the cognitive function of a patient in need thereof. Such methods may include administering a therapeutically effective amount of a MetAP2 inhibitor.

The invention generally relates to methods of treating a patient having, and/or at risk of, oxidative distress disorders and/or age-related disorders. The disclosure also generally relates to methods of treating memory impairment or enhancing the cognitive function of a patient in need thereof. Such methods may include administering a therapeutically effective amount of a MetAP2 inhibitor.

A flame-retardant aconitic acid-derived monomer, a process for forming a flame-retardant polymer, and an article of manufacture comprising a material that contains a flame-retardant aconitic acid-derived monomer are disclosed. The flame-retardant aconitic acid-derived monomer can have at least one phosphoryl or phosphonyl moiety with functional groups that can participate in a polymerization reaction, such as allyl, epoxy, or propylene carbonate functional groups. The process for forming the flame-retardant polymer can include forming an aconitic acid derivative, forming a phosphorus-based flame-retardant molecule, and reacting the aconitic acid derivative with the phosphorus-based flame-retardant molecule to form a flame-retardant aconitic acid-derived monomer, which is then polymerized. The aconitic acid derivative can be synthesized from aconitic acid obtained from a bio-based source. The material in the article of manufacture can be a resin or adhesive, and the article of manufacture can further comprise an electronic component.

A flame-retardant aconitic acid-derived monomer, a process for forming a flame-retardant polymer, and an article of manufacture comprising a material that contains a flame-retardant aconitic acid-derived monomer are disclosed. The flame-retardant aconitic acid-derived monomer can have at least one phosphoryl or phosphonyl moiety with functional groups that can participate in a polymerization reaction, such as allyl, epoxy, or propylene carbonate functional groups. The process for forming the flame-retardant polymer can include forming an aconitic acid derivative, forming a phosphorus-based flame-retardant molecule, and reacting the aconitic acid derivative with the phosphorus-based flame-retardant molecule to form a flame-retardant aconitic acid-derived monomer, which is then polymerized. The aconitic acid derivative can be synthesized from aconitic acid obtained from a bio-based source. The material in the article of manufacture can be a resin or adhesive, and the article of manufacture can further comprise an electronic component.

Disclosed are a polyene compound, preparation method and use thereof. Provided in the present invention is the preparation method of a polyene compound I, comprising the following steps: under an action of a base and in an organic solvent, conducting a Witting reaction on a compound II and a compound III to obtain the polyene compound I. By the preparation method in the present invention, a coupling reaction results in good product purity without producing an obvious by-product and involves no heavy metal, thus facilitating a control over product quality and costs, having a simple operation and mild reaction condition, enabling high reaction conversion, a high yield, few by-products, high resultant product purity, low production costs and simple post-processing, and being suitable for industrial production.

##STR00001##