Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I ##STR00001##
wherein X, Y, B, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n have the meanings found herein.

The invention features all-trans retinoic acid (ATRA)-related compounds capable of associating with Pin1 and methods of identifying the same. The invention also provides methods of treating a condition selected from the group consisting of a proliferative disorder, an autoimmune disease, and an addiction condition characterized by elevated Pin1 marker levels, Pin1 degradation, and/or reduced Pin1 Ser71 phosphorylation in a subject by administering a retinoic acid compound. Additionally, the invention features methods of treating proliferative disorders, autoimmune diseases, and addiction conditions (e.g., diseases, disorders, and conditions characterized by elevated Pin1 marker levels) by administering a retinoic acid compound in combination with another therapeutic compound. The invention also features a co-crystal including Pin1 and a retinoic acid compound. Finally, the invention also provides methods of developing and identifying enhanced Pin1-targeted ATRA-related compounds based on the newly defined unique binding pockets in the Pin1 active site revealed from the co-crystal structure, structure-activity relationship, and structural modeling.

The invention features all-trans retinoic acid (ATRA)-related compounds capable of associating with Pin1 and methods of identifying the same. The invention also provides methods of treating a condition selected from the group consisting of a proliferative disorder, an autoimmune disease, and an addiction condition characterized by elevated Pin1 marker levels, Pin1 degradation, and/or reduced Pin1 Ser71 phosphorylation in a subject by administering a retinoic acid compound. Additionally, the invention features methods of treating proliferative disorders, autoimmune diseases, and addiction conditions (e.g., diseases, disorders, and conditions characterized by elevated Pin1 marker levels) by administering a retinoic acid compound in combination with another therapeutic compound. The invention also features a co-crystal including Pin1 and a retinoic acid compound. Finally, the invention also provides methods of developing and identifying enhanced Pin1-targeted ATRA-related compounds based on the newly defined unique binding pockets in the Pin1 active site revealed from the co-crystal structure, structure-activity relationship, and structural modeling.

A method of reducing an aromatic ring or a cyclic, allylic ether in a compound includes preparing a reaction mixture including a compound including an aromatic moiety or a cyclic, allylic ether moiety, an alkali metal, and either ethylenediamine, diethylenetriamine, triethylenetetramine, or a combination thereof, in an ether solvent; and reacting the reaction mixture at from 20 C. to 30 C. for a time sufficient to reduce a double bond in the aromatic moiety to a single bond or to reduce the cyclic, allylic ether moiety.

A method of reducing an aromatic ring or a cyclic, allylic ether in a compound includes preparing a reaction mixture including a compound including an aromatic moiety or a cyclic, allylic ether moiety, an alkali metal, and either ethylenediamine, diethylenetriamine, triethylenetetramine, or a combination thereof, in an ether solvent; and reacting the reaction mixture at from 20 C. to 30 C. for a time sufficient to reduce a double bond in the aromatic moiety to a single bond or to reduce the cyclic, allylic ether moiety.

An artemisinic acid derivative includes: a water-soluble organic salt formed by a reaction of artemisinic acid or dihydroartemisinic acid with a small-molecule basic organic compound, or a water-soluble complex formed by a reaction of artemisinic acid or dihydroartemisinic acid with a small molecule peptide, or a water-soluble salt formed by a reaction of artemisinic acid or dihydroartemisinic acid with a basic metal compound. The artemisinic acid derivative provided by the present application solves the problem of difficulty in dissolving the artemisinic acid and the dihydroartemisinic acid in water, and combines whitening, anti-inflammatory, and anti-tumor biological activities, thus having a good research and development prospect.

An artemisinic acid derivative includes: a water-soluble organic salt formed by a reaction of artemisinic acid or dihydroartemisinic acid with a small-molecule basic organic compound, or a water-soluble complex formed by a reaction of artemisinic acid or dihydroartemisinic acid with a small molecule peptide, or a water-soluble salt formed by a reaction of artemisinic acid or dihydroartemisinic acid with a basic metal compound. The artemisinic acid derivative provided by the present application solves the problem of difficulty in dissolving the artemisinic acid and the dihydroartemisinic acid in water, and combines whitening, anti-inflammatory, and anti-tumor biological activities, thus having a good research and development prospect.