The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.

The present invention relates to a novel compound, which enables additional hydrogen bonding with amino acids at specific positions of histone acetyltransferase (HAT) p300, through structure analysis of HAT p300. The novel compound of the present invention has a remarkably excellent effect of inhibiting HAT p300 activity and thus can be very effectively used in the prevention, alleviation, or treatment of fibrosis, which is a disease associated with activation of HAT p300.

The present invention relates to a novel compound, which enables additional hydrogen bonding with amino acids at specific positions of histone acetyltransferase (HAT) p300, through structure analysis of HAT p300. The novel compound of the present invention has a remarkably excellent effect of inhibiting HAT p300 activity and thus can be very effectively used in the prevention, alleviation, or treatment of fibrosis, which is a disease associated with activation of HAT p300.

The present invention provides a polyethylene glycol derivative comprising a repeat unit having the structure of Formula (I) and a terminal group having the structure of Formula (II). The polyethylene glycol derivative provided by the present invention has good biocompatibility, due to the repeat unit having the structure of Formula (I); and can react with various groups such as amino, (acyl)hydrazino, and aminooxy with a fast reaction rate under mild reaction conditions, due to the o-phthalaldehyde terminal group having the structure of Formula (II). The polyethylene glycol derivative provided by the present invention is mixed with polyethylene glycol having an amino-containing terminal group in an aqueous medium, to rapidly form a chemically cross-linked hydrogel material. The hydrogel material has mild preparation conditions, fast gel-forming speed, high mechanical strength, and good stability. This polyethylene glycol hydrogel can be applied as drug sustained-release carrier, tissue engineering scaffold, etc. in the field of biomedical materials.

The present invention provides benzamide compounds, compositions containing the benzamides, and use of the benzamides for inhibiting androgen receptor (AR) and/or aldo-keto reductase family 1 member C3 (AKR1C3). Also described herein methods for the treatment of hormone-mediated diseases and conditions, including hormone-related cancers such as castration resistant prostate cancer.

Disclosed herein are methods for inducing insulin secretion in a glucose-dependent manner and compounds for use in these methods. The compounds may have the structure of formula I(a): ##STR00001##
wherein the substituents are as described in the description;
or a pharmaceutically acceptable form thereof.

Disclosed herein are methods for inducing insulin secretion in a glucose-dependent manner and compounds for use in these methods. The compounds may have the structure of formula I(a): ##STR00001##
wherein the substituents are as described in the description;
or a pharmaceutically acceptable form thereof.

Disclosed herein are tucaresol derivative compound and composition containing the same. Also disclosed herein are methods of enhancing immune response in a subject by administering the tucaresol derivative compound or by co-administering the tucaresol derivative compound and one or more additional agents. Also disclosed herein are use of the tucaresol derivative compound and composition containing the same in the manufacture of a medicament for treating cancer or enhancing immune response in a subject.

Disclosed herein are tucaresol derivative compound and composition containing the same. Also disclosed herein are methods of enhancing immune response in a subject by administering the tucaresol derivative compound or by co-administering the tucaresol derivative compound and one or more additional agents. Also disclosed herein are use of the tucaresol derivative compound and composition containing the same in the manufacture of a medicament for treating cancer or enhancing immune response in a subject.

Disclosed are compounds of formulas (I)-(IX) for treating or preventing a disease or disorder responsive to antagonism of a P2Y.sub.14R receptor agonist in a mammal in need thereof, wherein R.sup.1-R.sup.8, X, Y, Z, X′, Y′, Z′, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney. ##STR00001##