An AdipoR activator for activating both AdipoR1 and AdipoR2 is provided. A compound represented by the following formula (1), wherein A is a substituted or unsubstituted aryl group or the like, Y.sup.1 is (CHR.sup.2).sub.a— or the like, X is CH or N, R.sup.1 is a C.sub.1-7 alkyl group, m is an integer of 0-4, Y.sup.2 is *—O—CH.sub.2—CONH—, *—CONH—(CH.sub.2).sub.b—CO— or the like, Z is a cyclic group, B may be a substituent of the cyclic group represented by Z, and n is an integer of 0-3.

##STR00001##

Cyclooctene conjugates of therapeutic or diagnostic agents have improved aqueous solubility and can release the agents upon contact with a tetrazine-containing biomaterial. The cyclooctene conjugates provide site-selective delivery of agents at the location of the tetrazine-containing biomaterial in a subject. The compositions and methods have applications in the treatment of various diseases or conditions including cancer, tumor growths, and bacterial infections.

The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDMIA, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDMIA, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

The present invention relates to a composition comprising a polymeric network having at least one unit of formula (I), (II), and/or (III); (I) (II) (III) wherein said composition is obtained by contacting at least one compound A comprising at least two functions selected from the group of function of formula X—C(═O)—CHR.sup.1—C(═O)—R.sup.2, —C(═O)—C—R.sup.2; or —C(═O)—CR.sup.1═CR.sup.2—NR.sup.4R.sup.5; wherein at least 25% by weight of compounds A have a functionality ≦5, with % by weight relative to the total weight of compounds A; with at least one compound B comprising at least one NH.sub.2, or NH.sub.3.sup.+ groups; wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to a compound comprising at least two units and at most 5 units of formula (I), (II), and/or (III); wherein R.sup.1, R.sup.2, R.sup.3, X, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to processes for preparing said composition and said compounds, to material, articles, and polymers comprising or using said compositions and compounds, and the use thereof.

##STR00001##

The present invention relates to a composition comprising a polymeric network having at least one unit of formula (I), (II), and/or (III); (I) (II) (III) wherein said composition is obtained by contacting at least one compound A comprising at least two functions selected from the group of function of formula X—C(═O)—CHR.sup.1—C(═O)—R.sup.2, —C(═O)—C—R.sup.2; or —C(═O)—CR.sup.1═CR.sup.2—NR.sup.4R.sup.5; wherein at least 25% by weight of compounds A have a functionality ≦5, with % by weight relative to the total weight of compounds A; with at least one compound B comprising at least one NH.sub.2, or NH.sub.3.sup.+ groups; wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to a compound comprising at least two units and at most 5 units of formula (I), (II), and/or (III); wherein R.sup.1, R.sup.2, R.sup.3, X, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to processes for preparing said composition and said compounds, to material, articles, and polymers comprising or using said compositions and compounds, and the use thereof.

##STR00001##

A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.

A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.