Disclosed herein are small molecule Vascular Adhesion Protein-1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.

Disclosed herein are small molecule Vascular Adhesion Protein-1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.

The present invention provides a 1,4-disubstituted imidazole derivative of formula (1′) wherein ring Q.sup.1 is optionally-substituted C.sub.6-10 aryl group, etc.; R.sup.1 and R.sup.2 are independently hydrogen atom, etc.; W.sup.1 is optionally-substituted C.sub.1-4 alkylene group; W.sup.2 is —NR.sup.3aC(O)— wherein R.sup.3a is hydrogen atom or C.sub.1-6 alkyl group, etc.; ring Q.sup.2 is 5- to 10-membered heteroaryl group, etc.; W.sup.3 is optionally-substituted C.sub.1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R.sup.4 is independently halogen atom, optionally-substituted C.sub.1-6 alkyl group, etc.; R.sup.5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

##STR00001##

The present invention provides a 1,4-disubstituted imidazole derivative of formula (1′) wherein ring Q.sup.1 is optionally-substituted C.sub.6-10 aryl group, etc.; R.sup.1 and R.sup.2 are independently hydrogen atom, etc.; W.sup.1 is optionally-substituted C.sub.1-4 alkylene group; W.sup.2 is —NR.sup.3aC(O)— wherein R.sup.3a is hydrogen atom or C.sub.1-6 alkyl group, etc.; ring Q.sup.2 is 5- to 10-membered heteroaryl group, etc.; W.sup.3 is optionally-substituted C.sub.1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R.sup.4 is independently halogen atom, optionally-substituted C.sub.1-6 alkyl group, etc.; R.sup.5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.

##STR00001##

The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I), to the compound of the formula (I) in crystalline form and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders.

The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I), to the compound of the formula (I) in crystalline form and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders.

The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention.

The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention.

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.