A 4-(p-trifluoromethylbenzyl)-3-fluoro-1,2,4-triphenylamine derivative, a pharmaceutical composition and applications thereof are disclosed. The general chemical formula of the derivative is shown in formula I, where, R is a C.sub.1-C.sub.6 alkyl group, a cycloalkyl group, a heteroatom-containing cycloalkyl group, an aryl group or a heteroatom-containing aryl group, the heteroatom is selected from N or O, and the n is 0, 1, 2 or 3. The pharmaceutical composition contains any one of the above-mentioned 4-(p-trifluoromethylbenzyl)-3-fluoro-1,2,4-triphenylamine derivatives as an active ingredient, and one or more pharmaceutically acceptable carriers. The derivative and the pharmaceutical composition activate KCNQ channel currents. Thus, the derivative can be applied to prepare a KCNQ potassium channel opener, and can be used as the active ingredients of an antiepileptic pharmaceutical preparation, an antianxiety pharmaceutical preparation and a neuropathic pain-relieving pharmaceutical preparation.

A 4-(p-trifluoromethylbenzyl)-3-fluoro-1,2,4-triphenylamine derivative, a pharmaceutical composition and applications thereof are disclosed. The general chemical formula of the derivative is shown in formula I, where, R is a C.sub.1-C.sub.6 alkyl group, a cycloalkyl group, a heteroatom-containing cycloalkyl group, an aryl group or a heteroatom-containing aryl group, the heteroatom is selected from N or O, and the n is 0, 1, 2 or 3. The pharmaceutical composition contains any one of the above-mentioned 4-(p-trifluoromethylbenzyl)-3-fluoro-1,2,4-triphenylamine derivatives as an active ingredient, and one or more pharmaceutically acceptable carriers. The derivative and the pharmaceutical composition activate KCNQ channel currents. Thus, the derivative can be applied to prepare a KCNQ potassium channel opener, and can be used as the active ingredients of an antiepileptic pharmaceutical preparation, an antianxiety pharmaceutical preparation and a neuropathic pain-relieving pharmaceutical preparation.

An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action. In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclic. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R.sub.1 and R.sub.2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G.sub.1)-Q.sub.1 or —C(=G.sub.1)-G.sub.2Q.sub.2, and G.sub.1 to G.sub.3 each represent oxygen atoms or the like. Q.sub.1 and Q.sub.2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y.sub.1 and Y.sub.5 each represent a halogen atom or the like, Y.sub.2 and Y.sub.4 each represent a hydrogen atom or the like, and Y.sub.3 represents a C2-C5 haloalkyl group. ##STR00001##

An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action. In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclic. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R.sub.1 and R.sub.2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G.sub.1)-Q.sub.1 or —C(=G.sub.1)-G.sub.2Q.sub.2, and G.sub.1 to G.sub.3 each represent oxygen atoms or the like. Q.sub.1 and Q.sub.2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y.sub.1 and Y.sub.5 each represent a halogen atom or the like, Y.sub.2 and Y.sub.4 each represent a hydrogen atom or the like, and Y.sub.3 represents a C2-C5 haloalkyl group. ##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.

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.

Disclosed herein are compounds for activating the Reelin signaling system for the treatment of neurological disorders Further provided are compounds and methods for activating a lipoprotein receptor, such as ApoER 2 or VLDLR.

Disclosed herein are compounds for activating the Reelin signaling system for the treatment of neurological disorders Further provided are compounds and methods for activating a lipoprotein receptor, such as ApoER 2 or VLDLR.