The invention provides compounds having activity as bacterial RNA polymerase inhibitors and antibacterial agents, as well as compositions comprising the compounds and methods for their use. Specifically, phenylalanineamide and tyrosinamide compounds are disclosed that have inhibitory activity toward mycobacterium tuberculosis RNA polymerase. Use of these compounds in the treatment or prevention of M. tuberculosis infections in a mammal, is disclosed.

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 heterocyclie. 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 heterocyclie. 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 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##

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.

The present disclosure is directed to a covalent organic framework comprising repeating units of a moiety comprising Formula (I):

##STR00001##

wherein X, Y, R, R, n.sub.1, and n.sub.2 are as described herein. The present disclosure is also directed to a method of making the covalent organic frameworks and a method of separating rare-earth elements using the covalent organic frameworks.

The present disclosure is directed to a covalent organic framework comprising repeating units of a moiety comprising Formula (I):

##STR00001##

wherein X, Y, R, R, n.sub.1, and n.sub.2 are as described herein. The present disclosure is also directed to a method of making the covalent organic frameworks and a method of separating rare-earth elements using the covalent organic frameworks.

A compound represented by Formula I described below or a salt of the compound:

##STR00001## wherein R.sup.1 is a substituent and R.sup.1H has a pKa of 4 to 14, R.sup.2 or R.sup.3 has an IgG-binding peptide that specifically binds to an Fc region of an IgG, and R.sup.4 is H or a substituted or unsubstituted alkyl group having 1 to 8 carbon atoms.