The present application provides a one-pot catalytic process which involves the formation of 1,4-dibenzodiazepines from o-haloaldimines (either pre-formed or formed in situ) of formula (I) and o-haloanilines of formula (II) via a palladium catalyzed Buchwald-Hartwig reaction and a cyclization sequence, to afford the 1,4-dibenzodiazepine products of formula (III). The present application describes the preparation of the 1,4-dibenzodiazepine products of formula (III) from simple commercial raw materials by efficient processes.

##STR00001##

The present application provides a one-pot catalytic process which involves the formation of 1,4-dibenzodiazepines from o-haloaldimines (either pre-formed or formed in situ) of formula (I) and o-haloanilines of formula (II) via a palladium catalyzed Buchwald-Hartwig reaction and a cyclization sequence, to afford the 1,4-dibenzodiazepine products of formula (III). The present application describes the preparation of the 1,4-dibenzodiazepine products of formula (III) from simple commercial raw materials by efficient processes.

##STR00001##

The present invention relates to MLL fusion proteins (e.g., AF9 and ENL), which activate target genes in part via recruitment of histone methyltransferase DOT1L. In particular, the present invention provides the AF9/ENL binding site in DOT1L and agents that block the protein-protein interactions between AF9/ENL and DOT1L, therefore inhibiting the activity of DOT1L, and inhibiting MLL-fusion protein associated leukemia.

A diazepine derivative represented by formula (I), where R.sup.1 and R.sup.2 represent hydrogen, or R.sup.1 and R.sup.2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 each represents hydrogen, X represents C, CH or N, Y represents N, NH or C(O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(O), Z represents oxygen or sulfur, A represents benzene ring and the like, B represents NHC(O) and the like, D and E each represents an atomic bond, G represents benzene which may be substituted, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist.

##STR00001##

A diazepine derivative represented by formula (I), where R.sup.1 and R.sup.2 represent hydrogen, or R.sup.1 and R.sup.2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 each represents hydrogen, X represents C, CH or N, Y represents N, NH or C(O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(O), Z represents oxygen or sulfur, A represents benzene ring and the like, B represents NHC(O) and the like, D and E each represents an atomic bond, G represents benzene which may be substituted, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist.

##STR00001##

G protein-coupled receptor (GPCR) regulators and methods for their use are provided herein. The GPCR regulators described herein are useful in treating and/or preventing conditions or diseases associated with a GPCR, including ageing, cancer, cardiovascular disorders, hematologic disorders, infectious diseases, inflammatory diseases, metabolic diseases, neurodegenerative disorders, respiratory diseases, or urological disorders. Also provided are methods of regulating a G protein-coupled receptor in a cell using the compounds and compositions described herein.

G protein-coupled receptor (GPCR) regulators and methods for their use are provided herein. The GPCR regulators described herein are useful in treating and/or preventing conditions or diseases associated with a GPCR, including ageing, cancer, cardiovascular disorders, hematologic disorders, infectious diseases, inflammatory diseases, metabolic diseases, neurodegenerative disorders, respiratory diseases, or urological disorders. Also provided are methods of regulating a G protein-coupled receptor in a cell using the compounds and compositions described herein.

The present invention pertains to a medicament for preventing or treating cough, including, as an active ingredient, a compound having P2X4 receptor antagonistic action, a tautomer, stereoisomer, or pharmaceutically acceptable salt of the compound, or a hydrate or solvate thereof.

The present invention is directed to a compound represented by Structural Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.

The present invention is directed to a compound represented by Structural Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.