C07D239/10

Process to prepare propylene amines and propylene amine derivatives

A process is provided to prepare propylene amines of the formula NH.sub.2—(A-NH—).sub.pR, wherein R is a hydrogen atom or an alkyl group, p is at least 1 when R is an alkyl group, and at least 2 when R is a hydrogen atom, or derivatives or precursors thereof wherein one or more units —NH-A-NH— may be present as a cyclic urea unit ##STR00001## or a cyclic unit ##STR00002## or between two units —NH-A-NH— a carbonyl bond is present, each unit -A- can be independently an alkylene unit and at least one unit -A- is a —C.sub.3H.sub.6— unit, wherein each —C.sub.3H.sub.6— unit can be linear or branched. The process includes reacting (i) at least one of a hydroxy-functional compound chosen from the alkanolamine-functional compounds, and dihydroxyalkylene compounds, with (ii) an amine-functional compound, in the presence of (iii) a carbon oxide delivering agent, wherein at least one of the alkanolamine-functional compound, the amine-functional compound and/or the carbon oxide delivering agent contains at least one alkylene unit (A) that is a propylene unit.

METHOD OF PREPARING PYRIMIDINE CYCLOHEXYL GLUCOCORTICOID RECEPTOR MODULATORS

The present invention provides methods of preparing 2-amino-6-((1r,4r)-4-phenylcyclohexyl)-5-(3-(trifluoromethyl)benzyl)pyrimidin-4(3H)-one, and 2-amino-6-((1r,4r)-4-phenylcyclohexyl)-5-(3-(trifluoromethyl)benzyl)pyrimidin-4(3H)-one monohydrate, as well as new intermediate compounds.

METHOD OF PREPARING PYRIMIDINE CYCLOHEXYL GLUCOCORTICOID RECEPTOR MODULATORS

The present invention provides methods of preparing 2-amino-6-((1r,4r)-4-phenylcyclohexyl)-5-(3-(trifluoromethyl)benzyl)pyrimidin-4(3H)-one, and 2-amino-6-((1r,4r)-4-phenylcyclohexyl)-5-(3-(trifluoromethyl)benzyl)pyrimidin-4(3H)-one monohydrate, as well as new intermediate compounds.

N-BENZYL-N-ARYLSULFONAMIDE DERIVATIVE AND PREPARATION AND USE THEREOF

The invention provides an N-benzyl-N-arylsulfonamide derivative, which is an N-benzyl-N-arylsulfonamide compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof. The N-benzyl-N-arylsulfonamide derivative is obtained by condensing a substituted nitrobenzene with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B), reducing the nitro group to an amino group, and subjecting the amino group to reductive amination, sulfonamidation; or by subjecting a substituted nitrobenzene to nitro reduction, reductive amination and sulfonamidation, and condensing the resultant intermediate with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B). It has been experimentally demonstrated that the N-benzyl-N-arylsulfonamide derivative of the invention can specifically bind to Kv1.3 potassium channel and inhibit or decrease its activity, and is useful in the treatment of autoimmune diseases caused by abnormal activation of the Kv1.3 potassium channel in human or animals. The invention further provides a medicament or a pharmaceutical composition comprising the N-benzyl-N-arylsulfonamide derivative.

##STR00001##

MATERIAL FOR FORMING ORGANIC FILM, METHOD FOR FORMING ORGANIC FILM, PATTERNING PROCESS, AND COMPOUND

The present invention is a material for forming an organic film, including: a compound shown by the following general formula (1); and an organic solvent, where in the general formula (1), X represents an organic group with a valency of “n” having 2 to 50 carbon atoms or an oxygen atom, “n” represents an integer of 1 to 10, and R.sub.1 independently represents any of the following general formulae (2), where in the general formulae (2), broken lines represent attachment points to X, and Q.sub.1 represents a monovalent organic group containing a carbonyl group, at least a part of which is a group shown by the following general formulae (3), where in the general formulae (3), broken lines represent attachment points, X.sub.1 represents a single bond or a divalent organic group having 1 to 20 carbon atoms optionally having a substituent when the organic group has an aromatic ring, R.sub.2 represents a hydrogen atom, a methyl group, an ethyl group, or a phenyl group, and ** represents an attachment point. An object of the present invention is to provide a material for forming an organic film for forming an organic film having dry etching resistance, and also having high filling and planarizing properties and adhesion to a substrate.

##STR00001##

MATERIAL FOR FORMING ORGANIC FILM, METHOD FOR FORMING ORGANIC FILM, PATTERNING PROCESS, AND COMPOUND

The present invention is a material for forming an organic film, including: a compound shown by the following general formula (1); and an organic solvent, where in the general formula (1), X represents an organic group with a valency of “n” having 2 to 50 carbon atoms or an oxygen atom, “n” represents an integer of 1 to 10, and R.sub.1 independently represents any of the following general formulae (2), where in the general formulae (2), broken lines represent attachment points to X, and Q.sub.1 represents a monovalent organic group containing a carbonyl group, at least a part of which is a group shown by the following general formulae (3), where in the general formulae (3), broken lines represent attachment points, X.sub.1 represents a single bond or a divalent organic group having 1 to 20 carbon atoms optionally having a substituent when the organic group has an aromatic ring, R.sub.2 represents a hydrogen atom, a methyl group, an ethyl group, or a phenyl group, and ** represents an attachment point. An object of the present invention is to provide a material for forming an organic film for forming an organic film having dry etching resistance, and also having high filling and planarizing properties and adhesion to a substrate.

##STR00001##

SULFONAMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE ACID-ADDITION SALT

The present invention aims to provide a novel low-molecular-weight compound showing an orexin receptor agonist activity and expected to be useful as a prophylactic or therapeutic agent for narcolepsy and the like. The present invention provides a compound represented by the formula (I):

##STR00001##

wherein each symbol is as described in the description, or a pharmaceutically acceptable acid addition salt thereof, which has an orexin receptor agonist activity, and an orexin receptor agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

SULFONAMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE ACID-ADDITION SALT

The present invention aims to provide a novel low-molecular-weight compound showing an orexin receptor agonist activity and expected to be useful as a prophylactic or therapeutic agent for narcolepsy and the like. The present invention provides a compound represented by the formula (I):

##STR00001##

wherein each symbol is as described in the description, or a pharmaceutically acceptable acid addition salt thereof, which has an orexin receptor agonist activity, and an orexin receptor agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

LUMINESCENT JANUS-TYPE, TWO-COORDINATED METAL COMPLEXES

The co-linear or near co-linear structure of bimetallic Janus-type two-coordinated metal complexes may allow for a large transition dipole moment that can enhance the radiative lifetime. The symmetric nature of the bimetallic Janus complexes diminishes or eliminates the polar nature of the monometallic carbene-metal-amide/arene complexes.

PROCESS TO PREPARE PROPYLENE AMINES AND PROPYLENE AMINE DERIVATIVES

A process is provided to prepare propylene amines of the formula NH.sub.2(ANH).sub.pR, wherein R is a hydrogen atom or an alkyl group, p is at least 1 when R is an alkyl group, and at least 2 when R is a hydrogen atom, or derivatives or precursors thereof wherein one or more units NHANH may be present as a cyclic urea unit

##STR00001##

or a cyclic unit

##STR00002##

or between two units NHANH a carbonyl bond is present, each unit A can be independently an alkylene unit and at least one unit A is a C.sub.3H.sub.6 unit, wherein each C.sub.3H.sub.6 unit can be linear or branched. The process includes reacting (i) at least one of a hydroxy-functional compound chosen from the alkanolamine-functional compounds, and dihydroxyalkylene compounds, with (ii) an amine-functional compound, in the presence of (iii) a carbon oxide delivering agent, wherein at least one of the alkanolamine-functional compound, the amine-functional compound and/or the carbon oxide delivering agent contains at least one alkylene unit (A) that is a propylene unit