The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

##STR00001##

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

##STR00001##

A method for producing an alkylamine derivative having a urea bond represented by formula (I), or a salt thereof, comprises the following steps (a) and (b), step (a):

##STR00001##

and step (b): deprotecting as necessary the reaction product obtained in step (a). The production method suitable for industrialization of the alkylamine derivative having a urea bond represented by formula (I), which is a compound highly useful as an agent having CaSR agonist effects is provided.

The present invention is directed to a method for enhancing the rate of formation of the reaction products of a carboxylic acid and a urea having the formula: ##STR00001##
where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, substituted and unsubstituted alkyl, allyl, vinyl and alkoxyl groups having from 1-6 carbon atoms, substituted and unsubstituted phenyl groups and the halides. The rate of formation is enhanced by adding acid to a solution including the carboxylic acid and the urea. Preferably, the reaction product of the present invention is N,N-diformylurea or N,N-diacetylurea. These reaction products, e.g., diformylurea, have been found to produce significantly improved growth in a variety of agricultural products when applied to the seed, to the surrounding soil or to the foliage of the emerging plant.

A compound of formula (I) or pharmaceutically acceptable salts or hydrates thereof:

##STR00001## wherein R is chosen from phenyl, a 6-membered heteroaryl group, cyclohexyl, a 5-membered heteroaryl group; a bicyclo [3.1.0] hexanyl group; a C.sub.2-C.sub.5 alkynyl group; and a cubanyl group; wherein R1 and R2, independently, are chosen from H; C.sub.1-C.sub.6 alkyl (optionally substituted with one or more halogens); C.sub.1-C.sub.6 alkyl-S(O).sub.n; CO.sub.2H (or C.sub.1-C.sub.6 alkyl esters thereof or C.sub.1-C.sub.6 alkyl amides thereof); halogen; C.sub.1-C.sub.6 alkoxy; CN; NO.sub.2; and NR.sub.7R.sub.8; wherein R.sub.7 and R.sub.8, independently, each represent H, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkylcarbonyl, C.sub.1-C.sub.6 alkoxycarbonyl, arylsulphonyl, heteroarylsulphonyl, heterocyclosulphonyl, arylcarbonyl, heteroarylcarbonyl, heterocyclocarbonyl, or C.sub.1-C.sub.6 alkylsulphonyl, or R.sub.7, R.sub.8 and the nitrogen to which they are attached form a 5 or 6 membered heterocyclic ring (such as morpholine or piperidine); and wherein n represents 0-2.

This invention relates to a crosslinking component for binder resins which is especially suitable to be used together with epoxy-group containing binders and/or (poly)isocyanates such as blocked (poly)isocyanates and which comprises at least two blocked isocyanate groups per molecule of the crosslinking component whereby at least one of the at least two blocked isocyanate groups is a group according to structural unit (I), wherein the ratio of structural units of formula (II), if present, to structural units of formula (I) is 0.40 or below. The cross-linking component may also be self-cross-linkable. The present invention further relates to a coating composition, e.g. a one-component coating composition comprising the crosslinking component and a method of its manufacture.

The present disclosure provides compounds that can inhibit the type III secretion system (TTSS) to decrease the pathogenesis of gram-negative bacteria. These compounds may have wide applications for treating bacteria diseases caused by gram-negative bacteria in a host species, including but not limited to, plants and animals. The present invention further relates to compositions that inhibit pathogenesis of gram-negative bacteria without killing the bacteria. Methods relating to preventing and/or treating infection of a host species by bacterial pathogens are also provided herein.

A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to ATR-101) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome.

A method for continuously preparing biuret polyisocyanate, comprising: a mixed solution of a diisocyanate and a catalyst with water vapour, in an aerosol form, are continuously reacted in a first reactor; the product obtained therefrom is brought into a second reactor for a further reaction; a tail gas from the second reactor is condensed and refluxed, and the non-condensable gas is brought into a tail gas treatment system; a reaction liquid obtained in the second reactor is further reacted in a third reactor; and then separation is performed for removing monomers, so as to obtain biuret polyisocyanate.

The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions.