Abstract: Carmustine may be safely and efficiently produced by reacting 2-chloroethylamine hydrochloride and 1,1?-carbonyldiimidazole to afford 1,3-bis(2-chloroethyl)-1-urea, followed by nitrosation to give the final product.

Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.

Abstract: Disclosed is an industrially advantageous process for producing O-methyl-N-nitroisourea. Disclosed is a process for obtaining O-methyl-N-nitroisourea represented by the following chemical formula (1) or a salt thereof in a high yield by performing the nitration of O-methylisourea represented by the following chemical formula (2) or a salt thereof with nitrating agents in the presence of fuming sulfuric acid.

Abstract: Disclosed is an improved process for producing nitroisourea derivatives which is necessary for producing nitroguanidine derivatives having an insecticidal activity.

Abstract: Disclosed is an industrially advantageous process for producing O-methyl-N-nitroisourea. Disclosed is a process for obtaining O-methyl-N-nitroisourea represented by the following chemical formula (1) or a salt thereof in a high yield by performing the nitration of O-methylisourea represented by the following chemical formula (2) or a salt thereof with nitrating agents in the presence of fuming sulfuric acid.

Abstract: The present invention relates to the compound N-4-nitrophenyl-N?-4?-nitrophenylurea as a urease and ?-chymotrypsin (anti HCV) enzyme inhibitory drug named “Urchym”. N-4-nitrophenyl-N?-4?-nitrophenylurea is prepared and screened for their urease and ?-chymotrypsin inhibition effects, the said compound, showed strong urease inhibition (IC50=1.25 ?M). We found, that the same compound is also an efficient ?-chymotrypsin inhibitor having an IC50 value of 3.15 ?M.

Abstract: The present invention is directed to blocked biuret group-containing polyisocyanate compositions, wherein the blocking agent is of the formula: wherein R1, R2, R3 and R4 may be the same or different and represent a moiety selected from the group consisting of hydrogen, C1-C6-alkyl and C3-C6-cycloalkyl, R5 represents a moiety selected from the group consisting of C1-C10-alkyl and C3-C10-cycloalkyl, and B is a group according to one of the following structural formulas wherein each occurrence of R6, R7, and R8 may be the same or different and represent a moiety selected from the group consisting of C1-C6-alkyl and C3-C6-cycloalkyl and R9 is a moiety selected from the group consisting of hydrogen, C1-C6-alkyl and C3-C6-cycloalkyl.

Abstract: A process for the preparation of a nitrosourea derivative, in particular 1,2-bis(2-chloroethyl)-1-nitrosourea, comprises reacting a non-nitrosated urea derivative with a metal nitrite in a two-phase solvent system comprising an aqueous acid and a non-miscible organic solvent.

Abstract: Compounds having the general formula (I), ##STR1## wherein X and Y represent individually H or --NO, at least one of them being a group-NO, n is 0, 1 or 2, R represents hydrogen, an aliphatic, cycloaliphatic, cycloaliphatic-alkyl, aryl or aralkyl radical, or a group of formula, ##STR2## wherein R.sub.1 is a lower alkyl radical or an aryl, all these radicals being optionally substituted. The present invention also relates to the compounds hereabove defined in the form of mixtures of their position isomers. Furthermore, the present invention discloses processes for preparing such compounds, as well as compositions, useful particularly in anticancerous chemotherapy, containing at least one of said compounds as an active principle.

Abstract: The invention concerns N-nitroso compounds having the general formula: ##STR1## wherein A is lower alkyl or halolower alkyl;B is hydrogen; lower alkenyl; lower alkynyl; 3-6 C cycloalkyl; --RSO.sub.2 NR.sup.3 R.sup.4, or lower alkyl optionally monosubstituted with lower alkoxy, or 3-6 C cycloalkyl;R is straight or branched 2-5 C alkylene, optionally monosubstituted with SO.sub.2 NR.sup.3 R.sup.4 or CONR.sup.3 R.sup.4, said alkylene always containing at least two carbon atoms separating the nitrogen atom of the urea from any SO.sub.2 NR.sup.1 R.sup.2 or SO.sub.2 NR.sup.3 R.sup.4 ;R.sup.1 and R.sup.2 are the same or different and selected from hydrogen, 5-6 C cycloalkyl, lower alkoxy, phenyl, benzyl, and straight or branched 1-6 C alkyl, optionally monosubstituted with hydroxy, lower alkoxy, SO.sub.2 NR.sup.3 R.sup.4, or CONR.sup.3 R.sup.4 ; R.sup.1 and R.sup.2 may also together form a 4-5 C alkylene; and R.sup.3 and R.sup.4 are the same or different and selected from hydrogen or lower alkyl, or R.sup.3 and R.

Abstract: Cystamine derivatives of the formula: ##STR1## [wherein n represents 2 or 3, R.sup.1 and R.sup.2 each represents a hydrogen atom, or an alkyl group optionally substituted by a hydroxy, amino, alkylamino or dialkylamino group, or represents a cycloalkyl or aryl group, and X.sup.1 represents a group selected from the formulae .dbd.N--CN, .dbd.N--NO.sub.2, .dbd.N--COR.sup.3, .dbd.N--COOR.sup.3, .dbd.N--NH--CONH.sub.2, .dbd.N--SO.sub.2 R.sup.3, .dbd.CH--NO.sub.2, .dbd.CH--SO.sub.2 R.sup.3, .dbd.C(CN).sub.2, .dbd.C(CN)COOR.sup.3 and .dbd.C(CN)CONH.sub.2 (wherein R.sup.3 represents an alkyl or aryl group), or R.sup.1 represents a hydrogen atom, R.sup.2 represents an alkyl group optionally substituted by a hydroxy, amino, alkylamino or dialkylamino group, or represents a cycloalkyl or aryl group and X.sup.1 represents an oxygen or sulphur atom] have been found to be useful in the promotion of the growth of non-human animals including birds.

Abstract: The invention is an improved process for the production of methylnitramine y nitrating dimethylurea with a mixture of sulfuric acid and nitric acid with subsequent separation of 1,3-dimethyl-1,3-dinitrourea by the use of a suitable solvent with recovery of a dimethyl dinitrourea in organic solvent, with hydrolysis of the dimethyldinitrourea with hot water to yield methylnitramine.

Abstract: A process for preparing 2,4-dinitro-2,4-diazapentane by(1) nitrating dimethylurea to form dimethyldinitrourea;(2) hydrolyzing the dimethyldinitrourea to form methylnitramine;(3) reacting one mole of methylamine with one mole of formaldehyde in aqus solution to form 2-nitro-2-aza-1-propanol; and(4) reaction one mole of methylnitramine with each mole of 2-nitro-2-aza-1-propanol to form one mole of 2,4-dinitro-2,4-diazapentane.

Abstract: Nitrosourea derivatives are provided which possess a high level of inhibitory activity against leukemia and tumors and which are therefore useful for pharmaceutical purposes. The compounds have the structure represented by formulae (I), (II) and (III): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.4 may be the same or different and each represent a hydrogen atom or an alkyl, aryl, aralkyl, alkanoyl or a heterocyclic group; R.sup.3 represents the residual group on the .alpha.-carbon atom of an .alpha.-amino acid; n represents 2 or 3; X represents a halogen atom selected from chlorine, fluorine and bromine; and Ac represents an alkanoyl group.

Abstract: The invention relates to new chemical compounds.The compounds according to the invention are compounds of the following formula ##STR1## in which one of the substituents A and B is hydrogen and the other is the radical -N.dbd.O.These compounds are suitable for use as medicaments.

Abstract: 1-Branched-alkyl-3-(2-haloethyl)-3-nitrosoureas which exhibit antitumor activity. Pharamaceutical compositions containing these novel compounds and methods of using them are also disclosed.

Abstract: A process for preparing 2,4-dinitro-2,4-diazapentane by(1) nitrating dimethylurea to form dimethyldinitrourea;(2) hydrolyzing the dimethyldinitrourea to form methylnitramine;(3) reacting one mole of methylamine with one mole of formaldehyde in aqus solution to form 2-nitro-2-aza-1-propanol; and(4) reaction one mole of methylnitramine with each mole of 2-nitro-2-aza-1-propanol to form one mole of 2,4-dinitro-2,4-diazapentane.

Abstract: This invention relates to compounds having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are selected from the group consisting of hydrogen, acyl, trifluoroacetyl, straight chained and branched alkyl groups with up to 6 carbon atoms, such alkyl groups with up to 3 substituents selected from the group consisting of OH, OSO.sub.2 CH.sub.3, COOH, COOR, CONH.sub.2 and Hal, where R is an alkyl group with up to 6 carbon atoms, and R.sub.1 and R.sub.2 together form a heterocyclic ring containing 4 to 6 carbon atoms and optionally further heteroatoms and such rings with up to 3 substituents selected from the group consisting of lower alkyl, OH, COOH, COOR, CONH.sub.2, where R has the above meaning, the chloroethyl nitrosoureido group and Hal, and Hal is selected from the group consisting of chlorine and fluorine, which heterocyclic ring is not the para-methyl piperazine group, said nitroso ureas having a tumor inhibiting effect.

Abstract: The present invention relates to novel aminoalkyl substituted nitrosourea derivatives as well as their acid addition salts with pharmaceutically acceptable acids showing pronounced antineoplastic effectiveness in animal experiments.The novel compounds of the present invention may be represented by the following formula: ##STR1## wherein X and Y are the same or different, and are selected from the group consisting of a phenyl group and a cyclohexyl group, said phenyl and cyclohexyl groups being optionally substituted with one or two substituents selected from a halogen atom, a lower alkyl group having from one to four carbon atoms inclusive, a trifluore methyl group, a cyano group, a phenyl group, a cyclohexyl group and a lower alkyloxy group having from one to four carbon atoms inclusive."Alkylene" is an alkylene group, branched or unbranched, having from one to four carbon atoms inclusive, and R.sup.1 and R.sup.

Abstract: The specification describes a nitrosourea derivative having the general formula: Cl--(CH.sub.2).sub.2 --N(NO)CO--NHR, wherein --NHR represents a 2-(1,3,4-thiadiazolyl)amino group, an amino residue of a neutral .alpha.-amino acid, or an amino residue of a neutral .alpha.-amino acid whose carboxyl group is amidated with 2-(1,3,4-thiadiazolyl)amine, or a pharmaceutically acceptable acid addition salt thereof. The above nitrosourea derivative and its salt are useful as antitumor drugs. The above nitrosourea derivative may be prepared either by nitrosating a urea derivative of the general formula: Cl--(CH.sub.2).sub.2 NHCONHR or by reacting N-(2-chloroethyl)-N-nitrosocarbamic acid or a reactive derivative thereof with an amino compound of the general formula: R--NH.sub.2.

Abstract: The invention relates to new chemical compounds.The compounds according to the invention are compounds of the following formula ##STR1## in which one of the substituents A and B is hydrogen and the other is the radical --N.dbd.O.These compounds are suitable for use as medicaments.