Abstract: The complex crystal of the present disclosure is a complex crystal having a structure in which supramolecular units each composed of two or more types of molecules are arrayed. Each of the supramolecular units contains a cyanoacrylic acid derivative and a trisubstituted methylamine as the molecules. The complex crystal has, between the supramolecular units, molecular cavities in each of which a guest molecule for which the supramolecular unit is a host is not disposed. The complex crystal of the present disclosure can have a property of incorporating a chemical substance therein and can exhibit a great change in a characteristic when incorporating the chemical substance therein.

Abstract: This invention provides REL inhibitors which interfere with the DNA binding capacity of a REL protein. Additionally this invention provides methods of treating, abrogating, or preventing diseases which respond with a positive clinical score to a REL inhibitor. Methods of identifying REL inhibitor based on a REL protein three dimensional model are described.

Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

Abstract: The present invention provides, for example, a compound of the following formula (I): wherein R1 is substituted amino and the like, R2 is halogen and the like, R3 is substituted or unsubstituted lower alkyl and the like, RA and RB are each independently hydrogen, substituted or unsubstituted lower alkyl and the like, RC and RD are each independently hydrogen, substituted or unsubstituted lower alkyl, or RC and RD together with the carbon atom to which they are attached may form a substituted or unsubstituted carbocycle, and ring A is a carbocycle or a heterocycle, its pharmaceutically acceptable salt, or a solvate thereof as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-?proteins.

Abstract: The identification of MreB as essential for bacterial chromosome segregation provides a new target for antibiotic action. The MreB function is useful in the development of screening assays for new antibiotics, which may use, for example, genetic mutants in MreB, tests of MreB mediated chromosome segregation, and the like. In one embodiment of the invention, the antibiotic is an isothiourea compound, which may comprise a polyhalogenated benzyl group, e.g. at the 4 position, the 2,4 position, etc. A pharmaceutical composition comprising an MreB targeted antibiotic as an active agent is administered to a patient suffering from a microbial infection, particularly bacterial infections.

Abstract: Compounds of formula (I) and (II) are provided as modulators of Rb:Raf-1 interactions which are potent, selective disruptors of Rb:Raf-1 binding. Therapeutic methods of using the compounds, for example for treating or ameliorating a cell proliferation disorder such as cancer, are provided.

Abstract: This invention is directed to compounds of formula (I): wherein m, n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.

Abstract: A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitrites or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.

Abstract: The present invention relates to novel N,N,-Substituted S-Aryl-Isothioureas, and N,N,N′-Substituted S-Aryl-Isothioureas and combinatorial libraries thereof, as well as methods of preparing N,N,-Substituted S-Aryl-Isothioureas, and N,N,N′-Substituted S-Aryl-Isothiourea derivative compounds.

Abstract: Compounds represented by the general formula (I): ##STR1## (where R.sub.1 denotes a hydrogen atom, a straight-chained or branched alkoxycarbonyl group having 1-6 carbon atoms in which the alkyl portion may optionally have a substituent, or an optionally substituted straight-chained or branched acyl group having 1-9 carbon atoms;R.sub.2 denotes a hydrogen atom or an optionally substituted straight-chained or branched alkyl group having 1-6 carbon atoms;R.sub.3 denotes an optionally substituted straight-chained or branched alkyl group having 1-6 carbon atoms or an optionally substituted straight-chained or branched alkenyl group having 2-6 carbon atoms;R.sub.4 denotes a hydrogen atom;or alternatively R.sub.3 and R.sub.4 may combine together to form an optionally substituted 5- to 7-membered ring; andn denotes an integer of 2-4, provided that when R.sub.3 is a methyl group, n is not 3 at the same time) or pharmaceutically acceptable salts thereof.

Abstract: The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular cerebral ischemia, and pharmaceutical formulations therefor are disclosed. Novel N-substituted urea derivatives and processes for the preparation thereof are also described.

Abstract: Carbohydrate substituted dibenzo[d,f][1,3,2]dioxaphosphepin compounds of formula I ##STR1## where A is a carbohydrate residue are effective stabilizers for polymers processed at elevated temperatures and subject to thermal or oxidative degradation.

Abstract: Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of disorders.

Abstract: Novel isothiuronium surfactant salts are useful as hair conditioning agents. Aqueous composition containing such salts, and method of using the salts are disclosed.

Abstract: The invention relates to novel substituted aryloxyphenylthioureas, aryloxyphenylisothioureas and aryloxyphenylcarobodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.8 cycloalkyl, unsubstituted or substituted by one or more C.sub.1 -C.sub.3 alkyl groups; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 and R.sub.3 are each C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen, methyl or --CHO,R.sub.5 is halogen; C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted by one or more halogen atoms; C.sub.1 -C.sub.4 alkoxy, unsubstituted or substituted by one or more halogen atoms; or is a --CH.dbd.CH).sub.2, --CH.sub.2).sub.3 or --CH.sub.2).sub.4 bridge in 2,3- or 3,4-position,n is 0, 1, 2, 3 or 4,Z is --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N--; andR.sub.6 is C.sub.1 -C.sub.

Abstract: Formamidine compounds of general formula I ##STR1## in which: R.sub.1 represents H or C.sub.1-4 alkyl,R.sub.2 represents benzoyl, benzyl, or alpha-hydroxybenzyl, the aromatic ring being optionally substituted by a halogen atom,R.sub.3 and R.sub.4, which are identical or different, represent hydrogen, lower-alkyl, or lower-alkenyl, or form between them with the formamidine function a heterocycle,R.sub.5 represents hydrogen or C.sub.1-4 lower-alkyl or forms with R.sub.4 a double bond (--N.dbd.R.sub.4) in the case of pseudoaromatic heterocycles,n equals 0 or 1,A represents a linear or branched C.sub.1-4 alkylene chain,X represents hydrogen, halogen, C.sub.1-4 lower-alkyl, C.sub.1-4 lower-alkoxy, or nitro, and pharmaceutically-acceptable salts thereof, are disclosed.The compounds and pharmaceutical compositions thereof are used, optionally in combination with other active principles, as drugs for the treatment of gastrointestinal ailments, especially as gastric antisecretory and antiulcer agents.

Abstract: The invention relates to novel substituted anilinophenylthioureas, anilinophenylisothioureas and anilinophenylcarbodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.8 cycloalkyl, unsubstituted or substituted by one or more C.sub.1 -C.sub.3 alkyl groups; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 and R.sub.3 are each C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen, methyl or --CHO,R.sub.5 is halogen; C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted by one or more halogen atoms; C.sub.1 -C.sub.4 alkoxy, unsubstituted or substituted by one or more halogen atoms; or is a --CH.dbd.CH--.sub.2, --CH.sub.2--3 or --CH.sub.2--4 bridge in 2,3- or 3,4-position,n is 0, 1, 2, 3 or 4,Z is --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N--; andR.sub.6 is C.sub.1 -C.sub.

Abstract: The invention relates to novel phenoxyphenylthioureas, phenoxyphenylisothioureas and phenoxyphenylcarbodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.6 cycloalkenyl,R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl or C.sub.5 -C.sub.6 cycloalkyenyl,R.sub.3 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.6 cycloalkyl, 1-cyclopropylethyl or C.sub.3 -C.sub.5 alkenyl,R.sub.4 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy or CF.sub.3,n is an integer from 1 to 3,Z is --NH--CS--NH--, --N.dbd.C(SR.sub.5)--NH-- or --N.dbd.C.dbd.N--, andR.sub.5 is C.sub.1 -C.sub.5 alkyl or allyl,and to salts thereof, to the preparation of these compounds and to intermediates for their synthesis. The invention further relates to the use of the novel compounds in pest control and to pesticidal compositions which contain at least one compound of formula I. The preferred utility is the control of pests of animals and plants.

Abstract: The present invention is directed to a process for desulfurizing a compound selected from isothioureas and isothioamides comprising heating the compound to be desulfurized in the presence of a mercaptanol to produce the corresponding desulfurized keto compound.

Abstract: Novel substituted aryloxyphenyl-thioureas, -isothioureas and -carbodiimides of formula I ##STR1## in which R.sub.1 represents C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkyl mono- or poly-substituted by halogen and/or by C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl mono- or poly-substituted by C.sub.1 -C.sub.3 alkyl, or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl;R.sub.2 represents hydroben or C.sub.1 -C.sub.5 alkyl;R.sub.3 represents a C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl;R.sub.4 represents hydrogen or methyl;R.sub.5 represents a --CH.dbd.CH--.sub.2, --CH.sub.2 --.sub.3 or --CH.sub.2 --.sub.4 bridge in the 2,3- or 3,4-position;Z represents --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N-- andR.sub.6 represents C.sub.1 -C.sub.

Abstract: S-trifluorobutenyl thiocarbonic acid esters of the formula ##STR1## and salts thereof, wherein X is R.sup.1 N or S and Y is RS or R.sup.3 R.sup.2 N;wherein R is a metal or a radical selected from alkyl, cycloalkylalkyl, halocycloalkylalkyl, alkenyl, haloalkyl, haloalkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonylalkyl, halophenoxyalkyl, trialkylsilylalkyl, (vinyl)dialkylsilylalkyl, (allyl)dialkylsilylalkyl, 2-chlorothiophene-5-ylmethyl, phenylalkyl, halophenylalkyl, nitrophenylalkyl, haloalkylphenylalkyl, dialkyl-2,3-dihydrobenzofuran-7-yl, [2-methyl-(1,1'-biphenyl)-3-yl]methyl, 3-phenoxybenzyl, phenylthioalkyl, halophenylthioalkyl, dialkylphosphoryl, dialkylthiophosphoryl, dialkylisoxazolylalkyl and thienylisoxazolylalkyl;wherein R.sup.1 is alkyl, cycloalkyl, cyano, dialkyl-2,3-dihydrobenzofuran-7-yl, halophenyl, halophenylalkyl, haloalkoxyphenyl, pyridinyl, halopyridinyl, alkyl-1,3,4-thiadiazolyl, haloalkyl-1,3,4-thiadiazolyl, benzothiazolyl, dialkyloxazolyl or thiazolinyl;wherein R.sup.

Abstract: The invention relates to a process for the preparation of compounds of the formula I and salts or acid addition compounds thereof ##STR1## in which R denotes hydrogen, (halogenated) alkyl with the exception of CF.sub.3, a (substituted) aromatic radical, (substituted) heteroaryl, (substituted) phenoxy, (substituted) phenylthio, (substituted) phenylamino, halogen, hydroxyl, alkoxy, mercapto, (halogenated) cycloalkyl, alkylmercapto, amino, monoalkylamino or dialkylamino,R.sup.1 denotes (substituted alkyl, (substituted) phenyl or naphthyl, alkenyl, alkinyl, cycloalkyl, (substituted) benzyl or heteroaryl, and X denotes oxygen or sulfur, which comprises reacting a nitrile of the formula II with a compound of the formula IIIR--C.tbd.N (II)R.sup.

Abstract: According to the present invention there are provided isothiuronium salts of the general Formula I ##STR1## wherein R.sup.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, aralkyl or aryl, the said groups being optionally substituted by one or more hydroxy, mercapto and/or halogen;R.sup.2 stands for hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.3-6 cycloalkyl;X represents an organic or inorganic anion/.The compounds and salts of the present invention can be prepared by reacting a compound of the general Formula II ##STR2## with an agent capable of introducing a R.sup.1 group. The compounds of the general Formula I exhibit antitumor and immunostimulant effect and are useful in therapy.

Abstract: This invention relates to novel cyanoguanidine compounds and the intermediate N'-cyano-N-(1,2,3,4-tetrahydro-1-naphthyl)-S-methylisothiourea. These novel compounds are useful as animal growth promoting agents.

Abstract: This invention relates to novel cyanoguanidine compounds and the intermediate N'-cyano-N-(1,2,3,4-tetrahydro-1-naphthyl)-S-methylisothiourea. These novel compounds are useful as animal growth promoting agents.

Abstract: S-(Aminoalkyl)isothioureas which have immunosuppressant activity. Two specific compounds are 2-(3-dimethylaminopropylthio)-2-imidazoline and N,N'-dimethyl-S-(3-dimethylaminopropyl)isothiourea.

Abstract: A process for the preparation of a sulphonyliso(thio)urea of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical from the group consisting of alkyl, aralkyl, aryl and heteroaryl,R.sup.2 represents an optionally substituted and/or optionally fused, six-membered aromatic heterocycle containing at least one nitrogen atom,R.sup.3 represents an optionally substituted radical from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl and aralkyl, andQ represents oxygen or sulphur,comprising reacting a sulphonylguanidine of the formula ##STR2## in which R.sup.4 represents an optionally substituted hydrocarbon radical,with a compound of the formulaH--Q--R.sup.3at a temperature between 0.degree. C. and 150.degree. C. The products are known herbicides.

Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.2 R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.