Abstract: A cyclohexane derivative as shown by formula IB or a stereoisomer or a salt thereof, has a high affinity for D3 receptors and 5-hydroxytryptamine, has a lower affinity for D2 receptors, shows a high selectivity for D3/D2 receptors, and can be used as a therapeutic drug against neuropsychiatric diseases. wherein; X is N or CH; R is R is optionally substituted with one or more substituents selected from the group consisting of F, Cl, Br, I and C1-C6 alkyl; and the C1-C6 alkyl is optionally substituted with one or more substituents selected from the group consisting of F, Cl, Br, and I.

Abstract: The present disclosure relates to a method for preparing a disubstituted urea and carbamate compounds simultaneously through a one-pot reaction of an amine, carbon dioxide and an alkylene oxide compound in the presence of an ionic liquid-based complex catalyst system containing indium. In accordance with the present disclosure, a disubstituted urea and carbamate compounds can be prepared simultaneously at high yield. In addition, the ionic liquid-based catalyst containing indium according to the present disclosure is economical because it can be reused several times.

Abstract: The disclosure provides curable inks including a bis-urea gelator having the structure of Formula I. wherein R and R? each, independently of the other, is a saturated aliphatic hydrocarbon group selected from the group consisting of (1) linear aliphatic groups, (2) branched aliphatic groups, (3) cyclic aliphatic groups, (4) aliphatic groups containing both cyclic and acyclic portions, any carbon atom of the saturated aliphatic hydrocarbon group may be optionally substituted with an alkyl group (cyclic or acyclic), wherein (1) and (2) groups have a carbon number of from about 1 to about 22 carbons, and wherein (3) and (4) groups have a carbon number of from about 4 to about 10 carbons; and X is selected from the group consisting of: (i) an alkylene group, (ii) an arylene group, (iii) an arylalkylene group, and (iv) an alkylarylene group.

Abstract: The present invention is directed towards an electrocoating composition comprising a cyclic guanidine.

Abstract: Melanocortin receptor modulators, processes for preparing them and use thereof in human medicine and cosmetics are described. Melanocortin receptor modulators corresponding to formula (I): compositions containing them, processes for their preparation and their use in pharmaceutical or cosmetic compositions are also described.

Abstract: The disclosure provides curable inks including a bis-urea gelator having the structure of Formula I. wherein R and R? each, independently of the other, is a saturated aliphatic hydrocarbon group selected from the group consisting of (1) linear aliphatic groups, (2) branched aliphatic groups, (3) cyclic aliphatic groups, (4) aliphatic groups containing both cyclic and acyclic portions, any carbon atom of the saturated aliphatic hydrocarbon group may be optionally substituted with an alkyl group (cyclic or acyclic), wherein (1) and (2) groups have a carbon number of from about 1 to about 22 carbons, and wherein (3) and (4) groups have a carbon number of from about 4 to about 10 carbons; and X is selected from the group consisting of: (i) an alkylene group, (ii) an arylene group, (iii) an arylalkylene group, and (iv) an alkylarylene group.

Abstract: The present invention relates to a polymer composition comprising at least one polyamide and at least one urea compound of the formula I where x is 1, 2 or 3; R1 and R2 are selected from hydrogen, linear C1-C7-alkyl, branched C3-C10-alkyl, unsubstituted or substituted C3-C12-cycloalkyl, unsubstituted or substituted C3-C12-cycloalkyl-C1-C4-alkyl, unsubstituted or substituted aryl and unsubstituted or substituted aryl-C1-C4-alkyl; and Z is selected from C3-C10-alkanediyl, unsubstituted or substituted arylene, unsubstituted or substituted aryl unsubstituted or substituted ene-C1-C4-alkylene-arylene, unsubstituted or substituted heteroarylene, unsubstituted or substituted heteroarylene-C1-C4-alkylene-heteroarylene, unsubstituted or substituted C5-C8-cycloalkylene, C5-C8-cycloalkylene-C1-C4-alkylene-C5-C8-cycloalkylene, unsubstituted or substituted heterocycloalkylene and heterocycloalkylene-C1-C4-alkylene-heterocycloalkylene.

Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.

Abstract: The present invention provides arachidonic acid (AA) analogs and compositions containing those analogs as active agents for use in analgesic treatments. Various methods of manufacturing the inventive compounds are provided and pharmaceutical formulations, including injectable and oral dosages, are described. Certain analogs are additionally useful as antipyretic compositions and in related fever reducing treatments.

Abstract: Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.

Abstract: Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.

Abstract: Dendritic or hyperbranched polyurethanes are prepared by 1) reacting diols or polyols having at least one tertiary nitrogen atom and at least two hydroxyl groups of differing reactivity toward isocyanate groups with diisocyanates or polyisocyanates to form an addition product, with the diols or polyols and diisocyanates or polyisocyanates being selected so that the addition product has, on average, one isocyanate group and more than one hydroxyl group or one hydroxyl group and more than one isocyanate group, 2) converting the addition product from step 1) into a polyaddition product by intermolecular reaction of the hydroxyl groups with the isocyanate groups, and with a reaction with a compound containing at least two hydroxyl groups, mercapto groups, amino groups or isocyanate groups also being able to be carried out first, 3) if desired reacting the polyaddition product from step 2) with a compound containing at least two hydroxyl groups, mercapto groups, amino groups or isocyanate groups.

Abstract: Treating pain in mammals with a compound having the formula (I) is disclosed herein.

Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.

Abstract: This invention is directed to functionalized higher diamondoids having at least one functional group. Preferably these derivatives have the following Formula I: wherein D is a higher diamondoid nucleus and wherein R1, R2, R3, R4, R5 and R6 are independently selected from a group consisting of hydrogen and functional groups, provided that there is at least one functional group on the derivative. The functionalized higher diamondoid compounds may also be of the formula D—L—(D)n wherein D is a higher diamondoid nucleus and L is a linking group and n is 1 or more. The functionalized higher diamondoid compounds additionally may be of the formula R38—D—D—R39 wherein D is a higher diamondoid nucleus and R38 and R39 are substituents.

Abstract: A rapid screening method for identifying acylfulvenes and acylfulvene analogs with improved chemotherapeutic properties has been developed. The mechanism of toxicity of irofulven, a potentially clinically useful member of the acylfulvene class, has been elucidated and provides guidance for design and testing of a new class of alkylating agents with structures related to irofulven. The role of alkenal/one oxidoreductase (AOR) is shown to be important in cancer cell susceptibility to this class of alkylating agent.

Abstract: Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.

Abstract: The present invention relates to aniline derivatives of the general formula I or salts thereof, described therein, and their use.

Abstract: The present patent application is directed to novel fluoroethyl urea compounds and compositions and their therapeutic use in the treatment of pain and other conditions.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein Ar, X, m, R1, R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of 5-HT6-mediated diseases.

Abstract: The invention is directed to a process for the production of certain phosphorous, namely urea, thio-urea and sulphonamide phosphorous compounds. The present invention provides a process for the production of phosphorous compounds which process allows an easy and effective separation of the reaction products from impurities by applying a solid alkaline ion-exchange resin.

Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.

Abstract: The present invention relates to novel compounds, pharmaceutical compositions comprising the same, use of said compounds for the manufacture of a medicament for treatment of pain and disorders related thereto as well as a method for treatment of pain and disorders related thereto, wherein said compounds are administered. The compounds are represented by the general formula (I), as further defined in the specification.

Abstract: Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.

Abstract: High-functionality polyisocyanates are prepared by a process which comprises (i) preparation of an addition product (A) which contains one group which is reactive toward isocyanate and at least two isocyanate groups by reacting (a) a diisocyanate or polyisocyanate I with (b1) compounds having at least three groups which are reactive toward isocyanate or (b2) compounds containing two groups which are reactive toward isocyanate or mixtures of (b1) and (b2), where at least one of the components (a) or (b) has functional groups having differing reactivities toward the functional groups of the other component and the reaction ratio is selected so that the addition product (A) contains an average of one group which is reactive toward isocyanate, (ii) if desired, intermolecular addition reaction of the addition product (A) to form a polyaddition product (P) containing an average of one group which is reactive toward isocyanate and an average of more than two isocyanate groups, and (iii) reaction of the addition

Abstract: The invention relates to new 2,2,3,3-tetramethylcyclopropane carboxamide derivative compounds, pharmaceutical compositions thereof and uses thereof for treating psychotic disorders, neurodegenerative diseases, epilepsy and pain.

Abstract: Blocked polyisocyanates and one-component stoving systems containing these blocked polyisocyanates, and the preparation thereof and their use for the preparation of lacquers, paints, adhesives and elastomers, wherein blocked polyisocyanates are prepared by reacting polyisocyanates with secondary amines corresponding to the formula wherein R1—R4 can be identical or different and denote hydrogen, C1–C6-alkyl or cycloalkyl, R5 denotes C1–C10-alkyl, C3–C10-cycloalkyl, y denotes a number from 2 to 8, and B represents wherein R6–R8 can be identical or different and independently of one another denote C1–6-alkyl and/or C3–C6-cycloalkyl, R9 denotes hydrogen or C1–6-alkyl or C3–C6-cycloalkyl.

Abstract: The invention relates to a process for the preparation of tetrasubstituted ureas by reaction of the corresponding amines with phosgene in the presence of an aqueous inorganic base at a temperature in the range from 0 to 150° C., which comprises: feeding the corresponding amine, the phosgene and the aqueous inorganic base on average continuously to the reaction apparatus, forming a two-phase system in the reaction apparatus through the choice of the tetrasubstituted ureas to be prepared, through the mixing ratios of the substances and substance mixtures to be fed in, through the temperature during the reaction and, where appropriate, through the feed of an organic solvent which is not completely miscible with water, and discharging the reaction mixture on average continuously from the reaction apparatus.

Abstract: A process for preparing a cyclic compound comprising subjecting a starting material in the presence of a catalyst component to metathesis reaction in the presence of an ionic liquid, wherein the starting material is a &agr;,&ohgr;-diene bearing a &agr; substituent NRR1 in the &agr; position to a double bond, wherein R is hydrogen or an organic substituent, R1 is tert-butyl, P(R)2, P(R2)2, COR, SO2PhR, COOR or CONRR2, R2is alkyl or phenyl, or R and R1 together form and in which &agr;,&ohgr;-dienes optionally bear at least one further substituent R in any other position with the exception of the &agr; position, wherein R is selected from the group consisting of hydrogen, fused or unfused aryl, alkyl, CN, COOR2 or halogen, and wherein the starting material optionally contains a member selected from the group containing at least one further substituent that is inert in the metathesis reaction and a heteroatom selected from the group consisting of branched alkyl radicals, unbranched alkyl radical

Abstract: The present invention relates to the preparation of alkyl-ureas, starting from O,S-dimethyl dithiocarbonate, which provides the following steps: A) causing the O,S-dimethyl dithiocarbonate to react with a primary amine of general formula R1NH2 in order to obtain an O-methyl thiocarbamate; B) isomerising the O-methyl thiocarbamate in order to obtain an S-methyl thiocarbamate; C) causing the S-methyl thiocarbamate with a compound of general formula R′R″NH, wherein R′ and R″ may be equal or different one in respect of the other and of R1 and may be H, R2 or R3, in order to obtain one of the alkyl-ureas of formula (4), (5) or (6).

Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.

Abstract: The present application describes modulators of CCR3 of formula (I): 1

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: This invention is directed to functionalized higher diamondoids having at least one functional group.

Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example are valuable ligands for metal complexes of the d-8 metals of the periodic table of elements. The metal complexes in question are catalysts or catalyst precursors for the asymmetric hydrogenation or asymmetric transfer hydrogenation with hydrogen donors of prochiral organic compounds with carbon double bonds or carbon/hetero atom double bonds, for example ketones and imines.

Abstract: Derivatives of N-deacetyl-thiocolchicine or of the isoster thereof of formula (I) wherein n is an integer from 0 to 8, Y is a CH2 group or, when n is 1, can also be a group of formula NH. Compounds of formula (I) have anti-proliferative activity.

Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.

Abstract: Resins and waxes made by reacting selected nucleophiles, including alcohols and/or amines, with an isocyanate are disclosed. The order of addition of the isocyanate and the different nucleophiles can tailor the distribution of di-urethane, mixed urethane/urea, and/or di-urea molecules in the final resin product. The isocyanate-derived resin and wax materials are useful as ingredients as phase change ink carrier compositions used to make phase change ink jet inks.

Abstract: The present invention relates to blocked polyisocyanate cross-linking agents and their use in one-component stoving lacquers, in particular in solvent-containing or predominantly water-based plastics coatings having a soft-feel effect.

Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts for the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.

Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.

Abstract: Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects.

Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: Aliphatic tetraketimine of the present invention are a novel class of compounds represented by the formula: wherein Et is ethyl, Me is methyl, and R is a residue of an aliphatic diisocyanate. The tetraketimine is made by condensing a novel ketimine with a diisocyanate. The ketimine has a free secondary amine after a polyamine selected from the group consisting of: H2N—C2H4—NH—C2H4—NH2, H2N—C2H4—NH—C2H4—NH—C2H4—NH2, H2N—(CH2)6—NH—(CH2)6—NH2, or tris(2-aminoethyl)amine is reacted with a ketone.

Abstract: This invention relates to novel spiro compound derivatives of benzoisothiazolyl-urea and -thiourea and compositions thereof. These compounds are useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.

Abstract: The use of water-soluble quinacridones of the formula I ##STR1## where M.sup..sym. is a lithium, sodium, potassium or ammonium cation,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently are hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, sulfamoyl, mono- or di-(C.sub.1 -C.sub.4)-alkylsulfamoyl, carbamoyl, mono- or di-(C.sub.1 -C.sub.4)-alkylcarbamoyl, unsubstituted or substituted mono- or diphenylsulfamoyl, unsubstituted or substituted mono- or diphenylcarbamoyl, halogen, nitro or cyano,n is 0, 1 or 2 andm is 0, 1 or 2 and the sum n+m is at least 1,for dyeing and printing natural and synthetic fiber material.

Abstract: Describes a method of producing N-1-alkenyl carbonylamino compounds represented by the following general formula I, ##STR1## wherein R.sub.1 is the residue of an active hydrogen functional material, n is a number from 1 to a number equal to the number of active hydrogen groups of said active hydrogen functional material, X is selected from O, S and N(R.sub.5), R.sub.5 being hydrogen, hydrocarbyl, or R.sub.5 and R.sub.1 may together form a cyclic ring, R.sub.2, R.sub.3 and R.sub.4 are each independently selected from hydrogen, C.sub.1 -C.sub.4 alkyl and C.sub.2 -C.sub.4 alkenyl.