Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing multiple sclerosis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of neurodegenerative diseases and other neuro-inflammatory diseases.

Abstract: Chemical compositions, lubricant compositions, and methods of using the same are provided. The lubricant composition may comprise at least on carrier. In certain methods, the lubricant composition may be provided to at least one surface, wherein the lubricant composition reduces a coefficient of friction of the at least one surface. In certain methods, the lubricant composition may be provided to at least one surface, wherein the lubricant composition reduces wear of the at least one surface.

Abstract: The invention relates to a multistage process for the continuous preparation of organic, distillable polyisocyanates, preferably diisocyanates, particularly preferably aliphatic or cycloaliphatic diisocyanates, by reaction of the corresponding organic polyamines with carbonic acid derivatives and alcohols to form low molecular weight monomeric polyurethanes and thermal dissociation of the latter, in which the polyisocyanates produced and unusable residues are separated off at particular stages of the reaction and reusable by-products and intermediates are recirculated to preceding stages.

Abstract: The present invention relates to carbamoylation of amines, mercaptanes, thiophenols and phenols employing organic azides. More specifically, the invention relates to a method for generating urea derivatives, thiocarbamate derivatives and carbamate derivatives, and is based on the intermediate formation of isocyanate, starting from an organic azide. The reaction as described is useful in applications for modified nucleoside synthesis, oligonucleotide synthesis, as well as modification, labeling and conjugation of polymers and biomolecules.

Abstract: The present invention provides compound(s) selected from the group of compounds represented by structural Formula (I): wherein X, Y and R1 are as described herein, use of such compounds as anaerobic cure accelerators, and compostions including such compounds.

Abstract: This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain.

Abstract: Stable NCO prepolymers are produced from polyisocyanates having a melting point greater than 70° C., preferably, naphthalene diisocyanate, having advantageous physical properties. An important feature of the process of the present invention is the rapid cooling of the prepolymer. The process of the present invention may be carried out on a continuous or batch basis. The prepolymers of the present invention are particularly suitable for the production of cast polyurethane elastomers.

Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.

Abstract: The present invention provides methods of forming carbamates, ureas, and isocyanates. In certain embodiments these methods include the step of reacting an amine with an ester-substituted diaryl carbonate to form an activated carbamate which can be further derivitized to form non-activated carbamate or a urea. The urea or carbamate can be subjected to a pyrolysis reaction to form isocyanate.

Abstract: A process for the preparation of aminoalkyl phenyl carbamate compounds of Formula I, wherein R1 and R2 independently are hydrogen or a C1-6 alkyl; R3 and R4 are the same or different and each is a C1-6 alkyl; or R3 and R4 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; R5 and R6 independently are hydrogen, linear, branched or cyclic C1-6 alkyl; or R5 and R6 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; the carbon centre designated “*” can be racemic or enantiomerically enriched in the (R)- or (S)- configuration; and pharmaceutically acceptable acid addition salts thereof.

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.

Abstract: The present invention relates to an improved process for preparation of Rivastigmine of formula (I) or pharmaceutically acceptable salts thereof comprising a step of N-methylation of compound of formula (III), wherein R1=R2=H or R1=H and R2=CH3 or an acid addition salt thereof, using paraformaldehyde in the presence of Raney Nickel and hydrogen in a suitable solvent to obtain compound of formula (II).

Abstract: R-enantiomer of Bambuterol, its preparation and therapeutic uses are disclosed. A composition includes R-Bambuterol or its therapeutically acceptable salt. A composition of R-Bambuterol includes at least 80% by weight of the R-enantiomer and not more than 20% by weight of the S-enantiomer based on a total weight of the Bmbuterol. A process includes: (a) asymmetrically reducing a suitably substituted and suitably protected bromoacetophenone compound to a chiral phenyl-bromoethanol comprising a primary bromo group and a secondary hydroxyl group; (b) displacing the bromo group by a suitably substituted and optionally protected primary amine to produce a protected chiral phenylethanolamine, and (c) removing the protecting groups to convert the protected chiral phenylethanolamine to a chiral phenylethanolamine.

Abstract: The present invention relates to an improved process for preparation of Rivastigmine of formula (I) or pharmaceutically acceptable salts thereof comprising a step of N-methylation of compound of formula (III), wherein R1=R2=H or R1=H and R2=CH3 or an acid addition salt thereof, using paraformaldehyde in the presence of Raney Nickel and hydrogen in a suitable solvent to obtain compound of formula (II).

Abstract: A compound having formula (I) and a process for the preparation thereof are described.

Abstract: The invention is concerned with novel hexafluoroisopropanol substituted cyclohexane derivatives of formula (I) wherein R1 to R4, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Abstract: Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. Esters of alkylcarbamic acids are disclosed that are inhibitors of FAAH activity. Compounds disclosed herein inhibit FAAH activity. Described herein are processes for the preparation of esters of alkylcarbamic acid compounds, compositions that include them, and methods of use thereof.

Abstract: Enzymatic preparation of (meth)acrylic esters containing urethane groups, and their use in radiation-curable compositions.

Abstract: Herein are disclosed a process for increasing in purity, or purifying, an N-protected-?-aminoalcohol which process comprises (i) adding water to a polar organic solvent in which an N-protected-?-aminoalcohol such as a (2R,3S)- or (2S,3R)-3-tert-butoxycarbonylamino-1-halo-2-hydroxy-4-phenylbutane or the like, or (ii) crystallizing such an N-protected-?-aminoalcohol from a diol or a diol-based mixed solvent, and a process for producing the corresponding N-protected-?-aminoepoxide which process comprises treating, with a base, the thus purity-enhanced N-protected-?-aminoalcohol. Such N-protected-?-aminoalcohols and N-protected-?-aminoepoxides are both useful as synthetic intermediates for medicine compounds, such as, e.g., HIV protease inhibitor and the like.

Abstract: This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-[4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl]-L-glutamic acid: wherein: X2 is a halo group, and is —F, —Cl, —Br, or —I; n is an integer from 0 to 4; and, each RA is an aryl substituent. The methods comprise, at least, the steps of: glutamate conjugation (GC); silyloxy deprotection (SD); and, sulfonic esterification (SU). Certain preferred methods comprise the steps of: amine substitution (AS); silyloxy protection (SP); phenolic deprotection (PD); activation (AC); glutamate conjugation (GC); silyloxy deprotection (SD); sulfonic esterification (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).

Abstract: A method for preparing S-alkyl and S-aryl thiocarbamates comprising reacting a precursor thiol reagent with trichloroacetyl chloride to produce an S-alkyl and S-aryl trichloroacetyl thioester intermediate, which is reacted with an amine to yield the corresponding thiocarbamate product. Also disclosed is the method for preparing S-alkyl and S-aryl thiocarbamates comprising reacting an amine with trichloroacetyl chloride to produce a trichloroacetamide intermediate, which is then reacted with the precursor thiol to yield the corresponding thiocarbamate product.

Abstract: A novel method for synthesizing functional PNA having superior cost performance and which enables functional molecules to be-introduced extremely rapidly, and compounds used therein. Disclosed is a method for producing a functional PNA oligomer; wherein a PNA monomer unit having adenine, guanine, cytosine or thymine protected by a protecting group is reacted with. Fmoc-&ohgr;-amino acid-BocPNA-OH, and after synthesizing PNA oligomer, a functional molecule having free carboxylic acid is introduced into that PNA oligomer followed by deprotecting the protecting group; compounds synthesized by the method; and, Fmoc-&ohgr;-amino acid-BocPNA-OH that functions as a precursor PNA monomer unit.

Abstract: Novel addition products of isocyanates with oxyalkylene-substituted aminophenol compounds as intermediates for the production of urethane-substituted xanthene colorants, particularly triphenylmethane derivatives such as rhodamines, are provided. The xanthene colorants exhibit improved wax and/or oil solubility and high purity. The urethane-substituted xanthene colorant features very good wax and/or oil solubility, and is believed to be relatively nontoxic. A method for producing this novel colorant is also provided.

Abstract: Phenylurethane compounds of the following general formula (1); asymmetric urea compounds of the following general formula (10) obtained from the phenylurethane compounds; barbituric acid derivatives of general formula (18) produced from the asymmetric urea compounds, which have specific substituents and are useful in diazo thermal recording materials; and diazo thermal recording materials containing the barbituric acid derivative.

Abstract: A compound of the formula (I) 1

Abstract: A polyisocyanate of formula (I) OCN—R1—[—NX—CO—O—R2—O—CO—NH—R1—]n—NCO in which the units R1, X and R2 have the meanings: R1 is a unit of the formula (II): —CH2—CH2—CH2—CH2—CH2—CH2—  (II) X is hydrogen or a unit of the formula (III): —CO—NH—R1—NCO  (III), with the proviso that at least one of the units X in the polyisocyanates is a unit of formula (III); and R2 • is a 4-, 5- or 6-membered cycloalkylene group containing radical.

Abstract: A low monomer 1:1-monoadduct from a diisocyanate and a hydroxy(meth)acrylate with a free diisocyanate content of less than 0.7% by weight and a free NCO content of 10.4-16.4% by weight can be used as a starting material for an acrylic or NCO functionalized crosslinker; a bonding agent for coatings and adhesives; and a linker for solid-phase synthesis of oligo-nucleotides, polynucleotides or peptides. The monoadduct is obtained by converting 5-20 mol diisocyanate with 1 mol hydroxy(meth)acrylate at a temperature of 40-120° C. in the presence of at least one inhibitor; subsequently separating a non-converted diisocyanate from a reaction product by short-path distillation at 80-220° C./0.1-10 mbar; feeding air, nitrogen monoxide or oxygen or a mixture containing (a) air, oxygen or nitrogen monoxide and (b) a proportion of 1-90% by volume of carbon dioxide, nitrogen, an inert gas or a mixture thereof through a reaction apparatus.

Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The invention relates to positional isomer diethyloctandioldicarbamates and diethyloctandioldiallophanates, to a method for the production thereof and to the use thereof as synthetic building blocks and constituents of adhesives, luting compounds and coating materials.

Abstract: The present invention relates to the use of certain resorcinol derivatives as skin lightening agents.

Abstract: An aliphatic polyurea prepolymer prepared by the catalyst-free, exothermic reaction of a caprolactone monomer, an aliphatic primary polyamine, and an aliphatic monomer-free polyisocyanate, such as a hexamethylene diisocyanate dimer or trimer or mixtures thereof.

Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The present invention relates to a process for the production of polyisocyanates containing allophanate groups and having aliphatically and/or cycloaliphatically bound isocyanate groups by reacting organic compounds containing urethane groups with organic polyisocyanates containing aliphatically and/or cycloaliphatically bound isocyanate groups in the presence of tin compounds and to the use of these polyisocyanates, optionally blocked with blocking agents for isocyanate groups, as an isocyanate component in the production of polyurethanes, in particular polyurethane coatings.

Abstract: The reactivity of isocyanate formulations is controlled by including a chain extender corresponding to the formula HO—R1—NR2—X—NR3—R4—OH  (I) in which R1, R2, X, R3 and R4 represent specified groups is included in the isocyanate formulation.

Abstract: The present invention provides a compound of the formula wherein when X is S; R is selected from the group consisting of CH3, CH2CH3, CH2Ph, (CH2)2Ph, (CH2)2CH3, (CH2)3CH3, (CH2)4CH3, CH2)5CH3, (CH2)6CH3, (CH2)2O(CH2)3CH3, CH2HC═CH(CH2)3CH3, CH2C≡C(CH2)3CH3, CH2C≡C(CH2)2CH3, CH2C≡CCH2CH3, CH2C≡CCH3, CH2C≡CH, CH2C≡C(CH2)4CH3, CH2C≡C(CH2)5CH3, CH2C≡C(CH2)6CH3, (CH2)2C≡C(CH2)2CH3, CH(Ch3)C≡C(CH2)3CH3, (CH2)6I, (CH2)6Br, (CH2)5Br, (CH2)5COOH and (CH2)5OCOCH3, and R′ is selected from the group consisting of CH3, CF3, CH2Cl, CH2Br, CH2CH3, NH2, and OSO2CH3; wherein when R is CH3, R′ can not be CH3 or CH2Cl; wherein when R is CH2CH3, R′ can not be CH3; wherein when X is Se, R is (CH2)6CH3, and R′ is CH3 or a pharmaceutically acceptable salt or hydrate thereof; and wherein when X is O, R is CH2C≡C(CH2)3CH3, and R′ is CH3 or a pharmaceutically acceptable salt or hydrate thereof.

Abstract: The present invention provides a method for preparing a fluorochemical composition comprising a urethane by reacting: (A) fluorochemical oligomer of the formula (I): MfmMn—Q1—T1 wherein MfmMn represents a fluorochemical oligomer comprising m units derived from fluorinated monomer and n units derived from fluorine-free monomer and wherein the fluorinated monomers and fluorine-free monomers may be the same or different; m is a value of about 2 to 40; n is a value of about 0 to 20; T1 is an —OH or —NH2 moiety; Q1 and T1 together represent an organic residue obtained by removing a hydrogen atom from a chain transfer agent that is functionalized with T1; (B) monofunctional compound capable of reacting with an isocyanate and comprising a poly(oxyalkylene) group; (C) isocyanate blocking agent or a fluorine-free oligomer; and (D) isocyanate-reactive compound other than said fluorochemical oligomer, said isocyanate blocking agent, said fluorine-free oligomer and said monofunctional compound; wi

Abstract: Six-membered cyclic carbonates (2-oxo-1,3-ioxanes) in which keto or carbohydrocarbyloxy groups are bound to the 5 position of the ring are disclosed. They react surprising quickly with primary or secondary cyclic amines, and the novel product hydroxyurethanes are usefull as reactive diluents.

Abstract: A process for producing an aryl carbamate of a high purity at a high yield by reacting a diaryl carbonate with an amine compound having one or more hydrogen atoms bonded to the N position in the presence of carboxylic acid(s) of the following general formulae (I): R.sup.1 --COOH and/or (II): R.sup.2 --COOH (wherein R.sup.1 represents an alkyl or cycloalkyl group having an .alpha.-positioned carbon atom bonded to only one hydrogen atom, an alkyl group having an .alpha.-positioned carbon atom bonded to no hydrogen atom, or an aryl or heterocyclic group, and R.sup.2 represents an alkyl group having an .alpha.-positioned carbon atom bonded to two or more hydrogen atoms).

Abstract: Novel non-ionic contrast media are provided, which fulfill the requirements for x-ray visualization media, while being biodegradable. The compounds are characterized by being triiodo-3,5-diaminobenzoic acid derivatives, where the functional groups are derivatized with hydroxyalkyl groups and the amino functionalities are further derivatized with acyl substituents of one carbon acids. Also, triiodophloroglucinol oxyalkyl substituted derivatives are provided.

Abstract: The present invention provides medicinal compounds that are characterized by a cyclic moiety (A) linked through a carboxamido group (more specifically, a carbamate group or a urea group) to another cyclic moiety (B) which is in turn linked to another, N-substituted carboxamido group. These compounds can be used an anti-inflammatory and immunosuppressive agents, as demonstrated by their inhibition of the production of IL-1.beta. in vitro and TNF.alpha. in vivo.

Abstract: A process is disclosed for the preparation of an N-acylated activated derivative of an amino acid or a salt thereof.

Abstract: The present invention relates to coating compositions containinga) aldimines andb) polyisocyanates whichi) contain 2 to 35% by weight of allophanate groups, based on the weight of the polyisocyanates,ii) have a viscosity of less than 3000 mpa.s at 25.degree. C. when measured at a solids content of 100%,iii) are based on the reaction products of aliphatic polyisocyanates with1) 10 to 90 mole percent of monohydroxy compounds and2) 10 to 90 mole percent of polyhydric alcohols, wherein the mole percentages of 1) and 2) add up to 100, and the percentages are based on the total moles of monohydroxy compounds 1) and polyhydric alcohols 2) andiv) contain less than 10 mole percent of urethane groups, based on the total moles of urethane groups obtained from monohydroxy compounds 1) and polyhydric alcohols 2).

Abstract: Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.

Abstract: A mixture of lipophilic and amphiphilic/hydrophilic film-forming polymers of the formula (I)R--(CO).sub.m Y.sup.1 --(CH.sub.2 CHR.sup.1 O).sub.n --?CONH--Z--NHCO(OCH.sub.2 CHR.sup.2).sub.n' --Y.sup.2 --(CH.sub.2 CHR.sup.2 O).sub.n" !.sub.p --CONH--Z--NHCO--(OCH.sub.2 CHR.sup.1).sub.n --Y.sup.1 (CO).sub.m R (I)where R represents (i) an alkyl, alkenyl or alkaryl group of from 1 to 30 carbon atoms or (ii) a polypropylene oxide group or polybutylene oxide group; R.sup.1 and R.sup.2, each, independently, represent a hydrogen atom, or a methyl or ethyl group; Z represents a divalent linking hydrocarbyl group; m is 0 or 1; when m=0, Y.sup.1 represents O, NR.sup.3 or N.sup.+ R.sup.3 R.sup.4 X.sup.- and when m=1 Y.sup.1 represents O; Y.sup.2 represents O, NR.sup.3, N.sup.+ R.sup.3 R.sup.4 X.sup.-, (R.sup.3 NCH.sub.2 CH.sub.2).sub.t, or ?(R.sup.3 R.sup.4 N.sup.+ CH.sub.2 CH.sub.2)X.sup.- !.sub.t ; R.sup.3 and R.sup.4, independently, represent C.sub.1 -C.sub.

Abstract: The present invention relates to ethylenically unsaturated polyurethanes which are substantially free from isocyanate groups and havea) a total content of (meth)acryloyl groups (calculated as C=C, MW 24) of 1 to 20% by weight.b) an allophanate group content (calculated as N.sub.2 C.sub.2 HO.sub.3, MW 101) of 1 to 20% by weight andc) an isocyanurate group content (calculated as N.sub.3,C.sub.3,O.sub.3, MW 126) of up to 18% by weight,in which the allophanate and isocyanurate groups are prepared from aliphatic polyisocyanates.The present invention also relates to a one-component coating composition containing these ethylenically unsaturated polyurethanes.

Abstract: This invention relates to a class of aminimides structurally characterized as an acyl nitrogen-nitrogen ylide such that the acyl moiety possess the structural diversity element G, the quaternary nitrogen possess structural diversity elements E and F, and the quaternary nitrogen is bonded to a hydroxyethyl substituent, which in turn is bonded to an aminomethylene moiety that possess structural diversity elements A and B from the amino group and diversity element C from the methylene substituent, as shown below, ##STR1## wherein structural diversity element A, B, C, D, E, F and G are chosen from the set of elements consisting of substituted and unsubstituted as well as branched and straight chain alkyl, aryl, alkaryl, aralkyl, carbocyclic, heterocyclic, hydrogen, amino acid, peptide, polypeptide, protein, depsipeptide, carbohydrate derivatives, nucleotide derivatives, oligonucleotide derivatives, naturally occurring or synthetic organic structural motifs, reporter elements, organic moieties containing at least

Abstract: A composition of matter comprising ureas, biurets or allophanates structurally represented, respectively, by ##STR1## where R is hydrogen or a (C.sub.1 -C.sub.50) linear or branched aliphatic, alkenyl, alkynyl or aryl hydrocarbon; ##STR2## where R is hydrogen or a (C.sub.1 -C.sub.50) linear or branched aliphatic, alkenyl, alkynyl or aryl hydrocarbon; or ##STR3## where R is hydrogen or a (C.sub.1 -C.sub.50) linear or branched aliphatic, alkenyl, alkynyl or aryl hydrocarbon.

Abstract: The present invention relates to novel polyether-substituted compounds of imides and their use as surface-active agents.

Abstract: Polyalkyl hydroxy and amino aromatic carbamates having the formula: ##STR1## or a fuel-soluble salt thereof; wherein X is hydroxy or amino;R.sub.1 and R.sub.2 are independently hydrogen, hydroxy, lower alkyl having 1 to 6 carbon atoms, lower alkoxy having 1 to 6 carbon atoms, nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms;R.sub.3 is hydrogen or lower alkyl having 1 to 6 carbon atoms; andR.sub.4 is a polyalkyl group having an average molecular weight in the range of about 400 to 5,000.The polyalkyl hydroxy and amino aromatic carbamates of formula I are useful as fuel additives for the prevention and control of engine deposits.

Abstract: The present invention relates to novel benzoquinones which are useful as antihyperlipidemic agents. The present invention also provides a process for their preparation, pharmaceutical compositions, and a method for treating birds and mammals in need thereof which comprises administering to said host an effective amount of a benzoquinone of the present invention.