Abstract: A process for the preparation of an allophanate of one or more identical or different isocyanates, compositions obtained by the process, and uses of the compositions are disclosed. The process comprises reacting an isocyanate with at least one monoalcohol comprising an ether or polyether functional group in the presence of a bismuth-comprising catalyst and a metal compound as co-catalyst.

Abstract: A process for the preparation in high yields and purity of the compound 6-(7-4(1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.

Abstract: Provided are compositions and methods for intracellular detection of enzyme activity. One example of a composition is a histone deacetylase substrate comprising a compound of the following formula (I): One example of a method is a method for detecting histone deacetylase activity comprising introducing a compound according to formula (I) to a plurality of cells and monitoring the cells with magnetic resonance spectroscopy.

Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.

Abstract: Disclosed herein are accelerants for the formation of oxime-containing compounds from the reaction of a carbonyl-containing compound and a hydroxylamine-containing compound. The oxime-containing compound, the carbonyl-containing compound and the hydroxylamine-containing compound can each be a non-natural amino acid or a non-natural amino acid polypeptide. Also disclosed is the use of such accelerants to form oxime-containing compounds, the resulting oxime-containing compounds, and reaction mixtures containing such accelerants.

Abstract: The invention relates to an inhibitor of dimethylarginine dimethylaminohydrolase (DDAH) of general structural formula (I), wherein B is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromatic system having a ring size of 3 to 6; R1 is selected from the group of structures (i-vii), wherein R2, R3 and R4 are selected from the group consisting of hydrogen, an alkyl or aryl radical, R5 and R6 are selected from the group consisting of hydrogen, a hydrocarbon chain having a chain length of 1 to 8 and an aryl radical, R7, R8, R9 and R10 are selected from the group consisting of hydrogen, and alkyl or aryl radical; W is oxygen (O) or nitrogen (N); and X is a methylene group (CH2) or a secondary amino group (NH); Y is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromat

Abstract: The present invention relates to conjugates of a drug and an amino acid or an amino acid derivative or analog, pharmaceutical compositions that include the conjugates and methods of use thereof. In particular, the present invention relates to conjugates of anti-proliferative drugs and asparagine and glutamine and analogs thereof as compositions for treatment of cancer, and conjugates of imaging agent carriers and amino acids for the diagnosis of tumors and metastases.

Abstract: Provided is a Michael addition product prepared from a multifunctional acryl monomer having multiple hydroxyl groups allowing introduction of acryl functional groups, as a Michael acceptor, and a Michael donor. The Michael addition product is a novel multifunctional compound having an oligomer and a photoinitiator moiety in the molecule. Since it can be cured under a standard UV curing condition without having to add a photoinitiator, it is reduced to air pollution or health problem. Therefore the superior physical properties were obtained by cured coatings without surface tackiness. In addition, its hydroxyl groups allow, through isocyanate bonding or introduction of acryl groups, 3-dimensional crosslinking and molecular and compositional design for improving expandability, friction, and reactivity and hydrophilicity for self-adhesion, hardness of cured film, or the like. Consequently, a very useful, multifunctional or water-dispersible coating composition may be prepared.

Abstract: The present invention provides for a rheology control agent that includes a following compound represented by the following formula: wherein A, B, C and D equal CH2, CHR, NH, or O, and A, B, C and D may be the same or different and at least one of A and B equals NH and at least one of C and D equals NH; and wherein R1, R2, and R3 may be the same or different and represent a linear, branched, hyper-branched, or dendritic ether, polyether or hydrocarbon based chain, optionally forming at least one carbon-based ring, being saturated or unsaturated and R2 represents linear or branched alkylenes, ethers, polyethers, or polyester linkages and at least one of R1, R2, and R3 comprises an ester group or an amide group which is branched off from the main chain; excluded from Formula (1) is a compound wherein R2 is CH2—CH2—CH2—CH2—CH(C(O)OCH3), A, B, C, and D are equal to NH and R1 and R3 are both equal to a linear octyl hydrocarbon chain; the rheology control agent is suitable for solvent-borne and water-borne coat

Abstract: The present patent application relates to an improved process for the separation of enantiomerically pure compounds. Specifically it relates to separation of enantiomerically enriched Rivastigmine, Duloxetine, Escitalopram and their intermediates in high yields.

Abstract: A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C.

Abstract: A microfluidic system comprising a microchannel, a carrier fluid comprising a fluorinated oil in the microchannel, at least one plug comprising an aqueous plug-fluid in the microchannel and substantially surrounded on all sides by the carrier-fluid, and a fluorinated surfactant comprising a functional group capable of selectively binding a target molecule is disclosed. A compound for use therewith and a method of synthesizing a fluorinated surfactant are also provided.

Abstract: The present invention relates to the use of propamocarb and derivatives thereof for improving the tolerance of crops to chilling temperatures and/or frost.

Abstract: The present invention is a method for producing an N-substituted carbamic acid ester derived from an organic amine from an organic amine, a carbonic acid derivative and a hydroxy composition containing one or more types of hydroxy compounds, wherein the organic amine, the carbonic acid derivative and the hydroxy composition are reacted using a urethane production reaction vessel provided with a condenser, a gas containing the hydroxy composition, the compound having the carbonyl group derived from the carbonic acid derivative, and an ammonia formed as a by-product in the reaction, is introduced into the condenser provided in the urethane production reaction vessel, and the hydroxy composition and the compound having the carbonyl group derived from the carbonic acid derivative are condensed, and wherein a stoichiometric ratio of a hydroxy compound contained in the condensed hydroxy composition to the condensed compound having the carbonyl group derived from the carbonic acid derivative is 1 or more, and a rati

Abstract: The invention relates to a compound suited as entity carrier, having the general formula (I) wherein X is an amine-containing residue further defined herein. The invention further relates to the use of such compounds, a nanocarrier system, a kit comprising such compounds and methods for gene silencing and anti-cancer treatment.

Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I), wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R1, R1a, R2, R2a, R3, R3a, X, X1, X2, X3 have the meaning as indicated in the description and the claims and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer; and Z is a carrier group. The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.

Abstract: Disclosed herein are accelerants for the formation of oxime-containing compounds from the reaction of a carbonyl-containing compound and a hydroxylamine-containing compound. The oxime-containing compound, the carbonyl-containing compound and the hydroxylamine-containing compound can each be a non-natural amino acid or a non-natural amino acid polypeptide. Also disclosed is the use of such accelerants to form oxime-containing compounds, the resulting oxime-containing compounds, and reaction mixtures containing such accelerants.

Abstract: The invention provides compounds that are useful as linkers for solid phase synthesis and as protecting groups, and methods for producing and using the same.

Abstract: The present invention provides novel synthesis's for obtaining a protecting group aminoxy PEG-6 linker from cost effective, and readily available starting materials and chemicals or modified polyethylene glycols. More specifically, a novel synthesis of obtaining a modified Boc-protected aminoxy PEG-6 linker was achieved so that said linker may be attached to a vector such as a peptide based fragment.

Abstract: The invention relates to alcohol-modified glycidyl carbamate resins wherein at least some of the glycidol groups in the resin have been replaced with an alcohol. The invention also relates to coating compositions containing the resins.

Abstract: Provided are methods of screening compounds for any aspirin-related activity other than TAFI inhibition, and also for non-inhibition of TAFI. Compounds identified by the screening methods can be used to treat, prevent or manage in a patient pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder. Also provided is a method of evaluating test compounds for TAFI inhibitory activity wherein the TAFI inhibitory activity of these test compounds is compared to the TAFI inhibitory activity of aspirin or its derivatives or metabolites. Further provided is a method of treating, preventing or managing in a patient, a hemorrhagic or thrombotic disease or disorder with high dose aspirin or aspirin derivatives or metabolites.

Abstract: The present disclosure provides processes for the preparation of lipid conjugated cyclic carbonate derivatives. More specifically, the present disclosure is based on the finding that reacting lipids, such as, ceramides, with N,N?-disuccinimidyl derivative, resulted in the formation of, isolatable, substituted cyclic [1,3]-dioxan-2-one and [1,3]-dioxan-2-thione compounds. These isolatable cyclic substituted compounds and derivatives thereof may be used for various applications, such as in vaccination.

Abstract: The present invention relates generally to branched macromolecules and their use as imaging or contrast agents. In particular, the invention relates to dendrimers, derived from lysine or lysine analogues, bearing a plurality of functional moieties and their application to imaging techniques in which a disease state may be imaged with a targeted contrast agent.

Abstract: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds and compositions of this invention.

Abstract: The present invention relates to a process for the preparation of particularly reactive and low-viscosity reaction products of polyisocyanates which contain activated ethylenically unsaturated groups which react by polymerization under the action of actinic radiation, and the use of these reaction products in coating compositions, and particularly scratch-resistant coatings obtainable therefrom.

Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.

Abstract: The present invention provides for a rheology control agent that includes a following compound represented by the following formula: wherein A, B, C and D equal CH2, CHR, NH, or O, and A, B, C and D may be the same or different and at least one of A and B equals NH and at least one of C and D equals NH; and wherein R1, R2, and R3 may be the same or different and represent a linear, branched, hyper-branched, or dendritic ether, polyether or hydrocarbon based chain, optionally forming at least one carbon-based ring, being saturated or unsaturated and R2 represents linear or branched alkylenes, ethers, polyethers, or polyester linkages and at least one of R1, R2, and R3 comprises an ester group or an amide group which is branched off from the main chain; excluded from Formula (1) is a compound wherein R2 is CH2—CH2—CH2—CH2—CH(C(O)OCH3), A, B, C, and D are equal to NH and R1 and R3 are both equal to a linear octyl hydrocarbon chain; the rheology control agent is suitable for solvent-borne and water-borne coat

Abstract: This invention describes reagent precursors and methods for chemical and biochemical reactions. These reagent precursors that can be activated in solution upon irradiation to generate reagents required for the subsequent chemical reactions. Specifically, photogenerated reagents (PGR) are useful for controlling parallel combinatorial synthesis and various chemical and biochemical reactions.

Abstract: Provided are compositions and methods for intracellular detection of enzyme activity. One example of a composition is a histone deacetylase substrate comprising a compound of the following formula (I): One example of a method is a method for detecting histone deacetylase activity comprising introducing a compound according to formula (1) to a plurality of cells and monitoring the cells with magnetic resonance spectroscopy.

Abstract: The invention relates to compounds of the formula I as defined herein, which are inhibitors of activated thrombin-activatable fibrinolysis inhibitor. The compounds of the formula I are suitable for manufacturing medicaments for the prophylaxis, secondary prevention and therapy of one or more disorders which are associated with thromboses, embolisms, hypercoagulability or fibrotic changes.

Abstract: The present invention relates to a method of treating pain using a compound of formula wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to certain novel derivatives of formula (I).

Abstract: Disclosed are hydrophilic choline/N-heterocycle ester compounds containing single amino acids, peptides, or derivatives thereof which have the potential to express anti-oxidant activity capable of reducing reactive oxygen species in cells. These compounds may be used to inhibit oxidative stress-induced cell injury or death both in vivo and ex vivo. In addition, methods for the synthesis of these compounds are disclosed.

Abstract: The present invention relates to a process for preparing amino-functional polyurethane prepolymers by a) preparing an NCO-functional polyurethane prepolymer by reacting an excess of one or more di- and/or polyisocyanates with at least one isocyanate-reactive compound having a functionality of at least 1.5, b) reacting the free NCO groups of the resulting polyurethane prepolymer with at least one compound containing one or more silanol groups to obtain the corresponding silylurethanes, and then c) converting the silylurethanes to amino-functional polyurethane prepolymers by hydrolysis and/or alcoholysis with decarboxylation. The present invention also relates coatings, adhesives, sealants, casting compounds or moldings obtained from these amino-functional polyurethene prepolymers.

Abstract: Disclosed herein are accelerants for the formation of oxime-containing compounds from the reaction of a carbonyl-containing compound and a hydroxylamine-containing compound. The oxime-containing compound, the carbonyl-containing compound and the hydroxylamine-containing compound can each be a non-natural amino acid or a non-natural amino acid polypeptide. Also disclosed is the use of such accelerants to form oxime-containing compounds, the resulting oxime-containing compounds, and reaction mixtures containing such accelerants.

Abstract: The invention provides compounds that are useful as linkers for solid phase synthesis and as protecting groups, and methods for producing and using the same.

Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.

Abstract: The invention provides conjugates of fatty amines and pharmaceutical agents useful in treating cancer, viruses, psychiatric disorders. Compositions, pharmaceutical preparations, and methods of preparations of the fatty amine-pharmaceutical agent conjugates are provided.

Abstract: The present invention provides a branched polyalkylene glycol wherein three or more single-chain polyalkylene glycols and a group having reactivity with an amino acid side chain, the N-terminal amino group or the C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity are bound; and a physiologically active polypeptide modified with the branched polyalkylene glycol.

Abstract: The invention relates to compounds suitable for use in an imaging agent said imaging agent showing an improved pharmacokinetic profile.

Abstract: A process for amino acid derivatives shown by the below general formula (I): (wherein R1 means a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms.) having an object to provide a process of the amino acid derivatives of the formula (I) and their synthetic intermediate, t-butoxycarbonylamino-ethylamine, whereby it requires no tedious procedure and is also good in yield, and its application to a mass production is easy, and to provide novel amino acid derivatives of the formula (IV), their synthetic intermediates, and a process thereof, characterized in that it comprises a step to obtain the amino acid derivatives shown by the general formula (I) by hydrolysis of compounds shown by the below formula (II): (wherein R1 has the same meaning as described above, and R2 means a straight chain or branched chain alkyl group with 1-4 carbon atoms.

Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

Abstract: A new process for the production of 1-hydroxymethyl-1,3,5-triazapentane, trihydrochloride is described.

Abstract: The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions ameliorated by inhibition of matriptase or MTSP1.

Abstract: A readily available and inexpensive natural ?-amino acid is converted into a compound represented by formula (1), which is then reacted with an organometallic reagent represented by formula (2) to give an optically active 5-hydroxyoxazolidine represented by formula (3), which is then treated with an acid to provide an optically active aminoketone represented by formula (4). The product is then converted into an optically active aminoalcohol represented by formula (5) or (6) by, for example reduction.

Abstract: A class of compounds is disclosed which are diasteroisomers of a known class of protease inhibitors. The compound inhibit gamma-secretase, and find use in the treatment of and/or prevention of Alzheimer's disease.

Abstract: A process for amino acid derivatives shown by the below general formula (I): (wherein R1 means a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms.) having an object to provide a process of the amino acid derivatives of the formula (I) and their synthetic intermediate, t-butoxycarbonylamino-ethylamine, whereby it requires no tedious procedure and is also good in yield, and its application to a mass production is easy, and to provide novel amino acid derivatives of the formula (IV), their synthetic intermediates, and a process thereof, characterized in that it comprises a step to obtain the amino acid derivatives shown by the general formula (I) by hydrolysis of compounds shown by the below formula (II): (wherein R1 has the same meaning as described above, and R2 means a straight chain or branched chain alkyl group with 1-4 carbon atoms.

Abstract: This invention relates to a process for the preparation of alkyl-N-(3-dimethylamino)alkylcarbamates by reacting an alkyl-chloroformate in an alcohol.

Abstract: The present invention provides a purification process whereby deferoxamine B produced by a microorganism and in mixture with other polyhydroxamates produced by the microorganism may be converted into its mesylate salt substantially free of the other polyhydroxamates and substantially free of chloride ion. The process includes adsorption and desorption of the deferoxamine B on an adsorption resin, direct precipitation of the deferoxamine free base out of the eluent from the adsorption resin, contacting of the deferoxamine B free base with methanesulfonic acid and isolation of the deferoxamine B mesylate salt by precipitation. This process minimizes decomposition of deferoxamine B.

Abstract: Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.

Abstract: Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.