Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.

Abstract: The invention relates to a process for the preparation of liquid, storage-stable isocyanate mixtures of low color number containing carbodiimide (CD) and/or uretonimine (UI) groups, the isocyanate mixtures obtainable by this process and the use thereof for the preparation of blends with further isocyanates and for the preparation of prepolymers containing isocyanate groups and of polyurethane plastics, preferably polyurethane foams.

Abstract: The present invention pertains to a novel method for preparing a carbamate, in which the method comprises reacting an aliphatic substituted urea and/or its derivatives, with a hydroxyl group containing compound to obtain a carbamate. In addition, the present invention provides a novel catalyst which is suitable for catalyzing the reaction to form a carbamate, and a method for preparing the novel catalyst. The method of the present invention for preparing a carbamate does not involve the application of carbon monoxide which is toxic, and the reaction conditions are relatively mild with high catalytic activity, high reaction selectivity of the catalyst, and a relatively short reaction time. Furthermore, the catalyst is separated from the reaction system and reused easily, which will facilitates scale up and industrial application.

Abstract: The invention relates to hydroxamic acid derivatives having carbamate linkage with the structural formula that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous systems (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Abstract: This invention is directed to compositions and methods for the isolation and further characterization of eukaryotic, mammalian, and/or human PC-PLC. In addition, the present invention discloses methods for the synthesis of an affinity chromatography resin for the isolation and purification of biologically active proteins, including eukaryotic PC-PLC.

Abstract: The present invention relates to a polyacylurethane having the following general formula (I) and a process for the preparation of such polyacylurethane. Preferred embodiments of the polyacylurethanes according to the invention have elastomeric properties. The polyacylurethanes can suitable be used in biodegradable, biocompatible and/or biomedical devices.

Abstract: The ring-containing modified resin is represented by the following chemical formula (1) R1[—(—O—CO—NH—R2—NH—CO—O—R3—)p—O—R4]q??(1) (in the chemical formula (1), R1 is a dehydroxyl residue of a resin having a benzene ring and/or a condensed ring and hydroxyl group: —R2— is deisocyanate group derived from an organic diisocyanate: —R3— is a dehydroxyl residue of polyol having number-average molecular weight of 200 to 30000: p is 1 to 3: —R4 is a hydrogen atom, alkyl group having 1 to 18 carbons, phenyl group: q is the same number as the number of the dehydroxyl residue of R1).

Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2. The present invention is also directed to intermediates useful in the preparation of formula I compounds.

Abstract: Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.

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 invention is directed to D-homoandrosta-17-yl-carbamate derivatives as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.

Abstract: Gabapentin enacarbil was prepared and purified from intermediates such as 1-haloalkyl carbamate or carbonate and diacid acetal skeleton. For example, a 1-haloalkyl carbonate or carbamate was prepared by combining a C1 to C10 alcohol or C1 to C10 primary amine, a solvent selected from the group consisting of: acetonitrile, C3 to C7 ketone, C5 to C10 ether, C2 to C7 ester, C5 to C10 hydrocarbon and a combination thereof; a 1-haloalkyl haloformate of the following formula: wherein each X is independently selected from Br, I, or Cl; R1 is alkyl or H; and a C6 to C21 tertiary amine.

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: 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: Disclosed are novel hybrid compounds having a fullerene core residue, one or more bioavailability enhancing moieties and one or more glutamate receptor ligand residues, whereby the bioavailability enhancing moiety allow the compound to reach an effective concentration in physiological media and pass the blood-brain barrier, as defined in the specification. Also disclosed are pharmaceutical compositions containing these hybrid compounds and uses thereof as antioxidants and/or neuroprotective agents for the treatment of medical conditions associated with oxidative stress and/or neural damage, such as, for example, neurological diseases, disorders and trauma, and hence in the treatment of CNS-associated diseases, disorders and trauma, as well as to uses thereof as antiviral, antibacterial, antiglycemic, antiarrhythmic, antidepressant and antitumor agents.

Abstract: The present invention describes novel prodrugs of formula (I) or their salts, process of preparation and uses thereof.

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: The present invention concerns methods of synthesis of trans-tert-butyl-2-aminocylcopentylcarbamate comprising contacting 6-tosyl-6-azabicyclo[3.1.0]hexane with TMSN3 and TBAF to produce 2-azido-N-tosylcyclopentananiine; reducing the 2-azido-N-tosylcyclopentanamine to produce 2-amino-N-tosylcyclopentanamine; contacting the 2-amino-N-tosylcyclopentanamine with di-tert/-butyl dicarbonate to produce tert-butyl-2-(tosylamino)cyclopentylcarbamate; and detosylation of tert-butyl O(tosylamino) cyclopentylcarbamate to produce trans-tert-butyl-2-aminocyclopentylcarbamate. The invention also concerns PNAs comprising residues of the monomers of the invention in the backbone and uses of such PNAs. The PNAs of the invention can be used to detect DNAs of infectious agents or to suppress expression of protein associated with cancer.

Abstract: The invention relates to starting compounds which can be used for the preparation of polyurethanes and can be prepared by reaction of hydroxyl-containing oligomers of formaldehyde.

Abstract: Compounds of Formula I are disclosed: (I), wherein XA, k, R1, R2, R3, R4, R5, R5A, R6, R6A, R7 and R8 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: The present disclosure relates to methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs and to intermediates used in the methods.

Abstract: The present disclosure relates to methods of synthesizing N-hydroxysuccinimidyl-carbonate intermediates from the corresponding sulfones useful in the preparation of 1-(acyloxy)-alkyl carbamate prodrugs.

Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.

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 biuret compounds of the general formula in which R1 is C2-C18 alkylene, cycloalkylene, arylene or aralkylene, Y is —O— and/or —NH—, R2 is C4-C22 alkyl, C3-C18 alkenyl, cycloalkyl, aralkyl, CmH2m+1(O—CnH2n)x—(O—CH(C6H5)—CH2)u-, CmH2m+1(OOC—CvH2v)x-, X—C6H4—(O—CnH2n)x—(O—CH(C6H5)—CH2)u-, where m=1-22, n=2-4, x=0-15, u=0-15, v=4-5, X is C1-C12 alkyl, —(C6H5)1-4 and R3, R4 and R5 are C2-C18 alkylene, cycloalkylene, arylene or aralkylene, it being possible for R3, R4 and R5 to be identical or different, Z is —COO—, NHCO—, NHCOO—, NHCONH— and/or mixtures thereof and a is 1-20. The invention also relates to a process for preparing biuret compounds and to their use as rheology control agents. The invention further relates to urethane- and/or urea-containing uretdiones which are useful intermediates for preparing the biuret compounds.

Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.

Abstract: Modified stable polyisocyanates are described having at least one isocyanate function modified by a group having cross-linking functionality.

Abstract: The present invention relates to a process for producing amino acid derivatives such as optically active ?-amino acid in short steps with good yield and high optical purity, which comprises reacting a keto acid of the formula (1): wherein R1 is hydrogen, an optionally substituted hydrocarbon, etc.; R2 is a spacer; and R3 is an optionally substituted alkoxy, etc., or a salt thereof, with ammonia or an amine or a salt thereof in the presence of a chiral catalyst and in the presence or absence of an acid and/or a fluorine-containing alcohol, to give an amino acid derivative of the formula (2): wherein Q is a group formed by removing one hydrogen atom from ammonia or an amine; X? is an acid and/or a fluorine-containing alcohol; and b is 0 or 1.

Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.

Abstract: In one embodiment, the present application relates to a process of making a compound of formula I: and to certain intermediate compounds that are made within the process of making the compound of formula I.

Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.

Abstract: Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

Abstract: Mesophasic forms of (3S)-aminomethyl-5-hexanoic acid prodrugs and methods of preparing and methods of using mesophasic forms of (3S)-aminomethyl-5-hexanoic acid prodrugs are provided.

Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

Abstract: A polyether polyol composition, the reactivity of which with a polyisocyanate can be controlled, to thereby obtain an isocyanate group-terminated prepolymer having excellent storage stability. A polyether polyol composition comprising a polyether polyol obtained by a ring-opening polymerization of an alkylene oxide in the presence of a composite metal cyanide complex catalyst, and a phosphoric acid compound comprising a phosphoric acid selected from orthophosphoric acid, polyphosphoric acid and polymetaphosphoric acid, and/ or a partial ester of such a phosphoric acid, wherein the polyether polyol composition contains metals derived from the composite metal cyanide complex catalyst in an amount of from 1 to 30 ppm based on the polyether polyol, and the above phosphoric acid compound in an amount of from 0.5 to 100 ppm based on the polyether polyol.

Abstract: An organic polyisocyanate with at least one unsaturated functional group is capable of copolymerizing when exposed to actinic radiation. The polyisocyanate comprises structural units with the formula (1): wherein: X is an electron-attracting group; R1, and R2 are hydrogen atoms, a saturated or unsaturated aliphatic or cycloaliphatic radical, or an aromatic or araliphatic radical; and n is an integer from 0 to 5. A process for producing this polyisocyanate is also disclosed.

Abstract: Novel cycloalkane carboxamide derivatives having an action that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkane carboxamide derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein R1 and R2 represent (substituted) alkyl groups, (substituted) alkenyl groups, (substituted) alkynyl groups, (substituted) aromatic hydrocarbon groups or (substituted) heterocyclic groups, ring A represents an alkylidene group having 5 to 7 carbon atoms, and ring B represents a formyl group or a hydroxymethyl group).

Abstract: Methods of preparing cinacalcet, cinacalcet derivatives, and salts thereof is disclosed herein. Also disclosed herein are polymorphs of cinacalcet, compositions of cinacalcet, and methods of treating a subject by administering cinacalcet, wherein cinacalcet is prepared by the disclosed methods.

Abstract: The invention relates to novel compounds of the formula (I) and their use in stabilization of Factor Vila or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof.

Abstract: A process for making aminoalkylphenyl carbamates, especially rivastigmine, can use less severe conditions using bis(p-nitrophenyl)carbonate (IX) as a phenol activator compound.

Abstract: This invention relates to hydroxamic acid derivatives having a carbamate linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.

Abstract: There is provided a compound represented by a general formula (B1-1) shown below, an acid generator composed of the above compound, a resist composition containing an acid generator composed of the above compound, and a method of forming a resist pattern: (wherein RX represents a hydrocarbon group which may contain a substituent group; Q1 represents an alkylene group of 1 to 12 carbon atoms which may contain a substituent group, or a single bond; n represents an integer of 0 or 1; Y1 represents an alkylene group of 1 to 4 carbon atoms, or a fluorinated alkylene group of 1 to 4 carbon atoms; and A+ represents an organic cation which contains a nitrogen atom).

Abstract: The invention is directed to a process for producing intermediates of a compound which exhibits an activated blood coagulation factor Xa inhibitory action and which is a useful preventive and a therapeutic agent for thrombotic diseases. The intermediate production process is represented by the following reaction scheme.

Abstract: Phase change ink carrier compositions comprising an admixture of (1) at least one urethane resin; and/or (2) at least one mixed urethane/urea resin; and/or (3) at least one mono-amide; and/or (4) at least one polyethylene wax are provided. In addition, a phase change colored ink of such carrier compositions comprising a phase change ink compatible colorant are also provided. Embodiments of the present invention also include methods for producing a layer of the above phase change colored ink on the surface of a substrate by either direct or indirect printing. Such methods also encompassing using a polyethylene wax as an overcoat layer above such a phase change ink layer on a printed substrate.

Abstract: Methods, compositions, and compounds for inhibiting monoacyglycerol lipase, and for treating pain, for modulating stress-induced analgesia or for treating stress-induced disorders in mammals are provided.

Abstract: The syntheses and in vitro antitumor properties of carbamate-containing, dicarbamate-containing, and ureido-containing phospholipid compounds that have an ether linkage at the C-1 position of a glycerol backbone, a carbamate, dicarbamate, or ureido moiety at the C-2 position of the glycerol backbone, and a phosphocholine, phosphonocholine, or glycoside moiety at the C-3 position of the glycerol backbone are described. The synthesis and antiproliferative activity of ether lipids with a naphthol moiety at the C-1 position are also described. These compounds were shown to be potent inhibitors of cancer cell growth. These compounds are useful for killing cancer cells and treating cancer.

Abstract: Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. The alkylcarbamic acid aryl ester of Formula (I), KDS-4103, is a FAAH inhibitor. Described herein is a process for the preparation of the compound of Formula (I), characterization of polymorphs of the FAAH inhibitor, and their uses therof.

Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.

Abstract: A process for the preparation of indole derivatives of formula (I): which are useful as intermediates in the preparation of pharmaceutically active compounds.