Abstract: A cyclic polycarboxylic acid anhydride, a polycarboxylic acid, or a mixture of them is allowed to react with hydroxylamine or a salt thereof in an organic solvent under dewatering conditions to yield a corresponding cyclic N-hydroxyimide compound. The cyclic polycarboxylic acid anhydride can be, for example, succinic anhydride or glutaric anhydride. The polycarboxylic acid can be, for example, succinic acid, glutaric acid, or adipic acid. In this process, the reaction is preferably carried out using an organic solvent capable of undergoing azeotropy with water as all or part of a reaction solvent while removing water from the reaction system by azeotropy with the organic solvent. This process produces a cyclic N-hydroxyimide compound in a good yield from any of a cyclic polycarboxylic acid anhydride and a polycarboxylic acid.

Abstract: The present invention includes methods and compositions for increasing the fluorous nature of an organic compound by reacting it with at least one fluorous compound to produce a fluorous tagged organic compound. The increased fluorous nature of the fluorous tagged organic compound can then be utilized to separate the fluorous organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom. The resultant fluorous tagged organic compound can be subjected to subsequent chemical transformations, wherein the fluorous nature of the tagged compound is utilized to increase the ease of separation of the fluorous tagged organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom, after each chemical transformation.

Abstract: The present invention relates to a novel class of compounds mainly, substituted leucinamide-carboxylate derivatives of formula (I) wherein X is O or NR9, Y is CR1R2, —SO2, C?O or NR9; Z is CR1R2, O, S, —SO2 or NR9 and each G is independently a CR1CR2 and pharmaceutical compositions thereof. Said compounds are cathepsin cysteine protease inhibitors, including but not limited to, inhibitors of cathepsin K, L, S and B. These compounds are useful for treating and preventing cathepsin dependent conditions in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases.

Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.

Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.

Abstract: The invention relates to compounds of formula (I) which are effective inhibitors of histone deacetylases.

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: Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:

Abstract: The present invention discloses novel compounds of Formula I: (I) possessing 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11?-HSD type 1 activity.

Abstract: The present invention relates to the use of at least one compound capable of cleaving the diketone crosslinking bonds between two proteins, in a composition applied topically to the skin, as an agent for preventing or treating the signs of ageing of the skin or the orange-peel appearance. The above compound is preferably a N-hydroxy imide of formula (I). These N-hydroxy imides have inhibitory properties on the glycation of proteins and also antioxidant properties. The invention also relates to novel N-hydroxy imides included in formula (I) above.

Abstract: The present invention provides a compound of the formula: (IIa); having a reactive functional group M, capable of reacting with a biopolymer, BP, having at least one group capable of reacting with M to form a covalent linkage, to provide a biopolymer derivative of the formula: (IIIa). The biopolymer derivatives of the invention have enhanced ionisability with respect to free 10 biopolymer (Bp) enabling improved analysis of the biopolymer using mass spectrometry. The invention further provides specific examples of compounds formula (IIa), e.g. compounds of formula: (IIa-2a) and (IIa-58a).

Abstract: The present invention provides polymeric delivery systems including an aromatic allyllic acyl group. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

Abstract: Disclosed herein is a method for inhibiting the premature polymerization of ethylenically unsaturated monomers comprising adding to said monomers an effective amount of: A) at least one nitroxyl compound, and B) at least one quinone alkide compound having an electron-withdrawing group at the 7-position. Additionally, a composition is disclosed that comprises: A) at least one nitroxyl compound, and B) at least one quinone alkide compound having an electron-withdrawing group at the 7-position.

Abstract: This invention generally relates to the derivatives of 1-substituted-3-pyrroli dines having the structure of Formula (I): The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention. pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.

Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.

Abstract: The present invention relates to benzsulfonamide derivatives of formula I and methods of use thereof. The benzsulfonamide derivatives of the present invention are efficient modulators of the JNK pathway. In particular the benzsulfonamide derivatives of the present invention are selective inhibitors of JNK 2 and 3.

Abstract: Compounds of formula (IIa): are provided where: X is a group capable of being cleaved from the ?-carbon atom to form an ion of formula (I?) C is a carbon atom bearing a single positive charge or a single negative charge; The invention further provides compounds of formula (IIb): where: X is a counter-ion to C. The compounds of formula (IIa) and (IIb) may form ions of formula (I?) by either cleaving the C—X bond between X and the ?-carbon atoms in the case of the compounds of formula (IIa) or dissociating X in the case of compounds of formula (IIb).

Abstract: Multifunctional compounds having acylsulfonamide amine-reactive groups are described that can be used for the capture of amine containing materials.

Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

Abstract: Compounds having two reactive functional groups are described that can be used as a tethering compound to immobilize an amine-containing material to a substrate. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonyldicarboximide group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a connector group between the substrate and the amine-containing material. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: The present invention relates to novel mixtures and maleic and succinic acid derivatives from mycelium of Antrodia camphorata and the medical use thereof. The present invention relates to the composition or mycelium comprising the compounds of the invention.

Abstract: Compounds of a certain formula (I) in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.

Abstract: The present invention provides azulenyl nitrones, such as those having the following general formula: (I) compositions comprising the same and methods of their use for the treatment or prevention of oxidative, ischemic, ischemia/reperfusion-related and chemokine-mediated conditions.

Abstract: Metal chelators of formula (I) and formula (II) are disclosed or a farmaceutically acceptable salt thereof. Also disclosed are metal chelator-targeting moiety complexes, metal chelator-targeting moiety-metal conjugates, kits, and methods of their preparation and use in diagnosis and/or treatment of diseases and conditions, including, inter alia, cancer and thrombosis.

Abstract: The invention relates to novel N-substituted imides and polymerizable compositions comprising these N-substituted imides. The invention further relates to the use of N-substituted imides as polymerization initiators.

Abstract: Sulfonate salts have the formula: R1COOCH2CH2CF2CF2SO3?M+ wherein R1 is alkyl, aryl or hetero-aryl, M+ is a Li, Na, K, ammonium or tetramethylammonium ion. Onium salts, oxime sulfonates and sulfonyloxyimides derived from these salts are effective photoacid generators in chemically amplified resist compositions.

Abstract: Compounds having two reactive functional groups are described that can be used as a tethering compound to immobilize an amine-containing material to a substrate. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonyldicarboximide group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a connector group between the substrate and the amine-containing material. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: Compounds having two reactive functional groups are described that can be used as a tethering compound to immobilize an amine-containing material to a substrate. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonyldicarboximide group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a connector group between the substrate and the amine-containing material. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: A compound having the formula Y-A-Z, wherein: A is a 5, 6, or 7 member ring that is monocyclic or is fused to 1 to 3 additional 4 to 8 member rings; wherein ring A and, independently, the fused additional rings are carbocyclic or heterocyclic, and saturated or unsaturated, wherein unsaturated rings are aromatic or non-aromatic; wherein Y and Z are substituents at adjacent positions on ring A; Y represents: Z represents: X and E represent O, S, or NRa or NRb; each of a, b, c, d, e and f independently represents 0 or 1; a+c equals 0, 1, or 2; b+d equals 0, 1, or 2; a+b+c+d+e+f equals 1, 2, or 3; provided that when f is 1, then d is 1, and when d is 0, then f is 0; and when both e and b are 0, then neither R1 nor R2 is chloro or bromo; v represents 0 or 1, provided that when v is 0, then J is hydrogen, a metal ion, or a quaternary ammonium ion; and X is O and G is H; either G is hydrogen, a metal ion, a quaternary ammonium ion, lower alkyl, or comprised of a pharmaceutically active chemica

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

Abstract: New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

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: A process for preparing an amine which comprises in preparing an amine by decarboxylating an ?-amino acid under heating in a high boiling liquid polymer having average molecular weight 200 to 6000, and directly recovering this amine by distillation in the same reaction system, namely in one pot.

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.

Abstract: A carbamate compound is disclosed.

Abstract: The present invention provides a method for the analysis of a compound with amino group (e.g., an amino acid or peptide) contained in a sample and convenient manner with a high sensitivity. The compound with amino group in a sample containing the compound with amino group is labeled with a specific carbamate compound such as p-trimethylammonium anilyl-N-hydroxysuccinimidyl carbamate iodide to enhance the selectivity and sensitivity. The present invention is preferably used in conjunction with mass spectrometry such as MS/MS method to facilitate quantitative analysis. The present invention further provides labeling reagents for mass spectrometry.

Abstract: The present invention relates to novel mixture and maleic and succinic acid derivatives from mycelium of Antrodia Camphorata and the medical use thereof. The present invention relates to the composition or mycelium comprising the compounds of the invention.

Abstract: Compounds of formula I: wherein Ar1 and Ar2 are optionally substituted aryl or heteroaryl, L is a bond, ?CH— or —(CHRa)n—, and X is SCN, SR1, S(O)R1, (CRaRb)mSO2R1, SO2N(R2)2, SO2NHCOR1, SO2NHN(R2)2, OSO2N(R2)2, OS(O)N(R2)2, OSO2NHCOR1, COR4, NHCOR1, NHCO2R1, NHCON(R2)2, NHSO2R1 or NHSO2N(R2)2, inhibit the processing of APP by gamma secretase, and hence are useful in treatment of Alzheimer's disease.

Abstract: The present invention relates to the preparation of polyethylene glycol carbonate active esters useful for the PEGylation of biological active and pharmaceutically useful peptides and proteins. The invention involves the use of activated carbonate and oxalate esters in the formation of polyethylene glycol mixed carbonate active esters that then react with a linker or directly with a target peptide or protein.

Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.

Abstract: Process for the preparation of stable activated derivatives of carbamic acid, comprising at least one protected amino group and an activated carbamic acid function, from an amino acid derivative in which the amino group is protected. The process includes: a) a step of transformation of the —COOH group of the amino acid derivative into a —CON3 group to obtain an acyl azide; b) a step of transformation of the —CON3 group of the acyl azide into a —NCO group to obtain an isocyanate; c) a step of treating the isocyanate to obtain a stable derivative of carbamic acid.

Abstract: A process for converting an aryl triflate, heteroaryl triflate, aryl halide or heteroaryl halide to an N-hydroxysuccinimido ester is disclosed. The process involves reacting the triflate or halide with carbon monoxide and N-hydroxysuccinimide in a solvent in the presence of a palladium catalyst and a base.

Abstract: The present invention relates to a process for the preparation of 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, the enantiomers and its salts, characterised in that 5-(4-fluorophenyl)pyridine-3-carbaldehyde is reacted directly with aminomethylchroman or its salts under reducing conditions to give 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, and the latter is, if desired, converted into one of its physiologically acceptable salts by treatment with an acid.

Abstract: The invention relates to substituted pyrrole Mannich bases of general formula (I), wherein R1=H, a C1-10-alkyl-, aryl, a heteroaryl- or an aryl, heteroaryl-, CN, Br—, Cl or OH radical bound by a C1-6 alkylene group, R2=CH(R4)N(R5)(R6), R3, R3?, R3? identically or individually represent H, F, Cl, Br, CF3, CN, NO2, SO2NH2, NHR7, SR8, OR9, CO(OR10), CH2CO(OR11), COR15, a C1-10-alkyl-, aryl-, heteroaryl-aryl radical or a heteroalkyl radical bound by a C1-6 alkylene group, R4=an unsubstituted phenyl radical or a phenyl radical substituted at least with C1-4 alkyl, C1-3-alkoxy-, halogen-, a method for the production of the above-mentioned compounds, medicaments containing said compounds, and the use of said compounds in the production of medicaments.

Abstract: The present invention is a series of compounds that are derivatives of 1-sulfonyl-pyrrolidine and that demonstrate affinity towards metabotropic glutamate receptors. The invention further relates to medicaments containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.

Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.

Abstract: An initiator system for radical polymerization, which comprises a combination of compounds of the formulae: