Abstract: The disclosure relates to a compound of formula (I): wherein m, n, Ar, and R are as defined in the disclosure, to compositions containing them and to their therapeutic use. The disclosure also relates to processes for preparing these compounds and to certain intermediate compounds.

Abstract: Compounds of Formula (I): wherein: A represents bond, C1-6alkyl or CH?CH—C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1? each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl;

Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.

Abstract: The invention relates to a nitrogen heterocycle compound of formula 1: Also disclosed are a method of synthesizing the compound and use of the compound for treating various diseases and conditions.

Abstract: Compounds of general formula (I) or general formula (II):— wherein R1, P1, P2, Q, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.

Abstract: The present application relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs that includes forming a compound of formula (VIII).

Abstract: The present invention relates to a time temperature indicator for indicating temperature change over time, comprising an immobilized enzyme and a substrate of the enzyme, wherein the reaction of the substrate catalyzed by the enzyme produces a reaction product in a time and temperature dependent manner and wherein the formation of the reaction product can be detected by monitoring a physical characteristic of the substrate and/or the product which is linked to its concentration. The invention further relates to a method of time temperature indication comprising the step of an enzyme-catalyzed reaction, a method of printing the enzyme-based time temperature indicator on a packaging material or a label, a printing ink or printing ink concentrate comprising components of the enzyme-based time temperature indicator and a packaging material or a label comprising the enzyme-based time temperature indicator.

Abstract: The present invention is directed to novel compounds of Formula (I) wherein the variables are defined as herein. The compounds of Formula (I) are useful as CRTH2 antagonists and as such would be useful in treating certain conditions and diseases, especially asthma, allergic asthma, allergic inflammation, rhinitis, allergic rhinitis or atopic dermatitis.

Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.

Abstract: The present invention relates to a new crystalline modification of 6-(4-chlorophenyl)-2,2-dmethyl-7-phenyl-2, S-dihydro-1H-pyrrolizin-S-ylacetic acid which is referred to as polymorph B. It has a peak in the solid state 13C-NMR spectrum (with adamantane as external reference standard; CH group d=29.45 ppm) in the range from 179.8 to 180.2 ppm and can be processed directly to a pharmaceutical formulation.

Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.

Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

Abstract: Disclosed are methods of modulating biosynthesis of Salinosporamide A and its analogs, which are useful in treating cancer, inflammatory conditions, and/or infectious disease. The methods involve, for example, genetic manipulation, selection of reagents in the fermentation feedstock, and selection of fermentation conditions.

Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; and R8 is C1-8-alkyl or C3-8-cycloalkyl.

Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.

Abstract: A diketopyrrolo-pyrrole compound according to Formula (I): wherein R1, R2, and R3 are independently selected from the group consisting of hydrogen, a halogen atom, a methyl group, an ethyl group, an tert.-butyl group, a phenyl group, a cyano group, and an acid group; R4—, R5, and R6 are independently selected from the group consisting of hydrogen, a halogen atom, a methyl group, an ethyl group, an tert.-butyl group, a phenyl group, and a cyano group; and wherein one of R7 and R8 is a group including two acid functions while the other one of R7 and R8 represents hydrogen. Pigment dispersions, methods for forming pigment dispersions, and use of the diketopyrrolo-pyrrole compound may include Formula (I).

Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.

Abstract: A family of N-substituted 3,4-alkylenedioxypyrrole includes monomers for of formula (I) electropolymerization to conjugated polymers and key intermediates for the preparation of the monomers. The preparation of the //-substituted 3,4-alkylenedioxypyrroles is carried out via a synthetic intermediate, an ester substituted dihydroxypyrrole. The synthetic method to prepare the //-substituted 3,4-alkylenedioxypyrrole intermediates and ultimately the N-substituted 3,4-alkylenedioxypyrrole monomers begins with a reaction to form the ester substituted dihydroxypyrrole.

Abstract: Compounds of Formulae I-VI and derivatives thereof having anti-cancer, anti-inflammatory, and anti-microbial properties and to compositions that include one or more of compounds and their derivatives or analogs having anti-cancer, anti-inflammatory and anti-microbial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating cancer, inflammatory conditions, and microbial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.

Abstract: Benzoimidazole and indole compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease and diseases involving matrix or cartilate degradation.

Abstract: The invention-provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.

Abstract: The invention relates to a diketopyrrolopyrrole pigment of formula (I) in which R10, R11, R12 and R13 independently of one another denote hydrogen, halogen, C1-C4-alkyl, C1-C4-alkoxy, cyano or phenyl, characterized by a first maximum of the frequency distribution (according to weight fractions) of the crystal sizes at or below 700 nm and at least one further maximum of the frequency distribution (according to weight fractions) of the crystal sizes which is at least 100 nm above the first maximum.

Abstract: Disclosed herein are analogs of Salinosporamide A, having the Formulae Ia-IVa as follows: Like Salinosporamide A, the compounds of the present invention will inhibit the proteasome, an intracellular enzyme complex that destroys proteins the cell no longer needs. Without the proteasome, proteins would build up and clog cellular machinery. Fast-growing cancer cells make especially heavy use of the proteasome, so thwarting its action is a compelling drug strategy.

Abstract: The present invention includes methods, articles, compositions and colorant dyes and pigments that include biocidal N-halamine dye composition having two or more heterocyclic ring structures attached to one or more N-halamine groups, wherein one or more halogens associate with the one or more one or more N-halamine groups to affect biocidal activity.

Abstract: Syntheses of a new blue EC monomer (ProDOT-MePro), and a new red EC monomer (ProDOP-Et2) are described. Two additional new types of EC monomers based on 3,4-alkylenedioxythiophene include fluorinated EC monomers and an EC monomer including silicon. EC polymer devices having more than one different color EC polymer to enable additional colors to be provided using subtractive color mixing are also described, as well as EC polymer devices incorporating a logo, image, or text, are generally obscured when the device is colored, but become visible when the device is not colored. Also described are EC polymer devices that include a cathodic EC polymer layer, a gel electrolyte, a counter electrode, and a reference electrode. Working prototypes of such devices exhibit significant increases in the speed of transition of the EC device from a colored state to a transparent state.

Abstract: There is provided compounds of formula I: wherein the dotted lines, U5 V5 X1, Y R1, R2 and R4 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.

Abstract: The invention is the discovery of an actinomycete genus, given the name Salinospora gen. nov., that displays an obligate requirement of seawater (Na+) for growth and unique 16S rRNA signature nucleotides. The invention is also the use of the genus for the production and discovery of active biomolecules such as pharmaceutical agents, agrichemicals, immunomodifiers, enzymes and enzyme inhibitors.

Abstract: Disclosed herein are analogs of Salinosporamide A, having the Formula I as follows: Like Salinosporamide A, the compounds of the present invention will inhibit the proteasome, an intracellular enzyme complex that destroys proteins the cell no longer needs. Without the proteasome, proteins would build up and clog cellular machinery. Fast-growing cancer cells make especially heavy use of the proteasome, so thwarting its action is a compelling drug strategy.

Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.

Abstract: The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.

Abstract: The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.

Abstract: Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq? is H or Rq and Rq? define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl- moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.

Abstract: The present invention relates to novel compounds suitable for or already radiolabelled with 18F, methods of making such compounds and use of such compounds for diagnostic imaging.

Abstract: A compound of the formula (II) wherein one of R1 and R2 is halo and the other is H or halo; R3 is —C1-C5 straight or branched chain, optionally fluorinated, alkyl or —CH2CR5C3-C4-Cycloalkyl; R4 is H; R5 is H, C1-C2 alkyl, C1-C2 haloalkyl, hydroxyl, OC1-C2alkyl, fluoro; R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle wherein the or each ring has 4, 5 or 6 ring atoms and 0 to 3 hetero atoms selected from S, O and N; Rb is haloalkyl; Rc is H or C1-C4 alkyl; and pharmaceutically acceptable salts, hydrates or N-oxides thereof have utility in the treatment of disorders characterised by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.

Abstract: Provided are muscarinic receptor antagonists, which can be useful in treating various diseases of the respiratory, urinary or gastrointestinal system mediated through muscarinic receptors. Also provided are processes for preparing compounds described herein, pharmaceutical compositions comprising compounds described herein, and methods for treating diseases mediated through muscarinic receptors.

Abstract: The present invention relates to a process for preparing a compound of formula I, wherein R1 is Pg1 or P1?; P1? is CO-hydrocarbyl; P2 is CH2, O or N-Pg2; and Pg1 and Pg2 are each independently nitrogen protecting groups; (i) reacting a compound of formula II with a dioxirane to form an epoxide of formula III; where X is selected from CN, CH2N3, CH2NH-Pg2, ONH-Pg2, NHNH-Pg2, N(Pg2)NH-Pg2; (ii) converting a compound of formula III to a compound of formula I

Abstract: A diketopyrrolo-pyrrole compound according to Formula (I): wherein R1, R2, and R3 are independently selected from the group consisting of hydrogen, a halogen atom, a methyl group, an ethyl group, an tert.-butyl group, a phenyl group, a cyano group, and an acid group; R4—, R5, and R6 are independently selected from the group consisting of hydrogen, a halogen atom, a methyl group, an ethyl group, an tert.-butyl group, a phenyl group, and a cyano group; and wherein one of R7 and R8 is a group including two acid functions while the other one of R7 and R8 represents hydrogen. Pigment dispersions, methods for forming pigment dispersions, and use of the diketopyrrolo-pyrrole compound may include Formula (I).

Abstract: The present invention relates to a process for the preparation of a mixture comprising at least two structurally different diketopyrrolopyrrole pigments of formula wherein A1 and A2 are each independently of the other an aromatic or heteroaromatic radical, by reacting a succinic acid ester with at least one unsubstituted or substituted aromatic or heteroaromatic nitrile, which process comprises carrying out the reaction in the presence of at least one compound of formula wherein A is an aromatic or heteroaromatic radical, R3 is hydrogen, halogen, methyl, methoxy, —CF3 or —CN, R4 is a linear or, from C3 upwards, optionally branched C1-C30alkyl, C6-C10aryl or C6-C24aralkyl radical, X is —S—, —O—, —CR5R5?—, —COO—, —CONR5—, —SO—, SO2—, —SO2NR5— or —NR5— and R5 and R5? are each independently of the other hydrogen or a linear or, from C3 upwards, optionally branched C1-C30alkyl, C6-C10aryl or C6-C24aralkyl radical, to the use of such a mixture in the colouring of organic material and in cosmetics, and a

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: The present invention relates to a process for the preparation of furopyrroles of general formula (I), comprising (a) heating a compound of the formula (II) under microwave irradiation optionally in the presence of an inert solvent, wherein A1 and A2 are C1-C18alkyl, C2-C18alkenyl, C2-C18alkynyl, C5-C8cycloalkyl, C5-C8cycloalkenyl, aryl or heteroaryl, A3 is hydrogen, C1-C18alkyl, cyanomethyl, Ar3, —CR30R31—(CH2)m—Ar3 or Y—R32, wherein R30 and R31 independently of each other stand for hydrogen or C1-C4alkyl, or phenyl which can be substitute up to three times with C1-C4alkyl, Ar3 stands for aryl, C5-C8 cloalkyl, C5-C8cycloalkenyl or heteroaryl, which can be substituted one to three times with C1-C8alkyl, C1-C8alkoxy, halogen or phenyl, which can be substituted with C1-C8alkyl or C1-C8alkoxy one to three times, and m stands for 0, 1, 2, 3 or 4, R is C1-C18alkyl, in particular C1-C4alkyl, aryl, in particular phenyl, or aralkyl, in particular benzyl, which can be substituted one to three times with C1-C8alkyl, C1

Abstract: Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The compounds of the invention are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

Abstract: Compounds are provided that act as potent modulators of one or more of the CCR1, CCR2 and CCR3 receptors. The compounds are generally fused-, spiro- or bridged-nitrogen heterocycles having an aryl and heteroaryl component and are useful in pharmaceutical compositions, methods for the treatment of CCR1-, CCR2- and/or CCR3-mediated diseases, and as controls in assays for the identification of competitive receptor antagonists for the above chemokine receptors.

Abstract: Compounds are provided that act as potent modulators of one or more of the CCR1, CCR2 and CCR3 receptors. The compounds are generally fused-, spiro- or bridged-nitrogen heterocycles having an aryl and heteroaryl component and are useful in pharmaceutical compositions, methods for the treatment of CCR1-, CCR2- and/or CCR3-mediated diseases, and as controls in assays for the identification of competitive receptor antagonists for the above chemokine receptors.

Abstract: A process for producing dichlorodiketopyrrolopyrrole pigment of the ? modification, which comprises wet milling crude dichlorodiketopyrrolopyrrole pigment wherein an ? modification and a ? modification coexist in the presence of a milling agent and a wetting agent, dichlorodiketopyrrolopyrrole pigment of the ? modification obtained the process and a color composition which contains the pigment and a pigment carrier.

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I

Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.

Abstract: Compounds of general formula (I) or general formula (II) wherein R1, P1, P2, Q, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.