Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.

Abstract: The present invention is aimed at a process for the preparation of compounds of the general formula (I). The objective process is in this case based on the Michael reaction of compounds of the general formula (III) with compounds of the general formula (IV), with subsequent hydrogenation and cyclization of the intermediates of the formula (II) obtained.

Abstract: The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.

Abstract: The present invention provides for a process for preparing the pyrrole compounds of Formula Va and Vb.

Abstract: ?-crystalline form of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful as inhibitors of angiotensin I converting enzyme.

Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.

Abstract: The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.

Abstract: This invention relates to novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1]octane useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: Benzenesulfonamide derivative compounds corresponding to the general formula (I): and their pharmaceutically acceptable addition salts; a process for preparation of such compounds; pharmaceutical compositions containing such compounds, and the use of such compounds as a pharmacologically active substance, in particular in the treatment of neurodegenerative diseases, cardiovascular diseases, inflammatory diseases; hypercholesterolemia, and diabetes.

Abstract: The invention relates to a coordination complex system comprising a ligand having the formula: R1—SO2—NH—P (XR2)2 (1a); or R1—SO2—N?PH (XR2)2 (1b); or R1—SO(OH)?N—P(XR2)2 (1c); wherein X is independently O, S, NH, or a bond; R1 and R2 are independently selected from hydrogen and substituted or unsubstituted alkyl or aryl; wherein at least one equivalent of the ligand is complexed to an equivalent of a metal selected from a transition metal and lanthanide. The invention also relates to the use of said coordination complexes as catalysts in the hydroformylation, hydrogenation, transfer hydrogenation, hydrocyanation, polymerization, isomerization, carbonylation, cross-coupling, metathesis, CH activation, allylic substitution, aldol condensation, or Michael addition.

Abstract: Compounds of formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.

Abstract: The present invention relates to the preparation of ramipril (formula [1]) from unprotected (2S,3S,6S)-octahydrocyclopenta[b]pyrrole-2-carboxylic acid and to a method for preparing unprotected (2S,3S,6S)-octahydrocyclopenta[b]pyrrole-2-carboxylic acid.

Abstract: The present invention relates to new salts of perindopril, particularly to a new calcium salt and new amine salts of perindopril, to a process for their preparation and to a pharmaceutical formulations containing the new salts.

Abstract: The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (?)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.

Abstract: The present invention relates to C. I. Pigment Red 254 for coloring, which can color an object to be colored so as to have a higher chroma than that with conventional technology and a production method for easily producing it. For the purpose, the inventors provide the production method for the pigment, wherein the intersection of mass tone ?H* and ?C* of a color coating film in an acrylic-melamine coating test is, on X-Y coordinate plane to which the ?H* is defined as the X-axis and the ?C* is defined as the Y-axis, within the surrounded region determined by specific three equations; and a production method for the pigment provides the production method of the pigment, including a process of heating crude pigment at 100-130° C. for 2-10 hours in an aprotic polar organic solvent which is strongly alkaline.

Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

Abstract: The present invention relates to a compound of the formula (I) wherein R1 is H, C1-C6-alkyl which may be substituted by C3-C6-cycloalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alk

Abstract: The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.

Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

Abstract: The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.

Abstract: Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula (I) or (III) The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds. Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl), inhibiting Wnt signaling.

Abstract: The present invention relates to an enzyme substrate for detecting nitroreductase activity of formula (I) below: in which X is S, NX1, O or NX1-CO; R1 is nothing or a substituent selected from Cl, CH3, Br, F, I, alkyl, aryl and carboxyl; R2 is nothing or a substituent selected from Cl, O—CH2—O, O—CH3, F, diethylenediamine-CH3, NR3R4, Br, I, alkyl, aryl, carboxyl, NO2 and R3 and R4 are independently H or an alkyl group containing from 1 to 4 carbon atoms; and X1 is selected from H, CH3, C2H4Ph, OH, alkyl and aryl.

Abstract: N-(benzenesulphonyl)-2,3-dihydro-1H-indols, wherein the indol is substituted by cyano, carboxy or alkylcarbonyloxy and their use as therapeutical agents.

Abstract: The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.

Abstract: The present invention is concerned with novel processes for the preparation of (+)-1-aryl-3-azabicyclo[3,10]hexanes or a pharmaceutically acceptable salt thereof, and (?)-1-aryl-3-azabicyclo[3,10]hexanes or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., pain, depression, anxiety disorders, eating disorders and urinary incontinence.

Abstract: The invention relates to a bicycloazaheterocyclyl carboxylic acid sulfonamide derivative of formula I herein, pharmaceutical preparation comprising it, process for preparing it and method for its pharmaceutical use.

Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

Abstract: The invention provides peptide synthons having protected functional groups for attachment of desired moieties (e.g. functional molecules or probes). Also provided are peptide conjugates prepared from such synthons, and synthon and conjugate preparation methods including procedures for identifying the optimum probe attachment site. Biosensors are provided having environmentally sensitive dyes that can locate specific biomolecules within living cells and detect chemical and physiological changes in those biomolecules as the living cell is moving, metabolizing and reacting to its environment. Methods are included for detecting GTP activation of a Rho GTPase protein using polypeptide biosensors. When the biosensor binds GTP-activated Rho GTPase protein, the environmentally sensitive dye emits a signal of a different lifetime, intensity or wavelength than when not bound.

Abstract: Disclosed are two new crystalline forms, ? and ?, of perindopril erbumine. Those forms are suitable as therapeutic active substances for medicaments for the treatment of cardiovascular diseases, especially high blood pressure and heart failure. The ? crystalline form is obtained in the crystallisation of perindopril erbumine at from 30 to 45° C., preferably from 34 to 45° C., from MTBE containing from 1.5 to 2.5% (v/v) water; the crystallisation is advantageously carried out with stirring. If the water is then removed, advantageously by azeotropic distillation, preferably at from 35 to 37° C., and stirring is then continued for at least 15 h at from 30 to 45° C., preferably from 35 to 37° C., the ? crystalline form is converted to the ? crystalline form. The ? crystalline form can also be obtained by stirring the ? or ? crystalline form at from 33 to 38° C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the ? crystalline form.

Abstract: The present invention relates to a novel method for obtaining (2S,3aS,6aS)-1-[(S)-2-[[(S)-1-(ethoxycarbonyl)-3-phenylpropyl]-amino]propanoyl]octahydro cyclopenta[b]pyrrole-2-carboxylic acid, viz. Ramipril(I) in high optical purity, free of other stereoisomers, and in high bulk density. The present invention also relates to a novel hydrated form of Ramipril(I) and a process for preparation thereof.

Abstract: There are disclosed bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X and n are defined herein.

Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands, Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid (“D-DTTA”) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt (“L-DTTA”) in a high enantiomeric excess. This invention also provides for a process for preparing a (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (“D-DBTA”) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (“L-DBTA”) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.

Abstract: The present invention relates to a process for preparing nitrooxy esters, nitrooxy thioesters, nitrooxy carbonates and nitrooxy thiocarbonates of compounds having at least an hydroxyl or thiol functional group, according to the following reaction scheme The invention also relates to intermediates useful in said process and to their preparation.

Abstract: The present invention relates to new hydroxyadamantyl inhibitors of dipeptidylpeptidase IV activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: To provide an optical recording medium on which recording/retrieving of high density optical information is possible by a short wavelength light such as a blue laser. An optical recording medium comprising a substrate and a recording layer capable of recording or retrieving information by irradiation with light, formed on the substrate, wherein the recording layer contains the cyanine dye represented by the following formula (I): wherein each of A1 and B1 which are independent of each other, is an aromatic ring which may have a substituent, provided that at least one aromatic ring of A1 and B1 contains a nitrogen atom; each of R1 and R2 which are independent of each other, is a substituent, provided that R1 and/or R2 may be bonded to other cation; each of X1, X2, X3 and X4 which are independent of one another, is an organic group, provided that a pair of X1 and X2, and/or a pair of X3 and X4, may be mutually bonded to form a cyclic structure; Y1 is a hydrogen atom or an organic group; and Z is an anion.

Abstract: Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.

Abstract: The invention provides novel compounds useful as intermediates for the production of polymethine compounds containing a desired counter ion with high purity and in high yields. Thus provided are polymethine ether compounds of the general formula (I) given below and a method of producing polymethine compounds which comprises bringing those compounds into contact with an acid. In the above formula, R represents an alkyl group, an alkoxyalkyl group or an aryl group which may optionally be substituted, R1 and R2 each independently represents a hydrogen atom, halogen atom, nitro group, alkyl group, alkoxyalkyl group, alkoxy group or alkoxyalkoxy group and R1 and R2 may be bound to each other to form a ring; R3 represents an alkyl group, which may optionally be substituted; L is an alkylene group required for the formation of a ring structure; and X represents a hydrogen atom, halogen atom, alkoxy group, aryloxy group, alkylthio group, arylthio group or substituted amino group.

Abstract: The present invention is directed to certain hydroxymethyl ether hydroisoindoline 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, LUTS, depression, and anxiety.

Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

Abstract: The invention relates to nitric oxide donor compounds and their use for treating cardiovascular diseases, inflammation, pain, fever, gastrointestinal disorders, ophthalmic diseases, hepatic disorders, renal diseases, respiratory disorders, immunological diseases, bone metobolismsdysfunctions, central and peripheral nervous system diseases, sexual dysfunctions, infectious diseases, for the inhibition of platelet aggregation and platelet adhesion, for treating pathological conditions resulting from abnormal cell proliferation, vascular diseases. The invention also relates to compositions comprising at least one nitric oxide releasing compounds of the invention and composition comprising at least one nitric oxide releasing compounds according to the invention and at least one 15 therapeutic agent.

Abstract: The present invention provides novel C-linked cyclic compounds and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

Abstract: The present invention relates to (1S,6R)-6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane, pharmaceutically acceptable salts, prodrugs or solvates thereof; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

Abstract: The present disclosure provides substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, wherein A, M, M?, and R5 are as described herein, and to biocatalytic processes for their preparation, and to the enzymes used in those processes.

Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

Abstract: A process for preparing perindopril (III) or a pharmaceutically acceptable salt thereof, which process comprises a substituted benzyl ester of (2S,3aS,7aS)-octahydroindole-2-carboxylic acid (I) with N—[(S)-carbethoxybutyl]-(S)-alanine (II) where R represents a halo, C1-4 alkoxy or nitro substituent.

Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.