Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(?O) or formula C(?O)NH(OH); R1 represents hydrogen, methyl or trifluromethyl, or except when Z is a radical of formula —N(OH)(?O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1–C6) alkyl or phenyl(C1–C6)alkyl-; and R5 and R6 are as defined in the specification.

Abstract: Compounds that may be used to inhibit histone deacetylase having the formula Z-Q-L-M or Z-L-M wherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0–10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.

Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: The present invention relates to N-methyl-substituted benzamidazole derivatives of formula (I): as defined in the specification; pharmaceutical compositions and methods of use thereof.

Abstract: Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.

Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.

Abstract: A compound represented by formula (IA) or (IIA): wherein R11, R12 and R13 each represents a hydrogen atom, an aliphatic hydrocarbon group, an aryl group or a heterocyclic group; L1 represents a connecting group; R11 and R12, R11 and L1 and R12 and L1 may each combine with each other to form a ring when possible; R14, R15, R16 and R17 each represents a hydrogen atom or a substituent; and R13 to R17 may each combine with each of R11 to R17 or L1 to form a ring when possible; wherein R13 to R17 and L1 have the same meaning as in formula (IA); Q represents an atomic group necessary for forming a 5-, 6- or 7-membered ring with N; and R13, R14, R15, R16 and R17 may each combine with each of R13 to R17, the connecting group L1 or the atomic group Q to form a ring.

Abstract: The present application describes cyclic diamino compounds, derivatives thereof, and pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.

Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.

Abstract: Compounds of general formula (I), are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain

Abstract: This invention relates to a family of benzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy, asthma, or any diseases where IgE is pathogenic.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F1F0 ATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.

Abstract: This invention relates to a family of phenylbenzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.

Abstract: The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1? converting enzyme and other cysteine proteases in the ICE family are described. In one embodiment, the compound is described by the generalized structure: and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof. In addition, methods of treating stroke, inflammatory diseases, septic shock, repurfusion injury, Alzheimer's disease, and shigellosis, using a compound of the invention or a pharmaceutical composition thereof, are described.

Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.

Abstract: A 2-iminoimidazole derivative represented by the formula: 1

Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

Abstract: The present invention relates to compounds according to the general formula (I), wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B, C and D are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.

Abstract: The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to benzimidazole molecules that are cellular proliferation inhibitors and thus are useful as anticancer agents.

Abstract: The invention relates to compounds of general formula (I), in which A, X, Y and R1 are delined in claim 1. These compounds may be used in the treatment of pathologies associated with insulin resistane syndrome.

Abstract: The present invention relates to acylamino-substituted heteroaromatic compounds of formula I, 1

Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.

Abstract: Compounds of the formula I or II and their tautomeric forms, possible enantiomeric and diastereomeric forms, possible cistrans isomers on the rings in A and prodrugs thereof, pharmaceutical compositions containing these compounds and methods of treating neurodegenerative diseases or neuronal damage with these compounds.

Abstract: Compounds characterized generally as imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension.

Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.

Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N, and S, etc.; A is 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl; etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.

Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.

Abstract: An antibiotic additive and an ink composition including the antibiotic additive include a compound produced by binding of an antibiotic substance having the following formula (I) to a predetermined additive via a chemical reaction. The ink composition includes a colorant, a solvent and an antibiotic additive produced by binding of an antibiotic substance having the following formula (I) to a predetermined additive via a chemical reaction. The antibiotic additive prevents surface dry, improves storage stability and inhibits propagation and growth of bacteria in an ink and has excellent compatibility with a general dye or pigment.

Abstract: The invention relates to methods of synthesizing libraries of diverse and complex 2-substituted azole compounds of the general formula (I) or (II) wherein X, R2 and the ring components are as described herein, novel intermediates useful for synthesizing such substituted azole compounds and methods for identifying and isolating the compounds.

Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented.

Abstract: Disclosed are compounds of the formula: 1

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.

Abstract: Benzoic acid derivatives of the formula where X is oxygen, sulfur, —NH, —NR1, —N—CN, —N—OR1 or —N—NO2; Y is a single bond, —C═C—, or —NH; R1 is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclo, or (heterocyclo)alkyl; and R2 is aryl or heterocyclo. The compounds of formula I are useful in the treatment of arrhythmia.

Abstract: The invention relates to a write-once optical data carrier in which organic and/or inorganic light-absorbing compounds are used as the information layer, especially for high-density optical data carriers which function with a blue laser in the wavelength range of 360-460 nm. The invention also relates to the application of the above-mentioned light-absorbing compound to a suitable substrate (especially polycarbonate), e.g. by spin coating.

Abstract: Heterocyclically substituted benzoylguanidines of the formula I in which the substituents R(1) to R(4) have the meanings indicated in the claims. These compounds I are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment, and also for the treatment of angina pectoris. They also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias.

Abstract: Provided, among other things, is a compound of the formula:

Abstract: The subject invention provides useful and novel calcium channel blockers based upon mibefradil. The subject invention also provides methods for synthesizing the compounds of the invention. The invention also provides methods for the control or prevention of hypertension, angina pectoris, ischemia, arrhythmias, and cardiac insufficiency in a patient by administering a compound, or composition, of the invention to an individual in need of such treatment.

Abstract: The use of compounds of the formula I in which R1 and R2 are identical or different, electron-withdrawing radicals chosen from the group consisting of cyano, alkyl- or arylcarbonyl, alkyloxy- or aryloxycarbonyl and optionally substituted aminocarbonyl, R3 is a hydrogen atom, a C1-C20-alkyl radical or a C3-C20-cycloalkyl radical or a radical of the formula —CH2—CH2—SO3—M+, where M+ is a cation, X is the divalent radical of oxygen, sulfur or the radical where R3 is as defined above, is the divalent radical of the formula II or III, which forms a fused system with the radical of the formula I where R4 can be bonded one or more times to the benzylidene ring I or naphthylidene ring II, and is hydrogen, alkyl, cycloalkyl, alkyloxy, cycloalkyloxy, alkoxycarbonyl, mono- or dialkylaminocarbonyl, alkylamino, dialkylamino, each having up to 20 carbon atoms, and also cyano, amino and SO3—M+, where M+ is a cation,

Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formula

Abstract: The &agr;-substituted carboxylic acid derivatives having the formula (I): wherein R1 is an alkyl group, etc., R2 is a hydrogen atom, etc., R3 is a hydrogen atom, etc., A is ═CH-group, etc., B is an oxygen atom, etc., W1 is a C1-C8 alkylene group, W2 is a single bond or a C1-C8 alkylene group, X is a hydrogen atom, etc., Y is an oxygen atom, etc., and Z1 is an alkoxy group, etc., and pharmacologically acceptable salts, esters and amides thereof are useful for treatment and/or prevention of diabetes mellitus, impaired glucose tolerance, gestational diabetes mellitus, or the like. Some of the derivatives of the formula (I) are novel compounds.

Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein; A is N or CH; R1 and R2 represents hydrogen or lower alkyl; G, R3, R4, R5, R6, R7 and R8 are variables defined herein. These compounds are modulators of CRF receptors and are therefore useful for treating affective disorders, anxiety, depression, eating disorders, and stress disorders in humans and other animals. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

Abstract: The present invention relates to a novel blocked phenylenediamine developer useful, in reactive association, for enabling, on development, a non-magenta color, for example a cyan color, from a dye-forming coupler. In one embodiment, the developer has the property that the dye color formed with the coupler is distinctly different from the color formed by the same coupler with an oxidized form of the conventional developer 4-(N-ethyl-N-2-hydroxyethyl)-2-methylphenylenediamine. The invention is also directed to a light-sensitive silver-halide color photographic element comprising the blocked developing agent according to the present invention.

Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonists, 1