Abstract: The present invention relates to compounds of formula I wherein R1, R2 and R3 are defined herein, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.

Abstract: Novel VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridones and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are selected.

Abstract: A pesticidal composition comprising a pesticidally effective amount of at least one of a pyridic compound of the formula (I) or it salt and at least one of other pesticides: wherein Y is a haloalkyl group, m is 0 or 1, and Q is or a substituted or unsubstituted heterocyclic group, (wherein X is an oxygen atom or a sulfur atom, R1 and R2 are respectively independently a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted cycloalkyl group, and the like.

Abstract: The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (a

Abstract: Novel pyraole derivatives of formula (I), wherein: X is oxygen or sufu, R1 is C1–C3alkyl, C1–C3haloalkyl, C1–C3alkoxy-C1–C3alkyl or C1–C3haloalkoxy-C1–C3alkyl; R2 is C1–C3haloalkyl; and R3 is halogen. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.

Abstract: Fungicidal compounds of the general formula (I): wherein X and Y are independently H, halo, C1-8 alkyl, C3-6 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 alkoxy, C1-8 alkylthio, nitro, amino, mono- or di-(C1-6)alkylamino, mono- or di-(C2-6)alkenylamino, mono- or di-(C2-6)alkynylamino, formylamino, C1-4 alkyl(formyl)amino, C1-4 alkylcarbonylamino, C1-4 alkyl(C1-4 alkylcarbonyl)amino, cyano, formyl, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-4)alkylaminocarbonyl, carboxy, C1-4 alkylcarbonyloxy, aryl(C1-4)alkylcarbonyloxy, C1-4 alkylsulphinyl, C1-4 alkylsulphonyl, C1-4 alkylsulphonyloxy, aryl, heteroaryl, aryloxy, arylthio, heteroaryloxy or heteroarylthio wherein any of the foregoing alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, groups or moieties are optionally substituted; R1 is phenyl, cyano, C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl in which the alkyl, alkenyl and alkynyl groups are optionally substituted on their terminal carbon atom with one, two or three halogen atoms,

Abstract: This invention is directed to methods of using a compound of the formula and pharmaceutically acceptable salts thereof, wherein n, X, R1 and R2 are disclosed herein, for treating inflammatory events in an animal subject.

Abstract: A Vpr function regulating composition useful in the treatment of subjects infected with HIV or having AIDS, wherein the composition comprises an aminostilbazole derivative represented by the following formula [1] or a salt thereof as an active ingredient: A-B-D-E[1] wherein A represents heteroaryl or an oxide thereof, B represents ethenylene, D represents phenylene, and E represents the formula: —N(R)—SO2-G wherein G represents phenyl, R represents hydrogen, alkyl, or —COR0 (R0 represents alkyl, alkoxy, aryloxy, 5- to 6-membered heteroaryl, heteroarylmethyl, aminoalkylene, or cyclic amino alkylene)or the like.

Abstract: Disclosed are compounds of formula X, which are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.

Abstract: Methods for treating cardiovascular and related diseases such as arrhythmia are described. The methods are directed to concurrently administering a compound such as pyridoxal-5?-phosphate, pyridoxamine, pyridoxal, or a 3-acylated pyridoxal analogue with a therapeutic cardiovascular compound.

Abstract: 2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5?-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent effects of lowering ocular tension, promoting blood flow in retina, and protecting optic nerve failure and are highly soluble in water. Owing to these characteristics, the compounds are useful as drugs such as remedies for glaucoma and ocular hypertension.

Abstract: The invention relates to compounds of formula I

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: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.

Abstract: Methods for treating cardiovascular and related diseases such as blood clots are described. The methods are directed to concurrently administering a compound such as pyridoxal-5?-phosphate, pyridoxamine, pyridoxal, or a 3-acylated pyridoxal analogue with a therapeutic cardiovascular compound.

Abstract: The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.

Abstract: Methods for treating cardiovascular and related diseases such congestive heart failure are described. The methods are directed to concurrently administering a compound such as pyridoxal-5?-phosphate, pyridoxamine, pyridoxal, or a 3-acylated pyridoxal analogue with a therapeutic cardiovascular compound.

Abstract: Methods for treating cardiovascular and related diseases such as ischemia, ischemia reperfusion injuries, and myocardial ischemia, are described. The methods are directed to concurrently administering a compound such as pyridoxal-5?-phosphate, pyridoxamine, pyridoxal, or a 3-acylated pyridoxal analogue with a therapeutic cardiovascular compound.

Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.

Abstract: The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.

Abstract: The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.

Abstract: A method for treating diabetic neuropathy is disclosed consisting of administering pyridoxamine or a salt thereof.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: A compound of the formula: wherein R1 and R2 each is H or a hydrocarbon group which may be substituted, or R1 and R2 form a 3- to 8-membered carbo or heterocyclic ring which may be substituted; R3 is H, a lower alkyl which may be substituted or an aromatic group which may be substituted; R4 is (1) an aromatic group which may be substituted, (2) an aliphatic hydrocarbon group substituted by an aromatic group which may be substituted, which hydrocarbon group may be further substituted or (3) an acyl; X and Y each is oxygen or sulfur which may be oxidized; and ring A is a benzene ring which may be further substituted, or a salt thereof, is useful for an agent for suppressing neurodegeneration.

Abstract: The present invention provides a pharmaceutical composition for use as a Th2 differentiation inhibitor comprising a compound represented by Formula (I): wherein each of ring A, ring B and ring C is an aromatic carbocyclic ring, a heterocyclic ring and the like, X is a single bond, —O—, —CH2—, —NH—, —SO— and the like, Y is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl and the like, each of V1 and V2 is a single bond, —O—, —NH—, —OCH2— and the like, a prodrug, pharmaceutically acceptable salt or solvate thereof.

Abstract: Peptido and peptidomimetic compounds of the formula: wherein the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also provided.

Abstract: The invention relates to novel stilbene compounds having the general formula (I): as well as to pharmaceutical compositions for use in human or veterinary medicine, including dermatological, rheumatic, respiratory, cardiovascular and ophthalmic conditions and cosmetic compositions and methods of use thereof.

Abstract: The present invention relates to an excellent remedial agent for chronic rheumatoid arthritis, comprising an aminostilbazole derivative represented by the following formula [1] or a salt thereof as an active ingredient: A-B-D-E??[1] Wherein A represents heteroaryl or an oxide thereof, B represents ethenylene, D represents phenylene, E represents the formula: —N(R)SO2—G [wherein G represents phenyl, R represents hydrogen, alkyl, or —COR0 (R0 represents alkyl, alkoxy, aryloxy, 5- to 6-membered heteroaryl, heteroarylmethyl, aminoalkylene or cyclicaminoalkylene) or the like].

Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.

Abstract: A compound selected from those of formula (I): wherein: p represents an integer of from 0 to 6 inclusive, n represents an integer of from 0 to 6 inclusive, R1, and R2 represent a group selected from hydrogen, alkyl, aryl and arylalkyl, or R1+R2 form together with nitrogen carrying them saturated, monocyclic, or bicyclic system, X represents a group selected from oxygen, sulphur, a group —CH?CH—, methylene, a group of formula —HC?N—O— and a group of formula —O—CH2—CH?CH—, in which groups oxygen is linked to Y of the compounds of formula (I), Y represents a group selected from aryl, heteroaryl, arylalkyl, heteroarylalkyl, —C(O)-A, and —C(S)-A, A represents a group selected from alkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, and NR3R4 wherein R3, and R4 represent a group selected from hydrogen, alkyl, aryl, and arylalkyl, or R3+R4 form together with nitrogen carrying them monocyclic, or bicyclic (C3-C10) system, its isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, a

Abstract: This invention relates generally to N-cycloalkylglycines of the Formula (I): or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits including the same, methods for using the same for treating viral infection or an assay standards or reagents, and intermediates and processes for making the same.

Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.

Abstract: 2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5?-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent effects of lowering ocular tension, promoting blood flow in retina, and protecting optic nerve failure and are highly soluble in water. Owing to these characteristics, the compounds are useful as drugs such as remedies for glaucoma and ocular hypertension.

Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: Phenylalanine derivatives of formula (1) are described: wherein L1 is a linker atom or group; X1 is a group selected from —N(R3)CO—, —N(R3)SO2—, —N(R3)C(O)O— or —N(R3)CON(R3a)—; and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of a 4 integrins to their ligands and are of use in the prophylaxis and treatment of diseases or disorders involving inflammation.

Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula I: It has been surprisingly discovered that the pharmaceutical composition of the present invention is effective for the treatment of increased urge to urinate or urinary incontinence. Also disclosed are methods of treatment using the pharmaceutical compositions.

Abstract: The present invention provides novel heterocyclic amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A, B and Z are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said heterocyclic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment or prevention of of heparin induced thrombocytopenia (HIT, stroke, and ischemia, and in the treatment of symptoms thereof. The the pyridoxal and pyridoxine analogues can be used in neuroprotection.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: Compounds of general formula (I): where A, E, G, X, Y and the bond - - - take various meanings are of use in the preparation of a pharmaceutical formulation, for example in the treatment of a disease in which GSK-3 is involved, including Alzheimer's disease or the non-dependent insulin diabetes mellitus, or hyperproliferative disease such as cancer, displasias or metaplasias of tissue, psoriasis, arteriosclerosis or restenosis.

Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.

Abstract: The present invention relates to a class of compounds represented by the Formula 1. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula 1, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or the &agr;v&bgr;5 integrin.

Abstract: A composition for accelerating the disposal of ethanol from bodily fluid. Certain additives can accelerate the metabolic oxidation of ethanol, and others in addition act as catalysts or “pseudo” enzymes for the oxidation. Additives include the oxidant Nicotinamide Adenine Dinucleotide and a variety of other additives such as transition metal ions and complexes thereof which favor the oxidation reaction. The compositions described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.

Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.

Abstract: This invention relates to new RAR selective retinoid agonists of formula I wherein the symbols are as defined in the specification to their pharmaceutically acceptable salts, individual isomers or to a racemic or non-racemic mixture; to pharmaceutical compositions containing them, and to methods for their use as therapeutic agents.

Abstract: The present invention generally relates to an assay for identifying inhibitors of Human Papillomavirus (HPV), comprising: a) contacting a HPV E2 transactivation domain with a probe to form a E2:probe complex and measuring a signal from said probe to establish a base line level; b) incubating the E2:probe complex with a test compound and measuring the signal from said probe; c) comparing the signal from step b) with the signal from step a); wherein said probe is a compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein R1, A, X, W, Y, R3 and R4 are as defined herein; or a derivative thereof, wherein said derivative is a probe of formula (I) labeled with a detectable label or an affinity tag, wherein wavy lines represent bonds of unspecified stereochemistry; and wherein said signal is selected from: fluorescence, resonance energy transfer, time resolved fluorescence, radioactivity, fluorescence polarization, change in the intrinsic spectral properties, luminescence

Abstract: The present invention relates to compositions comprising various vitamins and minerals and methods for using these compositions for nutritional supplementation in, for example, pregnant or lactating subjects.

Abstract: The invention relates to compounds of formula I

Abstract: The present invention provides an AP-1 activation inhibitor, a NF-kappaB activation inhibitor, an inflammatory cytokine production inhibitor, a production inhibitor for matrix metalloprotease or an inflammatory cell adhesion factor expression inhibitor, which contains a heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient.