Abstract: The present invention relates to the use of aminoazoline and urea derivatives for com-bating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds and to specific azoline and urea derivatives.

Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.

Abstract: The present invention relates to new pharmaceutical uses of an isoxazolic derivative or a pharmaceutically acceptable salt thereof in the preparation of a medicament useful for treating the neuropathic pain.

Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;

Abstract: The present invention provides a method for treating or preventing one or more types of migraines by administering a monoamine oxidase inhibitor, preferably isocarboxazid, in a rapid-release formulation. The present invention also provides a pharmaceutical composition suitable for treating or preventing migraines and having at least one monoamine oxidase inhibitor.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR.

Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.

Abstract: Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.

Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl or the like, One of R2 and R3 is a group of the formula: —C(?O)—Y—R4, wherein Y is —NR9— or the like, R4 is optionally substituted cycloalkyl or the like, R9 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, The other is a group of the formula: —V—R5, wherein V is a bond, —O— or the like, R6 is hydrogen or optionally substituted alkyl, R5 is hydrogen, optionally substituted alkyl or the like, X is a bond, —S—, —SO— or the like, U is a bond or optionally substituted alkylene, R7 is hydrogen or optionally substituted alkyl, Z is —S—, —O— or —NR8—, R8 is hydrogen, optionally substituted alkyl or the like.

Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments

Abstract: A fungicidal compound of formula (1): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by groups R7, R8 and R9; R1 is hydrogen, optionally substituted (C1-4)alkylC(?O), optionally substituted (C1-4)alkylC(?O)O, optionally substituted (C1-4)alkoxy(C1-4)alkyl, optionally substituted allyl, optionally substituted propargyl or optionally substituted allenyl; R2, R3, R4and R5 are each, independently, hydrogen, halogen, optionally substituted (C1-4)alkoxy(C1-4)alkoxy or optionally substituted (C1-4)alkoxy(C1-4)alkyl; R6 is an organic group containing three to thirteen carbon atoms and at least one silicon atom and, optionally, one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, and is optionally substituted by one to four independently selected halogen atoms; R7, R8 and R9are each, independently, hydrogen, halogen, C1-3alkyl, C1-3haloalkyl, C1-3alkoxy(C

Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).

Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.

Abstract: A compound of Formula 1: A-C(O)-Cy, wherein A is a diazabicyclic core, containing 7, 8, or 9 ring atoms, and selected from the following: 2,6-diazabicyclo[3.2.0]heptane; 3,6-diazabicyclo[3.ZO]heptane; 2,7-diazabicyclo[4.2.0]octane; 3,7-diazabicyclo[4.2.0]octane; 3,8-diazabicyclo[4.2.0]octane; 2,7-diazabicyclo[3.3.0]octane; 2,7-diazbicyclo[4.3.0]nonane; 2,8-diazbicyclo[4.3.0]nonane; 3,7-diazabicyclo[4.3.0]nonane; 3,8-diazabicyclo[4.3.0]nonane; 3,9-diazabicyclo[4.3.0]nonane; 2,6-diazabicyclo[3.2.1]octane; 3,6-diazabicyclo[3.2.1]octane; wherein the diazabicycle is attached as a radical to the depicted carbonyl via either one of the two ring nitrogen atoms, such that the carbonyl forms an amide bond with the ring nitrogen; Cy is a heteroaryl group; The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?402 subtype in the central nervous system (CNS).

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).

Abstract: A process for preparing isoxazole compounds of formula I: in which a nitroaryl of the formula (II): is contacted with an alkyl acetoacetate of the formula (III) or a salt thereof: in the presence of an activating agent and a base to provide the isoxazole compound.

Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.

Abstract: Compounds of formula I and IV are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorder: wherein the variables A-B, R1, R2, m, and Q are described herein.

Abstract: Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): wherein A is any one of the following groups (i) and (ii): (i) —CO—B— wherein B is a C1-6 alkylene group and (ii) —CO—Ba— wherein Ba is a C2-6 alkenylene group, and include optical isomers and salts of the compounds.

Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.

Abstract: The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.

Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.

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

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

Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4, and X are as defined herein or to pharmaceutically acceptable acid addition salts thereof, with the exception of 4-methoxy-N-[2-oxo-2-(phenylamino)ethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[5-chloro-2-methoxyphenyl)amino]-2-oxoethyl]-N-benzamide, 4-methyl-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide, N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-methyl-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide and N-[2-[(2,4-dimethoxyphenyl)amino]-2-oxoethyl]-N-[(2-fluorophenyl)methyl]-benzeneacetamide. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.

Abstract: Compounds active on phosphodiesterase PDE4B are provided. Also provided herewith are compositions useful for treatment of PDE4B-mediated diseases or conditions, and methods for the use thereof.

Abstract: The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,

Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: The present invention relates to an isoxazoline derivative as an inhibitor against various caspases, a process for preparing the same, and a therapeutic composition for preventing inflammation and apoptosis comprising the same.

Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions: (I)

Abstract: The invention relates to a method of developing a main proteinase SARS inhibitor. Human coronaviruses are major causes of upper respiratory tract illnesses in humans, in particular, the common cold. Recent investigations have shown that a novel coronavirus causes the Severe Acute Respiratory Syndrome (SARS), a disease that is characterized by high fever, malaise, rigor, headache, non-productive cough or dyspnea, which is rapidly spreading. Within the scope of the invention, based on the structural analysis of the binding mode of the SARS Mpro enzyme, a group of prototype inhibitors is provided that acts as suitable drugs targeting a majority of viral infections of the respiratory tract, including SARS.

Abstract: The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula wherein R1, R2, R3, R4, and R5, and m are as defined herein and with their pharmaceutically acceptable acid addition salts. This class of compounds have high affinity and selectivity for GABA A ?5 receptor binding sites and therefore may be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

Abstract: Disclosed herein are isoxazole derivaties and uses thereof. Serving as agonists of Wnt, the isoxazole derivatives activate Wnt/?-catenin signaling and thus can be used in the treatment and prevention of diseases related to the signal transduction. Also, pharmaceutically acceptable salts of the isoxazole derivatives are disclosed.

Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.

Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

Abstract: The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.

Abstract: The present invention relates to screens for compounds that can induce stem cell differentiation. In addition, isoxazoles and sulfonyl hydrazones are identified as general classes of compounds that can induce differentiation of stem cells into cells of neuronal and cardiac fate, respectively.

Abstract: There is provided with a method for manufacturing an isoxazole derivative at a high yield and without discharging waste products, and a novel isoxazole derivative. An isoxazole derivative expressed by Formula (8) is produced by reacting a 1-alkyne compound expressed by Formula (7) with iron(III) nitrate in the presence of acetone or acetophenone: (where R1 is an alkyl, cycloalkyl, phenyl, or other such group); and (where R2 is a methyl or a phenyl).

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: Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R1, R3, Q, X and R4 are as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed.

Abstract: Liquid or semi-liquid pharmaceutical compositions for topically treating immune-mediated skin disorders such as psoriasis, eczema, acne, dermatitis, and skin cancer and methods of treating patients having such immune-mediated skin disorders using the compositions.

Abstract: The present invention relates to compounds and methods for inducing neuronal differentiation in normal neural stem cells and brain cancer stem cells. The methods may take place in vitro, such as in isolates from the adult mammalian brain, or in vivo. Compounds and methods described herein may find use in the treatment of neurodegenerative and psychiatric diseases, the repair and regeneration of the nervous system, and in treatment of neurologic malignancy.

Abstract: Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.