Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.

Abstract: The present invention relates to a catalytic process for preparing 3-triazolyl sulphoxide derivatives in enantiomerically pure or enantiomerically enriched form.

Abstract: To provide a triazole compound which has remarkably excellent pesticidal activities.

Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: The present invention constitutes new 3-[1-(3-haloalkyl)triazolyl]phenyl sulphide derivatives of the formula (I) in which A1, A2, B0, B1, B2, B3, R1, R2 and n are as defined in the description, to their use as acaricides and insecticides for controlling animal pests, and to processes for preparing them.

Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: An aryl (1H-1,2,4-triazol-1-yl) compound is useful for producing a 3-(1H-1,2,4-triazol-1-yl)phenylsulfide compound (useful, e.g., as an insecticide). Also disclosed is a process for producing the compound. The aryl (1H-1,2,4-triazol-1-yl) compound is represented by the general formula (1), below, wherein R represents a C1-C6 alkyl group or a cyclic C3-C6 alkyl group; A1 represents a hydrogen atom, an amino group, a mono(C1-C6 alkyl amino group or a di (C1-C6 alkyl) amino group; A2 represents a halogen atom, a C1-C6 alkyl group or a cyclic C3-C6 alkyl group; and Z represents a hydrogen atom, a halo-sulfonyl group or a mercapto group.

Abstract: To provide a triazole compound which has remarkably excellent pesticidal activities.

Abstract: A process for production of a (1H-1,2,4-triazol-1-yl)benzene compound represented the general formula (5) [wherein R is a C1 to C6 alkyl group or a cyclic C1 to C6 alkyl group; A1 is a hydrogen atom, an amino group, a mono(C1 to C6 alkyl)amino group or a di(C1 to C6 alkyl)amino group; and A2 is a halogen atom, a C1 to C6 alkyl group or a cyclic C1 to C6 alkyl group], which comprises reacting a triazole compound represented by the general formula (2) (wherein A1 has the same definition as given above) with a phenylboronic acid compound represented by the general formula (3) (wherein R and A2 have the same definitions as given above) or a phenylboroxine compound represented by the general formula (4) (wherein R and A2 have the same definitions as given above) in the presence of a copper catalyst.

Abstract: The present invention relates to a catalytic process for preparing 3-triazolyl sulphoxide derivatives in enantiomerically pure or enantiomerically enriched form.

Abstract: An energetic ionic liquid catalytic decomposition gas generator uses stoichiometric and nonstoiciometric mixtures of specific energetic ionic liquids and iridium catalyst. The catalyst temperature used and gas production versus ignition may be controlled by combining one or more cationic species with one or more anionic species of the ionic liquid(s).

Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Abstract: To provide novel 3-triazolylphenyl sulfide derivatives having excellent soil treatment activity as insecticides, miticides or nematicides for agricultural and horticultural plants. 3-Triazolylphenyl sulfide derivatives represented by the formula [1]: wherein R is a cyclopropylmethyl group or a trifluoroethyl group, B2 is a hydrogen atom, a halogen atom or a methyl group, B4 is a halogen atom, a cyano group, a nitro group or a C1-C6 alkyl group, and each of A1 and A3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group which may be substituted or an amino group which may be substituted.

Abstract: An aryl (1H-1,2,4-triazol-1-yl) compound is useful for producing a 3-(1H-1,2,4-triazol-1-yl)phenylsulfide compound (useful, e.g., as an insecticide). Also disclosed is a process for producing the compound. The aryl (1H-1,2,4-triazol-1-yl) compound is represented by the general formula (1), below, wherein R represents a C1-C6 alkyl group or a cyclic C3 alkyl group; A1 represents a hydrogen atom, an amino group, a mono(C1-C6 alkyl amino group or a di(C1-C6 alkyl) amino group; A2 represents a halogen atom, a C1-C6 alkyl group or a cyclic C3 alkyl group; and Z represents a hydrogen atom, a halo-sulfonyl group or a mercapto group.

Abstract: This invention is directed to compounds of formula (I), wherein m, formula (II), R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.

Abstract: The invention provides a) a method for making improved ionic halide salts, e.g., 1-methyl-4-amino-1,2,4-triazolium iodide and b) a method for making energetic ionic salts, e.g., 1-methyl-4-amino-1,2,4-triazolium nitrate, in high yield and purity from triazolium precursors. Also provided are the resulting novel salts from the above methods.

Abstract: To provide novel 3-triazolylphenyl sulfide derivatives having excellent soil treatment activity as insecticides, miticides or nematicides for agricultural and horticultural plants. 3-Triazolylphenyl sulfide derivatives represented by the formula [1]: wherein R is a cyclopropylmethyl group or a trifluoroethyl group, B2 is a hydrogen atom, a halogen atom or a methyl group, B4 is a halogen atom, a cyano group, a nitro group or a C1-C6 alkyl group, and each of A1 and A3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group which may be substituted or an amino group which may be substituted.

Abstract: The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is a bond, a carbonyl group, a derivative of a carbonyl group, an ethylene group or an ethylenecarbonyl group, R1 is optionally substituted amino or hydroxy, and the substituents R2 to R6 have the meanings given in the specification, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to intermediates, to the use of a compounds of formula (I) as a medicament and for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.

Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is a bond, a carbonyl group, a derivative of a carbonyl group, an ethylene group or an ethylenecarbonyl group, R1 is optionally substituted amino or hydroxy, and the substituents R2 to R6 have the meanings given in the specification, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to intermediates, to the use of a compounds of formula (I) as a medicament and for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.

Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These 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, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: A compound of formula (I): compositions containing them and methods of use to control pests.

Abstract: New energetic salts of 1,2,4-triazole; 3,4,5-triamino-1,2,4-triazole and of 4-amino 1,2,4-triazole were synthesized, characterized and their thermal and safety properties evaluated as possible new propellant ingredients. Energetic anions, including the nitrate anion, NO3, the perchlorate anion, ClO4, & the dinitramide anion, N(NO2)2, were paired with the protonated heterocycles through facile, high yield synthetic routes to give crystalline, energetic salts. Using such a heterocycle system, either 1,2,4-triazole; 3,4,5-triamino-1,2,4-triazole or 4-amino 1,2,4-triazole, a new family of salts were synthesized through the direct reaction of the heterocycle with the corresponding acid form of the desired anion. These reactions were carried out in commonly available polar solvents, and at ambient temperatures, to give high purity, high yield products.

Abstract: The present invention relates to a process for the preparation of products of formula (1): in which R denotes H or an alkyl group containing from 1 to 10 carbon atoms, it being possible for this alkyl group to be substituted by one or more aryl, heteroaryl, hydroxyl or alkenyl groups, in which process hydrazine is reacted with a deficiency of carboxylic acid RCOOH and then the water of reaction and optionally the water of dilution of the hydrazine and of the acid is removed. It is particularly useful for preparing 4-amino-1,2,4-triazole.