Abstract: In order to manufacture a higher yield of a 4-benzyl-1-methyl-6-oxabicyclo[3,2,0]heptane derivative, the present invention is a method for manufacturing a compound represented by General Formula (I) which includes a step for reducing a compound represented by General Formula (II) using a hydride-type reducing agent in an aprotic solvent having an amide bond.

Abstract: Tetrazol-5-yl- and triazol-5-yl-aryl compounds of the general formula (I) as herbicides are described. In this formula (I), X, Z, W and R are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B are N and CY. Q is cyanoalkylcarbonyl or isoxazolyl.

Abstract: The use of an aromatase blocker or an estrogen blocker is described in a method for increasing spermatogenesis and Seritolli cell function, and/or improving Leydig cell function, in order to to increase endogenous testosterone levels in a male mammal. The levels of active materials used are significantly lower than the levels of these materials used to treat female estrogen sensitive tumors.

Abstract: [PROBLEMS] The present invention provides a novel alkoxyimino derivative or a salt thereof, as well as to a pest control agent containing the derivative or salt thereof as an active ingredient, which shows an excellent pest control effect on a wide range of pests in the agricultural and horticultural field and is also capable of controlling resistant pests. [MEANS FOR SOLVING PROBLEMS] The novel alkoxyimino derivative is characterized by being represented by general formula [I] (in the formula, X, R1, R2 and Q are as defined in the specification) and the post control agent is characterized by containing as an active ingredient the alkoxyimino derivative or a salt thereof.

Abstract: An azole derivative according to the invention is represented by Formula (I), wherein each of Ra and Rb denotes a hydrogen atom, or a C1-C6 alkyl group, a C2-C6 alkenyl group or a C2-C6 alkynyl group; Ra and Rb may be substituted with Xa or Xb which is a halogen atom; each of na and nb denotes 0 or the number of Xa- or Xb-substituted hydrogen atoms among the hydrogen atoms in Ra or Rb; each Y denotes a halogen atom, a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C1-C4 alkoxy group, a C1-C4 haloalkoxy group, a phenyl group, a cyano group or a nitro group; m denotes 0 to 5; and A denotes a nitrogen atom or a methyne group. As a result, an azole derivative contained as an active ingredient in an agro-horticultural agent having an excellent controlling effect on diseases can be provided.

Abstract: Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided.

Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).

Abstract: To provide a novel 5-benzyl-4-azolylmethyl-4-spiro[2.4]heptanol derivative, a method for producing the same, and an agro-horticultural agent and an industrial material protecting agent containing as an active ingredient the abovementioned 5-benzyl-4-azolylmethyl-4-spiro[2.4]heptanol derivative. To be a 5-benzyl-4-azolylmethyl-4-spiro[2.4]heptanol derivative represented by Formula (I): wherein X denotes a halogen atom, a C1-C5 alkyl group, a C1-C5 haloalkyl group, a C1-C5 alkoxy group, a C1-C5haloalkoxy group, a phenyl group, a cyano group or a nitro group; n denotes an integer of 0 to 5; when n is not less than 2, Xs may be the same or different; R1, R2, R3, R4 each independently denotes a hydrogen atom, a halogen atom or a C1-C5 alkyl group; and A denotes a nitrogen atom or a methyne group.

Abstract: This invention relates to novel, substituted aralkyl heterocyclic compounds according to formula I, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering aromatase inhibitors. Formula (I), or a pharmaceutically acceptable salt thereof, wherein: each R1 is independently selected from CH3, CH2D, CHD2 or CD3; each R2 is independently selected from CH3, CH2D, CHD2 or CD3; each Y is independently selected from H or D; and when each R variable is CH3, at least one Y is D.

Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.

Abstract: Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.

Abstract: The present invention discloses two new related substances (6) and (7) of Anastrozole synthesis from Q.A. Salt (5) as in Scheme-1 and purification procedures to get Anastrozole (1) free from (6) and (7).

Abstract: A process for the preparation of anastrozole.

Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.

Abstract: The present invention relates to a family of guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.

Abstract: A process for the preparation of anastrozole which comprises: a) brominating 3,5-bis(2-cyanoprop-2-yl)toluene (II) in an organic solvent using a brominating agent to obtain 3,5-bis(2-cyanoprop-2-yl)benzylbromide (III); b) heating the reaction mass of step a) to the reflux temperature of the organic solvent for a period of time no longer than 3 hours; c) isolating and purifying the bromo intermediate (III) using an organic solvent; d) alkylating the bromo intermediate in the presence of a base, optionally a phase transfer catalyst, a 1,2,4-triazole and an organic solvent to obtain anastrozole; and e) isolating and purifying the anastrozole from an organic solvent.

Abstract: A process for preparing Anastrozole is provided. In the process the steps of a. combining 3,5-bis(2-cyanoisopropyl)toluene, a solvent selected from the group consisting of acetonitrile, dichloromethane and chlorobenzene, a brominating reagent selected from a group consisting of N-bromosuccinimide and 1,3-dibromo-5,5-dimethylhydantoin, and 2,2?-azobis(2-methylpropionitrile); b. heating; c. combining with 1,2,4-triazole, a solvent selected from a group consisting of N-methylpyrrolidine, dimethylformamide, mixtures of NMP and DMF, dimethylsulfoxide, mixtures of DMSO and toluene, acetone, ACN, and tetrahydrofuran, a base selected from a group consisting of NaOH, KOH, K2CO3, and Na2CO3, and 1,3-benzendiacetonitrile-5-(bromomethyl)-?,?,{acute over (?)},{acute over (?)}-tetramethyl, at a temperature below ?20° C. are performed.

Abstract: A nitrile compound shown by the formula (1) has an excellent pesticidal activity and it is useful as an active ingredient of pesticide.

Abstract: The present application describes deuterium-enriched viramidine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present invention relates to the use of a lower dosage of bis(cyanophenyl)methyl-triazole of the formula (I) or a pharmaceutically acceptable salts thereof, for the preparation of a pharmaceutical composition for the prevention of conditions responsive to aromatase inhibition and to inhibition of estrogen biosynthesis, especially breast cancer, in mammals.

Abstract: The present invention discloses a process for the preparation of Anastrozole of the formula I in high purity and in high yield. 3,5-bis(halomethyl)toluene is prepared by reacting mesitylene with N-halosuccinimide in the presence of light or dibenzoyl peroxide or azobis isobutyronitrile as a catalyst and in a chlorinated solvent. 3,5-bis(halomethyl)toluene is cyanated with metal cyanide in the presence of a catalyst and in water, organic solvent or mixture thereof at temperature of 40 to 60° C. to obtain 2,2?-(5-methyl-1,3 phenylene)diacetonitrile which is further methylated with iodomethane in the presence of base and an organic solvent at temperature of 0 to 15° C. to obtain 2,2?-(5-methyl-1,3-phenylene)di(2-methyl-propiononitrile). The product obtained is treated with N-halosuccinimide in the presence of a catalyst and in a chlorinated solvent at temperature of 60 to 100° C.

Abstract: The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.

Abstract: The present invention relates to a novel diaryl 1,2,4-triazole derivative of the following formula (1) as a highly selective cyclooxygenase-2 inhibitor, wherein R1, R2, R3, R4, R5, W and A is as defined in this specification.

Abstract: A 1,2,4-Triazole derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided.

Abstract: 5-aryl-1H-triazole compounds of the formula are potent and selective COX-2 inhibitors. The invention further relates to pharmaceutical compositions containing these compounds.

Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.

Abstract: Benzoylguanidines of the formula (I) in which R1 to R4 have the meanings given in the specification and claims are suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. The compounds of the invention also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the triggering of ischemically induced cardiac arrhythmias.

Abstract: The present application relates to novel guanidine derivatives of the formula (I) in which R1 represents a five- or six-membered heterocyclic group; R2 represents hydrogen or alkyl, R3 represents the groupings —OR4, —OCOR5, —OCOOR6, —OCONR7R8 and —OSO2R9, where R4, R5 and R6 independently of one another represent alkyl, alkoxyalkyl, halogenoalkyl, alkenyl, alkinyl, alkylaminoalkyl, dialkylaminoalkyl, optionally substituted cycloalkyl and in each case optionally substituted phenyl or benzyl, R7 and R8 independently of one another represent hydrogen, alkyl, alkenyl and in each case optionally substituted phenyl or benzyl and R9 represents alkyl or optionally substituted phenyl, A represents the groupings —CH2CH2—, (CH2)3 and —CH═CH— and z represents cyano or nitro, with the proviso that, if Z represents NO2 and A represents —CH2CH2—, the radical R2 represents hydrogen; and the compound of the formula (I) in which

Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: Compounds of the following formula (I) and pharmaceutically acceptable esters and salts thereof: Ar is a phenyl group which may optionally be substituted by from 1 to 3 substituents selected from the group consisting of halogen atoms and trifluoromethyl groups. Said compounds (and pharmaceutically acceptable esters and salts thereof) have excellent antifungal activity.

Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.

Abstract: A compound represented by general formula (I) or a salt thereof, a process for producing the same, an intermediate for the production thereof, and a bactericide (fungicide) containing the same as the active ingredient wherein R1 represent optionally substituted aryl, optionally substituted heterocycle, mono- or di-substituted methyleneamino, optionally substituted (substituted imino)methyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, substituted carbonyl or substituted sulfonyl; R2 represents alkyl, alkenyl, alkynyl or cycloalkyl; R3 represents optionally substituted heterocycle; R4 represents hydrogen, alkyl, alkoxy, halogen, nitro, cyano or haloalkyl; M represents oxygen, S(O)i (i being 0, 1 or 2), NR16 (R16 being hydrogen, alkyl or acyl) or a single bond; n represents 0 or 1, provided n represent 1 when R3 represents imidazol-1-yl or 1H-1,2,4-triazol-1-yl; and the symbol˜represents the E form, Z form or a mixture thereof.

Abstract: Compounds of the following formula (I) and pharmaceutically acceptable esters and salts thereof: Ar is a phenyl group which may optionally be substituted by from 1 to 3 substituents selected from the group consisting of halogen atoms and trifluoromethyl groups. The compounds (and pharmaceutically acceptable esters and salts thereof) have excellent antifungal activity.

Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocy

Abstract: Block copolymers containing a fluorinated hydrocarbon unit, a hydrocarbon unit, and a poly(oxyethylene) unit are useful in fluid formulations of pharmaceutical agents. A typical embodiment is: C11H23—CONHC2H4NHCO—C8F16—CONHC2H4NHCOO—(C2H4O)34—H.

Abstract: 3-(Substituted phenyl)-5-(substituted cyclopropyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.