Abstract: The present invention relates to compounds having formula I and to pharmaceutically acceptable salts thereof. Compounds of formula I inhibit &agr;1 adrenoreceptors and may be useful for treating benign prostatic hyperplasia (also called benign prostatic hypertrophy) and other urological diseases such as bladder outlet obstruction, neurogenic bladder and gynecological syndromes.

Abstract: Methods and compounds for the synthesis of heterocycles, including pyrimidine-2,4-diones, are disclosed. Also disclosed are solid supports useful for solid phase synthesis, and methods for making the solid supports.

Abstract: This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1-6 carbon atoms; R′ is hydrogen, alkyl of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, trifluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, trifluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least one of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorde

Abstract: The present invention provides pyrazolo[1,5-a]pyrimidine derivatives represented by the formula (1) wherein R1 represents lower alkyl or the like; one of R2 and R3 represents hydrogen and the other represents phenyl having lower alkoxy or the like, and R4 is hydrogen, carboxyl, lower alkoxy-carbonyl or the like. The derivatives of the invention have pharmacological effects such as analgesic action, inhibitory effect on nitrogen monoxide synthetase and the like and are useful as analgesics. The derivatives of the invention are also useful as therapeutic or prophylactic agents for septicemia, endotoxin shock, chronic articular rheumatism, etc.

Abstract: The instant invention provides processes and intermediates employed in the synthesis of ((2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)-amino-3-hydroxy-5-(2S-(1-tetrahydropyrimid-2-onyl)-3-methyl-butanoyl)amino-1,6-diphenylhexane and analogs thereof.

Abstract: The invention concerns a method for preparing polyazacycloalkanes immobilised on a silica gel from a polyazacycloalkane of formula (A) in which: R1 and R2 represent a hydrogen atom, an alkyl radical, or a [hetero(aryl)]alkyl radical; W1, W2 and W3 represent a radical of formula (B): —[(CT1T2)n—[N(R3)]p—(CT3T4)m]l— such as defined in the description; R3 represents a hydrogen atom, an alkyl radical or a [hetero(aryl)]alkyl radical, provided that the polyazacycloalkane ring of the compound of formula (A) comprises not more than 30 cyclic carbon atoms, and not more than 6 cyclic nitrogen atoms.

Abstract: Triazolo[4,5-d]pyrimidine compounds are provided of the formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification. Compositions containing the compounds are also provided, together with processes for their preparation and methods of use in the treatment of diseases, including myocardial infarction and unstable angina.

Abstract: A therapeutic agent for spinal canal stenosis is provided, which contains a pyridazinone compound of the formula (I) wherein R1, R2 and R3 are each independently a hydrogen atom or a lower alkyl, X is a halogen atom, a cyano or a hydrogen atom, Y is a halogen atom, a trifluoromethyl or a hydrogen atom, and A is a C1-C8 alkylene optionally substituted with a hydroxyl, or its pharmacologically acceptable salt.

Abstract: The invention relates to nitro- and cyano-1,2,4,5-tetrahydro-heterocycloazepinyl pyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing such compounds and a process for the preparation of such compounds. The compounds of the invention are group I mGluR antagonists and are therefore useful for the control or prevention of acute and/or chronic neurological disorders.

Abstract: 2-Methyl-4-amino-5-aminomethylpyrimidine of the formula 1 is prepared by reacting 2-methyl-4-amino-5-alkoxymethylpyrimidine of the formula 2 where R=C1-C6-alkyl, with ammonia in the presence of a catalyst.

Abstract: The invention relates to substituted phenyluracils of the general formula (I) in which the radicals R1 to R5, Q and n are each as defined in the description, and to processes for their preparation and to their use as herbicides.

Abstract: 2-Amino-5, 8-dimethoxy[1,2,4]triazolo[1,5-c]-pyrimidine is prepared from a 5-chloro or 5-methoxy substituted 3-amino-8-methoxy[1,2,4]triazolo[4,3-c]-pyrimidine by reaction with methoxide in an alcohol solvent. Both rearrangement and, when the 5-substituent is chloro, methoxy substitution can be accomplished directly.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.

Abstract: The invention relates to novel halogenopyrimidines, to two processes for their preparation and to their use as pesticides.

Abstract: The invention relates to novel substituted optically active aminotriazines having at least two asymmetrically substituted carbon atoms of the formula (I), in which A represents a single bond or represents in each case straight-chain or branched alkanediyl or oxaalkanediyl having in each case up to 6 carbon atoms, Z represents certain carbocyclic or heterocyclic radicals and the substituents R1, R2, R3, R4 and Y are as defined in the description,  with the proviso that in each individual case R2, R3 and Y are different from one another and that the substituents at the two carbon atoms to which R2 and R3 or R4 are attached are configured as follows: (a) R configuration at the carbon atom to which R2 and R3 are attached and R configuration at the carbon atom to which R4 is attached (“R,R-diastereomers”), (b) R configuration at the carbon atom to which R2 and R3 are attached and S configuration at the carbon atom to which R4 is attached (“R,S-diastereomers”), (

Abstract: A method for producing &bgr; crystals of ethyl (R)-2-[4-(6-chloro-2-quinoxalin-2-yloxy)phenoxy]propionate, which is characterized by heating &agr; crystals, or &agr; a crystals and &bgr; crystals, within a range of from 50° C. to lower than the melting point of the &agr; crystals.

Abstract: The present invention relates to novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof which possess an excellent anti-secretory activity, pharmaceutical compositions containing the same as an active ingredient, their novel intermediates, and processes for the preparation thereof wherein: when A is piperidin-1-yl or —NH—B, wherein B is C3-C4 alkyl, C3-C4 alkenyl, C3-C7 cycloalkyl, C1-C3 alkoxyethyl, phenylethl which may be substituted or unsubstituted, 3-trifluoromethylphenylmethyl, 1-naphthylmethyl, 4-methylthiazol-2-yl or 4-phenylthiazol-2-yl, R1 is hydrogen or methyl; and R2, R3, R4 and R5 are hydrogen; or when A is a group of formula (II); when R1 is hydroxymethyl or C1-C3 alkoxymethyl, R2, R3, R4, R5 and R6 are hydrogen; and R7 is hydrogen or halogen; or when R1 is hydrogen or methyl, R7 is hydrogen or halogen; and one or two of R2, R3, R4, R5 and R6 is hydroxy, methoxy, or a group of formula (III) wherein Z is C1-C4 alkyl, substituted or unsubstituted C1-C4

Abstract: CL-20 is crystallized from a solution containing a CL-20 organic solvent and a CL-20 non-solvent miscible with the solvent. The CL-20 non-solvent is a nitrate ester, preferably poly(glycidyl nitrate) and/or triethyleneglycol-dinitrate, although other nitrate ester plasticizers having acceptable volatilities and impact sensitivities can be used. The solution is saturated with CL-20, and CL-20 is then crystallized from the saturated solution by adding &egr;-polymorph CL-20 crystalline seeds to the solution and evaporating off the CL-20 solvent, preferably under vacuum. The nitrate ester non-solvent is then separated from the crystalline CL-20, such as by filtration of the CL-20 crystals or by diluting the slurry of non-solvent and CL-20 with an environmentally acceptable solvent that is miscible with the non-solvent but in which the CL-20 is insoluble.

Abstract: A 1,2,3-thiadiazole derivative represented by general formula (I): [wherein R1 is hydrogen atom, halogen atom, (C1-C6) alkyl, phenyl, etc., R2 is the following group (A) or group (B): (wherein R3 is halogen atom, cyano, etc., R4 is hydrogen atom, halogen atom, cyano, etc., X and Y, same or different, are oxygen atom or sulfur atom, n is 0-3, R5 is hydrogen atom, (C1-C20) alkyl, etc., R6 is (C1-C20) alkyl, (C2-C20) alkenyl, etc., and m is 0-2)]; a plant disease controller containing said compound as active ingredient; and a method for using said controller.

Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula where X is S or Se; Y is H, I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R1 is H or an acyclo tail having the general formula where R2 is H, CH2 OH or CH2 NH2; R3 is OH, NH2, or OCOCH2CH2CO2H; and R4 is O, S, or CH2. The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging. Further, they can be administered alone to prevent and/or treat disorders of pyrimidine catabolism and other physiological disorders.