Abstract: Novel pyrazolopyrimidinethione compounds of formula 1: wherein R1 and R2 are independently each hydrogen atom, a C1-C6 alkyl group, or a C3-C6 cycloalkyl group, R3 is a C1-C6 alkyl group. C3-C6 cycloalkyl group or C3-C6 alkenyl group which is substituted or unsubstituted, X is O or NR4, and R4 is hydrogen atom, or a C1-C6 alkyl group, a C3-C6 cycloalkyl group or a C3-C6 alkenyl group which is unsubstituted or substituted with OH or an alkoxy group, pharmacologically acceptable salts or hydrates thereof, and preparation methods thereof are disclosed. Pharmaceutical compositions comprising the compounds are effectively used for the treatment of erectile dysfunction.

Abstract: The present invention relates to substituted pyrrolidinone compounds of formula 1, wherein n is 0 or 1; Aza is a heterocycle optionally substituted with C1-4 alkyl, or C1-4 alkyl substituted with a heterocycle, which represents a saturated or unsaturated five- or six-membered ring having nitrogen(s) as a heteroatom, which are muscarinic acetylcholine receptor agonists and useful as nootropics and therapeutic agents for cerebral neural diseases such as Alzheimer's disease; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.

Abstract: The present invention relates to novel tetrahydropyridine derivatives of formula 1 having an appropriately substituted pyrrolidinone and oxime, wherein m is 0 or 1, n is 1 or 2, R1 is hydrogen, C1-4alkyl, C2-4 alkynyl or aryl, R3 is C1-4 alkyl, which show high efficacy, low cholinergic adverse effects and high affinity for muscarinic acetylcholine receptor; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.

Abstract: The present invention relates to novel tetrahydropyridine derivatives of formula 1 having an appropriately substituted pyrrolidinone and oxime, 1

Abstract: The present invention relates to substituted pyrrolidinone compounds of formula 1, 1

Abstract: There is disclosed a method for the preparation of pyrido benzoxazine derivative having the following formula I, that is improved in both production coat and yield.The method comprises reacting a compound of the following general formula II with tetraalkyl ammonium fluoride or with a mixture of tetraalkyl ammonium halide and metal fluoride in an organic solvent at a reaction temperature of about 30 to about 100.degree. C. for 1 to 3 hours under stirring; and reacting the resulting solution with a metal hydroxide or a metal carboxylate dissolved in water or in a mixture of water and alcohol, for 1 to 3 hours under heat. ##STR1## wherein X is a fluorine or chlorine atom and X.sub.1 and X.sub.2 each is a halogen atom or a nitro group, R is an alkyl group containing 1 to 4 carbon atoms and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each is an alkyd group or allyl group containing 1 to 8 carbon atoms.

Abstract: A process for preparing (-)3(S)-methylbenzoxazine derivative of formula (I) comprising the steps of reacting the compound of formula (II) with benzoic acid, triphenylphosphine and diethyl azodicarboxylate in an organic solvent to obtain the compound of formula (III); hydrogenating the compound of formula (III) in the presence of a metallic catalyst to provide the compound of formula (IV); hydrolyzing the compound of formula (IV) to give the compound of formula (V); and reacting the compound of formula (V) with diethyl azodicarboxylate, triphenylphosphine, and zinc chloride in an organic solvent. The obtained (-)3(S)-methylbenzoxazine derivative is a useful intermediate for preparing an antibacterial agent which has a potent bacteriocidal effect.

Abstract: There are disclosed (+)2-benzoyl-3-[prop-2(S)-yl)amino] acrylate derivatives of following the formula and a method for the preparation of the same; ##STR1## wherein X is a halogen; X.sub.1 and X.sub.2 are independently selected from a halogen and a nitro; and R and R.sub.1 each is an alkyl group containing 1 to 4 carbon atoms.

Abstract: There is disclosed a method for the preparation of the antibacterial (-) piperazine benzoxazine derivative having formula I comprising the steps of reacting (+)2-aminomethylene-3-oxo-3-phenylpropionate derivative of formula II with a base in an organic polar solvent, to give a (-) benzoxazine derivative of formula III: and reacting the (-) benzoxazine derivative of formula III with a piperazine derivative of formula IV in an organic polar solvent.

Abstract: (+)2-benzoyl-3-(silyloxyprop-2(S)-yl)aminoacrylate derivative of following formula I which can be an useful starting material for producing a potent antibacterial compound and a method for the preparation of the same: ##STR1## wherein X is fluoro or chloro; X.sub.1 and X.sub.2 can be halogen or nitro; and R, R.sub.1, R.sub.2 and R.sub.3 each can be C.sub.1-8 alkyl group.