Abstract: A process for the preparation of 14-alkoxyindolomorphinans and 14-alkoxybenzofuranomorphinans is disclosed. The process facilitates the preparation of a large variety of 14-alkoxy substituted indolomorphinans and benzofuranomorphinans in which a 3-hydroxy substituent is present.

Abstract: New morphinane derivatives of the formula (I) ##STR1## their pharmaceutically acceptable salts, a process for their preparation and their use in therapy. The variables in the above structure are as follows: R.sub.1 is selected from the group consisting of C.sub.1 -C.sub.6 alkyl and hydrogen;R.sub.2 is selected from the group consisting of hydrogen; hydroxy; C.sub.1 -C.sub.6 alkoxy; C.sub.7 -C.sub.16 arylalkyloxy, wherein the aryl is C.sub.6 -C.sub.10 aryl and the alkyloxy is C.sub.1 -C.sub.6 alkyloxy;R.sub.3 is a C.sub.1 -C.sub.6 alkyl;R.sub.4 is a hydrogen; hydroxy; or a C.sub.1 -C.sub.6 alkoxy;R.sub.5 and R.sub.6 each and independently are selected from the group consisting of hydrogen; and C.sub.1 -C.sub.6 alkyl;X is NR.sub.9, wherein R.sub.9 is selected from the group consisting of hydrogen; and C.sub.1 -C.sub.6 alkyl;and wherein any aryl group in the compound may be unsubstituted or mono-, di-, or tri-substituted independently with hydroxy; halo; nitro; cyano; thiocyanato; trifluoromethyl; C.sub.1 -C.

Abstract: The title compounds are obtained by racemate resolution of D,L-homoalanin-4-yl(methyl)phosphinic acid via precipitation of one of the diastereomeric salts using chiral bases such as quinine or cinchonine. It is possible to increase the yield of desired enantiomer by transformed racemate resolution when the precipitation of the diastereomeric salt takes place with the racemization of the undesired enantiomer in the presence of (hetero)--aromatic aldehydes. The racemization method is also suitable for structurally different optically active amino acids.

Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

Abstract: The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: Compounds are provided of the formula: ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl, trans(C.sub.4 -C.sub.5)alkenyl, allyl or furan-2-ylalkyl, R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, (C.sub.1 -C.sub.5)alky or (C.sub.1 -C.sub.5)alkylCO; X is O, S or NY, wherein Y is H, benzyl or (C.sub.1 -C.sub.5)alkyl; R is CH(Z)CO.sub.2 Y, wherein Z is H, CH.sub.2 CO.sub.2 Y or (CH.sub.2).sub.n N(R.sup.4)(R.sup.5), wherein n is 1-5 and R.sup.4 and R.sup.5 are individually H, (C.sub.1 -C.sub.4)alkyl, phenyl, (C.dbd.NH)NH.sub.2, benzyloxycarbonyl or (C.dbd.NHNO.sub.2); and the pharmaceutically acceptable salts thereof.

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.

Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

Abstract: Compounds of the formula: ##STR1## are provided, which are selective kappa opioid receptor antagonists, wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl, trans (C.sub.4 -C.sub.5) alkenyl, allyl or furan-2-ylalkyl; R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.5)alkylCO; X is O, S or NY, wherein Y is H or (C.sub.1 -C.sub.5)alkyl; R.sup.4 is CH.sub.2 (methylene) or C.dbd.O (carbonyl), R.sup.5 is CH.sub.2, C.dbd.O or C.dbd.NH (imino) and R.sup.6 is (C.sub.1 -C.sub.4)alkyl or NH(C.sub.1 -C.sub.4)alkyl, optionally substituted by a non-terminal (C.sub.1 -C.sub.2)alkyl group or by N(R.sup.7) (R.sup.8) wherein R.sup.7 and R.sup.8 are individually H or (C.sub.1 -C.sub.3) alkyl, with the proviso that one of R.sup.4 or R.sup.5 is CH.sub.2, and the pharmaceutically acceptable salts thereof.

Abstract: The present invention provides novel substituted opioid analgesic compounds of Formula I: ##STR1## which are opioid agonists, and which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

Abstract: The present invention provides novel substituted opioid analgesic compounds of Formula I: ##STR1## which are opioid agonists, and which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are opioid agonists which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: A compound represented by the formula I: ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen or (C.sub.2 -C.sub.10) alkanoyl in substantially chemically pure form, and pharmaceutical compositions thereof are disclosed.

Abstract: An organic photochromic compound with improved long term preservability, thermal stability, the repetition character of the record and the like and useful as recording-memory materials or photosensitizers, comprising dimers of the compounds selected from the group consisting of pyrido[3,4-g]isoquinoline, pyrido[2,3-g]quinoline, pyrido[3,2-g]quinoline and pyrido[3,2-g]quinoline derivatives.

Abstract: Antibiotic LL-D42067.beta. derived by aerobic fermentation of the microorganism Actinomadura madurae subspecies simaoensis NRRL 15734, useful as an antibacterial and antiparasitic agent.

Abstract: Antibiotic LL-D42067.alpha. derived by aerobic fermentation of the microorganism Actinomadura madurae subspecies simaoensis NRRL 15734, useful as an antibacterial and antiparasitic agent.

Abstract: The present invention is concerned with an improved process for the production of highly active optical isomers of (-) 7 or 8 fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide having the structural formula ##STR1## in which the fluoro substituent replaces a hydrogen in the 7 or 8 position. The two active isomers represented by formula II are S(-)7-fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide and R(-)8-fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide. It is especially concerned with the resolution of the racemic 7 or 8 fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide by first forming and separating diastereomers of said racemic carboxylic acids by salt formation with brucine or ephedrine followed by crystallization and regeneration of the desired (-) isomers and recycling of the (+) isomer by racemization of the regenerated isomer.

Abstract: Resolution of racemic 5-phenyl-2-pentanol via the hemiphthalate ester, followed by diastereomer salt formation with (+)-brucine, separation of the brucine salt of (S)-5-phenyl-2-pentanol hemiphthalate and recovery of the (S)-alcohol therefrom. The (S)-5-phenyl-2-pentanol is a valuable intermediate for organic synthesis.

Abstract: There is described a new process for the preparation of optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-1-carboxylic acids substituted in the 3 position, and derivatives thereof. A racemate of certain cyclobutanones is reacted with a sulfurous acid salt of an optically active base to obtain a mixture of diastereomeric 4-(2',2',2'-trihalogenoethyl)-cyclobutane-2-sulfonic acid salts; this mixture is then separated into the pure diastereomeric sulfonic acid salts. Either the pure diastereomeric sulfonic acid salts are converted directly to the desired optically active products, or the optically active cyclobutanones obtained from the pure diastereomeric sulfonic acids salts by decomposition are converted, in the presence of a base, to the desired product. Optionally, the product, optically active 2-(2',2'-dihalogenovinyl)-cyclopropane-2-carboxylic acids can be converted to their 1',2'-dibromo derivatives.

Abstract: A method for stereospecifically preparing chiral 2-substituted-4-hydroxy-2-cyclopenten-1-one which comprises asymmetrically reducing 2-substituted cyclopentane-1,3,4-trione to the corresponding 2-substituted-4(R)-hydroxy-cyclopentane-1,3-dione, enolizing the said dione to obtain the enol ester or enol ether configuration, reducing the enol ester or ether and recovering the desired compound. The chiral 2-substituted-4-hydroxy-2-cyclopenten-1-one are key intermediates in the preparation of prostaglandins.