Abstract: The subject invention concerns a process for the preparation of a compound of formula (2), which comprises phenolic oxidation of a compound of formula (1) wherein X.sup.1 and X.sup.2 are independently selected from H or a protecting group for the phenolic function, e.g. acyl or trialkylsilyl; groups A.sup.1, A.sup.2, B.sup.1, B.sup.2 and Y are selected so as to render the nitrogen atom non-basic; Z is a blocking group, e.g. Br or t-butyl; and R is H, C.sub.1-20 alkyl, C.sub.3-20 aryl, C.sub.4-20 arylalkyl, and wherein the process is carried out in a two-phase liquid system comprising an aqueous base and an organic solvent having a dielectric constant below 4.8.

Abstract: A compound of formula (Ia) of (Ib), wherein A and B each independently represents hydrogen or one, two or three naphthylidene substituents, which substituents are selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, aryl, aryloxy, silyl and silyloxy; R.sup.1 represents phenyl, C.sub.1-6 alkyl, phenyl C.sub.1-6 alkyl or a moiety of formula (a): wherein R.sup.2 represents C.sub.1-6 alkyl, phenyl or benzyl, R.sup.3 represents H or OR.sup.4 wherein R.sup.4 is C.sub.1-6 alkyl or C.sub.1-6 alkylsilyl and n is zero or an integer 1 or 2; and X.sup.- is a counter ion; a process for the preparation of such compounds and the use of such compounds for enantioselectively epoxidising a prochiral olefin.

Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.

Abstract: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.

Abstract: Tetrahydroisoquinoline derivatives of the formula: ##STR1## or a pharmaceutically acceptable salt, ester, or prodrug thereof, having activity as an LHRH antagonist, as well as pharmaceutical compositions containing the same, and methods for their use and preparation.

Abstract: Compounds based on the benzoxazine ring system are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number or strength of excitatory synapses or in the number of AMPA receptors. The compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors, for improving the performance of subjects with memory deficiencies, for treating schizophrenia, and for improving memory encoding.

Abstract: An aromatic tertiary amine compound of formula (I): ##STR1## wherein (A) and (B) are each a substituted or unsubstituted vinylene or o-arylene group; R.sup.1 to R.sup.4 are each a halogen atom, or a substituted or unsubstituted alkyl, aryl, alkoxy, aryloxy, dialkylamino, N-alkyl-N-arylamino or diarylamino group; R.sup.5 is a halogen atom, or a substituted or unsubstituted alkyl, alkoxy or dialkylamino group; h, i, j, k and l are each an integer of 0-4; and m is an integer of 1-6.

Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R.sup.1 represents hydrogen atom or a C.sub.1-6 alkyl group; R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-6 alkyl group, or R.sup.2 and R.sup.3 may combine together to represent a 5- or 6-membered cycloalkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.5 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group; x represents --NR.sup.7 --, --O--, --CHR.sup.7 -- or --S-- in which R.sup.7 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.

Abstract: A bicyclic, non-aromatic hydrocarbon compound, optionally having one or more N, O or S atoms in the bicyclic skeleton, and having as substituents an acid group and an amido group, which are vicinal and in a syn-position, wherein the amido group is not anilido and the acid group is carboxyl or carboxyl in a form metabolizable to a free carboxyl group, and wherein said bicyclic skeleton is optionally unsaturated, except in the bond between said groups, acid-cleavably links an amide-containing active agent to a targeting agent, which is linked by a linker arm to the bicyclic skeleton.

Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: In a process for reprocessing devices for the transdermal application of active substances or their process waste, active substance-containing components are brought into solution and the active substances are recovered therefrom.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: Compounds based on the benzoxazine ring system ##STR1## are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number or strength of excitatory synapses or in the number of AMPA receptors. The compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors, for improving the performance of subjects with memory deficiencies, for treating schizophrenia, and for improving memory encoding.

Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), wherein R.sup.1 and R.sup.2 i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, or ii) taken together are a --CH.sub.2 -- group forming a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond; R.sup.3 is preferably hydrogen, halogen or lower alkyl, R.sup.4 is preferably hydrogen or lower alkyl, X is preferably CH.sub.2, Y is preferably hydrogen and Z is preferably CONR.sup.14 R.sup.15 and R.sup.14 and R.sup.15 are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: This invention comprises a process for production of a compound of the formula: ##STR1## in which R.sup.1 is selected from the group consisting of H, lower alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), bromo, chloro, fluoro, iodo, --COlower alkyl(C.sub.1 -C.sub.3), and --CF.sub.3 ;R.sup.2 is selected from the group consisting of H, lower alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), amino, bromo, chloro, fluoro, iodo, and --COlower alkyl(C.sub.1 -C.sub.3);or R.sup.1 and R.sup.2 taken together are methylenedioxy or ethylenedioxy;R.sup.3 is an aldehyde or carboxcylic acid moiety;the moiety ##STR2## wherein Z represents substituted or unsubstituted phenyl ring or an optionally substituted 5 or 6-membered aromatic heterocyclic ring.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. ##STR1## wherein: R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9, R.sup.10, R.sup.11 or R.sup.12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)-amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxy-carbonyl; R.sup.7 and R.sup.