Abstract: Substituted 1,2,3,6-tetrahydropyridines are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.

Abstract: Fungicidal acetic acid esters of the formula ##STR1## in which A.sup.1 is an optionally substituted phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, thienyl, furanyl, pyrrolyl, thiazolyl, pyrazolyl, oxazolyl, phenoxy, phenylacetylenyl or phenylethylenyl radical, andA.sup.2 and A.sup.3 each is a lower alkyl radical.

Abstract: A novel piperidine derivative is defined by the formula (I), including a slt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.

Abstract: Substituted tetrahydropyridines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.

Abstract: Novel cyclic beta-ketoamides which contain an aryl moiety having utility as blood cholesterol lowering agents rendering them useful in the treatment of atherosclerosis.

Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.

Abstract: The invention provides novel compounds and salts thereof, have the structure ##STR1## wherein R.sub.1 is a guianidinobenzoyloxy group and R.sub.2 is a hydrogen atom, a hydroxy, cyano, --COR.sub.3 (wherein R.sub.3 is an amino or lower alkyl group) or --COOR.sub.4 group [wherein R.sub.4 is a hydrogen atom, lower alkyl, phenyl, benzyl or --CH.sub.2 CONR.sub.5 R.sub.6 group (wherein R.sub.5 and R.sub.6 are the same or different and selected from a hydrogen atom and lower alkyl groups)], and wherein R.sub.1 is a hydroxy group and wherein R.sub.2 is a --COR.sub.3 (wherein R.sub.3 is an amino or lower alkyl group) or --COOR.sub.4 group [wherein R.sub.4 is a (C.sub.1, C.sub.3 or C.sub.4) alkyl, phenyl, benzyl or --CH.sub.2 CONR.sub.5 R.sub.6 group (wherein R.sub.5 and R.sub.6 are the same or different and selected from a hydrogen atom and lower alkyl groups)]. The compounds, wherein R.sub.1 is a guanidinobenzoyloxy group, are useful protease inhibitors as anti-trypsin agents.

Abstract: Disclosed herein is a process for cyclizing pyridinecarboxylate derivatives with 5-(haloalkyl) carboxamide or 5(haloalkyl)carbamate substitutions to prepare compounds useful as herbicides.

Abstract: There are described compounds of the formula ##STR1## where n is 1, 2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, ##STR5## R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR6## taken as a whole is ##STR7## R.sub.3 is hydrogen or loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.

Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits born absorption inhibiting effects and is useful as a medicament for treating osteoporosis.

Abstract: Alkylating analogs of prazosin were synthesized and found to compete with nanomolar potency at .sup.3 H-prazosin binding sites of rat tissues. The compounds were found to be irreversible ligands at .sup.3 H-prazosin binding sites, and denoted a subtype of alpha.sub.1 -adrenoceptors.

Abstract: Compounds of the formula (I) ##STR1## wherein R represents H or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 represent H, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkythio, C.sub.1-6 alkoxycarbonyl, carboxyl, hydroxy, nitro, cyano, optionally C.sub.1-4 alkyl mono- or disubstituted carbamoyl, optionally C.sub.1-4 alkyl mono- or disubstituted amino, C.sub.1-6 acylamino, C.sub.1-4 alkoxy carbonylamino, C.sub.1-6 alkylsulphynyl, C.sub.1-6 alkylsulphonyl or C.sub.1-6 acyl;R.sub.3 represents H, C.sub.1-6 alkyl, aryl or aralkyl, or it may be absent;A represents CO or C.dbd.S;E represents nitrogen;D represents CO or CR.sub.4 R.sub.5 when the E--D bond is single, or D is C--R when the D--E bond is double, in which R.sub.4 represents H, C.sub.1-6 alkyl, aryl, aralkyl, hydroxy or C.sub.1-4 alkoxy and R.sub.5 represents H;X represents oxygen or N--R, or it is absent;Y represents a basic group selected from: ##STR2## in which n is 2 or 3; p is 0 or 1 at the same time or not; q is 0,2 or 3; R.sub.6 and R.sub.

Abstract: In the preparation of 2-chloro-5-methyl-pyridine of the formula ##STR1## by reacting 3-methyl-pyridine-1-oxide of the formula ##STR2## with a chlorinating agent, the improvement which comprises effecting the reaction in the presence of a chlorinating agent of the formula ##STR3## in which A represents oxygen or the grouping ##STR4## in which R.sup.2 and R.sup.3 individually represent alkyl, cycloalkyl or aryl or together represent alkanediyl or oxaalkanediyl andR.sup.1 represents hydrogen, chlorine, alkyl, cycloalkyl, aryl or the grouping ##STR5## in which R.sup.2 and R.sup.3 have the abovementioned meanings,and where, if R.sup.1 represents aryl, A must represent the grouping ##STR6## in the presence of a basic organic nitrogen compound and in the presence of a diluent at a temperature between about -20.degree. C. and +120.degree. C. The product is known to be useful in the systhesis of pharmaceuticals and insecticides.

Abstract: There are disclosed various compounds of the formula below, ##STR1## where n is 0 or 1;X is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;Y is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkynyl, loweralkanoyl, arylloweralkanoyl, heteroarylloweralkyl or heteroarylloweralkanoyl;R.sub.2 is hydrogen, loweralkyl, formyl or cyano;R.sub.3 is hydrogen or loweralkyl;R.sub.4 is loweralkyl, arylloweralkyl, cycloalkyl, aryl or heteroaryl; or alternatively, --NR.sub.3 R.sub.4 taken together constitutes ##STR2## R.sub.5 being hydrogen, loweralkyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl,which compounds are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.

Abstract: Compounds of formula I ##STR1## in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2,X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, andR represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: ##STR2## (in which: R.sub.1 and R.sub.

Abstract: Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0, 1 or 2, R.sub.1 denotes hydrogen (C.sub.1 -C.sub.6)-alkyl which can optionally be substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 C.sub.2)-alkyl, (C.sub.1 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, [which can be substituted as defined previously in the aryl radical], a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.

Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: A process for the preparation of enantiomerically homogeneous aminopyrrolidinyl naphthyridine carboxylic acids and quinolone carboxylic acids, and for the preparation of intermediates that are useful in the production of these carboxylic acids.

Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.

Abstract: The invention concerns pharmaceutially useful heterocyclic nitromethane compounds of the formula I: ##STR1## in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula --NRa--, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R.sup.1 R.sup.2 and R.sup.3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R.sup.1, R.sup.2 and R.sup.3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completion ring Q is of 3 atoms then at least one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen; and salts thereof.