Abstract: Compounds of Formula (I) have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man where subnormal levels of this neurochemical are found, such as in Alzheimer's disease, and other conditions involving learning and cognition.

Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine and thus may be useful in the treatment of diseases learning and cognition.The compounds of this invention are ##STR1## where Q is ##STR2## A and B are independently selected from H, R.sup.4, --OH and --OCOR.sup.4, orA and B together form .dbd.O, .dbd.S, .dbd.CH.sub.2, .dbd.CHR.sup.4, .dbd.C(R.sup.4), .dbd.NOH, .dbd.NOR.sup.4, 1,3-dioxane, 1,3-dioxolane, 1,3-dithiane or 1,3-dithiolane;R.sup.1 is 4-,3-, or 2-pyridyl, 2-fluoro-4-pyridyl or 3-fluoro-4-pyridyl;R.sup.3, R.sup.4 and R.sup.5 are herein defined;and physiologically suitable salts thereof.

Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man, such as in Alzheimer's disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found.The compounds of this invention can be described as shown in Formula I ##STR1## where Q is ##STR2## R.sup.1 is 4-,3-, or 2-pyridyl, pyrimidyl, pyrazinyl, or fluoro-4-pyridyl; R.sup.2 and R.sup.3 are independently H, F, Cl, Br, NO.sub.2, OH, --R.sup.4, --O--R.sup.4, --CO.sub.2 R.sup.4, --COR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sup.4 R.sup.4', --S(O).sub.m2 -- R.sup.4, NH.sub.2, CF.sub.3, NHR.sup.4, NR.sup.4 R.sup.4' ;R.sup.4 and R.sup.4' are independently H, alkyl of 1 to 4 carbons, CH.sub.2 Phe-W or Phe-W;and hydrates and physiologically suitable salts thereof.

Abstract: This invention relates to the preparation of cyclic urea compounds. More specifically, this invention is directed to methods for selectively alkylating diamines, methods for selectively converting a mixture of alkylated and non-alkylated diamines to cyclic urea compounds, methods to purify cyclic urea compounds having a single N-substitution, methods to convert a cyclic urea compound having a single N-substitution to a cyclic urea compound having either symmetrical or non-symmetrical N,N'-disubstitution, and methods to remove protecting groups from cyclic urea compounds.

Abstract: Compounds of the following formula have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man involving learning and cognition, where subnormal levels of this neurochemical are found ##STR1## wherein R.sup.1 is 4-,3-, or 2-pyridyl, 2-fluoro-4-pyridyl or 3-fluoro-4-pyridyl;R.sup.2 is alkyl of 1 to 10 carbons, cycloalkyl of 3 to 8 carbons, 2-,3-, or 4-pyridyl, Phe or Phe-W;Phe is a phenyl group;W is F, Cl, Br, R.sup.4, --OH, --OR.sup.4, --NO.sub.2, --NH.sub.2, --NHR.sup.4, --NR4R.sup.4, --CN, --S(O)m --R.sup.4 ;R.sup.3 is H, F, Cl, Br, --CN, --OH, --NO.sub.2, --NH.sub.2, --CF.sub.3, --NHR.sup.4, --NR.sup.4 R.sup.4, R.sup.4, --OR.sup.4, --S(O).sub.m --R.sup.4R.sup.4 is alkyl of 1 to 4 carbons, CH.sub.2 Phe-- or Phe--;R.sup.5 is --(CH.sub.2).sub.n --Y or --OCOR.sup.4 ;Y is NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.4, --NHCOR.sup.4, --NHCO.sub.2 R.sup.4, F, Cl, Br, OR.sup.4, --S(O).sub.m R.sup.4, --CO.sub.2 H, --CO.sub.2 R.sup.

Abstract: This invention relates to monoamine oxidase-B (MAO-B) inhibitory 5-substituted 2,4-thiazolidinediones, such as Formula I, to pharmaceutical compositions thereof, process of preparation, and methods of use in mammals to treat cognitive disorders, neurological dysfunction, and/or mood disturbances such as, but not limited to degenerative nervous system diseases.

Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitters acetylcholine, dopamine and serotonin; and thus may be useful in the treatment of diseases of man where subnormal levels of this neurochemical are found such as in Alzheimer's disease and other conditions involving learning and cognition; and Parkinson's disease.The compounds of this invention can be described as shown in Formula I ##STR1## where A is a heteroaromatic system.

Abstract: The invention relates to benylalcohol phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylalcohol phospholipase A.sub.2 inhibitor.

Abstract: The invention relates to benzylketone phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylketone phospholipase A.sub.2 inhibitor. These compounds are also intermediates in the synthesis of other PLA.sub.2 inhibitors.

Abstract: The invention relates to benzylamine phosphilipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylamine phospholipase A.sub.2 inhibitor.

Abstract: The invention relates to benzylketone phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylketone phospholipase A.sub.2 inhibitor. These compounds are also intermediates in the synthesis of other PLA.sub.2 inhibitors.

Abstract: Antihypercholesterolemic thioimidazoles of the formula ##STR1## or a pharmaceutical acceptable salt thereof, wherein R.sup.1 and R.sup.2 independently are H, F, Cl, CF.sub.3, alkyl of 1 to 4 carbon atoms, or alkoxy of 1 to 4 carbon atoms;A is alkylene of 7-20 carbon atoms or an alkenyl residue thereof with no more than 2 double bonds;R.sup.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; andn is 0, 1 or 2,are provided, such as 8-(4,5-diphenyl-1H-imidazol-2-ylthio)octanoic acid ethyl ester.

Abstract: Antiinflammatory 2-halo-4,5-diarylpyrroles are provided. These pyrroles have the formula: ##STR1## wherein Y.sub.1 is F, Cl, Br, or I;Y.sub.2 is H, Cl, or Br;R.sub.1 is H, CH.sub.3, C.sub.2 H.sub.5, acetyl, or ##STR2## where R.sub.4 is methyl, ethyl, t-butyl, or benzyl; R.sub.2 is pyridyl or ##STR3## R.sub.3 is pyridyl or ##STR4## X and X' are independently H, F, Cl, Br, OR.sub.5, or R.sub.5 S(O).sub.n where n is 0, 1 or 2 and R.sub.5 is C.sub.1 -C.sub.2 alkyl; provided that one of R.sub.2 or R.sub.3 must be ##STR5## or a pharmaceutically suitable salt thereof. Intermediates to the above pyrroles are provided where R.sub.1 in the above formula is replaced by R.sup.1 which is benzenesulfonyl or 4-toluenesulfonyl.

Abstract: Novel 4,5-diaryl-2-halo imidazoles, for example, 2-bromo-4,5-bis-(4-chorophenyl)imidazole, and their acid addition salts are useful for treating inflammation in mammals. Some of the compounds are also useful as analgesics.