Abstract: The present invention relates to substituted .omega.-?phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl! ?alkyl, alkenyl or alkynyl!amine carboxamides, sulfonamides and phosphonylamides which are useful as antiarrhythmic agents.

Abstract: This invention relates to 3-(4-acrylamidobenzoyl)benzo?b! thiophenes, to the process for their preparation, to pharmaceutical compositions and to their use for modifying the balance between bone resorption and bone production in a mammal. The compounds useful in this invention are represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl containing 1-8 carbon atoms, or R.sup.1 and R.sup.2 together with the interposed nitrogen forms a 5-7 membered ring optionally containing an additional heteroatom selected from nitrogen, sulfur or oxygen.

Abstract: This invention concerns a compounds of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds with the nitrogen ring optional bonds being between one adjacent pair on ring atoms,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; said aryl or heteroaryl radicals being optionally substituted by one or more substituents the same or different,R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, optionally substituted C.sub.6 -C.sub.10 aryl, optionally substituted heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl,R' represents one or more optional substituents the same or different, selected from one or more of the following: halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.

Abstract: This invention relates to the use of 2-thioxotetrahydropyrimidin-4-one derivatives to increase HDL cholesterol concentration and as therapeutic compositions for treating atherosclerotic conditions such as dyslipoproteinemias and coronary heart disease. The compounds of this invention are represented by the formula: ##STR1## wherein: R is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.2 -C.sub.6 alkynyl; andR.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, halogen or lower alkyl.

Abstract: This invention relates to novel compounds which bind to central cholinergic muscarinic M1 receptors and may be useful for treatment of diseases attributed to cholinergic insufficiency such as presenile dementia, senile dementia of the Alzheimer's type, Parkinson's disease, Down's syndrome, and dementia pugilistica. The compounds useful in this invention have the formula ##STR1## or a 6, 7, 8, 9 tetrahydro analog thereof, where R.sup.1 is selected from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, cyano, halo, nitro, and --NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently selected from H, C.sub.1 -C.sub.6 alkyl and phenyl, optionally substituted with halo, cyano, hydroxy, nitro, amino, mono or di C.sub.1 -C.sub.6 alkylamino, phenylamino, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy;R.sup.2 is CF.sub.3 --, CF.sub.3 CH.sub.2 --, or --CH.sub.2 --X--R.sup.6 where X is oxygen or NH and R.sup.6 is C.sub.1 -C.sub.6 alkyl, phenyl-(CH.sub.2).sub.n -- or --(CH.sub.2).

Abstract: This invention concerns a compound of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; optionally substituted by one or more substituents the same or different,R' represents one or more optional substituents the same or different, selected from the following: halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6 )alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxylamino, optionally substituted C.sub.6 -C.sub.10 or heteroaryl or an optionally substituted (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical; andR" represents one or more optional mono- or di- valent substituents in the 5, 7 or 8 positions the same or different: monovalent substituents being selected from the following: C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkanoyloxy, hydroxy, amino, C.

Abstract: This invention relates to clear aqueous solutions of hydrocortisone which are free of lower alcohols. When applied to the skin, either directly or by wipe, the solution is practically invisible and has a further advantage that the solution will not irritate or dry the skin or give the stinging sensation of an alcohol containing solution. Dissolution of hydrocortisone without alcohol is accomplished by using the anionic surfactant sodium dioctyl sulfosuccinate in mixtures of glycerin, propylene glycol and polyethylene glycol diluted to final volume with water.

Abstract: Compounds are disclosed which have the general formula A: ##STR1## where R.sup.a and R.sup.b are each hydrogen or methyl and R.sup.c is hydrogen, halo or C.sub.1-4 alkyl optionally in the form of a pharmaceutically acceptable acid addition salt. The compounds are useful in the treatment of CNS disorders.

Abstract: The compound of the formula: ##STR1## where R.sub.1 is H, alkyl, perhaloalkyl, arylalkyl, alkenyl or alkynyl; R.sub.2 is H when R.sub.4 is other than H, and, when R.sub.4 is H, R.sub.2 is ##STR2## in which R.sub.5 is hydrogen or alkyl; R.sub.3 is hydrogen or halogen; R.sub.4 is H or ##STR3## X and Y are nitrogen and Z is carbon; n is 1 or 2; n.sub.1 is 0, 1, 2, 3, 4, or 5; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.

Abstract: This invention relates to methods of treating neurological illnesses related to acetylcholine deficiency in the CNS including memory loss attending senility, Parkinson's disease, Down's syndrome or senile pugilistica by administering a therapeutically effective compound of the formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are, independently, H, alkyl, halo, perhaloalkyl, hydroxy, alkoxy, aryl or arylalkyl; n is an integer from 0-5; R is azabicyclo?2.2.2!octyl or azabicyclo?2.2.1!heptyl when n.sub.1 is zero, or R is NR.sub.4 R.sub.5 when n.sub.1 is 1, 2, 3, 4, or 5, in which R.sub.4 and R.sub.5 are alkyl or R.sub.4 and R.sub.5, taken with the nitrogen atom to which they are attached, are N-(substituted aryl)piperazinyl in which said substituent is alkoxy, halo or perhaloalkyl; N-(pyridyl)piperazinyl; N-(pyrimidinyl)piperazinyl; or 3-azabicyclo-?3.2.2!non-3-yl; X is oxygen or NH; n and n.sub.1 are, independently, one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof.

Abstract: This invention concerns compounds of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted line represents an optional bond,one of R.sup.1 and R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.16 aralkyl, --(CHR.sup.6).sub.n CHR.sup.7 CN, --(CHR.sup.6).sub.n CHR.sup.7 CONH.sub.2, --(CHR.sup.6).sub.n CHR.sup.7 COOR.sup.8, --(CHR.sup.6).sub.n CHR.sup.7 CH.sub.2 OH wherein n is 0 or 1, R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.1 -C.sub.6 alkyl- or C.sub.7 -C.sub.16 aralkyl-, and R.sup.7 also represents hydroxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.2 -C.sub.7)alkanoyloxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6 alkoxy)carbonyl- and R.sup.8 is hydrogen or C.sub.1 -C.sub.6 alkyl;the other of R.sup.1 and R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl; R.sup.3 is C.sub.6 -C.sub.10 aryl or heteroaryl group optionally substituted by one or more substituents the same or differnet,R.sup.2 and R.sup.

Abstract: Piperazine derivatives of formula (I) and their salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, R, R.sup.2 and R.sup.4 are hydrogen or lower alkyl, R.sup.1 is mono- or bicyclic aryl or heteroaryl, R.sup.3 is lower alkyl or cycloalkyl, A is an alkylene chain and X is --CO--. --CR.sup.5 OH-- (where R.sup.5 is hydrogen, lower alkyl or cycloalkyl), --S--, --SO-- or --SO.sub.2 -- or X can also be --(CH.sub.2).sub.n -- (where n is 0, 1 or 2) when R.sup.3 is cycloalkyl.

Abstract: This invention relates to compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are both hydrogen or R.sup.1 and R.sup.2 form a bond;m=1 and n=3 and p=6,or m=3, 5 or 7 and n=1 and p=6,or m=4 and n=2 and p=6 or 8,and the E (trans) and Z (cis) isomers when R.sup.1 =R.sup.2 =H;and the basic addition salts thereof which are inhibitors of phospholipase A.sub.2 and are thus useful agents in the treatment of inflammatory diseases where arachidonic acid metabolic products are implicated, such as rheumatoid arthritis, inflammatory bowel diseases such as ulcerative colitis, atopic dermatitis conditions such as psoriasis and immediate hypersensitivity reactions such as allergic bronchial asthma and allergic rhinitis; and as gastric cytoprotective agents.

Abstract: This invention concerns a compound of generic formula ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group;R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl C.sub.6 -C.sub.10 aryl, heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl;R' represents one or more optional substituents the same or different, selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6)alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxylamino, C.sub.6 -C.sub.10 or heteroaryl or an (C.sub.6 -C.sub.

Abstract: This invention relates to 4-formyl-2-(naphthalenylmethyl)phenoxyacetic acids and pharmaceutically acceptable salts thereof according to formula I below, pharmaceutical compositions thereof, a method of treating hyperglycemia due to non-insulin dependent diabetes mellitus, and a method of prevention or treatment of complications associated with diabetes. ##STR1## wherein the group A is selected from the group consisting of 1-naphthyl, 2-naphthyl, optionally substituted with alkyl of from one to six carbon atoms, fluorine, chlorine, bromine, iodine, trifluoromethyl, alkoxy of from one to six carbon atoms; R.sup.1 is hydrogen or alkyl of from one to six carbon atoms; R.sup.2 is selected from hydrogen, fluorine, chlorine, bromine, iodine, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, and hydroxyl; or a pharmaceutically acceptable metal salt thereof.

Abstract: Amide Derivatives of formula (I) wherein R.sup.1 is a mono or bicyclic heteroaryl radical, R.sup.2 is cycloalkyl, R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl, and R.sup.5 is a group of formula (A) or (B) or (C): R.sup.8 --CH.sub.2 --CH.sub.2 -- or (D) or (E): R.sup.9 OCH.sub.2 CHOHCH.sub.2 -- or (F): R.sup.9 OCH.sub.2 CH.sub.2 -- and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.

Abstract: Piperazine derivatives of formula (I) and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, A is an optionally substituted alkylene chain, Z is a specified bicyclic nitrogen containing heteroaromatic radical, R is hydrogen or lower alkyl, R.sup.1 is aryl or aryl(lower)alkyl and R.sup.2 and R.sup.3 are hydrogen or specified organic radicals or --NR.sup.2 R.sup.3 represents a heterocyclic ring.

Abstract: This invention relates to a technique for treating a mammal with rapamycin which comprises removal of blood from the patient, treatment of the formed blood elements with rapamycin which binds rapidly and reversibly with erythrocytes, and returning the treated blood cells to the circulatory system of the patient for the treatment of any of the diseases, syndromes, conditions, or immune responses which respond to treatment with rapamycin. Alternatively, blood to be treated with rapamycin can be obtained from a hematologically compatible donor mammal.

Abstract: Piperazine derivatives of formula (I) and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, R and R.sup.3 are hydrogen or lower alkyl or R.sup.3 is spirocycloalkyl, R.sup.1 and R.sup.2 are aryl or heteroaryl radicals and n is 1 or 2 and m is 1 to 3 and the total of n+m is 2-4.

Abstract: Amide Derivatives of formula (I): R.sup.5 NR.sup.4 (CR.sub.2).sub.2 CHR.sup.3 CONR.sup.1 R.sup.2 and their pharmaceutically acceptable salts are 5-HT1A binding agents and may be used, for example, as anxiolytics. The radicals, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have specified meanings.