Abstract: The invention relates to bridged aza-bicyclic derivatives of formula (I). These compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. Also disclosed are intermediates used in the synthesis of compound of formula (I).

Abstract: The present invention is directed to a method of blocking N-methyl-D-aspartic (NMDA) acid receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and antiischemic) amount of 5-(1-hydroxy-2-piperidino)-propyl-2(1H,3H)-indolone analogs and the pharmaceutically acceptable salts thereof; methods of using these compounds in the treatment of stroke, head trauma, spinal cord trauma, traumatic brain injury, multiinfarct dementia, CNS degenerative diseases such as Alzheimer's disease, senile dementia of the Alzheimer's type, Huntington's disease, Parkinson's disease, epilepsy, amyotrophic lateral sclerosis, pain, AIDS dementia, psychotic conditions, drug addictions, migraine, hypoglycemia, anxiolytic conditions, urinary incontinence and an ischemic event arising from CNS surgery, open heart surgery or any procedure during which the function of the cardiovascular system is compromised.

Abstract: This invention relates to novel processes for synthesizing intermediates in the preparation of N-aryl and N-heteroarylamide inhibitors of the enzyme acyl coenzyme A: cholesterol acyltransferase (ACAT), and to novel intermediates used in such processes.

Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 55080. This novel antibiotic is useful as an anticoccidial in poultry, in the prevention and treatment of swine dysentery and as a growth promotant in cattle and swine.

Abstract: A compound of the formula ##STR1## is a novel immunosuppressant agent prepared by fermenting Steptomyces braeaensis subsp. pulcherrimus, ATCC 55150, or another compound of the formula I producing strain and extracting the compound of the formula I from the fermentation medium. The compound is useful in treating transplant rejection and autoimmune diseases.

Abstract: 2,4-diaminopyrimidine derivatives as potentiators of chemotherapeutic agents in the treatment of cancer.

Abstract: Process for the preparation of a dialkyl trans-piperidine-2,5-dicarboxylate from a corresponding dialkyl cis-piperidine-2,5-dicarboxylate via a trans-substituted pyridine derivative of the formula ##STR1## wherein R is a (C.sub.1 -C.sub.3)alkyl group.

Abstract: Selective muscarinic receptor antagonists of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are both optionally substituted phenyl, the broken line is an optional bond, X is >COH--, >SiOH-- or CH-- when the double bond is absent or is >C.dbd. when the double bond is present, X being attached to a carbon atom of A, A is selected from certain piperidine and pyrrolidine groups, n is 1 to 3 and R.sup.3 is optionally substituted phenyl or thienyl, pyridyl or pyrazinyl.

Abstract: The present invention relates to novel substituted hexahydroazepinones and tetrahydrobenzazepinones of the formulae ##STR1## wherein R.sup.1, Z.sup.1, Z.sup.2, W.sup.1, W.sup.2, Y.sup.1 and Y.sup.2 are as defined below, and to novel intermediates used in the synthesis of such compounds.Such compounds are useful in the treatment and prevention of gastrointestinal disorders, pain and anxiety disorders.

Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable salts thereof whereinR.sup.1 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or CONR.sup.5 R.sup.6 ;R.sup.2 is H or- C.sub.1 -C.sub.4 alkyl;R.sup.3 is C.sub.2 -C.sub.4 alkyl;R.sup.4 is H, C.sub.2 -C.sub.4 alkanoyl optionally substituted with NR.sup.7 R.sup.8, (hydroxy)C.sub.2 -C.sub.4 alkyl optionally substituted with NR.sup.7 R.sup.8, CH.dbd.CHCO.sub.2 R.sup.9, CH.dbd.CHCONR.sup.7 R.sup.8, CH.sub.2 CH.sub.2 CO.sub.2 R.sup.9, CH.sub.2 CH.sub.2 CONR.sup.7 R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, SO.sub.2 NH(CH.sub.2).sub.n NR.sup.7 R.sup.8 or imidazolyl;R.sup.5 and R.sup.6 are each independently H or C.sub.1 -C.sub.4 alkyl;R.sup.7 and R.sup.8 are each independently H or C.sub.1 -C.sub.4 alkyl, or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or 4-(NR.sup.10)-1-piperazinyl group wherein any of said groups is optionally substituted with CONR.sup.5 R.sup.6 ;R.sup.9 is H or C.sub.1 -C.sub.

Abstract: The compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein X, m, n, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined herein are useful in the treatment of shock and other TNF.alpha.-related disorders.

Abstract: Compounds of the formula ##STR1## wherein n is 1 to 5 and R is hydrogen, C.sub.1 to C.sub.4 alkyl, arylalkyl having from one to four carbon atoms in the alkyl moiety or arylalkyl substituted with one or more substituents selected independently from the group consisting of halogen, nitro, cyano, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, C.sub.1 to C.sub.6 halosubstituted alkyl, C.sub.1 to C.sub.6 hydroxysubstituted alkyl, C.sub.2 to C.sub.7 alkoxycarbonyl and aminocarbonyl, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.

Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 53764. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, and as a growth promotant in cattle and swine.

Abstract: This invention relates to certain azabicyclo hexane intermediates and processes for making and using the azabicyclo hexane intermediates. The intermediates are useful in the synthesis of quinolone antibacterial agents.

Abstract: 1S,4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.

Abstract: Benzimidazole anthelmintic agents of the formula (I) and their non-toxic salts, wherein R.sup.1, which is in the 5(6)-position, is either H or certain stated substituents, "alk" is a methylene or ethylene group; R.sup.2 is cyano, C.sub.1 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.2 -C.sub.4 alkanoyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenoxy, aryl, heteroaryl, aryl-(C.sub.1 -C.sub.4 alkoxy) or heteroaryl-(C.sub.1 -C.sub.4 alkoxy), in which "aryl" means phenyl optionally substituted by 1 to 3 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphinyl, and C.sub.1 C.sub.4 alkylsulphonyl in which "heteroaryl" means thienyl, furyl or pyridininyl all optionally substituted by 1 to 3 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphinyl and C.sub.1 -C.sub.4 alkylsulphonyl; and R.sub.3 is a C.

Abstract: Phosphorus containing polypeptides as renin inhibitors, useful as antihypertensive agents.

Abstract: A novel multi-step process for preparing the (4S)-enantiomer of 4-(3,4 -dichlorophenyl)-3,4-1(2H)- naphthalenone in a highly-optically pure form is disclosed. The process involved starts from the known 4-(3,4-dichlorophenyl)-4-ketobutanoic acid and proceeds through such intermediates as (1) isopropyl or tert.- butyl 4-(3,4 -dichlorophenyl)-4-ketobutanoate, (2) isopropyl or tert.-butyl 4-(3,4-dichlorophenyl)-(4R)-hydroxybutanoate, (3) isopropyl or tert.-butyl 4-(3,4-dichlorophenyl-(4R)-sulfonyloxybutanoate, (4) isopropyl or tert.-butyl 4-(3,4-dichlorophenyl)-(4R)-phenylbutanoate to finally yield the desired (4S)-4-(3,4-dichlorophenyl)-3,4-dihydro -1(2H)-naphthalenone compound in a highly-optically pure form. The latter compound, which is a (4S)-enantiomer per se, has utility as an intermediate that ultimately leads to pure cis-(1S)(4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthal eneamine (sertraline), which is a known antidepressant agent. The aforementioned isopropyl and tert.