Hydroxyalkyl and aryl or heterocyclic substituted-4,5-dihydropyridazin(2H)-3-ones and diazabicyclo-ene-ones e.g., 6-(p-chlorophenyl)-2-(2-hydroxybutyl)-4,5-dihydropyridazin(2H)-3-one are prepared by condensing 1-hydrazino-2-alkanols with aryl or heterocyclic-.gamma.-keto acids and are useful as central nervous system depressants.

Ozonolysis of 3-bromomethyl-2-cephem-4-carboxylic acid esters provides 1-(1-protected carboxy-2-hydroxy-3-bromo-1-propenyl)-3-amido(or imido)-4-formylthio-azetidin-2-ones, useful as intermediates in the preparation of cephalosporin antibiotics.

Novel 2-aryl-2-[.omega.-(diisopropylamino)alkyl]-.omega.-(azabicycloalkyl)alkana mides are described herein. The present compounds are useful as anti-arrhythmic agents. The compounds are prepared by reacting an appropriate disubstituted acetonitrile with an appropriate .omega.-(azabicycloalkyl)alkyl halide and subsequent hydrolysis of the resulting nitrile with concentrated sulfuric acid.

Compounds of formula (I) in which R.sup.1 and R.sup.2, which may be the same or different, is each selected from hydrogen, halogen or C.sub.(1-8) alkyl; R.sup.3 is aryl or aryl C.sub.(1-4) alkyl which may be optionally substituted; X is a linker group; Y is an optionally substituted aryl group; and n is 0, 1 or 2; are inhibitors of the enzyme Lp-PLA.sub.2 and thereof of use in treating atherosclerosis.

The present invention comprises a compound of formula I: ##STR1## R.sub.1 of Formula I is substituted amino represented by formula NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1-4 alkyl, and unsubstituted amino with the proviso that R.sup.5 and R.sup.6 are not both hydrogen, and further that R.sup.5 and R.sup.6 are not both amino. R.sub.2 and R.sub.3 of Formula I are independently selected from the group consisting of hydrog...

A method of preparing intermediates for carbapenem antibiotics characterized by treating a N-deprotected acetoxy conpound of the formula: ##STR1## in the presence of a Lewis acid or a silylating agent to yeild an intermediate; and cyclizing the intermediate in the presence of rhodium (II) acetate to form a bicyclic ketoester.

Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein m is three or four; wherein z is selected from the group consisting of ##STR2## wherein when Z is ##STR3## n and p are integers of from one to four, with a sum of four or five, and when Z is ##STR4## n and p are integers of from one to three, with a sum of three or four; wherein A is s...

A method for the treatment of cerebrovascular disorders and/or disorders associated with cerebral senility and/or allergic disorders, proliferative skin disorders, and bronchodilation which method comprises the administration of an effective, non-toxic amount of a compound of formula (I): ##STR1## or if appropriate a pharmaceutically acceptable salt thereof, wherein R.sup.1 and R.sup.2 each independently represent alkyl or a moiety of formula (a): wherein m represents zero or an integer 1, 2 or ...

This invention provides a process for preparing a compound of formula III ##STR1## wherein R.sup.1 is bromo, iodo or COOR.sup.2 ; R.sup.2 is H, C.sub.1 -C.sub.4 alkyl, phenyl which may be substituted or benzyl; and A is a 5- or 6-membered aromatic residue which may contain up to three hetero atoms and which may optionally be substituted with one or two groups selected from the group consisting of halo, hydroxy, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy; or a salt thereof, which compris...

The process for preparing 2-amino-6-iodopurine including the steps of suspending at least one chloropurine compound selected from 2-formylamino-6-chloropurine, 2-formylamino-6-chloropurine acetate and 2-amino-6-chloropurine in a solution comprising aqueous hydriodic acid and an alkyl ketone having 3 to 7 carbon atoms; and stirring the resulting suspension at 0.degree. to 50.degree. C. According to the process of the present invention, 2-amino-6-iodopurine can be simply, industrially, and advanta...