Abstract: A method of synthesizing fused ring pyridines (annulated) by co-oligomerization of .alpha.,.omega.-diynes with about molar equivalents of nitriles using a Co.sup.+1 catalyst preferably cyclopentadienyl cobalt dicarbonyl. Additionally, new compounds of tricyclic quinolizine-4-ones were produced where excess cyanoacetic ester starting materials were utilized (about 2:1 equivalent nitriles:diyne). The results with the catalyst employed indicated a stepwise mechanism in which cobalt(I) catalyst first forms a metallocycle intermediate derived from the bisacetylene. This cobalt(III) intermediate reacts preferentially with nitriles to give the product annulated pyridines in good yield. Generally, preferred conditions indicated roughly molar equivalents of reactants with no substantial excess of either reactant for the bicyclic compounds.

Abstract: A tetrahydroisoquinoline compound of the formula: ##STR1## wherein R.sup.1 is alkyl of one to six carbon atoms, cycloalkyl of three to six carbon atoms, allyl or propargyl, R.sup.2 is hydrogen or alkyl of one to six carbon atoms, and R.sup.3 is hydrogen, alkyl of one to six carbon atoms or benzyl. Methods for preparing the compound (I) are disclosed. The compound (I) and a pharmaceutically acceptable salt thereof are useful as a diagnostic or therapeutic agent for angiotensin-related hypertension.

Abstract: A 1,2,3,4-tetrahydroisoquinoline having smooth muscle relaxant activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or lower alkyl and X is --O-- or --S--, and pharmaceutically acceptable salts thereof.

Abstract: The compounds of formula I ##STR1## wherein R is(a) hydrogen,(b) cycloalkyl of 3 to 7 carbon atoms,(c) alkyl of 2 to 5 carbon atoms monosubstituted by hydroxy, with the proviso that the hydroxyl radical is separated by at least 2 carbon atoms from the carbonylthio moiety to which R is bound,(d) phenyl or phenylalkyl of 7 to 11 carbon atoms, each monosubstituted or independently disubstituted in the phenyl ring by alkyl of 1 to 4 carbon atoms or halogen of atomic number of from 9 to 35, or phenyl or phenylalkyl of 7 to 11 carbon atoms, each monosubstituted or independently disubstituted or independently trisubstituted in the phenyl ring by alkoxy of 1 to 4 carbon atoms, or(e) furyl, benzo[b]furyl, thienyl, benzo[b]thienyl, pyridyl, quinolyl, isoquinolyl, 2- or 3-pyrrolyl or indolyl other than 1-indolyl,R.sub.1 and R.sub.

Abstract: Isoquinoline derivatives of the formula ##STR1## wherein the substituent is such as chlorine or bromine; R.sub.1 is phenyl etc.; R.sub.2 is hydrogen, halogen etc.; R.sub.3 is e.g. aminoalkyl and their use as medicaments, in particular as antidepressants.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or methyl, is prepared by condensing a compound of the formula: ##STR2## wherein R.sup.2 is alkyl, aryl or aralkyl and R.sup.1 is same as above, or a reactive derivative thereof with 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid or an ester thereof to give a compound of the formula: ##STR3## wherein R.sup.3 is an ester residue and R.sup.1 and R.sup.2 are same as above, followed by hydrolysis or ammonolysis of said compound (IV). The compound (I) is useful as a diagnostic or therapeutic agent for angiotensin-related hypertension.

Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yields. The process involves reacting an alkylating agent and an activated methylene compound in the presence of an onium compound, an alkali metal compound and water, which while only necessary in trace amounts can be present in substantial quantities.

Abstract: The thiazepino-[4,3-b]-isoquinoline-1,5-diones of the formula: ##STR1## where R.sup.1 is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or halo;R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl;andR.sup.3 is hydrogen or alkyl of 1 to 3 carbon atoms and the open ring 3-carboxy isoquinoline precursors inhibit angiotensin converting enzyme and are useful anti-hypertensive agents.

Abstract: New chemical compounds, bis-quaternary carbamates, having the generic fora: ##STR1## wherein X is one equivalent of an anion selected from monovalent and polyvalent anions, n is 5-16, and R, R.sub.1, R.sub.2 are aliphatic radicals selected from the group consisting of methyl, ethyl, propyl, isopropyl, and butyl, and having utility as toxic agents.

Abstract: Useful intermediates for preparing a 1-dethia-1-oxacephalosporin and represented by the following formula: ##STR1## (wherein R is a monovalent group resulting from the elimination of the carbonyl function of an acyl group derived from a carboxylic or carbonic acid;COB is carboxy or protected carboxy; andX is hydrogen or a nucleophilic group)are prepared from the corresponding penicillin 1-oxides of the following formula: ##STR2## (wherein R, COB, and X are as defined above) by heating, if required in the presence of the desulfurizing reagent, or by exchanging the X group with another one under the condition of an appropriate nucleophilic substitution.

Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkanoyl; R.sub.2 is ##STR2## AND N IS 0, 1 OR 2; HAVE USEFUL HYPOTENSIVE PROPERTIES.

Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkanoyl; and one of R.sub.2, R.sub.3 and R.sub.4 is ##STR2## wherein R.sub.5 is alkyl, and the other groups are --CH.sub.2 --; have useful hypotensive activity.

Abstract: N.sup.2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.