Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.

Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers.

Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.

Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers.

Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.

Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.

Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anit-ulcer agents. Intermediates and processes for their preparation are disclosed.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, hydroxy, cyano, (lower)alkyl, (lower)alkoxy, halogen or amino; n is 2 or 3; X is NR.sup.3 or CHR.sup.3 ; R.sup.3 is cyano, nitro, SO.sub.2 Ar; or SO.sub.2 (lower)alkyl; R.sup.12 is hydrogen or (CH.sub.2).sub.p NR.sup.13 R.sup.14 ; p is an integer of from 1 to 4, inclusive; R.sup.13 and R.sup.14 each are independently hydrogen or (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents independently selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, hydroxy, cyano, (lower)alkyl, (lower)alkoxy, halogen or amino; n is 2 or 3; X is NR.sup.3 or CHR.sup.3 ; R.sup.3 is cyano, nitro, SO.sub.2 Ar; or SO.sub.2 (lower)alkyl; R.sup.12 is hydrogen or (CH.sub.2).sub.p NR.sup.13 R.sup.14 ; p is an integer of from 1 to 4, inclusive; R.sup.13 and R.sup.14 each are independently hydrogen or (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents independently selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, hydroxy, cyano, (lower)alkyl, (lower)alkoxy, halogen or amino; n is 2 or 3; X is NR.sup.3 or CHR.sup.3 ; R.sup.3 is cyano, nitro, SO.sub.2 Ar; or SO.sub.2 (lower)alkyl; R.sup.12 is hydrogen or (CH.sub.2).sub.p NR.sup.13 R.sup.14 ; p is an integer of from 1 to 4, inclusive; R.sup.13 and R.sup.14 each are independently hydrogen or (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents independently selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, (lower)alkyl, halogen or hydroxymethyl; m is 1 or 2, and n is 2 or 3, provided that the sum of m and n is 3 or 4; X and Y each are independently hydrogen, nitro, cyano, --SO.sub.2 Ar or --COR.sup.3, provided that X and Y are not both hydrogen; R.sup.3 is (lower)alkyl, Ar, (lower)alkoxy, amino or (lower)alkylamino; and Ar is an optionally substituted phenyl group; and nontoxic pharmaceutically acceptable acid addition salts thereof, are potent anti-ulcer agents. Also disclosed are processes for their preparation and novel intermediates of the formulae ##STR2## in which R.sup.1, X, Y and n are as defined above and R.sup.5 is (lower)alkyl, phenylalkyl or phenyl containing 1 or 2 substituents independently selected from nitro, chloro and bromo.

Abstract: Known cardiovascular agents of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently hydrogen, (lower)alkyl, (lower)alkoxy, (lower)alkylthio, trifluoromethyl, hydroxy, nitro, chloro, bromo or fluoro are prepared by reacting a compound of the formula ##STR2## in which R.sup.1 and R.sup.2 are as described above and R.sup.3 is hydrogen, (lower)alkyl or aryl, with a compound of the formula ##STR3## in which X is a leaving group as described herein.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 and R.sup.3 are the same or different and are hydrogen, (lower)alkyl, (lower)alkenyl, (lower)alkynyl or Ar; R.sup.4 is hydrogen or (lower)alkyl; n is an integer of from 1 to 6; p is 1 or 2 and q is 2 or 3, provided that the sum of p and q is 3 or 4; X is NR.sup.5 or CHR.sup.5 ; R.sup.5 is cyano, nitro, SO.sub.2 Ar or SO.sub.2 (lower)alkyl; and Ar is an optionally substituted phenyl group; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents. Processes for their preparation and novel intermediates are also disclosed.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 and R.sup.3 each are independently hydrogen, (lower)alkyl, guanidino or --(CH.sub.2).sub.p NR.sup.4 R.sup.5 ; R.sup.4 and R.sup.5 each are independently hydrogen, (lower)alkyl or phenyl; n is 2 or 3; p is 1, 2 or 3; X is NR.sup.6 or CHR.sup.6 ; R.sup.6 is cyano, nitro, SO.sub.2 Ar or SO.sub.2 (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, (lower)alkyl, halogen or hydroxymethyl; m is 1 or 2, and n is 2 or 3, provided that the sum of m and n is 3 or 4; X and Y each are independently hydrogen, nitro, cyano, --SO.sub.2 Ar or --COR.sup.3, provided that X and Y are not both hydrogen; R.sup.3 is (lower)alkyl, Ar, (lower)alkoxy, amino or (lower)-alkylamino; and Ar is an optionally substituted phenyl group; and nontoxic pharmaceutically acceptable acid addition salts thereof, are potent anti-ulcer agents. Processes for their preparation and novel intermediates are also disclosed.

Abstract: A series of novel 4-amino-2-(thiadiazole-carbonyl piperazinyl)-6,7-dimethoxyquinazolines is disclosed having antihypertensive properties. The thiadiazole substituent may be optionally substituted with alkyl or lower alkoxy carbonylamino groups. A representative embodiment of the invention is 4-amino-6,7-dimethoxy-2-[4-(5-ethoxy-carbonylamino-1,2,3-thiadiazole-4-car bonyl)-piperazin-1-yl]-quinazoline.

Abstract: Anti-ulcer agents of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive, are prepared by reacting a compound of the formula ##STR2## wherein X is a conventional leaving group, preferably in the form of its acid addition salt, with a compound of the formula ##STR3## wherein R.sup.1 is as defined above. The intermediates of Formula III may be prepared by reacting a cysteamine salt with an isothiourea of the formula ##STR4## wherein R.sup.1 is as described above, in the presence of a base.

Abstract: Novel compounds of the formula ##STR1## wherein each R.sup.1 is the same and is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive, which are useful intermediates in the preparation of anti-ulcer agents, are prepared by reacting cystamine (VI) with an N-cyano-N'-alkynyl-S-methylisothiourea of the formula ##STR2## in which R.sup.1 is as defined above.

Abstract: Anti-ulcer agents of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive, and non-toxic pharmaceutically acceptable acid addition salts thereof, are prepared by reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## wherein R.sup.1 is as defined above and R.sup.5 is (lower)alkyl, phenylalkyl or phenyl containing 1 or 2 substituents independently selected from nitro, chloro and bromo. The intermediates of Formula IV may be prepared by reacting the desired alkynylamine with a compound of the formula(R.sup.5 S).sub.2 C.dbd.NCN Vin which R.sup.5 is as described above.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive, and nontoxic pharmaceutically acceptable acid addition salts thereof, are potent anti-ulcer agents.