Carl Joseph Goddard

CP-66,948: An antisecretory histamine H2-receptor antagonist with mucosal protective properties

CP-66,948 is a histamine H2-receptor antagonist with gastric antisecretory activity and mucosal protective properties. The affinity of CP-66,948 for the guinea pig atria histamine H2-receptor is 15 times greater than that of cimetidine and seven times greater than that of ranitidine.In vivo, the ED50 value for inhibition of gastric acid secretion in pylorusligated rats is 2 mg/kg intraduodenally, and in histamine or pentagastrin-stimulated Heidenhain pouch dogs the antisecretory ED50 values are 0.3 mg/kgper os and 1.0 mg/kgper os, respectively. CP-66,948 also inhibits ethanol-induced gastric hemorrhagic lesions in rats following either oral or systemic administration (ED50 values of 12 mg/kgper os and 6 mg/kg subcutaneously). In addition, the mucosal protective activity is independent of prostaglandin synthesis. CP-66,948 inhibits gastric acid secretion in man, and its mucosal protective activity may provide additional benefits in peptic ulcer therapy.

An Improved Method of Chlorinating 2-alkoxynicotinic Acids

Abstract A novel chlorination process for preparing 5-chloro-2-alkoxynicotinic acids has been developed using commercial 5.25% sodium hypochlorite (Clorox®) as a chlorinating agent.

Synthesis Of N,N′-Diaralkyl 2H-1,2,6-Tetrahydrothiadiazines

Abstract Several derivatives of the 2H-1,2,6-Lctrahydrothiadiazine ring system have been synthesized by the interaction of the sulfur transfer reagent N,N-thiobisphthalimide (TBP) with appropriately substituted N,N′-bis-(benzyl)-1,3-diaminopropanes.