| 摘要 |
1,2,5-thiadiazole 1-oxides and 1,1-dioxides of formula (I) and their salts, hydrates, solvates and N-oxides are new where R1 is OH or NR2R3; R2 and R3 are H, lower alkyl alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, aminoalkyl, mono- or dialkylaminoalkyl, pyrrolidino-, piperidino-, morpholino-, piperazino- or pyridylalkyl, NH2, alkylamino, dialkylamino, CH2CF3, CH2CH2F, OH, alkoxy, 2,3-dihydroxypropyl, CN, cyanoalkyl, amidino, alkylamidino, A(CH2)mZ(CH2)n, or phenyl or phenylalkyl opt. ring-substd. by 1 or 2 gps. , provided that R2 and R3 are not both cycloalkyl, opt. substd. phenyl, NH2, (di)alkylamino, OH, alkoxy, CN, (alkyl) amidino or A(CH2)mZ(CH2)n; or R2+R3 is CH2CH2X(CH2)r, where r is 1-3 and X is CH2, S, O or NR4, provided that X is CH2 when r is 1; R4 is H, alkyl, alkenyl, alkynyl, alkanoyl or benzoyl. Each m is 0-2; each n is 2-4; each Z is S, O, or CH2; each A is a phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl gp. opt. substd. by 1 or 2 substituents, the 1st being selected from alkyl, OH, CF3, halogen, NH2, CH2OH, alkoxy, (CH2)qN:C(NHR4)2 and (CH2)qNR5R6, and the 2nd being selected from alkyl, OH, CF3, halogen, NH2, CH2OH and alkoxy; q is 0-6; each R4 is as defined above or the 2 R4 gps. together form CH2CH2; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl or phenyl, but not both cycloalkyl or phenyl, or NR5R6 is pyrrolidino, morpholino, piperidino, methylpiperidino, N-methylpiperazino or homopiperidino. p is 1 or 2. (I) are histamine H2 antagonists which inhibit gastric acid secretion and are thus useful as anti-ulcer agents. |
