摘要:
NEW BSICALLY SUBSTITUTED BENZYL PHTHALAZONE DERIVATIVES OF FORMULA I
2-((-Y-)>CH-(X)P-),4-(((R1)M-PHENYL)-CH2-),(R2)N-
PHTHALAZIN-1(2H)-ONE
AND THEIR PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF. THESE NEW BENZYL PHTHALAZONE DERIVATIVES ARE EXCELLENT ANTIBISTAMINES AND THEREFORE USEFUL IN THE TREATMENT OF HISTAMINE INDUCED DISTURBANCES.
摘要:
m-(1-(Cyclopropylmethyl)-3-isopentyl-3-azetidinyl)-phenol, and its acid-addition salts and phenolate salts. The compounds have pharmacological activity and exhibit a selective pattern of analgesic action. They can be produced by reducing the carbonyl group of m-(1-(cyclopropylcarbonyl)-3-isopentyl-3azetidinyl)phenol. The starting material can be obtained by a sequence of steps beginning with the reaction of diethyl carbonate, m-methoxyphenylacetonitrile, sodium ethoxide, and 1bromo-3-methylbutane, followed by operations to form the azetidine ring and introduce the N-cyclopropylcarbonyl group.
摘要:
DISCLOSED HEREIN ARE SUBSTITUTED 1-(1-ADAMANTYL)-2-CARBOXY-AZACYCLIC COMPOUNDS AND CERTAIN DERIVATIVES THEREOF. THEIR COMPOSITIONS ARE PARTICULARLY USEFUL IN THE TREATMENT OF PARKINSONISM.
摘要:
2,2-Disubstituted-azetidines, optionally substituted in addition at the 1,3, and 4 positions, useful as CNS stimulants and as blood pressure-lowering agents.
(WHEREIN R1 is an amino group or a blocked amino group; and R2 is an aliphatic, araliphatic or aromatic group while R3 is the residue of a thiophilic sulphur nucleophile or is a group of formula
OR R2 is a hydrogen atom while R3 is the residue of a thiophilic sulphur nucleophile or may, when R1 is a phenylacetamido or phenoxyacetamido group, be a group of formula II in which R2 is hydrogen) are provided. The new compounds are useful as intermediates in the production of cephalosporins, penicillins and related Beta -lactam antibiotic compounds. The new compounds may be obtained from penicillin 1-oxides by cleavage of the 1,2sulphur-carbon bond thereof and attachment of the group -SR3 to the sulphur atom in one or more stages.
摘要:
THE 1-LOWER ALKYL (AND 1-LOWER HYDROXYALKYL)-1-(3CHLORO-2-HYDROXYPROPLY)-3-HYDROXYAZETIDINIUM CHLORIDES ARE MONOFUNCTIONAL AND COMPATIBLE WITH WATER-SOLUBLE PROTEINS AT NORMAL STORAGE TEMPERATURES, BUT ACT AS BIFUNCTIONAL CROSS-LINKING AGENTS AT ELEVATED TEMPERATURES.
摘要:
DISCLOSED HEREIN ARE N-ADAMANTYL-3-AZETIDINOLS AND CERTAIN DERIVATIVES THEREOF. THESE NOVEL COMPOUNDS ARE USEFUL IN PROPHYLACTICALLY TREATING CERTAIN VIRTAL INFECTIONS.