Abstract: There are described compounds of formula I, ##STR1## in which R.sub.1 represents benzofurazanyl, pyridyl or phenyl, the pyridyl or phenyl being substituted,--COOR.sub.2 and --COOR.sub.3 are various ester groups,one of R.sub.7 and R.sub.8 represents alkyl Cl to 6 and the other represents --CONR.sub.10 R.sub.11 ; --CSNH.sub.2 ; --C(.dbd.NH)SR.sub.9 ; --S(O).sub.m R.sub.9 ; phenyl optionally substituted by one or more of alkyl Cl to 6, halogen, alkoxy Cl to 6 or nitro; alkyl Cl to 6 substituted by halogen; or furanyl;m is 0 or 1R.sub.9 is alkyl Cl to 6, andR.sub.10 and R.sub.11 each independently represent hydrogen or alkyl Cl to 6, or together with the nitrogen atom to which they are attached form a 5 or 6 membered heterocyclic ring.There are also described processes for making the compounds, and pharmaceutical, e.g. calcium antagonist, formulations containing them.
Type:
Grant
Filed:
April 17, 1984
Date of Patent:
August 11, 1987
Assignee:
Fisons plc
Inventors:
Andrew J. G. Baxter, John Dixon, Kenneth J. Gould, Alan C. Tinker
Abstract: Derivatives of C-076 compounds are described in which the C-076 molecule, a series of macrolides, has the 23-hydroxy group thereof oxidized to the 23-keto group. The 23-keto compounds are prepared by selectively oxidizing the suitably protected 23-hydroxy compound using such oxidizing agents as pyridinium dichromate, chromic acid-dimethyl pyrazole, chromic acid, chromic acid-acetic acid, and the like. Alternatively, selective oxidation of the unprotected 23-hydroxy compound may be accomplished by placing the compound in soil. Further reaction of the oxidized C-076 compounds is also possible. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal, and acaricidal activity. Compositions containing the described C-076 derivatives as the active ingredient thereof are also disclosed.
Type:
Grant
Filed:
May 2, 1980
Date of Patent:
September 15, 1981
Assignee:
Merck & Co., Inc.
Inventors:
Helmut H. Mrozik, John G. MacConnell, August J. Kempf
Abstract: Process for purification of crude pyromellitic acid dianhydride produced by vapor phase oxidation of 1,2,4,5-tetraalkylbenzene with an oxygen-containing gas, having a purity of more than about 95% pyromellitic acid dianhydride. In a first distillation stage, said crude pyromellitic acid dianhydride is distilled at pressure of less than about 310 Torr, and temperature of less than about 350.degree. C to distill overhead an impurities containing fraction amounting to less than about 20% of the crude introduced into the first stage, and provide a residue enriched in pyromellitic acid dianhydride. In a second distillation stage, the residue of the first stage is distilled at lower pressure and at temperature of less than about 325.degree. C to distill overhead the purified pyromellitic acid dianhydride, and provide an impurities containing residue of less than about 12% of the crude introduced into the first step.