Abstract: 2-(Pyrrol-1-yl)amino-4,5-dihydro-1H-imidazole derivatives of the following general formula I ##SPC1##wherein R, R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are independently selected from the class consisting of hydrogen, lower alkyl, carbo-lower alkoxy, phenyl, substituted phenyl, R.sub.4 represents hydrogen or lower alkyl, n is an integer and may be 2 or 3. The corresponding pharmaceutically acceptable acid addition salts of the substances of formula I above are considered as a part of the invention. The invention compounds display very interesting anthypertensive properties.
Abstract: Antimicrobial substances of the rifamycin family corresponding to the formula ##SPC1##Wherein R is a substituted lower alkyl radical of the formula --(CH.sub.2).sub.n --A wherein n is the number 2 or 3, A stands for a hydroxyl group or for an ##EQU1## group where R.sub.3 and R.sub.4 individually may be hydrogen, lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or cycloalkyl and together with the nitrogen atom to which they are attached a heterocyclic ring; R.sub.1 is hydrogen or taken with R it may represent a lower alkylene radical to complete with the nitrogen atoms to which they are attached a heterocyclic ring; R.sub.2 is hydrogen or, when the nitrogen atom to which it is attached is a part of a heterocyclic ring a lower alkyl group. The compounds are prepared by condensing 4-guanylazo-4-deoxyrifamycin SV with a substituted aliphatic amine derivative corresponding to the formula H.sub.2 N--(CH.sub.2).sub.n --A wherein n and A have the significance previously given.
Abstract: New reserpine-like compounds of the general formula ##SPC1##Wherein R is a member of the class consisting of hydrogen, lower alkyl, lower alkenyl and acyl; R.sub.1 is selected from hydrogen and lower alkyl, and R.sub.2 is hydrogen or lower alkyl. The new reserpine-like compounds are useful anti-hypertensive agents.
Type:
Grant
Filed:
May 24, 1974
Date of Patent:
August 31, 1976
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Emilio Occelli, Luigi Fontanella, Giangiacomo Nathansohn
Abstract: The novel antibiotic, lipiarmycin, is prepared by cultivating Actinoplanes deccanensis A/10655, ATCC 21983, under aerobic conditions in a fermentation broth, from which it is then recovered.
Type:
Grant
Filed:
October 31, 1974
Date of Patent:
August 31, 1976
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Carolina Coronelli, Francesco Parenti, Richard White, Hermes Pagani
Abstract: A new class of 2,3-benzoxazepine compounds of the formula ##SPC1##In the formula, R is heterocyclic acyl or heterocyclic acetyl. The compounds have central nervous system and anti-inflammatory activity.
Type:
Grant
Filed:
November 14, 1974
Date of Patent:
June 1, 1976
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Giorgio Pifferi, Amedeo Omodei-Sale', Pietro Consonni
Abstract: 2-Nitroimidazole derivatives of the general formula ##SPC1##Wherein R is a lower alkyl group and Y is a member of the group consisting of --CH.sub.2 OH, --CHO, CH.sub.3 CO--, vinyl, formylvinyl, styryl, substituted iminomethyl, 2-benzimidazolyl and 5-amino-1,3,4-thiadiazol-2-yl. The term "lower alkyl" designates aliphatic groups of from 1 to 4 carbon atoms; the term "substituted iminomethyl" designates nitrogen-containing functional derivatives of the aldehydic group. The compounds have antimicrobial activity.
Abstract: Process for preparing an .alpha.-aminoalcohol of formula ##EQU1## wherein R represents hydrogen or alkyl of from 1 to 5 carbon atoms, which comprises contacting a compound of formula ##EQU2## wherein R has the same meaning as above, with an alcohol of formula R'-OH wherein R' represents benzyl or the group ##EQU3## in which R" and R"' are independently selected from hydrogen and alkyl of from 1 to 4 carbon atoms in an organic solvent, in the presence of a basic catalyst, at from about 140.degree. to about 170.degree.C., treating the obtained product of formula ##EQU4## wherein R and R' have the above meanings, with at least an equimolecular amount of a p-toluene-sulfonyl halide, at from about -5.degree. to about 20.degree.C. in the presence of a tertiary organic nitrogen-containing base and reacting in a closed system the resulting compound of formula ##EQU5## wherein R and R' are as above defined, with an excess of gaseous ammonia, in the presence of an inert organic solvent, at from about 95.degree.
Abstract: 5,6,7,7A-Tetrahydro-1H-pyrrolo[1,2-c]imidazole-1,3-(2H)-diones of the formula ##SPC1##In which R is phenyl, substituted phenyl or cyclohexyl, X is oxygen or sulfur and R.sub.1 is hydroxy, lower alkoxy, di-lower alkylamino-lower alkoxy, an --NR.sub.2 R.sub.3 radical wherein R.sub.2 and R.sub.3 each independently represents hydrogen, lower alkyl, hydroxy-lower alkyl, phenyl, substituted phenyl, benzyl or together with the adjacent nitrogen atom represent a pyrrolidino, a piperidino, a morpholino or a piperazino radical. The compounds of the invention are useful as C.N.S. depressants and in particular as tranquilizing and anxiolytic agents.
Abstract: Antibiotic activities produced by a variety of Streptosporangium vulgare named Streptosporangium vulgare var. antibioticum var. nov. ATCC 21906. The antibiotic complex contains at least the active fractions named A, B and C.
Type:
Grant
Filed:
January 31, 1975
Date of Patent:
April 6, 1976
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Carolina Coronelli, Maria Rosa Bardone, Hermes Pagani
Abstract: Aminopropanols with .beta.-blocking activity having the general formula ##SPC1##Wherein R is hydrogen, C.sub.1 -C.sub.4 alkyl or hydroxy-(C.sub.2 -C.sub.4) alkyl, R.sub.1 is C.sub.1 -C.sub.4 alkyl or hydroxy-(C.sub.2 -C.sub.4) alkyl; R.sub.2 and R.sub.3 each independently represent hydrogen or C.sub.1 -C.sub.2 alkyl, R.sub.4 is hydrogen or alkoxy of 1 to 4 C, n is the number 1 or 2; and their pharmaceutically acceptable acid addition salts.
Abstract: The present invention is concerned with new derivatives of 3-formylrifamycin SV. More particularly the invention relates to O-substituted oximes of 3-formylrifamycin SV of formula I. ##SPC1##wherein R is selected from the group consisting of alkyl of at least 2 carbon atoms, alkenyl, alkynyl, cycloalkyl, alkoxyalkyl, cycloalkoxyalkyl, hydroxyalkyl, carboxyalkyl, carboalkoxyalkyl, carbamylalkyl, cyanoalkyl, nitroalkyl, aryloxyalkyl, aralkoxyalkyl, heterocycloxyalkyl, aminoalkyl, mono- and di-lower alkylaminoalkyl, substituted benzyl, mono- or poly-aryl substituted C.sub.2 -C.sub.8 alkyl and lower alkyl substituted with mono- or polynuclear heterocyclic rings containing at least one 1 to 3 heteroatom selected from oxygen, nitrogen and sulfur, with the exclusion of morpholine; R.sub.1 is H or CH.sub.3 CO; and the derivatives of the same oximes hydrogenated in at least one of the positions 16, 17; 18, 19; and 28, 29. These compounds have antimicrobial activity.