Abstract: 3H-naphtho[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for (C.sub.1-6)alkyl, (C.sub.3-6)alkenyl, (C.sub.3-6)alkynyl or (C.sub.3-7)cycloalkyl, R.sub.1 and R.sub.2, each independently may represent hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkylthio, (C.sub.1-4)alkoxy or halo(C.sub.1-4)alkoxy, R.sub.3 and R.sub.4, each independently, represent hydrogen or (C.sub.1-4)alkoxy, R.sub.5 stands for hydrogen, (C.sub.1-4)alkyl, (C.sub.3-4)alkoxy, mono- and di-(C.sub.2-4)alkylamino, (C.sub.2-4)alkanoylamino, carboxymethoxy and [carbo(C.sub.1-4)alkoxy]methoxy and R.sub.6 is hydrogen or R.sub.4 and R.sub.6 taken together may represent a methylenedioxy radical with the proviso that when R.sub.5 is hydrogen at least one of R.sub.3 and R.sub.4 must be different from hydrogen, useful as antimicrobial agents.
Abstract: The present invention relates to a glycopeptide antibiotic arbitrarily designated as A/16686 antibiotic, and to its physiologically-acceptable acid addition salts. Antibiotic A/16686 free base, and its acid addition salts are antibacterial agents, especially active against grampositive microorganisms. The process for producing antibiotic A/16686 by culturing a novel strain of the actinoplanes genus, designated as Actinoplanes sp. ATCC 33076, is a further object of the present invention.
Type:
Grant
Filed:
December 11, 1980
Date of Patent:
May 4, 1982
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Bruno Cavalleri, Hermes Pagani, Giancarlo Volpe
Abstract: New tricyclic ortho-fused nitrogen containing compounds of the following formula: ##STR1## wherein R and R.sub.1 are independently selected from hydrogen, fluoro, chloro, bromo and (C.sub.1 -C.sub.4)alkoxy; A may be --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --(CH.sub.2).sub.3 --; X represents a nitrogen atom or the group CH; and salts therewith of pharmaceutically acceptable acids.The compounds possess an outstanding antireproductive utility.
Abstract: The present invention relates to a glycopeptide antibiotic arbitrarily designated as A/16686 antibiotic, and to its physiologically-acceptable acid addition salts. Antibiotic A/16686 free base, and its acid addition salts are antibacterial agents, especially active against grampositive microorganisms. The process for producing antibiotic A/16686 by culturing a novel strain of the Antinoplanes genus, designated as Actinoplanes sp. ATCC 33076, is a further object of the present invention.
Type:
Grant
Filed:
March 31, 1980
Date of Patent:
December 1, 1981
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Bruno Cavalleri, Hermes Pagani, Giancarlo Volpe
Abstract: An apparatus for measuring the flowability of powder utilizes a container having a bottom wall with an opening therein. The bottom wall may be changed to provide openings of different sizes. The test consists of allowing the powder to flow through successively smaller holes. The smallest hole size through which the powder will freely flow is a measure of its flowability.
Abstract: New tricyclic ortho-fused nitrogen containing compounds of the following formula: ##STR1## wherein R and R.sub.1 are independently selected from hydrogen, fluoro, chloro, bromo and (C.sub.1 -C.sub.4)alkoxy; A may be --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --(CH.sub.2).sub.3 --; X represents a nitrogen atom or the group CH; and salts therewith of pharmaceutically acceptable acids.The compounds possess an outstanding antireproductive utility.
Abstract: The invention relates to new water soluble 3-formylrifamycin SV hydrazones wherein the hydrazone moiety contains a phosphonoxy lower alkyl radical which imparts water solubility. The compositions containing said rifamycin derivatives are also an object of this invention. The new rifamycin derivatives and their pharmaceutical compositions are particularly suitable for parenteral administration.
Abstract: New-pyrrolyl-3-pyridazineamines having a further aminic substituent in the position 6. The compounds are useful as antihypertensive agents and may be prepared from 6-amino substituted-3-hydrazino pyridazines and .beta.-dicarbonyl compounds. The use of the novel compounds as antihypertensives and compositions containing the novel compounds as active ingredients are also claimed.
Type:
Grant
Filed:
September 17, 1979
Date of Patent:
January 27, 1981
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Elvio Bellasio, Nunzio Di Mola, Ambrogio Campi, Emiliana Baldoli
Abstract: This invention relates to a novel antibiotic mixture and to the process for its production. This antibiotic mixture comprises a family of new antibiotic substances which may be separated and isolated as individual components.These antibiotic substances are referred to herein as antibiotic 8327 factor A, antibiotic 8327 factor B and antibiotic 8327 factor C.Antibiotic 8327 factor A is in turn a mixture of three fractions which will be referred to herein as teichomycin A.sub.1, teichomycin A.sub.2 and teichomycin A.sub.3. The novel antibiotic mixture is obtained by cultivation of strain Actinoplanes teichomyceticus nov. sp. ATCC 31121.
Type:
Grant
Filed:
April 16, 1979
Date of Patent:
December 16, 1980
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Carolina Coronelli, Grazia Beretta, Maria R. Bardone, Francesco Parenti
Abstract: Novel 4-desoxy-thiazole[5,4-c]rifamycin derivatives of formula I ##STR1## wherein R stands for a group --OR.sub.1, --NR.sub.2 R.sub.3 or --NHCOR.sub.4 wherein R.sub.1 represents alkyl, alkenyl, alkynyl, cycloalkyl, aryl or aralkyl, R.sub.2 and R.sub.3 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl and aralkyl or R.sub.2 and R.sub.3 taken together with the adjacent nitrogen atom may represent a 5 to 7 membered heterocyclic ring and R.sub.4 is a radical selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl and aralkyl; R.sub.5 is hydrogen or acetyl; and a process for preparing them.The novel compounds have an antibacterial utility.
Abstract: New tricyclic ortho-fused heterocyclic compounds of formula ##STR1## wherein A is the group ##STR2## or the group ##STR3## in which R represents hydrogen, (C.sub.1-4)alkyl, phenyl or tolyl and R.sub.1 and may be (C.sub.1-4)alkyl, phenyl or tolyl, R.sub.2 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkanoylmethyl, carbo(C.sub.1-3)alkoxymethyl, hydroxy(C.sub.2-4)alkyl, halo(C.sub.2-4)alkyl and a group ##STR4## wherein R.sub.3 is an alkylene group from 2 to 4 carbon atoms and R.sub.4 and R.sub.5 independently represent hydrogen or (C.sub.1-4)alkyl or, taken together with the nitrogen atom, a fully hydrogenated 5 or 6 membered heterocyclic radical which may contain a further heteroatom selected from O, N and S and be optionally substituted by a (C.sub.1-4)alkyl or phenyl group, or R.sub.2 may represent, nil the dotted lines x and y may represent nil or additional bonds; with the proviso that, when the symbol R.sub.
Abstract: A method for direct determination of the free fraction of an hormone in a biological fluid containing bound and unbound hormone in an equilibrium state. A fluid sample is contacted with a solid matrix capable of reversibly binding the free hormone without sensibly affecting the equilibrium state and the amount of adsorbed hormone is determined and directly correlated with the free hormone in the biological fluid. The method is particularly suitable for direct determination of free thyroxine and triiodothyronine in serum.
Abstract: Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 individually represent hydrogen or (C.sub.1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; carbo(C.sub.1-3)-alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, carbo(C.sub.1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R.sub.1 and R.sub.5 are methyl and R.sub.4 is carbethoxy, R.sub.2 and R.sub.
Abstract: Novel 4-desoxy-thiazolo[5,4-c]rifamycin derivatives of formula I ##STR1## wherein R stands for a group --OR.sub.1, --NR.sub.2 R.sub.3 or --NHCOR.sub.4 wherein R.sub.1 represents alkyl, alkenyl, alkynyl, cycloalkyl, aryl or aralkyl, R.sub.2 and R.sub.3 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl and aralkyl or R.sub.2 and R.sub.3 taken together with the adjacent nitrogen atom may represent a 5 to 7 membered heterocyclic ring and R.sub.4 is a radical selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl and aralkyl; R.sub.5 is hydrogen or acetyl; and a process for preparing them.The novel compounds have an antibacterial utility.
Abstract: Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 individually represent hydrogen or (C.sub.1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; carbo(C.sub.1-3)alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, carbo(C.sub.1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R.sub.1 and R.sub.5 are methyl and R.sub.4 is carbethoxy, R.sub.2 and R.sub.
Abstract: A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula ##STR1## wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; R is selected from hydrogen, amino, lower alkylamino, di-lower alkylamino, acylamino, diacylamino, ureido, thioureido, carbethoxythioureido, benzoylthioureido, sulfhydryl, lower alkyl, trifluoromethyl, phenyl, substituted phenyl, pyridyl, methylpyridyl and dimethylpyridyl; and R.sub.1 and R.sub.2 each independently represents hydrogen or lower alkoxy, by condensation of a 2-amino-3,4-dihydro-1(2H)-isoquinolinone with an imidolyl, cyanamide, cyanic or thiocyanic derivative.New compounds of the formula I wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, R has the same meaning as above with the exclusion of hydrogen, methyl, phenyl, and trifluoromethyl, R.sub.1 and R.sub.2 have the same meaning as above, with the proviso that when A represents the group --CH.dbd.CH--, R cannot be tolyl or pyridyl.
Type:
Grant
Filed:
April 23, 1979
Date of Patent:
December 23, 1980
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Amedeo Omodei-Sale, Pietro Consonni, Leonard Lerner