Abstract: Anthracycline glycosides of the formula (I) ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other of R.sub.1 and R.sub.2 is hydroxy, each of R.sub.3, R.sub.4 and R.sub.5 is independently selected from the group consisting of hydrogen and hydroxy and X is hydrogen or trifluoroacetyl, with the provisos that R.sub.4 and R.sub.5 are not simultaneously hydroxy and that if R.sub.3 is hydroxy, then X is hydrogen, which are useful in treating certain mammalian tumors are prepared by condensing an aglycone of the formula (II) ##STR2## wherein R.sub.1 and R.sub.2 are defined as above, with a suitable protected halosugar, after which the protecting groups are removed.
Type:
Grant
Filed:
May 26, 1982
Date of Patent:
August 14, 1984
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Francesco Angelucci, Sergio Penco, Federico Arcamone
Abstract: The present invention relates to new 6-substituted 6H-dibenzo [b,d]pyran derivatives, to a process for their preparation and pharmaceutical and veterinary compositions containing them.
Type:
Grant
Filed:
October 1, 1981
Date of Patent:
July 31, 1984
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Piero Melloni, Paolo Salvadori, Pier P. Lovisolo
Abstract: A method is disclosed for purifying non-homogeneous systems, known as liposomic suspensions, from non-entrapped drugs wherein said suspensions are treated with liquid or solid polymers of synthetic and organic nature having chemical functionality, which are used as ion-exchangers. The liquid or solid polymers are based on styrene, divinylbenzene, acrylic acid, methacrylic acid, and the like, normally known as ion-exchange resins, and may include carboxylic, phosphonic, or sulphonic functions of different matrices. The ion-exchange resins may also include salified quaternary ammonium, primary, secondary and tertiary amminic or phosphinic functions or other functions with different matrices, including phenolformaldehyde, styrene-divinylbenzene, acrylates, methacrylates, hydrocarbons and condensation-resins.
Type:
Grant
Filed:
January 14, 1980
Date of Patent:
July 17, 1984
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Luigi Moro, Guido Neri, Alessandro Rigamonti
Abstract: There are provided azino rifamycin compounds of the formula (I): ##STR1## Y.dbd.H or CH.sub.3 CO; R.sub.1 linear or branched C.sub.1 -C.sub.7 alkyl or C.sub.3 -C.sub.4 alkenyl- R.sub.2 =linear or branched C.sub.1 -C.sub.7 alkyl, C.sub.2 -C.sub.4 chloroalkyl, C.sub.3 -C.sub.4 alkenyl, Cycloalkyl having 3 to 7 C atoms in the ring, cycloalkyl alkyl having 3 to 6 C atoms in the ring, phenyl, or C.sub.7 -C.sub.8 aralkyl, unsubstituted or mono-substituted by a halogen atom in the aryl group; or NR.sub.1 R.sub.2 =a cyclic moiety having 5 to 8 C atoms, unsubstituted or substituted by 1 or 2 CH.sub.3 groups, morpholino.The compounds inhibit the growth of gram positive bacteria and Mycobacterium tuberculosis.Oxidized compounds, preparative methods and pharmaceutical compositions are also described and claimed.
Type:
Grant
Filed:
September 29, 1982
Date of Patent:
May 8, 1984
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Giovanni Franceschi, Leonardo Marsili, Aurora Sanfilippo, Sergio Vioglio
Abstract: Pharmacologically active thiazolo[3,2-a]pyrimidines of the formula ##STR1## wherein A is a bond between the .alpha. and .beta.-carbon atoms or (--CH.sub.2 --) group; R.sub.1 and R.sub.2 represent hydrogen or halogen, C.sub.1 -C.sub.4 alkyl, cyano, CF.sub.3, thienyl, pyridyl, biphenyl, naphtyl, phenyl optionally substituted, ##STR2## wherein R' and R" are hydrogen or alkyl; R.sub.3 represents hydrogen, halogen, alkyl, OH, formyloxy, alkanoyloxy, alkenyloxy; R.sub.4 represents pyridyl optionally substituted by alkyl. The compounds have antiinflammatory, antiulcerogenic and anti-gastric secretory activity.
Type:
Grant
Filed:
July 14, 1982
Date of Patent:
April 24, 1984
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Gianfederico Doria, Carlo Passarotti, Giuliana Arcari, Ada Buttinoni
Abstract: Starting from the known 4'-deoxy-4'-iodo-N-trifluoroacetyldaunorubicin, two new anthracycline glycosidic antibiotics, the 4'-deoxy-4'-iodo-daunorubicin and 4'-deoxy-4'-iodo-doxorubicin, have been prepared by known procedures. Both the new glycosides have been found to be endowed with outstanding antitumoral activity.
Type:
Grant
Filed:
April 14, 1982
Date of Patent:
March 20, 1984
Assignee:
Farmaitalia Carlo Erba S.p.A
Inventors:
Antonino Suarato, Sergio Penco, Federico Arcamone, Anna M. Casazza
Abstract: Substituted Pyrrolo [2,1-b] and Pyrido [2, 1 b] Quinazolines are provided, together with pharmaceutical compositions, containing them. The compounds have pharmaceutical utility, and are particularly useful for the treatment of or prevention of the formation of gastrointestinal ulcers.
Type:
Grant
Filed:
June 10, 1982
Date of Patent:
January 31, 1984
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Gianfederico Doria, Carlo Passarotti, Giuliana Arcari
Abstract: Fluoro-prostaglandin compounds are disclosed, such as, for instance, 18,19,20-trinor-17-cyclohexyl-16(S,R)-fluoro-PGF.sub.2.alpha.. The fluoro-prostaglandins of the present invention have the same therapeutical uses as natural prostaglandins, but have the advantage of being resistant to the enzyme 15-prostaglandin dehydrogenase, and also exhibit a more selective therapeutical action. Certain of the compounds of the present invention exhibit very favorable luteolytic and antiulcer activity.
Abstract: Anthracycline glycosides W, X, Y and Z which are prepared by the fermentation of mutant F.I. 416 of Streptomyces peucetius var. caesius. The new compounds are useful against both gram positive and gram negative bacteria and as antitumor agents.
Type:
Grant
Filed:
November 16, 1981
Date of Patent:
December 20, 1983
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Giovanni Rivola
Abstract: Anthracycline antibiotics of the formula: ##STR1## wherein R is --CO--CH.sub.2 OH, --CHOH--CH.sub.3, --CO--CH.sub.3 or --CH.sub.2 --CH.sub.3 having antitumor and antibacterial activity are prepared by culturing a new mutant strain of microorganism designated as Micromonospora peucetica sp. nova and which has been deposited with the American Type Culture Collection under number No. 31366 ATCC.
Type:
Grant
Filed:
September 2, 1981
Date of Patent:
October 25, 1983
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Giovanni Rivola
Abstract: Ethers of substituted hydroxymethylpyrazines, such as, for instance, the compound 2-methoxymethyl-5-methylpyrazine-4-oxide. The compounds exhibit elevated lipid-lowering activity, especially anti-lipolytic activity (decrease of plasma-free fatty acids), triglyceride-lowering activity, cholesterol-lowering activity, and plasma-phospholipid-lowering activity.
Type:
Grant
Filed:
November 16, 1981
Date of Patent:
September 27, 1983
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Paolo Cozzi, Antonio Pillan, Leone Bertone, Pier P. Lovisolo
Abstract: A method and apparatus for controllably and reproducibly introducing small amounts of a liquid sample into chromatographic systems, especially high resolution gas chromatographic systems and thin-layer chromatographic systems, order to obtain sampling extremely reduced in volume and presenting maximum reliability and reproducibility, uses a sample container having a pipette-like or nozzle-like outlet neck of very small diameter. The liquid placed in the container is submitted to at least one pressure pulse which is controlled in time and/or amplitude in order to determine emission of a corresponding and controlled quantity of liquid from the outlet neck. The pressure pulse can be a pneumatic pulse directly applied to the liquid sample in the container, or a mechanical pulse applied to the liquid sample through a device acting by magnetostriction or by a piezoelectric system.
Type:
Grant
Filed:
September 23, 1981
Date of Patent:
September 20, 1983
Assignee:
Carlo Erba Strumentazione S.p.A.
Inventors:
Giorgio Sisti, Sorin Trestianu, Ermete Riva
Abstract: An apparatus for controlling the injection passage of on-column injector is disclosed. The apparatus includes a valve having at least one channel inside it and leading to the injection passage for the injection syringe needle. The channel is connected outside the injector to a source for carrier gas introduction, when the valve is open, or to the atmosphere, when the valve is closed, so as to allow a quick-type injection without the drawbacks of this injection type, as well as to have a solvent exhaust after injection.
Type:
Grant
Filed:
December 30, 1980
Date of Patent:
September 13, 1983
Assignee:
Carlo Erba Strumentazione S.p.A.
Inventors:
Giorgio Sisti, Bruno Tosi, Sorin Trestianu, Mario Galli
Abstract: A method of treating pain of whatever origin and nature in human and animal which comprises administering to the patient in need an effective amount of a polypeptide of structure: ##STR1## wherein X is selected from the group consisting of hydrogen, t-butyloxycarbonyl(Boc), Asp, Pyr-Glu, Pyr-Gln-Asp, Pyr-Asn-Asp; Y is selected from the group consisting of Thr, Met, Leu, Nle, Val; W is selected from the group consisting of Met, Nle, Leu.
Type:
Grant
Filed:
March 5, 1982
Date of Patent:
August 23, 1983
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gerhard Zetler, Alessandro Rossi, Chiara De Paolis
Abstract: The invention relates to a connecting device for fluid circuits in column chromatography. To ensure an inert connection without dead volumes, the device comprises a glass or fused silica thick-wall body with an inner capillary channel connected to the outside through radial holes. In such holes, metal or fused silica capillaries are inserted and each fixed by means of a coupling carrying a capillary set screw and a coupling fixing screw, with said screws acting on opposite positions of said body wall.
Abstract: Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-threo-hexopyranosy l chloride; 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-arabino-hexopyrano syl chloride or 2,3,6-trideoxy-4-C-trifluoroacetamidomethyl-3-trifluoroacetamido-3-O-trifl uoroacetyl-L-lyxo-hexopyranosyl chloride.
Type:
Grant
Filed:
October 29, 1981
Date of Patent:
July 12, 1983
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Alberto Bargiotti, Giuseppe Cassinelli, Sergio Penco, Federico Arcamone, Annamaria Casazza
Abstract: Heteromonocyclic and heterobicyclic derivatives of unsaturated 7-ayclamide-3-cephem-4-carboxylic acid are disclosed, and process for preparing same. These compounds are suitable for treating infections caused by Gram-positive and Gram-negative microorganisms.
Type:
Grant
Filed:
August 21, 1981
Date of Patent:
June 14, 1983
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Giuliano Nannini, Ettore Perrone, Dino Severino, Giuseppe Meinardi, Gisella Monti, Alberta Bianchi, Angelo Forgione, Carlo Confalonieri
Abstract: This invention relates to a method and a device for vaporization injection of a liquid sample in a gas chromatographic column housed in an oven comprising a direct on column injector suitable for injecting a liquid sample into the initial zone of a capillary column and capable of pneumatically sealing the injection port at the end of injection. Between the injector and the gas chromatographic column itself an uncoated capillary column length is provided in which vaporization of the injected sample occurs using heat from an oven housing said capillary column length, said oven being the same or separate from the oven containing said gas chromatographic column.
Type:
Grant
Filed:
November 6, 1981
Date of Patent:
May 17, 1983
Assignee:
Carlo Erba Strumentazione S.p.A.
Inventors:
Giorgio Sisti, Mario Galli, Sorin Trestianu
Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen atom or a methoxy group;X represents an oxygen or sulphur atom or an NH or NCH.sub.3 group;R.sub.3 represents a hydrogen atom, a trifluoromethyl or phenyl group or a hydrocarbon group having from 1 to 4 carbon atoms;R.sub.4 represents a hydrogen atom, a methyl or acetyl group or a hydrocarbon having from 1 to 4 carbon atoms, or R.sub.3 and R.sub.4 together represent a 3- or 4-membered carbon atom chain;Y represents an electron-withdrawing group such as a cyano, nitro, alkylsulphonyl or alkylsulprinyl group or a group of the formula COR.sub.5 wherein R.sub.5 represents an alkyl group having from 1 to 4 carbon atoms or a phenyl, alkoxy, amino or N-substituted amino group or R.sub.5 and R.sub.3 together represent a 2- or 3-membered carbon atom chain;R.sub.6 represents a hydrocarbon group having from 1 to 4 carbon atoms or a benzyl or phenethyl group; andR.sub.