Patents Assigned to Alfa Farmaceutici S.p.A.
  • Patent number: 4557866
    Abstract: A new process for the synthesis of pyrido-imidazo-rifamycins of formula ##STR1## wherein R is hydrogen or acetyl, R.sub.1 and R.sub.2 independently represent hydrogen, (C.sub.1-4)-alkyl, benzyloxy, mono- or di-(C.sub.1-3)-alkylamino-(C.sub.1-4)-alkyl, (C.sub.1-3)-alkoxy-(C.sub.1-4)-alkyl, hydroxymethyl, hydroxy-(C.sub.2-4)-alkyl, cyano, halogen, nitro, mercapto, (C.sub.1-4)-alkylthio, phenylthio, carbamoyl, mono- or di-(C.sub.1-4)-alkyl-carbamoyl, or R.sub.1 and R.sub.2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups.The process comprises reacting the rifamycin O of formula ##STR2## with a 2-aminopyridine of formula ##STR3## wherein R.sub.1 and R.sub.2 have the same meanings as before.
    Type: Grant
    Filed: April 26, 1985
    Date of Patent: December 10, 1985
    Assignee: ALFA Farmaceutici S.p.a.
    Inventors: Vincenzo Cannata, Gian F. Tamagnone
  • Patent number: 4515809
    Abstract: Derivatives of benzoylphenoxyalkanoic acids corresponding to the formula: ##STR1## wherein: X represents for example a halogen, R.sup.1 and R.sup.2 represent for example alkyl groups, R represents for example an aminoacid; and the salts thereof are new products showing antilipaemic and anticholesterolemic pharmacological activity.
    Type: Grant
    Filed: April 20, 1981
    Date of Patent: May 7, 1985
    Assignee: Alfa Farmaceutici S.p.A.
    Inventors: Valerio Borzatta, Manlio Cristofori, Mauro Morotti, Giuseppe Mascellani
  • Patent number: 4454145
    Abstract: New compounds of general formula ##STR1## and salts therewith of pharmaceutically acceptable acids, wherein R and R.sub.1 independently represent a hydrogen atom or a straight or branched alkyl group having from 1 to 5 carbon atoms, and n is an integer from 4 to 12; and of general formula ##STR2## wherein R'.sub.1 represents a straight or branched alkyl group having from 2 to 4 carbon atoms, W represents hydroxymethyl or the COOM group in which M stands for a hydrogen atom, an alkali metal or an equivalent of an alkali earth metal and n is an integer from 6 to 8. The compounds are useful in treating hyperlipidaemia.
    Type: Grant
    Filed: April 19, 1982
    Date of Patent: June 12, 1984
    Assignee: Alfa Farmaceutici S.p.A.
    Inventors: Manlio Cristofori, Valerio Borzatta, Mauro Morotti
  • Patent number: 4399284
    Abstract: A new process for the optical resolution of mixtures of d- and 1-2-(6-methoxy-2-naphthyl)-propionic acids, which comprises preparing a solution of a mixture of d-and 1-2-(6-methoxy-2-naphthyl)-propionic acids and an optically active organic base in a predetermined organic solvent, slowly cooling the obtained solution and seeding with crystals of a salt of d-2-(6-methoxy-2-naphthyl)-propionic acid with the optically active organic base containing a certain amount by weight of the organic solvent, and treating the obtained product with mineral acids in suitable organic solvents to obtain the free d-2-(6-methoxy-2-naphthyl)-propionic acid.
    Type: Grant
    Filed: July 13, 1981
    Date of Patent: August 16, 1983
    Assignee: Alfa Farmaceutici S.p.A.
    Inventors: Vincenzo Cannata, Graziano Zagnoni
  • Patent number: 4378373
    Abstract: Derivatives of benzoylphenoxyalkanoic acids corresponding to the formula: ##STR1## wherein: X represents for example a halogen, R.sup.1 and R.sup.2 represent for example alkyl groups, R represents for example an aminoacid; and the salts thereof are new products showing antilipaemic and anticholesterolemic pharmacological activity.
    Type: Grant
    Filed: April 20, 1981
    Date of Patent: March 29, 1983
    Assignee: Alfa Farmaceutici S.p.A.
    Inventors: Valerio Borzatta, Manlio Cristofori, Mauro Morotti, Giuseppe Mascellani
  • Patent number: 4341785
    Abstract: New rifamicyn derivatives of the following general formula ##STR1## wherein: A may be the structure ##STR2## --x-- is a chemical bond or nil; R is hydrogen or acetylR.sub.1 and R.sub.2 independently represent hydrogen, (C.sub.1-4) alkyl, benzyloxy, mono- and di-(C.sub.1-3)alkylamino- (C.sub.1-4)alkyl, (C.sub.1-3)alkoxy- (C.sub.1-4)alkyl, hydroxymethyl, hydroxy-(C.sub.2-4)-alkyl, nitro or R.sub.1 and R.sub.2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups; R.sub.3 is a hydrogen atom or nil;with the proviso that, when A is A.sub.1, --x-- is nil and R.sub.3 is a hydrogen atom; with the further proviso that, when A is A.sub.2, --x-- is a chemical bond and R.sub.3 is nil.The compounds possess antibacterial utility.
    Type: Grant
    Filed: May 11, 1981
    Date of Patent: July 27, 1982
    Assignee: Alfa Farmaceutici S.p.A.
    Inventors: Egidio Marchi, Lauretta Montecchi
  • Patent number: 4340585
    Abstract: A non-toxic anionic resin selected from resins having a polymeric reticulated skeleton of styrenic or acrylic type, inert to the digestive enzymes, having a molecular weight higher than 1000 and containing ionizable amino groups, resins having a cellulosic reticulated skeleton modified by the introduction of free or substituted amino groups and resins having a polysaccharide reticulated skeleton modified by the introduction of free or substituted amino groups. The resin is capable of binding itself permanently to the biliary acids and is salified with an acid corresponding to the general formula: ##STR1## wherein: R' represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms,R represents a chlorine atom or a group selected from p-chlorobenzoyl, p-bromobenzoyl and p-fluorobenzoyl,W represents a group selected from OH, --N(R"')--CH(R")-(CH.sub.2).sub.n --COOH and O--CH.sub.
    Type: Grant
    Filed: December 11, 1979
    Date of Patent: July 20, 1982
    Assignee: Alfa Farmaceutici, S.p.A.
    Inventors: Valerio Borzatta, Manlio Cristofori, Angelo Brazzi
  • Patent number: 4246201
    Abstract: Compound of formula: ##STR1## wherein R represents hydrogen or an alkyl group having from 1 to 4 carbon atoms; R', R", R'" and R"", equal or different from each other represent hydrogen atoms or OH groups, with the limitation that when R', R", R'" and R"" are all hydrogen atoms R cannot be an hydrogen atom and their salts with organic and inorganic pharmaceutically acceptable salts.The process for the preparation of the compounds of the above general formula are disclosed.The compounds show a good pharmacological activity and can be used as antiulcer, antispastic spasmolytic drugs.The compounds can be administered as different pharmaceutical preparations containing an effective dose of the compound in combination or in admixture with excipients suitable for oral or parenteral administration or for topical use.
    Type: Grant
    Filed: June 11, 1979
    Date of Patent: January 20, 1981
    Assignee: Alfa Farmaceutici, S.p.A.
    Inventor: Valerio Borzatta
  • Patent number: 4200574
    Abstract: 8-amino and 8-iminorifamycins S and SV are prepared by reacting 8-methoxyrifamycin S with ammonia in an inert polar and hydrophillic solvent, converting the 8-iminorifamycin S into 8 aminorifamycin S by reaction with ammonium hydroxide in a mixture of chloroform and methanol and, if so desired, reducing the S forms to SV forms by reduction.
    Type: Grant
    Filed: December 11, 1978
    Date of Patent: April 29, 1980
    Assignee: Alfa Farmaceutici, S.p.A.
    Inventors: Egidio Marchi, Lauretta Montecchi
  • Patent number: 4200573
    Abstract: New compounds being derivatives of 3-carboxyrifamycin S and SV are prepared by oxidation of cyanohydrin of 3-formylrifamycin S to 3-(cyanocarbonyl)rifamycin S, condensation with a compound of formula HR (an alcohol, an amine or an substituted hydrazine) and, optionally, reduction of the derivative of 3-carboxyrifamycin S so obtained to the corresponding SV form. Alternatively 3-(cyanocarbonyl)rifamycin S may be converted to the SV form before condensing with the compound HR.
    Type: Grant
    Filed: December 11, 1978
    Date of Patent: April 29, 1980
    Assignee: Alfa Farmaceutici, S.p.A.
    Inventors: Mario Brufani, Egidio Marchi, Pierfranco Bellomo, Giuseppe Mascellani
  • Patent number: 4179438
    Abstract: A process is disclosed for the preparation of 3 iodo-3 bromorifamycin S which consists in reacting rifamycin S with at least 2 equivalents of the corresponding halogen in the presence of at least one mole of pyridine for each equivalent of halogen. The reaction is carried out in inert, polar, hydrofillic solvents at a temperature not above the room temperature. The yields are very high and the products obtained have a high degree of purity.
    Type: Grant
    Filed: November 6, 1978
    Date of Patent: December 18, 1979
    Assignee: Alfa Farmaceutici, S.p.A.
    Inventors: Egidio Marchi, Lauretta Montecchi
  • Patent number: 4168375
    Abstract: A process for the recovery of cephalosporin C from an aqueous medium, including the steps of treating the medium with a sulphonyl chloride of formula R--SO.sub.2 Cl, in which R is a substituted or unsubstituted alkyl group having from 4 to 10 carbon atoms, or a substituted or unsubstituted aryl group, to convert the cephalosporin C to the corresponding sulphonamide and extracting the sulphonamide with an essentially water immiscible solvent. The sulphonyl chloride may be toluene-p-sulphonyl chloride, p-isopropylbenzenesulphonyl chloride or .beta.-naphthalenesulphonyl chloride. The molar ratio of sulphonyl chloride to cephalosporin C present in the aqueous medium is from 3 to 10. The temperature of the reaction of sulphonyl chloride with cephalosporin C is maintained in the range from 10.degree. to 20.degree. C. The water immiscible solvent is selected from ethyl acetate, n-butanol and methylisobutylketone. The pH of the reaction medium is maintained at a value of from 7.5 to 9.5 by means of a buffering agent.
    Type: Grant
    Filed: February 11, 1975
    Date of Patent: September 18, 1979
    Assignee: Alfa Farmaceutici, S.p.A.
    Inventors: Renato Andrisano, Giuseppe Mascellani, Guido Guerra
  • Patent number: 3931161
    Abstract: Novel cephalosporin derivatives, for example N-acetoacetylcephalosporin C, N-decanoylcephalosporin C, N-dodecanoylcephalosporin C and N-hendecenoylcephalosporin C, are useful as readily-recoverable intermediates in the isolation of cephalosporin C value from fermentation broths and in the preparation of 7-aminocephalosporanic acid. They are prepared by treating an aqueous solution containing cephalosporin C, such as a fermentation broth, with diketene or an acid chloride such as decanoyl chloride, dodecanoyl chloride or hendecenoyl chloride, followed by solvent extraction. They are converted into 7-aminocephalosporanic acid by successively forming the silyl di-ester, halogenating to the imino-halide, converting the imino-ether and hydrolysing to 7-ACA.
    Type: Grant
    Filed: March 6, 1973
    Date of Patent: January 6, 1976
    Assignee: Alfa Farmaceutici S.p.A.
    Inventors: Carlo Buitar, Giuseppe Mascellani, Guido Guerra