Patents by Inventor Giovanni Franceschi

Giovanni Franceschi has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5416208
    Abstract: Antibacterial penems of formula (I), where R represents a hydrogen atom or a hydroxy protecting group, are prepared by reacting a .beta.-lactam of formula (II) with an oxalyl halide in an inert solvent in the presence of an organic or inorganic base or an acid scavenger to produce a compound of formula (III), wherein X is a halogen atom, treating the resultant compound of formula (III) with a 1,3-dioxolen-2-one of formula (IV), wherein Y is a hydroxy group, in the presence of molecular sieves or an organic or inorganic base to produce a compound of formula (V), and cyclizing the compound of formula (V) in the presence of a trialkylphosphite to provide the penems of formula (I).
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 16, 1995
    Assignee: Farmitalia Carlo Erba S r l
    Inventors: Ettore Perrone, Marco Alpegiani, Franco Zarini, Giuseppe Mazzini, Giovanni Franceschi
  • Patent number: 5374626
    Abstract: The present invention relates to the use as antivirals of compounds of formula: ##STR1## wherein B is a purinic or pyrimidinic heterocycle; X is oxygen or sulphur; R.sup.1 is a hydroxyl group or a hydrogen atom; R.sup.2 is a linear, branched or cyclic, alkyl group of up to twenty carbon atoms; R.sup.3 is as specified for R.sup.2 above or a hydrogen atom, a cation or a polyhydroxy group.
    Type: Grant
    Filed: March 12, 1993
    Date of Patent: December 20, 1994
    Assignee: Farmitalia Carlo ERBA
    Inventors: Carlo Battistini, Giovanni Franceschi, Domenico Ungheri, Maria A. Verini, Sergio Vioglio
  • Patent number: 5348952
    Abstract: Cephalosporins of the formula (I): ##STR1## wherein m is one or two; n is zero, one or two; A and B are organic residues; and R.sub.1 and R.sub.2 are halogen or hydrogen atoms or organic groups are endowed with elastase inhibitory activity. Two processes for their preparation starting from the corresponding 4-acyl cephem are also provided.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: September 20, 1994
    Assignee: Farmitalia Carlo Erba S.R.L.
    Inventors: Pierluigi Bissolino, Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Giuseppe Cassinelli, Giovanni Franceschi
  • Patent number: 5077286
    Abstract: Compounds of formulae Ia and Ib ##STR1## wherein A is hydrogen atom or an organic residue, R.sup.1 is halogen atom, or an organic group, R.sup.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, R.sup.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, benzyl or a methylene group and R.sub.4 is an organic residue are disclosed. Compounds (Ia) and (Ib) are endowed with elastase inhibitory activity. A two-step process for their preparation starting from the corresponding 4-carboxy cephem or 3-carboxy penam is also provided.
    Type: Grant
    Filed: April 10, 1989
    Date of Patent: December 31, 1991
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Pierluigi Bissolino, Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Giuseppe Cassinelli, Giovanni Franceschi
  • Patent number: 5051416
    Abstract: A method is provided for treating a warm-blooded animal having a susceptible bacterial infection which comprises administering orally to said animal a non-toxic, antibacterially effective amount of acetoxymethyl ester of (5R,6S)-2(5R,6S)-2-carbamoyloxymethyl-6-[1(R)-hydroxyethyl]-2-penem-3-carb oxylic acid.
    Type: Grant
    Filed: April 3, 1989
    Date of Patent: September 24, 1991
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Maurizio Foglio, Giovanni Franceschi, Aurora Sanfilippo
  • Patent number: 4956373
    Abstract: Orally administrable pharmaceutical compositions comprising 3-(N-piperidinomethyl-azino)methylrifamycin S as the active substance are disclosed. The active substance is easily soluble in water even at low pH values and is provided with good bioavailability. Such compositions are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: May 18, 1989
    Date of Patent: September 11, 1990
    Assignee: Farmitalia Carlo Erba S.R.L
    Inventors: Giovanni Franceschi, Sergio Vioglio, Roberto Bianchini
  • Patent number: 4952577
    Abstract: A substantially (.gtoreq.95%) optically pure (5R,6S,1'R) penem of formula ##STR1## and the pharmaceutically acceptable salts and the ester prodrugs thereof, are endowed with antibacterial activity.
    Type: Grant
    Filed: June 6, 1988
    Date of Patent: August 28, 1990
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Giovanni Franceschi, Ettore Perrone, Franco Zarini, Constantino Della Bruna
  • Patent number: 4886793
    Abstract: There are provided compounds of formula I: ##STR1## wherein R.sup.1 is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy or halogen atom;R.sup.2 is a free or esterified carboxy group or carboxylate anion;R.sup.3 and R.sup.4 are each independently hydrogen or organic group,X is --O--, ##STR2## --S--, Q is either(a") free or protected hydroxy, or(b") a C.sub.1 -C.sub.1 acyloxy, or(c") carbamoyloxy OCONH.sub.2, or(d") an optionally substituted heterocyclylthio group, or(e") an optionally substituted imido group, or(f") an optionally substituted quaternary ammonium group or(g") a halogen atom,A and the pharmaceutically or veterinarily acceptable salts thereof. There are provided also methods for preparing compounds of formula I. The compounds of formula I are useful as antibacterial agents.
    Type: Grant
    Filed: March 5, 1987
    Date of Patent: December 12, 1989
    Assignee: Farmitalia Carlo Erba, S.r.l.
    Inventors: Ettore Perrone, Marco Alpegiani, Angelo Bedeschi, Franco Zarini, Costantino Della Bruna, Giovanni Franceschi
  • Patent number: 4863914
    Abstract: Compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.4 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, A is a Z, Z--O--C--O-- or Z--C)-- residue, wherein Z is phenylene, naphthylene, heterocyclediyl, C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.4 alkenylene, alkynylene, ##STR2## C.sub.3 -C.sub.8 cycloalkylene, aralkylene radical optionally substituted, and O.sup.(+) represents a group +NR.sub.1 R.sub.2 R.sub.3, wherein R.sub.1, R.sub.2 and R.sub.3 are each either:(i) a optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2 and R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical, or(iii) R.sub.1, R.sub.2 and R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical, or(iv) R.sub.1, R.sub.2 and R.sub.
    Type: Grant
    Filed: April 8, 1986
    Date of Patent: September 5, 1989
    Assignee: Farmitalia Carlo Erba
    Inventors: Ettore Perrone, Marco Alpegiani, Angelo Bedeschi, Franco Zarini, Giovanni Franceschi, Costantino D. Bruna
  • Patent number: 4837215
    Abstract: Compounds of the following formula I ##STR1## wherein X represents a sulphur or an oxygen atom,R is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy group and halogen atom;A is a Z, Z--O--CO-- or --Z--CO-- residue, whereinZ represents(a) an optionally substituted phenylene or naphthylene group,(b) an optionally substituted heterocyclediyl radical wherein the hetero ring is mono or bicyclic, saturated or unsaturated containing at least one heteroatom selected from the group of oxygen, sulphur and nitrogen;(c) an optionally substituted linear or branched C.sub.1 -C.sub.7 alkylene radical;(d) a C.sub.2 -C.sub.4 alkenylene or alkynylene group or a group of formula ##STR2## (e) an optionally substituted C.sub.3 -C.sub.8 cycloalkylene ring; (f) an aralkylene radical of the formula ##STR3## wherein n is 1, 2 or 3; andQ.sup.(+) represents a +NR.sub.1 R.sub.2 R.sub.3 group, wherein(i) R.sub.1, R.sub.2, R.sub.
    Type: Grant
    Filed: April 8, 1986
    Date of Patent: June 6, 1989
    Assignee: Farmitalia Carlo Erba
    Inventors: Ettore Perrone, Marco Alpegiani, Angelo Bedeschi, Franco Zarini, Giovanni Franceschi, Costantino D. Bruna
  • Patent number: 4713450
    Abstract: A new process is described for the preparation of (5R)-penem derivatives of the general formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or an organic group; R.sub.2 represents a hydrogen atom or a carboxy protecting group and Y represents a hydrogen or halogen atom or an organic group. A 2-thiacephem derivative of the general formula II: ##STR2## wherein R.sub.1, R.sub.2 and Y have the meanings/given above is oxidized by means of organic peracids to the corresponding sulphone of the general formula III: ##STR3## which is subsequently submitted to a desulphurative ring contraction by extrusion of SO.sub.2 to give exclusively the desired (5R)-penem derivatives of the general formula I.
    Type: Grant
    Filed: January 24, 1986
    Date of Patent: December 15, 1987
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Franceschi, Ettore Perrone
  • Patent number: 4713378
    Abstract: There are provided compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.3 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, and Q.sup.(+) represents a group ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are each either: (i) optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2, R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical or(iii) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical or(iv) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted fused pyridinium radical or(v) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted pyrazimium, pyrazolium or pyridazinium radical, and the pharmaceutically or veterinarily acceptable salts thereof.A method of preparation is also provided.The compounds show high antibacterial activity.
    Type: Grant
    Filed: June 24, 1985
    Date of Patent: December 15, 1987
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Ettore Perrone, Marco Alpegiani, Franco Zarini, Costantino D. Bruna, Giovanni Franceschi
  • Patent number: 4631150
    Abstract: A process for preparing 2-methyl substituted penems useful as antibiotics agent and/or as intermediates thereof, by reacting an appropriate 1-imido-3,4-disubstituted azetidinone derivative with a trivalent organophosphorus compound in an inert solvent at a temperature of from 110.degree. to 150.degree. C. for a period of from 2 hours to a few days.
    Type: Grant
    Filed: August 6, 1984
    Date of Patent: December 23, 1986
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Carlo Battistini, Maurizio Foglio, Giovanni Franceschi, Cosimo Scarafile
  • Patent number: 4623643
    Abstract: Penem derivatives are disclosed characterized by a substituted pyridiniomethyl group in the 2-position of the penem nucleus. The compounds of the present application exhibit better antibacterial activity than other known penem derivatives.
    Type: Grant
    Filed: June 10, 1985
    Date of Patent: November 18, 1986
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Franceschi, Ettore Perrone
  • Patent number: 4585874
    Abstract: A new process is described for the preparation of (5R)-penem derivatives of the general formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or an organic group; R.sub.2 represents a hydrogen atom or a carboxy protecting group and Y represents a hydrogen or halogen atom or an organic group. A 2-thiacephem derivative of the general formula II: ##STR2## wherein R.sub.1, R.sub.2 and Y have the meanings/given above is oxidized by means of organic peracids to the corresponding sulphone of the general formula III: ##STR3## which is subsequently submitted to a desulphurative ring contraction by extrusion of SO.sub.2 to give exclusively the desired (5R)-penem derivatives of the general formula I.
    Type: Grant
    Filed: December 6, 1983
    Date of Patent: April 29, 1986
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Franceschi, Ettore Perrone
  • Patent number: 4577016
    Abstract: A process for the preparation of compounds of formula (I) ##STR1## wherein R.sub.1 is hydrogen or an organic group;R.sub.2 is hydrogen or a carboxy protecting group; andY is a group-S-heterocyclic, acyloxy, alkoxy, alkylthio, pyridyl, which group may be substituted, or azido, and penem derivatives falling within the scope of formula (I) and pharmaceutically or veterinarily acceptable salts thereof.The process involves displacing a group L in the Y position with a reagent Y-H.
    Type: Grant
    Filed: April 4, 1983
    Date of Patent: March 18, 1986
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Franceschi, Ettore Perrone
  • Patent number: 4558042
    Abstract: There are disclosed .beta.-lactam-containing compounds of the formula: ##STR1## where R is hydrogen, lower alkyl, trichloroethyl, acetonyl, benzyl, substituted benzyl, phenyl, substituted phenyl, benzidryl or a residue that will undergo metabolic activation "in vivo" and have favorable pharmacokinetic properties; R.sup.1 is a hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, or hydroxyalkyl, with the alcoholic function of the hydroxyalkyl being free or protected; Z is hydrogen, halogen, hydroxy, amino, carbamoyloxy, mercapto, pyridinium, OR.sup.2, OCOR.sup.2, NHCOR.sup.2, or SR.sup.3 wherein each of R.sup.2 and R.sup.3 is any of lower alkyl, aryl, or a heterocyclic ring, each of which may be substituted or unsubstituted, and n is 0 or 1. The compounds have broad spectrum antibacterial activity and .beta.-lactamase inhibiting activity. Processes for the production of the .beta.-lactam-containing compounds and various intermediates in the production of those compounds are also disclosed.
    Type: Grant
    Filed: March 30, 1984
    Date of Patent: December 10, 1985
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Maurizio Foglio, Giovanni Franceschi, Cosimo Scarafile, Federico Arcamone, Aurora Sanfilippo
  • Patent number: 4508649
    Abstract: Processes for the preparation of a penem derivative of formula I ##STR1## wherein n=0 or 1; R is a carboxy protecting group or H;R.sub.1 is hydrogen, a hydrocarbon group substituted or unsubstituted, or lower alkoxy; andR.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, carbamoyl N-substituted by lower alkyl or unsubstituted, or an acyl group;and the pharmaceutically acceptable salts thereof.These processes allow one to prepare stereospecifically only 5R derivatives, and are characterized by R.sub.2 -introduction at a very late stage in the synthesis, thereby enabling a great number of compounds of formula I to be prepared.Penem derivatives are useful antibacterial agents.
    Type: Grant
    Filed: December 6, 1982
    Date of Patent: April 2, 1985
    Assignee: Farmitalia Carlo Erba
    Inventors: Marco Alpegiani, Carlo Battistini, Angelo Bedeschi, Giovanni Franceschi, Maurizio Foglio, Franco Zarini
  • Patent number: 4507295
    Abstract: Azinomethyl-rifamycins I ##STR1## (wherein Y=H or COCH.sub.3 and either R.sub.1 =C.sub.1 -C.sub.7 alkyl or C.sub.3 -C.sub.4 alkenyl and R.sub.2 =C.sub.1 -C.sub.7 alkyl, C.sub.2 -C.sub.4 cloro-, hydroxy-, or alkoxy-alkyl C.sub.3 -C.sub.4 alkenyl, cycloalkyl having a C.sub.3 -C.sub.7 ring, cycloalkylalkyl having a C.sub.3 -C.sub.6 ring, phenyl or C.sub.7 -C.sub.8 aralkyl optionally monohalogen substituted in the aryl group or NR.sub.1 R.sub.2 = a cyclic moiety, said moiety being pyrrolidinyl, piperidinyl, hexahydroazepinyl or heptahydroazocinyl, each of which are unsubstituted or substituted with 1 or 2 methyl radicals, 4-alkyl-1-piperazinyl, morpholinyl or 1,2,3,4-tetrahydroisoquinolinyl) are prepared from rifamycin S by(a) dissolving the rifamycin S in tetrahydrofuran, CHCl.sub.3, dioxan, CH.sub.2 Cl.sub.2 or dichloroethane(b) adding (i) a Schiff's base CH.sub.2 =NR.sub.3 wherein R.sub.3 = t-alkyl or (ii) a compound R.sub.4 N(CH.sub.2 OR.sub.5).sub.2 wherein R.sub.
    Type: Grant
    Filed: March 19, 1984
    Date of Patent: March 26, 1985
    Assignee: Farmitalia Carlo Erba S.P.A.
    Inventors: Giovanni Franceschi, Sergio Vioglio
  • Patent number: 4482565
    Abstract: There are disclosed .beta.-lactam-containing compounds of the formula: ##STR1## where R is hydrogen, lower alkyl, trichloroethyl, acetonyl, benzyl, substituted benzyl, phenyl, substituted phenyl, benzidryl or a residue that will undergo metabolic activation "in vivo" and have favorable pharmacokinetic properties; R.sup.1 is a hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, or hydroxyalkyl, with the alcoholic function of the hydroxyalkyl being free or protected; Z is hydrogen, halogen, hydroxy, amino, carbamoyloxy, mercapto, pyridinium, OR.sup.2, OCOR.sup.2, NHCOR.sup.2, or SR.sup.3 wherein each of R.sup.2 and R.sup.3 is any of lower alkyl, aryl, or a heterocyclic ring, each of which may be substituted or unsubstituted, and n is 0 or 1. The compounds have broad spectrum antibacterial activity and .beta.-lactamase inhibiting activity. Processes for the production of the .beta.-lactam-containing compounds and various intermediates in the production of those compounds are also disclosed.
    Type: Grant
    Filed: May 6, 1981
    Date of Patent: November 13, 1984
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Maurizio Foglio, Giovanni Franceschi, Cosimo Scarafile, Federico Arcamone, Aurora Sanfilippo