Patents by Inventor Marco Alpegiani

Marco Alpegiani 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: 6482827
    Abstract: A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R1 and R2 are each hydrogen or an organic residue, R3 is an organic group, Q is a secondary or tertiary acyclic or cyclic amido group, and the pharmaceutically acceptable salts, solvates and hydrates thereof, are inhibitors of matrix metalloproteinases (MMPs) and of the release of tumor necrosis factor-alpha (TNF) from cells. They are therefore useful in the prevention, control and treatment of diseases in which MMPs or TNF are involved, especially tumoral and inflammatory diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: November 19, 2002
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Francesca Abrate, Ettore Perrone, Riccardo Corigli, Daniela Jabes
  • Publication number: 20010011085
    Abstract: The present invention relates to cephem-derivatives and to a process for their preparation, having proper substituents at C-2 position, i.e. heterocyclylthio or acyloxy group. They are potent protease inhibitors, in particular human leucocyte elastase (HLE) inhibitors.
    Type: Application
    Filed: August 14, 1997
    Publication date: August 2, 2001
    Inventors: MARCO ALPEGIANI, PIERLUIGI BISSOLINO, MASSIMILIANO PALLADINO, ETTORE PERRONE
  • Patent number: 6194451
    Abstract: A compound of formula (I), wherein W is —NHOH or —OH, R1 is either free or protected hydroxymethyl or mercaptomethyl or derivatives thereof, R2 is free or protected hydroxy, R3 and R4 is an organic group, R5 is hydrogen or methyl, or R4 and R5, together with the nitrogen atom to which they are attached, constitute an azaheterocyclyl group, and the solvates, hydrates and pharmaceutically acceptable salts thereof, can inhibit matrix metalloproteinases and the release of tumour necrosis factor (TNF). Processes for producing the compound, intermediates involved in the processes, and pharmaceutical compositions containing the compound are also described.
    Type: Grant
    Filed: July 30, 1999
    Date of Patent: February 27, 2001
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Marco Alpegiani, Massimiliano Palladino, Riccardo Corigli, Daniela Jabes, Ettore Perrone, Maria Francesca Abrate, Pierluigi Bissolino, Marina Lombroso
  • Patent number: 5777104
    Abstract: The present invention relates to the use of known cephem derivatives of the formula: ##STR1## wherein n is zero, one or two; R.sup.1 is hydrogen or an organic radical, R.sup.2 represents halo or an organic radical or R.sup.1 and R.sup.2 taken together with the C-2 carbon atom of the cephem nucleus constitute a carbocyclic or heterocyclyl group; R.sup.3 represents R.sup.2 as defined above or an organic radical, R.sup.4 is either R.sup.1 or an organic group, R.sup.5 is either R.sup.1 as defined above or halo or C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or C.sub.1 -C.sub.6 acylamino;R.sup.6 is R.sup.2 as defined above or an organic group,or a pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 8, 1995
    Date of Patent: July 7, 1998
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Enrico Pesenti
  • Patent number: 5587373
    Abstract: The present invention provides cephalosporin sulphones of formula (I) and the pharmaceutically and veterinarily acceptable salts thereof: ##STR1## wherein n is one or two: A and B are both or each independently hydrogen or an organic radical;R.sup.1 represents halogen, A, OA, --S(O).sub.m A wherein m is 0-2, --OC(O)A, --OS(O).sub.2 A, --NHC(O)A or --NH--Z wherein Z is a mono, di- or tripeptide and A is as defined above;R.sup.2 represents a halogen, A, --S(O).sub.m A, --O--A, --C(O)A, --C(O)OA, --CH.sub.2 --OA, --CH.sub.2 S(O).sub.m A, --CH.sub.2 OC(O)A, --CH.sub.2 O--Z, --CH.sub.2 SC(O) A, --CH.sub.2 --N(A)A, --CH.sub.2 N.sup.+ (A)(A')A", --CH.sub.2 NH--C(O)A or --CH.sub.2 NH--Z wherein A and Z are as defined above.The compounds of formula (I) and their salts are elastase inhibitors.
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: December 24, 1996
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone
  • Patent number: 5585372
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically or veterinarily salts thereof; ##STR1## wherein R.sub.1 is hydrogen or halogen or an organic group; R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.14 aralkyl group;R.sub.3 is hydrogen or halogen, or an organic groupR.sub.4 is hydrogen or a group defined as R.sub.2 above or R.sub.4 taken together with R.sub.3 constitutes a C.sub.2 -C.sub.6 alkanediyl or an alkanediyl radical optionally substituted by methyl or phenyland X is either oxygen or sulphur or NR.sub.6, wherein R.sub.6 is either hydrogen or a group as defined for R.sub.2. A process for their preparation by cyclization of appropriate intermediates is also described.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: December 17, 1996
    Assignee: Pharmacia S.p.A.
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Vincenzo Rizzo
  • Patent number: 5580865
    Abstract: The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R.sub.1 is hydrogen, halogen or an optionally substituted C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 carboxamido group;R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl group;R.sub.3 is hydrogen or acetoxymethyl, methoxymethyl, methyl or an optionally substituted heterocyclylthiomethyl group;R.sub.4 is an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.6 alkenyl, aryl(C.sub.1 -C.sub.8)alkyl or heterocyclyl(C.sub.1 -C.sub.8)alkyl group; andR.sub.5 is an optionally substituted C.sub.6 -C.sub.10 aryl or a heterocyclyl group.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.
    Type: Grant
    Filed: April 5, 1993
    Date of Patent: December 3, 1996
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Vincenzo Rizzo
  • Patent number: 5480880
    Abstract: The invention provides compounds of the general formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a negative charge or an ester residue; R is:a) --(CH.sub.2).sub.n --A--CO.sub.2 H, --(CH.sub.2)n--A--SO.sub.3 H or --(CH.sub.2).sub.n --A--PO.sub.3 H.sub.2, wherein n is either zero, one or two and A is a group --CH.dbd.CH-- (either E or Z), --OCH.sub.2 --, --SCH.sub.2 -- or --CHOH--;b) --(CH.sub.2).sub.n --PO.sub.3 H.sub.2, --(CH.sub.2).sub.n SO.sub.2 NHCN, --(CH.sub.2).sub.n NHSO.sub.3 H, --(CH.sub.2).sub.n CONHSO.sub.2 CH.sub.3 or --(CH.sub.2).sub.n CONHSO.sub.2 CF.sub.3, wherein n is as defined above;c) --(CH.sub.2 S).sub.m --W--(CH.sub.2).sub.n Z, wherein W is an arylene group or a heterocyclediyl group, m is 0 or 1, n is as above defined, and Z represents CO.sub.2 H, PO.sub.3 H.sub.2, SO.sub.2 NHCN, NHSO.sub.3 H, CONHSO.sub.2 CH.sub.3 or CONHSO.sub.2 CF.sub.3 ;d) ##STR2## wherein Y is O or NH and X is NH, N--OH or N--O--(CH.sub.2).sub.n+1 COOH wherein n is as defined above; ore) --(CH.sub.2 S).sub.
    Type: Grant
    Filed: April 9, 1993
    Date of Patent: January 2, 1996
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Giuseppina Visentin, Franco Zarini, Daniela Jabes, Ettore Perrone, Costantino della Bruna, Marco Alpegiani
  • 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: 5356888
    Abstract: There are provided compounds I ##STR1## wherein A is a hydrogen atom or an organic group,R.sub.1 is hydrogen or halogen atom or an organic group,R.sub.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or acyloxy group,R.sub.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy, benzyl group or a methylene andR.sub.4 is chloro, fluoro, hydrogen atom or an organic group.The compounds I are elastase inhibitors. A process for their preparation is also provided, as are pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 22, 1991
    Date of Patent: October 18, 1994
    Assignee: Farmitalia Carlo Erba
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Francesco Di Matteo, Piergiuseppe Orezzi, Giuseppe Cassinelli
  • 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: 5254680
    Abstract: There is provided a process for preparing a compound of the formula (I): ##STR1## wherein R.sub.1 is an organic residue, R.sub.2 is a hydrogen or a chlorine atom, a methoxy, ethoxy or an acetoxy group, and n represents 0, 1 or 2.The process comprises reacting a compound of the formula (II): ##STR2## wherein R.sub.2 and n are as defined above, with an inorganic or organic nitrite, in an alcohol R.sub.1 OH, wherein R.sub.1 is as defined above, or in a mixture R.sub.1 OH-organic solvent in the presence of an inorganic or organic acid.The compounds of the formula (I) are known intermediates in the synthesis of human leucocyte elastase inhibitors (HLE).
    Type: Grant
    Filed: April 25, 1991
    Date of Patent: October 19, 1993
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Matteo D'Anello, Ettore Perrone
  • Patent number: 5200403
    Abstract: Compounds of the formula I ##STR1## wherein R' is a free or esterified carboxy group or a carboxylate anion and R.sup.2 is an organic group have beta-lactamase inhibition activity. A process for the preparation of the same and pharmaceutical compositions containing these compounds are provided.
    Type: Grant
    Filed: July 23, 1991
    Date of Patent: April 6, 1993
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Stephen Hanessian, Giuseppe Meinardi, Ettore Perrone
  • Patent number: 5089489
    Abstract: 6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.
    Type: Grant
    Filed: April 5, 1990
    Date of Patent: February 18, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Paolo Carminati, Giuseppe Cassinelli
  • 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: 4954493
    Abstract: 6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl, or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.
    Type: Grant
    Filed: June 14, 1988
    Date of Patent: September 4, 1990
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Paolo Carminati, Giuseppe Cassinelli
  • 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