Patents by Inventor Graziano Castaldi

Graziano Castaldi 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: 6384226
    Abstract: A process for the preparation of 2-phenyl-imidazo[1,2-a]pyridine-3-acetamides comprises the reaction of a 2-phenyl-imidazo[1,2-a]pyridine with an oxalic ester reactive derivative, followed by reduction of the carbonyl group and reaction with an amine.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: May 7, 2002
    Assignee: Dinamite Dipharma S.p.A.
    Inventor: Graziano Castaldi
  • Publication number: 20020019528
    Abstract: A process for the preparation of 2-phenyl-imidazo[1,2-a]pyridine-3 -acetamides comprises the reaction of a 2-phenyl-imidazo[1,2-a]pyridine with an oxalic ester reactive derivative, followed by reduction of the carbonyl group and reaction with an amine.
    Type: Application
    Filed: July 12, 2001
    Publication date: February 14, 2002
    Applicant: DINAMITE DIPHARMA S.p.A.
    Inventor: Graziano Castaldi
  • Patent number: 5840964
    Abstract: A process for the preparation of 2-(2-fluoro-4-biphenyl)propianic acid enantiomers comprising a II order resolution of ketals of formula ##STR1## wherein R.sub.1 ad R.sub.2 have the meanings reported in the description; the asterisk shows the chiral carbon atom and the asymmetric carbon atoms marked by .alpha. and .beta. have both R or S configuration is described.
    Type: Grant
    Filed: December 22, 1995
    Date of Patent: November 24, 1998
    Assignee: Zambon Group S.P.A.
    Inventors: Claudio Pozzoli, Graziano Castaldi
  • Patent number: 5760220
    Abstract: A process is described for preparing a compound of the formula I: ##STR1## or a salt thereof; wherein X is a protecting group and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1-6 alkyl or C.sub.1-6 perfluoroalkyl, R.sub.5 is hydrogen or when n is 1 R.sub.5 taken together with R.sub.3 comprises a double bond; m is 1, 2 or 3; n is 0 or 1, and p is 0, 1 or 2.
    Type: Grant
    Filed: June 4, 1996
    Date of Patent: June 2, 1998
    Assignee: American Home Products Corporation
    Inventors: Pierre Giguere, Silvio Iera, Michel Bernatchez, Giuseppe Barreca, Graziano Castaldi, Vincenzo Cannata
  • Patent number: 5663432
    Abstract: A process for the preparation of 5-amino-2,4,6-triiodoisophthalic acid dichloride by chlorination of 5-amino-2,4,6-triiodoisophthalic acid with thionyl chloride in the presence of a suitable solvent characterized in that the reaction is carried out in the presence of catalytic amounts of a tetraalkylammonium salt of formulaR.sub.1 R.sub.2 R.sub.3 R.sub.4 NX (I)wherein X is halogen, mesylate or tosylate; R.sub.1, R.sub.2, R.sub.3 and R.sub.4, the same or different, are C.sub.1 -C.sub.20 alkyl groups so that the total number of carbon atoms of the groups R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is higher than 16.The 5-amino-2,4,6-triiodoisophthalic acid dichloride obtained according to the process of the present invention is useful as intermediate in the synthesis of iodinated contrast media.
    Type: Grant
    Filed: May 17, 1996
    Date of Patent: September 2, 1997
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Claudio Pozzoli, Laura Russo, Graziano Castaldi
  • Patent number: 5274186
    Abstract: Compounds of formula ##STR1## (wherein Ar, R, R.sub.1 and X have the meaning reported in the description) are useful intermediates for the preparation of a variety of organic compounds, also optically active, like alpha-haloketones, alpha-hydroxyketones or ketals, alpha-arylalkanoic acids.
    Type: Grant
    Filed: January 19, 1989
    Date of Patent: December 28, 1993
    Assignee: Zambon S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi
  • Patent number: 5191094
    Abstract: A process is described for the preparation of mono (2-ammonium-2-hydroxymethyl-1,3-propanediol) (2R,cis)-1,2-epoxypropyl-phosphonate with improved characteristics of stability, of processing for the preparation of pharmaceutical forms and of stability of the pharmaceutical forms that contain it.
    Type: Grant
    Filed: June 11, 1992
    Date of Patent: March 2, 1993
    Assignee: Zambon Group S.p.A.
    Inventors: Dario Tentorio, Graziano Castaldi, Claudio Girodano, Franco Pozzi
  • Patent number: 5186867
    Abstract: New compounds of the spiro-indoline-oxazine class possessing photochromatic and photosensitizing charecteristics are definable by the general formula (I): ##STR1## where the substituents R, R.sup.1 -R.sup.7 and A are as defined in the description. The process for preparing the compounds (I) is described, as is their use as photochromic agents able to confer photochromatic characteristics on the articles in which they are incorporated, and as photosensitizing agents.
    Type: Grant
    Filed: February 27, 1992
    Date of Patent: February 16, 1993
    Assignee: Enichem Synthesis, S.p.A.
    Inventors: Graziano Castaldi, Pietro Allegrini, Luciana Crisci, Fiorenzo Renzi
  • Patent number: 5171636
    Abstract: New photochromatic and thermochromatic compounds of the spirooxazepin-oxazine class are definable by the general formula (I): ##STR1## where the substituents R and R.sub.1 -R.sub.12 are as defined in the description.The process for the preparation of the compounds (I) is described, as is their use as photochromatic and thermochromatic agents.
    Type: Grant
    Filed: January 27, 1992
    Date of Patent: December 15, 1992
    Assignee: Enichem Synthesis S.p.A.
    Inventors: Graziano Castaldi, Pietro Allegrini
  • Patent number: 5162309
    Abstract: A process is described for the preparation of mono (2-ammonium-2-hydroxymethyl-1,3-propanediol) (2R,cis)-1,2-epoxypropyl-phosphonate with improved characteristics of stability, of processing for the preparation of pharmaceutical forms and of stability of the pharmaceutical forms that contain it.
    Type: Grant
    Filed: July 25, 1990
    Date of Patent: November 10, 1992
    Assignee: Zambon Group
    Inventors: Dario Tentorio, Graziano Castaldi, Claudio Giordano, Franco Pozzi
  • Patent number: 5110922
    Abstract: New photochromatic and thermochromatic compounds of the spiro-oxazepin-oxazine class are definable by the general formula (I): ##STR1## where the substituents R and R.sub.1 -R.sub.12 are defined in the description.The process for the preparation of the compounds (I) is described, as is their use as photochromatic and thermochromatic agents.
    Type: Grant
    Filed: July 31, 1991
    Date of Patent: May 5, 1992
    Assignee: Enichem Synthesis S.p.A.
    Inventors: Graziano Castaldi, Pietro Allegrini
  • Patent number: 5084569
    Abstract: A stereoconvergent process is described for preparing optically active alpha-arylalkanoic acids using as starting substance a diastereoisomeric mixture of ketals of formula ##STR1## in which the substitutents have the meanings given in the description. The described process leads to the formation of a single enantiomer.
    Type: Grant
    Filed: March 15, 1990
    Date of Patent: January 28, 1992
    Assignee: Zambon SpA
    Inventors: Marco Villa, Claudio Giordano, Graziano Castaldi, Silvia Cavicchioli
  • Patent number: 5055576
    Abstract: New photochromatic and thermochromatic compounds of the spiro-oxazepin-oxazine class are definable by the general formula (I): ##STR1## where the substituents R and R.sub.1 -R.sub.12 are as defined in the description.The process for the preparation of the compounds (I) is described, as is their use as photochromatic and thermochromatic agents.
    Type: Grant
    Filed: December 6, 1990
    Date of Patent: October 8, 1991
    Assignee: Enichem Synthesis, S.p.A.
    Inventors: Graziano Castaldi, Pietro Allegrini
  • Patent number: 5023365
    Abstract: A process is described for preparing an intermediate in the synthesis of naproxen.The intermediate, namely the methyl ester of S(+)-2-(5-bromo-6-methoxy-2-naphthyl)-propionic acid or of its 5-chloro analogue, is prepared by preferential crystallization from mixtures with its enantiomer.
    Type: Grant
    Filed: December 20, 1989
    Date of Patent: June 11, 1991
    Assignee: Zambon Group S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi, Maurizio Paiocchi
  • Patent number: 5004832
    Abstract: Compounds are described of formula ##STR1## in which: Ar represents an aryl, possibly substituted;R represents a C.sub.1 -C.sub.4 alkyl;R' represents a hydroxyl, an alkoxy, an amino group possibly mono or di-alkyl substituted, or an O.sup.-- M.sup.+ group where M.sup.+ represents the cation of an alkaline metal;X represents a hydrogen, chlorine, bromine or iodine atom, a hydroxyl, or an acyloxy, alkylsulphonyloxy or arylsulphonyloxy group.The compounds of formula I can be easily transformed into alpha-arylalkanoic acids of formula ##STR2## in which Ar and R have the aforesaid meanings.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: April 2, 1991
    Assignee: Zambon S.p.A.
    Inventors: Graziano Castaldi, Claudio Giordano
  • Patent number: 4973696
    Abstract: A stereoselective process is described for preparing optically active alpha,beta-disubstituted carbonyl compounds, comprising forming an acetal between an alpha,beta-unsaturated aldehyde or ketone and tartaric acid or a derivative thereof, halogenating the product thus obtained, and restoring the carbonyl compound.
    Type: Grant
    Filed: January 17, 1989
    Date of Patent: November 27, 1990
    Assignee: Zambon S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi, Silvia Cavicchioli, Francesco Minisci
  • Patent number: 4937367
    Abstract: A process is described for the preparation of intermediates useful in the synthesis of Fosfomycin.More particularly, an enantioselective process is described for the preparation of derivatives of (1S,2S)-1,2-dihydroxypropyl-phosphonic acid of formula ##STR1## wherein R.sub.2 and R.sub.3 have the meanings reported in the specification.
    Type: Grant
    Filed: July 12, 1988
    Date of Patent: June 26, 1990
    Assignee: Zambon Group S.p.A.
    Inventors: Graziano Castaldi, Claudio Giordano
  • Patent number: 4922009
    Abstract: A stereoconvergent process is described for preparing optically active alpha-arylalkanoic acids using as starting substance a diastereoisomeric mixture of ketals of formula ##STR1## in which the substituents have the meanings given in the description. The described process leads to the formation of a single enantiomer.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: May 1, 1990
    Assignee: Zambon SpA
    Inventors: Marco Villa, Claudio Giordano, Graziano Castaldi, Silvia Cavicchioli
  • Patent number: 4888433
    Abstract: A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represent a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration.This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.
    Type: Grant
    Filed: August 5, 1987
    Date of Patent: December 19, 1989
    Assignee: Zambon, S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
  • Patent number: 4861903
    Abstract: A process is described for preparing optically active alpha-arylalkanoic acids consisting of rearranging an optically active ketal of formula ##STR1## in which the substituents have the meaning given in the description of the invention.
    Type: Grant
    Filed: July 31, 1986
    Date of Patent: August 29, 1989
    Assignee: Zambon spa
    Inventors: Claudio Giordano, Graziano Castaldi