Patents by Inventor Francesco Makovec

Francesco Makovec 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).

  • Publication number: 20070135523
    Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or met
    Type: Application
    Filed: January 12, 2007
    Publication date: June 14, 2007
    Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Rovati
  • Patent number: 7202277
    Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p
    Type: Grant
    Filed: February 6, 2002
    Date of Patent: April 10, 2007
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
  • Patent number: 7145037
    Abstract: The invention describes compounds represented by the general formula (I) given below: in which: n is an integer between 1 and 4; R1 and R2 are chosen independently from hydrogen and a methyl group; R3 is chosen independently from a linear, branched or cyclic alkyl group containing from 1 to 3 carbon atoms (R3a) and a simple amino group (R3b) or an amino group substituted with a nitro group (R3c) The compounds are useful for treating central nervous system diseases or peripheral neuropathies.
    Type: Grant
    Filed: September 1, 2004
    Date of Patent: December 5, 2006
    Assignee: Rotta Research Laboraturium S.p.A.
    Inventors: Francesco Makovec, Roberto Artusi, Simona Zanzola, Lucio Claudio Rovati
  • Publication number: 20060154987
    Abstract: The present invention describes a novel method for the purification of dexloxiglumide by crystallization from isopropyl ether which permits the production, in a reproducible manner, of a product with morphological and particle-size characteristics such as to favour its use in the preparation of oral pharmaceutical forms on an industrial scale.
    Type: Application
    Filed: June 21, 2004
    Publication date: July 13, 2006
    Inventors: Francesco Makovec, Lucio Rovati
  • Publication number: 20060111304
    Abstract: Anthranylic compounds having anti-CCK activity of general formula (I) in which, n is a whole number lying between 0 and 7; R1 is chosen independently from the groups (II), in which X1 is chosen independently from, S, O, NR2 and X2 is a group chosen from: H, C1-C4 alkyl, F, Cl, CF3, OCH3, OC2H5, CN; R2 is chosen from H or CH3; R3 is chosen from H, CH3, F, Cl, CF3, OCH3; R4 is chosen from the groups: H, —S—(CH2)m-R5, —SO2—(CH2)m-R5 (n different from 0), a branched alkyl group, a cyclo alkyl, a cyclo alkenyl, the group 1 or 2 adamantile, a phenyl group optionally substituted; R5 is chosen from the groups: H, linear or branched alkyl, cyclo alkyl, the group 1 or 2 adamantile, a suitably substituted phenyl group.
    Type: Application
    Filed: July 23, 2003
    Publication date: May 25, 2006
    Applicant: ROTTAPHARM S.P.A.
    Inventors: Francesco Makovec, Antonio Varnavas, Lucia Lassiani, Lucio Rovati
  • Publication number: 20050197331
    Abstract: Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.
    Type: Application
    Filed: March 1, 2005
    Publication date: September 8, 2005
    Inventors: Francesco Makovec, Antonio Giordani, Roberto Artusi, Stefano Mandelli, Ilario Verpilio, Simona Zanzola, Lucio Rovati
  • Publication number: 20050049312
    Abstract: The invention describes compounds represented by the general formula (I) given below: in which: n is an integer between 1 and 4; R1 and R2 are chosen independently from hydrogen and a methyl group; R3 is chosen independently from a linear, branched or cyclic alkyl group containing from 1 to 3 carbon atoms (R3a) and a simple amino group (R3b) or an amino group substituted with a nitro group (R3c) The compounds are useful for treating central nervous system diseases or peripheral neuropathies.
    Type: Application
    Filed: September 1, 2004
    Publication date: March 3, 2005
    Inventors: Francesco Makovec, Roberto Artusi, Simona Zanzola, Lucio Rovati
  • Patent number: 6605722
    Abstract: Compounds which can be represented by general formula (I) indicated below and in which: R1 and R2 are selected, independently, from hydrogen, an alkyl group having from 1 to 4 carbon atoms, a halogen group such as a fluoro, chloro or bromo group, the methoxy group, the cyano group, or the trifluoromethyl group, and R3 is selected, independently, from a phenyl or a 2 (or 3 or 4)-pyridyl group, unsubstituted or mono- or di-substituted with an alkyl or alkoxy group having from 1 to 4 carbon atoms, with a halogen group such as a fluoro or chloro group, with the trifluoromethyl group, with the cyano group, with the nitro group, with the amino group, or with the phenyl group, a 1 (or 2)-naphthyl group, a 2 (or 3)-indolyl group as such or N-alkylated with an alkyl group having from 1 to 3 carbon atoms, a 2 (or 3, 4, 5, 6, 7 or 8)-quinolinyl or a 1 (or 3, 4, 5, 6, 7 or 8)-isoquinolinyl group, unsubstituted or mono- or di-substituted with a group selected, independently, from the methyl, ethyl, prop
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: August 12, 2003
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Walter Peris, Lucio Claudio Rovati
  • Publication number: 20030087910
    Abstract: Compounds which can be represented by general formula (I) indicated below and in which:
    Type: Application
    Filed: August 8, 2002
    Publication date: May 8, 2003
    Inventors: Francesco Makovec, Walter Peris, Lucio Claudio Rovati
  • Patent number: 6413978
    Abstract: Novel basic derivatives of benz[e]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones which can be represented by the general formula (I) indicated below are described: in which X is CH or N, R is H, Cl or OR1 in which R1 is H or an alkyl group having from 1 to 3 carbon atoms, Het is the 3-endotropyl group (that is, the 8-methyl-8-azadicyclo[3.2.l]oct-3-yl group) or the 3-quinuclidyl group (that is, the 1-azadicyclo[2.2.2]oct-3-yl group); these compounds have been found to be potent and selective antagonists of the 5-HT3 serotonin-like receptor and can therefore be used, for example, as anti-emetics as well as in various pathological conditions of the central nervous system, and as antitussives.
    Type: Grant
    Filed: October 2, 2001
    Date of Patent: July 2, 2002
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Andrea Cappelli, Maurizio Anzini, Salvatore Vomero, Lucio Claudio Rovati
  • Publication number: 20020042426
    Abstract: Novel basic derivatives of benz[e]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones which can be represented by the general formula (I) indicated below are described: 1
    Type: Application
    Filed: October 2, 2001
    Publication date: April 11, 2002
    Applicant: ROTTA RESEARCH LABORATORIUM S.p.A.
    Inventors: Francesco Makovec, Andrea Cappelli, Maurizio Anzini, Salvatore Vomero, Lucio Claudio Rovati
  • Patent number: 6323216
    Abstract: Novel basic derivatives of benz[e]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones which can be represented by the general formula (I) indicated below are described: in which X is CH or N, R is H, Cl or OR1 in which R1 is H or an alkyl group having from 1 to 3 carbon atoms, Het is the 3-endotropyl group (that is, the 8-methyl-8-azadicyclo[3.2.1]oct-3-yl group) or the 3-quinuclidyl group (that is, the 1-azadicyclo[2.2.2]oct-3-yl group); these compounds have been found to be potent and selective antagonists of the 5-HT3 serotonin-like receptor and can therefore be used, for example, as anti-emetics as well as in various pathological conditions of the central nervous system, and as antitussives.
    Type: Grant
    Filed: October 13, 1999
    Date of Patent: November 27, 2001
    Assignee: Rotta Research Laboratorium S.p.A
    Inventors: Francesco Makovec, Andrea Cappelli, Maurizio Anzini, Salvatore Vomero, Lucio Claudio Rovati
  • Patent number: 6156335
    Abstract: The invention is represented by a transdermal medicated patch for the extended release of 17.beta.-estradiol to the skin. The transdermal patch is formed by an outer covering, a matrix containing from 1% to 5% (w/w) 17.beta.-estradiol, and a protective liner which is removed before use. The matrix is formed of pressure-sensitive adhesive acrylic copolymers, in which the active ingredient is dissolved or dispersed. The acrylic copolymers are obtained by radical copolymerization of 2-ethylhexyl acrylate, methyl acrylate, acrylic acid, vinyl acetate, hydroxyethyl acrylate or a mixture thereof. Optionally quantities of less than 0.5% (w/w) of other substances may be added.
    Type: Grant
    Filed: July 15, 1994
    Date of Patent: December 5, 2000
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Luigi Rovati, Lucio Rovati, Francesco Makovec, Gunter Cordes, Wilfried Fischer
  • Patent number: 6075033
    Abstract: Compounds which can be represented by general formula (I) indicated below, ##STR1## and in which the anthranilic acid aromatic ring may be mono- or di-substituted by the R.sub.1 group which can be selected independently from hydrogen, methyl and chloro, and in which the substituents at the chiral center (marked with an asterik in formula (I)) have the R (Rectus) configuration.
    Type: Grant
    Filed: December 31, 1998
    Date of Patent: June 13, 2000
    Assignee: Rotta Research Laboratorium S.p.A
    Inventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
  • Patent number: 5985885
    Abstract: New quinazolines are described of general formula (I), in which Ar is an unsubstituted phenyl group or a phenyl group mono-substituted with a methoxy, ethoxy or methyl group; an unsubstituted pyridyl group (2-, 3- or 4-yl) or a pyridyl group mono-substituted with a methoxy or methyl group; an unsubstituted furyl group (2- or 3-yl) or a furyl group substituted with a methoxy or methyl group; a benzofuryl group (2- or 3-yl); an indolyl group (2- or 3-yl); a thiophenyl group (2- or 3-yl); a naphthyl group (1- or 2-yl) and their salts obtained from pharmaceutically acceptable inorganic or organic acids. These new quinazolines are useful in the treatment of hypertension, congestive heart failure, prostate hypertrophy, various urinary tract disorders and pathological symptoms caused by hyperactivity or disfunctioning of the noradrenergic neural system.
    Type: Grant
    Filed: October 9, 1998
    Date of Patent: November 16, 1999
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Walter Peris, Lucio Claudio Rovati, Luigi Angelo Rovati
  • Patent number: 5976576
    Abstract: A pharmaceutical composition comprising, as active ingredient, N-4-(1H-tetrazol-5-yl)phenyl-4-(1H-tetrazol-5-yl)benzamide disodium salt (CR 2039, Andolast) or another pharmaceutically-acceptable salt thereof and a flavoring, and optionally including a pharmaceutically-acceptable inert carrier and/or a pharmaceutically-acceptable sweetener, the composition being suitable for administration by oral inhalation.
    Type: Grant
    Filed: August 6, 1998
    Date of Patent: November 2, 1999
    Assignee: Rotta Research Laboratories S.p.A.
    Inventors: Francesco Makovec, Paolo Senin, Lucio Claudio Rovati
  • Patent number: 5962502
    Abstract: Derivatives of glutamic and aspartic of formula (I) are described ##STR1## where the compounds are potent receptor antagonists of gastrin at the peripheral level and of cholecystokinin at the level of the central nervous system.
    Type: Grant
    Filed: April 8, 1996
    Date of Patent: October 5, 1999
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
  • Patent number: 5922875
    Abstract: A compound represented by the general formula (I) shown below ##STR1## or a pharmaceutically acceptable salt thereof can be used as the active ingredient in a pharmaceutical preparation. The pharmaceutical preparation is desirable for its anti-ulcer activity, for therapeutic use against tumors sustained by gastrin and other bioactive polypeptides correlated therewith, for therapeutic use in treating disorders of the gastrointestinal tract, for the treatment of pathological conditions of the central nervous system linked to imbalances in the neural physiological levels of gastrin or other bioactive polypeptides correlated therewith, for use in the treatment and prevention of pathological eye conditions caused by surgical treatment of cataracts or chronic ocular inflammation, and for the prevention of diseases of other sensory organs.
    Type: Grant
    Filed: December 29, 1997
    Date of Patent: July 13, 1999
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
  • Patent number: 5744607
    Abstract: The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R.sub.1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, a 2(beta)naphthyl group, and heterocyclic, monocyclic and dicyclic groups; R.sub.2 is selected from heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group having from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group; and r is 1 or 2. The compounds have a potent antagonistic effect on gastrin and cholecystokinin and can be used to treat diseases which are linked to imbalances in the physiological levels of gastrin, cholecystokinin or other biologically active polypeptides related thereto.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: April 28, 1998
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati
  • Patent number: 5723494
    Abstract: Compounds represented by general formula (I) and (II), in which r is 1 or 2, R.sub.2 and R.sub.3 are selected independently from H, CH.sub.3, C.sub.2 H.sub.5 and CHO, provided that R.sub.2 and R.sub.3 are not simultaneously CHO, and in which R.sub.1 is selected from: an aminoalkyl adamantyl group, a monocyclic aminoalkyl group, a dicyclic aminospiro group, a dicyclic amino group (orthofused), a dicyclic amino group, and azacycloalkyl group, an azadicyclic group (orthofused), a dicyclic azaspiro group, and azadicyclic group, and azacycloalkyl group, and a linear or branched aminoalkyl group.
    Type: Grant
    Filed: September 11, 1995
    Date of Patent: March 3, 1998
    Assignee: Rotta Research Laboratorium S.P.A.
    Inventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati