Patents Assigned to Rotta Research Laboratorium S.p.A.
-
Patent number: 7560591Abstract: 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 pType: GrantFiled: April 30, 2008Date of Patent: July 14, 2009Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
-
Publication number: 20080207764Abstract: 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 pType: ApplicationFiled: April 30, 2008Publication date: August 28, 2008Applicant: ROTTA RESEARCH LABORATORIUM S.p.A.Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
-
Patent number: 7202277Abstract: 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 pType: GrantFiled: February 6, 2002Date of Patent: April 10, 2007Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
-
Patent number: 7025998Abstract: A composition for the relief and/or prevention of climacteric and menopausal disorders affecting women in pre-, peri- or post-menopause, comprising Soy Isoflavones and viable lactic acid bacteria preferably Lactobacillus sporogenes aimed to enhance the absorption of Soy Isoflavones, the composition being provided in dosage forms for oral administration. Preferably the composition also comprises Equisetum arvense dry extract and a pharmaceutically acceptable calcium salt and/or Vitamin D3.Type: GrantFiled: May 30, 2003Date of Patent: April 11, 2006Assignee: Rotta Research Laboratorium S.p.A.Inventors: Paolo Senin, Ivo Setnikar, Angelo Luigi Rovati
-
Patent number: 6605722Abstract: 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, propType: GrantFiled: August 8, 2002Date of Patent: August 12, 2003Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Walter Peris, Lucio Claudio Rovati
-
Patent number: 6413978Abstract: 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: GrantFiled: October 2, 2001Date of Patent: July 2, 2002Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Andrea Cappelli, Maurizio Anzini, Salvatore Vomero, Lucio Claudio Rovati
-
Publication number: 20020042426Abstract: 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: 1Type: ApplicationFiled: October 2, 2001Publication date: April 11, 2002Applicant: ROTTA RESEARCH LABORATORIUM S.p.A.Inventors: Francesco Makovec, Andrea Cappelli, Maurizio Anzini, Salvatore Vomero, Lucio Claudio Rovati
-
Patent number: 6323216Abstract: 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: GrantFiled: October 13, 1999Date of Patent: November 27, 2001Assignee: Rotta Research Laboratorium S.p.AInventors: Francesco Makovec, Andrea Cappelli, Maurizio Anzini, Salvatore Vomero, Lucio Claudio Rovati
-
Patent number: 6156335Abstract: 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: GrantFiled: July 15, 1994Date of Patent: December 5, 2000Assignee: Rotta Research Laboratorium S.p.A.Inventors: Luigi Rovati, Lucio Rovati, Francesco Makovec, Gunter Cordes, Wilfried Fischer
-
Patent number: 6075033Abstract: 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: GrantFiled: December 31, 1998Date of Patent: June 13, 2000Assignee: Rotta Research Laboratorium S.p.AInventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
-
Patent number: 5985885Abstract: 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: GrantFiled: October 9, 1998Date of Patent: November 16, 1999Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Walter Peris, Lucio Claudio Rovati, Luigi Angelo Rovati
-
Patent number: 5962502Abstract: 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: GrantFiled: April 8, 1996Date of Patent: October 5, 1999Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
-
Patent number: 5922875Abstract: 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: GrantFiled: December 29, 1997Date of Patent: July 13, 1999Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
-
Patent number: 5744607Abstract: 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: GrantFiled: October 18, 1996Date of Patent: April 28, 1998Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati
-
Patent number: 5723494Abstract: 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: GrantFiled: September 11, 1995Date of Patent: March 3, 1998Assignee: Rotta Research Laboratorium S.P.A.Inventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
-
Patent number: 5711962Abstract: Transdermal therapeutic systems containing as active ingredients oestradiol and norethisterone acetate have added thereto octyldodecanol to reduce or avert crystal formation after storage. The use of octyldodecanol thus makes it possible to produce a storage-stable system with the active ingredients oestradiol and norethisterone acetate with a high thermodynamic activity.Type: GrantFiled: March 27, 1996Date of Patent: January 27, 1998Assignee: Rotta Research Laboratorium S.p.A.Inventors: Gunter Cordes, Lucio C. Rovati
-
Patent number: 5602179Abstract: There are described optically active derivatives of (R) 5-pentylamino-5-oxopentanoic acid and their pharmaceutically acceptable salts, having antagonistic activity towards cholecystokinin, and with the formula: ##STR1## in which R.sub.1 is selected from the groups 2-naphthyl, 3,4-dichlorophenyl and 3,4-dimethylphenyl and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 carbon atoms, and in which the substituents on the central chiral group (marked with an asterisk in Formula (I)), have the R (rectus) conformation.Type: GrantFiled: December 1, 1994Date of Patent: February 11, 1997Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Rolando Chiste, Walter Peris, Luigi Rovati
-
Patent number: 5587479Abstract: Compounds of general formula (I), in which r is 1 or 2, R.sub.1 is selected independently from: unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, the 2(beta)-naphthyl group, and heterocyclic, monocyclic or dicyclic groups; R.sub.2 is selected independently 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 comprising from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group.Type: GrantFiled: October 11, 1994Date of Patent: December 24, 1996Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati
-
Patent number: 5500430Abstract: Amidic derivatives of glutamic, aspartic and 2-amino adipic acids represented by the following formula (I): ##STR1## wherein r is from 1 to 3, R.sub.1 is an aryl group or a substituted aryl group, R.sub.2 is a 8-azaspiro(4.5)decan-8-yl group or a 3-azaspiro(5.5)decan-3-yl group, wherein said compound has a chiral center marked with an asterisk in said formula (I), thus forming a racemic (R,S) form or an isomeric form. The amidic derivatives are useful in treating ulcers, hypergastrinaemia-activated tumors, pathological conditions of CNS, biliary dyskinesia, colitis, pancreatistis, and surgically induced myosis.Type: GrantFiled: June 10, 1993Date of Patent: March 19, 1996Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Luigi A. Rovati, Lucio C. Rovati
-
Patent number: 5391574Abstract: There are described optically active derivatives of (R) 5-pentylamino-5-oxopentanoic acid and their pharmaceutically acceptable salts, having antagonistic activity towards cholecystokinin, and with the formula: ##STR1## in which R.sub.1 is selected from the groups 2-naphthyl, 3,4-dichlorophenyl and 3,4-dimethylphenyl and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 carbon atoms, and in which the substituents on the central chiral group (marked with an asterisk in Formula (I)), have the R (rectus) conformation.Type: GrantFiled: October 4, 1993Date of Patent: February 21, 1995Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Rolando Chiste, Walter Peris, Luigi Rovati