Abstract: A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of allylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
Type:
Application
Filed:
December 18, 2014
Publication date:
April 16, 2015
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
Inventors:
Marcello MARCHETTI, Tommaso Iacoangeli, Giovanni Battista Ciottoli, Giuseppe Biondi
Abstract: The present invention relates to the 1H-indazole-3-carboxamide compounds having the following general formula (I) as glycogen synthase kinase 3 beta (GSK-3?) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; (viii) epilepsies; and (ix) neuropathic pain.
Type:
Application
Filed:
February 7, 2013
Publication date:
February 26, 2015
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.
Abstract: 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors. The present invention relates to the 1H-indazole-3-carboxamide compounds for use as glycogen synthase kinase 3 beta (GSK-33) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies.
Type:
Application
Filed:
February 8, 2013
Publication date:
December 25, 2014
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.
Inventors:
Maria Alessandra Alisi, Nicola Cazzolla, Barbara Garofalo, Guido Furlotti, Gabriele Magaro', Rosella Ombrato, Francesca Mancini
Abstract: The present invention relates to glycogen-based cationic polymers, to complexes of the said cationic polymers with anionic compounds, to pharmaceutical compositions comprising the said complexes, and to the use of the said complexes for delivering or transfecting the said anionic compounds to a specific pharmacological target, such as, for instance an organ, a tissue or a cell.
Type:
Application
Filed:
February 21, 2013
Publication date:
December 25, 2014
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.
Abstract: The present invention relates to a food formulation for the controlled release of glucose comprising glycogen and at least one other edible component, as well the use of glycogen for its preparation.
Type:
Grant
Filed:
July 29, 2010
Date of Patent:
November 18, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.
Type:
Grant
Filed:
February 15, 2013
Date of Patent:
October 28, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Maria Alessandra Alisi, Guido Furlotti, Nicola Cazzolla, Caterina Maugeri, Patrizia Dragone, Barbara Garofalo, Isabella Coletta, Giorgina Mangano, Beatrice Garrone
Abstract: A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.
Type:
Application
Filed:
June 16, 2014
Publication date:
October 2, 2014
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
Inventors:
Marcello MARCHETTI, Tommaso Iacoangeli, Giovanni Battista Ciotolli, Giuseppe Biondi
Abstract: A method of treating insulin resistance, obesity and metabolic syndrome by administering an indazolemethoxyalkanoic acid as described herein.
Type:
Grant
Filed:
May 8, 2012
Date of Patent:
September 30, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.
Type:
Grant
Filed:
December 23, 2008
Date of Patent:
September 23, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.
Type:
Grant
Filed:
March 5, 2009
Date of Patent:
September 16, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: It is disclosed a packaging material for a pharmaceutical product. The packaging material comprises a colored element which at about 38° C. discolors partially, revealing a marking. The element is formed by a first portion forming the marking printed with conventional ink, and a second portion printed with thermochromic ink. The thermochromic ink is colored below about 38° C. and becomes colorless when this temperature is reached or exceeded. The two portions are arranged so that the first portion is invisible below about 38° C., but becomes visible when this temperature is reached or exceeded.
Type:
Grant
Filed:
November 13, 2009
Date of Patent:
June 17, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: It is disclosed a packaging material (1) for a pharmaceutical product. The packaging material comprises a colored element (2) which at a predetermined temperature, below which the pharmaceutical product must be kept, discolors partially, revealing a marking. The element is formed by a first portion forming the marking (2?) printed with conventional ink, and a second portion (2?) printed with thermochromic ink. The thermochromic ink is colored below the predetermined temperature and becomes colorless when this predetermined temperature is reached or exceeded. The two portions are arranged so that the first portion is invisible below the predetermined temperature, but becomes visible when this temperature is reached or exceeded.
Type:
Grant
Filed:
November 13, 2009
Date of Patent:
May 13, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: Compound of formula (I) in which R1, R2 and R3 are defined in the following description, and the pharmaceutically acceptable acid-addition or base-addition salts thereof. The invention also relates to a process and an intermediate for preparing it, and to a pharmaceutical composition comprising it. The invention also relates to the use of a novel 2H-pyrrolo[3,4-c]quinoline compound for preparing a pharmaceutical composition that is active in the treatment of disturbances of the serotoninergic system.
Type:
Grant
Filed:
July 17, 2009
Date of Patent:
April 1, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Maria Alessandra Alisi, Nicola Cazzolla, Roberta Costi, Roberto Di Santo, Guido Furlotti, Angelo Guglielmotti, Lorenzo Polenzani
Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.
Type:
Grant
Filed:
May 3, 2006
Date of Patent:
April 1, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Lorenzo Polenzani, Giorgina Mangano, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri
Abstract: The present invention relates to novel benzoyl derivatives of 3-aminocarbazole, to a pharmaceutical composition containing them, to a method for preparing them and to the use of such compounds for the production of a drug that is useful in the treatment or prevention of disturbances associated with the production of prostaglandin E2 (PGE2), for instance inflammatory processes, pain, fever, tumours, Alzheimer's disease and atherosclerosis.
Type:
Grant
Filed:
May 11, 2009
Date of Patent:
January 28, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Maria Alessandra Alisi, Nicola Cazzolla, Isabella Coletta, Patrizia Dragone, Guido Furlotti, Barbara Garofalo, Angelo Guglielmotti, Giorgina Mangano, Caterina Maugeri
Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
October 29, 2013
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: The present invention relates to a method of preparation of metaxalone comprising reaction of triglycidyl isocyanurate (TGIC) with m-xylenol, characterized in that said reaction is carried out in a solvent mixture comprising an aprotic polar solvent with dielectric constant greater than or equal to 30 and at least one other solvent selected from the group comprising apolar solvents and aprotic polar solvents with dielectric constant below 30 said solvent mixture comprising from 5 to 40 wt. % of said first solvent and from 95 to 60 wt. % of said second solvent, adding the TGIC at a temperature between 30° C. and 50° C., and after adding the TGIC, raising the temperature of the reaction solution to a value between 80° C. and 180° C. in a time between 120 and 180 minutes at a rate of increase not greater that 1.25° C. per minute. The invention also relates to a metaxalone with a reduced content of impurities derived from incomplete reactions and/or side reactions of the method of production.
Type:
Application
Filed:
January 17, 2012
Publication date:
October 3, 2013
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
Inventors:
Tommaso Iacoangeli, Mario Chiavarini, Antonello Fazio, Marcello Marchetti, Giovanni Battista Ciottoli
Abstract: 2-Alkyl-indazole compound and its pharmaceutically acceptable salts of acid addition, method and intermediates for preparing them, a pharmaceutical composition containing them and use of the latter. The 2-alkyl-indazole compound has the following general formula (I) in which R1, R2, R3, R4, R6, R7, X, Y, W, n, p, and m have the meanings stated in the description.
Type:
Grant
Filed:
November 19, 2007
Date of Patent:
August 13, 2013
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri, Rosella Ombrato, Lorenzo Polenzani
Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.
Type:
Grant
Filed:
March 5, 2009
Date of Patent:
June 11, 2013
Assignee:
Aziende Chimiche Riunite Angelini Francesco A. C. R. A. F. S. p. A.
Abstract: The present invention relates to a compound of formula (I): in which: R is a linear or branched alkyl group containing between 1 and 3 carbon atoms, Y is CH or N, and p is an integer between 0 and 3 and preferably 0 and 1, and salts thereof, either acid-addition salts with a pharmaceutically acceptable organic or mineral acid, or base-addition salts with a pharmaceutically acceptable organic or mineral base. The invention also relates to a process for preparing the compound of formula (I), and to a pharmaceutical composition comprising it. The invention also relates to the use of an indazole for preparing a pharmaceutical composition that is active in the treatment of neuropathic pain.
Type:
Grant
Filed:
November 6, 2008
Date of Patent:
June 4, 2013
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Angelo Guglielmotti, Lorenzo Polenzani