Abstract: Tricyclic indazole compound and its pharmaceutically acceptable salts of acid addition, use thereof, method and intermediates for preparing them, and a pharmaceutical composition containing them. The tricyclic indazole compound has the following general Formula (I): in which R1, R2, L1, L2, X1, X2, X3, X4, X5, Y, W, m, and n have the meanings stated in the description.
Type:
Application
Filed:
March 4, 2011
Publication date:
January 24, 2013
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.
Abstract: The present invention relates to the process for the preparation of 1-benzyl-3-hydroxymethyl-1H-indazole according ing to formula (II), to be used in a subsequent process for the preparation of 1-benzyl-3-hydroxymethyl-1H-indazole according to formula (I).
Type:
Grant
Filed:
July 28, 2010
Date of Patent:
January 15, 2013
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: The present invention relates to the process for the conversion of 1-benzyl-3-hydroxymethyl-1H-indazole according to formula (II), to the 1-benzyl-3-hydroxylmethyl-1H-indazole according to formula (I).
Type:
Grant
Filed:
July 28, 2010
Date of Patent:
January 8, 2013
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
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:
Grant
Filed:
February 10, 2012
Date of Patent:
November 20, 2012
Assignee:
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 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:
March 6, 2009
Date of Patent:
November 20, 2012
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: A method of treating insulin resistance, obesity and metabolic syndrome by administering an indazolemethoxyalkanoic acid as described herein.
Type:
Application
Filed:
May 8, 2012
Publication date:
November 8, 2012
Applicant:
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 7, 2011
Date of Patent:
October 9, 2012
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: The present invention relates to a pharmaceutical composition comprising a combination of 1-benzyl-3-hydroxymethyl-indazole derivative, a pressure lowering agent selected from ACE-inhibitors, renin inhibitors, ARBs and CCBs, and/or a cholesterol lowering agent selected from statin derivatives. The combination showed an additive and synergistic activity in reducing MCP-1 levels, thus significantly improving inflammatory response inhibition and consequently reducing complications occurring in patients suffering from inflammatory diseases.
Type:
Application
Filed:
September 3, 2010
Publication date:
August 30, 2012
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F.S.p.A.
Inventors:
Angelo Guglielmotti, Beatrice Garrone, Alessandro Ble', Giuseppe Biondi, Roberta Petrosemolo, Enrica Biondi, Iacopo Biondi
Abstract: A method for treating an inflammatory process selected from the group consisting of oedema, erythema, articular inflammation, rheumatoid arthritis, arthrosis, a colorectal tumor, a pulmonary carcinoma, an adenocarcinoma, and combinations thereof, in a person in need thereof, the method comprising administering to the person in need thereof, in an amount sufficient to treat the inflammatory process, a 3-aminocarbazole or a salt thereof.
Type:
Grant
Filed:
October 28, 2010
Date of Patent:
June 26, 2012
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Maria Alessandra Alisi, Patrizia Dragone, Guido Furlotti, Nicola Cazzolla, Vincenzo Russo, Giorgina Mangano, Isabella Coletta, Lorenzo Polenzani
Abstract: Use of a compound of formula (I) in which R, R? and R? have the meanings given in the description, optionally in the form of a salt thereof with a pharmaceutically acceptable organic or mineral base, to prepare a pharmaceutical composition for reducing the blood triglyceride, cholesterol and glucose levels.
Type:
Grant
Filed:
November 13, 2007
Date of Patent:
June 12, 2012
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F.S.p.A.
Abstract: A process of production of trazodone or trazodone hydrochloride that comprises the steps of: (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:
Grant
Filed:
July 23, 2008
Date of Patent:
March 13, 2012
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Marcello Marchetti, Tommaso Iacoangeli, Giovanni Battista Ciottoli, Giuseppe Biondi
Abstract: A 2-arylindole compound substituted in position 5, of formula (I): in which X, Y, Z, W, A, R and R? have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.
Type:
Grant
Filed:
June 14, 2007
Date of Patent:
September 13, 2011
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Maria Alessandra Alisi, Nicola Cazzolla, Barbara Garofalo, Guido Furlotti, Caterina Maugeri, Rosella Ombrato, Isabella Coletta, Lorenzo Polenzani, Giorgina Mangano, Beatrice Garrone, Angelo Guglielmotti
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:
April 5, 2011
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: A compound of formula (I), in which R1, R2, R3, R4, R5, R6, X and Y have the meanings indicated in the description, and the pharmaceutically acceptable salts thereof. A pharmaceutical composition containing a compound of formula (I) or a pharmaceutically acceptable salt thereof. A method for preparing the abovementioned compound of formula (I) and the pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
July 25, 2006
Date of Patent:
February 1, 2011
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Inventors:
Maria Alessandra Alisi, Patrizia Dragone, Guido Furlotti, Nicola Cazzolla, Vincenzo Russo, Giorgina Mangano, Isabella Coletta, Lorenzo Polenzani
Abstract: Use of a 1-(3-chlorophenyl)-3-alkylpiperazine of formula (I), in racemic (R,S) form or in the form of the (S) enantiomer, in which R is a linear or branched alkyl group having from 1 to 3 carbon atoms, or of an addition salt thereof with a pharmaceutically acceptable organic or inorganic acid, for treating appetite disorder. A pharmaceutical composition that comprises a therapeutically effective amount of a 1-(3-chlorophenyl)-3-alkylpiperazine of formula (I) as previously defined or of an addition salt thereof with a pharmaceutically acceptable organic or inorganic acid, and at least one pharmaceutically acceptable excipient.
Type:
Grant
Filed:
June 2, 2006
Date of Patent:
February 1, 2011
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:
Application
Filed:
November 6, 2008
Publication date:
August 26, 2010
Applicant:
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
Abstract: Use of a compound of formula (I) in which R, R? and R? have the meanings given in the description, optionally in the form of a salt thereof with a pharmaceutically acceptable organic or mineral base, to prepare a pharmaceutical composition for reducing the blood triglyceride, cholesterol and glucose levels.
Type:
Application
Filed:
November 13, 2007
Publication date:
March 18, 2010
Applicant:
AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R. A.F. S.P.A.
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:
Application
Filed:
November 19, 2007
Publication date:
March 4, 2010
Applicant:
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