Abstract: Compounds of formula I:
wherein A is a heterocycle containing a nitrogen atom and optionally saturated or unsaturated and optionally further substituted by an oxo group (═O); R is: hydrogen, cyano, (C1-4)alkoxycarbonyl, carbamoyl; optionally substituted (C4-7)-cycloalkyl, aryl or heterocycle; (C1-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl optionally branched and/or substituted by (C4-7) cycloalkyl, aryl or heterocycle; aryloxy, heterocyclyloxy, aryl(C1-4)alkoxy, heterocyclyl(C1-4)alkoxy, amino substituted by one or two (C1-4)alkyl group(s), aryl-amino, heterocyclyl-amino, aryl(C1-4)alkyl-amino, or heterocyclyl(C1-4)alkylamino; Y is methylene or ethylene; W is an optionally substituted aryl or heterocycle; R1 is hydrogen, (C4-7)cycloalkyl or a (C2-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl group optionally substituted by hydroxy, oxo, (C4-7)cycloalkyl, aryl or heterocycle, and optionally interrupted by one or more heteroatom(s) or heterogroup(s); R2 is a (C1-6)alkyl or polyfluoro(C1-6)alkyl gr
Abstract: An isomerization process of trans-5-fluoro-2-methyl-1-[p-(methylthio)benzyliden]inden-3-acetic acid for the treatment of sodium salt in methanol and in the presence of a base at 70±2° C. is described.
Abstract: A process for the preparation of the compounds of formula
(wherein R has the meanings reported in the specification) by enzymatic transesterification of enantiomeric mixtures is described.
These compounds are intermediates useful in the synthesis of Diltiazem.
Abstract: The present invention provides a compound selected from the group including: N-3-acetyl-1-(3,5-dichloropyridin-4-ylmethyl)-5-cyclopentyloxy-6-methoxy-4H-phthalazine; 6,7-dimethoxy-1-pyridin-4-ylmethyl-4-thiazol-2-yl-phthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)ethanone; 2-methanesulphonyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 2-formyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)-1-imidazol-1-ylmethanone; 1-(3,5-dichloro-pyridin-4-ylmethyl)-3-methansulphonyl-6-difluoromethoxy-5-(tetrahydro-furan-2-yloxy)-4H-phthalazine; N→O derivatives thereof; and pharmaceutically acceptable salts thereof. The invention also provides a pharmaceutical composition, which contains a therapeutically effective amount of the above compound in admixture with a pharmaceutically acceptable carrier.
Abstract: The present invention provides a compound selected from the group including: 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-phenyl-phthalazine; 4-(3,5-dichloro-pyridin-4-ylmethyl)-7-methoxy-1H-phthalazin-2-carboxylic acid methyl ester; benzyl-{3-{1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl}-prop-2-ynyl}-methyl-amine; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-5-(5-morpholin-4-yl-pent-1-ynyl)-phthalazine dihydrochloride; 3-{1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl}-prop-2-yn-1-ol; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-morpholin-4-yl-phthalazine; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-(1,2,4)triazol-1-yl-phthalazine; N→O derivatives thereof; and pharmaceutically acceptable salts thereof. The invention also provides a pharmaceutical composition which includes a therapeutically effective amount of the above compound in admixture with a suitable carrier.
Type:
Grant
Filed:
January 22, 2001
Date of Patent:
December 11, 2001
Assignee:
Zambon Group S.p.A.
Inventors:
Mauro Napoletano, Gabriele Norcini, Giancarlo Grancini, Franco Pellacini, Gian Marco Leali, Gabriele Morazzoni
Abstract:
Compounds of formula (I) wherein A is an orthocondensed heterocycle optionally substituted by certain substituents and necessarily substituted by a —B—Cy group where the variables are as defined in the specification and the N→O derivatives and pharmaceutically acceptable salts thereof are phosphodiesterase-4 inhibitors.
Abstract: A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.
Type:
Grant
Filed:
April 27, 2000
Date of Patent:
August 7, 2001
Assignee:
Zambon Group S.p.A.
Inventors:
Marco Villa, Pietro Allegrini, Katiuscia Arrighi, Maurizio Paiocchi
Abstract: A method for the removal of heavy metals from solutions of organic compounds by treatment with cysteine or with an N-acylcysteine is described. Organic compounds with a content of heavy metal, for example palladium, particularly low and suitable for the preparation of compounds with pharmacologic activity can be isolated from the resultant solutions.
Type:
Grant
Filed:
December 30, 1999
Date of Patent:
May 29, 2001
Assignee:
Zambon Group S.p.A.
Inventors:
Marco Villa, Vincenzo Cannata, Alessandro Rosi, Pietro Allegrini
Abstract: Compounds of formula (I)
wherein R, R′, R″, R1, R2, R3, R4, R5, R6, X, Y, m, n, and p have the meanings reported in the description; and their pharmaceutically acceptable salts are described.
Type:
Grant
Filed:
August 12, 1999
Date of Patent:
May 15, 2001
Assignee:
Zambon Group S.p.A.
Inventors:
Stefania Montanari, Paolo Cavalleri, Francesco Santangelo, Cristina Fraire, Giancarlo Grancini, Napoletano Mauro, Francesco Marchini, Lorenzo Pradella, Claudio Semeraro
Abstract: Compounds of formula (I) wherein Ra and Rb the same or different, are hydrogen atoms, acyl groups deriving from a lower carboxylic acid or chains of formula (a) useful as reverse transcriptase inhibitors antiviral activity are described.
Type:
Grant
Filed:
January 31, 2000
Date of Patent:
April 10, 2001
Assignee:
Zambon Group S.p.A.
Inventors:
Franco Pellacini, Domenico Ungheri, Giovanna Schioppacassi, Jean-Louis Kraus, Michel Camplo, Nicolas Mourier, Jean-Claude Chermann
Abstract: A compound of formula (II), wherein R1 is chloro, fluoro or trifluoromethyl; R2 is hydrogen, chloro, fluoro or trifluoromethyl; and R is hydrogen or a protective group for the hydroxy moiety useful as an intermediate for the synthesis of antimycotic azole compounnds.
Abstract: A process for the preparation of heteroaryl-zinc halides of the formula (II): Het—Zn—X, wherein Het is an optionally substituted 5 or 6 membered aromatic heterocyclic group with one or two heteroatoms selected among nitrogen, oxygen or sulphur; X is a chlorine, bromine or iodine atom; comprising metallation reaction of heteroarylhalide with metallic zinc optionally activated by washing with acids, is described. Compounds of the formula (II) are intermediates useful in the synthesis for the preparation of compounds endowed with pharmacological activity.
Abstract: An analgesic composition useful in the preparation of fast dissolving tablets is provided, where the composition is the result of combining ibuprofen, arginine, linear PVP and an alkaline bicarbonate to which usual excipients for the preparation of tablets are added.
Type:
Grant
Filed:
May 26, 1999
Date of Patent:
March 6, 2001
Assignee:
Zambon Group S.p.A.
Inventors:
Alessandro Grassano, Maurizio Marchiorri, Mauro Di Toro, Franco Castegini
Abstract: Process for the preparation of a compound of formula (VII) wherein R1 is Cl, F or CF3; R2 is H, Cl, F or CF3; and R3 is C1-4 alkyl; characterized in that an olefin of formula (II) is epoxidized to give an oxirane of formula (III) which treated with alkyl-magnesium halide gives a triol of formula (IV) which is turned into an epoxide of formula (V), then treated with 1,2,4-triazole. The compounds (VII) are useful for preparing azole derivatives active as antifungal agent.
Type:
Grant
Filed:
June 2, 2000
Date of Patent:
February 27, 2001
Assignee:
Zambon Group S.p.A.
Inventors:
Marco Villa, Mauro Napoletano, Aldo Belli, Francesco Ponzini, Fabio Rondina
Abstract: A process for the preparation of I:
in which R and R1 have the meanings reported in the description, that comprises the enzymatic kinetic resolution by transesterification with aminoalcohols of 3-phenylglycidates of formula I:
is described.
Type:
Grant
Filed:
September 20, 1999
Date of Patent:
February 13, 2001
Assignee:
Zambon Group S.p.A.
Inventors:
Marco Villa, Dario Tentorio, Angelo Restelli, Sergio Riva
Abstract: A method for removing heavy metals, selected from palladium, tin and nickel, from heavy metal complexes with thiazole compounds in aqueous or alcoholic solution, by precipitation as sulfides, characterised in that such solutions are treated with a water-soluble ammonium, alkaline or alkaline-earth sulfide.
Abstract: Compounds of formula (I) wherein R, R.sub.1, R.sub.2, R.sub.3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
Abstract: A process for the preparation of S-alkylcysteines of formula ##STR1## wherein R is a lower or branched C.sub.1 -C.sub.4 alkyl group; by S-alkylation of cysteines with dialkylcarbonates.
Type:
Grant
Filed:
February 3, 1999
Date of Patent:
November 14, 2000
Assignee:
Zambon Group S.p.A.
Inventors:
Pietro Allegrini, Giuseppe Barreca, Elena Rossi
Abstract: A compound of Formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, wherein n is an integer between 2 and 6 and R.sub.1 is a methyl group or a group ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, methoxy, methylsulfonyl, or one of R.sub.2, R.sub.3 and R.sub.4 together with another one of the three substituents forms a --O--CH.sub.2 --O-- bridge. The asterisk marks an asymmetric carbon atom.
Type:
Grant
Filed:
December 6, 1999
Date of Patent:
August 22, 2000
Assignee:
Zambon Group S.p.A.
Inventors:
Felice Pocchiari, Claudio Masotto, Paolo Cavalleri, Stefania Montanari, Francesco Santangelo
Abstract: Compounds of formula ##STR1## wherein R.sub.1 is chloro, fluoro, bromo or trifluoromethyl;R.sub.2 is hydrogen, chloro , fluoro, bromo or trifluoromethyl;Z is CH or N;R.sub.3, R.sub.4 and R.sub.5, which are the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl, with the proviso that R.sub.4 is different from R.sub.5 when R.sub.3 is hydrogen;X is O, S, SO or SO.sub.2 ;R.sub.6 is a C.sub.1 -C.sub.5 polyfluoroalkyl group containing at least two fluorine atoms and optionally other halogen atoms selected from the group consisting of chloro and bromo; processes for their preparation and pharmaceutical compositions containing them are described.The compounds of formula II-A are endowed with a marked wide range antimycotic acitivity.