Abstract: The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of naproxen or bromonaproxen and R1–R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R—COOZ??(B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1–R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.
Type:
Grant
Filed:
August 6, 2003
Date of Patent:
April 3, 2007
Assignee:
Nicox S.A.
Inventors:
Piero Del Soldato, Giancarlo Santus, Francesca Benedini
Abstract: Nitro-oxyderivative compounds or salts thereof having the following general formula (I): A—(B)b0—(C)c0—NO2 wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A=R—T1—, wherein R is the radical of an analgesic drug for the chronic pain, in particular for the neuropathic pain; B is such that its precursor is selected from anminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid function; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.
Abstract: Compounds or their salts of general formula (I): A—B—N(O)s wherein: s is an integer equal to 1 or 2; A=R—T1—, wherein R is the drug radical and T1=(CO)t or (X)t?, wherein X=O, S, NR1c, R1c is H or a linear or branched alkyl or a free valence, t and t? are integers and equal to zero or 1, with the proviso that t=1 when t?=0; t=0 when t?=1; B=—TB—X2—O— wherein TB=(CO) when t=0, TB=X when t?=0, X being as above defined; X2 is equal to R1B—X—R2B radical wherein X is as above defined, R1B and R2B, equal to or different from each other, are linear or branched C1–C6 alkylenes, or X2 is a radical wherein two alkylene chains C1–C4 are linked to nonadjacent positions of a central ring having 4 or 6 atoms, said ring being an unsaturated cycloaliphatic ring, or a saturated or aromatic heterocylic ring, containing one or two heteroatoms, equal or different, selected from O, S, N; wherein the unsaturated cycloaliphatic ring does not have aromatic character according to Huckel's rule.
Abstract: Steroidal compounds or their salts having general formula: A—B—C—NO2 are described, wherein: A=R—, wherein R is a steroidal drug radical; B=—TB—X2—TBI—, wherein TB is (CO), TBI is O, S, NH, and X2 is a bivalent bridging group; and C is a bivalent radical.
Abstract: Captopril nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment or prophylaxis of cardiovascular, inflammatory and renal diseases.
Type:
Grant
Filed:
May 20, 2004
Date of Patent:
January 30, 2007
Assignee:
Nicox S.A.
Inventors:
Nicoletta Almirante, Ennio Ongini, Piero Del Soldato
Abstract: Statin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for treating and/or preventing several diseases, in particular coronary syndromes, neurodegenerative disorders as well as for reducing cholesterol levels.
Type:
Grant
Filed:
May 20, 2004
Date of Patent:
January 23, 2007
Assignee:
Nicox S.A.
Inventors:
Francesca Benedini, Ennio Ongini, Piero Del Soldato
Abstract: Use of organic compounds containing the —ONO2 function, or inorganic compound containing the —NO group or compositions comprising said compounds to reduce the toxicity caused by drugs to the gastrointestinal and/or renal apparatus, said compounds being characterized in that they are nitric oxide NO donors i.e., when they are put into contact in vitro with cells of the vasal endothelium or platelets.
Abstract: The present invention provides a new class of compounds presenting a high compatibility with tissues and organic fluids. Such new compounds are polysaccharides essentially formed of units of uronic acid and/or hexosamine, containing nitro groups —ONO2 covalently bonded to the saccharide structure. Preferably, the polysaccharides according to the invention are prevalently formed of disaccharide repeating units formed of uronic acid and hexosamine. These compounds, in psychological conditions, selectively release NO, allowing a reduction in the amount of NO needed to achieve a determined therapeutical effect. This result has been achieved by functionalizing polysaccharides essentially formed of units of uronic acid and/or hexosamine, with subsituents containing a ONO2 ? group.
Type:
Grant
Filed:
August 10, 2001
Date of Patent:
February 28, 2006
Assignee:
NicOx S.A.
Inventors:
Francesca Benedini, Benito Casu, Piero Del Soldato, Paolo Gresele, Annamaria Naggi, Giangiacomo Torri, Simona Venturini
Abstract: Compounds of their salts having general formulas (I) and (II) wherein: s=is an integer equal to 1 or 2, preferably s=2; b0=0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.
Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.