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US 2004/0023933 A1Published application
Nitroderivatives as drugs for diseases having an inflammatory basis
AssigneeNicox S.A.
InventorsPiero Del Soldato, Francesca Benedini, Patrizia Antognazza
Life of this patent
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Abstract
Use for the treatment of diseases having an inflammatory basis of compounds or salts thereof, having the following general formula (I): A-Xt-L-(W)p—NO2 wherein A contains the radical of a drug, Xt and W arc bivalent radicals, L, is a covalent bond or oxygen, sulphur, NRtc wherein Rtc is H or a C1-C5 linear or branched alkyl.
Claims10
Use for preparing drugs for pre cancer or cancer diseases on an inflammatory basis of nitroderivatives or salts thereof having the followin general formula (I):
- A-X1-(W)p—NO2 (I)
- wherein:
- p is an integer equal to 1 or 0;
- A=R-T1, wherein
- R is the radical of a precursor drug and it has the following formulas:
- 42
- wherein
- s is an integer and it is 1 or 0;
- RAI is H, CH3:
- R1 is OCOR3, R3 being a C1-C5 linear or branched radical, NHCOR3, wherein R3—has the above meaning, or R1 is OH, CH2CH(CH3)2, phenyl, benzoyl, 4,6-dichlorophenylamino;
- R6 is H, or one halogen atom, preferably fluorine;
- or R1 and R6, when are located in the adjacent positions 4 and 5 of the aromatic ring of formula (AI), form the radical of following formula (AIa):
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- or R can be the following formula:
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- T1=(CO)t or (X)t′, wherein X=O, S, NR1c, R1c is H or a linear or branched alkyl, having from 1 to 5 carbon atoms, 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;
- X1=-TB-Y-TBI—wherein
- TB and TBI are equal or different;
- TB=(CO) when t=0, TB=X when t′=0, X being as above;
- TBI=(CO)tx or (X)txx, wherein tx and txx have the value of 0 or 1;
- with the proviso that tx=1 when txx=0;
- and tx=0 when txx=1;
- X is as above;
- Y is a bivalent linking group selected from the following:
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- wherein:
- nIX is an integer in the range 0-3, preferably 1;
- nIIX is an integer in the range 1-3, preferably 1;
- RTIX, RTIX′, RTIIX, RTIIX′, equal to or different from each other are H or a C1-C4 linear or branched alkyl;
- preferably RTIX, RTIX′, RTIIX, RTIIX′ are H;
- Y3 is a saturated, unsaturated or aromatic heterocyclic ring, having 5 or 6 atoms, containing one or two nitrogen atoms,
- an alkylene group R′ wherein R′ is a C1-C20 linear or branched when possible, preferably having from (2 to 6 carbon atoms, optionally substituted with one or more of the following groups:
- —NHCOR3, wherein R3 is as above, —NH2, —OH or
- a cycloalkylene having from 5 to 7 carbon atoms, optionally substituted with side chains R′, R′ being as above, one or more carbon atoms of the cycloalkylene ring can optionally be substituted by heteroatoms;
- or
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- wherein n3 is an integer from 0 to 3 and n3′ is an integer from 1 to 3;
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- wherein n3 and n3′ have the above meaning,
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- wherein
- R4 is hydroxy, hydrogen, R5O— alkoxy wherein R5 is a C1-C10 linear or branched or cyclic alkyl group, preferably R5 is a methyl group;
- R2 is a C2-C10 linear or branched alkenylene group which can contain one or more double bonds, preferably R2 is the ethenylene group (—CH═CH—);
- or
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- wherein R1f=H, CH3 and nf is an integer from 0 to 6;
- preferably from 0 to 4;
- L=covalent bond, or L=X, X being as above, or L=CO;
- W=YTO wherein YT has the same meanings of Y and YT in the compound of formula (I) is equal to or different from Y.
47 more elements
Dependencies are inferred from the claim text.