Nitrate salts of antimicrobial agents for the preparation of antimicrobial medicaments, specifically antiviral, antifungal and antibacterial medicaments.
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1. A nitrate salt of an antimicrobial compound having formula II:wherein:X and Y, different from one another, are C or N,R 6 =cyclopropyl, C 2 H 5 , 4-fluorophenyl, 2,4-difluorophenyl, or 2-fluoroethyl,R 7 =H; amino, or CH 3 ,R 8 =H or F, or when Y=N, R 8 is the free electron doublet on the n
1. A nitrate salt of an antimicrobial compound having formula II:wherein:X and Y, different from one another, are C or N,R 6 =cyclopropyl, C 2 H 5 , 4-fluorophenyl, 2,4-difluorophenyl, or 2-fluoroethyl,R 7 =H; amino, or CH 3 ,R 8 =H or F, or when Y=N, R 8 is the free electron doublet on the nitrogen atom, which forms a double bond with the carbon atom adjacent the nitrogen,R 9 =H or CH 3 or one of the following substituents:wherein M=H, CH 3 , C 2 H 5 , OH,wherein T 1 is H, OHR 8 and R 9 taken together form the bivalent radical having formula: 2 —O— (IIP),R 10 =H, Cl, F, or when X=N, R 10 is the free electron doublet on the nitrogen atom, which forms a double bond with the carbon atom adjacent the nitrogen, or R 8 and R 10 taken together form the following bivalent radicals: 2. The nitrate salt according to claim 1, selected from the following:when R 6 =cyclopropyl, R 7 =H, R 8 =F, R 9 =(IIA) with M=H, R 10 =H, X=Y=C, the compound is known as Ciprofloxacin,when R 6 =cyclopropyl, R 7 =H, R 8 =F, R 9 =(IIF), R 10 =Cl, X=Y=C, the compound is known as Clinaloxacin,when R 6 =4-fluorophenyl, R 7 =H, R 8 =F, R 9 =(IID), R 10 =H, X=Y=C, the compound is known as Difloxacin,when R 6 =C 2 H 5 , R 7 =H, R 8 =F, R 9 =(IIA) with M=H, R 10 =free valence, X=N, Y=C, the compound is known as Enoxacin,when R 6 =cyclopropyl, R 7 =H, R 8 =F, R 9 =(IIA) with M=C 2 H 5 , R 10 =H, X=Y=C, the compound is known as Enrofloxacin,when R 6 =fluoroethyl, R 7 =H, R 8 =F, R 9 =(IIA) with M=CH 3 , R 10 =F, X=Y=C, the compound is known as Fleroxacin,when R 6 with R 10 forms the bivalent radical (IIM), R 7 =H, R 8 =F, R 9 =H, X=Y=C, the compound is known as Flumequine,when R 6 =cyclopropyl, R 7 =CH 3 , R 8 =F, R 9 =(IIB), R 10 =H, X=Y=C, the compound is known as Gre-pafloxacin,when R 6 =ethyl, R 7 =H, R 8 =F, R 9 =(IIB), R 10 =F, X=Y=C, the compound is known as Lomefloxacin,when R 6 with R 10 forms the bivalent radical (IIM), R 7 =H, R 8 =F, R 9 =(IIE) with T 1 =OH, X=Y=C, the compound is known as Nadifloxacin,when R 6 =C 2 H 5 , R 7 =H, R 8 =H, R 8 =CH 3 , R 10 =free valence, X=N, Y=C, the compound is known as Na-lidixic Acid,when R 6 =C 2 H 5 , R 7 =H, R 8 =F, R 9 =(IIA) with M=H, R 10 =H, X=Y=C, the compound is known as Norfloxacin,when R 6 with R 10 forms the bivalent radical (IIN), R 7 =H, R 8 =F, R 9 =(IIA) with M=CH 3 , X=Y=C, the compound is known as Ofloxacin,when R 6 =C 2 H 5 , R 7 =H, R 8 and R 9 form the bivalent radical (IIP), R 10 =H, X=Y=C, the compound is known as Oxolinic Acid,when R 6 with R 10 forms the bivalent radical (IIO), R 7 =H, R 8 =F, R 9 =(IIH), X=Y=C, the compound is known as Pazufloxacin,when R 6 =ethyl, R 7 =H, R 8 =F, R 9 =(IIA) with M=CH 3 , R 10 =H, X=Y=C, the compound is known as Pefloxacin,when R 6 =C 2 H 5 , R 7 =H, R 8 =free valence, R 9 =(IIA) with M=H, R 10 =free valence, X=Y=N, the compound is known as Pipemidic Acid,when R 6 =C 2 H 5 , R 7 =H, R 8 =free valence, R 9 =(IIE) with T 1 =H, R 10 =free valence, X=Y=N, the compound is known as Piromidic Acid,when R 6 with R 10 forms the bivalent radical (IIQ), R 7 =H, R 8 =F, R 9 =(IIA) with M=CH 3 , X=Y=C, the compound is known as Rufloxacin,when R 6 =cyclopropyl, R 7 =amino, R 8 =F, R 9 =(IIC), R 10 =F, X=Y=C, the compound is known as Sparfioxacin,when R 6 =2,4-difluorophenyl, R 7 =H, R 8 =F, R 9 =(IIE), R 10 =free valence, X=N, Y=C, the compound is known as Tosufloxacin,when R 6 =2,4-difluorophenyl, R 7 =H, R 8 =F, R 9 =(IIG), R 10 =free valence, X=N, Y=C, the compound is known as Trovafloxacin,when R 6 =cyclopropyl, R 7 =H, R 8 =F, R 9 =(IID), R 10 =H, X=Y=C, the compound is known as Danofloxacin, orwhen R 6 =4-fluorophenyl, R 7 =H, R 8 =F, R 9 =(IIA) with M=H, R 10 =H, X=Y=C, the compound is known as Sarafloxacin. 3. The nitrate salt according to claim 2 selected from the following:wh en R 6 =cyclopropyl, R 7 =H, R 8 =F, R 9 =(IIA) with M=H, R 10 =H, X=Y=C, the compound is known as Ciprofloxacin,when R 6 =C 2 H 5 , R 7 =H, R 8 =H, R 9 =CH 3 , R 10 =free valence, X=N, Y=C, the compound is known as Nali-dixic acid,when R 6 =C 2 H 5 , R 7 =H, R 8 =F, R 9 =(IIA) with M=H, R 10 =H, X=Y=C, the compound is known as Norfloxacin, orwhen R 6 with R 10 forms the bivalent radical (IIN), R 7 =H, R 8 =F, R 9 =(IIA) with M=CH 3 , X=Y=C, the compound is known as Ofloxacin. 4. The nitrate salt according to claim 1 wherein in their molecules there are one or more substituents having the formula (I-N) p —ONO 2 (I-N)wherein:p is 1 or 0;B=—T B —Y—T BI — wherein T B and T BI are same or different;T B is a chemical function covalently linked to the chemical or reacting function of the drug molecule and is (CO) or X, wherein X=O, S, NH, with the condition that X=(CO) when the reacting function of the drug is OH or NH 2 or SH; T B is X when the reacting function of the drug is a carboxyl group;T BI =(CO) tx or (X) txx , wherein tx and txx are 0 or 1; with the condition that tx=1 when txx=0, tx=0 when txx=1; X is as above defined;Y is a bivalent linking bridge chosen between the following structures: wherein:nIX is an integer selected from 0, 1, 2, or 3;nIIX is an integer selected from 0, 1, 2, or 3;R TIX , R TIX , R TIIX , R TIIX′ , same or different each from the other, are H or linear or branched C 1 -C 4 alkyl;Y 3 is a ring containing at least one salifiable nitrogen atom;an alkylene group R′ wherein R′ is a linear or branched C 1 -C 20 alkyl, optionally substituted with one or more of the following groups: —NHCOR 3Y , wherein R 3Y is a linear or branched C 1 -C 5 alkyl, —NH 2 , or —OH,a cycloalkylene ring C 5 -C 7 , optionally substituted with R′, being R′ as above defined, wherein one or more C atoms of the cycloalkylene can be optionally substituted with heteroatoms; wherein n3 is an integer from 0 to 3 and n3′ is an integer from 1 to 3; wherein n3 and n3′ have the meanings above indicated; wherein:R 4Y is OH, or H, alcoxy R 5Y O— wherein R 5Y is a linear or branched or cyclo C 1 -C 10 alkyl;R 2Y is a linear or branched alkenylene C 2 -C 10 containing one or more double bonds; wherein R 1f =H, CH 3 and nf is an integer from 0 to 6;W of formula (I-N) is the bivalent radical —T C —Y T -wherein:T c =(CO) when t x =0, T c =X when t xx =0;with the proviso that in formula (I-N) when p=1 Y T is different from Y and in the bivalent radical B:Y is R′ as above defined having a substituent NHCOR 3Y , orY is a bivalent radical of formula (V-Y), wherein R 4Y is OR 5Y and R 5Y isCH 3 , R 2Y is the group —CH═CH—. 5. The nitrate salt according to claim 4 wherein Y 3 in formula (II-Y) is selected from the following bivalent radicals: 6. The nitrate salt according to claim 5 wherein Y 3 is a 6-membered aromatic ring containing one nitrogen atom, said ring having the two free valences in the following positions: 2,6; 2,3; or 2,5. 7. The nitrate salt according to claim 6 wherein Y 3 is Y12 substituted at positions 2 and 6. 8. A composition comprising the nitrate salt according to claim 1 wherein one or more isomers of the compounds are included. 9. The nitrate salt according to claim 1 containing one nitrate ion mole/compound mole. 10. The nitrate salt according to claim 1 containing one substituent of the formula (I-N). 11. The nitrate salt according to claim 4 wherein R TIX , R TIX′ , R TIIX , and R TIIX′ are H. 12. The nitrate salt according to claim 4, wherein Y is a heterocyclic ring containing one or two nitrogen atoms, the ring saturated, unsaturated or aromatic. 13. The nitrate salt according to claim 4, wherein the ring has 5 or 6 atoms. 14. The nitrate salt according to claim 4, wherein R′ is a C 2 -C 6 alkyl and/or R 5Y is methyl. 15. The nitrate salt according to claim 4, wherein R 2Y is an ethylene group (—CH—CH). 16. The nitrate salt according to claim 4, wherein nf is an integer from 0 to 4. 17. The nitrate salt according to claim 4, wherein in formula (I-N) when p=1 Y T is different from Y and in the bivalent radical B:R′ is a C 2 saturated alkyl and R 3Y is CH 3 . 18. The nitrate salt according to claim 4, wherein in formula (I-N) when p=1 Y T is different from Y and in the bivalent radical B:Y is CH 2 —CH(NHCOCH 3 )— and B in formula (I-N) has the following structure: 19. The nitrate salt according to claim 4, wherein in formula (I-N) when p=1 Y T is different from Y and in the bivalent radical B:Y has the following formula: 20. A pharmaceutical composition, comprising a compound having formula II:wherein:X and Y, different from one another, are C or N,R 6 =cyclopropyl, C 2 H 5 , 4-fluorophenyl, 2,4-difluorophenyl, or 2-fluoroethyl,R 7 =H, amino or CH 3 ,R 8 =H or F, or when Y=N, R 8 is the free electron doublet on the nitrogen atom, which forms a double bond with the carbon atom adjacent the nitrogen,R 9 =H, CH 3 or one of the following substituents:wherein M=H, CH 3 , C 2 H 5 , or OH,wherein T 1 is H, OHR 8 and R 9 taken together form the bivalent radical having formula: —O—CH 2 —O— (IIP),R 10 =H, Cl, or F, or when X=N, R 10 is the free electron doublet on the nitrogen atom, which forms a double bond with the carbon atom adjacent the nitrogen, or R 6 and R 10 taken together form the following bivalent radicals:and a pharmaceutical carrier.
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