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US 7,605,151 B2Granted
Nitrate esters of corticoid compounds and pharmaceutical applications thereof
AssigneeNicox S.A.
InventorPiero Del Soldato
Life of this patent
Estimating the term…
Abstract
Compounds of the formula and use of the compounds as medicaments.
Claims2
A compound of formula
- B—R″—X1—NO2
- or their esters or salts,
- wherein B—R″ has the following structure:
- R″ is —(CO—L)t—(X)t1
- wherein in the place of H in the OH group or H2 in the CH2 group there may be the following substituents:
- at position 1-2:
- a double bond;
- at position 2-3
- at position 2, Cl or Br;
- at position 3, oxo, —O—CH2—CH2—Cl, or OH;
- at position 4-5, a double bond;
- at position 5-6, a double bond;
- at position 6, Cl, F, CH3, or CHO;
- at position 7, Cl;
- at position 9, Cl or F;
- at position 11, OH, oxo or Cl;
- at position 16, CH3, OH, or ═CH2;
- at position 17, OH, CH3, OCO(O)ua(CH2)va, CH2, or
- wherein ua is an integer equal to 0 or 1 and va is an integer from 0 to 4;
- at position 16-17,
- R and R′ are equal or different one from the other and may be hydrogen or linear or branched alkyls having from 1 to 4 carbon atoms,
- wherein in R″ t and t1 are integers where t is equal to 1, t1 equals 0, 1;
- wherein between B and X1 there is an ester or amid linkage;
- the bivalent bridging member L is selected from the group consisting of
- (CR4R5)na(O)nb(CR4R5)n′a(CO)n′b(O)n″b(CO)n′″b(C4R5)n″a,
- wherein na, n′a, and n″a are equal to or different one from the other and are integers from 0 to 6, nb, n′b, n″b and n′″b are equal to or different to each other and are equal to 0 or 1;
- R4 and R5 are equal or different one from the other and are selected from the group consisting of H, linear or branched alkyls having 1 to 5 carbon atoms, X is equal to Xo where Xo is O, NH, NR1c where R1c, is a linear or branched alkyl having from 1 to 10 carbon atoms;
- X1 is selected from the group consisting of
- wherein n3 is an integer from 0 to 3;
- and
- wherein B is a residue of a compound selected from the group consisting of:
- hydrocortisone, alclomethasone, algestone, beclomethasone, chloroprednisone, clobetasol, clobetasone, clocortolone, cortisone, coricosterone, deflazacort, desonide, desoximethasone, dexamethasone, diflorasone, diflucortolone, difluprednate, fluazacort, flucloronide, flumethasone, fluccinolone acetonide, fluocinonide, fluocortyn butyl, fluocortolone, fluorometholone, fluperolone acetate, fluprednidene acetate, fluprednisolone, flurandrenolide, halcinolide, halobetasol propionate, halomethasone, halopredone acetate, hydrocortamate, iotprednol etabonate, medrysone, meprednisone, methylprednisolone, mometasone, furoate, paramethasone, prenisolone, prednisolone 5-diethylaminoacetate, prednisolone sodium phosphate, prednisone, prednival, prednylidene, rimexolone, triamcinolone, 21-acetoxypregnenolone, fluticasone, propionate, mazipredone, and tixocortol.
29 more elements
Dependencies are inferred from the claim text.