IP Library Granted Patent US 7,205,288
Granted Patent B2
US 7,205,288 · App. 11/445,140 · Granted Apr 17, 2007

Nitrate esters of corticoid compounds and pharmaceutical applications thereof

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Quick Facts
Patent No.
US 7,205,288
App. No.
11/445,140
Granted
Apr 17, 2007
Kind
B2
Abstract

Compounds of the formula and use of the compounds as medicaments.

Claims (27)

1. A compound of formula

B—R″—X 1 —NO 2

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 CH group or H 2 in the CH 2 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—CH 2 —CH 2 —Cl, or OH;

at position 4–5, a double bond;

at position 5–6, a double bond;

at position 6, Cl, F CH 3 , or CHO;

at position 7, Cl;

at position 9, Cl or F;

at position 11, OH, oxo or Cl;

at position 16, CH 3 , OH, or ═CH 2 ;

at position 17, OH, CH 3 , OCO(O) ua (CH 2 ) va CH 3 , 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 X 1 there is an ester or amide linkage;

the bivalent bridging member L is selected from the group consisting of (CR 4 R 5 ) na (O) nb (CR 4 R 5 ) n′a (CO) n′b (O) n″b (CO) n′″b (CR 4 R 5 ) 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 from each other and are equal to 0 or 1; R 4 and R 5 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, NR 1c where R 1c is a linear or branched alkyl having from 1 to 10 carbon atoms;

X 1 is selected from the group consisting of

wherein n 3 is an integer from 0 to 3; and

wherein B is a residue of flunisolide.

2. Pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.

Assignments (1)
CHANGE OF ADDRESS Recorded Dec 1, 2006
From: NICOX S.A.
To: NICOX S.A.
Reel/Frame 018700/0268 →