IP Library Granted Patent US 6,909,007
Granted Patent B1
US 6,909,007 · App. 09/926,327 · Granted Jun 21, 2005

Steroidal pharmaceutical compounds

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Quick Facts
Patent No.
US 6,909,007
App. No.
09/926,327
Granted
Jun 21, 2005
Kind
B1
Abstract

Steroidal compounds or 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═R—, wherein R is the steroidal drug radical, C and C 1 are two bivalent radials. The precursors of the radicals B and B 1 are such as to the pharmacological tests repotted in the description.

Claims (18)

1. A steroidal compound or a salt thereof having the following formula:

A—B—C—NO 2

wherein:

A is a steroidal drug radical having the formula:

B=—T B —X 2 -T BI —, wherein:

T B is O,

T BI is (CO) or O, and

X 2 is a bivalent bridging group such as the corresponding precursor of B, having the formula Z—T B —X 2 —T BI —Z′ in which Z and Z′ are independently H or OH, is selected from the following compounds:

C is the bivalent radical —T C —Y—, wherein:

T C is (CO) when T BI is O,

T C is O when T BI is (CO), and

Y is a linear or branched C 1 to C 20 alkyleneoxy group or a cycloalkylene, wherein the cycloalkylene has from 5 to 7 carbon atoms, one or more carbon atoms in the cycloalkyleneic ring can be substituted by heteroatoms, and the cycloalkyleneic ring can have methyl side chains.

2. The steroidal compound or salt thereof according to claim 1 , wherein B is

3. The steroidal compound or salt thereof according to claim 1 , wherein Y is a linear or branched C 1 to C 6 alkylenoxy group.

4. The steroidal compound or salt thereof according to claim 1 , wherein A is ursodeoxycholic acid or chenodeoxycholic acid.

5. The steroidal compounds or salts thereof according to claim 1 selected from 3-[4-[(3α,5β,7β)-3,7-dihydroxycolan-24-oiloxy]-3-methoxyphenyl]-2-propenoic acid 4-nitroxybutyl ester or 3-[4-[(3α, 5β, 7α)-3,7-dihydroxycolan-24-oiloxy]-3-methoxyphenyl]-2-propenoic acid 4-nitroxybutyl ester.

6. A pharmaceutical formulation comprising the steroidal compound or salt thereof according to claim 1 and a pharmaceutically acceptable carrier.

7. A method for the treatment of oxidative stress and/or endothelial dysfunctions comprising administering the steroidal compound or salt thereof according to claim 1 .

Assignments (3)
CHANGE OF ADDRESS Recorded Dec 1, 2006
From: NICOX S.A.
To: NICOX S.A.
Reel/Frame 018700/0268 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 8, 2005
From: NICOX S.A.
To: AXCAN PHARMA INC.
Reel/Frame 016342/0463 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 15, 2001
From: DEL SOLDATO, PIERO
To: NICOX S.A.
Reel/Frame 012310/0787 →