US 2003/0199453 A1Published application

Small molecule inhibitors of secretion of proteins encoded by ARE-mRNAs

AssigneeMessage Pharmaceuticals

InventorsTony Giordano, Michael A. Sturgess

Life of this patent

Estimating the term…

Abstract

The invention features compounds that inhibit secretion of a protein encoded by an ARE-mRNA or that modulate regulation of an ARE-mRNA. These compounds are useful for the treatment or prevention of conditions involving proteins encoded by ARE-mRNAs, such as TNFα.

Claims20

Dependent claims

A compound having one of the following formulas:

50
or a derivative or salt thereof, wherein
R1 and R6 are independently selected from the group consisting of an alkyl and an aryl group;
R2 and R5 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group;
X is oxygen or H2N(HN)C(H)NN—;
and
m is at least one;
51
or a derivative or salt or salt thereof, wherein
R1 and R6 are independently selected from the group consisting of an alkyl and an aryl group;
R2 and R5 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl;
and
m is at least one;
52
or a derivative or salt or salt thereof , wherein
R1 and R2 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 and R4 are independently selected from the group consisting of an alkyl and an aryl group;
and
X is oxygen or H2N(HN)C(H)NN—;
53
or a derivative or salt or salt thereof, wherein
R1 and R4 are independently selected from the group consisting of an alkyl and an aryl group;
and
R2 and R3 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
54
or a derivative or salt or salt thereof, wherein
R1 and R5 are independently selected from the group consisting an aryl and an alkyl group;
R2 is hydrogen, an alkyl, or aryl group;
R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group;
X is oxygen or H2N(HN)C(H)NN—;
and
m is at least one;
55
or a derivative or salt or salt thereof, wherein
R1 and R6 are independently selected from the group consisting of an alkyl and an aryl group;
R3is hydrogen, an alkyl, or an aryl group;
R2, R4, and R5 are independently selected from the group consisting of hydrogen and an alkyl;
and
m is at least one;
or
56
or a derivative or salt or salt thereof, wherein
R1 and R2 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 is an aryl group;
and
m is at least one.

45 more elements

A method for treating or preventing a condition in a subject, said method comprising administering to said subject a chemical compound in an amount sufficient to inhibit secretion of a protein encoded by an ARE-mRNA or modulate regulation of an ARE-mRNA in said subject;

said compound having one of the following formulas:
57
or a derivative or salt or salt thereof, wherein
R1 and R6 are independently selected from the group consisting of an alkyl and an aryl group;
R2 and R5 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group;
X is oxygen or H2N(HN)C(H)NN—;
and
m is at least one;
58
or a derivative or salt thereof, wherein
R1 and R6 are independently selected from the group consisting of an alkyl and an aryl group;
R2 and R5 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl;
and
m is at least one;
59
or a derivative or salt thereof, wherein
R1 and R2 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 and R4 are independently selected from the group consisting of an alkyl and an aryl group;
and
X is oxygen or H2N(HN)C(H)NN—;
60
or a derivative or salt thereof, wherein
R1 and R4 are independently selected from the group consisting of an alkyl or an aryl group;
and
R2 and R3 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
61
or a derivative or salt thereof, wherein
R1 and R5 are independently selected from the group consisting an aryl or alkyl group;
R2 is hydrogen, an alkyl, or aryl group;
R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group;
X is oxygen or H2N(HN)C(H)NN—;
and
m is at least one;
62
or a derivative or salt thereof, wherein
R1 and R6 are independently selected from the group consisting of an alkyl and an aryl group;
R3 is hydrogen, an alkyl, and an aryl group;
R2, R4, and R5 are independently selected from the group consisting of hydrogen and an alkyl;
and
m is at least one;
or
63
or a derivative or salt thereof, wherein
R1 and R2 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 is an aryl group;
and
m is at least one.

46 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/117,955Filed 8 Apr 2002
Priority: 10 Apr 2001
Published: 23 Oct 2003
Term ends: Not estimatedThe source records don’t support an estimate.

Classification6 codes

C07D 295/185
Radicals derived from carboxylic acids: from aliphatic carboxylic acids
C07C 281/18
Compounds containing any of the groups [IMAGE cpc-sch-C07C-0974.gif], e.g. aminoguanidine: the other nitrogen atom being further doubly-bound to a…
C07D 213/56
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals: amides
C07D 217/06
With only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing…

Family

Application60/282,974Us provisional application · filed 10 Apr 2001
US 6,872,850 B2Related patent
US 2003/0199453 A1This patent

From the US filing history. Foreign family members aren’t listed.

Timeline

Citations

Open elsewhere

patentgrep

Loading patent…

Abstract

A compound having one of the following formulas:

50
or a derivative or salt thereof, wherein
R1 and R6 are independently selected from the group consisting of an alkyl and an aryl group;
R2 and R5 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group;
X is oxygen or H2N(HN)C(H)NN—;
and
m is at least one;
51
or a derivative or salt or salt thereof, wherein
R1 and R6 are independently selected from the group consisting of an alkyl and an aryl group;
R2 and R5 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl;
and
m is at least one;
52
or a derivative or salt or salt thereof , wherein
R1 and R2 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 and R4 are independently selected from the group consisting of an alkyl and an aryl group;
and
X is oxygen or H2N(HN)C(H)NN—;
53
or a derivative or salt or salt thereof, wherein
R1 and R4 are independently selected from the group consisting of an alkyl and an aryl group;
and
R2 and R3 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
54
or a derivative or salt or salt thereof, wherein
R1 and R5 are independently selected from the group consisting an aryl and an alkyl group;
R2 is hydrogen, an alkyl, or aryl group;
R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group;
X is oxygen or H2N(HN)C(H)NN—;
and
m is at least one;
55
or a derivative or salt or salt thereof, wherein
R1 and R6 are independently selected from the group consisting of an alkyl and an aryl group;
R3is hydrogen, an alkyl, or an aryl group;
R2, R4, and R5 are independently selected from the group consisting of hydrogen and an alkyl;
and
m is at least one;
or
56
or a derivative or salt or salt thereof, wherein
R1 and R2 are independently selected from the group consisting of hydrogen, an alkyl, and an aryl group;
R3 is an aryl group;
and
m is at least one.

45 more elements

Facts

Application

10/117,955Filed 8 Apr 2002

Priority

10 Apr 2001

Published

23 Oct 2003

Term ends

Not estimatedThe source records don’t support an estimate.

Classification6 codes

C07D 295/185
Radicals derived from carboxylic acids: from aliphatic carboxylic acids
C07C 281/18
Compounds containing any of the groups [IMAGE cpc-sch-C07C-0974.gif], e.g. aminoguanidine: the other nitrogen atom being further doubly-bound to a…
C07D 213/56
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals: amides
C07D 217/06
With only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing…