IP Library › Granted Patent US 8,778,931
Granted Patent B2
US 8,778,931 · App. 13/330,774 · Granted Jul 15, 2014

Substituted hydroxamic acids and uses thereof

Inventor: Alexandra E. Gould (Cambridge, MA)
Assignee: Millennium Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 8,778,931
App. No.
13/330,774
Granted
Jul 15, 2014
Kind
B2
Abstract

This invention provides compounds of formula (I) wherein R 1 , R 2 , X, p, q, m, n, and Ring C have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

Claims (41)

1. A compound of formula (IV):

wherein:

p is 0-3 and q is 1-4, and the total of p and q is 1-4;

R 9b is hydrogen, methyl, ethyl, isopropyl, or tert-butoxycarbonyl;

X is —C(O)—, —CH 2 —,

V 1 is a bond or —NH—C(O)—;

t is 0-2

Ring C is unsubstituted or substituted by 1-4 occurrences of R 5b ;

each occurrence of R 5b is independently chloro, fluoro, hydroxy, methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, —C(O)NH 2 , or —CO 2 H; and

z is 0 or 1.

2. The compound of claim 1 , wherein:

p is 0 and q is 1; or p is 1 and q is 1;or p is 0 and q is 2.

3. The compound of claim 1 , wherein z is 1;

Ring C is unsubstituted or substituted with one occurrence of R 5b ; and

R 5b is methyl.

4. The compound of claim 1 , represented by formula (V-a):

wherein R 5bb is hydrogen or methyl.

5. The compound of claim 4 , wherein:

R 9b is hydrogen, methyl, ethyl, or isopropyl.

6. The compound of claim 4 , wherein z is 1.

7. The compound of claim 4 , wherein R 5bb is methyl.

8. The compound of claim 4 , wherein:

X is —C(O)—, —CH 2 —,

9. The compound of claim 4 , wherein:

X is —C(O)—, —CH 2 —,

10. The compound of claim 1 , wherein the compound is:

N-hydroxy-2-[(4-methylpiperidin-4-yl)carbonyl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide,

2-[(1-ethyl-4-methylpiperidin-4-yl)carbonyl]-N-hydroxy-1,2,3,4-tetrahydroisoquinoline-6-carboxamide,

N-hydroxy-2-(4-piperidin-4-ylbenzyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide,

N-hydroxy-2-(4-{[(4-methylpiperidin-4-yl)carbonyl]amino}benzyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide,

tert-butyl 4-(4-{[6[(hydroxyamino)carbonyl]-3,4-dihydroisoquinolin-2(1H)-yl]methyl}phenyl)piperidine-1-carboxylate,

tert-butyl 4-{[(4-{[6-[(hydroxyamino)carbonyl]-3,4-dihydroisoquinolin-2(1H)-yl]methyl}phenyl)amino]carbonyl}-4-methylpiperidine-1-carboxylate,

N-hydroxy-2-(4-pyrrolidin-3-ylphenyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide,

N-hydroxy-2-[(6-{[(4-methylpiperidin-4-yl)carbonyl]amino}pyridin-3-yl)methyl]-2,3,4,5-tetrahydro-1H-2-benzazepine-7-carboxamide,

N-hydroxy-2-[(4-methylpiperidin-4-yl)methyl]isoindoline-5-carboxamide,

N-hydroxy-2-[2-(4-pyrrolidin-3 -ylphenyl)ethyl]-1,2,3,4-tetrahydroisoquinoline-7-carboxamide,

2-(2-{[(1-ethyl-4-methylpiperidin-4-yl)carbonyl]amino}pyridin-4-yl)-N-hydroxy-2,3,4,5-tetrahydro-1H-2-benzazepine-7-carboxamide,

N-hydroxy-2-[2-(4-piperidin-4-ylphenyl)ethyl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide,

tert-butyl 4-{[6[(hydroxyamino)carbonyl]-3,4-dihydroisoquinolin-2(1H)-yl]carbonyl}-4-methylpiperidine-1-carboxylate, or

a pharmaceutically acceptable salt thereof.

11. A pharmaceutical composition comprising a compound of claim l and a pharmaceutically acceptable carrier.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 30, 2012
From: GOULD, ALEXANDRA E.
To: MILLENNIUM PHARMACEUTICALS, INC.
Reel/Frame 027621/0130 →
Continuity (2)
Provisional Application 61426330 · Dec 22, 2010
Related Publication 20120165316A1 · Jun 28, 2012