IP Library › Granted Patent US 8,138,353
Granted Patent B2
US 8,138,353 · App. 12/830,962 · Granted Mar 20, 2012

Synthesis of UDP-glucose:

Assignee: Genzyme Corporation
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,138,353
App. No.
12/830,962
Granted
Mar 20, 2012
Kind
B2
Abstract

Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Claims (14)

1. A compound represented by the following structural formula:

the enantiomer of the compound, a salt of the compound, or a salt of the enantiomer, wherein:

R 1 is a substituted or unsubstituted aromatic group;

R 2 and R 3 are independently —H, a substituted or unsubstituted aliphatic group or, taken together with the nitrogen atom to which they are bonded, are a substituted or unsubstituted non-aromatic heterocyclic ring;

R 4 is O or H 2 ; and

R 5 is a substituted or unsubstituted aromatic group.

2. The compound of claim 1 wherein:

R 1 and R 5 are independently a substituted or unsubstituted phenyl group; and

R 2 and R 3 are independently —H, an unsubstituted C1-C5 alkyl group or, taken together with the nitrogen atom to which they are bonded, are an unsubstituted C3-C10 non-aromatic heterocyclic ring.

3. The compound of claim 2 wherein R 5 is a phenyl group.

4. The compound of claim 3 wherein R 2 and R 3 taken together with the nitrogen atom to which they are bonded, are pyrrolidinyl, piperazinyl, azetidinyl, morpholinyl, thiomorpholinyl, azacycloheptyl, piperidinyl or N-phenylpiperazinyl.

5. A compound represented by the following structural formula:

the enantiomer of the compound, a salt of the compound, or a salt of the enantiomer, wherein R 1 is a substituted or unsubstituted phenyl group and R 4 is H 2 or O.

6. The compound of claim 5 wherein the phenyl group represented by R 1 is substituted with —OCH 2 O—, —OCH 2 CH 2 O—, halo, —O(lower alkyl), —OH, lower alkyl thiol, —O(phenyl), —OCH 2 (phenyl), —O—CH 2 — (phenyl), lower alkyl, amino, lower alkyl amino or lower dialkyl amino.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 17, 2011
From: HIRTH, BRADFORD H.; SIEGEL, CRAIG
To: GENZYME CORPORATION
Reel/Frame 026289/0779 →
Continuity (5)
Continuation 11895632 · Aug 24, 2007
Division 10916824 · Aug 12, 2004
Division 10197227 · Jul 16, 2002
Provisional Application 60305814 · Jul 16, 2001
Related Publication 20110003987A1 · Jan 6, 2011