IP Library Granted Patent US 6,872,827
Granted Patent B2
US 6,872,827 · App. 10/350,158 · Granted Mar 29, 2005

Somatostatin analogue compounds

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Quick Facts
Patent No.
US 6,872,827
App. No.
10/350,158
Granted
Mar 29, 2005
Kind
B2
Abstract

Compounds having somatostatin activity of the following Formula I, wherein, R 1 is aryl, substituted-aryl, and aryl-(lower-alkyl)-; R 2 is lower alkyl, amino substituted lower alkyl, -carboxy-(lower-alkyl), -carbamic acid-(lower-alkyl) and -carboxy-(lower-alkyl)-aryl; and R 3 and R 4 are independently, lower-alkyl, aryl, substituted-aryl, (substituted-aryl)-(lower-alkyl)-, heteroaryl, (heteroaryl)-(lower-alkyl)-, substituted-heteroaryl, (substituted heteroaryl)-(lower-alkyl)-, heterocyclic, heterocyclic-(lower-alkyl)-, substituted-heterocyclic, (substituted-heterocylic)-(lower alkyl)-, -carboxy-(lower-alkyl), and -carboxy-(lower-alkyl)-aryl; or a pharmaceutically acceptable, ester, ether, or salt thereof; methods for their use; and preparation.

Claims (22)

1. A compound of Formula I,

wherein,

R 1 is aryl, substituted-aryl, or aryl-(lower-alkyl)-;

R 2 is lower alkyl, amino substituted lower alkyl, -carboxy-(lower-alkyl), -carbamic acid-(lower-alkyl) or -carboxy-(lower-alkyl)-aryl; and

R 3 and R 4 are independently, lower-alkyl, or lower alkyl substituted with indole;

or a pharmaceutically acceptable, ester, ether, or salt thereof.

2. The compound of claim 1 , wherein R 1 is aryl.

3. The compound of claim 1 , wherein R 1 is substituted-aryl.

4. The compound of claim 1 , wherein R 1 is -(lower-alkyl)-aryl.

5. The compound of claim 1 , wherein R 3 is lower-alkyl, or lower alkyl substituted with indole.

6. The compound of claim 1 , wherein R 4 is lower-alkyl, or lower alkyl substituted with indole.

7. A compound of Formula II,

wherein,

R 1 is lower-alkyl, substituted lower-alkyl, aryl, substituted-aryl, aryl-(lower-alkyl)-, (substituted-aryl)-(lower-alkyl)-, heteroaryl, heteroaryl-(lower-alkyl)-, substituted-heteroaryl, (substituted-heteroaryl)-(lower-alkyl)-, heterocyclic, heterocyclic-(lower-alkyl)-, substituted heterocyclic, or (substituted-heterocyclic)-(lower-alkyl)-; and

R 3 and R 4 are independently, lower-alkyl or lower alkyl substituted with indole.

8. A compound of Formula III,

wherein,

R 2 is lower alkyl, amino substituted lower alkyl, lower-alkyl carbonyl, -carboxy-(lower-alkyl), or -carboxy-(lower-alkyl)-aryl; and

R 3 and R 4 are independently, lower-alkyl or lower alkyl substituted with indole.

9. A compound of Formula IV,

wherein,

R 3 and R 4 are independently, lower-alkyl or lower alkyl substituted with indole.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 24, 2009
From: CHEMBRIDGE RESEARCH LABORATORIES, INC.
To: CHEMBRIDGE CORPORATION
Reel/Frame 022584/0926 →
CHANGE OF NAME Recorded Feb 11, 2005
From: CHEMBRIDGE RESEARCH LABORATORIES LLC
To: CHEMBRIDGE RESEARCH LABORATORIES, INC.
Reel/Frame 015708/0083 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 7, 2003
From: WEBB, THOMAS; CHIANELLI, DONATELLA; KIM, YONG-CHUL
To: CHEMBRIDGE RESEARCH LABORATORIES
Reel/Frame 014247/0498 →