IP Library Granted Patent US 7,273,869
Granted Patent B2
US 7,273,869 · App. 10/510,066 · Granted Sep 25, 2007

Inhibitors of Akt activity

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Quick Facts
Patent No.
US 7,273,869
App. No.
10/510,066
Granted
Sep 25, 2007
Kind
B2
Abstract

The present invention is directed to compounds comprising a ring-fused quinoxalinyl moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention

Claims (34)

1. The TFA salt of a compound which is selected from:

1-{1-[4-(7-phenyl-1H-imidazo[4,5-g]quinoxalin-6-yl)benzyl]piperidin-4-yl}-1,3-dihydro-2H-benzimidazol-2-one;

N,N-dimethyl-1-[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methanamine;

1-{1-[4-(3-phenylbenzo[g]quinoxalin-2-yl)benzyl]piperidin-4-yl}-1,3-dihydro-2H-benzimidazol-2-one;

or a stereoisomer thereof.

2. A compound which is selected from:

1-{1-[4-(7-phenyl-1H-imidazo[4,5-g]quinoxalin-6-yl)benzyl]piperidin-4-yl}-1,3-dihydro-2H-benzimidazol-2-one;

N,N-dimethyl-1-[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methanamine;

1-{1-[4-(3-phenylbenzo[g]quinoxalin-2-yl)benzyl]piperidin-4-yl}-1,3-dihydro-2H-benzimidazol-2-one;

or a pharmaceutically acceptable salt or a stereoisomer thereof.

3. A pharmaceutical composition comprising a pharmaceutical carrier, and dispersed therein, a therapeutically effective amount of a compound of claim 2 .

4. A method for treating cancer which comprises administering to a mammal in need thereof a therapeutically effective amount of a compound of claim 2 .

5. A compound of the Formula A:

wherein:

n is 0, 1 or 2;

p is 0, 1, 2 or 3;

is selected from:

R 1 is independently selected from:

1) OH,

2) OC 1 -C 6 alkyl, and

3) C 1 -C 6 alkyl;

R 2 is independently selected from:

1) C 1 -C 6 alkyl,

2) OH,

3) OC 1 -C 6 alkyl,

4) CF 3 ,

5) CN, and

6) halogen;

R 3 and R 4 are: H;

R 5 and R 6 are independently selected from: H and C 1 -C 6 alkyl; or

R 5 and R 6 can be taken together with the nitrogen to which they are attached to form:

optionally substituted with Q;

Q is selected from:

or a pharmaceutically acceptable salt or a stereoisomer thereof.

Assignments (4)
CHANGE OF NAME Recorded Aug 29, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028866/0511 →
MERGER Recorded Aug 27, 2012
From: MERCK SHARP & DOHME CORP.
To: SCHERING CORPORATION
Reel/Frame 028850/0515 →
CHANGE OF NAME Recorded Jan 29, 2010
From: MERCK & CO., INC.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 023861/0910 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 26, 2007
From: LINDSLEY, CRAIG W.; ZHAO, ZHIJIAN
To: MERCK & CO., INC.
Reel/Frame 019635/0004 →