IP Library Granted Patent US 7,056,910
Granted Patent B2
US 7,056,910 · App. 10/432,732 · Granted Jun 6, 2006

1,4,5.6-tetrahydroimidazo[4,5-d]diazepine derivatives or salts thereof

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Quick Facts
Patent No.
US 7,056,910
App. No.
10/432,732
Granted
Jun 6, 2006
Kind
B2
Abstract

To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.

Claims (20)

1. A compound of formula (I) or a pharmaceutically acceptable salt thereof:

wherein the ring D represents phenylene or pyridinediyl; X and Y may be the same or different and each represents CH or N; and R 1 , R 2 and R 3 may be the same or different and each represents a hydrogen atom, a hydroxyl group, a halogen, or a lower alkyl.

2. The compound or its pharmaceutically acceptable salt according to claim 1 , wherein the ring D represents 1,4-phenylene, pyridine-2,5-diyl, or pyridine-3,6-diyl.

3. The compound or its pharmaceutically acceptable salt according to claim 2 , wherein X and Y each represents OH, and R 1 represents a hydrogen atom.

4. The compound or its pharmaceutically acceptable salt according to claim 3 , wherein the ring D represents 1,4-phenylene, and R 2 and R 3 each represents a hydrogen atom.

5. The compound or its pharmaceutically acceptable salt according to claim 1 , wherein the compound is

N-{4-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]phenyl}biphenyl-2-carboxamide,

N-{3-fluoro-4-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]phenyl}biphenyl-2-carboxamide,

2′-fluoro-N-{4-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]phenyl}biphenyl-2-carboxamide,

N-{5-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]-2-pyridyl}biphenyl-2-carboxamide,

N-{6-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]-3-pyridyl}biphenyl-2-carboxamide, or

N-{2-hydroxy-4-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]phenyl}biphenyl-2-carboxamide.

6. A composition comprising the compound or its pharmaceutically acceptable salt according to any one of claims 1 to 5 , and a pharmaceutical carrier or excipient.

7. A composition comprising a compound or its pharmaceutically acceptable salt, and a pharmaceutical carrier or excipient, wherein the compound is

N-{4-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]phenyl}biphenyl-2-carboxamide,

N-{3-fluoro-4-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]phenyl}biphenyl-2-carboxamide,

2′-fluoro-N-{4-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]phenyl}biphenyl-2-carboxamide,

N-{5-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]-2-pyridyl}biphenyl-2-carboxamide,

N-{6-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]-3-pyridyl}biphenyl-2-carboxamide, or

N-{2-hydroxy-4-[2-(2-pyridyl)-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine-6-carbonyl]phenyl}biphenyl-2-carboxamide.

Assignments (2)
CHANGE OF NAME Recorded Nov 16, 2005
From: YAMANOUCHI PHARMACEUTICAL CO., LTD.
To: ASTELLAS PHARMA INC.
Reel/Frame 016784/0361 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 27, 2003
From: KOSHIO, HIROYUKI; KAKEFUDA, AKIO; SATO, IPPEI; WAKAYAMA, RYUTARO; SANAGI, MASANAO
To: YAMANOUCHI PHARMACEUTICAL CO., LTD.
Reel/Frame 014435/0704 →