EP0205334A2
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EP
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Benzazepine derivatives
Assignee: ER Squibb and Sons LLC
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Filing: 1986-06-09
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Granted: —
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Expires: 2006-06-09
Abstract
Abstract Vasodilating activity is exhibited by new compounds having the formula and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 . R 4 . R 5 and n are as defined herein.
Inventors
- 👤 David M. Floyd
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-08 17:34
CPC Classifications
C; C07; C07D; C07D223/00; C07D223/14; C07D223/16; A; A61; A61P; A61P11/00; A61P9/00; A61P9/06; A61P9/08; A61P9/10; A61P9/12
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
166 words
A compound having the formula or a pharmaceutically acceptable salt thereof wherein R 1 is hydrogen, alkyl, alkanoyl, alkenyl, arylcarbonyl, heteroarylcarbonyl or R 2 and R 3 are each independently alkyl or cycloalkyl or R 2 and R 3 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl, or morpholinyl; R 4 and R 5 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, arylalkyl, hydroxy, alkanoyloxy, difluoromethoxy, trifluoromethyl, -NX 3 X 4 , -S(O) m alkyl, or -S(O) m aryl; n is 2 or 3; m is 0, 1 or 2; X 1 and X 2 are each independently hydrogen, alkyl, aryl or heteroaryl, or X 1 and X 2 together with the nitrogen atom to which they are attached are a nitrogen containing heteroaryl; X 3 and X 4 are each independently alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl, or carbamoyl; with the proviso that if R 4 is a 7-alkyl group, it must have a tertiary carbon atom bonded to the ring.
Claim 2
Dependent Claim
166 words
A compound having the formula or a pharmaceutically acceptable salt thereof wherein R 1 is hydrogen, alkyl, alkanoyl, alkenyl, arylcarbonyl, heteroarylcarbonyl or R 2 and R 3 are each independently alkyl or cycloalkyl or R 2 and R 3 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl, or morpholinyl; R 4 and R 5 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, arylalkyl, hydroxy, alkanoyloxy, difluoromethoxy, trifluoromethyl, -NX 3 X 4 , -S(O) m alkyl, or -S(O) m aryl; n is 2 or 3; m is 0, 1 or 2; X 1 and X 2 are each independently hydrogen, alkyl, aryl or heteroaryl, or X 1 and X 2 together with the nitrogen atom to which they are attached are a nitrogen containing heteroaryl; X 3 and X 4 are each independently alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl, or carbamoyl; with the proviso that if R 4 is a 7-alkyl group, it must have a tertiary carbon atom bonded to the ring.
Claim 3
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is hydrogen.
Claim 4
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is alkyl.
Claim 5
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is alkanoyl.
Claim 6
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 1 is acetyl.
Claim 7
Dependent Claim
14 words
A compound in accordance with claim 1 wherein R 1is alkenyl, arylcarbonyl. heteroarylcarbonyl or
Claim 10
Dependent Claim
21 words
A compound in accordance with any one of claims 1 to 6 wherein R 2 and R 3 are each alkyl.
Claim 11
Dependent Claim
21 words
A compound in accordance with any one or claims 1 to 6 wherein R 2 and R 3 are each methyl.
Claim 12
Dependent Claim
21 words
A compound in accordance with any one of claims 1 to 6 wherein R 2 and R 3 are each cycloalkyl.
Claim 13
Dependent Claim
33 words
A compound in accordance with any one of claims 1 to 6 wherein R 2 and R 3 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl.
Claim 14
Dependent Claim
17 words
A compound in accordance with any one of claims 1 to 10 wherein R 4 is hydrogen.
Claim 15
Dependent Claim
12 words
A compound in accordance with claim 1 wherein R 4 is halogen.
Claim 16
Dependent Claim
27 words
A compound in accordance with any one of claims 1 to 10 wherein R 4 is chlorine and is located in the 7-position of the benzazepine nucleus.
Claim 17
Dependent Claim
17 words
A compound in accordance with any one or claims 1 to 13 wherein R 5 is alkoxy.
Claim 18
Dependent Claim
32 words
A compound in accordance with any one of claims 1 to 13 wherein R 5 is methoxy and is located in the 4-position of the phenyl ring to which it is attached.
Claim 19
Dependent Claim
16 words
A compound in accordance with any one of claims 1 to 15 wherein n is 2.
Claim 20
Dependent Claim
16 words
A compound in accordance with any one of claims 1 to 15 wherein n is 3.
Claim 21
Dependent Claim
14 words
The compound in accordance with claim 1, (cis)-3-(acetyloxy)-7-chloro-l-[2-(dimethylamino)-ethyl]-1,3,4,5-tetrahydro-4-(4-methoxyphenyl)-2H-1-benzazepin-2-one, or a pharmaceutically acceptable salt thereof.
Claim 22
Dependent Claim
15 words
The compound in accordance with claim 1, (cis)-3-(acetyloxy)-I-[2-(dimethylamino)ethyl]-1,3,4,5-tetrahydro-4-(4-methoxyphenyl)-2H-1- benzazepin-2-one, or a pharmaceutically acceptable salt thereof.
Claim 23
Dependent Claim
15 words
The compound in accordance with claim 1, (trans)-3-(acetyloxy)-1-[2-(dimethylamino)ethyl]-1,3,4,5-tetrahydro-4-(4-methoxyphenyl)-2H-1- benzazepin-2-one, or a pharmaceutically acceptable salt thereof.
Claim 24
Dependent Claim
15 words
The compound in accordance with claim 1, (cis)-3-(acetyloxy)-1-[2-(dimethylamino)ethyl]-1, 3,4,5-tetrahydro-4-(4-methoxyphenyl)-7-(trifluoromethyl)-2H-1-benzazepin-2-one, or a pharmaceutically acceptable salt thereof.
Claim 25
Dependent Claim
15 words
The compound in accordance with claim 1, (cis)-3-(acetyloxy)-7-(methoxy)-1-[2-(dimethylamino)-ethyl]-1,3,4,5-tetrahydro-4-(4-methoxyphenyl) 2H-1-benzazepin-2-one, or a pharmaceutically acceptable salt thereof.
References Cited (Backward Citations)
No citation records indexed.
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