US4634705A
Expired / Lapsed
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Adrenergic amidines
Assignee: Abbott Laboratories
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Filing: 1986-03-07
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Granted: 1987-01-06
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Expires: 2006-03-07
Abstract
Abstract Disclosed herein are adrenergic compounds represented by the formula ##STR1## wherein m is 0, 1 or 2; R 1 , R 2 , R 3 and R 7 are taken from the group consisting of hydrogen, hydroxy, loweralkyl, loweralkoxy, halo, amino, acetamido or NHSO 2 R wherein R is taken from the group consisting of hydrogen or loweralkyl, provided that R 1 , R 2 , R 3 and R 7 cannot simultaneously be hydrogen or halo, and provided that when one of R 1 , R 2 , R 3 and R 7 is halo, the others cannot simultaneously be hydrogen and when two of R 1 , R 2 , R 3 and R 7 are halo, the other two cannot simultaneously be hydrogen and provided that R 1 and R 7 cannot simultaneously be methoxy each when R 2 and R 3 are hydrogen; R 1 and R 2 or R 2 and R 3 or R 3 and R 7 taken together can form a methylenedioxy or ethylenedioxy bridge; or R 1 and R 2 or R 2 and R 3 or R 3 and R 7 taken together with the aromatic ring can form a benzimidazole or indole bridge; and R 4 and R 5 are hydrogen or taken together form a closed ring of the formula ##STR2## wherein n is 1 or 2, and the combined solid and dashed line represents a single or double bond when n is 1, and R 6 is taken from the group consisting of hydrogen or loweralkyl, and the pharmaceutically acceptable salts thereof.
Inventors
- 👤 John F. DeBernardis
- 👤 Fatima Z. Basha
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 18:24
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/06; C07D233/00; C07D233/04; C07D233/20; C07D233/22; C07D239/24; C07D239/26
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
284 words
A compound of the formula ##STR5## wherein m is 0, 1 or 2; R 1 , R 2 , R 3 and R 7 are taken from the group consisting of hydrogen, hydroxy, loweralkyl, loweralkoxy, halo, amino, acetamido or NHSO 2 R wherein R is taken from the group consisting of hydrogen or loweralkyl, provided that R 1 , R 2 , R 3 and R 7 cannot simultaneously be hydrogen or halo, and provided that when one of R 1 , R 2 , R 3 and R 7 is halo, the others cannot simultaneously be hydrogen and when two of R 1 , R 2 , R 3 and R 7 are halo, the other two cannot simultaneously be hydrogen and when three of R 1 , R 2 , R 3 and R 7 are halo, the other cannot simultaneously be hydrogen, and provided that R 1 and R 7 cannot simultaneously be methoxy each when R 2 and R 3 are hydrogen; R 1 and R 2 or R 2 and R 3 or R 3 and R 7 taken together can form a methylenedioxy or ethylenedioxy ring, or R 1 and R 2 or R 2 and R 3 or R 3 and R 7 taken together with the aromatic ring can form a benzimidazole or indole ring; and R 4 and R 5 are hydrogen or taken together form a closed ring of the formula ##STR6## wherein n is 1 or 2, and the combined solid and dashed line represents a single or double bond when n is 1, and R 6 is taken from the group consisting of hydrogen or loweralkyl, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
284 words
A compound of the formula ##STR5## wherein m is 0, 1 or 2; R 1 , R 2 , R 3 and R 7 are taken from the group consisting of hydrogen, hydroxy, loweralkyl, loweralkoxy, halo, amino, acetamido or NHSO 2 R wherein R is taken from the group consisting of hydrogen or loweralkyl, provided that R 1 , R 2 , R 3 and R 7 cannot simultaneously be hydrogen or halo, and provided that when one of R 1 , R 2 , R 3 and R 7 is halo, the others cannot simultaneously be hydrogen and when two of R 1 , R 2 , R 3 and R 7 are halo, the other two cannot simultaneously be hydrogen and when three of R 1 , R 2 , R 3 and R 7 are halo, the other cannot simultaneously be hydrogen, and provided that R 1 and R 7 cannot simultaneously be methoxy each when R 2 and R 3 are hydrogen; R 1 and R 2 or R 2 and R 3 or R 3 and R 7 taken together can form a methylenedioxy or ethylenedioxy ring, or R 1 and R 2 or R 2 and R 3 or R 3 and R 7 taken together with the aromatic ring can form a benzimidazole or indole ring; and R 4 and R 5 are hydrogen or taken together form a closed ring of the formula ##STR6## wherein n is 1 or 2, and the combined solid and dashed line represents a single or double bond when n is 1, and R 6 is taken from the group consisting of hydrogen or loweralkyl, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
15 words
The compound in accordance with claim 1 wherein m is 1 and n is 1.
Claim 4
Dependent Claim
15 words
The compound in accordance with claim 1 wherein m is 2 and n is 1.
Claim 5
Dependent Claim
15 words
The compound in accordance with claim 1 wherein m is 2 and n is 2.
Claim 6
Dependent Claim
16 words
The compound in accordance with claim 2 wherein R 1 and R 2 are each hydroxy.
Claim 7
Dependent Claim
16 words
The compound in accordance with claim 3 wherein R 1 and R 2 are each hydroxy.
Claim 8
Dependent Claim
16 words
The compound in accordance with claim 3 wherein R 1 and R 3 are each methoxy.
Claim 9
Dependent Claim
30 words
The compound in accordance with claim 2 wherein R 1 , R 2 , R 3 and R 7 are taken from the group consisting of hydrogen, hydroxy or methoxy.
Claim 10
Dependent Claim
21 words
The compound in accordance with claim 2 wherein R 1 and R 2 are taken together to form a methylenedioxy ring.
Claim 11
Dependent Claim
16 words
The compound in accordance with claim 2 wherein R 1 and R 2 are each hydroxy.
Claim 12
Dependent Claim
28 words
The compound in accordance with claim 2 wherein R 1 and R 2 taken together with the aromatic ring form a benzimidazole ring wherein R 6 is hydrogen.
Claim 13
Dependent Claim
30 words
The compound in accordance with claim 4 wherein R 1 , R 2 , R 3 and R 7 are taken from the group consisting of hydrogen, hydroxy or methoxy.
Claim 14
Dependent Claim
17 words
The compound in accordance with claim 4 wherein R 1 and R 2 form a methylenedioxy ring.
Claim 15
Dependent Claim
25 words
A composition with alpha-adrenergic activity in pharmaceutical dosage containing a carrier and a therapeutically effective amount of a compound of the formula of claim 1.
Claim 16
Dependent Claim
24 words
A method of treating hypertension which comprises administering to a patient a therapeutically effective amount of a compound of the formula of claim 1.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-01-05 | 1990-07-07 | 1991-01-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-01-05 | 1994-07-07 | 1995-01-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-01-05 | 1998-07-07 | 1999-01-06 | $7700.00 | Window Closed / Lapsed |