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US4496558A Expired / Lapsed US ⏱️ 0.0 years remaining

Pharmaceutical compositions and methods for producing alpha antagonism

Assignee: SmithKline Beecham Corp
•
Filing: 1983-01-26
•
Granted: 1985-01-29
•
Expires: 2003-01-26
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Abstract

Abstract Pharmaceutical compositions and methods for producing alpha 2 antagonism utilize, as active ingredients, 6-halo-N-substituted 2,3,4,5-tetrahydro-1H-3-benzazepines. These compositions are particularly useful for lowering intraocular pressure and for the treatment of abnormal cardiovascular conditions such as, for example, congestive heart failure, angina pectoris and thrombosis. The compositions and compounds of this invention, also, produce a reduction in blood pressure in hypertensive subjects and are, therefore, useful as antihypertensive agents.

Inventors

  • 👤 Robert M. DeMarinis
  • 👤 Jacob P. Hieble
  • 👤 William D. Matthews

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 22:34
CPC Classifications
C; C07; C07D; C07D223/00; C07D223/14; C07D223/16

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 47 words
A pharmaceutical composition for product alpha 2 antagonism comprising a pharmaceutically acceptable carrier and a nontoxic, effective amount to produce said antagonism of a 3-benzazepine compound of the formula: ##STR3## in which: R is allyl; and X is halogen; or a pharmaceutically acceptable, acid addition salt thereof.
Claim 2
Dependent Claim 47 words
A pharmaceutical composition for product alpha 2 antagonism comprising a pharmaceutically acceptable carrier and a nontoxic, effective amount to produce said antagonism of a 3-benzazepine compound of the formula: ##STR3## in which: R is allyl; and X is halogen; or a pharmaceutically acceptable, acid addition salt thereof.
Claim 3
Dependent Claim 25 words
A pharmaceutical composition for producing antihypertensive activity comprising a pharmaceutically acceptable carrier and a nontoxic, antihypertensive effective amount of a 3-benzazepine compound of claim 1.
Claim 4
Dependent Claim 11 words
The pharmaceutical composition of claim 2 in which X is chloro.
Claim 5
Dependent Claim 17 words
The composition of claim 3 in which the compound is in the form of its hydrochloride salt.
Claim 6
Dependent Claim 11 words
The pharmaceutical composition of claim 1 in which X is chloro.
Claim 7
Dependent Claim 17 words
The composition of claim 5 in which the 3-benzazepine is in the form of its hydrochloride salt.
Claim 8
Independent Claim 54 words
A method of producing alpha 2 antagonist activity in a subject in need of such activity comprising administering to said subject a nontoxic amount sufficient to produce said activity of a 3-benzazepine compound of the formula: ##STR4## in which: R is allyl; and X is halogen; or a pharmaceutically acceptable, acid addition salt thereof.
Claim 9
Independent Claim 54 words
A method of producing alpha 2 antagonist activity in a subject in need of such activity comprising administering to said subject a nontoxic amount sufficient to produce said activity of a 3-benzazepine compound of the formula: ##STR4## in which: R is allyl; and X is halogen; or a pharmaceutically acceptable, acid addition salt thereof.
Claim 10
Dependent Claim 10 words
The method of claim 7 in which X is chloro.
Claim 11
Dependent Claim 17 words
The method of claim 8 in which the compound is in the form of its hydrochloride salt.
Claim 12
Dependent Claim 30 words
A method of producing antihypertensive activity in a hypertensive subject comprising administering to said subject a nontoxic amount sufficient to produce said activity of a 3-benzazepine compound of claim 7.
Claim 13
Dependent Claim 38 words
The method of claim 10 in which said compound is administered orally or parenterally in a nontoxic, antihypertensive amount selected from the range of about 50 mg. to 250 mg. administered from about 2 to 4 times daily.
Claim 14
Dependent Claim 10 words
The method of claim 10 in which X is chloro.
Claim 15
Dependent Claim 17 words
The method of claim 12 in which the compound is in the form of its hydrochloride salt.

References Cited (Backward Citations)

US2520264A Cited
GB1268243A Cited
US4233217A Cited
US3716639A Cited
US3752892A Cited
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US4265890A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-01-29 1988-07-30 1989-01-29 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-01-29 1992-07-30 1993-01-29 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-01-29 1996-07-30 1997-01-29 $7700.00 Window Closed / Lapsed

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