US5543430A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Method and formulation of stimulating nitric oxide synthesis
Assignee: Palmetto Pharmaceuticals LLC
•
Filing: 1994-10-05
•
Granted: 1996-08-06
•
Expires: 2014-10-05
Abstract
Abstract A therapeutic mixture comprising a mixture of L-arginine and an agonist of nitric oxide synthase, namely nitroglycerin, is disclosed for the treatment of diseases related to vasoconstriction, wherein the vasoconstriction is relieved by stimulating the constitutive form of nitric oxide synthase (cNOS) to produce native nitric oxide (NO). The native NO having superior beneficial effect when compared to exogenous NO produced by a L-arginine independent pathway in terms of the ability to reduce clinical endpoints and mortality.
Inventors
- 👤 W. H. Kaesemeyer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 06:37
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/21; A61K31/185; A61K31/19; A61K31/195; A61K31/33; A61K31/395; A61K31/495; A61K31/50; A61P; A61P43/00; A61P9/00; A61P9/08; A61P9/12
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
62 words
A method of treating a disease condition in a subject by vasodilation or vasorelaxation comprising: selecting a subject; mixing L-arginine and a venous dilator, said venous dilator being different than L-arginine; administering to said subject a formulation comprising said mixture; obtaining periodic indicators of vasorelaxations for the subject; and; continuing administration of the formulation until a desirable state of vasorelaxtion is obtained.
Claim 2
Independent Claim
62 words
A method of treating a disease condition in a subject by vasodilation or vasorelaxation comprising: selecting a subject; mixing L-arginine and a venous dilator, said venous dilator being different than L-arginine; administering to said subject a formulation comprising said mixture; obtaining periodic indicators of vasorelaxations for the subject; and; continuing administration of the formulation until a desirable state of vasorelaxtion is obtained.
Claim 3
Dependent Claim
23 words
The method of claim 1, wherein the formulation is administered intravenously, buccal, intracoronary, intramuscularly, topically, intranasally, rectally, sublingually, orally, subcutaneously, or by patch.
Claim 4
Dependent Claim
23 words
The method of claim 1, wherein said disease is hypertension, hypertensive heart disease, coronary heart disease, cardiovascular disease, cerebrovascular disease, and renovascular ischemia.
Claim 5
Dependent Claim
16 words
The method of claim 3, wherein said venous dilator is an exogenous source of nitric oxide.
Claim 6
Dependent Claim
14 words
The method of claim 4, wherein said exogenous source of nitric oxide is nitroglycerin.
Claim 7
Dependent Claim
35 words
The method of claim 4, wherein said exogenous source of nitric oxide is selected from the group consisting of sodium nitroprusside, nitrate esters, isoamylynitrite, SIN-1, cysteine, dithiothreitol, N-acetylcysteine, mercaptosuccinic acid, thiosalicylic acid, and methylthiosalicylic acid.
Claim 8
Dependent Claim
15 words
The method of claim 5, wherein L-arginine and nitroglycerin are administered at a therapuetic concentration.
Claim 9
Dependent Claim
19 words
The method of claim 7, wherein the therapuetic concentration of L-arginine is from 7.5% to about 30% w/v (g/ml).
Claim 10
Dependent Claim
19 words
The method of claim 7, wherein the therapuetic concentration of L-arginine is from 10% to about 15% w/v (g/ml).
Claim 11
Dependent Claim
15 words
The method of claim 7, wherein the therapuetic concentration of L-arginine is 10% w/v (g/ml).
Claim 12
Dependent Claim
20 words
The method of claim 7, wherein the therapeutic concentration of nitroglycerin is from about 0.2 μg/kg/minute to about 5 μg/kg/minute.
Claim 13
Dependent Claim
20 words
The method of claim 7, wherein the therapeutic concentration of nitroglycerin is from about 0.5 μg/kg/minute to about 3 μg/kg/minute.
Claim 14
Dependent Claim
20 words
The method of claim 7, wherein the therapeutic concentration of nitroglycerin is from about 0.75 μg/kg/minute to about 2 μg/kg/minute.
Claim 15
Dependent Claim
15 words
The method of claim 7, wherein the therapeutic concentration of nitroglycerin is about 1 μg/kg/minute.
Claim 16
Dependent Claim
17 words
The method of claim 7, wherein the pH is maintained within the range of 6 to 8.0.
Claim 17
Dependent Claim
17 words
The method of claim 7, wherein the pH is maintained within the range of 7 to 7.4.
Claim 18
Dependent Claim
21 words
A therapeutic mixture comprising a mixture of L-arginine and an agonist of nitric oxide synthase said agonist being different than L-arginine.
Claim 19
Dependent Claim
21 words
A therapeutic mixture comprising a mixture of L-arginine and an agonist of nitric oxide synthase said agonist being different than L-arginine.
Claim 20
Dependent Claim
11 words
The therapeutic mixture of claim 17, wherein the agonist is nitroglycerin.
Claim 21
Dependent Claim
44 words
The therapeutic mixture of claim 17, wherein the agonist is further comprised of a receptor mediated agonist selected from the group consisting of: acetylcholine, substance P, Histamine, arginine vasopressin, bradykinin, Adenosine Triphosphate, Prostaglandin F 2a , Oxytocin, Endothelium B, and the calcium ionophore A23187.
Claim 22
Independent Claim
52 words
A method of stimulating nitric oxide synthase to produce nitric oxide, said method comprising: mixing L-arginine and an agonist of nitric oxide synthase said agonist being different than L-arginine; administering the mixture to a subject having a nitric oxide synthase receptor site; and; stimulating said nitric oxide synthase to a desirable level.
Claim 23
Independent Claim
52 words
A method of stimulating nitric oxide synthase to produce nitric oxide, said method comprising: mixing L-arginine and an agonist of nitric oxide synthase said agonist being different than L-arginine; administering the mixture to a subject having a nitric oxide synthase receptor site; and; stimulating said nitric oxide synthase to a desirable level.
Claim 24
Dependent Claim
14 words
The method of claim 20, wherein said L-arginine is in excess to said agonist.
Claim 25
Dependent Claim
10 words
The method of claim 20, wherein the agonist is nitroglycerin.
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) | 1999-08-06 | 2000-02-05 | 2000-08-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2003-08-06 | 2004-02-05 | 2004-08-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2007-08-06 | 2008-02-05 | 2008-08-06 | $7700.00 | Window Closed / Lapsed |