US4372974A
Expired / Lapsed
US
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Anticonvulsive compositions and method of treating convulsive disorders
Assignee: New York University
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Filing: 1981-06-02
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Granted: 1983-02-08
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Expires: 2001-06-02
Abstract
Abstract An orally administered pharmaceutical formulation comprising a solid dosage form containing an aliphatic amino acid compound in which the carboxylic acid and primary amine are separated by three or four units. Administered in an acid pH range, the formulation is useful in the treatment of convulsive disorders and also has anxiolytic and sedative properties.
Inventors
- 👤 Irving Fish
- 👤 Stephen A. Schwartz
- 👤 Stanley Samuels
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 10:38
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/16; A61K31/185; A61K31/19; A61K31/195
Claims Analysis
Total Claims: 44
Claim 1
Independent Claim
159 words
A method for controlling seizures in a mammal in need of such treatment which comprises administering to said mammal prior to the onset of a seizure a composition comprising a solid oral dosage form, said oral dosage form containing a pharmaceutical formulation comprising an effective amount for controlling seizures of a member selected from the group consisting of compounds having the general formula ##STR9## wherein R 1 is H, ##STR10## A is H, CH 3 , CH 3 CH 2 --, HO-CH 2 , HO-CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom and acid addition salts of such compounds, said formulation having a pH between about 1.8 and 6.0.
Claim 2
Independent Claim
159 words
A method for controlling seizures in a mammal in need of such treatment which comprises administering to said mammal prior to the onset of a seizure a composition comprising a solid oral dosage form, said oral dosage form containing a pharmaceutical formulation comprising an effective amount for controlling seizures of a member selected from the group consisting of compounds having the general formula ##STR9## wherein R 1 is H, ##STR10## A is H, CH 3 , CH 3 CH 2 --, HO-CH 2 , HO-CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom and acid addition salts of such compounds, said formulation having a pH between about 1.8 and 6.0.
Claim 3
Dependent Claim
15 words
The method of claim 1 which comprises administering a compound wherein n=0 to said mammal.
Claim 4
Dependent Claim
15 words
The method of claim 1 which comprises administering a compound wherein n=1 to said mammal.
Claim 5
Dependent Claim
19 words
The method as recited in claim 1 which comprises administering said compound substantially before the onset of a seizure.
Claim 6
Dependent Claim
12 words
The method of claim 4 wherein said compound is delta aminovaleric acid.
Claim 7
Dependent Claim
12 words
The method of claim 4 wherein said compound is delta aminovaleric acid.HCl.
Claim 8
Dependent Claim
12 words
The method of claim 4 wherein said compound is delta aminolevulinic acid.
Claim 9
Dependent Claim
24 words
The method of claim 4 which comprises administering said compound to said mammal at least 30 minutes prior to the onset of a seizure.
Claim 10
Dependent Claim
17 words
The method as recited in claim 6 wherein said pharmaceutical formulation has a pH of about 2.0.
Claim 11
Dependent Claim
27 words
The method of claim 4 wherein said oral dosage form is selected from the group consisting of a tablet, a pill, a compressed tablet and a capsule.
Claim 12
Dependent Claim
24 words
The method of claim 10 wherein said effective amount comprises from about 3.5 to about 4680 milligrams per kilogram of body weight per day.
Claim 13
Dependent Claim
26 words
The method as recited in claim 6 wherein said effective amount comprises from about 50 to about 200 milligrams per kilogram of body weight per day.
Claim 14
Dependent Claim
19 words
The method of claim 4 wherein said composition comprises an inert pharmaceutically acceptable carrier in combination with said compound.
Claim 15
Dependent Claim
28 words
The method of claim 4 wherein said pharmaceutical formulation comprises an optional acidifying agent to bring the pH of said formulation between about pH 1.8 and pH 6.0.
Claim 16
Independent Claim
167 words
A method of inhibiting epileptic seizures in a patient afflicted with epilepsy which comprises administering to a patient in need of such treatment and prior to the onset of said epileptic seizure a composition comprising a coated solid dosage form, said solid dosage form comprising a pharmaceutical formulation including an effective amount for inhibiting seizures of a member selected from the group consisting of compounds having the general formula ##STR11## wherein R 1 is H, ##STR12## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom and acid addition salts of said compounds, said formulation having a pH between about pH 1.8 and pH 6.0.
Claim 17
Independent Claim
167 words
A method of inhibiting epileptic seizures in a patient afflicted with epilepsy which comprises administering to a patient in need of such treatment and prior to the onset of said epileptic seizure a composition comprising a coated solid dosage form, said solid dosage form comprising a pharmaceutical formulation including an effective amount for inhibiting seizures of a member selected from the group consisting of compounds having the general formula ##STR11## wherein R 1 is H, ##STR12## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom and acid addition salts of said compounds, said formulation having a pH between about pH 1.8 and pH 6.0.
Claim 18
Independent Claim
139 words
A method of sedating a mammal which comprises orally administering to said mammal a composition comprising a coated solid dosage form comprising a pharmaceutical formulation containing a member selected from the group consisting of compounds having the general formula ##STR13## wherein R 1 is H, ##STR14## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom, and acid addition salts of said compounds, and said formulation having a pH in the range pH 1.8 to pH 6.0.
Claim 19
Independent Claim
139 words
A method of sedating a mammal which comprises orally administering to said mammal a composition comprising a coated solid dosage form comprising a pharmaceutical formulation containing a member selected from the group consisting of compounds having the general formula ##STR13## wherein R 1 is H, ##STR14## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom, and acid addition salts of said compounds, and said formulation having a pH in the range pH 1.8 to pH 6.0.
Claim 20
Independent Claim
145 words
A method of tranquilizing a mammal which comprises orally administering to said mammal a composition comprising a coated solid dosage form comprising a pharmaceutical formulation including an effective amount for tranquilizaton of a member selected from the group consisting of compounds of the general formula ##STR15## wherein R 1 is H, ##STR16## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom and acid addition salts of said compounds, and said formulation having a pH in the range pH 1.8 to pH 6.0.
Claim 21
Independent Claim
145 words
A method of tranquilizing a mammal which comprises orally administering to said mammal a composition comprising a coated solid dosage form comprising a pharmaceutical formulation including an effective amount for tranquilizaton of a member selected from the group consisting of compounds of the general formula ##STR15## wherein R 1 is H, ##STR16## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom and acid addition salts of said compounds, and said formulation having a pH in the range pH 1.8 to pH 6.0.
Claim 22
Dependent Claim
13 words
The method of claim 1 wherein said solid oral dosage form is coated.
Claim 23
Dependent Claim
116 words
A composition comprising a solid oral dosage form, containing a pharmaceutical formulation comprising an effective amount for controlling seizures in a mammal of a member selected from the group consisting of compounds having the general formula ##STR17## wherein R 1 is H, ##STR18## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0. said formulation having a pH between about pH 1.8 and pH 6.0.
Claim 24
Dependent Claim
116 words
A composition comprising a solid oral dosage form, containing a pharmaceutical formulation comprising an effective amount for controlling seizures in a mammal of a member selected from the group consisting of compounds having the general formula ##STR17## wherein R 1 is H, ##STR18## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 --HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0. said formulation having a pH between about pH 1.8 and pH 6.0.
Claim 25
Dependent Claim
7 words
The compound of claim 18 wherein n=0.
Claim 26
Dependent Claim
7 words
The compound of claim 18 wherein n=1.
Claim 27
Dependent Claim
28 words
The compound of claim 20 wherein R 1 is hydrogen or acyl, A is hydrogen or methoxy, Y is CH 2 or CH--OH and R 2 is hydroxy.
Claim 28
Dependent Claim
28 words
The compound of claim 21 wherein R 1 is hydrogen or acyl, A is hydrogen or methoxy, Y is CH--A, Z is CH--A and R 2 is OH.
Claim 29
Dependent Claim
12 words
The composition of claim 18 wherein said compound comprises delta aminovaleric acid.
Claim 30
Dependent Claim
18 words
The composition of claim 24 wherein said compound comprises an inorganic acid addition salt of delta aminovaleric acid.
Claim 31
Dependent Claim
19 words
The pharmaceutical formulation of claim 24 wherein said compound comprises an organic acid addition salt of delta aminovaleric acid.
Claim 32
Dependent Claim
12 words
The composition of claim 18 wherein said compound comprises delta aminolevulinic acid.
Claim 33
Dependent Claim
14 words
The composition of claim 25 wherein said oral dosage form comprises delta aminovaleric acid.HCl.
Claim 34
Dependent Claim
32 words
The composition of claim 24 or 27 wherein said solid form is a member selected from the group consisting of a tablet, a capsule, a pill, a beadlet and a compressed tablet.
Claim 35
Dependent Claim
26 words
The composition of claim 24 or 25 comprising an optional pharmaceutically acceptable buffering agent to bring said formulation to between about pH 1.8 and pH 6.0.
Claim 36
Dependent Claim
22 words
The pharmaceutical formulation of claim 25 or 26 wherein the pH of said formulation is between about pH 1.8 and pH 4.0.
Claim 37
Dependent Claim
17 words
The composition of claim 31 which comprises an inert pharmaceutically acceptable carrier in combination with said compound.
Claim 38
Dependent Claim
22 words
The pharmaceutical formulation of claim 25 or 26 wherein the pH of said formulation is between about pH 1.8 and pH 4.0.
Claim 39
Dependent Claim
149 words
A composition comprising a rectal suppository containing from about 5 at about 500 milligrams of a member selected from the group consisting of compounds having the general formula ##STR19## wherein R 1 is H, ##STR20## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 -- HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom, and acid addition salts of such compounds said composition having a pH between about pH 1.8 and 6.0, in a shapable base material having a melting point that will enable said suppository to melt slowly upon retention in the rectal cavity.
Claim 40
Dependent Claim
149 words
A composition comprising a rectal suppository containing from about 5 at about 500 milligrams of a member selected from the group consisting of compounds having the general formula ##STR19## wherein R 1 is H, ##STR20## A is H, CH 3 , CH 3 CH 2 --, HO--CH 2 , HO--CH 2 CH 2 , CH 3 OCH 2 -- HS--CH 2 --, HS--CH 2 CH 2 --, CH 3 SCH 2 --, Y is C═O, HC--OH or, CH--A, Z is CH--A, O, S; and R 2 is --OH, n is 1, and Y is CH--A when n=0; and A+Y+Z include no more than one Oxygen or Sulfur atom, and acid addition salts of such compounds said composition having a pH between about pH 1.8 and 6.0, in a shapable base material having a melting point that will enable said suppository to melt slowly upon retention in the rectal cavity.
Claim 41
Dependent Claim
14 words
The composition as described in a claim 34 wherein said compound is delta-aminovaleric acid.
Claim 42
Dependent Claim
13 words
The composition as described in claim 34 wherein said compound is delta-aminolevulinic acid.
Claim 43
Dependent Claim
12 words
The composition of claim 27 wherein said solid is in a suspension.
Claim 44
Dependent Claim
12 words
The composition of claim 19 comprising a coated solid oral dosage form.
References Cited (Backward Citations)
US3960927A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1986-02-07 | 1986-08-09 | 1987-02-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-02-07 | 1990-08-09 | 1991-02-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-02-07 | 1994-08-09 | 1995-02-08 | $7700.00 | Window Closed / Lapsed |