US4590180A
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Use of adenosine derivatives as psychopharmacological agents
Assignee: Merck Patent GmbH
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Filing: 1983-04-22
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Granted: 1986-05-20
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Expires: 2003-04-22
Abstract
Abstract Adenosine derivatives of formula I ##STR1## wherein X is F, Cl or Br and n is 1 or 2, and their physiologically acceptable acid addition salts, are valuable psychopharmacological agents.
Inventors
- 👤 Klaus Irmscher
- 👤 Rochus Jonas
- 👤 Jurgen Uhl
- 👤 Ernst Schorscher
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 19:54
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/16; A; A61; A61P; A61P25/00; A61P25/08
Claims Analysis
Total Claims: 37
Claim 1
Independent Claim
66 words
A method of achieving a CNS-depressant effect in a patient suffering from an indication which can be treated by achieving such an effect, which comprises administering to such a patient an amount of a compound of the formula ##STR3## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to achieve said CNS-depressant effect in the patient which relieves the indication.
Claim 2
Independent Claim
66 words
A method of achieving a CNS-depressant effect in a patient suffering from an indication which can be treated by achieving such an effect, which comprises administering to such a patient an amount of a compound of the formula ##STR3## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to achieve said CNS-depressant effect in the patient which relieves the indication.
Claim 3
Dependent Claim
23 words
A method of claim 1 wherein the amount of the compound administered is 0.2 to 20 mg/kg/day in unit doses of 10-1,000 mg.
Claim 4
Dependent Claim
10 words
A method of claim 2 wherein the administration is oral.
Claim 5
Dependent Claim
17 words
A method of claim 1 wherein the indication is a stress condition of endogenic or exogenic origin.
Claim 6
Dependent Claim
21 words
A method of claim 4 wherein the CNS-depressant effect is an anxiolytic, tranquilizing, anticonvulsive, muscle relaxing, sedative, anesthesia-potentiating or anesthesia-prolonging effect.
Claim 7
Dependent Claim
14 words
A method of claim 5 wherein the CNS depressant effect is an anxiolytic effect.
Claim 8
Dependent Claim
13 words
A method of claim 5 wherein the CNS-depressant effect is a tranquilizing effect.
Claim 9
Dependent Claim
13 words
A method of claim 5 wherein the CNS-depressant effect is an anticonvulsive effect.
Claim 10
Dependent Claim
14 words
A method of claim 5 wherein the CNS-depressant effect is a muscle relaxing effect.
Claim 11
Dependent Claim
37 words
A method of claim 5 wherein the indication is a stress condition with an attendant symptom of excitation, tension, anxiety, a psychoneurotic disorder, autonomic dystonia, a psychosomatic disorder, a sleep disorder, muscular tension, spasms or status epilepticus.
Claim 12
Dependent Claim
35 words
A method of claim 1 wherein the patient is not suffering from a condition which is treatable by administering a pharmaceutical which influences the transport of oxygen in the blood or affects the lipid metabolism.
Claim 13
Dependent Claim
17 words
A method of claim 11 wherein the patient is not suffering from angina pectoris, arteriosclerosis or hyperlipidemia.
Claim 14
Dependent Claim
15 words
A method of claim 8 which additionally comprises simultaneously administering a benzodiazepine having CNS-depressant activity.
Claim 15
Dependent Claim
56 words
A pharmaceutical composition consisting essentially of an amount of a benzodiazepine having CNS-depressant activity and an amount of an adenosine derivative of the formula ##STR4## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, these amounts together being effective to achieve anti-convulsant effects in a patient, and a pharmaceutically acceptable adjuvant.
Claim 16
Dependent Claim
56 words
A pharmaceutical composition consisting essentially of an amount of a benzodiazepine having CNS-depressant activity and an amount of an adenosine derivative of the formula ##STR4## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, these amounts together being effective to achieve anti-convulsant effects in a patient, and a pharmaceutically acceptable adjuvant.
Claim 17
Independent Claim
37 words
A method of potentiating the CNS-depressant activity of a benzodiazepine which comprises simultaneously administering a compound of the formula ##STR5## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, and a benzodiazepine.
Claim 18
Independent Claim
37 words
A method of potentiating the CNS-depressant activity of a benzodiazepine which comprises simultaneously administering a compound of the formula ##STR5## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, and a benzodiazepine.
Claim 19
Dependent Claim
57 words
A pharmaceutical composition consisting essentially of an amount of a compound of the formula ##STR6## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to potentiate the CNS-depressant activity of a benzodiazepine, and an amount of a benzodiazepine, the total amount of both ingredients being effective to achieve a CNS-depressant effect.
Claim 20
Dependent Claim
57 words
A pharmaceutical composition consisting essentially of an amount of a compound of the formula ##STR6## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to potentiate the CNS-depressant activity of a benzodiazepine, and an amount of a benzodiazepine, the total amount of both ingredients being effective to achieve a CNS-depressant effect.
Claim 21
Independent Claim
45 words
A method of achieving a psychopharmacological effect in a human patient comprising administering to the patient an amount of a compound of the formula ##STR7## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to achieve a psychopharmacological effect.
Claim 22
Independent Claim
45 words
A method of achieving a psychopharmacological effect in a human patient comprising administering to the patient an amount of a compound of the formula ##STR7## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to achieve a psychopharmacological effect.
Claim 23
Dependent Claim
13 words
A method of claim 5 wherein the CNS-depressant effect is a sedative effect.
Claim 24
Independent Claim
55 words
A method of increasing the number of benzodiazepine receptors in the brain of a patient comprising administering to the patient an amount of a compound of the formula ##STR8## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to increase the number of benzodiazepine receptors in the patient's brain.
Claim 25
Independent Claim
55 words
A method of increasing the number of benzodiazepine receptors in the brain of a patient comprising administering to the patient an amount of a compound of the formula ##STR8## wherein n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to increase the number of benzodiazepine receptors in the patient's brain.
Claim 26
Independent Claim
74 words
A method of achieving a CNS-depressant effect in a patient suffering from an indication which can be treated by achieving such an effect, which comprises administering to such a patient an amount of a compound of the formula ##STR9## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to achieve said CNS-depressant effect in the patient which relieves the indication.
Claim 27
Independent Claim
74 words
A method of achieving a CNS-depressant effect in a patient suffering from an indication which can be treated by achieving such an effect, which comprises administering to such a patient an amount of a compound of the formula ##STR9## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to achieve said CNS-depressant effect in the patient which relieves the indication.
Claim 28
Dependent Claim
64 words
A pharmaceutical composition consisting essentially of an amount of a benzodiazepine having CNS-depressant activity and an amount of an adenosine derivative of the formula ##STR10## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, these amounts together being effective to achieve anticonvulsant effects in a patient, and a pharmaceutically acceptable adjuvant.
Claim 29
Dependent Claim
64 words
A pharmaceutical composition consisting essentially of an amount of a benzodiazepine having CNS-depressant activity and an amount of an adenosine derivative of the formula ##STR10## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, these amounts together being effective to achieve anticonvulsant effects in a patient, and a pharmaceutically acceptable adjuvant.
Claim 30
Independent Claim
45 words
A method of potentiating the CNS-depressant activity of a benzodiazepine which comprises simultaneously administering a compound of the formula ##STR11## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, and a benzodiazepine.
Claim 31
Independent Claim
45 words
A method of potentiating the CNS-depressant activity of a benzodiazepine which comprises simultaneously administering a compound of the formula ##STR11## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, and a benzodiazepine.
Claim 32
Dependent Claim
65 words
A pharmaceutical composition consisting essentially of an amount of a compound of the formula ##STR12## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to potentiate the CNS-depressant activity of a benzodiazepine, and an amount of a benzodiazepine, the total amount of both ingredients being effective to achieve a CNS-depressant effect.
Claim 33
Dependent Claim
65 words
A pharmaceutical composition consisting essentially of an amount of a compound of the formula ##STR12## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to potentiate the CNS-depressant activity of a benzodiazepine, and an amount of a benzodiazepine, the total amount of both ingredients being effective to achieve a CNS-depressant effect.
Claim 34
Independent Claim
53 words
A method of achieving a psychopharmacological effect in a human patient comprising administering to the patient an amount of a compound of the formula ##STR13## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to achieve a psychopharmacological effect.
Claim 35
Independent Claim
53 words
A method of achieving a psychopharmacological effect in a human patient comprising administering to the patient an amount of a compound of the formula ##STR13## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to achieve a psychopharmacological effect.
Claim 36
Independent Claim
63 words
A method of increasing the number of benzodiazepine receptors in the brain of a patient comprising administering to the patient an amount of a compound of the formula ##STR14## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to increase the number of benzodiazepine receptors in the patient's brain.
Claim 37
Independent Claim
63 words
A method of increasing the number of benzodiazepine receptors in the brain of a patient comprising administering to the patient an amount of a compound of the formula ##STR14## wherein X is F, Br, o-Cl or m-Cl and n is 1 or 2 or a physiologically acceptable acid addition salt thereof, effective to increase the number of benzodiazepine receptors in the patient's brain.
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) | 1989-05-19 | 1989-11-18 | 1990-05-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-05-19 | 1993-11-18 | 1994-05-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-05-19 | 1997-11-18 | 1998-05-20 | $7700.00 | Window Closed / Lapsed |