GB2144410A - Therapeutic application of an imidazo (2,1a) isoindole derivative - Google Patents
Therapeutic application of an imidazo (2,1a) isoindole derivative Download PDFInfo
- Publication number
- GB2144410A GB2144410A GB08408819A GB8408819A GB2144410A GB 2144410 A GB2144410 A GB 2144410A GB 08408819 A GB08408819 A GB 08408819A GB 8408819 A GB8408819 A GB 8408819A GB 2144410 A GB2144410 A GB 2144410A
- Authority
- GB
- United Kingdom
- Prior art keywords
- imidazo
- therapeutic application
- effects
- evaluation
- mazindol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 230000001225 therapeutic effect Effects 0.000 title claims abstract description 5
- YNFXWRMIKILVHC-UHFFFAOYSA-N 3h-imidazo[2,1-a]isoindole Chemical class C1=CC=CC2=C3N=CCN3C=C21 YNFXWRMIKILVHC-UHFFFAOYSA-N 0.000 title 1
- 208000018737 Parkinson disease Diseases 0.000 claims abstract description 7
- DPFXKTGLDWZZBP-UHFFFAOYSA-N 4-(4-chlorophenyl)imidazolidine Chemical compound C1=CC(Cl)=CC=C1C1NCNC1 DPFXKTGLDWZZBP-UHFFFAOYSA-N 0.000 claims description 2
- ZPXSCAKFGYXMGA-UHFFFAOYSA-N Mazindol Chemical compound N12CCN=C2C2=CC=CC=C2C1(O)C1=CC=C(Cl)C=C1 ZPXSCAKFGYXMGA-UHFFFAOYSA-N 0.000 abstract description 9
- 229960000299 mazindol Drugs 0.000 abstract description 8
- 230000000694 effects Effects 0.000 description 11
- 238000011156 evaluation Methods 0.000 description 11
- 150000001875 compounds Chemical class 0.000 description 3
- 239000000902 placebo Substances 0.000 description 3
- 229940068196 placebo Drugs 0.000 description 3
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 description 2
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 description 2
- 206010034010 Parkinsonism Diseases 0.000 description 2
- 238000010586 diagram Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 230000001788 irregular Effects 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 208000008589 Obesity Diseases 0.000 description 1
- 208000027089 Parkinsonian disease Diseases 0.000 description 1
- 230000000578 anorexic effect Effects 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000000378 dietary effect Effects 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 230000007717 exclusion Effects 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
Abstract
A new therapeutic application of 5-(4-chlorophenyl)-5-hydroxy-2,5-dihydro-3H-imidazo (2,1-a)isoindole (known as "Mazindol") of formula <IMAGE> is in the treatment of the Parkinson's disease.o
Description
SPECIFICATION
Therapeutic application of mazindol
The present invention provides for a new therapeutic application of 5-(4-chlorophenyl)-2,5-dihydro-3Himidazol (2,1-a)iso-indol-5-ole (generally indicated as Mazindol), of formula I
for the treatment in the Parkinson's disease.
The Mazindol of formula lisa compound known in medical literature as being a central non-amphetaminic anoretic, presently used in the treatment of the exogenous obesity in association with dietetic restrictions. In these cases the drug is well tolerated, accompanied only by limited and slight side effects.
On the occasion of studies and experiments carried out recently by the Applicant, the compound of formula I surprisingly proved to be effective in the treatment of the Parkinson's disease. The tests were carried out on patients suffering from the Parkinson's disease, on whom the L-dopa therapy had irregular effects as well as a drop in effectiveness. The drug was experimentally administered to 16 patients over twelve months, according to the following criteria:
Admission criteria: patients suffering from Parkinson's disease and subjected to
L-Dopa therapy, which provoked a drop in effectiveness and the
setting in of irregular effects ("on-off" effects)
Exclusion criteria: the patients suffering from parkinsonisms of different nature
were not subjected to the tests.
Drug-administering diagram: 30 days Placebo
one week suspension
30 days Mazindol
Ways of administration: Random
Mazindol dosage: 2 mg
Evaluation of the effects: Webster scale - 2 basal evaluations;
one evaluation at the end of the first period;
one evalution at the end of the one-week suspension;
one evaluation at the end of the second period.
Evaluation of "on-off" effects if any;: the number and duration of the "on-off" effects was assessed and
the symptoms were evaluated according to a pre-established
scale.
The evaluation of the dosage-effect relation was effected over 24 months, on twelve patients suffering from initial Parkinson's disease. The patients suffering from any other Parkinson's syndrome were not subjected to the tests.
The tests were carried out as follows:
Drug-administration diagram: 30 days Placebo
30 days scalar dosages of 1-2-3-4 mg Mazindol
Evaluation of the effects: Webster scale: 2 basal evaluations;
one evaluation at the end of placebo;
one evaluation at the end of each 30 days period.
Evaluation of the appearance of side scale of the 'Centro del Sonno' of Bologna effects:
Mazindol was administered in scalar dosages (which were increased each month); the increase in dosage was suspended at the appearance of even the slightest side effects. From the carried out experiments there was proved the effectiveness of the treatment on all the tested patients, without the setting in of particular or new side effects other than those already known of the compound.
Claims (1)
1. A new therapeutic utilization of 5-(4-chlorophenyl)-2,5-di-hydro-3H-imidazol (2,1 -a)isoindol-5-ole of formula I
for the treatment of the Parkinson's disease.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT22370/83A IT1194359B (en) | 1983-08-01 | 1983-08-01 | THERAPEUTIC APPLICATION OF MAZINDOLO IN PARKINSON DISEASE |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GB8408819D0 GB8408819D0 (en) | 1984-05-16 |
| GB2144410A true GB2144410A (en) | 1985-03-06 |
Family
ID=11195337
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB08408819A Withdrawn GB2144410A (en) | 1983-08-01 | 1984-04-05 | Therapeutic application of an imidazo (2,1a) isoindole derivative |
Country Status (2)
| Country | Link |
|---|---|
| GB (1) | GB2144410A (en) |
| IT (1) | IT1194359B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2899476A1 (en) * | 2006-04-11 | 2007-10-12 | Assist Publ Hopitaux De Paris | ASSOCIATION OF MAZINDOL IN THE TREATMENT OF DEFICIT ATTENTION / HYPERACTIVITY |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1225412A (en) * | 1967-03-23 | 1971-03-17 |
-
1983
- 1983-08-01 IT IT22370/83A patent/IT1194359B/en active
-
1984
- 1984-04-05 GB GB08408819A patent/GB2144410A/en not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1225412A (en) * | 1967-03-23 | 1971-03-17 |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2899476A1 (en) * | 2006-04-11 | 2007-10-12 | Assist Publ Hopitaux De Paris | ASSOCIATION OF MAZINDOL IN THE TREATMENT OF DEFICIT ATTENTION / HYPERACTIVITY |
| WO2007116076A1 (en) * | 2006-04-11 | 2007-10-18 | Assistance Publique - Hopitaux De Paris | Mazindol combination in the treatment of attention deficit/hyperactivity |
| US8293779B2 (en) | 2006-04-11 | 2012-10-23 | Assistance Publique-Hopitaux De Paris | Mazindol combination in the treatment of attention deficit/hyperactivity |
| EP2564872A1 (en) * | 2006-04-11 | 2013-03-06 | Assistance Publique, Hopitaux De Paris | Combination of mazindol in the treatment of attention-deficit/hyperactivity disorder |
Also Published As
| Publication number | Publication date |
|---|---|
| GB8408819D0 (en) | 1984-05-16 |
| IT8322370A0 (en) | 1983-08-01 |
| IT1194359B (en) | 1988-09-22 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Birkmayer et al. | Implications of combined treatment with'Madopar'and L-deprenil in Parkinson's disease: a long-term study | |
| Mones et al. | Analysis of L-dopa induced dyskinesias in 51 patients with Parkinsonism | |
| RU94046311A (en) | Use of phosphonates and nonsteroid antiinflammatory medicinal agents for arthritis treatment, treatment method | |
| KR930702022A (en) | Treatment or prevention of type 1 diabetes by oral administration of insulin | |
| Joy et al. | Optic and peripheral neuritis: probable effect of prolonged chloramphenicol therapy | |
| CY1111088T1 (en) | PHARMACEUTICAL FORM FOR TOLTERODIN ADMINISTRATION WITH CONTROLLED LIBERTY | |
| PT980246E (en) | Therapy for constipation | |
| BR0009016A (en) | Composition of apomorphine and sildenafil | |
| ES2039262T3 (en) | USE OF ACETYL L-CARNITINE FOR THE PREPARATION OF A MEDICINE FOR THE THERAPEUTIC TREATMENT OF PERIPHERAL NEUROPATHIES. | |
| AU596296B2 (en) | Treatment of diabetes | |
| WO2002074318A1 (en) | Il-12 expression controlling agents | |
| US2761807A (en) | Glycocyamine and methylating agent in vivo creatine producing composition | |
| Shenker et al. | Treatment of Sydenham's chorea with haloperidol | |
| JP2872809B2 (en) | Pharmaceutical composition suitable for treating Parkinson's disease, comprising monosialoganglioside GM <1> or a derivative thereof | |
| IT1181682B (en) | USE OF ALCANOIL L-CARNITINE FOR THE THERAPEUTIC TREATMENT OF IDIOPATHIC OR INDUCED PARKINSONISM | |
| Okihiro et al. | Hypokalemic periodic paralysis: experimental precipitation with sodium liothyronine | |
| JPH08512311A (en) | Arsenic medicine for treating chronic fatigue syndrome | |
| PT891186E (en) | Nasal administration of agents for treatment of delayed onset emesis | |
| GB2144410A (en) | Therapeutic application of an imidazo (2,1a) isoindole derivative | |
| Bolding | Diethylpropion hydrochloride: an effective appetite suppressant. | |
| US4355029A (en) | Combination therapy for rheumatoid arthritis | |
| JPH0314812B2 (en) | ||
| Walter | Clinical impressions on treatment of obsessional states with intravenous clomipramine (Anafranil) | |
| Wurtman et al. | Dietary enhancement of CNS neurotransmitters | |
| ES2038847T3 (en) | PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION CONTAINING ZIDOVUDINE AND INOSIPLEX FOR THE TREATMENT OF AIDS AND RELATED SYNDROMES. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |