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Publication numberUS3699229 A
Publication typeGrant
Publication dateOct 17, 1972
Filing dateDec 18, 1970
Priority dateDec 18, 1970
Publication numberUS 3699229 A, US 3699229A, US-A-3699229, US3699229 A, US3699229A
InventorsNicholas Peter Plotnikoff
Original AssigneeAbbott Lab
Export CitationBiBTeX, EndNote, RefMan
External Links: USPTO, USPTO Assignment, Espacenet
2-oxo-5-phenyl-4-oxazolidinone as an anti-depressant agent
US 3699229 A
Covers a method of treating patients exhibiting symptoms of depression by administering to said patients a compound comprising 2-oxo-5-phenyl-4-oxazolidinone.
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Description  (OCR text may contain errors)

United States Patent Plotnikoff 51 Oct. 17, 1972 2-OXO-5-PHENYL-4-OXAZOLIDINONE [56] References Cited 0 AS AN PRE DE ss-ANT AGENT UNITED STATES PATENTS [72] Inventor: Nicholas Peter Plotnikoff, Village of r Lake Bl ff m 2,721,197 10/1955 'Sheehan ..260/ 239.l [73] Assignee: Abliott Laboratories, North a d, m s Friedman Chwago, Attorney-Robert L. Niblack [22] Filed: Dec. 18, 1970 [57] ABSTRACT [21] Appl. No.: 99,725

Covers a method of treating patients exhibiting symptoms of depression by administering to said patients a U-S- t on 2 xo 5 phenyl 4 0x [51 Int. Cl. ..A6lk 27/00 azolidinone. [58] Field of Search ..424/272; 260/307 C 4 Claims, No Drawings 2-OXO-5-PI'IENYL-4-OXAZOLIDINONE AS AN ANTI-DEPRESSANT AGENT BACKGROUND OF THE INVENTION Patients suffering from depression manifest one or more of a variety of symptoms. Generally speaking'a depressed patient feels incapable of dealing with his responsibilities. The predominate symptoms of depression are hypochondria, anoxeria, insomnia, anergia, an-

hedonia and pessimism. patients suffering from these symptoms are usually treated with anti-depressants. The present invention provides a method for treating patients exhibiting these symptoms of depression.

BRIEF SUMMARY OF THE INVENTION This invention relates to a method of treating patients exhibiting symptoms of depression. More particularly, it relates to a method of administering to said patients at least an effective dosage of a composition of 2-ox0-5-phenyl-4-oxazolidinone.

DETAILED DESCRIPTION OF THE INVENTION The just-mentioned'compound is known and its preparation disclosed, for example in US. Pat. No. 2,721,197. Its structure is as follows:

CsHs-CH C= The above compound can be administered orally or by injection. For the latter, solutions or suspensions may be prepared by slurrying l-l0 percent of compound in water containing 0.1-2.0 percent of carboxymethylcellulose. Suspensions may also be prepared by using 0.05-0.5 percent tragacanth solutions. For oral administration, tablets, pills, or capsules are easily prepared. Tablets may be prepared to contain between 5 and 25 mg. of the active material together with the usual tableting adjuvants, e.g., coloring agents, flavoring agents, diluents, lubricants, carriers and, if desired, dispersing agents or release retardants. The compound may also be combined with other active compounds such as tranquilizers.

The anti-depression agent disclosed here when administered to mammals such as humans is effective in a dosage range of from about 0.1 toabout 200 mg./kg. of body weight daily, either in single or divided dosages. More often the daily dosage range is 0.1- mgJkg.

This oxazolidinone compound also exhibits a sedative-tranquilizing activity.

EXAMPLE 1 One excellent way of testing the compounds for its anti-depressant activity is via the modified dopa-test described by G. M. Everett et al., Proc. lst lntJSymp.

' ing: when dl-dopa is given to untreated mice, no

Antidepressant Drugs, p. 164 (19661.

The above-modified dopa-test is based on the followresponse occurs because of the inactivation of the dopa by endogenous monoamine oxidase. However, if mice are pretreated with a monoamine oxidaseinhibitor, such as an oral administration of 40 ing/kg. of pargyline hydrochloride and then given 200 mg./kg. of dldopa orally, along with a known anti-depressant drug,

0 the mice show maximum motor reaction, violent activity umping and fighting.

TABLE I I Modified Dopa Oral Dose (mgJkgl) Test Rating 2S 1 slight activity 50 2 moderate activity 2 moderate activity 200 3 marked activity Eight hours after administration the activity of this compound was shown as follows:

TABLE II Modified Dopa Oral Dose (mg.(kg.) Test Rating 25 2 moderate activity 50 2 moderate activity 100 2 moderate activity What is claimed is:

1. A method of treating a patient exhibiting symptomsof depression comprising administering to said patient at least an anti-depressant effective dosage of a composition comprising 2-oxo-5-phenyl-4-oxazolidinone.

2. The method'of claim 1 wherein said dosage range is from about 0.1 to about 200 mg. /kg. of body weight daily.

3. The method of claim 2 wherein said dosage range is 0.1-20 mg./kg.

4. The method of claim 1 wherein said compound is administered in a unit dosage form in a pharmaceutically-acceptable carrier, said carrier comprising a major portion of said dosage form.

' Q a s I a a:

Patent Citations
Cited PatentFiling datePublication dateApplicantTitle
US2721197 *Jan 5, 1953Oct 18, 1955Bristol Lab IncBicyclic lactams
Referenced by
Citing PatentFiling datePublication dateApplicantTitle
US4332952 *Apr 23, 1981Jun 1, 1982Pfizer Inc.Hypoglycemic 5-substituted oxazolidine-2,4-diones
US4342771 *Apr 23, 1981Aug 3, 1982Pfizer Inc.Hypoglycemic 5-substituted oxazolidine-2,4-diones
US4367234 *Jan 2, 1981Jan 4, 1983Pfizer Inc.Hypoglycemic 5-substituted oxazolidine-2,4-diones
US4381308 *Mar 1, 1982Apr 26, 1983Pfizer Inc.Hypoglycemic 5-substituted oxazolidine-2,4-diones
US4407811 *Mar 1, 1982Oct 4, 1983Pfizer Inc.Hypoglycemic 5-substituted oxazolidine-2,4-diones
US4431810 *May 20, 1982Feb 14, 1984Pfizer Inc.Intermediates for the preparation of 5-substituted oxazolidine-2,4-diones
US4565820 *Jan 26, 1984Jan 21, 1986Pfizer Inc.Hypoglycemic 5-pyrrolyl, indolyl and quinolyl substituted oxazolidine-2,4-diones and their use
US4689336 *Oct 3, 1985Aug 25, 1987Pfizer Inc.Hypoglycemic 5-substituted oxazolidine 2,4-diones
US4753956 *May 28, 1987Jun 28, 1988Pfizer Inc.Hypoglycemic 5-substituted oxazolidine-2,4-diones
US4812471 *Feb 8, 1988Mar 14, 1989Pfizer Inc.Hypoglycemic 5-(isoxazolyl or isothiazolyl)-oxazolidine-2,4-diones
DE3129275A1 *Jul 24, 1981Apr 22, 1982PfizerHypoglykaemische 5-substituierte oxazolidin-2,4-dione
DE3129309A1 *Jul 24, 1981Mar 18, 1982PfizerHypoglykaemische 5-substituierte oxazolidin-2,4-dione
EP0097453A2 *Jun 9, 1983Jan 4, 1984Pfizer Inc.Alicyclic substituted oxazolidine-2,4-diones having hypoglycemic activity
U.S. Classification514/376
International ClassificationC07D263/44
Cooperative ClassificationC07D263/44
European ClassificationC07D263/44