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Last Updated: March 29, 2024

Claims for Patent: 4,238,485


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Summary for Patent: 4,238,485
Title: Novel pharmaceutical compositions
Abstract:Compositions containing substituted 1,2,5-thiadiazole .beta.-blocking agent and pyrazine and/or thiazide diuretic, and a method of treating hypertensive animals are disclosed.
Inventor(s): Sweet; Charles S. (Lansdale, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:06/088,900
Patent Claims: 1. Composition useful for treating hypertension comprising:

(A) .beta.-blocking agent selected from:

(i) compounds having the formula ##STR4## wherein R is morpholino or piperidino and R' is C.sub.3 -C.sub.6 alkyl, (ii) non-toxic pharmaceutically acceptable salts of (i); and

(iii) mixtures containing (i) and (ii); and

(B) diuretic selected from a 1,2,4 benzothiadiazine and

a pharmaceutically acceptable salt thereof

wherein the weight ratio of (A.):(B.) is about 1:1 to about 1:10.

2. A composition of claim 1 wherein said thiazide is selected from chlorothiazide, alkali metal salts of chlorothiazide, and hydrochlorothiazide.

3. A composition of claim 2 wherein R is morpholino or piperidino and R' is isopropyl or t-butyl.

4. Composition of claim 3 wherein R is morpholino.

5. Composition of claim 4 wherein said diuretic is hydrochlorothiazide.

6. Composition of claim 5 wherein R' is t-butyl.

7. Composition of claim 6 wherein said .beta.-blocking agent is said (ii) salt of the (i) (-) isomer.

8. Composition of claim 7 wherein said (ii) is the hydrogen maleate.

9. Composition of claim 8 wherein said ratio range 1:1.25-1:5.

10. Composition of claim 8 in tablet form containing 5 or 10 mg of (A.) and 10, 25 or 50 mg of (B.).

11. Composition of claim 8 in tablet form containing 10 mg of (A.) and 25 mg of (B.).

12. The composition of claim 1 wherein said 1,2,4 benzothiadazine is flumethiazide, benzthiazide, cyclopenthiazide, cyclothiazide, trichloromethiazide, benzhydroflumethiazide, methylcyclothiazide, polythiazide, thiabutazide, hydrochlorothiazide, chlorothiazide or a pharmaceutically acceptable salt thereof.

13. A method of treating a hypertensive animal to reduce blood pressure which comprises administration of a blood pressure reducing amount of a composition of claim 1.

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