Pharmaceutical compositions and methods of treating hypertension

• US 4,029,801 A
• Filed: 04/02/1975
• Issued: 06/14/1977
• Est. Priority Date: 09/03/1970
• Status: Expired due to Term

• Current Assignee: John Wyeth & Brother Limited (Pfizer Inc.)
• Original Assignee: John Wyeth & Brother Limited (Pfizer Inc.)
• Inventors: Archibald, John Leheup, Cavalla, John Frederick
• Primary Examiner(s): Schenkman, Leonard
• Application Number:
  US05/564,508
• Time in Patent Office: 804 Days
• Field of Search: 424/267, 260/293.77
• US Class Current: 514/329
• CPC Class Codes: C07C 45/63 by introduction of halogen; by substitution of halogen atoms by other halogen atoms
• CPC Class Codes: C07C 49/813 polycyclic
• CPC Class Codes: C07D 211/58 attached in position 4
• CPC Class Codes: C07D 211/72 with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
• CPC Class Codes: C07D 213/75 Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• CPC Class Codes: C07D 333/16 by oxygen atoms
• CPC Class Codes: C07D 333/56 Radicals substituted by oxygen atoms

Abstract

Pharmaceutical compositions containing a group of heterocyclic compounds and their use in treatment of disorders and diseases of the cardiovascular system and/or in the treatment of superficial and deep allergic phenomena is described. These compounds used in the composition and/or methods are piperidine compounds linked by the nitrogen atom to a substituted or unsubstituted cycloalkyl, aryl or heterocyclic radical through the intermediary of a group selected from a lower-alkylene radical, a monoketo lower-alkylene radical or a hydroxy-lower-alkylene radical, or a bivalent radical of the formula --NH.CO.(CH₂)_n -- where n is 1, 2 or 3, ##STR1## or --0-(lower-alkylene)--. The piperidine ring is further substituted by an acylamino residue.

Claims

1. A pharmaceutical composition for use in the treatment of hypertension comprising dosage form of a non-toxic pharmaceutically acceptable solid carrier and an effective amount of a heterocyclic compound of general formula (Ia), ##STR27## wherein W is phenyl, mono-halophenyl, dihalophenyl, (lower)alkoxyphenyl, di(lower)alkoxyphenyl, tri(lower)alkoxyphenyl, (lower)alkylphenyl, di-(lower)alkylphenyl, hydroxyphenyl, dihydroxyphenyl, methylenedioxyphenyl, ethylenedioxyphenyl, lower alkanoylaminophenyl, nitrophenyl, aminophenyl, di-(loweralkyl)-aminophenyl or acetylaminohydroxyphenyl;

A is alkylene of 1-6 carbon atoms; and

R is phenyl, or a pharmaceutically acceptable acid addition salt thereof, said unit dosage being in the form of a powder, capsule or tablet.

2. A pharmaceutical composition of claim 1 in which said heterocyclic compound is:

##STR28## or a pharmaceutically acceptable acid addition salt thereof.

3. A pharmaceutical composition of claim 1 in which said heterocyclic compound is:

##STR29## or a pharmaceutically acceptable acid addition salt thereof.

4. A pharmaceutical composition of claim 1 in which said heterocyclic compound is:

##STR30## or a pharmaceutical acceptable acid addition salt thereof.

5. A pharmaceutical composition of claim 1 in which said heterocyclic compound is:

##STR31## or a pharmaceutical acceptable acid addition salt thereof.

6. A pharmaceutical composition of claim 1 in which said heterocyclic compound is:

##STR32## or a pharmaceutically acceptable acid addition salt thereof.

7. A pharmaceutical composition of claim 1 in which said heterocyclic compound is:

##STR33## or a pharmaceutically acceptable acid addition salt thereof.

8. A pharmaceutical composition of claim 1 in which said heterocyclic compound is:

##STR34## or a pharmaceutically acceptable acid addition salt thereof.

9. A method for the treatment of hypertension in a mammal which comprises administering to said mammal a therapeutically effective amount of a heterocyclic compound of general formula (Ia) ##STR35## wherein W is phenyl, mono-halophenyl, dihalophenyl, lower alkoxyphenl, di(lower)alkoxyphenyl, tri(lower) alkoxyphenyl, (lower)alkylphenyl, di-(lower)alkylphenyl, hydroxyphenyl, dihydroxyphenyl, methylenedioxyphenyl, ethylenedioxyphenyl, lower alkanoylaminophenyl, nitrophenyl, aminophenyl, di-(loweralkyl)-aminophenyl or acetylaminohydroxyphenyl;

A is alkylene of 1-6 carbon atoms; and

R is phenyl, or a pharmaceutically acceptable acid addition salt thereof.

10. A method of claim 9 in which said heterocyclic compound administered is:

##STR36## or a pharmaceutically acceptable acid addition salt thereof.

11. A method of claim 9 in which said heterocyclic compound administered ##STR37##

12. A method of claim 9 in which said heterocyclic compound administered is:

##STR38##

13. A method of claim 9 in which said heterocyclic compound administered is:

##STR39##

14. A method of claim 9 in which said heterocyclic compound administered is:

##STR40##

15. A method of claim 9 in which said heterocyclic compound administered is:

##STR41##

16. A method of claim 9 in which said heterocyclic administered is:

##STR42##