Piperazine derivatives
AssigneeJanssen Pharmaceutica NV
InventorsJan Vandenberk, Ludo E. J. Kennis, Marcel J. M. C. Van der Aa, Albert H. M. Th. Van Heertum
Life of this patent
Estimating the term…
Abstract
Novel 1-substituted 4-(diarylmethyl)piperazine derivatives having antianaphylactic and antihistaminic properties.
Claims6
A chemical compound selected from the group consisting of a compound having the formula ##STR66## and the pharmaceutically acceptable acid addition salts thereof, wherein:
- Ar.sup.1 and Ar.sup.2 are each independently selected from the group consisting of phenyl, substituted phenyl and pyridinyl, wherein said substituted phenyl is phenyl having from 1 to 2 substituents independently selected from the group consisting of halo, lower alkyl, lower alkyloxy, trifluoromethyl and nitro;
- n is an integer of from 2 to 6 inclusive, provided that when C.sub.n H.sub.2n represents a branched alkylene chain, then at least 2 carbon atoms are present in the linear portion of the chain linking
- B with the piperazine nitrogen atom;
- and
- B is a radical having the formula ##STR67## wherein:
- R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, halo, lower alkyl and trifluoromethyl;
- and
- M is a member selected from the group consisting of phenyl, phenylmethyl, mercapto, lower alkylthio, amino, lower alkylcarbonylamino, lower alkyloxycarbonylamino, and cycloalkyl having from 3 to 6 carbon atoms.
A pharmaceutical composition comprising an inert carrier material and as an active ingredient an effective antihistaminic or anti-anaphylactic amount of a chemical compound selected from the group consisting of a compound having the formula ##STR68## and the pharmaceutically acceptable acid addition salts thereof, wherein:
- Ar.sup.1 and Ar.sup.2 are each independently selected from the group consisting of phenyl, substituted phenyl and pyridinyl, wherein said substituted phenyl is phenyl having from 1 to 2 substituents independently selected from the group consisting of halo, lower alkyl, lower alkyloxy, trifluoromethyl and nitro;
- n is an integer of from 2 to 6 inclusive, provided that when C.sub.n H.sub.2n represents a branched alkylene chain, then at least 2 carbon atoms are present in the linear portion of the chain linking B with the piperazine nitrogen atom;
- and
- B is a radical having the formula ##STR69## wherein:
- R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, halo, lower alkyl, and trifluoromethyl;
- and
- M is a member selected from the group consisting of phenyl, phenylmethyl, mercapto, lower alkylthio, amino, lower alkylcarbonylamino, lower alkyloxycarbonylamino, and cycloalkyl having from 3 to 6 carbon atoms.
A method of producing antihistaminic or anti-anaphylactic activity in a warm-blooded animal in need of same which comprises systemic administration to said warm-blooded animal of an effective antihistaminic or anti-anaphylactic amount of a chemical compound selected from the group consisting of a compound having the formula ##STR70## and the pharmaceutically acceptable acid addition salts thereof, wherein:
- Ar.sup.1 and Ar.sup.2 are each independently selected from the group consisting of phenyl, substituted phenyl and pyridinyl, wherein said substituted phenyl is phenyl having from 1 to 2 substitutents independently selected from the group consisting of halo, lower alkyl, lower alkyloxy, trifluoromethyl and nitro;
- n is an integer of from 2 to 6 inclusive, provided that when C.sub.n H.sub.2n represents a branched alkylene chain, then at least 2 carbon atoms are present in the linear portion of the chain linking B with the piperazine nitrogen atom;
- and B is a radical having the formula ##STR71## wherein:
- R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, halo, lower alkyl, and trifluoromethyl;
- and M is a member selected from the group consisting of hydrogen, lower alkyl, phenyl, phenylmethyl, mercapto, lower alkylthio, amino, lower alkylcarbonylamino, lower alkyloxycarbonylamino, and cycloalkyl having from 3 to 6 carbon atoms.
A method of producing antihistaminic or anti-anaphylactic activity in a warm-blooded animal in need of same which comprises systemic administration to said warm-blooded animal of an effective antihistaminic or anti-anaphylactic amount of a chemical compound selected from the group consisting of 1-{3-[4-(diphenylmethyl)-1-piperazinyl]propyl}-1H-benzimidazole and the pharmaceutically acceptable acid addition salts thereof.
A method of producing antihistaminic or anti-anaphylactic activity in a warm-blooded animal in need of same which comprises systemic administration to said warm-blooded animal of an effective antihistaminic or anti-anaphylactic amount of a chemical compound selected from the group consisting of 1-[4-{4-[(4-fluorophenyl)phenylmethyl]-1-piperazinyl}butyl]-1H-benzimidazo le and the pharmaceutically acceptable acid addition salts thereof.
A method of producing antihistaminic or anti-anaphylactic activity in a warm-blooded animal in need of same which comprises systemic administration to said warm-blooded animal of an effective antihistaminic or anti-anaphylactic amount of a chemical compound selected from the group consisting of 1-[4-{4-[bis(4-fluorophenyl)methyl]-1-piperazinyl}butyl]-1H-benzimidazole and the pharmaceutically acceptable acid addition salts thereof.
Dependencies are inferred from the claim text.