Patent US4377578A successfully refreshed from Google Patents.
US4377578A
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Piperazine derivatives
Assignee: Janssen Pharmaceutica NV
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Filing: 1981-07-24
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Granted: 1983-03-22
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Expires: 2001-07-24
Abstract
Abstract Novel 1-substituted 4-(diarylmethyl)piperazine derivatives having antianaphylactic and antihistaminic properties.
Inventors
- 👤 Jan Vandenberk
- 👤 Ludo E. J. Kennis
- 👤 Marcel J. M. C. Van der Aa
- 👤 Albert H. M. Th. Van Heertum
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 19:49
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/28; C07D213/30; C07C; C07C17/00; C07C17/093; C07C17/16; C07C45/00; C07C45/45; C07C45/46; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/40; C07D211/44; C07D211/46; C07D213/26; C07D213/44; C07D213/46; C07D213/50; C07D235/00; C07D235/02; C07D235/04; C07D235/06; C07D235/08; C07D235/18; C07D235/24; C07D235/26; C07D235/28; C07D295/00; C07D295/04; C07D295/06; C07D295/073; C07D295/12; C07D295/125; C07D295/13
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
174 words
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 1 and Ar 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 n H 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 1 and R 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.
Claim 2
Dependent Claim
174 words
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 1 and Ar 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 n H 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 1 and R 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.
Claim 3
Dependent Claim
194 words
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 1 and Ar 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 n H 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 1 and R 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.
Claim 4
Dependent Claim
194 words
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 1 and Ar 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 n H 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 1 and R 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.
Claim 5
Independent Claim
209 words
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 1 and Ar 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 n H 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 1 and R 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.
Claim 6
Independent Claim
209 words
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 1 and Ar 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 n H 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 1 and R 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.
Claim 7
Independent Claim
50 words
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.
Claim 8
Independent Claim
50 words
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.
Claim 9
Independent Claim
50 words
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-benzimidazole and the pharmaceutically acceptable acid addition salts thereof.
Claim 10
Independent Claim
50 words
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-benzimidazole and the pharmaceutically acceptable acid addition salts thereof.
Claim 11
Independent Claim
50 words
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.
Claim 12
Independent Claim
50 words
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.
References Cited (Backward Citations)
US3362956A
Cited
US3472854A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1986-03-21 | 1986-09-20 | 1987-03-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-03-21 | 1990-09-20 | 1991-03-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-03-21 | 1994-09-20 | 1995-03-22 | $7700.00 | Window Closed / Lapsed |