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Details for Patent: 4,454,143

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Details for Patent: 4,454,143

Title: Tricyclic antihistamines
Abstract:Antihistamines of the formula ##STR1## wherein ##STR2## is a 5 or 6 membered ring which is phenyl or heterocyclic; ##STR3## is a six membered ring which is 2,3, or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is ##STR4## is a nitrogen containing ring, ##STR5## must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is ##STR6## wherein p is 1 or 2 and n is 1 or 2, R.sup.1 is C.sub.1 to C.sub.6 alkyl, R.sup.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, and the dotted line represents an optional double bond, R.sup.2 being absent if the double bond is present, and Y is substituted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.
Inventor(s): Villani; Frank J. (West Caldwell, NJ)
Assignee: Schering Corporation (Madison, NJ)
Filing Date:Jul 29, 1982
Application Number:06/403,274
Claims:1. A compound of the formula ##STR14## wherein ##STR15## is selected from the group consisting of 2- or 3-thiophene; ##STR16## is 2-, 3- or 4-pyridyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen or a hydroxy group as a substituent; W is ##STR17## wherein n is 1 or 2 and p is 1 or 2, R.sup.1 is C.sub.1 to C.sub.6 alkyl, R.sup.2 is hydrogen or C.sub.1 to C.sub.3 alkyl, and the dotted line represents an optional double bond, R.sup.2 being absent if the double bond is present, and Y is --COOR or --SO.sub.2 R, with the proviso that when Y is --COOR, R is C.sub.1 to C.sub.12 alkyl, substituted C.sub.1 to C.sub.12 alkyl, C.sub.2 to C.sub.12 alkenyl, substituted C.sub.2 to C.sub.12 alkenyl, phenyl, substituted phenyl, C.sub.7 to C.sub.10 phenylalkyl or C.sub.7 to C.sub.10 phenylalkyl wherein the phenyl moiety is substituted, or R is -2, -3, or -4 piperidyl or N-substituted piperidyl, wherein the substituents on said substituted C.sub.1 to C.sub.12 alkyl and on said substituted C.sub.2 to C.sub.12 alkenyl are selected from amino or substituted amino and the substituents on said substituted amino are selected from C.sub.1 to C.sub.6 alkyl, the substituents on said substituted phenyl and on said substituted phenyl moiety of the C.sub.7 to C.sub.10 phenylalkyl are selected from C.sub.1 to C.sub.4 alkyl and halo, and the substituent on said N-substituted piperidyl is C.sub.1 to C.sub.4 alkyl, and with the proviso that when Y is --SO.sub.2 R, R is C.sub.1 to C.sub.12 alkyl, C.sub.2 to C.sub.12 alkenyl, phenyl, substituted phenyl, C.sub.7 to C.sub.10 phenylalkyl, C.sub.7 to C.sub.10 phenylalkyl wherein the phenyl moiety is substituted, wherein the substituents on said substituted phenyl and said substituted phenyl moiety of the C.sub.7 to C.sub.10 phenylalkyl are selected from C.sub.1 to C.sub.4 alkyl and halo.

2. A compound according to claim 1 wherein W is ##STR18##

3. An anti-allergic pharmaceutical composition comprising an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

4. A method of effecting an anti-allergic response to an animal in need of such treatment comprising administering to the animal an effective amount of a compound as claimed in claim 1.
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