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Details for Patent: 4,560,688

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Details for Patent: 4,560,688

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 substiuted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.
Inventor(s): Villani; Frank J. (West Caldwell, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Filing Date:Feb 08, 1984
Application Number:06/578,381
Claims:1. A compound of the formula ##STR14## wherein ##STR15## is a 5 or 6 membered ring which is an aromatic nitrogen heterocycle exclusive of pyridine; ##STR16## is ortho-phenylene or halo-substituted ortho-phenylene; Z is a bond or an alkylene chain of up 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 substituted carboxylate or substituted sulfonyl.

2. A compound according to claim 1, wherein 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.

3. A compound according to claim 1, wherein Y is --COOR, wherein R is as defined in claim 27, A is a 6-membered ring said compound having a single bond between the two bridge carbons of the 7-membered ring.

4. A compound according to claim 1, wherein Y is --SO.sub.2 R, wherein R is as defined in claim 27, A is a 6-membered ring said compound having a single bond between the two bridge carbons of the 7-membered ring.

5. A compound according to claim 3, wherein ##STR18## represents an ortho-phenylene radical.

6. A compound according to claim 3, wherein ##STR19## represents ##STR20##

7. A compound according to claim 3, wherein ##STR21## represents ##STR22##

8. A compound according to claim 1, wherein ##STR23## represents an ortho-phenylene radical.

9. An anti-allergic pharmaceutical composition which comprises an effective amount of a compound as defined in claim 1 in combination with a pharmaceutically acceptable carrier.

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