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Details for Patent: 6,951,938

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Details for Patent: 6,951,938

Title: Aryl fused azapolycyclic compounds
Abstract:Pharmaceutical compositions comprising compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein R.sup.1, R.sup.2, and R.sup.3 are defined as in the specification, in combination with another therapeutic agent and methods of using such combinations in the treatment of neurological and psychological disorders.
Inventor(s): Coe; Jotham Wadsworth (Niantic, CT), Brooks; Paige Roanne Palmer (North Stonington, CT)
Assignee: Pfizer Inc. (New York, NY)
Filing Date:Apr 22, 2002
Application Number:10/127,267
Claims:1. A compound of the formula ##STR26## wherein P is hydrogen, methyl, COOR.sup.16 wherein R.sup.16 is (C.sub.1 -C.sub.6)alkyl, allyl or 2,2,2-trichloroethyl; --C(.dbd.O)NR.sup.5 R.sup.6 ; --C(.dbd.O)H, --C(.dbd.O)(C.sub.1 -C.sub.6)alkyl wherein the alkyl moiety may optionally be substituted with from 1 to 3 halo atoms; --COOCH.sub.2 C.sub.6 H.sub.5, benzyl, t-butoxycarbonyl (t-Boc) or trifluoroacetyl, wherein R.sup.5 and R.sup.6 are each selected, independently, from hydrogen and (C.sub.1 -C.sub.6) alkyl, or R.sup.5 and R.sup.6 together with the nitrogen to which they are attached, form a pyrrolidine, piperidine, morpholine, azetidine, piperazine, N--(C.sub.1 -C.sub.6)alkylpiperazine or thiomorpholine ring, or a thiomorpholine wherein the ring sulfur is replaced with a sulfoxide or sulfone; and R.sup.14 and R.sup.15 are each amino.

2. A compound according to claim 1 wherein P is selected from the group consisting of --COCF.sub.3, --COCCl.sub.3, --COOCH.sub.2 CCl.sub.3, --COO(C.sub.1 -C.sub.6)alkyl and --COOCH.sub.2 C.sub.6 H.sub.5.

3. A compound according to claim 1 wherein P is t-butoxycarbonyl (t-Boc) or trifluoroacetyl.

4. A compound according to claim 1 wherein P is t-butoxycarbonyl (t-Boc).

5. A compound according to claim 1 wherein P is trifluoroacetyl.

6. A process for preparing a compound of formula IC ##STR27##

wherein R.sup.10 and R.sup.17 are selected, independently, from hydrogen; (C.sub.1 -C.sub.6)alkyl; phenyl and monocyclic heteroaryl. wherein said heteroaryl is selected from five to seven membered aromatic rings containing from one to four heteroatoms selected from oxygen, nitrogen and sulfur, comprising the steps of (i) allowing a compound according to claim 1 to react with a compound of formula ##STR28## or a compound of the formula ##STR29##

wherein R.sup.10 and R.sup.17 are defined as above; and (ii) removing the protecting group P.

7. The process according to claim 6 wherein P is selected from the group consisting of --COCF.sub.3, --COCCl.sub.3, --COOCH.sub.2 CCl.sub.3, --COO(C.sub.1 -C.sub.6)alkyl and --COOCH.sub.2 C.sub.6 H.sub.5.

8. A process according to claim 6 wherein P is t-butoxycarbonyl (t-Boc).

9. A process according to claim 6 wherein P is trifluoroacetyl.

10. A process according to claim 6 wherein R.sup.10 and R.sup.17 are selected, independently, from hydrogen or (C.sub.1 -C.sub.6)alkyl.

11. A process according to claim 6 wherein R.sup.10 and R.sup.17 are each hydrogen.

12. A process according to claim 6 comprising the prior step of reducing a compound of the formula ##STR30##

wherein P is hydrogen; methyl; COOR.sup.16 wherein R.sup.16 is (C.sub.1 -C.sub.6)alkyl; --C(.dbd.O)NR.sup.5 R.sup.6 ; --C(.dbd.O)H; --C(.dbd.O)(C.sub.1 -C.sub.6)alkyl wherein the alkyl moiety may optionally be substituted with from 1 to 3 halo atoms; t-butoxycarbonyl (t-Boc); or trifluoroacetyl; and R.sup.14 and R.sup.15 are each nitro; with a reducing agent.

13. A process according to claim 12 wherein the reducing step is conducted in the presence of hydrogen gas and a catalyst.

14. A process according to claim 12 wherein the reducing step is conducted in the presence of hydrogen gas and a palladium hydrogenation catalyst.
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