.

Deeper Knowledge, Faster

  • Analyze global market entry opportunities
  • Predict branded drug patent expiration
  • Obtain formulation and manufacturing information

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

Serving 500+ biopharmaceutical companies globally:

Covington
Healthtrust
Deloitte
Citi
Daiichi Sankyo
Cipla
QuintilesIMS
Dow
AstraZeneca
Fuji

Generated: June 22, 2017

DrugPatentWatch Database Preview

Details for Patent: 6,897,310

« Back to Dashboard

Details for Patent: 6,897,310

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 23, 2002
Application Number:10/131,278
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 nitro.

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 the formula ##STR27## 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 ring wherein the ring sulfur is replaced with a sulfoxide or sulfone; and R.sup.14 and R.sup.15 are each nitro; comprising the steps of (i) allowing a compound of the formula ##STR28## wherein P is defined as above; and R.sup.14 and R.sup.15 are both hydrogen to react in the presence of 4 or more equivalents of trifluoromethanesulfonic acid (CF.sub.3 SO.sub.2 OH) and 2 to 3 equivalents of nitric acid.

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 comprising the prior step of placing a protecting group P on a compound of formula ##STR29##
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Serving 500+ biopharmaceutical companies globally:

US Army
US Department of Justice
McKinsey
Accenture
Harvard Business School
Queensland Health
Fuji
Daiichi Sankyo
Colorcon
Boehringer Ingelheim

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

Copyright 2002-2017 thinkBiotech LLC
ISSN: 2162-2639

Secure SSL Encrypted

Follow DrugPatentWatch:



Google
Twitter
Google Plus
botpot