DrugPatentWatch Database Preview
« Back to Dashboard
Summary for Patent: 4,863,931
|Title:||Antihistaminic fluoro substituted benzocycloheptapyridines|
|Abstract:||Certain benzocycloheptapyridine compounds with fluorine substitution across the exocyclic double bond are prepared and they are useful as antihistaminic agents.|
|Inventor(s):||Schumacher; Doris P. (Florham Park, NJ), Murphy; Bruce L. (Glen Ridge, NJ), Clark; Jon E. (Highland Park, NJ)|
|Assignee:||Schering Corporation (Kenilworth, NJ)|
|Patent Litigation and PTAB cases:||See patent lawsuits and PTAB cases for patent 4,863,931|
1. A compound represented by structural formula I ##STR13## or a pharmaceutically acceptable salt thereof, wherein: A, B, X and Y may be the same or different, and each independently
represents H, halo, --CF.sub.3, --OR.sup.10, --C(O)R.sup.10, --SR.sup.10, --N(R.sup.10).sub.2, --OC(O)R.sup.10, --CO.sub.2 R.sup.10, --OCO.sub.2 R.sup.11, alkyl, alkenyl or alkynyl, alkyl, alkenyl or alkynyl, which alkyl or alkenyl groups may be
substituted with halo, --OR.sup.10, or --CO.sub.2 R.sup.10 ;
R.sup.10 represents H, alkyl or aryl;
R.sup.11 represents alkyl or aryl;
R.sup.1 and R.sup.2 may be H and F respectively or F and H respectively; and
R is H, alkyl or --CO.sub.2 R.sup.10 wherein R.sup.10 is as previously defined.
2. A compound of claim 1 wherein A, B, X and Y may be the same or different and each independently represents H or halo.
3. A compound of claim 2 wherein one of A, B, X and Y is halo and the others are H.
4. The compound of claim 3 wherein one of X or Y is halo and A, B and the other of X or Y are H.
5. The compounds of claim 4 wherein the halo X or Y is chlorine.
6. A compound according to claim 4 wherein R is CO.sub.2 R.sup.10.
7. The compounds of claim 6 wherein R.sup.10 is selected from H or alkyl.
8. The compounds of claim 7 wherein R.sup.10 is alkyl.
9. The compounds of claim 8 wherein R.sup.10 is ethyl.
10. The compounds of claim 9 wherein R.sup.1 is fluorine and R.sup.2 is H.
11. A compound of claim 1 having the name:.
ethyl 4-[8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-4-fl uoro-1-piperidine carboxylate; or
ethyl 4-[8-chloro-11-fluoro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-1 1-yl]-1-piperidine carboxylate.
12. A compound of claim 10 having the formula: ##STR14##
13. A pharmaceutical composition which comprises a compound having structural formula I as defined in claim 1, in combination with a pharmaceutically acceptable carrier.
14. A method for treating allergic reactions in a mammal comprising administering to said mammal an antihistaminic effective amount of a compound as claimed in claim 1.
For more information try a trial or see the plans and pricing
Serving hundreds of leading biopharmaceutical companies globally:
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.