Patent number: 6008240
Abstract: The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of the general formula: ##STR1## R.sub.2 is a hydrogen or a methyl or ethyl group; R.sub.3 is a hydrogen or a methyl or ethyl group;n is 1, 2, 2, 3, 4, 5, or 6; andR.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) phenyl or substituted phenyl; (c) alkyl; (d) heterocyclic; (e) decahydronapthalene; and (f) octahydroindene;with the provisos thatwhen X is H, A can be --CH.sub.2 CH.sub.2 --,--COCH.sub.2 --,--CONH--,--CON(CH.sub.3), CH.dbd.CH, --c.ident.c--,--CH.sub.2 --NH--, --CH.sub.2 --N(CH.sub.3)--,--CH(OH)CH.sub.2 --,--NH--CH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --,--CH.sub.2 O--,--CH.sub.2 S--, and --NHCOO--;when X is NH.sub.2, NH(CH.sub.3), N(CH.sub.3).sub.2, OH, OCH.sub.3, CH.sub.3, SH, and SCH.sub.3 ; A can be --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.dbd.CH--; --COCH.sub.2, --CH.sub.2 CH.sub.2 --,--CH(OH)CH.sub.2, or --C.ident.
Type:
Grant
Filed:
December 15, 1997
Date of Patent:
December 28, 1999
Assignee:
Gliatech, Inc.
Inventors:
James G. Phillips, Clark E. Tedford, Amin Mohammed Khan, Stephen L. Yates, Syed M. Ali
Patent number: 5652258
Abstract: The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of the general formula: ##STR1## where X is H, A is --CH.sub.2 CH.sub.2 --, --COCH.sub.2 --, --CONH--, --CON(CH.sub.3)--, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 --NH--, --CH.sub.2 --NCH.sub.3 --, --CH(OH)CH.sub.2 --, --NH--CH.sub.2 --, --N(CH.sub.3) --CH.sub.2 --, --NHSO.sub.2 --, --CH.sub.2 O--, --CH.sub.2 S--, CH.sub.2 SO.sub.2 --, or --CH.sub.2 S(O)--;R.sub.2 is a hydrogen or a methyl or ethyl group;R.sub.3 is a hydrogen or a methyl or ethyl group;n is 0, 1, 2, 3, 4, 5, or 6; andR.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) H; (c) phenyl or substituted phenyl; (d) alkyl; (e) heterocyclic; and (f) bicyclic alkyl; andwhenX is NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, OH, OCH.sub.3, NHR.sub.4, OR.sub.4, SH, SR.sub.4, or SO.sub.2 R.sub.4 ; A is --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --NHSO.sub.2 --, --CH.dbd.CH--, --CH.dbd.CHF--, --COCH.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
July 29, 1997
Assignee:
Gliatech, Inc.
Inventors:
James G. Phillips, Clark E. Tedford, Amin Mohammed Khan, Stephen L. Yates