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US RE35,218 EGranted
Azatetracycle compounds
AssigneeG. D. Searle & Co.
InventorsDaniel P. Becker, Daniel L. Flynn, Roger Nosal, Dale P. Spangler, Daniel L. Zabrowski
Life of this patent
Estimating the term…
Abstract
An azatetracycle compound useful as 5HT.sub.3 antagonists of the general formula ##STR1## wherein D is a tetracycle of the structure ##STR2## wherein Ar is an aromatic moiety and B is either NH or O.
Claims52
A compound of the formula ##STR39## wherein D is ##STR40## wherein B is NH or O;
- wherein A is NH or a bond;
- wherein p is 1 or 0;
- and
- when p is 1, Ar is ##STR41## and when p is 0, Ar is ##STR42## wherein X is O,S,N(R.sup.4) or CH.sub.2 ;
- wherein Y is N or CH;
- wherein n is 1 or 2;
- wherein Z is ##STR43## wherein R.sup.1 is alkoxy of 1 to 6 carbon atoms;
- wherein R.sup.2 and R.sup.3 are the same or different and is hydrogen, halogen, CF.sub.3, hydroxyl, C.sub.1-2 alkoxy, C.sub.2-7 acyl, amino, amino substituted by one or two C.sub.1-6 alkyl groups, C.sub.2-7 acyl amino, amino carbonyl, or amino sulfone optionally substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-6 alkyl sulfone or nitro groups;
- wherein R.sup.4 and R.sup.4 ' can be the same or different and is hydrogen, alkyl or arylalkyl;
- wherein R.sup.5 and R.sup.6 is the same or different and is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-7 acyl, C.sub.1-7 acylamino, or amino, amino carbonyl or amino sulfonyl, optionally substituted by one or two C.sub.1-6 alkyl or C.sub.3-8 cycloalkyl groups, or by C.sub.4-5 polymethylene or biphenyl, C.sub.1-6 alkylsulfonyl, C.sub.1-6 alkylsulfinyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy or nitro or when R.sup.5 and R.sup.6 are taken together are methylenedioxy or ethylenedioxy;
- wherein R.sup.9 and R.sup.10 can be the same or different and is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.1-4 alkynyl or together are C.sub.2-4 polymethylene;
- wherein R.sup.7 and R.sup.8 are the same or different and is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulfonylamino, N-(C.sub.1-6 alkylsulfonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulfinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulfonyl, aminosulfonylamino or N-(aminosulfonyl)-C.sub.1-4 alkylamino optionally N'-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, phenyl, or phenyl C.sub.1-4 alkyl groups or optionally N'-disubstituted by C.sub.4-5 polymethylene;
- and wherein R.sup.11 and R.sup.12 can be the same or different and is hydrogen or C.sub.1-4 alkyl or taken together are a covalent bond;
- and
- wherein R.sup.13 is H, halogen or OR.sup.4.
12 more elements
##STR64##
Dependencies are inferred from the claim text.