Derivatives of 2-aminotetralins and pharmaceutical analogs thereof exhibiting differentail cns receptor activity and behavior
AssigneeWayne State University
InventorAloke K Dutta
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Abstract
Aminotetralin derivatives and pharmacological analogs thereof which contain an N-propynyl group exhibit differential dopaminergenic receptor activity. The subject compounds are useful in affecting dopamine receptor activity, particularly in exhibiting differing activity among the various dopamine receptor subtypes. The compounds are useful in treating CNS disorders in mammals in general, and humans in particular.
Claims31
A compound exhibiting differential activity between dopamine receptor subtypes, said compound being an 2-aminotetralin or biosteric analog thereof containing a fused ring structure, one ring comprising an optionally ring substituted moiety
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- or a pharmaceutically acceptable salt or derivative of said compound, wherein
- X is0, NH, or S,
- n is 0 or 1, and
- R is a C2-20 hydrocarbon, which may optionally contain one or more heteroatoms selected from the group consisting of O, N, and S, and which may contain a keto, thio, ester, carbonate, urea, amide, or urethane group.
An aminotetralin derivative exhibiting differential binding activity with respect to D2 and D3 dopamine receptors, having the formula
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- wherein A is hydroxyl or an ester or ether thereof in the 5- or 7-ring positions, and B is fluoro or chloro in the 6-ring position;
- wherein R14 is a hydrocarbon radical selected from the group consisting of C1-18 alkyl, C2-18 alkenyl, C2-18 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, C6-10 aryl, C6-10 heteroaryl, C7-18 alkaryl, C7-18 aralkyl, C7-18 alkheteroaryl, and C7-18 heteroaralkyl, each of said hydrocarbon radicals optionally substituted by one or more substituents selected from the group consisting of hydroxyl, C1-8 alkyl ester, halo, nitro, and cyano.
Dependencies are inferred from the claim text.