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US 6,207,716 B1Granted
Non-steroidal ligands for the estrogen receptor
AssigneeGlaxo Wellcome Inc.
InventorTimothy Mark Willson
Life of this patent
Estimating the term…
Abstract
Novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.
Claims19
A compound of Formula I:
- wherein
- R1 is —(CH2)nCR5═CR6R7;
- —(CH2)mC(X)NR8R9;
- or
- R2 and R3 are independently H, —CH3, —OH, —OCH3, —OCH2CH3 or —CH2(CH3)2;
- R4 is —CN, —NO2, —CH3, —CH2CH3, —CH2CH2—Y or —Y;
- R5 and R6 are independently H, —C1-4alkyl, —C2-4alkenyl, —C2-4alkynyl, —X—C1-3alkyl, —X—C2-4alkenyl, —X—C2-4alkynyl or —Y;
- R7 is —CN, —C1-4alkyl—OH, —C(O)O(CH3)3, —C(O)NR10R11, —C(O)NR12R13, —C1-4alkyl—NR10R11, —C(O)R12, —C(O)OR12, —C(O)NR12OR13, —C(O)NHC(O)R12, —C(O)NHCH2R12, —C(NH2)(NOR12), —S(O)R12, —S(O)(O)(OR12), —S(O)(O)(NHCO2R12), PO3R12, —P(O)(NR12R13)(NR12R13), —P(O)(NR12R13)(OR14), —CONR12(CH2)q OCH3, —CONR12(CH2)qNR8R9 or oxadizole substituted with methyl;
- R8 and R9 are independently hydrogen, —C1-7alkyl, —C3-7cycloalkyl, —O—C1-7alkyl, —C1-7alkyl—Y or phenyl;
- R10 and R11 are independently methyl or ethyl or, taken together form a morpholino group bonded via its nitrogen atom;
- R12, R13 and R14 are independently H, —C1-12alkyl, —C2-12alkenyl, —C2-12alkynyl, —O—C1-12alkyl, —O—C2-12alkenyl, —O—C2-12alkynyl, —C3-7cycloalkyl, —C3-7cycloalkenyl, linear and cyclic heteroalkyl, aryl, heteroaryl or —Y;
- X is oxygen or sulfur;
- Y is a halogen;
- n is an integer selected from 0, 1 or 2;
- m is the integer 1 or 2;
- p is an integer selected from 1 to 4;
- and
- q is an integer from 1-12.
15 more elements
Dependencies are inferred from the claim text.