Back to results
US 6,204,286 B1Granted
Estrogen agonists/antagonists
AssigneePfizer Inc.
InventorsKimberly O. Cameron, Paul A. DaSilva Jardine, Robert L. Rosati
Life of this patent
Estimating the term…
Abstract
Compounds of the formula: are disclosed useful for treating osteoporosis, obesity, breast cancer, endometriosis, cardiovascular disease and prostatic disease. Substituents A, B, E, D, Z1, G, Y and e have the same meaning as defined in the specification.
Claims20
A compound of the formula:
- wherein:
- A is CH2;
- B, D and E are CH;
- Y is
- (a) phenyl, optionally substituted with 1-3 substituents independently selected from R4;
- (b) naphthyl, optionally substituted with 1-3 substituents independently selected from R4;
- (c) C3-C8 cycloalkyl, optionally substituted with 1-2 substituents independently selected from R4;
- (d) C3-C8 cycloalkenyl, optionally substituted with 1-2 substituents independently selected from R4;
- Z1 is
- (b) —O(CH2)pCR5R6—;
- (c) —O(CH2)pW(CH2)q;
- or
- (d) —OCHR2CHR3—;
- G is
- W is
- (a) —CH2—;
- (b) —CH═CH—;
- (c) —O—;
- (d) —NR2—;
- (e) —S(O)n—;
- (f)
- (g) —CR2(OH);
- (h) —CONR2—;
- (i) —NR2CO—;
- (j)
- (k) —C═C—;
- R is hydrogen or C1-C6 alkyl;
- R2 and R3 are independently
- (a) hydrogen;
- or
- (b) C1-C4 alkyl;
- R4 is
- (a) hydrogen;
- (b) halogen;
- (c) C1-C6 alkyl:
- (d) C1-C4 alkoxy;
- (e) C1-C4 acyloxy;
- (f) C1-C4 alkylthio;
- (g) C1-C4 alkylsulfinyl;
- (h) C1-C4 alkylsulfonyl;
- (i) hydroxy (C1-C4)alkyl;
- (j) aryl (C1-C4)alkyl;
- (k) —CO2H;
- (l) —CN;
- (m) —CONHOR;
- (n) —SO2NHR;
- (o) —NH2;
- (p) C1-C4 alkylamino;
- (q) C1-C4 dialkylamino;
- (r) —NHSO2R;
- (s) —NO2;
- (t) —aryl;
- or
- (u) —OH;
- R5 and R6 are independently C1-C8 alkyl or together form a C3-C10 carbocyclic ring;
- e is, 1;
- m is 1, 2 or 3;
- n is 0, 1 or 2;
- p is 0, 1, 2 or 3;
- q is 0, 1, 2 or3;
- and optical and geometric isomers thereof;
- and nontoxic pharmacologically acceptable acid addition salts, N-oxides, esters, and quaternary ammonium salts thereof.
59 more elements
A method of lowering serum cholesterol levels in a mammal which comprises administering to a mammal in need of such treatment an effective amount of a compound of formula I.
Dependencies are inferred from the claim text.