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5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis

  • US 5,552,412 A
  • Filed: 01/09/1995
  • Issued: 09/03/1996
  • Est. Priority Date: 01/09/1995
  • Status: Expired
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First Claim
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1. A compound of the formula:

  • ##STR19## 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 ;

    (e) a five membered heterocycle containing up to two heteroatoms selected from the group consisting of -O-, -NR2 - and -S(O)n -, optionally substituted with 1-3 substituents independently selected from R4 ;

    (f) a six membered heterocycle containing up to two heteroatoms selected from the group consisting of -O-, -NR2 - and -S(O)n - optionally substituted with 1-3 substituents independently selected from R4 ;

    or(g) a bicyclic ring system consisting of a five or six membered heterocyclic ring fused to a phenyl ring, said heterocyclic ring containing up to two heteroatoms selected from the group consisting of -O-, -NR2 -, NR2 - and -S(O)n -, optionally substituted with 1-3 substituents independently selected from R4.Z1 is(a) -O(CH2)P CR5 R6 -;

    (b) -O(CH2)P W(CH2)q ;

    or(c) -OCHR2 CHR3 -;

    G is -NR7 R8 ;

    W is(a) -CH2 -;

    (b) -CH═

    CH-;

    (c) -O-;

    (d) -NR2 -;

    (e) -S(O)n -;

    ##STR20## (g) -CR2 (OH)-;

    (h) -CONR2 -;

    (i) -NR2 CO-;

    ##STR21## or (k) -C═

    C-;

    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) -CO2 H;

    (I) -CN;

    (m) -CONHOR;

    (n) -SO2 NHR;

    (o) -NH2 ;

    (p) C1 -C4 alkylamino;

    (q) C1 -C4 dialkylamino;

    (r) -NHSO2 R;

    (s) -NO2 ;

    (t) -aryl;

    or(u) -OH.R5 and R6 are independently C1 -C8 alkyl or together form a C3 -C10 carbocyclic ring;

    R7 and R8 in ring form may optionally be substituted with up to three substituents independently selected from C1 -C6 alkyl, halogen, alkoxy, hydroxy and carboxy;

    a ring formed by R7 and R8 may be optionally fused to a phenyl ring;

    e is 1 or 2;

    p is 0, 1, 2 or 3;

    q is 0, 1, 2 or 3;

    and optical and geometric isomers thereof; and

    nontoxic pharmacologically acceptable acid addition salts, N-oxides, esters, and quaternary ammonium salts thereof.

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