Claims
- 1. A compound having the formula: ##STR46## wherein R.sup.1 is CH.sub.3, Br, Cl, OH, C.sub.2 H.sub.5, COR.sup.17, COOR.sup.18, CONR.sup.19 R.sup.20, phenyl, --N(R.sup.12)(R.sup.13), ##STR47## S(O).sub.p lower alkyl where p is 0, 1, or 2, SO.sub.2 NH.sub.2, or --NHSO.sub.2 lower alkyl optionally substituted with F;
- R.sup.2 and R.sup.3 independently are H, CH.sub.3, C.sub.2 H.sub.5, CH.sub.3 O, or C.sub.2 H.sub.5 O; R.sup.4 is ##STR48## R.sup.7 is ##STR49## R.sup.9 is H or C.sub.1 -C.sub.4 alkyl; R.sup.12 and R.sup.13 independently are H, C.sub.1 -C.sub.4 alkyl, or together are (CH.sub.2).sub.4-5 ;
- R.sup.14 is H, C.sub.1 -C.sub.4 alkyl, OR.sup.9, O-phenyl, OCH.sub.2 COOR.sup.9, O-benzyl, COOR.sup.9, CF.sub.3, Cl, Br, I, N(R.sup.12)(R.sup.13), or S(O).sub.w R.sup.9 where w is 0-2 with the proviso that if w is 1, then R.sup.9 is not H; and
- R.sup.15 and R.sup.16 are independently H, C.sub.1 -C.sub.4 alkyl, OR.sup.9, O-benzyl, F or Cl;
- R.sup.17 is lower alkyl, phenyl optionally monosubstituted with Cl, Br, F, CH.sub.3, CH.sub.3 O, pyridyl, thienyl or furyl;
- R.sup.18 is H or lower alkyl;
- R.sup.19 and R.sup.20 independently are H or lower alkyl, or taken together are (CH.sub.2).sub.4-5 ; and
- R.sup.21 is H.
- 2. A compound of claim 1 wherein R.sup.21 is H.
- 3. A compound of claim 1 wherein R.sup.2 and R.sup.3 are H.
- 4. A compound of claim 1 wherein R.sup.7 is phenyl.
- 5. A compound of claim 1 wherein R.sup.1 is CON(CH.sub.3).sub.2, CONH.sub.2, COR.sup.17, COOR.sup.18, SO.sub.2 NH.sub.2, phenyl, Br, Cl, or CH.sub.3.
- 6. A compound of claim 1 wherein R.sup.2, R.sup.3 and R.sup.21 are H; R.sup.7 is phenyl; and R.sup.1 is CON(CH.sub.3).sub.2, CONH.sub.2, COR.sup.17, COOR.sup.18, SO.sub.2 NH.sub.2, phenyl, Br, Cl, or CH.sub.3.
- 7. A pharmaceutical composition comprising a suitable pharmaceutical carrier and a 5-lipoxygenase inhibiting amount of a compound of claim 1.
- 8. A pharmaceutical composition comprising a suitable pharmaceutical carrier and a 5-lipoxygenase inhibiting amount of a compound of claim 2.
- 9. A pharmaceutical composition comprising a suitable pharmaceutical carrier and a 5-lipoxygenase inhibiting amount of a compound of claim 3.
- 10. A pharmaceutical composition comprising a suitable pharmaceutical carrier and a 5-lipoxygenase inhibiting amount of a compound of claim 4.
- 11. A pharmaceutical composition comprising a suitable pharmaceutical carrier and a 5-lipoxygenase inhibiting amount of a compound of claim 5.
- 12. A pharmaceutical composition comprising a suitable pharmaceutical carrier and a 5-lipoxygenase inhibiting amount of a compound of claim 6.
- 13. A method of inhibiting 5-lipoxygenase in a mammal which comprises administering to the mammal an effective amount of a compound of claim 1.
- 14. A method of inhibiting 5-lipoxygenase in a mammal which comprises administering to the mammal an effective amount of a compound of claim 2.
- 15. A method of inhibiting 5-lipoxygenase in a mammal which comprises administering to the mammal an effective amount of a compound of claim 3.
- 16. A method of inhibiting 5-lipoxygenase in a mammal which comprises administering to the mammal an effective amount of a compound of claim 4.
- 17. A method of inhibiting 5-lipoxygenase in a mammal which comprises administering to the mammal an effective amount of a compound of claim 5.
- 18. A method of inhibiting 5-lipoxygenase in a mammal which comprises administering to the mammal an effective amount of a compound of claim 6.
Parent Case Info
This is a division of application Ser. No. 06/839,912, now U.S. Pat. No. 4,833,164 filed on Mar. 19, 1986, which is a continuation-in-part of copending application Ser. No. 731,791, filed May 8, 1985, now abandoned.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4737519 |
Yamashita et al. |
Apr 1989 |
|
4833164 |
Batt |
May 1989 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
2072174 |
Feb 1989 |
GBX |
Non-Patent Literature Citations (3)
Entry |
Hassner, A., "The Chemistry of Derivatives of Benzaltetralone". |
J. Am. Chem. Soc. 80, 893-900 (1958). |
Chemical Abstracts, (63), 9891a, Zenichi Horii, Takefumi Momose, and Yasumitsu Tamnra. |
Divisions (1)
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Number |
Date |
Country |
Parent |
839912 |
Mar 1986 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
731791 |
May 1985 |
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