Back to results
US 4,667,032 AGranted
Phenothiazone derivatives and analogs
AssigneeMerck Frosst Canada, Inc.
InventorsCheuk K. Lau, Christiane Yoakim, Joshua Rokach, Rejean Fortin, Yvan Guindon
Life of this patent
Estimating the term…
Abstract
Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.
Claims22
The compounds of the Formula:
- ##STR63## wherein the substituents are:
- ______________________________________ Y R.sub.a R.sub.b R.sub.c ______________________________________ S H SCH.sub.3 H S H H SCF.sub.3 S H H CHO S H H COCF.sub.3 S H H H S H H H S H H H S H H H S H H H S H H H S H H Cl S H H Cl S H H Cl S H H Cl S H H Cl S H Obenzyl Cl S H OEt Cl S H OEt Cl S CH.sub.3 H Cl S H CH.sub.3 Cl S H OMe Br S H OMe Cl S H OEt Br S H OEt Cl S H OMe Cl S H OMe H O H OMe Br O H OMe Cl S H OMe Br SO.sub.2 H H OH SO.sub.2 H OMe OH SO.sub.2 OMe OMe Me SO.sub.2 H H OMe SO.sub.2 H OMe OMe S OCH.sub.3 OCH.sub.3 Me S H H COCH.sub.3 S OCH.sub.3 H Br S OCH.sub.3 Cl Cl S OCH.sub.3 H Cl S H ##STR64## H S H ##STR65## Br SO.sub.2 H OCH.sub.3 OH SO.sub.2 NHPr H NHPr SO.sub.2 ##STR66## H ##STR67## SO.sub.2 H OCH.sub.3 ##STR68## SO.sub.2 H OCH.sub.3 Br S NHPr H NHPr S NHPr H NHPr S H NHPr NHPr S H NHPr NHPr S H OCH.sub.3 NH.sub.2 S H OCH.sub.3 NHPr SO.sub.2 H OCH.sub.3 NHPr O OCH.sub.3 H Cl O OCH.sub.3 H Br O NHPr H NHPr SO.sub.2 H OCH.sub.3 CN SO.sub.2 H OCH.sub.3 NHCH.sub.2 CO.sub.2 R SO.sub.2 H OCH.sub.3 Sn-Bu SO.sub.2 H OCH.sub.3 CH.sub.2 CO.sub.2 R SO.sub.2 H OCH.sub.3 SO.sub.2 CH.sub.3 S H Sn-Bu H S H H Sn-Bu S H CH.sub.3 Sn-Bu S H OMe Br S H OMe Br S H OMe Br S H OMe Br S H OMe Br S H OMe Br S H OMe Br S H OMe Br ______________________________________ R.sub.d R.sub.e R.sub.f R.sub.g ______________________________________ H H H H H H H H H H H H H H H H H SCH.sub.3 H H H CO.sub.2 CH.sub.3 H H H CO.sub.2 H H H H CHO H H H CONH.sub.2 H H H CH.sub.2 OH H H H Co.sub.2 Me H H H CO.sub.2 H H H H CHO H H H COHN.sub.2 H H H CH.sub.2 OH H H H H H H H F H H H CH.sub.3 H H H CH.sub.3 H H H CH.sub.3 H H H OMe H H H OMe H H H OEt H H H OEt H H H OEt H H H SMe H H H OMe H H H OMe H H H Me H H H H H H H OMe H H H H H H H H H H H OMe H H H H H H H H H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H H H H H H H H H OCH.sub.3 H H H OCH.sub.3 H H H H H H H OCH.sub.3 H H H H H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H H H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H OCH.sub.3 H H H H H H H H H H H H H H H CF.sub.3 H H H F H H H Cl H H H Br H H H NMe.sub.2 H H H SMe H H H SO.sub.2 Me H H H Ph H H and R is H or C.sub.2 to C.sub.4 alkyl. ______________________________________
The compounds of the formula:
- ##STR74## wherein the substituents are:
- ______________________________________ R.sub.a R.sub.b R.sub.c R.sub.d ______________________________________ t-Bu t-Bu H H t-Bu t-Bu F H t-Bu t-Bu Me H t-Bu t-Bu SMe H t-Bu t-Bu H OMe. ______________________________________
The compounds:
- 2-S-glutathionyl-3H-phenothiazin-3-one;
- and 4-chloro-2-S-glutathionyl-phenothiazin-3-one.
Dependencies are inferred from the claim text.