Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1989-09-01
1991-03-05
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546155, A61K 3147, C07D21522
Patent
active
049978403
DESCRIPTION:
DESCRIPTION
20% cellulose acetate phthalate and 3% diethyl phthalate in ethanol:dichloromethane (1:1).
EXAMPLE 34
In the preparation of suppositories, 100 parts by weight of active compound is incorporated in 1300 parts by weight of triglyceride suppository base and the mixture formed into suppositories each containing 100 mg of active ingredient.
EXAMPLE 35
In the preparation of capsules, 50 parts by weight of active compound and 300 parts by weight of lactose are de-aggregated and blended. The mixture is filled into hard gelatin capsules, each capsule containing 50 mg of active compound
1. A compound of formula I ##STR32## in which R.sub.1 is lower alkyl; R.sub.2 is lower alkyl; and R.sub.3 and R.sub.4, which may be the same or different, are hydrogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, halo, halogenated lower alkyl, halogenated lower alkoxy, cyano, phenyl or phenyl substituted by 1 or 2 groups independently selected from lower alkyl, lower alkoxy and halo and R.sub.5 is hydrogen.
2. A compound as claimed in claim 1 in which R.sub.1 is alkyl having 1 to 4 carbon atoms; R.sub.2 is alkyl having 1 to 4 carbon atoms; and R.sub.3 and R.sub.4, which may be the same or different, are hydrogen, lower alkyl having 1 to 4 carbon atoms, lower alkoxy having 1 to 4 carbon atoms, lower alkylthio having to 4 carbon atoms, lower alkylsulphinyl having 1 to 4 carbon atoms, lower alkylsulphonyl having 1 to 4 carbon atoms, halo, fluorinated lower alkyl having 1 to 4 carbon atoms, fluorinated lower alkoxy having 1to 4 carbon atoms, cyano, phenyl or phenyl substituted by 1 or 2 groups independently selected from alkyl having 1 to 4 carbon atoms, alkoxy having to 4 carbon atoms and halo.
3. A compound as claimed in claim 2 in which R.sub.1 is methyl or ethyl; R.sub.2 is methyl, ethyl, isopropyl or butyl; and R.sub.3 and R.sub.4, which may be the same or different, are hydrogen, methyl, methoxy, methylthio, methylsulphinyl, methylsulphonyl, fluoro, chloro, trifluoromethyl, trifluoromethoxy, 2,2,2-trifluoroethoxy, cyano or phenyl.
4. A compound as claimed in claim 3 in which R.sub.1 is methyl or ethyl; R.sub.2 is methyl; and R.sub.3 and R.sub.4, which may be the same or different, are hydrogen, methyl, methoxy, methylthio, methylsulphinyl, fluoro, chloro, trifluoromethyl, trifluoromethoxy or cyano.
5. A compound as claimed in claim 4 in which R.sub.4 is hydrogen.
6. A compound as claimed in claim 1 of formula II ##STR33## in which R.sub.1 is lower alkyl; R.sub.2 is lower alkyl; and R.sub.3 (in the 6-position) and R.sub.4 (in the 7-position), which may be the same or different, are hydrogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, halo, halogenated lower alkyl, halogenated lower alkoxy, cyano, phenyl or phenyl substituted by 1 or 2 groups independently selected from lower alkyl, lower alkoxy and halo.
7. A compound as claimed in claim 6 in which R.sub.1 is alkyl having 1 to 4 carbon atoms; R.sub.2 is alkyl having 1 to 4 carbon atoms; and R.sub.3 and R.sub.4, which may be the same or different, are hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms, alkylsulphinyl having 1 to 4 carbon atoms, alkylsulphonyl having 1 to 4 carbon atoms, halo, fluorinated alkyl having 1 to 4 carbon atoms, fluorinated alkoxy having 1 to 4 carbon atoms, cyano, phenyl or phenyl substituted by 1 or 2 groups independently selected from alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms and halo.
8. A compound as claimed in claim 7 in which R.sub.1 is methyl or ethyl, R.sub.2 is methyl and R.sub.3 and R.sub.4 are each independently selected from hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms and halo.
9. A compound is claimed in claim 6 in which R.sub.1 is methyl or ethyl; R.sub.2 is methyl, ethyl, isopropyl or butyl; and one of R.sub.3 and R.sub.4 is hydrogen and the other is hydrogen, methyl, methoxy, methylthio, methylsulphinyl, methylsulphonyl, fluoro,
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Brown Michael D.
Davies Roy V.
Holman Nicholas J.
Daus Donald G.
The Boots Company PLC
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