摘要:
Phenylbutanol derivatives of the formula Z-C(CH.sub.3) (OH)-CH.sub.2 -Y wherein Z is 4-biphenyl or 4-phenoxyphenyl wherein the phenoxy group is unsubstituted or substituted by F, Cl or Br and Y is COOR.sup.2 or CH.sub.2 OR.sup.3 wherein R.sup.2 is H or alkyl of 1 to 6 carbon atoms and R.sup.3 is H or alkanoyl of 1 to 6 carbon atoms, and their physiologically acceptable salts, possess anti-inflammatory activity and are produced by (a) treating with a solvolyzing agent a compound of the formula Z-C(CH.sub.3) (OH)-CH.sub.2 -W or Z-CX(CH.sub.3)-CH.sub.2 -Y wherein W is a functionally modified carboxy or methylol group different from Y and X is Cl, Br or I or a functionally modified hydroxyl group; or (b) reducing a compound otherwise corresponding to a desired final product but having instead of one of the hydrogen atoms a group which can be reduced or replaced by a hydrogen atom; or (c) oxidizing a compound otherwise corresponding to a desired final product but lacking the tertiary hydroxyl group; or (d) converting a compound otherwise corresponding to a desired final product wherein Z is a 4-phenoxyphenyl group but having instead a 4-OH-, Cl-, Br- or 1-substituted phenyl group into a desired final product; or (e) diazotizing a compound otherwise corresponding to a desired final product wherein Z is a halogen-substituted 4-phenoxyphenyl group but having an --NH.sub.2 -substituted phenoxy group and reacting the resulting diazonium salt with a halogenating agent.
摘要:
Sulfoxides and sulfones of the formula ##SPC1##Wherein R.sub.1 is COOH, COOR.sub.4, CH.sub.2 OH, or CH.sub.2 OR.sub.5 ; R.sub.2 is CH.sub.3 or C.sub.2 H.sub.5 ; R.sub.3 is H, F, Cl, or Br; R.sub.4 is alkyl of 1-8 carbon atoms; R.sub.5 is alkanoyl of 2-4 carbon atoms; one of the Y groups is SO or SO.sub.2 and the other Y group is CH.sub.2, O, S, SO, or SO.sub.2 ; and the physiologically acceptable salts thereof, which compounds possess anti-inflammatory activity, can be produced by converting in a compound of the formula ##SPC2##Wherein X is a group convertible into the group --CHR.sub.1 R.sub.2 wherein R.sub.1, R.sub.2, R.sub.3, and Y have the values given above, the group X into the group --CHR.sub.1 R.sub.3.
摘要:
Compounds of the formulaR--A--Zwherein R is a 4-biphenylyl or 4-phenoxyphenyl or a corresponding group monosubstituted or polysubstituted by one or more of F, Cl, and Br; A is --CH(CH.sub.3)--CH.sub.2 --(CH.sub.2).sub.n --, --C(CH.sub.3).dbd.CH--(CH.sub.2).sub.n -- or --C(OH)(CH.sub.3)--CH.sub.2 --(CH.sub.2).sub.n --, Z is --NR.sup.1 R.sup.2, imidazol-1-yl, phthalimido or 4,5-dihydro-4-oxophthalazin-1-yl-amino; R.sup.1 and R.sup.2 each are H or alkyl, azaalkyl or acyl, each of 1-6 carbon atoms or collectively are alkylene of 4-7 carbon atoms, 3-oxapentamethylene or 3-R.sup.3 -3-azapentamethylene; R.sup.3 is H or alkyl or hydroxyalkyl each of up to 6 carbon atoms; and n is 0, 1, or 2, and their physiologically acceptable acid addition salts possess anti-inflammatory, anti-arteriosclerotic and serum cholesterol and trigylyceride level lowering activities.
摘要:
Xanthenes of the formula Z-CHR.sub.1 R.sub.2 wherein Z is 2-xanthenyl or 2-xanthenyl substituted at the 1-, 3-, 4-, 5-, 6-, 7- or 8-position by F, Cl or Br, R.sub.1 is CH.sub.2 OH or CH.sub.2 OAc wherein Ac is alkanoyl of 2-4 carbon atoms, and R.sub.2 is H or alkyl of 1-4 carbon atoms, have antiphlogistic activity.
摘要翻译:式Z-CHR 1 R 2的Xanthenes,其中Z是在F,Cl或Br,R 1的1-,3-,4-,5-,6-,7-或8-位被2-取代的2-羟基苯基或2- CH2OH或CH2OAc,其中Ac是2-4个碳原子的烷酰基,R2是H或1-4个碳原子的烷基具有消炎活性。
摘要:
Compounds of the formulaR--A--Zwherein R is 4-biphenylyl or 4-phenoxyphenyl or a corresponding group monosubstituted or polysubstituted by one or more of F, Cl and Br; A is --CH(CH.sub.3)--CH.sub.2 --(CH.sub.2).sub.n --, --C(CH.sub.3).dbd.CH--(CH.sub.2).sub.n -- or --C(OH) (CH.sub.3)--CH.sub.2 --(CH.sub.2).sub.n --; Z is --NR.sup.1 R.sup.2, imidazol-1-yl, phthalimido or 4,5-dihydro-4-oxophthalazin-1-yl-amino; R.sup.1 and R.sup.2 each are H or alkyl, azaalkyl or acyl, each of 1 - 6 carbon atoms or, collectively, are alkylene of 4 - 7 carbon atoms, 3-oxapentamethylene or 3-R.sup.3 -3-azapentamethylene; R.sup.3 is H or alkyl or hydroxyalkyl each of up to 6 carbon atoms; and n is 0, 1 or 2, and their physiologically acceptable acid addition salts possess anti-inflammatory, anti-arteriosclerotic and serum cholesterol and triglyceride level lowering activities.
摘要:
Phenylbutanol derivatives of the formula Z--C(CH.sub.3) (OH)--CH.sub.2 --Y wherein Z is 4-biphenyl or 4-phenoxyphenyl wherein the phenoxy group is unsubstituted or substituted by F, Cl or Br and Y is COOR.sup.2 or CH.sub.2 OR.sup.3 wherein R.sup.2 is H or alkyl of 1 to 6 carbon atoms and R.sup.3 is H or alkanoyl of 1 to 6 carbon atoms, and their physiologically acceptable salts, possess anti-inflammatory activity and are produced by (a) treating with a solvolyzing agent a compound of the formula Z--C(CH.sub.3) (OH)--CH.sub.2 --W or Z--CX(CH.sub.3)--CH.sub.2 --Y wherein W is a functionally modified carboxy or methylol group different from Y and X is Cl, Br or I or a functionally modified hydroxyl group; or (b) reducing a compound otherwise corresponding to a desired final product but having instead of one of the hydrogen atoms a group which can be reduced or replaced by a hydrogen atom; or (c) oxidizing a compound otherwise corresponding to a desired final product but lacking the tertiary hydroxyl group; or (d) converting a compound otherwise corresponding to a desired final product wherein Z is a 4-phenoxyphenyl group but having instead a 4--OH--, Cl--, Br-- or I-substituted phenyl group into a desired final product; or (e) diazotizing a compound otherwise corresponding to a desired final product wherein Z is a halogen-substituted 4-phenoxyphenyl group but having an --NH.sub.2 -substituted phenoxy group and reacting the resulting diazonium salt with a halogenating agent.
摘要:
Pyrazolidinones of the formula ##SPC1##Wherein R is a phenyl, phenoxy or a corresponding group monosubstituted or polysubstituted by one or more of F, Cl and Br possess anti-inflammatory activity.
摘要:
Alkynols of the formula, ##STR1## wherein X is F, Cl or Br; n is 0 or 1; m is 0 or 1 and R (if m is 0) is hydroxyalkyl of 1-6 carbon atoms or (if m is 1) alkyl, straight-chain hydroxyalkyl or straight-chain tetrahydropyran-2-yloxyalkyl of 2-6 carbon atoms in the alkyl, have anti-inflammatory activity.
摘要:
Alkyne compounds of the formula ##STR1## wherein R.sup.1 is H, alkyl of up to 4 carbon atoms or phenyl; R.sup.2 is H, aliphatic acyl of up to 6 carbon atoms or aroyl of up to 11 carbon atoms; R.sup.3 and R.sup.4 are H, F, Cl or Br and n is 0 or 1, and physiologicaly acceptable metals salts thereof, have antiinflammatory activity. These compounds can be made from compounds of the formula ##STR2## wherein Q is a functionally-modified hydroxy and R.sup.1, R.sup.3, R.sup.4 and n are as above by treatment with a solvolyzing agent.
摘要:
Alkyne compounds of the formula ##STR1## wherein R.sup.1 is H, alkyl of up to 4 carbon atoms or phenyl; R.sup.2 is H, aliphatic acyl of up to 6 carbon atoms or aroyl of up to 11 carbon atoms; R.sup.3 and R.sup.4 are H, F, Cl or Br and n is 0 or 1, and physiologically acceptable metals salts thereof, have anti-inflammatory activity. These compounds can be made from compounds of the formula ##STR2## wherein Q is a functionally-modified hydroxy and R.sup.1, R.sup.3, R.sup.4 and n are as above by treatment with a solvolyzing agent.