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US 7,019,013 B2Granted
Sulfamidothienopyrimidines
AssigneeMerck Patent GmbH
InventorsHans-Michael Eggenweiler, Harry Schwartz, Pierre Schelling, Norbert Beier, Maria Christadler
Life of this patent
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Abstract
The invention relates to compounds of the formula (I) in which R1, E2 and X are as defined above.
Claims16
A compound of the formula I
- wherein
- R1 and R2 are each, independently of one another, H, OA1, OCOA1, OH or Hal, or
- R1 and R2 together are alkylene having 3–5 carbon atoms, —O—CH2—CH2—, —CH2—O—CH2—, —O—CH2—O— or —O—CH2—CH2—O—,
- X is —CH2SO2NR3R4,
- R3 and R4, independently of one another, are H, a heteroaromatic radical, alkyl or alkenyl having 1–10 carbon atoms, each of which is unsubstituted or terminally substituted by —NH2, —NHA1 or —NA1A2 and in which one or two CH2 groups may be replaced by one or more —CH═CH— groups, —O—, —NH— or —NA1—, or R3 and R4 together are cycloalkyl or cycloalkylene having 3–7 carbon atoms, which is unsubstituted, monosubstituted or polysubstituted by —Hal, —NH2, —NHA1, —NA1A2, —NHCOA1, —NHCOOA1, —COOH, —COOA1, —CONH2, —CONHA1, or —CONA1A2 and in which one or two —CH2— groups may be replaced by —O—, —NH—, —NA1—, —NCOA1— or —NCOOA1,
- A1 and A2 are each, independently of one another, alkyl or alkenyl having 1–10 carbon atoms, each of which may be substituted by 1–5 F and/or Cl atoms, or A1 and A2 together are cycloalkyl or cycloalkylene having 3–7 carbon atoms, in which one CH2 group may be replaced by —O—, —NH—, —NA1—, —NCOA1— or —NCOOA1—, and
- Hal is F, Cl, Br or I,
- or a physiologically acceptable salt thereof.
5 more elements
A compound of the formula II
- wherein
- X is —CH2SO2NR3R4,
- L is Cl, Br, OH, SCH3 or a reactive esterified OH group, and
- R3 and R4, independently of one another, are H, a heteroaromatic radical, alkyl or alkenyl having 1–10 carbon atoms, each of which is unsubstituted or terminally substituted by —NH2, —NHA1 or —NA1A2 and in which one or two CH2 groups may be replaced by one or more —CH═CH— groups, —O—, —NH— or —NA1—, or R3 and R4 together are cycloalkyl or cycloalkylene having 3–7 carbon atoms, which is unsubstituted, monosubstituted or polysubstituted by —Hal, —NH2, —NHA1, —NA1A2, —NHCOA1, —NHCOOA1, —COOH, —COOA1, —CONH2, —CONHA1, or —CONA1A2 and in which one or two —CH2— groups may be replaced by one or more —O—, —NH—, —NA1—, —NCOA1— or —NCOOA1,
- A1 and A2 are each, independently of one another, alkyl or alkenyl having 1–10 carbon atoms, each of which may be substituted by 1–5 F and/or Cl atoms, or A1 and A2 together are cycloalkyl or cycloalkylene having 3–7 carbon atoms, in which one CH2 group may be replaced by —O—, —NH—, —NA1—, —NCOA1— or —NCOOA1—, and
- Hal is F, Cl, Br or I.
3 more elements
A compound of the formula IV
- wherein
- Y is —CH2SO2Q,
- Q is Cl, Br, OH or a reactive esterified OH group, and
- R1 and R2 are each, independently of one another, H, OA1, OCOAl, OH or Hal, or R1 and R2 together are alkylene having 3–5 carbon atoms, —O—CH2—CH2—, —CH2—O—CH2—, —O—CH2—O— or —O—CH2—CH2—O—,
- A1 is, independently, alkyl or alkenyl having 1–10 carbon atoms, each of which may be substituted by 1–5 F and/or Cl atoms, and
- Hal is F, Cl, Br or l.
3 more elements
Dependencies are inferred from the claim text.