2-alkylidene hydroxycoumaranone derivatives
AssigneeRoche Diagnostics GmbH
InventorsWalter-Gunar Friebe, Bernhard Koenig, Hans-Willi Krell, Sabine Woelle
Life of this patent
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Abstract
New compounds of formula I wherein: R and R1 are independently selected from hydrogen, (C1-C6)alkyl, styryl and (C3-C6)cycloalkyl or, taken together with the carbon to which they are linked, form a (C3-C6)cycloalkyl group; A is selected from the following groups: —CH2C≡CCH2—, or —(CH2)q—NH—(CH2)q—, wherein q is an integer from 2 to 3 B is selected from T is selected from —CH2—C≡CH, —C≡CH, —(CH2)p—R3, —CH═CH—R3, —CH2—NHCO—R3, —(CH2)p—O—R3, —CH(NH2)—CH2R3, in which p is 0 or an integer from 1 to 4, R3 is a carbocyclic or heterocyclic ring as medicaments having antitumor and/or antimetastatic activities.
Claims18
A compound of formula I
- wherein:
- R and R1 are independently hydrogen, (C1-C6)alkyl, styryl or (C3-C6)cycloalkyl or, taken together with the carbon to which they are linked, form a (C3-C6)cycloalkyl group;
- T is —CH2—C≡CH, —C≡CH, —(CH2)p—R3, —CH═CH—R3, —CH2—NHCO—R3, —(CH2)p—O—R3, or —CH(NH2)—CH2R3, wherein p is 0 or an integer from 1 to 4, and
- R3 is phenyl, naphthyl, biphenyl, each being unsubstituted or substituted by one or more groups selected from chlorine, bromine, iodine, fluorine, (C1-C6)alkyl, cyano, nitro, mono- or polyfluoroalkyl, —SO2(C1-C4)alkyl, —SO2NH2, —SO2NH(C1-C4)alkyl, —SO2N[(C1-C4)alkyl]2, —CONH2, —CONH(C1-C4)alkyl, hydroxy, amino, carboxy, (C1-C4)alkoxy, (C1-C4)mono- or di-alkyl amino, (C1-C4)alkoxycarbonyl, mercapto, (C1-C4)alkylthio or R3 is a 5- or 6-membered unsubstituted or substituted heterocycle which contains 1 or 2 heteroatoms selected from oxygen, sulfur or nitrogen and which is or is not benzocondensed, wherein the substituents are one or more groups selected from chlorine, bromine, iodine, fluorine, (C1-C6)alkyl, cyano, nitro, mono- or polyfluoroalkyl, —SO2(C1-C4)alkyl, —SO2NH2, —SO2NH(C1-C4)alkyl, —SO2N[(C1-C4)alkyl]2, —CONH2, —CONH(C1-C4)alkyl, hydroxy, amino, carboxy, (C1-C4)alkoxy, (C1-C4)mono- or di-alkyl amino, (C1-C4)alkoxycarbonyl, mercapto, (C1-C4)alkylthio, or an enantiomer, diastereoisomer, racemate or mixture thereof, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.