Farnesyl protein transferase inhibiting...

C - Chemistry – Metallurgy – 07 – D

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C07D 401/06 (2006.01) A61K 31/4709 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 407/14 (2006.01) C07D 413/14 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2231105

This invention comprises the novel compounds of formula (I), wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 is hydrogen, C1-12alkyl, Ar1, Ar2C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula -Alk1-C(=O)-R9, -Alk1-S(O)-R9 or -Alk1-S(O)2-R9; R2, R3 and R16 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar1, Ar2C1-6alkyl, Ar2oxy, Ar2C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; R4 and R5 each independently are hydrogen, halo, Ar1, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1- 6alkylS(O)2C1-6alkyl; R6 and R7 each independently are hydrogen, halo, cyano, C1-6alkyl, 4,4-dimethyl-oxazolyl, C1-6alkyloxy or Ar2oxy; R8 is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1- 6alkyloxycarbonylC1-6alkyl, carboxyC1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, imidazolyl, haloC1- 6alkyl, C1-6alkyloxyC1-6alkyl, aminocarbonylC1-6alkyl, or a radical of formula -O-R10, -S-R10, -N-R11R12; R17 is hydrogen, halo, cyano, C1- 6alkyl, C1-6alkyloxycarbonyl, Ar1; R18 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R19 is hydrogen or C1-6alkyl; having famesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

L'invention concerne de nouveaux composés de la formule générale (I). Dans cette formule, la ligne en pointillé représente une liaison facultative; X est oxygène ou soufre; R<1> est un hydrogène, C1-12alkyle, Ar<1>, Ar<2>C1-6alkyle, quinoléinylC1-6alkyle, pyridiylC1-6alkyle, hydroxyC1-6alkyle, C1-6alkyloxyC1-6alkyle, mono- or di(C1-6alkyl)aminoC1-6alkyle, amino C1-6alkyle, un radical de la formule -Alk<1>-C(=O)-R<9>, Alk<1>-S(O)-R<9> ou -Alk<1>-S(O)2-R<9>; R<2>, R<3> et R<16> sont chacun d'une manière indépendante un hydrogène, hydroxy, halo, cyano, C1-6alkyle, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, aminoC1-6alkyloxy, mono- ou di(C1-6alkyl)aminoC1-6alkyloxy, Ar<1>, Ar<2>C1-6alkyle, Ar<2>oxy, Ar<2>C1-6alkyloxy, hydroxycarbonyle, C1-6alkyloxycarbonyle, trihalométhyle, trihalométhoxy, C2-6alcényle; R<4> et R<5> sont chacun d'une manière indépendante un hydrogène, halo, Ar<1>, C1-6alkyle, hydroxyC1-6alkyle, C1-6alkyloxyC1-6alkyle, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyle, C1-6alkyloxycarbonyle, C1-6alkylS(O)C1-6alkyle ou C1-6alkyl-S(O)2C1-6alkyle; R<6> et R<7> sont chacun d'une manière indépendante un hydrogène, halo, cyano, C1-6alkyle, 4,4-diméthyl-oxyzolyl, C1-6alkyloxy ou Ar<2>oxy; R<8> is hydrogène, C1-6alkyle, cyano, hydroxycarbonyle, C1-6alkyloxycarbonyle, C1-6alkylcarbonylC1-6alkyle, cyanoC1-6alkyle, C1-6alkyloxycarbonylC1-6alkyle, carboxyC1-6alkyle, hydroxyC1-6alkyle, aminoC1-6alkyle, mono- ou di(C1-6alkyl)aminoC1-6alkyle, imidazolyl, haloC1-6alkyle, C1-6alkyloxyC1-6alkyle, aminocarbonylC1-6alkyle, ou un radical de la formule -O-R<10>, -S-R<10>, -N-R<11>R<12>; R<17> est un hydrogène, halo, cyano, C1-6alkyle, C1-6alkyloxycarbonyle, Ar<1>; R<18> est un hydrogène, C1-6alkyle, C1-6alkyloxy ou halo; R<19> est un hydrogène ou C1-6alkyle. Ces composés sont des inhibiteurs de la protéine farnésyle transférase. L'invention concerne également la préparation de ces composés, des compositions les contenant et leur utilisation en médecine.

LandOfFree

Say what you really think

Search LandOfFree.com for Canadian inventors and patents. Rate them and share your experience with other people.

Rating

Farnesyl protein transferase inhibiting... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Farnesyl protein transferase inhibiting..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Farnesyl protein transferase inhibiting... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFCA-PAI-O-1553963

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.