7-(2h-pyrazol-3-yl)-3,5-dihydroxy-heptanoic acid derivatives...

C - Chemistry – Metallurgy – 07 – D

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C07D 231/14 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01) C07D 405/06 (2006.01)

Patent

CA 2590533

The present invention provides compounds of the formula (I), (IV) and (V) and intermediates of the formuale (VI) and (VII): (I), (IV), (V), (VI), (VII). wherein: R1 is hydrogen, halogen, C1-C7 alkyl, C3-C8 cycloalkyl, aryl, aralkyl, heteroaryt, or heteroaralkyl; more specifically, R1 is C1-C7 alkyl or C3-C8 cycloalkyl; even more specifically, R1 is isopropyl; where alkyl, cycloalkyt, aryl, aralkyt, heteroaryl, or heteroaralkyl of R1 is optionally substituted, R2 is hydrogen, halogen, C1-C7 alkyl, C3-C8 cycloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, NC-, R2bR2aNCO(CH2)n -, R2bR2a NS(O)n-, R2cS(O)n-, R2bR2a N(CH2)n-, R2b-J-C(O)NR2a(CH2)n-, R2b-J-~SO2NR2a(CH2)n-, R2b- J-SONR2a(CH2)n, R7OOC(CH2)n-, or R7CO(CH2)n-; more specifically, R2 is R2bR2aNCO(CH2)n-; even more specifically, R2 is R2bR2a NCO-; where alkyl, cycloalkyl, aryl , aralkyl, heteroaryl, or heteroaralkyl of R2 is optionally substituted, R3 is hydrogen, C1-6 aikyl, C3-6necycloafkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; more specifically, R3 is aryl; even more specifically, R3 is phenyl or p-fluorophenyl; where alkyl, cycloalkyl, aryl, aralkyl, heteroaryt, or beteroaralkyd of A3 is opltianally substituted and is a bond or is absent. The other substituents are defined in the claims. The present invention relates to compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents. Moree specifically, the present invention concerns certain potent inhibitors of the enzyme 3-hydroxy-3- methylglutaryl-coenzyme A reductase ("HMG CoA reciuctase"). The compounds are useful for the treatement of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis.

L'invention concerne des composés de formule (I), (IV) et (V) et des intermédiaires de formule (VI) et (VII): (I), (IV), (V), (VI), (VII): R1 est hydrogène, halogène, C1-C7 alkyle, C3-C8 cycloalkyle, aryle, aralkyle, hétéroaryle, ou hétéroaralkyle; plus précisément, R1 est C1-C7 alkyle ou C3-C8 cycloalkyle; plus précisément encore, R1 est isopropyle; sachant que alkyle, cycloalkyle, aryle, aralkyle, hétéroaryle, ou hétéroaralkyle de R1 est éventuellement substitué, R2 est hydrogène, halogène, C1-C7 alkyle, C3-C8 cycloalkyle, aryle, aralkyle, hétéroaryle, hétéroaralkyle, NC-, R2bR2aNCO(CH2)n -, R2bR2a NS(O)n-, R2cS(O)n-, R2bR2a N(CH2)n-, R2b-J-C(O)NR2a(CH2)n-, R2b-J--SO2NR2a(CH2)n-, R2b-J-SONR2a(CH2)n, R7OOC(CH2)n-, ou R7CO(CH2)n-; plus précisément, R2 est R2bR2a NCO(CH2)n-; plus précisément encore, R2 est R2bR2a NCO-; sachant que alkyle, cycloalkyle, aryle, aralkyle, hétéroaryle, ou hétéroaralkyle de R2 est éventuellement substitué, R3 est hydrogène, C1-6 alkyle, C3-8 cycloalkyle, aryle, aralkyle, hétéroaryle, ou hétéroaralkyle; plus précisément, R3 est aryle; plus précisément encore, R3 est phényle ou p-fluorophényle; sachant que alkyle, cycloalkyle, aryle, aralkyle, hétéroaryle, ou hétéroaralkyle de R3 est éventuellement substitué et que - - - est une liaison ou n'est pas présent. On décrit des composés et des compositions pharmaceutiques utiles comme agents hypocholestérolémiques et hypolipidémiques. Plus précisément, on décrit certains inhibiteurs puissants de l'enzyme 3-hydroxy-3-méthylglutaryl-coenzyme A réductase ("HMG CoA réductase"). Les composés considérés sont utiles pour le traitement de l'hyperlipidémie, de l'hypercholestérolémie, de l'hypertriglycéridémie, de l'athérosclérose, de la maladie d'Alzheimer's, de l'hypertrophie prostatique bénigne, du diabète et de l'ostéoporose.

LandOfFree

Say what you really think

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

Rating

7-(2h-pyrazol-3-yl)-3,5-dihydroxy-heptanoic acid derivatives... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with 7-(2h-pyrazol-3-yl)-3,5-dihydroxy-heptanoic acid derivatives..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 7-(2h-pyrazol-3-yl)-3,5-dihydroxy-heptanoic acid derivatives... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFCA-PAI-O-1474556

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