Phosphorus-containing squalene synthetase inhibitors and method

Details Phosphorus-containing squalene synthetase inhibitors and method Phosphorus-containing squalene synthetase inhibitors and method

C - Chemistry, Metallurgy

07

F

167/125, 167/250

C07F 9/38 (2006.01) A61K 31/66 (2006.01) C07F 9/40 (2006.01)

Patent

CA 2018470

HX18 Abstract PHOSPHORUS-CONTAINING SQUALENE SYNTHETASE INHIBITORS AND METHOD Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure Image wherein m is 1, 2 or 3; n is 0, 1, 2 or 3; Y1 and Y2 are H or halogen; R2, R3 and R4 may be the same or different and are independently H, metal ion, C1 to C8 alkyl or C3 to C12 alkenyl; X is O, S, NH or NCH2R15 wherein R15 is H or C1 to C5 alkyl; and R1 is R5-Q1-Q2-Q3- wherein Q1, Q2 and Q3 are the same or different and are independently , Image , -CH2-C?C-CH2- or a single bond, with the proviso that if Q1 is a bond, then Q2 and Q3 are bonds and if Q2 is a bond, then Q3 is a bond, and wherein R6 is H, alkyl, halo, or haloalkyl, R7 is H, halo, alkyl or alkylthio; R8 is H, halogen, trimethylsilyl or lower alkyl; R9 is H or lower alkyl-; R5 is Image , Image , R16-C?C-CH2- (wherein R16 is H or lower alkyl) or CH3(CH2)p where p is an integer from 2 to 7; R10, HX18 and R11 are the same or different and are independently H, lower alkyl, halogen, haloalkyl or lower alkenyl or R10 and R11 can be taken together to form (CH2) where s is an integer from 2 to 7; and R13 and R14 are the same or different and are independently lower alkyl, with the proviso that if all of Q1, Q2 and Q3 are bonds, then both R10 and R11 cannot be H and R5 cannot be alkyl(CH2)p- with p?4; including all stereoisomers thereof. New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.

Affiliated with

Also associated with

Rating

Phosphorus-containing squalene synthetase inhibitors and method does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Phosphorus-containing squalene synthetase inhibitors and method, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Phosphorus-containing squalene synthetase inhibitors and method will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1397341