EP 0766667 A1 19970409 - SUBSTITUTED AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS
Title (en)
SUBSTITUTED AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS
Title (de)
SUBSTITUIERTE AZETIDINONVERBINDUNGEN ALS HYPOCHOLESTEROLEMISCHE MITTEL
Title (fr)
COMPOSES D'AZETIDINONE SUBSTITUES UTILISES COMME AGENT HYPERCHOLESTEROLEMIANT
Publication
Application
Priority
- US 9507117 W 19950615
- US 26178594 A 19940620
Abstract (en)
[origin: WO9535277A1] Substituted azetidinone hypocholesterolemic agents of formula (I) or a pharmaceutically acceptable salt thereof, wherein: Ar<1> is aryl or R<3>-aryl; Ar<2> is aryl or R<4>-aryl; R<1> is selected from the group consisting of -(CH2)q-, wherein q is 2-6; -(CH2)e-Z-(CH2)r-, wherein Z is -O-, -C(O)-, phenylene, -NR<10>- or -S(O)0-2-, e is 0-5 and r is 0-5, provided that the sum of e and r is 1-6; -(C2-C6 alkenylene)-; and -(CH2)f-V-(CH2)g-, wherein V is C3-C6 cycloalkylene, f is 1-5 and g is 0-5, provided that the sum of f and g is 1-6; R<2> is -(lower alkylene)-COR<5> or -(CH=CH)-COR<5>; R<3> and R<4> are independently 1-3 substituents selected from lower alkyl, -OR<6>, -O(CO)R<6>, -O(CO)OR<9>, -O(CH2)1-5OR<6>, -O(CO)NR<6>R<7>, -NR<6>R<7>, -NR<6>(CO)R<7>, -NR<6>(CO)OR<9>, -NR<6>(CO)NR<7>R<8>, -NR<6>SO2R<9>, -COOR<6>, -CONR<6>R<7>, -COR<6>, -SO2NR<6>R<7>, S(O)0-2R<9>, -O(CH2)1-10-COOR<6>, -O(CH2)1-10CONR<6>R<7>, -(lower alkylene)-COOR<6>, -CH=CH-COOR<6>, -CF3, -CN, -NO2 and halogen; R<5> is -OR or -NRR<12>; R, R<6>, R<7>, R<8> and R<12> are independently selected from hydrogen, lower alkyl, aryl and aryl-substituted lower alkyl; R<9> is lower alkyl, aryl or aryl-substituted lower alkyl; and R<10> is hydrogen, lower alkyl, aryl lower alkyl or -C(O)R<6>; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, and pharmaceutical compositions containing them.
IPC 1-7
IPC 8 full level
A61K 31/395 (2006.01); A61K 31/397 (2006.01); A61P 3/06 (2006.01); A61P 9/10 (2006.01); C07D 205/08 (2006.01); C07D 205/085 (2006.01); C07D 401/04 (2006.01); C07D 403/04 (2006.01); C07D 405/04 (2006.01); C07D 405/10 (2006.01); C07D 409/04 (2006.01); C07F 7/08 (2006.01); C07F 7/18 (2006.01)
CPC (source: EP)
A61P 3/06 (2017.12); A61P 9/10 (2017.12); C07D 205/08 (2013.01); C07D 205/085 (2013.01); C07D 401/04 (2013.01); C07D 403/04 (2013.01); C07D 405/04 (2013.01); C07D 405/10 (2013.01); C07D 409/04 (2013.01); C07F 7/0812 (2013.01); C07F 7/1804 (2013.01)
Citation (search report)
See references of WO 9535277A1
Designated contracting state (EPC)
AT BE CH DE DK ES FR GB GR IE IT LI LU NL PT SE
DOCDB simple family (publication)
WO 9535277 A1 19951228; AU 2943095 A 19960115; CA 2191455 A1 19951228; EP 0766667 A1 19970409; JP H10501811 A 19980217; MX 9606319 A 19970531
DOCDB simple family (application)
US 9507117 W 19950615; AU 2943095 A 19950615; CA 2191455 A 19950615; EP 95925237 A 19950615; JP 50228995 A 19950615; MX 9606319 A 19950615