Nova Patents
EP0322033A2

New 2,5-diaryl tetrahydrofurans and analogs thereof as paf antagonists.

Abstract

A class of 2,5-diaryl tetrahydrofuran derivatives are PAF antagonists and are therefore useful in the treatment of various diseases including prevention of platelet aggregation, hypotension, inflammation, asthma, lung edema, adult respiratory distress syndrome, various shock syndromes, cardiovascular disorders and other related skeletal-muscular disorders.

EP0322033A2, drawing sheet 1
Sheet 1 of 101

Term

Term ended

Projected expiry passed 14 December 2008, 17.8 years ago.

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5 claims: 1 independent, 4 dependent

  1. 1
    A compound of formula:wherein R and R' independently are (a) hydrogen;(b) haloloweralkyl;(c) halo;(d) CONR2R3 wherein R2 and R3 independently represent 1) H;2) straight or branched chain C1-20 alkyl;3) C3-8 cycloalkyl;4) C2-20 alkenyl;5) C2-2o alkynyl;6) aryl of 6 to 14 carbons;7) aralkyl;(e) loweralkenyl;(f) -COR2;(g) -CH2OR2;(h) loweralkynyl;(i) -CH2NR2R3;(i) -CH2SR2;(k) = 0;or(I)-OR2;(m) -R2;Ar and Ar' are the same or different from each other and are (a) phenyl or substituted phenyl of formula where R4-R8 independently represent 1) R2;2) YO-;wherein Y is -R2 or Y' where Y' represents(1) -(CH2)1-6 O(CO)R2;(2)(3) -(CH2)1-6-C3-8 cycloalkyl;(4) -(CH2 )1-6-COOR2;(5) -(CHz)1-6 OR2;(6) -(CH2)1-6 Ph;(7) wherein n is 0, 1 or 2;(8) haloloweralkyl;(9) -(CH2)1-7OSO2R2;or(10) (CH2)1-6 NR2R3;3) 4) -S(O)n-(CH2)1-6OR2, where n is 0, 1 or 2;5)-OCOCF3;6)7) -OCOR2;8) Y1;9) R2R3N-;10)11) COOR2;12) -CONR2R3;13) -NR2COR3;14) -OCONR2R3;15) -CRR9 R9 wherein R8 is R2 and can be the same as or different from R2;16) -(CH2)1-6OCOR2;17) -(CH2)1-6NR2COR3;18) -NHCH2COOR2;19) -CONR2COR3;20) -(CH2)1-6NR2R3;21) halo;22) -NR2R3R9X- wherein X- is an anion;23) -(CH2)1-6R2R3R9X-;24) -NR2SO2R3;25) -COR2;26) -NO2;27) -CN;28) -(CH2)1-6CN;29) -N3;30) -(CH2)1-6N3;31) -CONR2 (CH2)1-6NR3R9;32) -PO3R2R3;33) -(CH2)1-6PO3R2R3;34) -PO3(R2)(CH2)1-6NR3R9;35) -R4-R5, R5-R6, R6-R7 and R7-R8 joined together and form a bridge;36) SO2(CH2)1-6-CO-OR2;37) 38) 39) -(CH2)1-6 pyridyl;40) -SO2NH(CH2)1-6-(2-pyridyl);41) 42) 43) heteroaryl as defined below;44) -SO2(CH2)1-6CONHz;45) -(CH2)1-6CONR2R3;46) -(CH2)1-6NR2SO2R3;47) -(CH2)1-6OSO2R2;48) -O(CH2)1 -6-NR2R3;49) -CO-NRz-CO-R3;50) -S-CO-NR2R3;51) -P03(CH2CH2N(CH3)2)(C2Hs);52) -S(O)n(CH2)0-5CH(OR2)R3;53) -S(O)n(CH2)0-5CH2CH(OR2)-(CO)R3;54) -S(O)n(CH2)0-5CH2CH(OR2)-(CO)NHR3;or55) -S(O)n(CH2)0-5CH2CH(OR2)-(CO)OR3;(b) monoheteroaryl, di-or polyheteroaryl or fused heteroaryl containing 1 to 3 of any one or more of the heteroatoms N, S or O;(c) heteroarylalkyl;(d) heterocycloalkyl;or(e) heterocycloalkenyl.