EP 0724573 A1 19960807 - PYRIMIDINONES AS ANTIARTHRITIC AND ANTI-INFLAMMATORIES
Title (en)
PYRIMIDINONES AS ANTIARTHRITIC AND ANTI-INFLAMMATORIES
Title (de)
PYRIMIDINONEN ALS ANTIARTHRITISCHE UND ENTZÜNDUNGS HEMMENDE MITTEL
Title (fr)
PYRIMIDINONES UTILISEES COMME ANTIARTHRITIQUES ET ANTI-INFLAMMATOIRES
Publication
Application
Priority
- US 9410571 W 19940921
- US 13907893 A 19931020
- US 16167693 A 19931203
Abstract (en)
[origin: WO9511235A1] Compounds useful in the treatment of inflammation structurally represented as formula (I) or pharmaceutically acceptable salts thereof, wherein R<2> is a) (CH2)n-Y i) where n is 1 then Y is C1-C6 alkoxy, morpholinyl, piperdinyl, pyrrolidinyl, phenoxy, phenylthio, phenylsulfonyl, phenylsulfinyl, -NHC(O)-C1-C6 carboxylic acid, N3, NH2, diethylamino, hydrogen (provided R<4> is benzyloxy), halogen (provided R<3> is a C1-C6 alkyl) or CH("EWG")2 where "EWG" is an electron withdrawing group each individually selected from the group consisting of CO2R<6> or PO(OR<7>)2, or ii) n is 2 then Y is CH("EWG")2, or b) a terminal olefin substituted with i) an aryl or heteroaryl, ii) hydroxyl and a C1-C6 alkyl, phenyl or (CH2)m-CO2R<6> where m is 1 to 3, or c) C3-C6 cycloalkyl (optionally substituted with a halogen, (PO(OC2H5)2)2 or CN); R<3> is hydrogen or C1-C6 alkyl; R<4> is hydrogen, hydroxyl, C1-C6 alkyl, alkoxy, benzyloxy or phenoxy; R<5> is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, phenoxy, C1-C6 alkylthio, thiophenyl, NH2, aryl (except that R<5> is other than phenyl when R<4> and Y are both hydrogen) or heteroaryl; R<6> is H, C1-C6 alkyl, benzyl, phenyl, phenyl substituted with one to five F, C1, Br, I, NO2, OCH3 or C1-C4 alkyl; and R<7> is H, C1-C6 alkyl, benzyl, phenyl, phenyl substituted with one to five F, C1, Br, I, NO2, OCH3 or C1-C4 alkyl, or where both R<7>'s are taken together to form a CH2-CH2, CH2-CH2-CH2 or CH2-C(CH3)2-CH2 whereby a heterocyclic ring containing the bonded P atom and the two O atoms is formed. The compounds are useful as anti-inflammatory and antiarthritic agents.
IPC 1-7
IPC 8 full level
C07D 239/34 (2006.01); A61K 31/505 (2006.01); A61P 29/00 (2006.01); C07D 239/36 (2006.01); C07D 239/46 (2006.01); C07D 239/52 (2006.01); C07D 239/56 (2006.01); C07F 9/6512 (2006.01)
CPC (source: EP)
A61P 29/00 (2017.12); C07D 239/36 (2013.01); C07D 239/47 (2013.01); C07D 239/52 (2013.01); C07D 239/56 (2013.01); C07F 9/6512 (2013.01)
Citation (search report)
See references of WO 9511235A1
Designated contracting state (EPC)
AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9511235 A1 19950427; AU 7798994 A 19950508; EP 0724573 A1 19960807; JP H09504010 A 19970422
DOCDB simple family (application)
US 9410571 W 19940921; AU 7798994 A 19940921; EP 94928624 A 19940921; JP 51106395 A 19940921