EP 1019386 A1 20000719 - REVERSE HYDROXAMATE DERIVATIVES AS METALLOPROTEASE INHIBITORS
Title (en)
REVERSE HYDROXAMATE DERIVATIVES AS METALLOPROTEASE INHIBITORS
Title (de)
HYDROXAMATDERIVATE ALS METALLOPROTEASEINHIBITOREN
Title (fr)
DERIVES D'HYDROXAMATE UTILISES COMME INHIBITEURS DE METALLOPROTEASE
Publication
Application
Priority
- EP 9801015 W 19980224
- US 3911297 P 19970226
Abstract (en)
[origin: WO9838179A1] A family of compounds having general structural formula (I) wherein W is a reverse hydroxamic acid group (a); R5 is hydrogen or lower alkyl; R6 is (b); where Z1 is heteroarylene; preferably: R1 is methyl, ethyl, isopropyl, n-propyl or 3,3,3-trifluoro-n-propyl; R2 is isobutyl or sec-butyl; R3 is hydrogen; R4 is tert-butyl, sec-butyl, 1-methoxy-1-ethyl or 2-(2-pyridylcarbonylamino)-1-ethyl; R5 is hydrogen; and R6 is 2-thiazolyl or 2-pyridyl. Such compounds show potent inhibition of MMP's, cell-free TNF convertase enzyme and TNF release from cells, and in some cases inhibit TNF convertase and TNF release from cells in preference to matrix metalloproteases.
IPC 1-7
C07D 277/46; A61K 31/425; C07D 213/75; A61K 31/44; C07D 285/12; C07D 239/42; C07D 417/12
IPC 8 full level
A61K 31/42 (2006.01); A61K 31/426 (2006.01); A61K 31/433 (2006.01); A61K 31/4402 (2006.01); A61K 31/4535 (2006.01); A61K 31/505 (2006.01); A61P 1/00 (2006.01); A61P 1/02 (2006.01); A61P 3/10 (2006.01); A61P 19/02 (2006.01); A61P 27/02 (2006.01); A61P 29/00 (2006.01); A61P 35/04 (2006.01); A61P 43/00 (2006.01); C07D 213/75 (2006.01); C07D 239/42 (2006.01); C07D 277/20 (2006.01); C07D 277/46 (2006.01); C07D 285/135 (2006.01); C07D 417/12 (2006.01); C07D 285/12 (2006.01)
CPC (source: EP KR)
A61P 1/00 (2017.12 - EP); A61P 1/02 (2017.12 - EP); A61P 3/10 (2017.12 - EP); A61P 19/02 (2017.12 - EP); A61P 27/02 (2017.12 - EP); A61P 29/00 (2017.12 - EP); A61P 35/04 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07D 213/75 (2013.01 - EP); C07D 239/42 (2013.01 - EP); C07D 277/46 (2013.01 - EP KR); C07D 285/135 (2013.01 - EP); C07D 417/12 (2013.01 - EP)
Citation (search report)
See references of WO 9838179A1
Designated contracting state (EPC)
AT BE CH DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9838179 A1 19980903; AP 9901631 A0 19990930; AR 013070 A1 20001213; AU 6822398 A 19980918; BR 9807763 A 20000222; CA 2281664 A1 19980903; EP 1019386 A1 20000719; HR P980096 A2 19981231; IS 5159 A 19990820; JP 2001513767 A 20010904; KR 20000075681 A 20001226; NO 994103 D0 19990825; NO 994103 L 19991025; PE 59199 A1 19990624; PL 335378 A1 20000425; TR 199902063 T2 19991221; ZA 981532 B 19990824
DOCDB simple family (application)
EP 9801015 W 19980224; AP 9901631 A 19980224; AR P980100842 A 19980225; AU 6822398 A 19980224; BR 9807763 A 19980224; CA 2281664 A 19980224; EP 98913575 A 19980224; HR P980096 A 19980224; IS 5159 A 19990820; JP 53728498 A 19980224; KR 19997007747 A 19990825; NO 994103 A 19990825; PE 00013898 A 19980225; PL 33537898 A 19980224; TR 9902063 T 19980224; ZA 981532 A 19980224