EP 1066268 A1 20010110 - 5-SUBSTITUTED PYRIMIDINE-2-YLOXY CARBOXYLIC ACID DERIVATIVES, THE PRODUCTION OF THE SAME AND THEIR UTILIZATION AS ENDOTHELIN ANTAGONISTS
Title (en)
5-SUBSTITUTED PYRIMIDINE-2-YLOXY CARBOXYLIC ACID DERIVATIVES, THE PRODUCTION OF THE SAME AND THEIR UTILIZATION AS ENDOTHELIN ANTAGONISTS
Title (de)
5-SUBSTITUIERTE PYRIMIDIN-2-YLOXY-CARBONSÄUREDERIVATE, DEREN HERSTELLUNG UND DEREN VERWENDUNG ALS ENDOTHELIN-ANTAGONISTEN
Title (fr)
DERIVES D'ACIDE PYRIMIDIN-2-YLOXY-CARBOXYLIQUE, LEUR PRODUCTION ET LEUR UTILISATION COMME ANTAGONISTES DE L'ENDOTHELINE
Publication
Application
Priority
- DE 19806438 A 19980217
- EP 9900776 W 19990205
Abstract (en)
[origin: WO9942453A1] The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the following meanings; R<1>= tetrazole or a group (1); R = a radical OR<7>(2), (3), a 5-membe red heteroaromatic bonded by a nitrogen atom such a pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R<2>, R<3> = hydrogen, hydroxy, NH2, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, C1-C4-halogen alkyl, C1-C4-alkoxy, C1-C4-halogen alkoxy or C1-C4-alkythio; X = halogen, C1-C4-halogen alkyl, hydroxy; R<4> and R<5> = phenyl or naphthyl, C3-C7-cycloalkyl, phenyl or naphthyl which are bonded in ortho position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO2-NH or an N-alkyl group or a 5-membered or 6-membered heteroaromatic; R<6> = hydrogen, phenyl or naphthyl, a five or six-membered heteroaromatic, C1-C8-alkyl, C3-C6-alkenyl, C3-C6-alkinyl or C3-C8-cycloalkyl, whereby said radicals can be substituted once or many times, with the proviso that R<6> can only stand for hydrogen if Z does not represent a single bond; Z = sulfur, oxygen or a single bond, in addition to the physiologically compatible salts and the enantiomeric-pure and diastereomeric-pure forms. The novel compounds are suitable for combating diseases, especially as endothelin antagonists.
IPC 1-7
C07D 239/60; A61K 31/505; C07D 239/46; C07D 239/52; C07D 239/36; C07D 405/12; C07D 417/12; C07D 403/12; C07D 409/12; C07D 401/12
IPC 8 full level
A61K 31/505 (2006.01); A61K 31/506 (2006.01); A61P 5/14 (2006.01); A61P 9/02 (2006.01); A61P 9/10 (2006.01); A61P 9/12 (2006.01); A61P 11/06 (2006.01); A61P 13/12 (2006.01); A61P 35/00 (2006.01); A61P 43/00 (2006.01); C07D 239/34 (2006.01); C07D 239/46 (2006.01); C07D 239/52 (2006.01); C07D 239/60 (2006.01); C07D 401/12 (2006.01); C07D 403/12 (2006.01); C07D 405/12 (2006.01); C07D 409/12 (2006.01); C07D 417/12 (2006.01)
CPC (source: EP KR)
A61P 5/14 (2018.01 - EP); A61P 9/00 (2018.01 - EP); A61P 9/02 (2018.01 - EP); A61P 9/04 (2018.01 - EP); A61P 9/10 (2018.01 - EP); A61P 9/12 (2018.01 - EP); A61P 11/00 (2018.01 - EP); A61P 11/06 (2018.01 - EP); A61P 13/12 (2018.01 - EP); A61P 35/00 (2018.01 - EP); A61P 43/00 (2018.01 - EP); C07D 239/47 (2013.01 - EP KR); C07D 239/60 (2013.01 - EP KR); C07D 403/12 (2013.01 - EP KR)
Designated contracting state (EPC)
AT BE CH DE DK ES FI FR GB GR IE IT LI LU NL PT SE
DOCDB simple family (publication)
WO 9942453 A1 19990826; AR 014960 A1 20010411; AU 3027199 A 19990906; BG 104577 A 20010330; BR 9907911 A 20001024; CA 2321182 A1 19990826; CN 1291190 A 20010411; DE 19806438 A1 19990819; EP 1066268 A1 20010110; HR P20000602 A2 20010630; HU P0100957 A2 20020228; HU P0100957 A3 20020328; IL 137038 A0 20010614; JP 2002503726 A 20020205; KR 20010086247 A 20010910; NO 20004075 D0 20000815; NO 20004075 L 20000815; PL 342311 A1 20010604; SK 11512000 A3 20010409; TR 200002376 T2 20001221; TW 579376 B 20040311; ZA 991214 B 20000816
DOCDB simple family (application)
EP 9900776 W 19990205; AR P990100634 A 19990216; AU 3027199 A 19990205; BG 10457700 A 20000704; BR 9907911 A 19990205; CA 2321182 A 19990205; CN 99803037 A 19990205; DE 19806438 A 19980217; EP 99911657 A 19990205; HR P20000602 A 20000913; HU P0100957 A 19990205; IL 13703899 A 19990205; JP 2000532405 A 19990205; KR 20007008925 A 20000816; NO 20004075 A 20000815; PL 34231199 A 19990205; SK 11512000 A 19990205; TR 200002376 T 19990205; TW 88102031 A 19990210; ZA 991214 A 19990216