Global Patent Index - EP 1066268 A1

EP 1066268 A1 2001-01-10 - 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

EP 1066268 A1 (DE)

Application

EP 99911657 A

Priority

  • DE 19806438 A
  • EP 9900776 W

Abstract (en)

[origin: DE19806438A1] Pyrimidinyloxy-propionic acid derivatives (I) are new. Also new are combinations of (I) with inhibitors of the renin-angiotensin system, beta -blockers, diuretics, calcium antagonists and VEGF blockers. (Pyrimidin-2-yloxy)-propionic acid derivatives of formula (I) and their salts are new: R<1> = tetrazolyl or C(O)R; R = OR<7>, N-bonded heteroaryl optionally substituted with halo, alkyl or alkoxy, -O-(CH2)p-S(O)k-R<8> or -NH-SO2-R<9>; R<7> = H, an alkali or alkaline earth cation, NH4<+>, an organic ammonium ion, cycloalkyl, alkyl, optionally substituted benzyl, optionally halogenated alkenyl or alkynyl or optionally substituted phenyl; R<8> = alkyl, cycloalkyl, alkenyl, alkynyl or optionally substituted phenyl; k = 0-2; p = 1-4; R<9> = optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl or phenyl; R<2> = H, OH, NH2, NH(alkyl), N(alkyl)2, halo, alkyl, alkenyl, alkynyl, hydroxyalkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or morpholinyl; X = halo, haloalkyl or OH; R<3> = H, OH, NH2, NH(alkyl), N(alkyl)2, halo, alkyl, alkenyl, alkynyl, hydroxyalkyl, haloalkyl, alkoxy, haloalkoxy, -NH-O-alkyl or alkylthio; R<4>, R<5> = optionally substituted phenyl or naphthyl; phenyl or naphthyl ortho-linked with one another via a bond, methylene, ethylene, ethenylene, O, S, SO2, NH or N(alkyl); optionally substituted heteroaryl; or cycloalkyl; Z' = S, O, or a single bond; and R<6> = H (when Z = S or O), optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphthyl or heteroaryl. The full definitions are given in the DEFINITIONS (Full Definitions) Field. An Independent claim is also included for combinations of (I) with inhibitors of the renin-angiotensin system, beta -blockers, diuretics, calcium antagonists and VEGF blockers.

IPC 1-7 (main, further and additional classification)

C07D 239/60; A61K 31/505; C07D 239/36; C07D 239/46; C07D 239/52; C07D 401/12; C07D 403/12; C07D 405/12; C07D 409/12; C07D 417/12

IPC 8 full level (invention and additional information)

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 (invention and additional information)

C07D 239/47 (2013.01); C07D 239/60 (2013.01); C07D 403/12 (2013.01)

Citation (search report)

See references of WO 9942453A1

Designated contracting state (EPC)

AT BE CH DE DK ES FI FR GB GR IE IT LI LU NL PT SE

EPO simple patent family

DE 19806438 A1 19990819; AR 014960 A1 20010411; AU 3027199 A 19990906; BG 104577 A 20010330; BR 9907911 A 20001024; CA 2321182 A1 19990826; CN 1291190 A 20010411; EP 1066268 A1 20010110; HR P20000602 A2 20010630; HU 0100957 A2 20020228; HU 0100957 A3 20020328; IL 137038 D0 20010614; JP 2002503726 A 20020205; NO 20004075 A 20000815; NO 20004075 D0 20000815; PL 342311 A1 20010604; SK 11512000 A3 20010409; TR 200002376 T2 20001221; TW 579376 B 20040311; WO 9942453 A1 19990826; ZA 9901214 B 20000816

INPADOC legal status


2004-09-29 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20040330

2003-05-07 [RAP1] TRANSFER OF RIGHTS OF AN EP PUBLISHED APPLICATION

- Owner name: ABBOTT GMBH & CO. KG

2002-11-20 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20021008

2001-01-10 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20000623

2001-01-10 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH DE DK ES FI FR GB GR IE IT LI LU NL PT SE

2001-01-10 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO

- Free text: RO PAYMENT 20000623;SI PAYMENT 20000623