Global Patent Index - EP 1037883 A1

EP 1037883 A1 2000-09-27 - NOVEL HETEROCYCLICALLY SUBSTITUTED $g(a)-HYDROXYCARBOXLIC ACID DERIVATIVES, METHOD FOR PRODUCING THE SAME AND THEIR USE AS ENDOTHELIN RECEPTOR ANTAGONISTS

Title (en)

NOVEL HETEROCYCLICALLY SUBSTITUTED $g(a)-HYDROXYCARBOXLIC ACID DERIVATIVES, METHOD FOR PRODUCING THE SAME AND THEIR USE AS ENDOTHELIN RECEPTOR ANTAGONISTS

Title (de)

NEUE HETEROCYCLISCH SUBSTITUIERTE $g(a)-HYDROXYCARBONSÄUREDERIVATE, IHRE HERSTELLUNG UND VERWENDUNG ALS ENDOTHELINREZEPTORANTAGONISTEN

Title (fr)

NOUVEAUX DERIVES D'ACIDE $g(a)-HYDROXYCARBOXYLIQUE HETEROCYCLIQUEMENT SUBSTITUES, LEUR PRODUCTION ET LEUR UTILISATION COMME ANTAGONISTES DU RECEPTEUR DE L'ENDOTHELINE

Publication

EP 1037883 A1 (DE)

Application

EP 98958900 A

Priority

  • DE 19750529 A
  • EP 9807026 W

Abstract (en)

[origin: DE19750529A1] Heterocyclic alpha -hydroxycarboxylic acid derivatives (I) are new. Heterocyclic alpha -hydroxycarboxylic acid derivatives of formula (I) and their salts, enantiomers and diastereomers are new. R<1> = tetrazolyl or CO-R; R = OR<5>, a 5-membered heteroaromatic group bound via an N atom, -O-(CH2)p-S(O)k-R<6> or -NH-SO2-R<7>; A = NR<8>R<9>, N3, OR<10>, SR<10> or 1-4C alkyl; X = O, S, CR<11> or NR<12>, provided that if X = CR<11>, then Y = O, S or NR<14>; Y = O, S, CR<13> or NR<14>; R<2>, R<3> = independently phenyl or naphthyl (which are optionally substituted or optionally bound via a methylene, ethylene, ethenylene, O, S, SO2, NH or N(1-4C alkyl) group) or 5- or 6C cycloalkyl; R<4>, R<11> = H, halo, or optionally substituted 1-4C alkoxy, 1-4C haloalkoxy, 3-6C alkenyloxy, 3-6C alkynyloxy, 1-4C alkylthio, (1-4C alkyl)carbonyl, (1-4C alkoxy)carbonyl, OH, NH2, NH(1-4C alkyl), N(1-4C alkyl)2, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, or CR<4> and CR<11> together form a 5- or 6-membered alkylene or alkenylene ring, which is optionally substituted and one or more of whose CH2 groups may be replaced by O, S, NH or N(1-4C alkyl); R<5> = H, an alkali or alkaline earth metal cation or an organic ammonium ion, or 3-8C cycloalkyl, 1-8C alkyl, benzyl, 3-8C alkenyl, 3-8C alkynyl or optionally substituted phenyl; k = 0-2; p = 1-4; R<6> = 1-4C alkyl, 3-8C cycloalkyl, 3-8C alkenyl, 3-8C alkynyl or optionally substituted phenyl; R<7> = 1-4C alkyl, 3-8C cycloalkyl, 3-8C alkenyl, 3-8C alkynyl, 1-4C haloalkyl or phenyl (all optionally substituted); R<8> = H, 1-8C alkyl, 3-8C alkenyl, 3-8C alkynyl or (1-5C alkyl)carbonyl, phenyl, naphthyl or 3-8C cycloalkyl (all optionally substituted), or R<8> and R<9> together form a 3-7C alkylene chain which may be substituted and whose alkylene chain may contain O or S atoms; R<9> = H or 1-4C alkyl; R<10> = H, 1-8C alkyl, 3-8C alkenyl, 3-8C alkynyl, phenyl, naphthyl or 3-8C cycloalkyl (all optionally substituted); R<12> = H or 1-4C alkyl, or NR<12> and CR<4> together form a 5- or 6-membered alkylene or alkenylene ring, which is optionally substituted and one or more of whose CH2 groups may be replaced by O or S; R<13> = H, halo, 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl (all optionally substituted); R<14> = H or 1-4C alkyl.

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

C07D 277/34; A61K 31/42; A61K 31/425; C07D 263/38; C07D 277/60; C07D 277/68

IPC 8 full level (invention and additional information)

C07D 249/12 (2006.01); A61K 31/41 (2006.01); A61K 31/415 (2006.01); A61K 31/4164 (2006.01); A61K 31/42 (2006.01); A61K 31/421 (2006.01); A61K 31/422 (2006.01); A61K 31/4245 (2006.01); A61K 31/425 (2006.01); A61K 31/426 (2006.01); A61K 31/427 (2006.01); A61K 31/428 (2006.01); A61K 31/433 (2006.01); A61P 9/04 (2006.01); A61P 9/08 (2006.01); A61P 9/10 (2006.01); A61P 9/12 (2006.01); A61P 11/06 (2006.01); A61P 13/08 (2006.01); A61P 13/12 (2006.01); A61P 35/00 (2006.01); A61P 43/00 (2006.01); C07D 231/20 (2006.01); C07D 233/70 (2006.01); C07D 261/12 (2006.01); C07D 263/38 (2006.01); C07D 271/06 (2006.01); C07D 271/10 (2006.01); C07D 273/01 (2006.01); C07D 275/02 (2006.01); C07D 275/03 (2006.01); C07D 277/20 (2006.01); C07D 277/32 (2006.01); C07D 277/34 (2006.01); C07D 277/60 (2006.01); C07D 277/68 (2006.01); C07D 285/00 (2006.01); C07D 285/08 (2006.01); C07D 285/12 (2006.01); C07D 291/04 (2006.01); C07D 413/12 (2006.01); C07D 417/12 (2006.01)

CPC (invention and additional information)

C07D 275/03 (2013.01); C07D 261/12 (2013.01); C07D 263/38 (2013.01); C07D 277/34 (2013.01); C07D 277/60 (2013.01); C07D 277/68 (2013.01)

Citation (search report)

See references of WO 9925701A1

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 19750529 A1 19990520; AR 017581 A1 20010912; AU 1487899 A 19990607; AU 752165 B2 20020905; BG 104400 A 20010131; BR 9814157 A 20001003; CA 2308746 A1 19990527; CN 1278805 A 20010103; CO 4990973 A1 20001226; EP 1037883 A1 20000927; HR P980591 A2 19990831; HU 0004341 A2 20011028; HU 0004341 A3 20011228; ID 24819 A 20000824; IL 135461 D0 20010520; JP 2001523671 A 20011127; NO 20002154 A 20000512; NO 20002154 D0 20000427; NZ 504289 A 20020301; PL 340756 A1 20010226; SK 4932000 A3 20010212; TR 200001365 T2 20000921; US 6358983 B1 20020319; WO 9925701 A1 19990527; ZA 9810425 B 20000515

INPADOC legal status


2004-09-08 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20040303

2003-12-10 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20031023

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

- Owner name: ABBOTT GMBH & CO. KG

2000-09-27 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20000411

2000-09-27 [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

2000-09-27 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO

- Free text: RO PAYMENT 20000411;SI PAYMENT 20000411