Global patent index - EP 1084123 A1

EP 1084123 A1 2001-03-21 - NOVEL ASYMMETRICALLY SUBSTITUTED XANTHINE DERIVATIVES, METHOD FOR PRODUCING THEM AND THEIR USE AS MEDICAMENTS WITH AN ADENOSINE-ANTAGONISTIC EFFECT

Title (en)

NOVEL ASYMMETRICALLY SUBSTITUTED XANTHINE DERIVATIVES, METHOD FOR PRODUCING THEM AND THEIR USE AS MEDICAMENTS WITH AN ADENOSINE-ANTAGONISTIC EFFECT

Title (de)

NEUE UNSYMMETRISCH SUBSTITUIERTE XANTHIN-DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL MIT ADENOSINANTAGONISTISCHER WIRKUNG

Title (fr)

NOUVEAUX DERIVES DE XANTHINE A SUBSTITUTION ASYMETRIQUE, LEUR PROCEDE DE PREPARATION ET LEUR UTILISATION COMME MEDICAMENTS A EFFET ANTAGONISTE DE L'ADENOSINE

Publication

EP 1084123 A1 (DE)

Application

EP 99916914 A

Priority

  • DE 19816857 A
  • EP 9902458 W

Abstract (en)

[origin: DE19816857A1] 3,8-Disubstituted-xanthines (I) are new. They are prepared via new intermediates (IA). 3-alk(en or yn)yl-8-(alkyl or bridged cycloalkyl)-xanthines (I). as racemates, enantiomers, diastereomers and mixtures, and their addition salts are new: a or b = double bond; R<1> = H; 1-6C alkyl; 3-6C alkenyl; or 3-6C alkynyl; R<2> = 1-6C alkyl, 3-6C alkenyl or 3-6C alkynyl substituted with OR<6>, SO2R<6>, OCOR<9>, COOR<9>, NR<7>R<8>, O(CH2)2-NR<7>R<8>, CONR<7>R<8>, OCH2CONR<7>R<8> or O(CH2)2-CONR<7>R<8> or optionally substituted with C-bonded 5-6 membered heterocyclic ring containing 1-4 O, N and/or S atoms and optionally substituted with 1-4C alkyl or benzyl; R<3> = 1-6C alkyl optionally substituted with OH; or norbornanyl, norbornenyl, adamantyl or noradamantyl optionally substituted with Me or OH; R<4> and R<5> (not present simultaneously) = H or benzyl optionally substituted with 1-3 OMe; R<6> = H or 3-6C cycloalkyl or 1-4C alkyl optionally substituted with OR<9> or OCOR<9>; R<7> and R<8> = H; SO2R<6>; 1-4C alkyl; COR<9>; or COOR<9>; or NR<7>R<8> forms a 5-6 membered ring containing a further N atom or an O atom and optionally substituted with 1-4C alkyl or benzyl; compounds are excluded when R<1> = R<2>. Independent claims are also included for the following: (1) the preparation of compounds (I); and (2) the intermediates of formula (IA): R<2>' = H or 1-6C alkyl, 3-6C alkenyl or 3-6C alkynyl substituted with CN, halo, 1-6C alkoxy, CH3SO2O, CF3SO2O or p-tosyloxy.

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

C07D 473/06; A61K 31/52

IPC 8 full level (invention and additional information)

A61K 31/522 (2006.01); A61K 31/5377 (2006.01); A61P 7/10 (2006.01); A61P 9/06 (2006.01); A61P 9/10 (2006.01); A61P 11/00 (2006.01); A61P 11/06 (2006.01); A61P 13/12 (2006.01); A61P 25/00 (2006.01); A61P 25/06 (2006.01); A61P 25/16 (2006.01); A61P 25/20 (2006.01); A61P 25/22 (2006.01); A61P 25/24 (2006.01); A61P 25/28 (2006.01); A61P 43/00 (2006.01); C07D 473/04 (2006.01); C07D 473/06 (2006.01)

CPC (invention and additional information)

C07D 473/06 (2013.01); C07D 473/04 (2013.01)

Citation (search report)

See references of WO 9954331A1

Designated contracting state (EPC)

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

EPO simple patent family

DE 19816857 A1 19991021; CA 2328264 A1 19991028; EP 1084123 A1 20010321; JP 2002512246 A 20020423; WO 9954331 A1 19991028

INPADOC legal status

2004-08-04 [18D] DEEMED TO BE WITHDRAWN

- Ref Legal Event Code: 18D

- Effective date: 20040203

2003-09-03 [17Q] FIRST EXAMINATION REPORT

- Ref Legal Event Code: 17Q

- Effective date: 20030721

2003-03-26 [RAP1] TRANSFER OF RIGHTS OF AN EP PUBLISHED APPLICATION

- Owner name: BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG

- Ref Legal Event Code: RAP1

2001-03-21 [17P] REQUEST FOR EXAMINATION FILED

- Ref Legal Event Code: 17P

- Effective date: 20001116

2001-03-21 [AK] DESIGNATED CONTRACTING STATES:

- Ref Legal Event Code: AK

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