Global Patent Index - EP 1255736 A2

EP 1255736 A2 2002-11-13 - SUBSTITUTED PIPERAZINE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN (MTP)

Title (en)

SUBSTITUTED PIPERAZINE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN (MTP)

Title (de)

SUBSTITUIERTE PIPERAZINDERIVATE UND IHRE VERWENDUNG ALS INHIBITOREN DES MIKROSOMALEN TRIGLYZERID-TRANSFERPROTEINS (MTP)

Title (fr)

DERIVES DE PIPERAZINE SUBSTITUES, LEUR PRODUCTION ET LEUR UTILISATION COMME MEDICAMENTS

Publication

EP 1255736 A2 (DE)

Application

EP 00991607 A

Priority

  • DE 19963234 A
  • EP 0012843 W

Abstract (en)

[origin: DE19963234A1] N,N-Disubstituted piperazine and diazacycloheptane derivatives (I) are new. N,N-disubstituted piperazine and diazacycloheptane derivatives of formula (I) and their isomers and salts are new. m = 1-2; n = 1-5; X = C-C bond, O, -CH2-, -CH2-CH2-, -NH- or -N(1-3C alkyl)-; Ra = bi- or tricyclic aryl, C-bonded bi- or tricyclic heteroaryl comprising a 5-membered heteroaryl containing 1-2 N fused via a vinylene group with a cyclopentadiene group optionally containing N in place of 1 CH, a 5-membered heteroaryl containing O, S, NH or N(Rx) fused via 1-2 vinylene groups either with phenyl and/or 6-membered heteroaryl containing 1-3 N or via 1-2 vinylene groups with naphthyl, or a 5-membered heteroaryl containing O, S, NH or N(Rx) and 1-2 N fused via a vinylene group with phenyl, naphthyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl, naphthyl or 6-membered heteroaryl containing 1-3 N fused via a vinylene group with pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl, phenyl fused via 1-2 vinylene groups with 6-membered heteroaryl containing 1-3 N, or pyridyl, pyrazinyl or pyridazinyl fused via 2 vinylene groups with phenyl or 6-membered heteroaryl containing 1-3 N; Rx = 1-3C alkyl, phenyl-1-3C alkyl, phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; Rb, Rc = H or 1-3C alkyl; Rf, Rg = H, or 1-6C alkyl optionally containing 1 or more F, 3-7C cycloalkyl, Ar, 1-3C alkoxy-CO-1-2C alkyl, COOH-1-2C alkyl, methoxy-2-3C alkyl, or Ar-1-3C alkyl; or NRfRg = 3-7 membered cycloalkyleneimino optionally containing O, S, SO, SO2, NH or N(1-3C alkyl) in the 4-position when 6- or 7-membered; Ar = phenyl or heteroaryl (both optionally C-substituted with 1-3 F, Cl, Br, 1-3C alkyl or 1-3C alkoxy (each optionally substituted with 1 or more F), OH, COOH, 1-3C alkoxycarbonyl, CONH2, CONH(1-3C alkyl), CON(1-3C alkyl)2, NO2 and/or NH2 and (when heteroaryl) optionally substituted on 1 N by 1-3C alkyl (optionally substituted with 1 or more F), 1-3C alkyl-CO or 1-4C alkoxy-CO; provided that an angular CH in Ra is optionally replaced with N; bi- and tricyclic groups are optionally C-substituted with 1-2 F, Cl, Br, I, 1-3C alkyl, OH, 1-3C alkoxy, COOH, 1-3C alkoxycarbonyl, CONH2, CONH(1-3C alkyl) and/or CON(1-3C alkyl)2; and alkyl and alkoxy are optionally substituted with 1 or more F; and the tricyclic group containing X is optionally substituted with 1-2 F, Cl, CH3 and/or OCH3. An Independent claim is included for the preparation of compounds (I).

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

C07D 215/38

IPC 8 full level (invention and additional information)

C07D 295/14 (2006.01); A61K 31/496 (2006.01); A61K 31/498 (2006.01); A61K 31/517 (2006.01); A61K 31/5377 (2006.01); A61K 31/551 (2006.01); A61P 3/06 (2006.01); A61P 9/10 (2006.01); C07D 215/38 (2006.01); C07D 235/30 (2006.01); C07D 239/84 (2006.01); C07D 241/44 (2006.01); C07D 263/58 (2006.01); C07D 277/82 (2006.01); C07D 295/145 (2006.01); C07D 401/12 (2006.01); C07D 409/12 (2006.01); C07D 471/04 (2006.01)

CPC (invention and additional information)

C07D 295/145 (2013.01); C07C 2603/18 (2017.05)

Designated contracting state (EPC)

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

EPO simple patent family

DE 19963234 A1 20020124; AU 3364101 A 20010709; CA 2395249 A1 20010705; CO 5251385 A1 20030228; EP 1255736 A2 20021113; JP 2003521484 A 20030715; JP 4005362 B2 20071107; MX PA02006231 A 20021205; US 2003166637 A1 20030904; US 6821967 B2 20041123; UY 26505 A1 20010731; WO 0147898 A2 20010705; WO 0147898 A3 20020404

INPADOC legal status


2009-08-26 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20090303

2008-07-02 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20080529

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

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

2002-12-04 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20021004

2002-11-13 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A2

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

2002-11-13 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO

- Free text: AL;LT;LV;MK;RO;SI