Global Patent Index - EP 1309551 A1

EP 1309551 A1 20030514 - INDOLINE DERIVATIVES AS 5HT2C ANTAGONISTS

Title (en)

INDOLINE DERIVATIVES AS 5HT2C ANTAGONISTS

Title (de)

INDOLIN DERIVATE ALS 5HT2C ANTAGONISTEN

Title (fr)

DERIVES D'INDOLINE EN TANT QU'ANTAGONISTES 5HT2C

Publication

EP 1309551 A1 20030514 (EN)

Application

EP 01976067 A 20010809

Priority

  • EP 0109273 W 20010809
  • GB 0019950 A 20000812

Abstract (en)

[origin: WO0214273A1] The invention relates to novel cinnamide compounds which have 5-HT2C antagonist activity and have the general formula (I), or is a pharmaceutically acceptable salt thereof: in which P is phenyl or naphthyl; R<1> is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkylthio, hydroxy, amino, mono- or di-C1-6alkylamino, nitro, CN, CF3, OCF3, aryl, arylC1-6alkyl, arylC1-6alkyloxy or arylC1-6alkylthio; a is 0, 1, 2, 3, 4 or 5; R<2> and R<3> are independently hydrogen or C1-6alkyl; R<4> is hydrogen, halogen, C1-6alkyl, C1-6alkocy, aryl, cyano, haloC1-6alkyl or OCF3; Z is carbon or nitrogen; R<5> is either: (i) a group NR<6>R<7> where R<6> and R<7> are independently hydrogen, optionally substituted C1-6alkyl; or (ii) an optionally substituted N-linked heterocycle; or (iii) an optionally substituted C-linked heterocycle; n is 0, 1, 2 or 3 subject to the proviso that n is not 0 when R<5> is a group (i) or (ii); <o>---</o> represents a single or double bond; X and Y are independently CR<8>R<9> (when <o>---</o> represents a single bond) or X and Y are independently CR<10> (when <o>---</o> represents a double bond) wherein R<8>, R<9> and R<10> are independently hydrogen or C1-6alkyl. Also disclosed are processes for their preparation, compositions containing them and their use in the treatment of CNS and other disorders.

IPC 1-7

C07D 209/08; C07D 401/12; C07D 403/12; C07D 403/14; C07D 413/12; C07D 417/12; C07D 493/10; A61K 31/4453; A61K 31/496; A61K 31/5377

IPC 8 full level

C07D 491/113 (2006.01); A61K 31/404 (2006.01); A61K 31/438 (2006.01); A61K 31/439 (2006.01); A61K 31/4439 (2006.01); A61K 31/454 (2006.01); A61K 31/4545 (2006.01); A61K 31/496 (2006.01); A61K 31/5377 (2006.01); A61K 31/55 (2006.01); A61P 1/00 (2006.01); A61P 3/10 (2006.01); A61P 9/10 (2006.01); A61P 11/00 (2006.01); A61P 25/00 (2006.01); A61P 25/06 (2006.01); A61P 25/08 (2006.01); A61P 25/20 (2006.01); A61P 25/22 (2006.01); A61P 25/24 (2006.01); A61P 25/28 (2006.01); A61P 25/30 (2006.01); A61P 25/32 (2006.01); A61P 25/36 (2006.01); C07D 209/08 (2006.01); C07D 209/14 (2006.01); C07D 401/12 (2006.01); C07D 403/12 (2006.01); C07D 405/06 (2006.01); C07D 405/12 (2006.01); C07D 413/12 (2006.01); C07D 451/02 (2006.01); C07D 491/08 (2006.01); C07D 491/10 (2006.01)

CPC (source: EP)

A61P 1/00 (2017.12); A61P 3/10 (2017.12); A61P 9/10 (2017.12); A61P 11/00 (2017.12); A61P 25/00 (2017.12); A61P 25/06 (2017.12); A61P 25/08 (2017.12); A61P 25/20 (2017.12); A61P 25/22 (2017.12); A61P 25/24 (2017.12); A61P 25/28 (2017.12); A61P 25/30 (2017.12); A61P 25/32 (2017.12); A61P 25/36 (2017.12); C07D 209/08 (2013.01); C07D 209/14 (2013.01); C07D 401/12 (2013.01); C07D 403/12 (2013.01); C07D 405/06 (2013.01); C07D 405/12 (2013.01); C07D 413/12 (2013.01); C07D 451/02 (2013.01); C07D 491/08 (2013.01); C07D 491/10 (2013.01)

Citation (search report)

See references of WO 0214273A1

Designated contracting state (EPC)

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

DOCDB simple family (publication)

WO 0214273 A1 20020221; AR 030332 A1 20030820; AU 9545501 A 20020225; EP 1309551 A1 20030514; GB 0019950 D0 20000927; JP 2004506040 A 20040226

DOCDB simple family (application)

EP 0109273 W 20010809; AR P010103816 A 20010809; AU 9545501 A 20010809; EP 01976067 A 20010809; GB 0019950 A 20000812; JP 2002519418 A 20010809