Global Patent Index - EP 1490324 A4

EP 1490324 A4 2007-10-10 - PROPARGYLAMINO INDAN DERIVATIVES AND PROPARGYLAMINO TETRALIN DERIVATIVES AS BRAIN-SELECTIVE MAO INHIBITORS

Title (en)

PROPARGYLAMINO INDAN DERIVATIVES AND PROPARGYLAMINO TETRALIN DERIVATIVES AS BRAIN-SELECTIVE MAO INHIBITORS

Title (de)

PROPARGYLAMINOINDANDERIVATE UND PROPARGYLAMINOTETRALINDERIVATE ALS HIRNSELEKTIVE MAO-INHIBITOREN

Title (fr)

DERIVES DE PROPARGYLAMINOINDANE ET DERIVES DE PROPARGYLAMINOTETRALINE UTILISES COMME INHIBITEURS DE LA MAO CEREBRO-SELECTIFS

Publication

EP 1490324 A4 (EN)

Application

EP 03716197 A

Priority

  • US 0305871 W
  • US 8567402 A

Abstract (en)

[origin: WO03072055A2] The subject invention provides derivatives of propargylamino indan (PAI) and propargylamino tetralin that selectively inhibit monoamine oxidase (MAO) in the brain, having the structure:, wherein R1 is OC (O) R9 and R2 is H, wherein R9 i s branched or unbranched C1 to C6 alkyl, aryl, or aralkyl, or R1 is OC (O) R4 and R2 is OC (O) R4, wherein R4 is branched or unbranched C1 to C6 alkyl, aryl, aralkyl or NR5R6, wherein R5 and R6 are each independently H, C1 to C8 alkyl, C6 to C12 aryl, C6 to C12 aralkyl or C6 to C12 cycloalkyl, each optionally substituted; wherein R3 is H or C1 to C6 alkyl; wherein n is 0 or 1; and wherein m is 1 or 2, or a pharmaceutically acceptable salt thereof. Additionally, the subject invention provides methods of treating neurological disorders using these compounds, uses of these compounds for the manufacture of medicaments for treating neurological disorders and processes for synthesis of these compounds.

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

C07C 211/00; C07C 261/00; C07C 269/00; C07C 271/00; A01N 33/02; A01N 47/10; A61K 31/27; A61K 31/135

IPC 8 full level (invention and additional information)

A61P 15/10 (2006.01); A61K 31/216 (2006.01); A61K 31/22 (2006.01); A61P 21/00 (2006.01); A61P 25/00 (2006.01); A61P 25/08 (2006.01); A61P 25/16 (2006.01); A61P 25/24 (2006.01); A61P 25/28 (2006.01); A61P 43/00 (2006.01); C07C 215/64 (2006.01); C07C 219/26 (2006.01); C07C 271/44 (2006.01); C07D 265/12 (2006.01)

CPC (invention and additional information)

C07C 215/64 (2013.01); C07C 219/26 (2013.01); C07D 265/12 (2013.01); C07C 2602/08 (2017.05)

Citation (search report)

  • [X] WO 9311761 A1 19930624 - LUNDBECK & CO AS H [DK]
  • [PX] STERLING, JEFFREY ET AL: "Novel Dual Inhibitors of AChE and MAO Derived from Hydroxy Aminoindan and Phenethylamine as Potential Treatment for Alzheimer's Disease", JOURNAL OF MEDICINAL CHEMISTRY , 45(24), 5260-5279 CODEN: JMCMAR; ISSN: 0022-2623, 2002, XP002296523
  • [X] HAZELHOFF, BERNARD ET AL: "N-Methyl,N-propargyl-2-aminotetralins: novel dopamine agonists with monoamine oxidase inhibiting properties", EUROPEAN JOURNAL OF PHARMACOLOGY , 109(2), 229-40 CODEN: EJPHAZ; ISSN: 0014-2999, 1985, XP002434896
  • [X] DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; CHUMPRADIT, SUMALEE ET AL: "Synthesis and optical resolution of (R)- and (S)-trans-7-hydroxy-2- [N-propyl-N-(3'-iodo-2'-propenyl)amino]tetralin: a new D3 dopamine receptor ligand", XP002434898, retrieved from STN Database accession no. 1994:8313 & JOURNAL OF MEDICINAL CHEMISTRY , 36(26), 4308-12 CODEN: JMCMAR; ISSN: 0022-2623, 1993JOURNAL OF MEDICINAL CHEMISTRY , 36(26), 4308-12 CODEN: JMCMAR; ISSN: 0022-26231993
  • See also references of WO 03072055A3

Designated contracting state (EPC)

AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LI LU MC NL PT SE SI SK TR

Designated extension state (EPC)

AL LT LV MK RO

EPO simple patent family

WO 03072055 A2 20030904; WO 03072055 A3 20031231; AU 2003219913 A1 20030909; AU 2003219913 A8 20030909; CA 2477218 A1 20030904; EP 1490324 A2 20041229; EP 1490324 A4 20071010; JP 2005523289 A 20050804

INPADOC legal status


2010-12-29 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20100619

2008-12-17 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20081112

2007-10-10 [A4] SUPPLEMENTARY SEARCH REPORT

- Effective date: 20070907

2004-12-29 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20040923

2004-12-29 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A2

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

2004-12-29 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO

- Countries: AL LT LV MK RO