EP 2150543 A2 20100210 - HETEROCYCLIC COMPOUNDS WITH AFFINITY TO MUSCARINIC RECEPTORS
Title (en)
HETEROCYCLIC COMPOUNDS WITH AFFINITY TO MUSCARINIC RECEPTORS
Title (de)
HETEROCYCLISCHE VERBINDUNGEN MIT AFFINITÄT ZU MUSKARINREZEPTOREN
Title (fr)
COMPOSÉS HÉTÉROCYCLIQUES AVEC AFFINITÉ DES RÉCEPTEURS MUSCARINIQUES
Publication
Application
Priority
- EP 2008054897 W 20080423
- EP 07106814 A 20070424
- US 91358407 P 20070424
- EP 08759382 A 20080423
Abstract (en)
[origin: WO2008129054A2] The present invention relates to heterocyclic compounds of the formula (I) wherein - the heterocycle comprises two double bonds which may be present at several positions, represented by the dashed lines ( -- ); - the heterocycle contains two heteroatoms, - W being N or NH; - Y being CH, O or NH, wherein if Y is O, X<SUB>1</SUB> is CH and X<SUB>2</SUB> is the residue C-Z-R2 or C-R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X<SUB>1</SUB> and X<SUB>2</SUB> is CH or N, the other being the residue C-Z-R2 or C-R3, wherein Z is NH or S; - R1 is selected from the structures (a), (b) and (c): - R2 is selected from (C<SUB>1</SUB>-C<SUB>10</SUB>)alkyl, (C<SUB>2</SUB>-C<SUB>10</SUB>)alkenyl and (C<SUB>2</SUB>-C<SUB>10</SUB>)alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, oxo, (C<SUB>1</SUB>-C<SUB>6</SUB>)alkoxy, (C<SUB>1</SUB>-C<SUB>6</SUB>)alkylthio, (C<SUB>1</SUB>-C<SUB>6</SUB>)alkenyloxy, (C<SUB>1</SUB>-C<SUB>6</SUB>)alkenylthio, (C<SUB>1</SUB>-C<SUB>4</SUB>)alkoxy(C<SUB>1</SUB>-C<SUB>4</SUB>)alkoxy, (C<SUB>5</SUB>-C<SUB>7</SUB>)cycloalkyl, a 5-membered unsaturated heterocycle (optionally substituted with halogen), phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or - R2 is an unbranched (C<SUB>2</SUB>-C<SUB>8</SUB>)alkyl substituted at the Za-symbol of a group with the formula (Ia) wherein if X<SUB>1 </SUB>is CH or N<SUB>1</SUB> X<SUB>1</SUB> is CH or N and X<SUB>2</SUB>a is C-Za-, or if X<SUB>1</SUB> is C-Z-R2, X<SUB>1</SUB>a is C-Za- and X<SUB>2</SUB>a is CH or N; and the symbols Wa, Ya and Za and the substituent R1a have the same meanings as defined previously for the symbols W, Y and Z and the substituent R1, and are not independently selected, each of the symbols Wa, Ya and Za and the substituent R1 a representing identical symbols and substituents, respectively, as the symbols W, Y and Z and the substituent R1 in the other part of the structure of formula (I); - R3 is selected from (C<SUB>4</SUB>-C<SUB>10</SUB>) alkyl, (C<SUB>2</SUB>-C<SUB>10</SUB>) alkenyl and (C<SUB>2</SUB>-C<SUB>10</SUB>) alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, (C<SUB>1</SUB>C<SUB>6</SUB>) alkoxy, (C<SUB>1</SUB>C<SUB>6</SUB>) alkylthio, (C<SUB>1</SUB>C<SUB>6</SUB>)alkenyloxy, (C<SUB>1</SUB>C<SUB>6</SUB>) alkenylthio, (C<SUB>1</SUB>-C<SUB>4</SUB>) alkoxy (C<SUB>1</SUB>-C<SUB>4</SUB>) alkoxy, (C<SUB>5</SUB>-C<SUB>7</SUB>) cycloalkyl, a 5-membered unsaturated heterocycle optionally substituted with halogen, phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to muscarinic receptors and may be used in the treatment, alleviation or prevention of muscarinic receptor mediated diseases and conditions.
IPC 8 full level
C07D 401/04 (2006.01); A61K 31/439 (2006.01); A61K 31/4427 (2006.01); A61K 31/4439 (2006.01); A61P 25/28 (2006.01); C07D 401/14 (2006.01); C07D 413/04 (2006.01); C07D 453/02 (2006.01); C07D 471/08 (2006.01)
CPC (source: EP)
A61P 25/18 (2017.12); A61P 25/28 (2017.12); C07D 401/04 (2013.01); C07D 401/14 (2013.01); C07D 413/04 (2013.01); C07D 453/02 (2013.01); C07D 471/08 (2013.01)
Citation (search report)
See references of WO 2008129054A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA MK RS
DOCDB simple family (publication)
WO 2008129054 A2 20081030; WO 2008129054 A3 20090205; AU 2008240704 A1 20081030; CA 2682994 A1 20081030; CN 101939311 A 20110105; EP 2150543 A2 20100210; JP 2010525020 A 20100722; MX 2009011499 A 20091109; RU 2009143353 A 20110527; RU 2446166 C2 20120327
DOCDB simple family (application)
EP 2008054897 W 20080423; AU 2008240704 A 20080423; CA 2682994 A 20080423; CN 200880016526 A 20080423; EP 08759382 A 20080423; JP 2010504671 A 20080423; MX 2009011499 A 20080423; RU 2009143353 A 20080423