EP 1931647 A2 20080618 - SELECTED CGRP ANTAGONISTS, METHODS FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICAMENTS
Title (en)
SELECTED CGRP ANTAGONISTS, METHODS FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICAMENTS
Title (de)
AUSGEWÄHLTE CGRP-ANTAGONISTEN, VERFAHREN ZU DEREN HERSTELLUNG SOWIE DEREN VERWENDUNG ALS ARZNEIMITTEL
Title (fr)
ANTAGONISTES DE CGRP SELECTIONNES, PROCEDE POUR LES PREPARER ET LEUR UTILISATION COMME AGENTS PHARMACEUTIQUES
Publication
Application
Priority
- EP 2006066783 W 20060927
- EP 05021236 A 20050929
- EP 06806843 A 20060927
Abstract (en)
[origin: EP1770086A1] Substituted piperidine compounds (I) and their tautomers and salts are new. Substituted piperidine compounds of formula (I) and their tautomers and salts are new. R 1>substituted 3,4-dihydro-1H-quinazolin-2-one compound of formula (1a), substituted 1,3,4,5-tetrahydro-benzo[d][1,3]diazepin-2-one compound of formula (2a) or 5-phenyl-2,4-dihydro-[1,2,4]triazol-3-one compound of formula (3a); R 1> 1>H or H 3C-O-; R 2>substituted toluene compound of formula (4a); R 2> 1>HO, H 3CO, H-C(O)-O or H 3C-C(O)-O-; R 2> 2>1-2C alkyl or H 3CO-; R 3>R4a-2-8C alkylene-NH- or heterocyclic compounds of formulae (5a-6a); R4a : H, H 2N, 13C-alkyl-NH, (1-3C alkyl) 2-N or 1-6C alkyl-O-C(O)-NH-; R 3> 2>, R 3> 4>H or 1-3C alkyl; R 3> 3>free electron pair or oxygen atom; R4b : H, 1-6C alkyl, H 2N-2-6C alkylene, 1-3C alkyl-NH-2-6C alkylene, (1-3C alkyl) 2-N-1-6C-alkylene, 3-6C cycloalkyl-1-3C-alkylene, NH 2, 1-3C alkyl-NH or (1-3C alkyl) 2-N; R 4>7 cyclic compounds e.g. heterocyclic compounds of formulae (7a-10a); and R 4> 2>R 3> 2>. Provided that: when X is C, R 4> 1> is H, OH or 1-3C alkyl; when X is N, R 4> 1> is a free electron pair or an oxygen atom; if X is N, then Y 1> is O, S, S(O), S(O) 2; if X is C, then Y 1> is S, S(O), S(O) 2; and provided that R 3> and R 4> are not bound to one another simultaneously via an N atom. [Image] [Image] [Image] [Image] ACTIVITY : Analgesic; Antidiabetic; Antiarthritic; Osteopathic; Antirheumatic; Antiallergic; Antiinflammatory; Antiasthmatic; Gastrointestinal-Gen.; Vasotropic; Antibacterial; Immunosuppressive; Dermatological; Vulnerary; Antipruritic; Cardiovascular-Gen. MECHANISM OF ACTION : Calcitonin gene related peptide (CGRP) receptor-antagonist. The ability of (I) to antagonize CGRP receptor was tested in SK-N-MC cells. The result showed that the IC 5 0 value of (I) was >= 10000 nM.
IPC 8 full level
C07D 249/12 (2006.01); C07D 243/10 (2006.01); C07D 401/12 (2006.01); C07D 403/12 (2006.01)
CPC (source: EP KR US)
A61P 1/04 (2017.12 - EP); A61P 1/12 (2017.12 - EP); A61P 3/10 (2017.12 - EP); A61P 5/00 (2017.12 - EP); A61P 5/50 (2017.12 - EP); A61P 9/00 (2017.12 - EP); A61P 11/00 (2017.12 - EP); A61P 11/02 (2017.12 - EP); A61P 11/06 (2017.12 - EP); A61P 17/00 (2017.12 - EP); A61P 17/04 (2017.12 - EP); A61P 19/02 (2017.12 - EP); A61P 25/06 (2017.12 - EP); A61P 29/00 (2017.12 - EP); A61P 31/04 (2017.12 - EP); A61P 37/08 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07D 243/10 (2013.01 - EP KR US); C07D 249/12 (2013.01 - EP KR US); C07D 401/12 (2013.01 - EP KR US); C07D 403/12 (2013.01 - EP KR US)
Citation (search report)
See references of WO 2007036532A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR
DOCDB simple family (publication)
EP 1770086 A1 20070404; AR 056205 A1 20070926; AU 2006296541 A1 20070405; CA 2623156 A1 20070405; CN 101273021 A 20080924; EP 1931647 A2 20080618; IL 190423 A0 20081103; JP 2009510022 A 20090312; KR 20080056252 A 20080620; RU 2008116320 A 20091110; TW 200800922 A 20080101; US 2007072847 A1 20070329; US 2009253680 A1 20091008; US 7582625 B2 20090901; US 7897603 B2 20110301; WO 2007036532 A2 20070405; WO 2007036532 A3 20070621; ZA 200800431 B 20090527
DOCDB simple family (application)
EP 05021236 A 20050929; AR P060104297 A 20060929; AU 2006296541 A 20060927; CA 2623156 A 20060927; CN 200680035239 A 20060927; EP 06806843 A 20060927; EP 2006066783 W 20060927; IL 19042308 A 20080325; JP 2008532773 A 20060927; KR 20087010220 A 20080428; RU 2008116320 A 20060927; TW 95135908 A 20060928; US 48543409 A 20090616; US 53309606 A 20060919; ZA 200800431 A 20080115