Title (en)

NOVEL NEUROKININ ANTAGONISTS, METHOD FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS

Title (de)

PIPERIDINSUBSTITUIERTE ARYLGLYCINAMIDE ALS NEUROKININANTAGONISTEN, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN

Title (fr)

ARYLGLYCINAMIDES A SUBSTITUTION PIPERIDINE SERVANT D'ANTAGONISTES DE NEUROKININE, LEUR PROCEDE DE PRODUCTION ET COMPOSITIONS PHARMACEUTIQUES CONTENANT CES COMPOSES

Publication

EP 1328516 A1 20030723 (DE)

Application

EP 01987744 A 20011016

Priority

• DE 10051320 A 20001017
• EP 0111906 W 20011016

Abstract (en)

[origin: DE10051320A1] 2-(4-Amino-piperidin-1-yl)-2-aryl-N-(phenylalkyl)-acetamides (I), having specific substituents on the amino group, are new. Piperidine derivatives of formula (I) and their salts are new. R1 = 3-hydroxypropyl, 1,3-dihydroxyprop-2-yl or (3-6C) cycloalkyl-methyl; R2 = H, 1-6C alkyl, 2-4C w-hydroxyalkyl, 1,3-dihydroxyprop-2-yl or (3-6C) cycloalkyl-methyl; Ar = phenyl (optionally substituted by 1-5 of halo, OH, T, OT or OCH2O); T = 1-4C alkyl or 1-4C fluoroalkyl; R3 = phenyl-(1-4C) alkyl (optionally ring-substituted by 1-3 of halo, OH, T or OT); R4 = H, 1-4C alkyl, 3-8C cycloalkyl, CH2COOH, CH2CONH2, OH or phenyl-(1-4C) alkyl. Independent claims are included for: (1) the preparation of (I); and (2) the use of NK1 receptor antagonists (I') containing an amino group of formula -NR1R2 (or their salts) in the production of a medicament having a prolonged duration of action in the treatment or prophylaxis of neurokinin-mediated diseases.

IPC 1-7

C07D 211/58; A61K 31/4468; A61P 9/02

IPC 8 full level

A61K 31/4468 (2006.01); A61K 31/4525 (2006.01); A61P 1/04 (2006.01); A61P 1/08 (2006.01); A61P 9/02 (2006.01); A61P 9/12 (2006.01); A61P 9/14 (2006.01); A61P 11/00 (2006.01); A61P 11/06 (2006.01); A61P 11/08 (2006.01); A61P 11/10 (2006.01); A61P 13/02 (2006.01); A61P 13/10 (2006.01); A61P 15/08 (2006.01); A61P 17/00 (2006.01); A61P 17/02 (2006.01); A61P 17/04 (2006.01); A61P 17/06 (2006.01); A61P 19/02 (2006.01); A61P 19/08 (2006.01); A61P 19/10 (2006.01); A61P 25/06 (2006.01); A61P 25/08 (2006.01); A61P 25/16 (2006.01); A61P 25/18 (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 27/02 (2006.01); A61P 27/16 (2006.01); A61P 29/00 (2006.01); A61P 31/22 (2006.01); A61P 35/00 (2006.01); A61P 37/02 (2006.01); A61P 37/08 (2006.01); A61P 43/00 (2006.01); C07D 211/58 (2006.01); C07D 405/06 (2006.01)

CPC (source: EP)

A61P 1/04 (2017.12); A61P 1/08 (2017.12); A61P 9/02 (2017.12); A61P 9/12 (2017.12); A61P 9/14 (2017.12); A61P 11/00 (2017.12); A61P 11/06 (2017.12); A61P 11/08 (2017.12); A61P 11/10 (2017.12); A61P 13/02 (2017.12); A61P 13/10 (2017.12); A61P 15/08 (2017.12); A61P 17/00 (2017.12); A61P 17/02 (2017.12); A61P 17/04 (2017.12); A61P 17/06 (2017.12); A61P 19/02 (2017.12); A61P 19/08 (2017.12); A61P 19/10 (2017.12); A61P 25/06 (2017.12); A61P 25/08 (2017.12); A61P 25/16 (2017.12); A61P 25/18 (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 27/02 (2017.12); A61P 27/16 (2017.12); A61P 29/00 (2017.12); A61P 31/22 (2017.12); A61P 35/00 (2017.12); A61P 37/02 (2017.12); A61P 37/08 (2017.12); A61P 43/00 (2017.12); C07D 211/58 (2013.01); C07D 405/06 (2013.01)

Citation (search report)

See references of WO 0232865A1

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)

DE 10051320 A1 20020425; AU 2361702 A 20020429; CA 2426221 A1 20030417; CA 2426221 C 20090224; EP 1328516 A1 20030723; JP 2004514658 A 20040520; JP 4426756 B2 20100303; MX PA03003334 A 20041202; PE 20020519 A1 20020711; WO 0232865 A1 20020425

DOCDB simple family (application)

DE 10051320 A 20001017; AU 2361702 A 20011016; CA 2426221 A 20011016; EP 0111906 W 20011016; EP 01987744 A 20011016; JP 2002536049 A 20011016; MX PA03003334 A 20011016; PE 2001001023 A 20011015