EP 1383486 A2 20040128 - COMPOSITIONS CONTAINING CGMP PDE INHIBITORS AND LOCAL ANAESTHETIC AGENTS FOR NASAL APPLICATION
Title (en)
COMPOSITIONS CONTAINING CGMP PDE INHIBITORS AND LOCAL ANAESTHETIC AGENTS FOR NASAL APPLICATION
Title (de)
ZUSAMMENSETZUNGEN ENTHALTEND CGMP PDE-INHIBITOREN UND LOKALANÄSTHETIKA ZUR NASALEN APPLIKATION
Title (fr)
COMPOSITIONS CONTENANT DES INHIBITEURS DE CGMP-PDE ET DES AGENTS ANESTHESIQUES LOCAUX POUR L'ADMINISTRATION NASALE
Publication
Application
Priority
- DE 10118305 A 20010412
- EP 0203977 W 20020410
Abstract (en)
[origin: DE10118305A1] A new composition comprises: (1) at least one cyclic guanosine monophosphate phosphodiesterase (cGMP PDE) inhibitor (I); and (2) at least one local anesthetic (II) (other than benzyl alcohol). A new composition comprises: (1) at least one cyclic guanosine monophosphate phosphodiesterase (cGMP PDE) inhibitor (I); and (2) at least one local anesthetic (II) (other than benzyl alcohol). (I) are selected from pyrazolo-pyrimidinone derivatives of formula (I'), pyrazino-pyridino-indole derivatives of formula (I'') and their salts, isomers and/or hydrates. R1 = H, 1-3C alkyl, 1-3C perfluoroalkyl or 3-5C cycloalkyl; R2 = T (optionally substituted (os) by 3-6C cycloalkyl), 1-3C perfluoroalkyl or 3-6C cycloalkyl; T = 1-6C alkyl; R3 = T (os by 3-6C cycloalkyl), 1-6C perfluoroalkyl, 3-5C cycloalkyl, 3-6C alkenyl or 3-6C alkynyl; R4 = 1-4C alkyl (os by OH, NR5R6, CN, CONR5R6 or COOR7); 2-4C alkenyl (os by CN, CONR5R6 or COOR7); 2-4C alkanoyl (os by NR5R6); 2-4C hydroxyalkyl (os by NR5R6); (2-3C) alkoxy-(1-2C) alkyl (os by OH or NR5R6); CONR5R6; COOR7; halo; NR5R6; NHSO2NR5R6; NHSO2R8; SO2NR9R10; or phenyl, pyridinyl, pyrimidinyl, imidazolyl, oxazolyl, thiazolyl, thienyl or triazolyl (all os by Me); R5, R6 = H or 1-4C alkyl; or NR5R6 = pyrrolidino, piperidino, morpholino, 4-(R11)-piperazino or imidazolyl (all os by Me or OH); R7 = H or 1-4C alkyl; R8 = 1-3C alkyl (os by NR5R6); NR9R10 = pyrrolidino, piperidino, morpholino or 4-(R12)-piperazino (all os by 1-4C alkyl, 1-3C alkoxy, NR13R14 or CONR13R14); R11 = H, 1-3C alkyl (os by Ph), 2-3C hydroxyalkyl or 1-4C alkanoyl; R12 = H; T (os by CONR13R14); 2-6C alkyl substituted by 1-3C alkyl, OH or NR13R14; or CONR13R14, CSNR13R14 or C(NH)NR13R14; Q = H, halo or T; Q1 = H, T (os by halo), 2-6C alkenyl, 2-6C alkynyl, 3-8C cycloalkyl, 3-8C cycloalkyl-(1-3C) alkyl or Ar-(1-3C) alkyl; Ar = phenyl, thienyl, furyl or pyridyl (all os by 1-3 of halo, T, OT and OCH2O); Q2 = phenyl, thienyl, furyl or pyridyl (all os); or phenyl fused with a 5- or 6-membered saturated or partially or completely unsaturated ring containing 0-2 of O, N and S as heteroatoms; Q3 = H or 1-3C alkyl; or Q1 + Q3 = 3- or 4-membered alkylene or alkenylene chain completing a 5- or 6-membered ring. (II) is selected from: (1) compounds of formula (II'); (2) compounds of formula (II''); (3) 2-methoxycarbonyl-4-methyl-3-(2-(propylamino)-propionamido)-thiophene; (4) 2-butoxy-4-(N-(2-diethylaminoethyl)-carbamoyl)-quinoline; (5) 3-butyl-1-(2-dimethylaminoethyl)-isoquinoline; (6) N-(N-(1,1-dimethylpropyl)-N-methylcarbamoylmethyl)-N-(2-hydroxyethyl)- glycine N-(1,1-dimethyl-2-phenylethyl)-N-methylamide; (7) polydodecanol; and (8) benoxinate. or their salts or hydrates. A1 = H, NH2, NHT, OT or OCH2Ph; A2 = OT (optionally substituted by NHT, NT2 or Het) or -(CH2)p-Het; Het = saturated 5- or 6-membered heterocycle, which contains and is bonded via N, optionally contains 1 or 2 other N, O or S heteroatoms and is optionally substituted by 1-3 T; A3 = H, halo or OT; B1 = H or OH; B2 = -T'-NT2 or Het'; T' = 1-6C alkylene (optionally substituted by one or more T); Het' = as for Het, but not necessarily bonded via N; B3 = T, halo or COOT; n = 1 or 2. Independent claims are included for nasal spray applicators or powder inhalers (both preferably of unit dose type) containing the compositions.
IPC 1-7
IPC 8 full level
A61K 9/72 (2006.01); A61P 15/10 (2006.01); A61K 9/00 (2006.01); A61K 31/00 (2006.01); A61K 31/165 (2006.01); A61K 31/167 (2006.01); A61K 31/245 (2006.01); A61K 31/381 (2006.01); A61K 31/47 (2006.01); A61K 31/4985 (2006.01); A61K 31/519 (2006.01); A61K 45/06 (2006.01); A61P 23/02 (2006.01); A61P 43/00 (2006.01)
CPC (source: EP US)
A61K 9/0043 (2013.01 - EP US); A61K 31/519 (2013.01 - EP US); A61K 45/06 (2013.01 - EP US); A61P 15/10 (2017.12 - EP); A61P 23/02 (2017.12 - EP); A61P 43/00 (2017.12 - EP)
C-Set (source: EP US)
Citation (search report)
See references of WO 02083108A2
Designated contracting state (EPC)
DE ES FR GB IT
DOCDB simple family (publication)
DE 10118305 A1 20021017; AU 2002308134 A1 20021028; CA 2443559 A1 20021024; EP 1383486 A2 20040128; JP 2004525956 A 20040826; US 2004142944 A1 20040722; WO 02083108 A2 20021024; WO 02083108 A3 20030410
DOCDB simple family (application)
DE 10118305 A 20010412; AU 2002308134 A 20020410; CA 2443559 A 20020410; EP 0203977 W 20020410; EP 02761908 A 20020410; JP 2002580912 A 20020410; US 47300004 A 20040223