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1. WO1996003377 - HETEROCYCLIC COMPOUNDS, USEFUL AS ALLOSTERIC EFFECTORS AT MUSCARINIC RECEPTORS

Publication Number WO/1996/003377
Publication Date 08.02.1996
International Application No. PCT/JP1995/001494
International Filing Date 27.07.1995
Chapter 2 Demand Filed 25.08.1995
IPC
C07D 209/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
08with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 209/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
12Radicals substituted by oxygen atoms
C07D 209/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 209/86 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56Ring systems containing three or more rings
80- or -condensed
82Carbazoles; Hydrogenated carbazoles
86with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
C07D 209/88 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56Ring systems containing three or more rings
80- or -condensed
82Carbazoles; Hydrogenated carbazoles
88with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
C07D 401/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
CPC
C07D 209/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
08with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 209/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
12Radicals substituted by oxygen atoms
C07D 209/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 209/86
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56Ring systems containing three or more rings
80[b, c]- or [b, d]-condensed
82Carbazoles; Hydrogenated carbazoles
86with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
C07D 209/88
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56Ring systems containing three or more rings
80[b, c]- or [b, d]-condensed
82Carbazoles; Hydrogenated carbazoles
88with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
C07D 401/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • SANKYO COMPANY, LIMITED [JP/JP]; 5-1, Nihonbashi Honcho 3-chome Chuo-ku Tokyo 103, JP (AllExceptUS)
  • BIRDSALL, Nigel [GB/GB]; GB (UsOnly)
  • LAZARENO, Sebastian [GB/GB]; GB (UsOnly)
  • NARUTO, Syunji [JP/JP]; JP (UsOnly)
  • KOYAMA, Kazuo [JP/JP]; JP (UsOnly)
  • SUGIMOTO, Masahiko [JP/JP]; JP (UsOnly)
  • MARUMOTO, Shinji [JP/JP]; JP (UsOnly)
Inventors
  • BIRDSALL, Nigel; GB
  • LAZARENO, Sebastian; GB
  • NARUTO, Syunji; JP
  • KOYAMA, Kazuo; JP
  • SUGIMOTO, Masahiko; JP
  • MARUMOTO, Shinji; JP
Agents
  • OGAWA, Nobuo ; Room 646 Shin-Tokyo Building 3-1, Marunouchi 3-chome Chiyoda-ku Tokyo 100, JP
  • GIBSON, Chris, J., R.; Marks & Clerk 57-60, Lincoln's Inn Field London WC2A 3LS, GB
Priority Data
9415175.027.07.1994GB
9423948.025.11.1994GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) HETEROCYCLIC COMPOUNDS, USEFUL AS ALLOSTERIC EFFECTORS AT MUSCARINIC RECEPTORS
(FR) COMPOSES HETEROCYCLIQUES UTILES COMME EFFECTEURS ALLOSTERIQUES AU NIVEAU DES RECEPTEURS MUSCARINIQUES
Abstract
(EN)
Compounds of formula (I) wherein Z represents a methylene group, a methine group, a group of formula $m(g)NH or a group of formula $m(g)N-, and W represents a methylene group, a methine group, a sulfur atom or a group of formula $g(m)S$m(7)(O)v, where v is 1 or 2; ... is a single or double bond; at least one of Y1, Y2, Y3 and Y4 represents a carboxyl group, a sulfonamide group or a group of formula -(A)p-B1-T1, wherein A is S or O, T1 is a carboxyl group, a thiocarboxy group, a dithiocarboxy group, a sulfonamide group or a tetrazolyl group, B1 is a bond, an optionally substituted alkylene group and p is 0 or 1; the rest of Y1, Y2, Y3 and Y4 are the same or different and are H, halogen, nitro, OH, SH, NH2, optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, aryl, aralkyloxy, aralkylthio and Y1 + Y2 may together be a lactone or keto; one of R1 and R2 is H, alkyl, alkanoyl, aryl, arylcarbonyl, aralkyl, carboxyl, sulfonamide or a group of formula -(O)q-B2-T2, wherein T2 is COOH, sulfonamide or tetrazolyl, B2 is an optionally substituted alkylene, and q is 0 or 1; the other of R1 and R2 is H, alkyl, aryl or aralkyl, or R1 and R2 together represent a group of formula (Ib'), wherein [R10, R11 and R12 are the same or different and each is H, OH, halogen, haloalkyl, optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl or alkylsulfonyl]; R3 is H or an amino protecting group; and pharmaceutically acceptable salts and esters thereof are allosteric effectors at muscarinic receptors, and are useful in the treatment and prophylaxis of disorders associated with muscarinic receptors.
(FR)
La présente invention concerne des composés représentés par la formule (I). Dans cette formule (I), Z représente un groupe méthylène, un groupe méthine, un groupe représenté par la formule spécifique $m(g)NH ou un groupe représenté par la formule $m(g)N-. W représente un groupe méthylène, un groupe méthine, un atome de soufre ou un groupe représenté par la formule $m(g)S$m(7)(O)v dans laquelle v vaut 1 ou 2. Dans la formule (I), .... représente une liaison simple ou double, l'un au moins des symboles Y1, Y2, Y3 et Y4 représente un groupe carboxyle, un groupe sulfonamide ou un groupe représenté par la formule -(A)p-B1-T1 dans laquelle A représente S ou 0, T1 représente un groupe carboxyle, un groupe thiocarboxy, un groupe dithiocarboxy, un groupe sulfonamide ou un groupe tétrazolyle, et B1 est une liaison ou un groupe alkylène éventuellement substitué, et p vaut 0 ou 1. Dans la formule générale (I), les symboles restants parmi Y2, Y3 et Y4 sont identiques ou différents, en l'occurrence H, halogène, nitro, OH, SH, NH2, alkyle éventuellement substitué, alcoxy, alkylthio, alkylsulfinyle, alkylsulfonyle, aryle, aralkyloxy, aralkylthio, Y1 + Y2 pouvant représenter ensemble un lactone ou un céto; l'un des symboles R1 et R2 représente H, alkyle, alcanoyle, aryle, arylcarbonyle, sulfonamide ou un groupe représenté par la formule -(O)q-B2-T2 dans laquelle T2 représente COOH, sulfonamide ou tétrazolyle, B2 représente un alkylène éventuellement substitué, et q vaut 0 ou 1. L'autre symbole, R1 ou R2, représente H alkyle, aryle ou aralkyle, ou R1 et R2 peuvent représenter ensemble un groupe représenté par la formule (Ib), dans laquelle, R10, R11 et R12 sont identiques ou différents, chacun pouvant représenter H, OH, halogène, haloalkyle, alkyle éventuellement substitué, alcoxy, alkylthio, alkylsulfinyle ou alkylsulfonyle. Dans la formule générale (I), R3 représente H ou un groupe protecteur amino. L'invention concerne également des sels et esters pharmaceutiquement acceptables de ces composés, ces composés, sels ou esters étant des effecteurs allostériques au niveau des récepteurs muscariniques, utiles pour le traitement et la prophylaxie des troubles liés aux récepteurs muscariniques.
Also published as
CZPV1997-241
FI970328
NO19970308
NZ290199
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