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1. WO2000027823 - GASTRIN AND CHOLECYSTOKININ RECEPTOR LIGANDS

Publication Number WO/2000/027823
Publication Date 18.05.2000
International Application No. PCT/GB1999/003733
International Filing Date 09.11.1999
Chapter 2 Demand Filed 24.05.2000
IPC
C07D 207/34 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
30having two double bonds between ring members or between ring members and non-ring members
34with 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 ring carbon atoms
C07D 233/54 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
C07D 233/88 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
66with 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 ring carbon atoms
88Nitrogen atoms, e.g. allantoin
C07D 233/90 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
66with 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 ring carbon atoms
90Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 263/34 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
263Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02not condensed with other rings
30having two or three double bonds between ring members or between ring members and non-ring members
34with 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 ring carbon atoms
C07D 277/56 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
277Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02not condensed with other rings
20having two or three double bonds between ring members or between ring members and non-ring members
32with 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 ring carbon atoms
56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
CPC
A61P 1/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
A61P 1/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
18for pancreatic disorders, e.g. pancreatic enzymes
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
A61P 25/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
A61P 25/22
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
22Anxiolytics
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • JAMES BLACK FOUNDATION LIMITED [GB]/[GB] (AllExceptUS)
  • KALINDJIAN, Sarkis, Barret [GB]/[GB] (UsOnly)
  • BUCK, Ildiko, Maria [GB]/[GB] (UsOnly)
  • LINNEY, Ian, Duncan [GB]/[GB] (UsOnly)
  • WRIGHT, Paul, Trevor [GB]/[GB] (UsOnly)
  • McDONALD, Iain, Mair [GB]/[GB] (UsOnly)
  • STEEL, Katherine, Isobel, Mary [GB]/[GB] (UsOnly)
  • HULL, Robert, Antony, David [GB]/[GB] (UsOnly)
  • ROBERTS, Sonia, Patricia [GB]/[GB] (UsOnly)
  • GAFFEN, John, David [GB]/[GB] (UsOnly)
  • VINTER, Jeremy, Gilbert [GB]/[GB] (UsOnly)
  • WALKER, Martin, Keith [GB]/[GB] (UsOnly)
  • BLACK, James, Whyte [GB]/[GB] (UsOnly)
  • WATT, Gillian, Fairfull [GB]/[GB] (UsOnly)
  • HARPER, Elaine, Anne [GB]/[GB] (UsOnly)
  • SHANKLEY, Nigel, Paul [GB]/[GB] (UsOnly)
  • TOZER, Matthew, John [GB]/[GB] (UsOnly)
  • DUNSTONE, David, John [GB]/[GB] (UsOnly)
  • PETHER, Michael, John [GB]/[GB] (UsOnly)
  • LILLEY, Elliot, James [GB]/[GB] (UsOnly)
  • SYKES, David, Andrew [GB]/[GB] (UsOnly)
  • LOW, Caroline, Minli, Rachel [GB]/[GB] (UsOnly)
  • GRIFFIN, Eric, Peter [GB]/[GB] (UsOnly)
  • WRIGHT, Laurence [GB]/[GB] (UsOnly)
Inventors
  • KALINDJIAN, Sarkis, Barret
  • BUCK, Ildiko, Maria
  • LINNEY, Ian, Duncan
  • WRIGHT, Paul, Trevor
  • McDONALD, Iain, Mair
  • STEEL, Katherine, Isobel, Mary
  • HULL, Robert, Antony, David
  • ROBERTS, Sonia, Patricia
  • GAFFEN, John, David
  • VINTER, Jeremy, Gilbert
  • WALKER, Martin, Keith
  • BLACK, James, Whyte
  • WATT, Gillian, Fairfull
  • HARPER, Elaine, Anne
  • SHANKLEY, Nigel, Paul
  • TOZER, Matthew, John
  • DUNSTONE, David, John
  • PETHER, Michael, John
  • LILLEY, Elliot, James
  • SYKES, David, Andrew
  • LOW, Caroline, Minli, Rachel
  • GRIFFIN, Eric, Peter
  • WRIGHT, Laurence
Agents
  • FISHER, Adrian, John
Priority Data
9824536.809.11.1998GB
9916786.816.07.1999GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) GASTRIN AND CHOLECYSTOKININ RECEPTOR LIGANDS
(FR) LIGANDS DES RECEPTEURS DE LA GASTRINE ET DE LA CHOLECYSTOKININE
Abstract
(EN)
Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently =N-, -N(R5)- =CH-, -S- or -O-. n is from 1 to 4; R1 is H or C1 to C15 hydrocarbyl R2 is selected from H, Me, Et, Pr and OH, R3 is selected from H, Me, Et and Pr; or (when n is greater than 1) each R3 is independently selected from H, Me, Et and Pr, or two R3 groups on neighbouring carbon atoms are linked to form a C3 to C6 carbocylic ring, or R2 and R3 on the same carbon atom together represent an =O group; R4 is C1 to C15 hydrocarbyl Z is -(NR7)a-CO-(NR8)b- (wherein a is 0 or 1, b is 0 or 1, -CO-NR7-CH2-CO-NR8-, -CO-O-, -CH2-CH2-, -CH=CH-, -CH2-NR8- or a bond; Q is -R9V, or (II), (wherein R9 is -CH2-; -CH2-CH2-; or (III), R9 and R8, together with the nitrogen atom to which R8 is attached, form a piperidine or pyrrolidine ring which is substituted by V; V is -CO-NH-SO2-Ph, -SO2-NH-CO-Ph, -CH2OH, or a group of the formula -R10U, (wherein U is -COOH, tetrazolyl, -CONHOH- or -SO3H; and R10 is a bond; C1 to C6 hydrocarbylene, -O-(C1 to C3 alkylene)-; -SO2NR11-CHR12-; -CO-NR11-CHR12-, or -NH-(CO)c-CH2-, c being 0 or 1).
(FR)
L'invention concerne des composés de formule (I), ainsi que leurs sels pharmaceutiquement acceptables, dans laquelle X et Y sont indépendamment =N-, -N(R5)-, =CH-, -S- ou -O-; n est compris entre 1 et 4; R1 est H ou hydrocarbyle C1-C15; R2 est choisi entre H, Me, Et, Pr et OH; R3 est choisi entre H, Me, Et et Pr, ou bien (quand n est supérieur à 1) chaque R3 est choisi indépendamment entre H, Me, Et et Pr, ou bien deux groupes R3 portés par des atomes de carbone adjacents sont liés de façon à former un anneau carbocyclique C3-C6, ou bien R2 et R3 portés par le même carbone représentent ensemble un groupe =O; R4 est hydrocarbyle C1-C15; Z est -(NR7)a-CO-(NR8)b- (où a est 0 ou 1, b est 0 ou 1, CO-NR7-CH2-CO-NR8-, -CO-O-, -CH2-CH2-, -CH=CH-, -CH2-NR8- ou une liaison); Q est -R9V ou (II) (où R9 est -CH2-; -CH2-CH2-, ou (III), ou bien R9 et R8, avec l'atome d'azote sur lequel est fixé R8, forment un anneau pipéridine ou pyrrolidine substitué par V; V est -CO-NH-SO2-Ph, -SO2-NH-CO-Ph, -CH2OH ou un groupe de formule -R10U (où U est -COOH, tétrazolyle, -CONHOH- ou -SO3H; et R10 est une liaison, hydrocarbylène C1-C6, -O-(alkylène C1-C3)-, -SO2NR11-CHR12-, -CO-NR11-CHR12- ou -NH-(CO)c-CH2-, c étant 0 ou 1). Ces composés et leurs sels sont des ligands des récepteurs de la gastrine et de la cholécystokinine.
Also published as
NO20012288
NZ510822
ZA200102768
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