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1. WO1996004233 - ARYLOXY AND ARYLTHIOPROPANOLAMINE DERIVATIVES USEFUL AS BETA 3-ADRENORECEPTOR AGONISTS AND ANTAGONISTS OF THE BETA 1 AND BETA 2-ADRENORECEPTORS AND PHARMACEUTICAL COMPOSITION THEREOF

Publication Number WO/1996/004233
Publication Date 15.02.1996
International Application No. PCT/EP1995/003037
International Filing Date 27.07.1995
Chapter 2 Demand Filed 05.02.1996
IPC
C07C 217/34 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
02having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
28having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines
30having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring
32the six-membered aromatic ring or condensed ring system containing that ring being further substituted
34by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
C07D 317/46 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
317Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
08having the hetero atoms in positions 1 and 3
44ortho- or peri-condensed with carbocyclic rings or ring systems
46condensed with one six-membered ring
C07F 9/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P-C bonds
30Phosphinic acids ; Thiophosphinic acids
C07F 9/32 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P-C bonds
30Phosphinic acids ; Thiophosphinic acids
32Esters thereof
C07F 9/40 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P-C bonds
38Phosphonic acids ; Thiophosphonic acids
40Esters thereof
CPC
A61P 1/00
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
A61P 1/04
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
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
C07C 217/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
02having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
28having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines
30having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring
32the six-membered aromatic ring or condensed ring system containing that ring being further substituted
34by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
C07C 2601/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2601Systems containing only non-condensed rings
12with a six-membered ring
14The ring being saturated
C07D 317/46
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
317Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
08having the hetero atoms in positions 1 and 3
44ortho- or peri-condensed with carbocyclic rings or ring systems
46condensed with one six-membered ring
C07F 9/301
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P—C bonds
30Phosphinic acids R2P(=O)(OH); Thiophosphinic acids ; , i.e. R2P(=X)(XH) (X = S, Se)
301Acyclic saturated acids which can have further substituents on alkyl
Applicants
  • SMITHKLINE BEECHAM PLC [GB/GB]; New Horizons Court Brentford Middlesex TW8 9EP, GB (AllExceptUS)
  • BEELEY, Lee, James [GB/GB]; GB (UsOnly)
  • THOMPSON, Mervyn [GB/GB]; GB (UsOnly)
  • DEAN, David, Kenneth [GB/GB]; GB (UsOnly)
  • KOTECHA, Nikesh, Rasiklal [GB/GB]; GB (UsOnly)
  • BERGE, John, Michael [GB/GB]; GB (UsOnly)
  • WARD, Robert, William [GB/GB]; GB (UsOnly)
Inventors
  • BEELEY, Lee, James; GB
  • THOMPSON, Mervyn; GB
  • DEAN, David, Kenneth; GB
  • KOTECHA, Nikesh, Rasiklal; GB
  • BERGE, John, Michael; GB
  • WARD, Robert, William; GB
Agents
  • RUTTER, Keith; SmithKline Beecham Corporate Intellectual Property SB House Great West Road Brentford, Middlesex TW8 9BD, GB
  • GIDDINGS, Peter, John; SmithKline Beecham Coporate Intellectual Property SB House, Great West Road Brentford Middlesex TW8 9BD, GB
Priority Data
9415304.629.07.1994GB
9423179.217.11.1994GB
9510485.724.05.1995GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ARYLOXY AND ARYLTHIOPROPANOLAMINE DERIVATIVES USEFUL AS BETA 3-ADRENORECEPTOR AGONISTS AND ANTAGONISTS OF THE BETA 1 AND BETA 2-ADRENORECEPTORS AND PHARMACEUTICAL COMPOSITION THEREOF
(FR) DERIVES D'ARYLOXY- ET D'ARYLTHIOPROPANOLAMINE UTILES EN TANT QU'AGONISTES D'ADRENORECEPTEURS BETA 3 ET QU'ANTAGONISTES DES ADRENORECEPTEURS BETA 1 ET BETA 2 ET COMPOSITION PHARMACEUTIQUE
Abstract
(EN)
A compound formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein R0 represents an aryl group optionally substituted with one, two or three substituents selected from the list consisting of: hydroxy, hydroxymethyl, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogen, alkoxy and allyl; X represents O or S; R1 and R1a each independently represents hydrogen or an alkyl group; R2 represents OCH2CO2H, or an ester or amide thereof, or R2 represents a moiety of formula (b), wherein R4 represents hydrogen, alkyl, hydroxyalkyl, arylalkyl, aryloxyalkyl, aralkyloxyalkyl or cycloalkyl and R5 represents hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, aryloxyalkyloxy, arylalkoxyalkyloxy or cycloalkyloxy or R5 represents hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, aryloxyalkyl, arylalkyloxyalkyl or R5 together with OR4 represents O(CH2)nO, wherein n is 2, 3 or 4; and R3 represents hydrogen, halogen, alkyl or alkoxy or R3 together with R2 represents a moiety of formula (c) or an ester or amide thereof; providing that 4-[2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]propyl]phenoxyacetic acid and salts and esters thereof and the compounds of examples 1 to 36 disclosed in EP0328251 are excluded from the scope of formula (I); a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.
(FR)
Composé de formule (I) ou sel ou solvat pharmaceutiquement acceptables dudit composé, dans laquelle Ro représente un groupe aryle éventuellement substitué à l'aide d'un, deux ou trois substituants choisis dans la liste comprenant hydroxy, hydroxyméthyle, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogène, alcoxy et allyle; X représente O ou S; R1 et R1a représentent chacun indépendamment hydrogène ou un groupe alkyle; R2 représente OCH2CO2H, ou un ester ou amide de ladite substance, ou R2 représente une fraction de formule (b) dans laquelle R4 représente hydrogène, alkyle, hydroxyalkyle, arylalkyle, aryloxyalkyle, aralkyloxyalkyle ou cycloalkyle et R5 représente hydroxy, alcoxy, arylalkyloxy, hydroxyalkyloxy, alcoxyalkyloxy, aryloxyalkyloxy, arylalcoxyalkyloxy ou cycloalkyloxy ou R5 représente hydrogène, alkyle, alkyle substitué, cycloalkyle, aryle, arylakyle, aryloxyalkyle, arylalkyloxyalkyle ou R5 combiné à OR4 représente O(CH2)nO dans laquelle n est 2, 3 ou 4; et R3 représente hydrogène, halogène, alkyle ou alcoxy ou R3 combiné à R2 représente une fraction de formule (c) ou un ester ou amide de ladite fraction; à condition que l'acide 4-[2-[2-hydroxy-3-(4-hydroxyphénoxy)propylamino] phénoxyacétique et les sels et esters dudit acide ainsi que les composés des exemples 1 à 36 décrits dans EP0328251 soient exclus de la portée de la présente invention. Une composition pharmaceutique contenant ledit composé, un procédé de préparation d'un composé de ce type et l'utilisation de ce composé en médecine sont également décrits.
Also published as
CZPV1997-255
KR1019970700616
NO19970372
NZ291420
Latest bibliographic data on file with the International Bureau