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1. WO1997032857 - KAPPA AGONIST COMPOUNDS AND PHARMACEUTICAL FORMULATIONS THEREOF

Publication Number WO/1997/032857
Publication Date 12.09.1997
International Application No. PCT/US1997/003353
International Filing Date 01.03.1997
Chapter 2 Demand Filed 26.09.1997
IPC
A61K 31/404 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
A61K 31/4439 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
C07D 209/42 2006.1
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
30with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 213/56 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24with substituted hydrocarbon radicals attached to ring carbon atoms
54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
56Amides
C07D 241/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
241Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02not condensed with other rings
04having no double bonds between ring members or between ring members and non-ring members
CPC
A61K 31/404
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
A61K 31/4439
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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
C07D 207/06
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
04having no double bonds between ring members or between ring members and non-ring members
06with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07D 209/32
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
30with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
32Oxygen atoms
C07D 209/42
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
30with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Applicants
  • ADOLOR CORPORATION [US]/[US] (AllExceptUS)
  • KRUSE, Lawrence, I. [--]/[US] (UsOnly)
  • CHANG, An-Chih [--]/[US] (UsOnly)
  • DEHAVEN-HUDKINS, Diane, L. [--]/[US] (UsOnly)
  • FARRAR, John, J. [--]/[US] (UsOnly)
  • GAUL, Forrest [--]/[US] (UsOnly)
  • MARELLA, Michael, Anthony [--]/[US] (UsOnly)
  • MAYCOCK, Alan, L. [--]/[US] (UsOnly)
  • ZHANG, Wei, Yuan [--]/[US] (UsOnly)
Inventors
  • KRUSE, Lawrence, I.
  • CHANG, An-Chih
  • DEHAVEN-HUDKINS, Diane, L.
  • FARRAR, John, J.
  • GAUL, Forrest
  • MARELLA, Michael, Anthony
  • MAYCOCK, Alan, L.
  • ZHANG, Wei, Yuan
Agents
  • BALOGH, Imre
Priority Data
08/612,68002.05.1997US
08/796,07808.03.1996US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) KAPPA AGONIST COMPOUNDS AND PHARMACEUTICAL FORMULATIONS THEREOF
(FR) COMPOSES AGONISTES DU KAPPA ET LEURS PREPARATIONS PHARMACEUTIQUES
Abstract
(EN) Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae (I), (II), (III) and (IV) have the structure wherein X, X4, X5, X7, X9; R1, R2, R3, R4; and Y, Z and n are as described in the specification.
(FR) L'invention porte sur des composés présentant une activité agoniste de l'opioïde kappa, sur des compositions les contenant et sur leurs méthodes d'utilisation comme analgésiques. Ces composés, de formules (I), (II), (III) et (IV) présentent une structure dans laquelle X, X4, X5, X7, X9, R1, R2, R3, R4; et Y, Z et n sont décrits dans la description.
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