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1. WO1996006078 - N-(2-(PYRROLIDINYL-1)-1-PHENYLETHYL)ACETAMIDES AS KAPPA RECEPTOR ANTAGONISTS

Publication Number WO/1996/006078
Publication Date 29.02.1996
International Application No. PCT/JP1994/001399
International Filing Date 24.08.1994
IPC
C07D 207/12 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
04having no double bonds between ring members or between ring members and non-ring members
10with 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
12Oxygen or sulfur atoms
C07D 207/335 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
32with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
33with substituted hydrocarbon radicals, directly attached to ring carbon atoms
335Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 401/12 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
12linked by a chain containing hetero atoms as chain links
C07D 405/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 409/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
CPC
C07D 207/12
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
10with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
12Oxygen or sulfur atoms
C07D 207/335
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
32with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
33with substituted hydrocarbon radicals, directly attached to ring carbon atoms
335Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 401/12
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
12linked by a chain containing hetero atoms as chain links
C07D 405/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 409/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 413/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • PFIZER PHARMACEUTICALS INC. [JP/JP]; Shinjuku Mitsui Building 1-1, Nishi-shinjuku 2-chome Shinjuku-ku Tokyo 163-04, JP
Inventors
  • ITO, Fumitaka; JP
Agents
  • KOBAYASHI, Hiroshi; Pfizer Pharmaceuticals Inc. Shinjuku Mitsui Building 1-1, Nishi-shinjuku 2-chome Shinjuku-ku Tokyo 163-04, JP
Priority Data
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) N-(2-(PYRROLIDINYL-1)-1-PHENYLETHYL)ACETAMIDES AS KAPPA RECEPTOR ANTAGONISTS
(FR) N-(2-(PYRROLIDINYL-1)-1-PHENYLETHYL)ACETAMIDES UTILISES EN TANT QU'ANTAGONISTES DU RECEPTEUR KAPPA
Abstract
(EN)
A compound of formula (I) and its pharmaceutically acceptable salt, wherein R is hydrogen or hydroxy; Ar is unsubstituted or substituted phenyl; X is unsubstituted or substituted phenyl or heterocyclic, mono-, di- or tri-halomethyl, cyano, or the like; and X1 is phenyl, furyl, thienyl, pyridyl, thiazolyl, benzofuryl, benzothienyl or the like. These compounds have agonist activity toward opiod kappa receptor and are thus useful as analgesic, antiinflammatory, diuretic, and neuroprotective agent.
(FR)
Composé de la formule (I) et ses sels pharmaceutiquement acceptables. Dans cette formule, R est hydrogène ou hydroxy; Ar est phényle substitué ou non; X est phényle ou mono-, di- ou tri-halométhyle hétérocyclique, substitué ou non, cyano, ou analogue; et X1 est phényle, furyle, thiényle, pyridyle, thiazolyle, benzofuryle, benzothienyle ou analogue. Ces composés exercent une activité agoniste vis-à-vis du récepteur opioïde kappa et s'avèrent utiles comme agent analgésique, anti-inflammatoire, diurétique ou neuroprotecteur.
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