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1. WO1996006077 - N-[2-(PYRROLIDINYL-1)-1-PHENYLETHYL]ACETAMIDES AS KAPPA RECEPTOR ANTAGONISTS

Publication Number WO/1996/006077
Publication Date 29.02.1996
International Application No. PCT/IB1995/000374
International Filing Date 18.05.1995
Chapter 2 Demand Filed 08.11.1995
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 Shinjuki-ku Tokyo 163-04, JP (JP)
  • PFIZER INC. [US/US]; 235 East 42nd Street New York, NY 10017, US (AT, AU, BE, CA, CH, CN, CZ, DE, DK, ES, FI, FR, GB, GR, HU, IE, IT, KR, LU, MC, MX, NL, NO, NZ, PL, PT, RU, SE)
  • ITO, Fumitaka [JP/JP]; JP (UsOnly)
Inventors
  • ITO, Fumitaka; JP
Agents
  • SPIEGEL, Allen, J.; Pfizer Inc. Patent Dept. 235 East 42nd Street New York, NY 10017, US
Priority Data
PCT/JP94/0139924.08.1994JP
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 DES RECEPTEURS 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, naphtyl, furyl, thienyl, pyridyl, thiazolyl, benzofuryl, benzothienyl or the like. These compounds have agonist activity toward opioid kappa receptor and are thus useful as analgesic, antiinflammatory, diuretic, and neuroprotective agent.
(FR)
Composé de la formule (I), ainsi que son sel acceptable sur le plan pharmaceutique, dans laquelle R représente hydrogène ou hydroxy; Ar représente phényle substitué ou non; X représente phényle substitué ou non, ou bien mono, di ou trihalométhyle, cyano, ou analogue hétérocyclique; et X1 représente phényle, naphtyle, furyle, thiényle, pyridyle, thiazolyle, benzofuryle, benzothiényle ou analogue. Ces composés possèdent une activité agoniste à l'égard du récepteur opioïde kappa et sont par conséquent utiles en tant qu'agent analgésique, anti-inflammatoire, diurétique et neuroprotecteur.
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