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1. WO1996033171 - 1H-PYRROL-1-YL AND 1H-INDOL-1-YL ARYL SULPHONES, PROCESSES FOR THEIR PREPARATION AND USE FOR THE THERAPY OF HIV-1 INFECTIONS

Publication Number WO/1996/033171
Publication Date 24.10.1996
International Application No. PCT/EP1996/001642
International Filing Date 19.04.1996
Chapter 2 Demand Filed 13.11.1996
IPC
C07D 207/48 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
46with hetero atoms directly attached to the ring nitrogen atom
48Sulfur atoms
C07D 209/42 2006.01
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
CPC
C07D 207/48
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
46with hetero atoms directly attached to the ring nitrogen atom
48Sulfur 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
  • ISTITUTO SUPERIORE DI SANITÁ [IT]/[IT] (AllExceptUS)
  • UNIVERSITA' DEGLI STUDI DI CAGLIARI [IT]/[IT] (AllExceptUS)
  • ARTICO, Marino [IT]/[IT] (UsOnly)
  • MASSA, Silvio [IT]/[IT] (UsOnly)
  • SILVESTRI, Romano [IT]/[IT] (UsOnly)
  • LOI, Anna, Giulia [IT]/[IT] (UsOnly)
  • DE MONTIS, Antonella [IT]/[IT] (UsOnly)
  • LA COLLA, Paolo [IT]/[IT] (UsOnly)
Inventors
  • ARTICO, Marino
  • MASSA, Silvio
  • SILVESTRI, Romano
  • LOI, Anna, Giulia
  • DE MONTIS, Antonella
  • LA COLLA, Paolo
Agents
  • GERVASI, Gemma
Priority Data
MI95A00081221.04.1995IT
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 1H-PYRROL-1-YL AND 1H-INDOL-1-YL ARYL SULPHONES, PROCESSES FOR THEIR PREPARATION AND USE FOR THE THERAPY OF HIV-1 INFECTIONS
(FR) SULFONES DE 1H-PYRROL-1-YLE ET DE 1H-INDOL-1-YLE ARYLE, LEURS PROCEDES DE PREPARATION ET LEUR UTILISATION DANS LA THERAPIE DES INFECTIONS A VIH-1
Abstract
(EN)
This invention relates to new 1H-Pyrrol-1-yl and 1H-Indol-1-yl Aryl Sulphones of Formula (I) that may by useful in the medical therapy of retrovirus infections and in particular of HIV-1 infections. The compounds reported herein may be used alone or in combination with other antiretroviral compounds, preferably chosen among reverse transcriptase inhibitors such as, for example, nucleoside analogues, wherein: R1 = NO2, NH2, halogen, NHCH2Z(Z = H, alkyl, aryl, heteroaryl), NHCOW (W = H, alkyl, aryl, heteroaryl); R2 = H, halogen; R3 = R4 = H, NO2, NH2, CH3, halogen; R5 = H, (2)-COX, (3)-COX, (X = OR, alkyl, aryl, CCl3, N(alkyl2); R = alkyl cycloalkyl, aryl arylmethyl; (2)-CONHY (Y = H, alkyl, aryl); R6 = H, halogen, NO2, NH2, OCH3; A = H, phenyl; K = H, CHO, CH2NC5H11, CH2NC4H8NCH3.
(FR)
L'invention concerne des nouvelles sulfones de 1H-pyrrol-1-yle et de 1H-indol-1-yle aryle de la formule (I) qui peuvent être utiles en thérapie médicale dans les infections à rétrovirus, et notamment dans les infections à VIH-1. On peut utiliser les composés de l'invention seuls ou en combinaison avec d'autres composés antirétroviraux, préférablement choisis parmi des inhibiteurs de la transcriptase inverse, tels que des analogues de nucléosides, par exemple. Dans cette formule, R1 représente NO2, NH2, halogène, NHCH2Z (où Z représente H, alkyle, aryle, hétéroaryle), NHCOW (où W représente H, alkyle, aryle, hétéroaryle); R2 représente H, halogène; R3 = R4 et ils représentent H, NO2, NH2, CH3, halogène; R5 représente H, (2)-COX, (3)-COX (où X représente OR, alkyle, aryle, CCl3, N(alkyle2)); R représente alkyle, cycloalkyle, aryle, arylméthyle; (2)-CONHY (où Y représente H, alkyle, aryle); R6 représente H, halogène, NO2, NH2, OCH3; A représente H, phényle et K représente H, CHO, CH2NC5H11, CH2NC4H8NCH3.
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