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1. WO2008042240 - ENANTIOMERICALLY PURE PHOSPHOINDOLES AS HIV INHIBITORS

Publication Number WO/2008/042240
Publication Date 10.04.2008
International Application No. PCT/US2007/020900
International Filing Date 28.09.2007
IPC
C07F 9/572 2006.1
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
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
553having one nitrogen atom as the only ring hetero atom
572Five-membered rings
A61K 31/675 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61P 31/18 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
18for HIV
CPC
A61K 2300/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
2300Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
A61K 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 9/20
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, tablets, ; discs, rods
A61K 9/48
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
A61P 31/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
18for HIV
Applicants
  • IDENIX PHARMACEUTICALS, INC. [US]/[US] (AllExceptUS)
  • STORER, Richard [GB]/[GB] (UsOnly)
  • ALEXANDRE, Francois-Rene [FR]/[FR] (UsOnly)
  • DOUSSON, Cyril [FR]/[FR] (UsOnly)
  • MOUSSA, Adel, M. [US]/[US] (UsOnly)
  • BRIDGES, Edward [US]/[US] (UsOnly)
Inventors
  • STORER, Richard
  • ALEXANDRE, Francois-Rene
  • DOUSSON, Cyril
  • MOUSSA, Adel, M.
  • BRIDGES, Edward
Agents
  • RIEGER, Dale, L.
Priority Data
60/848,58429.09.2006US
60/857,98009.11.2006US
60/903,11523.02.2007US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ENANTIOMERICALLY PURE PHOSPHOINDOLES AS HIV INHIBITORS
(FR) phosphoindoles ÉnantiomÉriquement purs utilisables en tant qu'inhibiteurs du vih
Abstract
(EN)
3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HLV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other antiviral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds. The 3-phosphoindole compounds are of the formula (A) or (B) and the pharmaceutically acceptable salts, solvates, hydrates, or esters thereof. In the formulae X is hydrogen; aryl or heterocyclyl; C2-6 alkenyl, C2-6 alkynyl or alkyl; Y is hydrogen, -R, -O-R, -NH-R, or -NRR; Z is -OR, -NHR, -NRR, carboxamido, arnido, carboxyl, carbonyl, or an amino acid residue; R1 is hydrogen, acyl, -S(O)n-R, carboxyl, carbonyl, or an amino acid residue; each R4', R5', R6' and R7' is independently hydrogen, C2-6 alkenyl, C2-6 alkynyl, aryl, heterocyclyl, halogen, -CN, -CF3, -OR, -NHR, -NRR, or -NO2; n is 0, 1, or 2; and each R is independently hydrogen, alkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, or heterocyclyl.
(FR)
La présente invention concerne des composés à base de 3-phosphoindole se présentant essentiellement sous la forme d'un énantiomère unique et utilisables pour le traitement des infections virales à Flaviviridae, et plus particulièrement pour le traitement des infections par le VIH. La présente invention concerne également des compositions pharmaceutiques comprenant les composés à base de 3-phosphoindole seuls ou en association avec au moins un autre agent anti-viral, des procédés de préparation de celles-ci et des procédés de fabrication d'un médicament dans lequel sont incorporés ces composés.
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