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1. WO2013190384 - PRODRUG DERIVATIVES OF (E)-N-METHYL-N-((3-METHYLBENZOFURAN-2-YL)METHYL)-3-(7-OXO-5,6,7,8-TETRAHYDRO-1,8-NAPHTHYRIDIN-3-YL)ACRYLAMIDE

Publication Number WO/2013/190384
Publication Date 27.12.2013
International Application No. PCT/IB2013/001780
International Filing Date 19.06.2013
Chapter 2 Demand Filed 01.04.2014
IPC
C07F 9/6561 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
6561containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero 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 31/04 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
C07F 9/60 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
576Six-membered rings
60Quinoline or hydrogenated quinoline ring systems
CPC
A61K 31/662
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
662Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
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
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 3/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
A61P 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
Applicants
  • DEBIOPHARM INTERNATIONAL SA [CH]/[CH]
Inventors
  • PARTRIDGE, John, J.
  • COLUCCI, John
  • GAREAU, Yves
  • THERIEN, Michel
  • ZAMBONI, Robert
  • HAFKIN, Barry
  • MARFAT, Anthony
  • ZAGHDANE, Helmi
Agents
  • GRAVELLE, Micheline
Priority Data
61/661,55919.06.2012US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PRODRUG DERIVATIVES OF (E)-N-METHYL-N-((3-METHYLBENZOFURAN-2-YL)METHYL)-3-(7-OXO-5,6,7,8-TETRAHYDRO-1,8-NAPHTHYRIDIN-3-YL)ACRYLAMIDE
(FR) DÉRIVÉS DE TYPE PROMÉDICAMENT DU (E)-N-MÉTHYL-N-((3-MÉTHYLBENZOFURAN-2-YL) MÉTHYL)-3-(7-OXO-5,6,7,8-TÉTRAHYDRO-L,8-NAPHTYRIDIN-3-YL)ACRYLAMIDE
Abstract
(EN) In part, the present disclosure is directed to derivatives of (E)-N-methy1-N-(( 3-methylta 1,8-naphthyndin-3-y1)acrylamide compounds with significant solubility, solid state stability and bioavailability profiles. Said compounds have been found to be effective inhibitors of bacterial fatty acid metabolism via the effective inhibition of FabL hi addition, certain compounds are shown to be stable towards gamma radiation sterilization treatments, and are thus well-suited to the production of a sterile formulation for use in the treatment of illnesses caused by bacterial infections.
(FR) La présente invention concerne, pour partie, des dérivés de type promédicament de composés de type (E)-N-méthyl-N-((3-méthylbenzofuran-2-yl) méthyl)-3-(7-oxo-5,6,7,8-tetrahydro-l,8-naphtyridin-3-yl)acrylamide présentant des profils de solubilité et de biodisponibilité intéressants.
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