Processing

Please wait...

Settings

Settings

1. WO1996002531 - WATER SOLUBLE ORALLY EFFECTIVE IRON CHELATOR

Publication Number WO/1996/002531
Publication Date 01.02.1996
International Application No. PCT/US1995/008519
International Filing Date 10.07.1995
Chapter 2 Demand Filed 14.02.1996
IPC
C07D 213/86 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with 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
78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
86Hydrazides; Thio or imino analogues thereof
CPC
C07D 213/86
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms 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
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
86Hydrazides; Thio or imino analogues thereof
Applicants
  • JACOBUS PHARMACEUTICAL CO., INC. [US/US]; 37 Cleveland Lane Princeton, NJ 08540, US (AllExceptUS)
  • LEWIS, Neil [US/US]; US (UsOnly)
  • PATEL, Vithal [US/US]; US (UsOnly)
  • TERPINSKI, Jacek [PL/US]; US (UsOnly)
  • BLISS, Robert [US/US]; US (UsOnly)
Inventors
  • LEWIS, Neil; US
  • PATEL, Vithal; US
  • TERPINSKI, Jacek; US
  • BLISS, Robert; US
Agents
  • BEHR, Omri, M.; 325 Pierson Avenue Edison, NJ 08837, US
Priority Data
08/275,23514.07.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) WATER SOLUBLE ORALLY EFFECTIVE IRON CHELATOR
(FR) CHELATEUR DU FER HYDROSOLUBLE EFFICACE ORALEMENT
Abstract
(EN)
There is provided a synthesis and description of diprotonated diacid derivatives of pyridoxal isonicotinoyl hydrazone (PIH) of formula (I), wherein q is 1 or 2, DPA is 2 mols of a monoprotic acid HX or 1 mol of a diprotic acid H2Y wherein X is a monovalent anion and Y is a divalent anion and both HX and H2Y are pharmaceutically acceptable acids. The unique properties of the PIH.DPA molecule make it particularly suitable and pharmaceutically acceptable for formulation as an oral dosage form by virtue of its ready solubility in water. There are further provided methods of utilizing such chemically unique and isolable crystalline compounds, such as PIH.2HCI, as a pharmaceutical chelator. There are further provided pharmaceutical formulations specifically for the reduction of iron overload, and related chelatable metals, in subjects susceptible to such overload.
(FR)
L'invention concerne des dérivés de diacides diprotonés de la pyridoxal isonicotinoyle hydrazone (PIH) de la formule (I) ainsi que leur synthèse. Dans cette formule, q est 1 ou 2, DPA correspond à 2 moles d'un acide monoprotonique HX ou à 1 mole d'un acide diprotonique H2Y, où X est un anion monovalent, Y est un anion divalent et HX et H2Y sont tous deux des acides acceptables sur le plan pharmaceutique. Les propriétés uniques de la molécule PIH.DPA, sa grande solubilité dans l'eau et son acceptabilité pharmaceutique la rendent particulièrement utile pour la réalisation de formes galéniques orales. L'invention concerne en outre des procédés d'utilisation de ces composés cristallins chimiquement uniques que l'on peut isoler tels que PIH.2HCl, comme agents chélateurs à usage pharmaceutique. Enfin, l'invention concerne des formulations pharmaceutiques destinées spécifiquement à réduire la surcharge en fer et en métaux similaires se prêtant à une chélation, chez des sujets présentant une telle surcharge.
Also published as
Latest bibliographic data on file with the International Bureau