
专利信息
专利号:WO-9602531-A1
优先权日:1994-07-14
标题:Water soluble orally effective iron chelator
发明人:LEWIS NEIL; PATEL VITHAL; TERPINSKI JACEK; BLISS ROBERT
权利人:JACOBUS PHARMA CO INC; LEWIS NEIL; PATEL VITHAL; TERPINSKI JACEK; BLISS ROBERT
摘要: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.
专利号:US-2025069787-A1
优先权日:2021-11-25
标 题:Method for preparing acid resistant magnetic particles and acid resistant magnetic particles
发明人:SILVESTRE MARTIN EDUARDO; EISOLD SABINE; HEINDL DIETER; PETERS KRISTINA
权利人:ROCHE DIAGNOSTICS OPERATIONS INC
摘要:In a first aspect, the invention relates to a method for preparing a magnetic bead comprising at least one magnetic particle (M) and a silica coating, wherein the silica coating comprises at least two silica layers, the method comprising steps (a) to (d), wherein at least one of steps (b), (c) and (d) is/are done under sonication, wherein sonication is done with an amplitude (peak-to-peak) in the range of from 50 to 250 μm. A second aspect of the invention is related to a magnetic bead comprising (i) at least one magnetic particle (M) and (ii) a silica coating, wherein the silica coating comprises at least two silica layers; wherein the magnetic bead is stable against 7.5 M hydrochlorid acid and has a metal (cation) leaching rate in 7.5 M hydrochloric acid in the range of from 0.1 to 10%, wherein the metal (cation) leaching is determined according to a complex formation of Fe2+ with bathophenanthroline according to Reference Example 8.2. In a third aspect, the invention relates to a functionalized magnetic bead comprising at least one, magnetic bead according to the second aspect, wherein an outer silica layer is functionalized with at least one group selected from the group consisting of amino group, azide group, alkyne group, carboxyl group, thiol group, epoxy group, aryl group and alkyl group. A fourth aspect of the invention is directed to a process for functionalizing a magnetic bead according to the second aspect comprising at least one magnetic particle (M) and a silica coating, wherein the silica coating comprises at least two silica layers. A fifth aspect of the invention is related to a method for preparing magnetic Fe3O4 supra particles and a sixth aspect relates to the use of a magnetic bead according to the second aspect or of a functionalized according to the fourth aspect for immobilization of acid stable biocatalysts or for solid-phase organic synthesis using acid-stable linker.
专利号:US-5834492-A
优先权日:1995-07-10
标题 :Water soluble orally effective iron chelator
发明人:LEWIS NEIL; PATEL VITHAL; TERPINSKI JACEK; BLISS ROBERT
权利人:JACOBUS PHARMACEUTICAL CO
摘要:PCT No. PCT/US95/08519 Sec. 371 Date Apr. 7, 1997 Sec. 102(e) Date Apr. 7, 1997 PCT Filed Jul. 10, 1995 PCT Pub. No. WO96/02531 PCT Pub. Date Feb. 1, 1996There 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.
专利号:CN-119119043-A
优先权日:2024-11-13
标题 :Synthesis method of 4,4' - (1, 10-phenanthroline-4, 7-diyl) sodium diphenyl sulfonate