Jean-Marie Lehn Ph.D.

The Nobel Prize in Chemistry 1987
Nobel co-recepients Donald J. Cram, Charles J. Pedersen

Chemist. Interests: Supramolecular chemistry, Self-assembly and self-organization, Constitutional dynamic chemistry; Music, Philosophy.

Founding director, 'Chemistry, a European Journal'. Gave starting impetus to other European journals, rare manifestation of European spirit and supranationality bridging historical divides!

President, International Organization for Chemical Sciences in Development, helping chemists in developing countries.

Patents

Compiled February 2015

Publication:	1/51
Publication No:	US20020173494A1
Title:	Ammonium salts of inositol hexaphosphate, and uses thereof
Publication Type:	United States Utility Patent
Publication Date:	Nov. 21, 2002
Filing Date:	Aug. 1, 2001
Inventors:	Jean-Marie Lehn, Yves Nicolau, Stephane Vincent
Assignee:	GMP Oxycell, Inc.
Abstract:	The present invention comprises compounds, compositions thereof, and methods capable of delivering inositol hexaphospahte (IHP) to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.
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Publication:	2/51
Publication No:	US20030054556A1
Title:	Transfection compound for use as tool in the transfer of genetic material
Publication Type:	United States Utility Patent
Publication Date:	Mar. 20, 2003
Filing Date:	Aug. 28, 2002
Inventors:	Jean-Marie Lehn, Pierre Lehn, Jean-Pierre Vigneron
Assignee:	AVENTIS PHARMA S.A.,CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS),INSTITUT NATIONALE DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)
Abstract:	Transfecting compounds which include an aminoglycoside linked to a lipid via a spacer, and their polyguanidylated derivatives are provided. These compounds are useful for the in vitro, ex vivo, or in vivo transfection of nucleic acids into various cell types.
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Publication:	3/51
Publication No:	US20040014642A1
Title:	Inositol pyrophosphates, and methods of use thereof
Publication Type:	United States Utility Patent
Publication Date:	Jan. 22, 2004
Filing Date:	Apr. 29, 2003
Inventors:	Yves Nicolau, Jean-Marie Lehn, Konstantina Fylaktakidou, Ruth Greferath
Assignee:	NORMOXYS, INC.
Abstract:	The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphospahte (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.
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Publication:	4/51
Publication No:	US20040029172A1
Family Member	EP1184359A1
Title:	Generation of combinatorial libraries and assessment thereof by deconvolution
Publication Type:	United States Utility Patent
Publication Date:	Feb. 12, 2004
Filing Date:	Sept. 4, 2001
Inventors:	Jean-Marie Lehn, Olof Ramstrom, Taridoporn Bunyapaiboonsri
Assignee:	THERASCOPE A.G.
Abstract:	The present invention deals with a method for the generation of a dynamic combinatorial library of ligands for a given target, capable of binding at least two functionalities, which method comprises the following steps: (i) selecting a set of n molecules carrying functionalities which may bind to the target, which molecules are capable of reversibly binding to each other under formation of an entity, n being an integer ≥1: (ii) mixing together said set of said n molecules: (iii) subjecting the mixture to conditions allowing a reversible bond formation and cleavage under formation of entities carrying different combinations of functionalities, until equilibrium is reached: (iv) optionally transforming the said entities into ligands: (v) repeating steps (i) to (iv) n-times, each time a different molecule of said set of n molecules being omitted: (vi) assessing the ability of each of the mixtures obtained to bind to a given target.
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Publication:	5/51
Publication No:	US20040034023A1
Title:	Dibenzophenanthrolines useful for treating cancer
Publication Type:	United States Utility Patent
Publication Date:	Feb. 19, 2004
Filing Date:	Jul. 30, 2001
Inventors:	Jean-Louis Mergny, Laurent Lacroix, Marie-Paule Teulade-Fichou, Jean-Pierre Vigneron, Jean-Marie Lehn, Claude Helene
Original Assignee:	Jean-Louis Mergny, Laurent Lacroix, Marie-Paule Teulade-Fichou, Jean-Pierre Vigneron, Jean-Marie Lehn, Claude Helene
Abstract:	The invention concerns the use of aromatic compounds capable of binding with G-quadruplex structures to produce medicines with anti-telomerase effect. Said compounds correspond to formula (I) wherein: R1, R2 and R3, identical or different, represent a hydrogen atom, or a -CH2-NH-(CH2)n-X group, wherein n is an integer from 2 to 4, and X is selected among -NH2-, -N(CH3)2 radicals, a heterocyclic radical such as piperidyl, imidazolyl, morpholinyl radical, or an indole-type condensed heterocyclic radical, -Z represents CH or N, each compound comprising two nitrogen atoms in the Z positions. The invention is useful for producing anticancer medicines.
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Publication:	6/51
Publication No:	US20040043417A1
Family Member	EP1130009A1
Title:	Generation and screening of a dynamic combinatorial library
Publication Type:	United States Utility Patent
Publication Date:	Mar. 4, 2004
Filing Date:	Mar. 1, 2001
Inventors:	Jean-Marie Lehn, Olof Ramstrom
Original Assignee:	Jean-Marie Lehn, Olof Ramstrom
Abstract:	The present invention concerns a method for selectively establishing a dynamic combinatorial library of ligands for a target which binds at least two functionalities, which method comprises the following steps: selecting a plurality of functionalities which upon combination with each other ire capable of forming an entity which may bind to the at least two functionalities in the target; selecting at least one spacer group to be located between the at least two functionalities, which spacer group is of an appropriate size and/or flexibility to allow the functionalities to fit into the binding sites on the target and allowing a reversible bond formation and cleavage; creating discrete ligands by linking at least two identical or different functionalities by at least one spacer group or; linking the functionalities to fragments of the spacer group which contain functions allowing the said reversible bond formation under formation of the spacer group and cleavage of it; mixing together a plurality of different discrete ligands and/or different functionalities; subjecting the mixture to conditions allowing a reversible bond formation and cleavage; adding the target to the mixture; identifying the functionality combinations which are most appropriate for the formation of a complex between the target and the active molecule. In a further embodiment of the invention, the target is added when the discrete ligands are mixed together, in order to be present when the scrambling takes place.
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Publication:	7/51
Publication No:	US20040072801A1
Family Member	WO2004002403A2
Title:	Supplying oxygen to red blood cells; complex of inositol and sterol; antiischemic agents; cardiovascular disorders
Publication Type:	United States Utility Patent
Publication Date:	Apr. 15, 2004
Filing Date:	June 11, 2003
Inventors:	Yves Nicolau, Jean-Marie Lehn, Konstantina Fylaktakidou, Stephane Vincent
Assignee:	GMP/OXYCELL,INC.
Abstract:	The present invention comprises compounds, compositions thereof, and methods capable of delivering a broad range of anionic molecules to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering a ligand for the allosteric site of hemoglobin to the cytoplasm of the red blood cells.
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Publication:	8/51
Publication No:	US20060106000A1
Title:	Use of inositol-tripyrophosphate in treating tumors and diseases
Publication Type:	United States Utility Patent
Publication Date:	May 18, 2006
Filing Date:	July 6, 2005
Inventors:	Claude Nicolau, Ruth Greferath, Konstantina Fylaktakidou, Jean-Marie Lehn
Assignee:	NORMOXYS, INC.
Abstract:	Inositol-tripyrophosphate is an allosteric effector of hemoglobin due to its ability to cross the plasma membrane of red blood cells and deliver oxygen to solid tumors, by lowering the oxygen affinity of the hemoglobin of red blood cells. The present invention is directed to the use of inositol-tripyrophosphate to reduce hemoglobin's affinity for oxygen in circulating red blood cells. The present invention is further directed to the use of inositol-tripyrophosphate to inhibit angiogenesis and enhance radiation sensitivity of hypoxic tumors. The present invention is further directed to the use of inositol-tripyrophosphate to enhance PO2 in hypoxic tumors.
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Publication:	9/51
Publication No:	US20060241086A1
Family Member	WO2006102060A1
Title:	Calcium salt of inositol tripyrophosphate; antihypoxic agent; cancer, stroke, alzheimer's
Publication Type:	United States Utility Patent
Publication Date:	Oct. 26, 2006
Filing Date:	Mar. 17, 2006
Inventors:	Claude Nicolau, Jean-Marie Lehn, Konstantina Fylaktakidou, Ruth Greferath
Original Assignee:	NORMOXYS, INC.
Abstract:	The present invention relates to various salts of inositol tripyrophosphate including the calcium, lithium, beryllium, magnesium, potassium, strontium, barium, rubidium and cesium salts of inositol tripyrophosphate, compositions comprising these salts, methods of making the various salts, and methods of use of the above salts. Methods of use include administering the above salts in an effective amount in individuals for the treatment of various types of cancers, Alzheimer's disease, stroke and osteoporosis
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Publication:	10/51
Publication No:	US20060258626A1
Family Member	WO2007120484A2
Title:	Use of inositol-tripyrophosphate in treating tumors and diseases
Publication Type:	United States Utility Patent
Publication Date:	Nov. 16, 2006
Filing Date:	Mar. 31, 2006
Inventors:	Claude Nicolau, Ruth Greferath, Jean-Marie Lehn, Konstantina Fylaktakidou
Assignee:	NORMOXYS, INC.
Abstract:	Inositol-tripyrophosphate is an allosteric effector of hemoglobin due to its ability to cross the plasma membrane of red blood cells and deliver oxygen to solid tumors, by lowering the oxygen affinity of the hemoglobin of red blood cells. The present invention is directed to the use of inositol-tripyrophosphate to reduce hemoglobin's affinity for oxygen in circulating red blood cells. The present invention is further directed to the use of inositol-tripyrophosphate to inhibit angiogenesis and enhance radiation sensitivity of hypoxic tumors. The present invention is further directed to the use of inositol-tripyrophosphate for the treatment of various types of cancers, Alzheimer's disease, stroke and osteoporosis
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Publication:	11/51
Publication No:	US20070135389A1
Title:	Calcium and sodium mixed salt of inositol tripyrophosphate; anticancer
Publication Type:	United States Utility Patent
Publication Date:	June 14, 2007
Filing Date:	Aug. 1, 2006
Inventors:	Claude Nicolau, Jean-Marie Lehn
Assignee:	NORMOXYS, INC.
Abstract:	The present invention relates to various salts of inositol tripyrophosphate including the calcium, lithium, beryllium, magnesium, potassium, strontium, barium, rubidium and cesium salts of inositol tripyrophosphate, compositions comprising these salts, methods of making the various salts, and methods of use of the above salts. Methods of use include administering the above salts in an effective amount in individuals for the treatment of various types of cancers, Alzheimer's disease, stroke and osteoporosis.
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Publication:	12/51
Publication No:	US20070141011A1
Family Member	EP1776334A1
Title:	Use of dynamic mixtures for a controlled release of fragrances
Publication Type:	United States Utility Patent
Publication Date:	June 21, 2007
Filing Date:	Jan. 31, 2007
Inventors:	Jean-Marie Lehn, Andreas Herrmann
Assignee:	FIRMENICH SA
Abstract:	The present invention relates to a delivery system in the form of a dynamic mixture obtained by reacting together, in the presence of water, at least one hydrazine derivative with at least one perfuming, flavoring, insect repellent or attractant, bactericide or fungicide aldehyde or ketone. The inventive mixture is capable of releasing in a controlled and prolonged manner the aldehyde or ketone in the surrounding environment. Furthermore, the present invention concerns also the use of these dynamic mixtures as perfuming ingredients as well as the perfuming compositions or perfumed articles that include such mixtures.
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Publication:	13/51
Publication No:	US20070281881A1
Title:	Methods And Compositions Comprising Non-Peptide Small Molecules That Solubilize Beta Amyloid Peptide Fiber
Publication Type:	United States Utility Patent
Publication Date:	Dec. 6, 2007
Filing Date:	Feb. 18, 2005
Inventors:	Yves Nicolau, Alexey Eliseev, Jean-Marie Lehn
Assignee:	AC IMMUNE SA
Abstract:	The present invention comprises novel compositions and methods for the treatment of neurological diseases associated with beta amyloid peptide. In particular, the present invention is directed to Aβ fiber solubilization, for the treatment of amyloid-associated diseases such as Alzheimer's disease, and is described herein as being achieved by using small molecules binding to Aβ fiber The present invention further comprises novel methods of designing and screening compositions for the treatment of neurological disease wherein the design aspect comprises the modeling of molecular scaffolds having optimal structural characteristics that enable the development of small molecule compositions of non-peptide nature having desirable solubilization effects on amyloid plaques. In one embodiment, the design of the compounds comprises a molecular structure with three chemical domains that include a melatonin-like domain, a nicotine-like domain and a peptide-like domain for binding to Aβ.
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Publication:	14/51
Publication No:	US20080057005A1
Family Member	WO2006100647A1, EP1863827A1
Title:	Hydrogels for the controlled release of bioactive materials
Publication Type:	United States Utility Patent
Publication Date:	Mar. 6, 2008
Filing Date:	Sep. 6, 2007
Inventors:	Jean-Marie Lehn, Nampally SREENIVASACHARY, Andreas Herrmann
Assignee:	UNIVERSITE LOUIS PASTEUR,CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Abstract:	The present invention relates to the formation of hydrogels based on guanosine hydrazide derivatives in the presence of cations. The hydrogels can be used as a carrier/delivery system for biologically active substances such as flavors, fragrances, insect attractants or repellents, bactericides, fungicides, pharmaceuticals or agrochemicals
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Publication:	15/51
Publication No:	US20080119492A1
Title:	Anticarcinogenic agent; composition with guanine G-quadruplex spacer structure that fixing themselves to the O-quadruplex structure formed by the telomeres, thus inhibiting telomerase activity; regulate cell proliferation, anticarcinogenic agent; synergistic with other chemotherapeutic agents
Publication Type:	United States Utility Patent
Publication Date:	May 22, 2008
Filing Date:	July 28, 2006
Inventors:	Jean-Marie Lehn, Jean-Louis Mergny, Anne Petitjean, Maia-Paule Teulade-Fichou, Andrei Tchirkov, Pierre Verrelle
Original Assignee:	Jean-Marie Lehn, Jean-Louis Mergny, Anne Petitjean, Maia-Paule Teulade-Fichou, Andrei Tchirkov, Pierre Verrelle
Abstract:	The present invention relates to compositions and methods for treating cancer and other disease states characterized by abnormal cell proliferation. In particular, the present invention relates to certain novel non-nucleoside pharmacologically active compounds that alter telomere and telomerase functions, regulate cell proliferation and/or treat cancer and other diseases characterized by abnormal cell proliferation. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and to treat cancer or to inhibit the proliferation of the rumor cells, and to treat other proliferative conditions.
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Publication:	16/51
Publication No:	US20080200437A1
Family Member	WO2008082658A2
Title:	Polyphosphorylated inositol derivatives; allosteric effectors, cell signaling molecule analogs; hypoxia related diseases
Publication Type:	United States Utility Patent
Publication Date:	Aug. 21, 2008
Filing Date:	Dec. 31, 2007
Inventors:	Jean-Marie Lehn, Srinivasu Pothukanuri, Alexandros Koumbis, Carolina Duarte, Claude Nicolau,
Assignee:	UNIVERSITE DE STRASBOURG
Abstract:	The present invention is directed to polyphosphorylated and pyrophosphate derivatives of cyclitols. More particularly, the invention relates to polyphosphorylated and pyrophosphate derivatives of inositols. The invention also relates to compositions of the polyphosphorylated and pyrophosphate derivatives of inositol and other similar, more lipophilic derivatives, and their use as allosteric effectors, cell-signaling molecule analogs, and therapeutic agents.
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Publication:	17/51
Publication No:	US20080312138A1
Family Member	WO2008134082A1
Title:	Erythropoietin complementation or replacement
Publication Type:	United States Utility Patent
Publication Date:	Dec. 18, 2008
Filing Date:	May 1, 2008
Inventors:	Claude Nicolau, Jean-Marie Lehn, Ruth Greferath
Assignee:	UNIVERSITE DE STRASBOURG
Abstract:	The present invention provides methods and compositions to replace up to 90% of erythropoietin use in the treatment of anemias and hypoxias. The method employs acid and salt forms of inositol-tripyrophosphate (ITPP) isomers to shift the P50 value of hemoglobin, thereby improving the rate and efficiency of oxygenation by blood even when red blood cell counts are low. Indications for the new method include anemias and hypoxia arising from infection, chemotherapy, premature birth, altitude change, compromised lung or heart function, aplastic anemia and anemia associated with a myelodysplastic syndrome, and other causes.
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Publication:	18/51
Publication No:	US20090029951A1
Title:	Antihypoxia agent; monocalcium tetrasodium salt of inositol tripyrophosphate; cancer, Alzheimer's
Publication Type:	United States Utility Patent
Publication Date:	Jan. 19, 2009
Filing Date:	May 30, 2008
Inventors:	Yvec Claude NICOLAU, Jean-Marie Lehn, Konstantina C. FYLAKTAKIDOU, Ruth Greferath
Assignee:	UNIVERSITE DE STRASBOURG
Abstract:	The present invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.
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Publication:	19/51
Publication No:	US20090306196A1
Family Member	WO2007113711A2
Title:	Imine based liquid crystals for the controlled release of bioactive materials
Publication Type:	United States Utility Patent
Publication Date:	Dec 10, 2009
Filing Date:	Mar. 19, 2007
Inventors:	Jean-Marie Lehn, Nicolas Giuseppone, Andreas Herrmann
Original Assignee:	FIRMENICH SA
Abstract:	The present invention relates to a delivery system based on a film of an imine forming liquid crystalline phase, mixed with at least with one biologically active substance, to which a constant or variable electric field can be applied. The delivery system can be used as a delivery system for biologically active substances such as flavors, fragrances, bactericides, fungicides, insecticides, insect attractants or repellents, agrochemicals or pharmaceuticals.
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Publication:	20/51
Publication No:	US20100029593A1
Title:	Calcium/sodium salt of inositol tripyrophosphate as an allosteric effector of hemoglobin
Publication Type:	United States Utility Patent
Publication Date:	Feb.4, 2010
Filing Date:	Sept. 4, 2009
Inventors:	Yves Claude Nicolau, Jean-Marie Lehn, Fylaktakidou Konstantina C, Ruth Greferath
Original Assignee:	NORMOXYS, INC.
Abstract:	The present invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.
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Publication:	21/51
Publication No:	US20100029594A1
Title:	Calcium/sodium salt of inositol tripyrophosphate as an allosteric effector of hemoglobin
Publication Type:	United States Utility Patent
Publication Date:	Feb. 4, 2010
Filing Date:	July 21, 2009
Inventors:	Yves Claude Nicolau, Jean-Marie Lehn, Konstantina C. FYLAKTAKIDOU, Ruth Greferath
Original Assignee:	NORMOXYS, INC.
Abstract:	The present invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.
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Publication:	22/51
Publication No:	US20100035974A1
Family Member	WO2008040792A2
Title:	Compositions comprising a sirna and lipidic 4,5-disubstituted 2-deoxystreptamine ring aminoglycoside derivatives and uses thereo
Publication Type:	United States Utility Patent
Publication Date:	Feb. 11, 2010
Filing Date:	Oct. 4, 2007
Inventors:	Jean-Marie Lehn, Jean-Pierre Vigneron, Pierre Lehn, Bruno Pitard
Original Assignee:	CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Abstract:	The present invention relates to a composition comprising a siRNA and a transfecting compound consisting of an aminoglycoside of the class of 4,5-disubstituted 2-deoxystreptamine ring linked via a spacer molecule to a lipid moiety of formula -(R1)R2 wherein R1 and R2 represent, independently of one another, a hydrogen atom or a fatty aliphatic chain or R1 or R2 is absent, with the proviso that at least one of R1 and R2 represents a fatty aliphatic chain; or -OR3 or -NR3 wherein R3 represents a steroidal derivative. The invention also concerns in vitro and in vivo applications of these compositions.
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Publication:	23/51
Publication No:	US20100098650A1
Family Member	WO2008093272A2
Title:	Controlled release of active aldehydes and ketones from equilibrated dynamic mixtures
Publication Type:	United States Utility Patent
Publication Date:	Apr. 22, 2010
Filing Date:	Jan. 28, 2008
Inventors:	Andreas Herrmann, Guillaume Godin, Jean-Marie Lehn
Original Assignee:	UNIVERSITE DE STRASBOURG,CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Abstract:	The present invention concerns a dynamic mixture obtained by combining, in the presence of water, at least one diamine derivative that includes at least one benzylamine moiety, with at least one active aldehyde or ketone. The inventive mixture is capable of releasing in a controlled and prolonged manner the active compound, in particular those that are perfuming ingredients, into the surrounding environment.
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Publication:	24/51
Publication No:	US20100226875A1
Family Member	WO2007085991A2
Title:	Controlled release of active aldehydes and ketones from equilibrated dynamic mixtures
Publication Type:	United States Utility Patent
Publication Date:	Sept. 9, 2010
Filing Date:	Jan. 19, 2007
Inventors:	Andreas Herrmann, Jean-Marie Lehn, Guillaume Godin
Assignee:	FIRMENICH SA
Abstract:	The present invention relates to a dynamic mixture in the form of a dynamic mixture obtained by reacting together, in the presence of water, at least one O-substituted hydroxylamine or S-substituted thiohydroxylamine derivative with at least one perfuming, flavoring, insect repellent or attractant, bactericide or fungicide aldehyde or ketone. This mixture is capable of releasing in a controlled and prolonged manner the aldehyde or ketone into the surrounding environment. Furthermore, the present invention concerns also the use of these dynamic mixtures as perfuming ingredients as well as the perfuming compositions or perfumed articles that include these mixtures.
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Publication:	25/51
Publication No:	US20110150803A1
Family Member	WO2010020954A1
Title:	Equilibrated dynamic mixtures containing stabilized hemiacetals for the controlled release of active alcohols
Publication Type:	United States Utility Patent
Publication Date:	June 23, 2011
Filing Date:	Aug. 19, 2009
Inventors:	Jean-Marie Lehn, Dusan Drahonovsky, Andreas Herrmann
Assignee:	FIRMENICH SA
Abstract:	The present invention concerns a dynamic mixture containing stabilized hemiacetals obtainable by combining at least one specific aldehyde derivative with at least one active alcohol and optionally a stabilizing salt. The dynamic mixture is capable of releasing into the surrounding environment and in a controlled and prolonged manner an active compound such as a perfuming or flavoring ingredient.
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Publication:	26/51
Publication No:	US20120003161A1
Title:	Use of inositol-tripyrophosphate in treating tumors and diseases
Publication Type:	United States Utility Patent
Publication Date:	Jan. 5, 2012
Filing Date:	Aug. 18, 2011
Inventors:	Claude Nicolau, Ruth Greferath, Konstantina C. FYLAKTAKIDOU, Jean-Marie Lehn
Assignee:	Normoxys, Inc
Abstract:	Inositol-tripyrophosphate is an allosteric effector of hemoglobin due to its ability to cross the plasma membrane of red blood cells and deliver oxygen to solid tumors, by lowering the oxygen affinity of the hemoglobin of red blood cells. The present invention is directed to the use of inositol-tripyrophosphate to reduce hemoglobin's affinity for oxygen in circulating red blood cells. The present invention is further directed to the use of inositol-tripyrophosphate to inhibit angiogenesis and enhance radiation sensitivity of hypoxic tumors. The present invention is further directed to the use of inositol-tripyrophosphate to enhance PO2 in hypoxic tumors.
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Publication:	27/51
Publication No:	US20120003327A1
Title:	Method of reducing multi-drug resistance using inositol tripyrophosphate
Publication Type:	United States Utility Patent
Publication Date:	Jan. 5, 2012
Filing Date:	Feb. 23, 2011
Inventors:	Yves Claude Nicolau, Jean-Marie Lehn, Claudine Kieda
Assignee:	Normoxys, Inc
Abstract:	Inositol trisphosphate (ITPP) causes normalization of tumor vasculature and is a particularly effective cancer therapy when a second chemotherapeutic agent is administered following partial vascularization. ITPP also treats, alone or in combination, multi-drug resistant cancers. ITPP can also be used to reduce the amount of a second chemotherapeutic drug required for anticancer activity. In addition, ITPP enhances immune response and treats hyperproliferative disorders.
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Publication:	28/51
Publication No:	US20140088036A1
Title:	Polyphosphate and pyrophosphate derivative of saccharides
Publication Type:	United States Utility Patent
Publication Date:	Mar. 27, 2014
Filing Date:	Sept. 30, 2011
Inventors:	Jean Marie Lehn, Yves Claude Nicolau, Rajamalleswaramma Jogireddy, Adam H. Brockman, John Hey, Yongxin Yu
Assignee:	Normoxys, Inc
Abstract:	The present invention provides, among other things, phosphorylated and pyrophosphate derivatives of mono-, di- and oligosaccharides, as well as structural derivatives of these compounds. These compounds have a variety of uses including for pharmaceutical applications. Also provided are methods of use in the treatment of disease, including diseases related to oxygen delivery.
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Publication:	29/51
Publication No:	US20140142052A1
Title:	Phosphorylated polyols, pyrophosphates, and derivatives thereof having biological activity
Publication Type:	United States Utility Patent
Publication Date:	May 22, 2014
Filing Date:	May 17, 2013
Inventors:	Jean-Marie Lehn, Yves Claude Nicolau, Srinivasu Pothukanuri, Adam Brockman, John Hey, Jeremy Yu
Assignee:	Normoxys, Inc
Abstract:	The present invention provides phosphorylated and pyrophosphate derivatives of polyols, and structural derivatives of these compounds, and provides pharmaceutical compositions comprising the same. The compounds and compositions disclosed herein have various biological activities, including for example, as allosteric effectors of hemoglobin and/or as kinase inhibitors. The present invention further provides methods for therapy in human or mammalian patients, and methods for synthesis of biologically active compounds and their intermediates.
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Publication:	30/51
Publication No:	US 3888877 A
Title:	Macrocyclic compounds and complexes thereof
Publication Type:	United States Utility Patent
Publication Date:	June 10, 1975
Filing Date:	Mar. 26, 1973
Inventors:	Jean-Marie Lehn
Assignee:	Schering Corp
Abstract:	No Abstract
Representative Figure:	No Figure
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Publication:	31/51
Publication No:	US3890278A
Title:	Anionic polymerization
Publication Type:	United States Utility Patent
Publication Date:	June 17, 1975
Filing Date:	Sept. 26, 1973
Inventors:	Sylvie Boileau, Alain Andre Cau, Bernd Kaempf, Jean-Marie Lehn, Jean Robert Moinard, Serge Fernand Raynal, Francois Schue
Assignee:	Poudres & Explosifs Ste Nale
Abstract:	A novel process for polymerization or copolymerization of monomers is described, according to which the reaction is carried out in the presence of an anionic initiator and a macroheterocyclic complexing agent of formula
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Publication:	32/51
Publication No:	US3966766A
Title:	Monocyclic macrocyclic compounds and complexes thereof
Publication Type:	United States Utility Patent
Publication Date:	June 29, 1976
Filing Date:	Mar. 20, 1975
Inventors:	Jean-Marie Lehn
Assignee:	Schering Corportion
Abstract:	Novel monocyclic macrocyclic compounds having nitrogen bridgehead atoms and having in the hydrocarbon bridging chains at least two additional hetero atoms selected from the group consisting of sulfur, oxygen, and nitrogen, when admixed with a compatible cation-donor compound form stable cation-containing macrocyclic complexes which, in turn, can be conveniently dissociated by addition of acid or a quaternizing agent. The novel macrocyclics are valuable for use in the same way and for the same purposes as chelating agents.
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Publication:	33/51
Publication No:
Title:	Polycyclic macrocyclic compounds
Publication Type:	United States Utility Patent
Publication Date:	Feb. 28, 1978
Filing Date:	Oct. 4, 1972
Inventors:	Jean-Marie Lehn
Assignee:	L'Agence Nationale de Valorisation de la Recherech (ANVAR)
Abstract:	Novel polycyclic macrocyclic compounds having four tertiary nitrogen bridgehead atoms and six bridging chains, each of which have not more than twelve directly connecting atoms between each pair of bridgehead nitrogens, said bridging chains being hydrocarbon chains and hetero-substituted hydrocarbon chains having at least one hetero connecting atom selected from the group consisting of oxygen, sulfur, and nitrogen, at least two of said chains being hetero substituted. When admixed with a compatible cation-donor compound, the polycyclic macrocyclic compounds form stable cation-containing macrocyclic complexes which, in turn, can be conveniently dissociated by addition of acid or a quaternizing acid. The novel polycyclic macrocyclics are valuable for use in the same way and for the same purposes as chelating agents. The polycyclic macrocyclic compounds are prepared by condensation reactions utilizing high dilution techniques, e.g. by condensing a monocyclic macrocyclic having secondary nitrogen bridgeheads with a substituted hydrocarbon di-carbonyl halide followed by reduction of the resulting lactam or, alternatively, by condensing a monocyclic macrocyclic having secondary nitrogen bridgeheads with a substituted hydrocarbon dihalide (or di-sulfonate).
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Publication:	34/51
Publication No:	US4116887A
Title:	Antionic polymerization
Publication Type:	United States Utility Patent
Publication Date:	Sept. 26, 1978
Filing Date:	Jan. 9, 1975
Inventors:	Jean-Marie Lehn, Francois Schue, Sylvia Boileau, Bernd Kaempf, Alain Andre Cau, Jean Robert Moinard, Serge Fernand Raynal
Assignee:	Societe Nationale Des Poudres Et Explosifs
Abstract:	A novel process for polymerization or copolymerization of monomers is described, according to which the reaction is carried out in the presence of an anionic initiator and a macroheterocyclic complexing agent of formula ##STR1## in which: EACH R1 is a hydrogen atom, a hydrocarbon group or an alkoxycarbonyl group, or the two R1 together can form a group of the general formula: ##STR2## THAT IS TO SAY FORMING A THIRD BRIDGE BETWEEN THE TWO NITROGEN ATOMS IN THE MOLECULE, A is a hydrocarbon group, D is an oxygen or sulfur atom or a hydrocarbon group, with the proviso that at least two of the groups D are oxygen or sulfur atoms and that, if each R1 is hydrogen, a hydrocarbon group or an alkoxycarbonyl group, one of these two groups D is oxygen or sulfur and the other is oxygen, n and p are integers ranging from 1 to 3, and m is 2 or 3.
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Publication:	35/51
Publication No:	US4156683A
Title:	Complexes of macrocyclic compounds
Publication Type:	United States Utility Patent
Publication Date:	May 29, 1979
Filing Date:	Mar. 20, 1975
Inventors:	Jean-Marie Lehn
Assignee:	Schering Corporation
Abstract:	Novel macrocyclic (monocyclic and bicyclic) compounds having nitrogen bridgehead atoms and having in the hydrocarbon bridging chains at least two additional hetero atoms selected from the group consisting of sulfur, oxygen, and nitrogen, when admixed with a compatible cation-donor compound form stable cation-containing macrocyclic complexes which, in turn, can be conveniently dissociated by addition of acid or a quaternizing agent. The novel macrocyclics are valuable for use in the same way and for the same purposes as chelating agents.
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Publication:	36/51
Publication No:	US4927923A
Title:	Immunology
Publication Type:	United States Utility Patent
Publication Date:	May 22, 1990
Filing Date:	Sept. 20, 1985
Inventors:	Gerald Mathis, Jean-Marie Lehn
Assignee:	Compagnie Oris Industries
Abstract:	The invention relates to macropolycyclic rare earth complexes, namely cryptates which are useful as fluorescent tracers.
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Publication:	37/51
Publication No:	US5162508A
Title:	Rare earth cryptates, processes for their preparation, synthesis intermediates and application as fluorescent tracers
Publication Type:	United States Utility Patent
Publication Date:	Nov. 10, 1992
Filing Date:	Jul. 16, 1991
Inventors:	Jean-Marie Lehn, Mathis Gerard, Beatrice Alpha, Robert Deschenaux, Etienne Jolu
Assignee:	Compagnie Oris Industries
Abstract:	The invention relates to rare earth cryptates consisting of at least one rare earth salt complexed by a macropolycyclic compound corresponding to one of formulae I or II below, in which: the ring ##STR1## is the N2 O4 macrocycle, the N2 O3 macrocycle or a bis-bipyridine macrocycle; Y is a spacer arm or group which consists of a divalent organic radical selected from linear or branched C1 to C20 alkylene groups optionally containing one or more double bonds and/or optionally being interrupted by one or more heteroatoms such as oxygen, nitrogen, sulfur or phosphorus, or from C5 to C8 cycloalkylene groups or C6 to C14 arylene groups, the said alkylene or arylene groups optionally being substituted by alkyl, aryl or sulfonate groups; Z is a functional group capable of bonding covalently with a biological substance; R is a methyl group or represents the group --Y--Z ##STR2##
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Publication:	38/51
Publication No:	US5220012A
Title:	Cryptates
Publication Type:	United States Utility Patent
Publication Date:	June 15, 1993
Filing Date:	Mar 5, 1990
Inventors:	Gerald Mathis, Jean-Marie Lehn
Assignee:	Compagnie Oris Industries
Abstract:	The invention relates to macropolycyclic rare earth complexes, namely cryptates which are useful as fluorescent tracers.
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Publication:	39/51
Publication No:	US5296475A
Title:	Methanediphosphonic acids and crown compounds for treatment of bone disorders or hypercalcemia
Publication Type:	United States Utility Patent
Publication Date:	Mar 22, 1994
Filing Date:	Dec. 17, 1992
Inventors:	Gerald Flesch, Jean-Marie Lehn
Assignee:	Ciba-Geigy Corperation
Abstract:	The invention relates to pharmaceutical compositions for peroral administration comprising (a) pharmaceutically useful methanediphosphonic acid derivatives, e.g. those of formula I ##STR1## wherein R1 and R2 are as defined in the specification, or pharmaceutically acceptable salts thereof, (b) specific macrocyclic polyethers and optionally (c) pharmaceutically acceptable adjuvants. The pharmaceutical compositions are prepared in a manner known per se. A method of treating hypercalcemia and osteolytic bone metastases with these compositions is also disclosed herein.
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Publication:	40/51
Publication No:	US5457184A
Family Member	WO 1993005049 A1
Title:	Rare earth macrocyclic complexes and use thereof for reduction of disturbances in an assay using fluorescence
Publication Type:	United States Utility Patent
Publication Date:	Oct 10, 1995
Filing Date:	Aug. 28, 1992
Inventors:	Jean-Marie Lehn, Christine O. Roth, Gerard Mathis
Assignee:	Cis Bio International
Abstract:	The invention relates to macrocyclic rare earth complexes which consist of at least one rare earth salt complexed by a macrocyclic compound of formula (I): ##STR1## in which: the bivalent radicals A, B, C and D, which are identical or different, are hydrocarbon chains optionally containing one or more heteroatoms, at least one of said radicals containing at least one molecular unit or essentially consisting of a molecular unit possessing a triplet energy greater than the energy of the emission level of the complexed rare earth ion, at least one of said radicals consisting of a substituted or unsubstituted nitrogen-containing heterocyclic system in which at least one of the nitrogen atoms carries an oxy group, and it being possible for one of the radicals C or D not to exist; and X1 and X2, which are identical or different, are hydrogen or a hydrocarbon chain (CH2)n optionally interrupted by 1 or more heteroatoms, n being an integer from 1 to 10, with the proviso that if the radicals A and/or B are a nitrogen-containing heterocyclic system in which at least one of the nitrogen atoms carries an oxy group, the radicals C and/or D are selected from biquinolines, biisoquinolines, bipyridines, terpyridines, coumarins, bipyrazines, bipyrimidines and pyridines, and to their use for reducing the perturbations in a fluorescent assay.
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Publication:	41/51
Publication No:	US6143729A
Family Member	WO 1997031935 A1
Title:	Compounds related to the amidinium family, pharmaceutical compositions containing same, and uses thereof
Publication Type:	United States Utility Patent
Publication Date:	Nov. 7, 2000
Filing Date:	Feb. 28, 1997
Inventors:	Jean-Marie Lehn, Pierre Lehn, Jean-Pierre Vigneron
Assignee:	Aventis Pharma S.A.
Abstract:	Novel amidinium derivatives of formula (I), wherein R1 is a cholesterol derivative or an alkylamino-NR'R" grouping, and each of R2 and R3 is independently a hydrogen atom or a grouping of formula (II), wherein each of R4 and R5 is independently a hydrogen atom or a grouping of formula (III), are disclosed. The corresponding pharmaceutical compositions, which are particularly useful in gene therapy for transferring therapeutic genes into cells, are also disclosed. ##STR1##
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Publication:	42/51
Publication No:	WO2004003044A2
Title:	Dynamers: polymeric materials exhibiting reversible formation and component exchange
Publication Type:	United States Utility Patent
Publication Date:	Jan 8, 2004
Filing Date:	Jun 24, 2003
Inventors:	Lehn Jean-Marie, Skine W G
Assignee:	Lehn Jean-Marie, Skene W G
Abstract:	Alternating co-polymers involving the polycondensation of dihydrazides or diamines with dialdehydes reversibly exchange either one or both of their fundamental repeating monomer units in the presence of different monomer units. Furthermore, upon exchange of one of the repeating monomer units, the original monomer unit displaced can be re-introduced into the polymer, or the remaining unexchanged original monomer unit may also be interchanged. The polymers subjected to monomer exchange/interchange exhibit vastly different physical properties than those of the original unexchanged polymer. These dynamic, reversible polymers are therefore able to incorporate, decorporate or reshuffle their constituting monomers, in particular, with respect to environmental physical or chemical factors (heat, light, chemical entities, etc.). They thus have combinatorial features and represent adaptive materials.
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Publication:	43/51
Publication No:	WO2006003905A1
Title:	Self-restorable material
Publication Type:	United States Utility Patent
Publication Date:	Jan 12, 2006
Filing Date:	Jun 22, 2005
Inventors:	Jean-Marie Lehn, Takashi Ono
Assignee:	Jean-Marie Lehn, Mitsui Chemicals Inc, Takashi Ono, Univ Pasteur
Abstract:	A self-restorable material which comprises a resin having a hydrazone bond represented by the chemical formula (1) (wherein R is hydrogen or a hydrocarbon group) in the main chain and/or a side chain. The self-restorable material has no limitation in its self-restorability and exerts the self-restorability even in an ordinary-pressure room-temperature air without the need of a specific external factor such as heating. Furthermore, various properties or functions can be imparted to the material at will. The material is extremely useful in material applications where self-restorability is required.
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Publication:	44/51
Publication No:	WO2007081315A1
Title:	Use of inositol-tripyrophosphate in treating tumors and diseases
Publication Type:	United States Utility Patent
Publication Date:	Jul 19, 2007
Filing Date:	Jan 6, 2006
Inventors:	Claude Nicolau, Ruth Greferath, Konstantina C Fylaktakidou, Jean-Marie Lehn
Assignee:	Oxyplus Inc, Claude Nicolau, Ruth Greferath, Konstantina C Fylaktakidou, Jean-Marie Lehn
Abstract:	Inositol-tripyrophosphate is an allosteric effector of hemoglobin due to its ability to cross the plasma membrane of red blood cells and deliver oxygen to solid tumors, by lowering the oxygen affinity of the hemoglobin of red blood cells. The present invention is directed to the use of inositol-tripyrophosphate to reduce hemoglobin's affinity for oxygen in circulating red blood cells. The present invention is further directed to the use of inositol-tripyrophosphate to inhibit angiogenesis and enhance radiation sensitivity of hypoxic tumors. The present invention is further directed to the use of inositol-tripyrophosphate to enhance PO2 in hypoxic tumors.
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Publication:	45/51
Publication No:	WO2009145751A1
Title:	Calcium/sodium salt of inositol tripyrophosphate as an allosteric effector of hemoglobin
Publication Type:	United States Utility Patent
Publication Date:	Dec 3, 2009
Filing Date:	May 30, 2008
Inventors:	Claude Nicolau, Jean-Marie Lehn, Konstantina C. Fylaktakidou, Ruth Greferath
Assignee:	Oxyplus, Inc
Abstract:	The present invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.
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Publication:	46/51
Publication No:	WO 1988008419 A1
Title:	Oligobipyridine ligands, process for obtaining them and application as complexing agents
Publication Type:	United States Utility Patent
Publication Date:	Nov 3, 1988
Filing Date:	Apr 29, 1988
Inventors:	Margaret Harding, Yong Bing He, Jean-Marie Lehn, Annie Rigault, Jay Siegel
Assignee:	Orus Sa
Abstract:	The invention concerns oligobipyridine ligands of formula (I), in which, Z1 and Z2, identical or different, stand for C1-C12 alkylene groups, Y is oxygen or sulphur or; Z1-Z2 stand for -CH=CH- or -CH2-CH2- groups, n is an integer between 1 and 6; R1 and R2 identical or different, stand for C1-C5 alkyl groups in particular the methyl group or the ethyl group, the radicals -Z1YH, -Z2YH, -Z1X or -Z2X in which Y is as defined above and X is a halogen atom or a group of formula (a), in which R4 is a C1-C5 alkyl group, R3 is hydrogen, a carboxy group or an amido group.
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Publication:	47/51
Publication No:	WO 1989005813 A1
Title:	Rare-earth cryptates, processes for obtaining them, intermediate synthesis products and use as fluorescent markers
Publication Type:	United States Utility Patent
Publication Date:	Jun 29, 1989
Filing Date:	Dec 16, 1988
Inventors:	Beatrice Alpha, Robert Deschenaux, Etienne Jean-Pierre Jolu, Jean-Marie Lehn, Gerard Mathis
Assignee:	Oris Sa
Abstract:	The invention concerns rare earth cryptates composed of at least one rare-earth salt complexed by a macropolycyclic compound having one of the formulae (I or II) in which the cycle (a) is the N2O4 macrocycle, the N2O3 macrocycle or the bis-bipyridine macrocycle, Y is a group or a spacing arm consisting of a bivalent organic radical chosen from the C1 to C20 linear or branched alkaline groups, possibly containing one or more double bonds and/or possibly being interrupted by one or more hetero atoms such as oxygen, nitrogen, sulphur or phosphorus or the C5 to C8 cycloalkaline groups or from the C6 to C14 arylene groups, said alkaline or arylene groups being possibly substituted by alkyl, aryl or sulfonate groups; Z is a functional group capable of forming a covalent bond with a biological substance; R is a methyl group or the -Y-Z- group; R' is hydrogen or a -COOR'' group in which R'' is a C1 to C10 alkyl group and preferably the methyl, ethyl or tertiobutyl group or R' is a CO-NH-Y-Z group.
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Publication:	48/51
Publication No:	WO 1995007275 A1
Title:	Composes photochromiques, procede et produits intermediaires pour leur production, et leur utilization
Publication Type:	United States Utility Patent
Publication Date:	Mar 16, 1995
Filing Date:	Sep 3, 1994
Inventors:	Sylvain Gilat, Stephen Kawai, Jean-Marie Lehn
Assignee:	Ciba Geigy Ag, Sylvain Gilat, Stephen Kawai, Lehn Jean Marie
Abstract:	The invention concerns compounds of formula (I ou II), or their salts, in which the radicals have for instance the following meaning: R1 and R2 are each hydrogen, C1-C8 alkyl, cyano or -NO2 or together are (-CF2-)m, -CF(OCH3)-CF2-CF(OCH3)-, -CF[NH2]-CF2-CF[-NH2]-, -C(=O)-O-C(=O)-, -C(=NH)-NH-C(=NH)- or -C(=O)-NH-C(=O)-; R3 and R4 are methyl; A1 and A2, independently of each other, are formyl, an acetal or thioacetal radical, phenyl, pyridiniumyl, pyridyl or other heterocyclic groups, or groups of formula (III or IV); X1 and X2 are S, O or N(R18); Y1 and Y2 are =CH- or =N-; R5 and R6 are hydrogen, halogen, -B(OH)2, C1-C8 alkyl, C1-C8 alkylthio, cyano, nitro, -N(R17)2, -C(=O)-R19, -C=CH, phenyl or pyridyl, and R9 is a bridging group containing up to three hetero-atoms. The invention also concerns the preparation of these compounds for example by reacting alkenes with 3-haloheterocycles in the presence of a strong base; intermediates of formula (VIb) used to produce these compounds, where A2, R4, X2 and Y2 are as above, where A2 cannot be -CHO, but additionally -B(OH)2 and -CH=NR26; compositions containing these compounds, and the use of the compounds or compositions described above as dyes, colour indicators, photo-switches or data stores.
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Publication:	49/51
Publication No:	DE 10146970 A1
Title:	Self-organizing assemblage of porphyrin molecules useful for converting light into chemical or electrical energy comprises porphyrin molecules with organophilic and hydrogen-bonding substituents
Publication Type:	United States Utility Patent
Publication Date:	Apr 17, 2003
Filing Date:	Sep 24, 2001
Inventors:	Teodor Silviu Balaban, Jean-Marie Pierre Lehn, Sergei Lebedkin, Marie-Josephe Brienne
Assignee:	Karlsruhe Forschzent
Abstract:	Self-organizing assemblage of porphyrin molecules comprises porphyrin molecules with at least four substituents, including at least one that increases solubility in organic solvents and at least one that forms hydrogen bonds with the substituents of adjacent molecules, where at least one of the H-bonding substituents comprises a recognition group that is attached to the porphyrin molecule though a spacer and is capable of forming multiple H bonds. An Independent claim is also included for the production of self-organizing assemblages by condensing dodecanal and/or an alkyl formylbenzoate with pyrrole and oxidizing the product to form a mixture of porphyrins with undecyl, 3,5-di-t-butylphenyl and/or alkoxycarbonylphenyl substituents; separating the porphyrins; hydrolyzing the alkoxycarbonyl groups to free acid groups; and esterifying these with alcohols bearing recognition groups.
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Publication:	50/51
Publication No:	FR2774998A1
Title:	Photochromic material undergoing stable light-induced variation in refractive index and/or birefringence useful in optical data recording and reading systems, ophthalmic lenses, etc.
Publication Type:	United States Utility Patent
Publication Date:	No Information
Filing Date:	No Information
Inventors:	BITEAU JOHN; CHAPUT FREDERIC; BOILOT JEAN PIERRE; PERETTI JACQUES; SAFAROV VIATCHESLAV; LEVY YVES; DARRACQ BRUNO; TSIVGOULIS GERASIMOS; LEHN JEAN MARIE
Assignee:	ECOLE POLYTECH
Abstract:	Photochromic material capable of undergoing a stable light-induced variation in refractive index and/or birefringence outside the absorption bands of the photochromic material comprises optically anisotropic photochromic molecules optionally covalently bonded to a solid matrix. An Independent claim is also included for a photochromic material capable of undergoing a stable light-induced variation in refractive index and/or birefringence in the infrared, comprising optically anisotropic photochromic molecules optionally covalently bonded to a solid matrix.
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Publication:	51/51
Publication No:	FR2829136A1
Title:	New transfection compounds having an aminoglycoside group linked via a spacer to a lipid such as cholesterol
Publication Type:	United States Utility Patent
Publication Date:	No Information
Filing Date:	No Information
Inventors:	LEHN JEAN MARIE; LEHN PIERRE; VIGNERON JEAN PIERRE
Assignee:	Avenis Pharma Sa
Abstract:	Transfection compounds, especially those of formula (I), having an aminoglycoside group linked via a spacer to a lipid, and their polyguanidyl derivatives, their isomers, mixtures and salts. Transfection compounds, especially those of formula A-Y-L (I), having an aminoglycoside group linked via a spacer to a lipid, and their polyguanidyl derivatives, their isomers, mixtures and salts. A = aminoglycoside or its polyguanidylated derivative; Y = spacing group; L = -(R1)R2 or -N(R3) or -O-R3; R1, R2 = H or an aliphatic chain, or one of these groups is absent, such that at least one of them is an aliphatic group; and R3 = steroid derivative. Independent claims are also included for: (1) compositions containing compounds as described together with a nucleic acid, preferably with one or more adjuvants such as lipids, peptides, proteins and polymers; and (2) a method of treating the human or animal body which comprises contacting the nucleic acid with a transfecting compound as described to form a complex, and contacting the human or animal cells with this complex.
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