Patent classifications
C07F9/6524
BIFUNCTIONAL do2pa DERIVATIVES, CHELATES WITH METALLIC CATIONS AND USE THEREOF
Disclosed are chelates resulting from the complexation of bifunctional do2pa derivatives ligands of formula (I), wherein the substituents R.sup.1, R.sup.1′, R.sup.2, R.sup.2′, R.sup.3, R.sup.3′, L.sup.1, L.sup.1′, L.sup.2 and L.sup.2′ are defined as in the claims, with metallic cations, especially Pb(II) and Bi(III). Also disclosed are bifunctional do2pa derivatives ligands of formula (I), as well as the use of chelates in nuclear medicine and the use of ligands in cations detection or epuration of effluents.
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BIFUNCTIONAL do2pa DERIVATIVES, CHELATES WITH METALLIC CATIONS AND USE THEREOF
Disclosed are chelates resulting from the complexation of bifunctional do2pa derivatives ligands of formula (I), wherein the substituents R.sup.1, R.sup.1′, R.sup.2, R.sup.2′, R.sup.3, R.sup.3′, L.sup.1, L.sup.1′, L.sup.2 and L.sup.2′ are defined as in the claims, with metallic cations, especially Pb(II) and Bi(III). Also disclosed are bifunctional do2pa derivatives ligands of formula (I), as well as the use of chelates in nuclear medicine and the use of ligands in cations detection or epuration of effluents.
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APPLICATION OF CLICK CHEMISTRY FOR SIGNAL AMPLIFICATION IN IHC AND ISH ASSAYS
Applicants have developed an amplification system and methodology for IHC and ISH staining that utilizes “click chemistry” to covalently bind reporter molecules to tissue.
APPLICATION OF CLICK CHEMISTRY FOR SIGNAL AMPLIFICATION IN IHC AND ISH ASSAYS
Applicants have developed an amplification system and methodology for IHC and ISH staining that utilizes “click chemistry” to covalently bind reporter molecules to tissue.
PYRAZOLYL QUINOXALINE KINASE INHIBITORS
- Gordon Saxty ,
- Christopher William Murray ,
- Valerio Berdini ,
- Gilbert Ebai Besong ,
- Christopher Charles Frederick Hamlett ,
- Christopher Norbert JOHNSON ,
- Steven John Woodhead ,
- Michael Reader ,
- David Charles Rees ,
- Laurence Anne Mevellec ,
- Patrick René Angibaud ,
- Eddy Jean Edgard Freyne ,
- Tom Cornelis Hortense Govaerts ,
- Johan Erwin Edmond Weerts ,
- Timothy Pietro Suren Perera ,
- Ronaldus Arnodus Hendrika Joseph Gilissen ,
- Berthold Wroblowski ,
- Jean Fernand Armand Lacrampe ,
- Alexandra Papanikos ,
- Olivier Alexis Georges Querolle ,
- Elisabeth Thérèse Jeanne Pasquier ,
- Isabelle Noëlle Constance Pilatte ,
- Pascal Ghislain André Bonnet ,
- Werner Constant Johan Embrechts ,
- Rhalid Akkari ,
- Lieven Meerpoel
The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
PYRAZOLYL QUINOXALINE KINASE INHIBITORS
- Gordon Saxty ,
- Christopher William Murray ,
- Valerio Berdini ,
- Gilbert Ebai Besong ,
- Christopher Charles Frederick Hamlett ,
- Christopher Norbert JOHNSON ,
- Steven John Woodhead ,
- Michael Reader ,
- David Charles Rees ,
- Laurence Anne Mevellec ,
- Patrick René Angibaud ,
- Eddy Jean Edgard Freyne ,
- Tom Cornelis Hortense Govaerts ,
- Johan Erwin Edmond Weerts ,
- Timothy Pietro Suren Perera ,
- Ronaldus Arnodus Hendrika Joseph Gilissen ,
- Berthold Wroblowski ,
- Jean Fernand Armand Lacrampe ,
- Alexandra Papanikos ,
- Olivier Alexis Georges Querolle ,
- Elisabeth Thérèse Jeanne Pasquier ,
- Isabelle Noëlle Constance Pilatte ,
- Pascal Ghislain André Bonnet ,
- Werner Constant Johan Embrechts ,
- Rhalid Akkari ,
- Lieven Meerpoel
The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Radioactive phospholipid metal chelates for cancer imaging and therapy
Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula: ##STR00001##
R.sub.1 includes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is —N.sup.+H.sub.3, —N.sup.+H.sub.2Z, —N.sup.+HZ.sub.2, or —N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.
Radioactive phospholipid metal chelates for cancer imaging and therapy
Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula: ##STR00001##
R.sub.1 includes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is —N.sup.+H.sub.3, —N.sup.+H.sub.2Z, —N.sup.+HZ.sub.2, or —N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.
Chelated PSMA inhibitors
Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells. ##STR00001##
Chelated PSMA inhibitors
Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells. ##STR00001##