Patent classifications
C09B29/30
CHEMICAL CONJUGATES OF EVANS BLUE DERIVATIVES AND THEIR USE AS RADIOTHERAPY AND IMAGING AGENTS FOR TARGETING PROSTATE CANCER
A compound of Formula (I) or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt wherein the definitions of R.sub.1-R.sub.13 and L.sub.1-L.sub.4 are provided in the disclosure, and wherein R.sub.14 is a group capable of binding to prostate-specific membrane antigen (PSMA).
##STR00001##
Chemical conjugates of Evans Blue derivatives and their use in the production of long-acting therapeutics
The present invention is directed to a compound of Formula I or Formula II or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula I Formula II The compounds of Formula I may be covalently bonded to a therapeutic compound or fragment thereof to provide a compound of Formula II and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases. ##STR00001##
Chemical conjugates of evans blue derivatives and their use as radiotherapy and imaging agents
The present invention is directed to a compound of Formula I or Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions R.sub.1-R.sub.13 and L.sub.1-L.sub.4 are provided in the disclosure, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.
CHEMICAL CONJUGATES OF EVANS BLUE DERIVATIVES AND THEIR USE IN THE PRODUCTION OF LONG-ACTING THERAPEUTICS
The present invention is directed to a compound of Formula I or Formula II or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula I Formula II The compounds of Formula I may be covalently bonded to a therapeutic compound or fragment thereof to provide a compound of Formula II and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.
##STR00001##
Labeled evans blue dye derivative for in vivo serum albumin labeling
Disclosed is a compound of formula (I): ##STR00001##
wherein L, R.sup.1-R.sup.5, A, B, M, and n are as defined in the specification, as well as a method of preparing the compound. Also disclosed are a method of blood-pool imaging in a mammal and a method of imaging a lymph node in a mammal, comprising use of the compound.
Labeled evans blue dye derivative for in vivo serum albumin labeling
Disclosed is a compound of formula (I): ##STR00001##
wherein L, R.sup.1-R.sup.5, A, B, M, and n are as defined in the specification, as well as a method of preparing the compound. Also disclosed are a method of blood-pool imaging in a mammal and a method of imaging a lymph node in a mammal, comprising use of the compound.
CHEMICAL CONJUGATES OF EVANS BLUE DERIVATIVES AND THEIR USE AS RADIOTHERAPY AND IMAGING AGENTS
The present invention is directed to a compound of Formula I or Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions R.sub.1-R.sub.13 and L.sub.1-L.sub.4 are provided in the disclosure, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.
Chemical conjugates of Evans Blue derivatives and their use as radiotherapy and imaging agents for targeting prostate cancer
A compound of Formula I or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: ##STR00001## wherein the definitions of R.sub.1-R.sub.13 and L.sub.1-L.sub.4 are provided in the disclosure, and wherein R.sub.14 is a group capable of binding to prostate-specific membrane antigen (PSMA).
Mixture of reactive dyes and their use for the dyeing or printing of textile fibre materials
A dye mixture comprising at least one dye of formula (formula) and at least one dye of formula (formula), wherein R.sub.1 is hydrogen or C.sub.1-C.sub.4alkyl, R.sub.2 is hydrogen or C.sub.1-C.sub.4alkyl, C.sub.1-C.sub.4alkoxy or sulfo, Q.sub.1 is a fibre-reactive radical of formula (CH.sub.2).sub.2- 3SO.sub.2Y.sub.2 (3a) or (CH.sub.2).sub.2-3O(CH.sub.2).sub.2-3SO.sub.2Y.sub.3 (3b), Q.sub.2 has the meaning of Q.sub.1, or is hydrogen or C.sub.1-C.sub.4alkyl, X.sub.1 and X.sub.2 are each independently of the other halogen, 3-carboxypyridin-1-yl or 3-carbamoylpyridin-1-yl, Y.sub.1, Y.sub.2 and Y.sub.3 are each independently of the others vinyl or a radical CH.sub.2CH.sub.2U and U is a group removable under alkaline conditions, Z.sub.1 and Z.sub.2 are each independently of the other S0.sub.2-Y, wherein Y is vinyl or a radical CH.sub.2CH.sub.2U and U is a group removable under alkaline conditions, M is hydrogen, an alkali metal or one equivalent of an alkaline earth metal, k and n are each independently of the other the number 0, 1 or 2, I and q are each independently of the other the number 0 or 1, m is the number 0 or 1, and wherein the diazo component of the dye of formula (1) and the diazo component of the dye of formula (2) each independently of the other are a benzene radical or a naphthyl radical, are suitable especially for the dyeing or printing of cellulosic fibre materials, exhibit a good build-up, a good fixation rate and good washing off properties of the unfixed dyes, and good all-round fastness properties. ##STR00001##
Mixture of reactive dyes and their use for the dyeing or printing of textile fibre materials
A dye mixture comprising at least one dye of formula (formula) and at least one dye of formula (formula), wherein R.sub.1 is hydrogen or C.sub.1-C.sub.4alkyl, R.sub.2 is hydrogen or C.sub.1-C.sub.4alkyl, C.sub.1-C.sub.4alkoxy or sulfo, Q.sub.1 is a fibre-reactive radical of formula (CH.sub.2).sub.2- 3SO.sub.2Y.sub.2 (3a) or (CH.sub.2).sub.2-3O(CH.sub.2).sub.2-3SO.sub.2Y.sub.3 (3b), Q.sub.2 has the meaning of Q.sub.1, or is hydrogen or C.sub.1-C.sub.4alkyl, X.sub.1 and X.sub.2 are each independently of the other halogen, 3-carboxypyridin-1-yl or 3-carbamoylpyridin-1-yl, Y.sub.1, Y.sub.2 and Y.sub.3 are each independently of the others vinyl or a radical CH.sub.2CH.sub.2U and U is a group removable under alkaline conditions, Z.sub.1 and Z.sub.2 are each independently of the other S0.sub.2-Y, wherein Y is vinyl or a radical CH.sub.2CH.sub.2U and U is a group removable under alkaline conditions, M is hydrogen, an alkali metal or one equivalent of an alkaline earth metal, k and n are each independently of the other the number 0, 1 or 2, I and q are each independently of the other the number 0 or 1, m is the number 0 or 1, and wherein the diazo component of the dye of formula (1) and the diazo component of the dye of formula (2) each independently of the other are a benzene radical or a naphthyl radical, are suitable especially for the dyeing or printing of cellulosic fibre materials, exhibit a good build-up, a good fixation rate and good washing off properties of the unfixed dyes, and good all-round fastness properties. ##STR00001##