Patent classifications
C07F9/10
Long-lived gadolinium based tumor targeted imaging and therapy agents
Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: ##STR00001##
or a salt therof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; 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. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.
Long-lived gadolinium based tumor targeted imaging and therapy agents
Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: ##STR00001##
or a salt therof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; 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. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.
NUTRITIONAL COMPOSITIONS CONTAINING PHOSPHATIDYLSERINE POWDER
Phosphatidylserine powder compositions of the present invention were found to provide more homogeneous dispersion and demonstrate reduced sedimentation, compared to conventional phosphatidylserine powders, when mixed without processing by high pressure homogenization in water or other liquids. The composition of the present invention comprises phosphatidylserine and at least 80% (w/w) of the composition has a particle size of 500 microns or less. Nutritional, nutraceutical, or pharmaceutical compositions including the phosphatidylserine powder compositions of the present invention are also provided. Process for preparing phosphatidylserine powder compositions according to the present invention is also provided and includes sieving.
IONIC LIQUID, SOLVENT, PREPARATION, AND TRANSDERMALLY ABSORBABLE AGENT
An ionic liquid has a structure represented by the following general formula (1). In the general formula (1), R represents a substituted or unsubstituted alkyl group or a substituted or unsubstituted alkenyl group, and at least one ethylene group comprising the alkenyl group may be substituted with a vinylene group. X.sup.+ represents a phospholipid with a cationic group.
R—COO.sup.−X.sup.+ General formula (1)
Cationic sulfonamide amino lipids and amphiphilic zwitterionic amino lipids
The present disclosure provides one or more amino lipids such as an amino lipids containing a sulfonic acid or sulfonic acid derivative of the formulas: ##STR00001##
wherein the variables are as defined herein. These amino lipids may be used in compositions with one or more helper lipids and a nucleic acid therapeutic agent. These compositions may be used to treat a disease or disorder such as cancer, cystic fibrosis, or other genetic diseases.
SILOXANE-CONTAINING PHOSPHOLIPIDS, COMPOSITIONS AND USES THEREOF
The present application relates to siloxane-containing phospholipids such as the compounds of Formula I, methods of preparation, compositions and uses thereof.
##STR00001##
SILOXANE-CONTAINING PHOSPHOLIPIDS, COMPOSITIONS AND USES THEREOF
The present application relates to siloxane-containing phospholipids such as the compounds of Formula I, methods of preparation, compositions and uses thereof.
##STR00001##
METHODS AND COMPOSITIONS TO TREAT TYPE-1 AND TYPE-2 DIABETES
The present disclosure is directed to novel methods of treating type-1 or type-2 diabetes by inactivating TLR2 and TLR4 genes together in cells capable of producing insulin and/or regenerating β cells, and providing the cells to a subject in need thereof.
Functional lipid constructs
The invention relates to methods for effecting qualitative and quantitative changes in the functional moieties expressed at the surface of cells and multi-cellular structures, and functional lipid constructs for use in such methods. In particular, the invention relates to functional lipid constructs and their use in diagnostic and therapeutic applications, including serodiagnosis, where the functional moiety is a carbohydrate, peptide, chemically reactive group, conjugator or fluorophore.
VIVO METHODS OF MONITORING BIODISTRIBUTION
Functional-lipid constructs of the structure F-S-L are disclosed, wherein F comprises a tyrosine or histidine residue, S is a spacer covalently linking F to L and L is a lipid. The functional residue may be iodinated and used to radiolabel a biological entity with 1251 and the iodinated constructs are used in a non-invasive method of monitoring the distribution of a biological entity in vivo.
##STR00001##