C07D213/807

RECONSTITUTED HDL NANOPARTICLES FOR DELIVERY OF RADIOACTIVE AGENTS AND USES THEREOF
20220008571 · 2022-01-13 ·

Despite the widespread use of nanotechnology in radio-imaging applications, lipoprotein based delivery systems received only limited attention so far. The subject application provides for the synthesis of a novel hydrophobic radio-imaging tracer. This tracer, comprising a hydrazinonicotinic acid (HYNIC)-N-dodecylamide and .sup.99mTc conjugate can be encapsulated into rHDL nanoparticles (NPs). These rHDL NPs can selectively target the Scavenger Receptor type B1 (SR-B1) that is overexpressed on most cancer cells due to excess demand for cholesterol for membrane biogenesis and thus can target tumors in-vivo. Details of the tracer synthesis, characterization of rHDL/tracer complex, in-vitro uptake, stability studies and in-vivo application of this new radio-imaging approach are provided.

RECONSTITUTED HDL NANOPARTICLES FOR DELIVERY OF RADIOACTIVE AGENTS AND USES THEREOF
20220008571 · 2022-01-13 ·

Despite the widespread use of nanotechnology in radio-imaging applications, lipoprotein based delivery systems received only limited attention so far. The subject application provides for the synthesis of a novel hydrophobic radio-imaging tracer. This tracer, comprising a hydrazinonicotinic acid (HYNIC)-N-dodecylamide and .sup.99mTc conjugate can be encapsulated into rHDL nanoparticles (NPs). These rHDL NPs can selectively target the Scavenger Receptor type B1 (SR-B1) that is overexpressed on most cancer cells due to excess demand for cholesterol for membrane biogenesis and thus can target tumors in-vivo. Details of the tracer synthesis, characterization of rHDL/tracer complex, in-vitro uptake, stability studies and in-vivo application of this new radio-imaging approach are provided.

Acetophenone compound, preparation method therefor, and application thereof in blood lipid regulation

Disclosed are a compound represented by Formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, the Formula I, and an application thereof in preparing drugs for regulating blood lipids. ##STR00001##

Acetophenone compound, preparation method therefor, and application thereof in blood lipid regulation

Disclosed are a compound represented by Formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, the Formula I, and an application thereof in preparing drugs for regulating blood lipids. ##STR00001##

Acetophenone Compound, Preparation Method Therefor, And Application Thereof In Blood Lipid Regulation

Disclosed are a compound represented by Formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, the Formula I, and an application thereof in preparing drugs for regulating blood lipids.

##STR00001##

Acetophenone Compound, Preparation Method Therefor, And Application Thereof In Blood Lipid Regulation

Disclosed are a compound represented by Formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, the Formula I, and an application thereof in preparing drugs for regulating blood lipids.

##STR00001##

Reconstituted HDL nanoparticles for delivery of radioactive agents and uses thereof

Despite the widespread use of nanotechnology in radio-imaging applications, lipoprotein based delivery systems received only limited attention so far. The subject application provides for the synthesis of a novel hydrophobic radio-imaging tracer. This tracer, comprising a hydrazinonicotinic acid (HYNIC)-N-dodecylamide and .sup.99mTc conjugate can be encapsulated into rHDL nanoparticles (NPs). These rHDL NPs can selectively target the Scavenger Receptor type B1 (SR-B1) that is overexpressed on most cancer cells due to excess demand for cholesterol for membrane biogenesis and thus can target tumors in-vivo. Details of the tracer synthesis, characterization of rHDL/tracer complex, in-vitro uptake, stability studies and in-vivo application of this new radio-imaging approach are provided.

Reconstituted HDL nanoparticles for delivery of radioactive agents and uses thereof

Despite the widespread use of nanotechnology in radio-imaging applications, lipoprotein based delivery systems received only limited attention so far. The subject application provides for the synthesis of a novel hydrophobic radio-imaging tracer. This tracer, comprising a hydrazinonicotinic acid (HYNIC)-N-dodecylamide and .sup.99mTc conjugate can be encapsulated into rHDL nanoparticles (NPs). These rHDL NPs can selectively target the Scavenger Receptor type B1 (SR-B1) that is overexpressed on most cancer cells due to excess demand for cholesterol for membrane biogenesis and thus can target tumors in-vivo. Details of the tracer synthesis, characterization of rHDL/tracer complex, in-vitro uptake, stability studies and in-vivo application of this new radio-imaging approach are provided.

Method for manufacturing 3-(alkylsulfonyl)pyridine-2-carboxylic acid

A 3-(alkylsulfonyl)pyridine-2-carboxylic acid or a salt thereof can be manufactured by comprising: allowing a compound represented by formula (1-N): ##STR00001## wherein X represents a halogen atom, to react with a compound represented by formula (2):
R.sup.2SM.sup.2(2) wherein R.sup.2 represents a C.sub.1-8 straight-chain alkyl group, and M.sup.2 represents a hydrogen atom or an alkali metal, to give a compound represented by formula (3-N): ##STR00002## wherein R.sup.2 and X are as defined above; allowing the compound (3-N) to react with hydrogen peroxide in the presence of a tungsten catalyst and an acid; reducing the product in the presence of a base and a heterogeneous transition metal catalyst; and hydrolyzing the product in the presence of a base.

Method for manufacturing 3-(alkylsulfonyl)pyridine-2-carboxylic acid

A compound represented by formula (7): ##STR00001## or a salt thereof can be manufactured by the following steps: a step of allowing a compound represented by formula (1-S): ##STR00002## to react with a compound represented by formula (2):
R.sup.2SM.sup.2(2) to give a compound represented by formula (3-S): ##STR00003## a step of allowing the compound represented by formula (3-S) to react with hydrogen peroxide in the presence of a tungsten catalyst and an acid to give a compound represented by formula (6-S) or a salt thereof: ##STR00004##
and a step of reducing the compound represented by formula (6-S) or salt thereof in the presence of a base and a heterogeneous transition metal catalyst to give a compound represented by formula (7) or a salt thereof, wherein X, R.sup.1, R.sup.2, and M.sup.2 are defined in the specification.