C09B23/0066

Compounds and methods to sensitize cancer cells to tyrosine kinase inhibitors

The present invention generally relates to sensitizer compounds and their use in combination with Tyrosine Kinase Inhibitors (TKIs) for sensitizing tumor, cancer or pre-cancerous cells to TKI treatment. In particular, the present invention relates to administration regimes that combine TKIs such as Gefitinib or Icotinib with TKI-sensitizing DZ1 esters and amides conjugated to statin or platin-based drugs, or to Artemisinin, including, without limitation: DZ1-Simvastatin amide, DZ1-Simvastatin ester, DZ1-Cisplatin ester, and DZ1-Cisplatin amide, DZ1-Artemisinin ester, and DZ1-Artemisinin amide. Furthermore, the present invention relates to improved TKI treatment of cancers by sensitizing tumor, cancer or pre-cancerous cells, in particular cancers that develop TKI resistance, including e.g. lung cancer and pancreatic cancer.

IR DYES FOR FLUORESCENCE IMAGING

A composition comprising: a polymorphic form of 2-((E)-2-((E)-3-(2-((E)-3,3-dimethyl-5-sulfonato-1-(4-sulfonatobutyl)indolin-2-ylidene)ethylidene)-2-phenoxycyclohex-1-en-1-yl)vinyl)-3,3-dimethyl-1-(4-ulfonatobutyl)-3H-indol- 1- ium-5-sulfonate or 2-((E)-2-((E)-3-(2-((E)-3,3-dimethyl-5-sulfonato-1-(4-sulfonatobutyl)indolin-2-ylidene)ethylidene)-2-(4-sulfonatophenoxy)cyclohex-1-en-1-yl)vinyl)-3,3-dimethyl-1-(4-sulfonatobutyl)-3H-indol-1-ium-5-sulfonate and an acceptable excipient.

HYDROGELS WITH BIODEGRADABLE CROSSLINKING
20200054756 · 2020-02-20 · ·

Hydrogels that degrade under appropriate conditions of pH and temperature by virtue of crosslinking compounds that cleave through an elimination reaction are described. The hydrogels may be used for delivery of various agents, such as pharmaceuticals.

4,4-DISUBSTITUTED CYCLOHEXYL BRIDGED HEPTAMETHINE CYANINE DYES AND USES THEREOF
20200049709 · 2020-02-13 ·

The invention relates to a family of compounds that comprise fluorescent cyanine dyes. The compounds are near infrared absorbing heptamethine cyanine dyes with a 4,4-disubstituted cyclohexyl ring as part of the polymethine chromophore. The compounds are generally hydrophilic and can be chemically linked to biomolecules, such as proteins, nucleic acids, and therapeutic small molecules. The compounds can be used for imaging in a variety of medical, biological and diagnostic applications.

ARTICLES AND COMPOSITIONS COMPRISING HOST POLYMERS AND CHROMOPHORES AND METHODS OF PRODUCING THE SAME

Compositions and articles including host polymers and chromophores and methods of producing the same are provided. In an exemplary embodiment, an article includes a host polymer with a host polymer refractive index. The article also includes a chromophore with a chromophore refractive index that is greater than the host polymer refractive index. The chromophore refractive index changes with changes in an electric field, and the chromophore is dissolved within the host polymer. The article has an article refractive index that is between the host polymer refractive index and the chromophore refractive index.

CA IX—NIR dyes and their uses

The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a ligand that binds to the active site of carbonic anhydrase, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid, amide, ureido, or polyethylene glycol derivative thereof. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.

Nanoprobe-Metal Chelator Complexes
20200040189 · 2020-02-06 ·

Provided herein are compounds that are able to bind metal ions (e.g., free metal ions or metal ions bound to low affinity ligands) in a sample or subject. Also provided herein are methods of using the compounds for chelating metal ions and for the treatment of diseases associated with abnormal levels of metal ions. Methods of preparing the compounds and pharmaceutical compositions are also provided.

IR dyes for fluorescence imaging

A method for organ imaging, comprising: administering to a subject a diagnostic effective amount of 2-((E)-2-((E)-3-(2-((E)-3,3-dimethyl-5-sulfonato-1-(4-sulfonatobutyl)indolin-2-ylidene)ethylidene)-2-phenoxycyclohex-1-en-1-yl)vinyl)-3,3-dimethyl-1-(4-sulfonatobutyl)-3H-indol-1-ium-5-sulfonate or 2-((E)-2-((E)-3-(2-((E)-3,3-dimethyl-5-sulfonato-1-(4-sulfonatobutyl)indolin-2-ylidene)ethylidene)-2-(4-sulfonatophenoxy)cyclohex-1-en-1-yl)vinyl)-3,3-dimethyl-1-(4-sulfonatobutyl)-3H-indol-1-ium-5-sulfonate. In one embodiment, the organ includes one or more of kidney, bladder, liver, gall bladder, spleen, intestine, heart, lungs and muscle.

Compositions of Near IR Closed Chain, Sulfo-Cyanine Dyes and Prostate Specific Membrane Antigen Ligands
20200030461 · 2020-01-30 ·

Compositions and methods for visualizing tissue under illumination with fusion compounds of near-infrared radiation using near IR, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are provided.

ENCODED CHROMOPHORIC POLYMER PARTICLES AND METHODS OF USE THEREOF
20200011874 · 2020-01-09 ·

The present disclosure provides encoded chromophoric polymer particles that are capable of, for example, optical and/or biomolecular encoding of analytes. The present disclosure also provides suspensions comprising a plurality of encoded chromophoric polymer particles. The present disclosure also provides methods of using the encoded chromophoric polymer particles and systems for performing multiplex analysis with encoded chromophoric polymer particles.