C07C239/20

Beta-substituted beta-amino acids and analogs as chemotherapeutic agents

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

Compositions for the treatment of fibrosis and fibrosis-related conditions
10035775 · 2018-07-31 · ·

The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions.

Compositions for the treatment of fibrosis and fibrosis-related conditions
10035775 · 2018-07-31 · ·

The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions.

Compounds for promoting liposomal and cellular adhesion and compositions and methods of use thereof
10017460 · 2018-07-10 · ·

The present application describes amphiphatic compounds like compound IIa below, compositions and methods for incorporating chemoselective and bio-orthogonal complementary functional groups into liposomes. Such compounds are incorporated in greater numbers in liposome and fused cell surfaces, leading to greater adhesion and conjugation efficiency. The present application also describes various uses of these modified liposomes including for tethering the chemoselective and bioorthogonal complementary functional groups from cell surfaces by liposome delivery toward the goal of rewiring the cell surface.

Compounds for promoting liposomal and cellular adhesion and compositions and methods of use thereof
10017460 · 2018-07-10 · ·

The present application describes amphiphatic compounds like compound IIa below, compositions and methods for incorporating chemoselective and bio-orthogonal complementary functional groups into liposomes. Such compounds are incorporated in greater numbers in liposome and fused cell surfaces, leading to greater adhesion and conjugation efficiency. The present application also describes various uses of these modified liposomes including for tethering the chemoselective and bioorthogonal complementary functional groups from cell surfaces by liposome delivery toward the goal of rewiring the cell surface.

β-substituted γ-amino acids and analogs as chemotherapeutic agents

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

β-substituted γ-amino acids and analogs as chemotherapeutic agents

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS
20180078517 · 2018-03-22 ·

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS
20180078517 · 2018-03-22 ·

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

COMPOSITIONS FOR THE TREATMENT OF FIBROSIS AND FIBROSIS-RELATED CONDITIONS
20180072682 · 2018-03-15 · ·

The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions.