A61K31/337

PROCESS FOR PREPARING AN ANTI-CANCER AGENT, 1-((4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-6-METHOXYQUINOLIN-7-YLOXY)METHYL)CYCLOPROPANAMINE, ITS CRYSTALLINE FORM AND ITS SALTS
20180002311 · 2018-01-04 ·

The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of A13818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I.

##STR00001##

PROCESS FOR PREPARING AN ANTI-CANCER AGENT, 1-((4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-6-METHOXYQUINOLIN-7-YLOXY)METHYL)CYCLOPROPANAMINE, ITS CRYSTALLINE FORM AND ITS SALTS
20180002311 · 2018-01-04 ·

The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of A13818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I.

##STR00001##

PROCESS FOR PREPARING AN ANTI-CANCER AGENT, 1-((4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-6-METHOXYQUINOLIN-7-YLOXY)METHYL)CYCLOPROPANAMINE, ITS CRYSTALLINE FORM AND ITS SALTS
20180002311 · 2018-01-04 ·

The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of A13818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I.

##STR00001##

COMBINATION THERAPY WITH AN ANTITUMOR ALKALOID

The present invention relates to the combination of PM01183 with several anticancer drugs, in particular other anticancer drugs selected from antitumor platinum coordination complexes, antimetabolites, mitotic inhibitors, anticancer antibiotics, topoisomerase I and/or II inhibitors, proteasome inhibitors, histone deacetylase inhibitors, nitrogen mustard alkylating agents, nitrosourea alkylating agents, nonclassical alkylating agents, estrogen antagonists, androgen antagonists, mTOR inhibitors, tyrosine kinase inhibitors, and other agents selected from aplidine, ET-743, PM02734 and PM00104, and the use of these combinations in the treatment of cancer.

COMBINATION THERAPY WITH AN ANTITUMOR ALKALOID

The present invention relates to the combination of PM01183 with several anticancer drugs, in particular other anticancer drugs selected from antitumor platinum coordination complexes, antimetabolites, mitotic inhibitors, anticancer antibiotics, topoisomerase I and/or II inhibitors, proteasome inhibitors, histone deacetylase inhibitors, nitrogen mustard alkylating agents, nitrosourea alkylating agents, nonclassical alkylating agents, estrogen antagonists, androgen antagonists, mTOR inhibitors, tyrosine kinase inhibitors, and other agents selected from aplidine, ET-743, PM02734 and PM00104, and the use of these combinations in the treatment of cancer.

THERAPEUTIC COMPOUNDS AND USES THEREOF

Provided herein are compounds of formula I:

##STR00001##

and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.

THERAPEUTIC COMPOUNDS AND USES THEREOF

Provided herein are compounds of formula I:

##STR00001##

and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.

MODIFIED CYCLODEXTRIN COATED MAGNETITE NANOPARTICLES FOR TARGETED DELIVERY OF HYDROPHOBIC DRUGS

The invention discloses a composition comprising surface modified iron oxide nanoparticles with citric acid modified cyclodextrin with a hydrodynamic diameter of less than 10 nm and a hydrophobic molecule.

The composition finds use in targeted delivery of a hydrophobic drug and as contrast agent in imaging applications.

Synchronizing Tumor Cells to the G2/M Phase Using TTFields Combined with Taxane or Other Anti-Microtubule Agents
20180008708 · 2018-01-11 ·

Cancer cells can be synchronized to the G2/M phase by delivering an anti-microtubule agent (e.g., paclitaxel or another taxane) to the cancer cells, and applying an alternating electric field with a frequency between 100 and 500 kHz to the cancer cells, wherein at least a portion of the applying step is performed simultaneously with at least a portion of the delivering step. This synchronization can be taken advantage of by treating the cancer cells with radiation therapy after the combined action of the delivering step and the applying step has increased a proportion of cancer cells that are in the G2/M phase. The optimal frequency and field strength will depend on the particular type of cancer cell being treated. For certain cancers, this frequency will be between 125 and 250 kHz (e.g., 200 kHz) and the field strength will be at least 1 V/cm.

Synchronizing Tumor Cells to the G2/M Phase Using TTFields Combined with Taxane or Other Anti-Microtubule Agents
20180008708 · 2018-01-11 ·

Cancer cells can be synchronized to the G2/M phase by delivering an anti-microtubule agent (e.g., paclitaxel or another taxane) to the cancer cells, and applying an alternating electric field with a frequency between 100 and 500 kHz to the cancer cells, wherein at least a portion of the applying step is performed simultaneously with at least a portion of the delivering step. This synchronization can be taken advantage of by treating the cancer cells with radiation therapy after the combined action of the delivering step and the applying step has increased a proportion of cancer cells that are in the G2/M phase. The optimal frequency and field strength will depend on the particular type of cancer cell being treated. For certain cancers, this frequency will be between 125 and 250 kHz (e.g., 200 kHz) and the field strength will be at least 1 V/cm.