A61K31/4745

MACROPHAGES EAT CANCER CELLS USING THEIR OWN CALRETICULIN AS A GUIDE
20180000865 · 2018-01-04 ·

Therapeutic and diagnostic methods are provided, which methods relate to the induction of expression of calreticulin on phagocytic cells. Specifically, the methods relate to macrophage-mediated programmed cell removal (PrCR), the methods comprising increasing PrCR by contacting a phagocytic cell with a toll-like receptor (TLR) agonist; or down-regulating PrCR by contacting a phagocytic cell with an inhibitor of Bruton's tyrosine kinase (BTK). In some embodiments, an activator of TLR signaling or a BTK agonist is provided in combination with CD47 blockade.

MACROPHAGES EAT CANCER CELLS USING THEIR OWN CALRETICULIN AS A GUIDE
20180000865 · 2018-01-04 ·

Therapeutic and diagnostic methods are provided, which methods relate to the induction of expression of calreticulin on phagocytic cells. Specifically, the methods relate to macrophage-mediated programmed cell removal (PrCR), the methods comprising increasing PrCR by contacting a phagocytic cell with a toll-like receptor (TLR) agonist; or down-regulating PrCR by contacting a phagocytic cell with an inhibitor of Bruton's tyrosine kinase (BTK). In some embodiments, an activator of TLR signaling or a BTK agonist is provided in combination with CD47 blockade.

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.

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FUROQUINOLINEDIONES AS INHIBITORS OF TDP2
20180009822 · 2018-01-11 ·

Compounds of Formula I and the pharmaceutically acceptable salts thereof are disclosed Formula I. The variables X.sup.1, X.sup.2, and R.sup.1-4 are disclosed herein. The compounds are useful for treating cancer and related proliferative diseases. Pharmaceutical compositions containing compounds of Formula I and methods of treatment comprising administering compounds of Formula I are also disclosed.

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FUROQUINOLINEDIONES AS INHIBITORS OF TDP2
20180009822 · 2018-01-11 ·

Compounds of Formula I and the pharmaceutically acceptable salts thereof are disclosed Formula I. The variables X.sup.1, X.sup.2, and R.sup.1-4 are disclosed herein. The compounds are useful for treating cancer and related proliferative diseases. Pharmaceutical compositions containing compounds of Formula I and methods of treatment comprising administering compounds of Formula I are also disclosed.

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HIGH-SOLUBILITY ACETONE-ADDED PYRROLOQUINOLINE QUINONE SALT
20180009803 · 2018-01-11 · ·

There are provided an alkali metal salt of 5-hydroxy-4-oxo-5-(2-oxopropyl)-4,5-dihydro-1H-pyrrolo[2,3-f]quinoline-2,7,9-tricarboxylic acid, a method for producing the alkali metal salt, and a cocrystal comprising the alkali metal salt.

Methods for Treating Pancreatic Cancer Using Combination Therapies

Provided are methods for treating pancreatic cancer in a patient by administering liposomal irinotecan (MM-398) alone or in combination with additional therapeutic agents. In one embodiment, the liposomal irinotecan (MM-398) is co-administered with 5-fluorouracil and leucovorin.

Methods for Treating Pancreatic Cancer Using Combination Therapies

Provided are methods for treating pancreatic cancer in a patient by administering liposomal irinotecan (MM-398) alone or in combination with additional therapeutic agents. In one embodiment, the liposomal irinotecan (MM-398) is co-administered with 5-fluorouracil and leucovorin.

Methods for Treating Pancreatic Cancer Using Combination Therapies

Provided are methods for treating pancreatic cancer in a patient by administering liposomal irinotecan (MM-398) alone or in combination with additional therapeutic agents. In one embodiment, the liposomal irinotecan (MM-398) is co-administered with 5-fluorouracil and leucovorin.

METHOD FOR PRODUCING BENZAZOLOQUINOLIUM (BQS) SALTS AND USING THE BIOLOGICAL ACTIVITY OF THE COMPOSITION

Disclosed is the synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of chloro-substituent, amino-substituent, and nitro-substituent resulting in several compounds. The compounds are further used as markers due to their fluorescent properties including in hypoxic environments.

This disclosure further describes anti-cancer screening of two BQS, namely, 7-benzyl-3-aminobenzimidazo[3,2-a]quinolinium chloride (ABQ-48: NSC D-763307) and the corresponding 7-benzyl-3-nitrobenzimidazo[3,2-a]quinolinium chloride (NBQ 48: NSC D-763303).