C07D277/40

PROCESS FOR THE PREPARATION OF MIRABEGRON FREE FROM GENOTOXIC IMPURITIES

The present invention relates to mirabegron substantially free from genotoxic impurities particularly nitrosamine impurities of Formula (I), (II), (III), (IV), (V) and processes for its preparation. In particular, the invention relates to processes for the preparation of high purity mirabegron free from nitrosamine impurities of Formula (I), (II), (III), (IV), (V) and other genotoxic and carcinogenic impurities below threshold concentration.

Sulfur derivatives as chemokine receptor modulators

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Sulfur derivatives as chemokine receptor modulators

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Inhibition of cell proliferation

The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC.sub.50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

Inhibition of cell proliferation

The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC.sub.50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

Amorphous mirabegron and processes for crystal forms of mirabegron

Aspects of the present invention relate to amorphous form of mirabegron, amorphous solid dispersion of mirabegron, process for its preparation, processes for preparation of form crystal and form crystal of mirabegron and pharmaceutical composition thereof.

Amorphous mirabegron and processes for crystal forms of mirabegron

Aspects of the present invention relate to amorphous form of mirabegron, amorphous solid dispersion of mirabegron, process for its preparation, processes for preparation of form crystal and form crystal of mirabegron and pharmaceutical composition thereof.

RIBONUCLEOTIDE REDUCTASE INHIBITORS AND METHODS OF USE
20170137392 · 2017-05-18 ·

Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.

Anti-migration and anti-invasion thiazole analogs for treatment of cellular proliferative disease

Thiazole analog compounds and their pharmaceutically acceptable salts are disclosed, including pharmaceutical compositions comprising the thiazole analog compounds, either alone or in combination with at least one additional therapeutic agent, and/or with a pharmaceutically acceptable carrier. Methods of using the thiazole analog compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative diseases, such as cancer, are also disclosed.

Anti-migration and anti-invasion thiazole analogs for treatment of cellular proliferative disease

Thiazole analog compounds and their pharmaceutically acceptable salts are disclosed, including pharmaceutical compositions comprising the thiazole analog compounds, either alone or in combination with at least one additional therapeutic agent, and/or with a pharmaceutically acceptable carrier. Methods of using the thiazole analog compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative diseases, such as cancer, are also disclosed.