C07D295/24

GLP-1 receptor stabilizers and modulators

Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.

GLP-1 receptor stabilizers and modulators

Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.

Protected amine labels and use in detecting analytes

The invention is directed towards novel amino acid based compounds, which may be isotopically enriched, and methods of use of such compounds for characterizing one or more molecules of a sample by mass spectrometry, the method comprising: (a) reacting the one or more molecules with the compound; and (b) characterizing the one or more molecules by mass spectrometry.

STAT3 INHIBITOR

Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.

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.

STAT3 inhibitor

Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.

STAT3 inhibitor

Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.

PROCESS FOR MAKING A SUBSTANTIALLY NITROSAMINE-FREE, SUBSTANTIALLY PEROXIDE-FREE, SUBSTANTIALLY COLORLESS AMINE OXIDE

A process for making a substantially nitrosamine-free, substantially peroxide-free, substantially colorless amine oxide solution comprises reacting a tertiary amine capable of forming an amine oxide with a less than stoichiometric amount of aqueous hydrogen peroxide in an aqueous medium while imposing on the aqueous medium a vapor space having a carbon dioxide partial pressure p(CO.sub.2) of less than 0.75 bar absolute. The process allows for obtaining amine oxides which are substantially nitrosamine-free, substantially peroxide-free, and substantially colorless. This unique combination of desirable features has not been achieved so far in a process only comprising oxidation and distillation.

PROCESS FOR MAKING A SUBSTANTIALLY NITROSAMINE-FREE, SUBSTANTIALLY PEROXIDE-FREE, SUBSTANTIALLY COLORLESS AMINE OXIDE

A process for making a substantially nitrosamine-free, substantially peroxide-free, substantially colorless amine oxide solution comprises reacting a tertiary amine capable of forming an amine oxide with a less than stoichiometric amount of aqueous hydrogen peroxide in an aqueous medium while imposing on the aqueous medium a vapor space having a carbon dioxide partial pressure p(CO.sub.2) of less than 0.75 bar absolute. The process allows for obtaining amine oxides which are substantially nitrosamine-free, substantially peroxide-free, and substantially colorless. This unique combination of desirable features has not been achieved so far in a process only comprising oxidation and distillation.