C07D249/14

1-PYRIDAZIN-/TRIAZIN-3-YL-PIPER(-AZINE)/IDINE/PYROLIDINE DERIVATIVES AND COMPOSITIONS THEREOF FOR INHIBITING THE ACTIVITY OF SHP2

The present invention relates to compounds of formula I:

##STR00001##

in which m, Y.sub.1, Y.sub.2, Y.sub.3, R.sub.1, R.sub.2a, R.sub.2b, R.sub.3a, R.sub.3b, R.sub.4a, R.sub.4b, R.sub.5a and R.sub.5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

1-PYRIDAZIN-/TRIAZIN-3-YL-PIPER(-AZINE)/IDINE/PYROLIDINE DERIVATIVES AND COMPOSITIONS THEREOF FOR INHIBITING THE ACTIVITY OF SHP2

The present invention relates to compounds of formula I:

##STR00001##

in which m, Y.sub.1, Y.sub.2, Y.sub.3, R.sub.1, R.sub.2a, R.sub.2b, R.sub.3a, R.sub.3b, R.sub.4a, R.sub.4b, R.sub.5a and R.sub.5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

METHODS FOR TREATING PROTOZOAN INFECTIONS

The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention.

NOVEL COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
20170281601 · 2017-10-05 ·

Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX

Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.

SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX

Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.

BICYCLIC ARYLCARBOXYLIC ACID AMIDES AND THEIR USE AS HERBICIDES

Bicyclic arylcarboxamides of the general formula (I) are described as herbicides.

##STR00001##

In this formula (I), Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4 and Z.sup.5 are a bond, O, S(O).sub.n or a substituted carbon atom. X is a radical such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a substituted heterocycle.

BICYCLIC ARYLCARBOXYLIC ACID AMIDES AND THEIR USE AS HERBICIDES

Bicyclic arylcarboxamides of the general formula (I) are described as herbicides.

##STR00001##

In this formula (I), Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4 and Z.sup.5 are a bond, O, S(O).sub.n or a substituted carbon atom. X is a radical such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a substituted heterocycle.

Compositions and methods for treating metabolic disorders

Methods for improving the gastrointestinal tolerability of biguanide compounds and for treating metabolic disorders and/or inducing weight loss in patients in need thereof, particularly in individuals having a contraindication for treatment with biguanide compounds, are provided comprising administering delayed release formulations of such biguanide compounds, including metformin, targeted to the small intestine.

Compositions and methods for treating metabolic disorders

Methods for improving the gastrointestinal tolerability of biguanide compounds and for treating metabolic disorders and/or inducing weight loss in patients in need thereof, particularly in individuals having a contraindication for treatment with biguanide compounds, are provided comprising administering delayed release formulations of such biguanide compounds, including metformin, targeted to the small intestine.