Abstract: Provided herein is a method for the manufacture of a compound of obicetrapib and salts thereof, such as calcium salts thereof. Also provided herein is amorphous obicetrapib hemicalcium. New intermediates for use in the synthesis of obicetrapib, and salts thereof are also provided, including obicetrapib HCl and a mesylate salt for the use in the synthesis of obicetrapib and amorphous obicetrapib hemicalcium.

Abstract: The present disclosure relates to stable pharmaceutical compositions comprising fixed dose combination of obicetrapib and ezetimibe, or their salts, solvates or derivatives thereof. The disclosure further describes the use of ezetimibe and obicetrapib, e.g. in the form of such fixed dose combinations, for preparation of medicaments and method of treatment of subjects requiring reduction in LDL-cholesterol or those suffering from hyperlipidemia or mixed dyslipidemia.

Abstract: Provided herein is a pharmaceutical composition comprising obicetrapib, or a pharmaceutically acceptable salt thereof, and an SGTL2 inhibitor, or a pharmaceutically acceptable salt thereof. Also provided are dosage forms including the same. In some embodiments, the dosage form is a solid dosage form, such as a tablet. Also provided are processes for the preparation of fixed dose formulations of obicetrapib and an SGTL2 inhibitor, and methods for using the same in the treatment of a metabolic disorder (e.g., type 2 diabetes). Also provided are methods of treating or preventing a metabolic disorder in a subject who has or is at risk of developing a metabolic disorder, comprising: administering a therapeutically effective amount of obicetrapib, or a pharmaceutically acceptable salt thereof; and a therapeutically effective amount of at least one SGLT2 inhibitor, or a pharmaceutically acceptable salt thereof.

Abstract: Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.

Abstract: Provided herein is a method for the manufacture of a compound of obicetrapib and salts thereof, such as calcium salts thereof. Also provided herein is amorphous obicetrapib hemicalcium. New intermediates for use in the synthesis of obicetrapib, and salts thereof are also provided, including obicetrapib HCl and a mesylate salt for the use in the synthesis of obicetrapib and amorphous obicetrapib hemicalcium.

Abstract: Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.

Abstract: Provided herein are pharmaceutical compositions comprising Compound (I), wherein Compound (I) is of the formula: or a pharmaceutically acceptable salt, polymorph, solvate, tautomer, stereoisomer, or isotopically labeled derivative thereof. Also disclosed are polymorphs of Compound (I) and methods of using the pharmaceutical compositions and polymorphs of Compound (I) as described herein to treat a disease (e.g., cystic fibrosis, and fibrotic diseases, such as pulmonary fibrosis) comprising administering to a subject in need thereof a therapeutically effective amount of a polymorph of Compound (I) or a pharmaceutical composition comprising Compound (I) as described herein. In some aspects, the compositions are formulated for inhalation (e.g., oral or nasal inhalation).

Abstract: Provided herein are free base crystalline forms, crystalline salts, and an amorphous salts of omecamtiv mecarbil.

Abstract: Provided herein is a method for the manufacture of a compound of obicetrapib and salts thereof, such as calcium salts thereof. Also provided herein is amorphous obicetrapib hemicalcium. New intermediates for use in the synthesis of obicetrapib, and salts thereof are also provided, including obicetrapib HCl and a mesylate salt for the use in the synthesis of obicetrapib and amorphous obicetrapib hemicalcium.

Abstract: Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.

Abstract: Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.

Abstract: Provided herein are free base crystalline forms, crystalline salts, and an amorphous salts of omecamtiv mecarbil.

Abstract: Provided herein is a method for the manufacture of a compound of obicetrapib and salts thereof, such as calcium salts thereof. Also provided herein is amorphous obicetrapib hemicalcium. New intermediates for use in the synthesis of obicetrapib, and salts thereof are also provided, including obicetrapib HCl and a mesylate salt for the use in the synthesis of obicetrapib and amorphous obicetrapib hemicalcium.

Abstract: Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound IA, wherein R1 is described herein. Compound IA can be useful in synthesizing compound A1, or a salt or solvate thereof, and compound A2, or a salt of solvate thereof.

Abstract: The present invention provides new methods for preparing compound 5, and pharmaceutically acceptable salts thereof, of structure Compound 5, or a pharmaceutically acceptable salt thereof, is an important intermediate in the synthesis of carfilzomib. The invention further provides methods of making a useful manganese catalyst that may be used in the epoxidation step of the present invention.

Abstract: Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound F, or a salt thereof, wherein R1 and OPG2 are described herein. Compound F can be useful in synthesizing compound A1, or a salt of solvate thereof, and compound A2, or a salt of solvate thereof.

Abstract: Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound F that can be used to prepare them where the variable PG is as defined herein. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof and compound A2, and salts and solvates thereof.

Abstract: Disclosed herein is an improved process for the synthesis of compound (A): (A), or a salt or solvate thereof via methylation of compound (B): (B), or a salt or solvate thereof, a crystalline hydrate of compound A, and pharmaceutical formulations comprising a crystalline hydrate of compound (A).

Abstract: Provided herein are free base crystalline forms, crystalline salts, and an amorphous salts of omecamtiv mecarbil.

Abstract: A method for preparing AMG 416, or a pharmaceutically acceptable salt thereof, is provided.