- APELIN RECEPTOR AGONISTS AND METHODS OF USE THEREOF
-
Provided herein are agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.
- -
-
Paragraph 0893-0894
(2019/02/25)
-
- Design and synthesis of aminothiazole modulators of the gamma-secretase enzyme
-
The design and construction of a series of novel aminothiazole-derived γ-secretase modulators is described. The incorporation of heterocyclic replacements of the terminal phenyl D-ring of lead compound 1 was conducted in order to align potency with favorable drug-like properties. γ-Secretase modulator 28 displayed good activity for in vitro inhibition of Aβ42, as well as substantial improvement in ADME and physicochemical properties, including aqueous solubility. Pharmacokinetic evaluation of compound 28 in mice revealed good brain penetration, as well as good clearance, half-life, and volume of distribution which collectively support the continued development of this class of compounds.
- Rynearson, Kevin D.,Buckle, Ronald N.,Barnes, Keith D.,Herr, R. Jason,Mayhew, Nicholas J.,Paquette, William D.,Sakwa, Samuel A.,Nguyen, Phuong D.,Johnson, Graham,Tanzi, Rudolph E.,Wagner, Steven L.
-
supporting information
p. 3928 - 3937
(2016/08/01)
-
- PYRAZOLYL-PYRIMIDINES AS KINASE INHIBITORS
-
Disclosed are compounds having the formula (I): wherein Z, n, R1, R1A, R3, R4, and R5 are as defined herein, and methods of making and using the same.
- -
-
Page/Page column 50
(2011/10/13)
-