- PLASMA KALLIKREIN INHIBITORS AND USES THEREOF
-
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
- -
-
Paragraph 0999; 1000
(2021/03/19)
-
- BICYCLIC HETEROARYL COMPOUNDS AS GPR119 RECEPTOR AGONISTS
-
The present invention provides a new class of bicyclic heteroaryl compounds represented by Formula (I), pharmaceutical compositions containing these compounds, and their use for modulating the activity of GPR119 in the treatment of metabolic disorders and complications thereof, as well as methods for the treatment of the metabolic disorders and complications thereof.
- -
-
Page/Page column 43
(2012/08/27)
-
- Azaindole hydroxamic acids are potent HIV-1 integrase inhibitors
-
HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication. Recently, HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Herein, we report the discovery of azaindole carboxylic aci
- Plewe, Michael B.,Butler, Scott L.,Dress, Klaus R.,Hu, Qiyue,Johnson, Ted W.,Kuehler, Jon E.,Kuki, Atsuo,Lam, Hieu,Liu, Wen,Nowlin, Dawn,Peng, Qinghai,Rahavendran, Sadayappan V.,Tanis, Steven P.,Tran, Khanh T.,Wang, Hai,Yang, Anle,Zhang, Junhu
-
experimental part
p. 7211 - 7219
(2010/06/13)
-
- INHIBITORS OF THE HIV INTEGRASE ENZYME
-
The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIV”) integrase enzyme.
- -
-
Page/Page column 61
(2008/06/13)
-
- PYRROLOPYRIDINE-2-CARBOXYLIC ACID AMIDE INHIBITORS OF GLYCOGEN PHOSHORYLASE
-
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.
- -
-
-
- Thrombin inhibitors
-
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2or N; d is CY3or N; e is CY4or N; f is CY5or N; g is CY6or N; Y4, Y5, and Y6are independently hydrogen, C1-4alkyl, or halogen; Y1and Y2are independently hydrogen, C1-4alkyl, C3-7cycloalkyl, halogen, NH2, OH or C1-4alkoxy, and Y3is hydrogen, C1-4alkyl, C3-7cycloalkyl, halogen, —CN, NH2, OH or C1-4alkoxy; A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.
- -
-
-
- Azaindoles: Moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors
-
Starting from a 2-amino-6-methylpyridine P1 group and following a strategy of enlarging it whilst reducing its polarity, we have developed a series of potent, moderately basic azaindoles which are intrinsically much more selective for thrombin versus tryp
- Sanderson, Philip E. J.,Stanton, Matthew G.,Dorsey, Bruce D.,Lyle, Terry A.,McDonough, Colleen,Sanders, William M.,Savage, Kelly L.,Naylor-Olsen, Adel M.,Krueger, Julie A.,Lewis, S. Dale,Lucas, Bobby J.,Lynch, Joseph J.,Yan, Youwei
-
p. 795 - 798
(2007/10/03)
-
