267875-30-9Relevant academic research and scientific papers
PLASMA KALLIKREIN INHIBITORS AND USES THEREOF
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Paragraph 0999; 1000, (2021/03/19)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
NITROGENATED FUSED RING DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND USE OF THE SAME FOR MEDICAL PURPOSES
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Page/Page column 26, (2010/01/29)
[Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, -OW1, -SW1, -COW2, -NW3W4, -SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, -CO-Y, -SO2-Y -S-(alkylene)-Y, -O-(alkylene)-Y, -SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
Azaindole hydroxamic acids are potent HIV-1 integrase inhibitors
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)
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
Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
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Page/Page column 66, (2008/06/13)
The present invention relates to certain substituted pyridinyl and pyrimidinyl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and com
INHIBITORS OF THE HIV INTEGRASE ENZYME
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Page/Page column 61-62, (2008/06/13)
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.
Azaindoles: Moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors
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)
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
Thrombin inhibitors
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, (2008/06/13)
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.
