85864-09-1Relevant articles and documents
POLYHETEROCYCLIC COMPOUNDS AS METTL3 INHIBITORS
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Page/Page column 245, (2021/06/11)
The present invention relates to compounds of formula (I) that function as inhibitors of METTL3 (N6-adenosine-methyltransferase 70 kDa subunit) enzyme activity: X-Y-Z (I) wherein X, Y and Z are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, and autoimmune diseases, as well as other diseases or conditions in which METTL3 activity is implicated.
MATRIPTASE 2 INHIBITORS AND USES THEREOF
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Paragraph 00176; 00177; 00227; 00228, (2020/05/15)
The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.
N-CYCLYL-3 - (CYCLYLCARBONYLAMINOMETHYL) BENZAMIDE DERIVATIVES AS RHO KINASE INHIBITORS
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Page/Page column 61-62, (2012/02/01)
The present invention relates to compounds of formula (I) : and pharmaceutically acceptable salts thereof, wherein R1and R2 are various ring systems. The invention also relates to pharmaceutical compositions comprising these compound
PHENYL DIAZEPANE CARBOXAMIDES AND ANNELATED PHENYL PIPERAZINE CARBOXAMIDES CONTAINING OXYGEN AND USED AS DOPAMINE D3 ANTAGONISTS
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Page/Page column 34, (2008/06/13)
The invention relates to annelated phenyl piperazine and phenyl diazepane carboxamides of general formula (I) containing oxygen.The compounds are suitable for medical purposes.
Preparation and pharmacological evaluation of novel glycoprotein (Gp) IIb/IIIa antagonists. 2. Condensed heterocyclic derivatives
Ono, Shin'ichiro,Yoshida, Tomohiro,Maeda, Kazuhiro,Kosaka, Keigo,Inoue, Yoshihisa,Imada, Teruaki,Fukaya, Chikara,Nakamura, Norifumi
, p. 1694 - 1712 (2007/10/03)
A novel series of platelet receptor glycoprotein (Gp) IIb/IIIa antagonists with condensed heterocycles as their basic core was synthesized. In an in vitro assay, trans-4-(5-amidinobenzofuran-2- carboxamido)cyclohexyl]oxyacetic acid 17e and trans-3-[4-(5-
Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists
Sall, Daniel J.,Arfsten, Ann E.,Bastian, Jolie A.,Denney, Michael L.,Harms, Cathy S.,McCowan, Jefferson R.,Morin Jr., John M.,Rose, Jack W.,Scarborough, Robert M.,Smyth, Mark S.,Um, Suzane L.,Utterback, Barbara G.,Vasileff, Robert T.,Wikel, James H.,Wyss, Virginia L.,Jakubowski, Joseph A.
, p. 2843 - 2857 (2007/10/03)
The use of 5,6-bicyclic amidines as arginine surrogates in the design of a novel class of potent platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists is described. The additional conformational restriction offered by the bicyclic nucleus results in 20-400-fold increases in potency compared to the freely flexible, acyclic benzamidine counterpart. The design, synthesis, structure-activity relationships (SAR), and in vitro activity of this novel class of GPIIb-IIIa antagonists are presented.
5,6-Bicyclic glycoprotein IIb IIIa antagonists useful in inhibition of platelet aggregation
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, (2008/06/13)
This invention relates to 5,6 fused ring bicyclic compounds inclusive of indoles, benzofurans, and benzothiophenes, and corresponding to the formula (I) substituted with both basic (B) and acidic (A) functionality, which are useful in inhibition of platelet aggregation.