16281-94-0Relevant academic research and scientific papers
Nonpeptide GPIIB/IIIA inhibitors. 10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation
Egbertson,Hartman,Gould,Bednar,Bednar,Cook,Gaul,Holahan,Libby,Lynch Jr.,Lynch,Sitko,Stranieri,Vassallo
, p. 2519 - 2524 (1996)
Potency enhancing features of two series of fibrinogen receptor antagonists were combined to give analogs with improved potency and oral activity. Antagonists containing either alkyl or aryl sulfonamides and a central isoindolinone structural constraint demonstrate high affinity for both activated and unactivated platelet receptors.
CENTRALLY ACTIVE P38ALPHA INHIBITING COMPOUNDS
-
, (2021/03/05)
Compounds that are inhibitors of p38alpha and centrally available are described.
SMALL MOLECULE DEGRADERS OF HELIOS AND METHODS OF USE
-
Paragraph 00190-00191, (2021/05/07)
Disclosed are compounds and pharmaceutically acceptable salts, hydrates, solvates, prodrugs, stereoisomers, or tautomers thereof that may cause degradation of various proteins e.g., IKZF2 (Helios). Also disclosed are pharmaceutical compositions containing
HETEROCYCLIC COMPOUNDS AS INHIBITORS OF RAS AND METHODS OF USE THEREOF
-
, (2018/04/21)
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R", Q, W, X, Y, Z, n1, n2and '--" are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also disclosed.
Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine
Walter, Niklas M.,Wentsch, Heike K.,Bührmann, Mike,Bauer, Silke M.,D?ring, Eva,Mayer-Wrangowski, Svenja,Sievers-Engler, Adrian,Willemsen-Seegers, Nicole,Zaman, Guido,Buijsman, Rogier,L?mmerhofer, Michael,Rauh, Daniel,Laufer, Stefan A.
, p. 8027 - 8054 (2017/10/18)
We recently reported 1a (skepinone-L) as a type I p38α MAP kinase inhibitor with high potency and excellent selectivity in vitro and in vivo. However, as a type I inhibitor, it is entirely ATP-competitive and shows just a moderate residence time. Thus, the scope was to develop a new class of advanced compounds maintaining the structural binding features of skepinone-L scaffold like inducing a glycine flip at the hinge region and occupying both hydrophobic regions I and II. Extending this scaffold with suitable residues resulted in an interference with the kinase's R-Spine. By synthesizing 69 compounds, we could significantly prolong the target residence time with one example to 3663 s, along with an excellent selectivity score of 0.006 and an outstanding potency of 1.0 nM. This new binding mode was validated by cocrystallization, showing all binding interactions typifying type I1/2 binding. Moreover, microsomal studies showed convenient metabolic stability of the most potent, herein reported representatives.
NOVEL ISOINDOLINONE DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST T-TYPE CALCIUM CHANNEL AND METHOD FOR PREPARATION THEREOF
-
Page/Page column 15, (2010/04/03)
Disclosed are isoindolinone derivatives having inhibitory activity against T-type calcium channels, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient
NOVEL ISOINDOLINONE DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST T-TYPE CALCIUM CHANNEL AND METHOD FOR PREPARATION THEREOF
-
Page/Page column 6, (2010/02/16)
Disclosed are isoindolinone derivatives, represented by Chemical Formula 1, having inhibitory activity against T-type calcium channels, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient. wherein R1?R6 are as defined in the specification.
Methods of making 2,6-diaryl piperidine derivatives
-
, (2008/06/13)
Methods for preparing 2,6-diaryl piperidine derivatives are described. More particularly, 2,6-diaryl piperidines having formula 1-4 are prepared by cyclocondensation of an aryl or heteroaryl aldehyde with 1,3-acetonedicarboxylic acid.
Compounds and methods for identifying activated platelets
-
, (2008/06/13)
The invention is directed to a series of novel compounds, and their pharmaceutically acceptable salts, of the formula STR1 wherein R is C0-6 alkyl substituted with R5 or a mono or polycyclic aromatic or heteroaromatic system comprised of 5 or 6-membered aromatic or heteroaromatic rings that are either unsubstituted or substituted with one or more of R1 and R2 ; R1 and R2 are independently C1-6 alkyl, carboxyl, hydroxyl, azido, nitro, amino, C1-6 alkylamino, C1-6 dialkylamino, arylamino, aryl C1-6 alkylamino, hydroxysulfonyl or arylazo; aryl is a phenyl or naphthyl ring which is unsubstituted or substituted with one or more of R3 and R4 ; R3 and R4 are independently C1-6 alkyl, azido, nitro, amino, C1-6 dialkylamino or hydroxysulfonyl; R5 is STR2 provided that when R is an unsubstituted monocyclic ring, the monocyclic ring is not phenyl or pyridyl. Such compounds are useful as fluorescent probes for identifying antiplatelet agents which selectively bind to activated platelets.
