72299-67-3Relevant academic research and scientific papers
A Continuous Flow Strategy for the Facile Synthesis and Elaboration of Semi-Saturated Heterobicyclic Fragments
Luise, Nicola,Wyatt, Eleanor W.,Tarver, Gary J.,Wyatt, Paul G.
, p. 1341 - 1349 (2019/01/14)
An efficient hydrogenation protocol under continuous flow conditions was developed for the synthesis of underrepresented semi-saturated bicyclic fragments containing highly sp3-rich skeletons for fragment-based drug discovery (FBDD) programs. Excellent yields were generally achieved by using Pd/C (10 % w/w) and RaNi at 25–150 °C under 4–100 bar of hydrogen pressure. The generated fragments, with appropriate physicochemical properties, present diverse hydrogen-bonding pharmacophores and useful vectors for their synthetic elaboration in the optimization stage. Successive, simple functionalizations in continuous flow were accomplished to demonstrate the opportunity to develop multi-step continuous flow synthesis of valuable starting points for FBDD campaigns. A conclusive quality control (QC) was essential to discard those structures which do not fit the typical fragment library parameters.
NOVEL PYRIDYLOXYACETYL TETRAHYDROISOQUINOLINE COMPOUNDS USEFUL AS NAMPT INHIBITORS
-
Page/Page column 19; 20, (2015/04/28)
The present invention provides novel pyridyloxyacetyl tetrahydroisoquinoline compounds that inhibit NAMPT and may be useful in the treatment of cancer.
METHODS FOR IDENTIFICATION OF JAK KINASE INTERACTING MOLECULES AND FOR THE PURIFICATION OF JAK KINASES
-
Page/Page column 37, (2009/06/27)
The present invention relates to immobilization compounds and methods useful for the identification of JAK interacting compounds or for the purification or identification of JAK.
Bronchorelaxing agents based on indol- and isoquinoline derivatives
-
Page/Page column 13-15, (2010/11/25)
A compound of formula (I) and its acid addition salts, wherein R1-FIj are H, lower (CrC6) alkyl; halogen; NR5R6, wherein R5, R6 are H, lower alkyl, C2-C6 acyl, SO2R7, wherein R7 is lower alkyl, CF3, aryl, substituted aryl; CN; COR8, wherein R8 is H, OH, lower alkyl, lower alkoxy; SO2R9, wherein R9 is OR10, wherein R10 is H, lower alkyl or NRnR12, wherein R11 and R12 is H or lower alkyl; ORi3, wherein R13 is H, lower alkyl, C2-C6 acyl, C1-C8 carboxy, C1-C8 carbamoyl; X is O or S; A is H, lower alkyl; B is C1-C18 alkyl optionally substituted; M is zero or 1; with the proviso that no more than three of R1-R4 are H, for treating and preventing bronchoconstructive pulmonary disease.
Fused bicyclic Gly-Asp β-turn mimics with specific affinity for GPIIb- IIIa
Fisher, Matthew J.,Arfstan, Ann E.,Giese, Ulrich,Gunn, Bruce P.,Harms, Cathy S.,Khau, Vien,Kinnick, Michael D.,Lindstrom, Terry D.,Martinelli, Michael J.,Mest, Hans-Jürgen,Mohr, Michael,Morin Jr., John M.,Mullaney, Jeffrey T.,Nunes, Anne,Paal, Michael,Rapp, Achim,Rühter, Gerd,Ruterbories, Ken J.,Sall, Daniel J.,Scarborough, Robert M.,Schotten, Theo,Sommer, Birgit,Stenzel, Wolfgang,Towner, Richard D.,Um, Suzane L.,Utterback, Barbara G.,Vasileff, Robert T.,V?elkers, Silke,Wyss, Virginia L.,Jakubowski, Joseph A.
, p. 4875 - 4889 (2007/10/03)
Disubstituted isoquinolones 2 and 3 have affinity for GPIIb-IIIa and represent leads for further structural evaluation. Structure activity studies centered on the bicyclic β-turn mimic contained in these molecules indicated that this moiety could accommodate a variety of modifications. Specifically, monocyclic, 6,5-bicyclic, and 6,7-bicyclic structures provide compounds with affinity for GPIIb-IIIa. Within the 6,6-series, isoquinoline, tetralin, tetralone, and benzopyran nuclei yield potent antagonists that are specific for GPIIb-IIIa. Attachment of the arginine isostere (benzamidine) to the supporting nucleus can be accomplished with an ether or amide linkage, although the latter enhances activity. Several compounds in this series provided measurable blood levels after oral dosing. Conversion of the acid moiety in these molecules to an ester generally provided compounds which gave greater systemic exposure after oral administration. Absolute bioavailabilities in the rat for the ethyl ester prodrug derivatives of the tetralin, tetralone, and benzopyran analogues of 3 were 28%, 23%, and 24%, respectively.
