81428-01-5Relevant articles and documents
BICYCLIC JAK INHIBITORS AND USES THEREOF
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Paragraph 000277, (2020/10/20)
Provided herein are compounds of Formulas (I), (II), (III), and (IV) and subformulas thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I), (II), (III), or (IV) and methods of using the compounds, e.g., in the treatment of immune disorders, inflammatory disorders, and cancer.
SGC STIMULATORS
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Paragraph 00274, (2014/09/29)
Compounds of Formulae (I') and (I) are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
Synthesis and QSAR of Quinazoline Sulfonamides As Highly Potent Human Histamine H4 Receptor Inverse Agonists
Smits, Rogier A.,Adami, Maristella,Istyastono, Enade P.,Zuiderveld, Obbe P.,Van Dam, Cindy M. E.,De Kanter, Frans J. J.,Jongejan, Aldo,Coruzzi, Gabriella,Leurs, Rob,De Esch, Iwan J. P.
experimental part, p. 2390 - 2400 (2010/09/11)
Hit optimization of the class of quinazoline containing histamine H 4 receptor (H4R) ligands resulted in a sulfonamide substituted analogue with high affinity for the H4R. This moiety leads to improved physicochemical properties and is believed to probe a distinct H4R binding pocket that was previously identified using pharmacophore modeling. By introducing a variety of sulfonamide substituents, the H4R affinity was optimized. The interaction of the new ligands, in combination with a set of previously published quinazoline compounds, was described by a QSAR equation. Pharmacological studies revealed that the sulfonamide analogues have excellent H4R affinity and behave as inverse agonists at the human H4R. In vivo evaluation of the potent 2-(6-chloro-2-(4-methylpiperazin-1-yl)quinazoline4-amino)-N- phenylethanesulfonamide (54) (pki = 8.31 ± 0.10) revealed it to have anti-inflammatory activity in an animal model of acute inflammation.
Quinazolines and related heterocyclic compounds and their therapeutic use
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Page/Page column 15, (2009/07/18)
A compound of the formula wherein X is CR1 or N; Y is CR3 or N; R1, R3, R4, R5 and R6 are independently H, F, Cl, Br, I, or a hydrocarbon group which optionally contains one or more heteroatoms; R7 is a heterocyclic group including one or more N atoms; R' is Rx or NRyRz wherein Rx, Ry and Rz are each H or the same or different groups, including cyclic groups formed by Ry and Rz with the N atom, of up to 20 C atoms and optionally including up to 3 further heteroatoms selected from N, O and S; or a pharmaceutically acceptable salt, ester or solvate thereof, has therapeutic utility.
Synthesis and biological properties of new 1β-methylcarbapenems
Shin, Kye Jung,Yoo, Kyung Ho,Kim, Dong Jin,Park, Sang Woo,Ko, Bong Suck,Lee, Sang Joo,Huh, Jae Doo,Park, Seung Yong
, p. 1607 - 1612 (2007/10/03)
The synthesis and biological activity of the novel series of 1β- methylcarbapenems, 1 and 2 were described. Most compounds displayed high potent antibacterial activity. The best compound in this series, 2a (IH201; R2=NH2) showed an excellent and a broad spectrum as well as high renal DHP- I stability. It also possessed good in vivo efficacy and high safety.
Synthesis and anticonvulsant properties of some 2-aminoethanesulfonic acid (taurine) derivatives
Andersen,Sundman,Linden,Kontro,Oja
, p. 106 - 108 (2007/10/02)
A series of 2-acylaminoethanesulfonamides were synthesized by treating the corresponding sulfonyl chlorides with ammonia, a primary, or a secondary amine. A few compounds displayed marked anti-convulsant activity in mice when tested for their potency in the maximal electroshock seizure test. The piperidino, benzamido, phthalimido, and phenylsuccinylimido derivatives were active, whereas the succinylimido, saccharinylimido, and norbornendicarboxylimido compounds showed no activity. The interference with the sodium-independent taurine binding to mouse brain synaptic membranes was assessed to elucidate the possible mode of anticonvulsant action.
