19090-03-0Relevant academic research and scientific papers
SUBSTITUTED PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
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, (2018/02/28)
The present invention relates to compounds according to Formula (I-1) and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent
Kerns, Jeffrey K.,Busch-Petersen, Jakob,Fu, Wei,Boehm, Jeffrey C.,Nie, Hong,Muratore, Michael,Bullion, Ann,Lin, Guoliang,Li, Huijie,Davis, Roderick,Lin, Xichen,Lakdawala, Ami S.,Cousins, Rick,Field, Rita,Payne, Jeremy,Miller, David D.,Bamborough, Paul,Christopher, John A.,Baldwin, Ian,Osborn, Ruth R.,Yonchuk, John,Webb, Edward,Rumsey, William L.
supporting information, p. 1164 - 1169 (2018/11/23)
IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the optimization of a series of 3,5-disubstituted-indole-7-carboxamides for oral activity. In doing so
Synthesis of Cyclic α-Diazo-β-keto Sulfoxides in Batch and Continuous Flow
McCaw, Patrick G.,Buckley, Naomi M.,Eccles, Kevin S.,Lawrence, Simon E.,Maguire, Anita R.,Collins, Stuart G.
, p. 3666 - 3679 (2017/04/11)
Diazo transfer to β-keto sulfoxides to form stable isolable α-diazo-β-keto sulfoxides has been achieved for the first time. Both monocyclic and benzofused ketone derived β-keto sulfoxides were successfully explored as substrates for diazo transfer. Use of continuous flow leads to isolation of the desired compounds in enhanced yields relative to standard batch conditions, with short reaction times, increased safety profile, and potential to scale up.
FUSED TRICYCLIC COMPOUNDS FOR USE AS INHIBITORS OF JANUS KINASES
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Page/Page column 107, (2013/03/26)
The invention provides novel compounds of formula (I) having the general formula (I) wherein R1, V, W, X, Y and Z are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2
De Savi, Chris,Morley, Andrew D.,Nash, Ian,Karoutchi, Galith,Page, Ken,Ting, Attilla,Gerhardt, Stefan
supporting information; experimental part, p. 271 - 277 (2012/02/16)
Directed screening has identified a novel series of non-zinc binding MMP13 inhibitors that possess good levels of activity whilst demonstrating excellent selectivity over related MMPs. A lead optimisation campaign has delivered compounds with enhanced MMP
INDOLE CARBOXAMIDES AS IKK2 INHIBITORS
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Page/Page column 96, (2008/12/04)
The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
SPIROCYCLOPROPYL PIPERIDINE DERIVATIVES
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Page/Page column 79, (2009/01/20)
Disclosed herein is at least one piperidine derivative, at least one pharmaceutical composition comprising at least one piperidine derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith
The search for TCP analogues binding to the low affinity PCP receptor sites in the rat cerebellum
Hamon, Jacques,Espaze, Florence,Vignon, Jacques,Kamenka, Jean-Marc
, p. 125 - 135 (2007/10/03)
With the aim of obtaining selective ligands of the low affinity binding sites of [3H]-1-[1-(2-thienyl)cyclohexyl]piperidine ([3H]TCP) in the rat cerebellum, oxygen and sulfur atoms were introduced in the TCP structure and derivatives to obtain analogues with a lowered lipophilicity. These compounds, and others already obtained, were assayed comparatively to determine their affinities for three sites labeled with [3H]TCP: one in the forebrain, the originally described PCP receptor, and two in the rat cerebellum. Lowering the lipophilicity and modifying the hetero-aromatic moiety yielded some ligands with increased affinity for the low affinity sites in the rat cerebellum and decreased affinity for the high affinity sites in the forebrain. Particularly, two compounds displaying both a high affinity and a good selectivity might be valuable tools to elucidate the pharmacology of the low affinity PCP sites labeled with [3H]TCP in the rat cerebellum.
Enzymes in organic syntheses. 19. Evaluation of the stereoselectivities of horse liver alcohol dehydrogenase; catalyzed oxidoreductions of hydroxy- and ketothiolanes, -thianes, and -thiepanes
Jones, J. Bryan,Schwartz, Harold M.
, p. 1574 - 1579 (2007/10/02)
The specificity of horse liver alcohol dehydrogenase (HLADH) with respect to unsubstituted five-, six-, and seven-membered ring 3- and 4-thiaketone and -thiaalcohol substrates has been examined.The enzyme is found to have a broad tolerance of the structural variations within this series.HLADH also exhibits encouraging (up to 46percent) enantiotopic and enantiomeric specifity in preparative-scale reduction and oxidation reactions of the heterocyclic ketones and alcohols respectively.
