291545-74-9Relevant academic research and scientific papers
SUBSTITUTED MORPHOLINE DERIVATIVES AS ROR GAMMA MODULATORS
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Page/Page column 23, (2018/07/29)
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, X1, X2, m and n are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORyt). These compounds prevent, inhibit, or suppress the action of RORyt and are therefore useful in the treatment of RORyt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer. (I)
Aminoheteroaryl benzamides as kinase inhibitors
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Page/Page column 265, (2016/02/15)
The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
TRICYCLIC MODULATORS OF TNF SIGNALING
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Page/Page column 144, (2016/11/02)
The invention provides tricyclic heterocyclic compounds, pharmaceutically acceptable salts, prodrugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the invention may be useful for treating immunological and oncological conditions.
Diastereoselective synthesis of novel 5-substituted morpholine-3-phosphonic acids: Further exploitation of N-acyliminium intermediates
Bonilla-Landa, Israel,Viveros-Ceballos, José Luis,Ordó?ez, Mario
, p. 485 - 487 (2014/05/06)
The first diastereoselective total synthesis of 5-substituted morpholine-3-phosphonic acids is reported. The principal feature of the synthesis is the introduction of a dimethyl phosphonate group into 5-substituted morpholin-3-ones. The procedure is based
Amine-promoted asymmetric (4+2) annulations for the enantioselective synthesis of tetrahydropyridines: A traceless and recoverable auxiliary strategy
Hu, Pengfei,Hu, Jian,Jiao, Jiajun,Tong, Xiaofeng
supporting information, p. 5319 - 5322 (2013/06/05)
Gone, without a trace: The in situ reaction of 2-(acetoxymethyl)buta-2,3- dienoate and a secondary amine produces a 2-methylene-3-oxobutanoate equivalent that can be used in asymmetric [4+2] annulations with N-tosylimines to provide tetrahydropyridines in
Reversal of stereoselectivity in the Cu-catalyzed conjugate addition reaction of dialkylzinc to cyclic enone in the presence of a chiral azolium compound
Shibata, Naoatsu,Okamoto, Masaki,Yamamoto, Yuko,Sakaguchi, Satoshi
experimental part, p. 5707 - 5715 (2010/10/21)
Reversal of enantioselectivity in a Cu-catalyzed asymmetric conjugate addition reaction of dialkylzinc to cyclic enone with use of the same chiral ligand was successfully achieved. The reaction of 2-cyclohexen-1-one (30) with Et2Zn catalyzed by
4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase
Alexander, Rikki,Balasundaram, Ahrani,Batchelor, Mark,Brookings, Daniel,Crepy, Karen,Crabbe, Tom,Deltent, Marie-France,Driessens, Frank,Gill, Andrew,Harris, Sue,Hutchinson, Gillian,Kulisa, Claire,Merriman, Mark,Mistry, Prakash,Parton, Ted,Turner, James,Whitcombe, Ian,Wright, Sara
scheme or table, p. 4316 - 4320 (2009/04/06)
4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo profiling of compound 18 is shown to demonstrate the utility of this class of compounds in xenograft models of tumor growth.
Forward- and reverse-synthesis of piperazinopiperidine amide analogs: A general access to structurally diverse 4-piperazinopiperidine-based CCR5 antagonists
Feng, Dong-Zhi,Song, Yan-Li,Jiang, Xiao-Hua,Chen, Li,Long, Ya-Qiu
, p. 2690 - 2697 (2008/03/12)
Piperazinopiperidine amide analogs are among the most promising CCR5 antagonists. As an effective extension of a previously-reported methodology to synthesize such compounds, forward- and reverse-syntheses were successfully developed in which the convergent synthesis of the piperazinopiperidine nucleus, with a building block of 4-substituent-4-aminopiperidine, served as a common key step. The two-way approach affords a comprehensive access to the piperazinopiperidine templated library with variation on the pharmacophore sites. Thus, a SAR study of our synthesized piperazinopiperidine-based CCR5 antagonists was conducted with respect to the structure and configuration of the substituent on the piperazine ring. The S-configuration of the benzylic-substituent is vital for the CCR5 binding, and the bulky or aryl substituent on the 2-position in the piperazine ring is detrimental to the activity. By using the forward-synthesis approach, the best compound in the chiral piperazine-based CCR5 antagonist series, Sch-D (Vicriviroc), was conveniently synthesized in an excellent yield. The Royal Society of Chemistry.
SUBSTITUTED HETEROCYCLIC COMPOUNDS
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Page 29, (2008/06/13)
Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.
Primary amides. A general nitrogen source for catalytic asymmetric aminohydroxylation of olefins
Demko, Zachary P.,Bartsch, Michael,Sharpless, K. Barry
, p. 2221 - 2223 (2007/10/03)
(equation presented) N-Bromo,N-lithio salts of primary carboxamides have been shown to be efficient nitrogen sources for catalytic asymmetric aminohydroxylation of olefins, behaving much like the parent N-bromoacetamide in these reactions. α-Chloro-N-brom
