223690-01-5Relevant articles and documents
S1P1 AGONIST AND APPLICATION THEREOF
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, (2021/10/02)
The present invention relates to a class of tricyclic compounds and an application thereof as a sphingosine 1-phosphate type 1 (S1P1) receptor agonist. The invention specifically relates to a compound represented by formula (II), and a tautomer and pharmaceutically acceptable salt of same.
Copper-catalyzed chan-lam cyclopropylation of phenols and azaheterocycles
Derosa, Joseph,O'Duill, Miriam L.,Holcomb, Matthew,Boulous, Mark N.,Patman, Ryan L.,Wang, Fen,Tran-Dubé, Michelle,McAlpine, Indrawan,Engle, Keary M.
, p. 3417 - 3425 (2018/04/14)
Small molecules containing cyclopropane-heteroatom linkages are commonly needed in medicinal chemistry campaigns yet are problematic to prepare using existing methods. To address this issue, a scalable Chan-Lam cyclopropylation reaction using potassium cyclopropyl trifluoroborate has been developed. With phenol nucleophiles, the reaction effects O-cyclopropylation, whereas with 2-pyridones, 2-hydroxybenzimidazoles, and 2-aminopyridines the reaction brings about N-cyclopropylation. The transformation is catalyzed by Cu(OAc)2 and 1,10-phenanthroline and employs 1 atm of O2 as the terminal oxidant. This method is operationally convenient to perform and provides a simple, strategic disconnection toward the synthesis of cyclopropyl aryl ethers and cyclopropyl amine derivatives bearing an array of functional groups.
NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES
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Page/Page column 91, (2016/06/28)
The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
PPAR AGONISTS AND METHODS OF USE THEREOF
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Page/Page column 147, (2016/05/02)
Provided herein are deuterated compounds and compositions useful in increasing PPAR5 activity. The compounds and compositions provided herein are useful for the treatment of PPAR5 related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
COMPOUNDS FOR THE TREATMENT OF ARENAVIRUS INFECTION
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Page/Page column 156, (2017/03/14)
The present invention relates to the use of piperazinones for inhibiting arenavirus infection in humans, other mammals, or in cell culture, to methods of treating arenavirus infection such as Lassa, Bolivian, Argentine, Venezuelan, Brazilian, Chapare and
PPAR AGONISTS
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Page/Page column 114, (2014/10/18)
Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists
Lemoine, Rémy C.,Petersen, Ann C.,Setti, Lina,Chen, Lijing,Wanner, Jutta,Jekle, Andreas,Heilek, Gabrielle,deRosier, André,Ji, Changhua,Rotstein, David M.
scheme or table, p. 1830 - 1833 (2010/07/02)
The bicyclic 5-amino-3-azabicyclo[3.3.0]octanes were shown to be effective replacements for the conformationally restricted 4-aminopiperidine ring found in several series of CCR5 antagonists.
A convenient method for the preparation of aryl cyclopropyl ethers from phenols
Hollingworth, Gregory J.,Dinnell, Kevin,Dickinson, Laura C.,Elliott, Jason M.,Kulagowski, Janusz J.,Swain, Christopher J.,Thomson, Christopher G.
, p. 2633 - 2636 (2007/10/03)
A general method for the synthesis of cyclopropyl ethers from phenols is described. Alkylation of a phenol using 1-iodo-1-(phenylthio)cyclopropane followed by removal of the phenylthio group furnishes the cyclopropyl ethers in modest to excellent yields. The procedure tolerates a wide range of functional groups.
