SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.
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Paragraph 0228
(2019/10/15)
Dehydration of Amides to Nitriles under Conditions of a Catalytic Appel Reaction
A highly expedient protocol for a catalytic Appel-type dehydration of amides to nitriles has been developed that employs oxalyl chloride and triethylamine along with triphenylphosphine oxide as a catalyst. The reactions are usually complete in less than 10 min with only a 1 mol % catalyst loading. The reaction scope includes aromatic, heteroaromatic, and aliphatic amides, including derivatives of α-hydroxy and α-amino acids.
Shipilovskikh, Sergei A.,Vaganov, Vladimir Yu.,Denisova, Elena I.,Rubtsov, Aleksandr E.,Malkov, Andrei V.
supporting information
p. 728 - 731
(2018/02/09)
MACROCYCLIC DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES
The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.
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Page/Page column 226
(2013/09/26)
Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents
A series of boron-containing benzoxaborole compounds was designed and synthesized for a structure-activity relationship investigation surrounding 7-(HOOCCH2CH2)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (1) with the goal of discovering
Zhang, Yong-Kang,Plattner, Jacob J.,Freund, Yvonne R.,Easom, Eric E.,Zhou, Yasheen,Gut, Jiri,Rosenthal, Philip J.,Waterson, David,Gamo, Francisco-Javier,Angulo-Barturen, Inigo,Ge, Min,Li, Zhiya,Li, Lingchao,Jian, Yong,Cui, Han,Wang, Hailong,Yang, Jian
experimental part
p. 644 - 651
(2011/03/18)
BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS
This invention provides novel compounds of the following formula useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
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Page/Page column 73-74
(2011/04/13)
Cleft-type diamidinium receptors for dicarboxylate binding in protic solvents
A series of potential cleft-type receptors for dicarboxylate substrates were prepared by attachment of two phenylamidinium ions to either naphthalene or 1,1'-binaphthalene scaffolds. Their synthesis (Schemes 1-4) involved the Pd0-catalyzed cros