138428-37-2Relevant articles and documents
Convenient Continuous Flow Synthesis of N-Methyl Secondary Amines from Alkyl Mesylates and Epoxides
Lebel, Hélène,Mathieu, Gary,Patel, Heena
, p. 2157 - 2168 (2020/11/23)
The first continuous flow process was developed to synthesize N-methyl secondary amines from alkyl mesylates and epoxides via a nucleophilic substitution using aqueous methylamine. A variety of N-methyl secondary amines were produced in good to excellent yields, including a number of bioactive compounds or their precursors. Up to 10.6 g (88% yield) of an N-methyl secondary amine was produced in 140 min process time. The amination procedure included an in-line workup, and the starting mesylate material was also produced in continuous flow from the corresponding alcohol. Finally, an in-line process combining the mesylate synthesis and nucleophilic substitution was developed.
triAZOLOtriAZINE DERIVATIVES AS A2A RECEPTOR ANTAGONISTS
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Page/Page column 49, (2020/01/24)
The present invention provides triazolotriazine derivatives of formula (1) as A2A receptor antagonists. Compounds of formula (1) and pharmaceutical compositions including the compounds can be used for the treatment of disorders related to A2A receptor hyperfunctioning, such as certain types cancers. Compounds of formula (1) and methods of preparing the compounds are disclosed in the invention.
Structure-based drug design, synthesis and biological assays of P. falciparum Atg3–Atg8 protein–protein interaction inhibitors
Villa, Stefania,Legnani, Laura,Colombo, Diego,Gelain, Arianna,Lammi, Carmen,Bongiorno, Daniele,Ilboudo, Denise P.,McGee, Kellen E.,Bosch, Jürgen,Grazioso, Giovanni
, p. 473 - 486 (2018/02/06)
The proteins involved in the autophagy (Atg) pathway have recently been considered promising targets for the development of new antimalarial drugs. In particular, inhibitors of the protein–protein interaction (PPI) between Atg3 and Atg8 of Plasmodium falc
Pyridine ethyoxyl coumarin plant growth regulator
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Paragraph 0019; 0020; 0021, (2017/07/19)
The invention discloses a pyridine ethyoxyl coumarin compound with a structure shown as a formula I, and the pyridine ethyoxyl coumarin compound serves as a plant growth regulator. The compound shown as the formula I has excellent effects of promoting germination and rooting, increasing the yield and improving the quality and can be widely used for increasing the yield or improving the survival rate in agriculture or forestry.
2,4,6-trichloro phenylpyridine ethyl ether plant growth regulator
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Paragraph 0017; 0018; 0019, (2017/07/20)
The invention discloses a 2,4,6-trichloro phenylpyridine ethyl ether compound structurally shown as a formula I. The 2,4,6-trichloro phenylpyridine ethyl ether compound is used as a plant growth regulator. The compound shown as a formula I has the advantages that the plant rooting and sprouting are promoted, the growth and the development are promoted; the obvious yield improving effect is achieved; the structure is simple; the production and use cost is low; the use is safe; the compound can be used for crop and fruit and vegetable yield improvement and quality improvement. The formula I is shown as the accompanying drawing.
CXCR4 INHIBITORS AND USES THEREOF
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Paragraph 00326; 00359; 00401, (2018/04/11)
The present invention provides compounds, compositions thereof, and methods of using the same.
CXCR4 INHIBITORS AND USES THEREOF
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Page/Page column 00320; 00347, (2018/04/11)
The present invention provides compounds, compositions thereof, and methods of using the same.
BICYCLIC HETEROCYCLIC DERIVATIVES AS BROMODOMAIN INHIBITORS
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Paragraph 0193, (2017/04/04)
The present disclosure provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n, and dotted line have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders associated as bromodomain inhibitors. The present disclosure also provides preparation of compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent, or excipient.
2,4-DIOXO-QUINAZOLINE-6-SULFONAMIDE DERIVATIVES AS INHIBITORS OF PARG
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Paragraph 00803, (2016/07/05)
The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
BICYCLIC HETEROCYCLIC DERIVATIVES AS BROMODOMAIN INHIBITORS
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Page/Page column 40; 41, (2015/07/23)
The present invention provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n and dotted line are have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder associated as bromodomain inhibitors. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
