56245-07-9Relevant articles and documents
INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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, (2020/02/16)
The present invention provides compounds of formula (I) wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases.
N2-(2-METHOXYPHENYL)PYRIMIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION FOR CANCER PREVENTION OR TREATMENT CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 0323; 0324; 0325, (2018/05/03)
The present invention relates to a N2-(2-methoxyphenyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The N2-(2-methoxyphenyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.
Role of the benzylic hydroxyl group of adrenergic catecholamines in eliciting α-adrebergic activity. Synthesis and α1- and α2-adrenergic activity of 3-phenyl-3-piperidinols and their desoxy analogs
Macchia, B.,Macchia, M.,Manera, C.,Martinotti, E.,Nancetti, S.,et al.
, p. 869 - 880 (2007/10/03)
In order to contribute to the definition of the role played by the benzylic hydroxyl group of adrenergic catecholamines in eliciting α-adrenergic activity, certain 3-phenyl-3-piperidinols (PPOs, 4) and their corresponding desoxy 3-phenylpiperidine analogs (PPEs, 6) were synthesized and tested for their α1- and α2-adrenergic activity by means of functional tests on isolated preparations.As regards the α1-adrenergic activity, the values of the activity indices of the cyclic catecholic compounds (PPO 4a and PPE 6a) indicate that the benzylic hydroxyl does notplay an essential role, provided that the other two active groups are in the pharmacophoric conformation.However, the fact that none of the other non-catecholic cyclic analogs are active on the α1-receptor does not allow us to generalize this observation.As regards the α2-adrenergic activity, the high values of the activity indices of PPEs 6, compared with those of the corresponding 1-phenyl-2-aminoethanols (PAEs,3), PPPOs (4) and 2-phenylethylamines (PEAs,5), confirm that when the aromatic moiety and the amino group are constrained into the pharmacophoric relationship, the presence of the alcoholic hydroxyl is not only unnecessary for the purposes of the expression of the activity at the level of the α2-adrenoceptor, but often has negative effect. adrenergic drug / 3-phenyl-3-piperidinol / 3-phenylpiperidine / 1-phenyl-2-aminoethanol / 2-phenylethylamine / α1-adrenergic agonist activity / α2-adrenergic agonist activity