39976-03-9Relevant academic research and scientific papers
IDO/TDO Inhibitor
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Paragraph 0735-0738; 0831-0834, (2020/08/19)
A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R1 and R2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R1 and R2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R4 represents, for example, —C(═NH)—HN2, and R6 represents, for example, a substituted or unsubstituted aryl group].
Preparation method of hydroxyamide
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Paragraph 0036-0039, (2020/02/10)
The invention discloses a preparation method of a hydroxyamide shown as formula (I). The hydroxyamide is prepared through homogeneous catalytic hydrogenation reaction of a cyclic imide represented byformula (II), wherein R1, R2 and R3 are respectively and
NOVEL ULK1 INHIBITORS AND METHODS USING SAME
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Page/Page column 243; 244, (2016/03/22)
In certain aspects, the invention provides a method for treating a disease or condition in a subject, the method comprising co-administering to a subject in need thereof a therapeutically effective amount of at least one ULK1-inhibiting pyrimidine, and a therapeutically effective amount of an mTOR inhibitor.
PROCESS FOR THE ASYMMETRIC HYDROGENATION OF IMIDES
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Page/Page column 46, (2010/12/31)
The present disclosure provides a process for the mono-reduction of one or more imide moieties in a compound comprising contacting the compound with hydrogen gas and a catalyst comprising a transition metal hydride in the presence of a base, under conditi
A new strategy for the preparation of secondary amines via o- (tetrahydropyranyloxymethyl)-benzamides
Fichert, Thomas,Massing, Ulrich
, p. 5017 - 5018 (2007/10/03)
The new synthesis strategy for the preparation of secondary amines starts from N-alkyl-phthalimides which are reduced to the corresponding o- hydroxymethyl-N-alkyl-benzamides. After protection of the hydroxy group as tetrahydropyranyl ether the N-alkyl-benzamides are alkylated to o- (tetrahydropyranyloxymethyl)-N,N-dialkyl-benzamides. The deprotection of the hydroxy group and the release of the secondary amines can be achieved in execellent yields in one reaction step using aqueous acetic acid.
Cyclic-fused azomethine-, imidate-, and thioimidate methylides: An efficient regiocontrolled entry into spiro-fused pyrrolidines
Fishwick, Colin W.G.,Foster, Richard J.,Carr, Robin E.
, p. 5163 - 5166 (2007/10/03)
Generation of azomethine ylides, imidate methylides, and thioimidate methylides which are exocyclic to indane, benzofuran, benzothiophene, and benzopyran moieties respectively, in the presence of electron deficient dipolarophiles, gives direct access to s
Some Studies on Peptide Analogues Involving the Sulphinamide Group
Merricks, David,Sammes, Peter G.,Walker, Edward R. H.,Henrick, Kim,McPartlin, Mary M.
, p. 2169 - 2176 (2007/10/02)
The title compounds are of interest as possible transition state inhibitors of peptidases.A route to N-(alkylsulphinyl)amino acids is described.A method for generating α-benzamidosulphinamides is reported; a general route to such systems failed owing to t
The mechanism of electrochemical reduction of N-haloamides in acetonitrile: trapping of intermediate amide anions and father-son protonation
Berube, Denis,Lessard, Jean
, p. 1127 - 1142 (2007/10/02)
The electrochemical reduction of N-haloamides (ZCONRX) in acetonitrile involves two consecutive one-electron transfers and generates the amide anions.Attempts to trap the intermediate amidyl radical resulting from first electron transfer were unssuccesful.In the case of the N-halo-N-hydroamides (R=H), the amide anion formed at the electrode abstracts a proton from an incoming N-halo-N-hydroamide molecule to give the parent amide and the conjugate base of the N-haloamide (father-son protonation).Thus, half of the N-halo-N-hydroamide reaching the electrode is reduced, the other half being converted to its conjugate base.In acetonitrile-LiClO4 (0.2 M) containing 0.2percent water, the conjugate base is reducible and polarograms therefore show two waves (irreversible and diffusion controlled) of equivalent intensities due respectively to the reduction of the N-halo-N-hydroamide and to the reduction of its conjugate base.In the case of the N-chloro-N-alkyl(aryl)amides (X=Cl, R=alkyl or aryl), the amide anion abstracts a proton from the medium to give the parent amide and anionic species that react with the starting N-chloroamide regenerating the amide anion.Hence, the coulometric results are low (0.5 F/mol).However, in the presence of acetic acid, the reduction consumes 2 F/mol as expected.The N-alkylamide anion has been trapped by N-alkylation and N-acylation.The voltammograms of N-chloro-N-alkyl(aryl)amides show multiple waves on mercury and platinum due to passivation-adsorption phenomena but a single wave on vitreous carbon.
