211315-47-8Relevant articles and documents
IDO inhibitor
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Paragraph 0058-0063, (2019/10/01)
The invention relates to a compound with a structure of formula I or pharmaceutically acceptable salts, solvates, hydrates, active metabolites, polymorphs, esters, isotope compounds, stereoisomers orprodrugs thereof, a pharmaceutical composition containing the compound with a structure of formula I and application thereof as an IDO inhibitor for preparing drugs for preventing or treating cancer,virus infection, depression, cataract, organ transplant rejection or autoimmune diseases.
Atropisomer Control in Macrocyclic Factor VIIa Inhibitors
Glunz, Peter W.,Mueller, Luciano,Cheney, Daniel L.,Ladziata, Vladimir,Zou, Yan,Wurtz, Nicholas R.,Wei, Anzhi,Wong, Pancras C.,Wexler, Ruth R.,Priestley, E. Scott
supporting information, p. 4007 - 4018 (2016/05/19)
Incorporation of a methyl group onto a macrocyclic FVIIa inhibitor improves potency 10-fold but is accompanied by atropisomerism due to restricted bond rotation in the macrocyclic structure, as demonstrated by NMR studies. We designed a conformational constraint favoring the desired atropisomer in which this methyl group interacts with the S2 pocket of FVIIa. A macrocyclic inhibitor incorporating this constraint was prepared and demonstrated by NMR to reside predominantly in the desired conformation. This modification improved potency 180-fold relative to the unsubstituted, racemic macrocycle and improved selectivity. An X-ray crystal structure of a closely related analogue in the FVIIa active site was obtained and matches the NMR and modeled conformations, confirming that this conformational constraint does indeed direct the methyl group into the S2 pocket as designed. The resulting rationally designed, conformationally stable template enables further optimization of these macrocyclic inhibitors.
HYDROXAMIC ACIDS AND USES THEREOF
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Paragraph 0071; 0073, (2016/10/31)
Compounds of formula I are provided Formula (I) R1 is an alkoxy or O(CH2)pX, p is an integer from 2 to 3 and X is OH, NH2, or CO2H, m is an integer from 0 to 5, n is an integer from 0 to 5, each Rsub
PYRROLOPYRIDINES AS KINASE INHIBITORS
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Page/Page column 44, (2009/09/04)
Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Formula, (I).
PYRAZOLOPYRIDINES AS KINASE INHIBITORS
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Page/Page column 50, (2009/09/04)
Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
Sulphonamide derivatives
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, (2008/06/13)
Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formulaR1—L—NHSO2R2??Iin whichR1 represents an unsubstituted or substituted aromatic or heteroaromatic group;R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R3R4N in which R3 and R4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; andL represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring;and pharmaceutically acceptable salts thereof.Also disclosed are compounds of formula I, processes for preparing them and pharmaceutical compositions containing them.