37784-17-1Relevant articles and documents
RAS INHIBITORS
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Paragraph 1184-1185, (2021/05/07)
The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
METHODS FOR DELAYING, PREVENTING, AND TREATING ACQUIRED RESISTANCE TO RAS INHIBITORS
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Page/Page column 342-343, (2022/01/04)
The present disclosure relates to compositions and methods for the treatment of diseases or disorders (e.g., cancer) with bi-steric inhibitors of mTOR in combination with RAS inhibitors. Specifically, in some embodiments this disclosure includes compositions and methods for inducing apoptosis of tumor cells and/or for delaying, preventing, or treating acquired resistance to RAS inhibitors using bi-steric mTOR inhibitors.
Evidence and exploitation of dicationic ammonium-nitrilium superelectrophiles: direct synthesis of unsaturated piperidinones
Cantin, Thomas,Morgenstern, Yvonne,Mingot, Agnès,Kornath, Andreas,Thibaudeau, Sébastien
supporting information, p. 11110 - 11113 (2020/10/05)
Exploiting superacid activation, the reactivity of aminonitriles was enhanced through the transient formation of highly reactive ammonium-nitrilium superelectrophiles. Demonstrated by usingin situlow-temperature NMR experiments and confirmed by X-ray diffraction analysis, these dications can be intramolecularly trapped by non-activated alkenes to generate unsaturated piperidinones, including enantioenriched ones, in a straightforward way.
MORPHINAN DERIVATIVE
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Paragraph 0113-0114; 0115-0116, (2019/06/27)
A compound represented by the following general formula (I), wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, or the like, R2 represents a 4- to 7-membered saturated heterocycle containing one or two heteroatoms which may be the same or different and are selected from N, O, and S, and two or more carbon atoms as ring-constituting atoms, the heterocycle may be substituted with a substituent such as an oxo group, R2 binds to Y via a carbon atom as a ring-constituting atom of R2, R3, R4, and R5, which are the same or different, represent hydrogen; hydroxy; or the like, R6a and R6b, which are the same or different, represent hydrogen or the like, R7 and R8, which are the same or different, represent hydrogen or the like, R9 and R10, which are the same or different, represent hydrogen or the like, X represents O or CH2, and Y represents C(= O) or the like), a tautomer of the compound, a stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic, an antidepressant, or the like.
Synthesis of novel phase transfer catalysts derived from proline-mandelic acid/tartaric acid: their evaluation in enantioselective epoxidation and Darzen condensation
Mahajan, Deepak P,Godbole, Himanshu M,Singh, Girij P,Shenoy, Gautham G
, (2019/02/27)
Abstract : Herein, we have described the synthesis of novel chiral cyclic phase transfer catalysts (PTCs). These catalysts are synthesized from proline, mandelic acid and tartaric acid by using simple synthetic methods with competitive yields. These chira
SUBSTITUTED AMINO TRIAZOLES USEFUL AS HUMAN CHITINASE INHIBITORS
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Page/Page column 156; 157, (2017/03/21)
Disclosed are amino triazole compounds substituted with a piperidinyl ring that is itself substituted with a heterocyclic ring. These compounds are inhibitors of acidic mammalian chitinase and chitotriosidase. Also disclosed are methods of using the compounds to treat asthma reactions caused by allergens, as well as acute and chronic inflammatory diseases, autoimmune diseases, dental diseases, neurologic diseases, metabolic diseases, liver diseases, polycystic ovary syndrome, endometriosis, and cancer.
NOVEL BETULINIC SUBSTITUTED AMIDE DERIVATIVES AS HIV INHIBITORS
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Page/Page column 49, (2017/02/24)
The present invention relates to novel betulinic substituted amide compounds of formula (I); and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y, Z1, Z2, Z3 and are Formula (II) as defined herein. The invention novel betulinic substituted amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
Aggregation propensity of amyloidogenic and elastomeric dipeptides constituents
Kumar, Vikas,Krishna, K. Vijaya,Khanna, Shruti,Joshi, Khashti Ballabh
supporting information, p. 5369 - 5376 (2016/08/05)
This study demonstrates the self-assembly of N- and C-terminal protected dipeptides Phe–Gly and Pro–Gly which were derived from amyloidogenic and elastomeric peptide sequences. These constituents afforded nanostructured supramolecular ensembles through va
NOVEL BETULINIC ACID PROLINE DERIVATIVES AS HIV INHIBITORS
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Paragraph 0264, (2014/07/21)
The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases. These compounds are esterified in position 3 and are substituted in position 17 of the betulinic acid structure, via a linking group W, by a saturated 5-7 membered nitrogen-heterocycle.
Catalytic anions embedded into avidin: Importance of their chirality and the chiral environment on the stereocontrol of the aldol reaction
Gauchot, Vincent,Schmitzer, Andreea R.
, p. 2694 - 2701 (2014/04/17)
Several catalytic anions bearing a pseudo-dipeptide scaffold, in combination with a biotinylated imidazolium cation, were prepared. The assembly of these salts with avidin resulted in the formation of stable biohybrid catalysts, active in ionic liquid/aqueous media for the aldol reaction. By using natural and non-natural amino alcohols as "side chains" for the proline derivative anion, we studied the cooperativity between the anion and its position in avidin. Taking advantage of the large freedom of movement of the anion inside avidin, we also investigated the substrate scope of this type of biohybrid catalyst.
