1131223-44-3Relevant articles and documents
CDK6 inhibitor of pyrimidine benzo six-membered ring mother nucleus as well as preparation method and application of CDK6 inhibitor
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Paragraph 0048; 0092; 0095-0096; 0111; 0114-0115, (2021/08/19)
The invention discloses a CDK6 inhibitor of a pyrimidine benzo six-membered ring mother nucleus and a preparation method and application of the CDK6 inhibitor, the compound structure of the CDK6 inhibitor is shown as a formula (C), and A is selected from O, C (O) or-NR1; R1 is selected from hydrogen or C1-C8 alkyl; B is selected from O or C; X is selected from C, C (O) or-NR2; R2 is selected from hydrogen or C1-C8 alkyl; Y is selected from C (O) or (CH2) n; n is 0 or 1; and Z is selected from hydrogen, C1-C8 alkyl or-C (O) OC1-C3. The invention also discloses a preparation method and application of the compound.
NAPHTHYRIDINE DERIVATIVES AS PRC2 INHIBITORS
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Paragraph 0419-0420, (2020/11/03)
Disclosed are compounds of formula (I) or (II) that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
IMIDAZO[1,2-C]PYRIMIDINE DERIVATIVES AS PRC2 INHIBITORS FOR TREATING CANCER
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Paragraph 0360-0361, (2020/12/29)
Disclosed are compounds that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, disclosed are compounds of Formula (I) and pharmaceutical compositions thereof, and methods of using the compounds and pharmaceutical compositions in, for example, methods of treating cancer.
INHIBITORS OF FIBROBLAST ACTIVATION PROTEIN
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, (2020/07/14)
Compounds and compositions for modulating fibroblast activation protein (FAP) are described. The compounds and compositions may find use as therapeutic agents for the treatment of diseases, including hyperproliferative diseases.
PRC2 INHIBITORS
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Paragraph 0369-0370, (2019/08/26)
The present invention relates to compounds that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention. (Formula (I))
HETEROCYCLYLAMINO-SUBSTITUTED TRIAZOLES AS MODULATORS OF RHO-ASSOCIATED PROTEIN KINASE
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Page/Page column 105, (2019/08/12)
This invention relates to novel compounds and pharmaceutical compositions comprising. Compounds of the invention useful as modulators of Rho-associated protein kinase (ROCK), for example ROCK1 and/or ROCK2 inhibitors. Methods of treatment employing the compounds are also contemplated by the present invention. The compounds of the invention are useful in treating ROCK mediated diseases.
Heterocyclic Compounds and Methods of Use
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, (2018/03/10)
This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.
Fused Pyrazoles as FGFR Inhibitors
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Paragraph 0250, (2014/06/25)
The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
Exploration of a series of 5-arylidene-2-thioxoimidazolidin-4-ones as inhibitors of the cytolytic protein perforin
Spicer, Julie A.,Lena, Gersande,Lyons, Dani M.,Huttunen, Kristiina M.,Miller, Christian K.,O'Connor, Patrick D.,Bull, Matthew,Helsby, Nuala,Jamieson, Stephen M. F.,Denny, William A.,Ciccone, Annette,Browne, Kylie A.,Lopez, Jamie A.,Rudd-Schmidt, Jesse,Voskoboinik, Ilia,Trapani, Joseph A.
, p. 9542 - 9555 (2014/01/06)
A series of novel 5-arylidene-2-thioxoimidazolidin-4-ones were investigated as inhibitors of the lymphocyte-expressed pore-forming protein perforin. Structure-activity relationships were explored through variation of an isoindolinone or 3,4-dihydroisoquinolinone subunit on a fixed 2-thioxoimidazolidin-4-one/thiophene core. The ability of the resulting compounds to inhibit the lytic activity of both isolated perforin protein and perforin delivered in situ by natural killer cells was determined. A number of compounds showed excellent activity at concentrations that were nontoxic to the killer cells, and several were a significant improvement on previous classes of inhibitors, being substantially more potent and soluble. Representative examples showed rapid and reversible binding to immobilized mouse perforin at low concentrations (≤2.5 μM) by surface plasmon resonance and prevented formation of perforin pores in target cells despite effective target cell engagement, as determined by calcium influx studies. Mouse PK studies of two analogues showed T1/2 values of 1.1-1.2 h (dose of 5 mg/kg iv) and MTDs of 60-80 mg/kg (ip).
COMPOUNDS, PREPARATIONS AND USES THEREOF
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Page/Page column 131, (2011/07/09)
The present invention provides novel compounds of the Formula (I), pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susc