- CDK6 inhibitor of pyrimidine benzo six-membered ring mother nucleus as well as preparation method and application of CDK6 inhibitor
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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.
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Paragraph 0048; 0076-0078; 0111-0113
(2021/08/19)
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- INHIBITORS OF FIBROBLAST ACTIVATION PROTEIN
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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.
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Paragraph 0280
(2020/07/14)
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- Heterocyclic Compounds and Methods of Use
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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.
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- TYK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
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- SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C
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This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)- amides of formula (1) and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
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Page/Page column 209-210
(2014/09/29)
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- SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C
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This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
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Paragraph 0537; 0538
(2014/09/29)
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- Exploration of a series of 5-arylidene-2-thioxoimidazolidin-4-ones as inhibitors of the cytolytic protein perforin
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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).
- 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.
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supporting information
p. 9542 - 9555
(2014/01/06)
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- COMPOUNDS, PREPARATIONS AND USES THEREOF
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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
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Page/Page column 131
(2011/07/09)
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- Sulfonamide bicyclic compounds
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The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts and solvates, their pharmaceutical compositions, and their uses in inhibiting β-amyloid peptide (β-AP) production.
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Page/Page column 11
(2010/10/20)
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