1052714-11-0Relevant articles and documents
NITROGEN HETEROCYCLIC COMPOUNDS AND METHODS OF USE
-
Paragraph 1808; 1819, (2021/06/26)
The present disclosure relates to compounds of formula (I): and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of preparing the compounds, compositions comprising the compounds, and methods of using the compounds as inhibitors of receptor tyrosine kinases, in particular oncogenic mutants of ErbB-receptors e.g. in the treatment of cancer.
FUSED QUADRACYCLIC COMPOUNDS, COMPOSITIONS AND USES THEREOF
-
Paragraph 0300, (2017/08/01)
Provided herein are substituted fused quadracyclic compounds useful as inhibitors of MK2. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted fused quadracyclic compounds.
Pyridine derivative PIM kinase inhibitor and preparation method therefor and application thereof in pharmacy
-
Paragraph 0164; 0165; 0166; 0167, (2016/10/07)
The present invention provides a PIM kinase inhibitor and a preparation method therefor and an application thereof. The PIM kinase inhibitor is a compound with the structural formula shown in the formula I (the formula is shown in description). The present invention further provides a stereoisomer, a tautomer and pharmaceutical salt of the compound shown in the formula I. According to the present invention, the compound has an obvious inhibition effect on kinase activity. The PIM kinase inhibitor can be used for preparing drugs for curing or preventing cancer, autoimmune diseases, allergic reaction diseases or organ transplant rejection resistance and the like, and the PIM kinase inhibitor has relatively large value in clinical application.
SUBSTITUTED PYRIDINES AND METHOD OF USE
-
Paragraph 00308, (2016/12/22)
The invention discloses compounds of Formula (I) wherein X, R1, R2, and R3 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
ALKYNYL ALCOHOLS AND METHODS OF USE
-
Paragraph 0332; 0333; 0660; 0661; 1101; 1102, (2015/03/04)
The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
ALKYNYL ALCOHOLS AND METHODS OF USE
-
Page/Page column 95; 159, (2015/03/13)
The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
N-(3-PYRIDYL) BIARYLAMIDES AS KINASE INHIBITORS
-
Page/Page column 82, (2014/03/25)
The present invention provides a compound of formula (I): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds.
NOVEL RING-SUBSTITUTED N-PYRIDINYL AMIDES AS KINASE INHIBITORS
-
Page/Page column 75-76, (2014/01/07)
The present invention provides a compound of formula (A): I as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
Structure guided optimization, in vitro activity, and in vivo activity of pan-PIM kinase inhibitors
Burger, Matthew T.,Han, Wooseok,Lan, Jiong,Nishiguchi, Gisele,Bellamacina, Cornelia,Lindval, Mika,Atallah, Gordana,Ding, Yu,Mathur, Michelle,Mcbride, Chris,Beans, Elizabeth L.,Muller, Kristine,Tamez, Victoriano,Zhang, Yanchen,Huh, Kay,Feucht, Paul,Zavorotinskaya, Tatiana,Dai, Yumin,Holash, Jocelyn,Castillo, Joseph,Langowski, John,Wang, Yingyun,Chen, Min Y.,Garcia, Pablo D.
supporting information, p. 1193 - 1197 (2014/01/06)
Proviral insertion of Moloney virus (PIM) 1, 2, and 3 kinases are serine/threonine kinases that normally function in survival and proliferation of hematopoietic cells. As high expression of PIM1, 2, and 3 is frequently observed in many human malignancies, including multiple myeloma, non-Hodgkins lymphoma, and myeloid leukemias, there is interest in determining whether selective PIM inhibition can improve outcomes of these human cancers. Herein, we describe our efforts toward this goal. The structure guided optimization of a singleton high throughput screening hit in which the potency against all three PIM isoforms was increased >10,000-fold to yield compounds with pan PIM Kis 10 pM, nanomolar cellular potency, and in vivo activity in an acute myeloid leukemia Pim-dependent tumor model is described.
CYCLIC ETHER COMPOUNDS USEFUL AS KINASE INHIBITORS
-
Page/Page column 64, (2012/02/01)
The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof, as further described herein. Also provided are formulations comprising compounds of formula I, and a method to use such compounds for treating a disease or condition mediated by Provirus Integration of Maloney Maloney Kinase (PIM Kinase), GSK3, PKC, KDR, PDGFRa, FGFR3, FLT3, or cABL.