42098-25-9Relevant academic research and scientific papers
Synthesis and Biological Profiling of Pyrazolo-Fused 7-Deazapurine Nucleosides
Fleuti, Marianne,Bártová, Kate?ina,Slavětínská, Lenka Po?tová,Tlou?t'Ová, Eva,Tichy, Michal,Gurská, Soňa,Pavli?, Petr,D?ubák, Petr,Hajdúch, Marián,Hocek, Michal
, p. 10539 - 10551 (2020/09/18)
A series of 8-substituted 1-methyl-1,4-dihydropyrazolo[3′,4′:4,5]pyrrolo[2,3-d]pyrimidine (methylpyrazolo-fused 7-deazapurine) ribonucleosides have been designed and synthesized. Two synthetic approaches to the key heterocyclic aglycon 7, (i) a six-step c
PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR
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Paragraph 0109, (2020/11/23)
The present invention relates to a pyrrolo(pyrazolo)pyrimidine derivative having efficacy as an LRRK2 inhibitor, a preparation method therefor, and a pharmaceutical composition for preventing or treating degenerative brain diseases, containing the same.
NOVEL MACROCYCLIC DERIVATIVES, PROCESS FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
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Paragraph 0385-0387, (2020/08/25)
Compound of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, X, Y and G are as defined in the description, and their use in the manufacture of medicaments.
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma
Wang, Xiaojing,Blackaby, Wesley,Allen, Vivienne,Chan, Grace Ka Yan,Chang, Jae H.,Chiang, Po-Chang,Diène, Coura,Drummond, Jason,Do, Steven,Fan, Eric,Harstad, Eric B.,Hodges, Alastair,Hu, Huiyong,Jia, Wei,Kofie, William,Kolesnikov, Aleksandr,Lyssikatos, Joseph P.,Ly, Justin,Matteucci, Mizio,Moffat, John G.,Munugalavadla, Veerendra,Murray, Jeremy,Nash, David,Noland, Cameron L.,Del Rosario, Geoff,Ross, Leanne,Rouse, Craig,Sharpe, Andrew,Slaga, Dionysos,Sun, Minghua,Tsui, Vickie,Wallweber, Heidi,Yu, Shang-Fan,Ebens, Allen J.
, (2019/03/07)
Pim kinases have been targets of interest for a number of therapeutic areas. Evidence of durable single-agent efficacy in human clinical trials validated Pim kinase inhibition as a promising therapeutic approach for multiple myeloma patients. Here, we report the compound optimization leading to GDC-0339 (16), a potent, orally bioavailable, and well tolerated pan-Pim kinase inhibitor that proved efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models and has been evaluated as an early development candidate.
Kinase inhibitor, and preparation and application of kinase inhibitor
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Paragraph 0237-0239; 0242; 0243; 0290; 0294, (2018/09/11)
The invention provides a compound shown as a formula (I), or a stereoisomer, a tautomer, nitrogen oxide, metabolite, a prodrug, pharmaceutically acceptable salt or solvate of the compound, and application of the compound to preparing drugs or drug compositions for treating Pim kinase-mediated diseases.
ORGANIC COMPOUNDS
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Paragraph 0021, (2016/06/28)
The present invention relates to novel PDE2 inhibitory compounds of Formula I as described above, their use as pharmaceuticals and pharmaceutical compositions comprising them.
FURO- AND THIENO-PYRIDINE CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
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Paragraph 0714, (2015/03/04)
The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
OXEPAN-2-YL-PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE
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Page/Page column 59, (2015/11/11)
Oxepan-2-yl pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for in
CYCLIC ETHER PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE
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Page/Page column, (2014/04/03)
Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE
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Paragraph 0177; 0178; 0179, (2013/04/10)
Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
