30742-63-3Relevant academic research and scientific papers
MACROCYCLIC COMPOUND SERVING AS WEE1 INHIBITOR AND APPLICATIONS THEREOF
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Paragraph 0231-0234, (2020/11/30)
Disclosed in the present invention are a macrocyclic compound serving as a Weel inhibitor, and applications thereof in the preparation of drugs for treating Weel-related diseases. The present invention specifically relates to a compound represented by for
Pyrrolopyrimidine compound, pharmaceutical composition containing thereof, and preparation method and applications
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Paragraph 0220-0224, (2019/11/29)
The invention relates to a pyrrolopyrimidine compound represented by formula I, a pharmaceutical composition containing thereof, and a preparation method and applications in preventing or treating Weel protein kinase related diseases.
Ruthenium catalyzed β-C(sp3)-H functionalization on the 'privileged' piperazine nucleus
Murugesh,Bruneau, Christian,Achard, Mathieu,Sahoo, Apurba Ranjan,Sharma, Gangavaram V. M.,Suresh, Surisetti
supporting information, p. 10448 - 10451 (2017/09/25)
β-C(sp3)-H functionalization on the 'privileged' piperazine nucleus has been disclosed using ruthenium catalysis. The ruthenium catalyzed synthesis of a variety of piperazine fused indoles from ortho-piperazinyl (hetero)aryl aldehydes is presented. This transformation takes place via the dehydrogenation of piperazine followed by an intramolecular nucleophilic addition of the transient enamine moiety onto the carbonyl group and aromatization cascade.
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7, 26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27) ,16,21,23-decaene (SB1518), a potent Janus Kinase 2/Fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma
William, Anthony D.,Lee, Angeline C.-H.,Blanchard, Stéphanie,Poulsen, Anders,Teo, Ee Ling,Nagaraj, Harish,Tan, Evelyn,Chen, Dizhong,Williams, Meredith,Sun, Eric T.,Goh, Kee Chuan,Ong, Wai Chung,Goh, Siok Kun,Hart, Stefan,Jayaraman, Ramesh,Pasha, Mohammed Khalid,Ethirajulu, Kantharaj,Wood, Jeanette M.,Dymock, Brian W.
experimental part, p. 4638 - 4658 (2011/09/14)
Discovery of the activating mutation V617F in Janus Kinase 2 (JAK2 V617F), a tyrosine kinase critically involved in receptor signaling, recently ignited interest in JAK2 inhibitor therapy as a treatment for myelofibrosis (MF). Herein, we describe the design and synthesis of a series of small molecule 4-aryl-2-aminopyrimidine macrocycles and their biological evaluation against the JAK family of kinase enzymes and FLT3. The most promising leads were assessed for their in vitro ADME properties culminating in the discovery of 21c, a potent JAK2 (IC50 = 23 and 19 nM for JAK2 WT and JAK2V617F, respectively) and FLT3 (IC50 = 22 nM) inhibitor with selectivity against JAK1 and JAK3 (IC50 = 1280 and 520 nM, respectively). Further profiling of 21c in preclinical species and mouse xenograft and allograft models is described. Compound 21c (SB1518) was selected as a development candidate and progressed into clinical trials where it is currently in phase 2 for MF and lymphoma.
PYRIDYL SUBSTITUTED PYRIMIDINE DERIVATIVES
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Page/Page column 62-63, (2009/01/20)
The present invention relates to pyridyl substituted pyrimidine compounds that are useful as agents for the treatment of kinase related disorders such as proliferative disorders. More particularly, the present invention relates to oxygen linked and pyridy
