Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Nathaniel L, Segraves"'
Challenges in the structure determination of a dimeric impurity found during development of GDC-0326
Autor:
Nathaniel L, Segraves, Stefan G, Koenig, Jeffrey, Stults, Shengli, Ma, Antonio G, DiPasquale, Sarah J, Robinson, David J, Russell
Publikováno v:
Journal of Pharmaceutical and Biomedical Analysis. 213:114627
While developing a synthetic route for GDC-0326, a PI3Kα selective inhibitor, a side product was identified which was adversely impacting process chemistry development. To aid in optimization of a viable synthetic pathway for the drug, it was decide
Autor:
Nathaniel L. Segraves, Herbert Yajima, Remy Angelaud, Francis Gosselin, Andreas Stumpf, Andrew McClory
Publikováno v:
Organic Process Research & Development. 20:751-759
An improved, efficient process with a significantly reduced process mass intensity (PMI) led to the multikilogram synthesis of a brain penetrant PI3K inhibitor GDC-0084. Highlights of the synthesis include a phase transfer catalyzed annulation in wat
Autor:
Sebastian Rieth, David Askin, Barbara Müller, C. Gregory Sowell, Nadja Neubauer, Michael Jansen, Francis Gosselin, Nicholas Wong, Stefan G. Koenig, Stephan Bachmann, Xin Linghu, Nathaniel L. Segraves, Ifat Abramovich, Serena Fantasia
Publikováno v:
Chemistry (Weinheim an der Bergstrasse, Germany). 24(12)
A practical synthesis of the complex payload for an anti-Staphylococcus aureus THIOMABTM antibody-antibiotic conjugate (TAC) is described. The route takes advantage of a delicate oxidative condensation, achieved using a semi-continuous flow procedure
Autor:
Jing Wang, Nathaniel L. Segraves, S. Cyrus Khojasteh, Ryan H. Takahashi, Jae H. Chang, Shuguang Ma, Xiaojing Wang
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 45(10)
GDC-0339 is a novel small molecule pan-Pim kinase inhibitor that was discovered as a potential treatment for multiple myeloma. During the in vitro and in vivo metabolite profiling of GDC-0339, a metabolite was detected that had the same elemental com
Autor:
Jun Guo, Binqing Wei, Leanna Staben, Carl Ng, Shang-Fan Yu, Tao Wang, MaryAnn Go, Yanzhou Liu, Aimee Fourie-O'Donohue, Katherine R. Kozak, Xin Linghu, Nathaniel L. Segraves, Sophie M. Lehar, Richard Vandlen, Gail Lewis Phillips, John A. Flygare, Keyang Xu, Sanjeev Mariathasan, Stefan G. Koenig, Jinhua Chen, Thomas H. Pillow, Donglu Zhang, Josefa Chuh
Publikováno v:
Nature chemistry. 8(12)
The reversible attachment of a small-molecule drug to a carrier for targeted delivery can improve pharmacokinetics and the therapeutic index. Previous studies have reported the delivery of molecules that contain primary and secondary amines via an am
Publikováno v:
Magnetic Resonance in Chemistry. 50:256-259
During impurity analysis of maytansinol (2), produced from the reduction of ansamitocin P-3 (AP-3, 1), a surprisingly stable acyclic hemiacetal (4) was isolated. A combination of 1D and 2D NMR experiments, along with liquid chromatography-mass spectr
Autor:
Sebastian Rieth, Nadja Neubauer, Serena Fantasia, Barbara Müller, David Askin, Nicholas Wong, C. Gregory Sowell, Ifat Abramovich, Michael Jansen, Stephan Bachmann, Xin Linghu, Nathaniel L. Segraves, Francis Gosselin, Stefan G. Koenig
Publikováno v:
Chemistry - A European Journal. 24:2792-2792
Autor:
Nathaniel L. Segraves, Phillip Crews
Publikováno v:
Journal of Natural Products. 68:1484-1488
Chemical investigation of an NCI-DTP collection of Thorectandra sp. and a UCSC collection of Smenospongia sp. yielded six new brominated tryptophan derivatives: 6-bromo-1'-hydroxy-1',8-dihydroaplysinopsin (4), 6-bromo-1'-methoxy-1',8-dihydroaplysinop
Autor:
Phillip Crews, Nathaniel L. Segraves
Publikováno v:
Journal of Natural Products. 68:118-121
Three new C-alkylated iminosugars, batzellasides A (3), B (4), and C (5), along with the known halitoxin (2) polymer were isolated from a Batzella sp. sponge, collected off the west coast of Madagascar. Although this class of azasugars is well known
Autor:
Nathaniel L. Segraves, Frederick A. Valeriote, Halina Pietraszkiewicz, Sarah J. Robinson, Sadri A Said, Francis J. Schmitz, Xiong Fu, Phillip Crews, Daniel Garcia
Publikováno v:
Journal of Natural Products. 67:783-792
The fascaplysin class of compounds have been further investigated from six organisms consisting of four sponge collections (Fascaplysinopsis reticulata) and two tunicate collections (Didemnum sp.). This work is an extension of an earlier communicatio