Publications
睿智医药是一家以科学为基础，以技术为导向的全球型CRO+CDMO企业。
Approach to Rational Identification of Lead Molecular Glue Degraders for Casein Kinase 1a
EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry, 2023, September, Zagreb
Rapid Discovery of CD28-specific Antibodies from Rabbits Through Single B cell Cloning on the Beacon® Platform
Antibody Engineering and Therapeutics, 2023, June, Amsterdam
Characterization of 405B8H3(D‐E), a newly engineered high affinity chimeric LAG‐3 antibody with potent antitumor activity
FEBS open bio vol. 13,7 (2023): 1253-1265
Discovery and Optimization of the First Highly Effective and Orally Available Galectin-3 Inhibitors for Treatment of Fibrotic Disease
J. Med. Chem. 2022, 65, 19, 12626–12638
Accelerated Discovery of Unique Anti-PD-L1 Antibodies from Spleen Versus Bone Marrow of Immunized Mice by Single Plasma B Cell Cloning on the Beacon® Platform
Antibody Engineering and Therapeutics, 2019, Amsterdam
Accelerated Discovery of Unique Anti-PD-L1 Antibodies from Spleen Versus Bone Marrow of Immunized Mice by Single Plasma B cell Cloning on the Beacon® Platform
Antibody Engineering and Therapeutics, 2018, Dec., Amsterdam
Identification of GNE-131: A potent and selective hNaV1.7 inhibitor for the treatment of pain
National Medicinal Chemistry Symposium, 2016, Jun. 26-29, Chicago
From Ergolines to Indoles: Improved Inhibitors of the Human H3 Receptor for the Treatment of Narcolepsy
ChemMedChem. 2015 Feb;10(2):266-75.
Neuroactive Steroids.1.Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders
J. Med. Chem., 2015, 58 (23), 9154–9170
Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety
ACS Med. Chem. Lett., 2015, 6 (12), 1241–1246.
SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF
WO/2015/078374
Discovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide
Bioorganic & Medicinal Chemistry Letters 25 (2015) 5589–5593
Neuroactive Steroids.1.Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21
J. Med. Chem. 2015, 58, 3500-3511.
Virtual screening and biological evaluation of novel small molecular inhibitors against protein arginine methyltransferase 1 (PRMT1)
Org. Biomol. Chem., 2014, 12, 9665–9673
Identifying Novel Selective Non-Nucleoside DNA Methyltransferase 1 Inhibitors through Docking-Based Virtual Screening
J. Med. Chem. 2014, 57, 9028−9041
Steric and Electronic Factors Influence Regio-isomeric Thiazole Formations Between Substituted Benzothioamides and Ethyl Bromopyruvate
J. Heterocyclic. Chem. 2014, 51, 1137−1146
Novel synthesis of isoxazoline indolizine amides for potential application to tropical diseases
Tetrahedron Letters, Volume 55, 2014, Pages 1936–1938
Establishment and Characterization of 7 Novel Hepatocellular Carcinoma Cell Lines from Patient-Derived Tumor Xenografts
Plos One. 9(1): e85308
Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation
Science,2013, 340(6132),622-6
人源性食管癌移植瘤模型的建立、评价及其应用的初步研究
实验动物与比较医学: 33(1)
Vortioxetine disinhibits pyramidal cell function and enhances synaptic plasticity in the rat hippocampus.
J Psychopharmacol. 2014 Oct;28(10):891-902.
食管癌动物模型的建立
上海师范大学学报(自然科学版). 42(4): 398-404
Small Molecule Activation of PKM2 in Cancer Cells Induces Serine Auxotrophy
Chem. Biol. 2012, 19(9), 1187-98
HZ08 reverse the aneuploidy-induced cisplatin-resistance in Gastric cancer by modulating the p53 pathway.
European Journal of Pharmacology. 720(1-3): 84-97
Identification of NME5 as a contributor to innate resistance to gemcitabine in pancreatic cancer cells.
FEBS J. 279(7): 1261-73
Transactivation of the human NME5 gene by Sp1 in pancreatic cancer cells.
Gene. 503(2): 200-7
Intrinsic gemcitabine resistance in a novel pancreatic cancer cell line is associated with cancer stem cell-like phenotype.
Int J Oncol. 40 (3): 798-806
INHIBITORS OF AKT ACTIVITY
WO/2011/130921
Differential Aspartate Usage Identifies a Subset of Cancer Cells Particularly
Cell Reports 17, 876–890, October 11, 2016
Full-length human glutaminase in complex with an allosteric inhibitor
Biochem. 2011, 50(50), 10764 -70
AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency
Blood. 2017 Sep 14;130(11):1347-1356.
AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations
Cancer Discov. 2017 May;7(5):478-493.
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions
ACS Med Chem Lett. 2017 Nov 28;8(12):1224-1229.
A small molecule activator of Nav1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo
European Journal of Neuroscience, Vol. 46, pp. 1887–1896, 2017
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers
ACS Med Chem Lett. 2018 Jan 19;9(4):300-305.
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma
Cancer Res. 2017 Dec 15;77(24):6999-7013.
Precision Targeted Therapy with BLU-667 for RET -Driven Cancers
“Cancer Discovery (July 1 2018 8 (7) 836-849; DOI:10.1158/2159-8290.CD-18-0338)”
First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway
Cancer Discov. 2015 Apr;5(4):424-37.
EZH2 inhibition by tazemetostat results in altered dependency on B-cell activation signaling in DLBCL
AACR August 23, 2017; DOI: 10.1158/1535-7163.MCT-16-0840
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma
SCIEntIfIC Reports | (2017) 7:17993 | DOI:10.1038/s41598-017-18446-z
“Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2”
PNAS | May 7, 2013 | vol. 110 | no. 19 | 7923
“Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas”
PLOS ONE| DOI:10.1371/journal.pone.0111840 December 10, 2014
Patent Application Publication
US 2016/0303135 A1
Selective Killing of SMARCA2- and SMARCA4- deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models
AACR Mol Cancer Ther; 16(5) May 2017
Pyrimidine hydroxyl amide compounds as protein deacetylase inhibitors and methods of use thereof.
WO2011307115
Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo
ACS Med. Chem. Lett. 3, 10, 850-855
“Discovery of A‑971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders”
J. Med. Chem. 2015, 58, 9154-9170
一类黄酮衍生物及其制备方法和用途
CN1172946
一种6-甲氧基水杨醛的制备方法
CN101768065A
ANALOGS OF CELASTROL
WO2017070615A1
一种螺环丙基甲酰衍生物的中间体化合物的制备方法
CN102557941B
一种米诺环素的制备方法及其中间体
CN103387512B
一类磺内酰胺类化合物及其制备方法和中间体
CN102115466B
一种3-氯-5,6,7,8-四氢异喹啉的制备方法
201810781489.9
一种4-溴甲基-2-三甲基硅乙炔苯基-1-磺酰氟的制备方法
201810781490.1
一种山环素的制备方法
CN103387511B
一种5-氨甲基-哌啶-2-酮的制备方法
201810785216.1
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions
ACS Med. Chem. Lett. 2017, 8, 1224-1229
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