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Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.

Principia Biopharma
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.

Chugai Pharmaceutical
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.

Chinese Academy of Sciences
2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors.

Chinese Academy of Sciences
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.

The First Affiliated Hospital of Zhengzhou University
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck
Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

Chugai Pharmaceutical
Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.

East China University of Science & Technology
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.

Southeast University
Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.

Experimental Therapeutics Centre
Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors.

Chinese Academy of Sciences (Cas)
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).

Icahn School of Medicine At Mount Sinai
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.

Sichuan University
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.

Hanyang University
Nintedanib: from discovery to the clinic.

Boehringer Ingelheim Pharma
Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs.

Health Science Center Xi'An Jiaotong University
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.

Zhejiang University
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.

Sichuan University
Irreversible protein kinase inhibitors: balancing the benefits and risks.

Covalution Pharma
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.

University of Genoa
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.

Abbott Laboratories
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.

Merck Research Laboratories
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.

Chinese Academy of Sciences
A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.

National Cancer Institute-Bethesda
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.

Harvard Medical School
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.

Amgen
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.

Targegen
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.

Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation.

Chugai Pharmaceutical
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.

Ludwig-Maximilians University of Munich
Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.

Boehringer Ingelheim Pharmaceuticals
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.

Hanyang University
Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Novartis Institute For Biomedical Research
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.

Chugai Pharmaceutical
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Ariad Pharmaceuticals
Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.

East China University of Science and Technology
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.

Chugai Pharmaceutical
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.

Boehringer Ingelheim Austria
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.

Curis
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.

Chugai Pharmaceutical
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.

Hanmi Research Center
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.

Center for Lymphoid Malignancies
The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.

ARIAD Pharmaceuticals, Inc.
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.

Tufts Medical Center
BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.

Bristol-Myers Squibb Company
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.

Eli Lilly and Company
Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model.

University of California Irvine (UCI)
The latest perspectives of small molecules FMS kinase inhibitors.

University of Sharjah
A review: FDA-approved fluorine-containing small molecules from 2015 to 2022.

Iran University of Medical Sciences
Design, synthesis, and biological evaluation of 1,6-naphthyridine-2-one derivatives as novel FGFR4 inhibitors for the treatment of colorectal cancer.

Wenzhou Medical University
Design, synthesis and biological evaluation of indazole derivatives as selective covalent inhibitors of FGFR4 in wild-type and gatekeeper mutants.

Sichuan University
CSF1R inhibitors are emerging immunotherapeutic drugs for cancer treatment.

Shenyang Pharmaceutical University
Recent advances in c-Met-based dual inhibitors in the treatment of cancers.

Liaoning University
Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.

Tyra Biosciences, Inc.
Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2V564F gatekeeper mutation based on a pan-FGFR inhibitor.

Sichuan University
Research progress of multi-target HDAC inhibitors blocking the BRD4-LIFR-JAK1-STAT3 signaling pathway in the treatment of cancer.

Jincheng People's Hospital
Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles.

Eberhard Karls University Tubingen
Identification of Piperazinyl-Difluoro-indene Derivatives Containing Pyridyl Groups as Potent FGFR Inhibitors against FGFR Mutant Tumor: Design, Synthesis, and Biological Evaluation.

Peking Union Medical College and Chinese Academy of Medical Sciences
Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations.

Kinnate Biopharma
Discovery of LHQ490 as a highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor.

East China Normal University
Discovery of 2,6-Naphthyridine Analogues as Selective FGFR4 Inhibitors for Hepatocellular Carcinoma.

Sungkyunkwan University
Design, synthesis, and biological evaluation of selective covalent inhibitors of FGFR4.

Central South University
Insight into the design of FGFR4 selective inhibitors in cancer therapy: Prospects and challenges.

Jingzhou Hospital Affiliated to Yangtze University
Discovery of N-(4-((6-(3,5- Dimethoxyphenyl)-9H-purine derivatives as irreversible covalent FGFR inhibitors.

Southeast University
The Hitchhiker's Guide to Deep Learning Driven Generative Chemistry.

Insilico Medicine Hong Kong
Medicinal chemistry approaches to target the MNK-eIF4E axis in cancer.

Northwestern University
Discovery and Structural Optimization of Novel Quinolone Derivatives as Potent Irreversible Pan-Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors.

Skyrun Pharma Co.
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.

China Pharmaceutical University
Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach.

Incyte
Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use.

Taiho Pharmaceutical
Structural Optimization of Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors.

Shanghai Institute of Materia Medica
4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.

Yangtze University
Recent advances of dual FGFR inhibitors as a novel therapy for cancer.

Southwest Jiaotong University
Discovery of 2-Amino-7-sulfonyl-7

China Pharmaceutical University
Targeting Gatekeeper Mutations for Kinase Drug Discovery.

Jinan University
Recent advance in the development of novel, selective and potent FGFR inhibitors.

China Pharmaceutical University
Development of selective FGFR1 degraders using a Rapid synthesis of proteolysis targeting Chimera (Rapid-TAC) platform.

University of Wisconsin-Madison
Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2-

Jinan University
Discovery of 1,6-Naphthyridin-2(1

Nanjing University of Chinese Medicine
Discovery of Novel 7-Azaindole Derivatives as Selective Covalent Fibroblast Growth Factor Receptor 4 Inhibitors for the Treatment of Hepatocellular Carcinoma.

Peking University
Novel Sphingosine Kinase 1 Inhibitor Suppresses Growth of Solid Tumor and Inhibits the Lung Metastasis of Triple-Negative Breast Cancer.

China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.

Jinan University
Design and Synthesis of Fibroblast Growth Factor Receptor (FGFR) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Cancer.

Sichuan University
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.

University of Arkansas For Medical Sciences
Identification of Pyridinyltriazine Derivatives as Potent panFGFR Inhibitors against Gatekeeper Mutants for Overcoming Drug Resistance.

Korea University
Kinase Inhibitors as Underexplored Antiviral Agents.

Complutense University of Madrid
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.

Johnson & Johnson Pharmaceutical Research and Development
Discovery of ASP5878: Synthesis and structure-activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity.

Astellas Pharma
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.

Chugai Pharmaceutical
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.

Central South University
Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.

Kirin Brewery
A small molecule-kinase interaction map for clinical kinase inhibitors.

Ambit Biosciences
Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors.

Jinan University
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.

Prelude Therapeutics
Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.

Central University of Punjab
Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3).

Celon Pharma
Characterization of an aromatic trifluoromethyl ketone as a new warhead for covalently reversible kinase inhibitor design.

Jinan University
Design, Synthesis, and Biological Evaluation of 2-Formyl Tetrahydronaphthyridine Urea Derivatives as New Selective Covalently Reversible FGFR4 Inhibitors.

Jinan University
From Fragment to Lead: De Novo Design and Development toward a Selective FGFR2 Inhibitor.

University of Leeds
Discovery and Optimization of a Novel 2

Nankai University
Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.

Chinese Academy of Sciences
Discovery, Synthesis, and Evaluation of Highly Selective Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) Inhibitor for the Potential Treatment of Metastatic Triple-Negative Breast Cancer.

West China Hospital of Sichuan University
Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors.

Sichuan University
Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.

Kirin Brewery
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-

The Genomics Institute of The Novartis Research Foundation
Design, synthesis and biological evaluation of quinazoline derivatives as potent and selective FGFR4 inhibitors.

Zhejiang University
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

Incyte
From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.

Sichuan University
Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer.

Wenzhou Medical University
Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma.

Bristol Myers Squibb
Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency.

Astellas Pharma
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.

Novartis Institutes For Biomedical Research
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.

Beijing Normal University
Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.

Jinan University
Targeting Cysteine Located Outside the Active Site: An Effective Strategy for Covalent ALKi Design.

West China Hospital of Sichuan University
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.

Merck Research Laboratories
Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2.

Astellas Pharma
Efficacy and Tolerability of Pyrazolo[1,5-

The Genomics Institute of The Novartis Research Foundation
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.

Merck And
Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors.

Shanghai Institute of Materia Medica
Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects.

Jinan University
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.

Chinese Academy of Sciences
Discovery of 4

TBA
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.

Sun Yat-Sen University
Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.

University of Naples Federico Ii
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.

Southeast University
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.

China Pharmaceutical University
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.

University of Florida
Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an

Chinese Academy of Sciences
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.

Takeda Pharmaceutical
Discovery and Development of a Series of Pyrazolo[3,4-

Shanghai University
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.

Novartis Institutes For Biomedical Research
Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors.

Chinese Academy of Sciences
Design and synthesis of potent RSK inhibitors.

Novartis Institutes For Biomedical Research
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.

Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Vertex Pharmaceuticals
Identification of an Indazole-Based Pharmacophore for the Inhibition of FGFR Kinases Using Fragment-Led

University of Leeds
Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors.

Fudan University
2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors.

Guangzhou Institutes of Biomedicine and Health
Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors.

Chinese Academy of Sciences
Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.

University of Chinese Academy of Sciences
TREATING CANCER WITH SMALL MOLECULES THAT INHIBIT ACSS-2

Drexel University
Factor XIa inhibitors

Merck Sharp & Dohme
2-hydroxycycloalkane-1-carbamoyl

Idorsia Pharmaceuticals
ISOINDOLINES AS PMS2 INHIBITORS

Neophore
INHIBITORS AND DEGRADERS OF PIP4K PROTEIN

Dana-Farber Cancer Institute
PYRIDINAMINE DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS

Xenon Pharmaceuticals
2-aminoaryl-5-aryloxazole analogs for the treatment of neurodegenerative diseases

Southern Research Institute
USE OF PRIDOPIDINE AND ANALOGS FOR TREATING RETT SYNDROME

Prilenia Neurotherapeutics
COMPOUNDS WITH SEMIOCHEMICAL PROPERTIES AND BIOSENSORS

Rothamsted Research
COMPOSITIONS AND METHODS FOR THE PREVENTION AND/OR TREATMENT OF MITOCHONDRIAL DISEASE, INCLUDING FRIEDREICH'S ATAXIA

Stealth Biotherapeutics
Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists

Hoffmann-La Roche
Polypeptide compound, pharmaceutical composition, preparation method and application thereof

Chengdu Sintanovo Biotechnology
Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof

Enanta Pharmaceuticals
Indole compounds and analogues thereof

Biocryst Pharmaceuticals
Quinazoline compounds, preparation method, use, and pharmaceutical composition thereof

Institute of Materia Medica, Chinese Academy of Medical Sciences
Indole and azaindole inhibitors of pad enzymes

Bristol-Myers Squibb
Alcoxyamino derivatives for treating pain and pain related conditions

Esteve Pharmaceuticals
Substituted penta-fused hexa-heterocyclic compounds, preparation method therefor, drug combination and use thereof

Xiamen University
Substituted [1,2,4]triazolo[4,3-A]pyrazines as prolyl endopeptidase inhibitors

Bayer Aktiengesellschaft
Tetrahydro-imidazo quinoline compositions as CBP/P300 inhibitors

Forma Therapeutics
4-pyrazin-2-ylmethyl-morpholine derivatives and the use thereof as medicament

Boehringer Ingelheim International
4-pyrimidin-5-ylmethyl-morpholine derivatives and the use thereof as medicament

Boehringer Ingelheim International
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto

Arena Pharmaceuticals
7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitors

Eli Lilly
Inhibitors of protease-activated receptor-2

Heptares Therapeutics
Quinoline and isoquinoline derivatives for treating pain and pain related conditions

Esteve Pharmaceuticals
3,4-bipyridyl pyrazole derivative, and preparation method therefor and medical application thereof

Jiangsu Hengrui Medicine
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors

Boehringer Ingelheim International
Imidazopyrazine inhibitors of Bruton's tyrosine kinase

Acerta Pharma
Substituted 2,4-diaminopyrimidines as kinase inhibitors

Celgene Car
Bicyclic compounds as dual ATX/CA inhibitors

Hoffmann-La Roche
2-aminoquinazoline derivatives as P70S6 kinase inhibitors

Sentinel Oncology
LXR agonists and uses thereof

Rgenix
Substituted pyrimidines for preventing or treating cancer and inflammatory diseases

Korea Research Institute of Chemical Technology
Epoxyketone compounds for enzyme inhibition

Centrax International
Tricyclic heterocycles as BET protein inhibitors

Incyte
Dopamine D3 receptor antagonists having a morpholine moiety

Indivior
Cot modulators and methods of use thereof

Gilead Sciences
4-azaindole compounds

Bristol-Myers Squibb
Cyclopropanamine compound and use thereof

Takeda Pharmaceutical
Thienomethylpiperazine derivatives as inhibitors of soluble epoxide hydrolase

Sanofi
Inhibitors of bruton's tyrosine kinase

F. Hoffmann-La Roche
4-oxo-3,4-dihydro-1,2,3-benzotriazine modulators of GPR139

Takeda Pharmaceutical
Thienopyrimidine compounds

Hoffmann-La Roche
Enhancer of zeste homolog 2 inhibitors

Glaxosmithkline
Acid ceramidase inhibitors and their use as medicaments

Fondazione Istituto Italiano Di Technologia
Method for the treatment of neurological disorders by enhancing the activity of β-glucocerebrosidase

Amicus Therapeutics
Substituted hetero-azepinones

F. Hoffmann-La Roche
Carbonic anhydrase inhibitors: in vitro inhibition of a isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids.

Ondokuz Mayis University
Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics

Galderma Research & Devlopment
In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II.

Balikesir University
Cyanomethylpyrazole carboxamides as janus kinase inhibitors

Merck Sharp & Dohme
The different inhibition mechanisms of OXA-1 and OXA-24 ß-lactamases are determined by the stability of active site carboxylated lysine.

Case Western Reserve University
Delineation of the Pasteurellaceae-specific GbpA-family of glutathione-binding proteins.

Ghent University
Small-Molecule Inhibitors of the SOX18 Transcription Factor.

The University of Queensland
Chimeric small molecules for the recruitment of antibodies to cancer cells

Yale University
Amino-pyrroline derivatives, and use thereof in the prevention and/or treatment of metabolic syndrome

Universite De Strasbourg
The SUMO1-E67 interacting loop peptide is an allosteric inhibitor of the dipeptidyl peptidases 8 and 9.

Georg-August-University of Goettingen
Azabenzimidazole hexahydrofuro[3,2-b]furan derivatives

Merck Sharp & Dohme
Substituted dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity

Boehringer Ingelheim International
Functional reversal of (-)-Stepholidine analogues by replacement of benzazepine substructure using the ring-expansion strategy.

Fudan University
Bicarbocyclic and tricarbocyclic ethynyl derivatives and uses of same

H. Lundbeck
4-piperidinyl compounds for use as tankyrase inhibitors

Novartis
Method for selectively inhibiting ACAT1 in the treatment of alzheimer's disease

Dartmouth College
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.

German Cancer Research Center (Dkfz)
2-heteroaryl carboxamides

Bayer Intellectual Property
Cyclohexyl-azetidinyl antagonists of CCR2

Janssen Pharmaceutica
Method for enhancing anti-tumor effect of a microtubule-targeting drug, and a method for treatment of tumor

Taiho Pharmaceutical
Sulfonamide compounds useful as CYP17 inhibitors

Bristol-Myers Squibb
1′-substituted pyrimidine N-nucleoside analogs for antiviral treatment

Gilead Sciences
Substituted spiro[cycloalkyl-1,3′-indo]-2′(1′H)-one derivatives and their use as P38 mitogen-activated kinase inhibitors

Almirall
26- and 27-Methyl groups of 2-substituted, 19-nor-1a,25-dihydroxylated vitamin D compounds are essential for calcium mobilization in vivo.

University of Wisconsin-Madison
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.

Roche Bioscience
Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.

Amgen
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.

Upjohn