Synthetic Approaches to the New Drugs Approved during 2019

Clinical Pharmacokinetics and Pharmacodynamics of Imipenem–Cilastatin/Relebactam Combination Therapy

(2020) Matthew W. McCarthy   CLINICAL PHARMACOKINETICS

Voxelotor: First Approval

(2020) Hannah A. Blair   DRUGS

Lumateperone: First Approval

(2020) Hannah A. Blair   DRUGS

Lemborexant: First Approval

(2020) Lesley J. Scott   DRUGS

Ubrogepant: First Approval

(2020) Lesley J. Scott   DRUGS

An overview of lefamulin for the treatment of community acquired bacterial pneumonia

(2020) Vicenç Falcó et al.   EXPERT OPINION ON PHARMACOTHERAPY

Current and future role of fedratinib in the treatment of myelofibrosis

(2020) Monica Ragheb et al.   Future Oncology

Characterization of Ubrogepant: A Potent and Selective Antagonist of the Human Calcitonin Gene‒Related Peptide Receptor*

(2020) Eric Moore et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

A phase 1, open-label, single-dose study of the pharmacokinetics of zanubrutinib in subjects with varying degrees of hepatic impairment

(2020) Ying C. Ou et al.   LEUKEMIA & LYMPHOMA

Cenobamate for focal seizures — a game changer?

(2020) Jacqueline A. French   Nature Reviews Neurology

Review of Synthetic Routes and Crystalline Forms of the Antiandrogen Oncology Drugs Enzalutamide, Apalutamide, and Darolutamide

(2020) David L. Hughes   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Imipenem‐Cilastatin‐Relebactam: A Novel β‐Lactam–β‐Lactamase Inhibitor Combination for the Treatment of Multidrug‐Resistant Gram‐Negative Infections

(2020) Jordan R. Smith et al.   PHARMACOTHERAPY

Cystic Fibrosis Transmembrane Conductance Regulator Modulator Therapy: A Review for the Otolaryngologist

(2020) Saangyoung E. Lee et al.   American Journal of Rhinology & Allergy

Design, synthesis, antitumor activity and theoretical calculation of novel PI3Ka inhibitors

(2020) Ru-Yi Jin et al.   BIOORGANIC CHEMISTRY

The COVID-19 and Cancer Consortium: A Collaborative Effort to Understand the Effects of COVID-19 on Patients with Cancer

(2020) Samuel M. Rubinstein et al.   CANCER CELL

Treatment of Patients with Relapsed or Refractory Mantle Cell Lymphoma With Zanubrutinib, a Selective Inhibitor of Bruton's Tyrosine Kinase

(2020) Yuqin Song et al.   CLINICAL CANCER RESEARCH

Safety and Efficacy of Ubrogepant for the Acute Treatment of Episodic Migraine: A Meta-Analysis of Randomized Clinical Trials

(2020) Yanbo Yang et al.   CNS DRUGS

Efficacy and Safety of Remogliflozin Etabonate, a New Sodium Glucose Co-Transporter-2 Inhibitor, in Patients with Type 2 Diabetes Mellitus: A 24-Week, Randomized, Double-Blind, Active-Controlled Trial

(2020) Mala Dharmalingam et al.   DRUGS

Trastuzumab Deruxtecan: First Approval

(2020) Susan J. Keam   DRUGS

Synthetic Approaches to New Drugs Approved during 2018

(2020) Andrew C. Flick et al.   JOURNAL OF MEDICINAL CHEMISTRY

Highly Enantioselective, Hydrogen-Bond-Donor Catalyzed Additions to Oxetanes

(2020) Daniel A. Strassfeld et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing

(2020) David E. Gordon et al.   NATURE

Cystic fibrosis 2019: Year in review

(2020) Iolo Doull   Paediatric Respiratory Reviews

Quizartinib, a selective FLT3 inhibitor, maintains antileukemic activity in preclinical models of RAS-mediated midostaurin-resistant acute myeloid leukemia cells

(2020) Tomoya Aikawa et al.   Oncotarget

New Drug Approvals for 2019: Synthesis and Clinical Applications

(2020) Shuo Yuan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Efficacy and Safety of Tofacitinib, Baricitinib, and Upadacitinib for Rheumatoid Arthritis: A Systematic Review and Meta-Analysis

(2020) Faping Wang et al.   MAYO CLINIC PROCEEDINGS

Process Development of Sotagliflozin, a Dual Inhibitor of Sodium–Glucose Cotransporter-1/2 for the Treatment of Diabetes

(2020) Matthew M. Zhao et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

In vitro activity of the new β-lactamase inhibitors relebactam and vaborbactam in combination with β-lactams against Mycobacterium abscessus complex clinical isolates

(2019) Amit Kaushik et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

The journey from gene knockout to clinical medicine: telotristat and sotagliflozin

(2019) Marc S. Rendell   Drug Design Development and Therapy

Randomized Phase 3 Evaluation of Trifarotene 50 μG/G Cream Treatment Of Moderate Facial And Truncal ACNE

(2019) Jerry Tan et al.   JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY

Esaxerenone: First Global Approval

(2019) Sean Duggan   DRUGS

Mirogabalin: First Global Approval

(2019) Emma D. Deeks   DRUGS

Cefiderocol: A Siderophore Cephalosporin with Activity Against Carbapenem-Resistant and Multidrug-Resistant Gram-Negative Bacilli

(2019) George G. Zhanel et al.   DRUGS

Efficacy and Safety of IV-to-Oral Lefamulin, a Pleuromutilin Antibiotic, for Treatment of Community-Acquired Bacterial Pneumonia: The Phase 3 LEAP 1 Trial

(2019) Thomas M File et al.   CLINICAL INFECTIOUS DISEASES

The Latest Research and Development into the Antibody–Drug Conjugate, [fam-] Trastuzumab Deruxtecan (DS-8201a), for HER2 Cancer Therapy

(2019) Takashi Nakada et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Sotagliflozin, the first dual SGLT inhibitor: current outlook and perspectives

(2019) Chiara Maria Assunta Cefalo et al.   Cardiovascular Diabetology

Peficitinib: First Global Approval

(2019) Anthony Markham et al.   DRUGS

Synthetic Approaches to the New Drugs Approved During 2017

(2019) Andrew C. Flick et al.   JOURNAL OF MEDICINAL CHEMISTRY

FLT3 inhibitor quizartinib (AC220)

(2019) Kiran Naqvi et al.   LEUKEMIA & LYMPHOMA

Efficacy and safety of peficitinib (ASP015K) in patients with rheumatoid arthritis and an inadequate response to conventional DMARDs: a randomised, double-blind, placebo-controlled phase III trial (RAJ3)

(2019) Yoshiya Tanaka et al.   ANNALS OF THE RHEUMATIC DISEASES

Efficacy and safety of peficitinib (ASP015K) in patients with rheumatoid arthritis and an inadequate response to methotrexate: results of a phase III randomised, double-blind, placebo-controlled trial (RAJ4) in Japan

(2019) Tsutomu Takeuchi et al.   ANNALS OF THE RHEUMATIC DISEASES

Evaluation and use of an anti‐cynomolgus monkey CD79b surrogate antibody‐drug conjugate to enable clinical development of polatuzumab vedotin

(2019) Dongwei Li et al.   BRITISH JOURNAL OF PHARMACOLOGY

Inhibitors of nuclear transport

(2019) David A Jans et al.   CURRENT OPINION IN CELL BIOLOGY

Alpelisib: First Global Approval

(2019) Anthony Markham   DRUGS

Entrectinib: First Global Approval

(2019) Zaina T. Al-Salama et al.   DRUGS

Remogliflozin Etabonate: First Global Approval

(2019) Anthony Markham   DRUGS

Effects of cenobamate (YKP3089), a newly developed anti-epileptic drug, on voltage-gated sodium channels in rat hippocampal CA3 neurons

(2019) Michiko Nakamura et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Efficacy and safety of lasmiditan in patients using concomitant migraine preventive medications: findings from SAMURAI and SPARTAN, two randomized phase 3 trials

(2019) Li Shen Loo et al.   JOURNAL OF HEADACHE AND PAIN

Pexidartinib versus placebo for advanced tenosynovial giant cell tumour (ENLIVEN): a randomised phase 3 trial

(2019) William D Tap et al.   LANCET

Solriamfetol for the treatment of excessive daytime sleepiness associated with narcolepsy

(2019) Junyi Yang et al.   Expert Review of Clinical Pharmacology

Fedratinib: First Approval

(2019) Hannah A. Blair   DRUGS

A translational pharmacokinetic/pharmacodynamic model to characterize bacterial kill in the presence of imipenem-relebactam

(2019) Pratik Bhagunde et al.   INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

(2019) Yunhang Guo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Advances in potential treatment options for myeloproliferative neoplasm associated myelofibrosis

(2019) Prithviraj Bose   Expert Opinion on Orphan Drugs

Comparative Efficacy and Safety of Peficitinib 25, 50, 100, and 150 mg in Patients with Active Rheumatoid Arthritis: A Bayesian Network Meta-Analysis of Randomized Controlled Trials

(2019) Young Ho Lee et al.   CLINICAL DRUG INVESTIGATION

Cefiderocol: Discovery, Chemistry, and In Vivo Profiles of a Novel Siderophore Cephalosporin

(2019) Takafumi Sato et al.   CLINICAL INFECTIOUS DISEASES

Pretomanid: First Approval

(2019) Susan J. Keam   DRUGS

Darolutamide: First Approval

(2019) Anthony Markham et al.   DRUGS

Pexidartinib: First Approval

(2019) Yvette N. Lamb   DRUGS

Sotagliflozin: A Review in Type 1 Diabetes

(2019) Emma D. Deeks   DRUGS

Elexacaftor/Ivacaftor/Tezacaftor: First Approval

(2019) Sheridan M. Hoy   DRUGS

Upadacitinib: First Approval

(2019) Sean Duggan et al.   DRUGS

Leave it to Lefamulin: A Pleuromutilin Treatment Option in Community-Acquired Bacterial Pneumonia

(2019) Young Ran Lee et al.   DRUGS

Trifarotene: First Approval

(2019) Lesley J. Scott   DRUGS

Lasmiditan: First Approval

(2019) Yvette N. Lamb   DRUGS

Tenapanor: First Approval

(2019) Anthony Markham   DRUGS

Aryl Hydrocarbon Receptor in Atopic Dermatitis and Psoriasis

(2019) Masutaka Furue et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Exportin 1 inhibition induces nerve growth factor receptor expression to inhibit the NF-kB pathway in preclinical models of pediatric high-grade glioma

(2019) John A. DeSisto et al.   MOLECULAR CANCER THERAPEUTICS

Elexacaftor–Tezacaftor–Ivacaftor for Cystic Fibrosis with a Single Phe508del Allele

(2019) Peter G. Middleton et al.   NEW ENGLAND JOURNAL OF MEDICINE

Patent Review of Synthetic Routes and Crystalline Forms of the CFTR-Modulator Drugs Ivacaftor, Lumacaftor, Tezacaftor, and Elexacaftor

(2019) David L. Hughes   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer’s disease model

(2019) Elizabeth Spangenberg et al.   Nature Communications

Selinexor (KTP-330) - a selective inhibitor of nuclear export (SINE): anti-tumor activity in diffuse large B-cell lymphoma (DLBCL)

(2019) Sharon Ben-Barouch et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Double-Blind Randomized Phase 3 Study Comparing Esaxerenone (CS-3150) and Eplerenone in Patients With Essential Hypertension (ESAX-HTN Study)

(2019) Sadayoshi Ito et al.   HYPERTENSION

Diastereoselective FeCl3·6H2O/NaBH4 Reduction of Oxime Ether for the Synthesis of β-Lactamase Inhibitor Relebactam

(2019) John Y. L. Chung et al.   JOURNAL OF ORGANIC CHEMISTRY

Safety and efficacy of adjunctive cenobamate (YKP3089) in patients with uncontrolled focal seizures: a multicentre, double-blind, randomised, placebo-controlled, dose-response trial

(2019) Gregory L Krauss et al.   LANCET NEUROLOGY

Entrectinib in ROS1 fusion-positive non-small-cell lung cancer: integrated analysis of three phase 1–2 trials

(2019) Alexander Drilon et al.   LANCET ONCOLOGY

Ubrogepant for the Treatment of Migraine

(2019) David W. Dodick et al.   NEW ENGLAND JOURNAL OF MEDICINE

Trastuzumab Deruxtecan in Previously Treated HER2-Positive Breast Cancer

(2019) Shanu Modi et al.   NEW ENGLAND JOURNAL OF MEDICINE

Analgesic mechanisms of gabapentinoids and effects in experimental pain models: a narrative review

(2018) M. Chincholkar   BRITISH JOURNAL OF ANAESTHESIA

Ion Channel Modulators in Cystic Fibrosis

(2018) Martina Gentzsch et al.   CHEST

Cefiderocol (S-649266), A new siderophore cephalosporin exhibiting potent activities against Pseudomonas aeruginosa and other gram-negative pathogens including multi-drug resistant bacteria: Structure activity relationship

(2018) Toshiaki Aoki et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A phase III study evaluating the efficacy and safety of remimazolam (CNS 7056) compared with placebo and midazolam in patients undergoing colonoscopy

(2018) Douglas K. Rex et al.   GASTROINTESTINAL ENDOSCOPY

Phosphatidylinositol 3-Kinase α–Selective Inhibition With Alpelisib (BYL719) in PIK3CA-Altered Solid Tumors: Results From the First-in-Human Study

(2018) Dejan Juric et al.   JOURNAL OF CLINICAL ONCOLOGY

Synthetic Approaches to New Drugs Approved During 2016

(2018) Andrew C. Flick et al.   JOURNAL OF MEDICINAL CHEMISTRY

Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances

(2018) Marian C. Bryan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Binding Characteristics and Analgesic Effects of Mirogabalin, a Novel Ligand for theα2δSubunit of Voltage-Gated Calcium Channels

(2018) Yuki Domon et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Targeted CGRP Small Molecule Antagonists for Acute Migraine Therapy

(2018) Philip R. Holland et al.   Neurotherapeutics

Lefamulin: Review of a promising novel pleuromutilin antibiotic

(2018) Michael P. Veve et al.   PHARMACOTHERAPY

The Orexin/Receptor System: Molecular Mechanism and Therapeutic Potential for Neurological Diseases

(2018) Chunmei Wang et al.   Frontiers in Molecular Neuroscience

Sickle cell disease

(2018) Gregory J. Kato et al.   Nature Reviews Disease Primers

In vitro activity of lascufloxacin, a novel fluoroquinolone antibacterial agent, against various clinical isolates of anaerobes and Streptococcus anginosus group

(2018) Yuka Yamagishi et al.   ANAEROBE

Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor

(2018) Hisao Hamaguchi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Insomnia in Elderly Patients: Recommendations for Pharmacological Management

(2018) Vivien C. Abad et al.   DRUGS & AGING

RDX5791, a First-in-Class Minimally Systemic NHE3 Inhibitor in Clinical Development for CIC and IBS-C, Increases Intestinal Sodium Leading to Enhanced Intestinal Fluid Volume and Transit

(2018) Andrew G. Spencer et al.   GASTROENTEROLOGY

Brexanolone injection in post-partum depression: two multicentre, double-blind, randomised, placebo-controlled, phase 3 trials

(2018) Samantha Meltzer-Brody et al.   LANCET

Advances in pharmaceutical treatment options for narcolepsy

(2018) Tatsunori Takahashi et al.   Expert Opinion on Orphan Drugs

Solriamfetol for the treatment of daytime sleepiness in obstructive sleep apnea

(2018) Vivien C. Abad et al.   Expert Review of Respiratory Medicine

Efficacy and safety of sotagliflozin in treating diabetes type 1

(2017) Marc S. Rendell   EXPERT OPINION ON PHARMACOTHERAPY

30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development

(2017) Peter Kolkhof et al.   JOURNAL OF ENDOCRINOLOGY

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1′-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor

(2017) Gabriel Martinez Botella et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthetic Approaches to the New Drugs Approved During 2015

(2017) Andrew C. Flick et al.   JOURNAL OF MEDICINAL CHEMISTRY

Brexanolone (SAGE-547 injection) in post-partum depression: a randomised controlled trial

(2017) Stephen Kanes et al.   LANCET

Targeting NTRK fusion in non-small cell lung cancer: rationale and clinical evidence

(2017) Biagio Ricciuti et al.   MEDICAL ONCOLOGY

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

(2017) Timothy P.S. Perera et al.   MOLECULAR CANCER THERAPEUTICS

Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin

(2017) Brian Metcalf et al.   ACS Medicinal Chemistry Letters

Synthetic approaches to the 2014 new drugs

(2016) Andrew C. Flick et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads

(2016) Takashi Nakada et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

GBT440 increases haemoglobin oxygen affinity, reduces sickling and prolongs RBC half-life in a murine model of sickle cell disease

(2016) Donna Oksenberg et al.   BRITISH JOURNAL OF HAEMATOLOGY

Entrectinib is a potent inhibitor of Trk-driven neuroblastomas in a xenograft mouse model

(2016) Radhika Iyer et al.   CANCER LETTERS

DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1

(2016) Y. Ogitani et al.   CLINICAL CANCER RESEARCH

Lumacaftor/Ivacaftor: A Review in Cystic Fibrosis

(2016) Emma D. Deeks   DRUGS

ITI-007 in the treatment of schizophrenia: from novel pharmacology to clinical outcomes

(2016) Robert E. Davis et al.   Expert Review of Neurotherapeutics

Use of a dose-response model to guide future clinical trial of benvitimod cream to treat mild and moderate psoriasis

(2016) Yan-Nan Zang et al.   INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS

Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor

(2016) Maria Menichincheri et al.   JOURNAL OF MEDICINAL CHEMISTRY

Comparative pharmacokinetics of three SGLT-2 inhibitors sergliflozin, remogliflozin and ertugliflozin: an overview

(2016) Ranjeet Prasad Dash et al.   XENOBIOTICA

ITI-007 in the treatment of schizophrenia: from novel pharmacology to clinical outcomes

(2016) Robert E. Davis et al.   Expert Review of Neurotherapeutics

Synthetic approaches to the 2013 new drugs

(2015) Hong X. Ding et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and Evaluation of 1H-Pyrrolo[2,3-b]pyridine Derivatives as Novel Immunomodulators Targeting Janus Kinase 3

(2015) Yutaka Nakajima et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Progress report on new antiepileptic drugs: A summary of the Twelfth Eilat Conference (EILAT XII)

(2015) Meir Bialer et al.   EPILEPSY RESEARCH

Pharmacological profile of CS-3150, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist

(2015) Kiyoshi Arai et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Remogliflozin etabonate: a novel SGLT2 inhibitor for treatment of diabetes mellitus

(2015) Nasser Mikhail   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome

(2015) Marta Zielińska et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Entrectinib: a potent new TRK, ROS1, and ALK inhibitor

(2015) Christian Rolfo et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist

(2015) Yu Yoshida et al.   JOURNAL OF MEDICINAL CHEMISTRY

Insomnia disorder

(2015) Charles M. Morin et al.   Nature Reviews Disease Primers

Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies

(2015) Anu-Maarit Moilanen et al.   Scientific Reports

Synthetic approaches to the 2012 new drugs

(2014) Hong X. Ding et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Mutational Analysis of PI3K/AKT Signaling Pathway in Tamoxifen Exemestane Adjuvant Multinational Pathology Study

(2014) Vicky S. Sabine et al.   JOURNAL OF CLINICAL ONCOLOGY

Design, Synthesis and Antimicrobial Evaluation of Novel Tricyclic Benzoxazine Fluoroquinolones under Conventional and Microwave Methods

(2014) B. Guruswamy et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Discovery of a Tetracyclic Quinoxaline Derivative as a Potent and Orally Active Multifunctional Drug Candidate for the Treatment of Neuropsychiatric and Neurological Disorders

(2014) Peng Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

N-Boc Deprotection and Isolation Method for Water-Soluble Zwitterionic Compounds

(2014) Zhijian Liu et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthetic approaches to the 2011 new drugs

(2013) Hong X. Ding et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation

(2013) Pascal Furet et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator

(2013) Shifeng Pan et al.   ACS Medicinal Chemistry Letters

Synthetic approaches to the 2010 new drugs

(2012) Kevin K.-C. Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of tricyclic cores for kinase inhibition

(2012) Stacy Van Epps et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Non-Systemic Drugs: A Critical Review

(2012) Dominique Charmot   CURRENT PHARMACEUTICAL DESIGN

Highly Selective Primary Alkoxycarboxylation and Esterification of Unprotected Pyranose Derivatives Mediated by Scandium(III) Triflate Catalysis

(2012) Michael S. McClure et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Comprehensive molecular portraits of human breast tumours

(2012) Daniel C. Koboldt et al.   NATURE

Large-Scale Carbonyl Reductions in the Pharmaceutical Industry

(2012) Javier Magano et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Orexin Receptors: Pharmacology and Therapeutic Opportunities

(2011) Thomas E. Scammell et al.   Annual Review of Pharmacology and Toxicology

Discovery of 1-{4-[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor

(2011) Kazuhiro Miwa et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Concise Synthesis of a β-Lactamase Inhibitor

(2011) Ian K. Mangion et al.   ORGANIC LETTERS

Enhancement of GABAergic Activity: Neuropharmacological Effects of Benzodiazepines and Therapeutic Use in Anesthesiology

(2011) T. I. Saari et al.   PHARMACOLOGICAL REVIEWS

Synthetic approaches to the 2009 new drugs

(2010) Kevin K.-C. Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A Concise and Convergent Synthesis of PA-824

(2010) Maurice A. Marsini et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthetic Approaches to the 2008 New Drugs

(2010) Kevin K.-C. Liu et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Synthesis, Crystal Structure, and Spectral Characterization of Flumatinib Mesylate

(2010) Gang Xu et al.   SYNTHETIC COMMUNICATIONS

Preparation of steroid sulfamates and their interaction with GABAA receptor

(2009) Vojtěch Kapras et al.   COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS

Identification ofN-(5-tert-Butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor

(2009) Qi Chao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Structure−Activity Studies of Biphenyl Analogues of the Tuberculosis Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

(2009) Brian D. Palmer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bacterial Biosynthesis of a Multipotent Stilbene

(2008) Susan A. Joyce et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Synthesis, Reduction Potentials, and Antitubercular Activity of Ring A/B Analogues of the Bioreductive Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

(2008) Andrew M. Thompson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthetic Approaches to the 2007 New Drugs

(2008) Kevin Liu et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

PA-824 Kills Nonreplicating Mycobacterium tuberculosis by Intracellular NO Release

(2008) R. Singh et al.   SCIENCE