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This industry update covers the period from January 1 through January 31, 2022, and is based on information sourced from company press releases, scientific literature, patents and news websites. January 2022 saw Janssen and Midatech expand their collaboration on bioresorbable polymer microsphere technology for drug delivery. Takeda announced its plans to acquire UK-based Adaptate Biotherapeutics and Gandeeva raised further investment funds to support its drug discovery and development platform focused on the evaluation of protein–drug interactions. Biogen announced that it will sell its stake in a biosimilars joint venture and ABL Bio and Sanofi announced a collaboration around a novel treatment for Parkinson's disease. New regulatory announcements this month included US FDA approvals of a new insomnia treatment for Idorsia and a treatment for atopic dermatitis developed by Pfizer. Insulet gained FDA clearance for a closed-loop insulin pump and Ascendis Pharma followed up its United States approval last year for a once-weekly treatment for growth hormone deficiency with European approval. Pfizer and Ionis announced the discontinuation of the clinical development of a novel cardiovascular drug. In terms of collaborations, Novartis and Alnylam announced they will work together to explore targeted therapies to restore liver function; Scorpion Therapeutics partnered with AstraZeneca to develop novel cancer treatments and Nutriband Inc. and Kindeva Drug Delivery will work together to develop a transdermal fentanyl patch. Collaborations were also announced between Century Therapeutics and Bristol Myers Squibb and Lilly and Entos Pharmaceuticals in the areas of stem cell therapies for cancer treatment and neurology, respectively. A team from the Massachusetts Institute of Technology reported progress in developing oral mRNA treatments and West Pharmaceutical Services published a blog describing the development of a proof-of-principle system for a closed-loop feedback system targeting opioid overdose. A report on the BBC website highlighted the benefits of more sustainable inhalers.

This Industry Update covers the period from 1 to 31 January 2019 and is based on information sourced from company press releases, scientific literature, patents and various news websites. Bristol-Myers Squibb (NY, USA) and Celgene (NJ, USA) announced a merger to create one of the largest oncology-focused pharmaceutical businesses. Also, with a focus on oncology, Lilly (IN, USA) announced it is acquiring Loxo Oncology (CT, USA). Alphabet’s life sciences business, Verily (CA, USA), announced it had raised new funds to invest in new business opportunities and acquisitions. Talee Bio (PA, USA) and Agenus (MA, USA) announced that they had won grants to support their work in cystic fibrosis and vaccine development, respectively. Biogen (MA, USA) established two new collaborations aimed at expanding its neuroscience pipeline and Voyager Therapeutics (MA, USA) and Neurocrine Biosciences (CA, USA) agreed a collaboration to develop and commercialize gene therapy treatments also in neuroscience. In digital health, Proteus Digital Health (CA, USA) continued the development of digital pill technology, with the initiation of a study in oncology and Otsuka (Tokyo, Japan) agreed a collaboration with Click Therapeutics (NY, USA) to develop digital therapies to treat major depressive disorder. This month also finally saw the approval of Mylan’s (PA, USA) generic version of GSK’s (Brentford, UK) blockbuster inhaled drug, ADVAIR. Several developments in novel drug delivery methods were reported including the use of microneedles to deliver contraceptives, inhaled delivery of mRNA and a study supporting the use of peptoids to deliver gene therapies into cells. A publication from the Salk Institute (CA, USA) suggested a cellular mechanism might be important in reducing the risk of cancer, and a study by a team at Washington University (MO, USA) supported the possibility of gene therapy to treat neuropathy.

This industry update covers the period from 1 to 31 October 2018 and is based on information sourced from company press releases, scientific literature, patents and various news websites. With the ...

This industry update covers the period from 1 September through 30 September 2017, and is based on information sourced from company press releases, scientific literature, patents and various news websites. The month saw the US FDA approve three new molecular entities, Aliqopa (copanlisib dihydrochloride) (Bayer Healthcare); Solosec (secnidazole) (Symbiomix Therapeutics) and Verzenio (abemaciclib) (Eli Lilly and Co). Intarcia Therapeutics Inc. has its application for approval of a novel drug device combination of exenatide for the treatment of diabetes rejected by FDA but said that it will work to address the concerns and refile the application. The impact of biosimilars in the market is steadily increasing with seven biosimilars approved in the USA and Sandoz hoping to add to this with its announcement that FDA has accepted its Biologics License Application for a biosimilar version of Roche's Rituxan. Circassia announced positive top line results of a respiratory drug, Duaklir (for the treatment of chronic obstructive pulmonary disease) and Sarepta (for its new treatment for Duchenne muscular dystrophy). Axovant Sciences Ltd announced the failure if its drug Intepirdine in the treatment of Alzheimer's, adding to a growing list of drug failures in this area. There were a number of developments in the area of oncology with Bristol-Myers Squibb and Infinity Pharmaceuticals announcing an expansion of their collaboration looking at combination treatments, as well as Eli Lilly and Co's approval for Verzenio. Rani Therapeutics and Intra-Cellular Therapies announced successful funding rounds to support their drug programs. Allergan announced a novel licensing deal for its dry eye drug, Restasis, which it hopes would allow it to stave off patent challenges from several companies looking to develop generic versions of the drug. New research suggests that loss of sense of smell can be linked to an increased risk of developing Parkinson's disease.

This industry update covers the period from 1 to 31 October 2018 and is based on information sourced from company press releases, scientific literature, patents and various news websites. With the expiry in Europe of AbbVie's (IL, USA) principal patent on Humira this month, the first biosimilar versions of the drug have been launched. AstraZeneca (Cambridge, UK) announced that is has out-licensed two none core drugs to Grunenthal (Aachen, German), while Pfizer (NY, USA) announced the creation of a new company, set up in collaboration with Bain Capital (MA, USA) to exploit Pfizer's clinical and preclinical assets in the neuroscience field. In digital health, 23andMe (CA, USA) announced that the US FDA has authorized marketing of one of its consumer genetic tests, that assesses the genetic factors that affect drug metabolization, hence the safety and efficacy of some drugs. Novartis (Basel, Switzerland) continued to grow its activities in digital health with the creation of the Novartis Biome, an incubator and support program for early-stage companies in this area. Novartis also announced that it has filed applications in the EU and USA for the approval of siponimod, a drug targeting secondary progressive multiple sclerosis and Roche (Basel, Switzerland) gained FDA approval for an antiviral treatment for influenza. Janssen (Beerse, Belgium) announced it had won a label extension for its blood glucose-lowering drug, Invokana®, for the reduction of cardiovascular events in diabetes. Roche presented data at ECTRIMS, a major annual conference on multiple sclerosis (MS), held in Berlin, Germany this month (10–12 October 2018), showing the potential benefits of administering its drug, Ocrevus, earlier in the treatment pathway for MS compared with other standard treatment. At the same event, Celgene (NJ, USA) presented results from a survey that showed MS patients’ concern around brain atrophy and cognitive loss in MS, highlighting that the disease has a neurodegenerative as well as an inflammatory component. Novartis also presented a significant amount of data supporting its marketed drugs as well as its development pipeline in the disease. This month, presentation of data from two studies at the American Academy of Ophthalmology annual meeting (27–30 October 2018, Chicago, IL, USA) further supporting the potential of eye scans in the early detection of Alzheimer's. A paper by a research team at the University of Rochester (NY, USA) demonstrated the feasibility of a new mechanism to transport drugs across the blood–brain barrier, which could help development more effective CNS drugs.

Spleen tyrosine kinase (SYK) is a non-receptor cytosolic kinase. Due to its pivotal role in B cell receptor and Fc-receptor signaling, inhibition of SYK has been targeted in a variety of disease areas. Herein, we report the optimization of a series of potent and selective SYK inhibitors, focusing on improving metabolic stability, pharmacokinetics and hERG inhibition. As a result, we identified 30, which exhibited no hERG activity but unfortunately was poorly absorbed in rats and mice. We also identified a SYK chemical probe, 17, which exhibits excellent potency at SYK, and an adequate rodent PK profile to support in vivo efficacy/PD studies.

Spleen Tyrosine Kinase (SYK) is a well-studied enzyme with therapeutic applications in oncology and autoimmune diseases. We identified an azabenzimidazole (ABI) series of SYK inhibitors by mining activity data of 86,000 compounds from legacy biochemical assays with SYK and other homologous kinases as target enzymes. A structure-based design and hybridization approach was then used to improve the potency and kinase selectivity of the hits. Lead compound 23 from this novel ABI series has a SYK IC50 = 0.21 nM in a biochemical assay and inhibits growth of SUDHL-4 cells at a GI50 = 210 nM.

This Industry Update covers the period 1–31 March 2014 and is based on information sourced from company press releases, scientific literature, patents and various news websites. This month saw some significant commercial activity with Baxter (IL, USA) announcing a split, Corium an initial public offering and Vectura a major acquisition, which both expands its development pipeline and also gives it access to another inhalation device platform. A number of technologies are under development that enable the transfer of drugs across the blood–brain barrier and MedImmune (MD, USA) continued its interest in the area by announcing a new deal with BiOasis (Vancouver, Canada). In another drug-delivery deal, Caisson (TX, USA) announced an expansion of its HEPtune collaboration with Novo Nordisk (Bagsværd, Denmark). Clinical progress was reported by Arrowhead Research Corporation for its RNAi therapeutic for the treatment of chronic hepatitis, which began a Phase IIa study, and Ocular Therapeutix (MA, USA) embarked on its Phase III clinical program to evaluate the safety and efficacy of its dexamethasone formulation. In the regulatory arena, the US FDA approved oral treatment from Celegene (NJ, USA) for psoriatic arthritis and Avanir (CA, USA) announced the FDA has accepted its new drug application for a nasally delivered sumatriptan for the treatment of migraine. A paper in Nature described an 'on-skin' system that can monitor patients, deliver drugs and communicate data. A paper published by a group form University of Illinois (IL, USA) described a biodegradable battery that could be used to power implanted devices used to deliver drugs.

This Industry Update covers the period from 1 through 30 April 2017, and is based on information sourced from company press releases, scientific literature, patents and various news websites. Biogen expanded its portfolio of developmental drugs targeting neurological diseases by licensing a drug from Bristol-Myers Squibb which is currently under investigation for the treatment of progressive supranuclear palsy. Takeda announced a deal with NuBiyota focused on developing treatments for gastrointestinal disorders, based on the manipulation of microbes living in the gut. Novartis announced an expansion of its neuroscience collaboration with Amgen as well as licensing of a developmental compound to treat dry eye. EmulateBio announced a collaboration with the US FDA to explore and evaluate its organs-on-chip technology in toxicological testing of food products, but which has wider opportunities in drug development. In the treatment of pulmonary hypertension, Vectura announced the commercial launch of its Fox nebulizer technology to deliver a Bayer drug and Respira announced a deal in which it exclusively licensed an inhaled drug-device product to United Therapeutics. Published research suggested that the benefit of pumps over multiple injections in the treatment of diabetes maybe more due to training than technology, and a group from the University of Pennsylvania showed that electrical stimulation of the brain can improve memory function but only when applied at the right time. Alzheon published work that explains the mechanism behind its developmental Alzheimer's drug.

This Industry Update covers the period from 1–31 December 2013 and is based on information sourced from company press releases, scientific literature, patents and various news websites. In the parenteral area there was news about the development of pump technology for noninsulin applications, which provides evidence for the growth in demand for large volume subcutaneous drug delivery, a need that cannot be met using conventional injection technology. There was also considerable activity in the respiratory area with announcements on genetic competition to GlaxoSmithKline (London, UK) Advair/Seretide, a global top five selling drug as well as some news on the development and launch new respiratory drugs. The largest mergers and acquisitions deal was the much anticipated buyout of Bristol-Myers Squibb (NY, USA) by AstraZeneca (London, UK) from their diabetes joint venture and the second US $1 billion plus deal for AstraZeneca in 2013 as they strive to rebuild a late stage pipeline to offset the generic threat to their revenues over the next few years.

We disclose a novel series of insulin-like growth factor-1 receptor kinase inhibitors based on the 3-(pyrimidin-4-yl)-imidazo[1,2-a]pyridine scaffold. The influence on the inhibitory activity of substitution on the imidazopyridine and at the C5 position of the pyrimidine is discussed. In the course of this optimization, we discovered a potent and selective inhibitor with suitable pharmacokinetics for oral administration.

A series of carboxylic acid glycogen phosphorylase inhibitors, which have potential as oral antidiabetic agents, is described. Defining and applying simple physicochemical design criteria was used to assess the opportunity and to focus synthetic efforts on compounds with the greatest probability of success. The study led to compound 17, which exhibits a good balance of properties including potent inhibition of recombinant human liver glycogen phosphorylase in vitro, a good DMPK profile including excellent bioavailability and low clearance and good in vivo activity in a glucagon challenge model of diabetes in Zucker rats.

Following the discovery of imidazopyridine 1 as a potent IGF-1R tyrosine kinase inhibitor, the aniline part has been modified with the aim to optimize the properties of this series. The structure–activity relationships against IGF-1R kinase activity as well as inhibition of the hERG ion channel are discussed.

Matched molecular pair analysis has been used in design of inhibitors of glycogen phosphorylase.