- ANTI-HUMAN VISTA ANTIBODIES AND USE THEREOF
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The invention provides anti-VISTA antibody drug conjugates which may be used for targeted delivery of anti-inflammatory agents such as steroids to immune cells, e.g., myeloid cells. The invention also provides methods of using anti-VISTA antibody drug conjugates in the treatment of inflammatory and/or autoimmune conditions and/or for alleviating the toxicity of anti-inflammatory agents such as steroids.
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Paragraph 442; 579
(2021/10/30)
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- GLUCOCORTICOID RECEPTOR AGONIST AND IMMUNOCONJUGATES THEREOF
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Provided herein are glucocorticoid receptor agonist immunoconjugates, glucocorticoid receptor agonists, and methods of using the same.
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Paragraph 0141
(2019/06/14)
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- ANTI-CD40 ANTIBODY DRUG CONJUGATES
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Provided herein are anti-CD40 antibody drug conjugates comprising a radical of Formula (I), wherein R1, R2, and R3 are as defined herein. Further provided are anti-CD40 antibody drug conjugates of Formula (II), wherein Z, R, AA1, AA2, AA3, m, p, q, n, w, R1, R2, and R3 are as defined herein. Further provided are pharmaceutical compositions and kits thereof, and methods of using same.
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Paragraph 00143
(2019/06/17)
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- GLUCOCORTICOID RECEPTOR AGONIST AND IMMUNOCONJUGATES THEREOF
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Provided herein are glucocorticoid receptor agonist immunoconjugates, glucocorticoid receptor agonists, and methods of using the same, e.g., to treat autoimmune or inflammatory diseases.
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Page/Page column 00974; 00975
(2018/01/17)
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- Kilogram-scale synthesis of an inhaled corticosteroid
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The development and implementation of a safe and scalable process for the manufacture of corticosteroid PF-4714224 (1) is described. Initial routes used to synthesise analogues from this series directly from fluocinolone acetonide (2) were unsuitable for large-scale use. Key aspects of the route are the efficient and simple method for the preparation of the steroid tetraol (6), acetal formation by reaction of the tetraol with a bisulphite adduct (12), and isolation of the product by sequential recrystallisations.
- Knight, Craig J.,Millan, David S.,Moses, Ian B.,Robin, Aurelie A.,Selby, Matthew D.
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experimental part
p. 697 - 703
(2012/08/07)
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- Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma
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In this Letter we present data for a novel series of ICS for the treatment of asthma. 'Inhalation by design' principles have been applied to a series of highly potent steroidal GR agonists, with a focus on optimising the potential therapeutic index in human. Pharmacokinetic properties were tuned with high intrinsic clearance and low oral bioavailability in mind, to minimise systemic exposure and reduce systemically driven adverse events. High CYP mediated clearance as well as glucuronidation were targeted to achieve high intrinsic clearance coupled with multiple routes of clearance to minimise drug-drug interactions. Furthermore, pharmaceutical properties such as stability, crystallinity and solubility were considered to ensure compatibility with a dry powder inhaler. This work culminated in the identification of the clinical candidate 15, which demonstrates preclinically the desired efficacy and safety profiles confirming its potential as an inhaled agent for the treatment of asthma.
- Millan, David S.,Ballard, Stephen A.,Chunn, Sara,Dybowski, Joseph A.,Fulton, Craig K.,Glossop, Paul A.,Guillabert, Edouard,Hewson, Christopher A.,Jones, Rhys M.,Lamb, David J.,Napier, Carolyn M.,Payne-Cook, Toby A.,Renery, Emmanuelle R.,Selby, Matthew D.,Tutt, Michelle F.,Yeadon, Michael
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scheme or table
p. 5826 - 5830
(2011/10/18)
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- NOVEL GLUCOCORTICOID RECEPTOR AGONISTS
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This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
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Page/Page column 32-33
(2009/07/03)
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- Mucosal adhesive device for long-acting delivery of pharmaceutical combinations in oral cavity
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Mucosal adhesive devices are provided for use in the oral cavity for therapy against infections. The devices are dosage units which comprise a combination of antimicrobial agents such as antifungal agents and anti-inflammatory agents, optionally also a local anesthetic. The dosage units yield a gradual and relatively constant release of the pharmaceuticals over at least a 12-hour period.
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