Browsing ICR Divisions by author "Newton, Gary"
Now showing items 1-17 of 17
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(2-carboxamido)(3-amino)thiophene compounds
Newton, G; Wynne, G; Keily, J; Smyth, D; Crew, A (2005-09-27)Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is R2 is and R3 is C 0-4 alkyl, are useful in the treatment of cancer. -
5-(PYRIMIDIN-4-YL)-2-(PYRROLIDIN-1-YL)NICOTINONITRILE COMPOUNDS AS IKKE, TBK1 AND/OR SIK2 KINASES INHIBITORS
Newton, G; Stewart, M (2018-08-30)The invention provides compounds of formula (I) wherein R is −CH3 or −CH2CH3 and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of diseases or disorders mediated by IKKE, ... -
ALDEHYDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN AND THEIR USE
Newton, G; Robinson, C; Jenkins, K; Kimberley, M; Garrod, D; et al. (2012-01-12)The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aldehyde compounds of the following formula (A) (for convenience, collectively referred to herein as "ALD ... -
Allergen Delivery Inhibitors: A Rationale for Targeting Sentinel Innate Immune Signaling of Group 1 House Dust Mite Allergens through Structure-Based Protease Inhibitor Design.
Zhang, J; Chen, J; Newton, GK; Perrior, TR; Robinson, C (AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS, 2018-09-01)Diverse evidence from epidemiologic surveys and investigations into the molecular basis of allergenicity have revealed that a small cadre of "initiator" allergens promote the development of allergic diseases, such as asthma, ... -
Allergen Delivery Inhibitors: Characterisation of Potent and Selective Inhibitors of Der p 1 and Their Attenuation of Airway Responses to House Dust Mite Allergens.
Zhang, J; Chen, J; Zuo, J; Newton, GK; Stewart, MR; et al. (MDPI, 2018-10-15)Group 1 allergens of house dust mites (HDM) are globally significant triggers of allergic disease. They are considered as initiator allergens because their protease activity enables the development of allergy to a spectrum ... -
COMPOUNDS AND THEIR USES
Newton, G; Lord, C; Ashworth, A; Perrior, T (2013-02-21)The invention provides a compound that is an inhibitor of one or both of TBK1 and IKKe, or a down-regulator of the expression of one or both of TBK1 and IKKe, for use in a method of treating a cancer that is dependent on ... -
Determination of Ligand-Binding Affinity (Kd) Using Transverse Relaxation Rate (R2) in the Ligand-Observed 1H NMR Experiment and Applications to Fragment-Based Drug Discovery.
Liu, M; Mirza, A; McAndrew, PC; Thapaliya, A; Pierrat, OA; et al. (AMER CHEMICAL SOC, 2023-08-10)High hit rates from initial ligand-observed NMR screening can make it challenging to prioritize which hits to follow up, especially in cases where there are no available crystal structures of these hits bound to the target ... -
Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1.
Wilding, B; Pasqua, AE; E A Chessum, N; Pierrat, OA; Hahner, T; et al. (PERGAMON-ELSEVIER SCIENCE LTD, 2021-06-15)ERAP1 is a zinc-dependent M1-aminopeptidase that trims lipophilic amino acids from the N-terminus of peptides. Owing to its importance in the processing of antigens and regulation of the adaptive immune response, dysregulation ... -
MAP4K4 Inhibition Promotes Survival of Human Stem Cell-Derived Cardiomyocytes and Reduces Infarct Size In Vivo.
Fiedler, LR; Chapman, K; Xie, M; Maifoshie, E; Jenkins, M; et al. (CELL PRESS, 2019-04-04)Heart disease is a paramount cause of global death and disability. Although cardiomyocyte death plays a causal role and its suppression would be logical, no clinical counter-measures target the responsible intracellular ... -
MAP4K4 Inhibitors
Newton, G; Schneider, M; Chapman, K; Aqil, R; Jarvis, A (2020-06-11)This invention relates to compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these compounds, for example in a method ... -
MAP4K4 Inhibitors
Newton, G; Schneider, M; Chapman, K; Perrior, T; Aqil, R; et al. (2019-04-18)This invention relates to pyrrolopyrimidine comprising compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these ... -
Preclinical trial of a MAP4K4 inhibitor to reduce infarct size in the pig: does cardioprotection in human stem cell-derived myocytes predict success in large mammals?
Te Lintel Hekkert, M; Newton, G; Chapman, K; Aqil, R; Downham, R; et al. (SPRINGER HEIDELBERG, 2021-05-20)Reducing infarct size (IS) by interfering with mechanisms for cardiomyocyte death remains an elusive goal. DMX-5804, a selective inhibitor of the stress-activated kinase MAP4K4, suppresses cell death in mouse myocardial ... -
PYRIMIDINE COMPOUNDS AS INHIBITORS OF PROTEIN KINASES IKK EPSILON AND/OR TBK-1, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
Newton, G; Stewart, M; Perrior, T; Aqil, R (2012-01-26)Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKKe and/or TBK-1 : in which: R1 represents an aliphatic heterocyclyl ... -
PYRIMIDINE COMPOUNDS USEFUL IN THE TREATMENT OF DISEASES MEDIATED BY IKKE AND/OR TBK1 MECHANISMS
Newton, G; Stewart, M; Jenkins, K; Perrior, T; Negoita-Giras, G; et al. (2014-08-28)Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases &Igr;&Kgr;&Kgr;&egr; and/or TBK-1 in which one of V and W is N, and ... -
PYRUVAMIDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN AND THEIR USE
Newton, G; Robinson, C; Jenkins, K; Kimberley, M; Zhang, J; et al. (2011-07-28)The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as "PVA compounds"), ... -
Selective protection of human cardiomyocytes from anthracycline cardiotoxicity by small molecule inhibitors of MAP4K4.
Golforoush, PA; Narasimhan, P; Chaves-Guerrero, PP; Lawrence, E; Newton, G; et al. (NATURE PUBLISHING GROUP, 2020-07-21)Given the poor track record to date of animal models for creating cardioprotective drugs, human pluripotent stem cell-derived cardiomyocytes (hPSC-CMs) have been proposed as a therapeutically relevant human platform to ... -
Targeting an Initiator Allergen Provides Durable and Expansive Protection against House Dust Mite Allergy.
Zhang, J; Chen, J; Richardson, JP; Francis-Newton, N-J; Lai, PF; et al. (AMER CHEMICAL SOC, 2022-09-09)Whereas treatment of allergic diseases such as asthma relies largely on the targeting of dysregulated effector pathways, the conceptually attractive alternative of preventing them by a pharmaceutical, at-source intervention ...