446880-81-5Relevant articles and documents
Formulated and/or co-formulated liposome compositions containing TFGB antagonist prodrugs useful in the treatment of cancer and methods thereof
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, (2021/08/27)
Formulated and/or co-formulated liposomes (LNP) and solid-lipid nanoparticles (SLNP) comprising TB Prodrugs and methods of making the LNPs and SLNPs are disclosed herein. The TB prodrug compositions comprise a drug moiety, a lipid moiety, and linkage unit
ALK5 INHIBITOR CONJUGATES AND USES THEREOF
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, (2021/07/17)
The present disclosure relates to targeted drug conjugates comprising ALK5 inhibitors and targeting moieties that direct the ALK5 inhibitors to cells involved in fibrosis and cancer, for example myofibroblasts, activated fibroblasts and transitioning fibr
ANTIBODY-ALK5 INHIBITOR CONJUGATES AND THEIR USES
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Paragraph 0150; 0158-0160, (2020/02/06)
The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.
ANTIBODY-ALK5 INHIBITOR CONJUGATES AND THEIR USES
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Paragraph 0166; 0174-0176, (2020/06/07)
The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.
ANTIB0DY-ALK5 INHIBITOR CONJUGATES AND THEIR USES
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Paragraph 0155; 0163-0165, (2021/01/21)
The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.
2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling
Ciayadi, Rudy,Potdar, Mahesh,Walton, Kelly L.,Harrison, Craig A.,Kelso, Geoffrey F.,Harris, Simon J.,Hearn, Milton T.W.
, p. 5642 - 5645 (2011/10/09)
Novel inhibitors of TGF-β1 and activin A signalling based on a 2-aryl-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridine pharmacophore have been synthesised. Compounds containing phenyl or aromatic nitrogen heterocycle substituents inhibited both types of signalling with HEK-293T cells in culture, with a selectivity preference for TGF-β1. Synthetic compounds containing pyridin-3-yl, pyrazol-4-yl, pyrazol-1-yl or 1H-imidazoyl-1-yl substituents exhibited structural and functional attributes suitable for further investigation related to the development of more potent TGF-β inhibitors.
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N- (tetrahydro-2H-pyran-4-yl)benzamide (GW788388): A potent, selective, and orally active transforming growth factor-β type I receptor inhibitor
Gellibert, Fran?oise,De Gouville, Anne-Charlotte,Woolven, James,Mathews, Neil,Nguyen, Van-Loc,Bertho-Ruault, Cécile,Patikis, Angela,Grygielko, Eugene T.,Laping, Nicholas J.,Huet, Stéphane
, p. 2210 - 2221 (2007/10/03)
Inhibitors of transforming growth factor β (TGF-β) type I receptor (ALK5) offer a novel approach for the treatment of fibrotic diseases such as renal, hepatic, and pulmonary fibrosis. The optimization of a novel phenylpyridine pyrazole series (1a) led to the identification of potent, selective, and orally active ALK5 inhibitors. The cellular potency and pharmacokinetics profiles of these derivatives were improved and several compounds presented antifibrotic activity when orally administered to rats in an acute liver model of dimethylnitrosamine- (DMN-) induced expression of collagen IA1 mRNA, a major gene contributing to excessive extra cellular matrix deposit. One of the most potent ALK5 inhibitors identified in this chemical series, compound 13d (GW788388), reduced the expression of collagen IA1 by 80% at a dose of 1 mg/kg twice a day (b.i.d.). This compound significantly reduced the expression of collagen IA1 mRNA when administered orally at 10 mg/kg once a day (u.i.d.) in a model of puromycin aminonucleoside-induced renal fibrosis.