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Donald J P Pinto

Explore the profile of Donald J P Pinto including associated specialties, affiliations and a list of published articles. Areas
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Articles 27
Citations 363
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Recent Articles
1.
Dilger A, Pabbisetty K, Corte J, De Lucca I, Fang T, Yang W, et al.
J Med Chem . 2021 Sep; 65(3):1770-1785. PMID: 34494428
Factor XIa (FXIa) is an enzyme in the coagulation cascade thought to amplify thrombin generation but has a limited role in hemostasis. From preclinical models and human genetics, an inhibitor...
2.
Corte J, Pinto D, Fang T, Osuna H, Yang W, Wang Y, et al.
J Med Chem . 2019 Dec; 63(2):784-803. PMID: 31833761
Factor XIa (FXIa) inhibitors are promising novel anticoagulants, which show excellent efficacy in preclinical thrombosis models with minimal effects on hemostasis. The discovery of potent and selective FXIa inhibitors which...
3.
Clark C, Rossi K, Corte J, Fang T, Smallheer J, De Lucca I, et al.
Bioorg Med Chem Lett . 2019 Aug; 29(19):126604. PMID: 31445854
This manuscript describes the discovery of a series of macrocyclic inhibitors of FXIa with oral bioavailability. Assisted by structure based drug design and ligand bound X-ray crystal structures, the group...
4.
Quan M, Pinto D, Smallheer J, Ewing W, Rossi K, Luettgen J, et al.
J Med Chem . 2018 May; 61(17):7425-7447. PMID: 29775297
With the introduction of thrombin and factor Xa inhibitors to the oral anticoagulant market, significant improvements in both efficacy and safety have been achieved. Early clinical and preclinical data suggest...
5.
Pinto D, Orwat M, Smith 2nd L, Quan M, Lam P, Rossi K, et al.
J Med Chem . 2017 Oct; 60(23):9703-9723. PMID: 29077405
Factor XIa (FXIa) is a blood coagulation enzyme that is involved in the amplification of thrombin generation. Mounting evidence suggests that direct inhibition of FXIa can block pathologic thrombus formation...
6.
Corte J, Fang T, Osuna H, Pinto D, Rossi K, Myers Jr J, et al.
J Med Chem . 2017 Jan; 60(3):1060-1075. PMID: 28085275
A novel series of macrocyclic FXIa inhibitors was designed based on our lead acyclic phenyl imidazole chemotype. Our initial macrocycles, which were double-digit nanomolar FXIa inhibitors, were further optimized with...
7.
Corte J, Fang T, Pinto D, Orwat M, Rendina A, Luettgen J, et al.
Bioorg Med Chem . 2016 Apr; 24(10):2257-72. PMID: 27073051
Pyridine-based Factor XIa (FXIa) inhibitor (S)-2 was optimized by modifying the P2 prime, P1, and scaffold regions. This work resulted in the discovery of the methyl N-phenyl carbamate P2 prime...
8.
Smith 2nd L, Orwat M, Hu Z, Han W, Wang C, Rossi K, et al.
Bioorg Med Chem Lett . 2015 Dec; 26(2):472-478. PMID: 26704266
The synthesis, structural activity relationships (SAR), and selectivity profile of a potent series of phenylalanine diamide FXIa inhibitors will be discussed. Exploration of P1 prime and P2 prime groups led...
9.
Pinto D, Smallheer J, Corte J, Austin E, Wang C, Fang T, et al.
Bioorg Med Chem Lett . 2015 Mar; 25(7):1635-42. PMID: 25728130
Compound 2 was previously identified as a potent inhibitor of factor XIa lacking oral bioavailability. A structure-based approach was used to design analogs of 2 with novel P1 moieties with...
10.
Orwat M, Qiao J, He K, Rendina A, Luettgen J, Rossi K, et al.
Bioorg Med Chem Lett . 2014 Jun; 24(15):3341-5. PMID: 24951330
In an effort to identify a potential back-up to apixaban (Eliquis®), we explored a series of diversified P4 moieties. Several analogs with substituted gem-dimethyl moieties replacing the terminal lactam of...