1329166-69-9

Upstream product

• 10403-47-1 2-bromo 5-nitroaniline 
• 201733-56-4 2-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-5,5-dimethyl-1,3,2-dioxaborinane 

Downstream Products

• 1329167-88-5 (S)-N-((1S)-1-(4-(2-amino-4-nitrophenyl)pyridin-2-yl)but-3-en-1-yl)-2-methylpropane-2-sulfinamide 
• 1329167-89-6 (S)-N-((1R)-1-(4-(2-amino-4-nitrophenyl)pyridin-2-yl)but-3-en-1-yl)-2-methylpropane-2-sulfinamide 
• 1329167-98-7 tert-butyl 1-(6-(2-amino-4-nitrophenyl)-3-chloropyridazin-4-yl)but-3-enylcarbamate 
• 1329167-90-9 tert-butyl N-[(1S)-1-[4-(2-amino-4-nitrophenyl)pyridin-2-yl]but-3-en-1-yl]carbamate 
• 1329167-91-0 C₁₅H₁₆N₄O₂ 
• 1329167-92-1 {(S)-1-[4-(4-nitro-2-pent-4-enoylaminophenyl)pyridin-2-yl]but-3-enyl}carbamic acid tert-butyl ester 
• 1329167-94-3 C₂₅H₃₂N₄O₃ 
• 1329167-93-2 {4-[2-((S)-1-tert-butoxycarbonylaminobut-3-enyl)pyridin-4-yl]-3-pent-4-enoylaminophenyl}carbamic acid methyl ester 

Relevant academic research and scientific papers

Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups

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 are also orally bioavailable has been a challenge. Here, we describe optimization of the imidazole-based macrocyclic series and our initial progress toward meeting this challenge. A two-pronged strategy, which focused on replacement of the imidazole scaffold and the design of new P1 groups, led to the discovery of potent, orally bioavailable pyridine-based macrocyclic FXIa inhibitors. Moreover, pyridine-based macrocycle 19, possessing the phenylimidazole carboxamide P1, exhibited excellent selectivity against relevant blood coagulation enzymes and displayed antithrombotic efficacy in a rabbit thrombosis model.

MACROCYCLIC SPIROCARBAMATE DERIVATIVES AS FACTOR XIA INHIBITORS, PHARMACEUTICALLY ACCEPTABLE COMPOSITIONS AND THEIR USE

The present invention provides a compound of Formula (I) and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds and said stereoisomers, and pharmaceutical compositions thereof, and methods for using said compounds and compositi

The second factor as inhibitor XIA pyridonecarboxylic dihydropyridines P1

The present invention provides compounds of Formula (X):(Formula (X), or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

CYCLIC P1 LINKERS AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

NOVEL MACROCYCLES AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

MACROCYCLES AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.