Publication number: 20240199680
Abstract: The present invention relates to efficient processes useful in the preparation of fluorinated cyclic dinucleosides, such as [P(R)]-2?-deoxy-2?-fluoro-5?-O—[(R)-hydroxymercaptophosphinyl]-P-thio-?-D-arabino-adenylyl-(3??5?)-3?-deoxy-3?-fluoroguanosine cyclic nucleotide, which is also known as (2R,5R,7R,8S,10R,12aR,14R,15S,15aR,16R)-7-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-14-(6-amino-9H-purin-9-yl)-15,16-difluoro-2, 10-bis(sulfanyl)octahydro-2H,10H, 12H-2?5,10?5-5,8-methanofuro[3,2-1][1, 3,6,9,11,2,10]pentaoxadiphosphacyclotetradecine-2,10-dione. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
Type:
Application
Filed:
March 28, 2022
Publication date:
June 20, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Chihui An, Patrick S. Fier, Kaori Hiraga, Zhijian Liu, Nicholas M. Marshall, John McIntosh, Steven P. Miller, Jeffrey C. Moore, Grant S. Murphy, Jennifer V. Obligacion, Weilan Pan, Feng Peng, Nastaran Salehi Marzijarani, Matthew S. Winston
Publication number: 20240182511
Abstract: Novel forms of 2-amino-9-[(2R,5R,7R,8S,10R,12aR,14R,15S,15aR,16R)-14-(6-amino-9H-purin-9)-yl)-15,16-difluoro-2,10-dihydroxy-2,10-disulfidooctahydro-12H-5.8-methanofuro[3,2-1][1,3,6,9,11,2,10]pentaoxa-diphosphacyclotetradecin-7-yl]-1,9-dihydro-6H-purin-6-one, which include crystalline salts and hydrates of 2-amino-9)-[(2R,5R,7R,8,S,10R,12aR,14R,15S,15aR,16R)-14-(6-amino-9H-purin-9-yl)-15,16-difluoro-2,10-dihydroxy-2,10-disulfido-octahydro-12H-5,8-methanofuro[3,2-1][1,3,6,9,11,2,10]pentaoxa-diphosphacyclotetradecin-7-yl]-1,9-dihydro-6H-purin-6-one, may be useful as inductors of type I interferon production, specifically as STING active agents.
Type:
Application
Filed:
April 4, 2022
Publication date:
June 6, 2024
Applicant:
Merck Sharp & Dohme LLC
Inventors:
Stephanus Axnanda, Zachary E. Dance, David J. Lamberto, Zhijian Liu, Feng Peng, Marc Poirier, Matthew S. Winston