Gregory S. Wayne - Vernon Hills IL, US Sean M. Mellican - Gurnee IL, US Geoff G. Z. Zhang - Libertyville IL, US David R. Willcox - Ridgefield CT, US Jeffrey M. Breting - Evanston IL, US
Assignee:
Abbott Laboratories - Abbott Park IL
International Classification:
C07D 487/04
US Classification:
5462767
Abstract:
The present invention relates to the salt (1S,5S)-3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo[3. 2. 0]heptane benzenesulfonate and to methods of preparing the salt.
Gregory S. Wayne - Vernon Hills IL, US Sean M. Mellican - Gurnee IL, US Geoff G. Z. Zhang - Libertyville IL, US David R. Willcox - Ridgefield CT, US Jeffrey M. Breting - Evanston IL, US
Assignee:
Abboott Laboratories - Abbott Park IL
International Classification:
C07D 487/04
US Classification:
5462767
Abstract:
The present invention relates to the salt (1S,5S)-3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo[3. 2. 0]heptane benzenesulfonate and to methods of preparing the salt.
Gregory S. Wayne - Vernon Hills IL, US Sean M. Mellican - Gurnee IL, US Geoff G. Z. Zhang - Libertyville IL, US David R. Willcox - Ridgefield CT, US Jeffrey M. Breting - Evanston IL, US
Assignee:
Abbott Laboratories - Abbott Park IL
International Classification:
C07D 487/04
US Classification:
5462767
Abstract:
The present invention relates to the salt (1S,5S)-3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo[3. 2. 0]heptane benzenesulfonate and to methods of preparing the salt.
Solid Forms Of A Thiophosphoramidate Nucleotide Prodrug
Ales Medek - Winchester MA, US Lori Ann Ferris - Medford MA, US Praveen Mudunuri - Waltham MA, US Young Chun Jung - Lexington MA, US David Richard Willcox - Wellesley MA, US Michael Waldo - Grafton MA, US William Aloysius Nugent - Manomet MA, US
International Classification:
C07H 19/10 A61K 45/06 A61K 31/7072
US Classification:
424 857, 536 268, 514 51, 424 854
Abstract:
The present application relates to solid state forms, for example, crystalline forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.
Solid Forms Of A Thiophosphoramidate Nucleotide Prodrug
- South San Francisco CA, US Ales Medek - Winchester MA, US Lori Ann Ferris - Medford MA, US Praveen Mudunuri - Waltham MA, US Young Chun Jung - Lexington MA, US David Richard Willcox - Wellesley MA, US Michael Waldo - Grafton MA, US William Aloysius Nugent - Manomet MA, US
International Classification:
C07H 19/10 A61K 45/06 A61K 31/7072
Abstract:
The present application relates to solid state forms, for example, crystalline forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.
Solid Forms Of A Thiophosphoramidate Nucleotide Prodrug
- SOUTH SAN FRANCISCO CA, US Ales Medek - Winchester MA, US Lori Ann Ferris - Medford MA, US Praveen Mudunuri - Waltham MA, US Young Chun Jung - Lexington MA, US David Richard Willcox - Wellesley MA, US Michael Waldo - Grafton MA, US William Aloysius Nugent - Manomet MA, US
International Classification:
C07H 19/10 A61K 45/06 A61K 31/7072
Abstract:
The present application relates to solid state forms, for example, crystalline forms of 2′-C-methyluridine-5′-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2′-C-methyluridine-5′-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.
- Boston MA, US David Willcox - Wellesley MA, US Stefanie Roeper - Medford MA, US Kan-Nian Hu - Brighton MA, US Hoa Q. Luong - Newton MA, US
Assignee:
Vertex Pharmaceuticals Incorporated - Boston MA
International Classification:
C07D 333/40
US Classification:
514447, 549 69, 435184
Abstract:
Polymorph Forms M, H, P, X, and ZA of Compound (1) represented by the following structural formula:are described. A method of preparing polymorph Form M of Compound (1) includes stirring a mixture of Compound (1) and a solvent system that includes isopropanol, ethyl acetate, n-butyl acetate, methyl acetate, acetone, 2-butanone (methylethylketone (MEK)), or heptane, or a combination thereof at a temperature in a range of 10 C. to 47 C. to form From M of Compound (1). A method of preparing polymorph Form H of Compound (1) includes stirring a solution of Compound (1) at a temperature in a range of 48 C. to 70 C. to form Form H of Compound (1). A method of preparing polymorph Form P of Compound (1) includes stirring a mixture of Compound (1) and a solvent system that includes a solvent selected from the group consisting of dichloromethane and tetrahydrofuran (THF), and a mixture thereof at room temperature to form Form P of Compound (1). A method of preparing polymorph Form X of Compound (1) includes removing ethyl acetate from ethylacetate solvate G of Compound (1). A method of preparing polymorph Form ZA of Compound (1) includes removing n-butyl acetate from n-butyl acetate solvate A of Compound (1).
- Boston MA, US Piero L. Ruggiero - Cambridge MA, US Stefanie Roeper - Medford MA, US David Willcox - Wellesley MA, US Michael Waldo - Grafton MA, US Dahrika Milfred Yap Guerette - Cambridge MA, US Billie J. Kline - Kingston MA, US Hoa Q. Luong - Newton MA, US
Assignee:
Vertex Pharmaceuticals Incorporated - Boston MA
International Classification:
C07D 409/12 C07D 333/40
US Classification:
549 60, 549 69
Abstract:
A method of preparing Compound (1):or a pharmaceutically acceptable salt thereof includes: a) reacting Compound (A) with 3,3-dimethylbut-1-yne in the presence of one or more palladium catalysts selected from the group consisting of Pd(PPh)and Pd(PPh)Cl, and one or more copper catalysts selected from the group consisting of CuI, CuBr, and CuCl, to generate Compound (B); b) treating Compound (B) with an acid to generate Compound (C): c) reducing the cyclohexanone of Compound (C) to cyclohexanol to generate Compound (D); and d) reacting Compound (D) with a base to generate Compound (1), wherein Compounds (A), (B), (C), and (D) are each as depicted herein.