Title:
AZA-, OXA AND THIA-PREGNAN-20-ONE-3.ALPHA.-OL COMPOUNDS FOR USE IN TREATING CNS DISORDERS
Document Type and Number:
WIPO Patent Application WO/2019/140272
Kind Code:
A1
Abstract:
Provided herein is a compound of Formula (I-I), or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I), and methods of using the compounds, e.g., in the treatment of CNS-related disorders.
Inventors:
ROBICHAUD ALBERT (US)
SALITURO FRANCESCO (US)
BLANCO-PILLADO MARIA (US)
LA DANIEL (US)
HARRISON BOYD (US)
SALITURO FRANCESCO (US)
BLANCO-PILLADO MARIA (US)
LA DANIEL (US)
HARRISON BOYD (US)
Application Number:
PCT/US2019/013315
Publication Date:
July 18, 2019
Filing Date:
January 11, 2019
Export Citation:
Assignee:
SAGE THERAPEUTICS INC (US)
International Classes:
C07J73/00; A61K31/58; A61P25/00; C07J75/00
Domestic Patent References:
| WO1996016076A1 | 1996-05-30 | |||
| WO2014169833A1 | 2014-10-23 | |||
| WO2014169833A1 | 2014-10-23 |
Foreign References:
| US5376645A | 1994-12-27 |
Other References:
DURAN F J ET AL: "Synthesis of 6-thia analogs of the natural neurosteroid allopregnanolone", TETRAHEDRON, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 62, no. 20, 15 May 2006 (2006-05-15), pages 4762 - 4768, XP025001929, ISSN: 0040-4020, [retrieved on 20060515], DOI: 10.1016/J.TET.2006.03.025
CRISTINA SUÑOL ET AL: "Activity of B-Nor Analogues of Neurosteroids on the GABA A Receptor in Primary Neuronal Cultures", JOURNAL OF MEDICINAL CHEMISTRY, vol. 49, no. 11, 1 June 2006 (2006-06-01), US, pages 3225 - 3234, XP055570705, ISSN: 0022-2623, DOI: 10.1021/jm060002f
NICOLETTI D ET AL: "Synthesis and GABA"A receptor activity of 6-oxa-analogs of neurosteroids", STEROIDS, ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, US, vol. 65, no. 6, 1 June 2000 (2000-06-01), pages 349 - 356, XP004198899, ISSN: 0039-128X, DOI: 10.1016/S0039-128X(00)00088-X
KASAL A ET AL: "Neurosteroid analogues: synthesis of 6-aza-allopregnanolone", TETRAHEDRON, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 61, no. 9, 28 February 2005 (2005-02-28), pages 2269 - 2278, XP027860834, ISSN: 0040-4020, [retrieved on 20050228]
LAN, N. C. ET AL., NEUROCHEM. RES., vol. 16, 1991, pages 347 - 356
MAJEWSKA, M. D. ET AL., SCIENCE, vol. 232, 1986, pages 1004 - 1007
HARRISON, N. L. ET AL., JPHARMACOL. EXP. THER., vol. 241, 1987, pages 346 - 353
"Handbook of Chemistry and Physics"
THOMAS SORRELL: "Organic Chemistry", 1999, UNIVERSITY SCIENCE BOOKS
SMITH; MARCH: "March's Advanced Organic Chemistry", 2001, JOHN WILEY & SONS, INC.
LAROCK: "Comprehensive Organic Transformations", 1989, VCH PUBLISHERS, INC.
CARRUTHERS: "Some Modern Methods of Organic Synthesis", 1987, CAMBRIDGE UNIVERSITY PRESS
JACQUES ET AL.: "Enantiomers, Racemates and Resolutions", 1981, WILEY INTERSCIENCE
WILEN ET AL.: "Tetrahedron", vol. 33, 1977, pages: 2725
ELIEL: "Stereochemistry of Carbon Compounds", 1962, MCGRAW-HILL
WILEN: "Tables of Resolving Agents and Optical Resolutions", 1972, UNIV. OF NOTRE DAME PRESS, pages: 268
BERGE ET AL., J. PHARM. SCI., vol. 66, no. 1, 1977, pages 1 - 79
T. W. GREENE; P. G. M. WUTS: "Protecting Groups in Organic Synthesis", 1999, JOHN WILEY & SONS
"Remington's Pharmaceutical Sciences", 1985, MACK PUBLISHING COMPANY
E. W. MARTIN: "Remington's Pharmaceutical Sciences", 1980, MACK PUBLISHING CO.
REMINGTON: "The Science and Practice of Pharmacy", 2005, LIPPINCOTT WILLIAMS & WILKINS
"Remington: The Science and Practice of Pharmacy", 2005, LIPPINCOTT WILLIAMS & WILKINS
T. W. GREENE; P. G. M. WUTS: "Protecting Groups in Organic Synthesis", 1991, WILEY
TETRAHEDRON, 2006, pages 4384 - 4392
GEE ET AL., J PHARMACOL. EXP. THER., vol. 241, 1987, pages 346 - 353
HAWKINSON ET AL., MOL. PHARMACOL., vol. 46, 1994, pages 977 - 985
LEWIN, A.H ET AL., MOL. PHARMACOL., vol. 35, 1989, pages 189 - 194
CRISTINA SUÑOL ET AL: "Activity of B-Nor Analogues of Neurosteroids on the GABA A Receptor in Primary Neuronal Cultures", JOURNAL OF MEDICINAL CHEMISTRY, vol. 49, no. 11, 1 June 2006 (2006-06-01), US, pages 3225 - 3234, XP055570705, ISSN: 0022-2623, DOI: 10.1021/jm060002f
NICOLETTI D ET AL: "Synthesis and GABA"A receptor activity of 6-oxa-analogs of neurosteroids", STEROIDS, ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, US, vol. 65, no. 6, 1 June 2000 (2000-06-01), pages 349 - 356, XP004198899, ISSN: 0039-128X, DOI: 10.1016/S0039-128X(00)00088-X
KASAL A ET AL: "Neurosteroid analogues: synthesis of 6-aza-allopregnanolone", TETRAHEDRON, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 61, no. 9, 28 February 2005 (2005-02-28), pages 2269 - 2278, XP027860834, ISSN: 0040-4020, [retrieved on 20050228]
LAN, N. C. ET AL., NEUROCHEM. RES., vol. 16, 1991, pages 347 - 356
MAJEWSKA, M. D. ET AL., SCIENCE, vol. 232, 1986, pages 1004 - 1007
HARRISON, N. L. ET AL., JPHARMACOL. EXP. THER., vol. 241, 1987, pages 346 - 353
"Handbook of Chemistry and Physics"
THOMAS SORRELL: "Organic Chemistry", 1999, UNIVERSITY SCIENCE BOOKS
SMITH; MARCH: "March's Advanced Organic Chemistry", 2001, JOHN WILEY & SONS, INC.
LAROCK: "Comprehensive Organic Transformations", 1989, VCH PUBLISHERS, INC.
CARRUTHERS: "Some Modern Methods of Organic Synthesis", 1987, CAMBRIDGE UNIVERSITY PRESS
JACQUES ET AL.: "Enantiomers, Racemates and Resolutions", 1981, WILEY INTERSCIENCE
WILEN ET AL.: "Tetrahedron", vol. 33, 1977, pages: 2725
ELIEL: "Stereochemistry of Carbon Compounds", 1962, MCGRAW-HILL
WILEN: "Tables of Resolving Agents and Optical Resolutions", 1972, UNIV. OF NOTRE DAME PRESS, pages: 268
BERGE ET AL., J. PHARM. SCI., vol. 66, no. 1, 1977, pages 1 - 79
T. W. GREENE; P. G. M. WUTS: "Protecting Groups in Organic Synthesis", 1999, JOHN WILEY & SONS
"Remington's Pharmaceutical Sciences", 1985, MACK PUBLISHING COMPANY
E. W. MARTIN: "Remington's Pharmaceutical Sciences", 1980, MACK PUBLISHING CO.
REMINGTON: "The Science and Practice of Pharmacy", 2005, LIPPINCOTT WILLIAMS & WILKINS
"Remington: The Science and Practice of Pharmacy", 2005, LIPPINCOTT WILLIAMS & WILKINS
T. W. GREENE; P. G. M. WUTS: "Protecting Groups in Organic Synthesis", 1991, WILEY
TETRAHEDRON, 2006, pages 4384 - 4392
GEE ET AL., J PHARMACOL. EXP. THER., vol. 241, 1987, pages 346 - 353
HAWKINSON ET AL., MOL. PHARMACOL., vol. 46, 1994, pages 977 - 985
LEWIN, A.H ET AL., MOL. PHARMACOL., vol. 35, 1989, pages 189 - 194
Attorney, Agent or Firm:
UITTO, Olivia, D. (US)
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