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Title:
RAPAMYCIN ANALOGUES AND THEIR PHARMACEUTICAL USE
Document Type and Number:
WIPO Patent Application WO/2015/004455
Kind Code:
A3
Abstract:
Novel rapamycin analogues and methods for their production with FKBP and/or MIP inhibitory activity with reduced mTOR inhibitory activity with therapeutic potential e.g. as bacterial virulence inhibitors.

Inventors:
GREGORY, Matthew Alan (Isomerase Therapeutics Ltd, Science VillageChesterford Research Park, Cambridge Cambridgeshire CB10 1XL, GB)
KENDREW, Steven Gary (Isomerase Therapeutics Ltd, Science VillageChesterford Research Park, Cambridge Cambridgeshire CB10 1XL, GB)
MOSS, Steven James (Isomerase Therapeutics Ltd, Science VillageChesterford Research Park, Cambridge Cambridgeshire CB10 1XL, GB)
WILKINSON, Barrie (Isomerase Therapeutics Ltd, Science VillageChesterford Research Park, Cambridge Cambridgeshire CB10 1XL, GB)
Application Number:
GB2014/052091
Publication Date:
January 15, 2015
Filing Date:
July 09, 2014
Export Citation:
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Assignee:
ISOMERASE THERAPEUTICS LIMITED (Science Village, Chesterford Research Park, Cambridge Cambridgeshire CB10 1XL, GB)
International Classes:
C07D498/18; A01N43/90; A61K31/439; A61P31/00; C12P17/18
Domestic Patent References:
WO2000009109A22000-02-24
Other References:
NELSON F C ET AL: "Manipulation of the C922)-C(27) region of rapamycin: stability issues and biological implications", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 9, no. 2, 18 January 1999 (1999-01-18), pages 295 - 300, XP004152620, ISSN: 0960-894X, DOI: 10.1016/S0960-894X(98)00735-5
FRANCES C. NELSON ET AL: "A novel ring contraction of rapamycin", TETRAHEDRON LETTERS, vol. 35, no. 41, 1994, pages 7557 - 7560, XP055104826, ISSN: 0040-4039, DOI: 10.1016/S0040-4039(00)78342-0
J. S. SKOTNICKI ET AL.: "Ring expanded rapamycin derivatives", TETRAHEDRON LETTERS, vol. 35, no. 2, 1994, pages 201 - 202, XP002730496
HOLT D A ET AL: "STRUCTURE-ACTIVITY STUDIES OF NONMACROCYCLIC RAPAMYCIN DERIVATIVES", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 3, no. 10, 1993, pages 1977 - 1980, XP000852549, ISSN: 0960-894X, DOI: 10.1016/S0960-894X(01)80998-7
Attorney, Agent or Firm:
TEUTEN, Andrew et al. (Sagittarius IP, Three GlobesideFieldhouse Lane,Marlow, Buckinghamshire SL7 1HZ, GB)
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