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US 2016/0176893 A1Published application
Rapamycin analogues and their pharmaceutical use
AssigneeIsomerase Therapeutics Ltd.
InventorsMatthew Alan Gregory, Steven Gary Kendrew, Steven James Moss, Barrie Wilkinson
Life of this patent
Estimating the term…
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.
Claims23
A rapamycin analogue of formula (I) or a pharmaceutically acceptable salt thereof.
- wherein:
- R1 represents Me or H;
- R2 and R3 represent H or R2 and R3 taken together represent keto;
- X1 and X2 are connected by a moiety selected from:
- or X2 is connected as follows:
- and X1 is H;
- or X1 represents H and X2 represents Z;
- Ra is selected from H, OH and OMe;
- Z represents
- Y represents methylene or is absent;
- M is selected from bond, CH2, CHMe, CHF, CHOH, CH2CH2CH(OMe), CMe2, CHEt and CF2;
- Q is selected from bond, CH2, CHMe, CHF, CHOH, CH2CH2, 0, S, CHCH2OH, C(OH)Me and CH(OMe);
- provided that:
- (i) when Q is not O or S then one of M or Q must represent CHOH CHCH2OH or C(OH)Me;
- and
- (ii) if Q is O or S, then M does not represent CHF, CF2, CHOMe, CHOH;
- and
- (iii) M and Q do not both represent bond;
- either R4 represents CH2OH and R5 represents H or R4 represents H and R5 represents CH2OH;
- and
- either R6 represents OH, R7 represents NH2 or H and X represents CH;
- or
- R6 represents H, R7 represents H and X represents N.
20 more elements
19-21. (canceled)
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Dependencies are inferred from the claim text.