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US 7,256,286 B2Granted
Bryostatin analogues, synthetic methods and uses
AssigneeThe Board of Trustees of the Leland Stanford Junior University
InventorsPaul A. Wender, Blaise Lippa, Cheol-Min Park, Kevin W. Hinkle
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Abstract
Biologically active compounds related to the bryostatin family of compounds, having simplified spacer domains and/or improved recognition domains are disclosed, including methods of preparing and utilizing the same.
Claims19
A compound having the structure represented by a formula:
- wherein:
- R3 is H′, or OH;
- R7 is absent or represents from 1 to 4 substituents on the ring to which it is attached, independently selected from:
- lower alkyl, hydroxyl, amino, alkoxyl, alkylamino, ═O, acylainino and acyloxy;
- R20 is H, OH, or -T-U—V—R′ where:
- T is —O—, —S—, —N(H)— or —N(Me)-;
- U is absent or is —C(O)—, —C(S)—, —S(O)— or —S(O)2—;
- and
- V is absent or is —O—, —S—, —N(H)— or —N(Me)-, provided that V is absent when U is absent;
- R21 is ═CR3Rb or R21 represents independent moieties R6 and Rd where:
- Ra and Rb are independently H, CO2R′, CONRaRd or R′;
- Rc and Rd are independently H, alkyl, alkenyl, alkynyl or (CH2)pCO2R′;
- R26 is H, OH or R′;
- R′ is independently selected from:
- H, C1–C10 alkyl, naphthyl, anthracyl, phenanthryl, alkenyl, alkynyl, heteroaryl, aralkyl and heteroaralkyl;
- X is —CH2—, —O—, —S— or —N(Re)— where Re is COH, CO2R′ or SO2R′, Z is —O— or —N(H)—;
- p is 1, 2 or 3;
- or a pharmaceutically acceptable salt thereof,
- excluding the compounds of Formula 1998a where R3 is H or OH and where R20 is —O—C(O)—CH3, or —O—C(O)—(CH2)6—CH3
16 more elements
A compound having the structure represented by a formula of the group:
- wherein:
- R3 is H, or OH;
- R20 is H, OH, or -T-U—V—R′ where:
- T is —O—, —S—, —N(H)— or —N(Me)-;
- U is absent or is —O—, —C(S)—, —S(O)— or —S(O)2—;
- and
- V is absent or is —O—, —S—, —N(H)— or —N(Me)-, provided that V is absent when U is absent;
- R′ is independently selected from:
- H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, aralkyl and heteroaralkyl;
- or a pharmaceutically acceptable salt thereof.
7 more elements
Dependencies are inferred from the claim text.