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US 6,806,267 B1Granted
Apoptosis-inducing compounds
AssigneesThe Universita'di Siena, The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabeth Near Dublin
InventorsDavid Clive Williams, Daniela M. Zisterer, Vito Nacci, Giuseppe Campiani
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Abstract
The present invention relates to pyrrolobenzoxazepines, pyrrolobenzthiazepines and related compounds having the ability to induce apoptosis, to pharmaceutical compositions comprising these compounds and to their use as anti-tumour agents.
Claims10
A compound having the general formula (I):
- wherein:
- (i) R1 represents an unsubstituted C6 or C10 aryl group;
- or a C6 aryl group substituted with Me or OMe;
- (ii) A represents O, S or a sulfur atom oxidized to a sulfoxide;
- (iii) the cyclic group labeled F represents an unsubstituted C6 or C10 aryl or a C5 heteroaryl group having nitrogen as a heteroatom or a phenyl group substituted with ethoxycarbonyl function;
- and
- (iv) Y represents the group
- wherein R2 and R3 are independently hydrogen;
- or methyl or ethyl;
- or Y represents the group CH3, or (CH2)2CH3 or an unsubstituted C5 heteroaryl group having nitrogen as a heteroatom.
7 more elements
A method for selective apoptosis in cancerous conditions selected from the group consisting of leukemia, lymphoma, cervical cancer and breast cancer, comprising:
- administering to a subject in need thereof, a pharmaceutically effective amount of a compound of formula I
- wherein:
- (i) R1 represents an unsubstituted C6 or C10 aryl group;
- or a C6 aryl group substituted with Me or OMe;
- (ii) A represents O, S;
- or a sulfur atom oxidized to sulfoxide;
- (iii) the cyclic group labeled F represents an unsubstituted C6 or C10 aryl or a C5 heteroaryl group having nitrogen as a heteroatom or a phenyl group substituted with ethoxycarbonyl function;
- and
- (iv) Y represents the group
- wherein R2 and R3 are independently hydrogen;
- or methyl or ethyl;
- or Y represents the group CH3;
- or (CH2)2CH3 or an unsubstituted C5 heteroaryl group having nitrogen as a heteroatom;
- and
- assessing the affects of the administration.
12 more elements
Dependencies are inferred from the claim text.