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US 2010/0075997 A1Published application
Use of pkc inhibitors in transplantation
OwnerAlexander Korn, Philip Lake +1inventors
InventorsAlexander Korn, Philip Lake, Axel Maibucher
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Abstract
The present invention pertains to the use of a PKC inhibitor in the treatment of insulin-producing cell and tissue rejection, such as islet transplantation rejection or rejection of transdifferentiated insulin-producing hepatocytes.
Claims10
A method of treating, preventing or delaying insulin-producing cell rejection comprising administering an effective amount of a PKC inhibitor of formula (I) or (IIa),
- wherein
- Ra is H;
- C1-4alkyl;
- or C1-4alkyl substituted by OH, NH2, NHC1-4alkyl or N(di-C1-4alkyl)2;
- and
- R is a radical of formula (a) or (b)
- wherein
- each of R1 and R11 is a heterocyclic residue;
- NR4R5 wherein R4 and R5 form together with the nitrogen atom to which they are bound a heterocyclic residue;
- each of R2, R3, R12 and R13, independently, is H, halogen, C1-4alkyl, CF3, OH, SH, NH2, C1-4alkoxy, C1-4alkylthio, NHC1-4alkyl, N(di-C1-4alkyl)2 or CN;
- and
- ring A is optionally substituted,
- R1a is
- wherein either s′ is 0 and R′12 is hydrogen or C1-4alkyl;
- or s′ is 1 and R′12 is pyridyl, preferably 2-pyridyl, and
- R′1a is hydrogen or C1-4alkyl,
- or a pharmaceutically acceptable salt thereof to a subject in need of such treatment, prevention or delay.
14 more elements
(canceled)
Dependencies are inferred from the claim text.