DEUTERATED CYCLOSPORINE ANALOGS AND THEIR USE AS IMMUNOMODULATING AGENTS

Japanese Patent JP2007119489

A

To provide a new cyclosporine derivative which possess enhanced efficacy and modified pharmacokinetic and pharmacodynamic parameters.

The invention discloses the cyclosporine derivative which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivative of the invention is produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by (1) chemical substitution and optional deuterium substitution of amino acid 1, and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. The most active derivative of the invention has both chemical and deuterium substitutions. The method of producing the cyclosporine derivative and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivative are also disclosed.

JP4099065	Pharmaceutical compositions that inhibit vascular growth and methods of their use
WO/1997/026341	CYSTEINYL-tRNA SYNTHETASE FROM STAPHYLOCOCCUS AUREUS
WO/2002/085940	NEW POLYNUCLEOTIDES AND POLYPEPTIDES OF THE ERYTHROPOIETIN GENE

NAICKER S SELVERAJ (CA)
FOSTER ROBERT T (CA)
YATSCOFF RANDALL W (CA)

JP2007017196A

May 17, 2007

January 26, 2007

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ISOTECHNIKA INC (CA)

A61K38/00; C07K7/64; A61P1/04; A61P7/06; A61P13/12; A61P17/06; A61P19/00; A61P19/02; A61P19/08; A61P21/04; A61P25/00; A61P29/00; A61P37/00; A61P37/02; A61P37/06; A61P41/00; C07B59/00; C07K1/107; C07K1/12; C07K1/13; C07K7/06

Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita

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