Factor iia inhibitors

Details Factor iia inhibitors Factor iia inhibitors

C - Chemistry, Metallurgy

07

K

C07K 5/08 (2006.01) A61K 38/04 (2006.01) A61K 38/08 (2006.01) C07K 5/02 (2006.01) C07K 5/068 (2006.01) C07K 5/107 (2006.01) C07K 7/02 (2006.01) C07K 7/06 (2006.01) C07K 14/815 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2101331

2101331 9213877 PCTABS00014 Disclosed are compounds of the formula: X Y Z A P Q T which are highly potent, selective factor IIa inhibitors. X, when present, may be connected to T, may be H, CH3, an acyl group, or a general protective group. Y is D-DPA, D-Phe, D-Val, D-Ile, D-Nle, a phenylsulfonyl, Dansyle, or 8-(1,2,3,4-tetrahydroquinolinosulfonyl) compound. Z, when present, is Gly, L/D-Pro, L/D-Ala, L/D-Leu, aminoisobutyric acid, a substituted or unsubstituted L/D-Pro ring homologue, or L/D-Val. A may be (I) wherein M is -CO-CF2-(CO)s-, -(CO)d-NH-, -(CO)d-(CH2)p-, or -CH(OH)-(CH2)p-, d is 0-2, p and q are 0-5, and s is 0 or 1, or A is a proline-like group. P and Q (if Q is present) are substituted or unsubstituted amino acids selected from the group consisting of L/D-Phe, L/D-Cha, L/D-Nal(1), L/D-Nal(2), L/D-phenylglycinyl, L/D-Leu, L/D-Ile, L/D-Nle, L/D-Arg, L/D-Lys, or L/D-His. T may be connected to X, or may be -OH, -OR4, -NH2, -NHR4, or -NR4R5, wherein R4 and R5 are independently selected form alkyl, aryl, (ar)alkyl, and wherein R4 and R5 can be cyclically bonded one to another.

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