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Selective caspase inhibitors and their uses
专利权人:
Genesis Technologies Limited
发明人:
AHLFORS, Jan-Eric,MEKOUAR, Khalid
申请号:
ES09749369
公开号:
ES2640814T3
申请日:
2009.05.21
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of Formula IA ** (See formula) ** in which a is 0 or 1; b is 0 or 1 with the proviso that when b is 0, a is 0; A is 1) H, 2) C1-C6 alkyl, 3) aryl, 4) heteroaryl, 5) heterocyclyl, 6) R3-OC (O) -, 7) PhCH2OC (O) -, or 8) R3-S ( O) 2-; AA2 is the side chain of the (R) or (S) amino acid of Val, Leu, Pro, Met, Ala, Thr, His, Ser or Lys; AA3 is the side chain of (R) or (S) amino acid of Trp, Tyr, Ala, Asp, Gln, Glu, Phe, Ser, Thr, Val, Gly, Leu, His, or Ile, or AA3 is phenylglycine, indanylglycine , or Ala- (2'-quinolyl); AA4 is the side chain of the (R) or (S) amino acid of Asp, Ile, Leu, Glu, Ala, Val, Tyr, Trp, Phe, or Pro; AA5, when present, is the side chain of the (R) or (S) amino acid of Val or Leu; AAx, when present, is the side chain of the (R) or (S) amino acid of any amino acid residue D or L; the wavy line represents the cis or trans orientation of R1 and R2; R1 is 1) aryl, 2) heteroaryl, 3) heterocyclyl, 4) alkene C2-C6-R20, 5) SO2R5, 6) SO3R5, 7) SOR5, 8) SONHR5, 9) SO2NHR5, 10) CN, 11) CO2R5 , 12) COR5, 13) PO3R5, 14) PO (OR5) 2, or 15) PO (OR5), wherein aryl, heteroaryl, or heterocyclyl, are optionally substituted with one or more R30 substituents; R2 is 1) R1; or 2) H, 3) halogen, 4) haloalkyl, 5) C1-C6 alkyl, 6) C2-C6 alkene, ...Un compuesto de Fórmula IA **(Ver fórmula)** en la que a es 0 o 1; b es 0 o 1 con la condición de que cuando b es 0, a es 0; A es 1) H, 2) alquilo C1-C6, 3) arilo, 4) heteroarilo, 5) heterociclilo, 6) R3-OC(O)-, 7) PhCH2OC(O)-, o 8) R3-S(O)2-; AA2 es la cadena lateral del (R) o (S) aminoácido de Val, Leu, Pro, Met, Ala, Thr, His, Ser o Lys; AA3 es la cadena lateral del (R) o (S) aminoácido de Trp, Tyr, Ala, Asp, Gln, Glu, Phe, Ser, Thr, Val, Gly, Leu, His, o Ile, o AA3 es fenilglicina, indanilglicina, o Ala-(2'-quinolilo); AA4 es la cadena lateral del (R) o (S) aminoácido de Asp, Ile, Leu, Glu, Ala, Val, Tyr, Trp, Phe, o Pro; AA5, cuando está presente, es la cadena lateral del (R) o (S) aminoácido de Val o Leu; AAx, cu
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