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Prodrugs of epoxy ketone protease Peptide inhibitors
专利权人:
INC.;ONYX THERAPEUTICS
发明人:
申请号:
ARP130102446
公开号:
AR091716A1
申请日:
2013.07.10
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
The current diffusion shows that it is an effective component of cycloketoproteinase inhibitor. Pharmaceutical ingredients. Treatment. 1. Claim 1: compound according to formula (1),Or a pharmaceutically acceptable salt, wherein R1 is defined according to (a) or (b) as follows: (a) R1 has a formula (2), wherein het is isomerized, including 5-6 atoms in the ring, at least one of which is a nitrogen atom selected from n (H),-N (m) - o-n (lease c833218331-83323) -,There, the nitrogen atom on the ring is replaced by an R1 groupthus forming a quaternary nitrogen atom and where the positive charge associated with the quaternary nitrogen atom is balanced by a pharmaceutically acceptable anion; and M is C₁₋₁₂ alkyl;O (b) r 1 is heteromorphic, including 5-6 atoms in the ring, at least one atom in the ring is the nitrogen atom selected from = n-y-n (coke tar c83321331);And the nitrogen atom on the ring was replaced by an R1 groupThus, a fourth-generation nitrogen atom is formed, and the positive and negative charges related to the fourth-generation nitrogen atom are balanced by a medically acceptable anion; R2 and R3,Add the carbon atoms connected to each person to form a ring; or R2,R83088 and r83099;Combined with carbon atoms, they form a carbon group; or r830808 and r83099;They combine with carbon atoms to form R1 cube;RS1,RS2,RS3,and RS⁴ each is independently selected from C₁₋₆ alkyl,C₁₋₆ hydroxyalkyl,alcoxi C alquilo Caryl C₆₋₁₀,and aralkyl C₇₋₁₂,Each of these alternatives is replaced by a selected group of substances, including: Amida, Amina, carboxyl acid, or a pharmaceutically acceptable salt, carbamate, thioether, and thioether of these substances; RN1,RN,RN-3H rn830808 and rn830808 are selected from between H and r1830808 respectively;R1 is a kind of residual substance that can be removed from pH gt; 7 kinds can be removed from the surface of mat; R2 2 is a polishing group; R3 is a kind of masked carbide that can be removed from pH lt; 6.5 is a kind of enzyme or a
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