JASON ALLAN WILES,AVINASH S. PHADKE,MILIND DESHPANDE,ATUL AGARWAL,XIANGZHU WANG,DAWEI CHEN,AKIHIRO HASHIMOTO,GODWIN PAIS,VENKAT RAO GADHACHANDA,QIUPING WANG
申请号:
ARP160102591
公开号:
AR105808A1
申请日:
2016.08.24
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
Compounds, Methods of use and processes to develop inhibitors of Complement Factor D comprising formula (1) or a pharmaceutically acceptable Salt or composition of the same, where r\u00b9\u00b2 or r\u00b9\u00b3 in Group a is a Substituent of amida (r\u00b3\u00b2).The inhibitors described herein are directed against the factor D and inhibit or regulate the complement Cascade in an early and essential of the alternative complement pathway, and reduces the capacity of factor d to modulate the classical and Lectin Pathways of complement.Inhibitors of factor d is described in the present have the capacity to reduce the excessive Activation of complement has been associated with some autoimmune diseases, inflammatory and neurodegenerative and ischemia-reperfusion injury and cancer.Claim 1: an amide Compound is selected from formula (1): (a) where a is a Select portion of Figure 1 (b) or (c) b is a portion of Figure 2 is selected (B, C, d or E (Figure 7 (a) b, C, d or e) or Figure 8 c is a portion that Selects figu Ra 3 (B, C, D, e, F, G, h, I, J, K, L,M or n) or Figure 5 l is a link or a selected portion of Figure 4 (B, C, D, e or f) and r\u00b3\u00b2 is a Select portion of Figure 6 (a) or (b) (b) a portion of which is selected Figure 1 (d) or (e) b is a portion of Figure 2 is selected (B, C, d or e) C is a portion of Figure 3 is selected (B, C, D, e, F, G, h, I, J, K, L,M or n) or Figure 5 l is a link or a selected portion of Figure 4 (B, C, D, e or f) and r\u00b3\u00b2 is a Select portion of Figure 6 (a) or (b) (c) a portion of which is selected Figure 1 (B, C, D, or e) b is a portion of Figure 2 is selected (B, C, d Figura7), or E (A, B, C, D, or e) or Figure 8 c is a portion of Figure 3 is selected (B, C, D,E, F, G, h, I, J, K, L, M and N) l is a link or a selected portion of Figure 4 (B, C, D, e or f) and r\u00b3\u00b2 is a portion that is selected (Figure 6 a and b) (d) a Compound of Table 2 or (e) a compound of Figure 9 (A, B, C, D, e, F, G, or H) where s is r\u00b