JOHN R. KOENIG,ANDREW BOGDAN,ERIC VOIGTH,BO LIU,ROBERT J. ALTENBACH,MING C. YEUNG,XENIA B. SEARLE,XUEQING WANG,PHILIP R. KYM
申请号:
ARP150103536
公开号:
AR102492A1
申请日:
2015.10.30
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
Agents used to treat diseases and conditions mediated and regulated by CFTR include chemical fibrosis, SJ v gren syndrome, pancreatic failure, chronic obstructive pulmonary disease, and chronic air flow obstructive disease. Pharmaceutical compounds containing one or more formulation compounds (1) are also provided. 1. Claim 1: a formula compound (1) or a formula salt in which X is CR2 E and CR3;Or X is n, y is CR3;or X is CR² and Y is N; m is 0, 1, 2, or 3; R are optional substituents on the cyclopropyl ring, and in each case are independently of one another halogen, C₁₋₆ haloalkyl, or C₁₋₆ alkyl; R¹ and R²,independently of one another are hydrogen, halogen, C₁₋₆ haloalkyl, C₁₋₆ alkyl, -OR¹A, -C (O) OR¹B, -NR¹AR²A, or -C (O) NR¹AR²A; R¹A and R²A, in each case, are independently of each other hydrogen, C₁₋₆ haloalkyl, G¹A, or C₁₋₆ alkyl; wherein the C₁₋₆ haloalkyl and C₁₋₆ alkyl are each optionally substituted with one or two substituents independently selected from the group consisting of -ORZA, -SRZA, -S (O) ₂RZA, -C (O) RZA, -C (O) ORZA, -C (O) N (RZA) ₂,-N (RZA)-N (RZA) C (O) RZB, -N (RZA) S (O) ₂RZB, -N (RZA) C (O) ORZB, -N (RZA) C (O) N (RZA),-CN, and G¹A; or R¹A and R²A together with the nitrogen atom to which they are attached form a 4-6 membered heterocycle where the 4-6 membered heterocycle is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of in halogen, C₁₋₆ alkyl, C₁₋₆ haloalkyl, -ORʲ,y N (R)RZA is independent hydrogen in each case, c832131;a. In each case, there are separate c8321; 8331; 8326 asphalt; R3 and r18308;a. Hydrogen, halogen, c83218331-832626 halogen tar, c83218331;R⁴ is hydrogen, C₁₋₆ haloalkyl, or C₁₋₆ alkyl; R⁵ is hydrogen, -C (O) Rⁱ,-C (O) OH -C (O) O (C alquilo)-C (O) N (R)C₁₋₆ haloalkyl, C₁₋₆ alkyl, or G²A; wherein the C₁₋₆ haloalkyl and C₁₋₆ alkyl are each optionally substituted with one or two substituents independently selected from the group consisting of -ORʰ,-OC (O) N (R)-C (O)