Back to results
US 12,630,521 B2Granted
Arylamides and methods of use thereof
AssigneeGenzyme Corporation
InventorsJunkai Liao, Mark Munson, Zhongli Gao, Gregory Hurlbut, Hans Peter Nestler, Ingrid Mechin, Martin Smrcina, Ronghua Li, Ryan Hartung, William Bock, Bertrand Vivet, Andrew Scholte
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to heterocyclic compounds, pharmaceutically acceptable salts thereof, and pharmaceutical preparations thereof. Also described herein are compositions and the use of such compounds in methods of treating diseases and conditions mediated by deficient CFTR activity, in particular cystic fibrosis.
Claims23
A compound of formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- A is selected from
- wherein * marks the point of attachment to Y and ** marks the point of attachment to —C(O)—;
- Z1 and Z2 are each independently CH, S or N, wherein at least one of Z1 and Z2 is N or S;
- Y is —O—;
- E is C3-9-cycloalkyl, C6-10-aryl, 3-10 membered heteroaryl, or a 3-9 membered heterocycloalkyl, each of which is optionally substituted with one, two, three, four, or five occurrences of R5;
- V is —C(O)—O—R7;
- R1 is
- wherein
- Ra is C1-6 alkyl,
- Rb is C1-6 alkyl,
- Rc is C1-6 alkyl or C6-10 aryl, or
- any two of Ra, Rb, and Rc, taken together with the atoms to which they are attached, form a C3-9 cycloalkyl ring;
- each R2 is independently halo, C1-6 alkyl, haloC1-6 alkyl, —O—C1-6 alkyl, —O-halo C1-6 alkyl, C3-9-cycloalkyl or 3-10 membered heteroaryl;
- R3 is H or alkyl;
- each R5 is independently halo, C1-6 alkyl, C1-6 haloalkyl, —O— C1-6alkyl, —O—C1-6haloalkyl, and —S— C1-6haloalkyl;
- R7 is hydrogen, C1-6-alkyl, C6-10-aryl, or benzyl;
- and
- m is 0, 1, or 2.
16 more elements
A compound selected from:
- Com-
- pound
- Structure
- 1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10
- 11
- 12
- 13
- 14
- 15
- 16
- 17
- 18
- 19
- 20
- 21
- 22
- 23
- 24
- 25
- 26
- 27
- 28
- 29
- 30
- 31
- 32
- 33
- 34
- 35
- 36
- 37
- 38
- 39
- 40
- 41
- 42
- 43
- 44
- 45
- 46
- 47
- 48
- 49
- 50
- 51
- 52
- 53
- 54
- 55
- 56
- 57
- 58
- 59
- 60
- 61
- 62
- 63
- 64
- 65
- 66
- or a pharmaceutically acceptable salt thereof.
67 more elements
Dependencies are inferred from the claim text.