Modulators of Alpha-4-beta-7 Integrin and MAdCAM
Assignee48HD Biopharma Inc.
InventorsJohn J. DWYER, Jessica CAO
Life of this patent
Estimating the term…
Abstract
The instant disclosure describes novel modulators of alpha α4β7 and/or MAdCAM and their use for the treatment of diseases and conditions associated with their biological function. Further described herein are methods of treating diseases or conditions associated with α4β7 and/or MAdCAM.
Claims26
A compound comprising a peptide scaffold and one or more of a linker, a sulfide or disulfide bond, wherein the linker, sulfide, or disulfide bond is covalently bonded to the peptide scaffold.
(canceled)
(canceled)
-20. (canceled)
A compound selected from the group consisting of scaffold A, B, C, D, E, F, G, H I, and J, wherein
- each X independently is Ser, Cys, Gly, Arg, R(NMe), Ac-Ser, or Ac-Cys;
- each Y1 independently is any amino acid;
- each Y2 independently is any amino acid;
- each X independently is any amino acid;
- each X″ independently is any amino acid or absent;
- each C″ independently is Cys or an Ac-Cys;
- each X″ independently is any amino acid;
- each Z1 independently is Cys, Asp, or Thr;
- each Z2 independently is Leu, Ile, Val, or Lys;
- each Z4 independently is Trp or absent;
- each Z5 independently is Gln or absent;
- and
- each of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R14 and R15 independently, is a corresponding side chain specific to each amino acid.
A compound selected from the group consisting of scaffold A-S, B-S, C-S, D-S, E-S, F-S, G-S, H-S, I-S, and J-S, wherein
- each X independently is Ser, Cys, Gly, Arg, R(NMe), Ac-Ser, or Ac-Cys;
- each Y1 independently is any amino acid;
- each Y2 independently is any amino acid;
- each X independently is any amino acid;
- each X″ independently is any amino acid or absent;
- each C″ independently is Cys or an Ac-Cys;
- each X″ independently is any amino acid;
- each Z1 independently is Cys, Asp, or Thr;
- each Z2 independently is Leu, Ile, Val, or Lys;
- each Z4 independently is Trp or absent;
- each Z5 independently is Gln or absent;
- and
- each of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R14 and R15 independently, is a corresponding side chain specific to each amino acid.
A compound selected from the group consisting of:
- No.
- 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
(canceled)
-33. (canceled)
The method of claim 33, wherein the disease comprises inflammatory bowel disease, ulcerative colitis, Crohn's disease, Celiac disease, colitis, diverticulitis, eosinophilic gastroenteritis, gastrointestinal cancer, autoimmune hepatitis, pancreatitis, encephalomyelitis, psoriasis and other inflammatory dermatoses such as dermatitis, eczema, atopic dermatitis, allergic contact dermatitis, urticarial, and pruritus, autoimmune diseases, such as fibromyalgia, scleroderma, ankylosing spondylitis, juvenile rheumatoid arthritis (RA), Still's disease, polyarticular juvenile RA, pauciarticular juvenile RA, polymyalgia rheumatica, RA, psoriatic arthritis, osteoarthritis, polyarticular arthritis, multiple sclerosis, lupus, systemic lupus erythematosus, type I diabetes (T1DM), type diabetes (T2DM), glomerulonephritis, graft-v-host disease (including both acute and chronic), and HIV infection.
-42. (canceled)
Dependencies are inferred from the claim text.