US2023174511A1PendingUtilityA1
Pyrimidinyl tyrosine kinase inhibitors
Est. expiryJun 8, 2032(~5.9 yrs left)· nominal 20-yr term from priority
Inventors:Brian T. HopkinsTimothy ChanTracy J. JenkinsPatrick R. ConlonXiongwei CaiMichael HumoraXianglin ShiRoss A. MillerAndrew Thompson
C07D 401/14A61P 35/00A61P 35/02A61P 29/00A61P 9/06A61K 31/506A61P 43/00A61P 37/08A61P 1/16A61P 37/02A61P 17/00A61P 37/00A61P 37/06A61P 7/06A61P 19/02A61P 19/10
77
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton’s tyrosine kinase and which exhibit desirable characteristics for the same.
Claims
exact text as granted — not AI-modified1 . A compound of formula I:
or a pharmaceutically acceptable salt thereof, wherein:
each R 1 is independently hydrogen, an optionally substituted C 1-6 aliphatic group, an optionally substituted 3-7 membered monocyclic heterocyclic group, or an optionally substituted heterocyclylalkyl group having 3-7 carbon atoms and 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
or two R 1 groups are taken together with their intervening atoms to form an optionally substituted 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
wherein optionally substituted groups may be substituted with halogen, —NO 2 , —CN, —OR, —SR, —N(R) 2 , —C(O)R, —CO 2 R, —N(R)C(O)OR, —C(O)N(R) 2 , —OC(O)R, —N(R)C(O)R, —S(O)R, —S(O) 2 R, or —S(O) 2 N(R) 2 ;
each R is independently hydrogen or C 1-6 aliphatic;
or two R groups attached to the same nitrogen are taken together with their intervening atoms to form an optionally substituted 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms, in which any second heteroatom is independently selected from nitrogen, oxygen, and sulfur;
Ring A is
R 2 is —Cl or —F; and
R 3 is —CF 3 , —OCF 3 , or —F.
2 . The compound of claim 1 , wherein the compound is of formula II-a:
or a pharmaceutically acceptable salt thereof.
3 . The compound of claim 1 , wherein the compound is of formula II-b:
or a pharmaceutically acceptable salt thereof.
4 . The compound of claim 1 , wherein the compound is of formula III:
.
5 . The compound of claim 1 , wherein the compound is formula IV:
.
6 . The compound of claim 5 , wherein R 3 is —CF 3 .
7 . The compound of claim 5 , wherein R 3 is —F.
8 . The compound of claim 5 , wherein both R 1 are hydrogen.
9 . The compound of claim 5 , wherein one R 1 is hydrogen and the other R 1 is an optionally substituted C 1-6 aliphatic.
10 . The compound of claim 9 , wherein one R 1 is hydrogen and the other R 1 is methyl.
11 . The compound of claim 5 , wherein both R 1 are optionally substituted C 1-6 aliphatic groups.
12 . The compound of claim 1 , wherein one R 1 is hydrogen and the other is optionally substituted C 1-6 aliphatic.
13 . The compound of claim 1 , wherein both R 1 are optionally substituted C 1-6 aliphatic groups.
14 . The compound of claim 1 , wherein both R 1 are hydrogen.
15 . The compound of claim 1 , wherein R 2 is —Cl or —F.
16 . (canceled)
17 . The compound of claim 1 , wherein R 3 is —CF 3 , —OCF 3 , or-F.
18 - 19 . (canceled)
20 . A compound selected from the group consisting of:
.
21 . A method of decreasing the enzymatic activity of Bruton’s tyrosine kinase comprising contacting Bruton’s tyrosine kinase with an effective amount of a compound of claim 1 or a composition thereof.
22 . A method of treating a disorder responsive to inhibition of Bruton’s tyrosine kinase comprising administering to a subject an effective amount of a compound of claim 1 or a composition thereof.
23 . A method of treating a disorder selected from the group consisting of autoimmune disorders, inflammatory disorders, and cancers comprising administering to a subject an effective amount of a compound of claim 1 or a composition thereof.
24 - 27 . (canceled)Join the waitlist — get patent alerts
Track US2023174511A1 — get alerts on status changes and closely related new filings.
We store only your email — no account needed. See our privacy policy.