IP Library Granted Patent US 12,162,892
Granted Patent B2
US 12,162,892 · App. 17/990,427 · Granted Dec 10, 2024

CD16a binding agents and uses thereof

Inventors: Anna Bunin (Rego Park, NY); Lawrence G. Iben (Bethany, CT); Douglas Manion (Madison, CT); David Adam Spiegel (Hamden, CT); Matthew Ernest Welsch (New Haven, CT)
Assignee: KLEO PHARMACEUTICALS, INC.
C07D495/04A61K47/6849
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Quick Facts
Patent No.
US 12,162,892
App. No.
17/990,427
Granted
Dec 10, 2024
Kind
B2
Abstract

Among other things, the present disclosure provides compounds, compositions thereof, and methods of using the same. In some embodiments, compounds of the present disclosure bind to Fc receptors, e.g., CD16a. In some embodiments, compounds of the present disclosure are useful for treating various conditions, disorders or diseases including cancer.

Claims (37)

1. A method of treating a patient having a lymphoma, comprising administering to said patient a compound according to formula I: cells would be therapeutically beneficial in a

or a pharmaceutically acceptable salt thereof, wherein:

Ring A is phenyl;

Ring B is

or

Ring C is where Ring

where Ring C can be bonded to another ring C;

L 1 is a covalent bond, CH 2 —, —CH (R)—, or —C(R) 2 —;

L 2 is a covalent bond, —NHC (O)—, —C(O)NH—, —CH 2 —, —CH (R)—, —C(R) 2 —, —C(O)—, or —S(O) 2 —;

L 3 is a covalent bond or a bivalent, saturated or unsaturated, straight or branched C 1-50 hydrocarbon chain, wherein 0-6 methylene units of L are independently replaced by -Cy-, —O—, —NR—, —S—, —OC(O)—, —C(O)O—, —C(O)—, —S(O)—, —S(O) 2 —, —NRS (O) 2 —, —S(O) 2 NR—, —NRC(O)—, —C(O)NR—, —OC(O)NR—, —NRC(O)O—,

wherein:

each -Cy- is independently is

mAb is a monoclonal antibody selected from; adalimumab, cetuximab, daratumumab, rituximab;

each R is independently hydrogen or an optionally substituted group selected from C 1-6 aliphatic;

each instance of R 1 , is independently hydrogen, halogen, —CN, —NO 2 , C(O)R, —C(O) OR, —C(O)N(R) 2 , —N(R) 2 , —NRC (O)R, —NRC (O)N(R) 2 , —NRC (O) OR, —NRS (O) 2 R, —NRS (O) 2 N(R) 2 , —OR, —P(O) (R) 2 , —SR, —S(O)R, —S(O) 2 R, —S(O) (NH)R, —S(O) 2 N(R) 2 , or R;

each instance of R 2 is independently hydrogen, halogen, —CN, —NO 2 , or C 1-3 aliphatic;

m is 0, 1, 2, 3, 4 or 5;

each instance of n is independently selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;

p is 0, 1, or 2;

q is 0, 1, 2, 3, or 4.

2. The method of claim 1 , wherein the lymphoma is Hodgkins lymphoma, Non-Hodgkins lymphoma, diffuse large B-cell lymphoma (DLBCL), ABC DLBCL, chronic lymphocytic leukemia (CLL), chronic lymphocytic lymphoma, primary effusion lymphoma, Burkitt lymphoma/leukemia, acute lymphocytic leukemia, B-cell prolymphocytic leukemia, lymphoplasmacytic lymphoma, Waldenström's macroglobulinemia (WM), splenic marginal zone lymphoma, multiple myeloma, plasmacytoma, or intravascular large B-cell lymphoma.

3. The method of claim 1 , where the compound of formula I is a compound of formula I-a or I-b:

4. The method of claim 1 , wherein Ring A is selected from phenyl or 2,5-dimethyoxy-phenyl.

5. The method of claim 1 , wherein

Ring B is

6. The method of claim 1 , wherein

L 1 is a covalent bond or —CH 2 —;

L 2 is a covalent bond, —NHC (O)—, —C(O)NH—, —CH 2 —, —CH (R)—, —C(O)—, or —S(O) 2 —; and

L 3 is a bivalent, saturated or unsaturated, straight or branched C 1-50 hydrocarbon chain, wherein 0-6 methylene units of L are independently replaced by -Cy-, -O—, —NR—, —S—, —OC (O)—, —C(O)O—, —C(O)—, —S(O)—, —S(O) 2 —, —NRS (O) 2 —, —S(O) 2 NR—, —NRC (O)—, —C(O)NR—, —OC (O)NR—, —NRC (O)O—

7. The method of claim 1 , wherein m is 0, 1, 2, 3, or 4;

p is 0 or 1; and

q is 0, 1, 2, or 3.

8. The method of claim 3 , wherein the compound is of formula I-a:

9. The method of claim 3 , wherein

10. The method of claim 1 , wherein Ring C is

where Ring C is bonded to another Ring.

11. Selected The method of claim 1 , wherein the compound is a compound selected from

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 21, 2022
From: BUNIN, ANNA; IBEN, LAWRENCE G.; MANION, DOUGLAS; SPIEGEL, DAVID ADAM; WELSCH, MATTHEW ERNEST
To: KLEO PHARMACEUTICALS, INC.
Reel/Frame 061841/0953 →
Continuity (3)
Division 16960534
Provisional Application 62614607 · Jan 8, 2018
Related Publication 20240051966A1 · Feb 15, 2024