# US 2023/0056447 A1 · Tyk2 inhibitors and uses thereof

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- Number: US 2023/0056447 A1
- Document ID: US20230056447A1
- Status: Published application
- Kind: A1
- Application number: 17/447,648
- Filed: 2021-09-14
- Published: 2023-02-23
- Earliest claimed: 2017-07-28
- Assignees: Nimbus Lakshmi, Inc.
- Applicants: Nimbus Lakshmi, Inc.
- Inventors: Craig E. Masse; Jeremy Robert Greenwood; Sayan Mondal; Scott D. Cowen; Thomas H. Mclean
- Web page: https://patentgrep.com/patent/US20230056447A1

## CPC

- C07D 487/04: Ortho-condensed systems
- A61P 11/06: Antiasthmatics
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- C07D 519/00: Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

## Claims

### Claim 1

A compound of formula I:
or a pharmaceutically acceptable salt thereof, wherein:
R3 is —C(O)NH2; —C(O)NHR3A; or —C(O)N(R3A)2;
R5 is -L1-R5A;
R6 is hydrogen, RA, or RB;
R7 is hydrogen, halogen, —NH2, —NHR7A, or —NHC(O)R7A;
L1 is —N(R);
R3A is a 5-membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur; or a 5-membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur; each of which is substituted by q instances of RC;
R5A is RA or RB, and is substituted by r instances of RC;
R7A is RB, and is substituted by q instances of RC;
each instance of RA is independently oxo, halogen, —CN, —NO2, —OR, —SR, —NR2, —S(O)2R, —S(O)2NR2, —S(O)R, —S(O)NR2, —C(O)R, —C(O)OR, —C(O)NR2, —C(O)N(R)OR, —OC(O)R, —OC(O)NR2, —N(R)C(O)OR, —N(R)C(O)R, —N(R)C(O)NR2, —N(R)C(NR)NR2, —N(R)S(O)2NR2, or —N(R)S(O)2R;
each instance of RB is independently C1-6 aliphatic; phenyl; a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur; an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur; a 3-7 membered saturated or partially unsaturated carbocyclic ring; a 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur; or a 7-12 membered saturated or partially unsaturated bicyclic heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
each instance of RC is independently oxo, halogen, —CN, —NO2, —OR, —SR, —NR2, —S(O)2R, —S(O)2NR2, —S(O)R, —S(O)NR2, —C(O)R, —C(O)OR, —C(O)NR2, —C(O)N(R)OR, —OC(O)R, —OC(O)NR2, —N(R)C(O)OR, —N(R)C(O)R, —N(R)C(O)NR2, —N(R)C(NR)NR2, —N(R)S(O)2NR2, or —N(R)S(O)2R or an optionally substituted group selected from C1-6 aliphatic, phenyl, a 3-7 membered saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur, and a 5-6 membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur; or wherein two optional substituents on adjacent carbons are optionally taken together to form a 3-6 membered saturated or partially unsaturated fused heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
each R is independently hydrogen, or an optionally substituted group selected from C1-6 aliphatic, phenyl, a 3-7 membered saturated or partially unsaturated heterocyclic having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur, and a 5-6 membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, or: two R groups on the same nitrogen are taken together with their intervening atoms to form a 4-7 membered saturated, partially unsaturated, or heteroaryl ring having 0-3 heteroatoms, in addition to the nitrogen, independently selected from nitrogen, oxygen, and sulfur;
wherein each hydrogen bound to carbon can be optionally and independently replaced by deuterium; and
each instance of q and r is independently 0, 1, 2, 3, or 4.

### Claim at position 2

2-32. (canceled)

### Claim 33 (depends on 1)

The compound of claim 1, of formula VII, IX, or XVI:
or a pharmaceutically acceptable salt thereof.

### Claim 34 (depends on 33)

The compound of claim 33, wherein —N(R)— in L1 is —N(H)—.

### Claim 35 (depends on 34)

The compound of claim 34, wherein R6 is hydrogen.

### Claim 36 (depends on 35)

The compound of claim 35, wherein R7 is —NHR7A.

### Claim 37 (depends on 36)

The compound of claim 36, wherein R7A is C1-6 aliphatic.

### Claim 38 (depends on 37)

The compound of claim 37, wherein R7A is methyl.

### Claim 39 (depends on 38)

The compound of claim 38, wherein R3 is —C(O)NHR3A.

### Claim 40 (depends on 39)

The compound of claim 39, wherein R3A is a pyrrolidinyl ring substituted by q instances of RC.

### Claim 41 (depends on 40)

The compound of claim 40, wherein the r instances of RC are selected from the group consisting of methyl,

### Claim 42 (depends on 40)

The compound of formula VII of claim 40, wherein r is 2 and the two RC groups on R5A are on adjacent atoms and form a 3-6 membered saturated or partially unsaturated fused heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur.

### Claim 43 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.