# US 12,594,339 B2 · Lipid prodrugs of JAK inhibitors and uses thereof

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- Number: US 12,594,339 B2
- Document ID: US12594339B2
- Status: Granted
- Kind: B2
- Application number: 17/310,871
- Filed: 2020-02-28
- Published: 2022-04-28
- Granted: 2026-04-07
- Earliest claimed: 2019-02-28
- Assignees: Seaport Therapeutics, Inc.; Monash University
- Applicants: Seaport Therapeutics, Inc.; Monash University
- Inventors: Joseph Bolen; Daniel Kenneth Bonner; Ketki Karanam; Christopher John Porter; Jamie Simpson; Natalie Trevaskis; Dan Zheng; Nathania Leong; Garima Sharma; Mitchell McInerney; Tim Quach; Sifei Han
- Web page: https://patentgrep.com/patent/US12594339B2

## CPC

- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/542: {Carboxylic acids, e.g. a fatty acid or an amino acid}
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/529: forming part of bridged ring systems
- A61P 17/06: Antipsoriatics
- 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 37/00: Drugs for immunological or allergic disorders
- C07D 487/04: Ortho-condensed systems
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, and methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a disclosed lipid prodrug or a pharmaceutical composition thereof.

## Claims

### Claim 1

A compound of Formula VII-b:
or a pharmaceutically acceptable salt thereof, wherein:
R1 and R2 are each —C(O)R3;
each R3 is independently a saturated or unsaturated, straight or branched, optionally substituted C1-37 hydrocarbon chain;
each R4 and R5 is independently hydrogen or C1-4 alkyl optionally substituted with 1, 2, 3, 4, 5, or 6 deuterium or halogen atoms;
wherein at least one R4 is a C1-4 alkyl.

### Claim 2 (depends on 1)

A pharmaceutically acceptable composition comprising a compound according to claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient, carrier, adjuvant, or vehicle.

### Claim 3 (depends on 1)

A method of treating an autoimmune or inflammatory disease, disorder, or condition in a patient in need thereof, comprising administering to the patient an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 3)

The method according to claim 3, wherein the autoimmune or inflammatory disease, disorder, or condition is selected from alopecia areata; ankylosing spondylitis; atopic dermatitis; Crohn's disease; cutaneous lupus erythematosus; dermatomyositis; eczema; eosinophilia; graft versus host disease; hypereosinophilic syndrome; juvenile rheumatoid arthritis; polycythemia vera; primary biliary cholangitis; psoriasis; psoriatic arthritis; rheumatoid arthritis; Sjögren's syndrome; spondylarthrite; systemic lupus erythematosus; ulcerative colitis; uveitis; and vitiligo.

### Claim 5 (depends on 4)

The method according to claim 4, further comprising the step of administering an additional therapeutic agent.

### Claim 6

A compound of Formula I-6:
or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 6)

A method of treating rheumatoid arthritis, ulcerative colitis, ankylosing spondylitis, or psoriatic arthritis in a patient in need thereof, comprising administering to the patient an effective amount of the compound of claim 6, or a pharmaceutically acceptable salt thereof, wherein said rheumatoid arthritis, ulcerative colitis, ankylosing spondylitis, or psoriatic arthritis is treated in the patient.