# US 11,078,195 B2 · Compound for inhibiting nicotinamide phosphoribosyltransferase and composition containing same

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- Number: US 11,078,195 B2
- Document ID: US11078195B2
- Status: Granted
- Kind: B2
- Application number: 16/085,774
- Filed: 2017-03-17
- Published: 2020-08-06
- Granted: 2021-08-03
- Earliest claimed: 2016-03-17
- Assignees: Checkmate Therapeutics Inc.
- Applicants: Checkmate Therapeutics Inc.
- Inventors: Hyun Seok Kim; Gyoon Hee Han
- Web page: https://patentgrep.com/patent/US11078195B2

## CPC

- A61P 35/00: Antineoplastic agents
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- A61K 31/47: Quinolines; Isoquinolines
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61P 37/00: Drugs for immunological or allergic disorders
- C07D 209/14: Radicals substituted by nitrogen atoms, not forming part of a nitro radical
- C07D 213/82: in position 3
- C07D 277/82: Nitrogen atoms
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 403/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 417/12: linked by a chain containing hetero atoms as chain links
- C07D 417/14: containing three or more hetero rings
- C07D 419/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D 498/04: Ortho-condensed systems
- C07D 513/04: Ortho-condensed systems
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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)

## Abstract

The present invention relates to a novel compounds for inhibiting nicotinamide phosphoribosyltransferase (NamPT), a composition comprising the same, and various uses thereof.

## Claims

### Claim 1

A compound selected from a compound represented by following Chemical Formula 5, a pharmaceutically acceptable salt, an optical isomer, a hydrate and a solvate thereof:
wherein in Chemical Formula 5,
X1 is N;
X2 is C(H);
p is an integer of 1 to 3;
L6 is a direct bond; and
R17 is represented by Chemical Formulae 3, a1 or a4:
in Chemical Formula 3,
Y1 is O;
Y2 is N;
Z1, Z2 and Z4 are C(H);
R21 is hydrogen or C1˜C6 alkyl group;
Z3 is C(C1˜C6 alkyl;
wherein in Chemical Formula a1,
* is a bonding site;
o is an integer of 0 to 2;
R23 can be selected from the group consisting of halogen, nitro group, C6˜C14 alkyl group, in case that the R23 is plural, they can be the same as or different from each other;
wherein in Chemical Formula a4,
* is a bonding site;
O is an integer of O or 2;
R23 is selected from the group consisting of a halogen, a nitro group and C6˜C14 aryl group, in case that the R23 is plural, they can be the same as or different from each other.

### Claim 2 (depends on 1)

The compound of claim 1, wherein the compound is selected from the group of following compounds:
4) N-(4-(5-methylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;
5) N-(4-(5-ethylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;
7) N-(4-(5-isopropylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;
10) N-(4-(6-chlorobenzo[d]oxazol-2-yl)benzyl)nicotinamide;
11) N-(4-(6-nitrobenzo[d]oxazol-2-yl)benzyl)nicotinamide;
12) N-(4-(5-phenylbenzo[d]oxazol-2-yl)benzyl)nicotinamide;
13) N-(4-(naphtho[2,3-d]oxazol-2-yl)benzyl)nicotinamide.

### Claim 3 (depends on 1)

A pharmaceutical composition for preventing or treating NamPT-related diseases, comprising the compound of claim 1 as an active ingredient.

### Claim 4 (depends on 3)

The pharmaceutical composition of claim 3, wherein the NamPT-related diseases are selected from the group consisting of cancer, viral infection, human immunodeficiency virus, hepatitis virus, herpes virus, herpes simplex, inflammatory disorder, irritable bowel syndrome, inflammatory bowel disease, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, osteoarthritis, osteoporosis, dermatitis, atopic dermatitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, graft versus host disease, Alzheimer's disease, cerebrovascular accident, atherosclerosis, diabetes, glomerulonephritis and metabolic syndrome.