# US 8,569,286 B2 · Notch pathway signaling inhibitor compound

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- Number: US 8,569,286 B2
- Document ID: US8569286B2
- Status: Granted
- Kind: B2
- Application number: 13/551,681
- Filed: 2012-07-18
- Published: 2013-01-31
- Granted: 2013-10-29
- Earliest claimed: 2011-07-27
- Assignees: Eli Lilly and Company
- Applicants: Philip Arthur Hipskind; Gregory Alan Stephenson
- Inventors: Philip Arthur Hipskind; Gregory Alan Stephenson
- Web page: https://patentgrep.com/patent/US8569286B2

## CPC

- C07K 5/06026: {the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala}
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 471/04: Ortho-condensed systems
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- 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 provides a compound, or a pharmaceutically acceptable salt or hydrate, and a pharmaceutical composition containing said compound, or a pharmaceutically acceptable salt or hydrate, useful as a Notch pathway signaling inhibitor for the treatment of cancer.

## Claims

### Claim 1

A compound of the structure:
or a pharmaceutically acceptable salt or hydrate thereof.

### Claim 2 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt or hydrate thereof, in association with a pharmaceutically acceptable carrier.

### Claim 3 (depends on 1)

A method of treating a cancer which is T-cell acute lymphoblastic leukemia, acute lymphoblastic leukemia, acute myelogenous leukemia, chronic myelogenous leukemia, erythroleukemia, breast cancer, ovarian cancer, melanoma, lung cancer, pancreatic cancer, glioblastoma, colorectal cancer, head and neck cancer, cervical cancer, prostate cancer, liver cancer, squamous cell carcinoma (oral), skin cancer or medulloblastoma in a patient comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt or hydrate.

### Claim 4 (depends on 1)

A method of treating a cancer which is T-cell acute lymphoblastic leukemia, acute lymphoblastic leukemia, chronic myelogenous leukemia, erythroleukemia, breast cancer, ovarian cancer, melanoma, pancreatic cancer, glioblastoma or colorectal cancer in a patient comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt or hydrate thereof.

### Claim 5

A crystalline hydrate of 4,4,4-trifluoro-N-[(1S)-2-[[(7S)-5-(2-hydroxyethyl)-6-oxo-7H-pyrido[2,3-d][3]benzazepin-7-yl]amino]-1-methyl-2-oxo-ethyl]butanamide characterized by an X-ray powder diffraction pattern using CuKα radiation having a peak at 22.97±0.2 degrees 2-theta in combination with one or more peaks at 11.96±0.2, 18.81±0.2, 20.78±0.2 or 21.07±0.2 degrees 2-theta at ambient temperature and relative humidity.

### Claim 6 (depends on 5)

A pharmaceutical composition comprising a compound of claim 5, in association with a pharmaceutically acceptable carrier.