# US 10,117,954 B2 · Compositions and methods for in vivo imaging

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- Number: US 10,117,954 B2
- Document ID: US10117954B2
- Status: Granted
- Kind: B2
- Application number: 15/581,386
- Filed: 2017-04-28
- Published: 2018-01-18
- Granted: 2018-11-06
- Earliest claimed: 2010-11-22
- Assignees: The General Hospital Corporation
- Applicants: The General Hospital Corporation
- Inventors: Thomas Reiner; Edmund J. Keliher; Ralph Weissleder
- Web page: https://patentgrep.com/patent/US10117954B2

## CPC

- A61K 51/0459: {having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine}
- A61K 49/0021: {the fluorescent group being a small organic molecule}
- A61K 51/1251: {micro- or nanospheres, micro- or nanobeads, micro- or nanocapsules}
- 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

This document relates to compounds useful for targeting PARP1. Also provided herein are methods for using such compounds to detect and image cancer cells.

## Claims

### Claim 1

A compound, which is selected from the group consisting of:
wherein R is Texas Red, a cyanine dye, Alexafluor-680, a BODIPY dye, a xanthene derivatives, a naphthalene dye, a courmarin derivative, an oxadiazole derivative, a pyrene derivative, an oxazine derivative, an acridine derivative, an arylmethine derivative, or a tetrapyrrole derivative.

### Claim 2 (depends on 1)

The compound of claim 1, wherein the compound is selected from the group consisting of:

### Claim 3 (depends on 1)

The compound of claim 1, which is:

### Claim 4 (depends on 1)

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

### Claim 5 (depends on 1)

A method for detecting a cancer in a subject, the method comprising:
(a) administering to the subject an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt form thereof; and
(b) detecting the compound in the subject.

### Claim 6 (depends on 5)

The method of claim 5, wherein detecting the compound comprises performing a detection method selected from the group consisting of, fluorescence detection, chemiluminescence detection, magnetic resonance imaging, nuclear magnetic resonance imaging, positron emission tomography, and single-photon emission computed tomography.

### Claim 7 (depends on 5)

The method of claim 5, wherein the cancer is selected from the group consisting of: pancreatic cancer, ovarian cancer, and breast cancer.

### Claim 8 (depends on 5)

The method of claim 5, wherein the compound is administered before and after surgical removal of the cancer.

### Claim 9 (depends on 1)

A method for monitoring the cancer treatment of a patient, the method comprising:
(a) administering to the patient, prior to a treatment, an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt form thereof, and imaging the patient;
(b) administering to the patient, at a point following treatment, an effective amount the compound of claim 1, or a pharmaceutically acceptable salt thereof, and imaging the patient; and
(c) comparing the image collected in step (a) with the image collected in step (b) to monitor the treatment.

### Claim 10 (depends on 9)

The method of claim 9, wherein the treatment comprises administration of an anti-cancer agent.

### Claim 11 (depends on 1, 9)

The method of claim 9, wherein the method further comprises:
administering to the patient an effective amount of the compound of claim 1 during treatment and imaging the patient.

### Claim 12 (depends on 1)

The compound of claim 1, which is selected from the group consisting of:
wherein R is Texas Red, a cyanine dye, Alexafluor-680, a BODIPY dye, a xanthene derivatives, a naphthalene dye, a courmarin derivative, an oxadiazole derivative, a pyrene derivative, an oxazine derivative, an acridine derivative, an arylmethine derivative, or a tetrapyrrole derivative.

### Claim 13 (depends on 12)

The compound of claim 12, wherein the compound is selected from the group consisting of:

### Claim 14 (depends on 2)

A pharmaceutical composition comprising a compound of claim 2, or a pharmaceutically acceptable salt form thereof and a pharmaceutically acceptable carrier or diluent.

### Claim 15 (depends on 2)

A method for detecting a cancer in a subject, the method comprising:
(a) administering to the subject an effective amount of a compound of claim 2, or a pharmaceutically acceptable salt form thereof; and
(b) detecting the compound in the subject.

### Claim 16 (depends on 15)

The method of claim 15, wherein detecting the compound comprises performing a detection method selected from the group consisting of fluorescence detection, chemiluminescence detection, magnetic resonance imaging, nuclear magnetic resonance imaging, positron emission tomography, and single-photon emission computed tomography.

### Claim 17 (depends on 15)

The method of claim 15, wherein the cancer is selected from the group consisting of: pancreatic cancer, ovarian cancer, and breast cancer.

### Claim 18 (depends on 15)

The method of claim 15, wherein the compound is administered before and after surgical removal of the cancer.

### Claim 19 (depends on 2)

A method for monitoring the cancer treatment of a patient, the method comprising:
(a) administering to the patient, prior to a treatment, an effective amount of a compound of claim 2, or a pharmaceutically acceptable salt form thereof, and imaging the patient;
(b) administering to the patient, at a point following treatment, an effective amount the compound of claim 2, or a pharmaceutically acceptable salt thereof, and imaging the patient; and
(c) comparing the image collected in step (a) with the image collected in step (b) to monitor the treatment.

### Claim 20 (depends on 19)

The method of claim 19, wherein the treatment comprises administration of an anti-cancer agent.

### Claim 21 (depends on 2, 19)

The method of claim 19, wherein the method further comprises: administering to the patient an effective amount of the compound of claim 2 during treatment and imaging the patient.