IP Library Granted Patent US 9,273,032
Granted Patent B2
US 9,273,032 · App. 13/279,876 · Granted Mar 1, 2016

Photolabile compounds

Inventors: Roberto Etchenique (Buenos Aires, AR); Rafael Yuste (New York, NY); Luis Baraldo (Buenos Aires, AR)
Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
C07D401/14
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,273,032
App. No.
13/279,876
Granted
Mar 1, 2016
Kind
B2
Abstract

The present invention describes photolabile compounds and methods for use of the compounds. The photolabile compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect.

Claims (22)

1. A compound of Formula IVb:

wherein:

L 1 is 4-aminopyridine, whose pyridyl nitrogen atom forms a bond with Ru;

L 2 is (R 2 ) 3 P, wherein each R 2 is phenyl, and m is 2;

R 1 to R 8 are independently —H, —C 1 -C 18 alkyl; —NH 2 , —COOH, —(C 1 -C 18 alkyl)-O—(C 1 -C 18 alkyl), or —OC(O)(C 1 -C 18 alkyl); and

X is Cl − , F − , Br − , I − , PF 6 − , CF 3 SO 3 − , (C 1 -C 18 alkyl)-CO 2 − , or (C 1 -C 18 alkyl)-SO 3 − .

2. A method for releasing an organic molecule from a photolabile compound, comprising:

exposing a compound of claim 1 to light under conditions sufficient to release the organic molecule, wherein the organic molecule is 4-aminopyridine (4-AP).

3. A method for making an organic molecule bioavailable to a subject, comprising:

(a) administering a compound of claim 1 to the subject; and

(b) exposing the compound to light under conditions sufficient to release the organic molecule from the compound, thereby making the organic molecule bioavailable to the subject, wherein the organic molecule is 4-aminopyridine (4-AP).

4. The method of claim 3 , wherein the light is sunlight, photo-optic light, or laser light.

5. The method of claim 3 , wherein the light is visible light or infrared light.

6. The method of claim 3 , wherein the exposing occurs at the site of a tumor, cancer, or neoplasm.

7. The method of claim 3 , wherein the administering occurs intravenously, topically, intradermally, intramuscularly, transdermally, subcutaneously, intranasally, parenterally, intrathecally, vaginally, rectally, colorectally, orally, intracranially, retroorbitally, intrasternally, or by injection.

8. A composition comprising a compound of claim 1 and a physiologically acceptable carrier, vehicle, diluent, or excipient.

9. A kit comprising a compound of claim 1 and instructions for use of the compound.

10. A method for assaying an organic molecule, comprising exposing a photolabile compound of claim 1 to light under conditions sufficient to release the organic molecule from the photolabile compound, and determining an effect of the organic molecule on the biological sample, wherein the organic molecule is 4-aminopyridine (4-AP).

11. A method for protecting an organic molecule from an effect of an enzyme, comprising:

allowing the organic molecule and a compound of Formula IVb′:

wherein m is 2; R 1 to R 8 are independently —H, —C 1 -C 18 alkyl; —NH 2 , —COOH, —(C 1 -C 18 alkyl)-O—(C 1 -C 18 alkyl), or —OC(O)(C 1 -C 18 alkyl); and X is Cl − , F − , Br − , I − , PF 6 − , CF 3 SO 3 − , (C 1 -C 18 alkyl)- CO 2 − , or (C 1 -C 18 alkyl)-SO 3 − ,

to react under conditions sufficient to make a compound of claim 1 , wherein the organic molecule is 4-aminopyridine, whose pyridyl nitrogen atom forms a bond with Ru.

Assignments (1)
CONFIRMATORY LICENSE Recorded Jun 20, 2012
From: COLUMBIA UNIV NEW YORK MORNINGSIDE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 028407/0611 →
Continuity (3)
Division 10585013
Provisional Application 60532976 · Dec 29, 2003
Related Publication 20120116287A1 · May 10, 2012