Therapeutic and imaging agents for targeting myocardial tissue
AssigneeThe Board of Regents of the University of Oklahoma
InventorsVenkateswararao Eeda, Vibhudutta Awasthi
Life of this patent
Estimating the term…
Abstract
Analogs and derivatives of omecamtiv mecarbil (OM), including an 18F-labeled analog, and methods of synthesis thereof. Cardiac myosin targeting vectors comprising a lipid anchoring/solubilizing moiety conjugated to a head made of OM or the OM analog or derivative. Liposomes comprising a cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of treating a cardiac condition or disease in a subject by administering to the subject the cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of synthesizing an 18F-labeled analog of OM.
Claims16
A cardiac myosin targeting vector, comprising:
- a head, and a lipid anchoring/solubilizing moiety conjugated to the head via a linker molecule, wherein the head comprises omecamtiv mecarbil (OM) or an OM analog or derivative selected from the group consisting of:
- where n=2-10,
- where n=1-2000, and
- where
- n=1-2000,
- X=OH, OCH3, F, 18F, and NH2, and
- Z=CH3;
- acetyl;
- carbamoyl;
- —(CH2)pCH3, where p=1-20;
- or HO—(CH2CH2O)q—H, where q=2-2,000.
An omecamtiv mecarbil (OM) analog or derivative, comprising a structure selected from the group consisting of:
- where n=2-10,
- where n=1-2000, and
- where
- n=1-2000,
- X=OH, OCH3, F, 18F, and NH2, and
- Z=CH3;
- acetyl;
- carbamoyl;
- —(CH2)pCH3, where p=1-20;
- or HO—(CH2CH2O)q—H, where q=2-2,000.
A method of treating a cardiac condition or disease in a subject in need of such therapy, comprising administering to the subject (1) a cardiac-treating drug and (2) a cardiac myosin targeting vector, wherein the cardiac myosin targeting vector comprises:
- a head, and a lipid anchoring/solubilizing moiety conjugated to the head via a linker molecule, wherein the head comprises omecamtiv mecarbil (OM) or an OM analog or derivative selected from the group consisting of:
- where n=2-10,
- where n=1-2000, and
- where
- n=1-2000,
- X=OH, OCH3, F, 18F, and NH2, and
- Z=CH3;
- acetyl;
- carbamoyl;
- —(CH2)pCH3, where p=1-20;
- or HO—(CH2CH2O)q—H, where q=2-2,000.
Dependencies are inferred from the claim text.