# US 10,308,591 B2 · Preparation of (R,R)-fenoterol and (R,R)- or (R,S)-fenoterol analogues and their use in treating congestive heart failure

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- Number: US 10,308,591 B2
- Document ID: US10308591B2
- Status: Granted
- Kind: B2
- Application number: 15/874,747
- Filed: 2018-01-18
- Published: 2018-05-24
- Granted: 2019-06-04
- Earliest claimed: 2006-08-10
- Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services
- Applicants: The United States of America, as represented by the Secretary, Department of Health and Human Services
- Inventors: Irving William Wainer; Weizhong Zhu; Khalid Chakir; Rui-Ping Xiao; Darrell R. Abernethy; Farideh M. Beigi Abhari
- Web page: https://patentgrep.com/patent/US10308591B2

## CPC

- C07C 215/60: the chain having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This disclosure concerns the discovery of (R,R)- and (R,S)-fenoterol analogs which are highly effective at binding β2-adrenergic receptors. Exemplary chemical structures for these analogs are provided. Also provided are pharmaceutical compositions including the disclosed (R,R)-fenoterol and fenoterol analogs, and methods of using such compounds and compositions for the treatment of cardiac disorders such as congestive heart failure and pulmonary disorders such as asthma or chronic obstructive pulmonary disease.

## Claims

### Claim 1

A method for treating congestive heart failure in a subject, comprising:
administering to the subject with the cardiovascular disorder a therapeutically effective amount of a compound having the formula

### Claim 2 (depends on 1)

The method of claim 1, wherein the compound is

### Claim 3 (depends on 1)

The method of claim 1, wherein administering a therapeutically effective amount of the compound comprises administering a pharmaceutical composition comprising the therapeutically effective amount of the compound and at least one pharmaceutically acceptable carrier.

### Claim 4 (depends on 1)

The method of claim 1, wherein administering the therapeutically effective amount of the compound to the subject increases cardiomyocyte contractility.