# US 8,541,448 B2 · Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders

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- Number: US 8,541,448 B2
- Document ID: US8541448B2
- Status: Granted
- Kind: B2
- Application number: 13/172,394
- Filed: 2011-06-29
- Published: 2012-10-18
- Granted: 2013-09-24
- Earliest claimed: 2008-12-31
- Assignees: Ardelyx, Inc.
- Applicants: Dominique Charmot; Jeffrey W. Jacobs; Michael Robert Leadbetter; Marc Navre; Christopher Carreras; Noah Bell
- Inventors: Dominique Charmot; Jeffrey W. Jacobs; Michael Robert Leadbetter; Marc Navre; Christopher Carreras; Noah Bell
- Web page: https://patentgrep.com/patent/US8541448B2

## CPC

- A61K 31/4725: containing further heterocyclic rings
- A61K 31/18: Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63)
- A61K 31/472: Non-condensed isoquinolines, e.g. papaverine
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 31/662: Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/55: the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 7/10: Antioedematous agents; Diuretics
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 9/12: Antihypertensives
- C07C 311/29: having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07D 215/14: Radicals substituted by oxygen atoms
- C07D 217/04: with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
- C07D 217/14: other than aralkyl radicals
- C07D 217/16: substituted by oxygen atoms
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07F 9/3808: {Acyclic saturated acids which can have further substituents on alkyl}
- C07F 9/3834: {Aromatic acids (P-C aromatic linkage)}
- C07F 9/3882: {Arylalkanephosphonic acids (C07F9/3839 takes precedence)}
- C07F 9/5765: {condensed with carbocyclic rings or carbocyclic ring systems}
- C07F 9/60: Quinoline or hydrogenated quinoline ring systems
- C07F 9/65583: {each of the hetero rings containing nitrogen as ring hetero atom}
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.

## Claims

### Claim 1

A compound or a pharmaceutically acceptable salt thereof, wherein the compound has the structure:

### Claim 2 (depends on 1)

The compound of claim 1.

### Claim 3 (depends on 1)

A pharmaceutically acceptable salt of the compound of claim 1.

### Claim 4 (depends on 3)

The pharmaceutically acceptable salt of claim 3, wherein the pharmaceutically acceptable salt is:

### Claim 5

A pharmaceutical composition, wherein the composition comprises:
a compound or a pharmaceutically acceptable salt thereof, wherein the compound corresponds to the structure:
and
a pharmaceutically acceptable carrier, diluent or excipient.

### Claim 6 (depends on 5)

The pharmaceutical composition of claim 5, wherein the pharmaceutically acceptable salt is: