# US 7,612,088 B2 · Heterocyclic compounds and their use as aldosterone synthase inhibitors

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- Number: US 7,612,088 B2
- Document ID: US7612088B2
- Status: Granted
- Kind: B2
- Application number: 11/597,620
- Filed: 2005-05-27
- Published: 2007-09-06
- Granted: 2009-11-03
- Earliest claimed: 2004-05-28
- Assignees: Speedel Experimenta AG
- Inventors: Peter Herold; Robert Mah; Vincenzo Tschinke; Christoph Schumacher; Michael Quirmbach
- Web page: https://patentgrep.com/patent/US7612088B2

## CPC

- C07D 471/04: Ortho-condensed systems
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/12: for electrolyte homeostasis
- A61P 5/40: Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
- A61P 7/10: Antioedematous agents; Diuretics
- 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 9/12: Antihypertensives
- A61P 13/12: of the kidneys
- A61P 19/04: for non-specific disorders of the connective tissue
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 417/04: directly linked by a ring-member-to-ring-member bond
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The application relates to novel heterocyclic compounds of the general formula (I) in which R, R1, R2, W, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.

## Claims

### Claim 1

A compound of the formula
W is C, or if X is C, is also N;
X is C or N;
Y is C;
Z is a bond;
R a) is hydrogen; or
b) is C1-C8-alkyl, C1-C8-alkoxy, halogen or trifluoromethyl;
R1 is C3-C8-cycloalkyl-C0-C4-alkyl or a saturated, 4-8-membered, monocyclic heterocyclyl-C0-C4-alkyl, each of which is unsubstituted or substituted by 1-4 C1-C8-alkoxy, C1-C8-alkoxycarbonyl, C1-C8-alkyl, C0-C8-alkylcarbonyl, C1-C8-alkylsulfonyl, aryl-C0-C4-alkoxycarbonyl, aryl, cyano, halogen, unsaturated heterocyclyl, oxo, trifluoromethoxy, trifluoromethyl or tri-C1-C4-alkylsilyl, wherein the heterocycle contains 1-3 heteroatoms selected from N, O, and S;
R2 is hydrogen;
n is 0-2; or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The compound according to claim 1, characterized in that it corresponds to the formulae
where the meanings of the substituents R, R1 and R2 are as indicated for compounds of the formula (I) according to claim 1.

### Claim 3 (depends on 1)

The compound according to claim 1, where R is hydrogen or C1-C8-alkyl.

### Claim 4 (depends on 1)

The compound according to claim 1, where n is a number 0 or 1.

### Claim 5 (depends on 2)

The compound according to claim 2, where
R is hydrogen or C1-C8-alkyl;
R1 is C3-C8-cycloalkyl-C0-C4-alkyl or heterocyclyl, in each case optionally substituted by halogen, cyano, trifluoromethyl, heterocyclyl or C0-C8-alkylcarbonyl; and
R2 is hydrogen.

### Claim 6 (depends on 1)

A pharmaceutical product comprising a compound of the formula (I) according to claim 1, and conventional excipients.

### Claim 7 (depends on 2)

The compound according to claim 2, where R is hydrogen or C1-C8-alkyl.

### Claim 8 (depends on 2)

A pharmaceutical product comprising a compound of the formula (Ia), or (Ib) according to claim 2, and conventional excipients.

### Claim 9 (depends on 3)

The compound according to claim 3, where R is hydrogen or methyl.

### Claim 10 (depends on 7)

The compound according to claim 7, where R is hydrogen or methyl.

### Claim 11 (depends on 1)

The compound according to claim 1, wherein the compound is: