# US 4,393,070 A · Dihydropyridine derivative, and pharmaceutical composition comprising the same

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- Number: US 4,393,070 A
- Document ID: US4393070A
- Status: Granted
- Kind: A
- Application number: 06/213,047
- Filed: 1980-12-04
- Granted: 1983-07-12
- Earliest claimed: 1978-09-08
- Assignees: Fujisawa Pharmaceutical Co., Ltd.
- Inventors: Yoshinari Sato; Tsutomu Teraji
- Web page: https://patentgrep.com/patent/US4393070A

## CPC

- C07D 401/12: linked by a chain containing hetero atoms as chain links
- A61P 9/08: Vasodilators for multiple indications
- 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
- C07C 323/00: Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07D 211/90: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

1,4-dihydropyridine derivatives of the general formula: ##STR1## having vasodilating and anti-hypertensive activity, processes for preparing same, and pharmaceutical compositions thereof for treating cardiovascular diseases.

## Claims

### Claim 1

A compound of the formula: ##STR17## wherein R.sup.1 is cyano or trifluoromethyl,
R.sup.2 is [N-lower alkyl-N-mono- or dihalophenyl(lower)alkyl]amino(lower)alkyl;
R.sup.3 and R.sup.4 are each lower alkyl, and
R.sup.5 is formyl, di(lower) alkoxymethyl or hydroxymethyl, and
pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

A compound according to claim 1, wherein
R.sup.1 is cyano or trifluoromethyl,
R.sup.2 is [N-lower alkyl-N-mono- or dihalophenyl(lower)alkyl]amino(lower)alkyl,
R.sup.3 and R.sup.4 are each lower alkyl and
R.sup.5 is hydroxymethyl, and pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 2)

A compound according to claim 2, wherein
R.sup.2 is [N-lower alkyl-N-mono- or dihalobenzyl]-amino(lower)alkyl, and R.sup.1, R.sup.3, R.sup.4 and R.sup.5 are each as defined in claim 2.

### Claim 4 (depends on 3)

A compound according to claim 3, wherein
R.sup.1 is 2-cyano or 2-trifluoromethyl,
R.sup.2 is 2-(N-methyl-N-4-mono- or 3,4-dichlorobenzylamino)ethyl,
R.sup.3 is ethyl, R.sup.4 is methyl and R.sup.5 hydroxymethyl.

### Claim 5 (depends on 4)

A compound according to claim 4, wherein
R.sup.1 is 2-cyano, R.sup.2 is 2-(N-methyl-N-4-chlorobenzylamino)ethyl, R.sup.3 is ethyl, R.sup.4 is methyl and R.sup.5 is hydroxymethyl, and its hydrochloride.

### Claim 6 (depends on 4)

A compound according to claim 4, wherein
R.sup.1 is 2-trifluoromethyl,
R.sup.2 is 2-(N-methyl-N-3,4-dichlorobenzylamino)ethyl,
R.sup.3 is ethyl,
R.sup.4 is methyl, and
R.sup.5 is hydroxymethyl.

### Claim 7 (depends on 1)

A pharmaceutical composition for treatment of hypertension comprising, as an active ingredient, an effective amount of the compound of claim 1, in association with a nontoxic, pharmaceutically acceptable carrier or excipient.