# US 10,369,120 B2 · T type calcium channel inhibitors

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- Number: US 10,369,120 B2
- Document ID: US10369120B2
- Status: Granted
- Kind: B2
- Application number: 14/933,237
- Filed: 2015-11-05
- Published: 2016-05-19
- Granted: 2019-08-06
- Earliest claimed: 2004-08-20
- Assignees: University of Virginia Patent Foundation
- Applicants: University of Virginia Patent Foundation
- Inventors: Lloyd S. Gray; Timothy L. Macdonald; Doris M. Haverstick; Jaclyn R. Patterson; William F. McCalmont
- Web page: https://patentgrep.com/patent/US10369120B2

## CPC

- A61K 31/14: Quaternary ammonium compounds, e.g. edrophonium, choline (betaines A61K31/205)
- A61K 31/085: having an ether linkage to aromatic ring nuclear carbon
- A61K 31/12: Ketones
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/138: Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine (atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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 25/02: for peripheral neuropathies
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/10: for petit-mal
- A61P 25/12: for grand-mal
- A61P 27/00: Drugs for disorders of the senses
- A61P 27/02: Ophthalmic agents
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 217/58: with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
- C07C 217/60: linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
- C07C 217/62: linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
- 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

## Abstract

The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, wherein R1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; Z is NH, NCH3, O, S, or CH2; Y is NH, O, or CH2 with the proviso that Y and Z are not the same; R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; and R3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.

## Claims

### Claim 1

A method for treating a disease or condition selected from the group consisting of hypertension and cardiac arrhythmia in a mammal in need of such treatment comprising administering to the mammal a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof, wherein the compound has a structure represented by Formula (1):
wherein
R1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;
Z is NH, O, S, or CH2;
R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;
m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 4-9; and
R3 is chloro or C1-C4 alkoxy.

### Claim 2 (depends on 1)

The method according to claim 1, wherein R1 is hydroxy or C1-C4 alkoxy; Z is NH or O; and R2 is H, halo, NH2 or hydroxy.

### Claim 3

A method for treating a disease or condition selected from the group consisting of unstable angina, hypertension, epilepsy, neuropathic pain, petit mal seizure, absence seizure, age related, macular degeneration and cancer in a mammal in need of such treatment comprising administering to the mammal a therapeutically effective amount of a T type calcium channel inhibitor or a pharmaceutically acceptable salt of said inhibitor, wherein the inhibitor is selected from the group consisting of the following compounds: