# US 10,501,427 B2 · Deuterated 1-piperazino-3-phenyl indanes for treatment of schizophrenia

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- Number: US 10,501,427 B2
- Document ID: US10501427B2
- Status: Granted
- Kind: B2
- Application number: 16/146,625
- Filed: 2018-09-28
- Published: 2019-01-31
- Granted: 2019-12-10
- Earliest claimed: 2011-06-20
- Assignees: H. Lundbeck A/S
- Applicants: H. Lundbeck A/S
- Inventors: Morten Jorgensen; Peter Hongaard Andersen; Klaus Gjervig Jensen
- Web page: https://patentgrep.com/patent/US10501427B2

## CPC

- C07D 295/073: with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- A61K 31/451: having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
- A61K 31/454: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
- A61K 31/4545: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/551: having two nitrogen atoms, e.g. dilazep
- A61K 31/554: having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- C07B 59/002: {Heterocyclic compounds}
- C07C 45/61: by reactions not involving the formation of >C = O groups
- C07C 45/67: by isomerisation; by change of size of the carbon skeleton
- C07D 241/04: having no double bonds between ring members or between ring members and non-ring members
- C07B 2200/05: Isotopically modified compounds, e.g. labelled
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.

## Claims

### Claim 1

A hydrogen fumarate salt of a deuterium enriched compound of formula Y:
wherein,
R1-R10 are independently hydrogen or deuterium, wherein at least two of R1-R10 are deuterium.

### Claim 2 (depends on 1)

The hydrogen fumarate salt of claim 1, wherein the compound is

### Claim 3 (depends on 1)

The hydrogen fumarate salt of claim 1, wherein the compound is

### Claim 4 (depends on 1)

The hydrogen fumarate salt of claim 1, wherein the compound is

### Claim 5 (depends on 1)

The hydrogen fumarate salt of claim 1, wherein the compound is

### Claim 6 (depends on 1)

The hydrogen fumarate salt of claim 1, wherein the compound is