1-(4-(2-((1-(3,4-difluorophenyl)-1H-pyrazol-3-Yl)methoxy)ethyl)piperazin-1- Yl)ethanone salts

• US 10,640,468 B2
• Filed: 09/01/2016
• Issued: 05/05/2020
• Est. Priority Date: 09/02/2015
• Status: Active Grant

• Current Assignee: Esteve Pharmaceuticals S.A. (Corporation Quimico Farmaceutica Esteve SA)
• Original Assignee: Esteve Pharmaceuticals S.A. (Corporation Quimico Farmaceutica Esteve SA)
• Inventors: Torrens-Jover, Antoni, Almansa-Rosales, Carmen
• Primary Examiner(s): Yoo, Sun Jae
• Application Number:
  US15/757,177
• Publication Number:
  US 20180251430A1
• Time in Patent Office: 1,342 Days
• CPC Class Codes: A61P 1/12 Antidiarrhoeals
• CPC Class Codes: A61P 17/02 for treating wounds, ulcers, burns, scars, keloids, or the like
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: 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
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 25/32 Alcohol-abuse
• CPC Class Codes: A61P 25/34 Tobacco-abuse
• CPC Class Codes: A61P 25/36 Opioid-abuse
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/06 : Antiarrhythmics
• CPC Class Codes: A61P 9/10 : for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 : Antihypertensives
• CPC Class Codes: C07B 2200/13 : Crystalline forms, e.g. polymorphs
• CPC Class Codes: C07D 231/12 : with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• CPC Class Codes: C07D 403/12 : linked by a chain containing hetero atoms as chain links

Abstract

The present invention relates to 1-(4-(2-((1-(3,4-difluorophenyl)-1H-pyrazol-3-yl)methoxy)ethy)piperazin-1-y)ethanone salts, specifically to the hydrochloride and to the maleate, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of sigma receptor associated diseases.

Claims

1. A crystalline salt of 1-(4-(2-((1-(3,4-difluorophenyl)-1H-pyrazol-3-yl)methoxy)ethyl)piperazin-1-yl)ethanone, wherein said salt is selected from hydrochloride, maleate, fumarate, succinate, oxalate and/or hydrobromide.

2. The crystalline salt according to claim 1 wherein the salt is the hydrochloride salt of 1-(4-(2-((1-(3,4-difluorophenyl)-1H-pyrazol-3-yl)methoxy)ethyl)piperazin-1-yl)ethanone.

3. The crystalline salt according to claim 1 wherein the salt is the maleate salt of 1-(4-(2-((1-(3,4-difluorophenyl)-1H-pyrazol-3-yl)methoxy)ethyl)piperazin-1-yl)ethanone.

4. A pharmaceutical composition comprising at least a crystalline salt according to claim 1.

5. A method for the manufacture of a medicament comprising combining the crystalline salt as defined in claim 1 with a pharmaceutically acceptable excipient.