Abstract

The subject invention provides a method for treating a subject afflicted with Rett syndrome comprising administering to the subject an effective amount of pridopidine so as to thereby treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

Abstract

This application provides a composition comprising pridopidine or pharmaceutically acceptable salt thereof and at least one of compounds 1-8 (described herein) or pharmaceutically acceptable salt thereof for use in the treatment of neurodegenerative eye disease, symptoms thereof, and additional neurodegenerative disorders.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/28 - Drugs for disorders of the nervous system 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
• A61P 27/06 - Antiglaucoma agents or miotics

Abstract

Provided herein a method of treating Juvenile Huntington disease in a subject in need thereof comprising orally administering a pharmaceutical composition comprising pridopidine and/or its analog or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

Disclosed herein are methods treating prodromal HD in a subject, wherein the subject has at least 36 CAG repeats in the huntingtin (Htt) gene, wherein the method comprises administering a composition comprising pridopidine or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

Provided herein is a method for treating a human subject afflicted with ALS by administering to the subject a therapeutically effective amount of pridopidine or pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

The invention provides a method of treating a subject afflicted with a dystonia, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system

Abstract

The invention provides a method of reducing anxiety and/or depression in a subject comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine effective to reduce anxiety and/or depression in a subject.

IPC Classes  ?

• A61K 31/4453 - Non-condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61P 25/22 - Anxiolytics
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61P 25/24 - Antidepressants

Abstract

The subject invention provides a modified release solid oral dosage form comprising a therapeutically effective amount of Pridopidine or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable rate controlling excipient, wherein the solid oral dosage form provides an in vivo plasma pridopidine concentration profile having a Mean Cmax of about 1,400 ng/ml or less. The subject invention also provides a method of treating an individual afflicted with a neurodegenerative disease or disease related to dopamine, comprising once daily administration of a modified release solid oral dosage form.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61K 9/20 - Pills, lozenges or tablets

Abstract

The subject invention provides a method for treating a subject afflicted with Rett syndrome comprising administering to the subject a pharmaceutical composition comprising pridopidine or pharmaceutical acceptable salts and at least one of compounds or pharmaceutical acceptable salt thereof disclosed herein, so as to thereby treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The invention provides a method of reducing anxiety and/or depression in a subject comprising administering to the subject a pharmaceutical composition comprising pridopidine or pharmaceutical acceptable salts and at least one of compounds 1-8 or pharmaceutical acceptable salt thereof described herein, effective to reduce anxiety and/or depression in a subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

Provided herein a method of maintaining, improving, or lessening the decline of functional capacity, cognition, motor function and quality of life of a subject afflicted with Huntington disease, including those afflicted with early-stage Huntington disease (HD1 and HD2, TFC 7-13) by orally administering to the subject a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

Provided herein processes and intermediates for the preparation of pridopidine.

IPC Classes  ?

• C07D 211/04 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
• C07D 211/68 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
• C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• C07D 213/127 - Preparation from compounds containing pyridine rings
• C07D 213/133 - Preparation by dehydrogenation of hydrogenated pyridine compounds
• C07D 213/16 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
• C07D 213/06 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
• B01J 23/42 - Platinum
• B01J 23/44 - Palladium
• C08K 5/49 - Phosphorus-containing compounds

Abstract

This invention provides a method of maintaining, improving or lessening the decline of functional capacity or motor function in a human patient in a human patient with Huntington disease (HD) comprising orally administering to the patient a pharmaceutical composition comprising pridopidine.

IPC Classes  ?

• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

Provided herein is a method for treating a human subject afflicted with ALS by administering to the subject a therapeutically effective amount of pridopidine or pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

This invention provides a method of maintaining functional capacity, improving functional capacity, or lessening the decline of functional capacity in a human patient comprising periodically orally administering to the patient a pharmaceutical composition comprising pridopidine such that a dose of 90 mg of pridopidine is administered to the patient per day, so as to thereby maintain functional capacity, improve functional capacity, or lessen the decline of functional capacity in the human patient.

IPC Classes  ?

• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

The subject invention provides a method for treating a subject afflicted with Rett syndrome comprising administering to the subject an effective amount of pridopidine so as to thereby treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

Abstract

This application provides a method of treating a subject afflicted with a neurodegenerative diseases comprising administering to the subject an amount of pridopidine and one of analogs 1-8 effective to treat the subject, pharmaceutical composition and uses and applications thereof.

IPC Classes  ?

• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61P 27/02 - Ophthalmic agents
• A61P 27/06 - Antiglaucoma agents or miotics

Abstract

This application provides a method of treating a subject afflicted with a neurodegenerative diseases comprising administering to the subject an amount of pridopidine and one of analogs 1-8 effective to treat the subject, pharmaceutical composition and uses and applications thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61P 27/02 - Ophthalmic agents
• A61P 27/06 - Antiglaucoma agents or miotics

Abstract

This invention provides a method of treating depression or anxiety in a human subject by administering a composition comprising pridopidine or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/24 - Antidepressants
• A61P 25/22 - Anxiolytics

Goods & Services

Pharmaceutical preparations for the prevention and treatment of neurodegenerative diseases and disorders; pharmaceutical preparations for the prevention and treatment of neurodevelopmental conditions and diseases; pharmaceutical preparations for the prevention and treatment of peripheral nervous system diseases and disorders; pharmaceutical preparations for the treatment and prevention of diseases and disorders of the central nervous system; pharmaceutical preparations for the prevention and treatment of Huntington disease and other neurological disorders.

Goods & Services

Pharmaceutical preparations for the prevention and treatment of neurodegenerative diseases and disorders; pharmaceutical preparations for the prevention and treatment of neurodevelopmental conditions and diseases; pharmaceutical preparations for the prevention and treatment of peripheral nervous system diseases and disorders; pharmaceutical preparations for the treatment and prevention of diseases and disorders of the central nervous system; pharmaceutical preparations for the prevention and treatment of Huntington disease and other neurological disorders.

Abstract

The subject invention provides a method for treating, reducing the incidence, suppressing or inhibiting a viral infection, disease, disorder or symptoms thereof in a subject in need thereof comprising administering to the subject a selective S1R agonist. In another aspect, the viral disease is COVID-19, and the selective S1R agonist is pridopidine or pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 31/14 - Antivirals for RNA viruses

Goods & Services

(1) Pharmaceutical preparations for the prevention and treatment of neurodegenerative diseases and disorders; pharmaceutical preparations for the prevention and treatment of neurodevelopmental conditions and diseases; pharmaceutical preparations for the prevention and treatment of peripheral nervous system diseases and disorders; pharmaceutical preparations for the treatment and prevention of diseases and disorders of the central nervous system; pharmaceutical preparations for the prevention and treatment of Huntington disease and other neurological disorders.

Goods & Services

Pharmaceutical preparations for the prevention and treatment of neurodegenerative diseases and disorders; pharmaceutical preparations for the prevention and treatment of neurodevelopmental conditions and diseases; pharmaceutical preparations for the prevention and treatment of peripheral nervous system diseases and disorders; pharmaceutical preparations for the treatment and prevention of diseases and disorders of the central nervous system; pharmaceutical preparations for the prevention and treatment of Huntington disease and other neurological disorders

Goods & Services

Pharmaceutical preparations for the prevention and treatment of neurodegenerative diseases and disorders; pharmaceutical preparations for the prevention and treatment of neurodevelopmental conditions and diseases; pharmaceutical preparations for the prevention and treatment of peripheral nervous system diseases and disorders; pharmaceutical preparations for the treatment and prevention of diseases and disorders of the central nervous system; pharmaceutical preparations for the prevention and treatment of Huntington disease and other neurological disorders

Goods & Services

(1) Pharmaceutical preparations for the prevention and treatment of neurodegenerative diseases and disorders; pharmaceutical preparations for the prevention and treatment of neurodevelopmental conditions and diseases; pharmaceutical preparations for the prevention and treatment of peripheral nervous system diseases and disorders; pharmaceutical preparations for the treatment and prevention of diseases and disorders of the central nervous system; pharmaceutical preparations for the prevention and treatment of Huntington disease and other neurological disorders.

Abstract

Disclosed herein are methods treating prodromal HD in a subject, wherein the subject has at least 36 CAG repeats in the huntingtin (Htt) gene, wherein the method comprises administering a composition comprising pridopidine or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

Disclosed herein are methods treating prodromal HD in a subject, wherein the subject has at least 36 CAG repeats in the huntingtin (Htt) gene, wherein the method comprises administering a composition comprising pridopidine or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

The invention provides a method of treating a subject afflicted with fragile X syndrome (FXS) or a FXS related disorder, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The subject invention provides a method for treating Parkinsonism or symptoms thereof by low dose pridopidine.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/16 - Anti-Parkinson drugs

Abstract

The subject invention provides a method for treating a subject afflicted with Rett syndrome comprising administering to the subject a pharmaceutical composition comprising pridopidine or pharmaceutical acceptable salts and at least one of compounds 1-8 or pharmaceutical acceptable salt thereof disclosed herein, so as to thereby treat the subject.

IPC Classes  ?

• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The subject invention provides a method for treating a subject afflicted with Rett syndrome comprising administering to the subject a pharmaceutical composition comprising pridopidine or pharmaceutical acceptable salts and at least one of compounds 1-8 or pharmaceutical acceptable salt thereof disclosed herein, so as to thereby treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system

Abstract

The invention provides a method of reducing anxiety and/or depression in a subject comprising administering to the subject a pharmaceutical composition comprising pridopidine or pharmaceutical acceptable salts and at least one of compounds 1-8 or pharmaceutical acceptable salt thereof described herein, effective to reduce anxiety and/or depression in a subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

The invention provides a method of reducing anxiety and/or depression in a subject comprising administering to the subject a pharmaceutical composition comprising pridopidine or pharmaceutical acceptable salts and at least one of compounds 1-8 or pharmaceutical acceptable salt thereof described herein, effective to reduce anxiety and/or depression in a subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants
• A61P 25/28 - Drugs for disorders of the nervous system 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
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

Abstract

This application provides a method of treating a subject afflicted with a neurodegenerative eye disease comprising administering to the subject an amount of pridopidine effective to treat the subject, pharmaceutical composition and uses and applications thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 27/06 - Antiglaucoma agents or miotics
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

This invention provides a composition comprising pridopidine or pharmaceutically acceptable salt thereof and at least one of compounds 1-8: This invention provides a composition comprising pridopidine or pharmaceutically acceptable salt thereof and at least one of compounds 1-8: This invention provides a composition comprising pridopidine or pharmaceutically acceptable salt thereof and at least one of compounds 1-8: or a pharmaceutically acceptable salt thereof; and to methods of use thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• C07D 211/52 - Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/42 - Oxygen atoms attached in position 3 or 5
• G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups

Abstract

The subject invention provides a method for treating, reducing the incidence, suppressing or inhibiting a viral infection, disease, disorder or symptoms thereof in a subject in need thereof comprising administering to the subject a selective SIR agonist. In another aspect, the viral disease is COVID-19, and the selective SIR agonist is pridopidine or pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 31/12 - Antivirals
• A61P 31/14 - Antivirals for RNA viruses

Abstract

The subject invention provides a method for treating, reducing the incidence, suppressing or inhibiting a viral infection, disease, disorder or symptoms thereof in a subject in need thereof comprising administering to the subject a selective SIR agonist. In another aspect, the viral disease is COVID-19, and the selective SIR agonist is pridopidine or pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 31/12 - Antivirals
• A61P 31/14 - Antivirals for RNA viruses

Abstract

A method of treating a human patient afflicted with Huntington's disease, comprising periodically orally administering to the patient a pharmaceutical composition comprising pridopidine, its analog or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/28 - Drugs for disorders of the nervous system 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
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The invention provides a method of treating a subject afflicted with a drug-induced movement disorder including levodopa-induced dyskinesia comprising periodically administering to the subject in need thereof an amount of pridopidine or pharmaceutically acceptable salt thereof effective to treat the subject. The invention further provides a method of treating a subject at risk of developing a drug-induced movement disorder, including levodopa-induced dyskinesia.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61P 25/16 - Anti-Parkinson drugs
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]

Abstract

Provided herein is a method for treating a human subject afflicted with ALS by administering to the subject a therapeutically effective amount of pridopidine or pharmaceutically acceptable salt thereof in combination with sodium phenylbutyrate (PB), tauroursodeoxy cholic acid, combination of sodium phenylbutyrate (PB )/tauroursodeoxy cholic acid (i.e. AMX0035), Zilucoplan, Verdiperstat, CNM-Au8 nanocrystalline gold, SLS-005 (trehalose), IC14 or combination thereof as combination or add-on therapy.

IPC Classes  ?

• A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
• A61K 33/242 - GoldCompounds thereof
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 31/7016 - Disaccharides, e.g. lactose, lactulose
• A61K 38/12 - Cyclic peptides
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

Provided herein is a method for treating a human subject afflicted with ALS by administering to the subject a therapeutically effective amount of pridopidine or pharmaceutically acceptable salt thereof in combination with sodium phenylbutyrate (PB), tauroursodeoxy cholic acid, combination of sodium phenylbutyrate (PB )/tauroursodeoxy cholic acid (i.e. AMX0035), Zilucoplan, Verdiperstat, CNM-Au8 nanocrystalline gold, SLS-005 (trehalose), IC14 or combination thereof as combination or add-on therapy.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 38/12 - Cyclic peptides
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 33/242 - GoldCompounds thereof
• A61K 31/7016 - Disaccharides, e.g. lactose, lactulose
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

The subject invention provides a method for treating a subject afflicted with a disease, disorder, or condition associated with mitochondrial dysfunction or ER stress, comprising administering to the subject a composition comprising pridopidine or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

This invention is directed to a method of treating a human patient afflicted with Huntington disease and/or symptoms thereof, comprising administering to the patient a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof and an analog thereof or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61P 25/00 - Drugs for disorders of the nervous system
• C07D 211/18 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
• C07D 211/20 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/30 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
• C07D 211/42 - Oxygen atoms attached in position 3 or 5
• C07D 211/52 - Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
• C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• C07D 295/04 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
• C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
• C07D 405/02 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings

Abstract

This invention is directed to a method of treating a human patient afflicted with Huntington disease and/or symptoms thereof, comprising administering to the patient a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof and an analog thereof or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61P 25/00 - Drugs for disorders of the nervous system
• C07D 211/42 - Oxygen atoms attached in position 3 or 5
• C07D 211/52 - Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
• C07D 211/30 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
• C07D 211/18 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
• C07D 211/20 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
• C07D 295/04 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
• C07D 405/02 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings

Abstract

The subject invention provides a method for treating a subject afflicted with a disease or disorder associated with mitochondrial disfunction, comprising administering to the subject a composition comprising pridopidine or pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/00 - Drugs for disorders of the nervous system
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The subject invention provides a method for treating a subject afflicted with a disease or disorder associated with mitochondrial disfunction, cornprising adrninistering to the subject a cornposition comprising pridopidine or pharrnaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine

Abstract

The subject disclosure provides a method and use of a phaimaceutical composition for treating Parkinsonism or symptoms thereof by low dose pridopidine. In particular, the disclosure relates to a pharmaceutical composition for use in preventing, treating, or slowing the progression of Parkinson's Disease associated with a glucocerebrosidase mutation (PD- GBA), the composition comprising pridopidine or pharmaceutically acceptable salt thereof in a dosage of between 1 to 100 mg per day.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/20 - Pills, lozenges or tablets
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/16 - Anti-Parkinson drugs

Abstract

The subject invention provides a method for treating Parkinsonism or symptoms thereof by low dose pridopidine.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/16 - Anti-Parkinson drugs
• A61K 9/20 - Pills, lozenges or tablets
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The subject invention provides a solid unit dosage form comprising pridopidine or pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient, wherein the dosage form has a volume and wherein the ratio of the amount of pridopidine to the volume of the dosage form is 135-600 mg/ml.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

Provided herein is a method for treating a human subject afflicted with ALS by administering to the subject a therapeutically effective amount of pridopidine as monotherapy or together with riluzole, edaravone, combination of dextromethorphan/quinidine, sodium phenylbutyrate (PB), tauroursodeoxycholic acid or combination of sodium phenylbutyrate (PB)/tauroursodeoxycholic acid (i.e. AMX0035) as combination or add-on therapy.

IPC Classes  ?

• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
• A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/4748 - QuinolinesIsoquinolines forming part of bridged ring systems
• A61K 31/49 - Cinchonan derivatives, e.g. quinine

Abstract

The invention provides a method of treating a subject afflicted with a drug-induced movement disorder including levodopa-induced dyskinesia comprising periodically administering to the subject in need thereof an amount of pridopidine in combination with one or more additional therapeutic agent effective to treat the subject. The invention further provides a method of treating a subject at risk of developing a drug-induced movement disorder, including levodopa-induced dyskinesia. The invention also provides pharmaceutical compositions suitable for carrying out these methods and kits containing such pharmaceutical compositions.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61K 31/13 - Amines, e.g. amantadine
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
• A61K 31/49 - Cinchonan derivatives, e.g. quinine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
• A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone

Abstract

This invention provides a method of improving cognitive function in a subject comprising periodically administering to the subject an amount of pridopidine or a pharmaceutically acceptable salt thereof effective to improve a cognitive function in the subject. The invention also provides a method of treating a subject afflicted with Alzheimer's disease, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine or a pharmaceutically acceptable salt thereof effective to treat the subject.

IPC Classes  ?

• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/28 - Drugs for disorders of the nervous system 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
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

This invention provides an isolated compound having the structure: or a salt thereof, processes for making the same and to compositions comprising pridopidine with these compounds.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• C07D 211/52 - Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/42 - Oxygen atoms attached in position 3 or 5
• G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups

Abstract

This invention relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a dopaminergic stabilizer known as Pridopidine, and an inhibitor of the vesicular monoamine transporter type 2 (VMAT) known as Tetrabenazine. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for improving the symptomatic therapeutic effects, and for reducing the adverse effects, of Tetrabenazine in the treatment of movement disorders, and in articular movement disorders associated with Huntington's disease, Gilles de la Tourette's syndrome, or tardive dyskinesia.

IPC Classes  ?

• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines

Abstract

The invention provides a method of treating a subject afflicted with a drug-induced movement disorder including levodopa-induced dyskinesia comprising periodically administering to the subject in need thereof an amount of pridopidine effective to treat the subject. The invention further provides a method of treating a subject at risk of developing a drug-induced movement disorder, including levodopa-induced dyskinesia. The invention also provides pharmaceutical compositions suitable for carrying out these methods and packages containing such pharmaceutical compositions.

IPC Classes  ?

• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 25/16 - Anti-Parkinson drugs
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]

Abstract

A method of treating a human patient afflicted with Huntington's disease, comprising periodically orally administering to the patient a pharmaceutical composition comprising pridopidine, its analog or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/28 - Drugs for disorders of the nervous system 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
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The invention provides a method of treating a subject afflicted with fragile X syndrome (FXS) or a FXS related disorder, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The invention provides a method of treating a subject afflicted with a dystonia, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The invention provides a method of treating a subject afflicted with a drug-induced movement disorder including levodopa-induced dyskinesia comprising periodically administering to the subject in need thereof an amount of pridopidine effective to treat the subject. The invention further provides a method of treating a subject at risk of developing a drug-induced movement disorder, including levodopa-induced dyskinesia. The invention also provides pharmaceutical compositions suitable for carrying out these methods and packages containing such pharmaceutical compositions.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

Abstract

The subject invention provides a solid unit dosage form comprising pridopidine and at least one pharmaceutically acceptable excipient, wherein the dosage form has a volume and wherein the ratio of the amount of pridopidine to the volume of the dosage form is 135-600 mg/ml.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - DrageesCoated pills or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine

Abstract

Provided herein is a method for treating a human subject afflicted with ALS by administering to the subject a therapeutically effective amount of pridopidine as monotherapy or together with riluzole, edaravone or dextromethorphan/quinidine as combination or add-on therapy.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

The subject invention provides a method of treating a subject afflicted with a neurodegenerative eye disease comprising administering to the subject an amount of pridopidine effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 27/02 - Ophthalmic agents
• A61P 27/06 - Antiglaucoma agents or miotics

Abstract

This invention provides an isolated compound having the structure: or a salt thereof. The invention also provides for a process for preparing 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-4-ol, 1-(3,3-bis(3-(methylsulfonyl)phenyl)propyl)-4-(3-(methylsulfonyl) phenyl)piperidone, 1,4-bis((3-(1-propylpiperidin-4-yl)phenyl)sulfonyl)butane, (3R,4S)-4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-3-ol, 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidine 1-oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine, and 4-(3-(methylsulfonyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine. This invention also provides an impurity or a salt thereof for use, as a reference standard to detect trace amounts of the impurity in a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof. This invention further provides a process for producing a pridopidine drug product comprising obtaining a pridopidine drug substance and. mixing the pridopidine drug substance with suitable excipients so as to produce the pridopidine drug product. This invention also provides a process for producing a pridopidine drug product. This invention also provides a process of distributing a pridopidine drug product.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/52 - Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
• C07D 211/42 - Oxygen atoms attached in position 3 or 5

Abstract

The present invention provides novel deuterated analogs of Pridopidine, i.e. 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine. Pridopidine is a drug substance currently in clinical development for the treatment of Huntington's disease. In other aspects the invention relates to pharmaceutical compositions comprising a deuterated analog of Pridopidine of the invention, and to therapeutic applications of these analogs.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/32 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
• C07B 59/00 - Introduction of isotopes of elements into organic compounds

Abstract

The invention provides a method of treating a subject afflicted with fragile X syndrome (FXS) or a FXS related disorder, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/28 - Drugs for disorders of the nervous system 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
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached

Abstract

The subject invention provides a method for treating a subject afflicted with Rett syndrome comprising administering to the subject an effective amount of pridopidine so as to thereby treat the subject.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - DrageesCoated pills or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system

Abstract

The invention provides a method of treating a subject afflicted with a dystonia, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine

Abstract

This invention provides the use of a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, for reducing, maintaining, or lessening an increase of the concentration of neurofilament light protein in a subject. Also provided is a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, wherein the composition is used to predict clinical responsiveness to pridopidine therapy by evaluating the amount of a neurofilament light protein in a human subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

Abstract

This invention provides a method of maintaining functional capacity, improving functional capacity, or lessening the decline of functional capacity in a human patient comprising periodically orally administering to the patient a pharmaceutical composition comprising pridopidine such that a dose of 90-225 mg of pridopidine is administered to the patient per day, so as to thereby maintain functional capacity, improve functional capacity, or lessen the decline of functional capacity in the human patient.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

This invention provides a method of maintaining functional capacity, improving functional capacity, or lessening the decline of functional capacity in a human patient comprising periodically orally administering to the patient a pharmaceutical composition comprising pridopidine such that a dose of 90-225 mg of pridopidine is administered to the patient per day, so as to thereby maintain functional capacity, improve functional capacity, or lessen the decline of functional capacity in the human patient.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

CA 03015512 2018-08-22 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization 111111110111101110101011111010111110111010111011111001110111011111011110111111 International Bureau (10) International Publication Number (43) International Publication Date WO 2017/147366 Al 31 August 2017 (31.08.2017) WIPO I PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 31/451 (2006.01) A61K 31/4704 (2006.01) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (21) International Application Number: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, PCT/US2017/019266 DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, 24 February 2017 (24.02.2017) KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (25) Filing Language: English NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (26) Publication Language: English RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, (30) Priority Data: ZA, ZM, ZW. 62/299,290 24 February 2016 (24.02.2016) US (84) Designated States (unless otherwise indicated, for every (71) Applicant (for all designated States except BB): TEVA kind of regional protection available): ARIPO (BW, GH, PHARMACEUTICALS INTERNATIONAL GMBH GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, [CH/CH]; Schlusselstrasse 12, 8645 Jona (CH). TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (71) Applicant BB only): TEVA PHARMACEUTICALS DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, USA, INC. [US/US]; 1090 Horsham Road, North Wales, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, PA 19454 (US). SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, (72) Inventors: RUSS, Hermann, Kurt; Zurcherstrasse 37c, GW, KM, ML, MR, NE, SN, TD, TG). 8852 Altendorf (CH). GEVA, Michal; Rozmarin 5, P.o. Published: Box 7253, Even-yehuda (IL). LAUFER, Ralph; Shenkin 55, 6523309 Tel Aviv (IL). ORBACH, Aric; Levona 1, ¨ with international search report (Art. 21(3)) 76350 Rehovot (IL). (74) Agent: GERSHIK, Gary, J.; Cooper & Dunham LLP, 30 Rockefeller Plaza, 20th Floor, New York, NY 10112 (US). = (54) Title: TREATMENT OF NEURODEGENERATIVE EYE DISEASE USING PRIDOPIDINE ' = ''' ;:;.:== ... = ...... === ......... ' ....... ...... =r r= . = .. . left/Normat Eye '"" : ..................... - = .... ..................................................... ...... = ....... ..................... ,..= ....... . .. ,.; õõ ..... k,4 , Right/Disease El = -==¨ cr) , .................................. ... 1-1 fig. I 1-1 (57) Abstract: The subject invention provides a method of treating a subject afflicted with a neurodegenerative eye disease compris - ing administering to the subject an amount of pridopidine effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/4704 - 2-Quinolinones, e.g. carbostyril

Abstract

This invention provides a pridopidine base in a solid form, a method of preparing the solid pridopidine base, and a composition comprising the pridopidine base and phamiaceutically acceptable components. The method comprises providing a solution comprising pridopidine base, washing with water and precipitating the solid pridopidine base. The method provides for less harsh processing conditions and reduces use of harsh chemicals. Additional embodiments comprise lithiation, coupling or vacuum distillation steps. By- product and impurity contents in the composition are reduced.

IPC Classes  ?

• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/20 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
• C07D 211/30 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom

Abstract

This invention provides a pridopidine base in a solid form, a method of preparing the solid pridopidine base, and a composition comprising the pridopidine base including a pharmaceutical composition.

IPC Classes  ?

• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached

Abstract

This invention provides a method of improving cognitive function in a subject comprising periodically administering to the subject an amount of pridopidine or a pharmaceutically acceptable salt thereof effective to improve a cognitive function in the subject. The invention also provides a method of treating a subject afflicted with Alzheimer's disease, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine or a pharmaceutically acceptable salt thereof effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

This invention provides a method of improving cognitive function in a subject comprising periodically administering to the subject an amount of pridopidine or a pharmaceutically acceptable salt thereof effective to improve a cognitive function in the subject. The invention also provides a method of treating a subject afflicted with Alzheimer's disease, comprising periodically administering to the subject a pharmaceutical composition comprising an amount of pridopidine or a pharmaceutically acceptable salt thereof effective to treat the subject.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/52 - Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
• C07D 211/42 - Oxygen atoms attached in position 3 or 5

Abstract

The subject invention provides pridopidine L-tartrate, compositions and a process for manufacture thereof.

IPC Classes  ?

• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07C 59/255 - Tartaric acid
• C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part

Abstract

This invention provides an isolated compound having the structure: The invention also provides for a process for preparing 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-4-ol, 1-(3,3-bis(3-(methylsulfonyl)phenyl)propyl)-4-(3-(methylsulfonyl) phenyl)piperidone, 1,4-bis((3-(1 -propylpiperidin-4-yl)phenyl)sulfonyl)butane, (3R,4S)-4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-3-ol, 4-(3-(methylsulfonyl)phenyl)-l-propylpiperidine 1- oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine, and 4-(3-(methylsulfonyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine. This invention also provides an impurity or a salt thereof for use, as a reference standard to detect trace amounts of the impurity in a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof. This invention further provides a process for producing a pridopidine drug product comprising obtaining a pridopidine drug substance and mixing the pridopidine drug substance with suitable excipients so as to produce the pridopidine drug product. This invention also provides a process for producing a pridopidine drug product. This invention also provides a process of distributing a pridopidine drug product.

IPC Classes  ?

• C07D 211/94 - Oxygen atom, e.g. piperidine N-oxide
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/42 - Oxygen atoms attached in position 3 or 5
• C07D 211/52 - Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4

Abstract

This invention provides an isolated compound having the structure: or a salt thereof. The invention also provides for a process for preparing 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-4-ol, 1-(3,3-bis(3-(methylsulfonyl)phenyl)propyl)-4-(3-(methylsulfonyl) phenyl)piperidone, 1,4-bis((3-(1-propylpiperidin-4-yl)phenyl)sulfonyl)butane, (3R,4S)-4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-3-ol, 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidine 1-oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridne, and 4-(3-(methylsulfonyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine. This invention also provides an impurity or a salt thereof for use, as a reference standard to detect trace amounts of the impurity in a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof. This invention further provides a process for producing a pridopidine drug product comprising obtaining a pridopidine drug substance and mixing the pridopidine drug substance with suitable excipients so as to produce the pridopidine drug product. This invention also provides a process for producing a pridopidine drug product. This invention also provides a process of distributing a pridopidine drug product.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• C07D 211/52 - Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached
• C07D 211/42 - Oxygen atoms attached in position 3 or 5
• G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups

Abstract

The subject invention provides a modified release solid oral dosage form comprising a therapeutically effective amount of Pridopidine or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable rate controlling excipient, wherein the solid oral dosage form provides an in vivo plasma pridopidine concentration profile having a Mean Cmax of about 1,400 ng/ml or less. The subject invention also provides a method of treating an individual afflicted with a neurodegenerative disease or disease related to dopamine, comprising once daily administration of a modified release solid oral dosage form.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/22 - Sustained or differential release type
• A61K 9/28 - DrageesCoated pills or tablets
• A61K 9/36 - Organic coatings containing carbohydrates or derivatives thereof
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

This invention relates to a new salt of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides the pharmaceutically acceptable hydrobromide salt, pharmaceutical compositions comprising this salt, and uses of this salt as a drug substance.

IPC Classes  ?

• A01N 43/00 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• C07D 211/20 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached

Abstract

A method of treating a human patient afflicted with Huntington's disease, comprising periodically orally administering to the patient a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof such that greater than 90 mg of pridopidine is administered to the patient per day.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine

Abstract

This invention provides a method of treating a human patient afflicted with Huntington's disease, comprising periodically orally administering to the patient a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof such that greater than 135 mg of pridopidine is administered to the patient per day. This invention further provides a method of treating a human patient afflicted with Huntington's disease, comprising periodically orally administering to the patient a pharmaceutical composition comprising pridopidine hydrochloride such that greater than 90 mg of pridopidine is administered to the patient per day.

IPC Classes  ?

• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61P 25/28 - Drugs for disorders of the nervous system 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

Abstract

This invention relates to a new crystalline form of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides polymorphic Form II of the Pridopidine hydrochloride salt, a process for the preparation of this polymorphic form, pharmaceutical compositions comprising polymorphic Form II, and methods of uses of this polymorphic form.

IPC Classes  ?

• C07D 211/20 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
• C07D 211/30 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached

Abstract

This invention relates to a new salt of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides the pharmaceutically acceptable hydrobromide salt, pharmaceutical compositions comprising this salt, and uses of this salt as a drug substance.

IPC Classes  ?

• A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• C07D 211/20 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached

Abstract

A compound having the general formula wherein A is selected from the group consisting of to the formation of a compound of the general formula (1) and a compound of the general formula (2) 3 does not represent n-propyl. The invention also relates to a pharmaceutical preparation containing said compound, the use of said compound for the manufacture of a pharmaceutical composition and a method for the treatment of a disorder in the central nervous system of a patient using said compound.

IPC Classes  ?

• C07D 211/94 - Oxygen atom, e.g. piperidine N-oxide
• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine

Abstract

The present invention is directed to processes for the preparation of 4-(3-methanesulfonyl-phenyl)-1-N-propylpiperidine (I) or a pharmaceutically acceptable salt thereof, which comprises: oxidizing a sulfide of the formula (II): with a catalytic oxidizing agent and an oxidant; to give a compound of the formula (III): followed by catalytic reduction of the compound of formula (III).

IPC Classes  ?

• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine

Abstract

The present invention is directed to processes for the preparation of 4-(3- methanesulfonyl-phenyl)-1-N-propylpiperidine (I) or a pharmaceutically acceptable salt thereof, which comprises: oxidizing a sulfide of the formula (II): with a catalytic oxidizing agent and an oxidant; to give a compound of the formula (III): followed by catalytic reduction of the compound of the formula (III).

IPC Classes  ?

• C07D 211/24 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by sulfur atoms to which a second hetero atom is attached