Abstract

The present invention relates in a first aspect to a compound of formula (I) for use in the treatment and/or in prevention of Alzheimer's dementia, wherein the compound of formula (I) is administered in a dosage<20 mg. In a second aspect, the invention relates to a pharmaceutical composition comprising the compound according to the first aspect.

IPC Classes  ?

• A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam

Abstract

In a first aspect the invention relates to a method for identifying a subject suffering from Alzheimer's dementia (AD) or being at risk of developing Alzheimer's dementia, the method comprising: (a) determining in a first body fluid sample of the subject the amount of at least a compound having a mass in gram/mol of 110.0367; (b) determining in a second body fluid sample of the subject the amount of the same compound as in (a); (c) determining the change of the amount of the compound determined according to (a) compared to the respective amount of the compound determined according to (b); (d) analyzing the change as determined in (c) using a computer-implemented prediction algorithm that is capable of predicting AD in a subject based on the compound, whereby a subject suffering from AD or being at risk of developing Alzheimer's dementia is identified if AD is predicted; wherein said first body fluid sample had been obtained prior to administration of thiethylperazine or a pharmaceutically acceptable salt thereof and said second body fluid sample had been obtained after the subject had been administered thiethylperazine or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• 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
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

In a first aspect the invention relates to a method for identifying a subject suffering from Alzheimer's dementia (AD) or being at risk of developing Alzheimer's dementia, the method comprising: (a) determining in a first body fluid sample of the subject the amount of at least a compound having a mass in gram/mol of 110.0367; (b) determining in a second body fluid sample of the subject the amount of the same compound as in (a); (c) determining the change of the amount of the compound determined according to (a) compared to the respective amount of the compound determined according to (b); (d) analyzing the change as determined in (c) using a computer-implemented prediction algorithm that is capable of predicting AD in a subject based on the compound, whereby a subject suffering from AD or being at risk of developing Alzheimer's dementia is identified if AD is predicted; wherein said first body fluid sample had been obtained prior to administration of thiethylperazine or a pharmaceutically acceptable salt thereof and said second body fluid sample had been obtained after the subject had been administered thiethylperazine or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
• 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 present invention relates in a first aspect to a compound of formula (I) for use in the treatment and/or in prevention of Alzheimer's dementia, wherein the compound of formula (I) is administered in a dosage < 20 mg. In a second aspect, the invention relates to a pharmaceutical composition comprising the compound according to the first aspect.

IPC Classes  ?

• A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• A61K 9/00 - Medicinal preparations characterised by special physical form
• 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 present invention relates in a first aspect to a compound of formula (I) for use in the treatment and/or in prevention of Alzheimer's dementia, wherein the compound of formula (I) is administered in a dosage < 20 mg. In a second aspect, the invention relates to a pharmaceutical composition comprising the compound according to the first aspect.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• 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

Goods & Services

Chemical products for the production of viral, retroviral and non-viral vectors. Pharmaceutical and veterinary products; sanitary preparations for medical purposes; dietetic products for medical purposes, food for babies; plasters, materials for dressings; tooth filling materials and dental impression materials; disinfectants; preparations for destroying vermin; fungicides, herbicides; therapeutic and prophylactic pharmaceutical products; chemical preparations for medical, pharmaceutical and veterinary purposes; balms for medical purposes, bandages for sanitary purposes, biological preparations for medical purposes, detergents for medical purposes, diagnostic means for medical purposes, enzymes and enzyme preparations for medical and pharmaceutical purposes, extracts, serums, ferments, oils and fats for medical and pharmaceutical purposes, medical and pharmaceutical preparations for skincare; products for gene therapy; pharmaceutical preparations and substances; small molecules, vaccines, biologicals, enzymes and enzyme preparations, pharmaceuticals for supplying genes to cells, all for medical purposes; viral, retroviral and non-viral vectors as carriers for administering of nucleic acid sequences for medical and veterinary purposes; biochemical and chemical products for use in medicine; pharmaceutical and biochemical products for treating or preventing inflammatory diseases, cancer, infectious diseases, fungal diseases, diseases caused by parasites, eye diseases, diseases of the central and peripheral nervous system, cardiovascular diseases, diseases, affecting the immune system, genetic diseases, single gene disorders, oral diseases, skin-diseases, hair-diseases and aural diseases, bone diseases and blood diseases as well as reproductive system diseases; pharmaceutical and biochemical products for contraception; biochemical and chemical products in the form of pills, tablets, dragées, capsules, creams, suppositories, gases, drops, dispersions, lotions, ointments, fluids, sprays for medical and pharmaceutical purposes; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine; biochemical and chemical preparations for medical purposes in particular those with the active ingredient thiethylperazine, for use in neurodegenerative diseases; biochemical and chemical preparations for medical purposes in particular those with the active ingredient thiethylperazine, for use in dementia disorders and their earlier stages, in particular for use in Alzheimer's disease and mild cognitive impairment; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for prevention against neurodegenerative diseases; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for preventing dementia disorders and their earlier stages, in particular for preventing Alzheimer's disease and mild cognitive impairment; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for the treatment of neurodegenerative diseases; biochemical and chemical preparations for medical purposes in oral administration forms, namely pills, tablets, dragées, capsules, liquids, drops, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of neurodegenerative diseases; biochemical and chemical preparations for medical purposes in oral administration form, namely pills, tablets, dragées, capsules, liquids, drops, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of Alzheimer's disease and mild cognitive impairment; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for the treatment of dementia disorders and their earlier stages, in particular for the treatment of Alzheimer's disease and mild cognitive impairment; biochemical and chemical preparations for medical purposes in parenteral administration form, namely injection solutions and infusion solutions, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of neurodegenerative diseases; biochemical and chemical preparations for medical purposes in parenteral administration forms, namely injection solutions and infusion solutions, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of Alzheimer's disease and mild cognitive impairment.

Goods & Services

Chemical products for the production of viral, retroviral and non-viral vectors. Pharmaceutical and veterinary products; sanitary preparations for medical purposes; dietetic products for medical purposes, food for babies; plasters, materials for dressings; tooth filling materials; dental impression materials; disinfectants; preparations for destroying vermin; fungicides, herbicides; therapeutic and prophylactic pharmaceutical products; chemical preparations for medical, pharmaceutical and veterinary purposes; balms for medical purposes, bandages for sanitary purposes, biological preparations for medical purposes, detergents for medical purposes, diagnostic means for medical purposes, enzymes and enzyme preparations for medical and pharmaceutical purposes, extracts, serums, ferments, oils and fats for medical and pharmaceutical purposes, medical and pharmaceutical preparations for skincare; products for gene therapy; pharmaceutical preparations and substances; small molecules, vaccines, biologicals, enzymes and enzyme preparations, pharmaceutical for genes to cell, all for medical purposes; viral, retroviral and non-viral vectors as carriers, for administering nucleic acid sequences for medical and veterinary purposes; biochemical and chemical products for use in medicine; pharmaceutical and biochemical products for treating of or preventing against inflammatory diseases, cancer, infectious diseases, fungal- diseases, diseases caused by parasites, eye diseases, diseases of the central and peripheral nervous systems, cardiovascular diseases, diseases affecting the immune system, genetic diseases, single gene disorders, oraldiseases, periodonthaldiseases, skindiseases, hairdiseases and eardiseases, bone and blood diseases as well as reproductive system diseases; pharmaceutical and biochemical products for contraception; biochemical and chemical products in the form of pills, tablets, dragées, capsules, creams, suppositories, gases, drops, dispersions, lotions, ointments, fluids, sprays for medical and pharmaceutical purposes; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for use in neurodegenerative diseases; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for use in trinucleotide repeat disorders, in particular for use in Huntington's Chorea; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for preventing neurodegenerative diseases; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for preventing trinucleotide repeat disorders, in particular for preventing Huntington's Chorea; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for the treatment of neurodegenerative diseases; biochemical and chemical preparations for medical purposes, in particular those with the active ingredient thiethylperazine, for the treatment of trinucleotide repeat disorders, in particular for the treatment of Huntington'a chorea; biochemical and chemical preparations for medical purposes in oral administration forms, namely pills, tablets, dragées, capsules, liquids, drops, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of neurodegenerative diseases; biochemical and chemical preparations for medical purposes in oral administration forms, namely pills, tablets, dragées, capsules, liquids, drops, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of trinucleotide repeat disorders; biochemical and chemical preparations for medical purposes in oral administration forms, namely pills, tablets, dragées, capsules, liquids, drops, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of Huntington's Chorea; biochemical and chemical preparations for medical purposes in parenteral administration forms, namely injection solutions and infusion solutions, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of neurodegenerative diseases; biochemical and chemical preparations for medical purposes in parenteral administration forms, namely injection solutions and infusion solutions, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of trinucleotide repeat disorders; biochemical and chemical preparations for medical purposes in parenteral administration forms, namely injection solutions and infusion solutions, in particular including as active ingredient thiethylperazine, for the prevention and/or treatment of Huntington's chorea.

Abstract

The invention relates to a method for the diagnosis or prediagnosis of a β-amyloidopathy or an α-synucleopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter, or for determining the risk of a proband suffering from such an illness, the proband already having accumulated substances transported by the cerebral ABCC1 transporter.

IPC Classes  ?

• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
• A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• C07D 279/24 - [b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom with hydrocarbon radicals, substituted by amino radicals, attached to the ring nitrogen atom
• C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• C07D 279/28 - [b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom with hydrocarbon radicals, substituted by amino radicals, attached to the ring nitrogen atom with other substituents attached to the ring system
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers

Abstract

The invention relates to 2-(R2-thio)-10-[3-(4-R1-piperazin-1-yl)propyl]-10H-phenothiazine according to general formula I, for treating a ß-amyloidopathy or an a-synucleinopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter. The invention also relates to a method for the diagnosis or prediagnosis of a ß-amyloidopathy or an a-synucleopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter, or for determining the risk of a proband suffering from such an illness, the proband already having accumulated substances transported by the cerebral ABCC1 transporter.

IPC Classes  ?

• A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• 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 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

This invention relates to 2- (R2-thio) -10- [3- (4-R1--piperazin-1-yl) propyl]-10H-phenothiazines according to the general formula I, for treating a .beta.-amyloidopathy or .alpha.-synucleinopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter. This invention also relates to a method for the diagnosis or prediagnosis of a .beta.-amyloidopathy or .alpha.-synucleopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter, or for determining the risk of a proband suffering from such an illness, the proband already having accumulated substances transported by the cerebral ABCC1 transporter.

IPC Classes  ?

• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers