Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—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
  • A61K31/47—Quinolines; Isoquinolines
  • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/06—Antimigraine agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/22—Anxiolytics

Definitions

• the present invention relates to a psychopharmaceutical preparation comprising an aromatic, multi-cyclic compound as active substance, in which both a pyridine ring and a benzene ring are present and to which is bonded an N-alkyl piperidene group.
• a psychopharmaceutical preparation is here understood to mean a preparation which is intended to be prescribed in the case of psychological complaints of diverse nature.
• Psychopharmaceutical preparations therefore find application on a large scale in psychotherapeutic and psychiatric treatments.
• An important role is set aside here for antidepressants which are utilized to positively influence the state of mind of the patient in the case of complaints of a depressive nature.
• Known antidepressants in this respect are agents commercially available under the brand names of Tolvon® and Remeron®, which are based on respectively mianserin hydrochloride and mirtazapine as tetracyclic aromatic active substance.
• the present invention has for its object, among others, to provide a psychopharmaceutical preparation which is able to effectively combat psychological disorders of diverse nature, and more particularly migraine and/or depression.
• a psychopharmaceutical preparation of the type stated in the preamble has according to a first aspect of the invention the feature that the active substance is characterized by the following structural formula:
• Rl represents hydrogen or a group substituted therefor from a collection of an alkyl group, an alkoxy group, a halogen, a hydroxy group, an SH group and trifluoromethyl in the benzene ring;
• R2 represents hydrogen or a group substituted therefor from a collection of an alkyl group and an aralkyl group; and
• R3 represents a single or a double bond.
• This substitution is seen as being responsible for a strong action of the compound as a whole as an antidepressant, in addition to an effective anti-migraine action.
• this substance can be synthesized relatively simply in that the pyridine group desired therein requires only a relatively simple substitution in the peripheral benzene ring thereof.
• a psychopharmaceutical preparation of the type stated in the preamble has according to a second aspect of the invention the feature that the active substance is characterized by the following structural formula:
• Rl represents hydrogen or a group substituted therefor from a collection of an alkyl group, an alkoxy group, a halogen, a hydroxy group, an SH group and trifluoromethyl in the benzene ring;
• R2 represents hydrogen or a group substituted therefor from a collection of an alkyl group and an aralkyl group.
• This tricyclic compound also comprises a pyridine group and has the intended action as antidepressant.
• this preparation with the N-alkyl piperidene group bonded to the tricyclic group, provides a strong action against migraine.
• the invention is herein based on the insight that these active substances have both a strong antidepressant action and an anti-migraine action.
• the invention hereby provides a remedy which can be utilized for both symptoms, which may or may not occur simultaneously.
• the psychopharmaceutical preparation according to the invention has the feature that Rl represents a hydrogen atom or an organic group substituted therefor in the benzene ring and having a chain of a maximum of four carbon atoms.
• the invention relates to an antidepressant comprising the psychopharmaceutical preparation according to the invention as specified above.
• the invention relates to a psychotherapeutic agent against depression and/or headache, in particular migraine, comprising the psychopharmaceutical preparation in accordance with the second aspect of the invention as specified above.
• Rl represents hydrogen in the benzene ring or a group substituted therefor from a collection of an alkyl group, an alkoxy group, a halogen, a hydroxy group, an SH group and trifluoromethyl
• R2 represents hydrogen or a group substituted therefor from a collection of an alkyl group and an aralkyl group
• R3 represents a single or a double bond.
• This compound is mixed with suitable quantities of binder, filler, flavouring and the like for manufacturing tablets therefrom which each contain a fixed dosage of active substance lying typically between 10 and 50 milligrams.
• the active substance is mixed with lactose and vegetable starch and pressed to form different tablets which each contain 30 mg respectively 50 mg of active substance per tablet.
• the tablets are therein provided halfway along with a break line so that the user will be readily able to take a half-dose.
• the relevant tablets are provided with visual markings such as a specific imprint or colour. Both types of tablet are then arranged per dozen in an air-tight blister pack and placed per two blister packs in a cardboard consumer packaging.
• an initial choice is preferably made for a relatively low dosage of for instance 15 mg of active substance per day. If a disorder persists, this dosage can be gradually increased to an optimal level.
• the agent must be used for 2 to 4 weeks and then evaluated in consultation with a doctor.
• Exemplary embodiment 2 Use is made as an active substance of
• Rl represents hydrogen in the benzene ring or a group substituted therefor from a collection of an alkyl group, an alkoxy group, a halogen, a hydroxy group, an SH group and trifluoromethyl
• R2 represents hydrogen or a group substituted therefor from a collection of an alkyl group and an aralkyl group.
• the dihydrochloride of the compound of the first exemplary embodiment is used as active substance. This substance is dissolved in water at a dosage of 10 grams per litre. The liquid is packaged in 50 millilitre bottles which are equipped with a precise drop dispenser. The delivery of the dispenser is set here to 1 millilitre per droplet. A precise individual daily dosage is thus possible in consultation with a doctor.
• the preparation according to the invention can thus be processed as desired into dosages and means of administering other than those described.
• other substitutes can also be applied within the tricyclic compound in order to enhance the effective action and/or reduce possible side effects.
• pharmaceutically acceptable acid addition salts of the intended tricyclic compound can in particular be applied in the preparation.
• the invention generally provides a particularly effective agent against psychological disorders of varying nature.

Landscapes

• Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Neurosurgery (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Neurology (AREA)
• Biomedical Technology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Epidemiology (AREA)
• Pain & Pain Management (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (2)

Publications (1)

Family

ID=35295339

Family Applications (1)

Country Status (2)

Cited By (2)

Citations (8)

• 2004
  • 2004-07-12 NL NL1026634A patent/NL1026634C2/nl not_active IP Right Cessation
• 2005
  • 2005-07-12 WO PCT/NL2005/000502 patent/WO2006006858A1/en active Application Filing

Patent Citations (8)

Non-Patent Citations (3)

Also Published As

Similar Documents

Legal Events