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WO1996012481A1 - Remede contre l'autisme - Google Patents

Remede contre l'autisme Download PDF

Info

Publication number
WO1996012481A1
WO1996012481A1 PCT/JP1995/002159 JP9502159W WO9612481A1 WO 1996012481 A1 WO1996012481 A1 WO 1996012481A1 JP 9502159 W JP9502159 W JP 9502159W WO 9612481 A1 WO9612481 A1 WO 9612481A1
Authority
WO
WIPO (PCT)
Prior art keywords
autism
therapeutic agent
present
methylaminobutoxy
active ingredient
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/JP1995/002159
Other languages
English (en)
Japanese (ja)
Inventor
Akihiro Tobe
Tadashi Tanaka
Tomoko Tamura
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Mitsubishi Chemical Corp
Original Assignee
Mitsubishi Chemical Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Mitsubishi Chemical Corp filed Critical Mitsubishi Chemical Corp
Publication of WO1996012481A1 publication Critical patent/WO1996012481A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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

Definitions

  • the present invention relates to a therapeutic agent useful for treating autism in children.
  • Childhood autism is the presence of developmental abnormalities and / or disabilities that appear in children younger than three years of age, as well as three aspects of reciprocal social relationships, communication, and limited repetitive behavior.
  • Pervasive Developmental Disorders Qualitative impairments in patterns of mutual social relations and communication, and localized stereotypes, defined by characteristic types of functional abnormalities in all areas. A group of obstacles characterized by repetitive interests and a range of activities.
  • pimozide (“Olap”: Fujisawa Pharmaceutical Co., Ltd.) is adapting to symptoms such as abnormal behaviors such as movements, emotions, motivations, and interpersonal relationships associated with autistic disorders in children.
  • tetrahydrobiopterin is being used in clinical trials.
  • pimozide has problems in administration to children due to its strong side effects, and the usefulness of tetrahydrobiopterin has not yet been established.
  • useful drugs for pediatric autism other than the above drugs, and doctors treat empirically or experimentally with drugs that have not been approved for autism Stays on.
  • an object of the present invention is to provide a therapeutic agent that enables effective drug therapy for pediatric autism.
  • Another object of the present invention is to provide a remedy for pediatric autism with reduced side effects.
  • a therapeutic agent for autism which comprises, as an active ingredient, 2- (4-methylaminobutoxy) diphenylmethane, a hydrate thereof, or a pharmacologically acceptable salt thereof represented by the formula: BEST MODE FOR CARRYING OUT THE INVENTION
  • the therapeutic agent of the present invention is applied to pediatric autism (pediatric autism).
  • pediatric autism aged 4 to 12 years can be treated.
  • Childhood autism is a pervasive developmental disorder, a group of disorders characterized by qualitative impairments in patterns of social relationships and communication, and a range of localized stereotyped, repetitive interests and activities. Of these, those that meet the following diagnostic criteria.
  • the compound of the above formula (I) contained in the therapeutic agent for autism of the present invention is described in Example 1 of JP-B-60-6349 or in columns 4 to 5 of JP-B-2-33689. It can be easily manufactured by the method described above.
  • the active ingredient of the therapeutic agent for autism according to the present invention may be any of the above compounds in a free form, but may be any hydrate thereof, or a physiologically active form of the above compound or any hydrate thereof. Acceptable acid addition salts can also be used.
  • Pharmaceutically acceptable acid addition salts include, for example, mineral salts such as hydrochloride, hydrobromide, hydroiodide, sulfate, nitrate and phosphate, or acetate , Maleate, fumarate, citrate, oxalate, succinate, tartrate, lingate, mandelate, methanesulfonate, p-toluenesulfonate, 10-camphorsulfone Organic acid salts such as acid salts can be mentioned. Among these, it is preferable to use the hydrochloride of the above compound. Hydrochloride is a substance clinically used under the generic name "Bif Hydrochloride X-Melan".
  • the administration form of the therapeutic agent for autism of the present invention is not particularly limited, and it can be administered orally or parenterally. Preferably, it is administered orally.
  • the compound of the formula (I) which is the active ingredient may be used as it is as the therapeutic agent for autism of the present invention. It should be provided in the form of a formulation well known to those skilled in the art, with the addition of pharmaceutically acceptable additives.
  • Pharmaceutically and pharmaceutically acceptable additives include, for example, excipients, disintegrants or disintegration aids, binders, lubricants, coating agents, pigments, diluents, bases, and dissolving agents.
  • a dissolution aid, a tonicity agent, a pH adjuster, a stabilizer, a propellant, an adhesive, and the like can be used.
  • formulations suitable for oral administration include, for example, tablets, capsules, powders, fine granules, granules, solutions, syrups, and the like.
  • formulations suitable for parenteral administration include, for example, injections, drops, suppositories, inhalants, patches, and the like.
  • compositions suitable for oral administration, or for transdermal or transcutaneous membrane administration Disintegrant or disintegration aid such as carboxymethylcellulose, starch, or calcium carboxymethylcellulose; binder such as hydroxypropyl cellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, or gelatin; stearin Lubricants such as magnesium acid or talc; Coating agents such as hydroxypropylmethylcellulose, sucrose, polyethylene glycol or titanium oxide; serine, liquid paraffin, polyethylene glycol, gelatin, kaolin, glycerin, purified water, or hard It can be used bases such as up and.
  • Disintegrant or disintegration aid such as carboxymethylcellulose, starch, or calcium carboxymethylcellulose
  • binder such as hydroxypropyl cellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, or gelatin
  • stearin Lubricants such as magnesium acid or talc
  • Coating agents such as hydroxypropylmethylcellulose, sucrose, poly
  • propellants such as chlorofluorocarbon, getyl ether, or compressed gas
  • adhesives such as sodium polyacrylate, polyvinyl alcohol, methylcellulose, polyisobutylene, and polybutene
  • preparations such as base cloth such as cotton cloth or plastic sheet The preparation may be manufactured using additives for use.
  • Cranial nerve function improvers containing the compound of the above formula (I) as an active ingredient have already been used in clinical practice (generic name “Bifumelan hydrochloride”: drug names of “arnath” and “celeport”, respectively) Sold by Fujisawa Pharmaceutical Company Limited and Eisai Co., Ltd.)
  • the above-mentioned commercial preparation may be used as it is as a therapeutic agent for the disease.
  • the dose of the therapeutic agent for autism of the present invention is not particularly limited, and may be appropriately selected depending on the administration form, the age, weight, and symptoms of the child.
  • a pediatric oral dose can be converted by setting the oral dose (the amount of the active ingredient) per adult to about 5 to 300 mg, preferably about 50 to 200 mg, particularly preferably 150 mg.
  • the therapeutic agent for autism of the present invention may be administered once or several times a day, and the administration period can be arbitrarily determined according to the age of the child, the degree of improvement in symptoms, and the like.
  • 2- (4-methylaminobutoxy) diphenylmethane which is an active ingredient of the therapeutic agent for autism of the present invention, is an extremely safe substance, and its acute toxicity is described in Japanese Patent Publication No. 2-33689. It is described in Table 1. Since the therapeutic agent for autism of the present invention is intended for application to children, it will be easily understood by those skilled in the art that the high safety of the therapeutic agent for autism of the present invention is a very advantageous property. .
  • Formulation examples of the therapeutic agent for autism of the present invention are shown below, but the dosage form of the therapeutic agent of the present invention is not limited to these examples.
  • Formulation Example 2 2- (4-methylaminobutoxy) diphenylmethane hydrochloride 100 g corn starch 200 g lactose 500 g carboxymethylcellulose calcium 150 g polyvinylpyrrolidone 75 g talc 75 g microcrystalline cellulose 250 g Mix the above ingredients according to the usual method Then, the mixture is granulated and compression-molded to produce a tablet of 120 mg per tablet.
  • Bifmelan hydrochloride was administered to three patients diagnosed with autism by a physician for 12 weeks.
  • the dosage was approximately 3 mg / kg, and the dose was increased based on symptoms.
  • the therapeutic agent of the present invention is useful because it shows high efficacy in treating pediatric autism and alleviating its pathology, and has high safety.

Landscapes

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

Abstract

L'invention concerne un remède contre l'autisme, contenant, comme principe actif, du 2-(4-méthylaminobutoxy)diphénylméthane représenté par la formule (I), un hydrate de ce composé, ou un sel pharmaceutiquement acceptable de ce composé. L'utilité de ce remède réside dans le fait qu'il est très efficace pour traiter l'autisme infantile (trouble profond du développement de l'enfant) et pour amoindrir l'état pathologique lié à ce trouble, et qu'il est très sûr.
PCT/JP1995/002159 1994-10-24 1995-10-20 Remede contre l'autisme Ceased WO1996012481A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP6257789A JPH08119858A (ja) 1994-10-24 1994-10-24 自閉症治療剤
JP6/257789 1994-10-24

Publications (1)

Publication Number Publication Date
WO1996012481A1 true WO1996012481A1 (fr) 1996-05-02

Family

ID=17311134

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP1995/002159 Ceased WO1996012481A1 (fr) 1994-10-24 1995-10-20 Remede contre l'autisme

Country Status (2)

Country Link
JP (1) JPH08119858A (fr)
WO (1) WO1996012481A1 (fr)

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, Vol. 111, Abstract No. 167182, NAKAMURA Y. et al., "Anticonvulsant Effects of Bifemelane Hydrochloride on Kindled Seizures from the Amygdala and Hippocampus in Rats"; & YAKUBUTSU, SEISHIN, KODO, 1989, 9(2), 241-4. *

Also Published As

Publication number Publication date
JPH08119858A (ja) 1996-05-14

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