WO2003049729A1 - Utilisation de creatine et/ou de derives de creatine dans des atteintes et ou des troubles de la fonction musculaire, non induits par des maladies - Google Patents
Utilisation de creatine et/ou de derives de creatine dans des atteintes et ou des troubles de la fonction musculaire, non induits par des maladies Download PDFInfo
- Publication number
- WO2003049729A1 WO2003049729A1 PCT/EP2002/013809 EP0213809W WO03049729A1 WO 2003049729 A1 WO2003049729 A1 WO 2003049729A1 EP 0213809 W EP0213809 W EP 0213809W WO 03049729 A1 WO03049729 A1 WO 03049729A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- creatine
- muscle
- use according
- disorders
- illness
- 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
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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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
Definitions
- creatine and / or one of its physiologically suitable derivatives for the prevention or alleviation of non-disease-related impairments and / or disorders of muscle function
- the present invention is the use of creatine and / or one of its physiologically suitable derivatives for the prevention or alleviation of non-disease-related impairments and / or disorders of muscle function.
- the term "not due to illness” excludes all pathogenic or pathological events, but also all age-related events, which are to be grouped together under the technical terms myopathies, dystrophies, atrophies and hypertrophies, but also all other muscle physiology Muscle function related acute or chronic disease or aging.
- the term “disease” should be understood as meaning all events and syndromes that are not transient but persistent and usually progressive and / or those that lead to massive and lasting impairments of quality of life through targeted changes in muscle or muscle cell structure and / or muscle function without targeted therapeutic measures ,
- the non-disease-related impairments and / or disturbances of the muscle function in the sense of the present invention thus include all the above-mentioned or equivalent definitions not attributable, acutely occurring and acute creeping events, not the muscle (cell) structure and / or function change sustainably and do not permanently affect the quality of life.
- the symptoms covered by this definition thus occur only acutely and temporarily, they There is no reference to an already altered or worsening muscle or muscle cell structure and / or muscle function and no potentially intermittent but continuous treatment or therapeutic measures need to be performed.
- muscle soreness manifested manifestations in particular in the occurrence of muscle pain, especially in and around moving body parts and usually 24 to 48 hours after the extraordinary muscular strain.
- the term “delayed-onset muscle soreness” (DOMS) is widespread, which can be translated as the “delayed onset of muscle pain” and which describes the onset of symptoms, which is typically delayed by the causative event.
- muscle weakness muscle loss or pain events as a result of muscle overload can be associated with such extensive use of selected muscle.
- the severity of such muscular pains is also dependent on the intensity and duration of the previous stress, on the type of muscle work as well as on the age and state of training of the person concerned.
- top athletes in the active training state can be affected by these negative effects, especially if type, intensity and duration of exercise significantly exceed the usual level.
- WO 2001/28360 describes a food product of galactose, creatine and an optional third component as an ergogenic adjuvant on exercise, the benefit of the product being based on maintaining or increasing glycogen storage and glucose availability and according to which its ingestion improves the performance and efficiency of the product Athletes as well as causes a short-term energy supply under anaerobic and aerobic conditions.
- US Pat. No. 6,193,973 describes a food supplement in the form of a combination of creatine with ginseng and astragalus and possibly glutamine, which promotes muscle growth, muscle strength and muscle strength increase.
- ginseng and astragalus and possibly glutamine which promotes muscle growth, muscle strength and muscle strength increase.
- glutamine glutamine
- metals such as magnesium, calcium, copper, zinc or iron
- 6,277,842 describes the supply of L-carnitine, chromium picolinate, coenzyme Q1 0, creatine, lipoic acid, niacin, pyruvate, riboflavin, and thiamine as a prerequisite for a reduction in body weight and fat reduction.
- EP-A 1 002 532 describes the use of creatine or creatine analogues for the treatment of muscle atrophies due to age or disease-related immobilization or limited physical activity, in particular for restoring muscle mass during rehabilitation training. According to Diabetes (2001), 50 (1), 18-33, oral creatine supplementation prevents the decrease in the level of muscle GLUT4 protein in the foot during a two-week immobilization period and increases the level during the subsequent rehabilitation phase.
- a topical dosage form of creatine in the form of an ointment can be used according to WO96 / 33707 for increasing the muscular efficiency in patients in the rehabilitation phase.
- creatine the power supplement (MH Williams, RB Kreider, JD Branch, Human Kinetics, Champaign 1 999) contains a large number of annotated studies that can be used to prove the ergogenic, ie power-enhancing, benefits of creatine (Page 1 1).
- the impact of creatine on athletic performance is described as "very helpful" (page 9), especially for one-off (sprints) or repetitive high-intensity short-term workloads, but also in less intense prolonged anaerobic exercise spurts (pages 34 and 41) and sports with resistance performance (eg weight lifting).
- Phosphocreatine may delay fatigue due to its buffering effect on the muscle tissue which prevents the pH from being lowered (page 23).
- Creatine supplementation in turn, can be achieved by increasing the availability of phosphocreatine, by increasing phosphocreatine re-synthesis, by reducing muscle hyperacidity, by increasing oxidative metabolism, by enabling a "training load” and / or by An increase in the especially fat-free body mass to prevent fatigue of muscles (page 39 ff).
- creatine is considered to be suitable for maintaining strength (page 108), for increasing endurance in training exercises (page 1 55), and for having an advantageous influence on interval training sessions (page 156). All uses of creatine or one of its precursors or metabolites described so far according to the prior art thus relate exclusively either to the treatment of persistent or progressive diseases of the muscular system, the muscle, its fibers or cells or else to the administration of creatine.
- Derivatives usually as a dietary supplement for sustained increase in muscle mass, for a short-term increase in performance or to increase the tolerance limit for fatigue, the administration is always in multiple, repeating single doses and over a "Influence period" away, so as to adjust a certain level of creatine in the tissue ,
- the object of the present invention is therefore to provide a new use of creatine and / or one of its physiologically suitable derivatives with regard to the muscular apparatus.
- creatine (derivatives) is particularly recommended for muscle soreness, muscle weakness, loss of muscle strength, muscle overload or muscle pain, particularly preferably delayed onset muscle soreness (DOMS), but also in muscle tremors (tremor), muscle twitching ( Myoclonus), spontaneous muscle contractions (myocardia), muscle hardening or muscle hardness (myogelosis), muscle bruising, muscle break (hernia, myocele), muscle callus, muscle stiffness (rigor), muscle tension, diffuse or localized myalgia (especially the head muscles with possibly headaches) Myasthenia syndrome, mechanically or chemically induced muscle inflammation, or muscle ossification (myositis), muscle metaplasia, muscle relaxation (paresis), muscle paralysis or muscle pleura, and any associated or associative symptoms.
- tremor muscle tremor
- muscle twitching Myoclonus
- spontaneous muscle contractions myocardia
- muscle hardening or muscle hardness myogelos
- non-disease-related impairments or disorders is also the spectrum of creatine components which are preferred for their prevention or alleviation in the context of the present invention.
- the present invention takes into account single doses of the creatine component, which is between 10 mg and 10.0 g, preferably between 1, 0 and 5.0 g are. However, it may also be convenient to sum the single doses below a daily dose for which creatine levels between 30 mg and 30.0 g and preferably between 3.0 and 1 5.0 g are recommended.
- Essential not only in this context is the fact that the use according to the invention is prophylactic, ie preventive or for the purpose of alleviating manifesting non-disease-related impairments or disorders of muscle function. The use according to the invention is thus always coupled to a defined and temporally limited, muscle-loading measure.
- the present invention also takes into account in addition to the administration of the creatine component as a single preparation corresponding dosage forms containing the creatine component in proportions of 1, 0 to 95.0 wt .-%, preferably in proportions of 5.0 to 90.0 wt .-% and particularly preferably in proportions of 25.0 to 85.0 wt .-%, each based on the total weight of the dosage form included.
- All doses or parts of the creatine component mentioned in the present context refer to pure creatine. This means that when creatine derivatives are used, the stated amounts of dosages must correspond to those of free creatine and thus have to be adapted to the altered molecular weight.
- the invention also takes into account that the creatine component is used in dosage forms which contain fillers, lubricants, flow aids, mold release agents, plasticizers, blowing agents, stabilizers, dyes, extenders, binders, disintegrants, wetting agents, flow agents, countercocks or mixtures contain, whereby the variety of applications is additionally increased.
- dosage forms which are particularly suitable for the use according to the invention, it is therefore also possible to use the customary formulation auxiliaries, which, however, are then to be regarded only as additional optional components.
- Suitable fillers are oxides of magnesium, aluminum, silicon or titanium, microcrystalline cellulose and cellulose powder, starches and their derivatives (for example maltodextrins), lactose, mannitol and calcium diphosphate, which are suitable as fillers from the broad spectrum of all possible formulation auxiliaries.
- stearates of aluminum and calcium are also suitable, such as talc or silicones; Magnesium stearate, colloidal silicon dioxide, talc or Aerosil, as plasticizers low molecular weight polyalkylene oxide, low molecular weight organic plasticizers such as glycerol, pentaerythritol, glycerol monoacetate, diacetate or triacetate, propylene glycol, sorbitol or Na diethylsulfone succinate, as dyes azo dyes , (or-) niche pigments or natural colorants or other customary auxiliaries such as sugars (alcohols), polymers, phosphates, flavorings and surfactants in question. If necessary, these formulation auxiliaries may be present individually or in any desired combinations in a total proportion of between 0.05 and 90% by weight and in particular between 1.0 and 50% by weight, based in each case on the total weight of the dosage form.
- the present invention also contemplates the use of the creatine component in aqueous solutions, gels, semi-solid dosage forms, solid solutions, in beverages, effervescent or instant powders, tablets, dragées, puddings, yogurts or bars.
- This listing reflects only the most appropriate dosage forms.
- Other forms such as patches, bandages, lozenges, sprays, etc. are just as suitable.
- the invention provides the preferred use of the creatine component in the context of a supplement or combination therapy.
- a corresponding supportive use for example during therapeutic measures during healing, convalescence, remission or regeneration after open or closed fractures of grade 1 to 4 in the context of reduction, retention, immobilization, occupational therapy or physiotherapy.
- Group 1 supplementation with 4 g creatine monohydrate 30 min before, with placebo 30 min after exercise.
- Group 2 supplementation with placebo 30 min before, with 4 g creatine monohydrate 30 min after exercise.
- Group 3 Supplementation with 4 g creatine monohydrate 30 min before and 30 min after exercise.
- Group 4 (control group): supplementation with placebo 30 min before and 30 min after exercise. All measurements and interviews were made once or twice a day and one day before to three days after induced muscle overload.
- Muscle pain sensation Subjects in groups 1 to 3 rated the extent of muscle pain on a subjective scale from 1 (low grade) to 1 0 (high grade) on average significantly less than control group 4 (G 1: 6; G2: 5; G3 : 3, G4: 8).
- Group 1 Supplementation with 6 g creatine monohydrate 60 min before each exercise.
- Group 2 supplementation with placebo 60 min before each exercise. All measurements and interviews were made once or twice a day and one day before the first to three days after the last load.
- Creatine kinase especially after the second load. Ahn- Liche findings can be found in Medicine Sei. Sports Exercise 1998, 30, 73 and in FASEB J. 1996, 10, A791.
- Muscle Pain Sensation Group 1 subjects rated the extent of muscle pain on a subjective scale from 1 (low) to 10 (high) on average significantly less than control group 2, especially after the second exercise (exercise 1: G1: 5; G2: 7. load 2: G1: 3, G2: 8). mean endurance: The subjects of group 1 had a significantly higher average endurance compared to control group 2. The difference increased from the first to the second
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- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
L'utilisation de créatine et/ou d'un de ses dérivés physiologiquement appropriés permet de prévenir ou d'apaiser des atteintes et/ou des troubles de la fonction musculaire non induits par des maladies, tels que les courbatures, la faiblesse musculaire, la perte de force musculaire et les tensions musculaires. La dose simple de constituant créatine recommandée dans ce contexte devrait se situer entre 10 mg et 10 g et la dose quotidienne recommandée devrait être comprise entre 30 mg et 30,0 g. L'utilisation préconisée par l'invention, notamment dans le cadre d'une thérapie complémentaire ou combinée, permet d'éviter ou de réduire sensiblement les troubles de la fonction musculaire non induits par des maladies, fréquemment ressentis subjectivement comme très intenses et invalidants.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10160485.8 | 2001-12-08 | ||
| DE10160485A DE10160485A1 (de) | 2001-12-08 | 2001-12-08 | Verwendung von Kreatin und/oder einem seiner physiologisch geeigneten Derivate zur Prävention oder Linderung von nicht krankheitsbedingten Beeinträchtigungen und/oder Störungen der Muskelfunktion |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2003049729A1 true WO2003049729A1 (fr) | 2003-06-19 |
Family
ID=7708597
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP2002/013809 Ceased WO2003049729A1 (fr) | 2001-12-08 | 2002-12-05 | Utilisation de creatine et/ou de derives de creatine dans des atteintes et ou des troubles de la fonction musculaire, non induits par des maladies |
Country Status (2)
| Country | Link |
|---|---|
| DE (1) | DE10160485A1 (fr) |
| WO (1) | WO2003049729A1 (fr) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006042728A3 (fr) * | 2004-10-15 | 2007-03-22 | Basf Ag | Utilisation de sels d'ammonium stables de l'acide lipoique dans le traitement de troubles diabetiques et autres troubles |
| EP1871183A4 (fr) * | 2005-04-11 | 2008-06-11 | New Cell Formulations Ltd | Composition de supplement dietetique destinee a augmenter la masse musculaire et la force |
| WO2008137137A1 (fr) * | 2007-05-03 | 2008-11-13 | Avicena Group, Inc. | Dérivés ascorbyle de la créatine et procédés d'utilisation de ces derniers |
| WO2017032665A1 (fr) * | 2015-08-25 | 2017-03-02 | Protina Pharmazeutische Gesellschaft Mbh | Compositions de matières minérales pour stimuler le métabolisme des hydrates de carbone |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996033707A1 (fr) * | 1995-04-28 | 1996-10-31 | Synergen Ag | Preparation topique pour favoriser le developpement musculaire |
| DE19929994A1 (de) * | 1998-07-09 | 2000-01-13 | Sueddeutsche Kalkstickstoff | Verwendung von Kreatin zur Behandlung von Dystrophien und Atrophien der Skelettmuskulatur |
| DE19929993A1 (de) * | 1999-06-30 | 2001-01-11 | Sueddeutsche Kalkstickstoff | Kreatin-alpha-ketoglutarate, Verfahren zu ihrer Herstellung und ihre Verwendung |
| WO2001006873A1 (fr) * | 1999-07-23 | 2001-02-01 | Sigma-Tau Healthscience S.P.A. | Composition destinee a la prevention de la fatigue musculaire et a une meilleure adaptation du muscle squelettique aux exercices difficiles |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1002532A1 (fr) * | 1998-11-19 | 2000-05-24 | K.U. Leuven Research & Development | Prevention des effects du vieillissement et traitement de l'atrophie musculaire |
| AU1800801A (en) * | 1999-11-17 | 2001-05-30 | Eric H. Kuhrts | Exercise and muscle enhancement formulations |
| US6277842B1 (en) * | 2000-10-17 | 2001-08-21 | James Alexander Carthron | Dietary supplemental method for fat and weight reduction |
-
2001
- 2001-12-08 DE DE10160485A patent/DE10160485A1/de not_active Withdrawn
-
2002
- 2002-12-05 WO PCT/EP2002/013809 patent/WO2003049729A1/fr not_active Ceased
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996033707A1 (fr) * | 1995-04-28 | 1996-10-31 | Synergen Ag | Preparation topique pour favoriser le developpement musculaire |
| DE19929994A1 (de) * | 1998-07-09 | 2000-01-13 | Sueddeutsche Kalkstickstoff | Verwendung von Kreatin zur Behandlung von Dystrophien und Atrophien der Skelettmuskulatur |
| DE19929993A1 (de) * | 1999-06-30 | 2001-01-11 | Sueddeutsche Kalkstickstoff | Kreatin-alpha-ketoglutarate, Verfahren zu ihrer Herstellung und ihre Verwendung |
| WO2001006873A1 (fr) * | 1999-07-23 | 2001-02-01 | Sigma-Tau Healthscience S.P.A. | Composition destinee a la prevention de la fatigue musculaire et a une meilleure adaptation du muscle squelettique aux exercices difficiles |
Non-Patent Citations (2)
| Title |
|---|
| GUERRERO-ONTIVEROS M L ET AL: "CREATINE SUPPLEMENTATION IN HEALTH AND DISEASE. EFFECTS OF CHRONIC CREATINE INGESTION IN VIVO: DOWN-REGULATION OF THE EXPRESSION OF CREATINE TRANSPORTER ISOFORMS IN SKELETAL MUSCLE", MOLECULAR AND CELLULAR BIOCHEMISTRY, NORWELL, MA, US, vol. 184, no. 1/2, 1998, pages 427 - 437, XP000856537, ISSN: 0300-8177 * |
| WYSS M ET AL: "The therapeutic potential of oral creatine supplementation in muscle disease", MEDICAL HYPOTHESES, EDEN PRESS, PENRITH, US, vol. 51, 1998, pages 333 - 336, XP002101314, ISSN: 0306-9877 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006042728A3 (fr) * | 2004-10-15 | 2007-03-22 | Basf Ag | Utilisation de sels d'ammonium stables de l'acide lipoique dans le traitement de troubles diabetiques et autres troubles |
| EP1871183A4 (fr) * | 2005-04-11 | 2008-06-11 | New Cell Formulations Ltd | Composition de supplement dietetique destinee a augmenter la masse musculaire et la force |
| AU2006235643B2 (en) * | 2005-04-11 | 2010-12-16 | New Cell Formulations Ltd. | Supplemental dietary composition for increasing muscle size and strength |
| WO2008137137A1 (fr) * | 2007-05-03 | 2008-11-13 | Avicena Group, Inc. | Dérivés ascorbyle de la créatine et procédés d'utilisation de ces derniers |
| WO2017032665A1 (fr) * | 2015-08-25 | 2017-03-02 | Protina Pharmazeutische Gesellschaft Mbh | Compositions de matières minérales pour stimuler le métabolisme des hydrates de carbone |
Also Published As
| Publication number | Publication date |
|---|---|
| DE10160485A1 (de) | 2003-10-02 |
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