Prophylaxis of post-traumatic heterotopic ossification in the elbow joint

 

(57) Abstract:

The invention relates to medicine. It is proposed to use chlorpromazine for prevention of post-traumatic heterotopic ossification. The invention expands the Arsenal of tools specified destination.

The method applies to experimental medicine and can be used in the study of the etiology and pathogenesis unescalated bone formation and selection of therapeutic drugs for use in clinical practice.

In clinical practice used method of prevention of heterotopic ossification in the elbow joint, the essence of which is oral administration of indomethacin (Cm. for example, source: G. I. Zhabin "Surgical treatment of fresh elbow joint injuries and their consequences", abstract. dis. D. M. N., St. Petersburg, 1995, 20 C.). However, using this drug is not pathogenic, because the mechanism of action of indomethacin anti - inflammatory, and heterotopic osteogenesis is a reaction to the proliferation of connective tissue; in addition, the use of indomethacin may lead to nonunion bone fractures.

It is also known that heterotopic ossified the example, source: C. A. Dyachenko "X-ray diagnosis of calcification and heterogeneous bones", 1960, M, Medgiz, 226 S.).

The objective of the invention is to increase the efficiency of the pathogenetic prevention of heterotopic ossification in the elbow joint through the use of chlorpromazine for a new purpose as a means of preventing post-traumatic heterotopic ossification. Currently chlorpromazine used in neurological practice for the treatment of disorders of the Central nervous system.

This object is achieved in that after the trauma of the elbow joint rabbits intramuscularly injected solution of chlorpromazine 2 times a day every 6 hours for 3 weeks.

Justification for the use of chlorpromazine was the following prerequisites (See. for example, source: M. D. Mashkovsky "Drugs", part I, S. 41 - 44): chlorpromazine is one of the main representatives of neuroleptics, the main feature of which is a strong sedative effect on the Central nervous system; the effect of chlorpromazine accompanied by a General calming down, there comes a state of reduced responsiveness to endogenous and exogenous stimuli, with full sohraneniem. Under local anaesthesia, an open dislocation of the bones of the forearm of a rabbit in the elbow joint. After surgery, the animal is injected solution of chlorpromazine 2 times a day every 6 hours for 3 weeks. Daily dose for each animal was 0.001 gram. To do this, 1.0 ml of 2.5% solution of chlorpromazine had saline to a volume of 25.0 ml, the resulting solution was injected into each animal in the amount of 0.5 ml 2 times a day. Due to the low dose of the drug activity of rabbits is almost not reduced. When x-ray examination within 6 months, not one animal treated with chlorpromazine, post-traumatic ossification in the elbow joint are identified. In control animals not treated with chlorpromazine, heterotopic ossification after injury of the elbow joint was developed in 40% of cases.

The use of chlorpromazine for prevention of heterotopic ossification will allow in clinical practice to choose to use other antipsychotic drugs with similar mechanism of action.

The use of chlorpromazine as a means of preventing post-traumatic heterotopic ossification in the region is

 

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FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of aryl carboxylic acids and describes a compound of the formula (I):

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27 cl, 64 ex

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3 ex

FIELD: medicine, arthrology, pharmacy.

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2 cl, 14 ex

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2 cl, 14 ex

FIELD: organic chemistry, biochemistry, pharmacy.

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EFFECT: valuable properties of compounds.

5 cl, 3 sch, 5 tbl, 6 ex

FIELD: medicine, pharmacology.

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EFFECT: higher efficiency of application.

7 cl, 1 dwg, 7 ex, 2 tbl

FIELD: medicine, pharmacology.

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EFFECT: higher efficiency of application.

7 cl, 5 ex, 2 tbl

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

21 cl, 5 tbl, 8 ex

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2 tbl, 3 dwg

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15 cl, 5 tbl, 6 ex

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8 dwg, 1 ex

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6 dwg

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

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EFFECT: valuable medicinal properties of compounds and composition.

9 cl, 2 sch, 2 tbl, 29 ex

FIELD: organic chemistry, steroids, medicine, pharmacy.

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EFFECT: valuable medicinal properties of compounds, improved method for treatment.

38 cl, 1 tbl, 18 ex

FIELD: medicine.

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EFFECT: higher efficiency of application.

11 cl, 2 ex

FIELD: organic chemistry and pharmaceutical compositions.

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EFFECT: new effective kinase p38 inhibitors.

23 cl, 6 dwg, 1 tbl, 1 ex

FIELD: medicine.

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EFFECT: accelerated treatment course.

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of adamantane of the general formula:

wherein m = 1 or 2; each R1 represents independently hydrogen atom; A represents C(O)NH or NHC(O); Ar represents the group:

or

wherein X represents a bond, oxygen atom or group CO, (CH2)1-6, CH=, O(CH2)1-6, O(CH2)2-6O, O(CH2)2-3O(CH2)1-3, CR'(OH), NR5, (CH2)1-6NR5, CONR5, S(O)n, S(O)nCH2, CH2S(O)n wherein n = 0, 1 or 2; R' represents hydrogen atom; one of R2 and R3 represents halogen atom, nitro-group, (C1-C6)-alkyl; and another is taken among R2 and R3 and represents hydrogen or halogen atom; either R4 represents 3-9-membered saturated or unsaturated aliphatic heterocyclic ring system comprising one or two nitrogen atoms and oxygen atom optionally being heterocyclic ring system is substituted optionally with one or more substitutes taken independently among hydroxyl atoms, (C1-C6)-alkyl, (C1-C6)-hydroxyalkyl, -NR6R7, -(CH2)rNR6R7; or R4 represents 3-8-membered saturated carbocyclic ring system substituted with one or more substitutes taken independently among -NR6R7, -(CH2)NR6R7 wherein r = 1; R5 represents hydrogen atom; R6 and R7 each represents independently hydrogen atom or (C1-C6)-alkyl, or (C2-C6)-hydroxyalkyl group eliciting antagonistic effect with respect to R2X7-receptors. Also, invention describes a method for their preparing, pharmaceutical composition comprising thereof, a method for preparing the pharmaceutical composition and their applying in therapy for treatment of rheumatic arthritis and obstructive diseases of respiratory ways.

EFFECT: improved method for preparing and treatment, valuable medicinal properties of compounds.

13 cl, 88 ex

FIELD: medicine, pharmacy.

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EFFECT: improved and valuable properties of formulation.

8 cl, 16 tbl, 39 ex

Substituted indoles // 2255087

FIELD: organic chemistry, biochemistry.

SUBSTANCE: invention relates to new substituted indoles of the formula (I): and/or stereoisometic form of compound of the formula (I) and/or physiologically acceptable salt of compound of the formula (I) wherein R3 means residue of the formula (II): wherein D means -C(O)-; R7 means hydrogen atom (H) or -(C1-C4)-alkyl; R8 means (a) typical residue of amino acid among the group: phenylalanine or homophenylalanine wherein phenyl residue is unsubstituted or substituted with halogen atom; or (b) -(C1-C4)-alkyl wherein alkyl is a linear or branched and (b) 1) mono- or multi-substituted independently of one another with pyrrole residue wherein this residue is unsubstituted or substituted with halogen atom; (b) 2) mono- or bi-substituted independently with residue -S(O)x-R10 wherein x = 0, 1 or 2, or (b) 3) mono- or bi-substituted independently of one another -N(R10)2 wherein R10 means (a) hydrogen atom (H); (b) means -(C1-C6)-alkyl wherein alkyl is unsubstituted or substituted with halogen atom from 1 to 3 times; (c) phenyl wherein phenyl is substituted or substituted with halogen atom from 1 to 3 times; in the case (R10)2 residues R10 have values independently of one another (a), (b), (c); Z means (a) residue of heterocycles group comprising benzothiadizine, pyrrole, pyridine, pyrimidine, pyrazine, imidazole, pyrazole, oxazole, isoxazole, thiazole, isothiazole, tetrazole, oxadiazolone, triazole being heterocycles are unsubstituted or substituted with -NH2=, =O, alkoxycarbonyl or aminocarbonyl from 1 to 3 times, or (b) means -C(O)-R11 wherein R11 means 1. -O-R10 or 2. -N(R10)2; R9 means (a) hydrogen atom (H); (b) means (C1-C6)-alkyl wherein alkyl is unbranched or branched and substituted with phenyl or =O independently of one another from 1 to 3 times; (c) phenyl wherein phenyl is unsubstituted or substituted with halogen atom; R1, R2 and R4 mean hydrogen atom (H); R5 means hydrogen atom (H); R6 means (a) phenyl wherein phenyl is unsubstituted or substituted with -NH2; (b) pyridine, or (c) pyrimidine being pyridine or pyrimidine is unsubstituted or substituted with groups -NH2, -NH-CH3. Compounds of the formula (I) are specific inhibitors of IkB kinase.

EFFECT: valuable biochemical properties of compounds.

3 cl, 3 tbl, 29 ex

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