Dihydrobenzofuran carboxamide or its pharmaceutically acceptable salts and method of production thereof

 

(57) Abstract:

The inventive product is dihydrobenzofuran carboxamide f-crystals, where m is 0.1. T square 290-300°C (with decomp.), or their salt. Reagent 1: Reagent 2: 2 S. and 3 C.p. f-crystals. table 2.

The invention relates to new dihydrobenzofuranyl carboxamide derivative, process for the preparation and pharmaceutical compositions based on them.

The invention provides compounds of formula I

(I) where m is 0 or 1, and the symbol means that azabicyclic ring can be either endo - or Exo-orientation.

The invention also includes pharmaceutically acceptable salts of the compounds of formula (I) as well as all isomers of the formula, both isolated and in a mixture. Preferably, in the formula (I) Deputy were in the endo orientation. Pharmaceutically acceptable salts of the compounds of formula (I) are salts of suitable pharmaceutically acceptable acids, such as salts of inorganic acids, for example hydrochloric or sulphuric acid, or salts of organic acids such as organic carboxylic acids, such as citric, tartaric, fumaric, etc., or organic sulphonic acids, for example methanesulfonates or econsultancy acids. In Castorama compounds of formula (I) are the following compounds or Exo-orientation, either endo-orientation, preferably in the endo orientation.

1) 4-amino-5-chloro-N-(8-methyl-8-azabicyclo [3.2.1]Oct-3-yl)-2,3-dihydrobenzo[b] furan-7-carboxamide,

2) 4-amino-5-chloro-N-(9-methyl-9-azabicyclo [3.3.1] non-3-yl)-2,3-dihydrobenzo [b] furan-7-carboxamide, and pharmaceutically acceptable salts based on them, especially hydrochloride.

Structural formulas listed compounds:

1)

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2)

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In the present description in cases where the formula is Deputy with the symbol of this formula can represent a connection with azabicyclic ring only endo-orientation or only in Exo-orientation, or the formula may represent a mixture of both compounds having azabicyclic ring in endo-orientation and connections with azabicyclic ring in Exo-orientation.

Compounds of the invention obtained by the method comprising: interaction of the compounds of formula (II)

(II) or a reactive derivative of this compound with the compound of the formula (III):

H2N A (III), in which a represents a group of the formula

and if necessary, the acidification of the free compounds of formula (I) or obtaining a free compound of formula (I) from its salt and/or cyanocobalmin compound of formula (II) may, for example, to be in compliance WITH1-C4-alkilany ether, the corresponding galoidoproizvodnykh, in particular chloride or mixed anhydride in a mixture with the corresponding carboxylic acid. Preferred mixed anhydride is the anhydride obtained by the reaction of the compounds of formula (II) c etelcharge.com. The reaction between the compound of formula (II) or a reactive compound based and compound of formula (III) can be carried out according to known methods. In particular, the reaction between the compound of formula (II) and the compound of the formula (III) may be, for example, carried out in an inert, preferably anhydrous organic solvent such as dimethylformamide, in the presence of a condensing means, for example N,N-carbonyldiimidazole, in accordance with standard techniques. Possible transformation into a salt of the free compounds of formula (I), the possible obtaining the compounds of formula (I) in free form of its salts can be made a standard by using known and conventional procedures of organic chemistry.

The compound of formula (II) is a known compound and can be obtained by known methods.

The compounds of formula (III) is a compound of formula (III), in which group a is endo-8-methyl-8-azabicyclo [3.2.1] Oct-3-yl, i.e., this compound endo-8-methyl-8-azabicyclo [3.2.1] Octan-3-amine, can be obtained according to known procedure. And the compound of formula (III), in which group a is endo-9-methyl-9-azabicyclo [3.3.1] non-3-yl, i.e., this compound endo-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine, can be obtained according to known procedure.

The compounds of formula (I) are antagonists NT3receptor, as evidenced, for example, the fact that they were found active in the fight against chemoreflexes of Bezold-Aricha provoked by 5-HT in shot rats.

In table. 1 shows antagonistic activity against T3obtained in this test for compounds of the invention are 4-amino-5-chloro-N-(9-methyl-9-azabicyclo[3.3.1] non-3-yl)-2,3-dihyd - robinso [b] furan-7-carboxamide (internal code FCE 27270) and 4-amino-5-chloro-N-(8-methyl-8-azabicyclo[3.2.1]Oct-3-yl)-2,3 - dihydrobenzo [b] furan-7-carboxamide) (internal code FCE 27271) in comparison with the known compounds of the prototype connection Ondansetron, namely ()-1.2.3.4-tetrahydro-9-methyl-3-(2-Mei-1 - yl-methyl)-carbazole-4-one. The data in the table. 1 suggests, what aktivnosti in comparison with the connection of the prototype.

Inhibition of the reflex Bezold-Aricha caused by 5-HT (20 mg/kg intravenously) by intravenous FCE 27270.FCE 2721 and Ondansetron shot rats. The data in the table. 1, correspond to the mean S. E. M. in a group of 6 animals.

It was also found that the proposed connection of active and are selective inhibitors bind 3N-GR 65630 (a selective antagonist of 5-HT3receptor).

In table. 2 presents the data obtained in this test for compounds of the invention FCE 27270 and FCE 27271 in comparison with the known compounds of the prototype ondansetrona, MDL 72222 and metoclopramide (Metoclopramide).

MDL 72222 this connection formulas

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CP 65630 this connection formulas

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Test compounds capable of interacting with the 5-HT3-serotonin receptors, marked interinale the cerebral cortex of rats with3N-GR 65630. Listed in the connection table FCE 27270, 27271 and Ondansetron interact in accordance with dvuhslotovoj nonlinear model of accession, while MDL 72222 and metoclopramide substitute3N-GR 65630 according nonlinear single-site connection that is the reason why these two what about the evidence of the activity of compounds of the invention is superior to the activity of the compounds of the prototype.

Compounds of the invention can be useful, for example, in the treatment of disorders of the Central nervous system, for example in the treatment of psychosis and fear and/or treatment of disorders of peristalsis of the small intestine, and/or vomiting. From the point of view of activity, manifested offer connections, they can also be useful, for example, as an anti-migraine or drug abuse, or against excessive addiction to drugs, or as activators abilities to cognition. It was also found that the compounds can be used as painkillers (analgesics). The activity of compounds as analgesics demonstrated in this test, as the test described Dubvisson and Dennis in "the Formalin test: a quantitative study of the analgesic potency of morphine, meperidine and stimulation of the brain stem in rats and mice".

Since the compounds of formula (I) have analgesic properties, they can be used, for example, in the treatment of pain in mammals, for example in the treatment of some forms of inflammatory pain in humans. Connect the current pills, capsules, suspensions, drops or syrups; you can assign for parenteral injection, for example, they can be administered intravenously, intramuscularly in the form of solutions or suspensions, or subcutaneously.

Pharmaceutical compositions containing the compounds, can be obtained by standard methods using conventional carriers or diluents. Traditional carriers or diluents are, for example, water, gelatine, lactose, starches, magnesium stearate, talc, vegetable oils, cellulose, etc., Tablets, pills or capsules may, for example, contain a binder, such as gum tragakant, environment, drugs, such as calcium phosphate, dezintegriruetsja tools, such as corn starch, lubricant, such as magnesium stearate, sweetening additives, such as, for example, sucrose or flavors, such as cherry flavoring.

Suitable pharmaceutical forms for parenteral use are sterile aqueous solutions or dispersions and sterile powders for the preparation of "extempore". The dosage of the compounds as in the appointment in the prevention and therapeutic treatment will depend on the Xia cure, and also on the nature and severity of the disease. A suitable effective therapeutic dosage may be, for example, the dosage, lying in the range of from about 0.01 to 20 mg/kg of body weight. Preferably, when the connection can for example be entered one time or over several sessions so that the total daily dose was in the range of from about 0.02 to about 10 mg/kg per day.

The examples are only illustrations and do not limit the scope of the invention.

P R I m e R 1. 4-Amino-5-chloro-N-(endo-8-methyl-8-azabicyclo[3.2.1]Oct-3-yl)-2,3 - dihydrobenzo [b] furan-7-carboxamide.HCl

< / BR>
To a stirred solution of 4-amino-5-chloro-2,3-dihydrobenzo [b]furan-7-carboxylic acid (2,13 g, 0.01 mol) in 30 ml of anhydrous dimethylformamide added N, N-carbonyldiimidazole (1,96 g, 0.012 mol). In the solution purge nitrogen and stirred at room temperature while continuing to stir overnight, then added dropwise a solution of endo-8-methyl-8-azabicyclo [3.2.1]Octan-3-amine (1.40 g, 0.01 mol) in 5 ml of anhydrous dimethylformamide. The reaction mixture is heated at 70aboutC for 18 h, cooled, poured into water and extracted with methylene chloride. The organic layer is washed twice restorea and the resulting product was then purified using flash chromatography (SiO2) (CH2Cl2-MeOH - NH4OH 30% to 80:20:1 as eluent), followed by those treated with hydrochloric acid in ethanol: the obtained solid residue is filtered off and recrystallized from ethanol, resulting in 1.6 g of the named product so pl. 290-300aboutC (with decomp.).

1H-NMR (200 MHz, DMSO)

1,8-2,5 (m, 8H, CH2+++)

of 2.64 (s, 3H, NCH3)

totaling 3.04 (t, J 8,8 Hz, 2H, och2C)

with 3.79 (m, 2H, +)

as 4.02 (9, J 6.2 Hz, 1H,)

to 4.73 (t, J 8,8 Hz, 2H, PRAS2)

5,95 (s, 2H, N)

7,42 (c, 1H, )

of 1.78 (d, J 7.2 Hz, 1H, CONH)

10,2 (Shir.with. 1H, NH+)

P R I m m e R 2. The following compounds can be also obtained from the corresponding carboxylic acid and the appropriate amine according to the procedure described in example 1: 4-amino-5-chloro-N-(endo-9-methyl-9-azabicyclo[3.3.1] non-3-yl)-2,3-dihydrobenzo about[b] furan-7-carboxamide x xHCl, so pl. 260-280aboutC (with decomp.):

< / BR>
1H-NMR (200 MHz, DMSO)

1,3-2,5 (m, 10H, CH2++++)

2,80 (s, 3H, NCH3)

totaling 3.04 (t, J 8,8 Hz, 2H, och2C)

of 3.60 (m, 2H, +)

to 4.52 (m, 1H, )

4,72 (t, J 8,8 Hz, 2H, PRAS2)

5,94 (s, 2H, N)

7,39 (d, J 7.7 Hz, 1H, CONH)

7,46 (c, 1H, )

9,20 (Shir.with. 1H, NH+)

P R I m e R 3. Tablets, each containing 60 is their ingredients, mg:

4-Amino-5-chloro-N-

(endo-8-methyl-8-azabi-

cyclo [3.2.1]Oct-3-yl)-2,3-

dihydrobenzo [b] furan-7-

carboxamide, chlorostoma - burly salt 60 Starch 50

Microcrystalline cellulose 30 Polyvinylpyrrolidone 5

Sodium salt carbon-

sometribove starch 4.5 magnesium Stearate 0.5 to

P R I m e R 4. Capsules, each containing 80 mg of the active substance and dosage 200 mg, can be obtained as follows. Composition mg:

4-Amino-5-chloro-N-

(endo-8-methyl-

8-azabicyclo[3.2.1]

Oct-3-yl)-2,3-dihyd - robinso[b]

furan-7-carboxamide, hydrochloric salt 80 Corn starch 60

Microcrystalline cellulose 59 Stearate 1

This composition can be encapsulated in capsules, consisting of two parts and is made of solid gelatin in each capsule load 200 mg of the composition.

1. Dihydrobenzofuran carboxamide General formula I

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where m is 0 or 1;

the symbol means that azabicyclic ring can be andorientation or actuarielle, or its pharmaceutically acceptable salt.

2. Dihydrobenzofuran carboxamide or its salt under item 1, characterized in that represents the connection, vibracija, 4-amino-5-chloro-N-(endo-9-methyl-9-azabicyclo [3.3.1] non-3-yl)-2,3-dihydrobenzo [b] furan-7-carboxamide,

3. Salt dihydrobenzofuran carboxamide of General formula 1 p. 1, representing hydrochloride.

4. The method of obtaining dihydrobenzofuran of carboxamido formula 1, characterized in that the compound of formula II

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or its reactive derivative is subjected to interaction with the compound of the formula III

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where m and symbol have the specified values,

and, if necessary, carry out the reaction of the salt formation of free compounds of formula 1, or get a free compound from a salt of this compound, and/or, if necessary, separate the mixture of isomers of compounds of formula 1 into individual isomers.

5. Dihydrobenzofuran carboxamid on PP. 1 to 3, or its pharmaceutically acceptable salt having antagonist activity 5 HT3-receptor.

 

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The invention relates to compounds of the formula I

(I) or pharmaceutically acceptable salt accession acids him or stereoisomeric form of the compound, where

-A1= AND2- A3= AND4- bivalent radical having the formula

-CH=CH-CH=CH- (a-1)

-N=CH-CH=CH- (a-2)

-CH=CH-CH=N (a-5) or

-N=CH-N=CH- (and-6),

n=1 or 2

IN - NR4or CH2< / BR>
R4is hydrogen or C1-C6alkyl

L is hydrogen, C1-C6alkyl, C1-C6allyloxycarbonyl, or a radical of the formula

-Alk - R5(b-1),

-Alk - Y - R6(b - 2),

-Alk - Z1- C(=X) - Z2- R7(b-3), or

-CH2- SNON - CH2- O - R8(b-4), where R5is cyano, phenyl optionally substituted C1-C6alkyloxy; pyridinyl; 4,5-dihydro-5-oxo-1-N-tetrazolyl; 2-oxo-3-oxazolidinyl; 2,3-dihydro-2-oxo-1-N-benzimidazolyl; or bicycling radical of formula (C-4-a)

Gwhere G2- CH=CH-CH=CH-, -S-(CH2)3,- -S-(CH2)/2-, -S-CH=CH - or-CH=C(CH3)-O-;

R6- C1-C6-alkyl, pyridinyl optionally substituted by nitro; pyrimidinyl; feast
R7- C1-C6-alkyl; halophenol; 1-methyl-1H-pyrrolyl; furanyl, thienyl, or aminopyrazine;

R8- halophenol;

Y is O or NH;

Z1or Z2each independently NH or a direct link X-O

each Аlk independently - C1-C6alcander

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