Cycloalkylamines, containing phenyl as substituent, as inhibitors of monoamine reuptake

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel derivatives of cycloalkylamines, possessing inhibiting activity with respect to, at least, one monoamine transporter, selected from group, consisting of serotonin transporter, dopamine transporter and norepinephrine transporter. In formula (IV): n equals 1; s equals 1; Y and Z each independently represents halogen; X represents OR5; where R5 stands for H or non-substituted C1-C10alkyl; A represents H, non-substituted C1-C10alkyl or halogen; R1 and R2 each independently represents H; R3 and R4 each independently represents H or on-substituted C1-C10alkyl.

EFFECT: invention relates to pharmaceutical composition, containing said compounds and to method of treatment or prevention of neurological disorder or eating disorder, mediated by activity of monoamine transporter, selected from group, consisting of serotonin transporter, dopamine transporter and norepinephrine transporter, such as depression, neurodegenerative disease, abuse with psychoactive substances, fibromyalgia, pain, sleep disorder, syndrome of attention-deficit disorder, syndrome of attention-deficit disorder with hyperactivity, restless legs syndrome, schizophrenia, anxiety, obsessive-compulsive disorder, panic disorder, post-traumatic stress, premenstrual dysphoria.

35 cl, 6 dwg, 8 ex

 

The text descriptions are given in facsimile form.

1. The compound having structural formula (IV)

or its pharmaceutically acceptable salt, enantiomer or diastereoisomer,
in which
n = 1;
s is 1;
Y and Z each independently represents a halogen;
X is a OR5; where R5 1-C10alkyl;
And represents H, unsubstituted C1-C10alkyl or halogen;
R1and R2each independently represents H;
R3and R4each independently represents H or unsubstituted C1-C10alkyl.

2. The compound according to claim 1, where R3and R4each independently represents an unsubstituted With1-C4alkyl.

3. The compound according to claim 1, where a represents H, F or CH3.

4. The compound according to claim 1, where a represents N.

5. The compound according to claim 1, having structural formula (IVa):

where the radicals R1, R2, R3, R4, A, X, Y, Z, n and s have the meanings indicated in claim 1.

6. The compound according to claim 1, having structural formula (IVb):

where the radicals R1, R2, R3, R4And, X, Y, Z, n and s have the meanings indicated in claim 1.

7. The compound according to claim 1, where Y and Z are chlorine.

8. The compound according to claim 1, where R5represents N or CH3.

9. The compound according to claim 1, where R3and R4each independently represents N or CH3.

10. The compound according to claim 1, having a structure selected from formula (Ve), (Vf):
and
where R4represents N or CH3.

11. The compound according to claim 1 or farmacevtichesky acceptable salt, having the formula:
.

12. The compound according to claim 1 or its pharmaceutically acceptable salt having the formula:

13. The compound according to claim 1 or its pharmaceutically acceptable salt having the formula:

14. The compound according to claim 1 or its pharmaceutically acceptable salt having the formula:
or

15. The compound according to claim 1 or its pharmaceutically acceptable salt selected from the group consisting of:
,,,
,,,
and.

16. The compound according to claim 1 or its pharmaceutically acceptable salt selected from the group consisting of:
,,,
,and,

17. The compound according to claim 1 or its pharmaceutically acceptable salt selected from the group consisting of:
,,,
,and

18. Connect the Addendum according to claim 1 or its pharmaceutically acceptable salt, selected from the group consisting of:
,,
and.

19. The pharmaceutical composition intended for inhibiting the activity of at least one monoamine Transporter selected from the group consisting of the serotonin Transporter, dopamine Transporter and norepinephrine Transporter, comprising a therapeutically effective amount of a compound according to any one of claims 1 to 18, or its pharmaceutically acceptable salt, and a pharmaceutically acceptable carrier, solvent, diluent or inert excipient.

20. Method of inhibiting reuptake of at least one monoamine selected from the group consisting of serotonin, dopamine and norepinephrine, comprising introducing the compound according to any one of claims 1 to 18, or its pharmaceutically acceptable salt.

21. A method of inhibiting one or more of the monoamine transporters selected from the group consisting of the serotonin Transporter, dopamine Transporter, norepinephrine Transporter, and combinations of two or more of them, including the introduction of compounds according to claims 1 to 18, or its pharmaceutically acceptable salt.

22. Method for the treatment or prevention of neurological disorders, and mediated by the activity of the conveyor monoamine selected the CSOs from the group consisting of the serotonin Transporter, dopamine Transporter and norepinephrine Transporter, comprising the administration to a subject in need, a therapeutically effective amount of a compound according to any one of claims 1 to 18, or its pharmaceutically acceptable salt.

23. The method according to item 22, where the specified neurological disorder is a depression or neurodegenerative disease.

24. The method according to item 22, where the specified neurological disorder selected from the group consisting of substance abuse, fibromyalgia, pain, sleep disorders, syndrome disorders of attention, syndrome disorders of attention with hyperactivity, tired leg syndrome, schizophrenia, anxiety, obsessive-compulsive disorder, panic disorder, post-traumatic stress, and premenstrual dysphoria.

25. The method according to paragraph 24, where the specified neurological disorder is a sleep disorder.

26. The method according A.25, where the specified sleep disorder is a sleep apnea.

27. The method according to paragraph 24, where the specified neurological disorder is a pain.

28. The method according to item 27, where this pain is a neuropathic pain.

29. The method according to paragraph 24, where the specified neurological disorder is a syndrome of impaired attention with hyperactives the Y.

30. The method according to paragraph 24, where the specified neurological disorder is substance abuse.

31. The method according to item 30, where the specified substance abuse is an abuse of cocaine or nicotine, or a combination.

32. The method according to item 23, where the specified neurological disorder is a neurodegenerative disease.

33. The method according to p, where the specified neurodegenerative disease is a disease of Parkinson.

34. Method for the treatment or prevention of eating disorders mediated activity conveyor monoamine selected from the group consisting of the serotonin Transporter, dopamine Transporter and norepinephrine Transporter, comprising the administration to a subject in need of such treatment, a therapeutically effective amount of a compound according to any one of claims 1 to 18, or its pharmaceutically acceptable salt.

35. Method for the treatment or prevention of obesity-mediated activity conveyor monoamine selected from the group consisting of the serotonin Transporter, dopamine Transporter and norepinephrine Transporter, comprising the administration to a subject in need of such treatment, a therapeutically effective amount of a compound according to any one of claims 1 to 18 or a pharmaceutically receiving the emnd salt.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to novel aminoindane derivatives of formula (Ia) or pharmaceutically acceptable salts thereof, which have NMDA receptor antagonist effect, and can be used to prepare a medicinal agent for treating dementia. In formula (Ia):

,

R1 is a lower alkyl, C5-C6 cycloalkyl, phenyl which can be substituted with OH, lower alkyl, halogen atom, O-alkyl, C5-C6 heteroaryl containing a S atom as a heteroatom, or lower alkyl substituted with one or more halogen atoms, R2 and R3 are identical or different, each denoting alkyl or phenyl, R4 and R5 are identical or different and each denotes a hydrogen atom, lower alkyl, -O-lower alkyl, -lower alkylene-OH or -lower alkylene-O-lower alkyl, R6-R9 are identical or different and each denotes a hydrogen atom, lower alkyl, -O-lower alkyl, halogen atom, lower alkyl substituted with one or more halogen atoms, OH, CN, lower alkenyl or nitrogen-containing C5-C6 heterocyclic group, R10 and R11 are identical or different and each denotes a hydrogen atom or lower alkyl. The invention also relates to a pharmaceutical composition containing the said compounds.

EFFECT: improved properties of the derivative.

6 cl, 15 tbl, 130 ex

FIELD: pharmaceutical chemistry, medicine.

SUBSTANCE: invention relates to new compounds of formula I ,

solvates or pharmaceutically acceptable salts having antiarrhythmic activity, including ventrical fibrillation, as well as pharmaceutical compositions containing the same. Compounds of present invention are useful in treatment or prevention of arrhythmia, modulation of ion channel activity, for topic or local anesthesia, etc. In formula I X is direct bond, -C(R6,R14)-Y- and C(R13)=CH-; Y is direct bond, O, S, and C1-C4-alkylene; R13 is hydrogen, C1-C6-alkyl, C3-C8-cycloalkyl, unsubstituted aryl or benzyl; R1 and R2 are independently C3-C8-alkoxyalkyl, C1-C8-hydroxyalkyl and C7-C12-aralkyl; or R1 and R2 together with nitrogen atom directly attached thereto form ring of formula II ,

wherein said ring is formed by nitrogen and 3-9 ring atoms selected independently from carbon, sulfur, nitrogen and oxygen, etc; R3 and R4 are independently attached to cyclohexane ring in 3-, 4-, 5-, or 6-position and represent independently hydrogen, hydroxyl, C1-C6-alkyl and C1-C6-alkoxy; and when R3 and R4 are bound with the same atom of cyclohexane ring they may form together 5- or 6-membered spiroheterocycle ring containing one or two heteroatoms selected from oxygen and sulfur; A is C5-C12-alkyl, C3-C13-carbocyclic ring, or ring structure as defined herein.

EFFECT: new antiarrhythmic drugs.

30 cl, 12 dwg, 34 ex

The invention relates to 1-phenyl-2 - dimethylaminomethylene-1-alowyn compounds, method of their production and to their use in medicinal products

FIELD: chemistry.

SUBSTANCE: invention relates to novel quinoline derivatives of formula or pharmaceutically acceptable salts thereof, where n equals 0 or 1; when n equals 0, then R1 is hydrogen or methyl, R2 is hydroxyl, and R3 is hydrogen; and when n equals 1, R1 is hydrogen, and one of R2 and R3 is hydroxyl, and the other of R2 and R3 is hydrogen. The invention also relates to specific compounds of formula (I) and a method of producing compounds of formula (I).

EFFECT: novel quinoline derivatives are obtained, having high P2X7 antagonist activity.

9 cl, 1 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted cyclohexylmethyl derivatives, having serotonin, noradrenaline or opioid receptor inhibiting activity, optionally in form of cis- or trans-diastereomers or mixture thereof in form of bases or salts with physiologically compatible acids. In formula (1): R2 denotes H or OH; R1 and R2 together denote or =N-OH, R3 denotes a phenyl residue which is unsubstituted or monosubstituted with a halogen atom or a heteroaryl residue selected from a five-member sulphur-containing heteroaryl such as a thienyl residue or an unsubstituted phenyl residue bonded through a C1-C4alkyl group, R4 and R5 independently denote an unsubstituted C1-C3alkyl or R4 and R5 together denote (CH2)3-6, R8 denotes a linear saturated C1-C4 alkyl group bonded with an aryl, which is unsubstituted or monosubstituted with halogen atoms, R9 denotes a saturated C1-C8alkyl; values of radicals R1, m, n, R6, R7, R10-R13 are given in the claim. The invention also relates to methods of producing compounds of formula (I), a medicinal agent containing said compounds, use of compounds of formula (I) to prepare a medicinal agent for anaesthetic treatment during sharp, neuropathic or chronic pain and for treating depression, urinary incontinence, diarrhoea and alcoholism.

EFFECT: high efficiency of using the compounds.

32 cl, 501 ex, 21 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel cyclohexylamine derivatives of formula (I), having inhibiting properties towards at least one monoamine transporter, such as serotonin transporter, dopamine transporter or norepinephrine transporter, or a combination of two or more transporters. The compounds can be used to treat and/or prevent central nervous system disorders such as pain, depression, anxiety, schizophrenia, sleep disorder etc. In formula (I) , n equals 0 or 1; s equals 1, 2 or 3, m equals a whole number from 0 to 12; Ar is

or where Y and Z are (i) both halogen; or (ii) one of Y and Z is CF3 or OCF3 and the other is hydrogen; Y1, Z1, Y2 and Z2 each independently denotes H or a halogen; each X independently denotes H, halogen, CF3, OR5, (C1-C4)alkyl, optionally substituted with halogen or OH, or NR6R7; each R1 and R2 independently denotes H or (C1-C6)alkyl; and each R3 and R4 independently denotes H or (C1-C9)alkyl optionally substituted with OH; where each R5 independently denotes H, (C1-C4)alkyl or phenyl; and each R6 and R7 independently denotes H or (C1-C4)alkyl; where at least two of R1, R2, R3, R4 and X together with atoms to which they are bonded are optionally bonded to form a 5-6-member ring, where the 5-6-member ring is selected from: a) R3 and R4 together with a nitrogen atom to which they are bonded optionally form a pyrrolidine, piperidine, piperazine or morpholine ring, which is optionally substituted with (C1-C4)alkyl; b) when R3 is H or lower alkyl, X and R4 together with atoms to which they are bonded optionally form a 1,3-oxazine ring; c) two X substitutes together with a carbon atom to which they are bonded optionally form a 1,3-dioxolane ring; and d) when R1 and R3 denote hydrogen, R2 and R4 together with atoms to which they are bonded optionally form a 5- or 6-member saturated heterocyclic ring containing one nitrogen atom.

EFFECT: high efficiency of using the compounds.

29 cl, 36 dwg, 11 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel aminoindane derivatives of formula (Ia) or pharmaceutically acceptable salts thereof, which have NMDA receptor antagonist effect, and can be used to prepare a medicinal agent for treating dementia. In formula (Ia):

,

R1 is a lower alkyl, C5-C6 cycloalkyl, phenyl which can be substituted with OH, lower alkyl, halogen atom, O-alkyl, C5-C6 heteroaryl containing a S atom as a heteroatom, or lower alkyl substituted with one or more halogen atoms, R2 and R3 are identical or different, each denoting alkyl or phenyl, R4 and R5 are identical or different and each denotes a hydrogen atom, lower alkyl, -O-lower alkyl, -lower alkylene-OH or -lower alkylene-O-lower alkyl, R6-R9 are identical or different and each denotes a hydrogen atom, lower alkyl, -O-lower alkyl, halogen atom, lower alkyl substituted with one or more halogen atoms, OH, CN, lower alkenyl or nitrogen-containing C5-C6 heterocyclic group, R10 and R11 are identical or different and each denotes a hydrogen atom or lower alkyl. The invention also relates to a pharmaceutical composition containing the said compounds.

EFFECT: improved properties of the derivative.

6 cl, 15 tbl, 130 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) in form of a separate stereoisomer, a mixture of stereoisomers or a racemic mixture of stereoisomers and their pharmaceutically acceptable salts. In formula (I) ring A, C or D is independently completely or partially saturated; each of C1, C4, C11, C12, C15 and C16 is independently substituted with two hydrogen atoms; each of C9 and C14 is independently substituted with a hydrogen atom; R1 represents -OR7 or -N(R7)2. Values of the rest of the radicals are given in the formula of invention. The invention also relates to a pharmaceutical composition with anti-inflammatory activity and contains an effective amount of the disclosed compound and to use of the said compounds to make a medicinal agent with anti-inflammatory activity.

EFFECT: disclosed compounds have anti-inflammatory activity.

23 cl, 47 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of 1-aminobutane-3-ol of the general formula (I): and their physiologically acceptable salts possessing analgesic effect and capacity for binding habapentin-site. In the general formula (I) R1 and R2 form in common (CH2)2-9-ring; each R3 and R4 independently of one another means (C1-C6)-alkyl that is branched or direct, saturated or unsubstituted, benzyl or phenethyl that are unsubstituted; R5 means (C1-C10)-alkyl that can be saturated, unsaturated, branched or direct or unsubstituted, (C3-C9)-cycloalkyl that is saturated, phenyl or 5-membered sulfur-containing heteroaryl possibly condensed with benzene ring, (C3-C6)-cycloalkyl bound through saturated or unsaturated (C1-C3)-alkyl, 5-membered possibly condensed with benzene ring sulfur-containing heteroaryl bound through saturated or unsaturated (C1-C3)-alkyl wherein each aryl, heteroaryl and cycloalkyl residue independently of one another can be unsubstituted or mono- or multi-substituted with residues chosen independently of one another from the group comprising atoms F, Cl, Br, J, -OR18, (C1-C10)-alkyl that is saturated or unsaturated, branched or direct and can be mono- or multi-substituted with halogen atoms wherein R18 represents hydrogen atom (H), (C1-C10)-alkyl that is saturated, branched or direct or unsubstituted; R6 means H; R7 means (C1-C6)-alkyl that is branched or direct, saturated or unsaturated or unsubstituted, (C3-C9)-cycloalkyl that is saturated or unsubstituted, phenyl that is unsubstituted or mono- or multi-substituted or phenyl bound through saturated (C1-C3)-alkyl that can be unsubstituted or mono- or multi-substituted wherein these substitutes can be chosen independently from the group comprising atoms F, Cl, Br, J, -OR18, (C1-C10)-alkyl that is saturated or unsaturated, branched or direct, in free form as their physiologically acceptable salts. Proposed compounds can be used in treatment of pain and first of all neuropathic, chronic and acute pain. Also, invention relates to a method for synthesis of compounds and preparing a medicinal agent.

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

9 cl, 89 ex

FIELD: medicine, pharmaceuticals.

SUBSTANCE: invention relates to new application method for adamantine derivative, namely (3-hydroxy-1-adamantyl-)-1-ethylamine hydrochloride of formula I as inhibitor of 1-type herpes simplex virus reproduction. Said derivative is useful in inhibition of both sensitive and resistant to main antiherpes pharmaceuticals (e.g. acyclovir) virus strains. Substance of present invention has activity by 10-times higher than tromantadin and by 5-times higher than etmantin.

EFFECT: new antiherpes drug.

2 tbl, 2 ex

The invention relates to a method for producing derivatives benzothiophenes formula I, including the interaction of amerosport formula (II) or its salt with the compound of the formula (III) or its reactive derivative, the oxidation of the resulting product in the presence of 2,2,6,6-tetramethylpiperidine-1-oxide and then liaising with ridom in the conditions of a Wittig reaction with subsequent optional unprotect

The invention relates to new aralkylamines derivatives and their salts of interest as medicines, especially as a means of improving brain function, which can be shown senile dementia, Alzheimer's disease, etc

FIELD: medicine.

SUBSTANCE: invention refers to an agent for activation of lipoprotein lipase containing a benzene derivative of general formula (1) which is used for preventing and treating hyperlipidemia and obesity. The invention also refers to the benzene derivatives of general formula (1a).

EFFECT: composition improvement.

8 cl, 6 tbl, 9 ex

FIELD: food industry.

SUBSTANCE: invention relates to food industry, in particular, to food compositions based on natural extracts. The composition includes green tea extract in an amount of 200 mg - 300 mg, guarana extract in an amount of 160 mg - 260 mg, mate grass extract in an amount of 100 mg - 300 mg and conjugated linoleic acid in an amount of 700 mg - 3400 mg.

EFFECT: invention allows to produce a composition that (due to simultaneous presence of all the four components in the specified quantity) promotes regulation of total cholesterol and LDL cholesterol content and/or weight loss and/or thermogenesis as well as ensures carefully controlled caffeine content in the composition.

33 cl, 5 dwg, 2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: what is presented is the use of bacteria of the strains Lactobacillus rhamnosus, Bifidobacterium lactis, Bifidobacterium longum, Bifidobacterium breve able to stimulate the development of initial bifidogenic intestinal microbiota in preparing a probiotic composition for reducing a risk of developing overweight or future obesity in a nursing infant wherein the probiotic is prescribed during a perinatal and/or postnatal period in dose 103-1012 CFU.

EFFECT: what is presented is reducing a body weight index in 4-year-old children taken the probiotics during the perinatal period vs placebo.

10 cl, 3 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: method refers to medicine and aims at body weight reduction within the integrated therapy of obesity. Eslidime is prescribed during meals for 35 days. The intake regimen involves 2 capsules 2-3 times a day daily. It is combined with a low-calorie diet (800-950 ccal/day) for 1-14 days, while on the 15-35th day a diet of 1000-1200 ccal/day is introduced. From the first day of treatment, the therapy is added with graduated physical exercises (hiking at various speed for 30-40 min.).

EFFECT: method provides the therapeutic course aiming at body weight reduction by 8,23±1,01 kg.

4 cl, 4 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: in general formula (I) p equals 1 or 2; R1 is methyl, ethyl, propyl, isobutyl, 2-fluoroethyl or cyclobutyl; m equals 0; each R2 is absent; n equals 0; each R3 is absent; R4 is a hydrogen atom; R5 is a hydrogen atom; R6 is -C(O)O-R6a; R6a is a C1-C6alkyl group which can have 1-3 substitutes selected from a group of substitutes α, where the group of substitutes α is a group consisting of a halogen atom, a hydroxyl group, a C1-C6alkoxy group, a C3-C7cycloalkyl group, an amino group, a mono- or di(C1-C6alkyl)amino group, a phenyl group, and a furyl group; and R7 is a hydrogen atom.

EFFECT: compounds have the property of reducing the blood glucose level and can be used to treat and/or prevent type 1 sugar diabetes, type 2 sugar diabetes or diabetes-associated diseases caused by low glucose tolerance, as well as to prevent obesity caused by low glucose tolerance.

11 cl, 2 tbl, 119 ex

FIELD: chemistry.

SUBSTANCE: invention relates to substituted sulphamide derivatives of formula I: , in which n, m, R1, R2a-c, R3, R4, R5 and R6 are as described in claim 1, in form of a racemate, enantiomers, diastereomers, mixtures of enantiomers or diastereomers or a separate enantiomer or diastereomer, bases and/or salts of physiologically compatible acids. The invention also relates to a method of producing said compounds, a medicinal agent having antagonist action on bradykinin receptor 1 (B1R), containing such compounds, use of such compounds to produce medicinal agents, as well as sulphamide-substituted derivatives selected from a group of compounds given in claim 8.

EFFECT: providing novel compounds which are suitable as pharmacologically active substances in medicinal agents for treating disorders or diseases which are at least partially transmitted through B1R receptors.

13 cl, 581 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel cycloalkylmethylamine derivatives of formula (II) and (IV), having monoamine transporter inhibiting activity. In formula (II): , n equals 1; SP denotes a spacer - C1-6alkylene-O-; X denotes O or NH; R2 denotes hydrogen or C1-6alkyl; R3 denotes hydrogen, -COO-C1-6alkyl or -COO-C1-6alkylene phenyl; R4 denotes hydrogen; R5 denotes hydrogen, halogen, C1-6alkoxy; and R6 denotes C1-6alkyl. In formula (IV): , n equals 1; SP denotes a spacer selected from a group consisting of C1-6alkylene or a single bond; X denotes O or NH; R2 denotes C1-6alkyl; R4 denotes hydrogen or phenyl C1-6alkyl; R5 denotes halogen, hydroxy group or C1-6alkoxy; R6 denotes C1-6alkyl; R7 denotes hydrogen, halogen, hydroxy group or C1-6alkoxy.

EFFECT: high effectiveness when treating or preventing obesity or depression.

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to aryl- and heteroarylsubstituted diasaspiropyridine derivatives of formula (I) to its pharmaceutically acceptable acid- or base-additive salt wherein A represents a radical of formula (II) wherein each k, l, m, n independently represents an integer equal to 0, 1, 2, 3 or 4, provided (k+1) and (m+n) are equal to 2, 3, 4 or 5; wherein one of -CH2-fragments can be substituted by atom O; and wherein one of -CH2-fragments can be substituted by an oxo group; X represents CH or N; R3 is specified in a group consisting of hydrogen, C1-5alkyl and C3-6cycloalkyl; each R4, R5 is independently specified in a group including hydrogen, halogen, oxo, C1-3alkyl and C1-3alkyloxy; p represents an integer equal to zero, 1, 2 or 3; q represents an integer equal to zero, 1, 2 or 3; each Y1, Y3, is independently specified in a group including a single bond and O; Y2 represents saturated or unsaturated C1-6hydrocarbon radical with a straight chain; B is specified in a group including phenyl optionally substituted by the number of the substitutes R6 each of which is independently specified in halogen; and wherein r represents an integer equal to zero, 1 or 2; alkyl represents a saturated hydrocarbon radical with a straight and branched chain containing said number of carbon atoms; wherein said radical can be optionally substituted by one or more carbon atoms or more radicals specified in a group including halogen, cyano, hydroxy, amino, oxo, carboxyl, nitro, thio and formyl; and halogen represents fluorine, chlorine, bromine or iodine. Also, the invention refers to a pharmaceutical composition based on the compounds of formula I as an active ingredient for preparing a drug for preventing and/or treating mental disorders, including but not limited to anxiety, eating behavior disorder, affective disorders, such as bipolar disorders and depression, psychosis, such as schizophrenia, and sleeping disorders; obesity, diabetes; sexual disorders and neurological disorders; to a method for preparing a pharmaceutical composition, and to using the compounds of formula I for preparing the drug.

EFFECT: there are prepared and described new compounds possessing melanin-concentrating hormone (MCH), particularly MCH-1 antagonist activity.

19 cl, 4 ex, 7 tbl

FIELD: medicine.

SUBSTANCE: present invention refers to pharmaceutics, medicine and organic chemistry and concerns compounds of formulae presented below, as well as a pharmaceutical composition exhibiting NPY Y5 receptor antagonist activity, or an anorectic composition or an anti-obesity composition containing the compound of formulae presented below

EFFECT: what is presented is an amine derivative possessing npy y5 antagonist activity, and application thereof.

5 cl, 1 dwg, 2 tbl, 3 ex

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