2,4-pyrimidine diamine compounds and use thereof

IPC classes for russian patent 2,4-pyrimidine diamine compounds and use thereof (RU 2493150):

C07D413/14 - containing three or more hetero rings

C07D413/12 - linked by a chain containing hetero atoms as chain links

C07D409/12 - linked by a chain containing hetero atoms as chain links

C07D405/14 - containing three or more hetero rings

C07D405/12 - linked by a chain containing hetero atoms as chain links

C07D403/14 - containing three or more hetero rings

C07D403/12 - linked by a chain containing hetero atoms as chain links

C07D401/14 - containing three or more hetero rings

C07D401/12 - linked by a chain containing hetero atoms as chain links

C07D239/48 - Two nitrogen atoms

C07D239/28 - with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms

A61P37/08 - Antiallergic agents (antiasthmatic agents A61P0011060000; ophthalmic antiallergics A61P0027140000)

A61P37 - Drugs for immunological or allergic disorders

A61P11/06 - Antiasthmatics

A61K31/519 -

A61K31/505 -

Another patents in same IPC classes:

5-aminocyclylmethyloxazolidin-2-one derivatives / 2492169

Invention relates to antibacterial compounds of formula (I) , where one or two of U, V, W and X represent N, the remaining ones represent CH or, in case X, can also represent CR^a, where R^a represents fluorine; R¹ represents alcoxygroup, halogen or cyanogroup; R² represents H, CH₂OH, CH₂N₃, CH₂NH₂, alkylcarbonylaminomethyl or triazol-1-ylmethyl; R³ represents H or, when n=1, R³ can also represent OH, NH₂, NHCOR⁶ or triazol-1-yl; A represents CR⁴; K represents O, NH, OCH₂, NHCO, NHCH_2; CH₂NH₅ CH₂CH₂, CH=CH, CHOHCHOH or CHR⁵; R³ represents H or together with R⁵ forms bond, or R⁴ can also represent OH, when K is not O, NH, OCH₂ or NHCO; R⁵ represents OH or together with R⁴ forms bond; R⁶ represents alkyl; m=0 or 1 and n=0 or 1; and G is specified in i.1 of the formula; and to salt of such compound.

Pyridine derivatives as s1p1/edg1 receptor modulators / 2492168

Invention relates to novel pyridine derivatives pyridine¹-A-pyridine² of formula (1), where pyridine¹ represents

Aminotriazole derivatives as alx agonists / 2492167

Described are novel aminitriazole derivatives of formula (I), where A is phenyl, heterocyclyl or propan-1,3-diyl; E is *-C_1-4alkyl-O-, -CH=CH- or , where asterisks stand for bond, through which binding with R¹; Q- O or S occurs; R³ is hydrogen, C_1-4alkyl, cyclopropyl, C_1-4alkoxy-C_1-4alkyl, benzyl or -CH₂CH₂C(O)O-tert-Bu; R¹ is pyridyl or phenyl, possibly substituted with halogen, C_1-4alkyl, C_1-4alkoxy, C_1-4fluoroalkyl, C_1-4fluoroalkoxy, di-( C_1-3alkyl)amino or C_1-4alkoxy-C_1-2alkyl; and R² is -CO-C_1-3alkyl,-CF₂-C_1-3alkyl or -SO₂-C_1-3alkyl; or their pharmaceutically acceptable salts, pharmaceutical composition, which contains them.

Compounds suitable for use as raf kinase inhibitors / 2492166

Invention relates to a compound of formula 1:

Novel ligands of estrogen receptors / 2492164

Invention relates to compound of formula (I): or to its pharmaceutically acceptable ester, amide, carbamate, solvate or salt, including salt of such ester, amide or carbamate and solvate of such ester, amide, carbamate or salt, where values R¹, R², R³, R⁴, R⁵ and R⁶ are given in item of the formula, with the exception: 4-[3-(4,5-dihydro-1H-imidazol-2-yl)-2-(3,5-dimethylisoxazol-4-yl)indole-1-yl]phenol; 1-(4-hydroxyphenyl)-2-(4-methylimidazol-1-yl)-1H-indole-3-carbonitryl; 1-(4-hydroxyphenyl)-2-(1H-pyrazol-3-yl)-1H-indole-3-carbonitryl; 1-(3-chloro-4-hydroxyphenyl)-2-(1-methyl-1H-pyrazol-4-yl)-1H-indole-3-carbonitryl; 1-(4-hydroxyphenyl)-2-prop-1-inyl-1H-indole-3-carboxylic acid amide.

Derivatives of aminopyrazol / 2489426

Invention relates to derivatives of aminopyrazol with the formula of , where A, E, R¹ and R² have values specified in the invention claims, and to their pharmaceutically acceptable salts. Compounds of the formula (I) are agonists of the ALX receptor. Besides, the invention relates to a pharmaceutical composition on the basis of the compound of the formula (I) or its pharmaceutically acceptable salt and to application of these compounds for production of a medicinal agent for prevention or treatment of a disease selected from inflammatory diseases, wheezing diseases, allergic states, HIV-mediated retrovirus infections, cardiovascular diseases, neuroinflammations, neurological disorders, pain, prion-mediated diseases and amiloid-mediated diseases; and for modulation of immune responses.

5-substituted indazole as kinase inhibitors / 2487873

Present invention refers to compounds of formula (I) or pharmaceutically acceptable salts thereof wherein A, R₁, R₂, R₃ and m are specified in the patent claim. The present invention also refers to the number of specific compounds, and to a pharmaceutical composition containing the above compounds effective for inhibition of kinases, such as glycogen synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus kinase (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

Novel amide derivative and use thereof as medicinal agent / 2487124

Invention relates to an amide derivative of formula (I), where A is benzene or pyridine, where the benzene or pyridine optionally contain 1 or 2 or 3 identical or different substitutes selected from an alkyl containing 1-6 carbon atoms, a cycloalkyl containing 3-6 carbon atoms, an alkoxy containing 1-6 carbon atoms, a halogen atom, nitro, cyano, alkylsulphonyl containing1-6 carbon atoms, amino, cyclic amine selected from 1,1-di-oxoisothiazolidinyl, 2-oxooxazolidinyl, oxopyrrolidinyl, 1,1-dioxothiazinyl and 2-oxoimidazolidinyl optionally having a substitute selected from an alkyl containing 1-6 carbon atoms and an alkylcarbonyl containing a total of 2-7 carbon atoms, acylamino containing a total of 2-7 carbon atoms, and an alkylsulphonyl amino containing 1-6 carbon atoms, wherein the right-side bond is linked to the carbonyl and the left-side bond is linked to the nitrogen atom, R¹ and R² are identical or different and each is a hydrogen, an alkyl containing 1-6 carbon atoms and optionally containing 3 halogen atoms as substitutes, a cycloalkyl containing 3-6 carbon atoms, a phenyl, a halogen atom or a cyano group and R¹ and R² are not a hydrogen atom at the same time, R³ is a hydrogen atom, an alkyl containing 1-6 carbon atoms, an alkenyl containing 2-6 carbon atoms, a cycloalkyl containing 3-6 carbon atoms, or a halogen, R^4a, R^4b and R^4c are each independently a hydrogen atom, an alkyl containing 1-6 carbon atoms, or an oxo, R^5a, R^5b and R^5c are identical or different and each is a hydrogen atom, an alkyl containing 1-6 carbon atoms and optionally containing substitute(s) selected from phenyl, an alkoxy group containing 1-6 carbon atoms, optionally substituted with an alkoxy group containing 1-6 carbon atoms, a phyenylcarbonyloxy group and a hydroxy group, or a phenyl, X is a carbon atom (any of R^4a, R^4b and R^4c can be bonded to a carbon atom, but the carbon atom is not substituted with oxo) or a nitrogen atom (if Y is a single bond, the nitrogen atom can be oxidised to form an N oxide), Y is a single bond, a carbonyl or an oxygen atom, Z¹ and Z² are each independently a carbon atom (substitute R³ is optionally bonded to a carbon atom) or a nitrogen atom, and m equals 1 or 2, a pharmacologically acceptable salt thereof. The amide derivative is used as a preventive/therapeutic drug for treating autoimmune diseases, inflammatory bowel diseases or osteoarthritis.

Pyrimidine derivatives as alk-5 inhibitors / 2485115

Invention relates to novel pyrimidine derivatives of formula (I) in free form or in form of a pharmaceutically acceptable salt or solvate, which are useful in treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders and other diseases which are mediated by activity of the ALK-5 receptor or ALK-4 receptor. The invention also relates to a method of producing compounds of formula (I) and pharmaceutical compositions. In formula , T is a pyridin-2-yl which is optionally substituted in one position with R¹; T¹ is a pyridinyl which is optionally substituted in one or two positions with R¹, R², R⁵, C₁-C₄-alkoxy group, C₁-C₄-alkoxycarbonyl or cyano group; and R^a and R^b are independently hydrogen; C₁-C₈-alkyl, optionally substituted in one, two or three positions with R⁴; C₃-C₁₀-cycloalkyl, which is optionally substituted in one or two positions with a hydroxy group, amino group, C₁-C₈-alkyl, C₁-C₈-alkoxy group, halogen, cyano group, oxo group, carboxy group or nitro group; or C₆-C₁₅-aryl, optionally substituted in one, two or three positions with a halogen, hydroxy group, amino group, cyano group, oxo group, carboxy group, nitro group or R⁵; R¹ is C₁-C₈-alkyl; R² is C₆-C₁₅-aryl, optionally substituted in one, two or three positions with a halogen, hydroxy group, R¹, R⁵, C₁-C₈-alkylthio group, amino group, C₁-C₈-alkylamino group, etc. The rest of the values of the radicals are given in the claim.

Cytokine inhibitors / 2485113

Invention refers to imidazole compounds of formula wherein the radical values A, X, R¹, R², R³ are presented in clause 1 of the patent claim.

Substituted methylphenyl ketones suitable for use as pde4 inhibitors / 2493149

Invention describes a compound of formula I , in which X₁, X₂, X₃, X₄ and X₅ independently denote -CH- or N; or X₃, X₄ and X₅ independently denote -CH- or N, and X₁ and X₂ independently denote C and are part of an additional 6-member aromatic ring; in which R₁ denotes methyl or ethyl, or R₁ denotes hydrogen; R₂ denotes methyl, ethyl, propyl, tert-butoxy carbonylmethyl, allyl, difluoromethyl, ethylbenzene, methylbenzene, butenyl, hydroxyethyl, tolyl, pentenyl, methoxyethyl, butynyl, propynyl, methylcarbonyloxy, cyclopentyl, each of which can be substituted with one or more identical or different substitutes selected from R₅; or R₂ denotes hydrogen; R₃ denotes alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, halogenalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, arylalkyl, alkylalkoxycarbonyl, alkylcarbonyloxy or alkoxyalkyl, each of which can be substituted with one or more identical or different substitutes selected from R₆; or R₃ denotes hydrogen, -CH₂-C(O)-heterocycloalkyl or -CH₂-C(O)NR₉-R₁₂; R₁₁ denotes one or more identical or different substitutes selected from hydrogen, halogen, cyano, amino, alkyl, methylthionyl, methylsulphonyl, amino, cyano or alkoxy; where R₅, R₆, R₉, R₁₂ are as indicated in claim 1, under the condition that R₁, R₂ and R₃ cannot be methyl at the same time; under the condition that when R₂ and R₃ both denote hydrogen, R₁ cannot be methyl or hydrogen; under the condition that when R₁ denotes methyl or hydrogen, R₂ denotes methyl and R₃ denotes hydrogen when ring B cannot be phenyl; and pharmaceutically acceptable salts and N oxides thereof. The invention also describes a pharmaceutical composition for use in case of skin diseases, said composition containing a compound of formula I, and use of said compound in preparing a medicinal agent for preventing conditions associated with skin wounds.

Aminotriazole derivatives as alx agonists / 2492167

Adrenergic compounds / 2491284

Invention relates to compounds, which represent (4,5-dihydrooxazol-2-yl)-(5,6,7,8-tetrahydroquinoxylan-5-yl)-amino and (4,5-dihydrooxazol-2-yl(-(5,6,7,8-tetrahydroquinolin-5-yl)-amino or their pharmaceutically acceptable salt. Said compounds are applied in methods of intraocular pressure reduction and treatment of pain in mammals who require it.

Novel amide derivative and use thereof as medicinal agent / 2487124

Compounds and methods for kinase modulation and indications for use of said compounds and methods / 2487121

Disclosed is a compound having chemical formula or a salt thereof, where: Ar is an optionally substituted heteroaryl; R¹ in each case is independently selected from a group which includes halogen, lower alkyl, optionally substituted with one or more substitutes selected from fluorine, lower alkoxy, fluorine-substituted lower alkoxy, monoalkylamino, dialkylamino, -O-R⁵, -N(R⁵)-R⁶ and -N(R⁵)-C(X)-R⁷; m equals 0 or 1; n equals 0, 1 or 2; R² is hydrogen or a halogen; L₂ is -S(O)₂-; R³ is a lower alkyl, optionally substituted with fluorine, C_3-6 cycloalkyl, optionally substituted with a lower alkyl, a 5- or 6-member nitrogen-containing heterocycloalkyl, optionally substituted with one or more substitutes selected from fluorine, lower alkyl, fluorine-substituted lower alkyl, lower alkoxy, fluorine-substituted lower alkoxy, lower alkylthio or fluorine-substituted lower alkylthio, aryl, optionally substituted with a halogen, lower alkyl, optionally substituted with a halogen or lower alkoxy, optionally substituted with a halogen, or a heteroaryl, optionally substituted with a halogen or a lower alkyl; L₁ is selected from a group which includes -O-, -C(R¹²R¹³)-X-, -X-C(R¹²R¹³)-, -C(R¹²R¹³)-N(R¹¹)-, -(R¹¹)-C(R¹²R¹³)-, -C(X)-N(R¹¹)-, -N(R¹¹)-C(X)-; X is O; R¹¹ is hydrogen; R⁴ is hydrogen or a lower alkyl; R⁵ and R⁶ in each case are independently selected from a group which includes hydrogen, lower alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, where each is optionally substituted with one or more substitutes selected from fluorine, lower alkoxy, fluorine-substituted lower alkoxy, lower alkylthio, fluorine-substituted lower alkylthio, monoalkylamino, dialkylamino; R⁷ in each case is independently selected from a group which includes lower alkyl; where the terms "lower alkyl", "lower alkoxy", "lower alkylthio", "monoalkylamino", "dialkylamino", "cycloalkyl", "heterocycloalkyl", "aryl", "heteroaryl", are as described in the claim. The invention also discloses a pharmaceutical composition for treating Raf kinase mediated diseases which is based on a compound of formula I; use of the compound of formula I to produce a medicinal agent is also disclosed.

3-(trinitromethyl-onn-azoxy)-4-nitraminofurazans and methods for production thereof / 2485108

Invention relates to organic chemistry, specifically to novel 3-(trinitromethyl-ONN-azoxy)-4-nitraminofurazans of general formula I . In formula I, R is Me, or . The invention also relates to methods of producing compounds of formula I.

Compounds exhibiting jak-kinase activity (versions), method of treating jak-kinase mediated diseases, method of inhibiting jak-kinase activity (versions), pharmaceutical composition of said compounds / 2485106

Invention refers to new compounds of general formula III which possess the properties of JAK pathway inhibitors and JAK-kinase inhibitors. In formula III: X is specified in a group consisting of C₁-C₁₀alkyl, amino, halogen, carboxyl, carboxylic acid ester, C₂alkynyl, substituted tri-C₁-C₆alkylsilyl; R represents hydrogen; the cycle A is specified in a group consisting of C₆aryl, bicycloheptene, five-and sis-member mono- or 10-member bicyclic heteroaryl including 1 to 3 heteroatoms specified in a group of heteroatoms, including N, O or S, and five- or six-member mono- or 10-member bicyclic heterocycle, including 1 to 2 heteroatoms specified in a group of heteroatoms, including N or O; p means 0, 1, 2 or 3; each of R² is independently specified in a group consisting of C₁-C₆alkyl, C₁-C₄alkyl substituted by 1 to 3 substitutes. The other substitute and radical values are specified in the patent claim.

New 1,2-dihydroquinoline derivatives possessing glucocorticoid receptor binding activity / 2485104

Present invention refers to organic chemistry, namely to new 1,2-dihydroquinoline derivatives of general formula , or to a pharmaceutically acceptable salt thereof, wherein R¹ represents a lower alkyl group; R² represents a hydrogen atom; each of R³ and R⁴ represents a lower alkyl group; R⁵ represents a lower alkyl group; R⁶ represents a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group; X represents -CO-, -C(O)NR⁸ - or -S(O)₂-; each of R⁷ and/or R⁸ may be identical or different, and represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower cycloalkyl group, a phenyl or naphthyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a lower alkoxy group, a phenoxy group; provided R⁷ and/or R⁸ represent a lower alkyl group, a lower alkoxy group, the mentioned lower alkyl group and lower alkoxy group may contain one or three groups specified in a halogen atom, a phenyl group, an unsubstituted monocyclic 6-member heterocyclyl with one heteroatom specified in a nitrogen atom, and 5 carbon atoms in a cycle, a lower alkoxy group, and -NR^aR^b as a substitute (substitutes); provided R⁷ and/or R⁸ represent a phenyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a phenoxy group, the mentioned phenyl group, saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, phenoxy group may contain one or two groups specified in a halogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, a phenyl group, a hydroxyl group, a lower alkoxy group, a halogen-substituted lower alkoxy group, a lower alkylthio group, a lower alkylcarbonyl group, a lower alkoxycarbonyl group, a lower alkylcarbonyloxy group, -NR^aR^b, a nitro group and a cyano group as a substitute (substitutes); R^a and R^b may be identical or different, and each of them represents a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl group; Y represents a lower alkylene group; Z represents an oxygen atom; p is equal to 2, provided p is equal to 2, R⁶ may be identical or different. The invention also relates to a pharmaceutical composition and a glucocorticoid receptor modulator of the compound of formula (1).

New pyrrol derivative having ureide and aminocarbonyl groups as substitutes / 2485101

Invention refers to pyrrol derivatives of formula (1): or a pharmaceutically acceptable salt thereof wherein the values A, R¹-R³, n are specified in clause 1 of the patent claim.

N-hydroxylsulphonamide derivatives as novel physiologically useful nitroxyl donors / 2485097

Invention relates to N-hydroxylsulphonamide derivatives of formula or , where R¹ is H; R² is H; n is 0; b is an integer in the range of 1-4; R³, R⁴, R⁵, R⁶ and R⁷ are independently selected from H, halogen, carboxyl, carboxyl ester selected from a group including -C(O)O-morpholino, -C(O)O-C₁-C₈alkyl and -C(O)O-substituted C₁-C₈alkyl, where the substitute is morpholino; acylamino, which is a -C(O)NR^aR^b group, where R_a and R_b are independently C₁-C₈alkyl, or R_a and R_b together with a nitrogen atom to which they are bonded form morpholino; and sulphonylamino, which is a SO₂NR₂ group, where two groups R, together with a nitrogen atom to which they are bonded, form morpholino; R⁸ is selected from halogen and carbonylamino, selected from a -CONH-substituted C₁-C₈alkyl, where the substitute is morpholino; and -CONR₂, where two groups R, together with a nitrogen atom to which they are bonded, form morpholino; C is a heteroaromatic ring which contains cyclic fragments Q⁹, Q¹⁰, Q¹¹, Q¹², Q¹³ and Q¹⁴, which are independently selected from C, CH and S, under the condition that at least one of the fragments Q⁹, Q¹⁰, Q¹¹, Q¹², Q¹³ and Q¹⁴ is S. The invention also relates to a method of modulating nitroxyl levels, a method of treating diseases which respond to treatment with nitroxyl, a treatment set and a pharmaceutical composition containing compounds of formula (I) or (III).

2h-chromen compound and derivative thereof / 2490266

Invention refers to a 2H-chromen compound or a derivative thereof having action of a S1P₁ agonist. The above may be used for preventing and/or treating a disease caused by undesired lymphocyte filtration, or a disease caused by abnormal cell proliferation or accumulation.

FIELD: chemistry.

SUBSTANCE: invention relates to novel of 2,4-pyrimidine diamine compounds of formula I, which inhibit degranulation of immune cells and can be used in treating cell reactions mediated by FcεRI or FcγRl receptors. In formula (I) each R² and R⁴ is independently phenyl substituted with one or more R⁸ groups or a heteroaryl selected from a group consisting of , where the heteroaryl is optionally substituted with one or more R⁸ groups and at least one of R² and R⁴ is a heteroaryl; R⁵ is selected from a group consisting of (C1-C6)alkyl, optionally substituted with one or more identical or different R⁸ groups, -OR^d, -SR^d, fluorine, (C1-C3)halogenalkyloxy, (C1-C3)perhalogenalkyloxy, -NR^cR^c, (C1-C3)halogenalkyl, -CN, -NO₂, -C(O)R^d, -C(O)OR^d, -C(O)NR^cR^c, -C(NH)NR^cR^c, -OC(O)R^d, -OC(O)OR^d, -OC(O)NR^cR^c; -OC(NH)NR^cR^c, - [NHC(O)]_nOR^d, R³⁵ is hydrogen or R⁸; each Y is independently selected from a group consisting of O, S and NH; each Y¹ is independently selected from a group consisting of O, S and NH; each Y² is independently selected from a group consisting of CH, CH₂, S, N, NH and NR³⁷. Other values of radicals are given in the claim.

EFFECT: improved efficiency.

19 cl, 6 tbl.

The text descriptions are given in facsimile form.

1. The compound of formula I:

each R²and R⁴independently represent phenyl, substituted by one or more R⁸groups or heteroaryl selected from the group consisting of

where heteroaryl optionally substituted by one or more R⁸groups and at least one of R²and R⁴is heteroaryl;
R⁵selected from the group consisting of (C1-C6)alkyl, optionally substituted by one or more identical or different R⁸groups
-OR^d, -SR^d, fluorine, (C1-C3)halogenations, (C1-C3)perhalogenated,
-NR^cR^c(C1-C3)halogenoalkane-CN, -NO₂, -C(O)R^d, -C(O)OR^d, -C(O)NR^cR^c, -C(NH)NR^cR^c, -OC(O)R^d, -OC(O)OR^d, -OC(O)NR^cR^c; -OC(NH)NR^cR^c, - [NHC(O)]_nOR^d,
R³⁵represents hydrogen or R⁸;
R⁸is an R^e, R^b, R^esubstituted by one or more identical or different R^aor R^b, -OR^asubstituted by one or more identical or different R^aor
R^b, -(CH₂)_m-R^b, -(CHR^a)_m-R^b, -O-(CH₂)_m-R^b, -S-(CH₂)_m-R^b, -O-CHR^aR^b, -O-CR^a(R^b)₂,
-O-(CHR^a)_m-R^b, -O-(CH₂)_m-CH[(CH₂)_m-R^b]R^b, -S-(CHR^a)_m-R^b,
-C(O)NH-(CH₂)_m-R^b, -C(O)NH-(CHR^a)_m-R^b, -O-(CH₂)_m-C(O)NH-(CH₂)_m-R^b,
-S-(CH₂)_m-C(O)NH-(CH₂)_m-R^b,-O-(CHR^a)_m-C(O)NH-(CHR^a)_m-R^b,
-S-(CHR^a)_m-C(O)NH-(CHR^a)_m-R^b, -NH-(CH₂)_m-R^b, -NH-(CHR^a)_m-R^b,
-NH[(CH₂)_m-R^b], -N[(CH₂)_mR^b]₂, -NH-C(O)-NH-(CH₂)_m-R^b,
-NH-C(O)-(CH₂)_m-CHR^bR^band-NH-(CH₂)_m-C(O)-NH-(CH₂)_m-R^b;
each R^aindependently of the selected group, the situation of the soup from hydrogen, (C1-C6)alkyl, (C3-C8)cycloalkyl, (C4-C11)cycloalkyl, phenyl or naphthyl, (C7-C16)arylalkyl, 2-6-membered heteroalkyl including 1-3 heteroatoms selected from O, S or N, 3-8-membered cyclogeranyl including 1-3 heteroatoms selected from O, S or N, 4-11-membered cyclohexanoltramadol including 1-3 heteroatoms selected from O, S or N, 5-10-membered heteroaryl including 1-3 heteroatoms selected from O, N or S, and 6-16-membered heteroaromatic where heteroaryl is a 5-10-membered heteroaryl including 1-3 heteroatoms selected from O, N or S;
each R^bis a group independently selected from the group consisting of =O, -OR^d(C1-C3)halogenations, -OCF₃, -NR^cR^c,
halogen, -CF₃, -CN, -NC, -C(O)OR^d, -C(NOH)R^a, -OC(O)R^d, -OC(O)OR^d-,
-[NHC(O)]_nR^d, -[NR^aC(O)]_nR^d, - [NHC(O)]_nOR^d, - [NR^aC(O)]_nOR^d, -[NHC(O)]_nNR^cR^c, -[NR^aC(O)]_nNR^cR^c;
each R^cis independently R^aor, alternatively, two R^ctaken together with the nitrogen atom to which they are attached, form a 5-8-membered cyclogeranyl including 1-3 heteroatoms selected from O, S or N, or 5-10-membered heteroaryl including 1-3 heteroatoms selected from O, N or S, which may not necessarily include one or more Odie is ukovich or different additional heteroatoms and which optionally can be substituted by one or more identical or different R ^aor R^bgroups;
each R^dindependently is R^a;
each R^eoptional selected from the group consisting of (C1-C6)alkyl, (C3-C8)cycloalkyl, (C4-C11)cycloalkyl, phenyl or naphthyl, (C7-C16) arylalkyl, 2-6-membered heteroalkyl including 1-3 heteroatoms selected from O, S or N, 3-8-membered cyclogeranyl including 1-3 heteroatoms selected from O, S or N, 4-11-membered cyclohexanoltramadol including 1-3 heteroatoms selected from O, S or N, 5-10-membered heteroaryl including 1-3 heteroatoms selected from O, N or S, and 6-16-membered heteroaromatic where heteroaryl is a 5-10-membered heteroaryl including 1-3 heteroatoms selected from O, N or S;
each Y is independently selected from the group consisting of O, S and NH;
each Y¹independently selected from the group consisting of O, S and NH;
each Y²independently selected from the group consisting of CH, CH₂, S, N, NH and NR³⁷;
R³⁶represents hydrogen or (C1-C6)alkyl;
R³⁷represents hydrogen;
and in the definitions arylalkyl - aryl represents phenyl or naphthyl; and alkyl - (C1-C6)alkyl;
each m independently is an integer from 1 to 3; and each n independently is an integer from 0 to 3.

2. The compound according to claim 1, where heteroaryl selected from

3. The compound according to claim 1, where R^{2 and R⁴are the same.}

4. The compound according to claim 1, where each R³⁵independently selected from the group consisting of hydrogen, -NR^cR^c, -(CH₂)_m-NR^cR^c, -C(O)OR^d, -(CH₂)_m-C(O)OR^dand -(CH₂)_m-OR^d.

5. The compound according to claim 1, where R²represents phenyl, optionally substituted one, two or three R⁸groups.

6. The compound according to claim 1, where R²represents phenyl, optionally substituted with one or two R⁸groups.

7. The compound according to claims 1, 2 or 3, where R²represents tizamidine phenyl.

8. The compound according to claim 1, where R²represents phenyl, substituted with one R⁸group selected from the group consisting of (C1-C6)alkyl, -OR^d, -O-(CH₂)_m-NR^cR^c, -O-C(O)OR^a, -O-(CH₂)_m-C(O)OR^a, -O-C(NH)NR^cR^c, -O-(CH₂)_m-C(NH)NR^cR^c, -NH-(CH₂)_m-NR^cR^cand-NH-C(O)NR^cR^c.

9. The compound according to claim 1, where R²represents phenyl, substituted with two R⁸substituents selected from the group consisting of (C1-C6)alkyl, -OR^d, -O-(CH₂)_m-NR^cR^c, -O-C(O)OR^a, -O-(CH₂)_m-C(O)OR^a, -O-C(NH)NR^cR^c, -O-(CH₂)_m-C(NH)NR^cR^c, -NH-(CH₂)_m-NR^cR^cand-NH-C(O)NR R^c.

10. The compound according to claim 1, where R²represents phenyl, substituted three R⁸substituents selected from the group consisting of (C1-C6)alkyl, -OR^d, -O-(CH₂)_m-NR^cR^c, -O-C(O)OR^a, -O-(CH₂)_m-C(O)OR^a, -O-C(NH)NR^cR^c, -O-(CH₂)_m-C(NH)NR^cR^c, -NH-(CH₂)_m-NR^cR^cand-NH-C(O)NR^cR^c.

11. The compound according to claim 1, where R is substituted at the 3-, 4 - and 5-positions.

12. The compound according to claim 1, where R⁴represents phenyl, optionally substituted one, two or three R⁸groups.

13. The connection section 12, where R⁴represents phenyl, substituted at the 3-position, 4-position, 5-position, or combinations thereof.

14. The connection indicated in paragraph 13, where R⁴represents phenyl, substituted with one R⁸Deputy selected from the group consisting of (C1-C6)alkyl, -OR^d, -O-(CH₂)_m-NR^cR^c, -O-C(O)OR^a, -O-(CH₂)_m-C(O)OR^a, -O-C(NH)NR^cR^c, -O-(CH₂)_m-C(NH)NR^cR^c, -NH-(CH₂)_m-NR^cR^cand-NH-C(O)NR^cR^c.

15. The connection section 12, where R⁴represents phenyl, substituted with two R⁸substituents selected from the group consisting of (C1-C6)alkyl, -OR^d, -O-(CH₂)_m-NR^cR^c, -O-C(O)OR^a, -O-(CH₂)_m-C(O)OR^a, -O-C(H)NR ^cR^c, -O-(CH₂)_m-C(NH)NR^cR^c, -NH-(CH₂)_m-NR^cR^cand-NH-C(O)NR^cR^c.

16. The connection section 12, where R⁴represents phenyl, substituted three R⁸substituents selected from the group consisting of (C1-C6)alkyl, -OR^d, -O-(CH₂)_m-NR^cR^c, -O-C(O)OR^a, -O-(CH₂)_m-C(O)OR^a, -O-C(NH)NR^cR^c, -O-(CH₂)_m-C(NH)NR^cR^c, -NH-(CH₂)_m-NR^cR^cand-NH-C(O)NR^cR^c.

17. The compound according to claim 1, where one of R²and R⁴represents phenyl, substituted with one or more R⁸groups, and other R²and R⁴represent a heteroaryl groupand heteroaryl group is optionally substituted by one or more R⁸groups.

18. Pharmaceutical composition for inhibiting the degranulation of immune cells, comprising an effective amount of a compound according to any one of the preceding paragraphs and a pharmaceutically acceptable carrier, diluent or excipient.

19. The use of compounds according to any one of claims 1 to 17 in the treatment of cellular responses mediated FcεRI or FcγR1 - receptors in animals.