Imidazolinylmethylaralkyl sulfonamides

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to imidazoline-2-yl-substituted derivatives of arylalkyl sulfonamide possessing agonistic activity with respect to α1A/L adrenoceptors, and to pharmaceutical compositions comprising these derivatives. Invention relates to compound of the formula: or its pharmaceutically acceptable salts wherein R1 represents (C1-C12)-alkyl; R2 represents hydrogen atom; each radical among R3, R4, R5 and R6 represents independently hydrogen atom, halogen atom, (C1-C12)-alkyl, -OR9 wherein R9 represents hydrogen atom, (C1-C12)-alkyl under condition that R3, R4, R5 and R6 don't represent (C1-C12)-alkyl simultaneously; or R3 and R4 in common with atoms to which they are bound form aromatic 5-membered ring comprising heteroatom, such as oxygen atom, and R14 represents hydrogen atom.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

10 cl, 1 tbl, 8 ex

 

The text descriptions are given in facsimile form.

1. The compound of the formula:

its pharmaceutically acceptable salt,

where R1represents a C1-C12alkyl;

R2represents hydrogen;

each of R3, R4, R5and R6independently represents hydrogen, halogen, C1-C12alkyl, -OR9(where R9represents hydrogen, C1-C alkyl), provided that R3, R4, R5and R6at the same time do not represent a C1-C12alkyl; or

R3and R4together with the atoms to which they are attached form an aromatic 5-membered ring including heteroatom such as an oxygen atom; and

R14represents hydrogen.

2. The compound according to claim 1, where R1selected from the group consisting of methyl, ethyl and isopropyl.

3. The compound according to claim 1, where at least one of R3, R4, R5and R6represents a C1-C12alkyl, halogen or-OR9.

4. The compound according to claim 1, where at least one of R3, R4, R5and R6represents bromine, chlorine, fluorine, methoxy, ethoxy, methyl and hydroxy.

5. The compound according to claim 1, where

(a) R3represents methoxy, and R4, R5and R6represent hydrogen;

(b) R3represents methyl, R6represents methoxy and R4and R5represent hydrogen;

(C) R3represents methyl, R6represents chlorine and R4and R5represent hydrogen;

(g) R3represents chlorine, R4represents methoxy and R5and R6represent hydrogen;

(d) R3is particularly the methyl, R4represents chlorine and R5and R6represent hydrogen;

(e) R3represents methyl, R4represents methoxy and R5and R6represent hydrogen;

(W) R4represents chlorine and R3, R5and R6represent hydrogen;

(C) R4represents methoxy and R3, R5and R6represent hydrogen;

(and) R3represents methyl, R6represents bromine and R4and R5represent hydrogen;

(K) R3represents bromine, R4represents methoxy and R5and R6represent hydrogen;

(l) R3represents methyl, R4represents bromine and R5and R6represent hydrogen; or

(m) R4represents bromine and R3, R5and R6represent hydrogen; or

(n) R3represents ethoxy and R4, R5and R6represent hydrogen.

6. The compound according to any one of claims 1 to 4, where R5represents methoxy and R, R4, R6represent N.

7. The compound according to claim 1, where R3and R4together with the atoms to which they are attached, form furanyl or dihydrofuran.

8. The connection according to claim 7 of the formula

or.

9. The compound according to any one of claims 1 to 8, having agonistic activity against α1A/Lthe adrenergic receptors.

10. Pharmaceutical composition having α1A/Lagonistic activity, including

(a) a therapeutically effective amount of a compound according to any one of claims 1 to 8, and

(b) a pharmaceutically acceptable carrier.

Priority items:

23.04.2002 and 08.05.2002 - apply equally to all claims.



 

Same patents:

FIELD: bioorganic chemistry, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel aspartyl derivatives of histamine of the general formula (I): , wherein R means hydrogen atom (H), or , or that are able to modulate activity of enzymes of antioxidant protection - superoxide dismutase (SOD) and catalase. Also, invention relates to using the known compounds of the general formula (I) for the same designation wherein at the same values of X the value R represents acetyl group, and to their pharmaceutically acceptable salts. Also, invention relates to a pharmaceutical composition possessing capacity to modulate activity of SOD and catalase and comprising the effective amount of compound of the general formula (I), and to a method for synthesis of compounds of the general formula (I). Method involves interaction of pentafluorophenyl ester Nα-Z-, β- or α-benzyl ester of aspartic acid with histamine followed by hydrogenolysis without isolation of intermediated protected derivatives of aspartyl histamine.

EFFECT: improved method of synthesis, valuable biochemical properties of derivatives.

12 cl, 3 tbl, 2 sch, 2 dwg, 8 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of adamantine of the formula (I): wherein D represents -CH2 or -CH2-CH2; E represents -C(O)NH or -NHC(O); each R1 and R2 represents independently hydrogen atom or halogen atom but R1 and R2 can't mean hydrogen atom simultaneously; R3 represents group of the formula: -R4-X-R5 (II) wherein R4 represents (C1-C6)-alkyl group; X represents oxygen or sulfur atom or the group NR13; R5 represents (C1-C6)-alkyl or (C2-C6)-alkenyl and each of them can be optionally substituted with at least one substitute taken among halogen atom, hydroxyl, di-(C1-C6)-alkylamino-group, -Y-R6, , and 5- or 6-membered heteroaromatic ring comprising 1-4 heteroatoms taken independently among nitrogen atom wherein heteroaromatic ring can be optionally substituted with at least one (C1-C6)-alkyl; Y represents oxygen or sulfur atom or the group -NH; R6 represents the group -R7Z wherein R7 represents (C2-C6)-alkyl group and Z represents -OH; when Y represents oxygen or sulfur atom or the group -NH then R6 represents additionally hydrogen atom, (C1-C6)-alkyl, (C1-C6)-alkylcarbonyl; R13 represents hydrogen atom, (C3-C8)-cycloalkyl, (C3-C8)-cycloalkylmethyl; or R13 represents (C1-C6)-alkyl group optionally substituted with at least one hydroxyl, or to its pharmaceutically acceptable salts or solvates. These compounds are effective antagonists of P2X7 receptors and can be used in treatment of rheumatic arthritis or lung chronic obstructive disease. Also, invention describes methods for preparing these compounds, pharmaceutical composition comprising indicated compounds, method for preparing pharmaceutical composition and their using in therapy.

EFFECT: improved preparing and treatment methods, valuable medicinal properties of compounds and composition.

19 cl, 1 tbl, 77 ex

FIELD: organic chemistry, medicine, cardiology, biochemistry.

SUBSTANCE: invention relates to benzoyl guanidines of the formula (I): wherein R1 means -CF3; R2 means -Y-para-(C6H4)-R11, -Y-meta-(C6H4)-R11 or -Y-ortho-(C6H4)-R11 wherein R11 means (C1-C9)-heteroaryl comprising two or more nitrogen atoms adjoining across nitrogen (N) atom; Y means oxygen atom; R3 means hydrogen atom; R4 means (C1-C4)-alkyl, and to their pharmaceutically acceptable salts. Indicated compounds elicit very high activity with respect to inhibition of Na+/H+ exchange and improved water solubility and therefore they can be used as anti-arrhythmic medicinal agents with cardioprotective component for prophylaxis of infarction and treatment of infarction and for treatment of stenocardia. Also, proposed compounds inhibit pathophysiological processes in arising disorders induced by ischemia, in particular, in treatment of cardiac arrhythmia induced by ischemia.

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

17 cl, 2 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of imidazole of the formula (I):

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

25 cl, 1 tbl, 14 ex

FIELD: organic chemistry, medicine, hormones.

SUBSTANCE: invention describes imidazole derivatives of the formula (I) , racemic-diastereomeric mixtures and optical isomers, pharmaceutical salts wherein ---- represents an optional bond; R1 represents hydrogen atom (H), -(CH2)m-C(O)-(CH2)m-Z1, -(CH2)m-Z1; R2 represents hydrogen atom (H), or R1 and R2 are joined with nitrogen atoms to which they are bound forming compounds represented by formulae (Ia), (Ib) or (Ic) wherein R3 represents -(CH2)m-E-(CH2)m-Z2; R4 represents hydrogen atom (H) or -(CH2)m-A1; R5 represents (C1-C12)-alkyl, (C0-C6)-alkyl-C(O)-NH-(CH2)m-Z3 and optionally substituted phenyl; R6 represents hydrogen atom (H); R7 represents (C1-C12)-alkyl or -(CH2)m-Z4; m = 0 or a whole number from 1 to 6; n is a whole number from 1 to 5. Proposed compounds bind with subtypes of somatostatin receptors selectively.

EFFECT: valuable properties of compounds.

20 cl, 13776 ex

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New drug substances // 2237657
The invention relates to organic chemistry and can find application in medicine

New drugs // 2237057
The invention relates to organic chemistry and can find application in medicine

The invention relates to new and nitrate salts of heterocyclic compounds of formulas (a) and (b), where R is hydrogen, alkoxyl, R1- alkyl, alkoxyl, R2is hydrogen, alkyl, R3- alkyl, alkoxyl, X denotes N-R11or oxygen, R11means the free valence, Y represents N-R16, sulfur or alkyl, R16means hydrogen; other values radicals presented in the description of the invention

The invention relates to new derivatives of phenyl - and aminobenzenesulfonamide formula

< / BR>
where a denotes (R1SO2NR2-), (R3R60NSO2NR2-); X represents-NH-, -CH2- or-OCH2-; Y represents 2-imidazoline, 2-oxazoline or 4-imidazole; R1means (NISS

FIELD: organic chemistry, medicine, pharmacy.

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

28 cl, 39 ex

The invention relates to new derivatives of phenyl - and aminobenzenesulfonamide formula

< / BR>
where a denotes (R1SO2NR2-), (R3R60NSO2NR2-); X represents-NH-, -CH2- or-OCH2-; Y represents 2-imidazoline, 2-oxazoline or 4-imidazole; R1means (NISS

FIELD: veterinary virology.

SUBSTANCE: it is necessary to feed calves due to supplementing milk with iodoantipyrine preparation at the dosage of 2 g once daily during 5 d. The innovation enables to decrease the reality in manifesting clinical signs of respiratory disease in calves and shorten the terms for virus releasing with nasal secrets.

EFFECT: higher efficiency of prophylaxis.

1 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: the present innovation deals with applying water-free warming lubricating compositions that contain multi-atomic alcohols, a gelatinization-inducing agent, a pH-regulating agent for treating fungous and bacterial infections and, also, with the methods to apply such compositions for warming, lubricating, introducing active ingredients and either preventing or treating fungous and bacterial infections. The innovation suggests nontoxic and nonirritating compositions being efficient for treating both fungous and bacterial infections.

EFFECT: higher efficiency of therapy.

10 cl, 11 dwg, 10 ex, 3 tbl

FIELD: pharmaceuticals, in particular topical drugs for treatment of skin and mucous membrane disorders.

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EFFECT: physically stable metronidazole aqueous solutions containing minimized amount of cyclodextrins.

48 cl, 6 tbl, 5 ex

FIELD: medicine, ophthalmology, chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to the development of the ophthalmic composition possessing with anti-histaminic activity. Anti-histaminic ophthalmic drops comprise zinc sulfate, diphenhydramine hydrochloride, naphazoline hydrochloride, sodium citrate, citric acid, benzalkonium chloride, methylene blue, sodium chloride, hydroxypropylmethylcellulose-4000, sodium hydroxide and distilled water taken in the definite weight ratio. Drops can be used in allergic conjunctivitis, blepharitis, eyelid nettle rash and insect stings. Invention provides expanding spectrum of pharmacological effect of agent in such diseases.

EFFECT: improved and valuable medicinal properties of drops.

2 cl, 2 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of imidazole of the formula (I):

or its pharmaceutically acceptable salts wherein X represents -CH2-(CH2)p-, -O-; R1 represents phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (C3-C7)-cycloalkyl wherein indicated phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (C3-C7)-cycloalkyl are substituted optionally with 1-3 substitutes taken independently among halogen atom, -OH, halogen-(C1-C6)-alkyl, (C1-C6)-alkyl, (C1-C6)-alkoxy group and OH-(C1-C6)-alkyl; R2 represents hydrogen atom (H) or (C1-C6)-alkyl; R3 represents H or (C1-C6)-alkyl; R4 represents H or (C1-C6)-alkyl; R5 represents H, or R5 and R7 form in common a bond; each R6 represents independently halogen atom, -OH, halogen-(C1-C6)-alkyl, (C1-C6)-alkyl, (C1-C6)-alkoxy group or OH-(C1-C6)-alkyl; R7 represents H, or R7 and R5 form in common a bond; each R8 represents independently -OH, (C1-C6)-alkyl, halogen-(C1-C6)-alkyl or (C1-C6)-alkoxy group; m = 0, 1, 2 or 3; n = 0 or 1; p = 0 or 1; r = 0 or 1; t = 0. Also, invention relates to a method for preparing compounds of the formula (I) and to a pharmaceutical composition showing affinity to alpha-2-adrenoceptors based on these compounds. Invention provides preparing new compounds and pharmaceutical composition based on thereof used in aims for treatment of neurological disturbances, psychiatric disorders or disturbances in cognitive ability, diabetes mellitus, lipolytic diseases, orthostatic hypotension or sexual dysfunction.

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

25 cl, 1 tbl, 14 ex

FIELD: medicine.

SUBSTANCE: method involves introducing effective quantity of imidazole derivative of formula 1.

EFFECT: enhanced effectiveness of treatment.

14 cl, 2 dwg, 1 tbl

FIELD: organic chemistry, medicine, pharmacy.

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EFFECT: valuable medicinal properties of compounds.

10 cl, 2 ex

FIELD: medicine, pharmacology, pharmacy.

SUBSTANCE: invention proposes the composition comprising xenon as NMDA-antagonist and alpha-2-adrenergic agonist used for treatment of tetanus or narcotics (alcohol) withdrawal syndrome, states with chronic pain syndrome. Also, invention relates to the anesthetic composition comprising xenon and alpha-2-adrenergic agonist and to a method for anesthesia. The synergistic interaction of xenon as NMDA-antagonist and alpha-2-adrenergic agonist provides reducing the dose and to maintain the prolonged effectiveness by prevention for arising the drug habitation to the claimed preparation.

EFFECT: valuable medicinal properties of composition.

9 cl, 6 dwg, 6 ex

The invention relates to new imidazole derivative of the formula (I):where R1represents phenyl or pyridinyl, substituted by substituents selected from the group comprising (1) phenyl, (2) furyl, thienyl, (3) halogen, (4) halogen(lower)alkyl, (5) lower alkylthio, (6) nitro, (7) lower alkenyl, optionally substituted phenyl, (8) lower quinil, optionally substituted phenyl, (9) lower alkoxy, optionally substituted cyclo(lower)alkyl or phenyl, (10) lower alkyl, optionally substituted, phenyloxy or (11) amino, optionally substituted protected carboxyla; R2represents lower alkyl; R3represents halogen or lower alkyl; R4represents (1) lower alkenyl, optionally substituted phenyl, (2) phenyl, optionally substituted lower alkyl or lower alkenyl, (3) lower alkyl or (4) thienyl, optionally substituted with halogen; a represents a lower alkylene and L represents a simple bond, a lower albaniles or lower alkylene, optionally substituted phenyl or pyridinyl, or-X-CH2- where X represents O or NR5where R5represents hydrogen or n is
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