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Invention relates to a method of producing 4-thioureidoiminomethyl pyridinium perchlorate, having high tuberculostatic activity by reacting 4-pyridinoaldehyde, perchloric acid and thiosemicarbazide in an aqueous medium, wherein thiosemicarbazide is added to the obtained 4-pyridine aldehyde perchlorate (concentration of 28-46%) in molar ratio 4-pyridine aldehyde: thiosemicarbazide: perchloric acid of 1:1:1.05. The technical result is a novel simple, practically feasible and ecologically clean single-reactor method of producing pharmacopoeial 4-thioureidoiminomethyl pyridinium perchlorate (PERCHLOZONE®). |
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Present invention refers to new compounds of formula I or their pharmaceutically acceptable salts showing an ability to inhibit sphingosine kinase, to a based pharmaceutical composition, to a method of inhibiting sphingosine kinase and a method of treating diseases specified in breast cancer, diabetic retinopathy, arthritis and colitis. , wherein X represents -C(R3,R4)N(R5)-, -C(O)N(R4)-; R1 represents phenyl unsubstituted or substituted by 1 or 2 halogens. The values of R2, R3, R4, R5 substitutes are such as specified in the patent claim. |
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Indene derivatives as pharmaceutical agents 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. |
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Substituted phenoxy-acetic acids, with modulating effect on crth2 receptors Invention relates to new substituted phenoxy-aceitic acids (I), in which: X is halogen, cyano, nitro or C1-4alkyl, which is substituted with one or more halogen atoms; Y is chosen from hydrogen, halogen or C1-C6alkyl, Z is phenyl, naphthyl or ring A, where A is a six-member heterocyclic aromatic ring containing one or two nitrogen atoms, or can be 6,6- or 6,5-condensed bicycle which contains one O, N or S atoms, or can be 6,5-condensed bicycle which contains two O atoms, where phenyl, naphthyl or ring A can all be substituted with one or more substitutes, independently chosen from halogen, CN, OH, nitro, COR9, CO2R6, SO2R9, OR9, SR9, SO2NR10R11, CONR10R11, NR10R11, NHSO2R9, NR9SO2R9, NR6CO2R6, NR9COR9, NR6CONR4R5, NR6SO2NR4R5, phenyl or C1-6alkyl, where the last group can possibly be substituted with one or more substitutes, independently chosen from halogen; R1 and R2 independently represent a hydrogen atom or C1-6alkyl group, R4 and R5 independently represent hydrogen, C3-C7cycloalkyl or C1-6alkyl, R6 is a hydrogen atom of C1-6alkyl; R8 is C1-4alkyl; R9 is C1-6alkyl, possibly substituted with one or more substitutes, independently chosen from halogen or phenyl; R10 and R11 independently represent phenyl, 5-member aromatic ring which contains two heteroatoms, chosen from N or S, hydrogen, C3-C7cycloalkyl or C1-6alkyl, where the last two groups are possibly substituted with one or more substitutes, independently chosen from halogen or phenyl; or R10 and R11 together with the nitrogen atom to which they are bonded, can form a 3- to 8-member saturated heterocyclic ring, which possibly contains one or more atoms chosen from O, S(O)n (where n= 0, 1 or 2), NR8. |
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Derivatives of 1-piperazine- and 1-homopiperazincarboxilates, their obtaining and use Claimed invention relates to compound of formula (I) in which m represents integer number, equal 1 or 2; R1 represents group, selected, in particular from phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, naphtyl, chinolinyl, isochinolinyl, benzisoxazolyl, tienopyridinyl, said group is possibly substituted with one or several groups of R3, similar or different from each other or by group R4, R2 represents group of general formula CHR5CONHR6, R3 represents halogen atom or one of the following groups: piano, nitro, C1-6-alkyl, C1-6-alkoxy, C1-6-trifluoralkyl, C1-6-trifluoralkoxy, benzyloxy, phenyloxy, R4 represents group, selected, in particular from phenyl, benzofuranyl, naphtyl; one orseveral groups R4 can by substituted with one or several groups R3, similar or different from each other; R5 represents hydrogen atom or C1-3-akyl group; R6 represents hydrogen atom or alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl -C1-3-alkylene group; as base, salts of binding of acid, hydrate or solvate. Also invention relates to method of obtaining compound of formula I, its use as medicine and to based on it pharmacological composition. |
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Compound with anti-hcv effect and method of its obtainment Inventive subject matter is compouns and their pharmaceutically acceptable salts which can be applied in prevention and treatment of diseases caused by HCV infection. Structural formulae of the compounds are presented in the claim. |
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Method for preparing phenyl-substituted derivatives of pyridine labeled with tritium Invention relates to a method for preparing N-phenylpicolinium salts and phenyl-substituted picolines labeled with tritium by phenyl ring of the general formula: [CH3C5H4N+C6H* 5]BF- 4 and CH3C6H* 5C5H3N. Method involves arylation of 2-, 3- and 4-picolines with free phenyl cations obtained in beta-decay of tritium in composition of two-fold labeled benzene in the presence of potassium tetrafluoroborate in the closed system. Method provides improving method of synthesis of labeled benzene and to use ion-molecular reaction of tritium-labeled phenyl cations for simultaneous, simple and a single-step synthesis of N-phenylpicolinium salts and phenyl-substituted picolines labeled with tritium that can be used in investigations of metabolism of biologically active heterocyclic derivatives. |
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4-thioureidoiminomethyl-pyridinium perchlorate is prepared from 4-pyridine aldehyde and thiosemicarbazide in the presence of 48-55% perchloric acid for a single stage. The parent reagents - 4-pyridine aldehyde : thiosemicarbazide are taken in the ratio = 1.3:1.0, reaction period is 3-4 h, and reaction temperature is maintained in the range 80-85°C. Invention provides increasing yield and purity of the end product, simplifying technology and reducing cost in its preparing. |
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Invention relates to compounds of formula I , |
Another patent 2544601.