Способ получения производных 1,2- дигидРОпиРиМидиНА

Способ получения 2-метил-5-нитроимидазола

Способ получения оксипиримидинов

Способ борьбы с нежелательной растительностью

СПОСОБ БОРЬБЫ С НЕЖЕЛАТЕЛЬНОЙ РАСТИТЕЛЬНОСТЬЮ путем обработки ее или почры на которой она произрастает , производными сульфонилмочевины , отличающийся тем, что, с целью повьшения эффективности способа, в качестве производных сульфонилмочевины используют соединение общей формулы Ki о X II ( СН2§02-ШСК-(О/ , I W- R где R - водород или метил; R; - хлор, метил, нитро, метил-, сульфонилокси, диметиламиносульфонил , трйфторметйл , или .-C,группы , в которых алкил, 2-хлорэтил, 2-метокСИЭТШ1 илиГаллил, Rj-C -Cj-алкил; водород или хлор R4и у независимо один от другого - метил или метокси; Z - -СН- или -N-, при условии, если R - хлор, X и У не означают одновременно метил-, в количестве 0,03-1 кг/га. I Приоритет по признакам: 03.11.80 при R - водород, R - хлор, СП метил, нитро, метьшсульс фонштокси, диметиламиносупьфонил , трифторметил, COOR, или S02Ra rpynnw, в которых R -C -Cj-алкил 2-хлорэтил, 2-метоксиэтил - или аллнл, а кил, R - водород или О5 хлор X и У независимо х один от другого - метил ел ...

1,6-DIHYDROPYRIDIN-1,5-DICARBONSAEURE-DERIVATE UND DIESE VERBINDUNG ENTHALTENDE ARZNEIMITTEL

DIHYDROPYRIMIDINES, PROCESS FOR THEIR PREPARATION AND THEIR USE IN MEDICAMENTS

Enzymatische Auflösung von Endo-bicyclo(2.2.1)-heptan-2-ol und pharmazeutische Derivate

5-PHENOXY-2-(1H)PYRIMIDINONE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE ENTHALTENDE ARZNEIMITTEL

N-(3-amino-2-hydroxy-propyl) substituted alkylamide compounds.

Disclosed are compounds of the formula (I): useful in treating Alzheimer' s disease and other similar diseases. These compounds include inhibitors of the betasecretase enzyme that are useful in the treatment of Alzeheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical composition and methods of treatment to reduce A beta peptide formation.

N-(3-amino-2-hydroxy-propyl)substituted alkylamidecompounds.

N-(3-amino-2-hydroxy-propyl) substituted alkylamide compounds.

N-(3-amino-2-hydroxy-propyl) substituted alkylamide compounds.

ENZYMATIC DISSOLUTION OF ENDO BICYCLO (2.2.1) - HEPTAN-2-OL AND PHARMACEUTICAL DERIVATIVES

PYRIMIDIN DERIVATIVES, PROCEDURES FOR THEIR PRODUCTION AND THESE CONTAINING COMPOSITIONS.

3 N-SUBSTITUTING 3,4-DIHYDROPYRIMIDINDERIVATE, PROCEDURE FOR YOUR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS.

N-SUBSTITUTING 3,4-DIHYDROPYRIMIDINVERBINDUNGEN AS MEANS FOR the TREATMENT OF ILLNESSES the KARDIOVASKULAREN of the SYSTEM.

ARTHROPODI CARBOXANILIDE

VZH OF NEW HYDROXYPIRIMIDINDERIVATE AND YOUR SALTS

Novel dihydropyrimidine derivatives

ENZYMATIC RESOLUTION OF ENDO-BICYCLO(2.2.1)HEPTAN-2-O1 AND DERIVED PHARMACEUTICAL AGENTS

OPTICALLY ACTIVE INTERMEDIATES

New derivatives of erythromycin, their preparation process, their use as medicaments

CIRCULATION-ACTIVE NEW DIHYDROPYRIMIDINES

Circulatory system-active novel dihydropyrimidines of the formula in which R1 to R6 are diverse organic radicals, and pharmacologically acceptable addition salts thereof.

PROCESS FOR PREPARING NOVEL N-SUBSTITUTED 3,4-DIHYDROPYRIMIDINE DERIVATIVES

A PROCESS FOR PREPARING NOVEL N-SUBSTITUTED 3,4-DIHYDROPYRIMIDINE DERIVATIVES : A N-substituted 3,4-dihydropyrimidine derivative of the formula (1): (1) wherein R1 is -(CH2)n-X; X is substituted aminoethyl, substituted sulfide-ethyl, substituted or non-substituted heterocyclo-ethyl wherein the ethylene group is directly bonded to a hetero atom in the heterocyclic ring, or substituted or non-substituted heterocyclo-methyl wherein the methylene group is directly bonded to a carbon atom in the heterocyclic ring; n is an integer from 0 to 8; R2 is straight, branched, cyclic or cyclo-straight alkyl having from one to thirteen carbon atoms, or aralkyl having from seven to thirteen carbon atoms and pharmacologically acceptable acid addition salts thereof have substantially strong and long lasting effects. Therefore the compounds are useful as agents for treating disorders of the cardiovascular system, for example, antihypertensive agent, circulation improver and antianginal agent. A process ...

MIXTURES OF OPTICALLY ACTIVE CYCLOHEXENONE OXIME ETHERS, THEIR PREPARATION, INTERMEDIATES FOR THIS PURPOSE AND THEIR USE AS HERBICIDES

... 2127464 9316061 PCTABS00025 Mixtures of optically active cyclohexenone oxime ethers, with an R and S configuration in the oxime ether section of formula (I) where R1 = C1-C6 alkyl; Z = (a), (b), (c), (d), (e); X = C1-C4 alkyl, C1-C4 halogen alkyl; m = 0-3 or 1-4 if all X substituents are halogen; n = 0-3 or 1-5 if all X substituents are halogen; R2 = C1-C4-alkoxy-C1-C6-alkyl, C1-C4-alkylthio-C1-C6-alkyl, optionally substituted C3-C7 cycloalkyl, optionally substituted C5-C7 cycloalkenyl, optionally substituted 5-membered saturated heterocylic ring, optionally substituted 6 or 7-membered heterocylic ring, optionally substituted aromatic 5-membered heterocylic ring, optionally substituted phenyl or pyridyl; and their agriculturally usable salts, and esters of C1-C10 carboxylic acids and inorganic acids.

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

A compound of formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

PROCEDE POUR LA PREPARATION DE NOUVELLES HYDROXY-PYRIMIDINES.

PROCEDE POUR LA PREPARATION DE NOUVELLES PYRIMIDINONES.

ПИРИМИДИЛМЕТИЛСУЛЬФОНАМИДНЫЕ СОЕДИНЕНИЯ

Настоящее изобретение касается новых пиримидилметилсульфонамидных соединений и их N-оксидов, их сельскохозяйственно приемлемых солей и их ветеринарно приемлемых солей, а также сельскохозяйственных композиций, содержащих по меньшей мере одно такое соединение в качестве активного компонента, а также их применения для борьбы с вредными грибами. Настоящее изобретение также касается способа борьбы с членистоногими вредителями.

СПОСОБЫ И ПРОМЕЖУТОЧНЫЕ ПРОДУКТЫ, ПОЛЕЗНЫЕ ДЛЯ ПОЛУЧЕНИЯ АНТИФОЛАТОВ

Данное изобретение относится к промежуточным продуктам и способам, относящимся к ним и начинающимся с них, ряду производных пиримидина формулы (V) которые являются промежуточными продуктами для получения полезных антифолатных соединений или сами представляют собой полезные антифолатные соединения. Международная заявка была опубликована вместе с отчетом о международном поиске.

4,4Æ-SULPHONYLBIS-(N,NÆ-DIMETHYL AMONIO METHYLEN ANILIN)-CHLORIDE 6-METHYL-2,4-DIOXO-1,2,3,4-TETRAHYDROPYRIMIDINE-5-SULPHONATE OF THE FORMULA (I) AND PHARMACEUTICAL COMPOSITION BASED THEREON

ANTIVIRAL AGENTS FOR TREATMENT OF HEPATITIS B

N-(3-AMINO-2-HYDROXY-PROPYL) SUBSTITUTED ALKYLAMIDE COMPOUNDS

New derivatives of erythromycin, their preparation process, their use as medicaments

Pyrimidylmethyl-sulfonamide compounds useful as fungicides and against arthropods

METHOD FOR PURIFYING PHENOXY-2(1H)-PYRIMIDINONE ANALOGUES THROUGH RECRYSTALLIZATION

The present invention relates to a method for purifying phenoxy-2(1H)-pyrimidinone derivatives. The method comprises the steps of: dissolving phenoxy-2(1H)-pyrimidinone into an aqueous solution of alkali metal hydroxide, alkaline earth metal hydroxide, alkali metal salt or alkaline earth metal salt with a concentration of 0.5-5N, or into a mixed solution of the above aqueous solution with a polar organic solvent, and adjusting pH with an organic acid or hydrochloric acid to carry out recrystallization; or (2) dissolving phenoxy-2(1H)-pyrimidinone analogues into an aqueous organic acid solution or a mixed solution thereof with a polar organic solvent, followed by cooling and recrystallization. According to the present invention, it is possible to purify phenoxy-2(1H)-pyrimidinone analogues, such as 5-(3-methylphenoxy)-2(1H)-pyrimidinone to high purity, and thus to reduce impurities, which, otherwise, are difficult to remove by the conventional method, to a level defined according to ICH ...

HETEROAROMATIC COMPOUNDS, PROCESS FOR PREPARING THE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, USES AND METHOD OF TREATING THE ACUTE CHRONIC PAIN

2-NITRO, - OXAZINAS, - IMIDAZOLES, PYRIMIDINES Y-TIAZOLES OF ACTION WEED KILLER AND ITS OBTAINING

NEW PYRIDINILPYRIMIDINE DERIVATIVES AND A PROTECTOR FOR ILLNESSES OF PLANTS THAT CONTAIN THEM AS AN ACTIVE INGREDIENT

ARTHROPODICIDAL CARBOXANILIDES

Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein A is H; E is H or C1-C3 alkyl; or A and E can be taken together to form -CH2-, -CH2CH2-, -O-, -S-, -S(O)-, -S(O)2-, -NR8-, -OCH2-, -SCH2-, -N(R8)CH2-, substituted -CH2- and substituted -CH2CH2-, the substituents independently selected from 1-2 halogen and 1-2 methyl; W is N or CR4;X is CR5R6, O, S, NR7 or a direct bond, provided that when W is N, then X is other than a direct bond; Y is H, C1-C6alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, C3-C6 cycloalkylalkyl, NR9R10, N=CR11R12, OR7, COR13, CO2R14 or C1-C6alkyl substituted by at least one group selected from halogen, C1-C3alkoxy, CN, NO2, S(O)rR15, COR13, CO2R14 and optionally substituted phenyl; Z is O or S; and R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, G, n and r are as defined in the disclosure.Also disclosed are compositions containing the compounds ...

INHIBITORS OF POLO-LIKE KINASES

Compounds that inhibit Plk1, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.

FUNGICIDAL 5-PHENYL SUBSTITUTED 2-(CYANOAMINO) PYRIMIDINES

Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or tri-alkyl-silyl, formyl or alkoxycarbonyl, wherein R1 groups are unsubstituted or substituted as defined in the specification; R2 represents phenyl, cycloalkyl or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which are unsubstituted or substituted; R3 represents hydrogen, halogen or alkyl, alkoxy, alkylthio, alkylamino or dialkylamino; which are unsubstituted or substituted; R4 represents hydrogen or alkyl, alkenyl or alkynyl; which are unsubstituted or substituted; and X represents O, S, NR5 or a single bond, wherein R5 represents hydrogen or alkyl; or R1 and R5 together with the interjacent nitrogen atom ...

Retroviral protease inhibiting compounds

A compound of the formula: см. иллюстрацию в PDF-документе is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Substituted tetracycline compounds

The present invention pertains to tetracycline compounds of formula (VIIa): R5*, R5*, R7r*, and R9m* are defined herein. These tetracycline compounds can be used to treat tetracycline compound-responsive states, such as multiple sclerosis and rheumatoid arthritis.

N-substituted 3,4-dihydropyrimidine derivatives, process for the production thereof and composition containing same for treating disorders of cardiovascular system

A N-substituted 3,4-dihydropyrimidine derivative of the formula (1):



wherein R1 is -(CH2)n-X; X is substituted aminoethyl, substituted sulfideethyl, substituted or nonsubstituted heterocyclo-ethyl wherein the ethylene group is directly bonded to a hetero atom in the heterocyclic ring, or substituted or nonsubstituted heterocyclo-methyl wherein the methylene group is directly bonded to a carbon atom in the heterocyclic ring; n is an integer from 0 to 8; R² is straight, branched cyclic or cyclo-straight alkyl having from one to thirteen carbon atoms, or aralkyl having from seven to thirteen carbon atoms and pharmacologically acceptable acid additional salts thereof have substantially strong and long lasting effects. Therefore the compounds are useful as agents for treating disorders of the cardiovascular system, for example, antihypertensive agent, circulation improver and antianginal agent.

A process for producing the above compounds economically and effectively ...

Retroviral protease inhibiting compounds

A compound comprising a substituent of the formula (II) is disclosed as an HIV protease inhibitor. Intermediates for making such compounds and processes for making such intermediates are also disclosed.

НОВЫЕ ПРОИЗВОДНЫЕ ФЛОРОГЛЮЦИНА, ОБЛАДАЮЩИЕ АКТИВНОСТЬЮ В ОТНОШЕНИИ ЛИГАНДА СЕЛЕКТИНА

Изобретение относится к химико-фармацевтической промышленности. Фармацевтические композиции, включающие в себя, по меньшей мере, одно соединение формулы (I), где -Х- представляет собой, например, группу формулы (II) и Y представляет собой, например, группу формулы III, или его фармацевтически приемлемые соли, сложные эфиры или амиды, или пролекарства и фармацевтически приемлемый носитель, который является пригодным в терапии, можно применять для модуляции in vitro и in vivo процессов связывания, опосредуемых связыванием Е-, Р- или L-селектина. 8 н. и 1 з.п. ф-лы, 3 табл.

Способ получения 3-гетероциклических производных 4-нитро-2-хлор(или 2,6-дихлор)-4-трифторметилдифениловых эфиров

CONNECTIONS TO THE TREATMENT AND PRECAUTION WITH DIABETES

PROCEDURE FOR THE PRODUCTION OF BETA ALANINE AMIDES

VERFAHREN ZUR HERSTELLUNG VON NEUEN 2-AMINO-1,4-DIHYDROPYRIDINEN

PROCEDURE FOR the PRODUCTION OF NEW ONE 2-AMINO-1,4-DIHYDROPYRIDINEN

CONNECTIONS THE RETROVIRALE PROTEASE RESTRAINING

4-SUBSTITUTED DIHYDROPYRIDO(4,3-D)PYRIMIDINES AS ANALGESICS AND TOPICAL ANTIINFLAMMATORY AGENTS FOR THE TREATMENT OF SKIN DISORDERS

RADIOACTIVE FLUORINE LABELING PRECURSOR COMPOUND AND METHOD FOR MANUFACTURING RADIOACTIVE FLUORINE LABELED COMPOUND USING THE SAME

... - 60 There is provided a labeling precursor compound represented by the following general formula (2): R2 R 3 (2) ON .S R7 n 02 wherein R1 represents an alkynyl group, an alkynyloxy group, an azide group, an azidoalkyl group, an arylazide group, a monocyclic or condensed polycyclic aryl group or a nitrogen-containing heterocycle; R2 and R3 each 10 independently represent an alkyl group or a hydroxyalkyl group which hydroxy group may be protected with a protecting group, and n is an integer of 1 or 2; R6 represents an alkyl group or -CONR 1 1 R 1 2 wherein R 11 and R1 2 each independently represent an alkyl group or a 15 monocyclic or condensed polycyclic aryl group; and R4, R5 , R 7 and R8 each independently represent a hydrogen atom, an alkyl group or an alkoxy group.

Hepatitis B antiviral agents

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

METHOD FOR CROSS-LINKING RUBBER

HERBICIDALLY ACTIVE 2-NITRO-5-PHENOXYPHENYLOXAZOLES, - OXAZINES, -IMIDAZOLES, -PYRIMIDINES AND -THIAZOLES, AND THE PRODUCTION AND USE THEREOF

Novel 2-nitro-5-phenoxyphenyloxazoles, -oxazines and -thiazoles are disclosed. These compounds have the formula (I) wherein A is a C2-C3alkylene or C2-C3alkenylene radical which can be substituted by C1-C4alkyl or C1-C4haloalkyl, each of R1, R2 and R3 independently is hydrogen, halogen, trifluoromethyl, nitro or cyano, and X is oxygen, sulfur or an imino group. The novel compounds have herbicidal and plant growth-inhibiting properties. They are especially suitable for use as selective herbicides in crops of cereals.

DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES

Provided herein are dihydropyrimidine derivatives which are useful in the treatment of HBV infection or HBV-induced diseases, as well as pharmaceutical or medical applications thereof.

SPECIFIC GLUCOCORTICOSTEROID COMPOUND HAVING ANTI- INFLAMMATORY ACTIVITY

A compound of formula (I): (I) wherein X represents O or S; R1 represents C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkylmethyl or C3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R1 represents aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 represents hydrogen, methyl, which may be in either the .alpha. or .beta. configuration, or methylene; R3 and R4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond; or a physiologically acceptable salt or solvate thereof.

ERYTHROMYCIN DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, AND USE THEREOF AS MEDICAMENTS

DE DIVULGATION L'invention a pour objet les composés de formule (I) : (I) dans lesquels, . ou bien R représente un radical (CH2)n Ar1, n représentant un nombre entier compris entre 1 et 6, Ar1 représentant : - soit un radical aryle carbocyclique substitué, soit un radical aryle hétérocyclique éventuellement substitué, . ou bien R représente un radical X Ar2, dans lequel X est un radical alkyle interrompu par O, S, SO, SO2, , , -C-NH, Ar2 étant un radical aryle ou hétéroaryle éventuellement substitué, Z représentant un atome d'hydrogène ou le reste d'un acide. Les composés de formule (I) présentent d'intéressantes propriétés antibiotiques. L'invention concerne également l'usage d'un ou plusieurs desdits composés pour la préparation de un ou plusieurs desdits composés et un procédé pour la préparation desdits composés.

4-SUBSTITUTED DIHYDROPYRIDO[4,3-D]PYRIMIDINES AS ANALGESICS AND TOPICAL ANTIINFLAMMATORY AGENTS FOR THE TREATMENT OF SKIN DISORDERS

... 4-Substituted Dihydropyrido[4,3-d]pyrimidines as Analgesics and Topical Antiinflammatoxy Agents for the Treatment of Skin Disorders There are described compounds of the formula (see formula I) where R1 is hydrogen, loweralkyl, arylloweralkyl or aryl; R2 when present is hydrogen, loweralkyl, arylloweralkyl; and R3 is hydrogen, loweralkyl, cycloalkyl or aryl; which compounds are useful as analgesics and topical antiinflammatory agents for the treatment of skin disorders.

4-SUBSTITUTED DIHYDROPYRIDO[4,3-D]PYRIMIDINES AS ANALGESICS AND TROPICAL ANTIINFLAMMATORY AGENTS FOR THE TREATMENT OF SKIN DISORDERS

... 1 HOE 90/S 020 4-Substituted Dihydropyrido¢4,3-d!pyrimidines as Analgesics and Topical Antiinflammatory Agents for the Treatment of Skin Disorders There are described compounds of the formula where R1 is hydrogen, loweralkyl, arylloweralkyl or aryl; R2 when present is hydrogen, loweralkyl, arylloweralkyl; and R3 is hydrogen, loweralkyl, cycloalkyl or aryl; which compounds are useful as analgesics and topical antiinflammatory agents for the treatment of skin disorders.

ГИДРОХЛОРИД 4-[[4-[[4-(2-ЦИАНОЭТЕНИЛ)-2,6-ДИМЕТИЛФЕНИЛ]АМИНО]-2-ПИРИМИДИНИЛ]АМИНО]БЕНЗОНИТРИЛА

Настоящее изобретение относится к фармацевтической композиции, включающей в качестве активного ингредиента соль соляной кислоты и 4-[[4-[[4-(2-цианоэтенил)-2,6-диметилфенил]амино]-2-пиримидинил]амино]бензонитрила, и способу ее получения.

N-- (OF 3 - AMINO - OF 2 - HYDRO KSIPROPIL) SUBSTITUTED ALKILAMIDNYE COMPOUNDS

СПОСОБЫ И ПРОМЕЖУТОЧНЫЕ ПРОДУКТЫ, ПОЛЕЗНЫЕ ДЛЯ ПОЛУЧЕНИЯ АНТИФОЛАТОВ

... 1. Соединение формулы III в которой Y представляет СН=СН, О или S; R предоставляет C1-С6-алкил; R1и R2 независимо представляют C1-С6-алкил или взятые вместе с азотом, к которому они присоединены, образуют гетероцикл; R3представляет водород, хлор или фтор; R4 представляет гидрокси, карбоксизащитную группу или NHC*H(С(О)R5)CH2CH2C(O)R5, в которой конфигурация у атома углерода, обозначенного *, представляет S; и R5 представляет водород или карбоксизащитную группу; или его соль или сольват. 2. Соединение по п.1, в котором Y представляет СН=СН или S, R представляет С1-С4-алкил, R1и R2 независимо представляют С1-С4-алкил, R3представляет водород и R4представляет C1-C4-алкокси или бензилокси; или его соль или сольват. 3. Соединение по п.2, в котором R представляет метил или этил, R1и R2, оба, представляют метил или этил и R4представляет метокси, этокси или бензилокси; или его соль или сольват. 4. Соединение формулы IV в которой Y представляет CH=CH, О или S; R3 представляет водород, хлор или фтор ...

4,4'-СУЛЬФОНІЛБІС-(N,N'-ДИМЕТИЛАМОНІОМЕТИЛЕНАНІЛІН)-ХЛОРИД 6-МЕТИЛ-2,4-ДІОКСО-1,2,3,4-ТЕТРАГІДРОПІРИМІДИН-5-СУЛЬФОНАТ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЙОГО ОСНОВІ

Запропоновано 4,4'-сульфонілбіс-(N,N'-диметиламоніометиленанілін)-хлорид 6-метил-2,4-діоксо-1,2,3,4-тетрагідропіримідин-5-сульфонат формули (І), що виявляє антибактеріальну, антимікобактеріальну та імунотропну активності, а також фармацевтичну композицію на його основі .

NOVEL PHLOROGLUCINOL DERIVATIVES HAVING SELECTIN LIGAND ACTIVITY

Pharmaceutical compositions comprising at least one compound of the formula (I) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning -X- is e.g. and Y being e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.

NOVEL COMPOUNDS WHICH HAVE A PROTECTIVE ACTIVITY WITH RESPECT TO THE ACTION OF TOXINS AND OF VIRUSES WITH AN INTRACELLULAR MODE OF ACTION

The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.

Novel antagonists of platelet activating factor

СПОСОБ ПОЛУЧЕНИЯ ОПТИЧЕСКИ АКТИВНОГО (2S)- ИЛИ (2R)-ЭНДО-БИЦИКЛО[2.2.1]ГЕПТАН-2-ОЛА, СПОСОБ ПОЛУЧЕНИЯ 5-(3-[(2R)-ЭКЗО-БИЦИКЛО[2.2.1]ГЕПТ-2-ИЛОКСИ]-4-МЕТОКСИФЕНИЛ)-3,4,5,6-ТЕТРАГИДРОПИРИМИДИН-2(1Н)-ОНА, ОПТИЧЕСКИ АКТИВНЫЙ 5-(3-[ЭКЗО-БИЦИКЛО[2.2.1]ГЕПТ-2-ИЛОКСИ]4-МЕТОКСИФЕНИЛ)-3,4,5, 6-ТЕТРАГИДРОПИРИМИДИН-2(1Н)-ОН, ОПТИЧЕСКИ АКТИВНЫЕ ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ И СПОСОБ ИХ ПОЛУЧЕНИЯ

Использование: биотехнология. Сущность изобретения: оптически активные (2S)-эндобицикло [2.2.1] гептан-2-ол или (2R)-эндо-бицикло [2.2.1] гептан-2ол получают путем трансэтерификации рацемического эндобицикло [2.2.1] гептан-2-ола и 2,2,2-трихлорэтилбутирата в реакционно инертном по существу безводном органическом растворителе в присутствии панкреатической липазы млекопитающих, 5-(3-[(2R)-экзо-бицикло [2.2.1] гепт-2-илокси-4-метоксифенил) -3,4,5,6-тетрагидропиринидин-2(1H)-он получают взаимодействием (2S)-эндо-бицикло [2.2.1] -гептан-2-ола с по меньшей мере одним моль-эквивалентом 3-гидрокси-4-метоксибензальдегида в присутствии одного моль-эквивалента каждого из веществ: трифенилфосфина и диэтилазодикарбоксилата в реакционно инертном растворителе при 50-100oC, образующийся 3-(3- [(2R)-экзо-бицикло-[2.2.1] гепт-2-илокси]-4метоксибензальдегид) обрабатывают двумя моль-эквивалентами цианоуксусной кислоты в пиридине в присутствии каталитического количества пиперидина, образующийся 3-(3-(2R)-экзобицикло ...

ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ АСПАРТИЛЬНОЙ ПРОТЕАЗЫ

... 1. Соединение, имеющее структурную формулу I ! ! или его стереоизомер, таутомер или фармацевтически приемлемая соль или сольват, где W представляет собой связь, -C(=S)-, -S(O)-, -S(O)2-, -С(=O)-, -O-, -C(R6)(R7)-, -N(R5)- или -C(=N(R5))-; ! X представляет собой -O-, -N(R5)- или -C(R6)(R7)-; ! U представляет собой связь или -(C(R3)(R4))b-, где b равен 1 или 2; ! R1, R2 и R5 независимо выбраны из группы, состоящей из атома водорода (Н), алкила, арилалкила, гетероарилалкила, циклоалкилалкила, гетероциклоалкилалкила, арилциклоалкилалкила, гетероарилциклоалкилалкила, арилгетероциклоалкилалкила, гетероарилгетероциклоалкилалкила, циклоалкила, арилциклоалкила, гетероарилциклоалкила, гетероциклоалкила, арилгетероциклоалкила, гетероарилгетероциклоалкила, алкенила, арилалкенила, циклоалкенила, арилциклоалкенила, гетероарилциклоалкенила, гетероциклоалкенила, арилгетероциклоалкенила, гетероарилгетероциклоалкенила, алкинила, арилалкинила, арила, циклоалкиларила, гетероциклоалкиларила, циклоалкениларила ...

СПОСОБ ПОЛУЧЕНИЯ 4-П-АЛКОКСИФЕНИЛ-2,6-ДИОКСОГЕКСАГИДРОПИРИМИДИНОВ

Способ получения 2-арил-2,3-дигидроперимидинов

Способ получения 2-(1',3'-диоксолан-2-илметил)-2,4(6)-диметил-2,3-дигидропиримидина

PYRIMIDINECARBOXYLIC ACID DERIVATIVES

Use of myocyanine derivatives for the protection of human hair and skin from UV radiation

The use of myocyanine derivatives of the general formula (1) for the protection of human hair and skin from the damaging effect of ultraviolet radiation: wherein Q is hydrogen, C1-22 alkyl, OH, OR7, NR R , or N=R ² ; R Ü or substituents; R4 is cyano, COR , COOR or other substituents; R Å is COR , COOR or other substituents; R6 is hydrogen, C1-22 alkyl, C1-22 alkoxy or COR ; R and R are hydrogen, C1-22 alkyl or other substituents including silicon-containing substituents; R ² is a C1-6 alkylidene radical; R Ü and R Þ ,R Ü and Q,R Ü and R Û , R Ü and T, R Þ and R ý , R Þ and R Ú , R2 and R6, R Þ and Q, R Ú and R6, R Ú and T, R Û and Q, T and Q may each be linked together so that 1-4 carbocyclic or N, O and/or S-containing heterocyclic rings are formed wherein each ring may be condensed with an aromatic or heteroaromatic ring; n is 1 to 4; wherein at least one of R Ü , R Û or Q is not hydrogen; and T is COR5, CN or other substituents. Cosmetic compositions and UV absorber dispersions comprising ...

PYRIMIDONES

... 1377308 Substituted 5-phenoxy and 5-thiophenoxy-2-(1H)-pyrimidinones PFIZER Inc 18 Feb 1972 [29 Oct 1971] 7748/72 Heading C2C Novel compounds of the Formula I: wherein R is hydrogen or methyl, R 1 is oxygen or sulphur, R 2 is hydrogen, halogen or methyl and R 3 is hydrogen, methyl, chloro or trifluoromethyl and pharmaceutically acceptable salts thereof may be prepared by reacting a compound wherein R 6 and R 7 are C 1-3 alkyl groups, with a reagent prepared from ethanol, sodium and urea and if necessary reacting the product with an alkali metal or alkaline earth metal salt and hot methyl iodide to introduce the methyl group at R. 2 - (p - Chlorophenoxy) - 3 - dimethylaminoacrolein may be prepared by reacting potassium p-chlorophenolate, prepared in situ, with chloroacetaldehyde diethylacetal to yield pchlorophenoxyacetaldehyde diethyl acetal which on reaction with dimethyl formamide in the presence of phosphorus oxychloride cyclizes to the required intermediate. Pharmaceutical compositions ...

PROCEDURE FOR the PRODUCTION OF NEW ONE 2-AMINO-1,4-DIHYDROPYRIDINEN

NEW DIHYDROPYRIMIDINE, PROCEDURES FOR YOUR PRODUCTION AS WELL AS YOUR USE IN DRUGS.

N-SUBSTITUTING 3,4-DIHYDROPYRIMIDINDERIVATE, PROCEDURE FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPILATION.

(7 - (3-DISUBSTITUTED AMINO) PHENYL> PYRAZOLO (1,5A>-PYRIMIDINES.

HETEROAROMATIC SUBSTITUTED CYCLOPROPANE AS CORTICOTROPIN RELEASING HORMONE

New derivatives of erythromycin, their preparation process, their use as medicaments

PYRIMIDINONES AND HYDROXY PYRIMIDINES

HERBICIDAL SULFONAMIDES

[7-(3-DISUBSTITUTED AMINO)PHENYL]-PYRAZOLO[1,5- A]PYRIMIDINES

SUBSTITUTED TETRACYCLINE COMPOUNDS

The present invention pertains, at least in part, to a substituted tetracycline compound of Formula (I): wherein X is CHC(R13VY), CR6 R6, C=CR6 R6, S, NR6, or O; E is NR7dR7.beta., OR7f or (CH2)o.iC(=W)WR7s; W is O, S, NR711 or CR75R7*; W is O, S or NR7*; These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.

ENZYMATIC RESOLUTION OF ENDO-BICYCLO[2.2.1]HEPTAN-2-OL AND DERIVED PHARMACEUTICAL AGENTS

Process for the pancreatic lipase mediated trans-esterification method for the optical resolution of endo-norborneol; derived optically active 5-(3-(exo-bicyclo¢2.2.1!hept-2-yloxy)-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-ones; and stepwise process and intermediates therefor.

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

A compound of formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

NEW COMPOUNDS

There are provided novel compounds of formula (I) including their 3,4dihydropyrimidine tautomer form, wherein R1, R2, R3, R4, R5, X and n are as defined in the specification, and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are antagonists of N-type neuronal calcium channels useful in the treatment of cerebrovascular ischaemia and pain.

COMPOUNDS FOR TREATING AND PREVENTING DIABETIC COMPLICATIONS

This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, (see above formula) wherein R is as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith ...

ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING SAME

The present invention relates to a novel organic compound represented by chemical formula 1 and to an organic electroluminescent device which has improved light-emitting efficiency, driving voltage, and lifespan properties by including the novel compounds in one or more organic layers. COPYRIGHT KIPO 2016 ...

ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE CONTAINING SAME

The present invention relates to a novel organic compound which is represented by chemical formula 6, and an organic electroluminescent device having improved characteristics such as luminous efficiency, driving voltage and lifespan by containing the same in one or more organic layers. COPYRIGHT KIPO 2018 ...

COMPOSITION, COMPOSITIONS HERBICIDA AND FOR DESSECAÇÃO AND/OR DESFOLIAÇÃO OF PLANTS, METHODS TO CONTROL THE UNDESIRABLE VEGETATION AND FOR THE DESSECAÇÃO/DESFOLIAÇÃO OF VEGETABLES, AND PROCESSES FOR THE PREPARATION OF A COMPOSITION AND THE PREPARATION OF A SULFAMOIL

Salt of dihydropyrimidine derivative

本发明涉及二氢嘧啶衍生物：4-(2-氯-4-氟苯基)-6-(吗啉-1-基甲基)－2－(2,4,6-三氟苯基)-1,4-二氢嘧啶－5－羧酸乙酯的富马酸盐或其药物学上可接受的溶剂化物及其在制备治疗乙型肝炎药物中的应用。

Novel n-substituted 3,4-dihydropyrimidine derivatives, processes for preparing them and pharmaceutical compositions

Novel N-substituted 3,4-dihydropyrimidine derivatives, processes for preparing them and pharmaceutical compositions

N-substituted 3,4-dihydropyrimidine derivatives of the formula:wherein X'. X², X³ and R', R² have the meanings shown in the claims, and pharmaceutically acceptable acid addition salts thereof. In form of pharmaceutical compositions they are useful as agents for treating disorders of the cardiovascular system, for example, as hypotensive agents, agents for ameriolation of brain circulation and anti-angina pectoris agents. Processes for producing the above compounds economically and effectively are also disclosed.

高純度イミダゾリウム塩の製造方法

【課題】建物又は乗用車の換気及び空気調整のための空調システムに用いられるジアルキルイミダゾリウムイオンを含有するイオン性液体の製造において、原料である揮発性化合物のＮ−アルキルイミダゾールの残留量を最小限にし、かつ、イオン性液体が着色されない、前記製造方法の提供。【解決手段】Ｎ−メチルイミダゾールに代表されるＮ−アルキルイミダゾール誘導体と、トリエチルホスフェートに代表されるトリアルキルホスフェートとを、水の存在下で反応させる工程を含む、１，３−ジアルキルイミダールジアルキルホスフェート誘導体の製造方法。【選択図】なし

Metodo para preparar pirimidas 2-il-aminas por reaccion entre un ester y una anilina.

Método de preparación de compuestos derivados de n-fenil-(2-piridin)-amina sustituida, útiles para tratar el cáncer.