БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, СПОСОБ ПОДАВЛЕНИЯ СЛИПАНИЯ ТРОМБОЦИТОВ И КОМПОЗИЦИЯ ДЛЯ ЕГО ОСУЩЕСТВЛЕНИЯ

Описываются новые бициклические соединения, имеющие ядро, сформированное из двух конденсированных шестичленных колец, А и В, представленное формулой I, либо фармацевтически приемлемая соль, сольват или пролекарственная производная этого соединения, в котором бициклическое ядро из колец А и В выбирается из группы, состоящей из формул (17)-(21), R3 является кислотной группой, содержащей кислотный радикал, выбранный из формул группы (С), n = 0-6; R0 является одинаковым или разным и выбирается независимо из водорода, алкила, связующая группа -(L)- является связью или выбирается из формул -C(=O)-N(H)- и -С(Н2)-O-, Q является основной группой и выбирается из амидиногруппы и пиперидина. Новые бициклические соединения полезны в качестве препаратов, нейтрализующих действие гликопротеина IIв/IIIа, для предотвращения тромбоза. Описывается также способ подавления слипания тромбоцитов и композиция для его осуществления. 13 с. и 12 з.п. ф-лы, 1 табл.

ПРОИЗВОДНЫЕ ИМИДАЗОЛА

Описываются производные имидазола общей формулы I, II или III, представляющие где m = 0; n = 1; r, s и t = 0 или 1; p = 0, 1 или 2; V представляет собой водород; W и X представляют собой независимо водород или кислород; Y представляет собой CHR9 или СО; Z представляет собой CHR9, CO, CО2, SО2, SО3, CONR12, CN(CN), CN(CN)NR13, или Z может отсутствовать; R4 представляет собой Н; R5 представляет собой Н, гало, нитро, циано или U-R23, где U представляет собой NR24, SO2, СО2, NR26СОNR27, NHSO2, CONH или NHCO или U может отсутствовать; R1, R2, R3 независимо представляют собой водород, низший алкил, необязательно замещенный гидрокси, фенилом, нафтилом или имидазолом; С3-C6 циклоалкил; алкокси; фенокси; пиридил; фенил; нафтил; имидазол; или любой из R1, R2 и R3 может быть соединен с образованием циклоалкильной группы; R6, R7, R8, R9, R12, R13, R26 и R27 независимо представляют собой водород, необязательно замещенный низший алкил, где указанным заместителем является амино или фенильная группа; или ...

ПРОИЗВОДНЫЕ 2-ГИДРОКСИЭТИЛ-1Н-ХИНОЛИН-2-ОНА И ИХ АЗАИЗОСТЕРИЧЕСКИЕ АНАЛОГИ С АНТИБАКТЕРИАЛЬНОЙ АКТИВНОСТЬЮ

Изобретение относится к соединениям формулы (I) и их фармацевтически приемлемым солям, обладающим антибактериальными свойствами, а также к фармацевтической композиции на их основе. В формуле (I) Rпредставляет собой алкоксигруппу; каждый из U и V представляет собой СН и W представляет собой N, или U представляет собой N, V представляет собой СН и W представляет собой СН или N, или каждый из U и V представляет собой N и W представляет собой СН; Rпредставляет собой водород или фтор, если W представляет собой СН, или Rпредставляет собой водород, если W представляет собой N; А представляет собой О или СН; Y представляет собой СН или N; Q представляет собой О или S; и n представляет собой 0 или 1. 2 н. и 21 з.п. ф-лы, 3 табл., 15 пр.

ПРОТИВОСУДОРОЖНЫЕ СУЛЬФАМАТЫ ПСЕВДОФРУКТОПИРАНОЗЫ

Соединение, имеющее формулу I где R1 и R2 могут быть одинаковыми или различными и выбираются из водорода, (C1-C6)алкила, (C3-C7)циклоалкила, аллила или бензила; R3 и R4 могут быть одинаковыми или различными и выбираются из водорода или (C1-C6)алкила; X выбирают из углерода (C) или серы (S), при условии, что когда X представляет собой углерод, R5 и R6 могут быть одинаковыми или различными и выбираются из водорода или (C1-C6)алкила, тогда как если X является серой, один из R5 и R6 является кислородом, а второй представляет собой свободную пару электронов, или оба они являются кислородами, или его фармацевтически приемлемая соль, гидрат, аномер, диастереомер или энантиомер. 2. Соединение по п. 1, в котором каждый из R1 и R2 является водородом. 3. Соединение по п. 1, в котором X является углеродом. 4. Соединение по п. 1, в котором X является серой. 5. Соединение по п. 4, в котором каждый из R5 и R6является кислородом. 6. Соединение по п. 4, в котором R5 и R6 представляют собой свободную пару ...

Способ получения гетероциклических соединений

N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung

CARBONAT- UND CARBAMAT-PRODRUGS VON THIAZOLO Ä4,5-DÜ-PYRIMIDINEN

Quinoline and quinazoline compounds useful in therapy

Antifungal sordan derivatives.

A compound of formula ...

Quinoline and quinazoline compounds useful in therapy.

The invention provides compounds of formula I. fluorine atoms; icier.. C1-6aikoxy and R1 represents C1-. alkoxy optionally substituted by one or —ore fluor R: represent H or C-6 alkax.y optionally substituted by one or more R3 represents one or more groups independently selected from H. h Cf; in addition. R: and one RJ srcup may together represent -OCH;-.the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyciic ring containing selected from N, 0 and S, the ring being optionally fused to a benzene membered heterocyciic ring containing 1 or 2 hereroatoms selected ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceuticaily acceptable salts thereof The compounds of formula I are useful in the treatment of inter alia prostatic hyperplasia ...

Quinoline and quinazoline compounds useful in therapy

Radiant energy collecting apparatus

Stable copper(i) complexes and methods related thereto

Quinoline and quinazoline compounds useful in therapy.

New derivatives of the pyrrole, their preparation and the compositions pharmaceutical which contain them.

New heterocyclic compounds and their preparation.

New derivatives of Oxathiinno (1,4) (2,3-C) wintergreen, their preparation and the compositions which contain them.

New derivatives of the carboxyméthoxy-E furo- (3,4-c) - therapeutic pyridine, their preparation and compositions containing these compounds.

Antifungal sordaridin derivatives

Radiant energy collecting apparatus

PROCEDURES FOR THE PRODUCTION OF OXAZOLINO AZETIDINYLPENTENCARBONSAEUREDERIVATEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN TRISUBSTI- TUIERTEN 1-PHENYL-2,3,4,5-TETRAHYDRO-1H-3- -BENZAZEPINEN UND IHREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN PIPERAZINDERIVATEN

HETERO-CYCLIC CONNECTIONS, YOUR PRODUCTION AND YOUR USE AS ANTIBACTERIAL MEANS

VERFAHREN ZUR HERSTELLUNG EINES NEUEN 5-MERCAPTOPYRIDOXINDERIVATES UND SEINER ADDITIONSSALZE

VERFAHREN ZUR HERSTELLUNG VON OXAZOLINO- AZETIDINYLPENTENCARBONSAEUREDERIVATEN

NEW CEFALOSPORINDERIVATE, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE

PURINYL AND PYRIMIDINYLTETRAHYDROFURANE

USE OF PERMANENT FREE RADICALS RESONANCE MAGNETIC FOR THE IMAGING OF MEANS

AMINOACYLLABDANE, PROCEDURE AND INTERMEDIATE PRODUCTS FOR YOUR PRODUCTION AND YOUR USE AS DRUGS.

CHINOLINE USEFUL AS ANTI-ALLERGY MEANS.

TRICYCLIC MONO SACCHARIDE DERIVATIVES USABLE WITH THE TREATMENT OF ACUTES ISCHAMISCH INDUCED NEURO DEGENERATIONS

PROCEDURE FOR the PRODUCTION OF NEW DERIVATIVES (1,4) OXATHIINO (2,3-C) of the PYRROLS AND OF THEIR SALTS

CYCLI UREA AND ANALOGUES USABLE AS RETROVIRALE OF PROTEASEHEMMER

FIBRINOGEN RECEPTOR ANTAGONISTS

Antifungal sordaridin derivatives

Quinoline and quinazoline compounds useful in therapy

CYCLIC UREAS AND ANALOGUES USEFUL AS RETROVIRAL PROTEASE INHIBITIORS

ANTIOXIDANTS

MODULATORS OF PROTEIN TYROSINE PHOSPHATASES

The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTP.alpha., PTP.epsilon., PTP.mu., PTP.delta., PTP.sigma., PTP, PTP.beta., PTPD1, PTPD2, PTPH1, PTP- MEG1, PTP-LAR, and HePTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes.

12,13-MODIFIED EPOTHILONE DERIVATIVES

The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.

TRICYCLIC MONOSACCHARIDE DERIVATIVES USEFUL IN TREATING ACUTE ISCHEMIA-INDUCED NEURODEGENERATION

Anticonvulsant compounds of general formula (I) where X, R1, R2, R3, R4, R5, and R6 are as herein defined; are useful in treating acute ischemia-induced neurodegeneration, such as occurs during and after stroke, head trauma, spinal injury, non-fatal cardiac arrest, or major surgical procedures. Furthermore, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use are disclosed.

DERIVATIVES AND ANALOGS OF N-ETHYLQUINOLONES AND N-ETHYLAZAQUINOLONES

Bicyclic nitrogen containing compounds and their use as antibacterials.

QUINOLINE AND QUINAZOLINE COMPOUNDS USEFUL IN THERAPY

The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent -OCH2-, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of inter alia benign prostatic ...

Verfahren zur Herstellung von Indolyloverbindungen

Subst 2-methyl 3-hydroxypyridines

A. Cyclic pyridoxol derivatives of general formula (I): X = a group derived from a polybasic inorganic acid or its derivatives, preferably its low alkyl- or phenyl derivative. B. Process: R = cyano, an ether bound hydrocarbon group such as an ether bound alkyl group with 1-10 C-atoms, a heterocyclic alkyl group, an aralkyl group or an aryl group. The compounds (I) are intermediates in the new process in which they can be converted easily to pyridoxine, vitamin B6. The new process is simple and economical.

Verfahren zur Herstellung von 1,2-Bis-(carboxy-methylthio)-3,6-dihydroxyaryl- -lacton

Verfahren zur Herstellung von Indolylverbindungen

Verfahren zur Herstellung von Benzodiazepinen

PROCEDURE FOR THE PRODUCTION OF NEW MERCAPTOMETHYLPYRIDIN DERIVATIVES.

PROCEDURE FOR THE PRODUCTION OF PYRIDINDERIVATEN.

PROCEDURE FOR the PRODUCTION of TRISUBSTITUTED 1-PHENYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE.

DERIVATIVES-FURO - [...]-TO-7 (3.4 C) - PYRIDINE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC COMPOSITIONS BASED ON SUCH COMPOUNDS.

АНТИБАКТЕРИАЛЬНЫЕ КОМПОЗИЦИИ, ИМЕЮЩИЕ ШИРОКИЙ СПЕКТР АКТИВНОСТИ

Изобретение относится к новым антибактериальным соединениям формулы (I), фармацевтическим композициям, содержащим эти соединения, а также к применению указанных соединений в качестве противомикробных лекарственных средств ...

MODULATORS OF, THE METHODS OF THEIR OBTAINING AND THEIR APPLICATION

ANTIBACTERIAL COMPOSITIONS, HAVING BROAD SPECTRUM ACTIVITY

КАРБАМОИЛЬНЫЕ ПРОИЗВОДНЫЕ БИЦИКЛИЧЕСКИХ КАРБОНИЛАМИНОПИРАЗОЛОВ В КАЧЕСТВЕ ПРОЛЕКАРСТВ

Обеспечиваются бициклические карбониламинопиразолы формулы (I), где переменные имеют значения, определенные в формуле изобретения, для использования в качестве лекарственного средства, в частности для лечения заболеваний, вызванных нарушением функции протеинкиназ (РК), таких как рак, фармацевтические композиции, включающие такие карбамоильные производные, и их применение в качестве пролекарств терапевтически активных веществ. Способ лечения и некоторые новые бициклические карбониламинопиразолы также являются объектом настоящего изобретения.

Oxadiazine derivatives

ACC INHIBITORS AND USES THEREOF

COMPOUNDS OF DIOXINEPYRIDINES, A METHOD FOR PRODUCING THEREOF (VARIANTS), A PHARMACEUTICAL COMPOSITION BASED THEREON AND A METHOD FOR PRODUCING THEREOF

КАРБАМОИЛЬНЫЕ ПРОИЗВОДНЫЕ БИЦИКЛИЧЕСКИХ КАРБОНИЛАМИНОПИРАЗОЛОВ В КАЧЕСТВЕ ПРОЛЕКАРСТВ

Обеспечиваются бициклические карбониламинопиразолы формулы (I), где переменные имеют значения, определенные в формуле изобретения, для использования в качестве лекарственного средства, в частности, для лечения заболеваний, вызванных нарушением функции протеинкиназ (PK), таких как рак, фармацевтические композиции, включающие такие карбамоильные производные и их применение в качестве пролекарств терапевтически активных веществ. Способ лечения и некоторые новые бициклические карбониламинопиразолы также являются объектом настоящего изобретения.

ПРОИЗВОДНЫЕ И АНАЛОГИ N-ЭТИЛХИНОЛОНОВ И N-ЭТИЛАЗАХИНОЛОНОВ

Бициклические азотсодержащие соединения общей формулы (I) и их применение в качестве противобактериальных средств.

МОДУЛЯТОРЫ АУРОРА КИНАЗЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ИХ ПРИМЕНЕНИЕ

Изобретение относится к химическим соединениям, имеющим общую формулу или их стереоизомерам или фармацевтически приемлемым солям, где A1, A2, C1, С2, L1, L2, Z, D, R3-4 и R6-8 определены в описании, которые способны модулировать ауроракиназы, влияя при этом на процесс клеточного цикла и пролиферацию клеток с целью лечения рака и болезней, связанных с раком. Изобретение также предусматривает способ получения указанных соединений, фармацевтические композиции, включающие указанные соединения, и применение указанных соединений при лечений болезненных состояний, связанных с активностью ауроракиназы, в частности различных форм рака.

DERIVATIVES OF SUGARS, CONTAINING SULFUR-CONTAINING FRAGMENTS, METHODS OF THEIR SYNTHESIS AND METHODS OF THEIR APPLICATION FOR TREATMENT OF THE MPS IIIC

АНТИБАКТЕРИАЛЬНЫЕ СОЕДИНЕНИЯ С ШИРОКИМ СПЕКТРОМ ДЕЙСТВИЯ

Изобретение относится к новым антибактериальным соединениям, фармацевтическим композициям, содержащим их, и их использованию в качестве антимикробных средств. Пункты: 4 независимых 12 зависимых Табл.: 3 ...

SUBSTITUTED BENZOL[E] [1,4] OXAZINO[3,2-G] ISOINDOLE DERIVATIVES, METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

ANTIBACTERIAL COMPOUNDS HAVING BROAD SPECTRUM OF ACTIVITY

(54) Azepin Derivatives to Inhibiting Farnesyl Protein Transferase and Method for Treatment

Process for the preparation of thiazolopyrimidines

式(I)化合物、其可药用盐或溶剂化物的制备方法：其是从式IV化合物开始制备的；其中L表示离去基团。

Heteroaryl and pyrimidine dione derivative and use thereof

Organic compound taking fluorene as core and application of organic compound in organic electroluminescent device

NEW DERIVATIVES OF CARBOXYMETHOXY-7 FURO- (3,4-C) - PYRIDINE LIKE THEIR METHOD OF PREPARATION

NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS USEFUL AS ANTI-INFLAMMATORY ANALGESIC STRONG STATEMENT

NOUVEAUX DERIVES DE LA CARBOXYMETHOXY-7 FURO-(3,4-C)-PYRIDINE AINSI QUE LEUR PROCEDE DE PREPARATION

L'INVENTION CONCERNE DE NOUVEAUX DERIVES DE LA DIHYDRO-1,3 METHYLE-6 FURO-(3,4-C)-PYRIDINE REPONDANT A LA FORMULE GENERALEI: (CF DESSIN DANS BOPI) DANS LAQUELLE CHACUN DES SUBSTITUANTS A ET A REPRESENTE DIVERS SUBSTITUANTS HYDROCARBONES AINSI QU'UN PROCEDE DE PREPARATION DE CES DERIVES CONSISTANT A TRAITER UN COMPOSE REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) PAR LE BROMOACETATE D'ETHYLE A UNE TEMPERATURE COMPRISE ENTRE 10 ET 70C, EN PRESENCE DE DIMETHYLFORMAMIDE, PUIS A HYDROLYSER L'ESTER RESULTANT PAR L'HYDROXYDE DE SODIUM.

NEW DERIVATIVES Of the OXATHIINNO (1,4) (2,3-C) PYRROLE, THEIR PREPARATION AND the COMPOSITIONS WHICH CONTAIN THEM

ANTIBACTERIAL COMPOUNDS HAVING BROAD SPECTRUM OF ACTIVITY

PROCESO PARA LA ELABORACION DE DERIVADOS DE PIRIDAZINA COMO INTERMEDIARIOS DE SINTESIS DE ANTIBIOTICOS

Un intermediario de síntesis utilizado comúnmente en la preparación de compuestos antibióticos, o para la elaboración de sales de ese compuesto. La presente se relaciona asimismo con compuestos intermedios utilizados en dicho proceso, es decir 6,7-dihidro-[1,4]oxatiino[2,3-c]piridazin-3(2H)-ona, trifluorometansulfonato de 6,7-dihidro-[1,4]oxatiino[2 ,3-c]piridazin-3-ilo y 6,7-dihidro-[1,4]oxatiino[2,3-c]piridazin-3-carboxilato de metilo y con las sales del mismo. Reivindicación 1: El compuesto de la fórmula (1) o una sal de dicho compuesto. Reivindicación 2: Un proceso para la elaboración del compuesto de la fórmula (1) de acuerdo con lo definido en la reivindicación 1, donde dicho proceso comprende los siguientes dos pasos: a) la reacción del compuesto de la fórmula (2) con 2-mercaptoetanol en presencia de una base en un solvente aprótico polar o una mezcla aprótica polar de solventes y b) la reacción del intermediario obtenido después del paso a) anterior con trifenilfosfina y azodicarboxilato ...

PREPARATION OF PYRIDINES 2-METHYL-3 DIHYDRO-4 5 DISUBSTITUTED

FORFARANDE FOR FRAMSTELLNING AV MERKAPTOALKYLPYRIDINER MED EN ETENYLSUBSTITUENT

ANTIBACTERIAL COMPOUNDS HAVING BROAD SPECTRUM OF ACTIVITY

The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.

5-AMINO-2-(1-HYDROXY-ETHYL)-TETRAHYDROPYRAN DERIVATIVES

The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy (notably methoxy); R2 represents H or F; each of R3, R4, R5 and R6 represents independently H or D; V represents CH and W represents CH or N or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH2; and A represents CH2, CH2CH2 or CD2CD2; and salts of such compounds.

INHIBITORS OF FARNESYL PROTEIN TRANSFERASE

This invention relates to compounds that inhibit farnesyl-protein transferase and ras protein farnesylation, thereby making them useful as anti-cancer agents. The compounds are also useful in the treatment of diseases, other than cancer, associated with signal transduction pathways operating through ras and those associated with proteins other than ras that are also post-translationally modified by the enzyme farnesyl protein transferase. The compounds may also act as inhibitors of other prenyl transferases, and thus be effective in the treatment of diseases associated with other prenyl modifications of proteins.

Method for 6-bromination of 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine compounds

The preparation of 6-bromo-7,8-dimethoxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines is described by direct bromination of the nucleus.

Compound useful for manufacturing salacinol, method for manufacturing the compound, method for manufacturing salacinol, methods for protecting and deprotecting diol group, and protective agent for diol group

... (In the formula, each of R1a and R1b is a hydrogen atom or a hydroxy protective group; R2 is a hydroxy group or the like; and R3 is a hydroxy group or the like.) ...

PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES

ЗАМЕЩЕННОЕ АРОМАТИЧЕСКОЕ СОЕДИНЕНИЕ С КОНДЕНСИРОВАННЫМ КОЛЬЦОМ, СПОСОБ ПОЛУЧЕНИЯ, ГЕРБИЦИДНАЯ КОМПОЗИЦИЯ И ЕЕ ПРИМЕНЕНИЕ

Изобретение относится к замещенному ароматическому соединению с конденсированным кольцом, представленному общей формулой I, которое может найти применение в качестве гербицида для борьбы с сорняками. В формуле I Q является Q-1-Q-6, Q-8-Q-12, Q-14-Q-17, Q-31 или Q-32, Y является галогеном, галоC1-C8 алкилом или циано; Z является галогеном; M является CH или N; Q1, Q2, Q3, Q4, Q5, Q6 каждый независимо является O или S; Het является циклической структурой, связанной посредством двух атомов углерода в 4- и 5-положениях с изоксазолиновым кольцом с образованием конденсированного кольца; циклическая структура является 3-8-членным насыщенным или ненасыщенным карбоциклилом или насыщенным или ненасыщенным гетероциклилом, содержащим 1 гетероатом, выбранный из O, S, CO или C=N-O-R14; за исключением 4- и 5-положений, которые соответственно замещены X2 или X1, другие положения на Het каждое независимо не замещено или замещено по меньшей мере одной группой, выбранной из галогена, С1-С8 алкила, -OR14 или ...

Оксатиепино[6,5-b]дигидропиридины и связанные с ними композиции и способы

... 1. Соединение формулы I где (a) R1, R2, R3, R4 и R5, независимо, выбраны из группы, состоящей из Н, ОН, галогена, циано, NO2, алкила, C1-8-алкокси, C1-8-алкилсульфонила, С1-4 -карбоалкокси, C1-8-алкилтио, дифторметокси, дифторметилтио, трифторметила и оксадиазола (образованного R1 и R2); (b) R6 выбран из группы, состоящей из H, неразветвленного или разветвленного C1-5-алкила, арила, 3-пиперидила, N-замещенного 3-пиперидила, N-замещенного 2-пирролидинилметилена и замещенного алкила, из которых указанный N-замещенный 3-пиперидил и указанный N-замещенный 2-пирролидинилметилен могут быть замещены C1-8-алкилом с неразветвленной или разветвленной цепью или бензилом, а указанный замещенный алкил может быть замещен C1-8-алкокси, С2-8-алканоилокси, фенилацетилокси, бензоилокси, гидрокси, галогеном, п-тозилокси, мезилокси, амино, карбоалкокси или группой NR’R’’, в которой (i) R’ и R’’, независимо, выбраны из группы, состоящей из Н, неразветвленного или разветвленного C1-8-алкила, С3-7-циклоалкила ...

Способ получения хиноксалино-(2,3-b)(1,4)-тиазинонов-2

Способ получения производных оксазо-лиНОАзЕТидиНилпЕНТЕНОВОй КиСлОТы

ANTIFUNGALE SORDARIDIN-DERIVATE

Verfahren zur Herstellung von Tetrathiafulvalen-Derivaten und ihrer Vorläufer

4,5,6,7-TETRAHYDRO-1H-IMIDAZO(4,5-C)PYRIDINDERIVATE UND ANALOGE MIT ANTIHYPERTENSIVER WIRKUNG.

NOVEL PHENAZINE DERIVATIVES AND THEIR USES

The present invention is directed to novel compounds of formula I 2. The compound according to and pharmaceutically acceptable salts and solvates thereof claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each H.11. A pharmaceutical composition comprising a compound according to or a pharmaceutically acceptable salt or solvate thereof and at least one pharmaceutically acceptable carrier claim 1 , diluent claim 1 , excipient and/or adjuvant.12. Medicament comprising a compound according to or a pharmaceutically acceptable salt or solvate thereof.1316-. (canceled)17. A method of treating cancer comprising administering to a patient in need thereof a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof.18. A method of treating an angiogenic disorder comprising administering to a patient in need thereof a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof.19. A method of treating an inflammatory claim 1 , immune or infectious disease comprising administering to a patient in need thereof a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof.20. A method for birth control claim 1 , comprising administering to a patient in need thereof a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof. The present invention relates to novel phenazine derivatives including their pharmaceutically acceptable salts and solvates, which are useful as anti-angiogenic and/or anti-tumor agents, in particular under hypoxic conditions.Angiogenesis is a highly regulated process, whereby new blood vessels form from preexisting ones (Folkman J. Nat. Rev. Drug Discov. 2007; 6: 273-86). In adult mammals, physiologic angiogenesis is largely limited to the ovaries, uterus, and placenta, with the turnover rate of vascular endothelial ...

CHROMENE COMPOUND

A novel photochromic compound which develops a color of a neutral tint (double peak characteristic) and has high color optical density, high fading speed and excellent durability. 2. A photochromic curable composition which comprises the chromene compound of and polymerizable monomers.3. A photochromic optical article having a polymer molded body containing the above chromene compound of dispersed therein as a constituent member.4. An optical article having an optical substrate at least one surface or all of which is covered with a polymer film containing the chromene compound of dispersed therein as a constituent member. The present invention relates to a novel chromene compound which is useful as a photochromic compound for photochromic spectacle lenses.Photochromism is the reversible function of a certain compound that it changes its color swiftly upon exposure to light including ultraviolet light such as sunlight or light from a mercury lamp and returns to its original color when it is put in the dark by stopping its exposure to light. A compound having this property is called “photochromic compound” and used as a material for photochromic plastic lenses.For the photochromic compound used for this purpose, the following properties are required: (I) the degree of coloration at a visible light range before ultraviolet light is applied (to be referred to as “initial coloration” hereinafter) should be low, (II) the degree of coloration upon exposure to ultraviolet light (to be referred to as “color optical density” hereinafter) should be high, (III) the speed from the time when the application of ultraviolet light is started to the time when the color optical density reaches saturation (to be referred to as “color development sensitivity” hereinafter) should be high; (IV) the speed from the stoppage of the application of ultraviolet light to the time when the compound returns to its original state (to be referred to as “fading speed” hereinafter) should be high, (V) ...

COMPOUND AND ORGANIC LIGHT-EMISSION DEVICE

The present invention provides a novel compound of an amine derivative including a spiro compound. The novel compound has excellent hole transport characteristics. Thus, when the novel compound is applied to a hole transport layer, an auxiliary hole transport layer and an electron blocking layer of an organic light-emitting device, the device realizes low driving voltage, high efficiency, high thermal stability and long life-span. Further, when the novel compound is applied as a blue light-emitting material, the device realizes a low driving voltage and high efficiency. 4. An organic light-emission device comprising:an anode,a cathode, and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'at least one organic material layer therebetween, wherein the organic material layer comprises a compound of .'}5. The organic light-emission device of claim 4 , wherein the organic material layer includes at least one of a hole transport layer claim 4 , an auxiliary hole transport layer and an electron blocking layer claim 4 , wherein the at least one of the hole transport layer claim 4 , the auxiliary hole transport layer and the electron blocking layer comprises the compound represented by Chemical Formula 1.6. The organic light-emission device of claim 5 , wherein the hole transport layer comprises the compound represented by Chemical Formula 1.7. The organic light-emission device of claim 5 , wherein the auxiliary hole transport layer comprises the compound represented by Chemical Formula 1.8. The organic light-emission device of claim 5 , wherein the electron blocking layer comprises the compound represented by Chemical Formula 1.9. The organic light-emission device of claim 4 , wherein the organic material layer comprises a blue light-emission layer comprising the compound represented by Chemical Formula 1 as a blue light-emission material.10. The organic light-emission device of claim 4 , wherein the organic material layer includes at least one of an electron transport ...

COMMERCIALLY VIABLE SYNTHESIS OF CANTHARIDIN AND BIOACTIVE CANTHARIDIN DERIVATIVES

The present disclosure provides methods for synthesizing cantharidin and cantharidin derivatives. 1. A method for generating a cantharidin formulation comprising cantharidin or a cantharidin derivative , the method comprising reacting a precursor of said cantharidin or cantharidin derivative to form said cantharidin formulation having said cantharidin or cantharidin derivative at an exo-to-endo ratio of at least 6:1.28-. (canceled)9. The method of claim 1 , wherein said reacting is conducted at a pressure less than about 100 atm.1012-. (canceled)14. A method for generating a cantharidin formulation comprising cantharidin or a cantharidin derivative claim 1 , the method comprising reacting a precursor of said cantharidin or cantharidin derivative to form said cantharidin formulation having said cantharidin or cantharidin derivative claim 1 , wherein said reacting is conducted (i) in the absence of diethyl ether claim 1 , (ii) in the absence of a lithium or magnesium salt claim 1 , and (iii) at a pressure less than about 980 atmospheres (atm).1521-. (canceled)22. The method of claim 14 , wherein said reacting is conducted with the aid of a catalyst.2324-. (canceled)25. The method of claim 22 , wherein said catalyst comprises bis(cyclopentadienyl)zirconium(IV) bis(trifluoromethanesulfonate)tetrahydrofuran complex.26. The method of claim 22 , wherein said catalyst comprises aluminum chloride.2729-. (canceled)30. A cantharidin formulation comprising (i) cantharidin or a cantharidin derivative claim 22 , (ii) less than 0.1% diethyl ether and (iii) less than 0.1% lithium salt claim 22 , wherein said cantharidin or cantharidin derivative is at an exo-to-endo ratio of at least 6:1.3136-. (canceled)37. A cantharidin formulation comprising (i) cantharidin or a cantharidin derivative and (ii) a Lewis catalyst comprising one or more Lewis metals selected from the group consisting of Li (I) claim 22 , Mg (II) claim 22 , B (III) claim 22 , Al (III) claim 22 , Ti (IV) claim 22 , Zr ...

SANDWICH ASSAY DESIGN FOR SMALL MOLECULES

Methods are disclosed of designing antibodies for a sandwich assay for a small molecule having a molecular weight of about 500 to about 2,000. The method comprises preparing a first antibody that binds to the small molecule, and preparing a second antibody that binds to the small molecule at a portion of the small molecule other than a portion to which the first antibody binds. The second antibody is prepared from an immunogen that comprises a predetermined portion of the small molecule. The antibodies may be employed in sandwich assays for the small molecule. 1(a) preparing a first monoclonal antibody that binds specifically to a binding domain extending approximately from ring atom 15 to ring atom 21 and includes a triene moiety from ring atom 17 to ring atom 22 of sirolimus, wherein the first antibody is prepared from an immunogen that comprises sirolimus, wherein sirolimus is linked at carbon atom 26 or 32 through an oxime functionality to an immunogenic carrier for eliciting antibodies; and(b) preparing a second monoclonal antibody that binds specifically to sirolimus in a portion other than the domain to which the first antibody binds, wherein said second antibody binds a binding domain extending approximately from the methyl group on atom 11 to the methoxy group on atom 39 or from the methyl group on ring atom 25 to atom 41, wherein the second monoclonal antibody is prepared from an immunogen that comprises sirolimus that is modified in the triene area extending approximately from ring atom 15 to ring atom 21 and including a triene moiety from ring atom 17 to ring atom 22, to which the first monoclonal antibody binds, wherein sirolimus is combined with a cyclic reagent IV under conditions for carrying out a Diels-Aider-reaction to produce a modified sirolimus of formula IA and IIB and the modified sirolimus is linked to an immunogenic carrier at ring atom 26 or ring atom 32 for eliciting antibodies;wherein IIA, IIB, and reagent IV are compounds of the formula ...

MODIFIED BIOTIN, MUTANT STREPTAVIDIN, AND USE THEREOF

It is an object of the present invention to provide a mutant streptavidin with a reduced affinity for natural biotin, and also to provide a modified biotin having a high affinity for the mutant streptavidin with a reduced affinity for natural biotin. According to the present invention, there is provided a reagent kit for use in treatments or diagnoses, which comprises: (a) a mutant streptavidin with a reduced affinity for natural biotin or biocytin; and a modified biotin having a high affinity for the above-described mutant streptavidin. 4. A mutant streptavidin comprising the amino acid sequence shown in any one of SEQ ID NOS: 3 to 12.5. DNA encoding the mutant streptavidin according to .6. A mutant streptavidin-molecular probe conjugate which is obtained by conjugating a molecular probe to the mutant streptavidin according to .7. A therapeutic agent or an in-vivo or in-vitro diagnostic agent claim 6 , which comprises the mutant streptavidin-molecular probe conjugate according to .8. A therapeutic claim 1 , or in-vivo or in-vitro diagnostic kit claim 1 , which comprises: (a) a mutant streptavidin-molecular probe conjugate which is obtained by conjugating a molecular probe to a mutant streptavidin comprising the amino acid sequence shown in any one of SEQ ID NOS: 3 to 12; and (b) an in-vivo or in-vitro diagnostic or therapeutic substance that has been labeled with the compound according to .9. A reagent kit for use in treatments or in-vivo or in-vitro diagnoses claim 1 , which comprises:(a) a mutant streptavidin with a reduced affinity for natural biotin or biocytin; and(b) a modified biotin having a high affinity for the above-described mutant streptavidin.10. A therapeutic claim 1 , or in-vivo or in-vitro diagnostic kit claim 1 , which comprises:(a) a conjugate of a mutant streptavidin with a reduced affinity for natural biotin or biocytin and a molecular probe; and(b) an in-vivo or in-vitro diagnostic or therapeutic substance that has been labeled with a modified ...

Sugar Derivatives Comprising Sulfur-Containing Moieties And Methods Of Making Same And Methods Of Using The Same For The Treatment Of MPS IIIC

Described herein are modified sugar, iminosugar and azasugar compounds and methods of making same. One or more of these modified compounds contain sulfates, sulfites, sulfamates and/or sulfonamides. Also described are pharmaceutical compositions/formulations comprising these compounds, as well as methods using these modified sugar compounds for the treatment of MPS IIIC (also known as Sanfilippo Type C). 7. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. the compound of ; and'}b. at least one pharmaceutically acceptable carrier.8. A method of making a pharmaceutical composition according to , the method comprising , adding to at least one pharmaceutically acceptable carrier to the compound of .9. A method of making the compound according to claim 4 , the method comprising reacting N-benzyl(N-acetyl 1 claim 4 ,2 deoxynojiimycin) with SOCland pyridine.10. A method of making the compound having a structure represented by formula (V) according to claim 6 , the method comprisinga. reacting 1-deoxygalactonojirimycin with EtOCOCl to produce an intermediate; and{'sub': '2', 'b. reacting the intermediate with SOCl and pyridine.'}11. A method of making the compound having a structure represented by formula (VI) according to claim 6 , the method comprisinga. reacting 1-deoxygalactonojirimycin with EtOCOCl to produce an intermediate; and{'sub': 2', '2, 'b. reacting the intermediate with SOCland pyridine.'}12. A method of making the compound having a structure represented by formula (VII) according to claim 6 , the method comprisinga. reacting 1-deoxynojirimycin with EtOCOCl to produce an intermediate; and{'sub': 2', '2, 'b. reacting the intermediate with SOCland pyridine.'}17. A method of preventing and/or treating MPS IIIC claim 1 , the method comprising administering to a patient in need thereof a therapeutically effective amount of the compound of .18. The method of claim 17 , further comprising administering an effective amount ...

PYRANOCHROMENYL PHENOL DERIVATIVE, AND PHARMACEUTICAL COMPOSITION FOR TREATING METABOLIC SYNDROME OR INFLAMMATORY DISEASE

Provided are a pyranochromenyl phenol derivative, a pharmaceutically acceptable salt thereof, or a solvate thereof. Also provided is a pharmaceutical composition for preventing or treating metabolic syndrome or inflammatory disease comprising same. 2. The compound of Formula (1) claim 1 , the pharmaceutically acceptable salt thereof claim 1 , or the solvate thereof of claim 1 , wherein Ris a hydrogen atom claim 1 , and Ris a hydrogen atom; a straight or branched C-Calkyl group; a straight or branched C-Calkoxy group; or a straight or branched C-Cthioalkyl group.3. The compound of Formula (1) claim 2 , the pharmaceutically acceptable salt thereof claim 2 , or the solvate thereof of claim 2 , wherein Ris a hydrogen atom claim 2 , and Ris methyl claim 2 , ethyl claim 2 , n-propyl claim 2 , n-butyl claim 2 , ethoxy claim 2 , n-propoxy claim 2 , n-butoxy or methoxymethoxy.6. The pharmaceutical composition of claim 5 , wherein in Formula (I′) claim 5 , Ris a hydrogen atom claim 5 , and Ris a hydrogen atom; a hydroxy group; a straight or branched C-Calkyl group; a straight or branched C-Calkoxy group; or a straight or branched C-Cthioalkyl group.7. The pharmaceutical composition of claim 6 , wherein in Formula (I′) claim 6 , R1 is a hydrogen atom claim 6 , and Ris methyl claim 6 , ethyl claim 6 , n-propyl claim 6 , n-butyl claim 6 , ethoxy claim 6 , n-propoxy claim 6 , n-butoxy or methoxymethoxy.9. The pharmaceutical composition of claim 5 , wherein the metabolic syndrome is one or more of obesity claim 5 , diabetes claim 5 , hyperlipidemia claim 5 , and fatty liver.10. The pharmaceutical composition of claim 9 , wherein the diabetes is type 2 diabetes mellitus.11. The pharmaceutical composition of claim 5 , wherein the metabolic syndrome is a complex disease of type 2 diabetes mellitus and obesity.13. The pharmaceutical composition of claim 12 , wherein in Formula (I′) claim 12 , Ris a hydrogen atom claim 12 , and Ris a hydrogen atom; a hydroxy group; a straight or ...

INHIBITORS OF DNA GYRASE FOR THE TREATMENT OF BACTERIAL INFECTIONS

The present invention relates to compounds which specifically inhibit bacterial DNA Gyrase and can be used for the treatment of respiratory tract infections. 2. The compound of wherein the compound is selected from the group consisting of claim 1 , VT-03-00014: 4-(2-(3-([1 claim 1 ,3]oxathiolo[5 claim 1 ,4-c]pyridin-6-ylmethylamino)-8 azabicyclo[3.2.1]octan-8-yl)ethyl)-6-methoxyquinoline-3-carbonitrile; VT-03-00017: N-(8-(2-(3-cyano-6-methoxyquinolin-4-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)-2-methylbenzenesulfonamide; VT-03-00021: N-(8-(2-(3-cyano-6-methoxyquinolin-4-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)-2 claim 1 ,3-dihydrobenzo[b][1 claim 1 ,4]dioxine-6-sulfonamide; VT-03-00021a: 4-(2-(3-((2 claim 1 ,3-dihydrobenzo[b][1 claim 1 ,4]dioxin-6-yl)methylamino)-8azabicyclo[3.2.1]octan-8-yl)ethyl)-6-methoxyquinoline-3-carbonitrile; VT-03-00022: N-(8-(2-(3-cyano-6-methoxyquinolin-4-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)naphthalene-2-sulfonamide; VT-03-00024: N-(8-(2-(3-cyano-6-methoxyquinolin-4-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)-2 claim 1 ,3-dihydrobenzo[b][1 claim 1 ,4]dioxine-6-carboxamide; VT-03-00026: 6-methoxy-4-(2-(3-((3-oxo-3 claim 1 ,4-dihydro-2H-benzo[b][1 claim 1 ,4]thiazin-6-yl)methylamino)-8-azabicyclo[3.2.1]octan-8-yl)ethyl)quinoline-3-carbonitrile; VT-03-00026a: 4-(2-(3-((3 claim 1 ,4-dihydro-2H-benzo[b][1 claim 1 ,4]thiazin-6-yl)methylamino)-8-azabicyclo[3.2.1]octan-8-yl)ethyl)-6-methoxyquinoline-3-carbonitrile; VT-03-00027: 4-(2-(3-((2 claim 1 ,3-dihydro-[1 claim 1 ,4]dioxino[2 claim 1 ,3-c]pyridin-7-yl)methylamino)-8-azabicyclo[3.2.1]octan-8-yl)ethyl)-6-methoxyquinoline-3-carbonitrile; VT-03-00028: 4-(2-((1R claim 1 ,4R)-5-((2 claim 1 ,3-dihydrobenzo[b][1 claim 1 ,4]dioxin-6-ylamino)methyl)-2 claim 1 ,5-diazabicyclo[2.2.1]heptan-2-yl)ethyl)-6-methoxyquinoline-3-carbonitrile;VT-03-00030: 6-methoxy-4-(2-(3-((3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)methylamino)-8-azabicyclo[3.2.1]octan-8-yl)ethyl)quinoline-3-carbonitrile; VT-03-00031: 4-(2 ...

SANDWICH ASSAY DESIGN FOR SMALL MOLECULES

Methods are disclosed of designing antibodies for a sandwich assay for a small molecule having a molecular weight of about 500 to about 2,000. The method comprises preparing a first antibody that binds to the small molecule, and preparing a second antibody that binds to the small molecule at a portion of the small molecule other than a portion to which the first antibody binds. The second antibody is prepared from an immunogen that comprises a predetermined portion of the small molecule. The antibodies may be employed in sandwich assays for the small molecule. 1. A method of designing antibodies for a sandwich assay for a small molecule having a molecular weight of about 500 to about 2 ,000 , the method comprising:(a) preparing a first antibody that binds to the small molecule, and(b) preparing a second antibody that binds to the small molecule in a portion of the small molecule other than a portion to which the first antibody binds, wherein the second antibody is prepared from an immunogen that comprises a predetermined portion of the small molecule.2. The method according to wherein the first antibody is prepared from an immunogen that comprises a portion of the small molecule other than the predetermined portion.3. The method according to wherein the predetermined portion of the small molecule is obtained by modification of the small molecule to alter a spatial conformation of the small molecule.4. The method according to wherein the predetermined portion of the small molecule is a compound that consists essentially of the predetermined portion.5. The method according to wherein the small molecule is a macrolide.6. The method according to wherein the small molecule is an immunosuppressant drug.7. The method according to wherein one or both of the first antibody and the second antibody are monoclonal antibodies.8. A method of determining a presence and/or amount of a small molecule having a molecular weight of about 500 to about 2 claim 1 ,000 in a sample ...

ANTIBACTERIAL COMPOUNDS HAVING BROAD SPECTRUM OF ACTIVITY

The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials. 4: The compound according to claim 1 , wherein G3 is N claim 1 , CH or C(CH).5: The compound according to claim 1 , wherein Ris hydrogen atom claim 1 , halogen atom claim 1 , cyano claim 1 , (C)alkyl or NR′R″ claim 1 , wherein R′ and R″ are hydrogen atom or (C)alkyl.6: The compound according to claim 1 , wherein Ris hydrogen atom claim 1 , F claim 1 , Cl claim 1 , cyano claim 1 , CH claim 1 , NHor N(CH).7: The compound according to claim 1 , wherein said Ris hydrogen atom claim 1 , fluorine atom claim 1 , chloride atom claim 1 , OH claim 1 , (C)alkyl-OH claim 1 , —COOR′ or —CON(R′)(R″) claim 1 , wherein R′ and R″ claim 1 , identical or different each other claim 1 , are hydrogen atom or (C)alkyl.8: The compound according to claim 1 , wherein said Ris hydrogen atom claim 1 , halogen atom claim 1 , cyano claim 1 , (C)alkyl claim 1 , (C)alkoxy claim 1 , or NR′R″ claim 1 , wherein R′ and R″ claim 1 , identical or different each other claim 1 , are hydrogen atom or (C)alkyl.9: The compound according to claim 1 , wherein said Y is (C)alkylenyl group claim 1 , —NH—(C)alkylenyl group or (C)cycloalkylenyl group claim 1 , said group being optionally substituted with one hydroxy group or an amino group.10: The compound according to claim 1 , wherein said Pis O claim 1 , S claim 1 , SOor CH.11: The compound according to claim 1 , wherein said Rand Rtogether form a 5- or 6-membered aromatic or aliphatic ring claim 1 , optionally comprising at least one heteroatom selected from N claim 1 , O and S claim 1 , wherein said ring optionally bears an oxo group.12: The compound according to claim 11 , wherein Rand Rtogether form a 6-membered ring selected from benzene or pyridine.13: A pharmaceutical composition claim 1 , comprising at least one compound of formula (I) according to claim 1 , a salt thereof with a pharmaceutically acceptable organic ...

Method of preparing tetrathiafulvalene precursor

FIELD: chemical industry. SUBSTANCE: tetrathiafulvalene (6) derivatives are used as organic conductors, organic superconductors, organic magnetic or like materials. Claimed method of preparing tetrathiafulvalene of formula I: wherein R 1 and R 2 are alkyl, aralkyl, alkene, alkoryl, hydroxyalkyl, trimethylsilyl and trimethylsilylethoxymethyl and when R 1 and R 2 are bonded to form ring, they are alkylene, dimethylenethio, dimethylenoether. Compound 1 is prepared by single reactor and single stage method without generation of difficultly removable by-products and hence with high yield and high purity for short period of time: one of two rings 1,3,4,6-tetrathiapentene -2,5-dione is selectively detached in alcoholic solution containing alkali metal methoxide in inert atmosphere at 30 C or lower. The resulting 1,3-diol-2-one-4,5-dithiolate dianion is reacted with compound having monovalent or divalent group which corresponds to R 1 and R 2 in formula I. Derivatives of formula (I) are prepared using above-indicated stage for preparing precursor and stage of reaction combination of two precursor molecules to obtain tetrathiafulvalene derivative with high yield and for short period of time. EFFECT: more efficient preparation method. 11 cl, 1 dwg, 8 ex ГооОосстс ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ” 2 122 001‘ 13) Сл С 070 339/06, 495/06 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 93054536/04, 29.09.1993 (30) Приоритет: 30.09.1992 ШР 4-262348 (46) Дата публикации: 20.11.1998 (56) Ссылки: ЕР 0281449, 1988. ЕР 0454814, 1990. 1$ 4691028, 1987. (71) Заявитель: Сумитомо Электрик Индастриз, Лтд. (Р) (72) Изобретатель: Харальд Дитмар Мюллер (4Р), Йосинобу Уэба (.Р) (73) Патентообладатель: Сумитомо Электрик Индастриз, Лтд. (ШР) (54) СПОСОБ ПОЛУЧЕНИЯ ПРЕДШЕСТВЕННИКА ТЕТРАТИАФУЛЬВАЛЕНА И СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНОГО ТЕТРАТИАФУЛЬВАЛЕНА (57) Реферат: Производные тетратиафульвалена (6) могут использоваться как ...

Polycyclic compounds and organic electroluminescence device employing the same

Provided are a polycyclic compound of a compound having such a structure that two benzene rings bond to a central benzene ring each other to form a fused ring and another fused ring bonds to a terminal thereof, and an organic electroluminescence device including one or more organic thin film layers containing a light emitting layer between a cathode and an anode, in which at least one of the organic thin film layers includes the polycyclic compound of the present invention. The organic electroluminescence device has high luminous efficiency, no defect in pixels, and long lifetime. In addition, provided is a polycyclic compound realizing the organic electroluminescence device.

Polycyclic compounds and organic electroluminescence device employing the same

Provided are a polycyclic compound of a compound having such a structure that two benzene rings bond to a central benzene ring each other to form a fused ring and another fused ring bonds to a terminal thereof, and an organic electroluminescence device including one or more organic thin film layers containing a light emitting layer between a cathode and an anode, in which at least one of the organic thin film layers includes the polycyclic compound of the present invention. The organic electroluminescence device has high luminous efficiency, no defect in pixels, and long lifetime. In addition, provided is a polycyclic compound realizing the organic electroluminescence device.

Polycyclic compound and organic electroluminescent device using the same

중심 벤젠환에 2개의 벤젠환이 축합환을 형성하도록 결합되고, 더욱이 그 말단에 다른 축합환이 결합된 구조를 갖는 화합물의 다환계 화합물, 및, 음극과 양극사이에, 발광층을 포함하는 1층 이상의 유기 박막층을 갖고, 상기 유기 박막층의 적어도 1층이, 본 발명의 다환계 화합물을 함유하는 유기 전기발광 소자는, 발광 효율이 높고, 화소 결함이 없고, 장수명인 유기 전기발광 소자 및 그것을 실현하는 다환계 화합물이다.

Fused quinazoline derivatives useful as tyrosine kinase inhibitors

The present invention is directed to a compound having the structure wherein A is a 7–18 membered ring that comprises 0 to 6 heteroatoms selected from O, S, and N; R 1 is selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C 1-8 alkyl, substituted or unsubstituted C 2-8 alkenyl, substituted or unsubstituted C 2-8 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, and substituted or unsubstituted heterocyclyl; m is an integer from 0 to 3; X is selected from the group consisting of NR 2 , CHR 3 , O, or S; wherein R 2 and R 3 are each individually H or C 1-8 alkyl; R is selected from the group consisting of unsubstituted aryl, and substituted or unsubstituted heteroaryl, substituted or unsubstituted aryl-(C 1-3 )alkyl, substituted or unsubstituted aryl-(C 3-7 )cycloalkyl, substituted or unsubstituted heteroaryl-(C 1-3 )alkyl, and substituted or unsubstituted heteroaryl-(C 3-7 )cycloalkyl; and pharmaceutically acceptable salts thereof; with the proviso that if A is a 7 or 8 membered ring, then R 1 is selected from the group consisting of other than H, C 1 –C 4 alkyl, (C 1 –C 4 alkoxy)C 1 –C 4 alkyl, C 1 –C 4 alkanoyl, C 1 –C 4 alkoxy or —S(O) x (C 1 –C 4 alkyl) wherein x is 0 to 2, and wherein said alkyl group and the alkyl moieties of said R 1 groups are optionally substituted by 1 to 3 halogens. The present invention is also directed to pharmaceutical compositions comprising the above compound, and methods of treating patients suffering from tyrosine kinase-mediated disorders using the above compound.

Hetero cyclic compound and organic light emitting device comprising the same

본 명세서는 화학식 1의 헤테로고리 화합물 및 이를 포함하는 유기 발광 소자에 관한 것이다. The present specification relates to a heterocyclic compound of Formula 1 and an organic light emitting device including the same.

Small molecules and their use as organic semiconductors

The invention relates to novel compounds based on thieno[3,2-b]thiophene- 2,5-dione and/or furo[3,2-b]furan-2,5-dione or their thioketone derivatives, methods for their preparation and intermediates used therein, mixtures and formulations containing them, the use of the compounds, mixtures and formulations as semiconductor in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices and organic photodetectors (OPD), and to OE, OPV and OPD devices comprising these compounds, mixtures or formulations.

Small molecules and their use as organic semiconductors

本発明は、チエノ［３，２−ｂ］チオフェン−２，５−ジオンおよび／もしくはフロ［３，２−ｂ］フラン−２，５−ジオンに基づく新規な化合物またはそれらのチオケトン誘導体、それらの製造方法およびそれにおいて使用する中間体、それらを含む混合物および配合物、該化合物、混合物および配合物の有機電子（ＯＥ）デバイスにおける、特に有機光起電力（ＯＰＶ）デバイスおよび有機光検出器（ＯＰＤ）における半導体としての使用、ならびにこれらの化合物、混合物または配合物を含むＯＥ、ＯＰＶおよびＯＰＤデバイスに関する。

CARBOXYMETHOXY-7 FURO- (3,4-C) -PYRIDINE MEDICINAL PRODUCTS

New acyl-CoA: Cholesterol acyltransferase (ACAT) activity inhibitor and preparation method thereof

본 발명은 토양으로부터 분리된 곰팡이 아스퍼질러스 푸미가투스(Aspergillus fumigatus) FM-F-37로부터 분리된, 아실-CoA : 콜레스테롤 아실전이효소의 저해제인 하기 구조식(I)의 GERI-BP001, 그의 유도체 및 그의 제조방법에 관한 것이다.

Tetrathiafulvalene derivative precursors, tetrathiafulvalene derivatives, and processes for producing them

A tetrathiafulvalene derivative precursor represented by formula (1), a tetrathiafulvalene derivative represented by formula (6), and processes for producing the tetrathiafulvalene derivative precursor and the tetrathiafulvalene derivative: ##STR1## wherein R 1 and R 2 may be the same or different and represent organic groups that may be linked together to form a ring.

Pseudofructopyranose sulfamates and pharmaceutical composition based on said

FIELD: organic chemistry, sugars, pharmacy. SUBSTANCE: invention relates to pseudofructopyranose sulfamates of the formula (I) where R 1 , R 2 , R 3 , R 4 is H, C 1-6 -alkyl; X is carbon or sulfur under condition that when X - carbon then R 5 and R 6 are H, C 1-6 -alkyl; if X - sulfur then one of R 5 and R 6 is hydrogen and other means electron pair, or both - oxygen, or its pharmaceutically acceptable salt, hydrate, anomer, diastereomer or enantiomer showing an anticonvulsant activity. EFFECT: compounds indicated above, an anticonvulsant activity. 10 cl, 4 ex зе гс пы Го (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ "” 2439 875‘ (51) МПК 13) СЛ 31/335, 31/38 С 070 493/04, 497/04, А 61 К 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 96115166/04, 15.12.1994 (24) Дата начала действия патента: 15.12.1994 (30) Приоритет: 23.12.1993 1$ 173399 10.11.1994 Ц$ 337597 (46) Дата публикации: 20.10.1999 (56) Ссылки: ЗИ 2187686 1968. Ц$ 4792569 А, 1988. ЕР 138441 АЗ, 1986. 4$ 4075351 А, 1978. (85) Дата перевода заявки РСТ на национальную фазу: 23.07.96 (86) Заявка РСТ: 0$ 94/14591 (15.12.94) (87) Публикация РСТ: М/О 95/17406 (29.06.95) (98) Адрес для переписки: 103735, Москва, ул.Ильинка 5/2, Союзпатент (71) Заявитель: Орто Фармасьютикал Корпорейшн (ЦЗ) (72) Изобретатель: Майкл Дж. Костензо (1$), Брюс Е Марьянов (Ц$), Дэвид Ф.Маккомси (0$), Сэмюель Д.Норти (ЦЗ) (73) Патентообладатель: Орто Фармасьютикал Корпорейшн (ЦЗ) (54) СУЛЬФАМАТЫ ПСЕВДОФРУКТОПИРАНОЗЫ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ (57) Реферат: Сульфаматы псевдофруктопиранозы формулы |, где К1-К4-Н, С1-6в-алкил; Х - углерод или сера при условии, что когда Х - углерод, Кв и ЕР - Н, С1-в-алкил, тогда как, если Х - сера, один из В5 и Вё- кислород, а другой представляет пару электронов или оба являются кислородом, или их фармацевтически приемлемая соль, гидрат, аномер, диастереомер или энантиомер, обладают противосудорожной активностью. 2 с. и8 з.п. Ф-лы. СН 050 МЕ Е 2 2 12 1 ...

Indolyl-aliphatic amines and their preparation

Biotin alterant, streptavidin mutant, and uses thereof

It is an object of the present invention to provide a mutant streptavidin with a reduced affinity for natural biotin, and also to provide a modified biotin having a high affinity for the mutant streptavidin with a reduced affinity for natural biotin. According to the present invention, there is provided a reagent kit for use in treatments or diagnoses, which comprises: (a) a mutant streptavidin with a reduced affinity for natural biotin or biocytin; and a modified biotin having a high affinity for the above-described mutant streptavidin.

Tetrathiafulvalene derivative precursors, tetrathiafulvalene derivatives, and processes for producing them

(Object) To provide a process for producing a high-purity tetrathiafulvalene derivative in a high yield, and novel tetrathiafulvalene derivatives and their precursors. (Constitution) The process for production comprises selectively cleaving one of the two rings of 1,3,4,6-tetrathiapentalene-2,5-dione to produce 1,3-dithiol-2-one-4,5-dithiolate dianion, and after reacting it with a compound having a monovalent or divalent organic group, effecting coupling of two molecules thereof. Novel tetrathiafulvalene derivatives and their precursors are represented by formulae (1) to (6) described in the specification.

CARBOXYMETHOXY-7 FURO- (3,4-C) -PYRIDINE MEDICINES

L'INVENTION CONCERNE DES MEDICAMENTS, COMPORTANT COMME PRINCIPE ACTIF, UNE QUANTITE SUFFISANTE D'AU MOINS UN DERIVE DE LA DIHYDRO-1,3 METHYLE-6 FURO-(3,4-C)-PYRIDINE REPONDANT A LA FORMULE GENERALE I: (CF DESSIN DANS BOPI) DANS LAQUELLE CHACUN DES SUBSTITUANTS A ET A REPRESENTE DIVERS SUBSTITUANTS HYDROCARBONES, OU D'UN DE SES SELS, ASSOCIEE A TOUT EXCIPIENT APPROPRIE. THE INVENTION CONCERNS MEDICINES, CONTAINING AS ACTIVE PRINCIPLE, A SUFFICIENT QUANTITY OF AT LEAST ONE DERIVATIVE OF DIHYDRO-1,3 METHYL-6 FURO- (3,4-C) -PYRIDINE RESPONDING TO GENERAL FORMULA I: ( CF DRAWING IN BOPI) IN WHICH EACH SUBSTITUTE HAS AND REPRESENTS VARIOUS HYDROCARBON SUBSTITUENTS, OR ONE OF ITS SALTS, ASSOCIATED WITH ANY APPROPRIATE EXCIPIENT.

ANTICONVULSIVE PSEUDOFRUCTOPYRANOSE SULFAMATE

3,4α-Di-O-derivatives of mercaptomethylpyridine and pyridylmethyldisulfide

Mercaptoalkylpyridines and various derivatives thereof have utility in the treatment of rheumatoid arthritis. The compounds useful in the method of treatment are generally prepared from known pyridine derivatives and, principally, from pyridoxine and related compounds.

Substituted pyridines having herbicidal activity

The present invention provides substituted pyridine compounds of the formula (I) or N-oxides or agriculturally suitable salts thereof, wherein the variables in the formula (I) are defined as in the description. Substituted pyridines of formula (I) are useful as herbicides.

Process for the preparation of tetrathiafulvalene derivatives and their precursors

Etoposide analogs and methods of use thereof

Etoposide analogs such as 4'-O-demethyl-4β-[4''-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4'-O-demethyl-4β-[4''-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Substituted hexahydroarylquinolidine

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

substituted pyridine compound of formula i, composition and method for controlling unwanted vegetation

Organic compound containing benzoanthracene, preparation method and application thereof

本发明涉及一种含苯并蒽的有机化合物及其制备方法和应用，属于半导体技术领域，本发明提供化合物的结构如通式(1)所示： 本发明还公开了上述化合物的制备方法及其应用。本发明提供的化合物具有较强的空穴传输能力，在恰当的HOMO能级下，提升了空穴注入和传输性能；在合适的LUMO能级下，又起到了电子阻挡的作用，提升激子在发光层中的复合效率；作为OLED发光器件的发光功能层材料使用时，搭配本发明范围内的支链可有效提高激子利用率和辐射效率。

Etoposide analogs and methods of use thereof

Condensed quinazoline derirative used as tyrosine kinase inhibitor

一种具有以下结构的化合物：其中A是7到18元环，R 1 是：氢，卤素，取代或未取代C 1-8 烷基、C 2-8 烯基、C 2-8 炔基、芳基、杂芳基及杂环基，C 1-8 烷酰基，C 1-8 烷氧碳酰基，C 1-8 烷基亚磺酰基，C 1-8 烷基磺酰基，芳磺酰基，氰基，硝基，羟基，氨基，羧基，氧代，氨甲酰基，C 1-8 烷氧基，C 2-8 烯氧基，C 2-8 炔氧基，C 1-8 烷硫基，N-(C 1-8 烷基)氨甲酰基，N，N-二-(C 1-8 烷基)，氨甲酰基，C 1-8 烷酰氧基，C 1-8 烷酰胺基，C 3-8 炔酰胺基，N-(C 1-8 烷基)氨磺酰基，N，N-二-((C 1-8 烷基)氨磺酰基；m是0到3的整数；X是NR 2 ，CHR 3 ，O或S；该R 2 和R 3 可分别为H或C 1-8 烷基；R是取代或未取代的芳基、杂芳基、芳基-C 1-3 烷基及芳基-C 3-7 环烷基；及其药学上可接受的盐；如果A是7元或8元环，那么R 1 不可以是H，C 1-4 烷基，C 1-4 烷氧基-C 1-4 烷基，C 1-4 烷酰基，C 1-4 烷氧基或-S(O) x (C 1-4 烷基)，其中X是0-2，所述烷基和所述R 1 中烷基部分可被1-3个卤原子取代。一种含上述化合物和一药学上可接受的载体的药学成分；及用于治疗酪氮酸激酶调节性疾病的一种方法。

Polycyclic compound and organic electroluminescent device using the same

Provided are a polycyclic compound of a compound having such a structure that two benzene rings bond to a central benzene ring each other to form a fused ring and another fused ring bonds to a terminal thereof, and an organic electroluminescence device including one or more organic thin film layers containing a light emitting layer between a cathode and an anode, in which at least one of the organic thin film layers includes the polycyclic compound of the present invention. The organic electroluminescence device has high luminous efficiency, no defect in pixels, and long lifetime. In addition, provided is a polycyclic compound realizing the organic electroluminescence device.

Tetrathiafulvalene derivative precursors, tetrathiafulvalene derivatives, and processes for producing them

(Object) To provide a process for producing a high-purity tetrathiafulvalene derivative in a high yield, and novel tetrathiafulvalene derivatives and their precursors. (Constitution) The process for production comprises selectively cleaving one of the two rings of 1,3,4,6-tetrathiapentalene-2,5-dione to produce 1,3-dithiol-2-one-4,5-dithiolate dianion, and after reacting it with a compound having a monovalent or divalent organic group, effecting coupling of two molecules thereof. Novel tetrathiafulvalene derivatives and their precursors are represented by formulae (1) to (6) described in the specification.

Fibrinogen receptor antagonists

Fibrinogen receptor antagonists having formula (I) for example formula (a).

Organic compound, light-emitting element, light-emitting device, electronic device, and lighting device

本發明提供一種新穎的化合物。另外，提供一種發光效率高且元件壽命長的發光元件。本發明提供一種由通式（G0）表示的具有苯并呋喃并[3,2-d]嘧啶骨架或苯并噻吩并[3,2-d]嘧啶骨架的有機化合物。苯并呋喃并[3,2-d]嘧啶骨架或苯并噻吩并[3,2-d]嘧啶骨架的2位具有取代基，在6至9位具有至少一個取代基。鍵合到6至9位的取代基中的任一個藉由伸苯基與苯并呋喃并[3,2-d]嘧啶骨架或苯并噻吩并[3,2-d]嘧啶骨架鍵合。另外，本發明提供一種包含該化合物的發光元件。

Sulfamate derivatives and pharmaceutical compositions containing them

1-(n, n-dibenzylamino)-2-[n'-(halo-loweralkanoyl)-n'-(substituted)]-loweralkylenediamines

NOVEL CARBOXYMETHOXY-7 FURO- (3,4-C) -PYRIDINE DERIVATIVES AND PROCESS FOR PREPARING THEM

L'INVENTION CONCERNE DE NOUVEAUX DERIVES DE LA DIHYDRO-1,3 METHYLE-6 FURO-(3,4-C)-PYRIDINE REPONDANT A LA FORMULE GENERALEI: (CF DESSIN DANS BOPI) DANS LAQUELLE CHACUN DES SUBSTITUANTS A ET A REPRESENTE DIVERS SUBSTITUANTS HYDROCARBONES AINSI QU'UN PROCEDE DE PREPARATION DE CES DERIVES CONSISTANT A TRAITER UN COMPOSE REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) PAR LE BROMOACETATE D'ETHYLE A UNE TEMPERATURE COMPRISE ENTRE 10 ET 70C, EN PRESENCE DE DIMETHYLFORMAMIDE, PUIS A HYDROLYSER L'ESTER RESULTANT PAR L'HYDROXYDE DE SODIUM. THE INVENTION CONCERNS NEW DERIVATIVES OF DIHYDRO-1,3 METHYL-6 FURO- (3,4-C) -PYRIDINE RESPONDING TO THE GENERAL FORMULA: (CF DRAWING IN BOPI) IN WHICH EACH OF THE SUBSTITUENTS A AND A REPRESENTS VARIOUS HYDROCARBON SUBSTITUENTS AS WELL AS A PROCESS FOR THE PREPARATION OF THESE DERIVATIVES CONSISTING OF TREATING A COMPOUND RESPONDING TO THE FORMULA: (CF DRAWING IN BOPI) WITH ETHYL BROMOACETATE AT A TEMPERATURE BETWEEN 10 AND 70C, IN THE PRESENCE OF AAMIDE PUETHYIS HYDROLYZE THE RESULTING ESTER WITH SODIUM HYDROXIDE.

Biotin variants, streptavidin variants and their use

本発明の課題は、天然ビオチンに対する親和性を低減させたストレプトアビジン変異体を提供し、更にこの天然ビオチンに対する低親和性のストレプトアビジン変異体に対して高い親和性を有するビオチン改変体を提供することである。本発明によれば、（ａ）天然ビオチン又はビオシチンとの親和性を低下させたストレプトアビジン変異体、及び（ｂ）上記ストレプトアビジン変異体に対して高い親和性を有するビオチン改変体を含む、治療又は診断のための試薬キットが提供される。 An object of the present invention is to provide a streptavidin variant having a reduced affinity for natural biotin, and further to provide a biotin variant having a high affinity for the low affinity streptavidin variant for natural biotin. That is. According to the present invention, a treatment comprising (a) a streptavidin variant having reduced affinity with natural biotin or biocytin, and (b) a biotin variant having a high affinity for the streptavidin variant. Alternatively, a reagent kit for diagnosis is provided.

Diuretic, antihypertensive and antihistaminic 7-carboxymethoxy-furo-(3,4-c)-pyridine derivatives

This invention relates to new 1,3-dihydro-6-methyl-furo-(3,4-c)-pyridine derivatives of the general formula: ##STR1## wherein, each of A 1 and A 2 represents various hydrocarbon groups, to pharmaceutically acceptable salts of them, to a process for the preparation of said derivatives from the corresponding 6-hydroxy compounds, treated by ethyl bromoacetate and then hydrolyzed. The invention further provides pharmaceutical compositions wherein said derivatives are used as active ingredients. The compounds are useful as diuretics, in lowering blood pressure and as antihistaminics.

New tetrahydrofuran bisphosphines useful for preparing transition metal complexes useful as catalysts for preparing stereoisomer-enriched compounds, e.g. pharmaceuticals and agrochemicals

Tetrahydrofuran bisphosphines of formula (I), are new. Tetrahydrofuran bisphosphines of formula (I): X1, X2 = bonds or O; R1, R2 = H, 1-20C alkyl, 1-20C fluoroalkyl, 2-20C alkenyl, 4-24C aryl, 5-25C aralkyl, 6-26C aralkenyl, NR7R8, OR8, AOR8, ANR7R8 or OCOR8 or R9SiR10R11R12; R7, R8 = 1-8C alkyl, 5-14C aralkyl or 4-15C aryl, or NR7R8 is a 4-20C cyclic amino group; A = 1-8C alkylene; R9 = a bond, O or CH2; R10-R12 = 1-12C alkyl, 5-15C aralkyl or 4-14C aryl; R3-R6 = R13, OR14 or NR15R16, or R3+R4 or R5+R6 is OR17O; R13-R16 = 1-12C alkyl, 5-15C aralkyl or 4-14C aryl, or NR15R16 is a 4-20C cyclic amino group; and R17 = 2-4C alkylene, o- or m-phenylene, 1,2-cyclohexylene, 1,1'- or 1,2-ferrocenylene, 2,2'-(1,1'-binaphthylene), 2,2'-biphenylylene or 2,2'-methylenediphenylene, all optionally substituted with F, Cl, 1-8C alkoxy and 1-8C alkyl. Independent claims are also included for: (1) compounds of formula (XIII); (2) a process for preparing compounds of formula (XV); (3) compounds of formula (XVIII), (XIX), (XXa), (XXIa) and (XXIb); (4) transition metal complexes of (I); (5) production of stereoisomer-enriched compounds by catalytic olefin, enamine, enamide, imine or ketone hydrogenation, 1,4-addition, hydroformylation, hydrocyanation or Heck reaction using the complexes as catalysts. Met2 = Li, Na or K; and R19 = 1-12C alkyl, 1-12C fluoroalkyl, 5-25C aralkyl or 4-24C aryl.

Method for producing mixtures containing 2-(2-hydroxyethyl)-piperidinyl carbamide acid secondary butyl ester

Die Erfindung umfasst ein verbessertes Verfahren zur Herstellung von Mischungen enthaltend 2-(2-Hydroxyethyl)-piperidinyl-carbamidsäure-sek.-butylester aus einem Rohprodukt durch thermische Behandlung mit kurzen Verweilzeiten, Vorrichtungen für dieses Verfahren, Verwendung solcher Vorrichtungen für solche Verfahren, sowie die aus dem Verfahren erhältlichen erfindungsgemäßen Mischungen.

Methods

A method for the preparation of a compound of formula (1) or a pharmaceutically acceptable salt or solvate thereof; from a compound of the formula: (IV); wherein L represents a leaving group.

FIBRINOGEN RECEPTOR ANTAGONISTS

Fibrinogen receptor antagonists having the formula

Annellated quinoline derivatives

Die vorliegende Anmeldung einer Erfindung betrifft die Verwendung von Chinolinderivaten der Formel DOLLAR F1 - in welcher die gestrichelte Bindung für eine Einfach- oder Doppelbindung steht und die Substituenten die in der Beschreibung angegebene Bedeutung haben - DOLLAR A als Pflanzenbehandlungsmittel, insbesondere zur Bekämpfung von tierischen Schädlingen; Pflanzenbehandlungsmittel auf Basis von bekannten und neuen annellierten Chinolinderivaten und neue Chinolinderivate. The present application of an invention relates to the use of quinoline derivatives of the formula DOLLAR F1 - in which the dashed bond represents a single or double bond and the substituents have the meaning given in the description - DOLLAR A as a plant treatment agent, in particular for controlling animal pests; Plant treatment products based on known and new fused quinoline derivatives and new quinoline derivatives.

Anthelmintic compounds comprising a thienopyridine structure

The present invention relates to new anthelmintic compounds. These compounds can for example be used in the treatment of the kind of worm disease caused by helminths such as Dirofilaria , in particular Dirofilaria immitis.

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Anthelmintic compounds comprising a thienopyridine structure

The present invention relates to new anthelmintic compounds. These compounds can for example be used in the treatment of the kind of worm disease caused by helminths such as Dirofilaria, in particular Dirofilaria immitis.

化合物及包含其的有机发光器件

本说明书提供化学式1的化合物及包含其的有机发光器件。

2-Methyl-3-hydroxy-4-alkanoylthiomethyl-5-vinylpyridines

Mercaptoalkylpyridines carrying an ethenyl or ethynyl substituent are prepared from known pyridine compounds, principally pyridoxine, by known chemical procedures, and are useful in the treatment of rheumatoid arthritis and related inflammatory diseases.

芳香族二卤化合物的制造方法

本发明提供一种不使用管制药品的亚硝酸叔丁酯的、由芳香族二胺化合物制造高纯度芳香族二卤化合物的工业制造方法。一种使芳香族二胺化合物、亚硝酸酯化合物以及卤化剂进行反应的芳香族二卤化合物的制造方法，所述亚硝酸酯化合物为从亚硝酸乙酯、亚硝酸己酯以及亚硝酸戊酯构成的群中选择的1种以上，所述方法包含所述反应的反应温度为35℃以上的反应工序1。

Chirale diphosphorverbindungen und deren übergangsmetallkomplexe

Verfahren zur herstellung von thiazolopyrimidinen

Process for the preparation of thiazolopyrimidines

チアゾロピリミジンの製造方法

式Ｉ： 【化１】 の化合物もしくはその薬学的に許容される塩またはそれらの溶媒和物の、式IV： 【化２】 [式中、Ｌは脱離基を表す]の化合物からの製造方法。

티아졸로피리미딘의 제조 방법

<화학식 I> <화학식 IV> 본 발명은 L이 이탈기를 나타내는 상기 화학식 IV의 화합물로부터, 상기 화학식 I의 화합물 또는 그의 제약학적으로 허용되는 염 또는 용매화물의 제조방법에 관한 것이다. 티아졸로피리미딘, 용매화물

Process for the preparation of thiazolopyrimidines

A method for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof; from a compound of the formula: (IV); wherein L represents a leaving group.

Process for the preparation of thiazolopyrimidines

Disclosed is a thiazolopyrimidine compound of the formula (V) or a pharmaceutically acceptable salt or solvate thereof and wherein R1 has the meaning as stated in the specification.

Process for the preparation of thiazolopyrimidines

Process for the preparation of thiazolopyrimidines

Disclosed is a method for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof; from a compound of the formula: (IV); wherein L represents a leaving group and the other variables are as defined in the specification.

Process for the preparation of thiazolopyrimidines

Process for the preparation of thiazolopyrimidines

Procedimiento para la preparacion de tiazolopirimidinas.

Un método para la preparación de un compuesto de la fórmula (I) o una de sus sales o solvatos farmacéuticamente aceptables: **(Ver fórmula)** en el que R1 representa un grupo carbocíclico C3-C7, alquilo C1-C8, alquenilo C2-C6 o alquinilo C2-C6, estando sustituido cada uno de los grupos opcionalmente con uno o varios grupos sustituyentes seleccionados, de modo independiente, de átomos de halógeno, -OR4, -NRR6, -CONR5R6, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9 o un grupo arilo o heteroarilo, los cuales pueden estar ambos opcionalmente sustituidos con uno o varios sustituyentes seleccionados, de modo independiente, de átomos de halógeno, grupos ciano, nitro, -OR4, -NR5R6 -CONR5R6, -COOR7, -NR8COR9, -SR10 -SO2R10, -SO2NR5R6, -NR8SO2R9, alquilo C1-C6 o trifluorometilo; R2 y R3 representan cada uno, de modo independiente, un átomo de hidrógeno, o un grupo carbocíclico C3-C7, alquilo C1-C8, alquenilo C2-C6 o alquinilo C2-C6, pudiendo estar los últimos cuatro grupos opcionalmente sustituidos con uno o varios grupos sustituyentes seleccionados, de modo independiente, de (a) átomos de halógeno, -OR4, -NR5R6, -CONR5R6, -COOR7, -NR8COR9, -SR10, -SO2R10, -SO2NR5R6, -NR8SO2R9; (b) un anillo de 3-8 miembros que opcionalmente contiene uno o varios átomos seleccionados de O, S, NR8 y opcionalmente sustituido en sí con alquilo C1-C3 o halógeno; o (c) un grupo arilo o un grupo heteroarilo cada uno de los cuales puede estar opcionalmente sustituido con uno o varios sustituyentes seleccionados, de modo independiente, de átomos de halógeno, grupos ciano, nitro, -OR4, -NR5R6, -CONR5R6, -NR8COR9, -SO2NR5R6, -NR8SO2R9, alquilo C1-C6 y trifluorometilo; R4 representa hidrógeno, alquilo C1-C6 o un grupo fenilo, cuyos dos últimos pueden estar opcionalmente sustituidos con uno o varios grupos sustituyentes seleccionados, de modo independiente, de átomos de halógeno, fenilo, -OR11 y -NR12R13. R5 y R6 representan, de modo independiente, un átomo de hidrógeno o un grupo alquilo C1-C6 ...

Process for the preparation of thiazolopyrimidines

티아졸로피리미딘의 제조 방법

<화학식 I> <화학식 IV> 본 발명은 L이 이탈기를 나타내는 상기 화학식 IV의 화합물로부터, 상기 화학식 I의 화합물 또는 그의 제약학적으로 허용되는 염 또는 용매화물의 제조방법에 관한 것이다. 티아졸로피리미딘, 용매화물

Sandwich assay design for small molecules

Methods are disclosed of designing antibodies for a sandwich assay for a small molecule having a molecular weight of about 500 to about 2,000. The method comprises preparing a first antibody that binds to the small molecule, and preparing a second antibody that binds to the small molecule at a portion of the small molecule other than a portion to which the first antibody binds. The second antibody is prepared from an immunogen that comprises a predetermined portion of the small molecule. The antibodies may be employed in sandwich assays for the small molecule.

유기 화합물, 발광 소자, 발광 장치, 전자 기기, 및 조명 장치

신규 화합물을 제공한다. 발광 효율이 높고 수명이 긴 발광 소자를 제공한다. 상기 화합물은 벤조퓨로[3,2-d]피리미딘 또는 벤조티에노[3,2-d]피리미딘 골격을 포함하는 유기 화합물(일반식(G0))이다. 벤조퓨로[3,2-d]피리미딘 또는 벤조티에노[3,2-d]피리미딘 골격의 2위치는 치환기를 가지고, 상기 골격의 6위치 내지 9위치에 적어도 하나의 치환기를 가진다. 6위치 내지 9위치와 결합된 상기 치환기 중 어느 하나는 페닐렌기를 통하여 벤조퓨로[3,2-d]피리미딘 또는 벤조티에노[3,2-d]피리미딘 골격과 결합된다. 상기 화합물을 포함하는 발광 소자를 제공한다.

Derivati della 7-carbossimetossi-furo-(3,4-c)-piri dina, loro preparazione e composizioni farmaceutiche che licontengono.

2-(2-히드록시에틸)-피페리디닐 카르바미드 산 2급 부틸 에스테르를 함유하는 혼합물을 제조하는 방법

본 발명은 짧은 체류 시간으로 열 처리하여 조 생성물로부터 2-(2-히드록시에틸)-피페리디닐 카르바미드 산 2급 부틸 에스테르를 포함하는 혼합물을 제조하기 위한 개선된 방법, 상기 방법을 위한 장치, 이러한 장치의 이러한 방법을 위한 용도, 및 이 방법을 사용하여 얻을 수 있는 본 발명에 따른 혼합물에 관한 것이다.

Method for producing mixtures containing 2-(2-hydroxyethyl)-piperidinyl carbamide acid secondary butyl ester

The invention relates to an improved method for producing mixtures containing 2-(2-hydroxyethyl)-piperidinyl carbamide acid secondary butyl ester from a raw product by means of a thermal treatment with short dwell times, to devices for said method, to the use of such devices for such methods, and to the mixtures according to the invention which can be obtained using the method.

用于制备包含2-(2-羟乙基)哌啶基氨基甲酸仲丁酯的混合物的方法

本发明包括一种用于通过具有较短停留时间的热处理从粗产物制备包含2‑(2‑羟乙基)哌啶基氨基甲酸仲丁酯的混合物的改进的方法，用于这种方法的设备，此类设备用于此类方法的用途，以及可以使用这种方法获得的根据本发明混合物。

방향족 디할로겐 화합물의 제조 방법

지정 약품인 아질산 tett-부틸을 사용하지 않고, 방향족 디아민 화합물로부터 고순도의 방향족 디할로겐 화합물을 공업적으로 제조하는 방법을 제공한다. 방향족 디아민 화합물, 아질산에스테르 화합물 및 할로겐화제를 반응시키는 방향족 디할로겐 화합물의 제조 방법으로서, 상기 아질산에스테르 화합물이, 아질산에틸, 아질산헥실 및 아질산아밀로 이루어진 군에서 선택된 1종 이상이며, 상기 반응이 반응 온도 35℃ 이상인 반응 공정 1을 포함하는 방향족 디할로겐 화합물의 제조 방법.

Gamma alkylation of a protected derivative of the enone of spectinomycin

Process for alkylatine protected spectinomycin enone derivatives in the gamma position in order to produce intermediates useful in the synthesis of 6'alkylspectinomycins. The intermediate have formula (III) which comprises reacting a compound having formula (V) with a strong base and an alkenyl halide, wherein R1 is selected from the group consisting of alkoxycarbonyl, halogenated alkoxycarbonyl, aralkoxycarbonyl, and arylsulfone; R2 is selected from the group consisting of hydrogen, trimethylsilyl (TMS), tetrahydropyran (THP), and triethylsilyl (TES); A is selected from the group consisting of oxygen and sulfur; M is selected from the group consisting of lithium and potassium; and n is an integer from 1 to 3.

Compuestos antihelminticos que comprenden una estructura de tienopiridina.

La presente invención se refiere a nuevos compuestos antihelmínticos. Estos compuestos se pueden usar, por ejemplo, en el tratamiento del tipo de enfermedad de gusanos causada por helmintos tales como Dirofilaria , en particular Dirofilaria immitis.

チエノピリジン構造を含む駆虫剤化合物

本発明は、新規な駆虫剤化合物に関する。これらの化合物は、例えば、ジロフィラリア（Ｄｉｒｏｆｉｌａｒｉａ）、特にジロフィラリア・イミティス（Ｄｉｒｏｆｉｌａｒｉａ ｉｍｍｉｔｉｓ）等の蠕虫によって引き起こされる種類の虫病の治療に使用され得る。

화합물 및 이를 포함하는 유기 발광 소자

본 명세서는 화학식 1의 화합물 및 이를 포함한 유기 발광 소자를 제공한다.

Luminescent probes for biological labeling and imaging, and process for preparing the same

The present invention relates to organic compounds, usable as ligands in the preparation of lanthanide complexes or of certain water-soluble transition metals, a method for preparation thereof, and the use of said organic compounds as fluorescent probes.

Method for producing aromatic dihalogen compound

An object of the present invention is to provide a method for industrially producing a high purity aromatic dihalogen compound from an aromatic diamine compound without the use of tert-butyl nitrite, which is a designated substance. A method for producing an aromatic dihalogen compound, comprising a reaction step 1 of reacting an aromatic diamine compound, an alkyl nitrite compound, and a halogenation reagent, wherein the reaction step 1 is conducted at a reaction temperature of 35°C or higher; and the alkyl nitrite compound is at least one selected from the group consisting of ethyl nitrite, hexyl nitrite, and amyl nitrite.

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Chiral diphosphorus compounds and their transition metal complexes

The present invention relates to chiral diphosphorus compounds and their transition metal complexes, to a process for preparing chiral diphosphorus compounds and their transition metal complexes and also to their use in asymmetric syntheses.

쿠마린 유도체 및 이를 포함하는 고효율 염료감응 태양전지용 염료

본 발명은 신규한 쿠마린 유도체 및 이를 포함하는 고효율 염료감응 태양전지용 염료에 관한 것으로, 하기 화학식 1로 나타내어지는 쿠마린 유도체는 우수한 광변환 효율을 가질 뿐만 아니라 장파장 영역까지 빛을 흡수하여 이러한 쿠마린 유도체를 함유하는 염료를 사용함으로써 고효율의 염료감응 태양전지 소자를 제조할 수 있다: 상기 식에서, R 1 은 , 또는 이다. 태양전지, 염료감응, 쿠마린 유도체, 태양전지 소자, 장파장 흡수, 좁은 띠간격

Gamma alkylation of a protected derivative of the enone of spectinomycin

Antikonvulsive pseudofructopyranose sulfamate

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手性二磷化合物及其过渡金属配合物

本发明涉及手性二磷化合物及其过渡金属配合物，涉及制备手性二磷化合物及其过渡金属配合物的方法，也涉及它们在不对称合成中的用途。

キラル二リン化合物、該キラル二リン化合物の製造法、該キラル二リン化合物を含む遷移金属錯体、立体異性的に富化された化合物および遷移金属錯体含有触媒の製造法

【課題】その立体的特性および電子的特性が容易に変更可能であり、不斉合成、殊に不斉水素化における触媒としてのその遷移金属錯体が高いエナンチオ選択性のみならず高い変換率をも可能にする配位子系を提供する。 【解決手段】式（Ｉ）の化合物。 これの具体例としては下式のようなものがある ２，３−ビス−Ｏ−（ジフェニルホスフィノ）−１，６−ジ−Ｏ−（ｔ−ブチルジフェニルシリル）−２，５−アンヒドロ−Ｄ−マンニトール。 【選択図】 なし

화합물 및 이를 포함하는 유기 발광 소자

본 명세서는 화학식 1의 화합물 및 이를 포함한 유기 발광 소자를 제공한다.

쿠마린 유도체 및 이를 포함하는 고효율 염료감응 태양전지용 염료

본 발명은 신규한 쿠마린 유도체 및 이를 포함하는 고효율 염료감응 태양전지용 염료에 관한 것으로, 하기 화학식 1로 나타내어지는 쿠마린 유도체는 우수한 광변환 효율을 가질 뿐만 아니라 장파장 영역까지 빛을 흡수하여 이러한 쿠마린 유도체를 함유하는 염료를 사용함으로써 고효율의 염료감응 태양전지 소자를 제조할 수 있다: 상기 식에서, R 1 은 , 또는 이다. 태양전지, 염료감응, 쿠마린 유도체, 태양전지 소자, 장파장 흡수, 좁은 띠간격

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光致变色化合物、萘酚衍生物、固化性组合物、光学物品、透镜和眼镜

本申请的目的在于，提供温度依赖性、退色速度和耐久性优异的光致变色化合物；能够成为该光致变色化合物的中间体的萘酚衍生物；能够成为该光致变色化合物的中间体的萘酚衍生物；包含该光致变色化合物的固化性组合物；光学物品；透镜；以及眼镜。根据实施方式，提供具有式(1)所示骨架的光致变色化合物。式(1)中，M为C、Si或Ge。R 1 为下述式(2)所示的基团。R 2 为式(2)所示的基团或者取代基任选包含卤素原子的烷基。