БЕНЗОПРОИЗВОДНЫЕ С ШЕСТИЧЛЕННЫМ КОЛЬЦОМ В КАЧЕСТВЕ ИНГИБИТОРА DPP-4 И ИХ ПРИМЕНЕНИЕ

Настоящее изобретение относится к соединению общей формулы I, его фармацевтически приемлемой соли, или его оптически активному изомеру:(I).В формуле (I) X выбран из O, S или NH; A представляет собой бензольное кольцо с 1-5 заместителями, где каждый заместитель независимо выбран из галогена или циано; R представляет собой H или гидрокси, n равно 1-2; кольцо B выбрано из ароматического бензольного кольца, ароматического гетероцикла, насыщенного или ненасыщенного 5-членного или 6-членного кольца, кислородсодержащего пяти- или шестичленного насыщенного или ненасыщенного гетероцикла, где заместитель Rнезависимо выбран из группы, состоящей из галогена, циано, гидрокси, Cалкила, Cалкокси, C алкоксиметокси, COOH, C алкоксикарбонила, NRR, Cалкилсульфонамидо, Cалкилсульфонила, C циклоалкилсульфонила или Cалкилсульфинила, m равно 1-4; Rи Rвместе образуют замещенный или незамещенный 5- или 6-членный циклоалкил или замещенную или незамещенную гетероциклическую группу, содержащую N, O. Также предложены ...

НОВЫЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ СТАБИЛИЗАЦИИ

Изобретение относится к фармацевтической композиции, содержащей бициклическое соединение формулыи глицерид. Изобретение также относится к самому указанному соединению и способу его стабилизации. Технический результат - повышение стабильности фармацевтической композиции за счет растворения в глицериде. 4 н. и 23 з.п. ф-лы, 3 табл.

Метод и реактивы для детекции активности люциферазы

Способ получения производных 3,4-дигидро-2H-тиопирана

FIELD: technological processes.SUBSTANCE: invention relates to the preparation of 3,4-dihydro-2H-thiopyran derivatives, that can potentially be used as monomers, intermediates in the synthesis of biologically active substances, fragrances and other practically meaningful compounds. Process for the preparation of 3,4-dihydro-2H-thiopyran derivatives from α,β-unsaturated ketones and dienophiles are carried out by Diels-Alder hetero-reaction at an elevated temperature, at atmospheric pressure in a dried aprotic non-polar solvent using the Lawesson's reagent as a sulfurizing agent, followed by isolation of the desired products, where the process is carried out in one stage at a temperature of 60 to 90 °C for 4–12 hours at a molar ratio α,β-Unsaturated ketone: Lawesson's reagent: dienophile from 1:0.5:0.9 to 1:1.2:1.2; with the subsequent isolation of the desired products by cooling the resulting mixture, filtering off the precipitate, recrystallization from the polar protic solvent, either by distilling off the solvent under reduced pressure, triturating the residue with a minimum amount of diethyl ether until crystallization, filtering off the precipitate, further purification by flash chromatography using dried methylene chloride as the eluent, or distilling off the solvent under reduced pressure, dissolving the precipitate in diethyl ether, cooling the resulting mixture to crystallization, and filtering off the precipitate.EFFECT: result of the invention is a novel simple process for the preparation of 3,4-dihydro-2H-thiopyran derivatives, which does not require the purification of products by column chromatography, a large solvent consumption, and provides a good yield of the product.1 cl, 2 tbl, 6 ex

НОВЫЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ СТАБИЛИЗАЦИИ

1-Амино-8,9-дигидро-5,8,8-триметил-3,6Н-пиразоло[3,4-B]тиопирано[4,3-D]пиридин или его гидрохлорид, обладающие противосудорожной активностью

Изобретение относится к гетероцинпическиг. соединениям в частности к 1-амино-89-дигидрс 5,88-триметил -ЗбН-пиразоло 34-Ытиог1ира ,3-б пиридину или его гидрохлориду проявляют противосудорожное действие Цель -выявление соединений обладающих указанной активностью Получение ведут из 22-диме.ил- 4-(1М-морфолино)-23-дигидро-6Н-тиопирача и хлорангидрида уксусной кислоты циклизацией полученного продукта с цианацетомидом греврп щением последнего полученного продукта в сгст ветствующее хлорпроизводное и циклизацией его гидразингидратом с поспедуюшим пер водог/ в гидрохлорид 1 табл ...

Способ получения тиациклогексанов или 1-тиадекалинов

Способ получения аза-1-диалкиламиноалкил-10-тиоксантенов

2-ARYLCYCLOPENTAN-1,3-DIONE

Neue Zusammensetzung enthaltend eine bicyclische Verbindung und ein Glycerid

HETEROCYCLIC ANATHRACYCLINONE & ANATHRACYCLINE ANALOGS

Heterocyclic anathracyclinone and anathracycline analogs

This invention relates to improved anthracyline derivatives, to process and to intermediates for preparing the derivatives, to pharmaceutical compositions containing them and to the use of these derivatives as antitumor agents in mammals. More specifically, the present invention relates to 8-heteroanthracycline derivatives.

“Proceeded of preparation of derived from alcanoïques acids benzocycloalcényl dihydroxy and drugs the container”.

Acetyl 2-hydroxy-1,3 diaminoalkanes.

New derivatives of the catéchol, a process for their preparation and compositions therapeutic containing these derivatives.

New derivatives of the catéchol, a process for their preparation and compositions therapeutic containing these derivatives.

HETEROCYCLIC ANATHRACYCLINONE & ANATHRACYCLINE ANALOGS

PROCEDURE FOR THE PRODUCTION OF NEW PIPERIDY EYELID DERIVATIVES OF BENZOXANTHENEN AND THEIR SAEUREADDITIONSSALZEN

PROCEDURE FOR THE PRODUCTION OF NEW TRICYCLI CONNECTIONS AND THEIR SALTS

PROCEDURE FOR THE PRODUCTION OF NEW SPIRO HYDANTOINEN

PROCEDURE FOR THE PRODUCTION OF NEW SPIRO HYDANTOINEN

DESCENDANTS OF BENZOCYCLOALKENYLDIHYDROXYALKANSAEUREN, PROCEDURES FOR THEIR PRODUCTION AND THESE CONTAINING PHARMACEUTICALS.

BIOLOGICALLY EFFECTIVE ONES, HETEROBICYCLI HYDROXIMIDATE AND THIOLHYDROXIMIDATE AND THEIR CARBAMATESTER DERIVATIVES.

BIZYCLI CONNECTIONS COMPOSITION AND PROCEDURE FOR YOUR STABILIZATION

IMINO-OXYMETHYL-ANILINE DERIVATIVES

Compounds for the treatment of paramoxyvirus viral infections

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

Restricted 9-CIS-retinoids

BIOLOGICALLY ACTIVE HETEROCYCLIC HYDROXIMIDATES AND THIOLHYDROXIMIDATES AND CARBAMATE ESTER DERIVATIVES THEREOF

Novel composition and method for stabilizing the same

7,9-SUBSTITUTED TETRACYCLINE COMPOUNDS

The present invention pertains to novel 7,9-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

PROCEDE DE PREPARATION DES NOUVEAUX DERIVES DU THIOCHROMANE

CERTAIN SUBSTITUTED 4-BENZOYL-3,5-DIOXOTETRAHYDROPYRANS AND THIOPYRANS

CERTAIN SUBTITUTED 4-BENZOYL-3,5-DIOXOTETRAHYDROPYRANS AND -THIOPYRANS Compounds of the formula wherein X is oxygen, sulfur or sulfonyl; R is halogen; C1-C2 alkyl; C1-C2 alkoxy; nitro; cyano; C1-C2 haloalkyl; or RaSOm- wherein m is 0 or 2 and Ra is C1-C2 alkyl; R1 is hydrogen or C1-C4 alkyl; R2 is hydrogen or C1-C4 alkyl; or R1 and R2 together are alkylene having 2 to 5 carbon atoms; R3 is hydrogen or C1-C4 alkyl; R4 is hydrogen or C1-C4 alkyl; or R3 and R4 together are alkylene having 2 to 5 carbon atoms; R5 and R6 independently are (1) hydrogen; (2) halogen; (3) C1-C4 alkyl; (4) C1-C4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C1-C4 haloalkyl; (9) RbSOn- wherein n is the integer 0, 1 or 2; and Rb is (a) C1-C4 alkyl; (b) C1-C4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) -NRcRd wherein Rc and Rd independently are hydrogen or C1-C4 alkyl; (11) ReC(O)- wherein Re is C1-C4 alkyl or C1-C4 alkoxy; or (12) -SO2NRcRd wherein Rc and Rd are as defined ...

SELECTIVE ESTROGEN RECEPTOR MODULATORS FOR THE TREATMENT OF VASOMOTOR SYMPTOMS

The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.

2-PHENYL-3-AROYLBENZOTHIOPHENES AND THEIR 1-OXIDES

Procédé de préparation de nouveaux dérivés du thiochromanne

PROCEDE DE PREPARATION DE COMPOSES PHARMACEUTIQUEMENT ACTIFS.

PROCEDE DE PREPARATION D'ACIDES CHROMONE-CARBOXYLIQUES.

PROCEDE DE PREPARATION DE COMPOSES PHARMACEUTIQUEMENT ACTIFS.

PROCEDURE FOR the PRODUCTION OF NEW ONES 2-PHENYL-3-AROYLBENZOTHIOPHENEN AND 2-PHENYL-3-AROYLBENZOTHIOPHEN-1-OXIDEN.

Process for the preparation of new hydantoin derivatives

PROCEDE DE PREPARATION DE COMPOSES PHARMACEUTIQUEMENT ACTIFS.

(thio)pyrano-indole derivs

... (thio)pyrano-indole derivs with antidepressant and antiulcer activity ...

PROCEDURE FOR THE PRODUCTION OF NEW PIPERIDYLIDENDERIVATE OF BENZOXANTHENEN, - THIOXANTHENEN AND - DIBENZOXEPINEN.

PROCEDURE FOR the PRODUCTION OF NEW ONE 2-PHENYL-3-AROYLBENZOTHIOPHENEN.

PROCEDURE FOR the PRODUCTION OF NEW ONES 2-PHENYL-3-AROYLBENZOTHIOPHENEN AND 2-PHENYL-3-AROYLBENZOTHIOPHEN-1-OXIDEN.

LIKE PROSTAGLANDIN I (1) AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.

BICYCLIC CATECHOL DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THERAPEUTIC COMPOSITIONS CONTAINING THE SAME.

SUBSTITUTED IMINODERIVATE OF DIHYDROBENZOPYRAN AND OF DIHYDROBENZOTHIOPYRAN AND YOUR PHARMACEUTICAL ACCEPTABLE ONES OF SALTS, PROCEDURES FOR YOUR PRODUCTION AND DRUG, WHICH THIS CONTAINING.

CATECHOL DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THERAPEUTIC COMPOSITIONS CONTAINING THE SAME.

DERIVATIVES OF ALKINILSODERZhAShchIKh HYDRO KSAMOVYKh ACIDS AND THEIR USE AS INHIBITORS OF TACE

АЦЕТИЛ 2-ГИДРОКСИ-1,3-ДИАМИНОАЛКАНЫ

Раскрываются соединения формулы (I), где переменные Z, X, R15,R2, R3 и Rc имеют определенное в описании значение. Раскрываемые соединения являются ингибиторами фермента бета-секретазы и поэтому полезны при лечении болезни Альцгеймера и других заболеваний, характеризующихся отложениями A бета пептида в организме млекопитающих. Отчет о международном поиске был опубликован 2005.06.23.

БІЦИКЛІЧНІ СПОЛУКИ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ВИКОРИСТАННЯ ЯК ЛІКАРСЬКИХ ЗАСОБІВ

Даний винахід відноситься до деяких біциклічних сполук, що мають ядро, утворене двома конденсованими шестичленними циклами, наприклад, ізохіноліном, ізохінолоном, тетрагідронафталіном, дигідронафталіном чи тетралоном, заміщеними як кислотними, так і основними функціональними групами, що викристовуються в інгібіюванні агрегації еритроцитів.

АЦЕТИЛ 2-ГИДРОКСИ-1,3-ДИАМИНОАЛКАНЫ

Раскрываются соединения формулы I, где переменные Z, X, R15, R2, R3 и Rc имеют определенное выше значение. Раскрываемые соединения являются ингибиторами фермента бета-секретазы и поэтому полезны при лечении болезни Альцгеймера и других заболеваний, характеризующихся отложениями А бета-пептида в организме млекопитающих.

СЕЛЕКТИВНЫЕ МОДУЛЯТОРЫ РЕЦЕПТОРОВ ЭСТРОГЕНА ДЛЯ ЛЕЧЕНИЯ ВАЗОМОТОРНЫХ СИМПТОМОВ

Данное изобретение относится к селективному модулятору рецепторов эстрогена формулы (I) или его фармацевтической соли с кислотой, полезных для лечения вазомоторных симптомов.

COMPOUNDS FOR THE TREATMENT OF PARAMOXYVIRUS VIRAL INFECTIONS

Plastic colorant GG orange and preparation method thereof

本发明提出一种塑料着色剂GG橙及其制备方法，N,N‑二甲基甲酰胺780‑820份、盐酸190‑200份、水105‑110份、3‑(2‑氨基苯巯基)苯绕蒽酮230‑240份、28‑32％的亚硝酸钠水溶液45‑50份、催化剂0.6‑0.9份。称取N,N‑二甲基甲酰胺、盐酸和水泵入反应釜中，再投入3‑(2‑氨基苯巯基)苯绕蒽酮，通冷冻盐水使温度降温至3‑6℃，再滴加亚硝酸钠水溶液，滴加量为25‑50kg/h，在常压、10‑20℃下保温反应1.5‑2.5h，压滤得滤液；滤液转至闭环釜内，再加入铜触酶，升温至75‑85℃保温2.5‑3.5h，进行压滤，得滤饼；滤饼加入打浆釜中，再加入剩余的水进行打浆1.5‑2.5h，放入抽滤缸进行真空吸滤、热水漂洗至pH为7‑9，滤饼进行烘干，打粉、拼混、包装得到产品。本发明制备的成品具有耐温高、高透明、强荧光、着色率高等特性，且制备过程副反应少，产品纯度高。

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

DERIVED PIPERIDYLIDENIQUES FROM BENZO-XANTHENES,

Analogues de la prostaglandine I1 et compositions pharmaceutiques les contenant.

L'invention concerne de nouveaux analogues de la prostaglandine I1 . Ces composés ont la formule ci-dessous, dans laquelle A = noyau pentagonal de type prostaglandinique, B = noyau pentagonal ou hexagonal incluant un atome de soufre, Y = éthylène, vinylène ou éthylène, Z = chaînon hydrocarboné, R**1 = groupe carboxy, ester, amide ou hydroxyméthyle éventuellement estérifié, R**2 = H, méthyle, éthyle, R**3 = liaison simple ou alcoylène, R** 4 = H, alcoyle, alcoxy, ou, phényle ou phénoxy éventuellement substitués. Applications pharmacologiques dans le domaine obstétrical et gynécologique.

NEW COMPOSE SPIROHETEROCYCLANIQUES, THEIR METHOD OF PREPARATION AND THEIR APPLICATION LIKE DRUG

MONO THIACHROMONE-2-CARBOXYLIC ACIDS

DERIVES PIPERIDYLIDENIQUES DE BENZO-XANTHENES, -THIOXANTHENES ET -DIBENZOXEPINES, LEUR PROCEDE DE PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE

L'invention a pour objet un composé répondant à la formule I : ...

OXA DERIVATIVES 16-AND 16-THIA-D-HOMO-ESTROGENS AND THEIR USE AS ORAL CONTRACEPTIVES

DRUGS CONTAINING NEW DERIVATIVES BICYCLIQUES OF THE CATECHOL

Derivados de fenilglicina

NOVEL THERAPEAUTIC AGENTS FOR THE TREATMENT OF CANCER, METABOLIC DISEASES AND SKIN DISORDERS

The present invention is directed to compounds having the structure (I) wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.

Cyclopropanoid cyanoesters and method of making same

Cyclopropanoid cyanoesters of the formula: см. иллюстрацию в PDF-документе where R' is --CH3 or --CH2 CH3, and A is (a) --H, or (b) A, B represents an aliphatic group joined to a carbon atom on the cyclopropanoid ring, thereby forming a spiro group, A, B being selected from structures having the formula: (i) --(CH2)n --, wherein n=3, 4, or 5, and (ii) --(CH2)2 --Y--(CH2)2 --, wherein Y is NCH3, O, or S); and, when A is --H, B is selected from the group consisting of: см. иллюстрацию в PDF-документе are disclosed. These compositions are useful in the synthesis of pyrethroids. A process for synthesis of cyclopropanoid cyanoesters by reacting 2-nitropropane with cyanoesters of the general formula: см. иллюстрацию в PDF-документе is also disclosed and claimed.

O- or S-substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity

Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Derivatives of cyclic ethers and sulfides for the treatment of atherosclerosis

The present invention provides compounds of Formula I, (I) or a pharmaceutically acceptable salt forms thereof, which are inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.

NOVEL 2,3-CYCLOPENTATHIOCHROMONE DERIVATIVE AND PREPARATION THEREOF

NEW MATERIAL:To compound of formula I (X is linked to the 5-, 6- or 7-position and hydroxy, alkoxyl acyloxy, etc.). EXAMPLE: 6-Methoxy-2,3-cyclopentathiochromone. USE: Useful as medicines having improved analgesic and anti-inflammatory action. PROCESS: A benzenethiol of formula II (X is linked to the m- p-position and represents hydroxy, alkoxyl, etc.) is reacted with a 2-cyclopentanonecarboxylic acid of formula III (R2 is H or alkyl) in the presence of excess polyphosphoric acid at 80W95°C for 30secWseveral minutes to give the aimed compound of formula I . The use of a compound of formula II (X is linked to the m-position) provides the compound of formula I (X is linked to the 5- or 7-position). The polyphosphoric acid prepared from phosphorus pentoxide and phosphoric acid is usually used. COPYRIGHT: (C)1984,JPO&Japio ...

НОВЫЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ СТАБИЛИЗАЦИИ

Изобретение относится к фармацевтической композиции, содержащей бициклическое соединение формулыи глицерид. Изобретение также относится к самому указанному соединению и способу его стабилизации. Технический результат - повышение стабильности фармацевтической композиции за счет растворения в глицериде. 4 н. и 23 з.п. ф-лы, 8 табл.

ПРОИЗВОДНЫЕ ДИКЕТОГИДРАЗИНА И ЛЕКАРСТВЕННЫЕ СРЕДСТВА, СОДЕРЖАЩИЕ ЭТИ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ АКТИВНОГО ИНГРЕДИЕНТА

... 1. Соединение формулы (I) где R представляет собой (1) водород, (2) СусА, (3) С1-8 алкил, необязательно замещенный 1-5 группами, выбранными из галогена, СусА, нитро, трифторметила и циано, или где СусА представляет собой С3-15 моно-, би- или трициклическое карбокольцо или 3-15-членное моно-, би- или трициклическое гетерокольцо, включающее 1-4 атома азота, 1-2 атома кислорода и/или 1-2 атома серы; R16 представляет собой (1) С1-8 алкил, (2) С2-8 алкенил, (3) С2-8 алкинил, (4) СусА или (5) С1-8 алкил, С2-8 алкенил или С2-8 алкинил, замещенный 1-5 группами, выбранными из галогена, нитро, трифторметила, циано, СусА, -NR18R19, -OR18, -SR18, -NHC(О)-CycA и -NHC(O)-(C1-8 алкила); R17, R18 и R19 каждый независимо представляет собой водород, С1-4 алкил, СусА, С1-4 алкил, замещенный СусА, АА1 представляет собой (1) связь, или где R1 и R2 каждый независимо представляет собой (i) водород, (ii) С1-8 алкил, (iii) СусА или (iv) С1-8 алкил, замещенный 1-5 группами, выбранными из следующих (а)-(и): (a) – ...

Способ получения пирено /3,4- с/ тиопиранона -3 (2н)

VERFAHREN ZUR HERSTELLUNG VON BENZOCYCLOALKENYLDIHYDROXYALKANSAEUREDERIVATEN

7-Diazo-beta-lactam derivatives

SPIROTETRAHYDROPYRANS AND SPIROTHIATETRAHYDROPYRANS

... 1456955 Spiro-(thia)tetrahydropyrans ROUSSEL UCLAF 8 May 1975 [8 May 1974] 19486/75 Heading C2C Novel compounds I in which X is O or S, R is H or C 1-4 alkyl, n is 2 to 4 and R1 is H or C 1-12 acyl, are prepared by reducing a compound II in which R1 1 is H or C 1-8 alkyl, and, if desired, esterifying the resulting compound I in which R1 is H to obtain a compound I in which R1 is C 1-12 aryl. Pharmaceutical compositions having antiinflammatory and analgesic activity, for oral, rectal, parenteral or topical administration, comprise a compound I together with a pharmaceutical carrier or excipient.

LIMITED 9-CIS-RETINOIDE

PHENYLGLYCIN DERIVATIVES

ALKINYLI HYDROXAMIC ACID CONNECTIONS AS TACE INHIBITORS

PROCEDURE FOR MANUFACTURING NEW OF SUBSTITUTING IMINODERIVATE OF DIHYDROBENZOPYRAN AND DIHYDROBENZOTHIOPYRAN AND OF THEIR SALTS AND ISOMERS

VERFAHREN ZUR HERSTELLUNG VON NEUEN 7-METHOXY-6-THIATETRACYCLINEN UND DEREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN 6-THIATETRACYCLINEN

SELECTIVE MODULATORS OF THE ÖSTROGENREZEPTORS FOR THE TREATMENT OF VASOMOTORI SYMPTOMS

HERSTELLUNGSVERFAHREN NEUER BICYCLISCHER BRENZCATECHINDERIVATE

This invention relates to bicyclic catechol derivatives having the general formulae I and II I II wherein R1, R2, R3 and Z represent various substituents, to a preparation process of the same comprising reacting a compound of formula III III wherein R1 and R2 have the meanings given above with an appropriately substituted propionic or butyric acid (or an ester or a salt of the same) of formula IV IV wherein R3 has the meaning given above, and to therapeutical compositions wherein the active ingredient is one of these compounds.

PROCEDURE FOR the PRODUCTION OF NEW ONE 6-THIATETRACYCLINEN

PROCEDURE FOR the PRODUCTION OF NEW ONE 2-PHENYL-3 AROYLBENZOTHIOPHENEN AND 2-PHENYL-3 - AROYLBENZOTHIOPHEN-1-OXIDEN AND OF THEIR SALTS

PROCEDURE FOR THE PRODUCTION OF NEW TRICYCLI CONNECTIONS AND THEIR SALTS

PROCEDURE FOR the PRODUCTION OF NEW ONE 6-THIATETRACYCLINEN

PROCEDURE FOR MANUFACTURING NEW OF SUBSTITUTING IMINODERIVATE OF DIHYDROBENZOPYRAN AND DIHYDROBENZOTHIOPYRAN AND OF THEIR SALTS AND ISOMERS

DIHYDROBENZOPYRAN AND SIMILAR CONNECTIONS USABLE AS ANTI-INFLAMMATION MEANS

HETERODIAMONDOIDS

DIKETOHYDRAZINE DERIVATIVE COMPOUNDS AND DRUGS CONTAIING THE COMPOUNDS AS THE ACTIVE INGREDIENT

THIOCHROMENONES USED TO COMBAT PAINFUL CONDITIONS AND NEURODEGENERATIVE DISEASES

HETEROCYCLIC CYCLOHEXANEDIONE DERIVATIVE, PRODUCTION THEREOF, AND HERBICIDE

HETEROCYCLIC ANTHRACYCLIONE AND ANTHRACYCLINE ANALOGS

1,4-benzoxazine compounds and derivatives thereof as therapeutic drugs for the treatment of neurodegenerative conditions

BICYCLIC COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES

Provided is a compound which has strong intraocular pressure lowering action and has no side effect on eyes such as ocular stimulating property, humor protein rise etc. 2. The compound according to , wherein Z is —(CH)— wherein all symbols represent the same meanings as those described in .3. The compound according claim 1 , wherein Y is —O—.4. The compound according to claim 1 , wherein the compound represented by the formula (I) is a compound selected from the group consisting of(1) methyl 4-{(2S,4aR,5R,6R,7aS)-6-hydroxy-5-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydrocyclopenta[b]thiopyran-2-yl}butanoate,(2) methyl 4-{(2R,4aR,5R,6R,7aS)-6-hydroxy-5-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydrocyclopenta[b]thiopyran-2-yl}butanoate,(3) 4-{(2S,4aR,5R,6R,7aS)-6-hydroxy-5-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydrocyclopenta[b]thiopyran-2-yl}butanoic acid,(4) 4-{(2S,4aR,5R,6R,7aS)-6-hydroxy-5-[(1E,3S)-3-hydroxy-5-phenyl-1-penten-1-yl]octahydrocyclopenta[b]thiopyran-2-yl}butanoic acid,(5) 4-{(2R,4aR,5R,6R,7aS)-6-hydroxy-5-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydrocyclopenta[b]thiopyran-2-yl}butanoic acid,(6) 4-{(2S,4aR,5R,6R,7aS)-5-[(1E,3R)-4-(4-fluorophenoxy)-3-hydroxy-1-buten-1-yl]-6-hydroxyoctahydrocyclopenta[b]thiopyran-2-yl}butanoic acid,(7) 4-{(2S,4aR,5R,6R,7aS)-5-[(1E,3R)-4-(3-chlorophenoxy)-3-hydroxy-1-buten-1-yl]-6-hydroxyoctahydrocyclopenta[b]thiopyran-2-yl}butanoic acid,(8) 4-{(2S,4aR,5R,6R,7aS)-6-hydroxy-5-[(1E,3R)-3-hydroxy-4-(3-methylphenoxy)-1-buten-1-yl]octahydrocyclopenta[b]thiopyran-2-yl}butanoic acid,(9) 4-{(2S,4aR,5R,6R,7aS)-5-[(1E,3R)-4-(2-fluorophenoxy)-3-hydroxy-1-buten-1-yl]-6-hydroxyoctahydrocyclopenta[b]thiopyran-2-yl}butanoic acid,(10) 4-{(2S,4aR,5R,6R,7aS)-5-[(1E,3R)-4-(3-fluorophenoxy)-3-hydroxy-1-buten-1-yl]-6-hydroxyoctahydrocyclopenta[b]thiopyran-2-yl}butanoic acid,(11) 4-[(2S,4aR,5R,6R,7aS)-6-hydroxy-5-{(1E,3R)-3-hydroxy-4-[3-(trifluoromethyl)phenoxy]-1-buten-1-yl}octahydrocyclopenta[b]thiopyran-2-yl]butanoic ...

Novel diazo benzothiapyrone photosensitive protecting groups and synthesis method thereof

本发明公开了新型重氮基苯并噻喃酮类光敏保护基及合成方法，本发明提供的化合物能够对磷酸官能团化合物的保护，新型苯并噻喃酮类光敏保护基光解离反应高效迅速，且在日常光照条件下具有良好的相对稳定性，且具有独特的既对光响应又能释放潜在荧光基团的光敏结构。便于对光控过程进行跟踪监测，达到释放的“可控性”、“可视性”。为在细胞生物环境下进行定量释放和积聚度研究提供新的研究方法。

Method of preparing thiochromane derivatives or their salts

A side chain -OCH2CHOHCH2NHR2 is fixed to a hydroxythiochroman of formula: <IMAGE> by a 2-stage synthesis, a) reaction with a glycerol halohydrin in basic medium and b) reaction of the 2,3-dihydroxypropoxythiochroman thus formed with an amine R2NH2 in the presence of an aminotriphenylphosphonium halide. The compounds (I) thus obtained and their salts are known as beta -blocking agents and used, especially, in the treatment of disorders of the cardiac rhythm. Compared with the prior process starting from the same compounds (II) and ending in the same compounds (I), the new process requires shorter reaction times and a reduced quantity of the amine R2NH2, which makes possible a selective amination of the primary alcohol functional group.

Prodn of a thiochromanone deriv

Prodn of a thiochromanone deriv. The deriv. is of general formula (I) (wherein R=H, lower alkyl or halogen, R'=R, also -CN) and is produced by oxidising the corresponding thio deriv.

New derivatives of benzothiopyrone and their preparation process

New derivatives of thiachromanes.

(4)-Hydroxy-(1)-thio-coumarin derivs. - for use as anticoagulant medicaments

Alkoxy carbonylmethyl derivs of condensed cyclic sulphides - - with antirheumatic and allied activity

4-Hydroxy-thiochromanes prodn. - from thiochromanones by catalytic hydrogenation with nickel, useful as medicinal inters

Process for the production of substituted 3, 4-dihydro-2-benzothiopyranes

Process for preparing thiochromes

Patent FR2125152B1

4-hydroxy-2h- 1-benzothiopyran-3-carboxamide 1,1-dioxides

Compounds having the following structural formula are disclosed: WHEREIN R1 is aryl which may be substituted or unsubstituted; R2 is alkyl, aryl, aralkyl, alkoxy, halogen, cyano, nitro, trifluoromethyl and the like. These compounds are prepared by treating a benzothiopyran-4-one 1,1-dioxide with a base and then treating the resulting anion with an appropriate arylisocyanate, or by aminolysis of the 3carboxylate ester of a benzothiopyran-4-one 1,1-dioxide. These compounds are useful as antiinflammatory agents.

Process for the preparation of derivatives of 4-oxycoumarin

4-hydroxy-2h-benzothiopyran-3-carboxamide 1,1-dioxides

PROCEDURE FOR THE PRODUCTION OF 6-TIATETRACICLIN-DERIVATIVES

Salt of benzothiopyrone compound and preparation method and application thereof

本发明属于医药技术领域，公开了苯并硫代吡喃酮类化合物的盐及其制备方法和用途，具体为式(I)所示的2‑(4‑(环己基甲基)哌嗪‑1‑基)‑6‑(三氟甲基)‑8‑硝基‑苯并硫代吡喃‑4‑酮的盐、其制备方法、药物组合物及在制备治疗和/或预防结核分枝杆菌引起的感染性疾病药物中的应用。本发明旨在制备一种药代性质和理化性质显著改善并具有强体内外抗结核分支杆菌活性的2‑(4‑(环己基甲基)哌嗪‑1‑基)‑6‑(三氟甲基)‑8‑硝基‑苯并硫代吡喃‑4‑酮的盐，其作为潜在的新药物，可用于由细菌引起的感染性疾病，特别是由结核分枝杆菌引起的肺结核(TB)疾病的治疗或预防性治疗，同时可用于克服与结核分枝杆菌耐药相关的问题。

Process for the preparation of thiochroman derivatives

A side chain -OCH2CHOHCH2NHR2 is fixed to a hydroxythiochroman of formula: < IMAGE > by a 2-stage synthesis, a) reaction with a glycerol halohydrin in basic medium and b) reaction of the 2,3-dihydroxypropoxythiochroman thus formed with an amine R2NH2 in the presence of an aminotriphenylphosphonium halide. The compounds (I) thus obtained and their salts are known as beta -blocking agents and used, especially, in the treatment of disorders of the cardiac rhythm. Compared with the prior process starting from the same compounds (II) and ending in the same compounds (I), the new process requires shorter reaction times and a reduced quantity of the amine R2NH2, which makes possible a selective amination of the primary alcohol functional group.

Process for preparing benzoxanthene and benzothioxanthene dyestuffs

Mixtures of isomers of benzoxanthene and benzothioxanthene dyestuffs of the formulae ##STR1## wherein X is oxygen or sulfur, R optionally substituted alkyl, acyl or arylsulfonyl, R 1 and R 2 are hydrogen or halogen, alkyl, aryl, acyl, acyloxy, carbalkoxy, alkoxy, nitro, alkylthio or alkylsulfonyl or they form together a condensed benzene ring, R 3 and R 4 are hydrogen or halogen, alkyl, alkoxy, aryl, carbalkoxy or nitrile, R 5 and R 6 are hydrogen or optionally substituted alkoxy, are obtained by condensing the corresponding benzoxanthene or benzothioxanthene-3,4-carboxylic acid anhydrides or esters with phenyl acetic acid anhydrides or esters in the presence of alkali at a temperature of about 150° to 260° C. and alkylating or acylating the so-obtained hydroxy intermediates without previous isolation thereof when condensation and alkylation or acylation are performed in a polar organic solvent.

Patent FR2219163B1

Isothiochromene derivative and preparation method thereof

本发明属于有机化学合成领域，具体涉及一种异硫代色烯类衍生物及其制备方法。为解决应用范围有限，使用贵金属催化剂，成本高，条件苛刻，反应产物中有金属残留物等问题，本发明所提供的异硫代色烯类衍生物的制备方法具体为：以N‑芳基硫代酰胺类化合物与炔烃为原料，尿素热聚缩合制得的石墨相氮化碳(g‑C 3 N 4 )为光催化剂，在温和条件下进行成环反应制得异硫代色烯类衍生物。本发明所述方法操作简单、催化剂廉价易得、反应条件温和、底物适用范围广、无需强氧化剂、无金属残留，为异硫代色烯类衍生物的合成提供了一种经济实用且绿色环保的新方法。

Fluorophore 3-hydroxyflavone

The present invention discloses the syntheses of new 3-hydroxyflavone salts suitable for sensor applications for sensing anions, cations, DNA chains and organic compounds soluble in highly polar solvent like water. The invention discloses a compound having formula (I): wherein A = F, CI, Br, I, CH3OSO3 or CH3PhSO3; R, R1, R2, R3, R4, R5 and R6 are independently or equally an atom, or an atom chain or group of 1-60 atoms; X = O, S or NR8, in which R is an atom, or an atom chain or group of 1-60 atoms; Y = O or S; and Ar = an aromatic group having 6-14 carbon atoms; an aromatic heterocyclic group having 4, 5 or 6 carbon atoms and at least one heteroatom of N, S or O; or an aromatic fused heterobicycle having 6-9 carbon atoms and at least one heteroatom of N, S or O.

Patent FR2054448B1

Process for the preparation of 4-hydroxythiocoumarin and nitrogen analogues thereof

본 발명은 일반식 (1)로 표시되는 쿠마린 유사체의 제조방법에 관한 것으로 일반식 (2)의 화합물과 일반식 (3)의 화합물을 염기조건 하에서 반응시킨 다음, 산 처리하여 일반식 (1)의 화합물을 제조한다. 상기식에서 X는 S 또는 -NH를 표시하고, R 및 R'은 같거나 다를 수 있으며, 각각 할로겐원자 또는 C 1-4 저급알콕시기이다. 본 발명은 상대적으로 저렴한 반응물질을 사용하여 용이한 반응공정으로, 순도가 높은 목적화합물을 높은 수율로 얻을 수 있으므로 산업상 이용가능성에서 뛰어난 효과를 기대할 수 있다.

No translation available

DE DIVULGATION L'invention concerne un nouveau procédé d'obtention des dérivés du thiochromanne répondant à la formule générale I: I dans laquelle A est de l'hydrogène ou un atome d'halogène, R1 est un hydrogène ou un radical alcoyle inférieur, et R2 est un radical alcoyle inférieur ou cycloalcoyle inférieur, dans lequel on fait réagir un hydroxy thiochromanne avec une halohydrine du glycérol, puis soumet le dérivé dihydroxyle ainsi forme à une amination sélective en présence d'un halogénure de triphénylamino phosphonium. Les composes obtenus par ce procédé sont utiles en thérapeutique humaine ou animale comme agents hypotenseurs ou cardiorégulateurs.

New derivatives of thiachromanes and method of preparation

New derivatives of thiochromanes and a process for the preparation thereof

The invention comprises compounds of the formula <FORM:1060694/C2/1> wherein A is a halogen atom or a C1- 4 alkyl radical and R1, R2 and R3 represent hydrogen atoms or C1- 4 alkyl radicals, and their preparation by treating an appropriate 1,7-unsubstituted thiochromane with an oxidizing agent such as hydrogen peroxide in acetic acid to form a thiochromane - 1,1 - dioxide, reacting this product with chlorosulphonic acid and treating the resulting sulphonyl chloride with ammonia or an amine R1NH2. 2 - R2 - 3 - R3 - 6 - A - Thiochromanes are made by condensing a p-halo- or p-alkylthiophenol with a substituted acrylic acid R2.CH : CR3.COOH; cyclising the resulting b -phenylthiopropionic acid derivative e.g. b -p-tolylthio-butyric acid to give a 4-thiochromanone and reducing e.g. by Clemmensen or Wolff-Kishner reaction to the thiochromane. Pharmaceutical preparations having diuretic activity comprise the above compounds of the invention and an excipient. The preparations may take conventional solid or liquid forms, e.g. tablets.

Derivatives of amino-thiochromanones and amino-thiochromones

The invention comprises 5-substituted-8-methyl-thiochromanones and thiochromones of the general formul : <FORM:0789430/IV (b)/1> wherein X represents an aliphatic chain, Y is a tertiary amino group, and the molecule can be substituted in the 2- or 3-position, e.g. by alkyl, alkoxy, aryl, halogen-aryl and alkoxy-aryl; and processes for their preparation: (a) by reacting a 5-aminothiochromanone or thiochromone with a reactive ester of an amino alcohol or a salt thereof, preferably in the presence of a dehydrating agent; (b) by reacting a 5-halogen-thiochromanone or thiochromone with an aliphatic diamine in which at least one amino group contains a free hydrogen atom; (c) by condensing a 5-hydroxy-thiochromanone or thiochromone or an ether thereof with a diamine as in (b); (d) by reacting an amino-thiochromanone or thiochromone with an alkylene oxide or alkylene halohydrin, treating the corresponding hydroxyalkyl compound with phosphorus oxychloride and reacting the resultant halide with an amine; (e) by addition of a 5-aminothiochromanone or thiochromone to acrylonitrile and subsequent hydrogenation of the cyano group to an aminomethyl group; (f) by condensation of a b -(5-aminophenylmercapto) fatty acid ester with a reactive ester of an amino alcohol and cyclization of the resulting, basically alkylated compound with a dehydrating agent. In examples: (1) sodium pyrosulphite is added to a solution of KI, 4-nitrotoluene - 2 - sulphochloride and HCl in aqueous dioxane, giving 2,21-dimethyl-5,51-dinitrodiphenyldisulphide (A), which is suspended in alcohol and treated with sodium sulphide in NaOH and then with chloropropionic acid to yield b - (2 - methyl - 5 - nitrophenylmercapto)-propionic acid; ferrous sulphate reduction yields the 5-amino derivative, which after cyclization with H2SO4 to 5-amino-8-methylthiochromanone is reacted with diethylaminoethyl chloride to give 5-diethylaminoethylamino - 8 - methylthiochromanone; (2) treatment of A as in (1) using b - ...

Novel heterocyclic compounds

Salt of benzothiopyrone compound and preparation method and application thereof

本发明公开了苯并硫代吡喃酮类化合物的盐，具体为式(I)所示的2‑(4‑(环己基甲基)哌嗪‑1‑基)‑6‑(三氟甲基)‑8‑硝基‑苯并硫代吡喃‑4‑酮的盐、其制备方法及在治疗和/或预防结核分枝杆菌引起的感染性疾病药物中的应用。具体地说，本发明涉及式(I)药学可接受的盐以及包含本发明化合物的药物组合物。本发明旨在制备一种药代性质和理化性质显著改善并具有强抗结核分枝杆菌活性的2‑(4‑(环己基甲基)哌嗪‑1‑基)‑6‑(三氟甲基)‑8‑硝基‑苯并硫代吡喃‑4‑酮的盐，其作为潜在的新药物，可用于由细菌引起的感染性疾病，特别是由结核分枝杆菌引起的肺结核(TB)疾病的治疗或预防性治疗，同时可用于克服与结核分枝杆菌耐药相关的问题。

Pharmaceutical compositions and methods of treatment with 1-oxo-1H-2-benzothio pyran-3-carboxylic acid derivatives

The method comprises administering to an animal a novel pharmaceutical composition containing a substituted-1-oxo-1H-2-benzothiopyran-3-carboxylic acid to inhibit antigen-antibody reaction in said animal. Representative of the compounds that can be used in the method are:

Ware x x x

Process for preparing 6-thiatetracyclinracemates with "natural configuration" and their optical antipodes.

Procedimiento para la obtención de derivados de 6-tiatetraciclina, caracterizado porque mezclas de epímero de 1,44a 5,5a,6,11,12a-octahidro-3,12-dihidroxi-1,11-dioxo-6-tia- natacen-2-carboxamidas se transforman por tratamiento con una base, en caso dado en presencia de un disolvente inerte a temperaturas entre 15 y 120º con una relación de tiempo que a 20º asciende a 12 horas y a 50º aproximadamente 1 hora.

Substd. spiro cyclohexane thioxanthene CNS depressants - prepd. from a spiro cyclohexanone thioxanthene

Thioxanthenes of formula (I) and their acid addn. and ammonium salts are new (where X is H, lower alkyl, halogen, CF3, -SR', -SO2R', or -SO2N(R')2; R' is lower alkyl; Y is H or F; the dotted line in ring A is an optional bond; and Am is a gp. of formula (II)-(V). Z is N- or R4 is lower alkyl; R2 and R3 are H, halogen or CF3). (I) are antipsychotics, anxiolytics, sedatives, hypnotics, and potentiators or anaesthesia. A typical product is 4- 4-(2-hydroxyethyl)-1-piperazinyl -2'-trifluoromethyl-spiro cyc- lohexane-1, 9'-thioxanthene . This was prepd. by heating 2'-trifluoromethyl-spiro cyclohexane-1, 9'-thioxenthene -4-one with N-(2-hydroxyethyl)piperazine and p-toluene sulphonic acid, eliminating water as it formed and reducing the product with sodium borohydride.

Derivatives of thiachromane as diuretics

Epithio derivatives of aminoalkyl substituted dibenzocycloheptenes

A method for the preparation of a compound of the general formula: **(See formula)** wherein R1 and R2 each represent hydrogen or an alcohol group of 1 to 4 carbon atoms, inclusive, provided that R1 and R2 do not both represent hydrogen, and X represents hydrogen, an alcohol group of 1 to 4 atoms carbon, an alkoxyloxy group of 1 to 4 carbon atoms, inclusive, halogen or trifluoromethyl, or a non-toxic acid addition salt thereof, comprising reacting a compound of formula: **(See formula)** wherein R1, R2 and X are as indicated above, or one of its acid addition salts, with a dehydrating agent, after which the compound of formula I is isolated in the form of the free amine or a non-toxic acid addition salt, and in the case where R1 and R2 each represent an alcohol group, if desired, react the compound of formula I with a chloroform acid ester of formula Cl.COOR3, wherein R3 represents an alcoholic group or a benzyl group, hydrolyzing the resulting compound, of formula: **(See formula)** and isolating the compound of formula I, in which R1 is an alcohol group of 1 to 4 carbon atoms and R2 is hydrogen, in the free amine state or in the form of a non-toxic acid addition salt. (Machine-translation by Google Translate, not legally binding)

Novel hetero-cyclic compound and organic light emitting device comprising the same

본 발명은 신규한 헤테로 고리 화합물 및 이를 이용한 유기 발광 소자를 제공한다. The present invention provides a novel heterocyclic compound and an organic light emitting device using the same.

Thiacoumarin derivatives and process for their preparation

PHARMACEUTICAL COMPOSITION WITH RENAL VASODILATOR PROPERTY

Une compositionpharmaceutique à propriété vasodilatatrice rénale. Elle renferme à titre de principe actif le 8-(3tertbutylamino,2-hydroxypropoxy)-thiachromanne ou un de ses sels d'addition. D'utiles sels d'addition sont le chlorhydrate,lemaliate,le bromhydrate,le phosphate,l'iodhydrate,le formiate,l'acétate,le butyrate,le lactate,le tartrate,le pyruvate etc.Application en thérapeutique,en particulier dans l'insuffisance rénale d'origine hypertensive.

Novel compound and organic light emitting device comprising the same

본 발명은 신규한 화합물 및 이를 이용한 유기 발광 소자를 제공한다. The present invention provides a novel compound and an organic light emitting device using the same.

Pharmaceutical containing 8-(3-tert.-butylamino-2- hydroxypropoxy)-thiachroman

PROCESS FOR PREPARING HETEROCYCLIC COMPOUNDS

Process for the preparation of 4,4-dimethyl-6-ethynylthiochroman

An improved process for the preparation of key intermediates for tazarotene, 4,4-dimethyl-6-ethynylthiochroman, is provided comprising (a) reacting 4,4-dimethyl-6-acetylthiochroman of the formula with an acid chloride and an amido-group containing compound of the general formula wherein R is hydrogen or a hydrocarbyl of from 1 to 15 carbon atoms and R 1 and R 2 can be the same or different and are hydrocarbyls of from 1 to 15 carbon atoms or R 1 and R 2 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms, or one of R 1 and R 2 together with the nitrogen atom to which it bonded are joined together with the carbonyl radical to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms to form a chloro vinyl carbonyl compound intermediate of the general formula wherein R has the aforestated meanings; and (b) reacting the β-chloro vinyl carbonyl compound intermediate with an alkali metal to provide the 4,4-dimethyl-6-ethynylthiochroman.

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化合物、有機エレクトロルミネッセンス素子用材料、有機エレクトロルミネッセンス素子、及び電子機器

下記式（１）で表される化合物： （式（１）中の各記号は明細書で定義したとおりである。）、該化合物を含む有機エレクトロルミネッセンス素子、及び該有機エレクトロルミネッセンス素子を含む電子機器。

Procedimento per la produzione di 6-tiatetraciclin-derivati

Salt of benzothiopyrone compound, and preparation method therefor and application thereof

The present invention relates to the technical field of medicine, and provides a salt of a benzothiopyrone compound, and a preparation method therefor and an application thereof, in particular, a salt of 2-(4-(cyclohexylmethyl)piperazin-1-yl)-6-(trifluoromethyl)-8-nitro-benzothiopyran-4-one as represented by formula (I), a preparation method therefor, a pharmaceutical composition thereof, and an application thereof in preparation of a drug for treating and/or preventing an infectious disease caused by Mycobacterium tuberculosis. The present invention aims to prepare a salt of 2-(4-(cyclohexylmethyl)piperazin-1-yl)-6-(trifluoromethyl)-8-nitro-benzothiopyran-4-one having significantly improved pharmacokinetic properties and physicochemical properties and having strong anti-Mycobacterium tuberculosis activity in vivo and in vitro; as a potential novel drug, the salt can be used for treatment or preventive treatment of an infectious disease caused by bacteria, particularly tuberculosis (TB) caused by Mycobacterium tuberculosis, and can also be used for overcoming a problem related to drug resistance of Mycobacterium tuberculosis.

シクロヘキセノンジオキソチオクロマノイル誘導体

(57)【要約】 本発明は、式(I)（式中、Ｘは任意に置換されていてもよい-O-(CH 2 ) n -鎖を形成するか、任意に置換されていてもよくかつ／また酸素もしくは硫黄が組み込まれていてもよい-(CH 2 ) p -鎖を形成し、ｎは１〜５の範囲であり、ｐは２〜６の範囲である）で表されるシクロヘキセノンジオキソチオクロマノイル誘導体に関する。また本発明は、農業目的で使用されるシクロヘキセノンジオキソチオクロマノイル誘導体の塩、シクロヘキセノンジオキソチオクロマノイル誘導体を製造するための方法および中間生成物、該誘導体を含む薬剤、並びに、望ましくない植物を防除するための該誘導体または該誘導体を含む薬剤の使用に関する。

Verfahren zur Herstellung von Thiochromonen

苯并硫代吡喃酮类化合物的盐及其制备方法和用途

本发明属于医药技术领域，公开了苯并硫代吡喃酮类化合物的盐及其制备方法和用途，具体为式(I)所示的2‑(4‑(环己基甲基)哌嗪‑1‑基)‑6‑(三氟甲基)‑8‑硝基‑苯并硫代吡喃‑4‑酮的盐、其制备方法、药物组合物及在制备治疗和/或预防结核分枝杆菌引起的感染性疾病药物中的应用。本发明旨在制备一种药代性质和理化性质显著改善并具有强体内外抗结核分支杆菌活性的2‑(4‑(环己基甲基)哌嗪‑1‑基)‑6‑(三氟甲基)‑8‑硝基‑苯并硫代吡喃‑4‑酮的盐，其作为潜在的新药物，可用于由细菌引起的感染性疾病，特别是由结核分枝杆菌引起的肺结核(TB)疾病的治疗或预防性治疗，同时可用于克服与结核分枝杆菌耐药相关的问题。

화합물 및 이를 포함하는 유기 발광 소자

본 명세서는 화학식 1의 화합물 및 이를 포함하는 유기 발광 소자에 관한 것이다.

Process for the preparation of acetylenic retinoid

A process for the preparation of acetylenic retinoid, ethyl-6-[2- (4,4- dimethylthiochroman-6-yl)ethynyl]nicotinate, a compound of formula 1,comprising, (a) cyclizing phenyl-3-methylbut-2-enylsulfide, a compound of formula 6, in presence of an acid selected from sulfuric acid or p-toluenesulfonic acid to yield 4,4-dimethylthiochroman, a compound of formula 2; (b)acetylating the compound of formula 2, to 4,4 -dimethyl-6-acetylthiochroman, a compound of formula 3; (c)(i) reacting the compound of formula 3 with hydrazine;(ii) reacting resultant product of step (i) with iodine; (iii) converting the resultant product of step (ii) to 4,4-dimethyl-6- ethynyl thiochroman, a compound of formula 4 and (d) reacting the compound of formula 4 with ethyl-6-halonicotinate, a compound of formula 5, wherein X is Cl or Br, in presence of cuprous halide, a transition metal and an inorganic base.

Thia-chromannone-4-oxime

a. Nouveau dérivé de la thia-chromannone-4-oxime ayant une activité diurétique. b. C'est le dioxyde-1,1 de chloro-7-hydroximino-4 thia-chromanne de formule :

Cyclohexenone dioxothiochromanoyl derivatives

Procedimiento de preparacion de nuevos derivados del benzo-tiopirano.

Composizione farmaceutica a base di derivanti di tiacromano, con proprieta' emobiologiche

Compisizone farmaceutica con proprieta' vasodilatatrice renale, abase di 8-(3-terz.butilammino-2idrossi-propossi)-tiacromano

一种合成3-磺酰化硫代黄酮类化合物的合成方法

本发明涉及一种合成3‑磺酰化硫代黄酮类化合物的合成方法，在催化剂和氧化剂的作用下，将甲硫基芳香炔酮类化合物和芳基磺酰肼类化合物置于溶剂中，在蓝光照射、氮气环境的条件下进行反应，反应结束后经分离得到3‑磺酰化硫代黄酮类化合物。该方法不需要使用过渡金属催化剂，也不需要使用传统的挥发性有机溶剂，而是以绿色溶剂乙二醇或水作为反应介质，在可见光的催化下使用有机光敏剂作为催化剂，一锅反应合成目标产物。该方法所涉及的操作简便安全、反应条件温和，而且该方法光源为可见光，绿色无公害，催化剂和反应介质对环境也较友好，此外，本方法合成产物的产率较高。

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Procédé de préparation des nouveaux dérivés du benzothiopyranne

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Benzothiopyranverbindungen, verfahren zu ihrer herstellung und sie enthaltende arzneimittel

Benzthiopyranverbindungen und Verfahren zu ihrer Herstellung. Arun: Science Union et Cie. Socie'te Francaise de Recherche Medicale, Suresnes (Prankreich)

Benzothiopyran compounds

BENZOTHIOPYRAN COMPOUNDS OF THE FORMULA: 1,2-(-S-B-A-),R'',(R-(CH2)N-O-)BENZENE WHEREIN A IS METHYLENE, HYDROXYMETHYLENE OR CARBONYL; B IS ETHYLENE OR VINYLENE WHICH ARE OPTIONALLY SUBSTITUTED BY LOWER ALKYL; N IS 2, 3 OR 4; R IS DI-LOWER ALKYL AMINO OR PYRROLIDINO, PIPERIDINO, MORPHOLINO, HEXAMETHYLENEIMINO, 3-AZABICYCLO (3,3,0)-3-OCTYL, OR ALL THESE HETEROCYCLIC RADICALS SUBSTITUTED BY ONE OR MORE LOWER ALKYLS; AND R'' IS HYDROGEN OR HALOGEN. THESE COMPOUNDS POSSES CARDIOVASCULAR AND CIRCULATORY PROPERTIES.

钯催化制备式苯并-1-亚砜基-2-苯基-2h-硫代吡啶基苯基甲酮类化合物的方法

本发明公开了钯催化制备式(Ⅳ)所示的苯并‑1‑亚砜基‑2‑苯基‑2H‑硫代吡啶基苯基甲酮类化合物的方法，其特征在于制备方法为：式(Ⅰ)所示的苯并‑2H‑硫代吡啶类化合物、式(Ⅱ)所示的苯甲醛类化合物和式(Ⅲ)所示的碘苯类化合物，以氯化钯为催化剂，以三乙胺为碱，在乙腈中充分反应，制备得到苯并‑1‑亚砜基‑2‑苯基‑2H‑硫代吡啶基苯基甲酮类化合物。本方法通过采用催化效率高的氯化钯作为催化剂，氧化剂选择无毒的、无有害副产物的氧气，产率优良，符合绿色合成的要求等优点，在有机亚砜类化合物相关的药物中间体合成领域具有重要的应用前景。

一种基于炔烃硫羧化合成硫代黄酮类化合物的方法

本发明公开了一种基于炔烃硫羧化合成硫代黄酮类化合物的方法，属于有机合成技术领域，该方法主要包括以下步骤：将硫酚化合物、碱和炔烃化合物混合，然后在CO 2 气氛下加入溶剂，于可见光照射和室温条件下，进行炔烃硫羧基化反应，反应完成后去除溶剂，然后加入添加剂进行付克酰化反应，最后淬灭，制得环化的硫代黄酮类产物。本发明的制备方法对于炔烃和硫酚底物，表现出优异的反应性，室温下实现了炔烃硫羧化反应，具有操作方便、原料廉价易得、反应条件温和、底物普适性广和产物收率高的特点。

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아민계 화합물, 이를 포함하는 유기 발광 소자 및 그 전자 장치

본 발명은 아민계 화합물, 이를 포함한 유기 발광 소자 및 유기 발광 소자를 포함하는 전자 장치에 관한 것으로, 본 발명에 따르면 높은 발광 효율, 낮은 구동 전압, 고내열성을 가지는 유기 발광 소자를 제공할 수 있고, 유기 발광 소자의 색순도 및 수명을 향상시킬 수 있다.

Hydroxybenzo[b]thiacyclohexadien-4-one und Verfahren zu ihrer Herstellung

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Verfahren zur Herstellung von Derivaten des Thiacumarins und deren Salzen

아민계 화합물, 이를 포함하는 유기 발광 소자 및 그 전자 장치

본 발명은 아민계 화합물, 이를 포함한 유기 발광 소자 및 유기 발광 소자를 포함하는 전자 장치에 관한 것으로, 본 발명에 따르면 높은 발광 효율, 낮은 구동 전압, 고내열성을 가지는 유기 발광 소자를 제공할 수 있고, 유기 발광 소자의 색순도 및 수명을 향상시킬 수 있다.

아민계 화합물, 이를 포함하는 유기 발광 소자 및 그 전자 장치

본 발명은 아민계 화합물, 이를 포함한 유기 발광 소자 및 유기 발광 소자를 포함하는 전자 장치에 관한 것으로, 본 발명에 따르면 높은 발광 효율, 낮은 구동 전압, 고내열성을 가지는 유기 발광 소자를 제공할 수 있고, 유기 발광 소자의 색순도 및 수명을 향상시킬 수 있다.

Composition pharmaceutique a base de 8-(3-tertbutylamino, 2-hydroxy-propoxy)-thiachromanne

L'INVENTION A POUR OBJET UNE COMPOSITION PHARMACEUTIQUE A PROPRIETE VASODILATATRICE RENALE. ELLE RENFERME A TITRE DE PRINCIPE ACTIF LE 8-(3-TERTBUTYLAMINO, 2-HYDROXYPROPOXY)-THIACHROMANNE OU UN DE SES SELS D'ADDITION. APPLICATION EN THERAPEUTIQUE, EN PARTICULIER DANS L'INSUFFISANCE RENALE D'ORIGINE HYPERTENSIVE.

Pharmaceutical containing 8-(3-tert.-butylamino-2- hydroxypropoxy)-thiachroman

Pharmaceutical composition having renal vasodilator properties

Composizione farmaceutica con proprieta' vasodilatatrice renale,a base di 8-(3-terz.butilammino-2-idrossi-propossi)-tiacromano

Pharmaceutical vasodilator compositions containing aminoalkoxy-thiochroman compounds

Composition pharmaceutique a propriete vasodilatatrice renale.

Procédé pour éliminer le groupe sulfonique de dérivés sulfonés de l'anthraquinone

Analogifremgangsmade til fremstilling af en 3,4-dihydro-3-phenyl-2h,5h-1-bensothiopyrano-(3,4-2)(1,3)-oxazin-2,4-dion-6,6-dioxid-forbindelse

Verfahren zur Herstellung von Derivaten des Thiacumarins

Analogifremgangsmade til fremstilling af n-acyl-4-acyloxy-2h-1-benzothiopyran-3-carboxanilid-1,1-dioxid-forbindelser

아민계 화합물, 이를 포함하는 유기 발광 소자 및 그 전자 장치

본 발명은 아민계 화합물, 이를 포함한 유기 발광 소자 및 유기 발광 소자를 포함하는 전자 장치에 관한 것으로, 본 발명에 따르면 높은 발광 효율, 낮은 구동 전압, 고내열성을 가지는 유기 발광 소자를 제공할 수 있고, 유기 발광 소자의 색순도 및 수명을 향상시킬 수 있다.

肟酯光引发剂、其制备方法及应用

本发明提供了一种肟酯光引发剂、其制备方法及应用。该肟酯光引发剂具有通式(I)所示结构，R 1 、R 1 ’、R 3 、R 4 分别独立地选自一价有机基团，可选地，R 1 和R 1 ’互相环合；m个R 2 分别独立地选自卤素原子、硝基、氰基、羟基、羧基、酰基、磺基、取代或未取代的C 1 ～C 20 的直链或支链烷基、取代或未取代的C 3 ～C 20 的环烷基、取代或未取代的C 4 ～C 20 的环烷基烷基、取代或未取代的C 4 ～C 20 的烷基环烷基、取代或未取代的C 5 ～C 20 芳基；m为0、1、2、3或4；n为1或0。本发明的肟酯光引发剂可以方便地应用于紫外光固化体系，尤其适合于汞灯固化，能够显著提升光刻胶的折射率和图案的分辨率，易合成、成本低。

Verfahren zur Herstellung von Derivaten des 5-Amino-8-methyl-thiochromons

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Acyl derivativs of -hydroxy-2h-1-benzothiopyran -3-carboxamide 1,1-dioxide

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Benzothiopyran derivatives

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Acylderivate von 4-hydroxy-2h-1-benzothiopyran-3-carboxamid-1,1-dioxiden

Analogifremgangsmåde til fremstilling af 4-acyloxy-2H-1-benzothiopyran-3-carboxanilid-1,1-dioxid-forbindelser.

一种手性联烯基硫代黄酮类衍生物的制备方法及手性烯基硫代黄酮类衍生物

本申请公开了一种手性联烯基硫代黄酮类衍生物的制备方法及手性烯基硫代黄酮类衍生物，所述制备方法用到的催化剂是钯的手性双膦配合物。通过该方法可以实现硫代黄酮类衍生物的联烯基化，以及高收率的得到具有光学纯度的含季碳硫代黄酮联烯类衍生物(对映体过量可达>99％，非对映体比例可达49/1)。本申请具有高度的对映选择性和非对映选择性，操作简单易行，催化剂商业可得，反应条件温和，能耗低，环境友好且产率好。

Verfahren zur Herstellung von Thiochromonen

近红外钙离子有机荧光探针、其合成方法及应用

本发明公开了一种近红外钙离子有机荧光探针、其合成方法及应用。所述近红外钙离子有机荧光探针的分子结构表示为： 本发明提供的近红外钙离子有机荧光探针将BAPTA钙离子螯合剂进行醛基修饰，再与荧光半体进行结合，可以增加荧光半体选择的种类同时钙离子螯合剂的引入增大了探针的共轭结构，使得所获得的钙离子荧光分子探针的吸收和发射达到近红外区域。能够通过中间基团的连接，从双键共轭拓展到苯环共轭，进一步增加探针共轭部分，增加电子传递，在已有的发射波段进一步红移发射峰。