НАФТОПИРАНЫ И СОДЕРЖАЩИЕ ИХ КОМПОЗИЦИИ И ИЗДЕЛИЯ

FIELD: organic chemistry. SUBSTANCE: invention describes novel naphthopyrans of the general formula (I) where R 1 , R 2 , R 4 and R 6 can be similar or different and each means independently hydrogen atom, linear or branched alkyl group with 1-12 carbon atoms; R 7 and R 8 can be similar or different and each means independently linear or branched alkyl group with 1-12 carbon atoms, cycloalkyl group with 3-12 carbon atoms, aryl group with 6-24 carbon atoms or heteroaryl group with 4-24 carbon atoms and at least one heteroatom as sulfur, oxygen or nitrogen atom; this aryl or heteroaryl group can be substituted with one or more substitutes taken among linear or branched alkyl group with 1-6 carbon atoms, linear or branched alkoxy-group with 1-6 carbon atoms and group NR'R'' where R' and R'' can be similar or different and each means independently linear or branched alkyl group with 1-6 carbon atoms or taken in common with nitrogen atom to which they are bound form 5-7 membered ring; the latter can include at least a single another heteroatom as oxygen atom or the group julolidine-9-yl; or groups R 7 and R 8 taken in common form adamantyl, norbornyl or fluorenylidene group; R 3 and R 5 can be similar or different and each means independently linear or branched alkoxy-group with 1-6 carbon atoms. New compounds show photochromic properties. Invention describes also photochromic compositions based on thereof and ophthalmological articles (for example, lens) that include naphthopyrans. EFFECT: valuable properties of new compounds. 10 cl, 1 dwg, 1 tbl, 10 ex росс дЬс ПЧ с» (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ” 2 175 321 (51) МПК” (13) С2 (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 99103332/04, 16.07.1997 (24) Дата начала действия патента: 16.07.1997 (30) Приоритет: 25.07.1996 РК 96/09384 (43) Дата публикации заявки: 20.12.2000 (46) Дата публикации: 27.10.2001 (56) Ссылки: 4$ 5369158 А, 29.11.1994. ...

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 ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

FIELD: pharmacy. SUBSTANCE: pharmaceutical composition as lyophilized preparation has, weight %: 6-(3-dimethylaminopropyl)-forscolin 20-80; buffer agent 5-50, and sugar 0-75. EFFECT: improved solubility of composition. 7 cl, 1 tbl ЕэоУ560с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВО” 2 095 061 ' ОМК А 64 К 31/35, 9/14 13) СЛ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5011313/14, 06.04.1992 (30) Приоритет: 15.06.1989 УР 01-150595 (46) Дата публикации: 10.11.1997 (56) Ссылки: ЕР, патент, 268256, кл. А 61 К 31/35, 1988. (61) Номер основного патента: 04830265/00-14 (14.06.90) (71) Заявитель: Ниппон Каяку Кабусики Кайся (.Р) (72) Изобретатель: Емико Ямасаки[уР], Такааки Охкума[/Р] (73) Патентообладатель: Ниппон Каяку Кабусики Кайся (/Р) (54) ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ (57) Реферат: Область применения: изобретение относится к химико-фармацевтической промышленности. Сущность: фармацевтическая композиция в виде лиофилизированного препарата содержит, мас.%: 6-/3-диметиламинопропионил/форсколина 20 - 80, буферного средства 5 - 50 ‚сахара 0 - 15. Предложенный состав обладает улучшенной растворимостью. 6 з.п. ф-лы, 1 табл. 2095061 С1 КО ЕэоУ560с ПЧ Го (19) КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ ВО” 2 095 061 ' т А бл К 31/35, 9/14 13) СЛ (21), (22) АррИсаНоп: 5011313/14, 06.04.1992 (30) Рнощу: 15.06.1989 УР 01-150595 (46) Рае ог рибИсаНоп: 10.11.1997 (61) Ааашоп ю рирИсаНоп: 04830265/00-14 (14.06.90) (71) АррИсапе: Мрроп Ка|аки Кабиз! Ка]за (Р) (72) пуетог. Ето ЧатазакУР], ТаКаак! Оклкита[Р] (73) Ргорпеюг: М'рроп Ка]аки Кабиз! Ка]за (Р) (54) РНАКМАСЕЦТ!САЕ СОМРОЗГОМ (57) АБзГасЕ: НЕЕО: рпагтасу. ЗУВЗТАМСЕ: рпагтасеийса! сотрозНоюоп аз ММорпхея ргерагаНоп паз, мечт %: 6-(3-Чтегпуатипоргору!)-РЮюгэсойп 20-80; риНег адепт 5-50, ап зидаг 0-75. ЕРЕЕСТ: ипргоуеа зомЬИЙу о{ сотрозШюп. 7 с|, 11Ы 2095061 С1 КО Еэ9э0о$560с ПЧ ГЭ Изобретение касается лиофилизованного препарата 6-(3-диметиламинопропионил) ...

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 6β -(3-АМИНОЗАМЕЩЕННЫХ ПРОПИОНИЛОКСИ)-ФОРСКОЛИНА ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫХ СОЛЕЙ

FIELD: in medicine for the treatment of cardiovascular diseases. SUBSTANCE: Reagent 1: forscoline, Reagent 2: acetone. Reaction conditions: in the presence of HCl. Reagent 3: a 1,9-isopropylidene derivative of forscoline. Reagent 4: alkali in alcohol. Reagent 5: a 7-diacetyl derivative or 1,9-isopropylidene derivative of forscoline. Reagent 6: beta-halopropionylhedine. Reaction conditions: in the presence of an organic base treatment of the resulting compound with alkali and deprotection at the 1,9-position of the resulting (3-substituted amino)propionyloxy derivative of forscoline and isolation of the desised product in the free state or as a pharmaceutically acceptable salt and optionally conversion into a 7-acetoxyderivative. The stage of reaction with an amine as well as a stage of reaction with an amine and a deprolection stage may be carried out in any sequence. The first and second stages as well as the fifth and sixth stages may be accomplished in a single stage. EFFECT: more efficient preparation process. 2 cl ССЧ9ЧЗУЗУОС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ “” 2045 523 ^^ С1 С О7 О 311/92/А 61 К 31/345 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5001102/04, 22.07.1991 (30) Приоритет: 24.07.1990 ЕР 90114124.2 (46) Дата публикации: 10.10.1995 (56) Ссылки: ЕР М 222413, кл. С 070311192, 1981. Зутпез5$. 1989, с.711. Патент Индии М 164675, кл. А 6б1К 27/00, 1988 .Патент ФРГ М 3623300, кл. С 0703111932, 1988 Патент Японии М 1-59638, М сб.6(4)-31(953), 1989. Патент ФРГ М 3737353, кл. С 070311192, 1989.Молекулярная фармакология. 1987, 32, с.133. (71) Заявитель: Хехст АГ (0Е) (72) Изобретатель: Ноель Джон де Соуза[М], Адольф Д'Са[М], Самба Лаксминераян Кэтгидж/[1М], Гулаб Баджирао Пэдвал[М], Юрген Блумбах[ОЕ] (73) Патентообладатель: Хехст АГ (0Е) (54) СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 68 -(3-АМИНОЗАМЕЩЕННЫХ ПРОПИОНИЛОКСИ)-ФОРСКОЛИНА ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫХ СОЛЕЙ (57) Реферат: Использование: в ...

СИНТЕЗ СОЕДИНЕНИЙ - ЧЕТВЕРТИЧНЫХ СОЛЕЙ

1. Способ получения соединения хлоридных четвертичных солей формулы (I): ! ! где A представляет собой карбонил; ! X представляет собой связь или -CH=CH-; ! R1 выбирают из арила, C5-C15циклоалкила или гетероциклила, ! где указанный арил необязательно замещен одним или несколькими заместителями, выбранными из низшего алкила, -(CH2)n-CF3, низшего алкоксила, алкоксикарбонила, цианогруппы, галогена или фенила, необязательно замещенного низшим алкилом, -(CH2)n-CF3, низшим алкоксилом, алкоксикарбонилом, цианогруппой или галогеном, ! где указанный C5-C15циклоалкил необязательно замещен одним или несколькими заместителями, выбранными из низшего алкила, -(CH2)n-CF3, низшего алкоксила, арила, галоген-замещенного арила, алкоксикарбонила, цианогруппы или галогена, или ! где указанный гетероциклил необязательно замещен одним или несколькими заместителями, выбранными изнизшего алкила, -(CH2)n-CF3, низшего алкоксила, арила, арил-замещенного низшего алкила, галоген-замещенного арила, алкоксикарбонила, цианогруппы или галогена; и ! где n равно 0, 1, 2, 3 или 4; ! Y представляет собой связь или -CH2-; ! X2 представляет собой -(CH2)m-, где m равно 1 или 2; ! R2 представляет собой -N+(R4R5)-ZR3; ! Z представляет собой -(CH2)p-, где p равно 0, 1 или 2; ! R3 выбирают из арила, C5-C15циклоалкила или гетероциклила, ! где указанный арил необязательно замещен одним или несколькими заместителями, выбранными из низшего алкила, -(CH2)n-CF3, низшего алкоксила, арила, галоген-замещенного арила, алкоксикарбонила, цианогруппы или галогена, ! где указанный C5-C15циклоалкил необязательно замещен одним или несколькими заместителями, выбранными из низшего алкила, -(CH2)n-CF3, низшего алкоксила, арила, галоген-замещенного арил РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2010 121 175 (13) A (51) МПК C07D 209/42 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (71) Заявитель(и): ЯНССЕН ФАРМАЦЕВТИКА Н.В. (BE) (21)(22) Заявка: 2010121175/04, 23.10.2008 Приоритет(ы): (30) ...

Способ получения производных 6-ацил-7-деацетилфорсколина

FORSKOLINDERIVATE.

NEUE POLYOXYGENIERTE LABDANDERIVATE, EIN VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL

Benzo[f]chromen- und Pyrano[3,2-f]chromen-Derivate

Die vorliegende Erfindung betrifft Benzo[f]chromen- und Pyrano[3,2-f]chromen-Derivate der Formel I $F1 worin L1, L2, R1, R2, A1, A2, Z1, Z2, m und n wie in Anspruch 1 definiert sind, ihre Herstellung, ihre Verwendung als Komponenten in flüssigkristallinen Medien sowie elektrooptische Anzeigeelemente, die die erfindungsgemäßen flüssigkristallinen Medien enthalten.

SUBSTITUIERTE NAPHTHOPYRANE

CHROMON-2-CARBONSAEUREN UND DEREN PHARMAKOLOGISCH NICHT GIFTIGE SALZE, VERFAHREN ZU IHRER HERSTELLUNG SOWIE DIESE VERBINDUNGEN ENTHALTENDE ARZNEIMITTEL

Verfahren zur Herstellung von Chromon-2carbonsaeuren und Estern derselben

POLYAMINE UND IHRE THERAPEUTISCHE VERWENDUNG

5,6-SUBSTITUIERTE, KONDENSIERTE 4-(2H)-AMINOALKOXY-2,3-PYRANONE, VERFAHREN ZU DEREN HERSTELLUNG UND SIE ENTHALTENDE ARZNEIMITTEL

Verwendung von alpha-Pyronen als Absorptionsmittel fuer ultraviolette Strahlen

NAPHTHOPYRYLIUM SALTS

... 1381279 Naphthopyrylium salts RICOH KK 22 Dec 1971 [29 Dec 1970(2)] 59567/71 Heading C2C [Also in Division G2] Novel naphthopyrylium salts having the general formula wherein R 1 represents a hydrogen atom, an alkyl group containing 1 to 10 carbon atoms, a phenyl group, a benzyl group, a p-alkylstyryl group in which the alkyl portion contains from 1 to 3 carbon atoms, a p-alkoxystyryl group in which the alkyl portion contains 1 or 2 carbon atoms, a 3,4-dialkoxystyryl group in which the alkyl portion contains 1 or 2 carbon atoms, a 3,4,5-trialkoxystyryl group in which the alkyl portion contains 1 or 2 carbon atoms, a pdialkylaminostyryl group in which the alkyl portion contains from 1 to 4 carbon atoms, apnitrostyryl group, a p-halogenoatyryl group or a p-carboxystyryl group; R 2 represents a phenyl group or a p-alkoxyphenyl group in which the alkyl portion contains 1 or 2 carbon atoms, a styryl group, a p-alkylstyryl group in which the alkyl portion contains from 1 to 3 carbon atoms, a p-alkoxystyryl ...

Improvements in or relating to the ozonisation of organic compounds

Homo- or co-polymers of polymerizable compounds, e.g olefines, styrene or acrylates, are converted into derivatives containing nitrile and hydroxy groups by ozonization in admixture with at least two mols of hydrogen cyanide per mol. of polymer, the ozonization being effected in a liquid medium under basic conditions. Derivatives containing nitrile and amino groups may be obtained by including in the reaction mixture up to five mols. of ammonia per mol. of hydrogen cyanide. The hydrogen cyanide may be used as such or formed from cyanide-generating compounds, e.g. potassium or sodium cyanide. The reaction mixture may be aqueous or anhydrous and, if aqueous, may include an emulsifier. The nitriles may be isolated or they may be converted directly in the reaction mixture into other products, e.g. hydroxy acids. Examples 30-35 describe the treatment of polybutene, polypropylene, polyisobutylene and polyethylene grease.ALSO:Hydroxynitriles are obtained by ozonizing unsaturated organic compounds ...

Bis(naphthalic)dianhydrides useful for preparing poly(naphthoylenebenzimidazoles)

Bis(naphthalic) dianhydrides of the general formula: wherein are useful for preparing poly(naphthoylenebenzimidazoles) of the general formula: wherein and n=25-500.

Red colouring hyperchromic 3 H-Naphtho[2,1-b]Pyrans

Red colouring hyperchromic compounds having general formula (I), where R1 is H, NR2R3, OR4, SR4 or R7 wherein R2 and R3 are alkyl or carbocyclic groups or together with the nitrogen to which they are attached form a heterocyclic ring; R4 is the same as R1 or is alkyl, perhaloallyl, aryl or heteroaryl; R7 is alkyl, haloalkyl, alkylthio, aryl, arylthio, heteroaryl, halogen, nitrile, carboxylate, ester, nitro, or a carbocyclic or heterocyclic ring fused to faces f, gh, i, j or k; and R5 is a cyclic aminoaryl group, an indolinoaryl group, a tricyclic nitrogen heterocycle, or an unsaturated cyclic aminoaryl group.

PHOTOSENSITIVE MATERIAL

... 1334752 Photo-sensitive materials EASTMAN KODAK CO 19 April 1971 [2 March 1970] 22821/71 Heading G2C A light-sensitive composition comprises a lightsensitive halocarbon and a 4H-pyran derivative having a 4H-pyran ring which may be fused to a mono- or bi-cyclic aromatic nucleus and having an aryl substituent on the 4H-pyran ring, the composition producing a coloured image on imagewise exposure. The composition may be dispersed in a binder such as polyvinyl butyrol or styrene/ butyl methacrylate copolymer coated on a support, imagewise exposed to produce a coloured image which may be stabilized by heating to remove unreacted halocarbon. The composition may contain sensitizers such as dialkylaminocoumarino, -stilbazoles and -benzaldehydes; preexposure stabilizers such as benzimidazoles, azoles and azines; and image stabilizers such as thiazines or alkoxyborines. Preferred 4H-pyran derivatives are those of formula: wherein R and R1 are H, alkyl or aryl and at least one of R and R' ...

DITERPENE DERIVATIVES

Phosphorus-containing derviatives of 6-chromanols

Novel esterified 5-phosphomethyl derivatives of 6-chromanol having the formula wherein R1 is a benzyl or C1- 5 alkyl radical, Y is a C1- 5 alkyl radical, R is -CH3 or -CH2(CH2CH2CH(CH3)CH2)nH where n is an integer from 1-9, and Z is -CH = CH-CH = CH- or two methoxy or methyl groups, are obtained by reacting the corresponding 5-halomethyl chromanol derivatives with silver dibenzyl phosphate, or by esterifying the corresponding 5-phosphomethyl compound with a C1- 5 diazoalkane. The former process may be carried out in a solvent for the halomethyl compound, e.g. benzene, toluene or acetonitrile, and at reflux temperature. The 5-phosphomethyl compounds used may be obtained by selectively reducing their dibenzyl esters, e.g. with hydrogen in the presence of palladium.

NOVEL 2-ALKYL-4-OXA-STEROIDS AND A PROCESS FOR THE MANUFACTURE THEREOF

... 1,207,048. 2-Alkyl-4-oxa-steroids. F. HOFFMAN-LA ROCHE & CO. A.G. 1 Nov., 1968 [2 Nov., 1967], No. 51935/68. Heading C2C. The invention comprises compounds of formula wherein m is 1 or 2, R1 is C 1-5 primary alkyl, R3, R4, R7 and R8 are each H or C 1-8 alkyl, R5 is C 1-8 alkyl, R2 is H, R6 is OH, or R2 and R6 together represent an extra bond, Z is carbonyl or C(#-OR9)(-R10) wherein R9 is H or C 1-7 acyl and R10 is H or C 1-5 hydrocarbyl, and the wavy lines indicate or #-configurations. The compounds wherein R2 + R6 represent an extra bond are prepared by acid cyclization of compounds of formula wherein R11 is C 1-8 alkoxy, and are converted to the compounds wherein R2 is H and R6 is OH by treatment with aqueous acid. The conversion of compounds of Formula I into steroids and the preparation of compounds of Formula II are ...

POLYCYCLIC COMPOUNDS

... 1335908 Polycyclic dihydropyran derivatives BADISCHE ANILIN- & SODA-FABRIK AG 19 April 1971 [2 April 1970] 25829/71 Heading C2C A polycyclic compound of the general Formula I in which R1 denotes hydrogen, a hydrocarbon radical of from 1 to 40 carbon atoms or an alkoxy group of 1 to 8 carbon atoms and R2 denotes hydrogen or a hydrocarbon radical of from 1 to 40 carbon atoms, and in which there is attached to the dihydropyran group D the structural element A, optionally followed by the structural element B and one or more structural elements A and B such that A elements alternate with B elements, to provide the formula where m is 0 or 1 and n is 0, 1, 2, 3, or 4, the total number of rings in the compound being from 2 to 10, is prepared by reacting a compound of formula when n is 1 to 9, with an acidic agent at -100‹ to +150‹C.

Intense colouring photochromic 2H-naphthol[1,2-b]pyrans and heterocyclic pyrans

SUBSTITUTED PYRANONES AND THEIR PREPARATION

NAPHTHOPYRAN DERIVATIVES

Organic pigments

Novel compounds useful as pigments in alkyd and lacquer paints and in plastics materials and having the general formula: wherein R1 and R3 are, each independently, a group of one of the following formulae II, III and IV:- in which X1 is H, C1-C4 alkyl, C1-C4 alkoxy, chlorine or bromine; X2 is H or a group - CONHAr in which Ar is phenyl or is phenyl substituted with one or more of C1-C4 alkyl, C1-C4 alkoxy chlorine, bromine, carbonamido, sulphonamido, benzimidazole and phthalimido; X3 is H, C1-C4 alkyl, C1-C4 alkoxy, chlorine or bromine; X4 is H, C1-C4 alkyl, chlorine or bromine; and X5 is H, C1-C4 alkyl, C1-C4 alkoxy, chlorine, bromine or nitro; and R2 is a group of one of the formulae V and VI below:- in which Y1 and Y2 are, each independently, H, C1-C4 alkyl, C1-C4 alkoxy, chlorine or bromine. The new compounds have low solubility in organic solvents and have excellent bleed resistance in the paints mentioned above and excellent resistance to migration in plastics ...

Substituted benzopyran derivatives for the treatment of inflammation.

A class of benzopyran derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by formula (i'), wherein x, a1, a2, a3, a4, r, r

Substituted benzopyran derivatives for the treatment of inflammation

Substituted benzopyran analogs for the treatment of inflamation

A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by formula (i')wherein x, a1, a2, a3, a4, r, r ...

Substituted benzopyran derivatives for the treatment of inflammation

Derived nitrogenized compounds oxo, proceeded of preparation and pharmaceutical compositions comprising them.

Substituted benzopyran analogs for the treatment of inflammation.

Substituted flavonoid compounds, their salts, their manufacture and medecines containing these materials.

Substituted benzopyran derivatives for the treatment of inflammation

PROCEDURE FOR THE ISOLATION OF A PHARMAKOLOGISCH EFFECTIVE SUBSTANCE FROM PLANTS, TO THE LABIATAE FAMILY HEARING

7-Acyloxy-6-aminoacyloxypolyoxylabdanes and process for their preparation

The present invention relates to 7-acyloxy-6- aminoacyloxypolyoxylabdanes and their physiologically acceptable salts and to a process for their preparation. The compounds of the invention display the pharmacological properties belonging to the class of polyoxylabdanes but show in particular a pronounced selective blood pressure-lowering effect.

PROCEDURE FOR THE PRODUCTION OF NEW HALOGEN-SUBSTITUTED BENZOPYRAN AND BENZOTHIOPYRAN-4-CARBONSAEUREN AND YOUR SALTS AND ALKYL ESTERS

VERFAHREN ZUM HERSTELLEN VON NEUEN 1-OXO-1H-NAPHTHO (2,1-B)PYRANDERIVATEN

6 (BIPHENYLESTER) - 3H-NAPHTHO Ä2,1-BÜPYRANE AS PHOTO CHROME DICHROI COLORING MATERIALS AND OPTICAL ARTICLE, WHICH CONTAIN THESE

7-ACYLOXY-6-AMINOACYLOXYPOLYOXYLABDANE AND PROCEDURE FOR YOUR PRODUCTION

PROCEDURE FOR THE ISOLATION OF A PHARMAKOLOGISCH EFFECTIVE SUBSTANCE FROM PLANTS, TO THE LABIATAE FAMILY HEARING

PHOTO CHROME NAPHTOPYRANVERBINDUNGEN

PROCEDURE FOR THE PRODUCTION OF 6 (SUBSTITUTED AMINOPROPIONYL) - DERIVATIVES OF FORSKOLIN

ANTI-IGNITING 4-AMINOPHENOL-DERIVATE.

PROCEDURE FOR THE PRODUCTION OF FORSKOLINDERIVATEN MEANS OF MIKROBIELLER TRANSFORMATIONS.

PROCEDURE FOR the PRODUCTION OF FORSKOLIN FROM 9DEOXY-FORSKOLINUND of INTERMEDIATE PRODUCTS FOR it.

AROMATIC POLYCYCLI DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE IN PHARMACEUTICAL AND COSMETIC PREPARATIONS.

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

REKOMBINANTE PRODUCTION OF NEW POLYKETIDEN

Procedures for the production of new Decahydro-3-H-benz indenen

CHINONVERBINDUNGEN FOR THE TREATMENT OF DISEASES

REKOMBINANTE PRODUCTION OF NEW POLYKETIDEN

TRICYCLI AMIDE CONNECTIONS, PROCEDURES FOR THEIR PRODUCTION AND IT ABSTENTION PHARMACEUTICAL COMPOSITIONS

ARYLODER HETEROARYL-SUBSTITUTED 3,4DIHYDROANTHRACENE AS WELL AS ARYLODER HETEROARYL-SUBSTITUTED BENZO (1,2G) - CHROM-3-EN, BENZO (1, 2G) - THIOCHROM-3-ENUND BENZO (1,2G) - 1,2DIHYDROCHINOLIN-DERIVATE WITH RETINOID MORE ANTAGONISTICALLY OR INVERSE of ANTAGONISTIC ACTIVITY

NEW ONE PHOTO CHROME NAPHTHO 2,1-B PYRANE AND PROCEDURE FOR YOUR PRODUCTION

Absorbent for ultraviolet radiation

HYDRAZINOCARBONYLOXYLABDANES, A PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

HETEROCYCLIC SUBSTITUTED 4-AMINO PHENOL DERIVATIVES

Polyalkoxylated naphthopyrans

Polyamines and their use in therapy

COMPOUNDS

PROCESS FOR THE PREPARATION OF 6-(SUBSTITUTEDAMINOPROPIONYL)-DERIVATIVES OF FORSKOLIN

Substituted benzopyran derivatives for the treatment of inflammation

Antiviral naphthoquinone compounds, compositions and uses thereof

Naphthopyrans annelated in C5C6 with an indene- or dihydronaphthalene-type and compositions and matrices containing them

New cyclic compounds having a cycloalkylene chain, a process for their preparation and pharmaceutical compositions containing them

2-adamantyl benzopyrans, the compositions and (co)polymer matrices containing them

Photochromic naphthopyrans

Tricyclic retinoids, methods for their production and use

Chromene compounds

NAPHTHOPYRANS

Aryl or heteroaryl substituted 3,4-dihydroanthracene and aryl or heteroaryl substituted benzo{1,2-g}-chrom-3-ene, benzo{1,2-g}-thiochrom-3-ene and benzo{1,2-g}-1,2-dihydroquinoline derivatives

CONFORMATIONALLY RESTRICTED POLYAMINE ANALOGS AS DISEASE THERAPIES

Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.

DERIVATIVES OF 2,2'-IMINOBISETHANOL

Derivatives of 2,2'-iminobisethanol having useful properties in the treatment and/or the prevention of disorders of the coronary-vascular system.

PHOTOCHROMIC MATERIALS

ANTIVIRAL AGENTS

The present invention provides a method of treatment or prophylaxis of hepatitis B virus in a subject comprising administering an effective amount of a compound of formula (1) or a pharmaceutically acceptable derivative, salt or prodrug thereof. In addition, there is provided compounds of formula (1) and pharmaceutical compositions thereof. Further, methods of preparing compounds of formula (1) are disclosed.

POLYMERIZABLE POLYALKOXYLATED NAPHTHOPYRANS

Described are novel photochromic polymerizable polyalkoxylated naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H- naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one polyalkoxylated substituent of from 1 to 50 alkoxy units per substituent which is end-capped with a polymerizable group. Specific substituents are also present on the naphtho, indeno and pyrano portions of the compounds. These compounds may be represented by graphic formulae (I), (II) or (III). Also described are various substrates, e.g., paper, glass, polymeric organic materials, etc., that contain or that are coated with such compounds. Optically clear articles such as contact lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, indenonaphthopyrans, benzopyrans, oxazine-type compounds, etc., are also described.

TETRAZOLYL CHROMONES

PROCESS FOR PRODUCTION OF ISOCHROMANS

CHEMICALLY ACTIVATED WATER-SOLUBLE PRODRUG

The present invention addresses the problem of providing a novel chemically activated water-soluble prodrug. The present invention provides a compound represented by formula (1), or a pharmacologically acceptable salt thereof (in the formula, A represents A-0; X1 and X2 are the same as or different from each other and each independently represent a hydroxyl group or -O-C(=O)-Y-(C(R1A)(R1B))n-NH-R2, where X1 and X2 are not simultaneously hydroxyl groups, n is 2, 3, or 4, Y represents an oxygen atom or -NR4, R1A and R1B are the same as or different from each other and each independently represent a hydrogen atom, etc., and R2 represents a hydrogen atom, etc.; and Ra to Rd are optionally present, are the same as or different from each other, and each independently represent a hydrogen atom, etc.).

IMMUNOSUPPRESSIVE PHARMACEUTICAL COMPOSITION AND USE THEREOF

Provided are a drug, a pharmaceutical composition, or a pharmaceutical kit for immunosuppression, for the treatment of conditions such as psoriasis, comprising a forskolin derivative or a salt thereof and optionally a prostaglandin compound or a glucocorticoid compound. Further provided is a method for immunosuppression, comprising administration of a forskolin derivative or a salt thereof and optionally a prostaglandin compound or a glucocorticoid compound. Forskolin derivatives show promise as a class of small-molecule drugs for achieving immunosuppression using new mechanisms, for the treatment of conditions such as psoriasis, when used alone or in combination with other substances. Compared with first-line antibody drugs, forskolin derivatives have significant advantages in process and price, and have comparable efficacy and fewer side effects compared with the first-line drug calcipotriol betamethasone ointment.

PHOTOCHROMIC COMPOUNDS

A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being -N3, -CN, -COOR', -CCR', -C(R')C(R')R', -OCOR', -OCOOR', -SR', -OSO2R''', and/or -CON(R')R', wherein each R' is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R"' is -CF3 or a perfluorinated alkyl group having from 2 to 18 carbon atoms The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound.

PROCESS FOR PREPARING A PHOTOCHROMIC POLYMERIC COMPOSITION, THUS OBTAINED POLYMERIC COMPOSITION AND USE THEREOF

The present invention discloses a process for preparing a photochromic polymeric composition, characterized in that the photochromic polymeric composition is prepared by comprising (meth) acrylamide compound in the reaction mixture useful for the preparation of the photochromic polymeric composition. The present invention also relates to the thus obtained polymeric composition, photochromic articles made from said polymeric composition, and use of said polymeric composition for preparing photochromic articles. The photochromic polymeric composition according to the present invention makes the absorption peak of the photochromic dye therein become longer, thus exhibiting a desired grey with a bit bluish green or grey with a bit blue.

INDENO-FUSED RING COMPOUNDS

The present invention relates to compounds represented by the following Formulas (I) and (II). Ring-A of Formulas I and II can be, for example, an aryl group, and Q' and Q''' can each be independently selected from groups, such as, halogen, -OH, -CN, amine groups, amide groups, carboxylic acid ester groups, carboxylic acid groups, alkenyl groups, alkynyl groups, carbonate groups, sulfide groups, and sulfonic acid ester groups. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula II.

PHOTOCHROMIC COMPOUNDS AND COMPOSITIONS

Described herein are compounds generally comprising an indeno[2',3':3,4]naptho[1,2-b] pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.

TREATMENT OF OVARIAN CANCER WITH 2-AMINO-4H-NAPHTHO[1,2-B]PYRAN-3-CARBONITRILES

Methods for inhibiting the growth of ovarian cancer cells or other serosal cancer cells are disclosed. The method involves exposing the cells to a 2-amino-4H-naphtho[1,2-b]pyran-3-carbonitrile of formula. (I). wherein Y is CR1 or N and Z is CR5 or N.

PROCESS FOR PRODUCING 6-(3-DIMETHYLAMINOPROPIONYL)FORSKOLIN

A process for producing 6-(3-dimethylaminopropionyl)forskolin, the process comprising the sequential steps of: (1) acetylating hydroxy groups in 1-position and 7-position of a compound represented by the formula (III): (see formula I) to prepare 1-acetyl-6-(3-dimethylaminopropionyl)forskolin represented by the formula (II): (see formula II) wherein Ac represents acetyl group; and (2) selectively removing the acetyl group in the 1-position of the compound represented by the formula (II) in the presence of dimethylamine in a solvent, to prepare 6-(3-dimethylamino-propionyl)forskolin represented by the formula (I): (see formula III) This compound has promise as a therapeutic agent for cardiac failure.

PROCESS FOR THE PREPARATION OF 6-ACYL, 7-ACYL, AND 6,7-DIACYL ANALOGUES OF FORSKOLIN AND INTERMEDIATES THEREOF

HOE 90/F 226 Process for the preparation of 6-acyl, 7-acyl, and 6,7-diacyl analogues of forskolin and intermediates thereof Process for the preparation of 6-acyl-, 7-acyl- or 6,7diacyl analogues of forskolin of the general formula ...

LYOPHILIZED PREPARATION OF 6-(3-DIMETHYLAMINOPROPIONYL) FORSKOLIN

AMINOALKYLCARBAMYL DERIVATIVES OF FORSKOLIN AS INTERMEDIATES FOR THE SYNTHESIS OF USEFUL FORSKOLIN DERIVATIVES

... 2081902 9117154 PCTABS00008 The subject matter of the present invention relates to aminoalkylcarbamates of forskolin and the methods of using these compounds. Specifically, the aminoalkylcarbamates may be utilized in the synthesis of forskolin derivatives. The final derivatives may, in turn, be used in the development of in vivo and in vitro assays designed to study different proteins.

PPAR GAMMA ANTAGONISTS FOR TREATING OBESITY

The present invention relates to a method of treating obesity, diabetes and other metabolic disorders in a mammal by administering to the mammal a pharmaceutical composition containing a compound that antagonizes the activi ty of PPAR.gamma. protein, or reduces the expression of PPAR.gamma. protein. Th is invention also features methods of screening for compounds for treating obesity, diabetes and other metabolic disorders.

SUBSTITUTED NAPHTHOPYRANS

Described are novel reversible photochromic 2H-naphtho¢1,2-b!pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho-portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.

Verfahren zur Herstellung eines Kondensationsproduktes.

Chromene compound

A chromene compound represented by the following formula (1): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m, and n are defined in the specification. The chromene compound is rarely deteriorated by exposure.

Pyrimidine derivatives and analogs, preparation method and use thereof

This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X 1 , X 2 , X 3 , X 4 are, independently at each occurrence, C, O, S, Se, N and P elements; R 1 , R 2 , R 3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.

Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

This invention discloses novel gamma secretase inhibitors of the formula: R 2 and R 3 , or R 2 and R 4 , or R 3 and R 4 , together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Use of rylene derivatives as photosensitizers in solar cells

Use of rylene derivatives I with the following definition of the variables: X together both —COOM; Y a radical -L-NR 1 R 2   (y1) -L-Z—R 3   (y2) the other radical hydrogen; together both hydrogen; R is optionally substituted (het)aryloxy, (het)arylthio; P is —NR 1 R 2 ; B is alkylene; optionally substituted phenylene; combinations thereof; A is —COOM; —SO 3 M; —PO 3 M 2 ; D is optionally substituted phenylene, naphthylene, pyridylene; M is hydrogen; alkali metal cation; [NR 5 ] 4 + ; L is a chemical bond; optionally indirectly bonded, optionally substituted (het)arylene radical; R 1 , R 2 are optionally substituted (cyclo)alkyl, (het)aryl; together optionally substituted ring comprising the nitrogen atom; Z is —O—; —S—; R 3 is optionally substituted alkyl, (het)aryl; R′ is hydrogen; optionally substituted (cyclo)alkyl, (het)aryl; R 5 is hydrogen; optionally substituted alkyl (het)aryl; m is 0, 1, 2; n, p m=0: 0, 2, 4 where: n+p=2, 4, if appropriate 0; m=1: 0, 2, 4 where: n+p=0, 2, 4; m=2: 0, 4, 6 where: n+p=0, 4, 6, or of mixtures thereof as photosensitizers in solar cells.

METHODS OF TREATING HIV INFECTION: INHIBITION OF DNA DEPENDENT PROTEIN KINASE

Methods of treating HIV-1 infection/AIDS in a patient infected with an HIV-1 virus comprising providing a DNA-PK inhibitor to the patient are provided herein. In one embodiment the DNA-PK inhibitor is compound of the Formula I 1. A method of treating HIV-1 infection in a patient infected with an HIV-1 virus comprising providing a therapeutically effective amount of a DNA-PK inhibitor to the patient.5. The method of claim 2 , wherein Ais N claim 2 , Ais O claim 2 , and Ais O.6. The method of claim 2 , wherein Ris hydrogen claim 2 , halogen claim 2 , C-Calkyl claim 2 , or C-Calkoxy.7. The method of wherein Ais CR claim 2 , Ais CR claim 2 , and Ais CR.8. The method of claim 7 , wherein Rand Rare independently chosen from hydrogen claim 7 , halogen claim 7 , C-Calkyl claim 7 , and C-Calkoxy.9. The method of claim 5 , wherein Rand Rare joined to form an optionally substituted phenyl ring.10. The method of claim 9 , wherein Rand Rare joined to form a phenyl ring that is unsubstituted or substituted with 1 claim 9 , 2 claim 9 , or 3 substituents independently chosen from hydrogen claim 9 , halogen claim 9 , hydroxyl claim 9 , cyano claim 9 , amino claim 9 , thiol claim 9 , C-Calkyl claim 9 , C-Calkoxy claim 9 , mono- or di-C-Calkylamino claim 9 , C-Chaloalkyl claim 9 , and C-Chaloalkoxy.11. The method of claim 9 , wherein Rand Rare joined to form an unsubstituted phenyl ring.13. The method of claim 12 , wherein Xis S.15. The method of claim 1 , wherein the DNA-PK inhibitor is provided together with instructions for treating an HIV-1 infection.16. A method of inhibiting CD4 cell death in a patient infected with HIV-1 comprisingPerforming a count of CD4 cells in the patient's blood; andAdministering an effective amount of a DNA-PK inhibitor to the patient. This application claims priority from U.S. Provisional Patent application No. 61/329,775, filed Apr. 30, 2010, which is hereby incorporated by reference in its entirety.This invention was made in part with government ...

Novel IDO Inhibitors and Methods of Use Thereof

Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed. 1. (canceled)3. (canceled)4. (canceled)5. A pharmaceutical composition for the treatment of cancer comprising a pharmaceutically acceptable carrier and an effective amount at least one indoleamine 2 claim 2 ,3-dioxygenase (IDO) inhibitor claim 2 , wherein at least one of said IDO inhibitors is the compound of .616-. (canceled)17. The pharmaceutical composition of claim 5 , further comprising at least one signal transduction inhibitor (STI).18. (canceled)19. (canceled)20. The pharmaceutical composition of claim 5 , further comprising at least one chemotherapeutic agent.21. (canceled)22. (canceled)23. The pharmaceutical composition of claim 20 , wherein said at least one chemotherapeutic agent is selected from the group consisting of paclitaxel (Taxol®) claim 20 , cisplatin claim 20 , docetaxol claim 20 , carboplatin claim 20 , vincristine claim 20 , vinblastine claim 20 , methotrexate claim 20 , cyclophosphamide claim 20 , CPT-11 claim 20 , 5-fluorouracil (5-FU) claim 20 , gemcitabine claim 20 , estramustine claim 20 , carmustine claim 20 , adriamycin (doxorubicin) claim 20 , etoposide claim 20 , arsenic trioxide claim 20 , irinotecan claim 20 , and epothilone derivatives.2434.-. (canceled)35. A compound which is the hydroquinone form of the compound of .36. (canceled)37. The compound of claim 2 , wherein X claim 2 , X claim 2 , X claim 2 , X claim 2 , X claim 2 , X claim 2 , and Xare H.38. The compound of claim 2 , wherein Xis R.39. The compound of claim 38 , wherein R is aryl.40. The compound of claim 37 , wherein Xis R.41. The compound of claim 39 , wherein R is aryl. This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 60/918,516, filed on Mar. 16, 2007. The foregoing application is incorporated by reference herein.Pursuant to 35 U.S.C. Section 202(c), it is acknowledged that the United ...

Method of inhibiting abcg2 and other treatment methods

Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): wherein R 1 , R 2 , R 3 , X 1 , X 2 , X 3 , a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.

PHARMACEUTICAL COMPOSITION FOR TREATMENT AND PREVENTION OF KIDNEY DISEASES

Provided is a pharmaceutical composition for the treatment and prevention of kidney diseases, containing (a) a therapeutically effective amount of a compound represented by Formulae 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof. 2. The method according to claim 1 , wherein X is O.5. The method according to claim 1 , wherein each of Rand Ris respectively hydrogen.9. The composition according to claim 1 , wherein the compound of Formula 1 or Formula 2 is contained in a crystalline structure.10. The method according to claim 1 , wherein the compound of Formula 1 is contained in an amorphous structure.11. The composition according to claim 1 , wherein the compound of Formula 1 or Formula 2 is formulated into the form of a fine particle.12. The composition according to claim 11 , wherein the formulation for form of a fine particle is carried out by using the particle micronization method selected from the group consisting of mechanical milling claim 11 , spray drying claim 11 , precipitation method claim 11 , homogenization claim 11 , and supercritical micronization.13. The composition according to claim 12 , wherein the formulation is carried out by using jet milling as a mechanical milling and/or spray drying.14. The composition according to claim 11 , wherein the particle size of fine particles is 5 nm to 500 μm.15. The method according to claim 1 , wherein the pharmaceutical composition is prepared into an intestine-targeted formulation.16. The method according to claim 15 , wherein the intestine-targeted formulation comprises a pH sensitive polymer.17. The method according to claim 15 , wherein the intestine-targeted formulation comprises a biodegradable polymer which is decomposable by an intestine-specific bacterial enzyme.18. The method according to claim 15 , wherein the intestine-targeted formulation comprises a biodegradable matrix ...

CHROMENE DERIVATIVES AND THEIR ANALOGA AS WNT PATHWAY ANTAGONISTS

Compounds of formula (IIc); wherein Xand Xindependently from each other are N or CRwherein Rmay be same or different; Y, Y, Yand Yindependently from each other are N or CRwherein Rmay be same or different and wherein up to 3 of the group Y, Y, Yand Ymay be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer. 116-. (canceled)18. A compound according to wherein at least one substituent Ris not H;and/or solvates; hydrates; and pharmaceutically acceptable salts thereof.19. A compound according to wherein at least 1 member of the group X claim 17 , X claim 17 , Y claim 17 , Y claim 17 , Yand Yis N;and/or solvates; hydrates; and pharmaceutically acceptable salts thereof.20. A compound according to wherein R; R; and Rare independently from each other selected from H; NH; NHCH; CHOH; CHOCH; CHNH; CHNHCH; OH; OCH; Br; F; and Cl; and Rand Rare independently from each other selected from H; NH; NHCH; CHOH; CHOCH; CHNH; CHNHCH; OH; OCH; Br; F; and Cl; or Rand Rare forming together OCHO;and/or solvates; hydrates; and pharmaceutically acceptable salts thereof.21. A compound according to wherein Ris selected from H; OH; OR; NH; NHR; N(RR); CHOH; CHOR; CHNH; CHNHR; CHN(RR); C(O)NH; C(O)NHR; C(O)N(RR); C(O)OH; and C(O)OR;{'sup': 8a', '8b', '16a', '16a', '16a', '16b, 'sub': 1', '6', '2, 'Rand Rare independently from each other selected from C-Calkyl which is optionally substituted with one or more halogen which are the same or different; OH, OR, NH; NHR; NRR;'}{'sup': 16a', '16b, 'sub': 1', '6', '1-6, 'Rand Rare independently from each other selected from C-Calkyl; wherein Calkyl is optionally substituted with one or more halogen which are the same or different;'}{'sup': 9', '9a', '9a', '9a', '9b', '13a', '13a', '13a', '13b', '9a', '9a', '9b', '9a, 'sub': 2', '2', '2', '2', '2', '2', '2', '2, 'and Ris selected H; OH; OR; NH; NHR; N(RR); ...

METHOD FOR PURIFYING COMPOUND OR RESIN

The method according to the present invention is a method for purifying a compound represented by a specific formula (1) or a resin having a structure represented by a specific formula (2), the method including a step of bringing a solution (A) including an organic solvent optionally immiscible with water, and the compound or the resin into contact with an acidic aqueous solution. 2. The method according to claim 1 , wherein the acidic aqueous solution is one or more aqueous solution of mineral acid selected from the group consisting of hydrochloric acid claim 1 , sulfuric acid claim 1 , nitric acid and phosphoric acid claim 1 , or one or more aqueous solution of organic acid selected from the group consisting of acetic acid claim 1 , propionic acid claim 1 , oxalic acid claim 1 , malonic acid claim 1 , succinic acid claim 1 , fumaric acid claim 1 , maleic acid claim 1 , tartaric acid claim 1 , citric acid claim 1 , methanesulfonic acid claim 1 , phenolsulfonic acid claim 1 , p-toluenesulfonic acid and trifluoroacetic acid.3. The method according to claim 1 , wherein the organic solvent optionally immiscible with water is toluene claim 1 , 2-heptanone claim 1 , cyclohexanone claim 1 , cyclopentanone claim 1 , methyl isobutyl ketone claim 1 , propylene glycol monomethyl ether acetate or ethyl acetate.4. The method according to claim 1 , wherein the organic solvent optionally immiscible with water is methyl isobutyl ketone or ethyl acetate.5. The method according to claim 1 , wherein the solution (A) comprises the organic solvent optionally miscible with water in an amount of 0.1 to 100 times by mass based on an amount of the compound represented by the formula (1) or the resin having the structure represented by the formula (2).6. The method according to claim 5 , wherein the organic solvent optionally miscible with water is N-methylpyrrolidone or propylene glycol monomethyl ether.7. The method according to claim 1 , further comprising a step of performing an ...

SUBSTITUTED CHROMANES, ANALOGS THEREOF, AND METHODS OF USE AND SYNTHESIS

Disclosed are chromane compounds, analogs thereof, and methods of their synthesis and use. The compounds may be synthesized by methods involving reductive annulations of arylidene malonates with unsaturated electrophiles using photoredox/Lewis acid cooperative catalysis. The compounds may be formulated in a pharmaceutical composition for treating one of the aforementioned diseases or disorders. 2. The compound of claim 1 , wherein Rand/or Ris carboxyalkyl.3. The compound of claim 2 , wherein the carboxyalkyl is a branched or unbranched carboxy-C-alkyl.4. The compound of claim 2 , wherein the carboxyalkyl is carboxymethyl.5. The compound of claim 2 , wherein the carboxyalkyl is carboxyethyl.6. The compound of claim 2 , wherein the carboxyalkyl is carboxyisopropyl.7. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris bromo.8. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris fluoro.9. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris chloro.10. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris a branched or unbranched C-alkyl.11. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris methyl.12. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris tert-butyl.13. The compound of claim 1 , wherein Rand Rjoin together to form an aryl group.14. The compound of claim 1 , wherein Ror Ris hydrogen.15. The compound of claim 1 , wherein Ris hydrogen and Ris selected from the group consisting of phenyl claim 1 , branched or unbranched carboxy-C-alkyl claim 1 , cyano claim 1 , and carboxyalkylaryl (e.g. claim 1 , carboxybenzyl).18. The method of claim 17 , wherein the reagents further comprise a reducing agent. This application claims the benefit of priority to U.S. Provisional Application Ser. No. 62/871,673 filed on Jul. 8, 2019, the entire contents of which are incorporated by reference herein. ...

PHARMACEUTICAL COMPOSITION FOR THE TREATMENT AND PREVENTION OF CARDIAC DISEASE

Provided is a pharmaceutical composition for the treatment and prevention of cardiac diseases, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof. 2. The method according to claim 1 , wherein X is O.5. The method according to claim 1 , wherein each of Rand Ris respectively hydrogen.9. The method according to claim 1 , wherein the compound of Formula 1 or Formula 2 is contained in a crystalline structure.10. The method according to claim 1 , wherein the compound of Formula 1 is contained in an amorphous structure.11. The method according to claim 1 , wherein the compound of Formula 1 or Formula 2 is formulated into the form of a fine particle.12. The method according to claim 11 , wherein the formulation into the form of a fine particle is carried out by using a method selected from the group consisting of mechanical milling claim 11 , spray drying claim 11 , precipitation claim 11 , homogenization claim 11 , and supercritical micronization.13. The method according to claim 12 , wherein the formulation is carried out by using jet milling as a mechanical milling and/or spray drying.14. The method according to claim 11 , wherein the particle size of fine particles is 5 nm to 500 μm.15. The method according to claim 1 , wherein the pharmaceutical composition is prepared into an intestine-targeted formulation.16. The method according to claim 15 , wherein the intestine-targeted formulation is carried out by addition of a pH sensitive polymer.17. The method according to claim 15 , wherein the intestine-targeted formulation is carried out by addition of a biodegradable polymer which is decomposable by an intestine-specific bacterial enzyme.18. The method according to claim 15 , wherein the intestine-targeted formulation is carried out by addition of a ...

Photochromic compounds

A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N 3 , —CN, —COOR′, —CCR′, —C(R′)C(R′)R′, —OCOR′, —OCOOR′, —SR′, —OSO 2 R′″, and/or —CON(R′)R′, wherein each R′ is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R′″ is —CF 3 or a perfluorinated alkyl group having from 2 to 18 carbon atoms. The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound.

TREATMENT OF ANGIOGENIC- OR VASCULAR-ASSOCIATED DISEASES

Described herein are methods and compositions comprising a compound of formula (I), e.g., dehydro-alpha-lapachone, or an analog, derivative, isomer, prodrug, or pharmaceutically acceptable salt thereof, for treatment and/or prevention of angiogenic- or vascular-associated diseases or disorders. The compound has anti-vascular activity. In some embodiments, the compound has anti-vascular activity that targets pathways other than VEGF pathways. In some embodiments, the compound or the composition further comprises anti-tumor activity. In some embodiments, the compound or the composition can decrease adhesion or motility of at least one cell (e.g., endothelial cells or cancer cells). 278-. (canceled)79. The method of claim 1 , wherein the composition is administered in pulses.80. The method of claim 1 , wherein the composition is administered via sustained release.81. The method of claim 80 , wherein the composition comprises a delivery system adapted for sustained release of the compound of formula (I).82. The method of claim 81 , wherein the delivery system is selected from the group consisting of polymer-based systems claim 81 , lipid-based systems claim 81 , hydrogel release systems claim 81 , liposome-based systems claim 81 , phospholipid-based systems claim 81 , silastic systems claim 81 , peptide-based systems claim 81 , implants claim 81 , stents claim 81 , transdermal patches claim 81 , and any combinations thereof.83. The method of claim 1 , wherein the compound of formula (I) is conjugated to a macromolecule.84. The method of claim 1 , wherein the composition is administered to the subject over a period of at least about 2 months.85. The method of claim 1 , wherein the compound of formula (I) is dehydro-alpha-lapachone or an analog claim 1 , derivative claim 1 , isomer claim 1 , prodrug claim 1 , or pharmaceutically acceptable salt thereof.86Tabebuia Avellaneda. The method of claim 85 , wherein the compound of formula (I) is derived from tree.87. The method ...

Plant Matter Fractional Distillation System Using Heated Air Induction into Precisely Heated Chamber to Extract a Plant's Organic Compounds Without Use of Solvents

The present disclosure provides a system for extracting terpenes and cannabinoids from plant matter without use of volatile solvents and without use of lipids as solvents. The system uses heated air, drawn through plant matter for volatilizing desired compounds, where the air is at a predetermined temperature, followed by collecting the desired compounds in a condenser. 1. A system for extracting and purifying chemicals from plant matter , wherein the extracting uses a flow of heated air to volatilized chemicals from plant matter , and wherein the extracting does not use any added solvent to extract chemicals from the plant matter , and wherein the purifying comprises a condenser that condenses at least a portion of the volatilized chemicals , the system comprising:(a) A source of inert gas,(b) A heat chamber vessel that comprises an interior chamber region, an inside wall that defines the interior chamber region, an outside wall, a base, an upper region of the interior chamber region, wherein the upper region is capable of receiving and supporting a heat chamber vessel lid, and wherein the base of the heat chamber vessel is operably linked to a source of heated inert gas,(c) A conduit for transmitting the inert gas to the heat chamber vessel,(d) A screen that is capable of supporting plant matter and capable of allowing a flow of heated air directly against at least a portion of the supported plant matter,(e) A rotator arm that is operably linked with a stirring rod, wherein the rotator arm is capable of agitating any plant matter that is supported by the screen,(f) A distillation rube comprising a proximal terminus and a distal terminus, wherein the proximal terminus is capable of receiving a vapor arriving from heat chamber vessel, and wherein the distillation tube is capable of at least partially condensing the vapor to produce a fluid, wherein the proximal terminus of distillation tube is operably linked with the heat chamber vessel, and wherein the distal ...

Substituted Beta-Lapachones and Uses Therefor

Compounds, compositions and methods useful for treating cancer and neurodegeneration are provided. The compounds comprise a mitochondria-targeting moiety linked to β-lapachone or a β-lapachone derivative. 120-. (canceled)22. The compound of claim 21 , or a pharmaceutically acceptable salt thereof claim 21 , wherein Rand Rare claim 21 , independently claim 21 , amine protecting groups.23. The compound of claim 22 , or a pharmaceutically acceptable salt thereof claim 22 , wherein the amine protecting group is selected from the group consisting of: 9-fluorenylmethyloxy carbonyl (Fmoc) claim 22 , t-butyloxycarbonyl (Boc) claim 22 , benzhydryloxycarbonyl (Bhoc) claim 22 , benzyloxycarbonyl (Cbz) claim 22 , O-nitroveratryloxycarbonyl (Nvoc) claim 22 , benzyl (Bn) claim 22 , allyloxycarbonyl (alloc) claim 22 , trityl (Trt) claim 22 , 1-(4 claim 22 ,4-dimethyl-2 claim 22 ,6-dioxacyclohexylidene)ethyl (Dde) claim 22 , diathiasuccinoyl (Dts) claim 22 , benzothiazole-2-sulfonyl (Bts) claim 22 , dimethoxytrityl (DMT) and monomethoxytrityl (MMT).24. The compound of claim 21 , or a pharmaceutically acceptable salt thereof claim 21 , wherein the mitochondrial targeting group is covalently bonded to formula (I) at one of R3 or R4.25. The compound of claim 24 , wherein Ris Boc and Ris Cbz.26. The compound of claim 24 , wherein Ris H.29. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of claim 21 , or a pharmaceutically acceptable salt thereof.30. The pharmaceutical composition of claim 29 , wherein the pharmaceutical composition further comprises a chemotherapeutic agent.31. The pharmaceutical composition of claim 30 , wherein the chemotherapeutic agent is selected from the group consisting of abiraterone acetate claim 30 , altretamine claim 30 , amsacrine claim 30 , anhydro vinblastine claim 30 , auristatin claim 30 , bafetinib claim 30 , bexarotene claim 30 , bicalutamide claim 30 , 2 claim 30 ,3 claim 30 ,4 claim 30 ,5 claim 30 ,6- ...

POLYPHENOL ANALOGS TO TREAT ISCHEMIA

The present invention provides methods of use of polyphenol compounds for treating, preventing, mitigating and delaying ischemia or a condition where ischemia occurs. In one embodiment, the method comprises providing a polyphenol analog; and administering the polyphenol analog to a subject to treat ischemia or a condition where ischemia occurs. Various embodiments of the present invention are useful for the treatment of patients having, or at risk for, any of (1) ischemic stroke, (2) hemorrhagic stroke, (3) cardiovascular disease, (4) ischemia related spinal cord injury, (5) ischemia in diabetic patients, or (6) embolic stroke. For example, use of the polyphenol compounds can maintain glutathione levels in the patient. 3. The method of claim 2 , wherein:{'sup': 1', '2', 'a', '3', '4, 'sub': 1-6', '1-6', '3-8', '4-11', '6-10', '7-16, '(a) the compound is of Formula IIA, and wherein each of Rand R, independent of the other, is —OR; Ris H or optionally substituted Calkyl; and Ris Calkyl, Ccycloalkyl, Ccycloalkylalkyl, Caryl or Carylalkyl;'}{'sup': 1', '2', 'a', '3', 'a, 'sub': '1-6', '(b) the compound is of Formula IIIA, and wherein each of Rand R, independent of the other, is —OR; Ris H, Calkyl or —OR;'}{'sup': 1', '2', '1', '2', 'a', 'c', '3', '4, 'sub': 1-6', '2', '1-6', '1-6', '3-8', '4-11', '6-10', '7-16, '(c) the compound is of Formula IIA, and wherein one of Rand Ris optionally substituted Calkyl and the other of Rand Ris H, —ORor —N(R); Ris H or optionally substituted Calkyl; and Ris Calkyl, Ccycloalkyl, Ccycloalkylalkyl, Caryl or Carylalkyl;'}{'sup': 1', '2', '1', '2', 'a', 'c', '3', 'a, 'sub': 1-6', '2', '1-6, '(d) the compound is of Formula IIIA, and wherein one of Rand Ris optionally substituted Calkyl and the other of Rand Ris H, —ORor —N(R); and Ris H, Calkyl or —OR;'}{'sup': 1', '2', 'a', '1', '2', 'c', '1', '2', '3', '4, 'sub': 2', '1-6', '1-6', '3-8', '4-11', '6-10', '7-16, '(e) the compound is of Formula IIA, and wherein one of Rand Ris H or —ORand ...

DICHROIC-PHOTOCHROMIC 2H-NAPHTHO[1,2-b]PYRAN COMPOUNDS AND DEVICES

A naphthopyran compound represented by the formula B 1 and B 2 are selected independently from the group consisting of a phenyl, naphthyl, or heterocyclic aromatic group, or may combine to form one or more aromatic rings. B 1 and B 2 may further include one or more substituents. R 3 , R 4 , R 5 , R 6 , and R 16 are selected independently from the group consisting of hydrogen, halogen, —R a , —OH, —OR a , —O—CO—R a , —CN, —NO 2 , —SO 2 R a , —SOR a , —SH, —SR a , —NH 2 , —NHR a , —NR a R a , or —NR b R c ; or wherein R 5 and R 6 combine to form a cyclic group. R a may include an alkyl, polycycloalkyl, alkenyl, polyalkenyl, haloalkyl, perhaloalkyl, alkynyl, polyalkynyl, hydroxyalkynyl, polyhydroxyalkynyl; or (C 3-20 )cycloalkyl group. R b and R c may include hydrogen or alkyl groups, or may combine to form a saturated heterocyclic group, or together with an adjacent phenyl group may form a julolidinyl group. R 7 is a mesogenic group. And the naphthopyran, which may be referred to as a dichroic-photochromic compound, may be incorporated into an optical article.

HIGHLY EFFICIENT FREE RADICAL PHOTOPOLYMERIZATIONS THROUGH ENABLED DARK CURE

A quaternary ammonium salt comprising a chromophore constituent, a tertiary amine cation constituent connected to the para-position of the chromophore constituent via a methylene linkage, and a borate anion constituent, wherein chromophore constituent is a 3-ketocoumarin constituent or a benzophenone constituent. Also, a photobase-redox initiating system comprising the quaternary ammonium salt and a peroxide. 20. The quaternary ammonium salt of claim , wherein each alkoxy group is independently selected from the group consisting of methoxy and butoxy.30. The quaternary ammonium salt of claim , wherein Ris —H or alkoxy.40. The quaternary ammonium salt of claim , wherein Ris —H.50. The quaternary ammonium salt of claim , wherein:{'sub': 1', '8', '1', '8', '1', '6, 'the substituted -phenyl group has one or more independently selected substituents selected from the group consisting of linear or branched C-Calkyl group, linear or branched C-C-alkoxy group, -halogen, and halogenated C-C-alkyl group;'}{'sub': 1', '8', '1', '8', '1', '6, 'the substituted -napthyl group has one or more independently selected substituents selected from the group consisting of linear or branched C-Calkyl group, linear or branched C-C-alkoxy group, -halogen, and halogenated C-C-alkyl group; and'}{'sub': 2', '10, 'the unsubstituted vinyl group is Cand the substituted vinyl group is an extended vinylene up to C.'}60. The quaternary ammonium salt of claim , wherein at least one of the Rgroups is the substituted aromatic ring.70. The quaternary ammonium salt of claim , wherein the amine cation constituent is selected from the group consisting of N-methyl morpholine , N-methyl pyrrolidine , N ,N-dimethyl aniline , N ,N ,4-trimethyl aniline , N-N-dimethyl-4-methoxyaniline , N ,N-pyrrolidine-4-methoxyaniline , and N ,N-ethoxy-4-methylaniline.80. The quaternary ammonium salt of claim , wherein the borate anion constituent is selected from the group consisting of tetraphenyl , tetra-4-methyl-phenyl , ...

Organic electroluminescent element and electronic device using same

An organic electroluminescence device comprising: a cathode, an anode, and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises a compound represented by the following formula (1), and a compound A having a Stokes shift of 20 nm or smaller and an emission peak wavelength of 440 nm to 465 nm (at least one of Ar1 and Ar2 is a monovalent group having a structure represented by the following formula (2)).

HETEROCYCLYL POLYMETHINE IR CHROMOPHORES

The present disclosure provides SWIR-active small molecule polymethine dyes with improved properties for use in optical imaging, photothermal therapy, photodynamic therapy, and SWIR-promoted drug delivery. 3. The compound of or , wherein Rand Rare independently selected from H or alkyl.4. The compound of or , wherein Rand Rtogether complete a cycloalkenyl ring.6. The compound of claim any one of the preceding claims , wherein A and B are the same.7. The compound of any one of the preceding claims , wherein A and B are different.8. The compound of any one of the preceding claims , wherein:{'sup': '7', 'A is optionally substituted by one or more substituents independently selected from R;'}{'sup': '7', 'B is optionally substituted by one or more substituents independently selected from R;'}{'sup': 6', '6, 'each instance of Ris independently selected from H, alkyl, such as fluoroalkyl or sulfonatoalkyl, acyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; or two instances of Rconnected to the same N may complete a heterocyclyl; and'}{'sup': 7', '6', '6, 'each instance of Ris independently selected from alkyl (such as haloalkyl, fluoroalkyl or sulfonatoalkyl), alkoxy (such as haloalkyloxy, fluoroalkyloxy or sulfonatoalkyloxy), acyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, N(R)R, sulfonate, carbonate, cyano, ester, amide, or halo.'}9. The compound of any one of the preceding claims , wherein:{'sup': '7', 'A is optionally substituted by one or more substituents independently selected from R;'}{'sup': '7', 'B is optionally substituted by one or more substituents independently selected from R;'}{'sup': 6', '6, 'each instance of Ris independently selected from H, alkyl, such as fluoroalkyl or sulfonatoalkyl, acyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; or two instances of Rconnected to the same N may complete a heterocyclyl; and'}{'sup': 7', '6', '6, 'each instance of Ris independently selected from alkyl, such as fluoroalkyl or sulfonatoalkyl, acyl, cycloalkyl, ...

Fused quinonic compounds

A compound having the formula (I): for use in treating a disease; a composition comprising said fused quinonic compound of formula (I) and at least one pharmaceutically acceptable carrier; as well as a method of modulating a Janus Kinase-Signal Transduction and Activators of Transcription (JAK-STAT) pathway. The activation of a JAK and/or STAT pathways are associated with several disease states such as immunological and inflammatory diseases, hyperproliferative disorders including cancer, and myeloproliferative diseases.

Novel block copolymer and micelle compositions and methods of use thereof

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises wherein R′ is —H or —CH 3 , wherein R is —NR 1 R 2 , wherein R 1 and R 2 are alkyl groups, wherein R 1 and R 2 are the same or different, wherein R 1 and R 2 together have from 5 to 16 carbons, wherein R 1 and R 2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

Mitochondria-Targeted Lapachone Compounds and Uses Therefor

Compounds, compositions and methods useful for treating cancer and neiirodegeneration are provided. The compounds comprise a mitochondria-targeting moiety linked to β-lapachone or a β-lapachone derivative. 1. A compound comprising a mitochondria-targeting group covalently linked to β-lapachone or a β-lapachone derivative , or a pharmaceutically-acceptable salt or ester thereof.2. The compound of claim 1 , comprising a β-lapachone derivative.4. The compound of claim 3 , wherein the β-lapachone or the β-lapachone derivative is linked to the mitochondria-targeting group at position Cor C.5. The compound of claim 4 , wherein the β-lapachone or the β-lapachone derivative is linked to a mitochondria-targeting group at position C.7. The compound of claim 6 , having the structure of (III) or (IV).8. The compound of claim 6 , having the structure of (V) or (VI).9. The compound of claim 6 , having the structure of (VII).12. A composition comprising a first compound comprising a mitochondria-targeting group covalently linked to β-lapachone or a β-lapachone derivative claim 6 , or a pharmaceutically-acceptable salt or ester thereof claim 6 , and a pharmaceutically-acceptable excipient.13. The composition of claim 12 , further comprising a chemotherapeutic agent that is different from the first compound.14. The composition of claim 13 , wherein the chemotherapeutic agent is either β-lapachone claim 13 , a β-lapachone derivative claim 13 , abiraterone acetate claim 13 , altretamine claim 13 , amsacrine claim 13 , anhydro vinblastine claim 13 , auristatin claim 13 , bafetinib claim 13 , bexarotene claim 13 , bicalutamide claim 13 , BMS 184476 claim 13 , 2 claim 13 ,3 claim 13 ,4 claim 13 ,5 claim 13 ,6-pentafluoro-N-(3-fluoro-4-methoxyphenyl)benzene sulfonamide claim 13 , bleomycin claim 13 , bosutinib claim 13 , busulfan claim 13 , cachectin claim 13 , cemadotin claim 13 , chlorambucil claim 13 , cyclophosphamide claim 13 , 3′ claim 13 ,4′-didehydro-4′-deoxy-8′-norvin- ...

COMPOUND FOR FORMING ORGANIC FILM, COMPOSITION FOR FORMING ORGANIC FILM, METHOD FOR FORMING ORGANIC FILM, AND PATTERNING PROCESS

A compound for forming an organic film shown by the formula (1A), 2. The compound for forming an organic film according to claim 1 , wherein the R is an organic group containing one or more quaternary carbon atoms each bonded to four aromatic rings claim 1 , and one or more of the four aromatic rings bonded to the quaternary carbon atom are the X.3. The compound for forming an organic film according to claim 2 , wherein the aromatic rings bonded to the quaternary carbon atom are benzene rings or naphthalene rings claim 2 , or a combination thereof.4. The compound for forming an organic film according to claim 2 , wherein two aromatic rings of the four aromatic rings bonded to the quaternary carbon atom are bonded to each other to form a cyclic structure.5. The compound for forming an organic film according to claim 1 , wherein the compound satisfies 1.00Mw/Mn1.25 where Mw is a weight average molecular weight and Mn is a number average molecular weight measured by gel permeation chromatography in terms of polystyrene.6. The compound for forming an organic film according to claim 1 , wherein the compound has a molecular weight of 2 claim 1 ,500 or less claim 1 , the molecular weight being calculated on the basis of the formula (1A).7. A composition for forming an organic film claim 1 , comprising the compound according to and an organic solvent.9. The composition for forming an organic film according to claim 7 , wherein the organic solvent is a mixture of one or more organic solvents having a boiling point of lower than 180° C. and one or more organic solvents having a boiling point of 180° C. or higher.10. A method for forming an organic film that functions as an organic planarizing film used in a semiconductor apparatus manufacturing process claim 7 , the method comprising:{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'applying the composition for forming an organic film according to on a substrate to be processed by spin coating; and heating the substrate, on ...

NOVEL PI-EXTENDED ACEDAN DERIVATIVES, THEIR APPLICATION FOR TWO-PHOTON MICROSCOPY IMAGING, AND THEIR APPLICATION FOR TWO-PHOTON MICROSCOPY IMAGING OF AMYLOID-BETA PLAQUE IN AN ALZHEIMER'S DISEASE ANIMAL MODEL

Provided are acedan derivatives having an extended π bond, a method for preparing the acedan derivatives, and a method for two-photon microscopy imaging of amyloid-beta plaque using the acedan derivatives; more particularly, to two-photon absorbing fluorescent compounds having a longer absorption wavelength and emission wavelength than acedan and acedan derivatives which are conventional two-photon absorbing fluorophores. The compounds provided may be usefully used for in vivo imaging studies by imaging cells or tissue using the compounds, and may also be usefully used for diagnosing Alzheimer's disease by imaging amyloid-beta plaque using the compounds. 3. The acedan derivative according to claim 1 , wherein the acedan derivative is a two-photon absorbing fluorophore.4. A cell or tissue imaging method using the acedan derivative according to .5. The method according to claim 4 , wherein the imaging method is a method for imaging amyloid-beta plaque in a tissue.6. The method according to claim 4 , wherein the imaging method comprises:treating a cell or tissue with the acedan derivative; andobserving the cell or tissue using a fluorescent microscope.7. The method according to claim 6 , wherein the fluorescent microscope is a one-photon fluorescence microscope or a two-photon fluorescence microscope.8. A method for diagnosing Alzheimer's disease claim 6 ,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'comprising administering the acedan derivative according to to a subject in need thereof.'}9. A method of preparing an acedan derivative represented by the Formula 4 claim 2 , according to claim 2 , from 6-(dimethylamino)-3-hydroxy-2-naphthaldehyde claim 2 , comprising synthesizing 8-(dimethylamino)-2 claim 2 ,3 claim 2 ,4a-tetrahydro-1H-benzo[b]xanthene-1-one by adding 2-cyclohexene-1-one and 1 claim 2 ,4-diazabicyclo[2.2.2]octane to 6-(dimethylamino)-3-hydroxy-2-naphthaldehyde.10. A method of preparing an acedan derivative represented by the Formula 5 claim 2 , ...

Photochromic Compounds

Described are novel photochromic naphthopyran compounds which exhibit a red coloring when in a red-colored state achieved upon exposure to ultraviolet light, whereby the red coloring has a lambda max in a range of between about 490 nanometers to about 510 nanometers or between about 490 nanometers to about 500 nanometers. 1. A photochromic formulation comprising:a naphthopyran compound which exhibits a red coloring when in a red-colored state achieved upon exposure to ultraviolet light, wherein said red coloring has a lambda max in a range of between about 490 nanometers to about 510 nanometers.2. The photochromic formulation of claim 1 , wherein said red coloring has a lambda max in a range of between about 490 nanometers to about 500 nanometers.5. The photochromic formulation of claim 1 , wherein said naphthopyran compound is selected from the group consisting of formulas II claim 1 , IV claim 1 , V claim 1 , VI claim 1 , VII claim 1 , VIII claim 1 , IX claim 1 , X claim 1 , XI claim 1 , XII claim 1 , XIII claim 1 , XIV claim 1 , XV claim 1 , XVI claim 1 , XVII claim 1 , XVIII claim 1 , XIX claim 1 , XX claim 1 , XXI claim 1 , XXII claim 1 , and XXIII.6. The photochromic formulation of claim 3 , wherein said carbonyl group comprises a carboxyl group having a carboxyl group carbon which is:singly bonded to a first oxygen;doubly bonded to a second oxygen; andsingly bonded directly to a corresponding ring.7. The photochromic formulation of claim 1 , wherein said naphthopyran compound is selected from the group consisting of formulas II claim 1 , IV claim 1 , VI claim 1 , VII claim 1 , VIII claim 1 , XI claim 1 , XII claim 1 , XIII claim 1 , XVII claim 1 , XVIII claim 1 , XIX claim 1 , XX claim 1 , XXI claim 1 , XXII claim 1 , and XXIII.8. The photochromic formulation of claim 3 , wherein said carbonyl group comprises a carboxyl group having a carboxyl group carbon which is:singly bonded to a first oxygen; anddoubly bonded to a second oxygen;wherein said first oxygen ...

Carbon Monoxide Releasing Molecules and Associated Methods

The present disclosure relates to carbon monoxide releasing molecules (“CORMs”), and methods of synthesizing and applying the molecules. More specifically, this disclosure relates to structurally tunable CORMS, compounds containing CORMS (and salts thereof). An exemplary compound includes: 2. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rare the same.13. A composition claim 1 , comprising the compound of .14. The composition of claim 13 , further comprising a pharmaceutically acceptable carrier. This application claims priority to U.S. Provisional Application No. 62/107,967, flied Jan. 26, 2015, the entirety of which is hereby incorporated by reference. This application is related to S. A. Anderson, J. M. Richards, H. J. Esquer, A. D. Benninghoff, A. M. Arif, L. M. Berreau, A Structurally-Tunable 3-Hydroxyflavone Motif for Visible Light-Induced Carbon Monoxide-Releasing Molecules (CORMs), 4 ChemistryOpen 590-594 (2015), the entirety of which is incorporated by reference in its entirety.This invention was made with government support under Contract No. CHE-1301092 awarded by the National Science Foundation. The government has certain rights in the invention.The present disclosure relates to carbon monoxide releasing molecules (“CORMs”), and methods of synthesizing and applying the molecules. More specifically, this disclosure relates to structurally tunable CORMs.The present disclosure provides structurally tunable CORMs, including, for example, the CORMs set forth below in Formula I.Y═O, NH, or S;X═O or S;R, R, R, R, R, R, Rmay each be selected from the group consisting of —H; —COOH; —CSOH; —COOR′; —CONH; —CONHR′; CON(R′); —COR′; —F; —Cl; —Br; —I; —CN; —NO; —OH; —OR′; —SH; —SR′; —O—CO—R′; —NH; —NHR′; —NR′; —NH(R′); —NH—CO—R′; —NR′—CO—R′; —SOR′; —OSOR′; —Caryl optionally substituted with —COOH; —CSOH; —COOR′; —CONH; —CONHR′; CON(R′); —COR′; —F; —Cl; —Br; —I; —CN; —NO; —OH; —OR′; —SH; —SR′; —O—CO ...

Double donor functionalisation of the peri-positions of perylene and naphthalene monoimide via versatile building blocks

The present invention provides the compounds of formulae (3) and (1) wherein n is 0 or 1, R 13 and R 14 are the same or different and are selected from the group consisting of NHR 310 , NR 311 R 312 , OR 313 , SR 314 and R 315 , or R 13 and R 14 together are selected from the group consisting of (a), (b) and (c), and X is CI, Br of I, and a process for the preparation of compounds of formula (3) comprising the compounds of formula (1) as key intermediates.

Method for the preparation of Intermediates for carboxy-fluoresceins and novel carboxy-fluorescein

The invention provides a method for the preparation of regioisomerically pure intermediates which are useful for the preparation of carboxy-fluorescein-type compounds. Such compounds have broad applications within bio-conjugation and/or fluorescent imaging. 3. The method according to any one of - , wherein hydrolysis steps (step ii.) are carried out at a pH of 12-14 , preferably using a 1:1 weight ratio mixture of NaOH and HO.4. The method according to any one of or , wherein the acidification steps (step iii) are carried out using 12 M HCl.5. The method according to any one of or , wherein , in step vi , steps (iv) and (v) are repeated in 2-3 additional cycles.8. The method according to any one of - , wherein Rand/or Ris independently hydroxyl.9. The method according to any one of or , wherein Ris halogen , preferably F or Cl.10. The method according to any one of or , wherein Ris —O—C-alkyl , such as —OCHor —OCH , or —C-alkyl substituted by —COOH , such as —C-alkyl substituted by —COOH.11. The method according to any one of or , wherein A is a dihydroxynaphthalene , preferably 1 ,3-dihydroxynaphthalene , 2 ,3-dihydroxynaphthalene , 2 ,6-dihydroxynaphthalene , 1 ,4-dihydroxynaphthalene , 1 ,5-dihydroxynaphthalene , 1 ,6-dihydroxynaphthalene , 1 ,8-dihydroxynaphthalene , 1 ,2-dihydroxynaphthalene , 2 ,7-dihydroxynaphthalene or 1 ,7-dihydroxynaphthalene. The present invention relates to a novel method for the preparation of regioisomerically pure intermediates which are useful for the preparation of carboxy-fluorescein-type compounds. Such compounds have broad applications within bio-conjugation and/or fluorescent imaging.5(6)-Carboxy-fluorescein is a well-known chromophore and mixtures of the two regioisomers can with great effort be separated into the pure regioisomers 5- and 6-carboxyfluorescein by HPLC. Burgess and co-workers [Y. Ueno, G.-S. Jiao, K. Burgess, (). 2004, 2591-2593] have reported a procedure using fractional crystallization in multi-gram amounts ...

CHEMICALLY ACTIVATED WATER-SOLUBLE PRODRUG

The present invention addresses the problem of providing a novel chemically activated water-soluble prodrug. The present invention provides a compound represented by formula (1), or a pharmacologically acceptable salt thereof (in the formula, A represents A-0; Xand Xare the same as or different from each other and each independently represent a hydroxyl group or —O—C(═O)—Y—(C(R) (R))n-NH—R, where Xand Xare not simultaneously hydroxyl groups, n is 2, 3, or 4, Y represents an oxygen atom or —NR, Rand Rare the same as or different from each other and each independently represent a hydrogen atom, etc., and Rrepresents a hydrogen atom, etc.; and Rto Rare optionally present, are the same as or different from each other, and each independently represent a hydrogen atom, etc.). 4. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sup': 3A', '3B', '3C', '3D', '3E', '3F', '3G', '3H, 'sub': 1-30', '3-10', '2-30', '1-20', '1-20', '6-10', '1-20, 'R, R, R, R, R, R, R, and Rare null, or the same or different, each independently a hydrogen atom, a hydroxyl group, an optionally substituted amino group, an optionally substituted 3- to 12-membered cyclic amino group, an optionally substituted Calkyl group, an optionally substituted Ccycloalkyl group, an optionally substituted Calkenyl group, an optionally substituted Calkoxy group, an optionally substituted Calkylcarbonyloxy group, an optionally substituted 3- to 12-membered monocyclic or polycyclic heterocyclic group, an optionally substituted Caryl group, an optionally substituted Calkylcarbonyl group, or a carboxyl group, or'}{'sup': 3A', '3B', '3B', '3C', '3C', '3D', '3D', '3E', '3E', '3F', '3F', '3G', '3G', '3H, 'sub': 3-10', '3-10, 'Rand R, Rand R, Rand R, Rand R, Rand R, Rand R, or Rand R, when adjacent to each other on an aromatic ring, together with 2 carbon atoms on the aromatic ring to which they are attached, may form an optionally substituted Ccycloalkane or an optionally ...

Photochromic annelated naphthopyrane systems with special substituents, for attaining rapid lightening speeds

The present invention relates to new photochromic, fused naphthopyran systems having specific substituents R1, which can be used to attain very rapid lightening speeds, without detriment to the depth of darkening after excitation, and also to the use thereof in plastics of all kinds.

METHOD FOR BIOCATALYTICALLY CYCLIZING GERANYLLINALOOL AND CYCLIZATION PRODUCTS THEREBY OBTAINED

The present invention relates to a novel process for cyclizing geranyllinalool using the squalene-hopene cyclase from (Zm-SHC) or a cyclase with at least 80% sequence identity to the Zm-SHC, and cyclization products obtained in this process. 2. The process according to claim 1 , wherein the cyclase is present in crude claim 1 , purified claim 1 , dissolved claim 1 , dispersed or immobilized form claim 1 , or in the presence of cyclase-displaying cells of a microorganism.3. The process according to in the presence of a recombinant microorganism which includes a nucleotide sequence which codes for the cyclase.4. The process according to claim 3 , wherein the nucleotide sequence is part of an expression cassette and claim 3 , therein claim 3 , is under the control of at least one regulatory sequence.5. The process according to claim 4 , wherein the expression cassette is part of an expression vector.6. The process according to claim 5 , wherein the expression vector is selected from among plasmids.7. The process according to claim 2 , wherein the microorganism is selected from among bacteria claim 2 , fungi and yeasts.8E. coli.. The process according to claim 7 , wherein the microorganism is9. The process according to in the presence of a recombinant microorganism which includes a nucleotide sequence which codes for the cyclase.10. The process according to claim 9 , wherein the nucleotide sequence is part of an expression cassette and claim 9 , therein claim 9 , is under the control of at least one regulatory sequence.11. The process according to claim 10 , wherein the expression cassette is part of an expression vector.12. The process according to claim 11 , wherein the expression vector is selected from among plasmids.13. The process according to claim 9 , wherein the microorganism is selected from among bacteria claim 9 , fungi and yeasts.14E. coli.. The process according to claim 13 , wherein the microorganism is15. The process according to claim 3 , wherein the ...

METHOD AND APPARATUS FOR PROCESSING HERBACEOUS PLANT MATERIALS INCLUDING THE CANNABIS PLANT

A method and associated system of treating a plant material consisting essentially of the plant cannabis in order to extract cannabinoids in liquid form from the plant material. The method includes heating the plant material; drying the plant material; grinding the dried plant material into a powder form; marinating the dried plant powder in a solvent for a predetermined time period to form a marinated mixture; shaking and heating the marinated mixture; filtering the mixture so that only a liquid part of the mixture remains; and evaporating from the liquid the solvent in order to provide the cannabinoid liquid extract. 1. A method of treating a plant material consisting essentially of the plant cannabis in order to extract cannabinoids in liquid form from the plant material , said method comprising the steps of:heating the plant material to cause decarboxylation;drying the plant material;grinding the dried plant material into a powder form;providing an alcohol solvent;marinating the dried plant powder in the solvent for a predetermined time period to form a marinated mixture;shaking and heating the marinated mixture;filtering the mixture so that only a liquid part of the mixture remains; andevaporating from the liquid the solvent in order to provide the cannabinoid extract.2. The method of including claim 1 , prior to the heating step claim 1 , harvesting the plant material.3. The method of including claim 1 , prior to the heating step claim 1 , freezing the plant material.4. The method of including freezing the plant material for up to 24 hours.5. The method of wherein the freezing step is at a temperature range of 15-30° F.6. The method of wherein the heating step is for 20-30 minutes.7. The method of wherein the heating step is in a temperature range of 120 to 500° F.8. The method of wherein the heating step is in a temperature range of 180 to 200° F.9. The method of wherein solvent is 190 to 200 proof ethyl alcohol.10. The method of wherein solvent is 99% ...

HETEROCYCLYL POLYMETHINE IR CHROMOPHORES

The present disclosure provides NIR- and SWIR-active small molecule polymethine dyes with improved properties for use in optical imaging, photothermal therapy, and photodynamic therapy. 2. (canceled)3. The compound of claim 1 , wherein Ris F claim 1 , D claim 1 , or T.4. (canceled)5. (canceled)6. The compound of claim 1 , wherein Ris F claim 1 , D claim 1 , or T.7. (canceled)8. (canceled)1012-. (canceled)13. The compound of claim 9 , wherein Rand Rtogether complete a cycloalkenyl ring.14. (canceled)15. The compound of claim 1 , wherein:{'sup': 7a', '7b, 'A is substituted by one or more substituents independently selected from Rand R;'}{'sup': 7a', '7b, 'B is substituted by one or more substituents independently selected from Rand R;'}{'sup': 7a', '7b', '6', '6, 'Each instance of Rand Ris independently selected from alkyl, alkoxy, acyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, N(R)R, sulfonate, carbonate, cyano, ester, amide, and halo; and'}{'sup': 6', '6, 'each instance of Ris independently selected from H, alkyl, hydroxyl, alkyloxy, aryloxy, acyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl; or two instances of Rconnected to the same N complete a heterocyclyl.'}16. (canceled)17. (canceled)18. The compound of claim 1 , wherein at least one Ror Ris a water-solubilizing group or an electron-withdrawing group.1927-. (canceled)30. (canceled)3235-. (canceled)36. The compound of claim 29 , wherein at least one Ror Ris alkyloxy claim 29 , aryl claim 29 , trifluoromethyl claim 29 , tert-butyl claim 29 , H claim 29 , aralkenyl claim 29 , aralkynyl claim 29 , cycloalkyl claim 29 , or heterocyclyl.3742-. (canceled)4447-. (canceled)48. The compound of claim 1 , wherein each Ris alkyl; or two instances of Rconnected to the same N complete a heterocyclyl or a heteroaryl.49. (canceled)50. The compound of claim 1 , wherein X is Cl.5154-. (canceled)56. The compound of claim 1 , wherein at least one of A and B is substituted with sulfate claim 1 , sulfonate claim 1 , ...

Photochromic Compounds

A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N, —CN, —COOR′, —CCR′, —C(R′)C(R′)R′, —OCOR′, —OCOOR′, —SR′, —OSOR′″, and/or —CON(R′)R′, wherein each R′ is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R″′ is —CFor a perfluorinated alkyl group having from 2 to 18 carbon atoms The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound. 2. (canceled)3. A photochromic composition comprising the photochromic material of incorporated into at least a portion of an organic material claim 1 , said organic material being a polymeric material claim 1 , an oligomeric material claim 1 , a monomeric material or a mixture or combination thereof.4. The photochromic composition of claim 3 , wherein said polymeric material comprises self-assembling materials claim 3 , polycarbonate claim 3 , polyamide claim 3 , polyimide claim 3 , poly(meth)acrylate claim 3 , polycyclic alkene claim 3 , polyurethane claim 3 , poly(urea)urethane claim 3 , polythiourethane claim 3 , polythio(urea)urethane claim 3 , polyol(allyl carbonate) claim 3 , cellulose acetate claim 3 , cellulose diacetate claim 3 , cellulose triacetate claim 3 , cellulose acetate propionate claim 3 , cellulose acetate butyrate claim 3 , polyalkene claim 3 , polyalkylene-vinyl acetate claim 3 , poly(vinylacetate) claim 3 , poly(vinyl alcohol) claim 3 , poly(vinyl chloride) claim 3 , poly(vinylformal) claim 3 , poly(vinylacetal) claim 3 , poly(vinylidene chloride) claim 3 , poly(ethylene terephthalate) claim 3 , polyester claim 3 , polysulfone claim 3 , polyolefin claim 3 , copolymers thereof claim 3 , and/or ...

Photochromic Compounds

A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N, —CN, —COOR′, —CCR′, —C(R′)C(R′)R′, —OCOR′, —OCOOR′, —SR′, —OSOR′″, and/or CON(R′)R′, wherein each R′ is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R′″ is —CFor a perfluorinated alkyl group having from 2 to 18 carbon atoms The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound. 115-. (canceled)18. (canceled) This application is a divisional of U.S. patent application Ser. No. 13/452,030, filed Apr. 20, 2012, which is a divisional of U.S. patent application Ser. No. 12/329,092 filed Dec. 5, 2008, which is a continuation-in-part of U.S. patent application Ser. No. 10/846,629, filed May 17, 2004, which claims the benefit of U.S. Provisional Application No. 60/484,100, filed Jul. 1, 2003, all of which are hereby specifically incorporated by reference.Not applicable.Not applicable.Various non-limiting embodiments disclosed herein relate generally to photochromic compounds. Other non-limiting embodiments relate to devices and elements made using the photochromic compounds disclosed herein.Conventional photochromic compounds have at least two states, a first state having a first absorption spectrum and a second state having a second absorption spectrum that differs from the first absorption spectrum, and are capable of switching between the two states in response to at least actinic radiation. Further, conventional photochromic compounds can be thermally reversible. That is, conventional photochromic compounds are capable of switching between a first state and a second state in response to at least ...

Photochromic Compounds

A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N, —CN, —COOR′, —CCR′, —C(R′)C(R′)R′, —OCOR′, —OCOOR′, —SR′, —OSOR″′, and/or —CON(R′)R′, wherein each R′ is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R″′ is —CFor a perfluorinated alkyl group having from 2 to 18 carbon atoms The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound. 115-. (canceled)17. The naphthol of wherein claim 16 , substituent Q comprises —CN claim 16 , —COOR′ claim 16 , —CCR′ claim 16 , —C(R′)C(R′)R′ claim 16 , —OCOR′ claim 16 , —OCOOR′ claim 16 , —SR′ claim 16 , —OSOR″′ claim 16 , or —CON(R′)R′ claim 16 , and wherein each R′ independently comprises an alkyl group having from 1 to 12 carbon atoms and R″′ comprises —CFor a perfluorinated alkyl group having from 2 to 12 carbon atoms.18. (canceled) This application is a divisional of U.S. patent application Ser. No. 13/452,030, filed Apr. 20, 2012, which is a divisional of U.S. patent application Ser. No. 12/329,092 filed Dec. 5, 2008, which is a continuation-in-part of U.S. patent application Ser. No. 10/846,629, filed May 17, 2004, which claims the benefit of U.S. Provisional Application No. 60/484,100, filed Jul. 1, 2003, all of which are hereby specifically incorporated by reference.Not applicable.Not applicable.Various non-limiting embodiments disclosed herein relate generally to photochromic compounds. Other non-limiting embodiments relate to devices and elements made using the photochromic compounds disclosed herein.Conventional photochromic compounds have at least two states, a first state having a first absorption ...

NOVEL BLOCK COPOLYMER AND MICELLE COMPOSITIONS AND METHODS OF USE THEREOF

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises 2. The block copolymer of claim 1 , wherein the hydrophilic polymer segment comprises PEO.3. The block copolymer of any one of - claim 1 , wherein n is 1 to 4.4. The block copolymer of any one of - claim 1 , wherein n is 2.5. The block copolymer of any one of - claim 1 , wherein R′ is —CH.6. The block copolymer of any one of - claim 1 , wherein R′ is —H.7. The block copolymer of any one of - claim 1 , wherein x is about 40 to about 100 in total.8. The block copolymer of any one of - claim 1 , wherein x is about 50 to about 100 in total.9. The block copolymer of any one of - claim 1 , wherein x is about 40 to about 70 in total.10. The block copolymer of any one of - claim 1 , wherein x is about 60 to about 80 in total.11. The block copolymer of any one of - claim 1 , wherein x is about 70 in total.12. The block copolymer of any one of - claim 1 , wherein Rand Rare each straight or branched alkyl.13. The block copolymer of any one of - claim 1 , wherein Rand Rjoin to form a ring.14. The block copolymer of any one of - claim 1 , wherein Rand Rare the same.15. The block copolymer of any one of - claim 1 , wherein Rand Rare different.16. The block copolymer of any one of - claim 1 , wherein Rand Reach have 3 to 8 carbons.17. The block copolymer of claim 13 , wherein Rand Rtogether form a ring having 5 to 10 carbons.18. The block copolymer of any one of - claim 13 , wherein Rand Rare propyl.19. The block copolymer of claim 18 , wherein propyl is iso-propyl.20. The block copolymer of any one of - claim 18 , wherein Rand Rare butyl.21. The block copolymer of claim 20 , wherein butyl is n-butyl.22. The block ...

STEREO-SPECIFIC SYNTHESIS OF (13R)-MANOYL OXIDE

The present invention relates to a method for manufacturing enantiomerically pure (13R)-manoyl oxide, said method comprising the steps of contacting geranylgeranyl diphosphate (GGPP) with a class II diterpene synthase to obtain labd-13-en-8,15-diol diphosphate (LPP), and then contacting the LPP with a class I diterpene synthase to obtain (13R)-manoyl oxide. The invention further relates to (13R)-manoyl oxide obtained by the method of the invention. 1. A method of manufacturing (13R)-manoyl oxide , said method comprising the steps of:(i) providing geranylgeranyl diphosphate (GGPP);(ii) contacting GGPP of step (i) with a first polypeptide having a sequence at least 75% identical to SEQ ID NO: 1 [CfTPS2] or SEQ ID NO: 2 [SsLPPS], thus obtaining labd-13-en-8,15-diol diphosphate (LPP); 'thus obtaining (13R)-manoyl-oxide.', '(iii) contacting the LPP of step (ii) with a second polypeptide having a sequence at least 75% identical to SEQ ID NO: 3 [CfTPS4], SEQ ID NO: 4 [CfTPS3] or SEQ ID NO: 5 [EpTPS8];'}2. The method according to any one of the preceding claims , wherein the (13R)-manoyl oxide obtained is enantiomerically pure.3. The method according to any one of the preceding claims , wherein the first polypeptide and the second polypeptide are present at a stoichiometry ratio between 2:1 and 1:2 , such as 1:1.4. The method according to any one of the preceding claims , further comprising a step of recovering the (13R)-manoyl oxide.5. The method according to any one of the preceding claims , where the method is performed in vivo.6. The method according to the preceding claims , wherein the first and second polypeptides are heterologously expressed in a host organism selected from the group comprising bacteria , yeast , fungi , plants , insects and mammals.7Escherichia coli, Saccharomyces cerevisiae, Schizosaccharomyces pombe, Nicotiana benthamianaPhyscomitrella patens.. The method according to any one of the preceding claims , wherein the host organism is selected from ...

SIX-MEMBERED RING BENZO DERIVATIVES AS DPP-4 INHIBITOR AND USE THEREOF

The present invention relates to six-membered ring benzo derivatives as a DPP-4 inhibitor and a use thereof. In particular, the present invention relates to a compound as shown in formula I, a pharmaceutical composition containing the compound as shown in formula I and a use of the compound in the preparation of drugs for treating DPP-4 related diseases or inhibiting DPP-4. 9. A pharmaceutical composition comprising a compound of any one of - or a pharmaceutically acceptable salt or prodrug thereof , and a pharmaceutically acceptable carrier or excipient.10. The pharmaceutical composition of claim 9 , wherein the pharmaceutical composition is in a dosage form suitable for oral administration claim 9 , including but not limited to a tablet claim 9 , a solution claim 9 , a suspension claim 9 , a capsules claim 9 , a granule claim 9 , a powder.11. Use of a compound of any one of - or a pharmaceutically acceptable salt thereof claim 9 , wherein said compound or a pharmaceutically acceptable salt thereof is used for preparing a medicament for inhibiting DPP-4 claim 9 , a medicament for treating to preventing dipeptidyl peptidase-4 (DPP-4)-related diseases claim 9 , or used as a diuretic or for preparing a medicament for treating and preventing inflammation.12. Use of claim 11 , wherein the dipeptidyl peptidase-4 (DPP-4)-related diseases are diabetes claim 11 , impaired glucose tolerance claim 11 , intestinal disease claim 11 , ulcerative colitis claim 11 , Crohn's disease claim 11 , obesity or metabolic syndrome.13. Use of claim 12 , wherein the diabetes is non-insulin dependent type 2 diabetes. The present invention relates to the field of pharmaceutical chemistry. In particular, the present invention relates to novel benzo six-membered ring derivatives, to synthesis methods thereof and uses in the preparation of a medicament for treating type 2 diabetes and related diseases.Diabetes mellitus (DM) is a metabolic disease characterized in that the level of glucose (blood ...

Methods and Materials for Biosynthesis of Manoyl Oxide

The invention relates to recombinant microorganisms and methods for producing manoyl oxide. 1. A recombinant host comprising:(a) a gene encoding a geranylgeranyl diphosphate synthase (GGPPS) polypeptide;(b) a gene encoding a polypeptide capable of catalyzing formation of copal-8-ol diphosphate from geranylgeranyl diphosphate (GGPP); and(c) a gene encoding a polypeptide capable of catalyzing formation of manoyl oxide from copal-8-ol diphosphate;wherein at least one of the genes is a heterologous gene; andwherein the recombinant host is capable of producing manoyl oxide.2. The recombinant host of claim 1 , wherein the GGPPS polypeptide comprises a GGPPS7 polypeptide having at least 70% identity to the amino acid sequence set forth in SEQ ID NO:2 or a GGPPS10 polypeptide having at least 70% identity to the amino acid sequence set forth in SEQ ID NO:2.3. The recombinant host of claim 1 , wherein the enzyme capable of catalyzing formation of copal-8-ol diphosphate from GGPP is a terpene synthase 2 (TPS2) polypeptide.4. The recombinant host of claim 1 , wherein the enzyme capable of catalyzing formation of manoyl oxide from copal-8-ol diphosphate is a terpene synthase 3 (TPS3) polypeptide or a terpene synthase 4 (TPS4) polypeptide.5. The recombinant host of claim 4 , wherein the TPS3 polypeptide comprises a TPS3 polypeptide having at least 70% identity to an amino acid sequence set forth in SEQ ID NO:9.6. The recombinant host of claim 4 , wherein the TPS4 polypeptide comprises a TPS4 polypeptide having at least 70% identity to an amino acid sequence set forth in SEQ ID NO:11.7. The recombinant host of any one of - claim 4 , wherein the recombinant host comprises a plant cell claim 4 , a mammalian cell claim 4 , an insect cell claim 4 , a fungal cell claim 4 , or a bacterial cell.8EscherichiaLactobacillusLactococcusCornebacteriumAcetobacterAcinetobacterPseudomonas. The recombinant host of claim 7 , wherein the bacterial cell comprises bacteria cells claim 7 , bacteria ...

NOVEL BLOCK COPOLYMER AND MICELLE COMPOSITIONS AND METHODS OF USE THEREOF

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises 2. The block copolymer of claim 1 , wherein the hydrophilic polymer segment comprises PEO.3. The block copolymer of any one of - claim 1 , wherein n is 1 to 4.4. The block copolymer of any one of - claim 1 , wherein n is 2.5. The block copolymer of any one of - claim 1 , wherein R′ is —CH.6. The block copolymer of any one of - claim 1 , wherein R′ is —H.7. The block copolymer of any one of - claim 1 , wherein x is about 40 to about 100 in total.8. The block copolymer of any one of - claim 1 , wherein x is about 50 to about 100 in total.9. The block copolymer of any one of - claim 1 , wherein x is about 40 to about 70 in total.10. The block copolymer of any one of - claim 1 , wherein x is about 60 to about 80 in total.11. The block copolymer of any one of - claim 1 , wherein x is about 70 in total.12. The block copolymer of any one of - claim 1 , wherein Rand Rare each straight or branched alkyl.13. The block copolymer of any one of - claim 1 , wherein Rand Rjoin to form a ring.14. The block copolymer of any one of - claim 1 , wherein Rand Rare the same.15. The block copolymer of any one of - claim 1 , wherein Rand Rare different.16. The block copolymer of any one of - claim 1 , wherein Rand Reach have 3 to 8 carbons.17. The block copolymer of claim 13 , wherein Rand Rtogether form a ring having 5 to 10 carbons.18. The block copolymer of any one of - claim 13 , wherein Rand Rare propyl.19. The block copolymer of claim 18 , wherein propyl is iso-propyl.20. The block copolymer of any one of - claim 18 , wherein Rand Rare butyl.21. The block copolymer of claim 20 , wherein butyl is n-butyl.22. The block ...

PLANT EXTRACT OBTAINED FROM KIELMEYERA AUREOVINOSA WHICH HAS ANTIBIOTIC ACTIVITY, ISOLATED CHEMICAL COMPOUND, COMPOSITIONS COMPRISING SAME, USES THEREOF AND METHODS FOR PREVENTING AND TREATING BACTERIAL INFECTIONS

The present invention refers primarily to a plant extract obtained from which has accentuated antibiotic activity. In a second modality, the invention describes a new chemical compound isolated from the same, as well as variations thereof. In other terms, the present invention provides compositions comprising a phytotherapic obtained from said plant extract, as well as veterinary pharmaceutical compositions comprising isolated compounds and variations of the same. 1Kielmeyera aureovinosa. An extract from , wherein said extract has antibiotic activity.227-. (canceled)28Kielmeyera aureovinosa.. The extract according to claim 1 , wherein said extract is from the roots of29. The extract according to claim 1 , wherein said extract is an organic solvent extract.30. The extract according to claim 29 , wherein the organic solvent is an alcohol.31. The extract according to claim 1 , wherein the extract is a methanol claim 1 , ethanol claim 1 , ethyl acetate or hexane extract.32Staphylococcus aureus. The extract according to claim 1 , wherein the extract has minimum inhibitory concentration (MIC) in a broth microdilution assay against of less than or equal to 1 μg/mL.33. The extract according to claim 1 , wherein the concentration of chemical markers mammeisine and isomammeisine in said extract is greater than 60%.36. The compound claim 34 , according to claim 34 , wherein said compound is an antibiotic.37Staphylococcus aureus. The compound claim 34 , according to claim 34 , wherein the compound has a minimum inhibitory concentration (MIC) in broth microdilution assay against of less than or equal to 1 μg/mL.38. A phytotherapic claim 1 , pharmaceutical claim 1 , or veterinary composition comprising the extract as defined in and a pharmaceutically or veterinarily acceptable excipient.39. The composition claim 38 , according to claim 38 , wherein said composition is formulated for topical administration.40. The composition claim 39 , according to claim 39 , wherein the topical ...

Photochromic Compounds

A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N, —CN, —COOR′, —CCR′, —C(R′)C(R′)R′, —OCOR′, —OCOOR′, —SR′, —OSOR′″, and/or —CON(R′)R′, wherein each R′ is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R′″ is —CFor a perfluorinated alkyl group having from 2 to 18 carbon atoms The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound. 2. (canceled)3. A photochromic composition comprising the photochromic material of incorporated into at least a portion of an organic material claim 1 , said organic material being a polymeric material claim 1 , an oligomeric material claim 1 , a monomeric material or a mixture or combination thereof.4. The photochromic composition of claim 3 , wherein said polymeric material comprises self-assembling materials claim 3 , polycarbonate claim 3 , polyamide claim 3 , polyimide claim 3 , poly(meth)acrylate claim 3 , polycyclic alkene claim 3 , polyurethane claim 3 , poly(urea)urethane claim 3 , polythiourethane claim 3 , polythio(urea)urethane claim 3 , polyol(allyl carbonate) claim 3 , cellulose acetate claim 3 , cellulose diacetate claim 3 , cellulose triacetate claim 3 , cellulose acetate propionate claim 3 , cellulose acetate butyrate claim 3 , polyalkene claim 3 , polyalkylene-vinyl acetate claim 3 , poly(vinylacetate) claim 3 , poly(vinyl alcohol) claim 3 , poly(vinyl chloride) claim 3 , poly(vinylformal) claim 3 , poly(vinylacetal) claim 3 , poly(vinylidene chloride) claim 3 , poly(ethylene terephthalate) claim 3 , polyester claim 3 , polysulfone claim 3 , polyolefin claim 3 , copolymers thereof claim 3 , and/or ...

CHROMENE DERIVATIVES AND THEIR ANALOGS AS WNT PATHWAY ANTAGONISTS

Compounds of formula (IIc); wherein Xand Xindependently from each other are N or CRwherein Rmay be same or different; Y, Y, Yand Yindependently from each other are N or CRwherein Rmay be same or different and wherein up to 3 of the group Y, Y, Yand Ymay be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer. 116-. (canceled)18. A compound according to claim 17 , wherein at least one substituent Ris not H claim 17 , and pharmaceutically acceptable salts thereof.19. A compound according to claim 17 , wherein at least one member of the group X claim 17 , X claim 17 , Y claim 17 , Y claim 17 , Yand Yis N; and pharmaceutically acceptable salts thereof.20. A compound according to claim 17 , wherein R; R; and Rare independently from each other selected from H; NH; NHCH; CHOH; CHOCH; CHNH; CHNHCH; OH; OCH; Br; F; and C; and Rand Rare independently from each other selected from H; NH; NHCH; CHOH; CHOCH; CHNH; CHNHCH; OH; OCH; Br; F; and Cl; or Rand Rare forming together OCHO;and pharmaceutically acceptable salts thereof.21. A compound according to claim 17 , wherein{'sup': 8', '8a', '8a', '8a', '8b', '16a', '16a', '16a', '16b', '8a', '8a', '8b', '8a, 'sub': 2', '2', '2', '2', '2', '2', '2', '2, 'Ris selected from H; OH; OR; NH; NHR; N(RR); CHOH; CHOR; CHNH; CHNHR; CHN(RR); C(O)NH; C(O)NHR; C(O)N(RR); C(O)OH; and C(O)OR;'}{'sup': 8a', '8b', '16a', '16a', '16a', '16b, 'sub': 1', '6', '2, 'Rand Rare independently from each other selected from C-Calkyl which is optionally substituted with one or more halogen which are the same or different; OH, OR, NH; NHR, NRR;'}{'sup': 16a', '16b, 'sub': 1', '6', '1, 'Rand Rare independently from each other selected from C-Calkyl; wherein C-6 alkyl is optionally substituted with one or more halogen which are the same or different;'}{'sup': 9', '9a', '9a', '9a', '9b', '13a', '13a', '13a', '13b', '9a ...

CHROMENE DERIVATIVES AND THEIR ANALOGS AS WNT PATHWAY ANTAGONISTS

Compounds of formula (IIc); wherein Xand Xindependently from each other are N or CRwherein Rmay be same or different; Y, Y, Yand Yindependently from each other are N or CRwherein Rmay be same or different and wherein up to 3 of the group Y, Y, Yand Ymay be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer. 2. The compound of claim 1 , wherein at least one substituent Ris not H; and pharmaceutically acceptable salts thereof.3. The compound of claim 1 , wherein at least 1 member of the group X claim 1 , X claim 1 , Y claim 1 , Y claim 1 , Yand Yis N; and pharmaceutically acceptable salts thereof.4. The compound of claim 1 , wherein R; R; and Rare independently from each other selected from H; NH; NHCH; CHOH; CHOCH; CHNH; CHNHCH; OH; OCH; Br; F; and Cl; and Rand Rare independently from each other selected from H; NH; NHCH; CHOH; CHOCH; CHNH; CHNHCH; OH; OCH; Br; F; and Cl; or Rand Rare forming together OCH2O; and pharmaceutically acceptable salts thereof.67.-. (canceled)8. The compound of claim 1 , wherein said compound is a modulator of the Wnt signalling pathway.9. A method for the treatment of a disorder or disease associated with an aberrant activation of Wnt signalling in a mammal claim 1 , said method comprising administering to said mammal a compound of .10. The method of claim 9 , wherein the Wnt associated disorder or disease is a cell proliferative disorder claim 9 , rheumatoid arthritis claim 9 , increased bone density claim 9 , aging or age-related disorders and/or diseases or Dupuytren disease (superficial fibromatosis).11. The method of claim 10 , wherein the cell proliferation disorder is cancer or a proliferative skin disorder.12. The method of claim 11 , wherein the cancer is member of the group multiple myeloma claim 11 , colon cancer claim 11 , breast cancer claim 11 , gastritic cancer claim 11 , ...

USE OF COMPOSITIONS OBTAINED BY CALCINING PARTICULAR METAL-ACCUMULATING PLANTS FOR IMPLEMENTING CATALYTICAL REACTIONS

The use of metal-accumulating plants for implementing chemical reactions especially catalytical reactions. 1AlyssumAlyssum murale, Alyssum fallacinum, Alyssum lesbiacum, Alyssun serpyllifolium, Alyssum bertoloniiNoccaeaNoccaea ochrleuca, Noccaea goesingense, Noccacea caerulescensGeissoisGeissois pruinosaPsychotriaPsychotria douarrei, Psychotria costivenia, Psychotria clementis, Psychotria vanhermaniiPcynandraPycnandra acuminataSebertia acuminataAnisopappusAnisopappus chinensis, Anisopappus davyiPhyllanthusP. balgooyi Phyllantthus serpentinus, Phyllanthus ngoyensisHomaliumHomalium kanaliense, Homalium guillainiihybanthusHybanthus austrocaledonicusAnisopappusAnisopappus chinensis, Anisopappus davyi, Centaurium erythraea, Bacopa monnieri, Anthyllis vulneraria.. A catalytic composition containing at least one metal catalyst originating from a calcined plant or a calcined plant part having accumulated at least one metal chosen in particular from zinc (Zn) , nickel (Ni) or copper (Cu) , the implementation of organic synthesis reactions involving said catalyst characterised in that the metal accumulating plant is chosen from the genus , such as , the genus , such as: , the genus , such as: , the genus , such as: , the genus such as (or ) , the genus such as , the genus such as , the genus such as , the genus such as , the genus such as2AlyssumAlyssum murale, Alyssum fallacinum, Alyssum lesbiacum, Alyssun serpyllifolium, Alyssum bertoloniiNoccaeaNoccaea ochrleuca, Noccaea goesingense, Noccacea caerulescensGeissoisGeissois pruinosaPsychotriaPsychotria douarrei, Psychotria costivenia, Psychotria clementis, Psychotria vanhermaniiPcynandraPycnandra acuminataSebertia acuminataAnisopappusAnisopappus chinensis, Anisopappus davyiPhyllanthusP. balgooyi Phyllantthus serpentinus, Phyllanthus ngoyensisHomaliumHomalium kanaliense, Homalium guillainiihybanthusHybanthus austrocaledonicusAnisopappusAnisopappus chinensis, Anisopappus davyi, Centaurium erythraea, Bacopa monnieri, Anthyllis ...

SUBSTITUTED PHENETHYLAMINE DERIVATIVES

Embodiments of the present disclosure describe substituted phenethylamine derivatives, compositions comprising the substituted phenethylamine derivatives, methods of making the substituted phenethylamine derivatives, and methods of using the phenethylamine derivatives, and the like. Exemplary compounds of the present disclosure include compounds of the formula (I) and (II): 3. The compound of claim 1 , wherein Ris selected from —H claim 1 , —CH claim 1 , and —CHCH-Ph.4. The compound of claim 1 , wherein Ris —CHCHor —CH═CH.5. The compound of claim 1 , wherein Ris —CHand Ris —CHCH.6. The compound of claim 1 , wherein Ris selected from —H claim 1 , —CH claim 1 , and —Ac.7. The compound of claim 1 , wherein Ris —CHand Ris selected from —H claim 1 , —CH claim 1 , and —Ac.8. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each independently selected from —H claim 1 , —OH claim 1 , —CH claim 1 , —Br claim 1 , —Cl claim 1 , —I claim 1 , -Ph claim 1 , —OCH claim 1 , and —OBn.11. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with one or more pharmaceutically acceptable carriers.12. A method of treating conditions claim 1 , disorders claim 1 , or deficits modulated by a receptor selected from the group consisting of a 5-HTreceptor claim 1 , 5-HTreceptor claim 1 , 5-HTreceptor claim 1 , 5-HTreceptor claim 1 , 5-HTreceptor claim 1 , 5-HTreceptor claim 1 , 5-HTreceptor claim 1 , 5-HTreceptor claim 1 , 5-HTreceptor claim 1 , 5-HTreceptor claim 1 , Alphareceptor claim 1 , Alphareceptor claim 1 , Alphareceptor claim 1 , Alphareceptor claim 1 , Alphareceptor claim 1 , Alphareceptor claim 1 , Betareceptor claim 1 , Betareceptor claim 1 , Betareceptor claim 1 , BZP receptor claim 1 , Dreceptor claim 1 , Dreceptor claim 1 , Dreceptor claim 1 , Dreceptor claim 1 , Dreceptor claim 1 , DAT receptor claim 1 , δ-OR receptor claim 1 , ...

Oxime compound, photosensitive composition, color filter, method for production of the color filter, and liquid crystal display element

Disclosed are: an oxime compound represented by the general formula (1); a photosensitive composition for which the oxime compound is used as a photopolymerization initiator; a method for producing a color filter by using the photosensitive composition; and a color filter produced by the method. (1) wherein R1 represents a hydrogen atom, an acyl group which may have a substituent, an alkoxycarbonyl group, or an aryloxycarbonyl group; R2's independently represent a halogen atom, an alkyl group, an aryl group, an alkyloxy group, an aryloxy group, an alkylthio group, an arylthio group, or an amino group; m represents an integer of 0 to 4, provided that, when m is 2 or greater, the R2's may together form a ring; and A represents a 4-, 5-, 6- or 7-membered ring.

Use of rylene derivatives as photosensitizers in solar cells

Verwendung von Rylenderivaten I DOLLAR F1 mit folgender Bedeutung der Variablen: DOLLAR A X zusammen DOLLAR F2 beide -COOM; DOLLAR A Y ein Rest DOLLAR F3 der andere Rest Wasserstoff; DOLLAR A zusammen DOLLAR F4 beide Wasserstoff; DOLLAR A R gegebenenfalls substituiertes (Het)Aryloxy, (Het)Arylthio; DOLLAR A P -NR·1·R·2·; DOLLAR A B Alkylen; gegebenenfalls substiutiertes Phenylen; Kombinationen davon; DOLLAR A A -COOM; -SO¶3¶M; -PO¶3¶M¶2¶; DOLLAR A D gegebenenfalls substituiertes Phenylen, Naphthylen, Pyridylen; DOLLAR A M Wasserstoff; Alkalimetallkation; [NR·5·]¶4¶+; DOLLAR A L chemische Bindung; gegebenenfalls indirekt gebundener, gegebenenfalls substituierter (Het)Arylenrest; DOLLAR A R·1·, R·2· gegebenenfalls substituiertes (Cyclo)Alkyl, (Het)Aryl; zusammen das Stickstoffatom enthaltender, gegebenenfalls substituierter Ring; DOLLAR A Z -O-; -S-; DOLLAR A R·3· gegebenenfalls substituiertes Alkyl, (Het)Aryl; DOLLAR A R' Wasserstoff, gegebenenfalls substituiertes (Cyclo)Alkyl, (Het)Aryl; DOLLAR A R·5· Wasserstoff; gegebenenfalls substituiertes Alkyl, (Het)Aryl; DOLLAR A m 0, 1, 2; DOLLAR A n, p, m = 0 : 0, 2, 4 mit: n + p = 2, 4, gegebenenfalls 0; DOLLAR A m = 1 : 0, 2, 4 mit: n + p = 0, 2, 4; DOLLAR A m = 2 : 0, 4, 6 mit: n + p = 0, 4, 6, DOLLAR A oder von deren Mischungen als Photosensibilisatoren in Solarzellen. Use of rylene derivatives I DOLLAR F1 with the following meaning of the variables: DOLLAR A X together DOLLAR F2 both -COOM; DOLLAR A Y one remainder DOLLAR F3 the other remainder hydrogen; DOLLAR A together DOLLAR F4 both hydrogen; DOLLAR A R optionally substituted (Het) aryloxy, (Het) arylthio; DOLLAR A P -NR x 1 x R x 2 x; DOLLAR A B alkylene; optionally substituted phenylene; Combinations thereof; DOLLAR A A COOM; -SO¶3¶M; -PO¶3¶M¶2¶; DOLLAR A D optionally substituted phenylene, naphthylene, pyridylene; DOLLAR A M hydrogen; Alkali metal cation; [NR · 5 ·] ¶4¶ +; DOLLAR A L chemical bond; optionally indirectly bonded, optionally substituted (Het) ...

Use of rylene derivatives as photosensitizers in solar cells

Use of rylene derivatives (I) in which the variables are defined as follows: X together Formulae (x1) (x2) (x3) both -COOM; Y a radical -L-NR1R2 (y1) -L- Z-R3 (y2) the other radical hydrogen; together Formulae (y3) (y4) both hydrogen; R optionally substituted (Het)aryloxy, (Het)arylthio; P -NR1R2; B alkylene; optionally substituted phenylene; combinations thereof; A -COOM; -SO3M; -PO3M2; D optionally substituted phenylene, naphthylene, pyridylene; M hydrogen; alkali metal cation; [NR5]4+; L chemical bond; optionally indirectly bonded, optionally substituted (Het)arylene radical; R1, R2 optionally substituted (cyclo)alkyl, (Het)aryl; together the nitrogen atom containing, optionally substituted ring; Z -O-; -S-; R3 optionally substituted alkyl, (Het)aryl; R' hydrogen; optionally substituted (cyclo)alkyl, (Het)aryl; R5 hydrogen; optionally substituted alkyl, (Het)aryl; m 0, 1, 2; n, p m=0: 0, 2, 4 with: n+p = 2, 4, optionally 0; m=1: 0, 2, 4 with: n+p = 0, 2, 4; m=2: 0, 4, 6 with: n+p = 0, 4, 6, or of mixtures thereof as photosensitizers in solar cells.

Method of inhibiting abcg2 and other treatment methods

Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): Formula (I), wherein R 1 , R 2 , R 3 , X 1 , X 2 , X 3 , a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.

Oxime compound, photosensitive composition, color filter, method for production of the color filter, and liquid crystal display element

Oxime compound, photosensitive composition, color filter, production method for the color filter, and liquid crystal display element

Provided are an oxime compound represented by General Formula (1), a photosensitive composition containing the oxime compound as a photopolymerization initiator, a production method for a color filter using the photosensitive composition, and a color filter obtained by the production method: in General Formula (1), R 1 represents a hydrogen atom, an acyl group, an alkoxycarbonyl group or an aryloxylcarbonyl group, each of which may have a substituent; R 2 represents or R 2 s each represent a halogen atom, an alkyl group, an aryl group, an alkyloxy group, an aryloxy group, an alkylthio group, an arylthio group or an amino group; m is an integer of 0 to 4; when m is an integer of 2 or more, R 2 s may be linked together to form a ring; and A represents a 4-, 5-, 6- or 7-membered ring.

Oxime compound, photosensitive composition, color filter, method for production of the color filter, and liquid crystal display element

Provided are an oxime compound represented by General Formula (1), a photosensitive composition containing the oxime compound as a photopolymerization initiator, a production method for a color filter using the photosensitive composition, and a color filter obtained by the production method: in General Formula (1), R 1 represents a hydrogen atom, an acyl group, an alkoxycarbonyl group or an aryloxylcarbonyl group, each of which may have a substituent; R 2 represents or R 2 s each represent a halogen atom, an alkyl group, an aryl group, an alkyloxy group, an aryloxy group, an alkylthio group, an arylthio group or an amino group; m is an integer of 0 to 4; when m is an integer of 2 or more, R 2 s may be linked together to form a ring; and A represents a 4-, 5-, 6- or 7-membered ring.

含福斯高林衍生物的口服制剂及制备药物制剂的方法

本发明涉及一种具有优异贮存稳定性且含有通式(1)所示的福斯高林衍生物的盐,如colforsin dapropate盐酸盐[6－(3－二甲基氨基丙酰基)福斯高林],以及碱金属卤化物的口服制剂,其中R 1 代表氢原子;R 4 代表乙烯基;且R 2 和R 3 之一代表－CO(CH 2 ) m NR 5 R 6 (其中R 5 和R 6 代表各种低级烷基等,且m为1-5的整数),同时另一个代表氢或－CO(CH 2 ) n X[其中X代表氢或－NR 7 R 8 (其中R 7 和R 8 代表各种低级烷基等),且n为1-5的整数]。

萘嵌苯衍生物在太阳能电池中作为光敏剂的用途

本发明涉及萘嵌苯衍生物(I)或其混合物在太阳能电池中作为光敏剂的用途：其中各变量如下所定义：X一起为式(x1)、(x2)或(x3)，均为－COOM基团；Y为基团－L－NR 1 R 2 (y1)，－L－Z－R 3 (y2)，且另一个基团为氢；一起为式(y3)或(y4)；或均为氢；R为任选取代的(杂)芳基氧基或(杂)芳基硫基；P为－N 1 R 2 ；B为亚烷基、任选取代的亚苯基或其组合；A为－COOM、－SO 3 M或－PO 3 M 2 ；D为任选取代的亚苯基、亚萘基或亚吡啶基；M为氢、金属阳离子、[NR 5 ] 4 + ；L为化学键；任选间接连接，任选取代的(杂)亚芳基；R 1 、R 2 为任选取代的(环)烷基或(杂)芳基；一起为含有氮原子的任选取代的环；Z为－O－或－S－；R 3 为任选取代的烷基、(杂)芳基；R′为氢；任选取代的(环)烷基或(杂)芳基；R 5 为氢；任选取代的烷基或(杂)芳基；m为0、1或2；n、p在m＝0时为0、2或4，其中n+p＝2、4，任选0；n、p在m＝1时为0、2或4，其中n+p＝0、2、4；n、p在m＝2时为0、4、6，其中n+p＝0、4或6。

4-aminophenol derivatives or their n-alkyl or salt derivatives showing antiinflammatory activity

FIELD: organic chemistry. SUBSTANCE: product: derivatives of 4-aminophenol of the formula (I) where R 1 group -C(O)YZ where Y a simple bond, O, -NR 7 or CO; Z H, pyridyl, phenyl that can be substituted for halogen, nitro, lower alkoxy or carboxy; lower alkyl which can be substituted for -OH, lower alkoxy, lower acyloxy, carboxy, lower alkoxycarbonyl, CONR 8 , phenyl(lower)alkoxy, phenyl, halide, cyano or NR 10 R 12 ; R 2 , R 3 , R 6 anf R 5 H, lower alkyl or alkenyl, lower alkoxy or halogen; R 4 and R 7 H or lower alkyl; X 4,5-dihydropyrazolyl or pyrazolyl which can be substituted for C 3 -C 6 -cycloalkyl or phenyl which can be substituted for trihaloidalkyl; R 8 , R 9 , R 10 and R 11 H, lower alkyl or benzylhydroxycarbonyl, or their N-acyl or salt derivatives. Synthesized compounds were used in medicine. EFFECT: improved method of synthesis. 6 cl 611670сС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВИ "” 2049 779‘ (51) МПК 13) СЛ 31/415 С 070 231/38, 401/12, А 61 К 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4894663/04, 17.05.1990 (30) Приоритет: 20.05.1989 СВ 8911654.5 20.05.1989 СВ 8911655.2 10.02.1990 СВ 9003044.6 (46) Дата публикации: 10.12.1995 (56) Ссылки: Майтаа!е; ТПе ехга рпагтасорета, 291 еЧШоп, ед. |атез Е.ЁГ.Кеупо!|С$, Гопаоп, ТПе Рвагтасеийса! Ргез$$, 1989, р.1584.А.Наскват К./. СиЯ\А$, С.НаНат, /.Мапп, Р.О. Мигпей, А.А. Моггзо| М\.Т. Зитрзоп, Адет5$ апа АсНопз, 30, 432.ЕР М 0254259, кл. С 07О 241/20, опублик. 1988. (86) Заявка РСТ: РСТ/СВ 90/00762 (17.05.90) (71) Заявитель: Физонз ПЛС (СВ) (72) Изобретатель: Джон Раймонд Бантик[СВ], Дэвид Норман Хардерн[ГСВ], Ричард Энтони Эпплтон[ СВ], Джон Диксон[ СВ], Дэвид Джон Уилкинсон[ СВ] (73) Патентообладатель: Физонз ПЛС (СВ) (54) ПРОИЗВОДНЫЕ 4-АМИНОФЕНОЛА ИЛИ ИХ М-АЛКИЛЬНЫЕ ИЛИ СОЛЕВЫЕ ПРОИЗВОДНЫЕ, ПРОЯВЛЯЮЩИЕ ПРОТИВОВОСПАЛИТЕЛЬНУЮ АКТИВНОСТЬ (57) Реферат: Использование: в медицине в качестве веществ, обладающих противовоспалительной активностью. Сущность ...

Method of preparing isochromans

一种高效合成1,1-二芳基烷烃类化合物的方法

本发明公开了一种高效合成1,1‑二芳基烷烃类化合物的方法。所述方法包括以下步骤：在气体保护下，在铜催化剂、双氮配体、碱和氧化剂的作用下，式I化合物和式II化合物在有机溶剂中进行如下反应，从而得到式III化合物。本发明的方法具有反应条件温和、操作简单、底物适应性广、官能团兼容性高等优点，具有较高的学术和应用价值。

태양 전지 중 감광제로서의 릴렌 유도체의 용도

본 발명은 하기의 변수 정의를 갖는 릴렌 유도체 (I) 또는 상기 릴렌 유도체의 혼합물의, 태양 전지 중 감광제로서의 용도에 관한 것이다: X는 함께 이거나, 상기 X 둘 모두가 -COOM이고; Y는 한 라디칼이 이거나, 다른 라디칼이 수소이며; 함께 이거나, 상기 Y 둘 모두가 수소이고; R은 임의로 치환된 (헤트)아릴옥시, (헤트)아릴티오이며; P는 -NR 1 R 2 이고; B는 알킬렌; 임의로 치환된 페닐렌; 이들의 조합이며; A는 -COOM; -SO 3 M; -PO 3 M 2 이고; D는 임의로 치환된 페닐렌, 나프틸렌, 피리딜렌이며; M은 수소; 알칼리 금속 양이온; [NR 5 ] 4 + 이고; L은 화학 결합; 임의로 간접 결합되고, 임의로 치환되는 (헤트)아릴렌 라디칼이며; R 1 , R 2 는 임의로 치환된 (시클로)알킬, (헤트)아릴; 함께 질소 원자를 포함하는 임의로 치환된 고리이고; Z는 -O-; -S-이며; R 3 는 임의로 치환된 알킬, (헤트)아릴이고; R'은 수소; 임의로 치환된 (시클로)알킬, (헤트)아릴이며; R 5 는 수소; 임의로 치환된 알킬 (헤트)아릴이고; m은 0, 1, 2이며; n, p은 m이 0이고 n + p가 2, 4, 필요한 경우 0인 경우에 0, 2, 4이고; m이 1이고 n + p가 0, 2, 4인 경우에 0, 2, 4이며; m이 2이고 n + p가 0, 4, 6인 경우에 0, 4, 6이다.

Versions of method of producing derivatives of 2,2,3-iminobisethanol or acid-additive salts thereof,or stereochemical isomeric forms thereof

Novel 2,2 min -iminobisethanol derivatives of the formula <CHEM> the pharmaceutically acceptable acid addition salts and possible stereochemically isomeric forms thereof, which compounds are useful for the treatment and/or prevention of disorders of the coronary vascular system; compositions containing such compounds as an active ingredient; novel intermediates useful in the preparation of such compounds and methods of preparing said compounds, pharmaceutical compositions and intermediates.

Dimer-Selective RXR Modulators and How to Use Them

본 발명은 RXR 호모다이머 및/또는 RXR 헤테로다이머와 관련한 작용제, 부분작용제 및/또는 길항제 활성을 갖는 다이머-선택적 RXR 변조제 화합물에 관한 것이다. 본 발명은 또한 이러한 다이머-선택적 RXR 변조제 화합물을 함유하는 약제학적 조성물 및 그의 치료학적 사용방법에 관한 것이다. The present invention relates to dimer-selective RXR modulator compounds having agonist, partial agonist and / or antagonist activity in connection with RXR homodimers and / or RXR heterodimers. The present invention also relates to pharmaceutical compositions containing such dimer-selective RXR modulator compounds and methods of therapeutic use thereof.

Film-forming composition, film, method for forming a resist underlayer film, method and compound for manufacturing a patterned substrate

평탄성이 우수함과 함께 용매 내성, 에칭 내성 및 내열성이 우수한 막을 형성할 수 있는 막 형성용 조성물, 막, 레지스트 하층막의 형성 방법, 패터닝된 기판의 제조 방법 및 화합물의 제공을 목적으로 한다. 본 발명은, 하기 식 (1)로 표시되는 기를 갖는 화합물과, 용매를 함유하는 막 형성용 조성물이다. 하기 식 (1) 중, R 1 내지 R 4 는 각각 독립적으로, 수소 원자 또는 탄소수 1 내지 20의 1가 유기기이거나, 또는 이들 기가 서로 합쳐져서 이들이 결합하는 탄소 원자 혹은 탄소쇄와 함께 구성되는 환원수 3 내지 20의 환 구조를 나타낸다. Ar 1 은 탄소수 6 내지 20의 아렌에서 (n+3)개의 방향환 상의 수소 원자를 제외한 기이다. R 5 는 히드록시기, 할로겐 원자, 니트로기 또는 탄소수 1 내지 20의 1가 유기기이다. n은 0 내지 9의 정수이다. An object of the present invention is to provide a film-forming composition, a film, a method for forming a resist underlayer film, a method for manufacturing a patterned substrate, and a compound capable of forming a film having excellent flatness and excellent solvent resistance, etching resistance and heat resistance. MEANS TO SOLVE THE PROBLEM This invention is a composition for film formation containing the compound which has group represented by following formula (1), and a solvent. In the following formula (1), R 1 to R 4 are each independently a hydrogen atom or a monovalent organic group having 1 to 20 carbon atoms, or a reduced number 3 formed by combining these groups with the carbon atom or carbon chain to which they are bonded to 20 ring structures. Ar 1 is a group in which (n+3) hydrogen atoms on aromatic rings are removed from arene having 6 to 20 carbon atoms. R 5 is a hydroxyl group, a halogen atom, a nitro group, or a monovalent organic group having 1 to 20 carbon atoms. n is an integer from 0 to 9;

- novel -extended acedan derivatives and their application for two-photon microscopy imaging of amyloid-beta plaque in an alzheimer's disease animal model

The present invention relates to a novel ascorbic analogue having an extended pi-bond, a method for preparing the same, and a method for two-photon microscopic imaging of an amyloid-beta plaque using the same. More specifically, Absorbing phosphor compounds with longer absorption and emission wavelengths compared to the azide and azide analogs of the phosphors. The compounds according to the present invention can be usefully used for in vivo imaging studies by imaging cells or tissues and can be useful for diagnosing Alzheimer's disease by imaging amyloid-beta plaques.

Light emitting device material, light emitting device and amine compound using the same

2,2'IMINOBISETHANOL DERIVATIVES AND PROCEDURES FOR PREPARING THEREOF

Process for preparing 6,7-discyl-7-deacetyl forsrolin derivati

내용 없음. No content.

Novel process for producing 6-acyl-7-deacetylforskolin derivatives

일반식(2)의 7-아실-7-데아세틸포르스콜린 유도체를 비양자성 용매 중에서 강염기와 반응시켜 일반식(1)의 6-아실-7-데아세틸포르스콜린 유도체를 제조하는 방법. A method of preparing the 6-acyl-7-deacetylphospholine derivative of the general formula (1) by reacting the 7-acyl-7-deacetylphospholine derivative of the general formula (2) with a strong base in an aprotic solvent.

Naphthopyran carbazone derivatives, and preparation method and application thereof

本发明涉及萘并吡喃卡巴腙衍生物及其制备方法和应用，属于有机合成技术领域。所述的萘并吡喃卡巴腙衍生物的制备方法包括如下步骤：S1：将3H‑萘并[2,1‑b]吡喃‑2‑甲醛加入有机溶剂中溶解，再加入卡巴肼，得混合物；S2：将S1所得混合物在常压下进行回流搅拌反应；S3：反应结束后，冷却至室温，有固体析出，减压过滤，取滤渣；S4：将S3所得滤渣进行洗涤，得到萘并吡喃卡巴腙衍生物。该萘并吡喃卡巴腙衍生物在作为比率荧光探针检测铜离子时具有较高的灵敏度和较强的选择性，特别是作为荧光探针在细胞内铜离子的方便检测的应用。

Method of obtaining dianhydrides of aromatic tetracarbonic acids

FIELD: technological processes.SUBSTANCE: proposed method for producing aromatic tetracarboxylic acid dianhydrides is carried out by condensation on C-C bonds in aromatic fragments of esters of aromatic halogenicarboxylic acids, preliminarily obtained by the reaction of the interaction of the corresponding aromatic halogenicarboxylic acid dianhydrides and lower monohydric alcohols, carried out at boiling in the presence of catalytic amounts of sulfuric acid, followed by isolation of the obtained products, moreover, the subsequent condensation reaction of esters of aromatic halocarboxylic acids is carried out in an atmosphere of inert gas, in an amide organic solvent in the presence of a catalytic mixture containing anhydrous nickel halide, triphenylphosphine and activated zinc powder, after which successive stages of processing the reaction mass are carried out: filtration, precipitation with water, boiling in the presence of an alkaline agent, cooling, washing and drying, where as the starting anhydrides of aromatic halo dicarboxylic acids are used compounds selected from the following group: 4-chloro-1,8-naphthalene dicarboxylic anhydride, 4-bromo-1,8-naphthalene dicarboxylic anhydride, 3-iodine-1-phthalic anhydride, 4-iodine-1-phthalic anhydride, which are converted to the corresponding esters by boiling with C-Cmonohydric alcohol, taken in 5-7-fold excess by weight of equimolar amount for 8–16 hours, followed by evaporation of the alcohol, and complete dissolution of the dry residue in toluene, alkalinization with sodium hydroxide solution with stirring, separation of the organic layer, washing it, drying, evaporating the solvent and distilling the residue in a vacuum, after which a solution of the obtained aromatic halogenicarboxylic acid ester in a dry amide organic solvent is slowly introduced into a previously prepared catalytic mixture having a temperature of 80–100 °C and containing 0.03–0.07 moles of anhydrous nickel (II)halide, 0.2–0.4 mol of ...

Method of using a COX-2 inhibitor and a topoisomerase II inhibitor as a combination therapy in the treatment of neoplasia

The present invention provides compositions and methods to treat, prevent or inhibit a neoplasia or a neoplasia-related disorder in a mammal using a combination of a COX-2 inhibitor and a topoisomerase II inhibitor.

Method of using a COX-2 inhibitor and an alkylating-type antineoplastic agent as a combination therapy in the treatment of neoplasia

The present invention provides compositions and methods to treat, prevent or inhibit a neoplasia or a neoplasia-related disorder in a mammal using a combination of a COX-2 inhibitor and an alkylating-type antineoplastic agent.

Preparation 6,7-diacyl-7-takes off the novel method of acetyl forskrine derivant

一种制备药用通式(I)所示6，7-二酰基-7-脱 乙酰福斯克林(forskolin)衍生物的方法，其中包括经 溶剂分解脱除通式(III)所示1，6，7-三酰基-7-脱乙 酰福斯克林衍生物中1倍上的酰基，在式(I)和(III) 中，R 1 和R 2 各自代表酰基而R 3 代表C 2-3 脂族基。

Chromene derivatives and their analoga as wnt pathway antagonists

Compounds according to the general formula (I) wherein X 1 , X 2 , X 3 and X 4 independently from each other are N or CR 8 wherein R 8 may be same or different, and wherein up to 3 of the group X 1 , X 2 , X 3 and X 4 may be N; A is a 5- or 6-membered aromatic or heteroaromtic cycle containing 1 to 3 heteroatoms selected from the group consisting of N, O and S wherein A may be substituted by 1 to 5 substituents R which may be same or different; their solvates, hydrates, and pharmaceutically acceptable salts for the treatment of a disorder or disease associated with an aberrant activation of Wnt signalling in a mammal selected from a cell proliferative disorder, rheumatoid arthritis, increased bone density, aging or age-related disorders and/or diseases or Dupuytren disease (superficial fibromatosis).

Chromene derivatives and their analogs as Wnt pathway antagonists

Compounds of formula (IIc); wherein X 3 and X 4 independently from each other are N or CR 8 wherein R 8 may be same or different; Y 1 , Y 2 , Y 3 and Y 4 independently from each other are N or CR 9 wherein R 9 may be same or different and wherein up to 3 of the group Y 1 , Y 2 , Y 3 and Y 4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.

Chromene derivatives and their analoga as Wnt pathway antagonists

Compounds of formula (IIc); wherein X 3 and X 4 independently from each other are N or CR 8 wherein R 8 may be same or different; Y 1 , Y 2 , Y 3 and Y 4 independently from each other are N or CR 9 wherein R 9 may be same or different and wherein up to 3 of the group Y 1 , Y 2 , Y 3 and Y 4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.

Chromene derivatives and their analoga as wnt pathway antagonists

Compounds of formula (IIc); wherein X 3 and X 4 independently from each other are N or CR 8 wherein R 8 may be same or different; Y 1 , Y 2 , Y 3 and Y 4 independently from each other are N or CR 9 wherein R 9 may be same or different and wherein up to 3 of the group Y 1 , Y 2 , Y 3 and Y 4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.

Hedgehog Pathway Antagonists

Aromatic compounds for treating various diseases and pathologies are disclosed. The methods use of such compounds are also provided. Accordingly, the present invention makes available methods and compositions for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function.

Ratiometric two-photon fluorescent probe for detecting mitochondrial pH value and method for preparing the same

The present invention relates to a variable color double-photon fluorescent probe for detecting a pH in mitochondria and a method for producing the same. More specifically, the present invention relates to a variable color double-photon probe capable of quantitatively imaging the pH change in mitochondria by selectively staining mitochondria in cells and tissues. A fluorescent probe and a method for producing the same. The variable color double-photon fluorescent probe according to the present invention selectively stains mitochondria and dehydrogenases according to pH changes, exhibits a strong fluorescence color change, can easily be loaded on cells due to its excellent solubility in water and small molecular weight, The pH can be selectively detected in cells and biological tissues of 100 to 200 mu m in depth for more than 60 minutes, so that the distribution and activity of pH inside the mitochondria can be quantitatively imaged in cells and living tissues.

Photochromic materials with reactive substituents

本发明公开内容的各种非限制性实施方案涉及含反应性取代基的光致变色材料。例如，本公开内容提供了光致变色材料，例如光致变色性萘并吡喃和具有反应性取代基的茚并稠合萘并吡喃，该反应性取代基包含通过一个或多个连接基与该光致变色性萘并吡喃连接的反应性结构部分。在某些非限制性实施方案中，所述反应性结构部分包括可聚合结构部分。在其它的非限制性实施方案中，所述反应性结构部分包括亲核结构部分或亲电结构部分。本公开内容的其它非限制性实施方案涉及光致变色制品、组合物和该光致变色制品的制备方法，其中该光致变色制品和组合物包含本文描述的光致变色性萘并吡喃。

GASOLINE DERIVATIVES WITH A SIX-RING RING AS A DPP-4 INHIBITOR AND THEIR APPLICATION

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 311/92 (2006.01) C07D 405/04 (2006.01) C07D 417/04 (2006.01) C07D 221/10 (2006.01) C07D 335/04 (2006.01) A61K 31/352 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61K 31/5377 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P 3/00 (2006.01) A61P 3/10 (2006.01) A61P 7/10 (2006.01) (12) 2017117559, 30.10.2015 Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 30.11.2018 Бюл. № 34 (71) Заявитель(и): ИСТ ЧАЙНА ЮНИВЕРСИТИ ОФ САЙЕНС ЭНД ТЕКНОЛОДЖИ (CN), ШАНХАЙ ИНСТИТЬЮТ ОФ МАТИРИА МЕДИКА, ЧАЙНИЗ ЭКЭДЕМИ ОФ САЙЭНСИЗ (CN) (86) Заявка PCT: CN 2015/093384 (30.10.2015) (87) Публикация заявки PCT: WO 2016/066134 (06.05.2016) Адрес для переписки: 191002, Санкт-Петербург, а/я 5, Общество с ограниченной ответственностью "Ляпунов и партнеры" 2 0 1 7 1 1 7 5 5 9 (72) Автор(ы): ЛИ Хунлинь (CN), ЦЗЯН Хуалян (CN), СЮЙ Юйфан (CN), ЛИ Цзя (CN), ЧЖАО Чжэньцзян (CN), ЛИ Цзиньгя (CN), СЮЙ Хунлин (CN), ЛИ Шилян (CN) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 31.05.2017 A A61P 29/00 (2006.01) R U 31.10.2014 CN 201410609270.2 (54) БЕНЗОПРОИЗВОДНЫЕ С ШЕСТИЧЛЕННЫМ КОЛЬЦОМ В КАЧЕСТВЕ ИНГИБИТОРА DPP4 И ИХ ПРИМЕНЕНИЕ A 2 0 1 7 1 1 7 5 5 9 A ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: R U (13) 2017 117 559 (57) Формула изобретения 1. Соединение общей формулы I или его фармацевтически приемлемая соль или пролекарство, или его оптически активный изомер или сольват: где X выбран из СН2, О, S и NH; А представляет собой незамещенное бензольное кольцо или бензольное кольцо с 1-5 заместителями, где каждый заместитель независимо выбран из галогена, циано, гидрокси, C1-6 алкила или C1-6 алкила, замещенного галогеном, предпочтительно F, более предпочтительно 1-5 F, C1-6 алкокси или C1-6 алкокси, замещенного галогеном, предпочтительно F, более предпочтительно 1-5 F; А также может быть выбран из азотсодержащего или серосодержащего пятичленного или шестичленного насыщенного или ненасыщенного гетероцикла с 1-4 заместителями, Стр.: 1 где каждый ...

New toralactone and its derivation and the use of decreasing blood-fat and losing weight

New toralactone of general formula [A] extracted from seed of cassiae obtusifollia L. and its derivative, wherein R3 is H or acyl of C¿2?-C4, R?1, R2¿ is identity or difference, independently H, saccharide group, acyl of C¿2?-C4. The said compound can reduce serumal general cholesterol and increase the amount of general bile acid, manifesting that these compounds have the effect of decreasing blood-fat and losing weight.

4-(2,4-dimethoxyphenyl)-2-(2-hydroxyphenyl)-5,6-dihydro-4n-benzo[h]chromene-3-carboxylic acid, having cytotoxic activity

FIELD: chemistry. SUBSTANCE: present invention relates to 4-(2,4-dimethoxyphenyl)-2-(2-hydroxyphenyl)-5,6-dihydro-4H-benzo[h]chromene-3-carboxylic acid of said formula, having cytotoxic activity. EFFECT: disclosed is 4-(2,4-dimethoxyphenyl)-2-(2-hydroxyphenyl)-5,6-dihydro-4n-benzo[h]chromene-3-carboxylic acid, having cytotoxic activity. 1 cl, 1 tbl, 3 dwg, 1 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 707 972 C1 (51) МПК C07D 311/92 (2006.01) A61K 31/352 (2006.01) A61P 35/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 311/92 (2019.08); A61K 31/352 (2019.08); A61P 35/00 (2019.08) (21)(22) Заявка: 2019103550, 08.02.2019 (24) Дата начала отсчета срока действия патента: Дата регистрации: 03.12.2019 (45) Опубликовано: 03.12.2019 Бюл. № 34 Адрес для переписки: 410012, г. Саратов, ул. Астраханская, 83, ЦПУ, СГУ, Гембицкой Е.И. 2 7 0 7 9 7 2 C 1 (56) Список документов, цитированных в отчете о поиске: Kello, Martin et al. Chalcone derivatives cause accumulation of colon cancer cells in the G2/M phase and induce apoptosis. Life Sciences, 2016, 150, 32-38. Drutovic, David et al. Benzylidenetetralones, cyclic chalcone analogues, induce cell cycle arrest and apoptosis in HCT116 colorectal cancer cells. Tumor Biology, 2014, 35(10), 9967-9975. (см. прод.) (54) 4-(2,4-ДИМЕТОКСИФЕНИЛ)-2-(2-ГИДРОКСИФЕНИЛ)-5,6-ДИГИДРО-4Н-БЕНЗО[H]ХРОМЕН3-КАРБОНОВАЯ КИСЛОТА, ОБЛАДАЮЩАЯ ЦИТОТОКСИЧЕСКОЙ АКТИВНОСТЬЮ (57) Реферат: Настоящее изобретение относится к 4-(2,4пр. диметоксифенил)-2-(2-гидроксифенил)-5,6дигидро-4Н-бензо[h]хромен-3-карбоновой кислоте указанной формулы, обладающей цитотоксической активностью. 1 табл., 3 ил., 1 (56) (продолжение): Katsori, A.-M. et al. Chalcones in cancer: understanding their role in terms of QSAR. Current Medicinal Chemistry, 2009, 16(9), 1062-1081. А.Л. Иванова и др. Арилидентетрагидронафталиноны в реакциях с С-нуклеофилами. ХХ Молодежная школа-конференция по органической химии, 18-21 сентября 2017 ...

Process for preparing 6, 7-diacyl-7-deacetyl forskolin derivatives

一种制备药用通式(I)所示6，7-二酰基-7-脱乙酰福斯克林(forskolin)衍生物的方法，其中包括经溶剂分解脱除通式(III)所示1，6，7-三酰基-7-脱乙酰福斯克林衍生物中1位上的酰基，在式(I)和(III)中，R 1 和R 2 各自代表酰基而R 3 代表C 2-3 脂族基。

The method of obtaining aromatic bis (ether anhydrides)

Lyophilized peparation of 6-(3-dimethylaminopropionyl) forskolin

내용없음 No content

Benzo-six-membered ring derivative and application thereof

本发明涉及作为治疗肝纤维化的苯并六元环衍生物及其应用。具体而言,本发明涉及Ⅰ所示化合物、含有Ⅰ式化合物的药物组合物及所述化合物在制备治疗肝纤维化相关疾病及其药物中的用途。

C5-C6 ANNELED NAPHTHOPYRANS, THEIR PREPARATION AND THE POLYMERIC COMPOSITIONS AND (CO) MATRICES CONTAINING THEM

Novel compound, fabrication method of the novel compound, and colorfilter for liquid crystal display including the novel compound

본 발명의 신규한 화합물, 이의 제조 방법, 및 이를 포함하는 액정표시장치용 컬러필터에서, 본 발명의 신규한 화합물은 하기 화학식 1로 나타낸다; [화학식 1] 화학식 1에서, R 1 및 R 2 는 각각 독립적으로 수소, 할로겐 원소, 이소티오시아네이트(isothiocyanate), 보론산(boronic acid), 니트로기(Nitro gourp), 니트릴기(Nitrile group), 알킬기(alkyl group), 알콕시기(alkoxy group), 알킬아미노기(alkylamino group), 하이드록시기(hydroxy group), 또는 카복시기(carboxyl group)를 나타낸다. In a novel compound of the present invention, a process for producing the same, and a color filter for a liquid crystal display device comprising the same, the novel compound of the present invention is represented by the following formula (1): [Chemical Formula 1] In formula (1), R 1 and R 2 are each independently selected from the group consisting of hydrogen, a halogen element, isothiocyanate, boronic acid, nitrogourp, nitrile group, alkyl group, an alkoxy group, an alkylamino group, a hydroxy group, or a carboxyl group.

New (meth) acryloyl compound and its production method

A reactive naphthopyran compound, a photocromic polyurethane coating composition containing the naphthopyran compound, a photocromic polyurethane grafted with the naphthopyran graft, and a photochromic optical article comprising the same

본 발명은 반응형 나프토피란(naphthopyran) 화합물, 이를 포함하는 광변색성 폴리우레탄 코팅액 조성물, 광변색성 폴리우레탄 및 이를 포함하는 광변색성 광학제품에 관한 것으로서, 보다 상세하게는 하기 화학식 1 또는 2로 표시되는 반응형 나프토피란 화합물, 이를 포함하는 광변색성 폴리우레탄 코팅액 조성물, 반응형 나프토피란이 그라프트된 광변색성 폴리우레탄, 및 이를 포함하는 광변색성 광학제품에 관한 것이다. The present invention relates to a reactive naphthopyran compound, a photochromic polyurethane coating liquid composition comprising the same, a photochromic polyurethane, and a photochromic optical article including the same, and more particularly, to Formula 1 or It relates to a reactive naphthopyran compound represented by 2, a photochromic polyurethane coating liquid composition comprising the same, a photochromic polyurethane grafted with a reactive naphthopyran, and a photochromic optical article comprising the same. 본 발명의 광변색성 폴리우레탄 코팅액 조성물은 폴리우레탄 분자에 직접 그라프트 될 수 있는 나프토피란 화합물을 포함함에 따라, 코팅액 중에서도 상분리 현상이 일어나지 않고, 이로부터 제조되는 광변색성 코팅막은 시간의 경과에 따른 블루밍(blooming) 현상이 없으며, 오랫동안 광변색성이 지속될 수 있는 장점이 있다. Since the photochromic polyurethane coating solution composition of the present invention includes a naphthopyran compound which can be grafted directly to a polyurethane molecule, phase separation does not occur even in the coating solution, and the photochromic coating film prepared therefrom may be used. There is no blooming phenomenon due to, there is an advantage that the photochromic properties can be maintained for a long time. [화학식 1] [화학식 2] [Formula 1] [Formula 2] 상기 화학식 1 및 2에서, X 1 내지 X 4 는 발명의 상세한 설명에서와 동일한 구조를 갖는다. In Chemical Formulas 1 and 2, X 1 to X 4 Has the same structure as in the detailed description of the invention. 반응형, 광변색성, 나프토피란, 폴리우레탄, 그라프트, 코팅막 Responsive, Photochromic, Naphthopyran, Polyurethane, Graft, Coating Film

Method for extracting diterpenoid compounds from Blumea aromatic DC.

一种从壮药山风中提取二萜类化合物的方法，属医药技术领域，发明公开了一种从艾纳香属植物山风(Blumea aromatica DC.)的地上部分提取制备二萜类化合物的方法，其特征是药材粗粉通过高浓度低级醇(如甲醇，乙醇，下同)提取，提取液浓缩后用少量水分散，经石油醚萃取除去低极性成分(如叶绿素等)，再用乙酸乙酯萃取，乙酸乙酯萃取液回收溶剂后，用适量低级醇溶解，依次经MCI树脂、聚酰胺、SephadexLH-20凝胶色谱柱，以低级醇洗脱、收集特定色段，再经低级醇的溶液低温结晶、重结晶可以得到二萜类化合物结晶或无定型粉末。这些化合物有潜在的药用价值。本发明具有良好的重复性，提取的化合物含量稳定，纯度高，工艺简单，成本低，对山风药材的推广应用有重要意义。