НОВЫЕ ФОСФОРСОДЕРЖАЩИЕ ТИРОМИМЕТИКИ

Настоящее изобретение относится к соединениям формулы VIII, пригодным в медицине качестве Т3 миметиков: ! ! где G - О, -S(=O)2- или -CH2-; R2 - галоген, алкил, -CF3, -OCF3, алкокси или циано; R3 и R4 - Н, галоген, алкил или -(CRa 2)mарил; Т выбран из -(CRa 2)k-, -CRb=CRb-(CRa 2)n-, -(CRa 2)n-CRb=CRb, -(CRa 2)-CRb=CRb-(CRa 2)-, -O(CRa 2)(CRa 2)n-, -S(CRa 2)(CRa 2)n-, -N(Rc)(CRb 2)(CRa 2)n-, -N(Rb)C(O)(CRa 2)n-, -(CRa 2)nCH(NRbRc)-, -C(O)(CRa 2)m -, -(CRa 2)mC(O)-, -(CRa 2)C(O)(CRa 2)n-, -(CRa 2)nC(O)(CRa 2)- и -C(O)NH(CRb 2)(CRa 2)p-; Ra, Rb, Rc, R1, R6, R7, R8 и R9 - Н, галоген или алкил; или R6 и Т с атомом С образуют 5-6-членное кольцо с 0-2 группами -NRi-, -О- или -S-; Ri - Н, -С(O)алкил, алкил или арил; R5 - ОН, алкокси, -OC(O)Re, -OC(O)ORh, -F, -NHC(O)Re, -NHS(=O)Re, -NHS(=O)2Re, -NHC(S)NH(Rh) или -NHC(O)NH(Rh); Re - алкил, -(CRa 2)n-арил, -(CRa 2)n-циклоалкил или -(CRa 2)n- гетероциклоалкил; Rh - Н или алкил; Х -Р(O)YR11Y'R11; Y и Y' - О или -NRv-; R11 - Н, алкил, -С(Rz)2-ОС(O)Ry, ...

СПОСОБ ПОЛУЧЕНИЯ МОНОГИДРОПЕРФТОРАЛКАНОВ, БИС(ПЕРФТОРАЛКИЛ)ФОСФИНАТОВ И ПЕРФТОРАЛКИЛФОСФОНАТОВ

Изобретение описывает способ получения моногидроперфторалканов, бис(перфторалкил)фосфинатов и перфторалкилфосфонатов, включающий, по крайней мере, обработку, по крайней мере, одного перфторалкилфосфорана, по крайней мере, одним основанием, где основание(я) выбирают из группы, состоящей из гидроксидов щелочноземельных металлов, органо-металлического соединения в пригодном растворителе или, по крайней мере, одного органического основания и при желании кислотой в пригодной реакционной среде. Также описываются новые перфторалкилфосфонаты и бис(перфторалкил)фосфинаты, применение новых перфторалкилфосфонатов и бис(перфторалкил)фосфинатов как ионных жидкостей, как катализаторов фазового переноса или поверхностно-активных веществ. 4 н. и 14 з.п. ф-лы.

КОНДЕНСИРОВАННЫЕ АРОМАТИЧЕСКИЕ ДИФТОРМЕТАНФОСФОНАТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ПРОТЕИНТИРОЗИНФОСФАТАЗЫ IB (PTP-1B)

Изобретение относится к ингибиторам протеинтирозинфосфатазы 1В формулы, пригодным для лечения диабета 2 типа и рака ! ! или его фармацевтически приемлемым солям, в которых X выбирают из СН и N; R1 выбирают из С1-3алкила, необязательно замещенного 1-3 галогенами или одной группой -ОН, -CN, -С(=О)Н, -С(=О)С1-3алкилом, -HC=NOH, -(CH3)C=NOH, ! -НС=NОС1-3алкилом, -(СН3)С=NOC1-3алкила, ! -С(=О)ОС1-3алкила, -C(=O)NHR6, -СН=СН-фенила, в котором фенил замещен -С(=О)ОН; R3 - галоген; R6 выбран из Н, С1-3алкила, фенила, и СН2-фенила, где фенил в обоих случаях необязательно замещен галогеном. Получены новые биологически активные соединения для лечения диабета 2 типа и рака, а также фармацевтические композиции на их основе. 5 н. и 5 з.п. ф-лы, 2 табл., 9 пр.

Способ синтеза альфа-аминоалкиленфосфоновой кислоты

Изобретение относится к способу синтеза альфа-аминоалкиленфосфоновой кислоты или ее сложного эфира, применяемых, например, для обработки воды, замедления процесса образования накипи, моющих присадок, комплексообразователей. Способ включает следующие стадии: а) получение реакционной смеси путем смешивания соединения, содержащего один или несколько ангидридных фрагментов Р-О-Р, причем указанные фрагменты содержат один атом Р со степенью окисления (+III) и другой атом Р со степенью окисления (+III) или (+V), альфа-аминоалкиленкарбоновой кислоты и кислотного катализатора, где указанное соединение, содержащее один или несколько ангидридных фрагментов Р-О-Р, которые содержат один атом Р в степени окисления (+III) и другой атом Р в степени окисления (+III) или (+V), выбирают из группы, состоящей из: тетрафосфорного гексаоксида, PO, PO, РО, тетрафосфорного декаоксида, тетраэтилпирофосфита, диметилфосфита и их комбинаций, и где указанная альфа-аминоалкиленкарбоновая кислота выбрана из группы, состоящей ...

ПРОИЗВОДНЫЕ ФОСФОНЯНТАРНОЙ КИСЛОТЫ И ИХ ФАРМАКОЛОГИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ И КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

Использование: в медицине для лечения нарушений кальциевого обмена. Продукты: производные фосфонянтарной кислоты формулы R-alk-CH(CO2R4-CH(CO2 R3)P(O)(OR5)2, где R - аминогруппа NR1R2, R1 и R2 - H, C1 - C6-алкил; азотсодержащее пятичленное гетероциклическое кольцо, которое выбирают из группы, включающей фталоилимид, имидазол, пирролидин, alk - ковалентная связь, метилен или алкилен, содержащий от 2 до 6 атомов углерода, R3, R4 и R5 -H, C1 - C6-алкил и их фармакологически приемлемые соли, причем в случае, когда R3, R4 и R5 - метил и alk-ковалентная связь, R не может обозначать диметиламиногруппу. Реагент I: производное карбоновой кислоты формулы R-alk-CH(y)-CO2R4, где R, alk и R4 имеют вышеуказанные значения, y - удаляемая группа. Реагент 2: соединение формулы H2C(CO2R3)P(O)(OR5)2, где R3 и R5 имеют вышеуказанные значения. Условия реакции: в среде органического растворителя в присутствии основания. 2 с. и 1 з.п.ф-лы, 1 табл.

ФОСФОНОКАРБОКСИЛАТНЫЕ СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ АНОРМАЛЬНОГО КАЛЬЦИЕВОГО И ФОСФАТНОГО МЕТАБОЛИЗМА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Изобретение относится к области медицины. Фармацевтические композиции содержат фармацевтически приемлемые носители и фосфонокарбоксилат или его фармацевтически приемлемую соль, имеющий структуру согласно формуле (I)где A выбран из группы, содержащей водород; галаген; SR; RSR; амино; гидрокси, и замещенный или незамещенный C- Cалкил; B означает NHи т.д. или A или B ковалентно связаны с Cдля образования моноциклического или бициклического кольца, имеющего структуру αПредложенные композиции обладают сильной антирезорбтивной костной активностью и полезны для лечения остеопороза и артрита. 4 с. и 7 з.п. ф-лы.

СПОСОБ СИНТЕЗА АМИНОАЛКИЛЕНФОСФОНОВОЙ КИСЛОТЫ

... 1. Способ синтеза аминоалкиленфосфоновой кислоты ее фосфонатных сложных эфиров, включающий следующие стадии:а) образования в присутствии альдегида или кетона и кислотного катализатора реакционной смеси посредством смешивания соединения (а.1.), содержащего по меньшей мере один фрагмент HNR1R2, или его соли с соединением (а.2.), содержащим один или несколько ангидридных фрагментов Р-О-Р, причем указанные фрагменты содержат один атом Р в степени окисления (+III) и один атом Р в степени окисления (+III) или (+V), где соотношение молей альдегида или кетона и фрагментов N-H составляет 1 или более, и где соотношение фрагментов N-H и ангидридных фрагментов Р-О-Р составляет 0,3 или более,и гдесоединение (а.1.), содержащее HNR1R2, характеризуется тем, что(а.1.1) R1 и R2 независимо выбраны из группы, состоящей из водорода, С1-С6алкила, С1-С6алкенила, С1-С6алкинила, С1-С6ацила, необязательно содержащего этиленненасыщенную двойную связь, и (мет)акрилоильного С1-С6-фрагмента, причем С1-С6-часть указанных ...

СПОСОБ ПОЛУЧЕНИЯ МОНОГИДРОПЕРФТОРАЛКАНОВ, БИС(ПЕРФТОРАЛКИЛ)ФОСФИНАТОВ И ПЕРФТОРАЛКИЛФОСФОНАТОВ

... 1. Способ получения моногидроперфторалканов, бис(перфторалкил)фосфинатов и перфторалкилфосфонатов, включающий, по крайней мере, обработку, по крайней мере, одного перфторалкилфосфорана, по крайней мере, одним основанием и, при желании, кислотой в пригодной реакционной среде. 2. Способ получения моногидроперфторалканов в соответствии с п.1, отличающийся тем, что, по крайней мере, один перфторалкилфосфоран взаимодействует с, по крайней мере, одним основанием (а) или органо-металлическим соединением в пригодном растворителе. 3. Способ получения бис(перфторалкил)фосфинатов и перфторалкилфосфонатов в соответствии с п.1, отличающийся тем, что, по крайней мере, один перфторалкилфосфоран взаимодействует с, по крайней мере, одним неорганическим основанием (б) в пригодном растворителе, бис(перфторалкил)фосфинаты и перфторалкилфосфонаты образовавшиеся в дополнение к моногидроперфторалканам превращают в соответствующие бис(перфторалкил)фосфиновые кислоты и перфторалкилфосфоновые кислоты, непосредственно ...

Способ синтеза альфа-аминоалкиленфосфоновой кислоты

Изобретение относится к способу синтеза альфа-аминоалкиленфосфоновой кислоты или ее сложного эфира, применяемых, например, для обработки воды, замедления процесса образования накипи, моющих присадок, комплексообразователей. Способ включает следующие стадии: а) получение реакционной смеси путем смешивания соединения, содержащего один или несколько ангидридных фрагментов Р-О-Р, причем указанные фрагменты содержат один атом Р со степенью окисления (+III) и другой атом Р со степенью окисления (+III) или (+V), альфа-аминоалкиленкарбоновой кислоты и кислотного катализатора, где указанное соединение, содержащее один или несколько ангидридных фрагментов Р-О-Р, которые содержат один атом Р в степени окисления (+III) и другой атом Р в степени окисления (+III) или (+V), выбирают из группы, состоящей из: тетрафосфорного гексаоксида, PO, PO, РО, тетрафосфорного декаоксида, тетраэтилпирофосфита, диметилфосфита и их комбинаций, и где указанная альфа-аминоалкиленкарбоновая кислота выбрана из группы, состоящей ...

ФОСФОНОКАРБОКСИЛАТНЫЕ СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ АНОРМАЛЬНОГО КАЛЬЦИЕВОГО И ФОСФАТНОГО МЕТАБОЛИЗМА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Изобретение относится к фармацевтическим композициям, содержащим фармацевтически приемлемые носители и фосфонокарбоксилат или его фармацевтически приемлемую соль, имеющий структуру согласно формуле I, приведенной в описании. Настоящее изобретение далее относится к новым фосфонокарбоксилатным соединениям и их фармацевтически приемлемым солям. Наконец, данное изобретение касается способов лечения и профилактики патологических состояний, характеризующихся анормальным кальциевым и фосфатным метаболизмом у человека и других млекопитающих. Эти способы включают введение человеку или другому млекопитающему при необходимости такого лечения безопасного и эффективного количества соединения или композиции по настоящему изобретению.

СЕРУСОДЕРЖАЩИЕ ФОСФОНАТНЫЕ СОЕДИНЕНИЯ, ИСПОЛЬЗУЕМЫЕ ДЛЯ ЛЕЧЕНИЯ АНОМАЛЬНОГО КАЛЬЦИЕВОГО И ФОСФАТНОГО ОБМЕНА ВЕЩЕСТВ, ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Изобретение относится к новым серусодержащим фосфонатным соединениям и новым тиозамещенным соединениям, включающим бифосфонаты, фосфоноалкилфосфонаты, фосфонокарбоксилаты и фосфоносульфонаты и их фармацевтически приемлемым солям и эфирам, а также к фармацевтическим композициям, содержащим безопасное и эффективное количество соединения данного изобретения и фармацевтически приемлемые наполнители, к способам лечения и предотвращения патологических состояний, характеризующихся аномальным кальциевым и фосфатным метаболизмом у человека и других млекопитающих, включая лечение или предотвращение остеспороза и артрита, особенно ревматоидного артрита и остеоартрита. Этот способ состоит во введении человеку или другому млекопитающему, нуждающемуся в таком лечении, безопасного и эффективного количества соединения или композиции данного изобретения или соединения и композиции, раскрываемых на его основе. Новые серусодержащие соединения данного изобретения имеют общую структурную формулу I, приведенную ...

СПОСОБ ИНГИБИРОВАНИЯ ОБРАЗОВАНИЯ ОТЛОЖЕНИЙ

... 1. Способ обработки воды для ингибирования образования отложений, например, отложений, содержащих барий, который включает добавление порогового количества ингибитора образования отложений, выбираемого из группы, включающей:i. аминокислоты, модифицированные алкилфосфоновыми кислотами, соответствующие следующей формуле:А-(В),в которой Асоответствует формулеHOOC-A-NH,в которой А независимо выбран из группы, включающей неразветвленные, разветвленные, циклические или ароматические С-С-углеводородные цепи, которые могут быть замещены неразветвленными, разветвленными, циклическими или ароматическими С-С-углеводородными группами, которые также могут быть замещены фрагментами ОН, СООН и/или NN, иВ представляет собой фрагмент алкилфосфоновой кислоты, содержащий в алкильной группе от 1 до 6 атомов углерода, и x представляет собой целое число, составляющее от 1 до 10, предпочтительно от 1 до 6,ii. аминокислоты, модифицированные алкилфосфоновыми кислотами, соответствующие следующей формулеA-B,в которой ...

ФУНКЦИОНАЛИЗИРОВАННЫЕ НАНОЧАСТИЦЫ, ИХ ПРИГОТОВЛЕНИЕ И ПРИМЕНЕНИЕ

... 1. Устойчивые комплексы, состоящие из оксидов металлов, железа, кобальта или их сплавов в форме наночастиц и бифункциональных соединений ! 2. Комплексы по п.1, где указанные оксиды металлов в форме наночастиц являются соединениями формулы: ! MIIMIII 2O4, ! где MII=Со, Ni, FeII, Zn, Mn и ! MIII=FeIII, Co, Al. ! 3. Комплексы по п.2, где указанные оксиды являются оксидами Fe2O3 типа магхемита. ! 4. Комплексы по п.3, где указанные оксиды выбирают из группы, состоящей из феррита кобальта CoFe2O4, магнетита FeFe2O4, магхемита Fe2O3. ! 5. Комплексы по п.1, где указанные бифункциональные соединения выбирают из группы, состоящей из тиолов, карбоновых кислот, гидроксамовых кислот, эфиров фосфорных кислот или их солей, имеющих алифатическую цепочку, содержащую вторую функциональную групп в конечном положении ω. ! 6. Комплексы по п.5, где указанную вторую функциональную группу выбирают из группы, состоящей из ОН, NR2, COOH, COOR3, где R3 обозначает щелочной металл или защитную органическую группу.

АЛКИНОВЫЕ И АЛКЕНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА СФИНГОЗИН 1-ФОСФАТА-1

... 1. Соединение, имеющее Формулу I, его энантиомеры, диастереоизомеры, гидраты, сольваты, кристаллические формы и индивидуальные изомеры, таутомеры или их фармацевтически приемлемые соли,где:«» представляет двойную связь «-CR=CR-» или тройную связь «-C≡C-»;A является Cарилом, гетероциклом, Cциклоалкилом или Cциклоалкенилом;B является Cарилом, гетероциклом, Cциклоалкилом или Cциклоалкенилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, Cарилом, гетероциклом, Cциклоалкилом, Cциклоалкенилом, NRRили гидроксилом;Rодинаково или независимо ...

Способ получения 2-хлорэтанфосфоновой кислоты

Способ получения кислот фосфора или их солей

Способ получения производных -фосфонометилглицина

Способ борьбы с фитопатогенными грибами

Branched aminoalkanephosphonic acids and phosphonic acid derivatives, i.e. compounds containing at least one alkyl substituent in the a-position of the phosphonic group are used as fungicides. They are particularly suitable for control of phytopathogenic fungi and for use as wood preservatives. 1-aminopropanephosphonic acid has been found very effective against several fungi and salts of the acids are also useful. The compounds can be used for example as seed-dressing agents and as foliar fungicides and they can be used in compositions with conventional solid and liquid carriers.

VERFAHREN ZUR HERSTELLUNG VON AMINOMETHANPHOSPHONSAEURE UND AMINOMETHYL-PHOSPHINSAEUREN

Aminomethanephosphonic acid and aminomethylphosphinic acids are interesting biologically active compounds or intermediates for the production of biologically active compounds. Such compounds having the formula (I), in which R<1> is OH, C1-C4-alkyl or phenyl, can be produced in a technically easy manner, by reacting with water at 80 to 300 DEG C compounds having the formula (II), in which R<2> is H, C1-C6-alkyl, benzyl, phenyl, if necessary substituted by C1-C4-alkoxy and/or halogen, and R<1> has the same meaning as above.

Chloroethane phosphonic acid derivs. prepn. - from vinyl acid derivs. and hydrogen chloride, intermediates for flame retardants, plant protecting agents and growth accelerators

Prepn. of phosphoric acid derivs. of formula (I): (where X is O or S, andY is Cl, except that when X is O, Y together with Y from another molecule can also be O) comprises reacting a vinyl phosphorus cpd. of formula (II): with HCl in the presence of N and/or P contg. organic cpds. (III) at elevated temps. NO 1-chloroethane phosphonic acid derivs. are formed. The process converts (II), which is formed as a by-prod. in previous prepns. of (I). (III) may be an amine, a heterocyclic N cpd., an acid amide, a quat. ammoniumor phosphonium salt, a tert. phosphine of an organic cpd. of 5-valent P. Reaction is at 50-180 (esp. 100-170 degree C).

PHOSPHONOMETHYL-GLYCINESTERANHYDRIDE UND DIESE VERBINDUNGEN ENTHALTENDE HERBIZIDE ZUBEREITUNGEN

SELBST-ÄTZENDE DENTALGRUNDIERUNG

Phosphonylationsprozess.

Elektronisches Schaltelement

Ein elektronisches Schaltelement (1), welche in dieser Reihenfolge eine erste Elektrode (16), eine molekulare Schicht (18), gebunden an ein Substrat, und eine zweite Elektrode (20) umfaßt wobei die molekulare Schicht im Wesentlichen aus Verbindungen der in Anspruch 1 angegebenen Formel I besteht, worin ein mesogener Rest über eine Abstandsgruppe (Sp) mittels einer Ankergruppe (G) an das Substrat gebunden ist, eignet sich zur Herstellung von Bauelementen (1) als memristive Vorrichtung zur digitalen Informationsspeicherung.

NEUE PHOSPHONATE UND IHRE VERWENDUNG ALS KATALYSATOREN ZUR HERSTELLUNG VON POLYISOCYANURATKUNSTSTOFFEN

Verwendung von Phenolen und Phenolderivaten als Arzneimittel mit fibrinogensenkender Wirkung

BETA-CHLORAETHANPYROPHOSPHONSAEURE UND IHRE VERWENDUNG ALS PFLANZENWACHSTUMSHORMON

Phosphorgruppenhaltige Carbonsäurederivate mit organisch polymerisierbaren Gruppen

Die vorliegende Erfindung betrifft Verbindungen der Formel (I) DOLLAR A [(R·1·)(R·2·)P(O)-(CHR·3·)-(CHR·4·)-(CHR·5·)¶m¶-C(O)X-]¶n¶{B}, DOLLAR A worin die Reste und Indices die folgende Bedeutung haben: DOLLAR A X ist O, NH, NR·6· oder S, DOLLAR A R·1·, R·2· sind unabhängig voneinander Wasserstoff oder ggf. substituiertes Alkyl, Alkenyl, Aryl, Alkylaryl oder Arylalkyl oder ggf. substituiertes Alkoxy, Alkenyloxy, Aryloxy, Alkylaryloxy oder Arylalkyloxy, DOLLAR A R·3·, R·4·, R·5· und R·6· sind unabhängig voneinander Wasserstoff oder ggf. substituiertes Alkyl, Alkenyl, Aryl, Alkylaryl oder Arylalkyl, DOLLAR A {B} ist ein geradkettiger oder verzweigter Rest mit mindestens einer organisch polymerisierbaren Gruppe und mindestens 2 Kohlenstoffatomen, DOLLAR A m ist eine ganze Zahl von 0 bis 20, DOLLAR A n ist eine ganze Zahl von 1 bis 20, DOLLAR A Homo- oder Copolymerisate aus oder unter Verwendung dieser Verbindungen sowie ein Verfahren zu ihrer Herstellung. Die Bindungen zwischen der phosphorhaltigen ...

PRODUCTION OF HALOGENATED ORGANIC PHOSPHORUS COMPOUNDS

... 1365809 2-Haloethylphosphonic acids GAF CORP 8 March 1972 [26 March 1971] 10726/72 Heading C2P 2-Chloro- or 2-bromoethylphosphonic acid is prepared by hydrolysing an ester of formula where X is chlorine or bromine and R 1 and R 2 are each C 1-8 alkyl, haloalkyl or hydroxyalkyl or together represent C 2-6 alkylene, optionally having -OH and/or halogen substituent(s), forming a heterocycle with the P atom, at an elevated temperature with aqueous HCl maintained at a concentration of at least 23% by injection of hydrogen chloride under pressure during the reaction. Preferably R 1 and R 2 are each 2-chloroethyl. The reaction mixture may contain between 5 and 10 moles of water per mole of ester. Preferably the reaction is carried out at 100-145‹ C. The products may be used as plant-growth regulating agents. In comparative examples the hydrolysis of bis- (2-chloroethyl) 2-chloroethyl phosphonate with aqueous HCl is carried out at atmospheric pressure and under autogenous pressure without addition ...

PROCESS FOR CONTINUOUS SEPARATION OF COMPONENTS OF A GAS OR LIQUID MIXTURE OR A SOLUTION

... 1462293 Chromatography; ion-exchange MAGYAR ASVANYOLAJ ES FOLDGAZ KISERLETI INTEZET 17 May 1974 [18 May 1973] 22004/74 Headings B1H, B1J and B1L In a process for the continuous separation of a fluid (liquid or gaseous) mixture on a solid charge capable of the temporary binding of one or more components of the mixture, using operative and pressure-balancing zones and periodically shifting said zones, one or more columns form a closed system for gas or liquid circulation, the top of the column being connected to its bottom or the top of each column being connected to the bottom of a respective one of the other columns, at least four column sections of the same length and cross-section being formed in said closed system by using means to introduce and, respectively, remove the liquids, slurries or gases and to support the solid charge, each of said column sections being filled with the same solid charge in identical amounts, filling at most 85% of the volume of the sections, operative and ...

Improvements in alkylene polyamino phosphonic acids and method of producing same

The invention comprises as new compounds those having the structure wherein Alk represents an alkylene radical CnH2n containing two to six carbon atoms, and the alkali metal salts thereof. The compounds are sequestering agents for metal ions in aqueous solutions being capable of chelating and complexing mono- and polyvalent metal ions to form non-ionic compounds. The compounds may be prepared by reacting a chloromethyl phosphonic acid with an alkylene diamine diacetic acid in heated alkaline aqueous solution, preferably at a pH of 10 to 11. In this process, the acetic acid groups of the amino acid may be immobilised by chelating the same with a divalent heavy metal such as copper which may be subsequently removed by precipitation with hydrogen sulphide, the substitution reaction with the chloromethyl phosphonic acid being thus facilitated. In an example of this procedure one mol. of ethylene diamine diacetic acid and one mol. of freshly precipitated copper hydroxide ...

PHOSPHORUS-CONTAINING HMG-COA REDUCTASE INHIBITORS,NEW INTERMEDIATES AND METHOD

Amine derivatives containing a phosphonic,phosphonous or phosphinic acid moiety

Production of fluoroethylene derivatives

... 1:1 Adducts (with respect to the ethylenic or acetylenic bond) are obtained by reacting an ethylenically or acetylenically unsaturated organic silicon compound containing at least one hydrogen atom, with an iodofluoroalkane having at least one -CF2CF2- group which is an a -iodoperfluoroalkane, a -iodoperfluorochloroalkane, a - iodo - o - hydroperfluoroalkane, a - diodo - o - hydroperfluorochloroalkane, a - iodo - o - haloperfluoroalkane (the halogen being Cl, Br or I) or an a -iodo-o -haloperfluorochloroalkane (the halogen being Br or I), at a temperature above 170 DEG C., a pressure below 5 atmospheres and residence time below 2 hours. In examples: (7) C10F21I is reacted with CH2 = CHSiCl3. The product is dissolved in methanol or ethylene glycol and the solution is hydrogenated or treated with NaHSO3 to give C10F21CH2CH2Si(OR)3, where R is CH3 or HOCH2CH2. R may also be derived from triethyleneglycol. (14) C10F21I is reacted with CH2 = CHSiCl2.CH3, the product dissolved in tetrahydrofuran ...

Lactam containing compounds

Phosphonamide substituted lactams of the formula are disclosed. These compounds are useful as hypotensive agents.

ISOMERIC O-PHOSPHONYLMETHYL DERIVATIVES

COMPOUNDS

PEPTIDYL DERIVATIVES

Aminoalkylene Phosphonic Acid Derivatives

PHOSPHONYLATION PROCESSES

Anticorrosive pigments

Preparation of hydroxymethylphosphonic acid

Hydroxymethylphosphonic acid is prepared by reacting phosphorus trichloride with paraformaldehyde and water, the paraformaldehyde being present in an amount from about a stoichiometric quantity to about a 0.5 mole excess, preferably in the presence of HCl. Alternatively, orthophosphorous acid may be used instead of water and PCl3. The reaction may be carried out under atmospheric pressure in a temperature range between 50 DEG and 150 DEG C. A preferred temperature range is between 90 DEG and 120 DEG C.

Method of Preparing Phosphonoalkylene Ammonium Compounds

Amino substituted phosphonic acid esters

Phosphonic acid esters of formula where R is C8- 24 tert-alkyl, R1 is H, C1- 8 alkyl, C8- 18 alkenyl, benzyl or (C1- 18 alkyl) - benzyl, R2 is C1- 4 alkyl, phenyl or cresyl, R3 is H or C1- 7 alkyl, and R4 is H or C1- 4 alkyl, are used as anti-rust additives for distillate fuels, e.g. gasolines, jet and diesel fuels and furnace oils, and as antiwear additives for mineral or synthetic oils and greases.ALSO: Novel compounds of Formula 1 where R is C8- 24 tert.-alkyl, R1 is H, C1- 8 alkyl, C8- 18 alkenyl, benzyl or (C1- 18 alkyl)-benzyl, R2 is C1- 4 alkyl, phenyl or cresyl, R3 is H or C1- 7 alkyl, and R4 is H or C1- 4 alkyl are prepared b (A) reacting HBr or HCl (dry or aqueous with azeotropic removal of water) or water alone under pressure with a compound II or (B) reacting a hydrobromide or hydrochloride of an azomethine CH2 = NR with a phosphite (R2O)2POH. In a modification of (A) using a compound II in which R1 is H, the hydrohalide ...

STABILIZATION OF PHOTOGRAPHIC SILVER HALIDE MATERIALS

... 1,214,982. Photographic anti-foggants. GEVAERT-AGFA N.V. April 19, 1968 [May 18, 1967; Oct.19, 1967], Nos.23048/67 and 47731/67. Heading G2C. Silver halide emulsions are developed in the presence of at least one Co (II) or Mn (II) chelate of a polyamino - polycarboxylic acid or watersoluble salt thereof, which acts as an anti-foggant/ stabilizer. Preferably the chelate is derived from an acid of formula: - (in which L is optionally substituted alkylene or cycloalkylene or alkylene interrupted by one or more hetero atoms, X is 0-2, R is optionally substituted C 1-5 lower alkylene, and R 1 and R 2 are each optionally substituted C 1 -5 alkyl or aryl groups). The chelate is preferably added to the silver halide layer in an amount of 0À1-20g. per mole of silver halide, or to a non-photo-sensitive layer, e.g. gelatin anti-stress overcoat layer, in an amount of 10-1000 mg. m 2 , and may be used in conjunction with a conventional hydroxy azaindolizine stabilizer and an onium or poly ( ...

Process for the production of methylaminomethylphosphonic acid esters and of the corresponding acid

A process for the production of methylaminomethylphosphonic acid and its esters is disclosed. It comprises heating trimethylhexahydro-s-triazine with at least 3 moles of a sterically hindered secondary phosphite and if desired converting the resulting diester or salt thereof into a corresponding hemiester or the methylaminomethylphosphonic acid. The invention also includes as novel compounds the diesters and hemiesters obtainable by the defined process.

N-ARYLSULPHONYL CARBAMATES

PROSTAGLANDIN DERIVATIVES

HYDROXYALIPHATIC ESTERS OF N-PHOSPHONOMETHYL GLYCINE AND THEIR USE AS HERBICIDES

... 1480019 Esters of N-phosphonomethyl glycine and salts thereof MONSANTO CO 4 Aug 1975 [5 Aug 1974] 32503/75 Heading C2P The invention comprises compounds of the formula wherein R is an alkylene or alkoxy substituted alkylene radical containing up to 18 carbon atoms, R1 is alkylene or alkoxy substituted alkylene each alkylene group containing 2 to 4 carbon atoms, and each alkoxy group, if present in R or R1 containing 1 to 4 carbon atoms, m is 0, 1, 2 or 3, M is H and M1 is H, alkali metal, ammonium, organic ammonium, or an equivalent of an alkaline earth metal. They may be obtained by reacting N-phosphonomethyl glycine with an excess (over stoichiometric) of a dihydric alcohol in the presence of an acid catalyst. The preferred acids are volatile acids, e.g. HCl and trifluoroacetic acid. The organic ammonium salts are preferably derived from amines having a molecular weight below 300 and such amines may be alkylamines, alkenyl amines, alkylene diamines or alkanolamines ...

Heterocyclic THR-# receptor agonist compound and preparation method and use therefor

A chemical compound shown in formula (I) below and an isomer thereof or a pharmaceutically acceptable salt thereof. The compound improves THR-β agonistic activity while also improving selectivity for THR-α, thereby improving pharmaceutical quality.

Substituted bisphenyl butanoic nep 'neutral endopeptidase' inhibitors

Phosphorus functional antimicrobal coatings for metal surfaces

Organophosphorous compounds and the use thereof.

The invention relates to organophosphorous compounds of general formula (i)wherein a corresponds to general formula (ii), wherein one or more of the carbon atoms, selected from the group c3, c4, c5 and their respective substituents can be omitted, and at least one substituent of b1 to b10 is a c3-8 cycloalkyl (c0-9)alkyl group, wherein both the c3-8 cycloalkyl group and the c0-9 alkyl group can have one or more double bonds and one or two carbon atoms of the cycloalkyl group can be substituted by nitrogen, oxygen or sulfur atoms, and wherein both the cycloalkyl group and the alkyl group can be substituted by hydrogen, halogen amine, oxo groups with branched or unbranched c1-9 alkyl groups and c2-9 alkenyl groups, wherein the c1-9 alkyl groups and c2-9 alkenyl groups can be substituted by hydrogen, hydroxy, amine, halogen, and oxo groups. The invention further relates to pharmaceutical preparations containing said compounds and to the use thereof for the therapy and prophylaxis of infectious ...

Phosphorous organic compounds and their use.

The invention relates to phosphourous organic compounds of general formula (I), wherein B is an ether group of formula (II)or a keto group of formula (III)or a pentagonal or hexagonal cyclic compound. The invention also relates to the use of these compounds for producing drugs for treatment or prevention of human or animal infections due to viruses, bacteria, fungi or parasites, as well as their use as fungicide, bactericide and herbecide in plants.

Substituted bisphenyl butanoic nep 'neutral endopeptidase' inhibitors

Use of aminophosphonates like weedkillers.

Organophosphorous compounds and the use thereof.

New derivatives of nitrosourée and their preparation.

Dipeptides substituted, proceeded for their preparation and pharmaceutical compositions the container and their use for inhibition of the encéphalinase.

Retarders of growth and weedkillers.

Method of preparation of derived from hydrocarbon acids hydroxy-aminophosphonic.

Phytotoxic compositions containing N-phosphonométhyl-glycine.

Method of preparation of derived from N-phosphono-méthylglycine, new products thus obtained and their use as weedkiller post-emergent.

O-aryl N-phosphonométhylglycinonitriles and their use as weedkillers.

Substituted bisphenyl butanoic nep 'neutral endopeptidase' inhibitors

Phosphorus functional antimicrobal coatings for metal surfaces

Phosphorus organic compounds and their use

Phosphorus functional antimicrobal coatings for metal surfaces

Organophosphorous compounds and the use thereof

PROCEDURE FOR THE PRODUCTION OF NEW PHOSPHONIC ACIDS

PROCEDURE FOR THE PRODUCTION OF NEW PEPTID DERIVATIVES

FLAME RETARDING COMPOSITIONS FROM METHANE PHOSPHONIC ACID, BORIC ACID AND ORGANIC BASE

PROCEDURE FOR THE PRODUCTION OF NEW PHOSPHONVERBINDUNGEN

CONTRAST MEANS WITH MORE HIGHLY RELAXIVITÄT FOR USE CONTAINING IN THE MAGNET RESONANCE IMAGE REPRESENTATION (MRI), A CHELATBILDENDE GROUP WITH POLYHYDROXYLIERTEN SUBSTITUENTS

PFLANZENWACHSTUMREGULIERENDES MITTEL

VERFAHREN ZUR HERSTELLUNG VON NEUEN PEPTID- DERIVATEN

HERBIZIDE ZUBEREITUNG

VERFAHREN ZUR HERSTELLUNG NEUER DERIVATE DES 11-DESOXY PROSTAGLANDINS F2

GIPSMASSEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN HYDROXYLAMINO-HYDROCARBYLPHOSPHONSAEUREDERIVATEN

PROCEDURE FOR THE PRODUCTION OF NEW N-SULFOHYDROXY-ALKANE-AMINOALKAN-PHOSPHONIC ACIDS AND OF THEIR ALKALI SALTS

PROCEDURE FOR THE PRODUCTION OF NEW N-SULFOALKAN AMINOALKANPHOSPHONSAEUREN AND THEIR ALKALI SALTS

PROCEDURE FOR THE PRODUCTION OF SUBSTITUTED ALPHA AMINO ACIDS

PROCEDURE FOR THE PRODUCTION OF NEW PEPTID DERIVATIVES

HERBICIDE MEANS

PROCEDURE FOR THE PRODUCTION OF NEW PEPTIDDERIVATEN AND THEIR SALTS

HERBICIDES PREPARATION

PHOSPHONO ARYLETHANOLAMIN CONNECTIONS WITH ANTIHYPERGLYKÄMI AND/OR ANTIOBESER EFFECT

RE-USABLE PRINTING FORM

HERBICIDES PREPARATION

HERBICIDES PREPARATION

PROCEDURE FOR THE PRODUCTION OF N-PHOSPHONOMETHYLGLYCIN

PROCEDURE FOR THE PRODUCTION OF NEW PHOSPHON SAEUREN

NEW PHOSPHONOBERNSTEINSÄUREDERIVATE, PROCEDURES FOR THEIR PRODUCTION AND THESE CONNECTIONS CONTAINING DRUGS

MIKROBIZIDE MEANS.

PROCEDURE FOR THE PRODUCTION OF ALPHAAMINOALKYLPHOSPHON AND OF ALPHA AMINOALKYL PHOSPHINE|UREN.

Method for the manufacture of phosphonoalkyl iminodiacetic acids

An improved method for the manufacture of phosphonoalkyl iminodiacetic acid (PAIDA) is disclosed. The iminodiacetic acid starting material is reacted with a considerable amount, in excess of stoichiometric requirements, of phosphorous acid to thereby yield a reaction medium insoluble reaction product which can be separated from the reaction medium. In a particularly preferred approach, the phosphorous acid is prepared in situ starting from liquid P 4 O 6 .

Compounds (cystein based lipopeptides) and compositions as tlr2 agonists used for treating infections, inflammations, respiratory diseases etc.

The invention provides a novel class of compounds viz. generally lipopeptides like Pam3CSK4, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness a vaccine.

Beta-Hydroxy-Gamma-Aminophosphonates and Methods for the Preparation and Use Thereof

The present invention provides β-hydroxy-γ-aminophosphonates, β-amino-γ-aminophosphonates, and analogs thereof that inhibit carnitine acyltransferases. The invention also provides compositions comprising these β-hydroxy-γ-aminophosphonates, β-amino-γ-aminophosphonates, and analogs, and methods of the use of such compounds and compositions in the treatment, amelioration or prevention of pathological conditions, diseases or disorders that are linked with fatty acid metabolism, such as non-insulin dependent diabetes or obesity. The invention also provides processes for the preparation of such compounds and compositions. 1114-. (canceled)121. (canceled)122. The method of claim 118 , further comprising administering to said patient one or more additional therapeutic agents.123. The method of claim 122 , wherein said one or more additional therapeutic agents is selected from the group consisting of anticholesterolemics claim 122 , anticoagulants claim 122 , anti-obesity or anti-diabetic drugs claim 122 , and combinations thereof.124. (canceled)125. The method of claim 118 , wherein said disorder or condition is selected from the group consisting of non-insulin dependent diabetes mellitus claim 118 , obesity claim 118 , hyperlipoproteinemia claim 118 , hyperlipidemia claim 118 , myocardial dysfunction claim 118 , renal anemia and Alzheimer's disease.126. The method of claim 125 , wherein said disorder or condition is non-insulin dependent diabetes.127. The method of claim 125 , wherein said disorder or condition is obesity.128. The method of claim 118 , wherein Z is O.129. The method of claim 128 , wherein:R is methyl;{'sup': '1', 'Ris selected from the group consisting of n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, benzyl, and phenyl;'}{'sup': 2', '3, 'Rand Rare independently selected from the group consisting hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, isopenyl, benzyl, and phenyl; and'}{'sup': '4', 'Ris ...

METHOD FOR THE MANUFACTURE OF PHOSPHONOALKYL IMINODIACETIC ACID

An improved method for the manufacture of phosphonoalkyl iminodiacetic acid MPO—X—N—(CHCOOM)wherein X is a Clinear or branched alkyl group; and M is selected from hydrogen, alkali, earth-alkali, ammonium and protonated amine is disclosed. The iminodiacetic acid starting material is reacted with a substantially stoichiometric amount of phosphorous acid, in the presence of a large excess of phosphoric acid to thereby yield a reaction medium insoluble reaction product (PAI-DA) which can be separated from the reaction medium. In a particularly preferred approach, the phosphorous acid is prepared in situ starting from liquid PO. 1. A method for the manufacture of a phosphonoalkyl iminodiacetic acid or a salt thereof having the formula:{'br': None, 'sub': 2', '3', '2', '2, 'MPO—X—N—(CHCOOM)'}{'sub': '1-6', 'wherein X is a Clinear or branched alkyl group; and M is selected from hydrogen, alkali, earth-alkali, ammonium and protonated amine; comprising the steps ofa) reacting iminodiacetic acid with phosphorous acid whereby the phosphorous acid is used in a molar ratio of phosphorous acid:iminodiacetic acid of from 0.7:1 to 1.5:1 in the presence of phosphoric acid whereby the molar ratio of phosphoric acid:phosphorous acid is of from 9:0.8 to 1:1 and formaldehyde in a molar ratio formaldehyde:iminodiacetic acid of from 2:1 to 0.5:1, at a temperature in the range of from 45° C. to 200° C. for a period of from 1 minute to 10 hours, to thereby yield a substantially reaction medium insoluble product;b) separating the insoluble reaction product from the reaction medium, and optionally water washing the insoluble reaction product.2. The method in accordance with wherein X is a Calkylene group.3. The method in accordance with wherein the molar ratio of phosphoric acid:phosphorous acid is from 6:1 to 1.2:1 and wherein the molar ratio of phosphorous acid:iminodiacetic acid is from 0.8:1 to 1.3:1.4. The method in accordance with wherein the molar ratio of phosphoric:phosphorous is ...

SUPERACID FUNCTIONAL COMPOUNDS

The invention relates to a novel synthesis method for forming superacid functional molecules that include monomers, as well as new polymers and copolymers formed from the monomers, and uses for these superacid molecules, polymers, and copolymers. The superacid molecules have an alpha,alpha-difluorosulfonic acid functionality that can be obtained by a reaction between various Grignard reagents and an alkyl(2-fluorosulfonyl)-1,1-difluoroacetate, such as methyl(2-fluorosulfonyl-1,1-difluoroacetate. The molecules, polymers and copolymers would be expected to have enhanced ion conductivity, and would be useful in a variety of applications, including as ion-conductive materials, surfactants, and ion exchange resins. 3. The composition of where one of the groups claim 2 , R claim 2 , is vinylic claim 2 , and the other groups Rare hydrogen.4. The composition of where Ris chosen from: sulfonate claim 1 , sulfinate claim 1 , or sulfonyl halide.5. The composition of where one of the groups claim 2 , R claim 2 , is vinylic claim 2 , the other groups Rare hydrogen claim 2 , and Ris sulfonyl halide or sulfonate.7. The composition of where the group claim 6 , Ris selected from the group consisting of: sulfonate claim 6 , sulfinate claim 6 , and sulfonyl halide.9. The copolymer of having a weight average molecular weight of 500 kg/mol or less.10. The copolymer of claim 8 , comprising three or more monomer units.14. A polymer blend comprising from 5 to 95 weight percent of said homopolymer or copolymer composition of claim 8 , with from 5 to 95 weight percent of a matrix polymer.15. The polymer blend of claim 13 , comprising a blend of at least two different sulfonated polyelectrolytes claim 13 , each comprising from 5 to 95 weight percent of said blend.16. The polymer blend of claim 13 , wherein said matrix polymer is fluorinated.17. The polymer blend of claim 15 , wherein said matrix polymer comprises a poly(vinylidene fluoride) homopolymer or copolymer.18. The polymer blend of ...

Sulfinylbenzyl and thiobenzyl derivatives as sphingosine 1-phosphate (s1p) receptor modulators

The present invention relates to novel thiobenzyl and sulfinylbenzyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Method of scale inhibition

A method is disclosed to inhibit scale formation in aqueous systems whereby a threshold amount of a scale inhibiting agent, represented by an aminoacid alkylphosphonic acid, is added to the aqueous system. The aminoacid moiety can be represented by α-species or by species having, at least, two or more carbon atoms between the carboxylic moiety and the amine group. These aminoacid based inhibitors exhibit unusually superior performance and system acceptability compared to leading state-of-the-art inhibitors.

Bifunctional chelating agents

A chelating agent, a metal-chelate, and a contrast agent are provided, wherein the chelating agent comprises a compound of structure (I) wherein R 1 , R 2 , R 3 , R 8 , R 7 , R′ 7 R′ 1 , R′ 2 , R′ 3 and R 8 ′ are selected from a hydrogen, a protected C 1 -C 3 hydroxyalkyl group, a C 1 -C 3 alkyl group; R 4 and R′ 4 are selected from a hydrogen, a hydroxyl group, a protected hydroxy group, a protected C 1 -C 3 hydroxyalkyl group, a C 1 -C 3 alkyl group; n is an integer between 0 and 4; R 5 and R′ 5 are selected from a hydrogen, a protecting group selected from the group consisting of C 1 -C 30 aliphatic radicals, C 3 -C 30 cycloaliphatic radicals, C 2 -C 30 aromatic radicals; R 9 and R′ 9 are selected form a hydrogen or a protecting group selected from the group consisting of C 1 -C 30 aliphatic radicals, C 3 -C 30 cycloaliphatic radicals, C 2 -C 30 aromatic radicals, m is an integer between 0 and 10; and at least one of R 7 and R′ 7 is acidic group or a protected acidic group.

HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE

Compounds represented by formula (I): 122-. (canceled)25. A method according to claim 23 , wherein R1 claim 23 , R2 claim 23 , R3 claim 23 , and R4 are each independently a hydrogen atom claim 23 , a nitro group claim 23 , or a halogeno group.27. A method according to claim 23 , wherein X is a lower alkylene group optionally having substituent(s) or a lower alkenylene group optionally having substituent(s) claim 23 , wherein said substituent(s) is selected from the group consisting of a halogeno group claim 23 , a hydroxyl group claim 23 , an amino group claim 23 , a lower alkyl group claim 23 , a lower alkoxyl group claim 23 , and a lower acyl group.28. A method according to claim 23 , wherein Y is a carbonyl group or a sulfonyl group.30. A method according to claim 29 , wherein R60 is a carboxyl group claim 29 , a sulfo group claim 29 , a lower alkoxycarbonyl group claim 29 , or a hydroxyl group claim 29 ,D is a lower alkylene group optionally having substituent(s), wherein said substituent(s) is selected from the group consisting of a halogeno group, a hydroxyl group, a thiol group, an amino group, a guanidino group, a carboxyl group, a sulfo group, a lower alkoxyl group, a lower alkylthio group, a lower alkylamino group, a lower acylamino group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkylsulfonylamino group, an arylsulfonylamino group optionally having substituent(s), an aryl group optionally having substituent(s), a heterocyclic group optionally having substituent(s), and an oxo group, andR70 is a hydrogen atom, a hydroxyl group, a lower alkyl group optionally having substituent(s), or a lower alkoxyl group optionally having substituent(s),or R70 and D may be bonded to form a cyclic amino group optionally having substituent(s).31. A method according to claim 23 , wherein R1 claim 23 , R2 claim 23 , R3 claim 23 , and R4 are each independently a hydrogen atom claim 23 , a nitro group claim 23 , or a fluorine atom ...

QUINONES HAVING HIGH CAPACITY RETENTION FOR USE AS ELECTROLYTES IN AQUEOUS REDOX FLOW BATTERIES

We disclose quinone compounds and related species (Formula I) that possess significant advantages when used as a redox active material in a battery, e.g., a redox flow battery. In particular, the compounds provide redox flow batteries (RFBs) with extremely high capacity retention. For example, RFBs of the invention can be cycled for 500 times with negligible loss of capacity, and such batteries could be employed for years of service. Thus, the invention provides a high efficiency, long cycle life redox flow battery with reasonable power cost, low energy cost, and all the energy scaling advantages of a flow battery. 2. The battery of claim 1 , wherein Xand Xare O.3. The battery of or claim 1 , wherein each of R-Ris independently H; halo; optionally substituted Calkyl; —X-L-C(O)O—Y; or —X-L-C(O)O—Y.4. The battery of any one of - claim 1 , wherein Ris —X-L-C(O)O—Yand Ris —X-L-C(O)O—Y.5. The battery of any one of - claim 1 , wherein Yand Yare H.6. The battery of claim 1 , wherein Xand Xare O.7. The battery of claim 6 , wherein each of R-Ris independently H; halo; optionally substituted Calkyl; —X-L-P(═O)(OY); or —X-L-P(═O)(OY).8. The battery of or claim 6 , wherein Ris —X-L-P(═O)(OY)and Ris —X-L-P(═O)(OY).9. The battery of any one of - claim 6 , wherein Yand Yare H.16. The battery of any one of - claim 6 , wherein the second redox active material is the hydroquinone of formula I claim 6 , which is oxidized to the corresponding quinone during discharge.17. The battery of any one of - claim 6 , wherein the pH of the second aqueous electrolyte is 7.18. The battery of claim 17 , wherein the pH is from 8 to 13.19. The battery of any one of - claim 17 , wherein the first redox active material comprises bromine claim 17 , chlorine claim 17 , iodine claim 17 , oxygen claim 17 , vanadium claim 17 , chromium claim 17 , cobalt claim 17 , iron claim 17 , aluminum claim 17 , manganese claim 17 , cobalt claim 17 , nickel claim 17 , copper claim 17 , or lead.21. The compound of claim ...

EMULSIFIER FOR EMULSION POLYMERIZATION

An emulsifier for emulsion polymerization contains a compound represented by the following general formula (I). 2. (canceled)3. The emulsifier for emulsion polymerization according to claim 1 , wherein in the general formula (I) claim 1 , X represents a hydrogen atom or SOM claim 1 , wherein M represents a hydrogen atom claim 1 , an alkali metal atom claim 1 , an alkaline earth metal atom claim 1 , an ammonium residue claim 1 , or an alkanolamine residue claim 1 , and A represents an alkylene group having 2 carbon atoms. The present invention relates to an emulsifier to be used in an emulsion polymerization step, more particularly relates to an emulsifier for emulsion polymerization, which can enhance the stability of a polymer dispersion, and also enhance the physical properties of a polymer film obtained from the polymer dispersion.Heretofore, as emulsifiers for emulsion polymerization, anionic surfactants such as soaps, sodium dodecylbenzene sulfonate, polyoxyethylene alkyl phenyl ether sulfate ester salts, and polyoxyethylene alkyl ether sulfate ester salts; and nonionic surfactants such as polyoxyethylene nonyl phenyl ethers and polyoxyethylene alkyl ethers have been used. However, a polymer film obtained from a polymer dispersion using any of the above emulsifiers has problems that the emulsifier used remains in a free form in the polymer film, and therefore, the water resistance and the adhesiveness of the film are poor, etc. Therefore, as measures for the problems, a lot of reactive emulsifiers having a copolymerizable unsaturated group have been proposed (for example, PTL 1 to PTL 3).A reactive emulsifier having an acrylic group or a methacrylic group as a copolymerizable unsaturated group, which has been proposed in the prior art, has high copolymerizability with a monomer, but has a problem that the polymerization stability during emulsion polymerization is deteriorated. For example, agglomerates during emulsion polymerization are increased, particles ...

Substituted bisphenyl butanoic phosphonic acid derivatives as nep inhibitors

The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.

AMINO- OR AMMONIUM-CONTAINING SULFONIC ACID, PHOSPHONIC ACID AND CARBOXYLIC ACID DERIVATIVES AND THEIR MEDICAL USE

The present invention relates to amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives, in particular the compounds of formula 1, 2, 3, 4, 5 or 6, and their medical use, including their use in the treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder.

S1PR2 ANTAGONISTS AND USES THEREFOR

Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are (Z)-2-cyano-1-(2,6-dichloropyridin-4-yl)-3-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis. 2. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein:{'sub': 1', '12', '12, 'Gis CRand Ris H; and,'}{'sub': 'd', 'Ris H.'}3. The compound of claim 2 , selected from the group consisting of:(E)-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)-1-methylguanidine;(E)-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-ethyl-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine;(E)-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)-1-propylguanidine;(E)-1-butyl-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine;(E)-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-isopropyl-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine;(E)-1-benzyl-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine; and,a diastereomer of the foregoing, wherein the cyano group is in the (Z) form; or the pharmaceutically acceptable salt of any of the foregoing.4. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein:{'sub': 1', '12', '12, 'Gis CRand Ris H; and,'}{'sub': 'c', 'Ris H.'}5. The compound of claim 4 , selected from the group consisting of:(Z)-2-cyano-1-(2,6-dichloropyridin-4-yl)-3-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)-1-methylguanidine;(Z)-2-cyano-1-(2,6-dichloropyridin-4 ...

Beta-hydroxy-gamma-aminophosphonates for Treating Immune Disorders

The present disclosure provides methods of treating, ameliorating, or preventing immune disorders, allergic disorders, or inflammatory disorders, or combinations thereof, or providing hepatoprotection in subject. In one aspect, the method comprises administering to a subject a therapeutically effective amount of a β-hydroxy-γ-aminophosphonate or β-amino-γ-aminophosphonate. 2. The method of claim 1 , wherein a compound having Formula I claim 1 , or a pharmaceutically acceptable hydrate claim 1 , crystalline form or amorphous form thereof claim 1 , or a stereoisomer thereof claim 1 , is administered to said subject.5. The method of claim 4 , wherein X is iodide.6. The method according to claim 1 , where said compound having Formula I or said compound having Formula II is administered to said subject as part of a pharmaceutical composition comprising one or more pharmaceutically acceptable excipients.7. The method according to claim 1 , wherein the production of T helper cells is stimulated.8. The method according to claim 1 , wherein the production of cytotoxic T cells is stimulated.9. The method according to claim 1 , wherein the production Tcells is stimulated.11. The method according to claim 10 , wherein a compound having Formula I claim 10 , or a pharmaceutically acceptable hydrate claim 10 , crystalline form or amorphous form thereof claim 10 , or a stereoisomer thereof claim 10 , is administered to said subject.14. The method according to claim 13 , wherein X is iodide.15. The method according to claim 10 , where said compound having Formula I or said compound having Formula II is administered to said subject as part of a pharmaceutical composition comprising one or more pharmaceutically acceptable excipients.16. The method according to for the treatment of an immune disorder.17. The method according to claim 16 , wherein said immune disorder is an autoimmune disorder.18. The method according to claim 10 , wherein said immune disorder claim 10 , allergic ...

Disubstituted aryl oxy derivatives as sphingosine-1 phosphate receptors modulators

The present invention relates to aryl oxy derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

ARYL DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS

The present invention relates to aryl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors 11. A compound according to which is selected from:3-{[9-(3-Chlorophenyl)-10-phenyldecyl]amino}propanoic acid;(3-{[9-(3-Chlorophenyl)-10-phenyldecyl]amino}propyl)phosphonic acid;3-{[8-(3,5-Difluorophenyl)-9-(3,4-dimethylphenyl)nonyl]amino}propanoic acid;(3-{[8-(3,5-Difluorophenyl)-9-(3,4-dimethylphenyl)nonyl]amino}propyl)phosphonic acid;(3-{[8-(3-Chlorophenyl)-9-(3,4-dimethylphenyl)nonyl]amino}propyl)phosphonic acid;3-{[8-(3-Chlorophenyl)-9-(3,4-dimethylphenyl)nonyl]amino}propanoic acid;(3-{[7-(3-Chlorophenyl)-8-(3,4-dimethylphenyl)octyl]amino}propyl)phosphonic acid; and(3-{[9-(3-Chlorophenyl)-10-(3,4-dimethylphenyl)decyl]amino}propyl)phosphonic acid.12. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluents or carrier.13. A pharmaceutical composition according to wherein the compound is which is selected from:3-{[9-(3-Chlorophenyl)-10-phenyldecyl]amino}propanoic acid;(3-{[9-(3-Chlorophenyl)-10-phenyldecyl]amino}propyl)phosphonic acid;3-{[8-(3,5-Difluorophenyl)-9-(3,4-dimethylphenyl)nonyl]amino}propanoic acid;(3-{[8-(3,5-Difluorophenyl)-9-(3,4-dimethylphenyl)nonyl]amino}propyl)phosphonic acid;(3-{[8-(3-Chlorophenyl)-9-(3,4-dimethylphenyl)nonyl]amino}propyl)phosphonic acid;3-{[8-(3-Chlorophenyl)-9-(3,4-dimethylphenyl)nonyl]amino}propanoic acid;(3-{[7-(3-Chlorophenyl)-8-(3,4-dimethylphenyl)octyl]amino}propyl)phosphonic acid; and(3-{[9-(3-Chlorophenyl)-10-(3,4-dimethylphenyl)decyl]amino}propyl)phosphonic acid. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/866,142 filed Aug. 15, 2013, the disclosure of which is hereby incorporated in its entirety by reference.The present invention relates to aryl ...

Biological buffers with wide buffering ranges

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

ALKYL DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS

The present invention relates to alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 12. A compound according to which is selected from:3-({4-[4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pentyl]benzyl}amino)propanoic acid;[3-({4-[4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pentyl]benzyl}amino) propyl]phosphonic acid;[3-({4-[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]benzyl}amino) propyl]phosphonic acid;[3-({4-[5-(3,5-difluorophenyl)-6-(3,4-dimethylphenyl)hexyl]benzyl}amino) propyl]phosphonic acid;3-({4-[5-(3,5-difluorophenyl)-6-(3,4-dimethylphenyl)hexyl]benzyl}amino) propanoic acid; and3-({4-[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]benzyl}amino)propanoic acid.13. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluents or carrier.14. A pharmaceutical composition according to wherein the compound is which is selected from:3-({4-[4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pentyl]benzyl}amino)propanoic acid;[3-({4-[4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pentyl]benzyl}amino) propyl]phosphonic acid;[3-({4-[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]benzyl}amino) propyl]phosphonic acid;[3-({4-[5-(3,5-difluorophenyl)-6-(3,4-dimethylphenyl)hexyl]benzyl}amino) propyl]phosphonic acid;3-({4-[5-(3,5-difluorophenyl)-6-(3,4-dimethylphenyl)hexyl]benzyl}amino) propanoic acid; and3-({4-[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]benzyl}amino)propanoic acid. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/868,226 filed Aug. 21, 2013, the disclosure of which is hereby incorporated in its entirety by reference.The present invention relates to alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of ...

Method of Preparing Phosphorus-Containing Flame Retardants and Their Use in Polymer Compositions

A phosphorus-containing flame retardant is produced by reacting at a reaction temperature a mixture including a metal or suitable metal compound and a stoichiometric excess relative to the metal or suitable metal compound of an unsubstituted or alkyl or aryl substituted phosphonic or pyrophosphonic acid, wherein the phosphonic or pyrophosphonic acid is in a molten state at the reaction temperature. The chemical composition of the resulting flame retardant product leads to excellent flame retardancy and exhibits high thermal stability. The presently disclosed flame retardants are useful, for example, in polymer compositions, particularly thermoplastics processed at high temperatures, over a wide range of applications. 1. A process for producing a phosphorus-containing flame retardant , comprising reacting at a reaction temperature a mixture comprising a metal or suitable metal compound and a stoichiometric excess relative to the metal or suitable metal compound of an unsubstituted or alkyl or aryl substituted phosphonic acid , wherein:{'sub': ['p', 'q'], 'sup': '(+)y', '#text': 'the metal is capable of forming a polycation or the suitable metal compound is represented by the formula MXwhere M is a metal, (+)y represents the charge of the metal cation, y is 2 or higher, X is an anion, and the values for p and q provide a charge balanced metal compound;'}the molar ratio of the unsubstituted or alkyl or aryl substituted phosphonic acid to the metal or suitable metal compound in the mixture is higher than 4:1;the reaction temperature is 105° C. or higher; andthe unsubstituted or alkyl or aryl substituted phosphonic acid is in a molten state at the reaction temperature.2. A process for producing a phosphorus-containing flame retardant , comprising reacting at a reaction temperature a mixture comprising a metal or suitable metal compound and a stoichiometric excess relative to the metal or suitable metal compound of an unsubstituted or alkyl or aryl substituted ...

NOVEL PEROXIDE STABILIZERS

Methods for stabilizing one or more peroxide compounds in solution comprising adding to the solution an effective amount of at least one compound selected from the group comprising (i) cyclic carbonates; (ii) poly-phosphonic acid chelating agents and salts thereof, and alkaline pH adjusting agents with a pKb value of up to 3.0, wherein the w/w ratio of the poly-phosphonic acid chelating agent or salt thereof to alkali or alkaline earth metal hydroxide is from about 1:1 to about 50:1; and (iii) mixtures thereof. Also disclosed are solutions comprising the above compounds, uses of the above compounds to stabilize peroxide compounds in solutions, and compounds recited above for use as novel stabilizers. 1. A method of stabilizing a peroxide compound in a solution comprising adding to the solution an effective amount of poly-phosphonic acid chelating agents or salts thereof , and alkaline pH adjusting agents with a pKb value of up to 3.0 , wherein the w/w ratio of the poly-phosphonic acid chelating agent or salt thereof to alkali or alkaline earth metal hydroxide is from about 1:1 to about 50:1.2. The method of claim 1 , wherein the solution is free of quaternary ammonium compounds.3. The method of claim 1 , wherein the peroxide compound is selected from the group comprising hydrogen peroxide claim 1 , hydrogen peroxide adducts claim 1 , group IIIA oxidizing agents claim 1 , or hydrogen peroxide donors of group VIA oxidizing agents claim 1 , group VA oxidizing agents claim 1 , group VIIA oxidizing agents claim 1 , sodium peroxide claim 1 , ureal peroxide claim 1 , perboric acid claim 1 , sodium/potassium perborate claim 1 , sodium persulfate claim 1 , calcium peroxide claim 1 , lithium peroxide claim 1 , sodium peroxide claim 1 , dibenzoyl peroxide claim 1 , diacetyl peroxide claim 1 , di(n-propyl) peroxydicarbonate claim 1 , butyl peroxybenzoate claim 1 , butyl hydroperoxide claim 1 , ethylidene peroxide claim 1 , ethyl hydroperoxide claim 1 , peroximonosulfuric acid ...

NOVEL DXR INHIBITORS FOR ANTIMICROBIAL THERAPY

The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particular embodiments, the compositions target DXR. In some cases, the antimicrobial agent comprises an electron-deficient hydrophobic group that has interacts with Trp211 of DXR. In specific embodiments, the compound contains electron-deficient heterocyclic rings that specifically interact with the electron-rich indole ring of Trp211. In certain aspects, the compositions comprise a phosphate group, a pyridine group, and a hydroxymate group. 1. As a composition of matter , a compound of , , , a derivative thereof , or a combination thereof.2. The composition of claim 1 , comprised in a pharmaceutically acceptable carrier.3. A method of treating and/or preventing a microbial infection in an individual claim 1 , comprising the step of administering to the individual a therapeutically effective amount of the following:{'figref': {'@idref': 'DRAWINGS', 'FIG. 3'}, 'a) a composition of ;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 7'}, 'b) a composition of ;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 9'}, 'c) a composition of ;'}d) a functionally active derivative of a composition of a), b), or c);e) a composition comprising at least one phosphate group, a pyridine group, and a hydroxymate; orf) a mixture thereof;4. The method of claim 3 , wherein the composition is delivered orally claim 3 , subcutaneously claim 3 , intramuscularly claim 3 , topically claim 3 , rectally claim 3 , or vaginally.5. The method of claim 3 , wherein the microbial infection is bacterial claim 3 , viral claim 3 , fungal claim 3 , or from a parasitic protist.6Plasmodium.. The method of claim 5 , wherein the microbial infection is7Plasmodium falciparum.. The method of claim 6 , wherein the microbial infection is8. The method of claim 6 , wherein the individual is given an additional treatment for malaria.9Toxoplasma gondii.. The method of claim 5 , wherein the microbial infection ...

Novel Phosphonate and Phosphonic Acid RAFT Agents and Monomers, Along with Methods of Their Manufacture and Use

An intermediate compound for forming a RAFT agent is provided that can have the formula: 2. The intermediate compound of claim 1 , wherein n is 2 to 10 claim 1 , and wherein Y is COOH.3. The intermediate compound of claim 1 , wherein Ris a methyl group claim 1 , and wherein Ris a methyl group.4. The intermediate compound of claim 1 , wherein m is 2 to 10 claim 1 , and wherein X is OH.6. The intermediate compound of claim 1 , wherein m is 0.7. The intermediate compound of claim 1 , wherein X is a benzyl ring.9. A salt of the intermediate compound of .10. A RAFT agent comprising a thiocarbonylthio-containing organic compound having a phosphonic end group.11. The RAFT agent as in claim 10 , wherein the phosphonic end group is a phosphonic acid group.13. The RAFT agent as in claim 12 , wherein R″ comprises an alkyl group terminating with a phenyl end group or a nitrophenyl end group.14. The RAFT agent as in claim 13 , wherein R″ comprises a benzyl group claim 13 , a nitrobenzyl group claim 13 , or a para-methyl benzyl group.15. The RAFT agent as in claim 12 , wherein Ris H or an alkyl group having a formula of CH claim 12 , with n being an integer of 1 to 6.16. The RAFT agent as claim 12 , wherein Ris a methyl group claim 12 , an ethyl group claim 12 , a propyl group claim 12 , an iso-propyl group; a butyl group claim 12 , or a tert-butyl group.17. The RAFT agent as claim 12 , wherein Ris H or an alkyl group having a formula of CH claim 12 , with n being an integer of 1 to 6.18. The RAFT agent as in claim 12 , wherein Ris a methyl group claim 12 , an ethyl group claim 12 , a propyl group claim 12 , an iso-propyl group; a butyl group claim 12 , or a tert-butyl group.19. The RAFT agent as in claim 12 , wherein the organic linkage of Z comprises an ester group or an ethyl acetate linkage.21. The RAFT agent as in claim 12 , wherein R″ is a benzyl group.22. The RAFT agent as in claim 21 , wherein a nitro group is positioned on the benzyl group.23. The RAFT agent as in claim ...

Biological Buffers with Wide Buffering Ranges

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability. 2. The biological buffer and its salts of wherein A═D═—CH3 and m=1.3. The biological buffer and its salts of wherein A═D═—CH2OH and m=1.4. The biological buffer and its salts of wherein A═D—CH2O(CH2CH2CH2N)H and n=m=1.5. The biological buffer and its salts of wherein A═—CH2CH3 claim 1 , D═—CH2O(CH2CH2CH2N)H and n=m=1.6. The biological buffer and its salts of wherein A═—CH3 claim 1 , D═—CH2O(CH2CH2CH2N)H and n=m=1.7. The biological buffer and its salts of wherein A is —CH3 and D is —CH2CH3.9. The quaternary ammonium compound and its salts of wherein A═D═—CH3 claim 8 , E═—CH2OH claim 8 , R═R′═—CH3 and G═—H.10. The quaternary ammonium compound and its salts of wherein A═D═E═—CH2OH claim 8 , R═R′═—CH3 and G═—H.11. The quaternary ammonium compound and its salts of wherein A═D═—CH3 claim 8 , E═—CH2OH claim 8 , R═R′═—CH3 and G═—CH2CH3.12. The quaternary ammonium compound and its salts of wherein A═D═E═—CH2OH claim 8 , R═R′=—CH3 and G═—CH2CH3. This is a continuation of U.S. application Ser. No. 15/649,869 filed Jul. 14, 2017 and other previous parent applications claimed in the Application Data Sheet. U.S. application Ser. No. 15/649,869 is hereby incorporated by reference in its entirety.The present invention relates generally to the field of amines and more particularly to a classes of amines used as buffers in biological systems.Amines are very useful compounds in the buffering of biological systems. Each class of amine has various limitations which require choosing an amine ...

Optically-active 2-amino-phosphonoalkane acid, optically-active 2-amino-phosphonoalkane acid salt, and hydrates of these

A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.

Self-assembly of nanostructures

Structures and methods that include selective electrostatic placement based on a dipole-to-dipole interaction of electron-rich carbon nanotubes onto an electron-deficient pre-patterned surface. The structure includes a substrate with a first surface having a first isoelectric point and at least one additional surface having a second isoelectric point. A self-assembled monolayer is selectively formed on the first surface and includes an electron deficient compound including a deprotonated pendant hydroxamic acid or a pendant phosphonic acid group or a pendant catechol group bound to the first surface. An organic solvent can be used to deposit the electron rich carbon nanotubes on the self-assembled monolayer.

Phosphonate functional antimicrobial coatings for metal surfaces

The invention relates to quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds, processes for preparing quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds, antimicrobial coating compositions comprising quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds and method of treating a surface with said compositions to provide a durable, antimicrobial-treated surface.

TERTIARY AMIDES AND METHOD OF USE

Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein G, G, G, L, L, and Lare as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by the modulation of lysophosphatidic acid receptor 1. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions. 5. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '2', 'sub': 1', '3', '1', '3', '1', '3', '1', '3, 'Gis phenyl; wherein the phenyl is unsubstituted or optionally substituted with 1, 2 or 3 substituents independently selected from C-Calkoxy, C-Calkyl, or halogen, wherein the C-Calkyl and C-Calkoxy are unsubstituted or optionally substituted with one, two, or three fluorines.'}6. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '2', 'sub': 1', '3', '1', '3, 'Gis selected from the group consisting of 2-furanyl and 2-thiophenyl; wherein the 2-furanyl and 2-thiophenyl are unsubstituted or optionally substituted with 1 or 2 substituents independently selected from halogen or C-Calkyl, wherein the C-Calkyl is unsubstituted or optionally substituted with one, two, or three fluorines.'}7. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '3', 'sub': '2', 'Gis —COH.'}8. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '3', 'sub': 2', '1', '6', '3, 'Gis selected from the group consisting of —P(O)(OH), —P(O)(OH)(OC-Calkyl), and —P(O)(CH)(OH).'}9. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '3', 'sub': 2', '3', '3, 'Gis selected from the group consisting of —B(OH), —SOH, —CH(OH)CF, —C(O)NH(OH), and —C(O)NH(CN).'}10. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 3', 'G3a', 'G3a', 'G3a', 'G3a', 'G3a', 'G3a', ' ...

BIFUNCTIONAL COMPOUNDS USEFUL AS LIGANDS OF URANIUM (VI), METHODS OF SYNTHESISING SAME AND USES THEREOF

New compounds which meet general formula (I): 3. The compound of claim 2 , wherein Rand R claim 2 , the same or different claim 2 , are a straight-chain or branched alkyl group having 6 to 12 carbon atoms.4. The compound of claim 3 , wherein Rand Rare the same and each are a branched alkyl group having 8 to 10 carbon atoms.5. The compound of claim 4 , wherein Rand Rare a 2-ethylhexyl group.6. The compound of claim 2 , wherein m equals 0.7. The compound of claim 2 , wherein Ris a hydrogen atom claim 2 , a straight-chain or branched alkyl group having 1 to 12 carbon atoms claim 2 , or a monocyclic aromatic group.8. The compound of claim 2 , wherein Ris a hydrogen atom.9. The compound of claim 7 , wherein Ris a hydrogen atom claim 7 , a methyl group claim 7 , an n-octyl group or a phenyl group.10. The compound of claim 2 , wherein Ris a straight-chain or branched alkyl group having 2 to 8 carbon atoms.11. The compound of claim 10 , wherein Ris a straight-chain or branched alkyl group having 2 to 4 carbon atoms.12. The compound of claim 11 , wherein Ris an ethyl group or an n-butyl group.13. The compound of claim 2 , wherein:{'sup': 1', '2', '3', '4', '5, 'Ethyl 1-(N,N-diethylhexylcarbamoyl)benzylphosphonate, wherein m equals 0, Rand Reach are a 2 ethylhexyl group, Ris a phenyl group, Ris an ethyl group and Ris a hydrogen atom;'}{'sup': 1', '2', '3', '4', '5, 'Ethyl 1-(N,N-diethylhexylcarbamoyl)ethylphosphonate, wherein m equals 0, Rand Reach are a 2-ethylhexyl group, Ris a methyl group, Ris an ethyl group and Ris a hydrogen atom;'}{'sup': 1', '2', '3', '4', '5, 'Ethyl 1-(N,N-diethylhexylcarbamoyl)nonylphosphonate, wherein m equals 0, Rand Reach are a 2 ethylhexyl group, Ris an n-octyl group, Ris an ethyl group and Ris a hydrogen atom;'}{'sup': 1', '2', '3', '4', '5, 'Butyl 1-(N,N-diethylhexylcarbamoyl)nonylphosphonate, wherein m equals 0, Rand Reach are a 2 ethylhexyl group, Ris an n-octyl group, Ris an n-butyl group and Ris a hydrogen atom; or'}{'sup': 1', '2', '3', ' ...

S1PR2 ANTAGONISTS AND USES THEREFOR

Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are compounds which contain bioisosteric replacements of the urea group of JTE-013 and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis. 3. The method of claim 2 , wherein{'sup': '1', 'sub': '3', 'Ris CH; and'}{'sup': '2', 'sub': '3', 'Ris CH.'}4. The method of claim 3 , wherein{'sup': '3', 'Ris H; and'}{'sup': '4', 'sub': 1', '6, 'Ris C-Calkyl.'}5. The method of claim 4 , wherein{'sup': '4', 'sub': 3', '2, 'Ris CH(CH).'}6. The method of claim 5 , wherein{'sup': '5', 'Ris halogen.'}7. The method of claim 6 , wherein{'sup': '5', 'Ris Cl; and'}n is 2.8. The method of claim 2 , wherein{'sup': '1', 'sub': '3', 'Ris CH;'}{'sup': '2', 'sub': '3', 'Ris CH;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'sub': 3', '2, 'Ris CH(CH);'}{'sup': '5', 'Ris Cl; and'}n is 2.9. The method of claim 1 , wherein the ocular diseases include familial exudative vitreoretinopathy.10. The method of claim 1 , wherein the compound of formula IX is a S1PR2 antagonist.13. The compound of claim 12 , wherein{'sup': '3', 'Ris H; and'}{'sup': '4', 'sub': 1', '6, 'Ris C-Calkyl.'}14. The compound of claim 13 , wherein{'sup': '5', 'Ris Cl; and'}n is 2.15. The compound of claim 11 , wherein{'sup': '1', 'sub': '3', 'Ris CH;'}{'sup': '2', 'sub': '3', 'Ris CH;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'sub': 3', '2, 'Ris CH(CH);'}{'sup': '5', 'Ris Cl; and'}n is 2.16. The compound of claim 11 , wherein the eye condition includes familial exudative vitroretinopathy.17. The compound of claim 11 , wherein the eye condition includes an inability to normally vascularize the eye.18. The compound of claim 11 , wherein the eye condition includes secondary aberrant neovascularization.20. The method of claim 19 , wherein ...

Bicyclic aryl sphingosine 1-phosphate analogs

Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Transparent self-healing omniphobic coatings

Processes for preparing oleophobic and hydrophobic coatings on a substrate. More particularly, the disclosure relates to omniphobic surface treatment of substrates such as glass, ceramic, glass-ceramic, and the like.

WATER TREATMENT CHEMICAL FOR MEMBRANE, AND MEMBRANE TREATMENT METHOD

A water treatment chemical for a membrane, being is a water treatment chemical for preventing membrane contamination caused by an organic compound having a phenolic hydroxy group and including an organic amine having two or more nitrogen atoms and having five or more carboxyl groups or four or more phosphate groups. A membrane treatment method including adding the water treatment chemical for a membrane to water to be treated which contains an organic compound having a phenolic hydroxy group and then subjecting the water to be treated to membrane separation treatment. 1. A water treatment chemical for a membrane , being a water treatment chemical for preventing membrane contamination caused by an organic compound having a phenolic hydroxy group , and comprising an organic amine having two or more nitrogen atoms and having five or more carboxyl groups or four or more phosphate groups.3. The water treatment chemical for a membrane according to claim 2 , wherein n in the general formula (1) claim 2 , p and q in the general formula (2) claim 2 , and m in the general formula (3) are each an integer of 1 to 5.4. The water treatment chemical for a membrane according to claim 1 , wherein a molecular weight of the organic amine is 100 to 1000.5. The water treatment chemical for a membrane according to claim 1 , being a water treatment chemical for a reverse osmosis membrane for carrying out reverse osmosis membrane treatment of water to be treated claim 1 , the water containing an organic compound having a phenolic hydroxy group claim 1 , wherein a concentration of non-purgeable organic carbon in concentrated water obtained by the reverse osmosis membrane treatment is 0.01 to 100 mg/L.6. The water treatment chemical for a membrane according to claim 5 , wherein a concentration ratio of the reverse osmosis membrane is 3 times or more.7. A membrane treatment method comprising adding the water treatment chemical for a membrane according to to water to be treated claim 1 , the ...

Phosphorus control for waste streams from glyphosate manufacturing processes

This invention relates to processes for the removal of phosphorous from aqueous waste streams comprising phosphorous-containing compounds produced in the manufacture of glyphosate, in order to meet and typically exceed environmental regulations. More particularly, various embodiments of the present invention relate to the removal of phosphorous-containing compounds utilizing biological treatment system(s), oxidizing agent(s), and/or precipitant(s). The processes of the invention are also applicable to the removal of phosphorous compounds from phosphorous-containing waste streams other than those waste streams resulting from the manufacture of glyphosate.

SUBSTITUTED BISPHENYL BUTANOIC PHOSPHONIC ACID DERIVATIVES AS NEP INHIBITORS

The present invention provides a compound of formula I; 3. The compound according to claim 1 , wherein Ris Cl and Ris F; or a pharmaceutically acceptable salt thereof.6. The compound of wherein Ris —Calkyl or Caryl; wherein alkyl is optionally substituted with one or more substituents independently selected from the group consisting of —O—C(O)—O—Ccycloalkyl claim 1 , —O—C(O)—Ccycloalkyl claim 1 , —O—C(O)—Caryl claim 1 , —O—C(O)—O—Caryl claim 1 , —O—C(O)—O—Calkyl claim 1 , —O—C(O)—Calkyl claim 1 , heteroaryl claim 1 , heterocyclyl claim 1 , —C(O)-heterocyclyl claim 1 , —C(O)NH claim 1 , —C(O)NH—Calkyl claim 1 , and —C(O)N(Calkyl); or a pharmaceutically acceptable salt thereof.10. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.11. A combination comprising: a compound according to or a pharmaceutically acceptable salt thereof and one or more therapeutically active agents selected from HMG-Co-A reductase inhibitor claim 1 , an anigiotensin receptor blocker claim 1 , angiotensin converting enzyme inhibitor claim 1 , a calcium channel blocker claim 1 , an endothelin antagonist claim 1 , a renin inhibitor claim 1 , a diuretic claim 1 , an ApoA-I mimic claim 1 , an anti-diabetic agent claim 1 , an obesity-reducing agent claim 1 , an aldosterone receptor blocker claim 1 , an endothelin receptor blocker claim 1 , an aldosterone synthase inhibitor claim 1 , a CETP inhibitor and a phophodiesterase type 5 (PDE5) inhibitor.12. A method of inhibiting neutral endopeptidase activity in a subject in need thereof claim 1 , comprising: administering to the subject a therapeutically effective amount of the compound according to or a pharmaceutically acceptable salt thereof.13. A method of treating a disorder or a disease associated with neutral endopeptidase activity in a subject in need thereof claim 1 , comprising: administering to the subject a therapeutically ...

GPR40 AGONISTS

This disclosure is directed, at least in part, to GPR40 agonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the GPR40 agonists are gut-restricted compounds. In some embodiments, the GPR40 agonists are full agonists or partial agonists. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome. 2. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer thereof claim 1 , wherein:{'sup': 1', '2', '3, 'sub': 1', '4, 'R, R, and Rare each independently hydrogen, halogen, or C-Calkyl; and'}{'sup': '4', 'sub': 3', '6, 'Ris unsubstituted C-Ccycloalkyl.'}4. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer thereof claim 1 , wherein:{'sup': '1', 'sub': 2', '2, 'Lis *—O—CH— or *—CH—O—; wherein * represents the connection to Ring B.'}5. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer thereof claim 1 , wherein:{'sup': 'B', 'Ring B is 3- to 6-membered heterocycloalkylene; wherein the heterocycloalkylene is unsubstituted or substituted with 1, 2, 3, or 4 Rsubstituents.'}10. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer thereof claim 1 , wherein:{'sub': 3', '6, 'sup': 'B', 'Ring B is C-Ccycloalkylene; wherein the cycloalkylene is unsubstituted or substituted with 1, 2, 3, or 4 Rsubstituents.'}13. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer thereof claim 1 , wherein:{'sub': 3', '2', '3', '3', '2', '3', '2, 'Z is —P(═O)(H)OH, —P(═O)(CH)OH, —P(═O)(CHCH)OH, —POH, —P(═O)(OCH)(OH), or —SOOH.'}14. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer ...

ENPP1 Inhibitors and Methods of Modulating Immune Response

Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with an ENPP1 inhibitor compound to inhibit the cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor compound is cell impermeable. ENPP1 inhibitor compounds can act extracellularly to block the degradation of cGAMP. Also provided are pharmaceutical compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of an ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject in conjunction with administering an ENPP1 inhibitor to the subject. The radiation therapy can be administered in the subject methods at a dosage and/or frequency effective to reduce radiation damage to the subject, but still instigate an immune response.

Novel alkenyl and beta-substituted phrosphonates as antimicrobial agents

The present disclosure relates to novel compounds, pharmaceutical compositions, and methods for treating or preventing microbial infection caused by parasites or bacteria, such as Plasmodium falciparum or related Plasmodium parasite species and Mycobacterium tuberculosis or related Mycobacterium bacteria species. The compounds are α,β-unsaturated analogs of fosmidomycin and can inhibit deoxyxylulose phosphate reductoisomerase (Dxr) in many microbes, such as P. falciparum.

METHOD FOR THE SYNTHESIS OF N-PHOSPHONOMETHYLIMINODIACETIC ACID

A method for synthesis of N-phosphonoalkyliminodiacetic acid or derivatives thereof by: 1) forming a reaction mixture having an acid catalyst, a compound having the general formula R—CH—NX—CH—Rand a compound having one or more P—O—P anhydride moieties, to form a compound having the general formula R—CH—N—CH(POH)—CH—R, its dehydrated forms or their derivatives, wherein the compound of the formula R—CH—NX—CH—Ris characterized in that: X is —CH—OH or —CH—COOH; and Rand Rare independently selected from the group consisting of nitrile, C-Calkyl carboxylate, or are both carbonyl groups linked by a hydrogen substituted nitrogen atom or a C-C-akyl substituted nitrogen atom; the P—O—P anhydride compound is characterized in that the anhydride moieties have one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V); and 2) hydrolysing the reaction mixture to form N-phosphonomethyliminodiacetic acid or one of its derivatives. 1. A method for the synthesis of N-phosphonomethyliminodiacetic acid or derivatives thereof selected from the group consisting of phosphonate esters of N-phosphonometyliminodiacetic acid , carboxylate esters of N-phosphonometyliminodiacetic acid , phosphonate and carboxylate esters of N-phosphonometyliminodiacetic acid , N-phosphonometyliminodiacetic acid salts , phosphonate esters of N-phosphonometyliminodiacetic acid salts , carboxylate esters of N-phosphonometyliminodiacetic acid salts and phosphonate-carboxylate esters of N-phosphonometyliminodiacetic acid salts , wherein the cation of the salt is selected from the group consisting of ammonium , isopropylammonium , ethanolammonium , dimethylammonium , trimethylsulfonium , sodium and potassium ,comprising the steps of:{'sup': 1', '2', '1', '2, 'sub': 2', '2', '2', '2', '3', '2', '2, 'claim-text': {'sup': 1', '2, 'sub': 2', '2, 'the compound of the formula R—CH—NX—CH—Ris wherein, 'a) forming a reaction mixture comprising an acid catalyst, a compound having the general ...

METHOD FOR PRODUCING PHOSPHORUS CHEMICALS FROM WET PROCESS PHOSPHATE

Preparation of phosphorus fine chemicals from phosphate sources is described. 1. A compound comprising a bis(silyl)phosphide and a cation.2. The compound of claim 1 , wherein the cation includes hydrogen claim 1 , a nitrogen-based cation claim 1 , a phosphorus-based cation claim 1 , an alkali metal cation claim 1 , an alkali-earth metal cation claim 1 , or an ionic liquid cation.3. The compound of claim 1 , where the cation is [RN] claim 1 , where R is nBu claim 1 , sBu claim 1 , iBu claim 1 , nPr claim 1 , iPr claim 1 , Et claim 1 , or Me.4. The compound of claim 1 , wherein the silyl is HSiXwhere X is a halogen claim 1 , alkoxy claim 1 , aryloxy claim 1 , amido or arylamido and n is 0 claim 1 , 1 claim 1 , 2 or 3.5. The compound of claim 1 , wherein the cation includes [RN] claim 1 , where R is nBu.6. The compound of claim 1 , wherein the silyl is SiX3 where X is a halogen.7. The compound of claim 1 , wherein the cation is [RN] claim 1 , where R is nBu and the silyl is SiXwhere X is chloro.8. The compound of claim 1 , wherein the silyl is SiXwhere X is fluoro.9. A method of preparing a bis(silyl)phosphide comprising contacting a phosphate-source with a silane reducing agent.10. The method of claim 9 , wherein the silane reducing agent is HSiXwhere X is a halogen claim 9 , alkoxy claim 9 , aryloxy claim 9 , amido or arylamido and n is 1 claim 9 , 2 or 3.11. The method of claim 9 , wherein the silane reducing agent is HnSiX4-n where X is a chloro and n is 112. The method of claim 9 , wherein the phosphate-source includes a phosphoric acid claim 9 , a metaphosphate or an orthophosphate.13. The method of claim 9 , wherein the phosphate-source includes HPOMHPOMHPOMPOwhere M is an alkali metal ion or organic cation.14. The method of claim 9 , wherein the phosphate-source includes a metaphosphates of varying ring size having a formula: [POm] claim 9 , where m is 3-6) or a linear metaphosphate having the formula (HPO) claim 9 , wherein m is 3-6 claim 9 , or salts thereof. ...

METHOD FOR REMOVING GLYPHOSATE FROM A SOLUTION USING FUNCTIONALIZED POLYMERIC NANOPARTICLES

A method for removing glyphosate from a solution by contacting the solution with a polymeric particle including a moiety selected from the group consisting of ammonium, amine and combinations thereof, wherein the moiety is positively charged in the solution. 1. A method comprising removing glyphosate from a solution by contacting the solution with a polymeric particle comprising a moiety selected from the group consisting of ammonium , amine and combinations thereof , wherein the moiety is positively charged in the solution.2. The method of claim 1 , wherein the polymeric particle comprises a hydrophobic core and hydrophilic arms claim 1 , and wherein the hydrophilic arms comprise a positively charged functional group selected from the group consisting of ammonium claim 1 , amine claim 1 , and combinations thereof.3. The method of claim 2 , wherein the positively charged functional group is an amine.4. The method of claim 1 , wherein the solution comprises less than about 5 ppm glyphosate.5. The method of claim 1 , wherein the solution comprises less than about 2 ppm glyphosate.6. The method of claim 1 , wherein the solution comprises less than about 500 ppb glyphosate.9. The method of claim 1 , wherein the solution comprises water.10. A method for removing glyphosate from an aqueous solution claim 1 , comprising:(a) adding an amine-functionalized polymeric particle into the aqueous solution containing glyphosate; and(b) filtering to remove from the aqueous solution a complex comprising the amine-functionalized polymeric particles having glyphosate adsorbed thereon, and residual amine-functionalized particles.11. The method of claim 10 , comprising stirring the aqueous solution following step (a).12. The method of claim 11 , wherein the aqueous solution is stirred for about 1 minute to about 1 hour.13. The method of claim 10 , wherein the concentration of glyphosate in the aqueous solution is about 5 parts per billion (ppb) to 1000 parts per million (ppm).14. The ...

S1PR2 ANTAGONISTS AND USES THEREFOR

Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are (Z)-3-((2,6-dichloropyridin-4-yl)amino)-3-(((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)amino)acrylonitrile and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis. 2. The compound of claim 1 , wherein:{'sub': 10', '10, 'G is CRand Ris H; and,'}{'sub': 'y', 'Ris H.'}3. The compound of claim 2 , selected from the group consisting of:(E)-3-((2,6-dichloropyridin-4-yl)amino)-3-(((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)(methyl)amino)acrylonitrile;(E)-3-((2,6-dichloropyridin-4-yl)amino)-3-(ethyl((4-isopropyl-1,3-dimethyl-1 H-pyrazolo[3,4-b]pyridin-6-yl)methyl)amino)acrylonitrile;(E)-3-((2,6-dichloropyridin-4-yl)amino)-3-(((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)(propyl)amino)acrylonitrile;(E)-3-(butyl((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)amino)-3-((2,6-dichloropyridin-4-yl)amino)acrylonitrile;(E)-3-((2,6-dichloropyridin-4-yl)amino)-3-(isopropyl((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)amino)acrylonitrile;(E)-3-(benzyl((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)amino)-3-((2,6-dichloropyridin-4-yl)amino)acrylonitrile; and,a structural enantiomer of the foregoing, wherein the cyano group is in the (Z) form.4. The compound of claim 1 , wherein:{'sub': 10', '10, 'G is CRand Ris H; and,'}{'sub': 'x', 'Ris H.'}5. The compound of claim 4 , selected from the group consisting of:(Z)-3-((2,6-dichloropyridin-4-yl)(methyl)amino)-3-(((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)amino)acrylonitrile;(Z)-3-((2,6-dichloropyridin-4-yl)(ethyl)amino)-3-(((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)amino) ...

PRESSURE-REDUCING AND INJECTION-ENHANCING ANTI-SCALING AGENT FOR LOW-PERMEABILITY WATER-INJECTION WELL AND PREPARATION METHOD THEREOF

The present disclosure provides a pressure-reducing and injection-enhancing anti-scaling agent for low-permeability water-injection wells and a preparation method thereof The anti-scaling agent is prepared from starting materials comprising: 10 to 12 parts of non-ionic surfactant(s), 18 to 20 parts of hexasodium triethylenetetramine-N,N,N′,N″,N′″,N′″-hexaacetate, 5 to 8 parts of anionic surfactant(s), 6 to 8 parts of an organic phosphonic acid-carboxylic acid scale inhibitor, 2 to 5 parts of a dispersant, 15 to 18 parts of a diluent, 8 to 10 parts of an organic amine salt, and 30 to 36 parts of water. The pressure-reducing and injection-enhancing agent according to the present disclosure is characterized by having multiple functions in one agent. When used in an amount being 0.5% of the water injected to a water injection well, it shows excellent anti-swelling property, shrinking property, anti-corrosive property, and calcium sulfate and barium (strontium) sulfate scale resistance. 1. A pressure-reducing and injection-enhancing anti-scaling agent for low-permeability water-injection wells , prepared from starting materials comprising the following components: 10 to 12 parts of non-ionic surfactant(s) , 18 to 20 parts of hexasodium triethylenetetramine-N ,N ,N′ ,N″ ,N′″ ,N′″-hexaacetate , 5 to 8 parts of anionic surfactant(s) , 6 to 8 parts of an organic phosphonic acid-carboxylic acid scale inhibitor , 2 to 5 parts of a dispersant , 15 to 18 parts of a diluent , 8 to 10 parts of an organic amine salt , and 30 to 36 parts of water.2. The anti-scaling agent according to claim 1 , prepared from starting materials comprising the following components: 11 parts of non-ionic surfactant(s) claim 1 , 18 parts of hexasodium triethylenetetramine-N claim 1 ,N claim 1 ,N′ claim 1 ,N″ claim 1 ,N′″ claim 1 ,N′″-hexaacetate claim 1 , 6 parts of anionic surfactant(s) claim 1 , 6 parts of an organic phosphonic acid-carboxylic acid scale inhibitor claim 1 , 3 parts of a dispersant ...

METHOD FOR THE SYNTHESIS OF AMINOALKYLENEPHOSPHONIC ACID

A method for the synthesis of an aminoalkylenephosphonic acid or its phosphonate esters including the following steps: a) forming, in the presence of an aldehyde or ketone and an acid catalyst, a reaction mixture by mixing a compound having at least one HNRRmoiety or a salt thereof, with a compound having one or more P—O—P anhydride moieties, the moieties having one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V), wherein the ratio of moles of aldehyde or ketone to N—H moieties is 1 or more and wherein the ratio of N—H moieties to P—O—P anhydride moieties is 0.3 or more, and b) recovering the resulting aminoalkylenephosphonic acid having compound or its phosphonate esters. 1. A method for the synthesis of an aminoalkylenephosphonic acid or its phosphonate esters , comprising the following steps:{'sup': 1', '2, 'a) forming, in the presence of an aldehyde or ketone and an acid catalyst, a reaction mixture by mixing a compound (a.1.) comprising at least one HNRRmoiety or a salt thereof, with a compound (a.2.) having one or more P—O—P anhydride moieties, said moieties comprising one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V), wherein the ratio of moles of aldehyde or ketone to N—H moieties is 1 or more and wherein the ratio of N—H moieties to P—O—P anhydride moieties is 0.3 or more,'}and wherein:{'sup': 1', '2, 'claim-text': [{'sup': 1', '2, 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '4, '(a.1.1) Rand Rare independently selected from the group consisting of hydrogen, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Cacyl, optionally comprising an ethylenically unsaturated double bond, and (meth)acryloyl C-Cmoiety, the C-Cpart of said moieties being normal chained, branched or cyclised and being optionally substituted by one or more moieties selected from the group consisting of C-Chydrocarbon, aryl and aralkyl and optionally comprising one or more heteroatoms selected ...

BICYCLIC ARYL SPHINGOSINE 1-PHOSPHATE ANALOGS

Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors. 1106-. (canceled)108. The method of claim 107 , wherein Tis —C(O)(OR) claim 107 , —C(O)N(R)S(OR) claim 107 , —O—P(O)(OR)OR claim 107 , —P(O)(OR) claim 107 , tetrazolyl or —S(O)OR.109. The method of claim 107 , wherein Rand Rare both hydrogen claim 107 , and Ris fluoro claim 107 , chloro claim 107 , bromo claim 107 , iodo claim 107 , methyl claim 107 , trifluoromethyl claim 107 , ethyl claim 107 , propyl claim 107 , isopropyl claim 107 , n-butyl claim 107 , i-butyl claim 107 , t-butyl claim 107 , n-pentyl claim 107 , isopentyl claim 107 , 1 claim 107 ,1-dimethylpropyl claim 107 , neopentyl claim 107 , cyclopentyl claim 107 , n-hexyl claim 107 , cyclohexyl claim 107 , methoxy claim 107 , trifluoromethoxy claim 107 , ethoxy claim 107 , n-propoxy claim 107 , i-propoxy claim 107 , n-butoxy claim 107 , i-butoxy claim 107 , t-butoxy claim 107 , n-pentyloxy claim 107 , i-pentyloxy claim 107 , 1 claim 107 ,1-dimethylpropoxy claim 107 , neopentyloxy claim 107 , cyclopentyloxy claim 107 , n-hexyloxy claim 107 , or cyclohexyloxy.112. The method of claim 107 , further comprising administering to said mammal an effective amount of one or more drugs selected from the group consisting of: a corticosteroid claim 107 , a bronchodilator claim 107 , an antiasthmatic claim 107 , an antiinflammatory claim 107 , an antirheumatic claim 107 , an immunosuppressant claim 107 , an antimetabolite claim 107 , an immunomodulator claim 107 , an antipsoriatic claim 107 , and an antidiabetic.114. The method of claim 113 , wherein Tis —C(O)(OR) claim 113 , —C(O)N(R)S(OR) claim 113 , —O—P(O)(OR)OR claim 113 , —P(O)(OR) claim 113 , tetrazolyl or —S(O)OR.115. The method of claim 113 , wherein Rand Rare both hydrogen claim 113 , and Ris fluoro claim 113 , chloro claim 113 , bromo claim 113 , iodo claim 113 , ...

LIGAND-FUNCTIONALIZED SUBSTRATES WITH ENHANCED BINDING CAPACITY

An article that can be used for biomaterial capture comprises 1. An article for biomaterial capture comprising(a) a porous substrate; and(b) borne on said porous substrate, a polymer comprising interpolymerized units of at least one monomer consisting of (1) at least one monovalent ethylenically unsaturated group, (2) at least one monovalent ligand functional group selected from acidic groups, basic groups other than guanidino, and salts thereof, and (3) a multivalent spacer group that is directly bonded to said monovalent groups so as to link at least one said ethylenically unsaturated group and at least one said ligand functional group by a chain of at least six catenated atoms {'br': None, 'sub': 2', 'n, 'sup': 1', '2', '2, 'CH═CR—C(═O)—X—R—[Z—R]-L'}, '(c) wherein said monomer is of the formula [{'sup': '1', 'Ris selected from hydrogen, alkyl, cycloalkyl, aryl, and combinations thereof;'}, {'sup': '2', 'each Ris independently selected from hydrocarbylene, heterohydrocarbylene, and combinations thereof;'}, {'sup': 3', '3, 'X is —O— or —NR—, where Ris selected from hydrogen, hydrocarbyl, heterohydrocarbyl, and combinations thereof;'}, 'Z is heterohydrocarbylene comprising at least one hydrogen bond donor, at least one hydrogen bond acceptor, or a combination thereof;', 'n is 1; and', 'L is a heteroatom-containing group comprising at least one monovalent ligand functional group selected from acidic groups, basic groups other than guanidino, and salts thereof., 'wherein'}2. The article of claim 1 , wherein said porous substrate is a porous membrane; and/or wherein said porous substrate is polymeric.3. The article of wherein said monovalent ethylenically unsaturated group is selected from ethenyl claim 1 , 1-alkylethenyl claim 1 , and combinations thereof.4. The article of or any other of the preceding claims claim 1 , wherein said monovalent ligand functional group is selected from carboxy claim 1 , phosphono claim 1 , phosphato claim 1 , sulfono claim 1 , sulfato ...

TRANSPARENT SELF-HEALING OMNIPHOBIC COATINGS

Processes for preparing oleophobic and hydrophobic coatings on a substrate. More particularly, the disclosure relates to omniphobic surface treatment of substrates such as glass, ceramic, glass-ceramic, and the like. 1. A process for obtaining an omniphobic coating on a substrate comprising:a. activating a substrate by contacting the substrate with a plasma of a gas; and,b. depositing a first layer of an omniphobic coating comprising at least one fluoride ion-encapsulated functionalized fluoropolyhedral oligomeric silsesquioxane, and at least one fluorocompound.3. The process of claim 1 , wherein the at least one fluorocompound is selected from the group consisting of a fluoroalkyl phosphonic acid (FAPA) claim 1 , a fluoroakyl phosphonate (FAPN) claim 1 , a fluoroalkyl silane (FAS) claim 1 , a fluoroalkyl halide (FAH) claim 1 , and combinations thereof.5. The process of claim 1 , wherein the step of depositing is carried out in the presence of a mixture of at least one polar solvent and an aqueous acid or base. This application is a divisional of co-pending U.S. patent application Ser. No. 15/353,078, filed Nov. 16, 2016, which claims priority to U.S. Provisional Patent Application No. 62/255,776, filed Nov. 16, 2015, and commonly assigned to the assignee of the present application, the disclosures of which are incorporated by reference in their entirety herein.The present disclosure relates, in exemplary embodiments, to processes for preparing oleophobic and hydrophobic coatings on a substrate. More particularly, the disclosure relates to omniphobic surface treatment of substrates such as glass, ceramic, glass-ceramic, and the like.The presence of liquids, often laden with dirt, is critical in safety particularly, for a transparent substrate of the glazing type, especially one used in the transportation. The nonwetting property of a substrate can be categorized into omniphobic. Omniphobic substrate means oil (including organic liquids) and water repellent substrate ...

Biological buffers with wide buffering ranges

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range. Derivatives that result in polyamines that have the same pKa yield a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

LIGAND-FUNCTIONALIZED SUBSTRATES WITH ENHANCED BINDING CAPACITY

An article that can be used for biomaterial capture comprises 123-. (canceled)24. A free radically polymerizable compound consisting of (a) at least one monovalent ethylenically unsaturated group , (b) at least one monovalent ligand functional group selected from phosphorus-containing acidic groups , boron-containing acidic groups , and salts thereof , and (c) a multivalent spacer group that is directly bonded to the monovalent groups so as to link at least one ethylenically unsaturated group and at least one ligand functional group by a chain of at least six catenated atoms , said monomer of the formula:{'br': None, 'sub': 2', 'n, 'sup': 1', '2', '2, 'CH═CR—C(═O)—X—R—[Z—R]—L'}wherein{'sup': '1', 'Ris selected from hydrogen, alkyl, cycloalkyl, aryl, and combinations thereof;'}{'sup': '2', 'each Ris independently selected from hydrocarbylene, heterohydrocarbylene, and combinations thereof;'}{'sup': 3', '3, 'X is —O— or —NR—, where Ris selected from hydrogen, hydrocarbyl, heterohydrocarbyl, and combinations thereof;'}Z is heterohydrocarbylene comprising at least one hydrogen bond donor, at least one hydrogen bond acceptor, or a combination thereof;n is 1; andL is a heteroatom-containing group comprising at least one monovalent ligand functional group selected from acidic groups, basic groups other than guanidino, and salts thereof.25. The compound of claim 24 , wherein said ligand functional group is selected from phosphono claim 24 , phosphato claim 24 , boronato claim 24 , and combinations thereof. This application claims the priority of U.S. Provisional Application No. 61/886177 filed Oct. 3, 2013, the contents of which are hereby incorporated by reference.This invention relates to articles comprising ligand-functionalized substrates and, in other aspects, to processes for preparing and using the articles.Detection, quantification, isolation, and purification of target biomaterials, such as viruses and biomacromolecules (including constituents or products of living ...

Method for the synthesis of alpha-aminoalkylenephosphonic acid

A method for the synthesis of alpha-aminoalkylenephosphonic acid or its phosphonate esters including the steps of forming a reaction mixture by mixing a P—O—P anhydride moiety including a compound, having one P-atom at the oxidation state (+III) and the other P-atom at the oxidation state (+III) or (+V), an aminoalkanecarboxylic acid and an acid catalyst, wherein the reaction mixture includes an equivalent ratio of alpha-aminoalkylene carboxylic acid to P—O—P anhydride moieties of at least 0.2, and recovering the resulting alpha-aminoalkylene phosphonic acid compound or an ester thereof from the reaction mixture.

PRODRUGS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR

Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA. 28. A method for treating a disease or a condition , the method comprising administering to a subject in need of treatment thereof , a compound of formula (I) , or a compound of formula (II) , or a pharmaceutical composition thereof , in an amount effective for treating the disease or condition.29. The method of claim 28 , wherein the disease or condition is selected from the group consisting of a neurodegenerative disease claim 28 , multiple sclerosis (MS) claim 28 , cancer claim 28 , angiogenesis claim 28 , and inflammatory bowel disease.30. The method of claim 29 , wherein the neurodegenerative disease is selected from the group consisting of amyotrophic lateral sclerosis (ALS) claim 29 , Parkinson's disease (PD) claim 29 , Alzheimer's disease (AD) claim 29 , Huntington's disease claim 29 , dementia with Lewy Bodies (DLB) claim 29 , schizophrenia claim 29 , pain claim 29 , epilepsy claim 29 , stroke claim 29 , and traumatic brain injury (TBI).31. The method of claim 30 , wherein the disease or condition results in excess PSMA activity.32. The method of claim 31 , further comprising an inhibiting the excess PSMA activity when the compound of formula (I) claim 31 , the compound of formula (II) claim 31 , or a pharmaceutical composition thereof claim 31 , is administered. This application claims the benefit of U.S. Provisional Application No. 62/033,926, filed Aug. 6, 2014, which is incorporated herein by reference in its entirety.This invention was made with government support under R01 CA161056-01 awarded by the National Cancer Institute (NCI). The government has certain rights in the invention.The prodrug approach is a well-established strategy to improve physicochemical, biopharmaceutic and pharmacokinetic properties of potential drug molecules. Approximately 5-7% of drugs approved worldwide are prodrugs with ...

Electrochromic compound, electrochromic composition, display element, and dimming element

To provide an electrochromic compound, represented by the following general formula (I), where Ar 1 is a pyridinium ring having a structure represented by the following general formula (IIa), (IIb), or (IIc), where Ar 2 is a monovalent heterocyclic ring which may have a substituent, but Ar 2 is not a pyridinium ring; R 1 to R 8 are each independently a monovalent group which may have a functional group, where the monovalent group may have a substituent; A is a monovalent group which may have a functional group, where the monovalent group may have a substituent; and B − is a monovalent anion.

COMPOUNDS AND COMPOSITIONS AS TLR2 AGONISTS

The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine. 2. The compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.3. The compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Ris —C(O)—Calkyl;4. The compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 2', '3, 'sub': 11', '11, 'Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 16', '16, 'or Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 16', '11, 'or Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 12', '12, 'or Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 7', '7, 'or Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 9', '9, 'or Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 8', '8, 'or Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 13', '13, 'or Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 12', '11, 'or Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 10', '10, 'or Ris —Calkyl and Ris —Calkyl;'}{'sup': 2', '3, 'sub': 15', '15, 'or Ris —Calkyl and Ris —Calkyl.'}5. The compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Ris —Calkyl and Ris —Calkyl.6. The compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Ris —NH claim 1 , —N(CHCH) claim 1 , —OH claim 1 , —OCH claim 1 , —P(O)(OH) claim 1 , —C(O)OH claim 1 , —S(O)OH claim 1 , —OS(O)OH claim 1 , —NHC(O)LR claim 1 , —OLR claim 1 , —C(O)NHLRor —C(O)NHLR.7. The compound of claim 6 , or pharmaceutically acceptable salt thereof claim 6 , wherein Ris —NH claim 6 , —N(CHCH) claim 6 , —OH claim 6 , —OCH claim 6 , —P(O)(OH) claim 6 , —C(O)OH claim 6 , —NHC(O)LR claim 6 , —S( ...

IMAGE RECORDING PAPER MEDIUM AND IMAGE RECORDING METHOD

The image recording paper medium contains at least one kind of organic phosphorus compound selected from an organic phosphonic acid represented by the following Formula (1), a salt thereof, an organic phosphoric acid represented by the following Formula (2), and a salt thereof. 2. The image recording paper medium according to claim 1 ,{'sup': 1', '2, 'wherein each of Rand Rrepresents an unsubstituted alkyl group having 6 to 24 carbon atoms.'}3. The image recording paper medium according to claim 1 , further comprising:a coat layer containing calcium carbonate,wherein the coat layer contains the organic phosphorus compound.4. The image recording paper medium according to claim 2 , further comprising:a coat layer containing calcium carbonate,wherein the coat layer contains the organic phosphorus compound.5. The image recording paper medium according to claim 3 ,wherein the content of the organic phosphorus compound contained in the coat layer is 1 part by mass to 30 parts by mass with respect to 100 parts by mass of the content of the calcium carbonate contained in the coat layer.6. The image recording paper medium according to claim 4 ,wherein the content of the organic phosphorus compound contained in the coat layer is 1 part by mass to 30 parts by mass with respect to 100 parts by mass of the content of the calcium carbonate contained in the coat layer.7. The image recording paper medium according to that is obtained by coating the coat layer of the paper medium having the coat layer containing calcium carbonate with a solution containing the organic phosphorus compound.9. The image recording method according to claim 8 ,{'sup': 1', '2, 'wherein each of Rand Rrepresents an unsubstituted alkyl group having 6 to 24 carbon atoms.'}10. The image recording method according to claim 8 ,{'sup': '2', 'wherein in the step (a), the applied amount of the organic phosphorus compound is equal to or less than 10 g/m.'}11. The image recording method according to claim 8 ,wherein ...

Preparation method of a cyclic phosphonate compound

A method for preparing the cyclic phosphonate compound of Formula Iis described. The method significantly improves the stereoselectivity of the compound with the required configuration.

Amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives and their medical use

The present invention relates to amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives, in particular the compounds of formula 1, 2, 3, 4, 5 or 6 and their medical use, including their use in treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder.

PRODRUGS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR

Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA. 140.-. (canceled)42. The method of claim 41 , wherein the disease or condition is selected from the group consisting of a neurodegenerative disease claim 41 , multiple sclerosis (MS) claim 41 , cancer claim 41 , angiogenesis claim 41 , and inflammatory bowel disease.43. The method of claim 42 , wherein the neurodegenerative disease is selected from the group consisting of amyotrophic lateral sclerosis (ALS) claim 42 , Parkinson's disease (PD) claim 42 , Alzheimer's disease (AD) claim 42 , Huntington's disease claim 42 , dementia with Lewy Bodies (DLB) claim 42 , schizophrenia claim 42 , pain claim 42 , epilepsy claim 42 , stroke claim 42 , and traumatic brain injury (TBI).44. The method of claim 41 , wherein the disease or condition results in excess PSMA activity.45. The method of claim 41 , further comprising inhibiting the excess PSMA activity when the compound claim 41 , or a pharmaceutical composition thereof claim 41 , is administered.46. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient. This application claims the benefit of U.S. Provisional Application No. 62/033,926, filed Aug. 6, 2014, which is incorporated herein by reference in its entirety.This invention was made with government support under R01 CA161056-01 awarded by the National Cancer Institute (NCI). The government has certain rights in the invention.The prodrug approach is a well-established strategy to improve physicochemical, biopharmaceutic and pharmacokinetic properties of potential drug molecules. Approximately 5-7% of drugs approved worldwide are prodrugs with annual sales in 2013 of $11.2 billion. Most prodrugs are simple chemical derivatives of the original molecule. Ester prodrugs, the most common prodrugs, constitute 49% of all marketed prodrugs. Reasons for the popularity of ester ...

NOVEL PHOSPHONATE AND PHOSPHONIC ACID RAFT AGENTS AND MONOMERS, ALONG WITH METHODS OF THEIR MANUFACTURE AND USE

An intermediate compound for forming a RAFT agent is provided that can have the formula: 1. A RAFT agent comprising a thiocarbonylthio-containing organic compound having a phosphonic end group.2. The RAFT agent as in claim 1 , wherein the phosphonic end group is a phosphonic acid group.4. The RAFT agent as in claim 3 , wherein R″ comprises an alkyl group terminating with a phenyl end group or a nitrophenyl end group.5. The RAFT agent as in claim 4 , wherein R″ comprises a benzyl group claim 4 , a nitrobenzyl group claim 4 , or a para-methyl benzyl group.6. The RAFT agent as in claim 3 , wherein Ris H or an alkyl group having a formula of CH claim 3 , with n being an integer of 1 to 6.7. The RAFT agent as claim 3 , wherein Ris a methyl group claim 3 , an ethyl group claim 3 , a propyl group claim 3 , an iso-propyl group; a butyl group claim 3 , or a tert-butyl group.8. The RAFT agent as claim 3 , wherein Ris H or an alkyl group having a formula of CH claim 3 , with n being an integer of 1 to 6.9. The RAFT agent as in claim 3 , wherein Ris a methyl group claim 3 , an ethyl group claim 3 , a propyl group claim 3 , an iso-propyl group; a butyl group claim 3 , or a tert-butyl group.10. The RAFT agent as in claim 3 , wherein the organic linkage of Z comprises an ester group or an ethyl acetate linkage.12. The RAFT agent as in claim 3 , wherein R″ is a benzyl group.13. The RAFT agent as in claim 12 , wherein a nitro group is positioned on the benzyl group.14. The RAFT agent as in claim 13 , wherein the nitro group is positioned on the benzyl group at the para position.15. The RAFT agent as in claim 3 , wherein A is O claim 3 , NH claim 3 , or S.17. A salt of the RAFT agent of .18. A method of forming a polymer chain on a surface of a nanoparticle claim 3 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'attaching the RAFT agent of to the surface of the nanoparticle, wherein the phosphonic group of the RAFT agent is covalently bonded to the surface ...

TREATMENT OF RETT SYNDROME

The present invention relates to agents and methods for treating autism spectrum disorders, such as Rett Syndrome. 1. A method for treating Rett Syndrome , comprising administering to a human subject in need thereof an effective amount of a therapeutic agent that is {[2-bromo-4-(2-carbamoyl-2-methanesulfonylaminoethyl)phenyl]difluoromethyl}-phosphonic acid (CPT157633) or a derivative or analog thereof.2. The method of claim 1 , wherein the therapeutic agent is administered to the subject after diagnosis of Rett Syndrome.3. The method of claim 1 , further comprising testing the subject for a mutation in a gene encoding methyl CpG-binding protein 2 (MECP2).4. The method of claim 3 , wherein the testing comprises nucleic acid detection and the nucleic acid detection is an assay selected from the group consisting of polymerase chain reaction (PCR) claim 3 , reverse transcription polymerase chain reaction (RT-PCR) claim 3 , quantitative PCR claim 3 , nucleic acid sequencing claim 3 , nucleic acid microarray analysis claim 3 , and fluorescence in situ hybridization.5. The method of wherein the testing comprises nucleic acid sequencing of one or more of the coding regions and exon/intron boundaries of the MECP2 gene.6. A system comprising a first pharmaceutical composition comprising an effective amount of a first therapeutic agent that is a small molecule inhibitor of PTP1B claim 3 , and a kit for diagnosing Rett Syndrome.7. The system of claim 6 , wherein the small molecule inhibitor of PTP1B is CPT157633.8. The system of claim 6 , wherein the kit comprises a reagent for detecting a mutation in a gene encoding methyl CpG-binding protein 2 (MECP2).9. The system of claim 8 , wherein the reagent comprises PCR primers for PCR-based sequencing of one or more of the coding regions and exon/intron boundaries of the MECP2 gene.1013.-. (canceled)14. The method of claim 2 , further comprising testing the subject for a mutation in a gene encoding methyl CpG-binding protein 2 (MECP2 ...

NANOCRYSTAL AND PREPARATION METHOD THEREOF

A nanocrystal represented by the following Formula 1 and a preparation method thereof: 1. A nanocrystal represented by Formula 1:{'br': None, 'sub': '3', 'AMXL \u2003\u2003Formula 1'}wherein A is selected from the group consisting of cesium (Cs), rubidium (Rb), and an ammonium salt,M is selected from the group consisting of germanium (Ge), tin (Sn), and lead (Pb),X is one or more selected from the group consisting of Cl, Br, and I, and{'sub': 3', '2', '6', '2', '3', '2', '7', '2', '3', '2', '8', '2', '3', '2', '9', '2', '3', '2', '10', '2', '3', '2', '11', '2', '3', '2', '12', '2, 'L is CH(CH)P(═O)(OH), CH(CH)P(═O)(OH), CH(CH)P(═O)(OH), CH(CH)P(═O)(OH), CH(CH)P(═O)(OH), CH(CH)P(═O)(OH)or CH(CH)P(═O)(OH).'}2. The nanocrystal of claim 1 , wherein the nanocrystal represented by Formula 1 is a compound represented by Formula 2:{'br': None, 'sub': x', '3-x, 'AMIBrL \u2003\u2003Formula 2'}wherein A is selected from the group consisting of cesium (Cs), rubidium (Rb), and an ammonium salt,M is selected from the group consisting of Ge, Sn, and Pb, and0 Подробнее

Biological Buffers with Wide Buffering Ranges

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

SHIELDING AGENTS AND THEIR USE

The present disclosure relates to compounds useful as shielding agents for PSMA therapies. The present disclosure relates to methods of treating PSMA expressing cancers with one or more radiotherapeutics agents in combination with one or more shielding agents. The present disclosure relates to methods of imaging using one or more imaging agents containing a radionuclide in combination with one or more shielding agents. The present disclosure also relates to methods of making shielding agents. 2. A method for treating a cancer in a patient comprising administering a therapeutically effective amount of a radiolabeled therapeutic in combination with a an effective amount of a shielding agent.4. The method of claim 3 , wherein the cancer is a prostate cancer.5. The method of claim 4 , wherein the cancer is a metastatic prostate cancer.6. The method of claim 4 , wherein the cancer is a metastatic castration-resistant prostate cancer.918.-. (canceled)19. A method for imaging a cancer in a patient comprising administering an effective amount of an imaging conjugate in combination with an effective amount of a shielding agent.21. The method of claim 19 , wherein the cancer is a prostate cancer.22. The method of claim 21 , wherein the cancer is a metastatic prostate cancer.23. The method of claim 21 , wherein the cancer is a metastatic castration-resistant prostate cancer.2635.-. (canceled) This application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Application Ser. No. 62/734,690 filed on Sep. 21, 2018, the entire disclosure of which is incorporated herein by reference.The present disclosure relates to compounds useful as shielding agents for PSMA therapies. The present disclosure relates to methods of treating PSMA expressing cancers with one or more radiotherapeutics agents in combination with one or more shielding agents. The present disclosure relates to methods of imaging using one or more imaging agents containing a radionuclide in combination with ...

Process For Preparing Ethylenedialkylphosphinic Acids, Esters And Salts And Use Thereof

The invention relates to a method for producing ethylenedialkylphosphinic acids, esters and salts, and to the use thereof as flame retardants. The claimed method is characterised in that •a) a phosphinic acid source (I) is reacted with olefins (IV) in the presence of catalyst A so as to obtain an alkylphosphonous acid, salt or ester (II) thereof, and •b) the alkylphosphonous acid, salt or ester (II) thereof obtained in this manner is reacted with acetylenic compound (V) in the presence of catalyst B in order to obtain the ethylenedialkylphosphinic acid derivative (III), •catalyst A being transition metals and/or transition metal compounds and/or catalyst systems composed of a transition metal and/or a transition metal compound and at least one ligand •and catalyst B being electromagnetic radiation.

LIGAND-FUNCTIONALIZED SUBSTRATES WITH ENHANCED BINDING CAPACITY

An article that can be used for biomaterial capture comprises 123.-. (canceled)24. An article for biomaterial capture comprising(a) a porous polymeric membrane; and [{'br': None, 'sub': 2', 'n, 'sup': 1', '2, 'CH═CR—C(═O)—X—R—[Z—R]-L'}, 'wherein', {'sup': '1', 'Ris selected from hydrogen, alkyl, cycloalkyl, aryl, and combinations thereof;'}, {'sup': '2', 'each Ris independently selected from hydrocarbylene, heterohydrocarbylene, and combinations thereof;'}, {'sup': 3', '3, 'X is —O— or —NR—, where Ris selected from hydrogen, hydrocarbyl, heterohydrocarbyl, and combinations thereof;'}, 'Z is heterohydrocarbylene comprising at least one hydrogen bond donor, at least one hydrogen bond acceptor, or a combination thereof;', 'n is 1; and', 'L is a heteroatom-containing group comprising at least one monovalent ligand functional group selected from acidic groups, basic groups other than guanidino, and salts thereof., '(b) grafted to said porous polymeric membrane, a polymer comprising interpolymerized units of at least one monomer of the formula25. The article of wherein said article comprises at least one filter element.26. A process for capture or removal of a target biomaterial comprising{'claim-ref': {'@idref': 'CLM-00024', 'claim 24'}, '(a) providing at least one article of ; and'}(b) allowing a moving biological solution containing a target biomaterial to impinge upon the upstream surface of said filter element for a time sufficient to effect binding of said target biomaterial.27. The process of claim 26 , wherein said target biological species is a protein.28. A free radically polymerizable compound consisting of (a) at least one monovalent ethylenically unsaturated group claim 26 , (b) at least one monovalent ligand functional group selected from phosphorus-containing acidic groups claim 26 , boron-containing acidic groups claim 26 , and salts thereof claim 26 , and (c) a multivalent spacer group that is directly bonded to the monovalent groups so as to link at ...

SINGLE PHASE LIQUIDS OF ALKANOLAMINE SALTS OF DICAMBA

The invention is a herbicidal composition containing an alkanolamine salt of an dicamba capable of remaining as a single phase liquid over a period of at least 1 week and containing low amounts of water and high loadings of the salt. Such herbicidal compositions are capable of remaining liquid in the absence of high amounts of water, thereby enhancing their capacity to remain liquid over an extended period of time when exposed to environmental conditions to improve their effectiveness to transport the active salt through a leafy substrate and can reduce transportation costs by increasing the salt loading without compromising the stability of the composition. 1. A herbicidal composition comprising water and an alkanolamine salt , said alkanolamine salt comprising the reaction product of an alkanolamine compound with dicamba , wherein said alkanolamine salt is capable of remaining a single phase liquid for at least 1 week , said capability determined by subjecting said alkanolamine salt to the following test conditions: 2 ml of a sample containing said alkanolamine salt and less than 5 wt. % water , based on the weight of the sample , and no non-aqueous solvents is placed onto a glass surface and exposed to the atmosphere at a temperature within a range of 20° C. to 25° C. and at approximately 1 atmosphere.2. The herbicidal composition of claim 1 , wherein sample undergoing said test does not contain solids dispersed throughout the liquid.3. The herbicidal composition of claim 1 , wherein the sample undergoing said test contains no added solvent other than water.4. The composition of claim 3 , wherein the sample undergoing the test conditions contains water in an amount of no more than 3 wt. % based on the weight of the sample claim 3 , and no other added solvents.5. The herbicidal composition of claim 4 , wherein the herbicidal composition contains water present in an amount of not more than 10 wt. % based on the weight of the herbicidal composition.6. The herbicidal ...

Biological Buffers with Wide Buffering Ranges

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability. 2. The biological buffer and its salts of wherein A=D=—CH3 and m=1.3. The biological buffer and its salts of wherein A=D=—CH2OH and m=1.4. The biological buffer and its salts of wherein A=D-CH2O(CH2CH2CH2N)H and n=m=1.5. The biological buffer and its salts of wherein A=—CH2CH3 claim 1 , D=—CH2O(CH2CH2CH2N)H and n=m=1.6. The biological buffer and its salts of wherein A=—CH3 claim 1 , D=—CH2O(CH2CH2CH2N)H and n=m=1.7. The biological buffer and its salts of wherein A is —CH3 and D is —CH2CH3.9. The quaternary ammonium compound and its salts of wherein A=D=—CH3 claim 8 , E=—CH2OH claim 8 , R=R′=—CH3 and G=—H.10. The quaternary ammonium compound and its salts of wherein A=D=E=—CH2OH claim 8 , R=R′=—CH3 and G=—H.11. The quaternary ammonium compound and its salts of wherein A=D=—CH3 claim 8 , E=—CH2OH claim 8 , R=R′=—CH3 and G=—CH2CH3.12. The quaternary ammonium compound and its salts of wherein A=D=E=—CH2OH claim 8 , R=R′=—CH3 and G=—CH2CH3.14. The surfactant of wherein A is —H and D is —CH3.15. The surfactant of wherein A is —CH3 and D is chosen from —CH3 claim 13 , —CH2CH3 claim 13 , —CH2CH2CH3 claim 13 , —CH2OH.16. The surfactant of wherein A is —CH3 and D is chosen from —CH2CH2CH3 claim 13 , —CH2OH.17. The surfactant of wherein A is —CH3 and D is —CH2OH. This is a continuation of application Ser. No. 15/255,654 filed Sep. 2, 2016 and other previous parent applications claimed in the Application Data Sheet. application Ser. No. 15/255,654 is hereby incorporated by reference ...

ELECTRONIC SWITCHING ELEMENT

An electronic switching element () which comprises, in this sequence, a first electrode (), a molecular layer () bonded to a substrate, and a second electrode (), where the molecular layer essentially consists of compounds of the formula I indicated in claim in which a mesogenic radical is bonded to the substrate via a spacer group (Sp) by means of an anchor group (G), is suitable for the production of components () as memristive device for digital information storage. 2120. Electronic switching element () according to claim 1 , characterised in that the first electrode () represents the substrate for the molecular layer.3122182018. Electronic switching element () according to claim 1 , characterised in that a diode () claim 1 , which represents the substrate for the molecular layer () claim 1 , is arranged between the first electrode () and the molecular layer ().41222426242620. Electronic switching element () according to claim 3 , characterised in that the diode () comprises an n+-doped layer () and a p+-doped layer () claim 3 , where the n+-doped layer () or the p+-doped layer () is designed as a combined electrode together with a semiconducting first electrode ().51221618. Electronic switching element () according to claim 1 , characterised in that a diode () is arranged between the second electrode () and the molecular layer ().611818. Electronic element () according to claim 1 , characterised in that an interlayer is arranged between the substrate and the molecular layer () claim 1 , where the interlayer is selected from an oxidic or fluoridic material and in that the molecular layer () is bonded to this oxidic or fluoridic interlayer.71. Electronic switching element () according to claim 6 , characterised in that the oxidic or fluoridic interlayer is formed from TiO claim 6 , AlO claim 6 , HfO claim 6 , SiOor LiF.81. Electronic switching element () according to claim 6 , characterised in that the anchor group (G) of the compounds of the formula I claim 6 , ...

INHIBITORS OF CREATINE TRANSPORT AND USES THEREOF

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer. 3. The method of claim 2 , wherein said method comprises the suppression of metastatic colonization of said migrating cancer in the liver.4. The method of claim 2 , wherein said migrating cancer is metastatic cancer.5. The method of claim 4 , wherein the metastatic cancer comprises cells exhibiting migration and/or invasion of migrating cells.6. The method of claim 4 , wherein said metastatic cancer comprises cells exhibiting endothelial recruitment and/or angiogenesis.7. The method of claim 2 , wherein said migrating cancer spreads via seeding the surface of the peritoneal claim 2 , pleural claim 2 , pericardial claim 2 , or subarachnoid spaces.8. The method of claim 2 , wherein said migrating cancer spreads via the lymphatic system.9. The method of claim 2 , wherein said migrating cancer spreads hematogenously.10. The method of claim 2 , wherein said migrating cancer is a cell migration cancer.11. The method of claim 10 , wherein said cell migration cancer is a non-metastatic cell migration cancer.12. The method of claim 11 , where said cell migration cancer is ovarian cancer claim 11 , mesothelioma claim 11 , or primary lung cancer.13. The method of claim 1 , wherein said cancer is breast cancer claim 1 , colon cancer claim 1 , renal cell cancer claim 1 , non-small cell lung cancer claim 1 , hepatocellular carcinoma claim 1 , gastric cancer claim 1 , ovarian cancer claim 1 , pancreatic cancer claim 1 , esophageal cancer claim 1 , prostate cancer claim 1 , sarcoma claim 1 , or melanoma.14. The method of claim 1 , wherein said cancer is gastrointestinal cancer.15. The method of claim 14 , wherein said gastrointestinal cancer is esophageal cancer claim 14 , stomach cancer claim 14 , pancreatic cancer claim 14 , liver cancer claim 14 , ...

PREPARATION OF A HYDROXYALKYL PHOSPHONIC ACID

The present invention is a process for converting a phosphonate to a hydroxyalkyl phosphonic acid comprising the step of contacting together water, the phosphonate, and a sulfonated or phosphonated heterogeneous catalyst under conditions sufficient to convert at least 50% of the phosphonate to the hydroxyalkyl phosphonic acid. The process of the present invention provides a way of preparing hydroxyalkyl phosphonic acids safely and economically, without corrosive effects. 1. A process for converting a phosphonate , which is a hydroxyalkyl- or acyloxyalkyl-phosphonate , to a hydroxyalkyl phosphonic acid comprising the step of contacting together water , the phosphonate , and a sulfonated or phosphonated heterogeneous catalyst under conditions sufficient to convert at least 50% of the phosphonate to the hydroxyalkyl phosphonic acid.2. The process of wherein the heterogeneous catalyst is a sulfonated crosslinked macroreticular ion exchange resin or a sulfonated microporous aluminosilicate mineral.3. The process of wherein the heterogeneous catalyst is a sulfonated crosslinked macroreticular ion exchange resin claim 2 , and wherein phosphonate is contacted with the sulfonated crosslinked ion-exchange resin at a temperature of from 80° C. to 120° C. for 1 to 24 hours to convert at least 70% of phosphonate to the hydroxyalkyl phosphonic acid.5. The process of wherein R is acetyl claim 4 , wherein methyl acetate and methanol are formed in addition to the hydroxyalkyl phosphonic acid.6. The process of wherein the methyl acetate and methanol are removed during the conversion of the phosphonate to the hydroxyalkyl phosphonic acid by way of azeotropic distillation.7. The process of wherein the phosphonate is dimethyl-2-(acetyloxy)ethyl phosphonate claim 6 , and the hydroxyalkyl phosphonic acid is 2-hydroxyethyl phosphonic acid.8. The process of wherein the dimethyl-2-(acetyloxy)ethyl phosphonate is contacted with the sulfonated ion-exchange resin at 90° C. to 110° C. for 1 to ...

Method for the synthesis of alpha-aminoalkylenephosphonic acid

The present invention is related to a new method for the synthesis of alpha-aminoalkylenephosphonic acid or its phosphonate esters comprising the steps of forming a reaction mixture by mixing a P—O—P anhydride moiety comprising compound, having one P-atom at the oxidation state (+III) and the other P-atom at the oxidation state (+III) or (+V), an aminoalkanecarboxylic acid and an acid catalyst, wherein said reaction mixture comprises an equivalent ratio of alpha-aminoalkylene carboxylic acid to P—O—P anhydride moieties of at least 0.2, and recovering the resulting alpha-aminoalkylene phosphonic acid compound or an ester thereof from the reaction mixture.

Substituted bisphenyl butanoic phosphonic acid derivatives as nep inhibitors

The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.

S1PR2 ANTAGONISTS AND USES THEREFOR

Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are compounds which contain bioisosteric replacements of the urea group of JTE-013 and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis. 3. The method of claim 2 , wherein{'sup': '1', 'sub': '3', 'Ris CH; and'}{'sup': '2', 'sub': '3', 'Ris CH.'}4. The method of claim 3 , wherein{'sup': '3', 'Ris H; and'}{'sup': '4', 'sub': 1', '6, 'Ris C-Calkyl.'}5. The method of claim 4 , wherein{'sup': '4', 'sub': 3', '2, 'Ris CH(CH).'}6. The method of claim 5 , wherein{'sup': '5', 'Ris halogen.'}7. The method of claim 6 , wherein{'sup': '5', 'Ris Cl; and'}n is 2.8. The method of claim 2 , wherein{'sup': '1', 'sub': '3', 'Ris CH;'}{'sup': '2', 'sub': '3', 'Ris CH;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'sub': 3', '2, 'Ris CH(CH);'}{'sup': '5', 'Ris Cl; and'}n is 2.9. The method of claim 1 , wherein the ocular diseases include familial exudative vitreoretinopathy.10. The method of claim 1 , wherein the compound of formula IX is a S1PR2 antagonist.13. The compound of claim 12 , wherein{'sup': '3', 'Ris H; and'}{'sup': '4', 'sub': 1', '6, 'Ris C-Calkyl.'}14. The compound of claim 13 , wherein{'sup': '5', 'Ris Cl; and'}n is 2.15. The compound of claim 11 , wherein{'sup': '1', 'sub': '3', 'Ris CH;'}{'sup': '2', 'sub': '3', 'Ris CH;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'sub': 3', '2, 'Ris CH(CH);'}{'sup': '5', 'Ris Cl; and'}n is 2.16. The compound of claim 11 , wherein the eye condition includes familial exudative vitreoretinopathy.17. The compound of claim 11 , wherein the eye condition includes an inability to normally vascularize the eye.18. The compound of claim 11 , wherein the eye condition includes secondary aberrant neovascularization.20. The method of claim 19 , wherein ...

PRODRUGS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR

Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA 140.-. (canceled)42. The composition of claim 41 , wherein the compound is a compound of formula (I) and:{'sub': '1', 'Ris H;'}{'sub': 2', '3', '5', '6', 'n', '7', '5', '6', 'n', '7', '5', '6', 'n', '7', '5', '6', 'n', '7', '5', '6', 'n', '7, 'Rand Rare each selected from the group consisting of H, —(CRR)—O—R, —(CRR)—Ar—O—C(═O)—R, —(CRR)—O—C(═O)—R, —Ar—C(═O)—O—(CRR)—R, and —(CRR)—O—C(═O)—O—R; and'}{'sub': 4', '5', '6', 'n', '7', '5', '6', 'n', '7', '5', '6', 'n', '7', '5', '6', 'n', '7', '5', '6', 'n', '7, 'Ris selected from the group consisting of —(CRR)—O—R, —(CRR)—Ar—O—C(═O)—R, —Ar—C(═O)—O—(CRR)—R, —(CRR)—O—C(═O)—Rand —(CRR)—O—C(═O)—O—R; or'}pharmaceutically acceptable salts thereof43. The composition of claim 41 , wherein the compound is a compound of formula (I) and:{'sub': '1', 'Ris alkyl;'}{'sub': 2', '3', '5', '6', 'n', '7', '5', '6', 'n', '7', '5', '6', 'n', '5', '6', 'n', 'm', '7', '5', '6', 'n', '7', '5', '6', 'n', '7, 'Rand Rare each independently selected from the group consisting of H, alkyl, —(CRR)—O—R, —(CRR)—Ar—O—C(═O)—R, —(CRR)—O—[(CRR)—O]—R, —(CRR)—O—C(═O)—Rand —(CRR)—O—C(═O)—O—R; and'}{'sub': 4', '5', '6', 'n', '7', '5', '6', 'n', '7', '5', '6', 'n', '5', '6', 'n', 'm', '7', '5', '6', 'n', '7', '5', '6', 'n', '7, 'Ris selected from the group consisting of —(CRR)—O—R, —(CRR)—Ar—O—C(═O)—R, —(CRR)—O—[(CRR)—O]—R, —(CRR)—O—C(═O)—Rand —(CRR)—O—C(═O)—O—R; or'}pharmaceutically acceptable salts thereof44. The composition of claim 41 , wherein the compound is a compound of formula (I) and:{'sub': 1', '5', '6', 'n', '7', '5', '6', 'n', '7, 'Ris selected from —(CRR)—O—C(═O)—Rand —(CRR)—O—C(═O)—O—R; and'}{'sub': 2', '3', '4', '5', '6', 'n', '7', '5', '6', 'n', '7, 'RR, and Rare each independently selected from H, Ar, —(CRR)—O—C(═O)—R, and —(CRR)—O—C(═O)—O—R; or'}pharmaceutically acceptable salts thereof45. ...

Electronic switching element

The invention relates to an electronic switching element (1), which comprises in this order a first electrode (16), a molecular layer (18), which is bonded to a substrate, and a second electrode (20), wherein the molecular layer essentially consists of compounds of formula (I) indicated in claim 1, wherein a mesogenic group is bonded to the substrate via a spacer group (Sp) by means of an anchor group (G). The electronic switching element is suitable for the production of components (1) as a memristive device for digital information storage.

Oxidation inhibitors for amine degradation

Inhibitors and methods for preventing oxidative degradation in amine scrubbing system are disclosed herein. The substances disclosed in the present invention will be affective for aqueous solutions of other amines (particularly primary amines) prone to oxidation by molecular oxygen, as well as other concentrations of MEA, which are used in CO2 capture systems (namely 3-11 molal). The inhibitors disclosed herein include hydroxyethylidene diphosphonic acid (HEDP), diethylene triamine penta acetic acid (DPTA), diethylenetriamine penta (methylene phosphonic acid) (DTPMP), ethylenediamine tetra (methylene phosphonic acid) (EDTMP), and citric acid. The compounds of the present invention act as potent chelating agents to sequester metal ions and prevent metal-catalyzed homolytic decomposition of reactive peroxides in solution, thus preventing amine oxidation.

Derivati di acidi amminofosfonici guamidati dotati di attivita' biocida e loro procedimento di preparazione

Method of making phosphono-phosphate containing compounds

A method of making a phosphono-phosphate compound is disclosed. The method involves a first step of mixing a first component comprising a phosphonic acid, a phosphonate or mixtures thereof, with a second component comprising a source of phosphoric acid or phosphate. The mixture has a molar phosphorous ratio of the first component to the second component of from 1:1 to 1:10. The second step involves either physically or chemically dehydrating the mixture to produce a phosphono-phosphate compound.

Pesticidally active salts and compositions containing them and processes for their manufacture and use

N-(benzyl)aminoalkylcarboxylates, phosphinates, phosphonates and tetrazoles as edg receptor agonists

The present invention encompasses compounds of Formula (I) as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Dental material on the basis of acryloester phosphonic acid

Acrylic ester phosphonic acids and their stereoisomers and mixtures are new. Novel acrylic ester phosphonic acids are of formula (I), their stereoisomers and mixtures also being new. R1 when n=1 = group of formula (A) or (B); R1 when n=2 = group of formula (C)-(E); R2 = 1-12C alkylene, 4-8C cycloalkylene or 7-15C alkylenephenylene; R3 = H, 1-5C alkyl or 1-5C O-alkyl; and R4 and R5 = 1-5C alkyl or 1-5C O-alkyl. An Independent claim is also included for compositions containing (I).

A PROCEDURE FOR THE MANUFACTURE OF N-PHOSPHONOMETILIMINODIACETIC ACID

Un procedimiento para la fabricacion de ácido N-fosfonometiliminodiacético (PMIDA) que comprende las etapas de: (a) neutralizacion de una solucion acuosade la sal de sodio o potasio del ácido iminodiacético (Na2IDA o K2IDA) con un ácido mineral fuerte a temperaturas de 10 a 80*C; (b) separacion del ácidoiminodiacético (IDA) de la solucion de reaccion de la etapa (a); (c) transformacion del ácido iminodiacético con formaldehído y ácido fosforoso en solucionacuosa, en presencia de un ácido mineralfuerte a temperaturas de 100 a 150*C, en caso dado bajo atmosfera de un gas de proteccion, para formar el ácidoN-fosfonometiliminodiacético; y (d) separacion del ácido N-fosfonometiliminodiacético de la solucion de reaccion de la etapa (c), por ejemplo por filtracion;método en el cual la solucion de reaccion acuosa de la etapa (d) (aguas madres), que contiene pequenas cantidades de ácido N-fosfonometiliminodiacético,componentes de reaccion y productos secundarios, es reciclada a la etapa de neutralizacion (a). De este modo es posible lograr no solamente una disminucion delnumero de corrientes de desechos, sino también una reduccion cuantitativa drástica de la cantidad total de la corriente de desechos, pudiéndose renunciar a laseparacion por esclusado de una cantidad parcial, usual con otros métodos de reciclado. A process for the manufacture of N-phosphonomethyliminodiacetic acid (PMIDA) comprising the steps of: (a) neutralization of an aqueous solution of the sodium or potassium salt of the iminodiacetic acid (Na2IDA or K2IDA) with a strong mineral acid at temperatures of 10 at 80 * C; (b) separation of the iminodiacetic acid (IDA) from the reaction solution of step (a); (c) transformation of the iminodiacetic acid with formaldehyde and phosphorous acid into a solution, in the presence of a strong mineral acid at temperatures of 100 to 150 * C, if necessary under the atmosphere of a protective gas, to form the N-phosphonomethyliminodiacetic acid; and (d) separation of the N ...

PROCEDURE FOR PREPARING N-PHOSPHONOMETILIMINE-DIACETIC ACID

La presente se refiere a un procedimiento para elaborar ácido N-fosfonometilimino-diacético por transformacion de una sal de metal alcalino del ácido imino-diacético con tricloruro de fosforo en solucion acuosa, formándose el clorhidrato del ácido imino-diacético, ácido fosforoso y el cloruro de metal alcalino correspondiente, subsiguiente transformacion con una fuente de formaldehído y, si se desea, la obtencion del ácido N-fosfonometilimino-diacético a partir de la mezcla reaccionante, eliminándose de la mezcla reaccionante agua que, dado el caso, contiene HCl, durante y/o después de la transformacion de la sal de metal alcalino del ácido imino-diacético con el tricloruro de fosforo, hasta que exista una concentracion de clorhidrato de ácido imino-diacético de por lo menos 40%, con respecto al peso de la mezcla reaccionante, descontando el peso del cloruro de metal alcalino. El procedimiento posibilita la elaboracion de ácido N-fosfonometilimino-diacético de manera sencilla y con alto rendimiento. This refers to a process for making N-phosphonomethylimino-diacetic acid by transforming an alkali metal salt of imino-diacetic acid with phosphorus trichloride into an aqueous solution, forming imino-diacetic acid hydrochloride, phosphorous acid and chloride. corresponding alkali metal, subsequent transformation with a source of formaldehyde and, if desired, obtaining N-phosphonomethylimino-diacetic acid from the reaction mixture, eliminating water from the reaction mixture which, if necessary, contains HCl, during and / or after the transformation of the alkali metal salt of the imino-diacetic acid with the phosphorus trichloride, until there is a concentration of imino-diacetic acid hydrochloride of at least 40%, with respect to the weight of the mixture reactant, discounting the weight of alkali metal chloride. The process allows the elaboration of N-phosphonomethylimino-diacetic acid in a simple way and with high yield.

A PROCEDURE FOR THE MANUFACTURE OF N-PHOSPHONOMETILIMINODIACETIC ACID.

Se describe un procedimiento para la fabricacion de ácido N-fosfonometiliminodiacético por medio de la transformacion de ácido iminodiacético con ácidofosforoso y formaldehído en solucion acuosa, en presencia de un ácido mineral fuerte,procedimiento que está caracterizado porque la reaccion es realizada auna temperatura de 110 a 150*C bajo una atmosfera de gas de proteccion. Las ventajas principales de este procedimiento son los elevados rendimientos y lapureza con respecto alácido N-fosfonome tiliminodiacético, como así también el consumo casi estequiométrico de materias primas y, por lo tanto, las menorescantidades de desechos. A process is described for the manufacture of N-phosphonomethyliminodiacetic acid by means of the transformation of iminodiacetic acid with acid phosphorus and formaldehyde into an aqueous solution, in the presence of a strong mineral acid, a procedure characterized in that the reaction is carried out at a temperature of 110 to 150 * C under a protective gas atmosphere. The main advantages of this procedure are the high yields and stiffness with respect to the N-phosphonome tiliminodiacetic acid, as well as the almost stoichiometric consumption of raw materials and, therefore, the lower amounts of waste.

Process

Process

Sett att framstella nya 11-desoxi-prostaglandin-f?712-derivat

Processo para a producao de ditiobis-alcanossulfonatos e fosfonatos

Poly (ethylene glycol) containing chemically disparate endgroups

The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Il-6 production inhibitors

IL-6 production inhibitors containing as the active ingredient hydroxamic acid derivatives represented by the following general formula (I) or equivalents thereto, non-toxic salts thereof or prodrugs of the same, (I) wherein each symbol is as defined in the description. Because of having an IL-6 production inhibitory activity, the compounds of the general formula (I) are useful as preventives and/or remedies for various inflammatory diseases, sepsis, multiple myeloma, plasmacytoid leukemia, osteoporosis, cachexia, psoriasis, nephritis, kidney cell cancer, Kaposi's sarcoma, rheumatoid arthritis, hypergamma globulinemia, Castleman's disease, intra-atrial myxoma, diabetes, autoimmune diseases, hepatitis, colitis, graft-versus-host disease, infections, endometriosis and solid cancer.

Method of preparing n-(perfluoroacyl)-n-phosphomethylglycins

1494603 N - (Perfluoroalkanoyl) - N - phosphonomethyl glycine compounds MONSANTO CO 21 May 1976 [23 May 1975] 21191/76 Heading C2P Novel N-phosphonomethyl glycine compounds have the formula where R is H or a group C n F 2n+1 CO- and each n is 1-4. The compounds are prepared from N-phosphonomethyl glycine and a perfluoroalkanoic acid anhydride of the formula (C n H 2n+1 CO) 2 O where each n is 1-4, in the presence of a perfluoroalkanoic acid of formula C n F 2n+1 COOH where n is 1-4, which produces a compound in which R is C n F 2n+1 CO-, followed by hydrolysis with water to produce the corresponding compound in which R is H. Preferably the perfluoroalkanoic acid has the same number of C atoms as both individual segments of the anhydride. The compounds are used in herbicidal compositions.

Herbicidic composition

This disclosure relates to N-hydroxy-N-phosphonomethylglycine and the herbicidally acceptable salts thereof which are useful as herbicides to control undesired plants.

Water treatment method

FIELD: chemistry. SUBSTANCE: invention relates to a water treatment method. The method, which enables to use an aqueous medium in conditions of excluding considerable interference from metal ions, involves adding a phosphonate compound to the water. The phosphonate compound contains a certain phosphonate fragment and a fragment selected from a limited number of compounds; or hydrocarbon chains containing substitutes in form of aminoalkylene phosphonic acids; or alkylaminoalkylene phosphonic acids containing an active fragment which includes N, O and S. EFFECT: invention can be used in secondary oil recovery, inhibiting formation of salt deposits, treating water used for industrial purposes, treating paper mass and as an agent which binds metal ions into a chelate complex or dispersant. 10 cl, 5 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 494 049 (13) C2 (51) МПК C02F 5/14 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2010134907/05, 21.01.2009 (24) Дата начала отсчета срока действия патента: 21.01.2009 (73) Патентообладатель(и): ДЕКВЕСТ АГ (CH) (43) Дата публикации заявки: 27.02.2012 Бюл. № 6 2 4 9 4 0 4 9 (45) Опубликовано: 27.09.2013 Бюл. № 27 (56) Список документов, цитированных в отчете о поиске: ЕР 0375800 А1, 04.07.1990. US 5112496 А, 12.05.1992. US 4080375 А, 21.03.1978. US 4079006 A, 14.03.1978. RU 2100294 C1, 27.12.1997. SU 859330 А1, 30.08.1981. 2 4 9 4 0 4 9 R U (86) Заявка PCT: EP 2009/050668 (21.01.2009) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 23.08.2010 (87) Публикация заявки РСТ: WO 2009/092738 (30.07.2009) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры" (54) СПОСОБ ОБРАБОТКИ ВОДЫ (57) Реферат: Изобретение относится к способу обработки воды. Способ, обеспечивающий применение водной среды в условиях исключения значительной помехи со стороны ионов металлов, включает добавление к воде фосфонатного ...

Herbicide

포스포네이트 결합 조성물

본 발명은 하나 이상의 포스포네이트 또는 포스피네이트 잔기, 및 방향족 니트로소 또는 방향족 니트로소 전구체 및 이들의 조합물로부터 선택된 하나 이상의 잔기를 포함하는 화합물을 제공한다. 이러한 화합물을 포함하는 접착제 조성물은 금속 및 또는 유리와 같은 히드록실화된 표면에 대한 중합체의 결합에서 유용성을 나타낼 수 있다. 적합한 중합체에는 천연 및 합성 고무가 포함된다. 방향족 니트로소 전구체는 하나 이상의 퀴논 디옥심 또는 퀴논 옥심과 같은 니트로소벤젠 전구체일 수 있다.

Acrylic ester phosphonic acid based dental materials

Poly(ethylene glycol) containing chemically disparate endgroups

The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Poly(ethylene glycol) containing chemically disparate endgroups

The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Poly(ethylene glycol) containing chemically disparate endgroups

The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Poly(ethylene glycol) containing chemically disparate endgroups

The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.