НОВЫЕ ПРОИЗВОДНЫЕ ГИДРОКСАМОВОЙ КИСЛОТЫ, ПОЛЕЗНЫЕ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С ДЕГЕНЕРАЦИЕЙ СОЕДИНИТЕЛЬНОЙ ТКАНИ

Изобретение относится к производным гидроксамовой кислоты формулы I, где X означает -CH2-, -NR5-, -C(O); Y означает -CH2-, -NR5, при условии, что если X является -NR5-, то Y означает -CH2-; R1 означает H, C1-C20 алкил, -(CH2)j арил, -(CH2)j циклоалкил и др.; R2 означает H, C1-C20-алкил, -(CH2)j -R8, -(CH2)j -NR6R7, -(CH2)j -NR5-; -C(O)R5 и др.; R3 означает H, C1-C6алкил, -(CH2)j-арил, -(CH2)j - C3-6-циклоалкил и др., R5 означает H, C1-C6алкил, возможно замещенный 1 - 3 галогенами и др.; R6 и R7, одинаковые или различные, и означают H, C1-C6алкил и др., R8 означает -S-R8 и др., R9-галоген, C1 -C6 алкил и др., R10 - H; арил - фенил, возможно замещенный, Het - пиридинил, тиенил и др., i - 1 - 6, j - 0 - 4. Соединения I ингибируют избыток матрицы металлопротеиназы, что позволяет использовать их в фармацевтической композиции. 2 с. и 12 з.п.ф-лы, 1 табл.

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ ИМИДАЗОЛИДИНА, СПОСОБ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ

Изобретение относится к замещенным производным имидазолидина формулы 1 где W обозначает R1 -A-C(R13) или где кольцевая система может быть замещена 1, 2 или 3 одинаковыми или различными заместителями R13 и где L обозначает C(R13) и ml и m2 независимо друг от друга означают 0, 1, 2, 3 или 4, причем сумма ml + m2 равна 3 или 4; Y обозначает карбонильную группу; A обозначает прямую связь или двухвалентный остаток фенилена, В обозначает двухвалентный (С1–C6 )-алкиленовый остаток, причем (С1 –C6)-алкиленовый остаток незамещен или замещен одним или несколькими одинаковыми или различными остатками из ряда (С1–C8 )-алкил и (С3–C10 )-циклоалкил-(С1–C6)-алкил, Е обозначает R10CO, HCO или R8O-CH2; R - Н или (C1-C8 )-алкил, (С3–C12 )-циклоалкил-(С1–C8)-алкил или в случае необходимости замещенный (С6–C14)-арил, причем все остатки R независимо друг от друга могут быть одинаковыми или различными; R1 - Н, (C1-C10)-алкил, который, при необходимости, может быть однократно или многократно замещен фтором, или ...

ПРОИЗВОДНЫЕ ИМИДАЗОЛИДИНА, ИХ ПОЛУЧЕНИЕ И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ НА ИХ ОСНОВЕ

Настоящее изобретение относится к новым производным имидазолидина формулы (I), в которой А означает циклопропилметил- или изобутил; Е означает -CO-R6 или -СН2-O-R7; Z означает кислород; R1 означает водород или метил; R2 означает фенил, пиридил или (С1-С4)алкил; R3 и R4 означают метил или трифторметил; R5 означает водород или (C1-С4)алкил; R6 означает гидроксил, (С1-С10)алкокси или амино; R7 означает водород; или его стереоизомерам R-конфигурации или S-конфигурации, или смеси стереоизомеров R/S-конфигурации, или физиологически толерантным солям указанного соединения. Соединения формулы (I) являются ценными фармацевтически активными соединениями, пригодными для лечения воспалительных заболеваний, например ревматоидного артрита, или аллергических заболеваний. Соединения формулы (I) являются ингибиторами адгезии и миграции лейкоцитов и/или антагонистами адгезионного рецептора VLA-4, относящегося к группе интегринов. Указанные соединения пригодны для лечения заболеваний, вызываемых нежелательной ...

СУЛЬФОНАМИДНОЕ ПРОИЗВОДНОЕ, ЛЕКАРСТВЕННОЕ СРЕДСТВО, СПОСОБЫ ЛЕЧЕНИЯ

Объектом изобретения является сульфонамидное соединение формулы I, обладающее действием, ингибирующим активность матриксной металлопротеиназы-13 и агликаназы, где R1- NHOH; R2 - группа -A-R6, где А - алкилен C1-С6; R6 - группа формулы II, где Х - группа -N(R10)-; R7и R8 , одинаковые или различные, - Н, C1-С6 алкил, СООН, низший алкокси, галоген, фенил или R7 и R8 вместе с атомами углерода, к которым они присоединены, образуют ненасыщенное С3-С7 кольцо, арил С6-С10, гетероарил С5-С7, содержащий 1 или 2 кольцевых атома азота или серы; R10 - Н, C1-6 алкил; R3 - Н, С1-6 алкил, возможно замещенный галогеном, фенилом, необязательно замещенным галогеном, или алкинил С3-10; R4 - фенилен; R5 - C1-6 алкил, необязательно замещенный по меньшей мере одним атомом галогена, 5- или 6-членный гетероарил, содержащий 1 или 2 атома N, фенил, необязательно замещенный по меньшей мере одним атомом галогена. Соединения I пригодны для лечения артрита или остеоартрита. 4 с. и 14 з.п. ф-лы, 11 табл.

ЦИКЛИЧЕСКИЕ АМИДЫ ИЛИ ИХ СЕЛЬСКОХОЗЯЙСТВЕННО ПРИГОДНЫЕ СОЛИ, ФУНГИЦИДНАЯ КОМПОЗИЦИЯ, СПОСОБ БОРЬБЫ С БОЛЕЗНЯМИ РАСТЕНИЙ, ВЫЗВАННЫМИ ФИТОПАТОГЕННЫМИ ГРИБАМИ

Изобретение относится к циклическим амидам , замещенным в α-положении различными арильными группами, их сельскохозяйственно пригодным солям и составам на их основе, и их использованию в качестве фунгицидов системного или избирательного действия. Указанные соединения представлены общей формулой I (значение радикалов см. в формуле изобретения). 3 с. и 8 з.п.ф-лы, 33 табл.

2-[(4-ГЕТЕРОЦИКЛ-ФЕНОКСИМЕТИЛ)ФЕНОКСИ]-АЛКАНОАТЫ, ГЕРБИЦИДНАЯ КОМПОЗИЦИЯ, СПОСОБ ПОДАВЛЕНИЯ НЕЖЕЛАТЕЛЬНОЙ РАСТИТЕЛЬНОСТИ

Обладающие гербицидной активностью новые 2-(/4-гетероцикл-феноксиметил/фенокси)-алканоаты общей формулы I, приведенной в формуле изобретения, где Q - 4-дифторметил-4,5-дигидро-3-метил-1,2,4-триазол-5/1H/-OH-1-ил, или 1-метил-6-трифторметил-2, 4-/1H, 3H/-пиримидиндион-3-ил; A - группа формулы RO-C(О)-C(R1)H-, где R' - H, CH3, R - H, низший алкил, незамещенный или замещенный хлором, или группа -(CHR7 - CH2 - O)nR8, где R7 - H или метил; R8 - низший алкил; n - 1 или 2; X - H, метил, F или Cl; W - O или S; Z - H, F, Cl, Br, низший алкил или метокси; Z' - H, F или Cl; или Z и Z' - взятые вместе могут представлять собой -(CH2)4 - для образования тетрагидронафтильной группы, используют в создании гербицидной композиции, которую применяют в способе борьбы с нежелательной растительностью. 3 с. и 17 з.п. ф-лы, 5 табл.

ИНГИБИТОРЫ МЕТАЛЛОПРОТЕИНАЗ

... 1. Соединение формулы I или его фармацевтически приемлемая соль или in vivo гидролизуемый эфир где X выбран из NR1, О, S; Y1 и Y2 независимо выбраны из О, S; Z выбран из NR2, О, S; m равно 0 или 1; А выбран из прямой связи, (С1-6)алкила, (С1-6)алкенила, (С1-6)галогеноалкила или (С1-6)гетероалкила, содержащего гетерогруппу, выбранную из N, О, S, SO, SO2, или содержащего две гетерогруппы, выбранные из N, О, S, SO, SO2 и разделенные по меньшей мере двумя атомами углерода; R1 выбран из Н, алкила, галогеноалкила; R2 выбран из Н, алкила, галогеноалкила; R3 и R6 независимо выбраны из Н, галогена (предпочтительно F), алкила, галогеноалкила, алкоксиалкила, гетероалкила, циклоалкила, арила, алкиларила, гетероалкил-арила, гетероарила, алкилгетероарила, гетероалкил-гетероарила, арилалкила, арил-гетероалкила, гетероарил-алкила, гетероарил-гетероалкила, бисарила, арил-гетероарила, гетероарил-арила, бисгетероарила, циклоалкила или гетероциклоалкила, содержащих от 3 до 7 кольцевых атомов, где алкильный ...

2, 5-ДИОКСОИМИДАЗОЛИДИН-4-ИЛ-АЦЕТАМИДЫ И ИХ АНАЛОГИ В КАЧЕСТВЕ ИНГИБИТОРОВ МЕТАЛЛОПРОТЕИНАЗЫ ММР-12

... 1. Соединение формулы (I) или его фармацевтически приемлемая соль или сольват где Х представляет собой атом кислорода или группу NR4 или СН2; Y представляет собой NH или N-метил; каждый из Z1 и Z2 независимо представляет собой атом кислорода или серы, при условии, что по меньшей мере один из Z1 и Z2 представляет собой атом кислорода; либо R1 представляет собой водород или группу, выбранную из C1-С6алкила и насыщенной или ненасыщенной 3-10-членной кольцевой системы, которая может содержать по меньшей мере один кольцевой гетероатом, выбранный из азота, кислорода и серы, причем каждая группа возможно замещена по меньшей мере одним заместителем, выбранным из галогена, гидроксила, циано, карбоксила, -NR5R6, -CONR7R8, C1-С6алкила, C1-С6алкокси, C1-С6алкилкарбонил(окси), -S(O)mC1-С6алкил, где m представляет собой 0, 1 или 2, C1-С6алкилсульфониламино, С1-С6алкоксикарбонил(амино), бензилокси и насыщенного или ненасыщенного 5-6-членного кольца, которое может содержать по меньшей мере один кольцевой ...

ИНГИБИТОРА МЕТАЛЛОПРОТЕИНАЗ

... 1. Соединение формулы I или его фармацевтически приемлемая соль или in vivo гидролизуемый эфир где Х выбран из NR1, О, S; Y1 и Y2 независимо выбраны из О, S; Z выбран из NR2, О, S; m равно 0 или 1; А выбран из прямой связи, (С1-6)алкила, (С1-6)алкенила, (С1-6)галогеноалкила или (С1-6)гетероалкила, содержащего гетерогруппу, выбранную из N, О, S, SO, SO2, или содержащего две гетерогруппы, выбранные из N, О, S, SO, SO2 и разделенные по меньшей мере двумя атомами углерода; R1 выбран из Н, алкила, галогеноалкила; R2 выбран из Н, алкила, галогеноалкила; R3 и R6 независимо выбраны из Н, галогена (предпочтительно F), алкила, галогеноалкила, алкоксиалкила, гетероалкила, циклоалкила, арила, алкил-циклоалкила, алкил-гетероциклоалкила, гетероалкил-циклоалкила, гетероалкил-гетероциклоалкила, циклоалкил-алкила, циклоалкил-гетероалкила, гетероциклоалкил-алкила, гетероциклоалкил-гетероалкила, алкиларила, гетероалкил-арила, гетероарила, алкилгетероарила, гетероалкил-гетероарила, арилалкила, арил-гетероалкила ...

КОСМЕТИЧЕСКИЕ ИЛИ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, ВКЛЮЧАЮЩИЕ ЛИПОСОМЫ, И СПОСОБ ИХ ПОЛУЧЕНИЯ

Предложены косметические и фармацевтические композиции, включающие липосомы, содержащие действующее начало формулы,где R- цианильный или нитрильный радикал или галогенный атом; R- трифторметильный радикал или галогенный атом; группа - A - B -,где X - атом кислорода; R- атом водорода или алкильный радикал; Y - атом кислорода, серы или радикал =NH.

СЛОЖНОЭФИРНОЕ СОЕДИНЕНИЕ И ЕГО ПРИМЕНЕНИЕ

... 1. Сложноэфирное соединение, представленное формулой (1):где Rобозначает C-Cалкил.2. Сложноэфирное соединение по п.1, где относительная конфигурация заместителя по положению 1 циклопропанового кольца и заместителя по положению 3 циклопропанового кольца представляет транс-конфигурацию в формуле (1).3. Сложноэфирное соединение по п.1, где абсолютная конфигурация положения 1 циклопропанового кольца представляет R-конфигурацию в формуле (1).4. Сложноэфирное соединение по п.1, где абсолютная конфигурация положения 1 циклопропанового кольца представляет R-конфигурацию, и относительная конфигурация заместителя по положению 1 циклопропанового кольца и заместителя по положению 3 циклопропанового кольца представляет транс-конфигурацию в формуле (1).5. Сложноэфирное соединение по любому из пп.1-4, где двойная связь заместителя по положению 3 циклопропанового кольца имеет E-конфигурацию или смесь E-конфигурации и Z-конфигурации, и доля конфигурации Е составляет 50% или более в формуле (1).6. Сложноэфирное ...

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ТИАЗОЛИДИНДИОНА, ОКСАЗОЛИДИНДИОНА И ГИДАНТОИНА

... 1. Способ получения производного тиазолидиндиона, оксазолидиндиона или гидантоина формулы (I) из соединения формулы (II): где Q означает атом кислорода или атом серы, - Q1 означает атом кислорода или атом серы, - R1 и R2, одинаковые или различные, означают атом водорода, C1-С10-алкил, циклоалкил, алкиларил, арилалкил, при этом указанные группы: алкил, циклоалкил, алкиларил и арилалкил необязательно замещены алкилом, алкокси или арилокси, галогеном, гидрокси, сульфино, сульфонилом, амином, таким как NH2, NHR3, N(R3)2, где R3 означает алкил, алкокси или алкилкарбонил, отличающийся тем, что соединение формулы (II) вводят в реакцию с муравьиной кислотой, используемой либо в качестве донора водорода при реакции переноса водорода, либо в качестве растворителя при реакции гидрогенизации, в присутствии катализатора на основе переходного металла для получения соответствующего соединения формулы (I). 2. Способ по п.1, отличающийся тем, что муравьиная кислота представляет собой 100%-ую муравьиную ...

Способ получения рацемического -окси-фЕНил- -гидАНТОиНА

1. A process of preparation of R.S. 5-p-hydroxyphenyl hydantoin, characterized by hot condensing in an acid medium R.S. p-hydroxymandelic acid on urea in excess.

Способ получения 5-[3-(бицикло[2.2.1]-гепт-2-илокси)-4-метоксифенил]гексагидро-2-пиримидинона

Изобретение относится к гетероциклическим соединениям, в частности к получению (бицикло 2.2„ ij-гепт- 2-илокси) -4-метоксиФенилТгексагидро- 2-пиримидинона, который может найти применение в медицине. Дель изобретения - разработка способа получения указанных соединений. Получение ведут циклизацией соответственно замещенного глутарамида в реакционно- инертном растворителе при комнатной температуре в присутствии тетрааце- тата свинца. I IB ...

Verfahren zur Herstellung chiraler, nicht racemischer (4-Aryl-2,5-dioxoimidazolidin-1-yl)essigsäuren

PHARMAKOLOGISCH AKTIVE CATECHOLDERIVATE

VERFAHREN ZUR HERSTELLUNG VON DL-BETA-ARYLAMINOSAEUREN

VERFAHREN ZUR HERSTELLUNG EINES SPIROIMIDAZOLIDINS

ESTERS OF CYCLOPROPANE-CARBOXYLIC ACIDS RELATED TO PYRETHRIC ACID, THEIR PREPARATION AND USE AS INSECTICIDES

PROCESS FOR THE PREPARATION OF HYDANTOINS

HYDANTOINE

HYDANTOIN DERIVATIVES AND SALTS THEREOF, THEIR SYNTHESIS AND INTERMEDIATES, AND PHARMACEUTICAL FORMULATIONS

Verfahren zur Darstellung von Hydantoinen

Polycarbonsaeureester

PROCESS FOR PRODUCING DIACYLAMINOACETOANILIDE DERIVATIVES

... 1420564 Preparation of -aliphatic acyl-- diacylamino-acetanilide derivatives FUJI PHOTO FILM CO Ltd 11 Feb 1974 [15 Feb 1973] 06216/74 Heading C2C -Aliphatic acyl--diacylamino-acetanilide derivatives are obtained by reacting the corresponding -aliphatic acyl--halogenoacetanilide derivative with the corresponding diacylamine derivative in the presence of a base (e.g. NaOH, KOH, (C 2 H 5 ) 3 N, diazabicyclooctane) and in an organic amide (e.g. lactam, urea) or sulphoxide as solvent. [Aliphatic acyl denotes that the carbonyl carbon is attached to a non-aromatic carbon atom.] Preferred solvents are those having a dielectric constant at 20‹ C. of 30 or more, particularly dimethylformamide, dimethylsulphoxide, dimethylacetamide, hexamethylphosphoramide, N-methyl-2-pyrrolidone and tetramethylurea. The following reaction sequences illustrate the condensation wherein R1 is an alkyl, alkenyl, cycloalkyl or aralkyl radical, R2 is an aromatic radical, X is a halogen atom and Z represents ...

5-carboxy-hydantoin chelates for use in the preparation of amino acids

Novel 5-carboxyhydantoin chelates of general formula wherein R1 and R2 are H or monovalent organic groups and M is Mg, Zn or Ca are prepared by (a) reaction of a metal alkyl carbonate of formula wherein M is Mg, Zn or Ca and R3 is an alkyl group, with a hydantoin of formula wherein R2 is as defined above and R1 is an organic group, (b) by reaction of a metal alkyl carbonate of the above formula with a hydantoin of the last formula above where R1 is replaced by an atom of an alkali metal, and R2 is an organic group or H, (c) by reaction of 2 moles of a metal alkyl carbonate of the above formula with hydantoin. In (a), (b) and (c) the reversable reaction is promoted by distilling off the alcohol, R3OH, formula. Amino acids and/or their acid addition salts are prepared from the above novel chelates via 5-substituted hydantoins by either substituting the chelate in the 5, or simultaneously in the 3 and 5, positions of the hydantoin ...

STABILIZATION OF 13-14-DIHYDRO-15-KETOPROSTAGLANDINS

HYDANTOIN DERIVATIVES

BINUCLEAR N-HETEROCYCLIC COMPOUNDS AND PROCESSES FOR THEIR MANUFACTURE

... 1332750 Heterocyclic alcohols CIBAGEIGY AG 19 April 1971 [5 March 1970 26 Oct 1970 21 Jan 1971] 55633/72 Divided out of 1332749 Addition to 1289772 Heading C2C Novel heterocyclic alcohols having the general formula wherein Y 1 and Y 2 each represent a hydrogen atom or a methyl group and Y 3 and Y 4 each represent a methyl or ethyl group, such that the sum of the carbon atoms in the two radicals Y 1 and Y 3 , or Y 2 and Y 4 , is 2; or Y 1 and Y 3 , or Y 2 and Y 4 together form a tri- or tetramethylene radical; Z 1 and Z 2 each represent a nitrogen-free, divalent radical which completes a five- or sixmembered, substituted or unsubstituted heterocyclic ring; A is a divalent aliphatic, cycloaliphatic, or araliphatic radical and m and n each has a value of from 0 to 30 such that m + n is at least 1, are prepared by reacting a compound of the formula with either (i) a butene oxide, (ii) 1,2-cyclopentene oxide; or (iii) 1,2-cyclohexene oxide, in one or more stages optionally in the presence of ...

Improvements in the manufacture of amino-acids

... 2 - Alkyl - 2 - amino - 3 - (3,4, - dihydroxyphenyl) propionic acids are prepared by condensing a 3,4-dialkoxybenzaldehyde with a C2- 5-nitroalkene (basic catalyst/alcohol), reducing the nitroalkene so formed to a 3,4-dialkoxybenzyl alkyl ketone, reacting the latter with alkali metal cyanide/ammonium carbonate to give a 5-alkyl-5-(3,4-dialkoxybenzyl) hydantoin, refluxing the hydantoin with hydrogen halide to give the corresponding salt of the desired amino-acid and finally treating the latter with ammonia or amine and adjusting the pH of the solution to precipitate free aminoacid. All alkyl groups in the intermediates and final product contain up to 4 carbon atoms.

A process for the production of 5-arylidene hydantoins

... 5-Arylidene hydantoins are obtained by condensing from 10 to 100 mole percent of an arylidene imine and from 90 to 0 mole percent of the aromatic aldehyde on which the arylidene imine is based with unsubstituted hydantoin or with hydantoin substituted in the 1-, 3-position or in the 1- and 3-positions. The arylidene imine may either be used in pure form or may be produced in situ from the aromatic aldehyde and 0.1 to 1.0 times the molar quantity of ammonia or of a primary amine.

PROCESS FOR THE PREPARATION OF (THIO) HYDANTOINS MODIFIED WITH AMIDE GROUPS

CARBOXYALKY AND CARBOXYALKOXY DIPHENYLHYDANTOIN DERIVATIVES AND THEIR PREPARATION

HINDERED HYDROXYPHENYLALKANOATES OF SUBSTITUTED ISOPROPANOLS AND STABILIZED COMPOSITIONS

... 1491825 Hydroxyphenyl alkanoates CIBAGEIGY AG 11 Dec1975 [12 Dec 1974] 50784/75 Heading C2C [Also in Divisions C3 and C5] The invention comprises compounds of the formula where R 1 is C 1 -C 30 alkyl, C 5 -C 12 cycloalkyl alkylthioethyl of 4-27 atoms in the chain or alkylpolyoxyalkylene of 4-27 atoms in the chain, having the general structure R0(OC n H 2n ) h or R0(OCH 2 CHR1) h where R‹ is C 1 -C 18 alkyl, n is 2-4, R1 is H, methyl or ethyl and h is 1-3, R 2 is a group of the formula where R 3 is H, C 1 -C 8 alkyl, C 5 -C 6 cycloalkyl or -methylbenzyl, R 4 is C 1 -C 8 alkyl or C 5 -C 6 cycloalkyl, R 5 is H or C 1 -C 4 alkyl or R 3 and R 5 together are a butylene chain, provided when R 3 is H, R 5 is alkyl and R 4 is located on the carbon atom ortho to the hydroxyl group, A is a covalent bond or C 1 -C 8 alkylene or alkylidene, Q is a group of the formula R 6 is H or C 1 -C 4 alkyl, R 7 is H or C 1 -C 8 alkyl, R 8 is H, C 1 -C 8 alkyl or C 6 -C 10 aryl ...

PROCESS FOR THE PRODUCTION OF HYDANTOINS AND POLYHYDANTOINS AND COMPOUNDS PRODUCED THEREBY

PROCESS FOR THE PREPARATION OF HYDANTOINS

Hydantoin derivatives

The invention comprises 5-(8-halo-butylidene)-hydantoins, other than the fluorine compound, which are prepared by treating 5-(tetrahydro-2-furyl)-hydantoin with a hydrohalic acid at a temperature above 50 DEG C., preferably at 50-150 DEG C. Thus the tetrahydrofuryl compound may be dissolved in concentrated hydrobromic acid and gaseous hydrogen bromide passed in at 100 DEG C., or hydrogen chloride gas can be passed into the molten material at 110 DEG C. A basic compound such as pyridine may serve as solvent and catalyst. Examples are given of these methods. The product is useful for the synthesis of lysine as in Specification 791,328. 5 - (Tetrahydro - 2 - furyl) - hydantoin is made by catalytic hydrogenation of 5-(2-furyl)-hydantoin in a neutral or acidic medium, preferably in water or a lower aliphatic alcohol or mixtures of these. Preferred conditions are 50-100 DEG C. and 10-50 p.s.i.g. using palladium on charcoal. The product exists in stereoisomeric forms, but separation of these is ...

Fungicidal optically active 2-imidazolin-5-one and 2-imidazole-5-thione

Derivative of 2,2-dimethyl 3-(2-fluoro vinyl) cyclopropane carboxylix acid their preparation process and their use as pesticides

Fungicidal 2-imidazolin-5-one derivatives

Synthetic excitatory amino acids

Synthetic excitatory amino acids.

The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.

Fungicidal 2-imidazolein-5-one derivatives.

The invention relates ...

"Fungicidal optically active 2-imidazolin-5-one and 2-imidazoline-5-thione derivatives".

An optically active ...

Aralkyl and aralkylidene heterecyclic lactams and imides.

The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Derivatives of 2,2-dimethyl 3- (2-fluoro vinyl) cyclopropane carboxylic acid, their praparation process and their use as pesticides.

Compounds of formula (i)in which r represents the remainder of an alcohol used in the pyrethroid series, in all their possible stereoisomer forms as well as their mixtures, and compositions comprising them. The compounds of formula (i)are useful as pesticides.

Aralkyl and aralklidene heterocyclic lactams and imides

Fungicidal 2-imidazolin-5-one derivatives

Synthetic excitatory amino acids

Fungicidal optically active 2-imidazolin-5-one and 2-imidazole-5-thione

Method of preparation of esters of derived from alpha-alkyl-thyronine.

Esters of acids cyclopropane, carboxylic related with the acid pyrethric, their method of preparation and their application to the fight against the parasites.

New derivatives of the carboxylic acid cyclopropane their preparation, their application to the fight against the parasites of the plants, of the animals and the buildings, the compositions containing them and new intermediaries obtained.

"Stabilization of 13,14-dihydro-15-ketoprostaglandins".

New derivatives of the acid cyclopropane carbocylic subbtitué into 3 by a substituted vinyl chain itself, their application like pesticide and compositions containing them.

Aralkyl and aralkylidene heterocyclic lactams and imides

Derivatives of 2,2-dimethyl 3-(2-fluoro vinyl) cyclopropane carboxylic acid, their preparation process and their use as pesticides.

Obtaining amino acids of the type L-alpha-alkyl-beta (3,4-dihydroxyphényl) alanine.

Aralkyl and aralklidene heterocyclic lactams and imides

Derivative of 2,2-dimethyl 3-(2-fluoro vinyl) cyclopropane carboxylix acid their preparation process and their use as pesticides

VERFAHREN ZUR HERSTELLUNG VON ARYLHYDANTOINEN

VERFAHREN ZUR HERSTELLUNG DES 5-(4-HYDROXYPHENYL)-HYDANTOINS

TO (TRIFLUOROMETHYL) HYDANTOINE AS INTERMEDIATE PHARMACEUTICAL OF ACTIVE COMPONENTS

VERFAHREN ZUR HERSTELLUNG VON ARYLHYDANTOINEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN 5-SUBSTITUIER-TEN HYDANTOINEN

VERFAHREN ZUR HERSTELLUNG EINES GEMISCHES VON AMIDEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN 1,5-DISUBSTITUIERTER HYDANTOINEN

CARBOXAMID SPIROHYDANTOIN CGRp REZEPTORANTAGONISTEN

HYDANTOIN DERIVATIVES AS ANTIBACTERIAL ACTIVE SUBSTANCES

NEW 5-SUBSTITUIERTE HYDANTOINE

PROCEDURE FOR THE PRODUCTION OF ALLANTOIN

PROCEDURE FOR THE PRODUCTION OF ARYLHYDANTOINEN

PROCEDURE FOR THE PRODUCTION OF NEW CONNECTIONS AND OF THEIR SALTS

PROCEDURE FOR the PRODUCTION of NEW 4 ((3,4-DIALKOXYPHENYL) - ALKYL) - 2-IMIDAZOL IDINON DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF A MIXTURE OF AMIDES

PROCEDURE FOR THE PRODUCTION OF ALLANTOIN.

PRODUCTION OF HYDROXYAROMATI KETOACETALE OUT HYDROXYAROMATI METHYLKETONE AND PROCEDURES FOR THE PRODUCTION OF 5 (4 ' - HYDROXYPHENYL) - HYDANTOIN AND D-P-HYDROXYPHENYLGLYCIN FROM 4 - HYDROXYACETOPHENON

1,3-DIHYDRO-2H-IMIDANO 4,5-B-QUINOLIN-2-EIN of DERIVATIVES AS PHOSPHODIESTENASE HEMMER

PROCEDURE FOR THE PRODUCTION OF HYDANTOINEN AND THEIR USE IN TEMPERATURE-STEADY LACQUERS, FOILS, ADHESIVES, FOAM MATERIALS OR MOLDED ARTICLES.

NEW HYDANTOINE, YOUR PRODUCTION AND USE.

PROCEDURE FOR THE PRODUCTION OF HYDANTOINESTERN.

PROCEDURE FOR THE PRODUCTION OF HYDANTOINEN.

SYNTHETIC SUGGEST-CASH AMINO ACIDS

CYCLI FUNGICIDES OF AMIDES

1 (ARYLALKYL AMINOALKYL) IMIDAZOLDERIVATE, MANUFACTURE PROCEDURE AND USE AS THERAPEUTIC MEANS

IMIDAZOLIDIN DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF NPHOSPHONOMETHYGLYZIN.

PROSTAGLANDINDERIVATE, PROCEDURE FOR YOUR PRODUCTION AND THEIR PHARMACEUTICAL COMPOSITIONS.

CYCLOPROPAN CARBOXYLSAEURE DERIVATIVES, YOUR PRODUCTION AND APPLICATION WITH THE FIGHT AGAINST PARASITS AGAINST PLANTS, ANIMALS AND RESTAURANTS, YOUR COMPOSITIONS AND INTERMEDIATE PRODUCTS.

PHENYLIMIDAZOLIDIN DERIVATIVES, YOUR PRODUCTION AND YOUR USE

SELECTIVE NEUROKININ ANTAGONISTS

DYNAMIC SEPARATION FROM ISOMERS AND SEPARATE ISOMERS

CYCLOPROPYL DERIVATIVES WITH PHARMACEUTICAL CHARACTERISTICS

Procedure for the production of optically active Hydantoinderivaten

PROCEDURE FOR THE PRODUCTION OF LIPOSOMEN ABSTENTION COSMETIC OR PHARMACEUTICAL COMPOSITIONS

PHENYLIMIDAZOLIDINE AND THEIR USE AS ANTI-ANDROGENS MEANS

SUBSTITUERTE PHENYLIMIDAZOLIDINE WITH ANTIANDROGENER ACTIVITY

PROCEDURE FOR THE CHEMICAL ONE RACEMISIERUNG OF 5 - MONOSUBSTITUTED HYDANTOINEN

IMIDAZOLIN DERIVATIVES, YOUR PRODUCTION AND YOUR USE AS RESOLVENTS

Procedures for the production of new α-alkyl-thyroninen

CIS-ALKOXY-SUBSTITUTED SPIROCYCLIC 1-H-PYRROLIDINE-2,4-DIONE DERIVATIVES

Process for preparing cis-alkoxy-substituted spirocyclic 1-H-pyrrolidine-2,4-dione derivatives and alkali metal salts and alkaline earth metal salts thereof. 2. The process according to claim 1 , where A represents C-C-alkyl.3. The process according to claim 1 , where A represents methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl or isobutyl.4. The process according to claim 1 , where A represents methyl.5. The process according to claim 1 , wherein lithium hydroxide claim 1 , sodium hydroxide claim 1 , potassium hydroxide claim 1 , cesium hydroxide claim 1 , magnesium hydroxide claim 1 , rubidium hydroxide claim 1 , calcium hydroxide or barium hydroxide is used.9. A hydrate of a compound of formula (cis-IV) according to . The present invention relates to processes for preparing cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives and alkali metal salts and alkaline earth metal salts thereof.Alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives of the general formula (I) having acaricidal, insecticidal and herbicidal action are known: EP-A 596 298, WO95/20572, WO 95/26954, WO 95/20572, EP-A 668 267, WO 96/25395, WO 96/35664, WO 97/01535, WO 97/02243, WO 97/36868, WO 98/05638, WO 99/43649, WO 99/48869, WO 99/55673, WO 01/74770, WO 01/96333, WO 03/035643, WO 04/007448, WO 04/065366, WO 04/111042, WO 05/066125, WO 05/049569, WO 05/044796, WO 05/092897, WO 06/056282, WO 06/056281, WO 06/029799, WO 07/096058, WO 08/067910, WO 08/138551, WO 10/102758.Such compounds are usually prepared starting with the corresponding cis-substituted hydantoins of the formula (cis-II).In the formulae (I), (II) and (cis-II),It is already known that in particular the cis-substituted compounds of the formula (I) have biologically advantageous properties (activity, toxicological profile) (WO2004/007448). Accordingly, there is an increased demand for cis-substituted hydantoins of the formula (cis-II) as starting materials.However, owing ...

METHOD FOR PRODUCING METHIONINE

The present invention pertains to a method for producing methionine or salts or derivatives thereof from hydrogen cyanide (HCN), the method comprising a step of producing 2-hydroxy-4-(methylthio)butyronitrile (MMP-CN), or a crude product mixture comprising MMP-CN, by contacting a hydrogen cyanide (HCN) process gas mixture prepared according to the Andrussow process from methane, ammonia and oxygen, with 3-methylmercaptopropionaldehyde (MMP), wherein the HCN process gas mixture is obtained from the crude HCN process gas mixture by adjusting the amount of ammonia to between 20% (v/v) and 60% (v/v) of the amount of the ammonia in the crude HCN process gas mixture. 17-. (canceled)8. A method for producing 2-hydroxy-4-(methylthio)butyronitrile (MMP-CN) , comprising: contacting a hydrogen cyanide (HCN) process gas mixture prepared according to the Andrussow process from methane , ammonia and oxygen , with 3-methylmercaptopropionaldehyde (MMP) , wherein the HCN process gas mixture is obtained from a crude HCN process gas mixture by adjusting the amount of ammonia to between 20% (v/v) and 60% (v/v) of the amount of the ammonia in the crude HCN process gas mixture.9. The method of claim 8 , wherein the ammonia adjustment is performed using an ammonia scrubber equipped with a bypass stream.10. The method of claim 8 , wherein the ammonia adjustment is performed using an ammonia scrubber enabling a partial ammonia breakthrough.11. The method of claim 8 , wherein the amount of ammonia in the HCN process gas mixture is adjusted to a maximum of 40% (v/v) of the ammonia in the crude HCN process gas mixture by passing a maximum of 40% (v/v) of the crude HCN gas mixture from the ammonia scrubber.12. A method for producing methionine or salts or derivatives thereof from HCN claim 8 , the method comprising: producing 2-hydroxy-4-(methylthio)butyronitrile (MMP-CN) claim 8 , or a crude product mixture comprising MMP-CN claim 8 , by contacting a hydrogen cyanide (HCN) process gas mixture ...

OLIGOMER AND LITHIUM BATTERY

A oligomer and a lithium battery are provided. The oligomer is obtained by a polymerization reaction of a compound containing at least one ethylenically unsaturated group and a nucleophile compound. The compound containing at least one ethylenically unsaturated group is selected from a group consisting of a maleimide-based compound, an acrylate ester-based compound, a methacrylate ester-based compound, an acrylamide-based compound, a vinylamide-based compound and a combination thereof. The nucleophile compound is selected from a group consisting of monomaleimide, trithiocyanuric acid, hydantoin, hydantoin derivative, thiohydantoin, thiohydantoin derivative and a combination thereof. 1. An oligomer obtained by a polymerization reaction of a compound containing at least one ethylenically unsaturated group and a nucleophile compound , wherein the compound containing at least one ethylenically unsaturated group is selected from a group consisting of a maleimide-based compound , an acrylate ester-based compound , a methacrylate ester-based compound , an acrylamide-based compound , a vinylamide-based compound and a combination thereof , and the nucleophile compound is selected from a group consisting of monomaleimide , trithiocyanuric acid , hydantoin , hydantoin derivative , thiohydantoin , thiohydantoin derivative and a combination thereof.2. The oligomer of claim 1 , wherein a mole ratio of the compound containing at least one ethylenically unsaturated group and the nucleophile compound is between 1:5 and 5:1.3. The oligomer of claim 1 , wherein the maleimide-based compound comprises monomaleimide or bismaleimide.4. The oligomer of claim 1 , wherein the acrylate ester-based compound comprises bisphenol A diacrylate or bisphenol A ethoxylate diacrylate.5. The oligomer of claim 1 , wherein the methacrylate ester-based compound comprises bisphenol A dimethacrylate.6. The oligomer of claim 1 , wherein the acrylamide-based compound comprises bisacrylamide.7. The oligomer of ...

HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING

In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition. 2. The compound of claim 1 , wherein Ris C═NH claim 1 , or C═O.3. (canceled)5. (canceled)810-. (canceled)1213-. (canceled)1517-. (canceled)1920-. (canceled)21. The compound of claim 1 , wherein said compound binds to APP and/or to the enzyme BACE and/or to an APP/BACE complex.22. The compound of claim 1 , wherein said compound binds to APP and inhibits the enzyme BACE.23. A pharmaceutical formulation comprising a pharmaceutically acceptable carrier and a compound of .2427-. (canceled)28. A method of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction claim 1 , and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction claim 1 , or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease claim 1 , said method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, "administering to a subject in need thereof a compound of in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease."}29. The method of claim 28 , wherein said method is a method of: ...

INHIBITORS OF CELLULAR NECROSIS AND RELATED METHODS

A compound having the following structure (I): 5. The compound of claim 4 , wherein Ris H.6. The compound of claim 4 , wherein Ris F.7. The compound of claim 4 , wherein Ris F.8. The compound of claim 4 , wherein Ris F.9. The compound of claim 4 , wherein Ris F.10. The compound of claim 4 , wherein Rand Rare F.11. The compound of claim 4 , wherein Rand Rare F.13. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , prodrug or tautomer thereof claim 1 , and a pharmaceutically acceptable carrier claim 1 , diluent or excipient.14. A method for treating a necrotic cell disease claim 13 , the method comprising administering an effective amount of the composition of to a subject in need thereof.15. The method of claim 14 , wherein the necrotic cell disease is trauma claim 14 , ischemia claim 14 , stroke claim 14 , cardiac infarction claim 14 , infection claim 14 , Gaucher's disease claim 14 , Krabbe disease claim 14 , sepsis claim 14 , Parkinson's disease claim 14 , Alzheimer's disease claim 14 , amyotrophic lateral sclerosis claim 14 , Huntington's disease claim 14 , HIV-associated dementia claim 14 , retinal degenerative disease claim 14 , glaucoma claim 14 , age-related macular degeneration claim 14 , rheumatoid arthritis claim 14 , psoriasis claim 14 , psoriatic arthritis or inflammatory bowel disease.16. A method for treating an inflammatory disorder claim 13 , the method comprising administering an effective amount of the composition of to a subject in need thereof.17. The method of claim 16 , wherein the inflammatory disorder is inflammatory bowel disease.18. The method of claim 16 , wherein the inflammatory disorder is Crohn's disease or ulcerative colitis.24. The method of claim 22 , wherein the leaving group is halogen.25. The method of claim 24 , wherein halogen is bromine or iodine.26. The method of claim 22 , wherein Ris C-Calkyl.27. The method of claim 26 , wherein Ris methyl.28. The method of ...

METHOD OF PRODUCTION OF A METHIONINE SALT

A method for production of a methionine salt in a reactive rectification column containing a weir having a height of 100 mm or more is provided. 1. A method for continuous production of a methionine salt , comprising:reacting 3-methylmercaptopropionaldehyde and hydrogen cyanide or a component that can be produced therefrom, thereby obtaining a solution containing 5-(2-methylmercaptoethyl)-hydantoin;alkaline hydrolysing the 5-(2-methylmercaptoethyl)-hydantoin to a methionine salt in a reactive rectification column, wherein only the solution containing 5-(2-methylmercaptoethyl)-hydantoin is fed on a topmost plate of the reactive rectification column and an alkaline circulating solution is fed on a plate located under the topmost plate.2. The method according to claim 1 , wherein the alkaline circulating solution contains an alkali metal carbonate.3. The method according to claim 1 , wherein water claim 1 , ammonia and COare removed from the top of the reactive rectification column and the NHremoved is condensed completely or partially and used in the synthesis of 5-(2-methylmercaptoethyl)-hydantoin.4. The method according to claim 1 , wherein a concentration of ammonia at the bottom of the rectification column is less than 120 ppm.5. The method according to claim 1 , wherein the reaction to 5-(2-methylmercaptoethyl)-hydantoin is carried out in a reactive absorber and then in a second reactor.6. The method according to claim 1 , wherein the reaction to 5-(2-methylmercaptoethyl)-hydantoin is carried out in a reactive absorber and then in a second reactor designed as a flow tube.7. The method according to claim 1 , wherein the temperature of the reaction mixture at the outlet of the reactive-rectification column is in the range from 180° C. to 190° C.8. The method according to claim 1 , wherein the temperature of the gas phase at the top of the reactive-rectification column is in the range from 160° C. to 170° C.9. The method according to claim 1 , wherein alkaline ...

AGGRECANASE INHIBITORS

The present invention provides compounds having the formula: wherein Ris selected from methyl, ethyl, propyl, cyclopropyl, and dimethyl, or a pharmaceutically acceptable salt thereof, along with methods and intermediates for their preparation, and uses thereof. 110-. (canceled)16. A pharmaceutical composition comprising a compound according to claim 11 , or a pharmaceutically acceptable salt thereof claim 11 , and at least one of a pharmaceutically acceptable carrier claim 11 , excipient claim 11 , or diluent.17. The pharmaceutical composition of claim 16 , wherein said pharmaceutical composition is adapted for oral administration.18. A method of treating arthritis in a patient in need thereof claim 11 , said method comprising administering an effective amount of a compound according to claim 11 , or a pharmaceutically acceptable salt thereof claim 11 , to said patient.19. The method of claim 18 , wherein said patient is administered at least one additional active agent.20. The method of claim 18 , wherein said patient is a human.21. The method of claim 18 , wherein said patient is a dog.22. The method of claim 18 , wherein said administration is oral administration.23. A method of inhibiting cartilage erosion in a patient in need thereof claim 11 , said method comprising administering an effective amount of a compound according to claim 11 , or a pharmaceutically acceptable salt thereof claim 11 , to said patient.24. The method of claim 23 , wherein said patient is administered at least one additional active agent.25. The method of claim 23 , wherein said patient is a human.26. The method of claim 23 , wherein said patient is a dog.27. The method of claim 23 , wherein said administration is oral administration. Connective tissue is a required component of all mammals. It provides rigidity, differentiation, attachments, and, in some cases, elasticity. Connective tissue components include, for example, collagen, elastin, proteoglycans, fibronectin, and laminin. These ...

FUMARATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE

Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. 2. The compound according to claim 1 , wherein Ris chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , tert-butyl claim 1 , phenyl claim 1 , benzyl claim 1 , (1 claim 1 ,3-dioxoisoindolin-2-yl) claim 1 , (2 claim 1 ,5-dioxopyrrolidin-1-yl) claim 1 , (2 claim 1 ,5-dioxopyrrol-1-yl) claim 1 , indol-1-yl claim 1 , morpholin-4-yl claim 1 , 1 claim 1 ,3-oxazinan-3-yl claim 1 , oxazolidin-3-yl claim 1 , (1-oxoisoindolin-2-yl) claim 1 , (2-oxomorpholin-4-yl) claim 1 , (4-oxo-1-piperidyl) claim 1 , (2-oxopyrrolidin-1-yl) claim 1 , (3-oxopyrrolidin-1-yl) claim 1 , 1-piperidyl claim 1 , tetrazol-1-yl claim 1 , triazol-1-yl claim 1 , 1 claim 1 ,2 claim 1 ,4-triazol-4-yl claim 1 , 1-benzoyloxyethyl claim 1 , benzoyloxymethyl claim 1 , (1 claim 1 ,3-dimethyl-2 claim 1 ,5-dioxo-imidazolidin-4-yl) claim 1 , (1 claim 1 ,3-dimethyl-2-oxo-imidazolidin-4-yl) claim 1 , (2 claim 1 ,5-dioxoimidazolidin-4-yl) claim 1 , (2 claim 1 ,5-dioxopyrrolidin-3-yl) claim 1 , (1-methyl-2 claim 1 ,5-dioxo-imidazolidin-4-yl) claim 1 , (3-methyl-2 claim 1 ,5-dioxo-imidazolidin-4-yl) claim 1 , (1-methyl-2 claim 1 ,5-dioxo-pyrrolidin-3-yl) claim 1 , (5-methyl-2-oxo-1 claim 1 ,3-dioxol-4-yl)methyl claim 1 , (3-methyl-2-oxo-oxazolidin-4-yl) claim 1 , (3-methyl-2-oxo-oxazolidin-5-yl) claim 1 , (1-methyl-2-oxo-pyrrolidin-3-yl) claim 1 , (1-methyl-5-oxo-pyrrolidin-2-yl) claim 1 , (1-methyl-5-oxo-pyrrolidin-3-yl) claim 1 , 1-(2-methylpropanoyloxy)ethyl claim 1 , 2-methylpropanoyloxymethyl ...

INHIBITORS OF PEPTIDYL ARGININE DEIMINASE (PAD) ENZYMES AND USES THEREOF

The present application relates to imidazolidinecliones, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions characterized by or associated with the hypercitrullination of proteins by peptidyl arginine deiminase (PAD) enzymes. In particular, the present application includes compounds of Formula I, and compositions and uses thereof: (I). 2. The compound of claim 1 , wherein Rand Rare independently Calkyl.3. (canceled)4. The compound of claim 1 , wherein Rand Rare independently CalkyleneR; wherein Ris selected from COOR claim 1 , Ph claim 1 , Ccycloalkyl and NHR; wherein Ris selected from H and Calkyl claim 1 , and Ris selected from H claim 1 , Ac and Bz.5. The compound of claim 4 , wherein Rand Rare independently selected from CHCOOCH claim 4 , CHCOOtBu claim 4 , CHCHCOOH claim 4 , CHCHCHCOOH claim 4 , CHPh claim 4 , CHCHPh claim 4 , CH-cyclohexyl claim 4 , CHCHNH claim 4 , CHCHCHNH claim 4 , CHCHNHAc claim 4 , CHCHNHBz claim 4 , CHCHCHNHAc and CHCHCHNHBz.9. (canceled)10. (canceled)11. (canceled)13. The compound of claim 1 , in the form of a pharmaceutically acceptable salt.14. (canceled)15. A pharmaceutical composition comprising one or more compounds of and a pharmaceutically acceptable carrier.17. The method of claim 16 , wherein Rand Rare independently Calkyl.18. (canceled)19. The method of claim 16 , wherein Rand Rare independently CalkyleneR; wherein Ris selected from COOR claim 16 , Ph claim 16 , Ccycloalkyl and NHR; wherein Ris selected from H and Calkyl claim 16 , and Ris selected from H claim 16 , Ac and Bz.20. The method of claim 19 , wherein Rand Rare independently selected from CHCOOCH claim 19 , CHCOOtBu claim 19 , CHCHCOOH claim 19 , CHCHCHCOOH claim 19 , CHPh claim 19 , CHCHPh claim 19 , CH-cyclohexyl claim 19 , CHCHNH claim 19 , CHCHCHNH claim 19 , CHCHNHAc claim 19 , CHCHNHBz claim 19 , CHCHCHNHAc and CHCHCHNHBz.24. (canceled)25. (canceled)26. (canceled)28. The method of claim ...

HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING

In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition. 2. The compound of claim 1 , wherein Ris C═NH or C═O.3. (canceled)5. (canceled)810-. (canceled)1213-. (canceled)1517-. (canceled)1920-. (canceled)21. The compound of claim 1 , wherein said compound binds to APP and/or to the enzyme BACE and/or to an APP/BACE complex.22. The compound of claim 1 , wherein said compound binds to APP and inhibits the enzyme BACE.23. A pharmaceutical formulation comprising a pharmaceutically acceptable carrier and a compound of .2427-. (canceled)28. A method of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction claim 1 , and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction claim 1 , or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease claim 1 , said method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, "administering to a subject in need thereof a compound of in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease."}29. The method of claim 28 , wherein said method is a method of:preventing ...

COMPOUNDS, POLYMERS AND COATING FORMULATIONS THAT COMPRISE AT LEAST ONE N-HALAMINE PRECURSOR, A CATIONIC CENTER AND A COATING INCORPORATION GROUP

The present disclosure relates to a compound that has biocidal activity or is a precursor of a compound with biocidal activity. The compound comprises an N-halamine precursor, at least one quaternary ammonium and at least one coating-incorporation group (CIG). In some embodiments of the present disclosure, the compound may be incorporated into a coating formulation. The coating formulation comprises the compound and at least one further component. In some embodiments of the present disclosure, the CIG reacts with the further component of the coating formulation to incorporate the compound into the coating formulation. In some embodiments, the coating formulation comprises a polymer. In some embodiments, the CIG of the compound reacts with the further component to incorporate the compound into the polymer of the coating formulation. The coating formulation may be used to coat a substrate. The coated substrate may demonstrate biocidal activity or the potential for increased biocidal activity. 3. The compound of or , wherein the N-halamine precursor group is selected from a group consisting of: an imidazolidine-2 ,4-dione; a hydantoin; a 5 ,5-dimethylhydantoin; a 4 ,4-dimethyl-2-oxazalidione; a tetramethyl-2-imidazolidione; a 2 ,2 ,5 ,5-tetramethylimidazo-lidin-4-one; a uracil; a substituted uracil; a piperidine and combinations thereof.4. The compound of any one of , or , wherein the N-halamine precursor group is converted into an N-halamine by a halogenation reaction.5. Use of the compound of any one of , , or in a thermoplastic polymer system.7. The coating formulation of claim 6 , wherein the at least one further component is selected from a group consisting of: an acetate polymer; a vinyl ester polymer; a vinyl acetate polymer; a vinyl acetate homopolymer; an acrylate polymer; a methacrylate polymer; a melamine polymer; a modified melamine polymer; a urethane polymer; a polyurethane polymer; an aliphatic urethane polymer; a polyester; a self-crosslinking polyester ...

Hydantoin derivative compounds, methods of use and methods of treatment

The present disclosure provides compositions including a hydantoin derivative compound, pharmaceutical compositions including a hydantoin derivative compound, methods of treatment of a condition (e.g., bacterial infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

Method for producing solid anhydrous methylol hydantoin

고체 무수 메틸올히단토인을 생성하기 위한 방법이 제공된다. 초기에, 교반할 수 있는 수성 배지를 탈수하고 가열시켜 교반할 수 있는 실질적인 무수 용융액을 생성한다. 교반할 수 있는 수성 배지는 (A)(i) 디메틸올디메틸히단토인, (ⅱ) 히단토인 반응물, (ⅲ) 포름알데히드원 반응물, 또는 (ⅳ) 상기의 임의 조합물로 구성된 군으로부터 선택되는 용질; 및 (B) 임의로 촉매를 포함한다. 그다음 교반할 수 있는 용융액에, (A)(ⅰ) 동일하거나 상이한 히단토인 반응물, (ⅱ) 포름알데히드원 반응물과 동일하거나 상이할 수 있는 실질적인 무수 포름알데히드원 반응물, 또는 (ⅲ) 그의 조합물 ; 및 (B) 임의로, 동일하거나 상이한 촉매를 포함하는 반응물 혼합물을 첨가하여 용융 시스템을 제공하며; 이때 용융 시스템은 (ⅰ) 적어도 하나의 히단토인 반응물 및 (ⅱ) 적어도 하나의 탈수 포름알데히드원 반응물 또는 실질적인 무수 포름알데히드원 반응물을 포함한다. 반응수를 제거시키면서, 용융 시스템에서 적어도 하나의 히단토인 반응물 및 적어도 하나의 탈수 포름알데히드원 반응물 또는 실질적인 무수 포름알데히드원 반응물을 반응시켜 무수 용융 메틸올히단토인을 생성한다. 마지막으로, 용융 메틸올히단토인을 고체화한다. 대안적으로, 고체 수성 메틸올히단토인은, 상기와 같은 교반할 수 있는 수성 매질에서, 적어도 메틸올히단토인의 용융 온도로 가열하는 동시에 실질적으로 모든 물을 제거하면서 ; (ⅰ) 동일하거나 상이한 히단토인 반응물, (ⅱ) 포름알데히드원 반응물과 동일하거나 상이할 수 있는 실질적인 무수 포름알데히드원 반응물, 또는 (ⅲ) 그의 조합물 및 (ⅳ) 임의로, 동일하거나 상이한 촉매의 반응물 혼합물을 반응시켜 용융 메틸올히단토인을 제공하고 ; 이때 (ⅰ) 적어도 하나의 히단토인 반응물 및 (ⅱ) 적어도 하나의 포름알데히드원 반응물 또는 실질적으로 무수 포름알데히드 반응물이 존재하며 ; 이어서 용융 메틸올히단토인을 고체화하여 생성된다. 이들 방법은 뱃치 공정으로서 또는 반 - 연속 공정으로 실행할 수 있다. A method for producing solid anhydrous methylolhydantoin is provided. Initially, the agitable aqueous medium is dehydrated and heated to produce a substantial anhydrous melt that can be stirred. The agitable aqueous medium is a solute selected from the group consisting of (A) (i) dimethyloldimethylhydantoin, (ii) hydantoin reactant, (iii) formaldehyde source reactant, or (iii) any combination of the foregoing. ; And (B) optionally a catalyst. Then, in the agitable melt, (A) (iii) a same or different hydantoin reactant, (ii) a substantially anhydrous formaldehyde source reactant, which may be the same or different from the formaldehyde source reactant, or (iii) a combination thereof; And (B) optionally, adding a reactant mixture comprising the same or different catalyst to provide a melting system; The melting system then comprises (i) at least one hydantoin reactant and (ii) at least one dehydrated formaldehyde source reactant or substantially anhydrous formaldehyde ...

Process for preparing methylolate hydantoins

내용없음 No content

Process for the preparation of hydantoins

Hericidal N-phenyl or N-pyridyl-hydantoin or thio-hydantoin cpds. of formula (I) are prepd. e.g. by acid catalyzed cyclization of an N- phenyl-N-carboxymethyl-urea. In (I), Q= -CH= or -N= ; A= -CR4R5- or (II); R1-R3 are each H, C1-4 alkyl; at least one of R1R3= H; R4 and R5 are each C1-4 alkyl, C3-6 cycloalkyl, phenyl or benzyl; W= O or S; X and Y are each halogen, C1-4 alkyl, C1-4 alkoxy or trifluoromethyl.

Substituted phenylimidazolidines, methods of their synthesis (variants) and pharmaceutical composition based on thereof

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to substituted phenylimidazolidines of the formula (I) where Y is O or NH; Z 2 is CF 3 ; Z 1 is cyano- or nitro-radical; X is O or S; R 3 is H or alkyl possibly substituted with halogen atom or cyano-radical R 4 , R 5 is alkyl possibly substituted with hydroxy 1 that can be protected in all possible isomeric, racemic, enentiomeric and diasteriameric forms and acidic or basic salts that show anti-androgenic activity. EFFECT: improved method of synthesis, valuable pharmacological properties. 8 cl, 38 ex тс босс ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВИ” 2 152 934 ' (51) МПК? 13) СЛ А 61 Р 5/28 С 07 О 233/86, А 61 К 31/4166, 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 96116993/04, 04.01.1995 (24) Дата начала действия патента: 04.01.1995 (30) Приоритет: 05.01.1994 ЕК 9400042 (46) Дата публикации: 20.07.2000 (56) Ссылки: ЗИ 887568, 07.12.81. ЕР 494819 АЛ, 15.07.92. (85) Дата перевода заявки РСТ на национальную фазу: 05.08.1996 (86) Заявка РСТ: ЕК 95/00004 (04.01.1995) (87) Публикация РСТ: М/О 95/18794 (13.07.1995) (98) Адрес для переписки: 129010, Москва, ул.Большая Спасская 25, стр.3, ООО "Городисский и Партнеры", Лебедевой Н.Г. (71) Заявитель: РУССЕЛЬ ЮКЛАФ (ЕК) (72) Изобретатель: Клосснер Андре (ЕК), Губэ Франсуа (ЕК), Тетч Жан-Жорж (ЕК) (73) Патентообладатель: РУССЕЛЬ ЮКЛАФ (ЕК) (54) ЗАМЕЩЕННЫЕ ФЕНИЛИМИДАЗОЛИДИНЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ (ВАРИАНТЫ) И (57) Реферат: Ззамещенные фенилимидазолидины формулы |, где У - О или МН; #2 - СЕз; 24 - циано- или нитрорадикал; Х - О или $; Вз - Н или алкил, возможно замещенный галогеном или цианорадикалом; К4, К - алпкил, возможно замещенный гидроксилом, который может быть защищен, во всех возможных изомерных, рацемических, энантиомерных и диастереомерных формах, а также соли ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ присоединения кислот или оснований, обладают антиандрогенной активностью. 6 с. и 2 3.п. ф-Лы. та ...

Patent SU400094A3

Saparation method of the high boiling point organic compounds in ionic liquid

본 발명은 이온성 액체 내에 존재하는 고비점 유기화합물을 제거하는 이온성 액체의 정제방법에 관한 것으로, 본 발명에 따른 이온성 액체 내의 고비점 유기 화합물을 제거하는 이온성 액체의 정제방법은 종래의 일반 유기용매를 이용한 정제보다 정제효과가 상당히 우수하여, 고순도 이온성 액체의 제조가 가능할 뿐만 아니라, 정제공정이 간단하여 시간 및 경제적인 효과가 뛰어나고, 고순도의 이온성 액체를 제조하기 위하여 많은 양의 유기용매를 사용해야 했던 종래의 정제방법에 비해 적은 양의 용매를 사용함으로써 폐용매가 적게 발생되는 환경적인 효과 또한 크므로 유기합성, 전기화학 생물공학, 화학공학 및 분리 공정을 포함하는 여러 분야에서 유용하게 사용할 수 있다.

Alkali-resistant radiation curable ene-thiol compositions

The invention is directed to alkali-resistant, radiation curable compositions comprising A. a polyene And B. a polythiol of the formula ##STR1## WHERE R is an aliphatic hydrocarbon moiety containing 2-6 carbon atoms, R 2 is an alkylene group containing 2-6 carbon atoms, R 1 is hydrogen or --OH, n is 2-6, and m is 1-2. A photosensitizer is added to the composition when curing is by U. V. radiation. The cured composition is operable as an additive plating resist in the manufacture of electronic circuitry.

Method for producing 5-arylhydantoins

Process for preparing methylolhydantoins

公开了一种制备固体无水羟甲基乙内酰脲的方法，该方法包括脱水和加热一种含水可搅拌介质，得到一种基本无水的可搅拌熔体；向所述的熔体中加入一种反应混合物，得到一种熔融体系；使至少一种乙内酰脲反应物和至少一种脱水甲醛源反应物或基本无水的甲醛源反应物在所述熔融体系中反应，同时除去反应生成的水，得到无水熔融羟甲基乙内酰脲；固化所述的熔融羟甲基乙酰脲。上述方法可以间歇法或半连续法实施。

Method for preparing arylhydantoin

본 발명은 알란토인산 알킬 에스테르를 상 전이제의 존재 또는 부재하에 실온 내지 150℃의 온도에서 진한 무기산중에서 아릴 화합물과 반응시켜 5-아릴하이단토인을 제조하는 방법에 관한 것이다.

Charge control agent and toner using the same

Method of preparing 5-(4-aminobutyl) hydantoin or mixture of 5-(4-aminobutyl) hydantoin and 1-ureido-5-aminocapronamide

5-(4-Aminobutyl) hydantoin is prepared by hydrogenation of 5-(3-cyanopropyl) hydantoin in the liquid phase with a catalyst and ammonia in the presence of greater than 0.4 up to about 2.0 of a dissolved alkali hydroxide per mole of hydantoin to be hydrolyzed. Use of the stated quantity of alkali hydroxide avoids catalyst loss by dissolution yet maintains hydrogenation efficiency.

Patent JPS5018467A

Methionine Production Method

Synergetic composition and method of inhibiting growth of microorganisms

FIELD: chemistry. ^ SUBSTANCE: invention relates to control of growth of microorganisms in industrial water supply systems. In particular, the invention relates to use of a composition which contains peracetic acid, hydantoin-stabilised halide or a hydantoin-based halide to inhibit growth of microorganisms, especially inhibiting growth of microorganisms and slime deposits in pulp-and-paper mill systems, steel plant and mining industry systems. Compositions used to inhibit growth of microorganisms contain effective amounts of hydantoin or halide of hydrantoin derivatives, a source-donor of halogen and peracetic acid, its derivatives and salts. Methods in which the disclosed compositions are used exhibit synergetic effect of components of the compositions when controlling growth of bacteria, particularly when controlling slime deposition, which lowers concentration of the biocidal compositions used to obtain an efficient result. ^ EFFECT: wood mass and cellulose obtained using the method for controlling growth of microorganisms in industrial water, as well as paper mass obtained from the wood mass and/or cellulose, treated using the method for controlling growth of microorganisms, are characterised by low total bacterial counts. ^ 20 cl, 3 tbl, 3 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 414 432 (13) C2 (51) МПК C02F 1/50 (2006.01) A61L 2/16 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2008103508/05, 09.05.2006 (24) Дата начала отсчета срока действия патента: 09.05.2006 (73) Патентообладатель(и): НАЛКО КОМПАНИ (US) R U Приоритет(ы): (30) Конвенционный приоритет: 15.07.2005 US 11/183,060 (72) Автор(ы): САЙМОНЗ Берт (NL) (43) Дата публикации заявки: 20.08.2009 Бюл. № 23 2 4 1 4 4 3 2 (45) Опубликовано: 20.03.2011 Бюл. № 8 (56) Список документов, цитированных в отчете о поиске: US 6447722 B1, 10.09.2002. US 2003/0211210 A1, 13.11.2003. US 5565109 A, 15.10.1996. RU 2004102201 A ...

Method of preparing 5-(4-aminobutyl)-hydantoin or mixture of 5-(4-aminobutyl)-hydantoin with 1-ureido-5-aminocapronamide

In the prodn. of 5-(4-aminobutyl)hydantoin (I) and/or 1-ureido-5-amino-capronamide (II) by hydrogenating 5-(3-cyanopropyl) hydantoin (III) and/or 1-ureido-4-cyanovaleramide (IV) in the liq. phase in presence of NH3, a fixed bed of hydrogenation catalyst is used and the materials to be hydrogenated are supplied as liq. Pref. reaction is at 80-160 degrees C. with H2 partial pressure 50-350 atmos. Th reaction products can be hydrolysed to lysine. Losses of catalyst in the reaction stream are lower than when a suspended catalyst is used.

Blocked polyisocyanates with improved thermal stability

The present invention relates to blocked polyisocyanates containing at least one isocyanate group which is reversibly blocked with a monofunctional blocking agent for isocyanate groups and at least one isocyanate group in the form of a thermally stable hydantoin group. The present invention also relates to one-component coating compositions containing these blocked polyisocyanates and compounds containing isocyanate-reactive groups.

Method of preparing solid anhydrous methylolhydantoin

FIELD: organic syntheses. SUBSTANCE: aqueous mobile medium is first dehydrated and heated to form essentially anhydrous melt capable to be agitated. The aqueous mobile medium contains dissolved substance selected from the group including dimethyloldimethylhydantoin, hydantoin reagent, formaldehyde source, or any combination of indicated components; and optionally a catalyst. Molten system is further prepared by adding to apt-to-agitation melt a reactive mixture containing the same or another hydantoin reagent, essentially anhydrous the same or another formaldehyde source, or their combination; and optionally the same or another catalyst. Finally, molten system contains at least one hydantoin reagent and at least one dehydrated formaldehyde source or essentially anhydrous formaldehyde source. At least one hydantoin reagent in molten system is allowed to react with at least one dehydrated or essentially anhydrous formaldehyde source, which reaction is accompanied by withdrawal of water and results in formation of anhydrous molten methylolhydantoin which is further solidified. Alternative version of invention consists in preparing solid anhydrous methylolhydantoin by reaction of reaction mixture containing the same or another hydantoin reagent, essentially anhydrous the same or another formaldehyde source, or their combination optionally in presence of the same or another catalyst in the above-indicated apt-to-agitation medium containing at least one hydantoin reagent and at least one formaldehyde source or essentially anhydrous formaldehyde reagent. Reaction is carried out at heating to a temperature at least equal to melting temperature of methylolhydantoin, while removing essentially all water, to form molten methylolhydantoin. The two methods may be performed both in periodical and semicontinuous modes. EFFECT: enhanced efficiency of preparation procedure. 23 cl О9%50ЕсС ПЧ ГЭ РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ "” 2 105 760 ' 13) Сл ...

Patent FR2432510B1

4-Amino-butyl-hydantoin and 1-ureido-5-amino-caproamide prodn. - by hydrogenating cyano precursors over a fixed catalyst, useful for making lysine

In the prodn. of 5-(4-aminobutyl)hydantoin (I) and/or 1-ureido-5-amino-capronamide (II) by hydrogenating 5-(3-cyanopropyl) hydantoin (III) and/or 1-ureido-4-cyanovaleramide (IV) in the liq. phase in presence of NH3, a fixed bed of hydrogenation catalyst is used and the materials to be hydrogenated are supplied as liq. Pref. reaction is at 80-160 degrees C. with H2 partial pressure 50-350 atmos. Th reaction products can be hydrolysed to lysine. Losses of catalyst in the reaction stream are lower than when a suspended catalyst is used.

Patent FR2376851B1

TRIOLS CONTAINING HYDANTONY CYCLES AND USED IN THE PREPARATION OF SYNTHETIC RESINS

PROCESS FOR THE PREPARATION OF 5- (4-AMINOBUTYL) -HYDANTOIN AND / OR 1-UREIDO-5-AMINO-CAPRONAMIDE

Process for making an alpha-amino acid

PROCESS FOR PREPARING HYDANTOINS OR THIOHYDRANTOINS MODIFIED BY CARBOXYLIC ACID ESTERS RADICALS

Patent FR2312494B1

NOVEL IMIDAZOLIDINES SUBSTITUTED BY A RADICAL HYDROXYMETHYL AND A RADICAL PHENYL SUBSTITUTED, THEIR PREPARATION METHOD, THEIR APPLICATION AS MEDICAMENTS, THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND AN INTERMEDIATE FOR THEIR PREPARATION

New phenylimidazolines optionally substituted, their process and preparation intermediates, their use as medicaments and the pharmaceutical compositions containing them.

New substd. phenyl-imidazolidine(s) which fix to androgen receptors

Substd. phenylimidazolidines of formula (I), their enantiomers, diastereomers and acid and base addn. salts, are new. Z1, Z2 = cyano, nitro, halo, CF3, carboxy (free, esterified, salified or converted to amide); -A-B- = a gp. -C(:X)-N(R3)- (i) or -C(SR3j)=N- (ii); X = O or S; R3 = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, max. 12C (opt. substd. by one or more halo, hydroxy (opt. esterified, etherified or protected), alkoxy, hydroxyalkyl, alkenyloxy, alkynyloxy, CF3, mercapto, cyano, acyl, acyloxy, aryl, S-alkyl, S-aryl (opt. substd.) (S is opt. oxidised to sulphoxide or sulphone), carboxy (free, esterified, salified or converted to the amide), amino, mono- or di-alkylamino, 3-6 link cyclic radical (opt. contg. one or more O, S, or N) or -O-C(:O)-R7; R3j = R3 except for H; alkyl, alkenyl, alkynyl are opt. interrupted by one or more O, S (opt. oxidised to the sulphoxide or sulphone) or N (opt. oxidised); aryl and aralkyl are opt. substd. by one alkyl, alkenyl or alkynyl, alkoxy, alkenyloxy, alkynyloxy or CF3; R7 = alkyl, hydroxy, alkoxy, aryl or aryloxy; Y = O, S or NH; R4, R5 = H, 1-12C alkyl (opt. substd. by one or more halo, -O-C(=O)-R7, hydroxyl (opt. esterified, etherified or protected), phenylthio or alkylthio contg. up to 8C (opt. oxidised to sulphoxide or sulphone, and opt. substd. by one or more halo, hydroxyl (opt. esterified, etherified or protected), carboxy (opt. esterified, salified or converted to amide), amino, mono- or di-alkylamino); with the exception of prods. in which: R4, R5 = H or 1-12C alkyl (opt. substd. by halo), or R4 or R5 = methyl and the other hydroxymethyl, Y = O or NH, -A-B- = a gp. -C(:O)-NH (iii), Z1 in position 4 = nitro and Z2 in position 3 = CF3, or Z1 and Z2 = halo; or Z1 or Z2 = halo and one of R4 and R5 = alkyl substd. by -S-CH3, and R3 = H or alkyl.

PROCESS FOR THE PRODUCTION OF RACEMIC ARYL-5 HYDANTOINS AND NEW PRODUCTS RESULTING THEREFROM

L'INVENTION CONCERNE UN PROCEDE DE FABRICATION D'ARYL-5 HYDANTOINES ET LES PRODUITS NOUVEAUX EN RESULTANT. CE PROCEDE CONSISTE A FAIRE REAGIR, A CHAUD, EN MILIEU ACIDE, L'ALLANTOINE SUR UN DERIVE AROMATIQUE POSSEDANT AU MOINS UN PROTON NUCLEAIRE. APPLICATION DE CE PROCEDE A L'OBTENTION D'ARYL-5 HYDANTOINES NOUVELLES. THE INVENTION RELATES TO A PROCESS FOR MANUFACTURING ARYL-5 HYDANTOINS AND THE NEW PRODUCTS THEREFORE. THIS PROCESS CONSISTS OF REACTING, AT HOT, IN AN ACID MEDIUM, THE ALLANTOIN ON AN AROMATIC DERIVATIVE HAVING AT LEAST ONE NUCLEAR PROTON. APPLICATION OF THIS PROCESS TO OBTAINING NEW ARYL-5 HYDANTOINS.

Patent FR2228777A1

PROCESS FOR PREPARING HYDANTOINS AND THIOHYDANTOINS MODIFIED BY AMID GROUPS, PRODUCTS OBTAINED AND THEIR USE IN THE MANUFACTURE OF LACQUERS

L'invention concerne un procédé pour préparer des hydantoïnes et des thiohydantoïnes modifiées par des groupes amides. Pour préparer les composés désirés, on fait réagir des imides maléiques ou des mono-amides maléiques avec des urées ou des thio-urées. Les produits de l'invention sont particulièrement utiles dans les domaines de la protection des végétaux, de la pharmacie, des adhésifs, des laques, des films et des articles moulés. The invention relates to a process for preparing hydantoins and thiohydantoins modified with amide groups. To prepare the desired compounds, maleic imides or maleic mono-amides are reacted with ureas or thioureas. The products of the invention are particularly useful in the fields of plant protection, pharmacy, adhesives, lacquers, films and molded articles.

Improvements to the 5-beta-methylmercaptoethylhydantoin manufacturing process

NOVEL PHENYLIMIDAZOLIDINES WHICH MAY BE SUBSTITUTED, THEIR PROCESS AND PREPARATION INTERMEDIATES, THEIR APPLICATION AS MEDICAMENTS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

PROCESS FOR PREPARATION OF AMINO ACIDS CONTAINING SELENIUM

Process for preparing aldehydes

Patent FR2347353B1

New substd. phenyl-imidazolidine(s) which fix to androgen receptors

Substd. phenylimidazolidines of formula (I), their enantiomers, diastereomers and acid and base addn. salts, are new. Z1, Z2 = cyano, nitro, halo, CF3, carboxy (free, esterified, salified or converted to amide); -A-B- = a gp. -C(:X)-N(R3)- (i) or -C(SR3j)=N- (ii); X = O or S; R3 = H, alkyl, alkenyl, alkynyl, aryl or arylalkyl, max. 12C (opt. substd. by one or more halo, hydroxy (opt. esterified, etherified or protected), alkoxy, hydroxyalkyl, alkenyloxy, alkynyloxy, CF3, mercapto, cyano, acyl, acyloxy, aryl, S-alkyl, S-aryl (opt. substd.) (S is opt. oxidised to sulphoxide or sulphone), carboxy (free, esterified, salified or converted to the amide), amino, mono- or di-alkylamino, 3-6 link cyclic radical (opt. contg. one or more O, S, or N) or -O-C(:O)-R7; R3j = R3 except for H; alkyl, alkenyl, alkynyl are opt. interrupted by one or more O, S (opt. oxidised to the sulphoxide or sulphone) or N (opt. oxidised); aryl and aralkyl are opt. substd. by one alkyl, alkenyl or alkynyl, alkoxy, alkenyloxy, alkynyloxy or CF3; R7 = alkyl, hydroxy, alkoxy, aryl or aryloxy; Y = O, S or NH; R4, R5 = H, 1-12C alkyl (opt. substd. by one or more halo, -O-C(=O)-R7, hydroxyl (opt. esterified, etherified or protected), phenylthio or alkylthio contg. up to 8C (opt. oxidised to sulphoxide or sulphone, and opt. substd. by one or more halo, hydroxyl (opt. esterified, etherified or protected), carboxy (opt. esterified, salified or converted to amide), amino, mono- or di-alkylamino); with the exception of prods. in which: R4, R5 = H or 1-12C alkyl (opt. substd. by halo), or R4 or R5 = methyl and the other hydroxymethyl, Y = O or NH, -A-B- = a gp. -C(:O)-NH (iii), Z1 in position 4 = nitro and Z2 in position 3 = CF3, or Z1 and Z2 = halo; or Z1 or Z2 = halo and one of R4 and R5 = alkyl substd. by -S-CH3, and R3 = H or alkyl.

PROCESS FOR THE PREPARATION OF 5-ARYLIDENE HYDANTOINS

ON FAIT REAGIR DE 10 A 100MOLES D'UNE ARYLIDENE-IMINE ET DE 90 A 0MOLES DE L'ALDEHYDE AROMATIQUE DONT DERIVE L'ARYLIDENE AROMATIQUE DONT DERIVE L'ARYLIDENE-IMINE AVEC L'HYDANTOINE NON SUBSTITUEE OU SUBSTITUEE EN POSITIONS 1, 3 OU 1 ET 3. ON UTILISE L'ARYLIDENE-IMINE A L'ETAT PUR OU FORMEE IN SITU A PARTIR DE L'ALDEHYDE AROMATIQUE ET D'UNE QUANTITE 0,1 A 1,0MOLAIRE D'AMMONIAC OU D'UNE AMINE PRIMAIRE. LE PROCEDE SELON L'INVENTION DONNE LES PRODUITS RECHERCHES, QUI SONT DES PRODUITS INTERMEDIAIRES IMPORTANTS DE LA PREPARATION DE PHENYLALANINES, AVEC DES RENDEMENTS PRESQUE QUANTITATIFS.

Improvements to the preparation of methionine-hydantoin

Hydantoin derivatives

Substituted hydantoins with formula wherein Z is hydrogen or alkyl and Z<1> and Z<2> represent the usual prostaglandin chains, having pharmacological properties related to those of prostaglandins and are useful in medicine, for example in the treatment of thrombosis.

Hydroxyalkyl derivatives of alkylene-bis-hydantoins

New diglycidyl ethers of binuclear, five-membered or sixmembered, unsubstituted or substituted, N-heterocyclic compounds containing two NH groups in the molecule and containing added-on butene oxide, produced by reaction of binuclear, five-membered or six-membered, unsubstituted or substituted, N-heterocyclic compounds, such as bis-(hydantoin) or bis-(dihydrouracil) compounds, for example 1,1''-methylene-bis-(5,5dimethylhydantoin), 1,6-bis-(5,5-dimethylhydantoinyl-3)-hexane or Beta , Beta ''bis-(5,5-dimethylhydantoinyl-3)-diethyl ether, with butene oxide, for example 1,2-butene oxide, to give monoalcohols or dialcohols, and subsequent glydidylation of the OH groups or of the OH group and the NH group to give the corresponding glycidyl ethers.

SELENE-CONTAINING AMINO ACIDS AND PROCEDURES FOR THE PREPARATION OF THESE

Production of 5-(delta-hydroxybutyl) hydantoin

Process for the preparation of intermediates of hydantoins or cyclic anhydrides of an aminoacid

Process for the production of hydantoins

The invention relates to a process for the production of compounds containing at least one hydantoin ring by reacting a carbodiimide with derivatives of succinic acid anhydride corresponding to the following general formula: ##STR1## wherein R 4 represents a halogen atom, an alkyl-carboxy or aryl-carboxy group; or with maleic acid anhydride in the presence of aromatic OH-functional compounds at temperatures of from about 20° to about 250° C., optionally in a solvent and optionally in the presence of a catalyst, and also to the use of the polyhydantoins obtained, where they have high molecular weights, as high temperature-resistant coating compositions, films, powders, adhesives, lacquers or mouldings.

Hydantoins modified with carboxylic acid ester groups

ABSTRACT OF THE DISCLOSURE This invention relates to a process for the preparation of a compound of general formula (I) in which R represents an alkyl groups Rl and R2 represent hydrogen or an alkyl group; R3 represents hydrogens an alkyl or cycloalkyl group which is unsubstituted or substituted with halogen, hydroxyl or alkoxy; an aryl group which is unsubstituted or substituted with nitro, halogen, alkyl, alkoxy, haloalkyl or hydroxyl; an aralkyl group or a heterocyclic group derived from furan, pyridine, thiophene, imidasole, pyrimidine or piperazine, R4 represents hydrogen; an alkyl or cycloalkyl group which are unsubstituted or substituted with halogen, hydroxyl or alkoxy; an aryl group which is unsubstituted or substituted with nitro, halogen, alkyl, alkoxy, haloalkyl and/or hydroxyl; an aralkyl group or a heterocyclic group as defined above, X represents oxygen or sulphur and n represents an integer from one to 30 by reaction with a urea with a corresponding 1,2-ethylene-dicar-boxylic acid ester which is either unsubstituted or alkyl substituted in a single stage reaction.

3-(3{40 ,5{40 -dihalogenophenyl)imidazolidine-2,4-dione derivatives

3-(3',5'-Dihalogenophenyl)imidazolidine-2,4-dione derivatives, which may be substituted with alkyl or phenyl in the 1 and/or 5 positions, are new compounds, and have high microbicidal activity on various fungi and bacteria and are non-toxic to plants and mammals. Those compounds are prepared by the intramolecular cyclization of a corresponding urea derivatives. [US3668217A]

Process for the production of methionine

Process for producing derivatives of hydantoin

Hydrantoins and methods of obtaining the same

Process for preparing methylolated hydantoins

A method for making methylolated hydantoins by reacting a hydantoin, a formaldehyde such as paraformaldehyde and an alkaline catalyst at conditions of temperature and pressure sufficient to induce reaction to obtain a product in essentially 100% active form. Dry methylolated hydantoin product made by this process may be stored or shipped more economically than an aqueous solution containing a methylolated hydantoin.

Charge control agent and toner using the same

本発明は、下記一般式（１）で表されるヒダントイン誘導体の１種又は２種以上を有効成分として含有する電荷制御剤を提供する。【化１】［式中、Ｒ１及びＲ２は、相互に同一でも異なってもよく、水素原子、置換基を有していてもよい炭素原子数１〜８の直鎖状若しくは分岐状のアルキル基等を示し、Ｒ３は、水素原子等を示し、Ｒ４〜Ｒ８は、相互に同一でも異なってもよく、水素原子、塩素原子、置換基を有していてもよい炭素原子数１〜８の直鎖状若しくは分岐状のアルキル基、置換基を有していてもよい炭素原子数１〜８の直鎖状若しくは分岐状のアルキルオキシ基等を示す。Ｒ３〜Ｒ８は、互いに結合して環を形成していてもよい。Ｖ、Ｗ、Ｘ、Ｙ及びＺは炭素原子又は窒素原子を示し、Ｖ、Ｗ、Ｘ、Ｙ及びＺはそのいずれか０〜３個が窒素原子であるものとし、この場合の窒素原子はＲ４〜Ｒ８の置換基を有さないものとする。］ The present invention provides a charge control agent containing one or more hydantoin derivatives represented by the following general formula (1) as an active ingredient. [Wherein, R1 and R2 may be the same or different from each other, and may be a hydrogen atom or a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent. R3 represents a hydrogen atom or the like, R4 to R8 may be the same as or different from each other, and may be a hydrogen atom, a chlorine atom, or a straight chain having 1 to 8 carbon atoms which may have a substituent. A chain or branched alkyl group, a linear or branched alkyloxy group having 1 to 8 carbon atoms which may have a substituent, and the like are shown. R3 to R8 may be bonded to each other to form a ring. V, W, X, Y and Z represent a carbon atom or a nitrogen atom, and V, W, X, Y and Z are any one of 0 to 3 nitrogen atoms. In this case, the nitrogen atom is R4. It shall not have a substituent of ~ R8. ]

5-(4-Hydroxyphenyl) hydantoin derivatives

Compounds of the formula (I) <IMAGE> (I) wherein R1 represents a hydrogen atom or a 1-hydroxy lower alkyl radical and the like; R2 represents a 1-hydroxy lower alkyl radical; and X represents a hydrogen or chlorine atom having broad spectrum antimicrobial activity and a process for their production.

Process for preparing 5- (3, 4-dihydroxybenzyl) -5-methyl-hydantoin

Synergistic composition and method for inhibiting growth of microorganisms

The present invention provides a composition and method for inhibiting the growth of microorganisms in industrial water systems. Methods employing the composition comprising halogen-based hydantoin or hydantoin-stabilized halogen in combination with peracetic acid demonstrate synergistic control of microbial growth, particularly control of slime deposition.

Patent FR2032788A5

3-(3{40 ,5{40 -dihalogenophenyl)imidazolidine-2,4-dione derivatives

3-(3',5'-Dihalogenophenyl)imidazolidine-2,4-dione derivatives, which may be substituted with alkyl or phenyl in the 1 and/or 5 positions, are new compounds, and have high microbicidal activity on various fungi and bacteria and are non-toxic to plants and mammals. Those compounds are prepared by the intramolecular cyclization of a corresponding urea derivatives. [US3668217A]

PROCESS FOR PREPARING HYDANTOINS AND POLYHYDANTOINS THUS OBTAINED

L'invention concerne un procédé pour préparer des hydantoïnes et les polyhydantoïnes ainsi obtenues. Pour préparer des hydantoïnes on fait réagir, à une température de 0 à 450 degrés C, un isocyanate ou un isothiocyanate organique éventuellement masqué avec des diamides insaturés. L'invention s'applique en particulier, à la préparation de polyhydantoïnes utiles pour réaliser des vernis, des feuilles minces, des adhésifs ou des articles moulés résistant à la chaleur. The invention relates to a process for preparing hydantoins and the polyhydantoins thus obtained. To prepare hydantoins is reacted at a temperature of 0 to 450 degrees C, an isocyanate or an organic isothiocyanate optionally masked with unsaturated diamides. The invention applies in particular to the preparation of polyhydantoins useful for making varnishes, thin sheets, adhesives or heat-resistant molded articles.

Patent FR2161722A5

Patent FR2458546B1

Comprehensive utilization method of allantoin synthetic mother liquor

本发明涉及一种尿囊素合成母液的综合利用方法,将其作为原料与苯酚和乙醛酸反应合成药物中间体对羟基苯海因，以原料苯酚计的对羟基苯海因合成摩尔收率为67%‑70%。本发明解决了尿囊素生产过程中的环境污染的问题，节省了废液处理费用，降低了尿囊素和对羟基苯海因的生产成本。

Preparation of dl-beta-aryl-amino acids

Hydantoin derivatives, their synthesis, pharmaceutical formulations and intermediates in their preparation

Production of 5-arylhydantoin

METHOD OF MANUFACTURING HYDANTOIN

2-(6-methoxy 2- naphthyl)propionic acid - antiinflammatory analgesic,antipyretic

Discovery of novel soluble crystalline anesthetics

The invention discloses compounds derived from propofal which have greater aqueous solubility than propofal and are useful as anesthetic agents. The invention further discloses methods of preparing compounds of the invention. The invention also discloses methods of inducing anesthesia in a subject by administering compounds of the invention to the subject.

Process for the preparation of 5-(4-aminobutyl)-hydantoin

Synthesis of hydantoin containing peptide products

Process for the production of hydantoin esters

Process for the preparation of aminoalkylhydantoin and aminoalkyl-alpha-amino acids

In order to prepare aminoalkylhydantoins, the amino function must be protected before the formation of the hydantoin ring. Since the protective group is difficult to remove again, however, in particular for subsequent enzymatic reactions in which the corresponding aminoacids are liberated, a simple method of preparing aminoalkyl compounds was sought. The invention calls for an acid-labile amino-protecting group to be used in the preparation of compounds of general formula (I) or (II) in which X is alkylene and Y is hydrogen or alkyl. This protective group can even be split off during the acid-catalysed hydantoin ring closure since, during this step, no competing reactions of the freed amino function take place. The method disclosed is suitable for use in the preparation of optically opposite D- and L-forms of natural and synthetic aminoacids.

Hydantoins,their preparation and their use as herbicides

A procedure for the preparation of 2- (6-metoxy-2-nafthy) - propionic acid. (Machine-translation by Google Translate, not legally binding)

A process for the preparation of 2- (6-methoxy-2-naphthyl) -propionic acid consisting of treating a compound of the formula: **(See formula)** where X is chlorine or bromine and each of the radicals R and R1 is hydrogen or methyl, with a catalyst selected from the group consisting of palladium on carbon, platinum and platinum oxide in the presence of hydrogen or with Raney nickel in an organic solvent inert until 2- (6-methoxy-2-naphthyl) -propionic acid is formed. (Machine-translation by Google Translate, not legally binding)

Device and method for preparing 5-(2-(methylthio)ethyl)hydantoin

Patent FR2374310B1

PROCESS TO MODIFY PLANT GROWTH

Production of methionine

Heterocyclic mono- and dialcohols

Phenylalanines

The invention comprises phenylalanines of the general formula: <FORM:0945892/C2/1> and their acid addition salts, where each of R1 and R2 is a hydrogen atom or a methyl radical, R3 is a C2-5 alkyl radical and R4 is a hydrogen atom or a C1-5 alkyl radical and the preparation thereof, wherein R1 and R2 are each methyl radicals, by reacting a compound of the formula: <FORM:0945892/C2/2> with a base in aqueous medium and, when R1 and R2 are both hydrogen atoms hydrolysing the dimethyl ether with aqueous hydrobromic acid at a temperature between 90 DEG C. and reflux temperature and neutralising the resulting compound. The processes may be combined with one wherein the starting material is prepared by reacting a ketone: <FORM:0945892/C2/3> with ammonium carbonate and a water soluble cyanide salt in a aqueous medium and also a process wherein the ketone may be prepared by reacting 3-dimethoxyphenylacetonitrile with a compound R3COOR5 where R5 is a C1-5 alkyl radical and reacting the product with an acid. Pharmaceutical compositions comprise the phenylalanines of the invention together with a non-toxic pharmaceutical diluent or carrier, preferably in the form of a capsule, tablet aqueous suspension or sterile injectable solution. The compositions are useful in the treatment of hypertension.

PROCESS FOR THE PREPARATION OF 5-ARYLDENEHYDANTOINS AND PRODUCTS OBTAINED

Hydantoin derivatives as intermediates for pharmaceutical active compounds

The present invention relates to hydantoin derivatives of the formula I (see formula I) in which R, R1, R2 and R3 have the meanings indicated in claim 1 and which are intermediates for the preparation of pharmaceutical active compounds, their preparation and their use in the preparation of the active compounds.

LINEAR POLYESTERS BASED ON HETEROCYCLIC DICARBOXYLIC ACIDS

Patent CS178062B2

Process for the preparation of 5-(4-aminobutyl) hydantoin and/or 1-ureido-5-aminocapronamide

5-(4-Aminobutyl) hydantoin is prepared by hydrogenation of 5-(3-cyanopropyl) hydantoin in the liquid phase with a catalyst and ammonia in the presence of greater than 0.4 up to about 2.0 of a dissolved alkali hydroxide per mole of hydantoin to be hydrolyzed. Use of the stated quantity of alkali hydroxide avoids catalyst loss by dissolution yet maintains hydrogenation efficiency.