Способ получения антибиотика

Мета-феноксибензиловые или @ -циано-мета-феноксибензиловые сложные эфиры 2-галоидалкил (окси-,тио-,сульфинил-или сульфонил) фенилалкановых кислот,проявляющие инсектицидную,иксодицидную активность

Метафеноксибензиловые или А -циано-метафеноксибензйловые сложные эфирЫ 2-галоидалкил(окси-, тио-, сульфинил или.сульфонил )фенилалкановых кислот общей формулы RpFjJC, - СО- о- . где RjCFj X- Y и Z находятся в метанли в пара-положении по отношению к углеродному атому, к которому прияреплена группа сложного эфира алкановой кислоты; X - О, S, SO или У и Z - по отдельности И, С1, F, Вг, NO, СН шш R - И, F, С1, CHFj или R - УОШ, н-пропил, изопропил, изопропьнил или трег-бутил;, R - Н, CN илн-С СН; R4 - И, F, С1, СН юш O€fl|. их оптические изомеры прт услов1т, что У -и Z - водород, RJ -| Н нли F;.X - О или S; : В 2 -пропил или изопропил, проявляю щие инсектшшдную и иксодщидную актнв (Л ; кость. Приоритет по признакам: 01.10.76 при X-S илих О; R - Н шга F; § R - этил, пропил или изопропкл; R - Н, ; CN или CyCHf RA - Н, F, Ct, СИ- или :OCHj. 11.07.77 при , SO или X Z и Y-H, ОТ, F, Br, NOj, ND ЭО , 01, F, CHF ШШ CFjj зтип, пропид , изопропил, трег-бутил или изопропе1аш; Rg-H. CN или -CsCK; H,F,C1 ...

Способ получения замещенной бифенилмасляной кислоты или ее эфиров или солей

Способ получения 2-(фенилметил)-1-нафтола

Композиция на основе полиолефина

Способ получения замещенных бензгидролов

Способ получения д-/-/-2-амино-2/ -оксифенил/ -уксусной кислоты или ее солей

Сособ получения 3-замещенных тетрагидропиридинов или их солей, или их алканоилпроизводных,или их тиокарбамоилпроизводных

Способ получения 3-замещенных тетрагидропиридинов или их солей,или их алканоилпроизводных, или их арилтиокарбамоилпроизводных

Способ борьбы с нежелательными растениями

Изобретение относится к химическим способам борьбы с сорной и нежелательной растительностью. Сорные растения уничто-жают, обрабатывая их производным цикло- гександиона общей формулыN0.^1^л^^ Подробнее

Способ получения -анилинокарбонитрилов

Способ получения фенилацетгидроксамовых кислот

Способ получения производных амина

Способ получения производныхфЕНэТАНОлАМиНА B СВОбОдНОМ ВидЕ,B ВидЕ СОли, РАцЕМАТА или ОпТичЕСКи- АКТиВНОгО АНТипОдА

Способ получения производных бензола

Изобретение относится к кислородсодержащим соединениям, в частности к получению производных бензола ф-лы но RI CH3C- Q}-CPZ- )-C|0)-A-R2 где RI - этил или пропил; R2 - СООН или 5-тетразолил; А - Ci-Ce-алкилиден с прямой или разветвленной цепью, которые являются антагонистами лейкотриенов. Цель изобретения - разработка способа получения более активных соединений. Получение ведут из соответствующего производного бен- зола и соответствующего фенола с последующим, при необходимости, гидролизом или взаимодействием с производным азида. 1 табл.

Способ получения замещенных п-галоген-фенил-2-пирролидинонов или их цис-и транс-диастереоизомеров

Способ получения производных бензолсульфамида

Способ получения производных @ -нафтоилглицина

Способ получения производных N-фенилпиразола

Изобретение относится к гетероциклическим соединениям, в частности к получению производных N-фенилпира- зола формулы (CN)(M), при М - CRj CR4-C CR,(CF3), где R, и R хлор, R и Rj - водород; или R( - хлор, Rj.- R4-водород; или R, - R - фтор или R , R- и R - хлор, R - водород, которые проявляют гербицидную активность и могут найти применение в сельском хоз.чйстве. Цель - получение более активных веществ указанного,класса. Получение их ведут из соединения формулы , где М указано выше, или его кислотно-аддитивной соли и соединения формулы (NC)(OR5)H, где Rf - С,-С4-алкил с прямой или разветвленной цепью, в присутствии ацетата щелочного металла в среде инертного органического растворителя (ИОР) при комнатной температуре. Полученное производное фенилгидразина под- . вергают циклизации в среде ИОР при температуре от комнатной до температуры кипения реакционной смеси с - обратным холодильником. 6 табл. § W ...

Гербицидная композиция

Изобретение относится к химическим средствам борьбы с сорной и нежелательной растительностью. Изобретение позволяет поражать на 60- 100% сорные растения - росичку кровяную , амарант, горец, камьш, кури- нов просо, не затрагивая культурные растения (рис, сого, кукурузу) за счет использования гербицидной композиции , содержащей.мас.г: активное вещество общей формулы 2-С1-4-СРз-0- -NO -5-CH2C(0)R, где R - OR,,SR2 или R - CHjCHjCl, CH CHjOCH, , CH CH SCIlpb -CHi, CH,;CH-jOC(0)CH3; СН(СООСНз)СНз; CHCCOGC H OCH ; СНССООСзН-у СН ; CH(COOCHaCHj-CH)CH3, CH(COOCH,2C5 СН)СНз; , , , , СН.СООСНз, CH jCOOC Hj;, CH,COOCH CH CH.j, CH COOCH.,, ;CH/iCONHCH3; R - СЕ,, i - CHiCH CH2, H, , i - 3, H -CjEf CE CN, CE, , , CHjCH OGjHj, CI-I,jCH(OH)ClLCH3, R - H, СНз, , при условии , что если R-f - CHg, то R - . CHjO, a если R - , то R. - H или ., 5-30; поверхностно-активное вещество 10-50; растворитель 40-85. Аналогичный гербицид м мати ловый эфир 2-нитро-5-(2-хлор-4-три- фторметилфенокси)фенилуксусной кислоты ...

Способ получения N-[3-(1-морфолино)-этилиденамино-2,4,6-трийодбензоил]- @ -амино- @ -метилпропионовой кислоты

Способ получения 2-замещенных 4-амино-6,7-диметоксихинолинов или их фармацевтически приемлемых солей

Способ получения 2-заме1ценных А-амино-6,7-диметоксихинолинов общей формулы° CHjOv V VR СНзО 1SH2 .НСН,СНз 3 - - Т НСН2СНз -N-N « или Y выбран из группы COR,, где R, - С, - Cg - алкил, бензил, С - циклоалкил, тирил или R -Л) 0/ где R -группа -N() , пипе- ридино группа 6,7-диметокси-1,2,3,4- -тетрагидроизохинол-2-нл или группа . где у - Н, С,-Сзалкил , бензил, фенил или азотсодержащая ароматическая группа, а именно .чЗ N о 0 группы - с-TSIHFI Д« R - фенил, , О - алкил, Cj-C -алкенилметил, Cj-C -циклоалкилметил, бензил, группы -COORj, где Я,- -алкил, .бензил, С,-С;,-алкенилметил, см ...

Способ получения R,S-изомера производных фенэтаноламина или их солей

Способ получения гетероциклических производных циклобутиламинометана

Изобретение касается гетероциклических производных, в частности циклобутйламинометана общей формулы I Я2ЯзЯ1 СбН2- с- СН2- СН2- СН2 GH(R01S1H2 где f2-фурил , 5-метилфурил-2; тиенил; 1метилЬиррол-2-ил; 1-метилимидазол-2ил; пиридил; 4-метилтиазол-2-ил; 1метилпиразол-5-ил; 1,3-дитиан-2-ил В бензольном кольце R, .а К зависимо друг от друга Н, С1, С , (СН , ОСИ,,, SCH, и Клвместе взятые с соседними атомами углерода, с которыми они связаны, образуют второе бензольное кольцо, которое может быть незамещенным или замещенным хлором, которые, как обладающие антйдепрессантной активностью, могут-использоваться в медицине. Для выявления физиологической активности в указанном ряду соединений получены новые соединения I. Процесс ведут восстановлением соответствующей группы C(R)NY при X - углеродном атоме, где Y - литий или группа MgBr или i MgCl. Восстановление ведут с помощью СО боргидрида натрия в среде оганического растворителя, например этанола, пропан-2-ола, диэтиленгликольдиметилового эфира при температуре ...

Способ получения оптически чистых моноэфиров винной кислоты и оптически активных алканоламинов или их солей

Изобретение касается производных оксикислот, в частности моноэфи- ров винной кислоты и алканоламинов общей формулы (1)А - С (OR,) - CH,j - - NHR,, где А - 4 нитрофенШ1, 1-наф- тилок симе тил, 4-индолилоксиметнл феноксильный остаток 4-R,, 2-R -CgHj- -O-CBj-, где R - метоксиэтил, -NHK; К - алканоил С,-С, в котором алкил С,-С 7 или дикарбамоил, в котором алкил С,-Сг; R4-H, СН,-С(0)-; RZ-, водород или разветвленный С,-С -алкил; R,- остаток дизамещенной (R, R)- или ...

Способ очистки адипонитрила

Способ получения производных бутирофенонпирролидина или их солей

Способ получения 3-(4-бифенилил) -масляной кислоты или ее солей

Способ получения производных хинолина или их солей

Способ получения производных 4-фенил-2-метил-1-бутен-1-карбоновой кислоты

Инсектоакарицидное средство

Средство, регулирующее рост подсолнечника

Изобретение относится к химическим средствам, воздействующим на рост и развитие растений, и может найти применение в сельском хозяйстве. Цель изобретения - повышение эффективности. Согласно изобретению средство, эффективно воздействующее на рост и развитие подсолнечника, содержит, мас.%: активное вещество формулы C6H5C(CN)(C2H5)CONR1R2,где R1-водород R2-водород, метил, изопропил, бензил или R1и R2вместе - группа (CH2CH2)O или (CH2)6- 80, натрийолеилметилтаурид - 10, лигнинсульфокислота - 10. Указанное средство позволяет повысить урожайность подсолнечника более чем на 10% по сравнению с известным торговым средством невирол, стимулирует прорастание семян и развитие растений подсолнечника. 5 табл.

Способ получения производных 2,4-диамино-5-бензил пиримидина

Гербицидное средство

The herbicide contains, as active substance, a compound of the formula I. The herbicide is prepared by mixing the carrier with a compound of the formula I. The compound of the formula I can be obtained by reacting a compound of the formula II with a compound Hal-Z or a suitably substituted phenoxypropionyl halide with a compound HYZ. The substituents in the compounds have the meanings given in patent claim 2. <IMAGE>

Способ получения замещенных 2,6-динитробензоламинов

Способ получения 5-[4-(4-ацетил-3-гидрокси-2-пропилбензилокси)бензил]-тетразола

Изобретение касается замещенных гетероциклических веществ, в частности получения 5-[4-(4-ацетил-3-гидрокси-2-пропилбензилокси)-бензил]тетразола, используемого для лечения аллергических заболеваний, например астмы. Цель - создание нового более активного вещества указанного класса. Синтез ведут реакцией азида тетраметилгуанидиния с 4-[4-ацетил-3-гидрокси-2-пропилбензилокси]фенилацетонитрилом в среде диметилформамида в атмосфере аргона при 120-123°С. Выход 55,8%, т.пл. 155-157°С, брутто-ф-ла C20H22N4O3. Новое вещество малотоксично и имеет более высокий срок службы (6 ч, против 0,6 мин в известном случае). 1 табл.

Способ получения производных акриловой кислоты

Изобретение относится к моноциклическим аминам, в частности к производным акриловой кислоты ф-лы @ , где R 1 - нитрил, группа - COOR 2, где R 2 - метил или этил X-CL или F X 1-H или F X 2 - CL или F, которые являются промежуточными продуктами для синтеза антибактериальных лекарственных средств. Цель - упрощение процесса и повышение выхода целевого продукта. Получение ведут реакцией бензоилгалогенида с производным карбоновой кислоты в среде инертного растворителя и акцептора кислоты с последующей обработкой полученного соединения циклопропиламином в среде инертного растворителя.

Способ очистки динитрила малоновой кислоты

Способ получения ди-н-пропилацетамида

Способ получения производных бензопирана или их солей

Способ получения 5-замещенных 2,4-диаминопиримидинов или их кислотно-аддитивных солей

Compounds of the formula (1): or a salt, N-oxide or acyl derivative thereof, wherein is a six membered ring optionally containing a hetero atom double bonds, both the phenyl ring and the being optionally substituted except that when does not contain a hetero atom either or both the phenyl ring or must be substituted other than solely by a hydroxy group at the 4-position of the phenyl ring, and that there are no substituents attached to the atom of adjacent to the 6-position of the phenyl ring are useful in the treatment of bacterial infections. A process for preparing these compounds and novel chemical intermediates used in their preparation are disclosed as is the first medical use of the compounds of the formula (I) and pharmaceutical compositions containing them.

Способ получения сульфонатов или гидрохлоридов динитрила аминомалоновой кислоты

Изобретение касается замещенных аминокислот, в частности получения сульфонатов или гидрохлоридов динитрила аминомалоновой кислоты, применяемых в органическом синтезе. Цель - повышение выхода целевого продукта. Его синтез ведут нитрозированием динитрила малоновой кислоты нитритом натрия в среде смеси 15 - 30 моль воды и 0,02 - 0,05 моль серной кислоты (в расчете на 1 моль динитрила малоновой кислоты) при PH 3,8 - 4,2 и комнатной температуре. Затем продукты нитрозирования, содержащие динитрил оксиаминомалоновой кислоты , подвергают экстракции с этилацетатом, экстракт гидрируют при 10 - 60°С в присутствии PT/C в смеси уксусной кислоты с этилацетатом при ее молярном соотношении с этилацетатом (2-15):1 и давлении 1-40 ат. После гидрирования продукт отфильтровывают от катализатора и ведут осаждение целевого продукта обработкой соответствующей кислотой. Эти условия повышают выход целевого продукта с 27 - 49% до 63 - 88,5%. 1 з.п. ф-лы, 2 табл.

Способ получения производных 1,1-бифенил-2-илалкиламина или их солей

1,1 min -biphenyl-2-yl alkylamine derivatives of formula (I): <CHEM> wherein: X is hydrogen or a halo substituent at any position in the phenyl ring; R<1> is hydrogen, hydroxy, C IDENTICAL N, CONR<5>R<6>, or CO2R<8> where R<5>, R<6>, R<8> independently represent hydrogen or alkyl; R<2> is hydrogen or alkyl; Z is -(CH2)n- or -CH2@@CH2-; where n is an integer of from 2 to 4; R<3> and R<4> independently are hydrogen, C1-6 alkyl, CH2C2-5 alkenyl, phenyl C1-3 alkyl, or taken together with the adjacent nitrogen atom form a heterocyclic group or a pharmaceutically-acceptable salt thereof. The compounds are prepared by the usual methods for analogous compounds. They have been found to be effective in the treatment of cardiac arrhythmias. Pharmaceutical formulations have been prepared.

Способ получения фениламиноалканов

Способ очистки адипонитрила

Process for the preparation of acyl-2 hexahydro-1, 2,3,4,6,7,11b-2h pyrazino (2,1-a) isoquinolène-4 and intermediaries.

New oximes, their method of preparation and their applications.

Process and composition for the adjustment and the stimulation of the growth of plants.

FLUOREBENZYL ESTERS

Fluorobenzyl esters.

R is selected from ...

COMPOSITIONS FOR THE TREATMENT OF HYPERTENSION AND/OR FIBROSIS

FLUOREBENZYL ESTERS

Phénoxy-and-thiophénoxynitriles and their applications as weedkillers.

Alcoyamino N-phényl pyrazole and N-phényl pyrazole lactams weedkillers.

Agents of fight against the harmful organizations.

Hydroxyimino-aminoacétonitriles and their preparation.

Pesticides compositions.

Process for the fixing of alkyl group on a carbonaceous chain carrying a functional grouping.

Improvements relative to compounds of 1-benzoyl-3- (arylpyridyl) ureas.

New method of preparation of the acid (benzole-3-phényl) - 2 propionic and analogues.

Derived from aminosulphényl chloride, proceeded for their prepation, proceeded for their preparation of derived from useful carbamates like insecticides, miticides or nematocides.

Pharmaceutical compounds, their preparation, use and intermediaries and their preparation.

New derivatives of the carboxylic acid cyclopropane, their preparation, their application to the fight against the parasites and the compositions containing them.

Crystalline pair of enantiomers of phenylacetate and preparation of a pair of énanciomère pesticide.

N-phenylpyrazole derivatives.

Derived propargyloxybenzyenes their fungicidal preparations the container.

Substituted and produced phenylic derivatives pesticides which contain some.

HERBICIDAL COMPOSITIONS CONTAINING 3,5-DIHALO-4-HYDROXY-BENZONITRILES

Method of preparation of new pentanol derivatives.

Improvements relative to derivatives of N-arylbenzamides.

Derived from alcadienes, their preparations, drugs the container and intermediate products

New derivatives of sydnone, useful in particular like disinfecting industrial and their method of preparation.

Derived from the pipéridinedione protective of the myocardium presenting a antiarythmic activity, their method of preparation and the drugs which contain the aforementioned derivatives.

Diamides of substituted hydroxymalonic acid, their process of production and their use as pesticides.

Method of preparation of news alcénylèneamines substituted into 3.

New pentagonal heterocycles containing of nitrogen, their processes of production like their use as pesticides.

New compounds weedkillers.

New weedkillers, their preparation and use.

Fluorobenzyl esters.

New pesticides.

Weedkillers compositions.

New agents pesticides and in particular mollusquicides.

Esters of acids thiophosphoric usable in particular like phytopharmacological active matters of products.

Process for the preparation of optically-active cyanomethyl esters.

New agents pesticides.

New cyclopropane derivatives, their method of preparation and their application like insecticides.

Ketones carrying of the basic substituents and their method of preparation.

Derived from the 1-hétéroaryl-4-/(2,5-pyrrolidinedion-1-yl) alkyl/piperazine.

Esters of substituted carboxylic a-cyané alcohol acids cyclopropane, their method of preparation, the pesticides compositions containing them and their applications in the fight against the acarina.

Method of preparation of new derivatives of benzofuran.

Pesticidal method using 2-phenylimidazole derivatives.

New derivatives of the benzopyranne and their method of preparation.

Derived from acids phenoxy-proprionic endowed with properties weedkillers.

Method of preparation of derived from the acid acetic and derived obtained by this process.

Esters of substituted acetic acid optically active and substituted benzylic alcohol racemic or optically credit, endowed with insecticidal properties, their method of preparation and compositions insecticidal containing them.

New esters of related acids cyclopropanecarboxylic to the acid pyrethric, their method of preparation and their application to the fight against the parasites.

Composed weedkillers, compositions the container and their processes of uses

New esters of carboxylic acids cyclopropane comprising a polyhalogéné substituent, method of preparation and pesticides compositions.

Method of preparation of a derivative of acétonitrile and derived obtained by this process.

Method for isolating methylglycinenitrile-n,n-diacetonitrile

A method for isolating methylglycinenitrile-N,N-diacetonitrile (MGDN) from an aqueous mixture comprising MGDN is provided The method comprises cooling the aqueous mixture in one or more steps In one of these steps the mixture is cooled at a cooling rate of at least 20 K/h from a temperature above the solidification point of MGDN to a temperature below the solidification point of MGDN The method is implemented continuously

New efficient process for the preparation of sitagliptin

Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.

CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 2. The compound of claim 1 , wherein each occurrence of Yand Yis independently OH claim 1 , COOR claim 1 , or COOH.3. The compound of claim 1 , wherein m is 0.4. The compound of claim 1 , wherein m is 1.5. The compound of claim 1 , wherein n is 4.6. The compound of claim 1 , wherein n is 5.7. The compound of claim 1 , wherein X is (CH)and z is 0.8. The compound of claim 1 , wherein each occurrence of Rand Rand the carbon to which they are both attached are taken together to form a (C-C)cycloakyl group.9. The compound of claim 1 , wherein Yand Yare each independently (C-C)alkyl.10. The compound of claim 1 , wherein Yand Yare each methyl.1157-. (canceled) This application claims the benefit of U.S. Provisional Application No. 60/441,795, filed Jan. 23, 2003, which is incorporated herein by reference in its entirety.The invention relates to cycloalkyl-hydroxyl compounds and pharmaceutically acceptable salts, hydrates, solvates, and mixtures thereof ...

Cycloalkyl-hydroxyl compounds and compositions for cholesterol management and related uses

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 157-. (canceled)59. The method claim 58 , wherein each occurrence of Yand Yis independently COORor COOH.60. The method of claim 58 , wherein Yand Yare each COOH.61. The method of claim 58 , wherein m is 0.62. The method of claim 58 , wherein m is 1.63. The method of claim 58 , wherein n is 4.64. The method of claim 58 , wherein n is 5.65. The method of claim 58 , wherein X is (CH)and z is 0.68. The method of claim 58 , wherein the compound of formula I is orally administered to the patient in the form of a pharmaceutical composition comprising the compound of formula I claim 58 , and a pharmaceutically acceptable vehicle.71. The method of claim 69 , wherein the compound of formula I is orally administered to the patient in the form of a pharmaceutical composition comprising the compound of formula I claim 69 , and a pharmaceutically acceptable vehicle.72. The method of claim 70 , wherein the compound is orally administered to the patient in the ...

Novel polygodial analogs for the treatment of cancer and other proliferative diseases

The present disclosure relates generally to derivatives of polygodial and methods of use thereof. In some aspects, the present disclosure relates to using polygodial derivatives to treat cancer or other hyperproliferative diseases.

Hydroxyl compounds and compositions for cholesterol management and related uses

The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 2. The compound of claim 1 , wherein each occurrence of Yand Yis independently OH claim 1 , COOR claim 1 , or COOH.3. The compound of claim 1 , wherein m is 0.4. The compound of claim 1 , wherein m is 1.5. The compound of claim 1 , wherein n is 4.6. The compound of claim 1 , wherein n is 5.7. The compound of claim 1 , wherein z is 0.8. The compound of claim 1 , wherein z is 1.9. The compound of claim 1 , wherein Yis (C-C)alkyl and Yis OH.10. The compound of claim 1 , wherein Yis methyl and Yis OH.1161-. (canceled) This application claims the benefit of U.S. Provisional Application No. 60/441,795, filed Jan. 23, 2003, which is incorporated herein by reference in its entirety.The invention relates to hydroxyl compounds and pharmaceutically acceptable salts, hydrates, solvates, and mixtures thereof; compositions comprising a hydroxyl compound or a pharmaceutically acceptable salt, hydrate, solvate, or ...

CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 2. The compound of claim 1 , wherein each occurrence of Yand Yis independently OH claim 1 , COOR claim 1 , or COOH.3. The compound of claim 1 , wherein m is 0.4. The compound of claim 1 , wherein m is 1.5. The compound of claim 1 , wherein n is 4.6. The compound of claim 1 , wherein n is 5.7. The compound of claim 1 , wherein X is (CH)and z is 0.8. The compound of claim 1 , wherein each occurrence of Rand Rand the carbon to which they are both attached are taken together to form a (C-C)cycloakyl group.9. The compound of claim 1 , wherein Yand Yare each independently (C-C)alkyl.10. The compound of claim 1 , wherein Y and Yare each methyl.1157-. (canceled) This application claims the benefit of U.S. Provisional Application No. 60/441,795, filed Jan. 23, 2003, which is incorporated herein by reference in its entirety.The invention relates to cycloalkyl-hydroxyl compounds and pharmaceutically acceptable salts, hydrates, solvates, and mixtures ...

HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 12-. (canceled)46-. (canceled)7. The method of claim 3 , wherein each occurrence of Yand Yis independently OH claim 3 , COOR claim 3 , or COOH.8. The method of claim 3 , wherein m is 0.9. The method of claim 3 , wherein n is 5.10. The method of claim 3 , wherein z is 0.11. The method of claim 10 , wherein R claim 10 , R claim 10 , R claim 10 , and Rare (C-C)alkyl.12. The method of claim 11 , wherein Yand Yis COOH.16. The method of claim 15 , wherein each occurrence of Yand Yis independently OH claim 15 , COOR claim 15 , or COOH.17. The method of claim 15 , wherein m is 0.18. The method of claim 15 , wherein n is 5.19. The method of claim 15 , wherein z is 0.20. The method of claim 19 , wherein R claim 19 , R claim 19 , R claim 19 , and Rare (C-C)alkyl.21. The method of claim 20 , wherein Yand Yis COOH.24. The method of claim 15 , wherein the compound of formula I is orally administered to the human ...

1,2,4-Triazine derivatives, process for preparing such compounds and pharmaceutical compositions containing them

The present invention provides compounds of the formula (III): or an acid addition salt thereof, wherein R 6 is chlorine, bromine, iodine, C 1 - 4 alkyl or trifluoromethyl, R 7 is hydrogen, halogen, C 1-4 alkyl or trifluoromethyl or R 6 and R 7 form a -CH=CH-CH=CH- group optionally substituted by a halogen atom or a C 1-4 alkyl or trifluoromethyl group, R 8 is hydrogen, halogen, C 1-4 alkyl or trifluoromethyl, R 9 is hydrogen, halogen, C 1-4 alkyl or trifluoromethyl, R 10 is hydrogen, methyl or fluorine and R" is amino, C 1-4 acylamino or di-substituted aminomethyleneamino provided that, at most, only two of R 7 ―R 10 are other than hydrogen and that R 7 ―R 10 are not all hydrogen when R 6 is chlorine. Also provided are pharmaceutical compositions containing compounds of the formula (III), the first medical use of compounds of the formula (III), a process for preparing such compounds and intermediates through which this process proceeds.

CYLINDER DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS

Benzylidene- and cinnamylidine-malononitrile derivatives for the inhibition of proliferative processes in mammalian cells

57 There are provided pharmaceutical compositions containing as an active ingredient a compound of the general formula (I): wherein R 1 and R 2 are each independently CN, CONH 2 or COOH or one of R 1 ad R 2 may be -CSNH 2 or, when R 1 is CN, R 2 can also be the group R 3 is H, CH 3 or OH, R 4 , Rs, R 6 , R 7 are each independently H, OH, C 1-5 alkyl, C 1-5 alkoxy, NH 2 , CHO, halogen, N0 2 or COOH, or R 4 and R 5 together may represent a group -O-CH 2 -O-; provided that: (a) when R 4 ad R 7 are each OH, R 3 , R 5 and R 6 are each H and one of R 1 and R 2 is CN, then the other of R 1 and R 2 cannot be CONH 2 ; and (b) when R 3 and R 7 are each H, R 5 is OH and R 4 and R 6 are both H or both C 1 -5 alkyl, then R 1 is CN and R 2 is CN or the group or a pharmaceutically acceptable salt thereof. There are also provided some novel compounds of formula (I) above. The compositions and compounds according to the invention are efficient protein-tyrosine kinase inhibitors and are suitable for the inhibition of proliferative processes in mammalian cells.

Werkwijze ter bereiding respectievelijk vervaardiging van een farmaceutisch preparaat en werkwijze ter bereiding van daarbij bruikbare nieuwe gesubstitueerde 1-(4-aminofenyl)-2-amino-ethanol-derivaten die, behalve een analgetische, uterusspasmolytische en anti-spastische werking op de dwarsgestreepte spieren, in het bijzonder een betaŸ2-mimetische en/of betaŸ1-blokkerende werking bezitten.

NEW DIARYLAMINES, THE PROCESS FOR THEIR MANUFACTURING AND THEIR USE

Insecticidal pyrazoline derivatives

SUBSTITUTED 5-ACYLAMINO-1-PHENYLPYRAZOLE

PROCESS FOR THE PRODUCTION OF RELIEF STRUCTURES

Patent FR2528420B1

PHARMACEUTICAL COMPOSITIONS CONTAINING CAMPHO-METHYLIDENE CINNAMIC ACID DERIVATIVES

Method for the arylation of olefines with aryl chlorides catalysed by Pd

Compounds of the formula I <IMAGE> in which A represents C2-12-alkenyl, C4-8-cycloalkenyl or a grouping -C(R)=C(R')-Y and Y, R, R', R1, R2, R3 and R'3 have the meaning given in Patent Claim 1, can be prepared in a simple and economical manner by reacting suitable chlorobenzenes in the presence of a base and catalytic amounts of a palladium compound which may contain arsenic or phosphorus at a temperature of at least 140 DEG C with a compound HA. Most of the compounds (I) are known and can be used, for example, directly as fluorescent brighteners or as intermediates for fluorescent brighteners or scintillators.

PROCESSING IN PROCESS FOR OBTAINING NITROLOTRIACETONITRILLA

Allylation of carbon compounds

Carbon acids are allylated by contacting with an allyl carbonate in the presence of a palladium catalyst.

Verfahren zur Herstellung von öllöslichen aeylierten Aminen

Method of flocculating suspended particulate matter from an aqueous medium

A catalyst for isomerization reaction

Method for preparing 3,5-disubstituted 4-hydroxybenzonitrile derivatives

Способ получени производных 3,5-диамино-1,2,4-триазина или их кислотно-аддитивных солей

1. Способ получени  производных . 3,5 ДV1aминo-1,2,-триазина общей формулы . (Г) где R - хлор, бром, иод, метил или трифторметилi R - водород или хлор, или R и R2 вместе образуют группу -СН СН-СН СН-; R - водород или бром; R - водород, хлор или бром} - водород, метил или фтор; R6 - амино-, ацетиламино- или ;диметиламиномети енаминогруппа,, при условии, что не более чем два заместител  из числа отличны . от водорода и что не все заместители из числа R -R  вл ютс  водородом, если R  вл етс  хлором, или их кислотно-аддитивных солей, отличающийс  тем, что соединение.общей формулы где К и R имеют указанные значени , нагревают при в инертном растворителе, в котором растворимы реагенты, с последующим выделением целевого продукта в виде основани  14ПН кислотно-аддитивной соли, или , СП а1 лированием дл  полумени  соедине01 ни  I, . со где Н - ацетиламиногруппа, или дисо метиламинометилированием дл  получени  соединени  1, где R - дииетил , аминометиленаминогруппа, и выделением .целевого про-дукта в виде основани  или кислотно-аддитивной соли. 2. Способ по По 1, о т л и ч а ющ и и с   тем, что процесс провод т в присутствии основани  в С -С -алканоле .

Process for preparing 2-amino-5-hydroxy-4-methyl-pyrimidine derivatives

Chemical process

Method of obtaining derivatives of n-arylbenzamide or salts thereof

N-arylbenzamide derivatives of formula (I) <CHEM> wherein Z is oxygen or sulfur, R1, R2, R3 are hydrogen or a substituent, R4 is an heteroaryl group linked to the nitrogen atom by a carbon atom, selected from possibly substituted isoxazole, isothiazole, pyrazole, imidazole, thiadiazole, oxadiazole or pyridazine. These compounds can be used as herbicides.

The method of obtaining phenylaminoalkanes

Reaction product of an aliphatic olefinpolymer-succinic acid producing compound with an amine and reacting the resulting product with a boron compound

Reaction product of high molecular weight succinic acids and succinic anhydrides with an ethylene poly- amine

Oil soluble acrylated nitrogen compounds having a polar acyl, acylimidoyl or acyloxy group with a nitrogen atom attached directly thereto

Derivatives of succinic acids and nitrogen compounds

Boron-containing acylated amine and lubricating compositions containing the same

Method of controlling undesirable vegetation

Способ получени бифенилилбутеновых кислот или их производных

Patent SU398031A3

Method of preparing benzopyrane derivatives or their salts

New benzopyrane derivatives of the general formula <IMAGE> (I) in which R is free, esterified or amidated carboxyl, Ph is 1,2-phenylene which contains the group R-CO-NR3- and is otherwise unsubstituted or is substituted, X is a group of the formula -CO-CR1=CR2-, in which R1 and R2 independently of one another are hydrogen, acyl or a substituted or unsubstituted hydrocarbon radical or a hetero-analogue thereof, or conjointly are 3-membered to 5-membered lower alkylene, and R2 can also be free or etherified hydroxyl or hydroxyl etherified by an organic carboxylic acid, and R3 is hydrogen or lower alkyl, are useful as anti-allergic agents.

Method of preparing benzoxazole derivatives

The invention provides novel 5- and 6-benzoxazolyl alkanoic acids, optionally substituted in the 2-position, and derivatives thereof which possess anti-inflammatory, anti-pyretic and analgesic activity. Also provided is a process for preparing such compounds by cyclising an appropriately substituted o-aminophenol and, if necessary, converting the resultant benzoxazole to the desired compound.

METHOD OF OBTAINING ETHANOANTHRACENES

ネマチツク化合物

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

The method of obtaining derivatives of ethylenebenzoyl

Method for preparing biphenyl derivatives

殺カビ剤

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

Method of preparing 4-(polyalkoxyphenyl)-2-pyrrolidones

4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula <IMAGE> wherein R1 and R2 are hydrocarbon; R3 is hydrogen or methoxy; R is O-alkyl, O-aryl, O-aralkyl, NH2, NH-alkyl, NH-aryl, NH-aralkyl, N(alkyl)2, N(aryl)2 or <IMAGE> AND X is O or S, are neuropsychotropic agents.

Process for producing 2,3,5-trichloropyridine and 2,4,4-trichloro-4-formylbutyronitrile (modifications)

Method of weed control

N-Phenylpyrazole derivatives of the formula:- <CHEM> (wherein each of R<5> and R<6> represents a C1-C4 alkyl or alkoxy radical, a trifluoromethyl, trifluoromethoxy, nitro, cyano or primary amino radical, or a fluorine, chlorine or bromine atom, each of R<7>, R<8> and R<9> represents a hydrogen atom, a C1-C4 alkyl or alkoxy radical, a trifluoromethyl, trifluoromethoxy, nitro, cyano or primary amino radical or a fluorine, chlorine or bromine atom, or R<5>, R<7>, R<8> and R<9> each represents a hydrogen atom and R<6> represents a trifluoromethoxy or trifluromethyl radical, and R<1><0> represents a cyano radical or substituted carbamoyl radical -CONHR<1><1>, wherein R<1><1> represents a methyl or ethyl radical) have been found to possess useful herbicidal properties. All such N-phenylpyrazole derivatives with the exception of 5-amino-4-cyano-1-(2,4-dichlorophenyl)pyrazole and 5-amino-4-cyano-1- (4-chloro-2-methylphenyl)pyrazole are new compounds. Herbicidal compositions containing such N-phenylpyrazole derivatives are described and also processes for the preparation of the new compounds.

Method of producing 2,4-diamino-5-(substituted)pyrimidines or their salts

Compounds of the formula (1): or a salt, N-oxide or acyl derivative thereof, wherein is a six membered ring optionally containing a hetero atom double bonds, both the phenyl ring and the being optionally substituted except that when does not contain a hetero atom either or both the phenyl ring or must be substituted other than solely by a hydroxy group at the 4-position of the phenyl ring, and that there are no substituents attached to the atom of adjacent to the 6-position of the phenyl ring are useful in the treatment of bacterial infections. A process for preparing these compounds and novel chemical intermediates used in their preparation are disclosed as is the first medical use of the compounds of the formula (I) and pharmaceutical compositions containing them.

The method of obtaining aminoethanol or their salts

Method of preparing 5-iodo-3-nitro-4-oxybenzonitrile salts

Salts of 5-iodo-3-nitro-4- hydroxybenzonitrile with certain amide or imidazole derivatives are useful for the treatment of liver conditions and as growth regulating and pesticidal agents for plants. For these uses the salts can be formulated in conventional manner.

피라졸린 유도체의 제법

내용 없음

The method of obtaining 3-fluoro-alanine

The method of obtaining derivatives of 3-amino-2-pyrazoline

Method of controlling fungi infection of plants

Disclosed is a method of fighting fungus infections by using compounds having the general formula: wherein R is H, C 1 -C 4 alkyl, alkenyl or alkynyl; n is 1 or 2; A represents a C 1 -C 6 alkylene bridge, an arylene or a heterocyclic bridge; X represents 0, S, SO or S0 2 ; R 1 is selected from C 1 -C 6 alkyl, optionally substituted phenyl, polyfluoroalkyl containing 1 to 4 carbon atoms and at least 2 fluorine atoms, and poiyfluoroalkenyl containing 2 to 4 carbon atoms and at least 2 fluorine atoms, excluding those compounds of general formula (l) wherein A is alkylene, n is 2 and R 1 is C 1 -C 6 alkyl.

Method of producing derivatives of 2-amino-5-oxy-4-methyl-pyrimidine or acid-additive salts thereof

Method of producing substituted acetamides or their salts

Condensation polymer containing the residue of a poly-methine compound and shaped articles produced therefrom

Composition useful for molding into articles which as food containers, beverage bottles, cured structural plastics and the like comprising molding grade linear or unsaturated polyester or polycarbonate having reacted therewith or copolymerized therein the residue of one or more poly-methine compounds having the formula: ##STR1## wherein each R 1 is independently selected from cyano, carboxy, alkenyloxycarbonyl, or a substituted or unsubstituted alkoxycarbonyl, cycloalkoxoycarbonyl or aryloxycarbonyl radical; each R 2 is independently selected from one of the groups specified for R 1 or an unsubstituted or substituted aryl, carbamoyl, alkanoyl, cycloalkanoyl, aroyl, alkylsulfonyl, cycloalkylsulfonyl, arylsulfonyl or aromatic, heterocyclic radical; each R 3 is independently selected from hydrogen or an unsubstituted or substituted alkyl, cycloalkyl or aryl radical; A 1 and A 2 are independently selected from 1,4-phenylene radicals; and L is an organic linking group bonded by non-oxo carbon atoms to the oxygen atoms adjacent to L; provided the poly-methine compound bears at least one substituent that is reactive with one of the monomers from which the condensation polymer is derived. The polymethine residues are present in the polymer as an integral part of the polymer chain and absorb ultraviolet radiation in the range of about 250 to about 390 nm. The residues are non-extractable from the polymer and stable at the conditions at which the polymers are manufactured and processed.

Condensation polymers containing methine ultraviolet radiation-absorbing residues and shaped articles produced therefrom

A composition useful for molding into articles such as food containers, soft drink bottles, cured structural plastics and the like, comprising molding grade linear or unsaturated polyester or polycarbonate having reacted or copolymerized therein a total of from 100 to about 800 ppm, of the residue of one or a mixture of methine reactants of the formula ##STR1## wherein R 1 is hydrogen or an unsubstituted or substituted alkyl, alkenyl, cycloalkyl or aryl radical; A 1 is an unsubstituted or substituted phenylene radical; A 2 is an unsubstituted or substituted 1,4-phenylene radical; R 2 is hydrogen or an unsubstituted or substituted alkyl, cycloalkyl or aryl radical; R 3 is cyano or ##STR2## and R 4 is one of the substituents which R 3 can represent or an unsubstituted or substituted carbamoyl, alkanoyl, aroyl, alkylsulfonyl, arylsulfonyl, aryl or aromatic heterocyclic radicals. The methine residues are present in the polymer as an integral part of the polymer chain and absorb ultraviolet radiation in the range of about 250 to about 390 nm. The residues are non-extractable from the polymer and stable at the conditions at which the polymers are manufactured and processed.

Method of preparing 5-or 6-benzoxazolic acid or salts thereof

The invention provides novel 5- and 6-benzoxazolyl alkanoic acids, optionally substituted in the 2-position, and derivatives thereof which possess anti-inflammatory, anti-pyretic and analgesic activity. Also provided is a process for preparing such compounds by cyclising an appropriately substituted o-aminophenol and, if necessary, converting the resultant benzoxazole to the desired compound.

Method of preparing aminopropane derivatives or their salts in the form of racemate or optically active antipodes

1450287 Pharmaceutical compositions BOBHRINGER INGELHElM GmbH 27 Feb 1974 [28 Feb 1973 26 Jan 1974] 8949/74 Heading A5B [Also in Division C2] Pharmaceutical compositions comprise a compound of the general formula R 1 = H, halogen, NO 2 , C 1-5 alkyl, C 1-4 alkoxy, C 2-5 alkenyl or alkynyl, C 1-6 alkylamino, di(C 1-6 alkyl)amino, C 1-6 alkoxy-(C 1-6 alkyl), C 1-6 alkyl- or di(C 1-6 alkyl)-amino- (C 1-6 alkyl), (CH 2 ) 0-3 -(CN, NH 2 or OH), COOH C 2-5 alkoxycarbonyl, C 3-6 alkenyloxy or alkylnyloxy, optionally substituted aliphatic or araliphatic acyl, acyloxy or acrylamino wherein each aliphatic moiety contains 1-6 carbon atoms, aromatic acyl, acyloxy or acylamino, C 3-7 cycloalkyl, QCONR 7 R 8 : Q = single bond, O, NH, CH 2 , CH 2 NH: R 7 , # =H, C 1-6 alkyl, aryl or aryloxy optionally bearing one or more substituents selected from halogen, alkyl, alkoxy, NO 2 ,CN, COOH, or NR 7 R 8 = heterocyclic group; R 2 = H, halogen, CN, NH 2 , NO 2 , C 1-4 alkyl or alkoxy, C 2-4 acyl or alkenyl, or R 1+2 = 3. 4-methylenedioxy: R 3 = H, halogen, C 1-4 alkyl or alkoxy. or R 2 +3 (bonded to adjacent carbon atoms) = (CH 2 ) 3-5 or -CH=CH-CH=CH-: R 4 = H, C 1-3 alkyl; R = C 1-3 alkyl, or R 4+5 = (CH 2 ) 4-6 or acid addition salt thereof, with or without a further active ingredient, e.g. coronary detectors, sympathicomimetics, cardiac glycosides, tranquilisers), in association with a carrier. The primary active ingredients are adrelytics and hypotensive agents.

Method for producing 2,4-diamino-5-(substituted) pyrimidines

Compounds of the formula (1): or a salt, N-oxide or acyl derivative thereof, wherein is a six membered ring optionally containing a hetero atom double bonds, both the phenyl ring and the being optionally substituted except that when does not contain a hetero atom either or both the phenyl ring or must be substituted other than solely by a hydroxy group at the 4-position of the phenyl ring, and that there are no substituents attached to the atom of adjacent to the 6-position of the phenyl ring are useful in the treatment of bacterial infections. A process for preparing these compounds and novel chemical intermediates used in their preparation are disclosed as is the first medical use of the compounds of the formula (I) and pharmaceutical compositions containing them.

The method of obtaining benzophenone derivatives or their salts

Composition for the treatment of pulmonary fibrosis

본 발명은 폐 섬유증 및/또는 관련 질환의 예방 및/또는 치료학적 치료에서의 화합물 및 이의 용도에 관한 것이다. The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related diseases.

Herbicidic composition

New compounds of the formula I are described in which the substituents have the meaning given in Patent Claim 1 and which are used as herbicides and, in particular, can be used in rice crops. Also described is a process for the preparation of the compounds mentioned, and the use of the compounds as herbicides. <IMAGE>

Method of producing derivatives of n-phenyl pyrazole

N-Phenylpyrazole derivatives of the formula:- <CHEM> (wherein each of R<5> and R<6> represents a C1-C4 alkyl or alkoxy radical, a trifluoromethyl, trifluoromethoxy, nitro, cyano or primary amino radical, or a fluorine, chlorine or bromine atom, each of R<7>, R<8> and R<9> represents a hydrogen atom, a C1-C4 alkyl or alkoxy radical, a trifluoromethyl, trifluoromethoxy, nitro, cyano or primary amino radical or a fluorine, chlorine or bromine atom, or R<5>, R<7>, R<8> and R<9> each represents a hydrogen atom and R<6> represents a trifluoromethoxy or trifluromethyl radical, and R<1><0> represents a cyano radical or substituted carbamoyl radical -CONHR<1><1>, wherein R<1><1> represents a methyl or ethyl radical) have been found to possess useful herbicidal properties. All such N-phenylpyrazole derivatives with the exception of 5-amino-4-cyano-1-(2,4-dichlorophenyl)pyrazole and 5-amino-4-cyano-1- (4-chloro-2-methylphenyl)pyrazole are new compounds. Herbicidal compositions containing such N-phenylpyrazole derivatives are described and also processes for the preparation of the new compounds.

Process for preparing derivatives of aminopropanol or their salts

The present invention relates to new compounds of the formula as well as their preparation, pharmaceutical preparations containing same, and method of treating acute myocardial infarction. The compounds which possess beta-adrenoceptor blocking activity are very shortacting and are preferably intended for treatment of acute myocardial infarction by administration by means of injection.

Patent GR74113B

Esters of trisubstituted hydroxyphenylalkonoic acids

Novel intermediate product and manufacture

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

1*1**biphenyll22yllalkylamine derivative

PHENYLETHER DERIVATIVES AND PROCEDURES FOR PREPARING THEREOF

Indene derivative and method for producing the same

Processes and intermediates useful to make antifolates

1. A. compound of formula III: where: Y is CH=CH, O, or S; R is C1-C6 alkyl; R<1> and R<2> are independently C1-C6 alkyl or taken together with the nitrogen to which they are attached form a heterocycle; R<3> is hydrogen, chloro, or fluoro; R<4> is hydroxy, a carboxy protecting group, or NHC*H(C(O)R<5>)CH2CH2C(O)R<5> where the configuration about the carbon atom designated * is S; and R<5> is hydrogen or a carboxy protecting group; or a salt or solvate thereof. 2. A compound according to Claim 1 where Y is CH=CH or S, R is C1-C4 alkyl, R<1> and R<2> are independently C1-C4 alkyl, R<3> is hydrogen, and R<4> is C1-C4 alkoxy or benzyloxy; or a salt or solvate thereof. 3. A compound according to Claim 2 where R is methyl or ethyl, R<1> and R<2> are both methyl or ethyl, and R<4> is methoxy, ethoxy, or benzyloxy; or a salt or solvate thereof. 4. A compound of formula IV: where: Y is CH=CH, O or S; R<3> is hydrogen, chloro or fluoro; R<4> is hydroxy, a carboxy protecting group. or NHC*H(C(O)R<5>)CH2CH2C(O)R<5> where the configuration about the carbon atom designated * is S; R<5> is hydrogen or a carboxy protecting group; R<6> is hydrogen or an amino protecting group; and R<7> is hydroxy; or a salt or solvate thereof. 5. A compound according to Claim 4 where Y is CH=CH or S and R<3> is hydrogen; or a salt or solvate thereof. 6. A compound according to Claim 5 where R<4> is methoxy, ethoxy, benzyloxy. or NHC*H(C(O)R<5>)CH2CH2C(O)R<5>;R<5> is C1-C6 alkyl; R<6> is an amino protecting group; and R<7> is hydroxy; or a salt or solvate thereof. 7. A compound according to Claim 6 where R<4> is NHC*H(C(O)R<5>)CH2CH2C(O)R<5 >; or a salt or solvate thereof. 8. A process for preparing a compound of formula IV: where: Y is CH=CH, O, or S; R<3> is hydrogen, chloro, or fluoro; R<4> is hydroxy, ...

Method of producing 5-(2-alkoxyphenyl)thiazolidindiones or their basic salts with alkali metals

A series of 5-(2-alkoxyphenyl)thiazolidinediones and pharmaceutically acceptable salts thereof useful as hypoglycemic agents, aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications; intermediates therefore; and processes for preparation of said compounds.

The method of obtaining biphenylbutyric acids or their salts, or racemates, or optically active antipodes

Tetracyanoquinodimethane derivative

The method of obtaining liquid crystal Schiff bases

Herbicide

Method of preparing substituted ketocarboxylic acids

Process for the preparation of a uv-absorbing mask

Method for preparing 3-substituted alkenylene amines or their salts, or their alkanoyl derivatives, or their arylthiocarbamoyl derivatives

1-phenoxy-3-hydroxyindolyl-alkylamino-3-propanols and preparing process thereof

A process for preparing 1-penoxy-3-hydroxy indolyl alkylamino -3- propanols of formula (1) comprises (a) coupling a methoxylated indonealkylamine with a R5-substd. penoxy epoxide in the presence or absence of inactive organic solvent and (b) obtaining formula (I) by converting methoxyl gp. of the intermediate into hydroxyl gp. In the formula, one of R1 or R2 is H and the other is H or C1-4 alkyl; each of R3 and R4 is H or C-14 alkyl; R5 is halogen, H, OH or C1-4 alkyl. (I) are useful as a cardiovascular and antihypertensive agents.

New substituted amines.

Phenethylamine derivatives

1,263,987. Phenethylamine derivatives. ALLEN & HANBURYS Ltd. 20 May, 1970 [30 May, 1969], No. 27407/69. Heading C2C. Novel compounds of the Formula I and physiologically acceptable addition salts thereof in which R<SP>1</SP> represents a hydrogen atom or a C 1-6 alkyl group; R<SP>2</SP> represents a hydrogen atom or a benzyl group; R<SP>3</SP> represents a hydrogen atom or a C 1-6 alkyl group or R<SP>3</SP> represents an arylalkyl or aryloxyalkyl radical, which radicals may optionally be substituted by one or more alkoxy or hydroxyl groups; Z represents a group of formula -(CH 2 ) n Y in which n has the value of 0, 1 or 2, and Y represents a hydroxyl radical (except when n has the value 0) or a group of formula (in which R<SP>4</SP>, R<SP>5</SP> and R<SP>6</SP> which may be the same or different and represent hydrogen atoms or C 1-6 alkyl groups and R<SP>7</SP> represents a C 1-6 alkyl group) except that when n = 0 and Y is -NR<SP>4</SP>SO 2 R<SP>7</SP>, then R<SP>4</SP> is not hydrogen, and in addition to the above those in which R 2 is a benzhydryl group, Y may also be an alkoxy carbonyl-COOR where R is hydrogen or a C 1-6 alkyl group or Y may be -CONR<SP>5</SP>R<SP>6</SP> may be prepared by (1) reduction of a CH 2 CN to CH 2 CH 2 NH 2 (R 1 , R 2 , R 3 = H); (2) condensation of a carbonyl -CH 2 COR<SP>1</SP> with an amine R<SP>2</SP>R<SP>3</SP>NH and reduction of the resulting imine to give CH 2 CHR<SP>1</SP>NR<SP>2</SP>R<SP>3</SP>; (3) reduction of -CH=CR 1 NO 2 to give CH 2 CHR 1 NH 2 , (1) to (3) optionally being preceded or followed by one or more of (a) formation of the Z group or conversion of one Z group to another; (b) N- alkylation by condensation of the amine with a ketone or aldehyde followed by reduction; (c) conversion of ...

Phenethanolamines,their preparation and pharmaceutical compositions containing the same

Phenethanolamines, compositions containing the same, and method for effecting weight control

Optically active N-3-(4-substituted phenyl)propyl-β-phenethanolamines are provided as well as pharmaceutical compositions containing such compounds. A method for effecting weight control in obese animals utilizing optically active phenethanolamines is disclosed. Novel intermediates useful in the preparation of optically active β-phenethanolamines are provided.

Phenethanolamines

Abstract The tertiary amines of the formula I wherein n represents a whole number of 1 to 5; x1 represents phenyl or phenyl mono-, di- or tri-substituted by R1, R2 and R3; x2 represents hydrogen, lower-alkyl, phenyl or phenyl mono-, di- or tri--substituted by R1, R2 and R3; Y represents hydrogen, lower-alkyl, hydroxymethyl, carboxy or lower--alkoxycarbonyl; Z represents a group of the formula (Z) R1, R2 and R3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, acylamino, lower-alkoxybenzylamino, nitro, carbamoyl, trifluoromethyl or lower-alkylsulphonylmethyl; R4 and R5 represent lower alkanoyl, carboxy, cyano, hydroxy-lower-alkyl, acyloxy or a group -C(R6)=C(R7) COOR8, -SO2R9, -C(O)R9 or -CH2R10; R6, R7 and R8 represent hydrogen or lower-alkyl; R9 represents amino, mono-lower-alkylamino or a group R; R represents di-lower-alkylamino, piperi-dino, morpholino, thiamorpholino, pip-erazino or the ether group of a lower aliphatic, cycloaliphatic or araliphatic alcohol or of a phenol; and R10 represents a group R and, where R1, R2 and R3 represent hydrogen, halogen, hy-droxy, benzyloxy, lower-alkyl, lower--alkoxy, hydroxymethyl, amino, lower-alkoxybenzylamino or tri-fluoromethyl and simultaneously Y represents hydrogen, lower--alkyl or hydroxymethyl, R10 can also represent amino or mono-lower--alkylamino, and the physiologically acceptable salts thereof have hypoglycaemic activity and reduce glycosuria. They are manufactured from corresponding primary or secondary amines.

Process for preparing 2-(3-phenoxyphenyl)-proprionic acid or its calcium salt

2-(3-phenoxy-phenyl)-propionic acid or its pharmaceutical treatments, are prepared by hydrolyzing and partially decarboxylating <IMAGE> wherein R=C1-C6 alkyl or amino, the latter compounds being themselves new and, where R=C1-C6 alkyl, have antiinflammatory pharmaceutical properties.

Preparation method of pyrazoline derivatives

Pyrazolines I[R1=H, alkyl, Ph, cyanoalkyl or alkoxyalkyl; R2, R3=H, alkyl, Ph; R4=H or alkyl; X=H or halogen; W=O or S; Y,Z=H, halogen, alkyl, alkoxy, NO2, CF3, alkylthio, acyl, CN, alkylsulphonyl, alkoxycarbonyl or haloalkyl-A' or Y+Z form OCH2O; A'=O,S,SO or SO2) are prepd.. Thus, 4-HOC6H4COCH2Ph is treated with ClCHF2 to give 4- CF2OC6H4COCH2Ph which is treated with CH2O to give 4-CF2HOC6H4CO Ph; CH2. The latter is cyclized with N2H4 to give 3-(4- difluoromethoxyphenyl)-4-phenyl-2-pyrazoline which is treated with 4- ClC6H4NCO to give I(X=R2=R4=H, R1=Ph, W=O). (I) are broad-spectrum insecticides and are active against both young and old larvae.

Fungicide azolyl derivative

Polymerizable liquid-crystal material and polymers exhibiting liquid-crystal phases

The invention relates to polymerizable liquid-crystal materials and to polymer materials which exhibit liquid-crystal phases and which contain, attached directly or via a spacer, mesogenic groups in which at least one transversely polarizing structural element of the formulae I to X, defined in claim 1, is present.