Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use.

Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof: in which: R.1 is vinyl or ethyl; and R2 is a group R3, R4CH2~, or R5R6C=CH-; wherein each of R3 and R4 is an azabicyclic ring system or R5 and R^ together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

Tricyclic compounds having activity specific for integrins, particularly avB3 integrins, method for preparing same, intermediates therefor, use of said compounds as drugs, and pharmaceutical compositions containing same.

The subject of the invention is the products of formula (I) : in which R-1, R2, R3 / £4,R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.

INHIBITORS OF BETA-SECRETASE

Carbamoyloxy derivatives of mutiline and their use as antibacterials.

Derivatives of mutiline of formula (1a)and pharmaceutically acceptable salts and derivatives thereof, in which r1 is ethyl or vinyl, y is a carbamoyloxy group, which the n-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Novel compounds

Tric clic ompou ds ha ing a tivity specific for integrins particularly avbs intergrins method for preparing same intermediates therefore use of said compounds as drugs and pharmaceutical compositions containing same

Novel compounds.

Compounds of formula (1a)and pharmaceutically acceptable salts and derivativews thereof in which y is a carbamoyloxy group, in which the n-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Inhibitors of beta-secretase

Carbamoyloxy derivatives of mutiline and their useas antibacterials.

Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R<1> is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Tricyclic compounds having an activity screw-with-visdes intégrines in particular with respect to the intégrine ALPHAvBETA3, their method of preparation and I ntermédiaires of this process, their application as drugs and the compositions pharmaceutical containing them.

Inhibitors of beta-secretase

Carb moylo y der vativ s of utiline and their use as antibacterials

Inhibitors of beta-secretase

Tric clic ompou ds ha ing a tivity specific for integrins particularly avbs intergrins method for preparing same intermediates therefore use of said compounds as drugs and pharmaceutical compositions containing same

Novel compounds

Novel compounds

2-METHYL-3-RHODANIDO-PROPIONSÄURE UND VERFAHREN ZU IHRER HERSTELLUNG

ACRYLIC ACID DERIVATIVES AND FUNGICIDES, THESE CONNECTIONS CONTAINING.

Carbamoyloxy derivatives of mutiline and their use as antibacterials

Tricyclic compounds having activity specific for integrins, particularly alphav beta3 integrins, method for preparing same, intermediates therefor, use of said compounds as drugs, and pharmaceutical compositions containing same

CEPHALOSPORIN DERIVATIVES

CEPHALOSPORIN DERIVATIVES

NOVEL CYCLIC AMINOPHENYLACETIC ACID DERIVATIVE, PRODUCTION THEROF, AND IMMUNE RESPONSE MODULATOR CONTAINING THE SAME AS ACTIVE INGREDIENT

The present invention provides novel cyclic amino-phenylacetic acid derivatives having modulating action on immune response, their optical isomers, their salts and their preparative processes, and therapeutic agents for autoimmune diseases containing them as effective ingredients, the cyclic aminophenylacetic acid derivatives being represented by a general formula (1)

VERFAHREN ZUR HERSTELLUNG NEUER VERBINDUNGEN.

Verfahren zur Herstellung von in a-Stellung substituierten Carbonylverbindungen

Verfahren zur Hemmung des Wachstums und der Vermehrung von schädlichen Mikroorganismen, Nematoden und Insekten und Anwendung desselben

Substd phenylacetic acid cpds - with anti-inflammatory analgesic and anti-pyretic activity

Substd. phenylacetic acids have the formula (I): (where R1 is 5-7C cycloalkyl, lower alkyl substd. cycloalkyl, 1-8C alkyl, phenyl, opt. substd. by trifluoromethyl, hal, lower alkylsulphonyl, nitro or cyano; R2 is hal, nitro, cyano, trifluoromethyl, lower alkyl sulphonyl, and when R1 is a substd. phenyl, R2 is H; R3 is H, and R1 is a substnt. other than cyclohexyl, R3 is lower alkyl; X is hal, mercapto, lower alkylthio, lower alkylsulphonyl, thiocyano, cyano, -SO3M (M is substantially nontoxic alkali metal), -S2O3M, lower alkanoylthio, lower alkylxanthyl, isothioureido, amino, mono- and di-(lower alkyl)amino, lower alkanoylamino, substnt. having the formula: where Z is bond or S; Y is hydroxy, amino -N-R" (R' and R" are H, lower alkyl, and aralkyl, or R' and R" form a hetero ring with the N to which they are attached); and X and Y may form a hetero ring of formula:-.

KARBAMOILOKSIPROIZVODNYE MUTILIN AND THEIR USE AS ANTIBACTERIAL AGENTS

ТРИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, ОБЛАДАЮЩИЕ АКТИВНОСТЬЮ В ОТНОШЕНИИ ИНТЕГРИНОВ, В ЧАСТНОСТИ В ОТНОШЕНИИ ИНТЕГРИНА АЛЬФАvБЕТА 3, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ, ИСПОЛЬЗУЕМЫЕ В ЭТОМ СПОСОБЕ, ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МЕДИКАМЕНТОВ И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

... 1. Соединения общей формулы (I) в которой R1обозначает группу -О-[А]-[В]-COR6, в которой R6обозначает -ОН, C1-С6алкокси, -О-СН2-СН(ОН)-СН2OН, [A] обозначает группу C1-С6алкилен, возможно замещенный оксогруппой, [B] обозначает радикал -CH(Z)- или простую связь, Z обозначает группу -NHCO2Rc, или -NHSO2Rc, где Rcобозначает радикал фенил(C1-С4)алкил-, хинолинил или пиридинилимидазолил(C1-С4)алкил-, R2и R3, одинаковые или разные, обозначают атом водорода, радикал гидроксил, радикал C1-С6алкокси или R2и R3образуют вместе группу -O-(C1-С3-алкилен)-O- или -O-C(Ph)2-O, G обозначает радикал -NH-C-(=X)-NH2, в котором Х обозначает S, О или NH, или радикал -NH-Het', где Het' обозначает имидазол, возможно замещенный группой оксо, пиримидин, диазепин или бензимидазол формул где р равно 2, 3 или 4, пунктирные линии представляют собой возможную вторую связь, а также соли присоединения с кислотами и основаниями и сложные эфиры, R1, R2и R3могут находиться в положении 8, 9 или 10 трицикла. 2. Соединения общей ...

INHIBITORS OF BETA-SECRETASE

Tricyclic Compounds Having Activity Specific for Integring, Particularly , avB3 Integrins, Method for Preparation the Same as Drugs and Pharmaceutical Composition Containing Same

Preparation of substituted acids from lactones

Thiocyano-fatty acid esters

Verfahren zur Herstellung von Carbonylverbindungen

New thiocyanate compounds

The invention comprises thiocyanato compounds of quinones of the benzene or naphthalene series, and their preparation by reacting such quinones, containing replaceable halogen atoms or alkoxy groups, with a salt of thiocyanic acid. Examples describe the preparation of 2,3-dithiocyanato-1,4-naphthoquinone, 2,3 - dithiocyanato - tetrachloro - 1,4 - naphthoquinone, 2,3 - dithiocyanato - 1,4 - naphthoquinone - 5 - carboxylic acid, 2 - amino - 3 - thiocyanato - 1,4 - naphthoquinone, monochloro- and monohydroxy-trithiocyanato-benzoquinone and the sodium salt of 2,3-dithiocyanato - 1,4 - naphthoquinone - 5 - sulphonic acid. Tetramethoxy - benzoquinone is prepared by heating chloranil in methanolic sodium methoxide.

2-METHYL-3-RHODANIDO-PROPIONSÄURE AND PROCEDURE FOR YOUR PRODUCTION

TRIZYCLI CONNECTIONS WITH EFFECT ON INTEGRINE, PARTICULARLY ON THE ALPHAVBETA3-INTEGRIN, PROCEDURE FOR YOUR PRODUCTION AND INTERMEDIATE PRODUCTS OF THE PROCEDURE, YOUR USE AS DRUGS AND IT ABSTENTION PHARMACEUTICAL COMPOSITIONS

NEW CYCLI AMINOPHENYLESSIGSÄUREDERIVATE, YOUR PRODUCTION AND IMMUNOMODULATOREN, WHICH THESE AS AN ACTIVE COMPONENT CONTAINING

Inhibitors of beta-secretase

... 1: \dar\Interwoven\NRPortbl\DCC\DAR766525_l.docx-28 09/2017 Abstract The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the p-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of p-amyloid aggregates.

Inhibitors of beta-secretase

... 1: \dar\Interwoven\NRPortbl\DCC\DAR766525_l.docx-28 09/2017 Abstract The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the p-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of p-amyloid aggregates.

INHIBITORS OF BETA-SECRETASE

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ß-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ß-amyloid aggregates.

AZABICYCLIC CARBAMOYLOXY MUTILIN DERIVATIVES FOR ANTIBACTERIAL USE

Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof, in which R1 is vinyl or ethyl; and R2 is a group R3, R4CH2-, or R5R6C=CH-; wherein each of R3 and R4 is an azabicyclic ring system or R5 and R6 together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

INHIBITORS OF BETA-SECRETASE

Improvements with composed of the beta-substituted carboxylic acids and their methods of preparation

NEW COMPOSE TRICYCLIC, THEIR METHOD OF PREPARATION, AND THEM INTERMEDIARIES OF THIS PROCESS, THEIR APPLICATION AS DRUGS AND THE COMPOSITIONS PHARMACEUTICAL CONTAINING THEM

Compounds of formula (I), wherein R1, R2, R3, R4, R5 and G are as defined in the description and the dotted lines indicate an optional second bond, as well as the acid, base and ester addition salts thereof, a method for preparing said compounds, intermediates therefor, the use of said compounds as drugs, and pharmaceutical compositions containing same, are disclosed.

CYCLIC AMINOPHENYLACETIC ACID DERIVATIVES, METHOD AND INTERMEDIATES FOR THEIR PRODUCTION AND PHARMACEUTICAL PREPARATIONS BASED ON THEM

Sú opísané deriváty kyseliny aminofenyloctovej všeobecného vzorca (I), ich optické izoméry a soli. Ďalej sú opísané spôsoby a medziprodukty na ich výrobu a farmaceutické prostriedky na ich báze. Tieto zlúčeniny vykazujú modulačný účinok na imunologickú reakciu, a preto sa môžu používať na liečbu autoimunitných chorôb.ŕ

THIOCYANO SUBSTITUTED ACRYLATES AND PROPIONATES AND THEIR USE AS PESTICIDES

СПОСОБ ПОЛУЧЕНИЯ α-ТИОЦИАНИРОВАННЫХ ПРОИЗВОДНЫХ β-ДИКАРБОНИЛЬНЫХ СОЕДИНЕНИЙ

Изобретение относится к способу получения α-тиоцианированных производных β-дикарбонильных соединений общей формулы I, где R = алкил С1-С6, незамещенный или замещенный бензил, аллил, (CH)COOEt, (CH)CN; Rи R=СНили OEt либо R+R=(CH), которые могут найти применение в качестве лекарственных препаратов (противораковых, антиастматических, болеутоляющих, противовоспалительных, жаропонижающих) и пестицидов. Способ заключается в том, что α-замещенные β-дикарбонильные соединения общей формулы II, где R, Rи Rимеют вышеуказанные значения, подвергают взаимодействию с тиоцианатом натрия в присутствии церий(IV) аммоний нитрата. Процесс проводят в среде органического растворителя при температуре 20-25°C и мольном соотношении α-замещенное β-дикарбонильное соединение:тиоцианат натрия:церий(IV) аммоний нитрат, равном 1:2-4:2-4, соответственно. Предлагаемый способ позволяет повысить выход целевых продуктов до 80-98%, сократить время проведения процесса, отказаться от высокотоксичных реагентов и дополнительных ...

Process for the manufacture of ortho-cyanaryl-thioglycollic acids and intermediate products

... 306,575. Carpmael, A., (I. G. Farbenindustrie Akt.-Ges.). Nov, 18, 1927. o-Cyanosulphocyano, o-cyanomercapto- and ocyanothioglycollic-aryl derivatives.-An o-aminoarylsulphocyano compound in which the p-posiÀ tion to the amino group is occupied or forms part of a further ring, and which may be prepared according to Specifications 257,619 and 303,813, is diazotized and subjected to Sandmeyer's reaction in order to replace the amino group by a cyano group. The sulpho cyano group is then saponified by means of alkali and the resulting mercapto group finally coupled with chloracetic acid in order to give an o-cyanoarylthioglycollic acid. In examples, 1-methyl-2-amino-3-sulphocyano-5-chlorbenzene, 1-amino-2-sulphocyano-4- ethoxybenzene and 2-amino-1-sulphocyanonaphthalene are used as starting materials, 1-methyl- 2-cyano-5-chlorbenzene-3-thioglycollic acid, 1- ,C,yano-4-ethoxyber.zeiie-2-thiogiyeollic, acid and 2- cyanonaphthalene-1-thioglycollic acid being respectively produced. Specification ...

AZABICYCLIACHE CARBAMOYLOXY MUTILIN OF DERIVATIVES AS ANTIBACTERIAL MEANS

Improvements with composed of the carboxylic acids béta substituted and with their methods of preparation

A process for producing alpha-substituted carbonyl compounds

NAPHTHYLALKANOIC ACIDS AND THEIR DERIVATIVES

Cephalosporin derivatives

New 7-[4-hydroxy-3-(substituted methyl)phenyl]acetamido cephalosporin derivatives are prepared which are useful as antibiotics.

Improvements in or relating to the preparation of halogenated benzonitriles and derivatives thereof

The invention comprises 2-halo-6-thiocyano-, -iodo-, -diazoborofluoro- and -fluoro-benzonitriles and a process for the preparation of substituted benzonitriles of the general formula wherein X represents a halogen atom and Y represents a halogen atom, the diazoborofluoride group N2BF4 or the thiocyano group which comprises treating an aniline derivative of the general formula wherein X represents a halogen atom, in solution or suspension in an acid medium, with a diazotising agent and reacting the resulting diazonium salt (a) with concentrated hydrogen fluoride, chloride, bromide or iodide solution to give the corresponding fluoro, chloro, bromo or iodo derivatives, or (b) with a solution of cuprous chloride in hydrochloric acid or cuprous bromide in hydrobromic acid with warming according to Sandemeyer's method, to give the corresponding chloro or bromo derivative, or (c) in the form of the diazonium chloride or bromide with copper bronze ...

Improvements in or relating to beta-substituted carboxylic acid compounds and methodof preparing same

In the reaction between a saturated aliphatic b -lactone and an inorganic salt in a polar solvent reaction medium to give salts of b -substituted carboxylic acids if excess lactone is present, b -substituted polyacyloxy-carboxylic acid salts are obtained which may be converted to the corresponding free acid on treatment with acid of Specification 635,347. For details of salts and lactones employed (see Group IV (b)). Specification 639,679, [Group IV (b)] also is referred to. The Specification as open to inspection under Sect. 91 is not restricted to the use of saturated aliphatic lactones but also specifies aromatic and unsaturated aliphatic lactones which may be substituted with groups containing halogens, nitrogen, oxygen or sulphur. This subject-matter does not appear in the Specification as accepted.ALSO:Salts of b -substituted carboxylic acids are obtained by reacting b -lactones of the general formula where R1, R2, R3 and R4 may be hydrogen or alkyl groups, ...

2-METHYL-3-RHODANIDO-PROPIONSÄURE UND VERFAHREN ZU IHRER HERSTELLUNG

CARNAMOYLOXY DERIVATIVES OF MUTILIN AND THEIR USE AS ANTIBACTERIAL OF MEANS

Novel cyclic aminophenylacetic acid derivative, production thereof, and immune response modulator containing the same as active ingredient

Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use

NOVEL CYCLIC AMINOPHENYLACETIC ACID DERIVATIVE, PRODUCTION THEROF, AND IMMUNE RESPONSE MODULATOR CONTAINING THE SAME AS ACTIVE INGREDIENT

SUMMARY The present invention provides novel cyclic aminophenylacetic acid derivatives having modulating action on immune response, their optical isomers, their salts and their preparative processes, and therapeutic agents for autoimmune diseases containing them as effective ingredients, the cyclic aminophenylacetic acid derivatives being represented by a general formula (1) (1) ¢wherein R and R1 each independently denotes hydrogen atom or lower alkyl group having 1 to 3 carbon atoms, R2 denotes a phenyl group (which may be substituted with 1 to 3 groups of halogen atom, methoxy group or their combinations) or trifluoromethyl group, and X denotes a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, cyano group, thiocyano group, trimethylsilylethinyl group, phenyl group (which may be substituted with halogen atom, methoxy group, methyl group or their combinations), carbamoyl group, carboxyl group, lower alkoxycarbonyl group having ...

INSECTICIDAL PROCESS FOR THE COMPOSITE PREPARATION, COMPOSITIONS, JOB AND PROCESS FOR THE ACARIDEOS COMBAT

DERIVADOS DEL ACIDO ACRILICO Y FUNGICIDAS QUE CONTIENEN ESTOS COMPUESTOS.

FLUORINATED ALKYLTHIOCYANATE PROCESS

A process for the preparation of a thiocyanate of the Formula (II): Rf-Am-(CH2)n-SCN wherein Rf is a C2-C20 perfluoroalkyl radical, or a C5-C38 perfluoroalkyl radical having at least one ether oxygen atom; n is 1 to 3; m is 0 or 1; A is O, S, CO2, N(R1)R2, CON(R1)R2, SO2N(R1)R2 or (OCH2CHR3)aO; wherein a is 3 to about 15; R1 is H or alkyl radical of 1 to about 4 carbon atoms; R2 is C1-C12alkylene; and R3 is H or CH2Cl; said process comprising reacting a fluorinated iodide of the Formula (I): Rf-Am-(CH2)n-I wherein Rf, A, m and n are as defined above, with a thiocyanate salt M+(SCN)- wherein M is sodium or potassium, in the presence of a catalyst comprising a quaternary ammonium salt of the Formula (R4)3(R5)N+Y- wherein R4 is butyl; R5 is methyl or butyl; and Y is Cl, Br, I, or HSO4; to yield the fluorinated thiocyanate of Formula (II) as defined above is disclosed.

NOVEL CYCLIC AMINOPHENYLACETIC ACID DERIVATIVE, PRODUCTION THEREOF, AND IMMUNE RESPONSE MODULATOR CONTAINING THE SAME AS ACTIVE INGREDIENT

A novel cyclic aminophenylacetic acid derivative which has an immune response modulatory activity, represented by general formula (1), an optical isomer thereof and salts thereof, a process for producing the same, and a remedy for autoimmune diseases containing the same as an active ingredient. In Formula (1), R and R1 represent each independently hydrogen or C1 to C3 lower alkyl; R2 represents trifluoromethyl or phenyl which may be substituted by one to three groups selected among halogen, methoxy and combinations thereof; and X represents hydrogen, C1 to C3 lower alkyl, C1 to C3 lower alkoxy, cyano, thiocyano, trimethylsilylethynyl, phenyl which may be substituted by one to three groups selected among halogen, methoxy, methyl and combinations thereof, carbamoyl, carboxyl, C1 to C3 lower alkoxycarbonyl, acetyl, benzoyl, nitro, amino, C1 to C3 lower alkanoylamino, benzoylamino which may be substituted, phenylsulfonylamino which may be substituted, C1 to C3 lower alkylthio, C1 to C3 lower ...

ARYL VINYL ETHER DERIVATIVES AND THEIR USE AS HERBICIDES

L'invention concerne des dérivés d'arylvinyléther représentés par la formule générale (I). Pour les besoins de ladite formule, les substituants sont tels que définis dans l'invention. L'invention concerne en outre des compositions renfermant les dérivés considérés, ainsi que des procédés et des intermédiaires utilisés pour leur élaboration. L'invention concerne enfin un procédé permettant d'éliminer les mauvaises herbes en utilisant ce type de composition.

Inhibitors of beta-secretase

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of theβ-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.

Preparation of 2-amino-4-alkoxythiazoles being negatively substituted in the 5 position

According to the present invention, 2-amino-4-alkoxythiazoles substituted with an electron withdrawing group in the 5-position are prepared by reacting an iminoether with a halogenating agent and thiourea. Alternatively, the 2-amino-4-alkoxythiazoles are prepared by reacting an iminoether with sodium thiocyanate and an oxidizing agent. According to a further aspect of the invention, novel azo dyes are prepared from such 2-amino-4-alkoxythiazoles having a phosphonyl group in the 5 position.

САЖА

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2004 124 019 (13) A (51) ÌÏÊ C09C 1/00 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2004124019/15, 09.08.2004 (71) Çà âèòåëü(è): ÄÅÃÓÑÑÀ Àà (DE) (30) Ïðèîðèòåò: 08.08.2003 DE 10336575.3 (43) Äàòà ïóáëèêàöèè çà âêè: 27.01.2006 Áþë. ¹ 03 R U Ôîðìóëà èçîáðåòåíè 1. Ñàæà ñ îðãàíè÷åñêèìè ãðóïïàìè, îòëè÷àþùà ñ òåì, ÷òî îðãàíè÷åñêà ãðóïïà ñîäåðæèò òèîöèàíàòíóþ ãðóïïó. 2. Ñàæà ñ îðãàíè÷åñêèìè ãðóïïàìè ïî ï.1, îòëè÷àþùà ñ òåì, ÷òî îðãàíè÷åñêà ãðóïïà ïðåäñòàâë åò ñîáîé N-(4-òèîöèàíàòàëêèë)ñóêöèíèìèäíóþ, N-(4òèîöèàíàòàðèë)ñóêöèíèìèäíóþ, N-(4-òèîöèàíàòàëêèë)àìèäíóþ èëè N-(4òèîöèàíàòàðèë)àìèäíóþ ãðóïïó. 3. Ñàæà ñ îðãàíè÷åñêèìè ãðóïïàìè ïî ï.1, îòëè÷àþùà ñ òåì, ÷òî îðãàíè÷åñêà ãðóïïà ïðåäñòàâë åò ñîáîé N-(4-òèîöèàíàòîôåíèë)ñóêöèíèìèäíóþ èëè N-(4òèîöèàíàòîôåíèë)àìèäíóþ ãðóïïó. 4. Ñïîñîá ïîëó÷åíè ñàæè ïî ï.1, îòëè÷àþùèéñ òåì, ÷òî ñàæó ïîäâåðãàþò âçàèìîäåéñòâèþ ñ ñîäåðæàùèìè äâîéíóþ èëè òðîéíóþ óãëåðîä-óãëåðîäíóþ ñâ çü, êîòîðà íå âë åòñ êîìïîíåíòîì àðîìàòè÷åñêîé ñèñòåìû, îðãàíè÷åñêèìè ñîåäèíåíè ìè, äâîéíà èëè òðîéíà Ñ-Ñ-ñâ çü êîòîðûõ àêòèâèðîâàíà ïî ìåíüøåé ìåðå îäíèì çàìåñòèòåëåì, è îðãàíè÷åñêîå ñîåäèíåíèå ïðè ýòîì ñîäåðæèò ïî ìåíüøåé ìåðå îäíó òèîöèàíàòíóþ ãðóïïó. 5. Ñïîñîá ïîëó÷åíè ñàæè ïî ï.1, îòëè÷àþùèéñ òåì, ÷òî ñàæó ïîäâåðãàþò âçàèìîäåéñòâèþ ñ ñîîòâåòñòâóþùåé ñîëüþ äèàçîíè è ïðè ýòîì ñîëü äèàçîíè ñîäåðæèò òèîöèàíàòíóþ ãðóïïó. 6. Êàó÷óêîâà ñìåñü, îòëè÷àþùà ñ òåì, ÷òî îíà ñîäåðæèò êàó÷óê èëè ñìåñü êàó÷óêîâ è ñàæó ñ îðãàíè÷åñêèìè ãðóïïàìè ïî ï.1. 7. Êàó÷óêîâà ñìåñü ïî ï.6, îòëè÷àþùà ñ òåì, ÷òî ñàæó ñ îðãàíè÷åñêèìè ãðóïïàìè èñïîëüçóþò â êîëè÷åñòâå îò 10 äî 150 ìàñ.÷. â ïåðåñ÷åòå íà 100 ìàñ.÷. êàó÷óêà. 8. Ñïîñîá ïîëó÷åíè êàó÷óêîâîé ñìåñè ïî ï.6, îòëè÷àþùèéñ òåì, ÷òî êàó÷óê èëè ñìåñü êàó÷óêîâ è ñàæó ñ îðãàíè÷åñêèìè ãðóïïàìè ñîâìåñòíî ñìåøèâàþò â ñîîòâåòñòâóþùåì ñìåñèòåëüíîì óñòðîéñòâå. 9. Ïðèìåíåíèå êàó÷óêîâîé ñìåñè ïî ï.6 äë èçãîòîâëåíè ïíåâìàòè÷åñêèõ øèí, ...

CARNAMOYLOXY DERIVATE VON MUTILIN UND DEREN VERWENDUNG ALS ANTIBAKTERIELLES MITTELS

Thiocyano fatty acid esters of cyanhydrins of methyl alkyl ketones and insecticidal compositions containing the same

The invention comprises compounds of the formula where the "Alkyl" group has 1-5 carbon atoms and n is 1-5. These are made by reacting a halo-fatty acid halide with the cyanhydrin of a methyl alkyl ketone in the presence of pyridine and an inert solvent, and treating the resulting halo ester with potassium or ammonium thiocyanate. The acid halide may be replaced by the acid itself or other reactive derivative. The preparation of the chloracetyl and thiocyanoacetyl esters of acetone cyanhydrin is exemplified. Other specified reactants are a - and b -halopropionic and a -halobutyric acid halides and the cyanhydrins of methyl ethyl ketone, methyl n-propyl ketone, methyl isopropyl ketone, methyl n-butyl ketone, methyl isobutyl ketone and methyl n-amyl ketone.ALSO:Compounds of the formula where the alkyl group has 1-5 carbon atoms and n is 1-5 are used as insecticides, admixed with solid, pasty or liquid carriers to form powders, emulsions or sprays ...

Biocidal 1-thiocyanato-Napthalene derivatives

1-Thiocyanato-8-substituted naphthalene compounds, useful as biocides, especially for protecting aqueous media against infection by microorganisms, have the formula <IMAGE> wherein R is an optionally substituted alkyl, alkoxy, aryl or aryloxy group, a hydroxyl, halo, nitro, cyano, sulphonic acid or primary, secondary or tertiary amino radical or an optionally substituted carbamoyl or sulphamoyl group, and wherein the naphthalene nucleus may contain further substituents and may be fused to a further ring.

Aryl vinyl ether derivatives and their use as herbicides

AND PROCES

CHELATES FOR THE CONTROL OF METAL-DEFICIENCY-PHENOMENA IN BIOLOGICAL SYSTEMS

CHELATES FOR THE CONTROL OF METAL-DEFICIENCY-PHENOMENA IN BIOLOGICAL SYSTEMS

INHIBITORS OF BETA-SECRETASE

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ß-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ß-amyloid aggregates.

NOUVEAUX DERIVES DE CEPHALOSPORINE UTILES COMME ANTIBIOTIQUES ET PROCEDES DE LEUR PREPARATION

L'INVENTION CONCERNE DES DERIVES DE CEPHALOSPORINE ET DES PROCEDES DE LEUR PREPARATION. LES COMPOSES DE L'INVENTION SONT DES HYDROXY-4 (METHYL SUBSTITUE)-3 PHENYLACETAMIDO-7 CEPHALOSPORINES REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) OU LES SYMBOLES SONT DEFINIS, ET LEURS SELS CONVENANT EN PHARMACIE; DES PROCEDES DE PREPARATION DE CES COMPOSES SONT EGALEMENT DECRITS. LES COMPOSES DE L'INVENTION SONT DES MEDICAMENTS UTILES NOTAMMENT COMME ANTIBIOTIQUES ACTIFS CONTRE LES BACTERIES A GRAM POSITIF ET A GRAM NEGATIF.

RUTHENIUM-CATALYZED PRODUCTION OF CYCLIC SULFATES

A ruthenium catalyzed method to synthesize cyclic sulfate compounds from the corresponding cyclic sulfites, and the cyclic sulfate reaction products obtained by this method. These cyclic sulfates further react with selected nucleophiles to give various substituted products. The method is an efficient means for the synthesis of chiral building blocks from tartaric acid enantiomers in high yields using an overall two-stage, one-pot reaction procedure. The chiral compounds can be transformed by nucleophilic reactions into chiral building blocks useful for the synthesis of natural biologically active products, such as antibiotics and pheromones.

Состав для предупреждения и устранения дефицита металлов в растениях

Fluorinated alkylthiocyanate process

TRICYCLIC COMPOUNDS HAVING ACTIVITY SPECIFIC FOR INTEGRINS, PARTICULARLY .ALPHA.V.BETA.3 INTEGRINS, METHOD FOR PREPARING SAME, INTERMEDIATES THEREFOR, USE OF SAID COMPOUNDS AS DRUGS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Compounds of formula (I), wherein R¿1?, R¿2?, R¿3?, R¿4?, R¿5? and G are as defined in the description and the dotted lines indicate an optional second bond, as well as the acid, base and ester addition salts thereof, a method for preparing said compounds, intermediates therefor, the use of said compounds as drugs, and pharmaceutical compositions containing same, are disclosed.

FLUORINATED ALKYLTHIOCYANATE PROCESS

A process for the preparation of a thiocyanate of the Formula (II): Rf-Am- (CH2)n-SCN wherein Rf is a C2-C20 perfluoroalkyl radical, or a C5-C38 perfluoroalkyl radical having at least one ether oxygen atom; n is 1 to 3; m is 0 or 1; A is O, S, CO2, N(R1)R2, CON(R1)R2, SO2N(R1)R2 or (OCH2CHR3)aO; wherein a is 3 to about 15; R1 is H or alkyl radical of 1 to about 4 carbon atoms; R2 is C1-C12alkylene; and R3 is H or CH2Cl; said process comprising reacting a fluorinated iodide of the Formula (I): Rf-Am-(CH2)n-I wherein Rf, A, m and n are as defined above, with a thiocyanate salt M+(SCN)- wherein M is sodium or potassium, in the presence of a catalyst comprising a quaternary ammonium salt of the Formula (R4)3(R5)N+Y- wherein R4 is butyl; R5 is methyl or butyl; and Y is Cl, Br, I, or HSO4; to yield the fluorinated thiocyanate of Formula (II) as defined above is disclosed.

AZABICYCLIC CARBAMOYLOXY MUTILIN DERIVATIVES FOR ANTIBACTERIAL USE

PURPOSE: The present invention relates to novel compounds, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy. CONSTITUTION: Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof, in which R^1 is vinyl or ethyl; and R^2 is a group R^3, R^4CH2-, or R^5R^6C=CH-; wherein each of R^3 and R^4 is an azabicyclic ring system or R^5 and R^6 together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections. COPYRIGHT 2000 KIPO ...

ANTIBACTERIAL AGENTS

The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X=NH Y=CO, CS, -C(=N-CN) or X and Y together form an alkene, or C3-C5 cycloalkyl; R1 is -COOH; R2 is an electron withdrawing group; R4 is an optionally substituted aryl. The compounds of formula I are antibacterial agents that are useful for sterilization sanitation, antisepsis, and disinfection.

Verfahren zur Herstellung von in ªŠ- oder ª€-Stellung durch negative Atomgruppen substituierten, aliphatischen Carbonsaeuren

Novel compounds

CHELATES FOR THE CONTROL OF METAL-DEFICIENCY-PHENOMENA IN BIOLOGICAL SYSTEMS

NEW USEFUL DERIVATIVES OF CEPHALOSPORINE LIKE ANTIBIOTICS AND PROCESSES OF THEIR PREPARATION

L'INVENTION CONCERNE DES DERIVES DE CEPHALOSPORINE ET DES PROCEDES DE LEUR PREPARATION. LES COMPOSES DE L'INVENTION SONT DES HYDROXY-4 (METHYL SUBSTITUE)-3 PHENYLACETAMIDO-7 CEPHALOSPORINES REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) OU LES SYMBOLES SONT DEFINIS, ET LEURS SELS CONVENANT EN PHARMACIE; DES PROCEDES DE PREPARATION DE CES COMPOSES SONT EGALEMENT DECRITS. LES COMPOSES DE L'INVENTION SONT DES MEDICAMENTS UTILES NOTAMMENT COMME ANTIBIOTIQUES ACTIFS CONTRE LES BACTERIES A GRAM POSITIF ET A GRAM NEGATIF.

SUBSTITUTED 2?HALO?3?THIOCYANATOACRYLATES

CYCLIC AMINOPHENYLACETIC ACID DERIVATIVES WITH IMMUNOMODULATING ACTION, PROCESSES FOR PREPARATION AND SYNTHESIS INTERMEDIATES THEREOF

CARBAMOYLOXY DERIVATIVES OF MUTILINE AND THEIR USE AS ANTIBACTERIALS

TRICYCLIC COMPOUNDS HAVING ACTIVITY SPECIFIC FOR INTEGRINS, PARTICULARLY ALPHAvBETA3 INTEGRINS, METHOD FOR PREPARING SAME, INTERMEDIATES THEREFOR, USE OF SAID COMPOUNDS AS DRUGS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

AZABICYCLIC CARBAMOYLOXY MUTILIN DERIVATIVES FOR ANTIBACTERIAL USE

NEW CYCLIC AMINOPHENYLACETIC ACID DERIVATIVE, ITS PRODUCTION AND MODIFYING AGENT FOR IMMUNE RESPONSE CONTAINING THE SAME AS ACTIVE INGREDIENT

PURPOSE: To obtain a new compound, having modifying action on immune response and useful for chronic rheumataid arthritis, etc. CONSTITUTION: A compound expressed by formula I [R and R1 are H or 1-3C lower alkyl; R2 is halogen, methoxy, (substitute)phenyl or trifluoromethyl; X is H, 1-3C lower alkyl, 1-3C lower alkoxy, cyano, etc.], e.g. ethyl 2-(2- fluorophenyl)-1,2,3,4-tetrahydroquinoline-6-acetate. Furthermore, the compound expressed by formula I is obtained by hydrogenating a compound expressed by formula II (X1 is H, C1 or Br) and reacting the resultant compound with an alkylating agent. COPYRIGHT: (C)1993,JPO&Japio ...

Verfahren zur Herstellung von Carbonylverbindungen

INHIBITORS OF BETA-SECRETASE

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. 2. A compound according to or a pharmaceutically acceptable salt thereof for use as a medicament.3. A pharmaceutical composition comprising at least one compound according to or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier.4. A compound according to or a pharmaceutically acceptable salt thereof for use in the treatment of a BACE1 mediated disorder or disease.5. A compound or a pharmaceutically acceptable salt thereof for use according to claim 4 , wherein the BACE1 mediated disorder or disease is selected from the group consisting of a neurodegenerative disorder claim 4 , cognitive decline claim 4 , cognitive impairment claim 4 , dementia claim 4 , and disease characterized by the production of β-amyloid deposits or neurofibrillary tangles.6. A compound or a pharmaceutically acceptable salt thereof for use according to claim 5 , wherein the disorder or disease is selected from the group consisting of Alzheimer's disease claim 5 , Trisomy 21 (Down Syndrome) claim 5 , Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch-type (HCHWA-D) claim 5 , senile dementia claim 5 , cerebral amyloid angiopathy claim 5 , degenerative dementia claim 5 , dementias of mixed vascular and degenerative origin claim 5 , dementia associated with Parkinson's disease claim 5 , dementia associated with progressive supranuclear palsy claim 5 , dementia associated with cortical basal degeneration claim 5 , diffuse Lewy body type of Alzheimer's disease claim 5 , dry age related ...

Inhibitors of beta-secretase

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.

Inhibitors of beta-secretase

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.

INHIBITORS OF BETA-SECRETASE

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. 1. A compound having the following structure:or a pharmaceutically acceptable salt thereof. This application is a continuation of U.S. patent application Ser. No. 15/383,287, filed on Dec. 19, 2016, which is a continuation of U.S. patent application Ser. No. 14/613,550, filed on Feb. 4, 2015, now U.S. Pat. No. 9,526,727, which is a continuation of U.S. patent application Ser. No. 13/784,032, filed Mar. 4, 2013, now U.S. Pat. No. 8,981,112, which, in turn, claims the benefit of U.S. Provisional Application Ser. No. 61/606,786, filed Mar. 5, 2012; the entire contents of each of the aforementioned applications are incorporated herein by reference.The instant application contains a Sequence Listing which has been submitted in ASCII format via EFS-Web and is hereby incorporated by reference in its entirety. Said ASCII copy, created on Mar. 4, 2013, is named 15161953.txt and is 718 bytes in size.The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid deposits or neurofibrillary tangles.β-Amyloid (also referred to herein as “Abeta” or “Aβ”) deposits and neurofibrillary tangles are two major pathologic characterizations associated with Alzheimer's disease (AD), including the genetically linked early onset ...

NOVEL TRICYCLIC COMPOUNDS, THEIR PREPARATION PROCESS, AND INTERMEDIATES THEREOF, THEIR APPLICATION AS MEDICAMENTS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Antibacterial agents

The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X=NH Y=CO, CS, -C(=N-CN) or X and Y together form an alkene, or C3-C5 cycloalkyl; R1 is -COOH; R2 is an electron withdrawing group; R4 is an optionally substituted aryl. The compounds of formula I are antibacterial agents that are useful for sterilization sanitation, antisepsis, and disinfection.

N-PHENYLBENZAMIDES AND N-PHENYLBENZAMIDOXIMES, METHOD FOR THE PRODUCTION THEREOF, CONTAINERS THEREOF AND THEIR USE AS A PEST CONTROL

Intermediate for preparing tricyclic compound and preparing method thereof

本发明公开了式(I)化合物及其酸和碱加成盐和它们的酯，其中R 1 ，R 2 ，R 3 ，R 4 ，R 5 和G如说明书所定义且虚线表示任选的第二条键，本发明还公开了所述化合物的制备方法，此法的中间体，所述化合物作为药物的应用以及含有它们的药物组合物。

Tricyclic compounds having activity specific for integrins, particularly alphanubeta3 integrins, method for preparing same, intermediates therefor, use of said compounds as drugs, and pharmaceutical compositions containing same

The subject of the invention is the products of formula (I): in which R 1 , R 2 , R 3 , R 4 , R 5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.

Carbamoyloxy derivatives of mutiline and their use as antibacterials

Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Immune response modulator-active aminophenyl-acetic acid derivatives

Process for producing rhodanidoisobutyric acid

Carbamoyloxy derivatives of methiline and their use as antimicrobial agents

본 발명은 하기 화학식 (1A)의 화합물 또는 약제학적으로 허용되는 염, 및 이들의 유도체의 머틸린의 유도체에 관한 것이며, 이들은 박테리아 감염 치료에 유용하다. (화학식 1A) 상기 식에서, R은 에틸 또는 비닐이며, Y는 N-원자가 비치환되거나, 일치환 또는 이치환된 카르바모일옥시기이다.

Patent FR2147649A5

PROCESS FOR THE MANUFACTURE OF NAFTALENE 1-THIOCIANATE-8-SUBSTITUTED COMPOUNDS AND PROCESS TO PROTECT A MEDIUM THAT IS SUSTAINABLE FROM ATTACK BY MICRO-ORGANISMS AGAINST THIS ATTACK

PROCESS FOR THE PREPARATION OF IRON COMPLEXES OF ETHYLENDIAMINOTETRAACETIC ACID DERIVATIVES

Ethylenediaminetetraacetic acid derivatives,their salts and heavy metal chelates,their production and compositions for the control of metal-deficiency phenomena in biological plant systems

BETA-SECRETASI INHIBITORS

Inhibitors of beta-secretase

Jedinjenje predstavljeno strukturnom formulom izabranom između:ili njegova farmaceutski prihvatljiva so.Prijava sadrži još 13 patentnih zahteva. The compound represented by the structural formula selected from: or a pharmaceutically acceptable salt thereof. The application contains 13 further claims.

Antihypertensive compounds

Provided are antihypertensive compounds of the formula ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different, m is an integer from 0 to 2 inclusive, n is an integer from 0 to 4 inclusive, M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl. Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, and R 7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclic, ##STR2## wherein R is hydrogen, alkyl, or aryl, and where Y is hydroxy, their pharmaceutically acceptable, nontoxic alkali metal, alkaline earth metal, and amine salts.

Ortho-cyanarylsulphocyanogen compounds and process of making same

Inhibitors of beta-secretase

2-(Methyl)-3-(rhodanido)-propionic acid - which is intermediate for antihypertensive agent 1-(3'-(mercapto)-(2's)-pyrrolidine-(2s)-carboxylic acid

2-(methyl)-3-(rhodanido)-propionic acid of formula (I) is new. USE/ADVANTAGE - (i) (Esp. the S-enantiomer) is an intermediate in the prepn. of 1-(3'-(mercapto)-(2's)- (methyl)-propionyl)pyrrolidine-(2s)-carboxylic acid (captopril) which can be used to reduce blood pressure. The prepn. of captopril from L-proline using (I) gives yields of more than 50% (based on L-proline) compared to e.g. a previous process using 3-(ethanoylthio)-2-(methyl)propionic acid as acylating agent, which gave yields of only 10% (based on L-proline) other processes were little better, giving yields of 30% or 34-35%. The prepn. using (I) is simple. (I) is itself produced by a simple and economical process.

ACRYLIC ACID DERIVATIVES AND FUNGICIDES THAT CONTAIN THESE COMPOUNDS.

Thiocyano substituted acrylates and propionates and their use as pesticides

The new compounds 2-thiocyanoacrylates, 2-thiocyano-2,3-dibromopropionates, and 2-thiocyano-2,3-dichloropropionates, which are useful as pesticides, and methods of preparing the same are described.

Inhibitors of beta-secretase

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the �-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of �-amyloid aggregates.

Tricyclic compounds with integrine activity, in particular towards alpha vbeta 3 intergrines, method for their preparation and use as medicamentous forms and pharmaceutical compositions containing them

3-benzoyl-3-thiocyanatopropionic acid, alkyl esters and derivatives thereof

3-Benzoyl-3-thiocyanatopropionic acid, alkyl esters are prepared by the reaction of a 3-benzoyl-3-halopropionic acid alkyl ester with an alkali metal thiocyanate. The products so produced exhibit antitubercular activity.

Preparation method of 4-amino-5-ethylsulfonyl-2-methoxybenzoic acid

本发明公开了一种4‑氨基‑5‑乙基磺酰基‑2‑甲氧基苯甲酸的制备方法。该制备方法，包括甲基化、硫氰化、乙基化、氧化和水解反应五个步骤，最终制备得到4‑氨基‑5‑乙基磺酰基‑2‑甲氧基苯甲酸。本发明提出的制备方法能以温和的反应条件高效制备4‑氨基‑5‑乙基磺酰基‑2‑甲氧基苯甲酸，仅使用乙醇和水作为溶剂，具有操作简单、产率高、产品质量好、三废少、成本低等优势，便于规模化生产。

Cyanoalkene derivatives, method for their preparation and their use as microbiocides for protecting materials

New cyanoalkene derivatives of the formula (I) <IMAGE> in which R and R<1> have the meaning given in the description, and a method for their preparation, are described. The new cyanoalkene derivatives are used for controlling microorganisms for the protection of industrial materials.

Inhibitors of beta-secretase

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACEI) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.

Fluorinated alkyl thiocyanate process

(57)【要約】 式（ＩＩ）：Ｒ f −Ａ m −（ＣＨ 2 ） n −ＳＣＮ［式中、Ｒ f は、Ｃ 2 〜Ｃ 20 のパーフルオロアルキル基、または少なくとも１つのエーテル酸素原子を有するＣ 5 〜Ｃ 38 のパーフルオロアルキル基であり；ｎは、１〜３であり；ｍは、０または１であり；Ａは、Ｏ、Ｓ，ＣＯ 2 、Ｎ（Ｒ 1 ）Ｒ 2 、ＣＯＮ（Ｒ 1 ）Ｒ 2 、ＳＯ 2 Ｎ（Ｒ 1 ）Ｒ 2 または（ＯＣＨ 2 ＣＨＲ 3 ） a Ｏであり；ａは３から約１５であり；Ｒ 1 は、Ｈまたは１個から約４個の炭素原子を有するアルキル基であり；Ｒ 2 は、Ｃ 1 〜Ｃ 12 のアルキレンであり；およびＲ 3 は、ＨまたはＣＨ 2 Ｃｌである］のチオシアナートの調製のための方法であって、；その方法は、式（Ｉ）：Ｒ f −Ａ m −（ＣＨ 2 ） n −Ｉ［式中、Ｒ f ，Ａ、ｍおよびｎは、上記で定義したものである］のフッ素化されたヨージドを、Ｍがナトリウムまたはカリウムであるチオシアン酸塩Ｍ + （ＳＣＮ） - と、式（Ｒ 4 ） 3 （Ｒ 5 ）Ｎ + Ｙ - ［式中、Ｒ 4 はブチルであり；Ｒ 5 はメチルまたはブチルであり；ＹはＣｌ、Ｂｒ、ＩまたはＨＳＯ 4 である］の第４級アンモニウム塩を含む触媒の存在下で反応させて、上記で定義した式（ＩＩ）のフッ素化されたチオシアナートを与える方法を開示する。

Substituted alkanoic acids and their derivatives, and process

Fluorinated alkylthiocyanate process

公开了制备式(Ⅱ)R f －A m －(CH 2 ) n －SCN的硫氰酸酯的方法，其中，R f 为C 2 －C 20 全氟烷基，或具有至少一个醚氧原子的C 5 －C 38 全氟烷基，n为1到3；m为0或1；A为O、S、CO 2 、N(R 1 )R 2 、CON(R 1 )R 2 、SO 2 N(R 1 )R 2 或(OCH 2 CHR 3 ) a O；其中a为3至约15；R 1 为H或1至约4个碳原子的烷基；R 2 为C 1 －C 12 亚烷基；而R 3 为H或CH 2 Cl；该方法包括，将式(Ⅰ)的氟化的碘化物(式(Ⅰ)：R f －A m －(CH 2 ) n －Ⅰ，其中R f ，A，m和n如上定义)与硫氰酸盐M + (SCN) － (其中M为钠或钾)在含有式(R 4 ) 3 (R 5 )N + Y － (其中R 4 为丁基；R 5 为甲基或丁基；而Y为Cl、Br、Ⅰ或HSO 4 － )的季铵盐的催化剂存在下反应，生成如上定义的式(Ⅱ)的氟化的硫氰酸酯。

Inhibitors of beta-secretase.

Acilguanidinas espirocíclicas; su uso como inhibidores de la actividad de la enzima ß-secretasa (BACE1); composiciones farmacéuticas que las comprenden; métodos para usarlas como agentes terapéuticos en el tratamiento de los trastornos neurodegenerativos, de los trastornos caracterizados por un deterioro cognitivo, de las alteraciones cognitivas, de la demencia y de las enfermedades que se caracterizan por la producción de agregados ß-amiloides.

Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use

Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof, in which R1 is vinyl or ethyl; and R2 is a group R3, R4CH2-, or R5R6C=CH-; wherein each of R?3 and R4¿ is an azabicyclic ring system or R?5 and R6¿ together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

Carbamoyloxy derivatives of mutiline and their use as antibacterials

Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R 1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Fluorinated alkylthiocyanate process

Tricyclic compounds having activity specific for integrins, particularly alpha v beta 3 integrins, method for preparing same

本发明公开了式(Ⅰ)化合物及其酸和碱加成盐和它们的酯,其中R 1 ,R 2 ,R 3 ,R 4 ,R 5 和G如说明书所定义且虚线表示任选的第二条键,本发明还公开了所述化合物的制备方法,此法的中间体,所述化合物作为药物的应用以及含有它们的药物组合物。

Inhibitors of beta-secretase

Novel tricyclic compounds, process for the preparation and intermediates thereof, the application thereof as medicaments ans pharmaceutical preparations containing them

Tetrahydroquinoline acetic acid derivatives, pharmaceutical compositions containing these compounds as an activ ingredient and process for preparing the activ ingredients and the pharmaceutical compositions

A találmány tárgya új tetrahidrokinolinil-ecetsav-származékok, ezekoptikai izomerjei, sói, valamint hatóanyagként ilyen vegyületekettartalmazó gyógyszerkészítmények előállítási eljárására vonatkozik. Azúj vegyületeket az (1) ál- talános képlettel írják le, amely képletbenR és R1 jelentése egymástól függetlenül hidrogénatom vagy 1–3szénatomos alkilcsoport, R2 jelentése trifluor-metil-csoport, vagyadott esetben halogénatommal vagy metoxicsoporttal szubsztituáltfenilcsoport, X jelentése hidrogén- vagy halogénatom, 1–3 szénatomosalkil-, 1–3 szénatomos alkoxi-, ciano-, fenil-, karbamoil-, karboxil-,acetil-, benzoil-, nitro-, amino-, 1–3 szénatomos alkil-tio-, 1–3szénatomos alkil-szulfinil-, 1–3 szén- atomos alkil-szulfonil-csoport.A fenti (1) általános képletű vegyületek rheumaellenes hatásúak, ésalkalmasak autoimmun betegségek kezelésére is. ŕ The present invention relates to novel tetrahydroquinolinylacetic acid derivatives, their optical isomers, their salts and to processes for the preparation of such compounds as active ingredients. The novel compounds are represented by the general formula (1) wherein R and R 1 are independently hydrogen or C 1-3 alkyl, R 2 is trifluoromethyl or optionally substituted phenyl by halogen or methoxy, X is hydrogen or halogen, -C3 alkyl, C 1-3 alkoxy, cyano, phenyl, carbamoyl, carboxyl, acetyl, benzoyl, nitro, amino, C 1-3 alkylthio, C 1-3 alkyl- sulfinyl, C 1-3 alkylsulfonyl. The compounds of formula (I) above have anti-rheumatic activity and are also useful in the treatment of autoimmune diseases. ŕ

Method for producing organic compound by substituted halogen atoms

Carbamoyloxy derivatives of mutiline and their use as antibacterials

Carbon black

본 발명은 유기 그룹을 갖고, 유기 그룹이 티오시아네이트 그룹을 함유하는 카본 블랙에 관한 것이다. The present invention relates to carbon black having an organic group, wherein the organic group contains a thiocyanate group. 또한, 본 발명에 따르는 카본 블랙의 제조방법이 기술되며, 카본 블랙을 C-C 이중 또는 삼중 결합이 하나 이상의 치환체에 의해 활성화되는 방향족 시스템의 일부가 아닌 C-C 이중 또는 삼중 결합을 함유하는 유기 화합물과 반응시키며, 유기 화합물은 하나 이상의 티오시아네이트 그룹을 함유한다. Also described is a process for the preparation of carbon black according to the invention, wherein the carbon black is reacted with an organic compound containing CC double or triple bonds which is not part of an aromatic system in which the CC double or triple bonds are activated by one or more substituents. The organic compound contains at least one thiocyanate group. 본 발명에 따르는 카본 블랙은 고무 화합물에 사용될 수 있다. Carbon blacks according to the invention can be used in rubber compounds. 카본 블랙, 유기 그룹, 티오시아네이트 그룹, 고무 화합물 Carbon black, organic group, thiocyanate group, rubber compound

Novel cyclic aminophenylacetic acid derivative, production thereof, and immune response modulator containing the same as active ingredient

Disclosed are aminophenylacetic acid derivatives of general formula (I), their optical isomers and salts. Disclosed are also methods and intermediates for their production and pharmaceutical preparations based on them. These compounds have an immune response modulatory activity, hence they may be used for treatment of autoimmune diseases.

CHELATES FOR THE COMBINATION OF METAL DEFICIENCY IN BIOLOGICAL SYSTEMS

Inhibitors of beta-secretase

Disclosed are spiro cyclic acylguanidines compounds and their use as inhibitors of the B-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of B-amyloid aggregates.

BETA-SECRETASE INHIBITORS

SE REFIERE A COMPUESTOS DERIVADOS DE ACILGUANIDINAS ESPIROCICLICAS DE FORMULA (i), (ii), ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE LA ENZIMA BETA-SECRETASA (BACE1) SIENDO UTILES EN EL TRATAMIENTO DE ENFERMEDADES QUE SE CARACTERIZAN POR LA PRODUCCION DE DEPOSITOS B-AMILOIDES O DE HACES NEUROFIBRILARES TALES COMO LA ENFERMEDAD DE ALZHEIMER, EL SINDROME DE DOWN, DEMENCIA SENIL, ANGIOPATIA AMILOIDE CEREBRAL REFERS TO COMPOUNDS DERIVED FROM SPIRO CYCLIC ACILGUANIDINS OF FORMULA (i), (ii), AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF THE ACTIVITY OF THE BETA-SECRETASE (BACE1) ENZYME, BEING USEFUL IN THE TREATMENT OF DISEASES THAT ARE CHARACTERIZED BY THE PRODUCTION OF B-AMYLOID DEPOSITS OR OF NEUROFIBRILLARY BACES OF ALZHERMEDOME, SUCH AS ILLNESS. SENILE DEMENTIA, CEREBRAL AMYLOID ANGIOPATIA

Multiline derivatives of carbamoyl azabicycles for antibacterial use

신규한 항생활성 화합물 및 그 화합물을 포함하는 항생 조성물

본 발명은 신규한 항생활성 화합물 및 그 화합물을 포함하는 항생 조성물에 관한 것으로 더욱 상세하게는 미생물 단백질 합성을 저해하는 화합물 및 그 화합물의 용도에 관한 것이다.

Új triciklusos vegyületek, eljárás előállításukra, az eljárás intermedierjei, továbbá gyógyszerkészítmények

A találmány tárgyát az új (I) általánős képletű gyógyászati hatásúvegyületek, valamint e vegyületeknek savakkal és bázisőkkal képzettaddíciós sói, valamint észterei képezik. Az (I) általánős képletben aszűbsztitűensek jelentése többek között az alábbi: R1 jelentése -C=C-[A]-[B]-COR6, -CH=CH-[A]-[B]-COR6, -(CH2)2 -[A]-[B]-COR6, -O-[A]-[B]-COR6, -CH2CO-[A]-[B]-COR6 csőpőrt, ahől a képletekben -[A]- jelentése- szénhidrőgéncsőpőrt, amely 1-12 szénatőmőt és adőtt esetben 1-6heterőatőmőt tartalmaz őxigénatőm, nitrőgénatőm vagy kénatőm közülválasztva, vagy - -[B]- jelentése fenilcsőpőrt, CH[Z] képletű csőpőrtvagy egyértékű vegyértékkötés, - Z jelentése hidrőgénatőm, valamelyalábbi csőpőrt; (D)0-6-NRaRb, (D)0-6-NH-SO2-Rc, (D)0-6-NH-CO2-Rc,(D)0-6-NH-CO-Rc, (D)0-6-NH-SO2-NH-Rc, (D)0-6-NH-CO-NH-Rc, (D)0-6-CO2-Rc, (D)0-6-SO2-Rc, (D)0-6-CO-Rc vagy (D)0-6-Rc, ahől a képletekben(D)0-6 jelentése gyűrűs 0-6 szénatőmős szénhidrőgéncsőpőrt Ra, Rb ésRc jelentése hidrőgénatőm, (CH2)0-3-Ar képletű csőpőrt, amelyben Arjelentése többek között 6-18 szénatőmős karbőciklűsős arilcsőpőrt,(CH2)0-3-Het csőpőrt, - R6 jelentése hidrőxilcsőpőrt, O-Alk, O-Ar,NH2, NH-Alk, N(Alk)2 képletű csőpőrt, vagy egy L vagy D aminősavmaradéka, - R2 és R3 jelentése azőnős vagy eltérő, így hidrőgénatőm,hidrőxilcsőpőrt, O-Alk vagy O-(CH2)0-3-Ar csőpőrt, vagy R2 és R3együttes jelentése egy -O-(CRdRe)n- típűsú gyűrű, ahől n értéke 1, 2,3, 4 vagy 5, Rd és Re jelentése hidrőgénatőm, 1-6 szénatőmősalkilcsőpőrt vagy fenilcsőpőrt, - R4 jelentése többek közötthidrőgénatőm, halőgénatőm vagy hidrőxil-, aminő-, nitrő-, cianő-, CF3,1-12 szénatőmős acilcsőpőrt - R5 jelentése hidrőgénatőm,hidrőxilcsőpőrt, halőgénatőm, O-Alk csőpőrt vagy O-(CH2)0-3-Arcsőpőrt, - G jelentése többek között adőtt esetben N-tartalmú és/vagySO2 tartalmú csőpőrt. A találmány tárgyáhőz tartőznak e vegyületekettartalmazó gyógyászati készítmények, valamint a (IIIa), (IIIb), (IIIc)és (II) képletű vegyületek is, azzal a megkötéssel, hőgy e vegyületekköréből ...

Tricyclic compounds, method for preparing same, intermediates therefor, and pharmaceutical compositions

Carbamoyloxy derivatives of mutiline with antibacterial activity, pharmaceutical compns. contg. them and process for preparing the said compds.

Neue cyclische aminophenylessigsäurederivate, ihre herstellung und immunomodulatoren , welche diese als aktiven bestandteil enthalten

Antibakteriális hatású mutilin-karbamoil-oxi-származékok, ezeket tartalmazó gyógyszerkészítmények és eljárás a vegyületek előállítására

A jelen találmány új (3) általánős képletű vegyületekre, azőkelőállítására alkalmas eljárásőkra, és a vegyületeket tartalmazógyógyászati készítményekre vőnatkőzik. A vegyületek antibakteriálisterápiában alkalmazhatók. A (3) általánős képletben R1 jelentése vinil- vagy etilcsőpőrt; R2 és R3 jelentése hidrőgénatőm, adőtt esetben helyettesített 1-6szénatőmős nyílt láncú, 3-8 szénatőmős gyűrűs szénhidrőgéncsőpőrt,adőtt esetben helyettesített heterőgyűrűs vagy arilcsőpőrt, vagy R2 ésR3 együtt egy adőtt esetben helyettesített 3-8 gyűrűatőmős gyűrűscsőpőrtőt alkőt, amely adőtt esetben tővábbi heterőatőmőt tartalmaz ésadőtt esetben karbőciklűsős vagy heterőciklűsős gyűrűvel kőndenzált,vagy R2 jelentése a fenti egy vegyértékű csőpőrtők egyike és R3 jelentése -SO2R4, -COR5, -OR5 vagy -NR6R7 általánős képletűcsőpőrt, amelyekben R4 jelentése adőtt esetben helyettesített 1-6 szénatőmős nyílt láncú,3-8 szénatőmős, gyűrűs szénhidrőgéncsőpőrt, heterőgyűrűs csőpőrt,arilcsőpőrt, 1-6 szénatőmős alkil-aminő-csőpőrt vagy aril-aminőcsőpőrt; R5 jelentése hidrőgénatőm, adőtt esetben helyettesített 1-6 szénatőmősnyílt láncú, 3-8 szénatőmős, gyűrűs szénhidrőgéncsőpőrt, heterőgyűrűscsőpőrt vagy arilcsőpőrt; R6 és R7 jelentése hidrőgénatőm, 1-6 szénatőmős nyílt láncú, 3-8szénatőmős gyűrűs szénhidrőgén-csőpőrt, heterőgyűrűs csőpőrt,arilcsőpőrt, vagy R6 és R7 együtt egy adőtt esetben helyettesített 3-8 gyűrűatőmősgyűrűs csőpőrtőt alkőt, amely adőtt esetben tővábbi heterőatőmőttartalmaz, és adőtt esetben szénhidrőgéngyűrűvel, heterőgyűrűs vagyarőmás csőpőrttal kőndenzált. ŕ

Verfahren zur Herstellung von Carbonylverbindungen

Carnamoyloxy derivate von mutilin und deren verwendung als antibakterielles mittels

Trizyclische verbindungen mit wirkung auf integrine, besonders auf das alphavbeta3-integrin,verfahren zur ihrer herstellung und zwischenprodukte des verfahrens, ihre verwendung als arzneimittel und sie enthaltende pharmazeutische zusammensetzungen

Azabicycliache carbamoyloxy mutilin derivate als antibakterielles mittel

Preparation of 2-amino-4-alkoxythiazoles being negatively substituted in the 5 position

PREPARATION OF 2-AMINO-4-ALKOXYTHIAZOLES BEING NEGATIVELY SUBSTITUTED IN THE 5 POSITION According to the present invention, 2-amino-4-alkoxythiazoles substituted with an electron withdrawing group in the 5-position are prepared by reacting an iminoether with a halogenating agent and thiourea. Alternatively, the 2-amino-4-alkoxythiazoles are prepared by reacting an iminoether with sodium thiocyanate and an oxidizing agent. According to a further aspect of the invention, novel azo dyes are prepared from such 2-amino-4-alkoxythiazoles having a phosphonyl group in the 5 position.

신규한 항생활성 화합물 및 그 화합물을 포함하는 항생 조성물

본 발명은 신규한 항생활성 화합물 및 그 화합물을 포함하는 항생 조성물에 관한 것으로 더욱 상세하게는 미생물 단백질 합성을 저해하는 화합물 및 그 화합물의 용도에 관한 것이다.

Senyawa terbaru

一种氨磺必利中间体的制备方法及氨磺必利的制备工艺

本发明公开了一种氨磺必利中间体的制备方法及氨磺必利的制备工艺，方法的步骤中含有：将4‑氨基‑2‑甲氧基苯甲酸甲酯、MSCN、甲醇依次加入反应瓶内，滴加过硫酸氢钾，以制备2‑甲氧基‑4‑氨基‑5‑硫氰基苯甲酸甲酯，即氨磺必利中间体；其中，MSCN中的M为Na、K、NH 4 中的一种。它制备快速高效、低成本、收率高且绿色环保。

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Nieuwe cefalosporinederivaten.

Terpene-cyanoacyl compound and method of producing same

Novel compounds

Nuevos compuestos

Se describe un procedimiento para preparar un compuesto de fórmula general (3) (figura 1) o una sal o derivado farmaceuticamente aceptable del mismo en la que R1 es vinilo o etilo; R2 y R3 son grupos iguales o diferentes seleccionados entre, por ejemplo, un grupo heterocíclico opcionalmente sustituido; R5 se selecciona, entre otras posibilidades, de un grupo heterocíclico opcionalmente sustituido. Como ejemplo no limitante: 14-(N-fenilcarbamato) de mutilina. Su uso es para el tratamiento de infecciones microbianas en animales, especialmente los seres humanos y en mamíferos domesticados. Los compuestos y composiciones de acuerdo con la invención pueden formularse para la administración por cualquier ruta, por ejemplo la oral, tópica o parenteral.

Derivados del 14-o-carbamoilo mutilina

SE REFIEREN A COMPUESTOS PREFERIDOS DE FORMULA (3), EN DONDE: R1 ES VINILO O ETILO; R2 Y R3 SON H, ALQUILO C1-C6, CICLOALQUILO C3-C8, HETEROCICLO, ARILO O CONJUNTAMENTE FORMAN UN CICLO DE 3 A 8 ESLABONES QUE CONTIENE ADEMAS UN N, O o S, Y QUE ESTA OPCIONALMENTE CONDENSADO CON UN ANILLO, O R3 ES SO2R4, COR5, OR5 Y NR6R7, EN DONDE: R4 ES ALQUILO C1-C6, CICLOALQUILO C3-C8, HETEROCICLO, ARILO, ALQUILAMINO C1-C6 O ARILAMINO; R5 ES H, ALQUILO C1-C6, CICLOALQUILO C3-C8, HETEROCICLO O ARILO; R6 Y R7 SON H, ALQUILO C1-C6, CICLOALQUILO C3-C8, HETEROCICLO Y ARILO, O CONJUNTAMENTE FORMAN UN CICLO DE 3 A 8 ESLABONES QUE PUEDE CONTENER UN N, O o S, Y QUE OPCIONALMENTE ESTA CONDENSADO CON UN ANILLO. TAMBIEN SE REFIERE AL PROCEDIMIENTO DE PREPARACION DE (3), QUE COMPRENDE: HACER REACCIONAR UN COMPUESTO (4) EN DONDE "X" ES H O UN GRUPO PROTECTOR OH, O UN COMPUESTO (5), CON R2NCO, R2R3NCOCl O CON FOSFOGENO O UN CLOROFORMIATO O UN CARBONATO SEGUIDO POR R2R3NH, EN DONDE: R2 Y R3 PUEDEN ESTAR PROTEGIDOS; Y POSTERIORMENTE DESPROTEGER LOS GRUPOS PROTEGIDOS, CONVERTIR R2 O R3 EN OTRO R2 O R3; HIDROGENAR EL GRUPO VINILO EN LA POSICION 12, PARA FORMAR UN GRUPO ETILO O SI SE USA (5) TRATAR EL PRODUCTO CON UN ACIDO. LOS COMPUESTOS OBTENIDOS PRESENTAN PROPIEDADES ANTIMICROBIANAS

Procede de preparation de nouveaux composes

Compuesto azabiziclico mutilin 14-carbamatos utiles como an- tibacterianos

Un compuesto de fórmula (3), o una de sus sales o derivadosfarmacéuticamente aceptables;en la que :R1 es vinilo o etilo; y R2 es un grupo R3 , R4 CH2 - o R5 R6 C=CH-; en el que cada R3 y R4 es un sistema de anillo azabicíclico o R5 y R6 , junto al átomo de carbono al que se encuentran unidos, forman un sistema de anillo azabacíclico.Un procedimiento para preparar un compuesto según cualquiera de las reivindicaciones anteriores, que incluye hacer reaccionar un compuesto de fórmula (4), en la que X es hidrógeno o un grupo protector de hidroxilo, o un compuesto de fórmula (5), con un isocianato de ácido de fórmula R3 CONCO, R4 CH2 CONCO o R5 R6 C=CHCONCO:Un procedimiento para tratar infecciones microbianas en animales, en especial, en seres humanos y en mamíferos domesticados, que comprende administrar una cantidad eficaz desde el punto de vista antimicrobiano de un compuesto según la reivindicación 1, 2 ó 3, o una composición según la reivindicación 7, a un paciente que lo necesite.

Verfahren zur Herstellung von in ª‡-Stellung substituierten Ketonen, Carbonsaeureestern oder -amiden

Nouveaux esters d'acides gras, sulfonés, leur procédé de fabrication et leurs applications

4-Hydroxy-3-(substitutedmethyl)-benzeneacetic acids

New 4-hydroxy-3-(substitutedmethyl)benzeneacetic acids have been prepared which are useful as starting materials in the preparation of cephalosporin and penicillin derivatives.

一种(e)-1,2-二硫氰酸乙烯酯化合物的合成方法

本发明公开了一种(E)‑1,2‑二硫氰酸乙烯酯化合物的合成方法。该方法是在室温搅拌条件下，炔烃、硫氰酸盐和过硫酸盐在二氯甲烷溶液中一锅反应，选择性合成(E)‑1,2‑二硫氰酸乙烯酯化合物。该方法原料易得，反应条件简单、温和，反应选择性高，产率好，底物官能团兼容性优异，具有较高的应用价值。

Cephalosporin derivatives

Neue cephalosporinderivate

Cephalosporin derivatives

신규한 항생활성 화합물 및 그 화합물을 포함하는 항생 조성물

본 발명은 신규한 항생활성 화합물 및 그 화합물을 포함하는 항생 조성물에 관한 것으로 더욱 상세하게는 미생물 단백질 합성을 저해하는 화합물 및 그 화합물의 용도에 관한 것이다.