НОВЫЕ ПРОИЗВОДНЫЕ АМИДИНОВ, ИХ ПОЛУЧЕНИЕ И ИХ ИСПОЛЬЗОВАНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Изобретение относится к новым производным амидинов общей формулы I: в которой R1 обозначает алкил; R2 обозначает алкил, алкенил, алкинил или цианоалкил; R3 обозначает водород; n обозначает 0 или 1; Х обозначает -(СН2)m-, где m есть 0 или 1; А обозначает гетероциклический 5-членный арильный радикал, содержащий атом S; или к солям этих соединений, их получению и их использованию в качестве лекарственных средств. Более конкретно, оно относится к применению названных производных для получения лекарственного средства, предназначенного для ингибирования NO-синтаз (NOS) и/или моноаминооксидаз (МАО). 3 н. и 3 з.п. ф-лы.

Способ получения хлорангидридов моно- или дисульфокислот 1-тиаинденов

СПОСОБ ПОЛУЧЕНИЯ 3-ГУАНИДИНОАЛКИЛТИОФЕНОВ

Способ получения производных бета-тиенила

Способ получения производных 1-оксо-5-инданилоксиуксусной кислоты

HALOGENALKOXIMINOESSIGSÄUREAMIDE

CARBONYLAMINO-SUBSTITUIERTE ACYL-PHENYL-HARNSTOFFDERIVATE, VERFAHREN ZU DEREN HERSTELLUNG UND DEREN VERWENDUNG

SUBSTITUTED SALICYLIC ACIDS AND THEIR DERIVATIVES

... 1,272,190. Salicylic acid derivatives. MERCK & CO. Inc. 18 June, 1970 [25 June, 1969; 20 April, 1970], No. 29667/70. Heading C2C. The invention comprises compounds of formula and their pharmaceutically acceptable salts and anhydrides (when R 1 is OH), wherein A is CH 2 or CO; Y is CH 2 , NH, N-alkyl, S or O; R 1 is OH, NH 2 , alkoxy, alkylamino, dialkylamino, dialkylaminoalkylamino, dialkylaminoalkoxy, hydroxyalkoxy, polyhydroxyalkoxy, alkoxyalkoxy, PhO (possibly substituted), alkanoylaminoalkoxy, hydrazino, morpholino, piperidino, anilino, hydroxyalkylamino or an N- attached naturally occurring aminoacid radical; R 2 is H, acyl, alkyl or alkoxycarbonyl; R 3 is H, alkyl, cycloalkyl, alkoxy, haloalkyl or halogen; and X is H, alkyl, OH, alkoxy, acyloxy, halogen, haloalkyl; NO 2 , NH 2 , alkylamino, dialkylamino, acylamino, SH, alkylmercapto, alkylsulphinyl, alkylsulphonyl, sulphanyl, aminosulphinyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, ...

New process for the industrial synthesis of tetraesters of 5-[bis(carboxymethyl)amino]-3-carboxymethyl-4-cyano-2-thiophenecarboxylic acid, and application to the synthesis of bivalent salts of ranelicacid and their hydrates.

Heteroaryl succinamides and their use as metalloprotein ase inhibitors

Heteroaryl succinamides and their use as metalloproteinase inhibitors.

The present invention is directed to compound of formula (i), wherein r1, r2, r3, r4, r5, x, y and (1a)are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.

Novel ?-oxygenated or ?-thiolated carboxylic acid penethylamide derivatives.

The invention relates to ?-oxygenated or ?-thiolated carboxylic acid phenethylamide derivatives of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein A stands for optionally substituted aryl or optionally substituted heteroaryl; X is oxygen or sulfur; Y is oxygen or sulfur; R1 is hydrogen, alkyl, alkenyl, alkynyl. cy-cloalkyl. haloalkyl, haloalkenyl, haloalkynyl or halocycloalkyl; R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloakyl, cycloalkylalkyl, alkoxy-alkyl, alkoxy-alkenyl, alkoxy-alkynyl, whereof all alkyl- alkenyl-, alkynyl-. or cycloalkyl-groups me be optionally substituted by halogen; or optionally substituted arylalkyl, optionally substituted aryl-alkenyl, optionally substitute aryl-alkynyl or optionally substituted aryloxy-alkyl; R3 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, alkoxy-a kyl, alkoxy-alkenyl, alkoxy-alkynyl, whereof all alkyl- alkenyl-, alkynyl-. or cycloalkyl-groups me be optionally substituted ...

Heteroaryl succinamides and their use as metalloprotein ase inhibitors

Novel alpha-oxygenated or alpha-thiolated carboxylic acid penethylamide derivatives.

New process for the industrial synthesis of tetraesters of 5-[bis(carboxymethyl)amino]-3-carboxymethyl-4-cyano-2-thiophenecarboxylic acid, and application to the synthesis of bivalent salts of ranelicacid and their hydrates.

New process for the industrial synthesis of tetraesters of 5-[bis(carboxymethyl)amino]-3carboxymethyl-4-cyano-2-thiophenecarboxylic acid, and application to the synthesis of bivalent salts of ranelic acid and their hydrates.

Heteroaryl succinamides and their use as metalloproteinase inhibitors

Synthesis of thiophenecarboxylic acid esters for the production of ranelic acids salts.

Novel alpha-oxygenated or alpha-thiolated carboxylic acid penethylamide derivatives.

New process for the industrial synthesis of tetraesters of 5-[bis(carboxymethyl)amino]-3-carboxymethyl-4-cyano-2-thiophenecarboxylic acid, and application to the synthesis of bivalent salts of ranelicacid and their hydrates.

Novel alpha-oxygenated or alpha-thiolated carboxylic acid penethylamide derivatives.

VERFAHREN ZUR HERSTELLUNG VON NEUEN CYANOMETHYLTHIOACETYLCEPHALOSPORINEN

INDUSTRIAL PROCEDURE FOR THE PRODUCTION OF 5 - TO (CARBOXYMETHYL) AMINO -3-CARBOXYMETHYL-4-CYANO-2-THIOPHENCARBONSÄURE ETRAESTERN AND USE TO THE SYNTHESIS OF BIVALENT RANETANSÄURESALZEN AND THEIR HYDRATES

VERFAHREN ZUR HERSTELLUNG VON NEUEN MERCAPTOACYLDERIVATEN VON 4-CIS-SUBSTITUIERTEN PROLINEN

NEW GAMMA-GLUTAMYL-4-AZOANILIDE, PROCEDURE FOR THE PRODUCTION OF THESE CONNECTIONS AS WELL AS THEIR USE FOR THE REGULATION OF GAMMAGLUTAMYLTRANSFERASE.

2-CYANO-3,5-DIHYDROXY-HEX-2-EN-CARBONSÄURE of AMIDE DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS DRUGS

PROCEDURE FOR THE PRODUCTION OF NEW CYANOMETHYLTHIOACETYLCEPHALOSPORINEN

1-ALKYL-, 1-ALKENYL- AND 1-ALKYNYLARYL-2-AMINO-1,3- PROPANEDIOLS AND RELATED COMPOUNDS, A PROCESS AND INTERMEDIATES FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

8-SUBSTITUTED 2-AMINOTETRALINS

Aromatic compounds derived from imine, their preparation and their use in human and veterinary medicine and in cosmetics

4-HETEROARYL-1,3-BENZODIAZEPINES AND 2-SUBSTITUTED-ALPHA- (HETEROARYL) BENZENEETHANAMINES, A PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

METHOD OF TREATING COTTON AND GRAIN SEEDS AND A COMPOSITION THEREFOR

NITROFURYL-AMIDINE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

SUBSTITUTED SALICYLIC ACID DERIVATIVES AND PROCESSES FOR THEIR PREPARATION

PROPARGYL FURAN- AND THIOPHENECARBOXYLATES

BASF Aktiengesellschaft Propargyl furan- and thiophenecarboxylates of the formulae Ia and Ib (Ia) (Ib) where R1, R2 and R3 are each hydrogen, chlorine, bromine, nitro, C1-C4-alkyl, C2-C4-alkenyl, C1-C4-haloalkyl, C2-C4-haloalkenyl, or phenyl which is unsubstituted or substituted by halogen, C1-C4-alkyl, or C1-C4-alkoxy, X is oxygen or sulfur, n is the integer 0 or 1, and, if X is sulfur, R1, R2 and R3 may furthermore be fluorine, cyano, C1-C4-alkoxy, C1-C-4-halo-alkoxy, C2-C4-alkenyloxy or C2-C4-haloalkenyloxy, processes for their manufacture, and their use for combating pests.

(1-OXO-2-ARYL OR THIENYL-2-SUBSTITUTED-5-INDANYLOXY (OR THIO)) NOIC ACIDS AND DERIVATIVES THEREOF AND PROCESSES FOR PREPARING SAME

1-ALKYL-, 1-ALKENYL- AND 1-ALKYNYLARYL-2-AMINO-1,3-PROPANEDIOLS AND RELATED COMPOUNDS, A PROCESS AND INTERMEDIATES FOR THEIR PREPARATIONAND THEEIR USE AS MEDICAMENTS

The present invention relates to novel 1-alkyl-, 1-alkenyl- and 1-alkynylary l- 2-amino-1,3- propanediols, intermediates and processes for the preparation thereof. The compounds of the invention are of the formula I RCH(OR1)CH(NR2R3)R4 (I) wherein R is wherein R5 is CH3(CH2)mC=C. CH3(CH2)m,CH=CH, CH3(CH2)m,CH2CH2, wherein m is 3 to 15, n is 0 to 12, W and X are independently hydrogen, (C1- C8) alkyl, (C1-C8) alkoxy, halogen or trifluoromethyl, and Z is S. O, or C=O: and A is S or O: R1 is hydrogen or wherein R6 is hydrogen, (C1-C8) alkyl. (C1-C8) alkoxy. or :R2 is hy drogen (C1-C3) alkyl. R3 is hydrogen (C1-C3) alKyl or wherein R6 is as above: R4 is wherein R7 is hydrogen (C1-C8) alkyl. or CH2 OR8 wherein R8 is hydrogen or wherein R6 is as above: R1 and R8 taken together with the oxygen to which th ey are attached form a group of the formula wherein R9 and R10 are independently hydrogen or alkyl, where alkyl is a straight or branched chain hydrocarbon having no unsaturation and 1 to 10 ...

2-CYANO-3, 5-DIHYDROXYHEX-2-ENECARBOXAMIDE DERIVATIVES

... 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives (see fig.I) are suitable for the production of pharmaceuticals for the prophylaxis and thera py of diseases or disorders whose course involves increased connective tissue or cartilage degradation.

AROMATIC DISELENIDES AND SELENOSULFIDES, THEIR PREPARATION AND THEIR USES, MORE PARTICULARLY THEIR THERAPEUTICAL USE

The objects of the present invention are: - novel organoselenium compounds: aromatic diselenides and selenosulphides; - the use of said novel compounds as antioxidant agents; - pharmaceutical compositions containing them; - a method of preparation of said novel compounds. Said novel cyclic organoselenium compounds have the general formula (I): (see fig. I) ...

NOVEL 3,4-DIARYL THIOPHENES AND ANALOGS THEREOF HAVING USE AS ANTIINFLAMMATORY AGENTS

A class of 3, 4-diary substituted thiophene, furan and pyrole derivatives and analogs thereof pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interes t are defined by formula (I), (see fig. I) wherein Y is selected from O. S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituents selected from hydrido, halo, lower alkcoxyc arbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals sel ected from sulfamyl, alkylsulfonyl, halo, lower alkcoxy and lower alkyl; or a pharmaceutically accept able slat thereof.

Verfahren zur Herstellung von Salicylsäure-Derivaten

Verfahren zur Herstellung entzündungshemmender Verbindungen

VERFAHREN ZUR HERSTELLUNG BASISCHER (BETA)-THIENYLDERIVATE.

Procédé de préparation d'esters d'acides cyclopropane-carboxyliques

Process for the preparation of [1-oxo-2-aryl- or -thienyl-2-subst.-5-indanyloxy-(or -thio)]alkanecarboxylic acids and their derivatives

Process for the preparation of cyclic compounds

Process for the preparation of [1-oxo-2-aryl- or -thienyl-2-subst.-5-indanyloxy- (or -thio)]alkanecarboxylic acids or their alkyl esters

... [1-Oxo-2-aryl- or -thienyl-2-subst.-5-indanyloxy- (or -thio)]alkanecarboxylic acids or their alkyl esters of the formula are prepared. The substituents in the formula are described in Claim 1. These compounds are obtained by reacting an appropriately substituted [1-oxo-2-aryl- or -2-thienyl-5-indanyloxy- (or -thio)]alkanecarboxylic acid or a lower alkyl ester thereof with an alkylating agent which supplies the radical R. The resulting compounds, which are in the form of the free acid, can be converted into lower alkyl esters or salts. The corresponding amides are likewise prepared from compounds of the formula I which are in the form of the free acid by converting the acid with thionyl chloride into the acid chloride and then reacting the latter with an amine. The resulting compounds have therapeutic activity and can be used, in particular, in diuretic and saluretic agents.

Process for the preparation of [1-hydroxy-5-indanyloxy (or indanylthio)]-alkanecarboxylic acids

PROCEDURE FOR THE PRODUCTION OF AMINOCYCLOPENTANSAEUREN AND YOUR PHYSIOLOGICALLY ACCEPTABLE ONE OF SALTS AND SOLVATE.

THE MERCAPTO-ACYLATED DERIVATIVES OF VARIOUS PROLINE 4-SUBSTITUTED HAS ANTI-HYPERTENSIVE.

Novel alpha-oxygenated - carboxylic or α - acid penethylamide derivatives

Способ получения производных 2-тиенилоксиуксусной кислоты или их фармацевтически приемлемых солей

Изобретение касается производных 2-тиенилоксиуксусной кислоты, в частности получения 5-[2-(бензолсульфониламино) этил] - или 5-[2-(4-хлорбензолсульфониламино) этил]-2-тиенилоксиуксусных кислот, которые могут быть использованы в медицине для лечения тромботических заболеваний. Цель - создание новых более активных веществ указанного класса. Синтез ведут окислением, например, амида N-[2-[2-(5-(2-гидрокси)-этокси)-тиенил]-этил]-бензолсульфоновой кислоты окисью серебра в водно-щелочной среде. Растворяют амид в 0.5-4 н. преимущественно в 2 н., растворе KOH или NaOH, окисляют 2-16 эквивалентами окиси серебра при 75-85°C в течение 2-3 ч. Исходную окись серебра предварительно получают растворением AgNO3 в дистиллированной воде с добавлением эквимолярных количеств NaOH. Целевой продукт выделяют в свободном виде или в виде фармацевтически приемлемой соли. Новые соединения малотоксичны и в 4 раза активнее, чем дазоксибен, при этом начало антитромбического действия наблюдается при 1 мг/кг и достигает ...

The method of obtaining of derivatives 2 thienyloxiacetic acide or of salt useful in pharmaceutic

(METHYLSULFONYL) PHENYL - OF 2 - (5H) - FURANONES AS INHIBITORS OF CYCLOOXYGENASE - 2 OF

(METHYLSULFONYL)PHENYL-2-(5H)-FURANONES AS CYCLOOVYGENASE-2 INHIBITORS

(54) Heteroaryl Succinamides, Pharmaceutical Compositions Containing the Same and Methods for Treatment of the Diseases Caused by Metalloproteinase Activity

PROLINES 4-CIS-SUBSTITUEES

NITROFURYL- AND NITROTHIENYL AMIDINE DERIVATIVES

SUBSTITUTED SALICYLIC ACIDS AND THEIR DERIVATIVES

PREPARATION Of ACIDS AMINOCYCLOPENTANIQUES

PROCESS FOR THE INDUSTRIAL SYNTHESIS OF TETRAESTERS OF 5-(BIS(CARBOXYMETHYL)AMINO)-3-CARBOXYMETHYL-4-CYANO-2-THIOPHENECARBOXYLIC ACID, AND APPLICATION TO THE SYNTHESIS OF BIVALENT SALTS OF RANELIC ACID AND THEIR HYDRATES

PURPOSE: A process for the industrial synthesis of tetraesters of 5-(bis(carboxymethyl)amino)-3-carboxymethyl-4-cyano-2-thiophenecarboxylic acid, and application to the synthesis of bivalent salts of ranelic acid and their hydrates are provided, thereby simply producing the compound of formula (I) in a very good yield, with a considerably shorter reaction time and excellent purity and in which the aqueous saline waste is completely avoided. CONSTITUTION: The process for the industrial synthesis of compounds of formula (I), wherein R and R' are the same or different, and each represents linear or branched (C1-C6)alkyl, comprises reacting a compound of formula (III), wherein R is as defined hereinbefore, with a compound of formula (IV), wherein R' is as defined hereinbefore, in the presence of a catalytic amount of a C8-C10-type quaternary ammonium compound, and in the presence of potassium carbonate, at the reflux of an organic solvent; subsequently filtering the reaction mixture; and concentrating ...

PROCESS FOR PREPARATION OF BASIC DERIVATIVES OF BETA-TIENILO

COMPOSED HETEROCYCLIC ORGANOZUFRADOS, COMPOSITIONS PESTICIDES CONTAIN THAT THEM AND USE OF THE SAME TO CONTROL PLAGUES OF ARTHROPODS.

Reivindicacion 1: Un compuesto de organoazufre que contiene halogeno representado por la formula (1) en donde m representa 0, 1 o 2, n representa 0, 1 o 2, A representa un grupo heterocíclico saturado de 3 a 8 miembros opcionalmente sustituido con un grupo seleccionado del grupo E1; Q representa un átomo de fluor o un grupo haloalquilo C1-5 que contiene al menos un átomo de fluor, R1, R1a y R3 representan, de modo independiente, un grupo hidrocarbonado de cadena C1-4 opcionalmente halogenado, un átomo de halogeno o un átomo de hidrogeno, R2, R2a y R4 representan, de modo independiente, un grupo hidrocarbonado de cadena C1-4 opcionalmente halogenado, C(=G)R5, un grupo ciano, un átomo de halogeno o un átomo de hidrogeno, G representa un átomo de O o un átomo de S; R5 representa un grupo alquilo C1-C4 opcionalmente halogenado, un grupo hidroxilo, alcoxi C1-4 opcionalmente halogenado, alquenil C3-6-oxi opcionalmente halogenado, alquinil C3-6-oxi opcionalmente halogenado, un grupo amino, un ...

Novel phenylacetic acid derivative

Disclosed is a compound represented by the formula (1) or a salt thereof, which has excellent inhibitory activity on the production of prostaglandin E2 and is useful as an active ingredient for a pharmaceutical agent having reduced adverse side effects including gastrointestinal disorders [in the formula, ---- represents a single bond or a double bond; R1 represents a hydrogen atom or an alkyl group; R2 and R3 independently represent a hydrogen atom or an alkyl group; R4 and R5 independently represent a hydrogen atom, a hydroxy group, an alkoxy group, a halogen atom, or a mono- or di-alkyl-substituted amino group; R6 represents a hydrogen atom, a cyano group, an alkoxycarbonyl group, or a carboxy group; R7 represents one or two substituents on the benzene ring (each of the substituents represents a hydrogen atom, a halogen atom, a nitro group, a cyano group, a hydroxy group, an amino group, an alkyl group, or an alkoxy group); A represents a non-aromatic 5- or 6-membered heterocyclic ring ...

Fungicides

Geminal carboxylic acids and esters thereof, pharmaceutical formulations containing them useful in the treatment of bone dysmetabolism

Compounds of formula I: wherein Ra, Rb, ¿, B and R are as defined in the disclosure, have antagonistic activity on osteoclast hyper-reactivity.

3,4-Diarylthiophene und Analoga davon, sowie deren Verwendung als entzündungshemmende Mittel

ARYLOXYCYCLOALKENYL- UND ARYLOXYIMINOCYCLOALKENYL-HYDROXYHARNSTOFFE MIT 5-LIPOXYGENASE INHIBIERENDER WIRKUNG

CEPHALOSPORINS

... 1437221 Cephalosphorin silyl esters E R SQIBB & SONS Inc 4 July 1973 [4 Aug 1972] 31882/73 Heading C3S [Also in Division C2] The novel cephem compound of formula wherein R is a trimethylsilyl group, R 1 is a group -CH 2 -CH = CH 2 , R 2 is H, R 3 is ethyl and X is H, is prepared by reacting trimethylsilyl ester of 7-amino-3-desacetoxycephalosporanic acid with a cyanomethylthioacetyl chloride of formula wherein R 1 , R 2 and R 3 are as defined above and R 5 is chlorine.

NITROFURYL- AND NITROTHIENYL AMIDINE DERIVATIVES

... 1309727 Nitrofuran and nitrothiophene derivatives BOEHRINGER MANNHEIM GmbH 16 June 1971 [20 June 1970] 28217/71 Heading C2C Novel compounds of Formula I (in which Het is a naphthyridine or s-triazolo- [4,3-b]pyridazine ring system which is optionally substituted by hydroxy, amino or C 1-3 alkyl groups, X is an oxygen or sulphur atom, and each of R 1 , R 2 and R 3 is a hydrogen atom or a C 1-3 alkyl or alkoxyalkyl radical, or two of R 1 , R 2 and R 3 , together with the atoms to which they are attached, can form a 5- or 6-membered ring which optionally contains 1 or 2 additional N, O or S atoms) and pharmacologically acceptable acid addition salts thereof, are prepared by (a) condensing a compound of the Formula II with a compound of the Formulµ III, VIII, IX or X (in which R 4 is alkyl ) or with a nitrile of Formula R 3 CN, or (b) reacting a compound of the Formula IV (in which Y is an alkoxy or alkylthio group and R 4 is H or C 1-3 alkyl) with an amine of Formula HNR 1 R 2 , or (c) reacting ...

PREPARATION OF AMINOCYCLOPENTANE ACIDS

AROMATIC DISELENIDE AND SELENOSULFIDE FOR USE AS ANTI-OXIDE TO MEANS

3,4-DIARYLTHIOPHENE AND ANALOGUES OF it, AS WELL AS THEIR USE AS RESOLVENTS

(METHYL SULPHONYL) PHENYL-2 (5H) - FURANONE AS COX-2 INHIBITORS

SUBSTITUTED TETRAHYDRONAPHTHALIN AND DIHYDRONAPHTHALIN DERIVATIVES WITH A RETINOIDEN AND/OR RETINOID ANTAGONIST-SIMILAR BIOLOGICAL ACTIVITY

PROCEDURE FOR the PRODUCTION OF NEW MERCAPTOACYLDERIVATEN OF 4-CIS-SUBSTITUIERTEN PROLINEN

PROCEDURE FOR THE PRODUCTION OF AMINOCYCLOPENTANSAEUREN

MOULD FIGHT MEANS.

Procedure for the production of new hetero-cyclic connections and their salts

PROCEDURE FOR the PRODUCTION OF NEW ONES (1-OXO-2-ARYL OR - THIENYL-2-SUBST. - 5-INDANYLOXY (OR - THIO))- ALKANE-CARBON-SOUR AND THEIR SALTS, AMIDES, ANHYDRIDES AND ESTERS

PROCEDURE FOR THE PRODUCTION OF NEW THIOPHEN DERIVATIVES AND YOUR SALTS

Novel 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents

Aromatic diselenides and selenosulphides, their preparation and their uses, notably therapeutic uses

(methylsulfonyl)phenyl-2-(5h)-furanones as cox-2 inhibitors

3-METHOXY-2-(SUBSTITUTED PHENYL)-PROPENOIC ACID ESTERS AS FUNGICIDES

NOVEL ALPHA-OXYGENATED OR ALPHA-THIOLATED CARBOXYLIC ACID PENETHYLAMIDE DERIVATIVES

The invention relates to .alpha.-oxygenated or .alpha.-thiolated carboxylic acid phenethylamide derivatives of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein A stands for optionally substituted aryl or optionally substituted heteroaryl; X is oxygen or sulfur; Y is oxygen or sulfur; R1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, haloalkenyl, haloalkynyl or halocycloalkyl; R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkoxy-alkyl, alkoxy-alkenyl, alkoxy-alkynyl, whereof all alkyl- alkenyl-, alkynyl-, or cycloalkyl-groups me be optionally substituted by halogen; or optionally substituted arylalkyl, optionally substituted aryl-alkenyl, optionally substituted aryl-alkynyl or optionally substituted aryloxy-alkyl; R3 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, alkoxy-alkyl, alkoxy-alkenyl, alkoxy-alkynyl, whereof all alkyl- alkenyl-, alkynyl-, or cycloalkyl-groups me be optionally ...

BCRP/ABCG2 INHIBITOR

... ²² The present invention is directed to a breast cancer ²resistance protein (BCRP/ABCG2) inhibitor.²The BCRP inhibitor contains, as an active ingredient, ²an acrylonitrile derivative represented by formula (1):²(see formula 1)² (E or Z)²wherein one of R1 and R2 represents a cyano group and the ²other represents a hydrogen atom;²Ar1 represents a group selected from among the groups ²represented by formulas (2) to (4):²(see formula 2) (see formula 3) (see formula 4)²and Ar2 represents an aromatic hydrocarbon group having a ²condensed ring which may be substituted by a halogen atom, or ²a group selected from among the groups represented by the ²following formulas (5) to (15):²(see formula 5) (see formula 6) ² (see formula 7) (see formula 8) (see formula 9) (see formula 10)²(see formula 11) (see formula 12) (see formula 13) (see formula 14) (see ²formula 15) ²²²² or a salt thereof. ² ...

SULFONYLIMIDO-CARBONIC ACID DIESTERS

Sulfonylimido-carbonic acid diesters of the formula < IMG > in which A is an aromatic group chosen from derivatives of phenyl, napthyl, or in which Y is oxygen, sulphur < IMG > or the grouping -C=N-in which R6 is hydrogen, methyl, fluorine, or methoxy, together with processes to prepare these diesters are described. These compounds find use as intermediates in the preparation of known sulfonylureas, having herbicidal and plant growth regulatory action, of the formula < IMG > which are pyrimidines (E=CH) or triazines (E=N) and in which Ra and Rb have a range of meanings.

IMINE-DERIVED AROMATIC COMPOUNDS, PROCESS FOR THEIR PREPARATION AND THEIR USE IN HUMAN AND VETERINARY MEDECINE, AND IN COSMETICS

A B R E G E "Nouveaux composés aromatiques dérivés d/imine, leur procédé de préparation et leur utilisation en médecine humaine et vétérinaire ainsi qu'en cosmétique." Composés bi-aromatiques répondant à la formule générale suivante : (I) dans laquelle : R1 est H, OH, -CH3, -CH2OH, -COR7, -CH(OH)CH3, -CH2OCOR8, etc, R7 est H, OH, -OR10, N(r'r"), alkyle inférieur, etc, R8 est àlkyle linéaire ou ramifié, ou le reste d'un sucre, R9 est OH, alkyle inférieur ou N(r'r"), R10étant alkyle ou alkényle, r' et r" sont H, alkyle inférieur, aryle, aralkyle, etc, ou r' et r" forment un hétérocycle, R2 et R6 sont H, OH, alkyle inférieur, etc, R3 et R5 sont alkyle .alpha.,.alpha.'-disubstitué ou cycloalkyle, R4 est H, OH, alkoxy, alkyle .alpha.,.alpha.'-disubstitué, R3 et R4 ou R4 et R5 pris ensemble peuvent former un cycle à 5 ou 6 C, Z est O, S, -CH=CR11- ou -N=CR12-, R11 étant H, OH ou alkyle inférieur, R12 étant H ou alkyle inférieur, X est (i) - CR13= N -, (ii) - N = CR13-,(iii) (iv) R13 étant R16 ...

HETEROARYL SUCCINAMIDES AND THEIR USE AS METALLOPROTEINASE INHIBITORS

The present invention is directed to compound of formula (I), wherein R1, R2, R3, R4, R5, X, Y and (Ia) are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.

SYNTHESIS OF THIOPHENECARBOXYLIC ACID ESTERS FOR THE PRODUCTION OF RANELIC ACID SALTS

HETEROARYL DERIVATIVES SUKTsINAMIDOV AND THEIR USE AS INHIBITORS OF METALLOPROTEINASE