ИНГИБИТОРЫ GSK-3

Изобретение касается применения производных мочевины или их фармацевтически приемлемых солей, охарактеризованных формулой (I), где RB выбирают из: ! ! a R3, R4, R′2, R′3, R′4, R′5 и R′6 представляют собой водород, в качестве ингибиторов GSK-3, фармацевтических композиций, содержащих их, и их использования для лечения и/или профилактики заболеваний, в развитие которых вовлечен GSK-3. 6 н. и 8 з.п. ф-лы, 2 пр., 1 табл., 4 ил.

ПРОИЗВОДНЫЕ ИНДЕНА В КАЧЕСТВЕ ФАРМАЦЕВТИЧЕСКИХ СРЕДСТВ

Настоящее изобретение относится к соединениям формулы (I) в виде отдельного стереоизомера, смеси стереоизомеров или рацемической смеси стереоизомеров и их фармацевтически приемлемым солям. Соединения настоящего изобретения обладают противовоспалительной активностью. В формуле (I) ! ! кольцо А, С или D независимо является полностью или частично насыщенным; каждый из С1, С4, С11, С12, С15 и С16 независимо замещен двумя атомами водорода; каждый из С9 и С14 независимо замещен атомом водорода; R1 означает -OR7 или -N(R7)2. Значения остальных радикалов указаны в формуле изобретения. Изобретение также относится к фармацевтической композиции, обладающей противовоспалительной активностью и содержащей эффективное количество соединения изобретения, и к применению соединений для получения лекарственного средства, обладающего противовоспалительной активностью. 3 н. и 20 з.п. ф-лы.

ИНГИБИТОРЫ ПРОТЕАЗ, РАСЩЕПЛЯЮЩИХ ЗА ПРОЛИНОМ

Изобретение относится к соединениям формулы 1 и их фармацевтически приемлемым солям в качестве ингибиторов пост-пролиновых аминопептидаз, а также к фармацевтической композиции на их основе и применение для изготовления такой композиции, и способу ингибирования с их использованием. Соединения могут найти применение для лечения заболеваний, опосредованных активностью пост-пролиновых аминопептидаз, таких как диабет типа II и нарушеной толерантности к глюкозе. В общей формуле 1 либо G1 представляет собой -CH2-Х2-(CH2)а-G3, и G2 представляет собой Н, либо G2представляет собой -CH2-(CH2)a-G3, и G1 представляет собой Н; G3 выбран из группы согласно общей формуле 2, группы согласно общей формуле 3 и группы согласно общей формуле 4; а равно 0, 1 или 2; b равно 1 или 2; X1 выбран из СН2, S, CF2, CHF и О; X2выбран из CH2; X3, X4 и X5 выбраны из N; X6 выбран из NH; X7 выбран из NH; R1 выбран из Н и CN; R2 представляет собой Н; R3 выбран из Н, Cl, ОН, NH2, NH-C1-С10алкила и N(С1-С10алкил)2; R4, R5, ...

5-АМИНО -2-МЕТИЛБЕНЗОДИОКСОЛАН -1,3(2,4- ДИХЛОРОФЕНОКСИ)АЦЕТАТ В КАЧЕСТВЕ ГЕРБИЦИДА И РЕГУЛЯТОРА РОСТА РАСТЕНИЙ

Использование: в качестве стимулятора роста растений и гербицида. Сущность изобретения: продукт- 5 -амино- 2 -метилбензодиоксолан- 1,3 (2,4 - дихлорофенокси)ацетат. Б.Ф. C16H12Cl2 NO5 т.пл. 115 117°С. Реагент 1:2,4-дихлофеноксиуксусная кислота. Реагент 2: 5-амино-2-метилдиоксолан-1,3. Условия реакции: диэтиловый эфир. В дозе 0,0001 мг/л увеличивает рост редьки и кукурузы и в дозе 1 кг/га д.в. снижает массу однодольных на 54% и двудольных на 92% в концентрации 0,0001% увеличивает всхожесть семян березы на 74% не уступая амминной соли 2,4-дихлорофеноксиуксусной кислоты. 3 табл.

Инсектицид

Riechstoff.

SULFONAMID-DERIVATE ALS 5-HT6 RECEPTOR ANTAGONISTEN UND VERFAHREN ZU IHRER HERSTELLUNG

OXYAMINOOXIMETHER, VERFAHREN UND ZWISCHENPRODUKTE ZU IHRER HERSTELLUNG UND SIE ENTHALTENDE MITTEL ZUR BEKÄMPFUNG VON SCHADPILZEN UND TIERISCHEN SCHÄDLINGEN

Substituierte Vinylharnstoff-Derivate und ihre Verwendung als ACAT-Inhibitoren

PREPARATION OF 1,4-DISUBSTITUTED-2-1H-QUINAZOLINONES

... 1385420 Preparation of 1,4-disubstituted- 2(1H)-quinazolinones SANDOZ Ltd 31 Oct 1972 [18 Nov 1971] 50104/72 Heading C2C A compound of formula wherein R 1 represents C 1-5 alkyl group (other than a tertiary alkyl radical in which the tertiary carbon atom is directly attached to the ring nitrogen atom), an allyl, methallyl orpropargyl radical; R 2 and R 3 , which may be the same or different, each signifies a hydrogen, fluorine, chlorine or bromine atom, an alkyl, alkylthio or alkoxy radical of 1 to 3 carbon atoms or a nitro or trifluoromethyl group, provided that no more than one of R 2 and R 3 signifies an alkylthio radical or a nitro or trifluoromethyl group, and R 4 signifies a radical of formula in which Y 1 and Y 2 , which may be the same or different, each signifies a hydrogen, fluorine, chlorine or bromine atom, an alkyl or alkoxy group of 1 to 3 carbon atoms or a trifluoromethyl group, provided that no more than one of Y 1 and Y 2 signifies a trifluoromethyl group, provided that ...

ISOCYANOPHENYL AND ISOCYANONAPHTHYL CARBAMATES AND INSECTICIDAL AND ACARICIDAL COMPOSITIONS CONTAINING THEM

... 1377728 Isocyanophenyl and isocyanonaphthyl carbamates MORTON-NORWICH PRODUCTS Inc 27 July 1973 [31 July 1972] 35934/73 Heading C2C The invention comprises compounds of formula wherein X 1 and X 2 are each oxygen or sulphur; R 1 and R 2 are each H, (C 1-4 ) alkyl, aryl, substituted aryl or a cycloaliphatic group; R 3 represents one or more (C 1-6 ) alkyl group(s), or an alkoxy, allyl, methylenedioxy, haloalkyl, propargyloxy or allyloxy group; n is 0, 1, 2, 3 or 4; and A is a phenyl or naphthyl group. Many compounds are specified. The Specification also describes the preparation of the following intermediates: p-formamido-phenol by the reaction of p-aminophenol with formic acid; and 4-formamidophenyl-N-methylcarbamate by the reaction of p-formamidophenol with The invention also comprises an insecticidal or acaricidal composition which contains as an active ingredient a compound according to the invention in admixture with a diluent or carrier.

SUBSTITUTED CARBOXYLIC ACIDS PROCESSES FOR THEIR PREPARATION AND COMPOSITIONS INCORPORATING THEM

... 1374520 Benzoylphenylalkanoic acids ROUSSEL UCLAF 4 Sept 1972 [3 Sept 1971] 40878/72 Heading C2C Novel compounds of formula (wherein: each W, which may be the same or different, and may be at any position in its phenyl ring, represents a hydrogen atom, a halogen atom, an alkyl radical, an alkyloxy radical, an alkylthio radical, the trifluoromethoxy radical, the trifluoromethylthio radical, the trifluoromethyl radical, a hydroxy group or a dialkylamino radical; R represents a hydrogen atom, an alkyl radical, the 2,3- dihydroxy n - propyl radical, a dioxolan radical of formula (wherein: P and Q, which may be the same or different, each represents an alkyl radical), or the ortho-oarboxyphenyl radical; X and Z, which may be the same or different, each represents a hydrogen atom or an alkyl radical; Y represents a hydrogen atom or a hydroxy radical; and the dotted line indicates the optional presence of either a 2(3) or a 3(4) double bond, when Y is hydrogen, and salts thereof, are prepared ...

DERIVATIVES OF 4-OXO-1, 4-DIHYDRONICOTINIC ACID

QUINOLINE DERIVATIVES

... 1398066 Quinoline derivatives CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA RT 21 Nov 1973 [22 Nov 1972] 54071/73 Heading C2C Novel quinoline derivatives of the formula wherein A and B are hydrogen atoms or together form a methylenedioxy group and R is (C 1 -C 4 ) alkyl, are prepared by alkylating a compound of the formula The alkylating agent is suitably triethyl phosphate and alkylation is preferably carried out in the presence of an acid-binding agent, e.g. an alkali metal carbonate, at a temperature of from 200‹ to 220‹ C. The compounds of the invention possess fungicidal properties. Exam - ples describe the preparation of N-ethyl-1,4- dihydro - 6,7 - methylenedioxy - 4 - oxo - quinoline - 3 - nitrile and N-ethyl - 1,4 - dihydro- 4-oxo-quinoline-3-nitrile. The starting materials may be prepared by reacting a compound of the formula with a compound of the formula and subjecting the resulting compound of the formula to ring closure. The ring closure reaction is suitably carried out in ...

PREPARATION OF N-SUBSTITUTED 6,7-METHYLENEDIOXY-4-QUINOLONE DERIVATIVES

... 1324332 Novel 6,7-methylenedioxy-quinoline carboxylic acids and their use to prepare N- substituted 6,7-methylenedioxy-4-quinoline derivatives SUMITOMOCHEMICAL CO Ltd 8 July 1970 [10 July 1969 2 Oct 1969 (3) 23 Feb 1970] 33641/72 Divided out of 1324331 Heading C2C Novel 3 - alkoxycarbonyl - 4 - halogeno - 6,7- methylenedioxy-quinolines of the general For mulae VI and III wherein R 1 is C 1-20 alkyl or hydrogen, X is halogen, R is C 1-20 alkyl or C 2-4 alkenyl and Y(-) is an anion may be prepared in the case of VI by (a) cyclization of a 3,4-methylene-dioxyanilino methylene malonate with a halogenating agent or (b) halogenation of a 3-alkoxycarbonyl- 4 - hydroxy - 6,7 - methylene - dioxy - quinoline and in the case of III by (a) cyclization of a dialkyl N-substituted 3,4-methylene-dioxy-anilino-methylene malonate or (b) N-alkylation or N-alkenylation of VI. The novel compounds III may be used to prepare compounds I by treating with an alkyl alcohol or water. The compounds I are ...

INDOLE DERIVATIVES

... 1382917 1-Acylindolines AMERICAN CYANAMID CO 3 May 1972 [27 May 1971] 56237/73 Divided out of 1382916 Heading C2C The invention comprises compounds of formula where R 1 is H, Cl, Br, C 1-4 alkoxy, NO 2 , NH 2 , AcNH or NMe 2 , and R 2 is H, C 1-4 alkoxy or NO 2 , or R 1 R 2 is -OCH 2 O-; R 3 is H or Me; Y is PhCO (possibly substituted by Cl or NO 2 ) or C 2-4 alkanoyl; and Z is OH, Cl, Br, MeSO 3 or p-TsO. In examples, these compounds are prepared by (a) acylating the corresponding N- unsubstituted compounds (and if necessary saponifying an initial compound where Z = (e.g.) OAc); (b) introducing an NO 2 group by nitration and if appropriate reducing to NH 2 ; (c) converting Z = OH to the other values for Z; (d) (for Z = OH) reducing a corresponding indoline-3-acetic acid or its ester, or its mixed anhydride with EEOCO 2 H. Intermediates otherwise prepared have the formulae RH, 3-R:C(OH)CO 2 Et, 3-RCH 2 CO 2 Et, [R being a 2-oxoindoline residue, substituted by 5,6-(MeO) 2 or 5,6-(OCH 2 O ...

Matrix metalloproteinase inhibitors

Water soluble derivatives of camptothecin.

The present invention relates to water soluble, camptothecin derivatives of formula (1)wherein n represents the integer 1 or 2; and r1 represents hydrogen, lower alkyl, (c3-7)cycloalkyl, (c3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, amino lower alkyl, lower alkylamino lower alkyl, amino lower alkul, lower alkoxy lower alkyl or (ch2)tar wherein: t is 0 to 5 and ar represents phenyl, furyl, pyridyl, n-methylpyrrolyl, imidazolyl; or phenyl, furyl, pyridyl, n-methylpyrrolyl, imidazolyl, with one or more substituents independtly selected from hydroxy, methoxy, halogen and amino; and r2 represents diphenylmenthyl or (ch2)tar; or r1 and r2 taken together with the linking nitrogen represents n-tetrahydroquinolyl or n-tetrahydroisoquinolyl; and pharmaceutically acceptable salts and solvents thereof; their use as topoisomerase inhibitors; their preparations; and their use in the treatment of cancer.

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.

Novel imidate insecticides.

A series of novel imidate insecticides ...

Water soluble camptothecin derivatives.

The invention relates to water soluble, camtothecin derivatives of formula wherein n represents the interger 1 or 2: and r1 and r2 represent independently, hydrogen, lower alkyl,(c3-7)cycloalkyl,, (c3_7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl.

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

NOVEL IMIDATE INSECTICIDES

WATER SOLUBLE CAMPTOTHECIN DERIVATIVES

Water soluble camptothecin derivatives

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.

News (phényl-4 pipérazinyléthyl) - 2 anilines, their preparation and their employment like drug.

New derivatives of triazole their method of preparation and the pharmaceutical compositions containing them

Carbamoyloxy derivatives of mutiline and their useas antibacterials.

Method of preparation of derived from quinazoline.

Il-8 receptor antagonists

Biocides compositions containing derived hydrazone aryls to fight against the diseases of the plants.

Water soluble camptothecin derivatives

New derivatives of the amino-2 phénéthylamines and their preparation.

Novel imidate insecticides.

NOVEL IMIDATE INSECTICIDES

Water solube drivatives of camtotheci n

Water soluble camptothecin derivatives

WATER SOLUBLE CAMPTOTHECIN DERIVATIVES

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

Novel compounds

Novel compounds

NPYY5-ANTAGONISTEN

PROCEDURE FOR the PRODUCTION of NEW n (BENZTHIAZOL 2-YL) - OXAMIDSAEURE DERIVATIVES AND THEIR SALTS

PROCEDURE FOR THE PRODUCTION OF NEW HYDRAULIC XY AETHYLIDEN CYANESSIGSAEURE ANILIDEN AS WELL AS OF THEIR PHYSIOLOGICAL COMPATIBLE ONE SALTS

SUBSTITUTED 2-PYRIDIN-CYCLOHEXAN-1,4 DIAMINE DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF NEW ONES 4 (M-BENZOYLPHENYL) - BUTTER ACIDS, THEIR SALTS OR ESTERS

PROCEDURE FOR THE PRODUCTION OF NEW CARBAMOYLAMINOALKYLBENZOLSULFONYLHARNSTOFFEN AND THEIR SALTS

UREA-LEFT CONNECTIONS AND YOUR USE AS PPAR MODULATORS

INDEN OF DERIVATIVES AS PHARMACEUTICALS

VERFAHREN ZUR HERSTELLUNG VON NEUEN 5-METHYL- ISOXAZOL-4-CARBONSAEUREANILIDEN

HERBIZIDE MITTEL

FÄRBEMITTEL FÜR KERATINFASERN UND INSBESONDERE HUMANHAARE, SOWIE VERFAHREN ZUM FÄRBEN VON KERATINFASERN

PROCEDURE FOR the PRODUCTION OF 1-ALKYL-4-PHENYL -2 (1H) - CHINAZOLINONEN

PROCEDURE FOR the PRODUCTION of NEW n (BENZTHIAZOL 2-YL) - OXAMIDSAEURE DERIVATIVES AND THEIR SALTS

PROCEDURE FOR MANUFACTURING NEW n (TRIMETHOXYBENZYL) - N' PHENYLPIPERAZINEN AND YOUR SAEUREADDITIONSSALZEN

PROCEDURE FOR MANUFACTURING NEW n (TRIMETHOXYBENZYL) - N' PHENYLPIPERAZINEN AND YOUR SAEUREADDITIONSSALZEN

Process for the preparation of 1-(2-(5--2-[furylmethylthio]ethyl))amino-1- (methylamino)-2-nitroethylene hydrochloride

WATER-SOLUBLE CAMPTOTHECINDERIVATE

INDAN-1,3-DION AND INDAN-1,2,3-TRIONDERIVATE, PROCEDURE FOR YOUR PRODUCTION AND THEIR THERAPEUTIC USE

THIOUREA DERIVATIVES AND IT ABSTENTION, ANTIMICROBIAL AND ANTIULCEROGENES MEANS

PIPERAZINYLDERIVATE WITH AFFINITY FOR 5-HT RECEPTORS.

ANILINE DERIVATIVES, THESE CONTAINING PHARMACEUTICAL PREPARATIONS AND PROCEDURES FOR YOUR PRODUCTION.

PROCEDURE FOR THE PRODUCTION OF NEW N-ISOTHIOUREIDO-PHTHALIMIDEN AND THEIR SALTS

ALKYLAMINOINDANVERBINDUNGEN, PROCEDURES FOR THEIR PRODUCTION AND THESE CONTAINING PHARMACEUTICAL COMPOSITIONS

IMIDATE WITH INSEKTIZIDER EFFECT.

DITHIOCARBONIMIDDERIVATE AS FUNGICIDES, INSECTICIDES AND AKARIZIDE

PHENYLIMINOTHIAZOLINDERIVATE, YOUR PRODUCTION AND INTERMEDIATE PRODUCTS FOR IT, IT ABSTENTIONS PHARMACEUTICAL PREPARATIONS AND THEIR PRODUCTION.

NEW AMIDINDERIVATE, YOUR PRODUCTION AND USE AS DRUGS WITH LTB4 OF ANTAGONISTIC EFFECT

(P-AMINO-HYDROXYPHENYL) - ACRYLAMIDE DERIVATIVES AND THESE CONNECTIONS ABSTENTION COLORING MEANS

PROCEDURE FOR THE PRODUCTION OF NEW BENZODIAZEPINDERIVATEN

2-AMINOALKYL-1,4-DIAMINOBENZOL-DERIVATE AND THESE CONNECTIONS ABSTENTION COLORING MEANS

GLUCAGON ANTAGONIST/INVERSE AGONISTEN

KATIONI METHYLENDIOXY BENZENE, THEIR USE FOR OXIDATIVE COLORING OF KERATINI FIBERS, COLORING MEANS AND DYEING METHODS

PENTAFLUOROBENZENSULFONAMIDEN AND SIMILAR ONE

PENTAFLUOROBENZENSULFONAMIDE AND SIMILAR ONE

KATIONI KUPPLER THEIR USE FOR OXIDATIVE COLORING

CONNECTIONS AND YOUR USE IN A BINARY SYNTHESIS STRATEGY

NEW DERIVATIVES OF BUTYRIC ACID

N-(BENZTHIAZOL-2-YL)-OXAMIC ACID DERIVATIVES

3-ALKOXY-2-AMINOPROPYLAMIDES

ARTIFICIAL SWEETENING AGENT

AMINO-METHYL SUBSTITUTED TETRACYCLINE COMPOUNDS

SUBSTITUTED ETHANELAMINES AND OXAZOLIDINES

INHIBITOR OF DENATURED LDL FORMATION

Indene derivatives as pharmaceutical agents

ALLOPHANYLPIPERAZINE DERIVATIVES

CINNAMOYL PIPERAZINES AND HOMOPIPERAZINES

METHYLATED ANILINES

Carbamoyloxy derivatives of mutiline and their use as antibacterials

NF-kappa inhibitors containing as the active ingredient phenylmethyl benzoquinone

Cationic methylenedioxy benzenes, their use for oxidation dyeing of keratin fibres, dyeing compositions and methods

METHYLENE DIOXYBENZENES AND BENZO 1,4 DIOXENS

SULFAMOYLBENZOIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION

LIGANDS FOR METALS AND METAL-CATALYZED PROCESSES

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon- heteroatom and carbon-carbon bond-forming reactions. The subject processes provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

ANTIHYPERTENSIVE N-PIPERAZINYLALKANOYLANILIDES

ANTIHYPERTENSIVE N-PIPERAZINYLALKANOYLANILIDES

TITLE: Antihypertensive N-Piperazinylalkanoylanilides N-piperazinylalkanoylanilides of formula (I) wherein n is 0, 1 or 2, each of R and R1 is H or alkyl, and each of R2,R3 and R4 is H, halogen, alkyl, hydroxyalkyl, alkoxy, aralkoxy, alkylthio, aralkylthio, alkylsulphonyl, alkylsulphenyl, NO2, NH2, alkylamino, acylamino, ureido, alkylureido, alkylsulphonylamino, CF3, acyl, CN, COOH, alkoxycarbonyl, NH2CO, SO3H, guanidinosulphonyl, NH2COO, OH, acyloxy, alkylsulphonyloxy,alkylenedioxy or SO2NR5R6 wherein each of R5 and R6 is H, alkyl, aryl or acyl, and their pharmaceutically acceptable acid addition salts, are antihypertensive agents. They may be prepared by condensing 1-(2-methoxyphenyl)- -piperazine with an alkanoylanilide of formula (II) (III) ...

METHOD FOR TREATING PAIN, ANXIETY OR DEPRESSION USING CARBAMOYLOXY ALKANOYL PIPERAZINE COMPOUND

There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof. 126-. (canceled)28. The method of claim 27 , wherein the compound is administered as a pharmaceutical composition comprising a pharmaceutically acceptable carrier.29. The method of claim 27 , wherein the pain is selected from the group consisting of acute pain claim 27 , chronic pain claim 27 , neuropathic pain claim 27 , post-surgery neuropathic pain claim 27 , diabetic neuropathic pain claim 27 , postherpetic neuralgia claim 27 , inflammatory pain claim 27 , joint pain and migraine headache.30. The method of claim 27 , wherein the pain is neuropathic pain or inflammatory pain.31. The method of claim 30 , wherein the pain is neuropathic pain.32. The method of claim 27 , wherein the compound is orally administered.33. The method of claim 27 , wherein the therapeutically effect amount is in the range of 10 to 500 mg.36. The method of claim 35 , wherein Xis straight- or branched-chain C-Calkoxy.37. The method of claim 36 , wherein Xis two methoxy substituents.38. The method of claim 27 , which is selected from the group consisting of:carbamic acid 3-[4-(4-fluoro-phenyl)-piperazin-1-yl]-3-oxo-1-phenyl-propyl ester,carbamic acid 3-[4-(4-methoxy-phenyl)-piperazin-1-yl]-3-oxo-1-phenyl-propyl ester,carbamic acid 3-[4-(3,4-dichloro-phenyl)-piperazin-1-yl]-3-oxo-1-phenyl-propyl ester,carbamic acid 3-oxo-1-phenyl-3-(4-p-tolyl-piperazin-1-yl)-propyl ester,carbamic acid 3-[4-(3,4-dimethoxy-phenyl)-piperazin-1-yl]-3-oxo-1-phenyl-propyl ester,carbamic ...

TRANSITION-METAL-FREE N-ARYLATION OF TERTIARY AMINES USING ARYNES

The present invention relates to transition-metal-free process for the synthesis of tertiary arylamines comprises coupling reaction between arynes and N,N-dimethyl aniline compounds in presence of 18-crown-6, KF and THF. 2. The process according to claim 1 , wherein the 2-trimethylsilylaryl trifluoromethyl sulphonate are selected from the group consisting of 3 claim 1 ,6-dimethyl-2-(trimethylsilyl)phenyl trifluoromethanesulfonate claim 1 , 4 claim 1 ,5-dimethyl-2-(trimethylsilyl)phenyl trifluoromethanesulfonate claim 1 , 6-(trimethylsilyl)benzo[d][1 claim 1 ,3]dioxol-5-yl trifluoromethanesulfonate claim 1 , 4 claim 1 ,5-difluoro-2-(trimethylsilyl)phenyl tri-fluoromethanesulfonate claim 1 , 3 claim 1 ,6-dimethyl-2-(trimethylsilyl)phenyl trifluoromethanesulfonate claim 1 , 2-methoxy-6-(trimethylsilyl)phenyl trifluoromethanesulfonate claim 1 , 2-(trimethylsilyl)-naphthalen-1-yl trifluoromethanesulfonate claim 1 , 4-methyl-2-(trimethylsilyl)-phenyl trifluoromethanesulfonate.3. The process according to claim 1 , wherein the tertiary amine compounds are selected from the group consisting of N claim 1 ,N-diethylaniline claim 1 , N-methyl-N-phenylaniline claim 1 , N claim 1 ,N-dimethylaniline claim 1 , N claim 1 ,N claim 1 ,4-trimethylaniline claim 1 , 3-(dimethylamino)phenol claim 1 , 4-bromo-N claim 1 ,N-dimethylaniline claim 1 , 4-iodo-N claim 1 ,N-dimethyl aniline claim 1 , 4-(dimethylamino)benzonitrile claim 1 , ethyl 4-(dimethylamino)benzoate claim 1 , 4-(dimethylamino)benzaldehyde claim 1 , N claim 1 ,N claim 1 ,3-trimethylaniline claim 1 , 3-bromo-N claim 1 ,N-dimethylaniline claim 1 , methyl 2-(dimethylamino)benzoate claim 1 , N claim 1 ,N claim 1 ,3 claim 1 ,5-tetramethyl aniline claim 1 , diethyl (4-(dimethylamino)benzyl)phosphonate claim 1 , (E)-N claim 1 ,N-dimethyl-4-(2-(thiophen-2-yl)vinyl)aniline claim 1 , N claim 1 ,N-dimethyl-4-(phenylethynyl)aniline claim 1 , N claim 1 ,N-dimethyl naphthalen-1-amine claim 1 , 5-(dimethyl-amino)naphthalene-1-sulfonyl ...

Human glut5 specific inhibitors and methods of treatment

The present invention relates to compounds which have been discovered to be potent ligands (inhibitors) of human GLUT5 (glucose transporter type 5), a facilitative glucose transporter that transports fructose, and their use as ligands assays which can uncover additional ligands of GLUT5, having the potential for being used as drugs. In addition, the present invention is directed to compounds, chemical compositions and methods for treating disease states and conditions which are mediated through GLUT5, including such disease states and conditions as GLUT5 deficiency syndrome, diabetes (type I and II), cancer, metabolic diseases including metabolic syndrome and fatty liver disease, among others.

ORTHO-ALKYNYL ANILINES AND PROCESS FOR PREPARATION THEREOF

The present invention relates to novel ortho alkynyl anilines of formula (I) which are useful in synthesis of drug intermediates and natural products and process for preparation of these ortho alkynyl anilines of formula (I) via copper catalyzed Multi Component Reactions (MCR). [Formula should be inserted here] Formula (I) 2. The compounds as claimed in claim 1 , wherein said compounds of formula (I) are selected from the group consisting of:i. Dibenzyl1-(2-(3-ethoxy-3-oxoprop-1-yn-1-yl)phenyl)hydrazine-1,2-dicarboxylate;ii. Dibenzyl1-(2-(3-ethoxy-3-oxoprop-1-yn-1-yl)-4,5-dimethoxyphenyl)hydrazine-1,2-dicarboxylate,iii. Dibenzyl1-(6-(3-ethoxy-3-oxoprop-1-yn-1-yl)benzo[d][1,3]dioxol-5-yl)hydrazine-1,2-dicarboxylate andiv. Dibenzyl1-(2-(3-ethoxy-3 -oxoprop-1-yn-1-yl)-4,5-dimethylphenyl) hydrazine-1,2-dicarboxylate.3. A one-pot process for the preparation of compound of formula (I) comprising the steps of:i. stirring the reaction mixture of (trimethylsilyl) aryl triflates with terminal alkyne and azodicarboxylate in presence of copper catalyst, cesium fluoride and solvent at temperature in the range of 80 to 110° C. for the period ranging from 8 to 15 h to obtain a mixture;ii. cooling the mixture as obtained in step (i) at room temperature in the range of 20 to 30° C. followed by filtering and purifying to obtain compound of formula 1.4. The process as claimed in claim 3 , wherein stirring is carried out at temperature ranging from 80 to 110° C.5. The process as claimed in claim 3 , wherein said copper catalyst used is copper (I) salt selected from the group consisting of copper chloride claim 3 , copper bromide claim 3 , copper iodide.6. The process as claimed in claim 3 , wherein (trimethylsilyl) aryl triflates are selected from the group consisting of 2-(trimethylsilyl)phenyl trifluoromethanesulfonate claim 3 , 4 claim 3 ,5-dimethoxy-2-(trimethylsilyl)phenyl trifluoromethanesulfonate claim 3 , 6-(trimethylsilyl)benzo[d][1 claim 3 ,3]dioxol-5-yl trifluoromethane- ...

METHOD FOR COUPLING A FIRST COMPOUND TO A SECOND COMPOUND

The present disclosure describes a method of coupling a first compound to a second compound, the method comprising: providing the first compound having a fluorosulfonate substituent; providing the second compound comprising an amine; and reacting the first compound and the second compound in a reaction mixture, the reaction mixture including a catalyst having at least one group 10 atom, the reaction mixture under conditions effective to couple the first compound to the second compound. The present disclosure further describes a one-pot method for coupling a first compound to a second compound. 1. A method of coupling a first compound to a second compound , the method comprising:{'sub': '2', 'providing the first compound having a fluorosulfonate substituent substituent of the formula —OSOF, the first compound comprising an aryl or a heteroaryl group;'}providing the second compound comprising an amine; andreacting the first compound and the second compound in a reaction mixture, the reaction mixture including a catalyst having at least one group 10 atom, the reaction mixture under conditions effective to couple the first compound to the second compound.2. The method of claim 1 , wherein the reaction mixture further includes a ligand.3. The method of wherein the catalyst is generated in-situ from a palladium precatalyst.4. The method of wherein the catalyst is generated in-situ from a palladium precatalyst claim 1 , the palladium precatalyst is selected from the group consisting of: Palladium(II) acetate claim 1 , Palladium(II) chloride claim 1 , Dichlorobis(acetonitrile)palladium(II) claim 1 , Dichlorobis(benzonitrile)palladium(II) claim 1 , Allylpalladium chloride dimer claim 1 , Palladium(II) acetylacetonate claim 1 , Palladium(II) bromideBis(dibenzylideneacetone)palladium(0) claim 1 , Bis(2-methylallyl)palladium chloride dimer claim 1 , Crotylpalladium chloride dimer claim 1 , Dichloro(1 claim 1 ,5-cyclooctadiene)palladium(II) claim 1 , Dichloro(norbornadiene) ...

New catechol molecules and their use as inhibitors to p450 related metabolic pathways

The present invention relates to the new catechol molecules and their use as inhibitors to P450 related metabolic pathways. The invention further relates to a method of controlling crop pests and/ or non-crop pests that are resistant to one or more insecticide(s) and method of controlling undesired vegetation that are resistant to one or more herbicide(s) by applying at least one inhibitor to P450 related metabolic pathways of formula (I).

Method of obtaining derivatives of n-(benzthiazolyl-2)-oxamine acids or esters of same or salts thereof

Method for preparing substituted 3- (2/4-phenyl-1-piperazinyl / -ethyl) indolines or their salts or their quaternary ammonium salts

Method of preparing indoline derivatives

A kind of preparation method and application of amine and imines N-methyl

本发明公开了一种胺和亚胺氮甲基化的制备方法及应用，步骤是：A、在舒伦克管中加入活性炭负载铂催化剂，抽真空换氩气后，加入溶剂；B、在氩气保护下，分别加入苯硅烷、起始原料和甲酸；C、整个反应体系在一定温度下搅拌进行反应；D、反应结束后，向体系中加入乙酸乙酯稀释，以氢氧化钠水溶液淬灭反应，乙酸乙酯萃取，分离出有机相后，干燥，过滤，旋转蒸发除去溶剂。残留物经不同比例的乙酸乙酯/石油醚混合溶剂柱层析，得到目标产物。该方法在同位素标记药物合成中的应用，催化剂用量极低，成本十分低廉，适合大规模生产，可适用于不同取代基的胺和亚胺，适合在天然产物结构中的氮原子上便利的实现甲基化，制备药物分子。

New sulfo-imido acid and amidine insecticides

本发明涉及一类杀虫化合物，其结构式为： 其中R是有选择取代的芳基；R 2 是有选择取代 的烷基，环烷基或烯基，X是硫，氨基或C 1 -C 4 -烷基 氨基；并且R 3 是：(a)有选择取代的3-苯氧基苯烷 基，3-苯氧基吡啶基烷基或3-(4-吡啶基氧基)苯烷 基；(b)五氟苄基；或(c)2-甲基-3-苯基苄基。

Novel cinnamoylpiperadine and homopiperadines and method for its production

Method for producing substituted indolines

Process for the production of 4-phenyl-2(1h)-quinazolinones

Patent FR2374317B1

NEW DERIVATIVES OF 3,3-DICHLORO-2-AZETIDINONE, USEFUL IN PARTICULAR AS ANTI-INFLAMMATORY AGENTS

Les médicaments selon l'invention sont des composés de formule générale :

Patent FR2139158A1

NOVEL CATIONIC DI-METHYLENEDIOXY-BENZENES, THEIR USE FOR OXIDATION DYEING OF KERATINIC FIBERS, TINCTORIAL COMPOSITIONS AND DYEING METHODS

Antimicrobial n-subst 6,7-methylenedioxy-4- - quinolone derivs prepn

1-Substd. 6,7-methylenedioxy-4-quinolone-3-carboxylic acid derivs. of formula (I): (where R is alkyl or alkenyl and R1 is H or alkyl) are prepd. by condensing a dialkyl N-substd. -3,4-methylenedioxyanilinomethylene malonate of formula (II): (where R1' is the same alkyl as defined for R1) at 0-200 degrees C using an acid anhydride, an acid, or mixtures of these, to obtain cpd. (I) or the 1-substd. 3-alkoxycarbonyl-4-halo-6,7-methylenedioxy quinolinium salt of formula (III): (where X and Y are halogen). Cpd. (III) is reacted at 0-200 degrees C with a cpd. R2-OH (where R2 is H or alkyl) to obtain (I). Cpds. (I) are specif. used in antimicrobial compns.

Cationic di-methylene- dioxy-benzenes for use as oxidation dye precursors in compositions for oxidation-dyeing of keratin fibres, contain at least one cationic group including quaternized cycles

Cationic di-methylene -dioxy-benzenes are new. Cationic methylene-dioxy- benzenes (claimed together with their acid-addition salts) have formula (I); B = (preferably 1-14C) linear or branched alkyl chain, which may be interrupted with Z group(s) and/or one or more heteroatoms (N, O or S), and optionally substituted with hydroxyl(s) or 1-6C alkoxy radicals, and may have ketone group(s); Ra, Rb, Ra' and Rb' = H, (1-6C)alkyl radical or hydroxy (1-6C)alkyl radical, or form together with C atom to which they are attached a saturated 5,6 or 7C cycle; R1-R3 and R1'-R3' = H, halogen atom, one of two valencies of B, group Z, group A2, group A2', 1-6C alkyl radical, (1-6C)alkyl carbonyl-, amino(1-6C)alkyl carbonyl-, N-Z-amino-(1-6C) alkylcarbonyl-, N-(1-6C)alkyl-amino-(1-6C) alkylcarbonyl-, etc.; R6 and R6' = 1-6C alkyl radical, mono- hydroxy (1-6C) alkyl, polyhydroxy (2-6C) alkyl, group Z, aryl (or benzyl) radical, trifluoro-, mono(or poly)- hydroxy-, (1-6C)-alkoxy-, cyano-, carbamyl-, N-(or N,N) (1-6C)-(di) alkylcarbamyl- radicals etc. A1 = -NR4R5 or hydroxyl radical; A1' = -NR4'R5' or hydroxyl radical; A2 = NR4''R5'' or hydroxyl radical; A2' = NR4'''R5''' or hydroxyl radical; R4, R5, R4', R5', R4'', R5'', R4''' and R5''' = one of two valencies of B, or H, Z, 1-6C alkyl radical, mono- hydroxy (1-6C) alkyl, polyhydroxy (2-6C) alkyl, aryl (or benzyl) radical, trifluoro-, sulfo-, thiocarbamyl-, cyano-, carbamyl, N-(1-6C)alkyl-carbamyl or N,N-di (1-6C) alkyl carbamyl, (1-6C)-alkyl-carboxy-, (1-6C) alkyl carbonyl-, (1-6C)alkyl sulfinyl-, aminosulfonyl-, N-Z-aminosulfonyl-, N-(1-6C)alkyl-aminosulfonyl-, N,N-di(1-6C)alkyl-aminosulfonyl-, and amino- (1-6C)alkyl radicals; Z = unsaturated cationic groups of formula (II) and (III), or saturated cationic groups of formula (IV); D = (preferably 1-14C) linear or branched alkyl chain, which may be interrupted ...

NOVEL NITROAMINOPHENOLS, PROCESS FOR THEIR PREPARATION AND THEIR USE IN DYEING KERATIN FIBERS, NEW INTERMEDIATE NITROAMINOBENZENES AND THEIR USE IN DYING KERATIN FIBERS

L'INVENTION CONCERNE UN NITROAMINOPHENOL DE FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE Z DESIGNE -CHW, W REPRESENTANT H, ALKYLE EN C-C, HYDROXYALKYLE EN C-C, POLYHYDROXYALKYLE EN C-C, ALCOXY (C-C) ALKYLE (C-C), HYDROXYALCOXY (C-C)ALKYLE (C-C) ET R DESIGNE H, ALKYLE (C-C) HYDROXYALKYLE EN C-C, POLYHYDROXYALKYLE EN C-C OU ALCOXY (C-C)ALKYLE (C-C), SON PROCEDE DE PREPARATION ET LE COMPOSE INTERMEDIAIRE DE FORMULE: (CF DESSIN DANS BOPI) OU R DESIGNE HYDROXYALKYLE EN C-C, POLYHYDROXYALKYLE EN C-C OU ALCOXY (C-C)ALKYLE (C-C) ET SON PROCEDE DE PREPARATION. LES COLORANTS DE FORMULE I ET II SONT UTILISABLES EN TEINTURE DIRECTE DES FIBRES KERATINIQUES, NOTAMMENT DES CHEVEUX HUMAINS. THE INVENTION RELATES TO A NITROAMINOPHENOL OF FORMULA: (CF DRAWING IN BOPI) IN WHICH Z DESIGNATES -CHW, W REPRESENTING H, ALKYL CC, HYDROXYALKYL CC, POLYHYDROXYALKYL CC, ALCOXY (CC) ALKYDRO (CC) ) ALKYL (CC) AND R DESIGNATES H, ALKYL (CC) HYDROXYALKYL IN CC, POLYHYDROXYALKYL IN CC OR ALCOXY (CC) ALKYL (CC), ITS PREPARATION PROCESS AND THE INTERMEDIATE COMPOUND OF FORMULA: (CF DRAWING IN BOPI) OR R DESIGNATED CC HYDROXYALKYL, CC POLYHYDROXYALKYL OR ALCOXY (CC) ALKYL (CC) AND ITS PREPARATION PROCESS. THE COLORANTS OF FORMULA I AND II CAN BE USED IN DIRECT DYING OF KERATINIC FIBERS, ESPECIALLY OF HUMAN HAIR.

NEW TRIMETHOXY CINNAMOYLES PIPERAZINES, THEIR PREPARATION PROCESS AND THEIR THERAPEUTIC APPLICATION

a. Nouvelles triméthoxy-3, 4, 5 cinnamoyles pipérazines. b. Ces composés répondent plus précisément à la formule générale : at. New trimethoxy-3, 4, 5 cinnamoyles piperazines. b. These compounds correspond more precisely to the general formula:

Patent FR2139158B1

Tri:methoxy cinnamoyl piperazine(s) - for treatment of cardiovascular disorders

Trimethoxy cinnamoyl piperazine derivatives of formula (I) and their salts, are new: where either X=0 and Ar= (IV)-(X). R= 2-ethyl -n-butyl, cyclopropylmethyl, cyclobutyl methyl, cyclobutyl ethyl, cyclopentyl methyl, 2-(diethylamino) ethyl, 3-methyl-n-butyl (in which case the cpd. (I) has the S (-) structure; n=1 or 3; m=1 or 2).

Novel cinnamoyles piperazines and homopiperazines,the method of preparing them and their application in therapeutics

PROCEDURE FOR THE PREPARATION OF ETHYL-8-HYDROXY-1,3-DIOXOLO (4.5G) QUINOLINE-7-CARBOXYLATE

The method of obtaining 1-alkyl-4-phenyl-2 (1H) quinazolinone

9-aminomethyl substituted minocycline compounds

The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and minocycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

N- (BENZTHIAZOL-2-YL) -OXAMID ACID DERIVATIVES AND METHOD FOR THE PRODUCTION THEREOF

Patent FI50973B

Fungicidal aniline derivatives

A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly strains thereof which are resistant to benzimidazole or thiophanate fungicides and/or cyclic imide fungicides.

Patent HU167203B

Novel imidate insecticides

A series of novel imidate insecticides distinguished by the general formula ##STR1## in which R 1 is an optionally substituted aryl group in which the substituents are halo, C 1 -C 4 alkyl, C 1 -C 4 haloalkoxy, C 1 -C 4 alkoxy, C 1 -C 4 haloalkylthio, C 3 -C 6 cycloalkyl, nitro, C 1 -C 4 haloalkyl, C 2 -C 5 carboalkoxy, C 1 -C 4 alkylthio, cyano, C 1 -C 4 alkylsulfonyl, C 1 -C 4 haloalkylsulfonyl, C 2 -C 5 alkylcarbonyl, C 2 -C 4 alkyleneoxy, C 1 -C 2 perhaloalkyleneoxy, C 1 -C 4 alkylenedioxy, C 1 -C 3 halo-substituted alkylenedioxy, phenyl, mono-substituted phenyl, pyridyloxy, C 2 -C 4 alkylene, C 2 -C 4 alkenyl, C 3 -haloalkenoxy, and/or amido; R 2 is cyclopropyl or mono- or poly- halo- or methyl-substituted cyclopropyl; and R 3 is (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl, 3-(pyridyloxy)phenalkyl moiety; 3-phenylaminophenalkyl, 3-benzylphenalkyl or benzyloxyphenalkyl moiety; (b) a benzylfuranylmethyl moiety; (c) a 3- or 4-substituted benzyl or tetrafluorobenzyl moiety; (d) 4-phenoxy-2-butyn-2-yl; (e) 2-methyl-3-phenylbenzyl, or (f) 4-(4-trifluoromethyl-2-pyridyloxy)benzyl.

Preparation of n-substituted 6,7-methylenedioxy-4-quinolone derivatives

Process for preparing new substituted 3-(2-/4-phenyl-1-piperazinyl/ethyl)indolines

Dyeing compositions for keratinous fibres, especially for human hair, containing oxidation dye precursors and heterocyclic couplers

The invention relates to a dyeing composition for keratinous fibres containing, in a cosmetically acceptable solvent medium, at least one para-type oxidation dye precursor in combination with at least one heterocyclic coupler of formula: ##STR1## in which R denotes a hydrogen atom, a C 1 -C 4 radical, a C 2 -C 4 hydroxyalkyl radical, a C 3 to C 6 polyhydroxyalkyl radical, or a C 2 -C 6 alkoxyalkyl radical, Z, independently of R, denotes a C 1 to C 4 alkyl radical, a C 2 to C 4 hydroxyalkyl radical, a C 3 to C 6 polyhydroxyalkyl radical, a C 2 -C 6 alkoxyalkyl radical or a trifluoroethyl radical, R 1 and R 2 independently of each other denote a hydrogen atom or a C 1 to C 4 alkyl radical, or one of the addition salts of the compound of formula (I) with an inorganic acid, a process for the oxidation dyeing of hair using this composition as well as the new couplers of formula (I) where Z is other than methyl when R 1 , R 2 and R=H, the process for their preparation, the new intermediate compounds of formula: ##STR2## and the process for their preparation.

N,n-diallyl-3,7,11-trimethyl-2,6,10-dodecatrienylamine

NEW TERPENOID COMPOUNDS, THEIR MANUFACTURE AND USE FOR INFLUENCING THE DEVELOPMENT OF INSECTS AND REPRESENTATIVES OF THE ORDER ACARINA. THE COMPOUNDS CORRESPOND TO THE FORMULA H3C-C(-Z1)(-R4)-CH(-Z2)-CH2-CH2-C(-R3)=CH-CH2-CH2- C(-CH3)=CH-CH2-N(-R1)-R2 WHEREIN Z1 AND Z2 ARE EACH HYDROGEN OR TOGETHER FORM A CARBON CARBON BOND OR AN OXYGEN BRIDGE, R1 IS C2-C4 ALKENYL, C2-C4 ALKINYL, CYCLOALKYL, C2-C4 HALOALKYL, SUBSTITUTED PHENYL, C2-C4 HALOLAKENYL OR ACYL, AND R2 IS HYDROGEN, C1-C4 ALKYL, C2-C4 ALKENYL, C2-C4 ALKINYL OR ACYL, OR R1 IS HYDROGEN, AND R2 IS C1-C4 ALKYL, OR R1 AND R2 TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED FORM A 3-MEMBERED RING, OR R1 AND R2 ARE EACH ACYL GROUPS WHICH, WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED FORM A SUBSTITUTED OR UNSUBSTITUTED HETEROCYCLIC RING, AND R3 AND R4 ARE EACH METHYL OR ETTHYL.

TINCTORIAL COMPOSITIONS FOR KERATINIC FIBERS IN PARTICULAR FOR HUMAN HAIR CONTAINING OXIDATION DYE PRECURSORS AND HETEROCYCLIC COUPLERS, DYEING PROCESS USING THE SAME, NEW HETEROCYCLIC COUPLERS AND PROCESS THEREOF

3,3-DICHLORO-2-AZETIDINONE DERIVATIVES, MEDICINAL PRODUCTS CONTAINING THESE DERIVATIVES AND USES

Patent PL92635B1

Method for preparing substituted 3- (2-4phenyl-1-piperazinyl-ethyl) -indolines or their salts, or their quaternary ammonium salts

4-Hydroxyl, 3-benzene dimethanol derivatives

Proceed «for the production of 8-hydroxy-1,3-dioxolo square brackets on 4.5-g square brackets to ethyl quinoline-7carboxylate

ARRANGEMENT FOR DETECTING AN OPTICAL TAPE IN A MAGNETIC TAPE CASSETTE.

Cationic di-methylenedioxy-benzenes, their use for oxidation dyeing of keratin fibres

The subject of the invention is novel dimethylenedioxybenzenes comprising at least one cationic group Z, Z being chosen from quaternized aliphatic chains, aliphatic chains comprising at least one quaternized saturated ring, and aliphatic chains comprising at least one quaternized unsaturated ring, their use as oxidation dye precursor for the oxidation dyeing of keratinous fibres, dyeing compositions containing them, as well as the oxidation dyeing methods using them.

Imidazo-and pyrimido-(2,7-b)-quinazolin-2-ones

METHOD OF ANALOGY FOR THE PREPARATION OF 2-HYDROXY-2- (4-HYDROXY-3- (HYDROXYMETHYL) -PHENYL) ETHYLAMINES OR SALTS THEREOF OR HYDRATES OF THE COMPOUNDS OR SALTS THEREOF

Process for the preparation of ethyl 8-hydroxy-1,3-dioxolo / 4.5 g / quinoline n-7-carboxylate.

Derivatives of 3-2-1-piperazinyl-ethyl- indoline

1382916 3-(2-Piperazinoethyl)-indoline derivatives AMERICAN CYANAMID CO 3 May 1972 [27 May 1971] 20674/72 Heading C2C The invention comprises compounds of formula and their pharmacologically acceptable acid addition and quaternary ammonium salts, wherein R 1 is H, Cl, Br, C 1-4 alkoxy, NO 2 , NH 2 , MeCOHN or Me 2 N, and R 2 is H, C 1-4 alkoxy or NO 2 (or R 1 -R 2 may be -OCH 2 O-); R 3 and R 4 are each H or Me; and R 5 is H, Cl, MeO, Me or CF 3 . These compounds are prepared by (1) reducing the corresponding indole; (2) reacting a corresponding 1 - acyl - 3 - XCH 2 CH 2 - indo- line (where X is Cl, Br, MeSO 3 or p-TsO) with a 4-phenylpiperazine, and removing by hydrolysis the 1-acyl groups from the 1-acyl derivative of I thus formed. Also prepared is an intermediate of Formula I where R 1 = MeO, R 2 = NH 2 , R 3 = Me and R 4 = R 5 = H.

Improvements in or relating to organic compounds

TINCTORIAL COMPOSITIONS FOR KERATINIC FIBERS IN PARTICULAR FOR HUMAN HAIR CONTAINING OXIDATION DYE PRECURSORS AND HETEROCYCLIC COUPLERS, DYEING PROCESS USING THE SAME, NEW HETEROCYCLIC COUPLERS AND PROCESS THEREOF

L'INVENTION CONCERNE UNE COMPOSITION TINCTORIALE POUR FIBRES KERATINIQUES CONTENANT DANS UN MILIEU SOLVANT COSMETIQUEMENT ACCEPTABLE, AU MOINS UN PRECURSEUR DE COLORANT D'OXYDATION DE TYPE PARA EN ASSOCIATION AVEC AU MOINS UN COUPLEUR HETEROCYCLIQUE DE FORMULE : (CF DESSIN DANS BOPI) DANS LAQUELLE R REPRESENTE UN ATOME D'HYDROGENE, UN RADICAL ALKYLE EN C-C, UN RADICAL HYDROXYALKYLE EN C-C, UN RADICAL POLYHYDROXYALKYLE EN C A C, UN RADICAL ALCOXYALKYLE EN C-C, Z, INDEPENDAMMENT DE R, REPRESENTE UN RADICAL ALKYLE EN C A C, UN RADICAL HYDROXYALKYLE EN C A C, UN RADICAL POLYHYDROXYALKYLE EN C A C, UN RADICAL ALCOXYALKYLE EN C-C OU UN RADICAL TRIFLUOROETHYLE, R ET R DESIGNENT INDEPENDAMMENT L'UN DE L'AUTRE UN ATOME D'HYDROGENE OU UN RADICAL ALKYLE EN C A C, OU L'UN DES SELS D'ADDITION AVEC UN ACIDE MINERAL DU COMPOSE DE FORMULE I, UN PROCEDE DE TEINTURE D'OXYDATION DES CHEVEUX A L'AIDE DE CETTE COMPOSITION AINSI QUE LES NOUVEAUX COUPLEURS DE FORMULE I OU Z EST DIFFERENT DE METHYLE LORSQUE R, R ET R H ET LEUR PROCEDE DE PREPARATION. THE INVENTION CONCERNS A TINCTORIAL COMPOSITION FOR KERATINIC FIBERS CONTAINING, IN A COSMETICALLY ACCEPTABLE SOLVENT MEDIUM, AT LEAST ONE PARA-TYPE OXIDIZATION DYE PRECURSOR IN ASSOCIATION WITH AT LEAST ONE HETEROCYCLIC COUPLER OF FORMULA: BOPI IN THE FORMULA: (CF DESSIN) REPRESENTS A HYDROGEN ATOM, A CC RADICAL ALKYL, A CC HYDROXYALKYL RADICAL, A CAC POLYHYDROXYALKYL RADICAL, A CC, Z ALCOXYALKYL RADICAL, INDEPENDENT OF R, REPRESENTS A HYDROXYALKYL RADICAL, CAC RADICAL A CAC POLYHYDROXYALKYL RADICAL, A CC ALCOXYALKYL RADICAL OR A TRIFLUOROETHYL RADICAL, R AND R SHALL INDEPENDENTLY DESIGNATE A HYDROGEN ATOM OR A CAC RADICAL ALKYL, OR ONE OF THE ADDITIONAL SALTS WITH A MINERAL ACID OF THE COMPOUND OF FORMULA I, A PROCESS FOR DYING OXIDIZING HAIR USING THIS COMPOSITION AS WELL AS THE NEW COUPLERS OF FORMULA I OR Z IS DIFFERENT FROM METHYL WHEN R , R AND R H AND THEIR PREPARATION METHOD.

Isothioureido isoindolediones and their use as plant growth regulators

Piperazine derivatives as blood circulation-enhancing substances

Aniline derivative, preparation thereof, and agricultural and horticultural fungicide containing said derivative as active component

(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。

A PIPERAZINILALCANOILANILIDA

Preparation method of sulfonyl formamidine derivative

本发明涉及一种磺酰基甲脒衍生物的制备方法,包括如下步骤：将胺类化合物与端炔酮类化合物、磺酰基叠氮反应，得到所述磺酰基甲脒衍生物。本发明的制备方法具有产物产率高、纯度高、原子经济性高等诸多优点，具有良好的科研价值和应用前景，为磺酰基甲脒衍生物的制备提供了全新路线，可在药物中间体、农药中间体等领域中发挥重要作用，降低生产成本，在工业和科研上具有良好的应用价值和潜力。

PROCEDURE FOR PREPARING 3- (PHENYL-PIPERAZINYL) ETHYLINDOLINES

NEW BENZODIOXAN AND BENZODIOXOLAN COMPOUNDS.

Piperazine derivatives as circulation-enhancing substances

ABSTRACT OF THE DISCLOSURE Novel N-(trimethoxybenzyl)-piperazines of the formula: (I), wherein A = , wherein R is trifluoromethyl, hydroxy, nitro, halogen, lower-alkyl, or lower-alkoxy; R' is hydrogen, trifluoromethyl, halogen, lower-alkyl, or lower-alkoxy; R" is hydrogen or lower-alkoxy, or wherein R and either R' or R" together stand for lower-alkylene dioxy, and acid addition salts thereof, a method of preparing same, pharmaceutical compositions thereof, and a method of enhancing circulation, especially cerebrovascular circulation, therewith, are disclosed.

Isothioureido isoindole-diones

PROCEDURE FOR PREPARATION OF BENZENDIMETHANE DERIVATIVES WITH PHARMACOLOGICAL EFFECT

Arylpiperazines

Patent FR2160385B1

Patent JPS5516424B2

A method of reduction thioamide analog compound

本发明提供了一种还原硫代酰胺类化合的方法，在80℃以及氮气保护条件下，以硫代酰胺为底物，加入自由基引发剂二叔丁氧基叠氮(TBHN)，4‑二甲氨基吡啶硼烷络合物(DMAP‑BH 3 )，以及催化量的苯硫酚，在乙腈中搅拌适当时间即可得到相应的胺。用三乙基硼/氧气做引发剂，25℃条件下，也能实现相同的转化。该反应具有无毒，反应条件温和，操作方便，官能团容忍性好，反应时间短，反应效率高等优点。

Isothioureido isoindolediones and use as plant agrowth regulators

Insecticide

Photographic colour material

1351789 Dioxolo- and dioxanoquinoxalines CIBA-GEIGY AG 2 Sept 1971 [4 Sept 1970] 41052/71 Heading C2C [Also in Division G2] The invention comprises compounds of general formula in which A 1 and A 2 are independently an alkyl group having 1-5 carbon atoms, a mono- or bicyclic aralkyl group having 1-5 carbon atoms in the alkyl moiety, a mono- or bicyclic aryl group or a 5 or 6-membered heterocyclic group having N, O or S as heteroatom, and n = 1 or 2, the oxygen-containing ring being connected to the quinoxaline ring in the 5, 6 or 6, 7 positions. The most preferred compounds are those in which A 2 is methyl and A 1 is phenyl or methyl. The compounds may be prepared by reacting the corresponding aromatic 1,2-diamine, optionally prepared in situ from the corresponding dinitro compound, with a 1,2-dicarbonyl compound, an α-substituted ketone in which the substituent is a nucleophilic group, e.g. halogen or OH, or an α-oxminoketone. The compounds of Formula I can be used as colour bleaching catalysts in photographic processes.

Acrylate compound, preparation process thereof and fungicide using the same

Novel thioimidate and amidine insecticides

Insecticidal compounds having the formula

Ortho-alkynyl anilines and process for preparation thereof

The present invention relates to novel ortho alkynyl anilines of formula (I) which are useful in synthesis of drug intermediates and natural products and process for preparation of these ortho alkynyl anilines of formula (I) via copper catalyzed Multi Component Reactions (MCR).

Patent FR2173988A1

3-(2-(4-phenyl-1-piperazinyl)-ethyl)indolines

THIS DISCLOSURE DESCRIBES COMPOUNDS OF THE CLASS OF SUBSTITUTED 3 - (2-(4-PHENYL-1-PIPERAZINYL)ETHYL)INDOLINES USEFUL AS TRANQUILIZING AGENTS.

Antimicrobial n-subst 6,7-methylenedioxy-4- - quinolone derivs prepn

3,3-dichloro-2-azetidinone derivatives

Abstract Compounds having the formula

Imidates with insecticidal activity.

Indolylacetic acid derivatives

NOVEL INDOLYLACETIC ACID DERIVATIVES, WHICH HAVE EXCELLENT ANTI-INFLAMMATORY, ANTIPYRETIC AND ANALGESIC ACTIVITIES, REPRESENTED BY THE FORMULA, 1-(R3-(A)M-CO-),2-R2,3-(R4-OOC-CH(-R1)-),5,6-(-X1-(CH2)N- X2-)INDOLE 1,2-(-X1-(CH2)N-X2-),4-(B=N-NH-)BENZENE WHEREIN X1, X2 AND N ARE THE SAME AS DEFINED ABOVE AND B IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF (-H)2 AND X (WHEREIN Z IS A NITROGEN PROTECTING SYSTEM COMPRISING AT LEAST ONE READILY REMOVABLE GROUP), WITH AN ACID HALIDE REPRESENTED BY THE FORMULA, R3-(A)M-CO-HAL WHEREIN R3, A AND M ARE THE SAME AS DEFINED ABOVE AND HAL IS HALOGEN, TO OBTAIN N1-ACYLATED COMPOUND OF THE FORMULA, 1,2-(-X1-(CH2)N-X2-),4-(R3-(A)M-CO-N(-N=B)-)BENZENE WHEREIN X1, X2 R3, A, B, M AND N ARE THE SAME AS DEFINED ABOVE, THEN REACTING THE RESULTANT N1-ACYLATED COMPOUND (II) WITH AN ALIPHATIC ACID DERIVATIVE REPRESENTED BY THE FORMULA, R2-CO-CH2-CH(-R1)-COO-R4 WHEREIN R1, R2 AND R4 ARE THE SAME AS DEFINED ABOVE. WHEREIN X1 AND X2 EACH IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF OXYGEN AND METHYLENE; A IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF UNSUBSTITUTED SATURATED HYDROCARBON CHAIN HAVING UP TO 5 CARBON ATOMS, UNSUBSTITUTED UNSATURATED HYDROCARBON CHAIN HAVING UP TO 5 CARBON ATOMS AND SUBSTITUTED SATURATED OR SUBSTITUTED ETHYLENICALLY UNSATURATED HYDROCARBON CHAIN HAVING UP TO 5 CARBON ATOMS AND SUBSTITUTED SATURATED STITUENTS ARE SELECTED FROM THE GROUP CONSISTING OF HALOGEN OR PHENYL, THE HYDROCARBON CHAIN BEING STRAIGHT OR BRANCHED ONE; M IS 0 OR 1; N IS 1 OR 2; R1 AND R2 EACH IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ALKYL HAVING UP TO 4 CARBON ATOMS; R3 IS A MEMBER SELECTED FROM THE GOUP CONSISTING OF ALKYL HAVING UP TO 4 CARBON ATOMS UNSUBSTITUTED OR A LOWER ALKYL-, LOWER ALKKOXY-, LOWER ALKYLTHIO-, NITRO-, METHYLENEDIOXY-, ETHYLENEDIOXY- OR HALOGEN-SUBSTITUTED ARYL, EACH OF SAID ALKYL, ALKOXY AND ALKYLTHIO SUBSTITUENTS CONTAINING UP TO 4 CARBON ATOMS, OR UNSUBSTITUTED, OR HALOGEN-, AKYL- OR ...

PROCESS FOR THE PREPARATION OF N-SUBSTITUTED-6,7-METHYLENE DIOXY-4-QUINOLONE-3-CARBONIC ACID ESTERS.

NEW CATIONIC DI-METHYLENE DIXY BENZOLES, THEIR USE FOR THE OXIDATION COLORING OF KERATINE FIBERS

Patent FR2387971B1

Antihypertensive n-piperazinylalkanoylanilides

Colouring agent for keratin fibres and, in particular, human hair, and a method for dyeing keratin fibres

Process for the preparation of optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones

A new process has been developed for the synthesis of optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones.

Patent FR2099951A5

Quinazolinone derivative

Optical tape end sensing arrangement for magnetic tape cassette

A tape cassette arrangement includes structures formed integrally with the cassette halves or simply fitted into the light transmission apertures. Specific embodiments of the invention include light polarizing elements which are fitted into apertures formed in the sides of the cassette, corrugations on the interior of the cassette proximate the apertures, and shielding walls which are located to block light and in particular that light which tends to enter through a large window provided in the upper surface of the cassette and through which the status of the tape is visible.

Benzylthio acetamide compound and preparation method and application thereof

本发明属于植物生长调节剂技术领域，具体公开了苄硫基乙酰胺类化合物及其制备方法与应用。所述化合物的结构如式Ⅰ所示。本发明提供的化合物的制备方法原料便宜，工艺简单，反应条件温和，产率高。相关活性研究发现式Ⅰ所示化合物对植物的生长有很好的调节活性，可有效促进作物根部生长，降低株高，并在高浓度时具有良好的除草效果，是潜在的植物生长调节剂。

PROCEDURE FOR THE PREPARATION OF N- (TRIMETOXIBENCIL) - N'-PHENYLPIPERAZINES

Ortho-arylidene-amino-phenethyl-amine(s) - having analgesic, antidepressant, anxiolytic and anticholinergic activity

Patent FR2143345B2

NEW PROCESS FOR THE PREPARATION OF 1-ALKYL-4-PHENYL-2 (1H) -CHINAZOLINONES

Antihypertensive n-piperazinylalkanoylanilides

Novel cationic di-methylenedioxy-benzenes, their use for oxidation dyeing of keratin fibres

L'invention a pour objet de nouveaux di-méthylènedioxy-benzènes comportant au moins un groupement cationique Z, Z étant choisi parmi des chaînes aliphatiques quaternisées, des chaînes aliphatiques comportant au moins un cycle saturé quaternisé, et des chaînes aliphatiques comportant au moins un cycle insaturé quaternisé, leur utilisation à titre de précurseur de colorant d'oxydation pour la teinture d'oxydation des fibres kératiniques, les compositions tinctoriales les contenant, ainsi que les procédés de teinture d'oxydation les mettant en oeuvre.

METHOD FOR PREPARING N-SUBSTITUTED-6,7-METHYLENE-DIOXY-4-QUINOLONE-3-CARBONIC ACID ESTERS.

Tetrahydroimidazo or hexahydropyrimido-2,1-b-quinasolin-2-ones

Improved optical tape end sensing arrangement for magnetic tape cassette

Preparation process of novel cinnamoyles piperazines and omopiperazines

3,3-dichloro-2-azetidinone derivatives

NOVEL CINNAMOYLES PIPERAZINES AND HOMOPIPERAZINES, THEIR PREPARATION PROCESS AND THEIR APPLICATION IN THERAPEUTICS

A.NOUVELLES CINNAMOYLES PIPERAZINES ET HOMOPIPERAZINES. B.CES NOUVELLES CINNAMOYLES PIPERAZINES REPONDENT A LA FORMULE: (CF DESSIN DANS BOPI) OU (N, R, X, M) (2, OH, OX, O) AR PHENYLE OU BENZODIOXANE SUBSTITUE; (1, H, OX, O) ET AR BENZODIOXANE SUBSTITUE; (1, OH, S, O) ET AR PHENYLE OU BENZODIOXANE SUBSTITUE; (1, OH, -N-O) ET AR PHENYLE; (CF DESSIN DANS BOPI) C.UTILISABLES COMME MEDICAMENTS.