ЗАМЕЩЕННЫЕ 1-АМИНОАЛКИЛЛАКТАМЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ И СПОСОБ ИХ ПОЛУЧЕНИЯ

Изобретение относится к органической химии и может найти применение в медицине. Описывается соединение, имеющее общую формулу I, где R1 и R2 означают независимо в каждом случае водород, галоген, (С1-С6)алкил, -OR', -SR', -NR'R", -SOR', -SO2R'. -COOR', -OCOR'-, -OCONR'R", -OSO2R', -OSO2NR'R", -NR'SO2R", -NR'COR", -SO2NR'R", -SO2(СН2)1-3 - CONR'R", -CONR'R", циангруппу, галоидалкил или нитрогруппу; или R' и R" означают независимо в каждом случае водород, (С1 -С6)алкил, замещенный (С1-С6)алкил, арил, гетероциклил, гетероарил, арил(С1-С3)-алкил, гетероарил(С1-С3)алкил, гетероциклил(С1-С3)алкил, циклоалкил-алкил, циклоалкил, или R' и R" вместе с атомом азота, с которым они связаны, могут также образовывать 5-7-членное кольцо, необязательно включающее дополнительный кольцевой гетероатом, выбранный из N, О или S(О)0-2; R3 независимо в каждом случае означает (С1-С6)алкил, (С1-С6)алкенил, (С1-С6)алкинил или циклоалкил; или один из X, Y или Z означает независимо -О- или >N-R4, другие означают -СН2 ...

ПРОИЗВОДНЫЕ 1-[2-(ЗАМЕЩЕННЫЙ ВИНИЛ)]-5Н-2,3-БЕНЗОДИАЗЕПИНА, СПОСОБ ИХ ПОЛУЧЕНИЯ, ПРОМЕЖУТОЧНОЕ СОЕДИНЕНИЕ, ФАРМАЦЕВТИЧЕСКИЙ СОСТАВ И СПОСОБ ЕГО ПОЛУЧЕНИЯ, СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ЦЕНТРАЛЬНОЙ НЕРВНОЙ СИСТЕМЫ

Изобретение относится к новым производным 1-[2-(замещенный винил)]-5H-2,3-бензодиазепина, способу их получения, фармацевтическому составу, способу его получения и способу лечения заболеваний центральной нервной системы. Соединения в соответствии с изобретением имеют общую формулу I, где A и B вместе образуют группу формулы =C=N или =CH-NH-; R1 представляет собой фенил, который может содержать от 2 до 3 гидроксильных групп или от 1 до 3 одинаковых или различных заместителей, выбранных из группы, включающей галоген, трифторметил, нитро-, циано-, амино, ди-(C1-3алкил)амино-, C1-4 алканоиламино-, C1-4 алкил, C1-4 алкокси-, карбоксил, (C1-4алкокси)-карбонил, метилендиоксил, нафтил, который может содержать заместитель, представляющий собой гидроксил, фурил, тиенил или индолил; R2 представляет собой водород или C1-4 алкил; R3 и R4 каждый представляет собой C1-4 алкоксигруппу, присоединенную в положениях 7 или 8 бензодиазепинового кольца, или R3 и R4 вместе образуют 7,8- или 8,9-метилендиоксильную ...

1-(3-ХЛОРФЕНИЛ)-4-ОКСИМЕТИЛ-7,8-ДИМЕТОКСИ-5Н-2,3-БЕНЗО-ДИАЗЕПИН ИЛИ ЕГО ТЕРАПЕВТИЧЕСКИ ПРИЕМЛЕМАЯ СОЛЬ ПРИСОЕДИНЕНИЯ КИСЛОТЫ

Сущность изобретения: продукт: 1-(3-хлорфенил)-4-оксиметил-7, 8-диметокси-5Н-2, 3-бензодиазепин, обладающий психотропной активностью. Реагент 1: 1-3(3,4-диметоксифенил)-пропан-1, 2-диол. Реагент 2: 3-хлорбензальдегид с последующим ацилированием и окислением хромовой кислотой. Реагент 3: гидразингидрат. Условия реакции: используют 3 - 7-кратный избыток 98 - 100%-ного гидразингидрата, т. пл. 159 - 161oС, выход 77,8%, хлоргидратная соль разлагается при 193 - 195oС, метансульфонатная соль - начиная с 186oС. 5 табл.

Способ получения производных 5Н-2,3-бензодиазепина или их солей присоединения кислот

Изобретение относится к гетероциклическим соединениям, в частности к получению производных 5Н-2, 3-бензодиаэепина формулы где R - Незамещенная или замещенная галоидом, трифторметильной или одной или двумя алкоксигруппами с 1-4 атомами углерода фенольная или 2-фуриль- ная группа; R,- С,- С -алкил; R - водород или С,- С -алкил; R - гидро- ксильная или алкоксигруппа с 1-4 атомами углерода; R - алкоксигруппа с 1-4 атомами углерода, причем в случае , когда R-3,4-диметоксифенильная 4 2 4 группа, R -метил, а R -этил,R и R каждый имеет иное значение, чем ме- токсигруппа, или их солей присоединения кислот, оказывающих воздействие на центральную нервную систему. Цель - разработка способа получения новых более активных соединений. Получение целевых соединений ведут из соответствующих 1,5-дикетона, или 2-бензопирилиевой соли, или 6Н- 2-бензопиран-6-она в среде полярного органического растворителя, такого , как низший спирт или карбоновая кислота с Г-3 атомами углерода, которые при 60-100 С вводят во ...

Способ получения производных бензазепина или их кислотно-аддитивных солей с неорганическими кислотами

... 1. Способ получения производных бензазепина общей формулы КНз л и 1 х-Xs т где А - группа -СН -СНг-, , Р -NH-CO- или , в которой R ал-кильная группа с числом атомов углерода 1-3; В - метиленовая или карбонильная группа} Е - этиленовая или и-пропиленовая группа; G - этиленовая группа, R и R, - одинаковые или различные означают гидроксил, алкильные, алкокси- или фенилалкоксигруппы, в коSU ,,,, 1160935 А 4 ...

Способ получения замещенных халькона

Benzamid-Derivate und ihre Verwendung als Vasopressin-Antagonisten

"BENZAZEPINDERIVATE, IHRE HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL"

Neue 2,3-Benzodiazepinderivate, deren Herstellung und Verwendung als Arzneimittel

The invention concerns compounds of formula (I), in which: X designates hydrogen or halogen; Y designates -NR<3>- or -N=; R<1>, R<2> and R<3> designate hydrogen or different substituents; R<4> designates optionally substituted C1-C6 alkyl; R<5> designates hydrogen; or R<4> and R<5> together designate oxygen; R<6> designates C1-C4 alkyl; and (a) designates a double bond or single bonds. Owing to their non-competitive inhibiting of the AMPA receptors, these compounds can be used as medicaments for treating diseases of the central nervous system.

1,2-DIAZEPANDERIVATE ALS INHIBITOREN DES INTERLEUKIN-1BETA UMWANDELNDEN ENZYMS

Verfahren zur Aufhebung des durch optische Aufheller erzielten Aufhelleffektes

UREA DERIVATIVES PROCESSES FOR THEIR PREPARATION AND COMPO SITIONS INCORPORATING THEM

... 1414213 Cyclic N-phenyl-urea derivatives ROUSSEL UCLAF 6 Aug 1973 [4 Aug 1972] 37189/73 Heading C2C The invention comprises an N-phenyl-urea derivative of the general Formula (I) wherein: A represents a straight- or branchedchain alkylene group containing from 2 to 6 carbon atoms; X, which may be at any available position in the benzene ring, represents a hydrogen or halogen atom, a trifluoromethyl radical, a nitro group, an acyl radical containing from 1 to 6 carbon atoms, an alkyl or alkoxy radical each containing from 1 to 6 carbon atoms, or an unsubstituted or halo-substituted alkenyloxy radical containing from 2 to 6 carbon atoms; Y, which may be at any available position in the benzene ring, represents a hydrogen or halogen atom, or an alkyl or alkoxy radical each containing from 1 to 6 carbon atoms; and R represents an alkoxy radical containing from 1 to 4 carbon atoms, an alkoxycarbonyl radical containing from 1 to 6 carbon atoms, or a chloroacetyl group. Compounds of general Formula ...

5H-2, 3-BENZODIAZEPINES

5H-2, 3-BENZODIAZEPINES

The invention relates to new 5H-2,3-benzodiazepine derivatives and a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same. The new 5H-2,3-benzodiazepine derivatives of the invention possess valuable central nervous effect and in particular exert antiaggressive, anxiolytic, narcosis potentiating and soporific properties.

Benzazepines and benzodiazepines

Compound of general formula I (wherein R1 to R6, A, B, E and G are as defined in claim 1) and acid addition salts thereof. The new compounds have valuable pharmacological properties, in particular a heart-rate lowering effect. Processes for preparing the new compounds and pharmaceutical compositions containing them are also described.

3,4-Dihydro-5H-2,3-benzodiazepine derivatives

The invention relates to new 3,4-dihydro-5H-2,3-benzodiazepine derivatives of general formula (I) and pharmaceutically acceptable acid addition salts thereof, (I) wherein R represents a phenyl group optionally carrying one or two substituents selected from the group consisting of halogen, hydroxy, C1-4 alkoxy and benzyloxy; a furyl or a thienyl group, R1 stands for a hydrogen atom or a C1-4 alkyl group, R2 and R3 each represent hydrogen atom, C1-4 alkoxy, C4-7 cycloalkoxy or benzyloxy group. The new compounds of the general formula (I) can be prepared by reducing a 5H-2,3-benzodiazepine derivative of the general formula (II) (II) wherein R, R1, R2 and R3 have the above-defined meanings, with an inorganic or organic hydride and/or complex metal hydride. The new compounds of the general formula (I) possess significant central nervous effects and can advantageously be used in the therapy.

DIAZ(EP)INE BIS(N-AMIDINOAMIDINE)DERIVATIVES

Diazacycloalkenes and the preparation thereof

The invention comprises compounds of the general formula: the acid addition and quaternary ammonium salts thereof (the latter having an alkyl group containing up to four carbon atoms) wherein R is an alkyl or alkenyl group containing up to eighteen carbon atoms; X is oxygen or sulphur; n is an integer from three to five; R1 is a hydrogen atom or an alkyl or alkenyl group containing up to six carbon atoms, the total number of carbon atoms in R and R1 being six to twenty-four; and further compounds wherein is two or three and adjacent carbon atoms in the heterocyclic ring form a conjugated system, and the preparation thereof (1) where X is sulphur and the heterocyclic residue is imidazole or pyrimidine, by reacting an alkyl or alkenyl halide with the sodium salt of a 2-mercaptoimidazole or 2-mercaptopyrimidine in an ether solvent at between 35 to 140 DEG C. for from about one to five hours; or (2) where X is sulphur and the heterocyclic residue is tetrahydropyrimidine ...

PRODUCTION OF 1,3-DIAZA-HETEROCYCLES

Sulfonamide inhibitors of aspartyl protease

Sulfonamide inhibitors of aspartyl protease

Sulfonamide inhibitors of aspartyl protease.

Substituted news trifluoroéthylamines, their processes of obtaining and their employment like drug.

New 2 (nitromethylene) - 1,3-diazacycloalcanes, insecticidal compositions the container and their use to fight against undesirable insects.

Sulfonamide inhibitors of aspartyl protease

Sulfonamide inhibitors of aspartyl protease

PROCEDURE FOR THE PRODUCTION OF NEW HYDRAZONVERBINDUNGEN AND OF PHARMAKOLOGISCH COMPATIBLE ONES SAEUREADDITIONSSALZEN AND QUATERNAEREN AMMONIUM SALTS THE SAME

USE OF RITONAVIR (ABT-538) FOR the IMPROVEMENT of the PHARMAKOKINETIK OF DRUGS, the BY CYTOCHROM P450 METABOLISIERT, IN the CONTEXT of a TREATMENT OF AIDS

VERFAHREN UND VORRICHTUNG ZUR HERSTELLUNG VON MIT OEFFNUNGSFAEDEN VERSEHENEN EINDOSENBEHAELTERN, GEFERTIGT AUS FLEXIBLEN FOLIENHAELFTEN

PROCEDURE FOR the PRODUCTION of NEW 1,3-DIAZACYCLOALKENDERIVATE AND YOUR HYDROCHLORIDES, HYDRAULIC BROMIDE OR HYDRAULIC IODIDES

PROCEDURE FOR THE PRODUCTION OF NEW HYDRAZON CONNECTIONS AND OF PHARMAKOLOGISCH EN TRAEGLICHEN ACID ADDITION SALTS AND QUATERNAEREN AMMONIUM SALTS THE SAME

NEW PROCEDURE FOR THE PRODUCTION OF CLONIDIN DERIVATIVES

DIHYDROBENZODIAZEPINEN AND THEIR USE FOR THE TREATMENT OF DYSLIPIDÄMIEN

PROCEDURE FOR THE PRODUCTION OF NEW ONES - ARYL-5H-2,3-BENZODIAZEPIN-DERIVATEN AND THEIR SAE

PROCEDURE FOR THE PRODUCTION OF NEW TETRAHYDROPYRIMIDINEN, IMIDAZOLINEN AND TETRAHYDRO-1,3-DIAZEPINEN AND THEIR ACID ADDITION SALTS

PROCEDURE FOR THE PRODUCTION OF NEW TETRAHYDROPYRIMIDINEN, IMIDAZOLINEN AND TETRAHYDRO-1,3-DIAZEPINEN AND THEIR ACID ADDITION SALTS

VERFAHREN ZUR HERSTELLUNG VON NEUEN 3,4-DIHYDOR-5H-2,3-BENZODIAZEPINDERIVATEN SOWIE VON DEREN SAEUREADDITIONSSALZEN

BENZAZEPINDERIVATE, YOUR PRODUCTION AND YOUR USE AS DRUGS.

PROCEDURE FOR the PRODUCTION OF 2-HYDRAZINO-1,3DIAZACYCLO-ALK-2-ENE HYDROHALIDEN.

N (2 (2-AMINO-2-PHENYLETHYL) PHENYL) - 2,2DIMETHYLPROPANAMID AND DERIVATIVES AND a PROCEDURE FOR the PRODUCTION THE SAME.

PROCEDURE FOR THE PRODUCTION OF NEW TETRAHYDROPYRIMIDINEN, IMIDAZOLINEN AND TETRAHYDRO-1,3-DIAZEPINEN AND THEIR ACID ADDITION SALTS

SUBSTITUTED 1-AMINOALKYL-LACTAME AND THEIR USE AS an MUSCARINREZEPTOR ANTAGONIST

Pre-sensibilized, photo-sensitive plate for the production of a pressure plate

COMBINATION OF RETROVIRALEN PROTEASEHENNERN

1,2-DIAZEPANDERIVATE AS INHIBITORS of the INTERLEUKIN-1BETA of CONVERTING ENZYME

BENZOXAZEPIN DERIVATIVES USABLE AS SQUALEN SYNTHETASE INHIBITORS

CYCLI UREA AND ANALOGUES USABLE AS RETROVIRALE OF PROTEASEHEMMER

USE OF RITONAVIR (ABT-538) TO IMPROVEMENT OF THE PHARMAKOKINETIK OF DRUGS, the BY CYTOCHROM P450 METABOLISIERT, IN THE CONTEXT OF A TREATMENT OF AIDS

AMINOGUANIDINE AND ALKOXYGUANIDINE AS PROTEASEHEMMER

SUBSTITUTED 1-AMINOALKYL-LACTAME AND YOUR USE AS MUSCARINREZEPTOR an ANTAGONIST

UREA DERIVATIVES OF ALPHA, OMEGA DIAMINOSÄUREN AND PEPTIDEN

ßNEUE 2,3-BENZODIAZEPINDERIVATE AND PHARMACEUTICAL COMPOSITIONS, THESE CONNECTIONS AS ACTIVE SUBSTANCE ENTHALTENß

SUBSTITUTED 2,3-BENZODIAZEPIN-4-ONE AND THEIR USE

PROCEDURE FOR THE PRODUCTION OF ALKYLIMIDAZOLIDINON (METH) ACRYLATES

PROCEDURES FOR the PRODUCTION OF N, N' DISUBSTITUIERTEN CYCLI UREA

BENZODIAZEPINES

POLYMETHYLENEIMINE DERIVATIVES

Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors

Use of ritonavir (abt-538) for improving the pharmacokinetics of drugs metabolized by cytochrome p450 in a method of treating aids

PROCESS FOR THE PREPARATION OF TOFISOPAM AND NEW INTERMEDIATES

Method for preparing alkylating agents and their use for alkylating cyclic ureas

CYCLIC UREAS AND ANALOGUES USEFUL AS RETROVIRAL PROTEASE INHIBITIORS

1,2-diazepane derivatives as interleukin-1beta converting enzyme inhibitors

2,3-benzodiazepine derivatives and their use as ampa-receptor inhibitors

1-AMINOALKYL-3-OXYSUBSTITUTED-4-ARYL-1,3,4,5-TETRAHYDRO-2H- 1,3-BENZODIAZEPINE-2-ONES, A PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

Aryl-fused and hetaryl-fused-2,4-diazepine and 2,4-diazocine antiarrhythmic agents

PENTADIENONE HYDRAZONE

HEART-RATE REDUCING BENZAZEPINONE DERIVATIVES

SEVEN-MEMBERED HETEROCYCLIC CARBENES AND THEIR METAL COMPLEXES

Disclosed are carbenes of the general formula (I), and including salts thereof, and metal complexes thereof. The carbenes are useful in any reaction where carbenes and carbene-metal complexes are used. The carbenes disclosed herein are particularly useful in asymmetric catalysis.

AMINOTETRAHYDRONAPHTHYLINE DERIVATES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND PROCESSES FOR THEIR PREPARATION

This invention relates to compounds of general formula I < IMG > (I) wherein A represents a -CH2-CH2-, -CH=CH-, -?H-CO- or -?H2-CO-group and B represents a methylene, carbonyl or thiocarbonyl group, or A represents a -CO-CO- or < IMG > group and B represents a methylene group wherein the mark x signifies that the carbon or nitrogen atom so marked is bonded to the phenyl nucleus; E represents a straight-chained alkylene group containing 2 to 4 carbon atoms optionally substituted by an alkyl group containing 1 to 3 carbon atoms, or represents a 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene group; R1 represents a hydrogen, fluorine, chlorine or bromine atom or a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, alkylthio, hydroxy, alkoxy or phenylalkoxy group (in which each alkyl moiety may contain 1 to 3 carbon atoms) and R2 represents a hydrogen, chlorine or bromine atom or a hydroxy, alkoxy, phenylalkoxy or alkyl group (in which each alkyl moiety may ...

ANTHRACENCE-9,10-BIS-CARBONYL-HYDRAZONES

Novel anthracence-9,10-bis carbonyl hydrazones of formula: (I) and the pharmaceutically aceptable acid addition salts thereof, useful as antibacterial agents, for inhibiting the growth of transplanted mouse tumors, and for inducing the rgression and/or palliation of leukemia and related cancers.

SUBSTITUTED 1-AMINOALKYL-LACTAMS AND THEIR USE AS MUSCARINIC RECEPTOR ANTAGONISTS

This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula (1) wherein one of X, Y, or Z is independently -S-, -O-, or > N-R4, the others are-CH2-; (p) is an integer from 0 to 3 inclusive; m is an integer from 0 to 3 inclusive; n is an integer from 1 to 6 inclusive; R3 is (C1-6)-alkyl, (C1-6)-alkenyl, (C 1-6)- alkynyl or cycloalkyl; and R1, R2 and R3 are hydrogen or specified substituents. These compounds are useful for treating diseases associated with smooth muscle disorders.

NOVEL 2,3-BENZODIAZEPINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT

The invention refers to novel 2,3-benzodiazepine derivatives of formula (I) and pharmaceutical compositions containing the same as the active ingredient. The novel compounds have antipasmodic, muscle relaxant and neuroprotective activities. In formula I; X represents a hydrogen atom, a chloro atom or a methoxy group; Y stands for a hydrogen atom or a halo atom; Z means a methyl group or a chloro atom; R is a C~1-4 alkyl group or a group of the formula - NR1~R~2, wherein R1~ and R2~ represent, independently, a hydrogen atom, a C~1- 4 alkyl group, a C~1-4 alkoxy group or a C3-6~ cycloalkyl group.

NOVEL SUBSTITUTED 2,3-BENZODIAZEPINE DERIVATIVES

The invention relates to new 2,3-benzodiazepine derivatives of formula (I), isomers and acid addition salts thereof and to pharmaceutical compositions containing the same, as well as to pharmaceutical compositions and methods of using the same suitable for treating conditions associated with muscle spasms, epilepsy, acute and chronic forms of neurodegenerative diseases as well as preventing, treating or alleviating the symptoms of acute and chronic inflammatory disorders.

5H-2,3-BENZODIAZEPINE DERIVATIVES AND A PROCESS FOR THE PREPARATION THEREOF

PROCESS FOR SELECTIVE REMOVAL OF CYCLIC UREA FROM HINDERED AMINE GAS TREATING SOLUTION

METHOD AND COMPOSITIONS FOR USING NON-IONIC CONTRAST AGENTS TO REDUCE THE RISK OF CLOT FORMULATION IN DIAGNOSTIC PROCEDURES

RA58 METHODS AND COMPOSITIONS FOR USING NON-IONIC CONTRAST AGENTS TO REDUCE THE RISK OF CLOT FORMATION IN DIAGNOSTIC PROCEDURES In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.

BICYCLIC FIBRINOGEN ANTAGONISTS

This invention relates to compounds of formulae (I), (II), (III), wherein A1 is O, S, N-R1 or CHR1; A4 is N-R4 or CHR4; R2 is a sidechain containing an acid or ester group; R1, R4 and R5 are substituents such as H, alkyl and aryl alkyl, and R6 is a sidechain containing a nitrogen group; and pharmaceutically acceptable salts thereof, which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.

SUBSTITUTED CYCLIC CARBONYLS AND DERIVATIVES THEREOF USEFUL AS RETROVIRAL PROTEASE INHIBITORS

This invention relates to substituted cyclic carbonyls and derivatives thereof useful as Human Immnunodifiency Virus (HIV) protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating HIV infection.

METHOD AND COMPOSITIONS FOR USING NON-IONIC CONTRAST AGENTS TO REDUCE THE RISK OF CLOT FORMULATION IN DIAGNOSTIC PROCEDURES

In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.

SUBSTITUTED GUANIDINES HAVING HIGH BINDING TO THE SIGMA RECEPTOR AND THE USE THEREOF

... 2083269 9118868 PCTABS00008 The invention relates to a method for the treatment or prophylaxis of psychosis, depression, hypertension, or anxiety in an animal by administering an effective amount of an N,N'-disubstituted guanidine or 2-imino-imidazolidine having a high affinity for the sigma receptor. The invention also relates to the novel guanidines of the invention as well as pharmaceutical compositions thereof.

AMINEDIOL PROTEASE INHIBITORS

AMINEDIOL PROTEASE INHIBITORS Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).

METHOD FOR PREPARING ALKYLATING AGENTS AND THEIR USE FOR ALKYLATING CYCLIC UREAS

This invention relates to methods for preparing alkylating agents and use of the agents prepared. In particular, this invention relates to preparation methods for hydroxy halide and organooxy halide alkylating agents and their use for alkylating cyclic urea compounds.

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

A compound of formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

USE OF RITONAVIR (ABT-538) FOR IMPROVING THE PHARMACOKINETICS OF DRUGS METABOLIZED BY CYTOCHROME P450 IN A METHOD OF TREATING AIDS

A method is disclosed for improving the pharmacokinetics of a drug which is metabolized by cytochrome P450 monooxygenase.

AMINOGUANIDINES AND ALKOXYGUANIDINES AS PROTEASE INHIBITORS

Aminoguanidine and alkoxyguanidine compounds, including compounds of formula (I) wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, R a R b, R c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula (1). The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation ...

2,4 benzodiazepine derivatives having coccidiostatic - and cns stimulant activity

... derivs. (I), their N-oxides & acid addn. & quat. salts, & pharmaceutical compns. Ph = 1,2-phenylene, opt. substd. R1, 4 = H2, (aliphatic)2, or 1 H & 1 aliphatic, araliphatic, aromatic, aromatic heterocyclic or aromatic heterocyclic-aliphatic residue R2 = H, OH, SH, amino or substd, amino, or an aliphatic, araliphatic, aromatic, aromatic heterocyclic or aromatic heterocyclic-aliphatic residue R3 = H, or aliphatic, araliphatic, aromatic, aromatic heterocyclic or aromatic heterocyclic-aliphatic residue, or carboxylic acyl.

Verfahren zur Herstellung von 2-Carbamyl-4,5,6,7-tetrahydro-1,3-diazepinen

Verfahren zur Herstellung von 4,5-Dihydro-3H-1,3-benzodiazepin-4-onen

Verfahren zur Herstellung von 2,4 Benzdiazepinen

Verfahren zur Herstellung von 2,4-Benzdiazepinen

Pesticide containing 2-(nitromethylene)-1,3-diazacycloalkanes

CYCLIC UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1

This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell Or the inhibition of the conversion of cortisone to Cortisol in a cell. 2. The compound of wherein claim 1 ,{'sup': 1a', '1b, 'sub': 1', '6', '2', '6', '2', '6', '1', '3', '1', '3', '1', '3', '2, 'Rand Rare each independently (a) hydrogen or (b) (C-C)alkyl, (C-C)alkenyl, (C-C)alkynyl or (C-C)alkoxy(C-C)alkyl, each of which are optionally substituted with up to three groups independently selected from fluorine, hydroxy, (C-C)alkoxy and HNC(═O);'}{'sub': 1', '8', '2', '8', '2', '8', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4', '4, 'A is straight or branched (C-C)alkyl, (C-C)alkenyl or (C-C)alkynyl, each of which are optionally substituted with up to 4 groups independently selected from fluorine, cyano, oxo, R, RO—, (R)N—, ROC—, RS, RS(═O)—, RS(═O)—, RC(═O)NR—, (R)NC(═O)—, (R)NC(═O)O—, (R)NC(═O)NR—, ROC(═O)NR—, (R)NC(═NCN)NR—, (RO)P(═O)O, (RO)P(═O)NR—, ROS(═O)NR—, (R)NS(═O)O—, (R)NS(═O)NR—, RS(═O)NR—, RS(═O)NHC(═O)—, RS(═O)NHC(═O)O—, RS(═O)NHC(═O)NR—, ROS(═O)NHC(═O)—, ROS(═O)NHC(═O)O—, ROS(═O)NHC(═O)NR—, (R)NS(═O)NHC(═O)—, (R)NS(═O)NHC(═O)O—, (R)NS(═O)NHC(═O)NR—, RC(═O)NHS(═O)—, RC(═O)NHS(═O ...

USE OF 3-CARBOXY-N-ETHYL-N,N-DIMETHYLPROPAN-1-AMINIUM SALTS IN THE TREATMENT OF CARDIOVASCULAR DISEASE

Salts of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium, method of preparation thereof and use in the treatment of cardiovascular disease. 19-. (canceled)14. A process for preparing the 3-carboxy-N-ethyl-N claim 10 ,N-dimethylpropan-1-aminium salt according to claim 10 , comprising:a. adding N,N-dimethylethylamine to ethyl 4-bromobutanoate in appropriate solvent to obtain 4-ethoxy-N-ethyl-N,N-dimethyl-4-oxo-1-butanaminium bromide;b. passing 4-ethoxy-N-ethyl-N,N-dimethyl-4-oxo-1-butanaminium bromide through ion exchange resin column to obtain 4-[ethyl(dimethyl)ammonio] butanoate;c. adding acid selected from the group, consisting of fumaric acid, orotic acid and phosphoric acid in appropriate solvent to obtain the corresponding 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium salt.15. The process according to claim 14 , wherein in step a) the appropriate solvent is acetonitrile or acetone.16. A method for treating cardiovascular diseases in a subject in need thereof claim 10 , comprising administration of an effective amount of the 3-carboxy-N-ethyl-N claim 10 ,N-dimethylpropan-1-aminium salt of .17. The method according to claim 16 , wherein the cardiovascular disease is ischemic heart disease.18. The method according to claim 16 , wherein wherein the ischemic heart disease is myocardial infarction. The present invention relates to new compound 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium salts, and to a method of preparation thereof (compound of formula 4)The present invention relates also to use of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium salts in the treatment of cardiovascular disease.Cardiovascular diseases (CVDs) are a group of disorders of the heart and blood vessels.An estimated 16.7 million—or 29.2% of total global deaths—result from the various forms of cardiovascular disease (CVD).Myocardial infarction (heart attack) is a serious result of coronary artery disease.Myocardial infarction (MI) is the irreversible necrosis of heart muscle secondary to ...

Process for the Synthesis of Cyclic Alkylene Ureas

The invention relates to a process for the synthesis of cyclic alkylene ureas comprising reacting in the presence of a basic catalyst, a difunctional amine A having two primary amino groups, and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA, wherein the ratio of the amount of substance Ji(—NH2) of primary amino groups —NH2 in the difunctional amine A to the sum M(C) of the amount of substance n(CD) of carbonate groups of a dialkyl carbonate CD and the amount of substance n(CA) of carbonate groups in an alkylene carbonate CA, is at least more than 2, and to the product obtained by this process. 122-. (canceled)23. A process for the synthesis of a cyclic alkylene urea comprisingreacting a difunctional aliphatic amine A having two primary amino groups and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA, in the presence of a basic catalyst,{'sub': 2', '2, 'wherein the ratio of the amount of substance n(—NH) of primary amino groups —NHof the difunctional aliphatic amine A to the sum n(C) of the amount of substance n(CD) of carbonate groups of a dialkyl carbonate CD and the amount of substance n(CA) of carbonate groups in an alkylene carbonate CA, is at least more than 2.'}24. The process of claim 23 , wherein the process is conducted in the presence of a basic catalyst selected from the group consisting of alkoxides of alkali metals of group 1 of the Periodic Table of Elements claim 23 , and of alkoxides of alkaline earth metals of group 2 of the Periodic Table of Elements.25. The process of wherein the alkoxides are generated in situ.26. The process of wherein the alkoxides are generated by reacting an alkanol with a compound selected from the group consisting of an alkali hydroxide claim 25 , an alkali hydride claim 25 , an alkali amide claim 25 , an alkaline earth hydroxide claim 25 , an alkaline ...

OX1 ANTAGONISTS

The disclosures herein relate to novel compounds of formula (1) and salts thereof, wherein X; Y; R; R; R; R; R; R; Rand Rare defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors. 2. The compound according to wherein X is CH.3. The compound according to wherein X is N.4. The compound according to any one of - wherein Y is CH.5. The compound according to any one of - wherein Y is N.6. The compound according to any one of - wherein Ris H.7. The compound according to any one of - wherein Ris F.8. The compound according to any one of - wherein Ris H claim 1 , CHor OCH.9. The compound according to any one of - wherein Ris CH claim 1 , OCH claim 1 , CDor OCD.10. The compound according to any one of - wherein Ris SCH claim 1 , SOCH claim 1 , CFCHor OCFH.11. The compound according to any one of - wherein Ris H claim 1 , F or CH.12. The compound according to any one of - wherein Ris H claim 1 , CN or F.13. The compound according to any one of - wherein Ris H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , OCH claim 1 , OCH(CH) claim 1 , OCD claim 1 , CHOCH claim 1 , CHOCD claim 1 , CHCHCH.14. The compound according to any one of - wherein Ris H or F.15. The compound according to any preceding claim wherein the compound is selected from;1-(4-bromo-2,6-difluorobenzyl)-3-[3-(1,1-difluoroethyl)-4-methylphenyl]-6-fluoro-1,3,4,5-tetrahydro-2H-1,3-benzodiazepin-2-one{'sub': '3', '1-(4-bromo-2,6-difluorobenzyl)-3-{5-(1,1-difluoroethyl)-6-[(2H)methyloxy]pyridin-3-yl}-6-fluoro-1,3,4,5-tetrahydro-2H-1,3-benzodiazepin-2-one'}1-(4-bromo-2,6-difluorobenzyl)-3-[5-(1,1-difluoroethyl)-6-methoxypyridin-3-yl]-6-fluoro-1,3,4,5-tetrahydro-2H-1,3-benzodiazepin-2-one3-[5-(1,1-difluoroethyl)-6-methoxypyridin-3-yl]-6-fluoro-1-(2-fluoro-4-methoxybenzyl)-1,3,4,5-tetrahydro-2H-1,3-benzodiazepin-2-one{'sup': '2', 'sub': '3', '3-[5-(1,1-difluoroethyl)-6-methoxypyridin-3-yl]-1-(2,6- ...

Reduction of Aldehydes in Amine Catalysts

The present disclosure provides a method for reducing the aldehyde content in an amine catalyst by treating the amine catalyst with a treating agent selected from a cyclic urea substituted with at least one isocyanate reactive group, a free radical scavenger and a mixture thereof. The treated amine catalyst may then be used in the production of polyurethane materials which exhibit reduced aldehyde emissions.

Crystalline Pharmaceutical

New crystalline forms of lopinavir are disclosed. 1. A hydrated crystalline form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 7.25°±0.1° , 8.53°±0.1° , 10.46°±0.1° , 11.05°±0.1° , 11.71°±0.1° , 14.76°±0.1° , 15.30°±0.1° , 16.67°±0.1° , 17.32°±0.1° , 19.10°±0.1° , 19.57°±0.1° , 21.24°±0.1° , 21.84°±0.1° and 22.46°±0.1°.2. A higher hydrated crystalline form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 3.89°±0.1° , 6.55°±0.1° , 7.76°±0.1° , 8.55°±0.1° , 9.70°±0.1° , 10.56°±0.1° , 14.76°±0.1° , 15.57°±0.1° , 18.30°±0.1° , 18.95°±0.1° and 22.74°±0.1°.3. A higher hydrated crystalline form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 3.89°±0.1° , 6.55°±0.1° , 7.76°±0.1° , 8.55°±0.1° , 9.70°±0.1° , 10.56°±0.1° , 14.76°±0.1° , 15.06°±0.1° , 15.57°±0.1° , 16.49°±0.1° , 17.51°±0.1° , 18.30°±0.1° , 18.95°±0.1° , 21.73°±0.1° and 22.74°±0.1°.4. A solvated crystalline form of lopinavir with characteristic peaks in the solid state infrared spectrum at a position within the ranges of 1661-1673 cm , 1645-1653 cmand 1619-1629 cm.5. A desolvated crystalline form of lopinavir with at least one characteristic peak in the solid state infrared spectrum at a position within the range 1655-1662 cm.6. A desolvated crystalline form of lopinavir with characteristic peaks in the solid state infrared spectrum at a position within the ranges of 1655-1662 cmand 1636-1647 cm.7. A desolvated crystal form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 4.85°±0.1° , 6.39°±0.1° , 7.32°±0.1° , 8.81°±0.1° , 12.20°±0.1° , 12.81°±0.1° , 14.77°±0.1° , 16.45°±0.1° and 17.70°±0.1°.8. A desolvated crystal form of lopinavir with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 4.85°±0.1° , 6.39°±0.1° , 7.32°±0.1° , 8.81°±0.1° , 12.20°±0.1° , ...

COMPOSITIONS AND METHODS FOR TREATMENT OF PRE-CANCEROUS SKIN LESIONS

The present disclosure encompasses compositions and methods for the treatment of precancerous skin lesions. Compositions of the invention comprise a cytotoxic agent and a thymic stromal lymphopoietin (TSLP) inducer. 1. A method to treat a precancerous skin lesion , the method comprising topically administering to the lesion a composition comprising a cytotoxic agent and a thymic stromal lymphopoietin (TSLP) inducer.2. The method of claim 1 , wherein the cytotoxic agent is 5-fluorouracil (5-FU).3. The method of claim 1 , wherein the TSLP inducer is a vitamin D analog.4. The method of claim 3 , wherein the vitamin D analog is calcipotriol.5. The method of claim 2 , wherein the composition comprises about 2% to about 5% 5-FU.6. The method of claim 4 , wherein the composition comprises about 0.002% to about 0.005% calcipotriol.7. The method of claim 1 , wherein the precancerous skin lesion is actinic keratosis.8. The method of claim 1 , wherein the composition is administered twice a day for 4 to 6 days.9. The method of claim 1 , wherein the precancerous skin lesion is reduced in size by 50% or greater.10. A method to prevent the transition of a precancerous skin lesion to skin cancer claim 1 , the method comprising:a) identifying a subject with one or more precancerous skin lesion(s); andb) topically administering to the precancerous skin lesion(s) a composition comprising a cytotoxic agent and a TSLP inducer, wherein the precancerous skin lesion(s) is reduced in size such that progression to skin cancer is prevented.11. The method of claim 10 , wherein the precancerous skin lesion is actinic keratosis and the skin cancer is squamous cell carcinoma.12. The method of claim 10 , wherein the cytotoxic agent is 5-FU.13. The method of claim 10 , wherein the TSLP inducer is a vitamin D analog.14. The method of claim 13 , wherein the vitamin D analog is calcipotriol.15. The method of claim 12 , wherein the composition comprises about 2% to about 5% 5-FU.16. The method of ...

Reactive cyclic carbonates and ureas used for modifying biomolecules, polymers, and surfaces

Disclosed are reactive cyclic carbonates and ureas of formula (I) or (II), wherein R and X have the meaning indicated in the description. Said carbonates and ureas allow functional groups to be specifically introduced into biomolecules, polymers, and surfaces in mild conditions.

Reactive cyclic carbonates and ureas used for modifying biomolecules, polymers, and surfaces

Disclosed are reactive cyclic carbonates and ureas of formula (I) or (II), wherein R and X have the meaning indicated in the description. Said carbonates and ureas allow functional groups to be specifically introduced into biomolecules, polymers, and surfaces in mild conditions.

PHENYL-5 BENZODIAZEPINES-1,3, METHODS OF PREPARATION AND INTERMEDIATES

New intermediate of Lamivudine and the preparation thereof

본 발명은 라미부딘의 신규한 중간체, 이의 제조방법 및 라미부딘의 제조방법을 제공한다. 본 발명의 신규한 중간체를 이용한 라미부딘의 제조방법은 경제적이며 공정이 간단하고 수율이 높아 상업적 생산에 적합하다. The present invention provides novel intermediates of lamivudine, a process for their preparation and a process for the manufacture of lamivudine. The process for preparing lamivudine using the novel intermediates of the present invention is economical, simple in process and high in yield, and suitable for commercial production. 라미부딘, 사이토신 유도체, 제조방법 Lamivudine, cytosine derivative, manufacturing method

Reactive cyclic carbonates and ureas for the modification of biomolecules, polymeres and surfaces

Cyclic carbonate and urea derivatives (I) and (II) are new. Cyclic carbonate and urea derivatives of formulae (I) and (II) are new. [Image] R : 1-12C alkylene; X : -CONHR 1>; R 1>1-30C alkyl (optionally substituted by halo, hydroxy, 1-6C alkoxy, 1-6C alkylcarbonyloxy, amino, 1-6C alkylamino, di(1-6C alkyl)amino, ammonio, polyoxyalkylene, polysiloxanyl, (meth)acryloyloxy, sulfono, phosphono, di(1-6C alkyl)phosphono, phosphonato or di(1-6C alkyl)phosphonato) or a sugar residue Independent claims are also included for the following: (1) reaction products (RP) of (I) and (II) with a polymer that includes the functional groups hydroxy, primary amino or secondary amino; (2) method for modifying biomolecules, polymers and surfaces that include the functional groups hydroxy, primary amino or secondary amino by covalent reaction with (I) or (II); and (3) method for modifying surfaces by contact with RP.

3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one

The present invention relates to a process for preparing the compound 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one of formula which is to be found as a structural element in CGRP antagonists which are suitable above all for the oral therapy of migraine.

Additives for petroleum products

4,5-dihydro-3h-1,3-benzodiazepine-4-ones as psycho - sedatives, hypnotics and muscle relaxants

as psycho sedatives, hypnotics and muscle relaxants. M3A. New cpds. are of formula:- (where R1 is 1-6C alkyl or phenyl, opt, substd. e.g. by Cl, NO2 or MeO) are prepd. by reacting compd. (II) with compd (III) (where X = OH, OAlkyl, OAralkyl, Cl or Br, and Y = NH2 Cl, Br or OAlkyl). Preferred compds. are (I; R1 = Ph, p-Cl-C6H4, p-NO2C6H4p-MeO, C6H4, Me or Et).

PROCESS FOR THE PREPARATION OF ALKYLIMIDAZOLIDONE (METH) ACRYLATES

Manufacturing process for cyclic urea derivatives

PROCESS FOR THE PREPARATION OF ALKYLIMIDAZOLIDONE (METH) ACRYLATES

Pour obtenir un composé de formule (I), on fait réagir un anhydride (II) avec un alcool hétérocyclique (III). Après la réaction, on peut hydrolyser l'excès d'anhydride (méth)acrylique en acide (méth)acrylique par ajout d'eau et chauffage entre 25 et 70 deg.C, de préférence entre 30 et 50 deg.C, afin d'obtenir le composé (I) en solution dans l'eau et l'acide (méth)acrylique (CF DESSIN DANS BOPI) R**1 = H ou CH3 ; A et B représentent chacun indépendamment un groupe alkylène à chaîne droite ou ramifiée, en C2 -C5 . To obtain a compound of formula (I), an anhydride (II) is reacted with a heterocyclic alcohol (III). After the reaction, the excess (meth) acrylic anhydride can be hydrolyzed to (meth) acrylic acid by adding water and heating between 25 and 70 deg C, preferably between 30 and 50 deg C, in order to 'obtain the compound (I) in solution in water and (meth) acrylic acid (CF DRAWING IN BOPI) R ** 1 = H or CH3; A and B each independently represent a straight chain or branched, C2 -C5 alkylene group.

Process for preparing 2-thione-4, 4, 6-trimethyltetrahydropyrimidine

Patent FR2518544B1

Patent FR1595659A

Cyclic formamidine prepn

Cpds. of formula: (where each R is H, aliphatic, cycloaliphatic, arylaliphatic, or aromatic, and n is 2,3 or 4) are prepd. by passing cpds. of formula NRR1- CR2 n -NHR1 (where one R1 is H or -CHO and the other is -CHO) over activated silica or silicate at 400-600 degrees C. The products are useful as chemical intermediates. Previous methods used reagents that were toxic or expensive; this method avoids these reagents.

Cyclic urea derivative

Nu-(acylamidoalkyl)-nu'-vinyl-nu, nu'-alkyleneureas, polymers thereof and methods of making them

Preparation of asymmetric cyclic ureas through a monoacylated diamine intermediate

The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas of formula (VI): wherein: R7 is selected from the following: C¿1?-C8 alkyl substituted with 0-3 R?11; C¿2-C8 alkenyl substituted with 0-3 R11; C2-C8 alkynyl substituted with 0-3 R11; and a C¿3?-C14 carbocyclic ring system substituted with 0-3 R?11; R10 is C1-C10¿ alkyl, benzyl, naphthylmethyl, 3,4-methylenedioxybenzyl, or C¿1?-C4 alkyl substituted with phenyl wherein said phenyl is substituted with 0-3 R?10a¿; G taken together along with the oxygen atoms to which G is attached forms a group selected from: -O-C(-CH¿2?CH2CH2CH2CH2-)-O-, -O-C(CH2CH3)2-O-, -O-C(CH3)(CH2CH3)-O-, -O-C(CH2CH2CH2CH3)2-O-, -O-C(CH3)(CH2CH(CH3)CH3)-O-, -O-CH(phenyl)-O-, OCH2O-, -OC(CH3)2O- and -OC(OCH3)(CH2CH2CH3)O-. In the process, a diamine of formula (I-a) is selectively monoacylated to give an asymmetric monoacylated diamine which can be converted into asymmetric intermediates. The asymmetric intermediates can be further alkylated, cyclized, and/or modified to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection. The invention allows for scalable preparation of a wide variety of asymmetrical cyclic ureas.

Process for the preparation of nitrogen heterocycle-substituted (meth) acrylic acid esters

Method for preparing 2-hydrazino-1,3-diazacycloalk-2-enehydrohalide

내용 없음

Process for preparing quaternized imidazoline fabric conditioning compounds

PROCESS FOR PREPARING QUATERNIZED IMIDAZOLINE FABRIC CONDITINOING COMPOUNDS Theresa Rosario Jansen Glen D. Lichtenwalter ABSTRACT OF THE DISCLOSURE Disclosed is a high yield process for quaternizing imidazoline ester compounds in the absence of lower alcohol solvents and under anhydrous conditions. The reaction product of this process contains a quaternized imidazoline ester fabric softening compound and, optionally, an imidazoline ester compound. In the process of this invention, an imidazoline ester compound is initially heated to form an anhydrous melt. This anhydrous melt is subsequently contacted with a quaternizing agent selected from small chain organic halides and sulfates. The imidazoline ester compound and quaternizing agent are then reacted under anhydrous conditions for a period of time sufficient for substantially all of said quaternizing agent to react with said imidazoline ester compound to form a quaternized imidazoline ester compound of the formula: X- (II)

PROCEDURE FOR THE PREPARATION OF (MET) ALKYLIMIDAZOLIDONE ACRYLATE.

SE PREPARA UN COMPUESTO (I) HACIENDO REACCIONAR AL MENOS UN (MET)ACRILATO (II) CON UN ALCOHOL HETEROCICLICO (III), EN PRESENCIA DE AL MENOS UN CATALIZADOR ELEGIDO ENTRE LOS DIALKILOXIDOS DE ESTAÑO, LOS DIALKILDIALCOXIDOS DE ESTAÑO. LOS ACRILATOS Y METACRILATOS DE ALKILIMIDAZOLIDONA SON CONOCIDOS POR SU PAPEL EN LA CONSTITUCION DE POLIMEROS UTILES COMO REVESTIMIENTOS Y ADHESIVOS, Y PARA EL TRATAMIENTO DEL PAPEL Y DE LOS TEXTILES, ASI COMO PARA SU UTILIZACION COMO AGENTES DE TRATAMIENTO DEL CUERO Y EN LA PRODUCCION DE PINTURAS EN EMULSION. R SUB 1 = H, C SUB 3, A, B= GRUPO ALKILENO DE CADENA RECTA O RAMIFICADA QUE TIENE ENTRE 2 Y 5 ATOMOS DE CARBONO. A COMPOUND (I) IS PREPARED BY REACTING AT LEAST ONE (MET) ACRYLATE (II) WITH A HETERO CYCLIC ALCOHOL (III), IN THE PRESENCE OF AT LEAST ONE CATALYST CHOSEN AMONG THE TIN DIALKYLOXIDES. THE ACRYLATES AND METHACRYLATES OF ALKYLIMIDAZOLIDONE ARE KNOWN FOR THEIR ROLE IN THE CONSTITUTION OF USEFUL POLYMERS AS COATINGS AND ADHESIVES, AND FOR THE TREATMENT OF PAPER AND TEXTILE PRODUCTS, AS WELL AS A TREATMENT AND PURIFICATION AGENT. IN EMULSION. R SUB 1 = H, C SUB 3, A, B = ALKYLENE GROUP OF STRAIGHT OR BRANCHED CHAIN THAT HAS BETWEEN 2 AND 5 CARBON ATOMS.

Lopinavir prepared by one-pot method

一锅法制备洛匹那伟(I)， 其由2,6‑二甲基苯氧基乙酸、羧基活化剂、式(III)所示化合物在有机溶剂中进行缩合反应

Process for the preparation of alkyl imidazolidone (meth)acrylate

On prépare un composé (I) en faisant réagir au moins un (méth)acrylate (II) avec un alcool hétérocyclique (III), en présence d'au moins un catalyseur choisi parmi les dialkyloxydes d'étain, les dialkyldialcoxydes d'étain. Les acrylates et méthacrylates d'alkylimidazolidone sont connus pour leur rôle dans la constitution de polymères utiles comme revêtements et adhésifs, et pour le traitement du papier et des textiles, ainsi que pour leur utilisation comme agents de traitement du cuir et dans la production de peintures en émulsion. R1 = H, CH3; A, B = groupe alkylène à chaîne droite ou ramifiée ayant de 2 à 5 atomes de carbone. A compound (I) is prepared by reacting at least one (meth) acrylate (II) with a heterocyclic alcohol (III), in the presence of at minus one catalyst chosen from tin dialkyloxides, tin dialkyldialcoxides. Alkylimidazolidone acrylates and methacrylates are known for their role in the constitution of useful polymers like coatings and adhesives, and for the treatment of paper and textiles, as well as for their use as leather treatment agents and in the production of emulsion paints. R1 = H, CH3; A, B = straight or branched chain alkylene group having from 2 to 5 carbon atoms.

Process for the preparation of alkyl imidazolidone (meth)acrylate

On prépare un composé (I) en faisant réagir au moins un (méth)acrylate (II) avec un alcool hétérocyclique (III), en présence d'au moins un catalyseur choisi parmi les dialkyloxydes d'étain, les dialkyldialcoxydes d'étain. Les acrylates et méthacrylates d'alkylimidazolidone sont connus pour leur rôle dans la constitution de polymères utiles comme revêtements et adhésifs, et pour le traitement du papier et des textiles, ainsi que pour leur utilisation comme agents de traitement du cuir et dans la production de peintures en émulsion.

2-Benzhydrylimino-1,3-diazacarbocyclic compounds as inhibitors of gastric secretion

Novel 2-benzhydrylimino-1,3-diazacarbocyclic compounds of the formula ##STR1## wherein R' and R" independently are selected from the group consisting of hydrogen and methyl, X and Y independently are selected from the group consisting of hydrogen, lower alkoxy, lower alkyl and halo, and n is an integer of from 2 to 4, inclusive; and their acid addition salts are disclosed. Compounds have antisecretory properties. Certain of the compounds also have hypoglycemic properties.

Plant growth regulators and herbicides

Method for preparing N, N'-disubstituted cyclic ureas

(57)【要約】 ジ置換環状尿素IVを、還元剤の存在下、アルデヒドR 22 -CHOまたはR 23 -CHOを用いた還元的アルキル化（段階１）、次いで、IIのシクロカルボニル化によるIIIの形成（段階２）およびIIIの脱保護によるジオールIVの形成（段階３）により、上記反応図に従って調製する。これらの環状尿素IVはHIVプロテアーゼ阻害剤として有用である。

Ureins derived from alpha,omega-diamino acids and their preparation

The fabric of preparation quaternized imidazoline is adjusted the method for immunomodulator compounds

本发明披露了一种在没有低级醇溶剂和无水的 条件下季铵化咪唑啉酯化合物的高产率的方法。该 方法的反应产物含有一种季铵化咪唑啉酯织物柔软 剂化合物和任意一种咪唑啉酯化合物。在本发明的 方法中，首先将咪唑啉酯化合物加热形成无水熔化 物，接着使该无水熔化物与选自短链有机卤化物或硫 酸酯的季铵化剂接触，然后该咪唑啉酯化合物和季铵 化剂在无水条件下反应足够的时间以使基本上所有 的上述季铵化剂与上述咪唑啉酯化合物反应生成季 铵化咪唑啉酯化合物。

Process for preparing alkylimidazolidone (meth)acrylates

L'invention concerne un procédé de préparation d'un composé de formule: (voir formule I) dans laquelle R1 représente un atome d'hydrogène ou un groupe méthyle et A et B représentent chacun indépendamment un groupe alkylène à chaîne droite ou ramifiée, ayant de 2 à 5 atomes de carbone. Le procédé selon l'invention est caractérisé par le fait que l'on fait réagir un anhydride de formule (II): (voir formule II) dans laquelle R1 a la signification précitée, avec un alcool hétérocyclique de formule (III): (voir formule III) dans laquelle A et B ont les significations précitées. Les composés de formule (I) sont connus pour leur rôle dans la constitution de polymères utiles comme revêtements et adhésifs, pour le traitement du papier et des textiles, ainsi que pour leurs utilisations comme agents de traitement du cuir, et dans la production de peintures en émulsion.

3 - (- PIPERIDINYL) -2,3,4,5-TETRAHYDRO-1,3-BENZODIAZEPIN-2 (1H) -OH

1. Способ получения соединения формулы I ! ! отличающийся тем, что ! а) 2-нитрофенилуксусную кислоту взаимодействием с 4-амино-N-фенилметилпиперидином превращают в 2-нитро-N-[1-(фенилметил)-4-пиперидинил]фенилацетамид формулы II ! ! б) нитрогруппу полученного 2-нитро-N-[1-(фенилметил)-4-пиперидинил]фенилацетамида формулы II гидрируют до аминогруппы с образованием соединения формулы III ! ! в) образовавшийся промежуточный продукт формулы III добавлением сложного эфира превращают в присутствии основания в карбамат общей формулы IV ! ! в которой R1 обозначает фенил, бензил, аллил, 2,2,2-трихлорэтил или C1-C6алкил с прямой либо разветвленной цепью, и ! г) полученное соединение общей формулы IV растворяют в апротонном органическом растворителе, карбонильную группу добавлением восстановителя переводят в метиленовую группу и в завершение путем циклизации получают 3-[1-(фенилметил)-4-пиперидинил]-2,3,4,5-тетрагидро-1,3-бензодиазепин-2(1Н)-он формулы V !! 2. Способ по п.1, отличающийся тем, что на стадии а) 4-амино-N-фенилметилпиперидин добавляют в виде раствора в полярном апротонном растворителе и реакцию проводят в присутствии агента конденсации. ! 3. Способ по п.2, отличающийся тем, что в качестве полярного апротонного растворителя используют тетрагидрофуран, 2-метилтетрагидрофуран, диметоксиэтан, толуол, диметилформамид или N-метилпирролидинон. ! 4. Способ по п.2, отличающийся тем, что в качестве агента конденсации на стадии а) используют карбонилдиимидазол, карбонилдитриазол, н-пропанфосфоновый ангидрид, дициклогексилкарбодиимид, тионилхлорид, тетрафтороборат O-(бензотриазол-1-ил)-N,N,N',N'-тетраметилурония или 1-этил-3-(3'-диметиламинопропил)карбодиимид. ! 5. С РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2008 130 259 (13) A (51) МПК C07D 243/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2008130259/04, 21.12.2006 (71) Заявитель(и): БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГМБХ (DE) ...

Preparation of asymmetric cyclic ureas via monoacylated diamine intermediates

(57)【要約】 本発明は、不斉環式尿素のより良い調製方法と、不斉環式尿素の調製における中間体とに関する。この方法では、式（Ｉ−ａ）のジアミンを選択的にモノアシル化して不斉モノアシル化ジアミンとし、これを変換して不斉中間体とすることができる。この不斉中間体をさらにアルキル化することにより、ＨＩＶ感染症治療用のＨＩＶプロテアーゼ阻害剤として有用である化合物を得ることができる。 【化７５】

Process for preparing 2-hydrazino-1,3-diazacycloalk-2-ene hydrohalides

Process for preparing 2-hydrazino-1,3-diazacycoalk-2-ene hydrohalides

Seven-membered heterocyclic carbenes and their metal complexes

Disclosed are carbenes of the general formula: and including salts thereof, and metal complexes thereof. The carbenes are useful in any reaction where carbenes and carbene-metal complexes are used. The carbenes disclosed herein are particularly useful in asymmetric catalysis.

Process for producing N-monosubstituted and N, N'-disubstituted asymmetric cyclic ureas

(57)【要約】 Ｎ−モノ置換およびN,N′−ジ置換非対称環状尿素の調製方法

Process for producing nitrogenous heterocycle

A process for producing a nitrogenous heterocycle represented by general formula (III) by the reaction of an N-nitroimidodithiocarbonate represented by general formula (I) with a diamine represented by general formula (II), wherein R?1 and R2¿ represent each alkyl; R?3 and R4¿ represent each hydrogen or alkyl which may be substituted with a heterocycle; R5 represents hydrogen or alkyl; and n represents 2 to 4.

Bis guanidines and fungicides containing same

Die vorliegende Erfindung betrifft Bis-Guanidin-Derivate der allgemeinen Formel I, <IMAGE> in der R¹ und R²: unabhängig voneinander Wasserstoff, Alkyl, Alkenyl, Alkinyl, Alkoxy-alkyl, Halogenalkenyl; oder eine Cycloalkylgruppe mit 5 bis 12 Kohlenstoffatomen im Ring, die gegebenenfalls substituiert ist, oder eine Benzylgruppe, die gegebenenfalls substituiert ist, mit der Maßgabe, daß nur einer der beiden Substituenten R¹ oder R² Wasserstoff sein kann; oder; R¹ und R²: zusammen mit den Atomen, deren Substituenten sie sind, einen heterocyclischen Ring bedeuten, der substituiert sein kann; X: CH2, O, eine C-C-Einfachbindung, NH, N-(Alkyl) oder N-Benzyl, wobei der Phenylring des Benzylrestes substituiert sein kann, n: 5 bis 8 bedeuten, sowie ihre pflanzenverträglichen Säureadditionssalze und ihre Metallkomplexe und diese Verbindungen enthaltende Fungizide. The present invention relates to bis-guanidine derivatives of the general formula I, <IMAGE> in which R 1 and R 2: independently of one another hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkenyl; or a cycloalkyl group having 5 to 12 carbon atoms in the ring, which is optionally substituted, or a benzyl group, which is optionally substituted, with the proviso that only one of the two substituents R¹ or R² can be hydrogen; or; R¹ and R²: together with the atoms whose substituents they are, represent a heterocyclic ring which may be substituted; X: CH2, O, a CC single bond, NH, N- (alkyl) or N-benzyl, where the phenyl ring of the benzyl radical may be substituted, n: 5 to 8, and their plant-tolerated acid addition salts and their metal complexes and these compounds Fungicides.

Process for the preparation of alkylimidazolidinone (meth)acrylates

A new process for the mfr. of cpd. of formula (I), where -R<1> = H or Me ; A, B (each) = 2 - 5C alkylene(opt. branched), whereby anhydride of formula (II) is reacted with a heterocyclic alcohol of formula (III).

Pentadienone hydrazones, method for preparing the same, and insecticidal use thereof

There are provided insecticidal pentadienone hydrazones and methods of preparation thereof. There is further provided a method for using the aforesaid compounds for the control of insects, especially Lepidopterous insects, and for the control of ants, Family Formicidae, especially fire ants.

Process for the preparation of hexahydropyrimidine derivatives

Method for preparing N, N'-disubstitued cyclic ureas

Process for the preparation of cyclic amidines

Process for the preparation of 2,4-benzdiazepines

Cyclic urea derivative

Disclosed is cyclic urea derivatives represented by the following formula (A): ##STR1## wherein n is an integer of 0 or 1; m is an integer of 1 to 15; X is oxygen, sulfur or --NR 1 -- (R 1 is hydrogen or an alkyl group having 1 to 5 carbon atoms); R is an alkyl-, cycloalkyl -, aryl-, aralkyl-, alkaryl- and glycidyl group having 1 to 27 carbon atoms, or an alkyl-, cycloalkyl-, aryl-, aralkyl- and alkaryl group containing at least one ##STR2## O, S and N and having 1 to 27 carbon atoms with a molecular weight of 15 to 500, said groups substituted by glycidyl-, hydroxylic-, nitro groups, halogens, cyano-, formyl- or amino groups, or polyester-, polyether-, polyurethane and polyamide groups having a molecular weight of 500 to 100,000.

CYCLIC UREA PROCESS

Preparation of asymmetric cyclic ureas through a monoacylated diamine intermediate

3-Hydroxy-ethyl 1,3,4,5-tetra:hydro 1,3-benzodiazepine-2-thione(s) - and related cpds. are antidepressants, intermediate 2-amino-phenyl-ethyl-amino-ethanol derivs. are also new

X1,X2 substd. 3-CHR1-CHR2-(CH2)n-O-A -S-R-1,3,4,5-tetrahydro-1, 3-benzo diazepine-2-thiones of formula (I) are new (where X1,X2 are H, halo or lower alkoxy; R is H, lower alkyl or phenyl; one of R1 and R2 is H, the other is H, lower alkyl or phenyl; A is H, lower alkyl or tetrahydropyranyl; and n is 0 or 1. "Lower" implies 1-6C, opt. branched). CNS active cpds. used to treat depressive states and psychic troubles. Reserpene antagonism and S-HTP potentiator tests are described. (I) may be used as antidepressants by oral administration in daily doses of 0.05-100 mg. Activity tests compare the cpds. with imipramine and amitriptyline and LD50 of tests cpds. is over 3200 mg/kg.

Method for preparing N-monosubstituted and N,N'-disubstituted unsymmetrical cyclic ureas

The present invention relates generally to methods for the preparation of unsymmetrically substituted cyclic ureas of the formulae ##STR1## which are useful as HIV protease inhibitors. The methods provided go through an isourea intermediate.

N,N'-Disubstituted unsymmetrical cyclic urea and its use in therapy

An isourea compound of formula

Novel process for preparation of clonidine derivatives

已发现一种制备可乐宁衍生物的新方法，它比以前所知的方法用时更短、费用更低、更安全。还发现了式(Ⅰ)的新硫脲复合物，式中：Ar是苯基或萘基，它是未取代的或被选自Cl、F、Br、I、C 1 至C 4 烷基、芳基、C 1 至C 4 烷氧基或芳烷氧基的一个或多个基团所取代；NO 2 在对位或邻位上；n是1至4，这种新硫脲复合物可直接环化生成相应的杂环产物。

Process for preparing 4-phenyl-1,3-benzodiazepines

Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.

Process for preparing quaternized imidazoline fabric conditioning compounds

PROCESS FOR THE PREPARATION OF A POLYURETHANE RESIN

Novel process for preparation of clonidine derivatives

본 발명은 이미 공지된 방법 보다 더 짧고, 덜 비싸고 더 안전한 클로니딘의 제조 방법에 관한 것이다. 직접 고리화되어 상응하는 헤테로 고리 화합물을 생성시키는 하기 일반식(Ⅰ)의 신규의 티오우레아 착물이 발견되었다 : The present invention relates to a process for preparing clonidine which is shorter, less expensive and safer than the methods already known. Directly cyclized to the corresponding heterocyclic compound.                 A novel thiourea complex of formula (I) was found to produce: 상기식에서, Ar은 페닐 또는 나프틸이며, 치환되지 않거나 또는 Cl, F, Br, I, C 1- C 4- 알킬, 아릴, C 1- C 4- 알콕시 또는 아릴알콕시로 구성된 군으로부터 선택된 하나 이상의 기로 치환되고, NO 2 는 파라 또는 오르토 위치에 있고, n은 1 내지 4이다. Wherein Ar is phenyl or naphthyl, at least one unsubstituted or selected from the group consisting of Cl, F, Br, I, C 1 -C 4 -alkyl, aryl, C 1 -C 4 -alkoxy or arylalkoxy Substituted with a group, NO 2 is in the para or ortho position and n is 1-4.

Cyclic urea derivative

Cyclic urea derivative

내용없음

Reactive cyclic carbonates and ureas used to modify biomolecules, polymers and substrate surfaces

Process for the preparation of clonidine derivatives, as well as thiourea complexes which may be intermediates in the process

Preparation of asymmetric cyclic ureas through a monoacylated diamine intermediate

Fungicidal compositions, fungicidal compounds, their production and use

##STR1## Agricultural fungicidal compositions comprising compounds of formula (I-A), (I-B) or (I-C), wherein R 1 and R 7 are each independently hydrogen or C 1 -C 3 alkyl, R 2 is hydrogen or C 1 -C 6 alkyl, R 3 and R 4 independently, and each R 5 independently are hydrogen or C 1 -C 4 alkyl, R 6 is a cyclohexyl group or a monocyclic or bicyclic aromatic group, substituted with from 1 to 5 groups of the formula R 8 , wherein R 8 is halogen, a C 1 -C 10 alkyl group, a C 1 -C 10 alkoxy group, a tri-C 1 -C 4 -alkylsilyl group, or a phenoxy, phenyl, phenyl-C 1 -C 2 -alkylene, or phenyl-C 2 -alkenylene group, each optionally substituted on the phenyl or phenoxy group with one or more of halogen atoms, C 1 -C 6 alkyl or C 1 -C 6 alkyl or C 1 -C 6 alkoxy group, trihalomethyl groups, phenyl groups, or phenoxy groups, p is 0, 1 or 2, Y is a group of the formula --(CR 9 R 9 ) n --, wherein n is 2, 3, or 4, each R 9 independently is hydrogen or C 1 -C 4 alkyl and X is a suitable counter-ion, together with an agriculturally acceptable carrier or diluent, and novel fungicidal compounds of formula (I-A), (I-B), or (I-C), wherein p is 1 or 2 and n is 3 or 4.

Method for preparing N-monosubstituted and N,N'-disubstituted unsymmetrical cyclic ureas

本发明涉及用作HIV蛋白酶抑制剂的式(Ⅵa)和(Ⅵb)不对称取代的环状脲类化合物的一般制备方法。所述方法经异脲中间体完成。

Process for the preparation of nitrogen heterocycle-substituted (meth) acrylic acid esters

Process for the preparation of alkylimidazolidone methacrylates

methods for reducing the aldehyde content in an amine catalyst and for reducing aldehyde emissions from a polyurethane material, amine catalyst and conditioned product

1 / 1 resumo “mã‰todos para reduzir o teor de aldeãdo em um catalisador de amina e para reduzir emissã•es de aldeãdo de um material de poliuretano, catalisador de amina, e, produto acondicionado” a presente descriã§ã£o fornece um mã©todo para reduzir o teor de aldeã­do em um catalisador de amina tratando o catalisador de amina com um agente de tratamento selecionado de uma ureia cã­clica substituã­da com pelo menos um grupo reativo de isocianato, um removedor de radical livre e uma mistura dos mesmos. o catalisador de amina tratado pode entã£o ser usado na produã§ã£o de materiais de poliuretano que apresentam emissãµes de aldeã­do reduzidas. 1 / 1 abstract “Methods for reducing the villager content in an amine catalyst and for reducing villager emissions from a polyurethane material, amine catalyst, and conditioned product†a The present description provides a method for reducing the aldehyde content in an amine catalyst by treating the amine catalyst with a treating agent selected from a cyclic urea substituted with at least one isocyanate reactive group, a scavenger of free radical and a mixture thereof. the treated amine catalyst can then be used in the production of polyurethane materials that exhibit reduced aldehyde emissions.

Process for preparation of alkylimidazolidone (meth) acrylates

为了获得化学式(I)的化合物，让化学式(II)的一种酐与化学式(III)的一种杂环醇反应。反应之后，水解在(甲基)丙烯酸中的过量的(甲基)丙烯酸酐，通过加入水并且加热至25和70℃之间，优选在30和50℃之间，以便获得在水和(甲基)丙烯酸中的化学式(I)的化合物溶液。R 1 ＝氢或甲基；A和B各独立地表示直链或支链的亚烷基，有2至5个碳原子。

Urea derivatives of alpha, omega-diamino acids and peptides

Ureins derived from alpha,omega-diamino acids and process for their preparation

A kind of organic solvent recrystallization purification butylene pitches the method and device of two ureas

本发明涉及一种利用有机溶剂重结晶提纯丁烯叉二脲的方法及装置，该方法包括溶解与热过滤、冷却重结晶、以及洗涤与干燥步骤，最终得到了提纯的丁烯叉二脲纯品。热溶解过程用到了专门设计的多滤芯双层夹套恒温过滤器，该过滤器具有相互连通的内层夹套和外层夹套，过滤器的漏斗喉部装有吸附滤芯和过滤滤芯。与现有技术相比，本发明的方法简便易行，适用于放大进行大规模生产，具有产量高，成本低，耗时短等特点，经液相色谱及质谱分析表明提纯后的丁烯叉二脲产品纯度高，品质好；还可以进行循环精制，逐步提高产品品质和附加值，具有广阔的应用前景。

Novel process for preparation of clonidine derivatives

A novel process preparing clonidine derivatives has been discovered which is shorter, less expensive and safer than previously known methods. A new thiourea complex of formula (I) wherein: Ar is a phenyl or naphthyl and unsubstituted or substituted with one or more moieties selected from the group consisting of: Cl, F, Br, I, C1 to C4 alkyl, aryl, C1 to C4 alkoxy or arylalkoxy; NO2 is in the para or ortho position; and n is 1 to 4, has also been discovered which can be directly cyclized to produce the corresponding heterocyclic product.

METHOD FOR PRODUCING 2-HYDRAZINO-1,3-DIAZACYCLOALK-2-EN-HYDROHALOLGENIDES

This invention provides a process for preparing a 2-hydrazino-1,3-diazacycloalk-2-ene hydrohalide The process comprises reacting a one molar proportion of either tautomeric isomer of a 2-nitroamino-1,3-diazacycloalk-2-ene represented by the following formulas:wherein R¹ is hydrogen, C₁-C₆ alkyl, C,- C₆ hydroxyalkyl, C,-C₆ alkoxyalkyl, phenyl, substituted phenyl, benzyl, or substituted benzyl, R² and R³ are independently hydrogen, C,- C₆ alkyl, C₁-C₆ alkoxy, C,-C_s alkoxyalkyl, hydroxyl, aryl, substituted aryl, aralkyl and substituted aralkyl, and n is an integer from 0 to 3 with about an equimolar proportion of an ammonium halide or hydrazonium halide, and about a 1 to 2 molar proportion of hydrazine hydrate in a composition selected from a C, to C, aliphatic alcohol, water or a mixture thereof, at a temperature from about ambient to the reflux, and isolating the end product as a monohydrohalide.This invention also provides a process for preparing a 2- hydrazino 1. 3-diazacycloalk-2-ene dihydrohalide. The process comprises reacting a compound of the formula:wherein R¹ is hydrogen, C, to C₆ alkyl, or C, to C₆ hydroxyalkyl, R² and R³ are independently hydrogen or C, to C₆ alkyl, n is 0 to 3 and X is a halide ion, with hydrogen halide wherein the halide ion is the same as defined above in a C, to C₄ alkyl alcohol at about 0 to 30C.; and recovering the corresponding 2-hydrazino-1, 3-diazacycloalk-2-ene dihydrohalide.

New cyclic urea derivatives

Method for preparing n, n'-disubstitued cyclic ureas

Disubstituted cyclic ureas IV are prepared by reductive alkylation of I with aldehydes R22-CHO or R23-CHO in presence of a reducing agent to form II (step 1), followed by cyclocarbonylation of II to form III (step2) and deprotection of III to form the diol IV (step 3), according to the above schemes. These cyclic ureas IV are useful as HIV protease inhibitors.

Process for the production of urea derived from alpha, omega-diamino acids

Pentadienone hydrazones and their inorganic acid addition salt

Intermediates for the preparation of 4-phenyl-1,3-benzodiazepins and methods for preparing the intermediates

The invention relates to compounds of the formulawhere Y is -OH; halogen;-NHCH₃; R₁SO₃-, where R₁ is a straight chain or branched chain alkyl group having 1 to 5 carbon atoms, or aryl; and R₂ is -C(CH₃)₃ or -O-C(CH₃)₃. Processes for preparing the compounds are provided. The compounds are useful as intermediates in the preparation of 4-phenyl-1,3-benzodiazepins, which exhibit activity as antidepressants, analgetics and anti-convulsants.

Method for preparing N-monosubstituted and N,N'-disubstituted unsymmetrical cyclic ureas.

Compounds for use as chemical vapor deposition precursors, thermochromic materials light-emitting diodes, and molecular charge-transfer salts and methods of making these compounds

Novel compounds that may be used as chemical vapor deposition precursors, thermochromic materials, conductive polymers, light-emitting diode precursors, and molecular charge-transfer salt precursors are provided. In addition, a novel compound that can be used to make the aforementioned compounds is provided. Still further, another aspect of the present invention is to provide methods for making and using the novel compounds provided.

Process for the preparation of substituted tetrahydropyrimidinone derivatives

Known, herbicidally active, substituted tetrahydropyrimidinone derivatives of the general formula <IMAGE> in which Ar<1> and Ar<2> are identical or different and represent optionally substituted aryl and R<1>, R<2> and R<3> represent hydrogen or lower alkyl, are obtained by a novel process by reacting N,N'-disubstituted ureas of the general formula II, <IMAGE> with 1,3-dihaloalkanes of the general formula III <IMAGE> in which Hal<1> and Hal<2> are identical or different and represent halogen, in the presence of a diluent and in the presence of a strong base and, if appropriate, in the presence of a catalyst, at temperatures between +20 DEG C and +160 DEG C.

Insensitive polynitramine compound

The energetic compound 2,4,8,10-tetranitro-2,4,8,10-tetraazaspiro [5.5]undecane(TNSU) is disclosed. A general method of making 1,3-dinitroso-1,3-diazacycloalkanes in a one pot synthesis by the condensation of the diamine and formaldehyde, followed by conversion to the nitroso compound with nitrous acid. The general method also provides for the production of the tetranitroso precusor of TNSU.

Pyrimidinone synthesis

Preparation of alkylating agents and their use for alkylating cyclic ureas

(57)【要約】 本発明は、アルキル化剤を製造する方法および製造したアルキル化剤の使用に関するものである。特に、本発明は、ヒドロキシハライドおよび有機オキシハライドアルキル化剤の製法および環式尿素化合物のアルキル化に対する該アルキル化剤の使用に関するものである。

Thiourea compositions and uses thereof

The invention provides N,N′-disubstituted monothiourea or bis-thiourea-Pd(0) complexes that are useful as catalysts for palladium-catalyzed Heck reaction of aryl iodides and bromides with olefins, and as catalysts for palladium catalyzed Suzuki reactions of organoboric compounds and aryl halides.

Bisguanidines and fungicides containing them

O.Z. 0050/41835 Abstract of the Disclosure: The present invention relates to bisguanidine derivatives of the formula I I where R1 and R2 are each, independently of one another, hydro-gen, alkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkenyl; or cycloalkyl which has 5 - 12 carbon atoms in the ring and may be substitu-ted, or benzyl which may be substituted, with the proviso that only one of R1 and R2 can be hydrogen; or R1 and R2 are, together with the atoms which they substitute, a heterocyclic ring which may be substituted; X is CH2, O, a single bond, NH, N-alkyl or N-benzyl whose phenyl ring may be substituted, n is 5 to 8, and their plant-compatible acid addition salts and their metal complexes and fungicides containing these compounds.

Bis(cyclic ureas) and polyurethanes derived therefrom 026

Process for producing cyclic ureas

ABSTRACT OF THE DISCLOSURE A process for producing a cyclic urea by reacting a diamine directly with phosgene with a high yield and a cheap cost is provided, which process comprises reacting a diamine expressed by the Formula R-HN-R'-NH-R wherein R represents hydrogen atom or a lower alkyl group and R' represents dimethylene group, trimethylene group, tetramethylene group or a lower alkyl group-substituted dimethylene group, trimethylene group or tetramethylene group except for three particular combinations of R with R', with phosgene substantially in the presence of water and a dehydrochlorinating agent to obtain a cyclic urea expressed by the formula

Intermediates for the preparation of 4-phenyl-1,3-benzodiazepins and methods for preparing the intermediates.

The invention relates to compounds of the formula < IMAGE > where Y is -OH halogen < IMAGE > R1SO3-, where R1 is a straight chain or branched chain alkyl group having 1 to 5 carbon atoms, or aryl and R2 is -C(CH3)3 or -O-C(CH3)3. Processes for preparing the compounds are provided. The compounds are useful as intermediates in the preparation of 4-phenyl-1,3-benzodiazepins, which exhibit activity as antidepressants, analgetics and anticonvulsants.

Preparation of acrylates and methacrylates

Acrylates or methacrylates I ##STR1## (A and B=C 2 -C 5 -alkylene, R 1 =H, CH 3 ) are prepared by reacting an acrylate or methacrylate II ##STR2## (R 2 =C 1 -C 4 -alkyl) with a heterocycle III ##STR3## in the presence of titanium alcoholates chelate compounds of the metals titanium, zirconium, iron and zinc with 1,3-dicarbonyl compounds.

Bis(cyclic ureas) and polyurethanes derived therefrom

ABSTRACT OF THE DISCLOSURE Bis(cyclic ureas) are disclosed which have the formula wherein R is -?-alkylenen(C1-11)-?- or and CnH2n is ethylene or 1,3-propylene each of which can be substituted by one or more inert substituents. These compounds are useful as masked diisocyanates which, on heating in the presence of a polyol and, optionally, a polyurethane catalyst give rise to polyurethane resins. Accordingly they are useful as a component of storage stable compositions which are convertible to polyurethanes upon heating. Such compositions are particularly useful as solvent-less coating compositions. The properties of the above compounds are distinguished in a number of respects from the known bis(cyclic ureas) in which CnH2n has 4 or more carbon atoms in the chain between the valencies. Illustratively, the above compounds are more stable on exposure to heat in the absence of catalysts but, in the presence of polyurethane catalysts react with polyois at a significantly faster rate than the prior art compounds.

4-Phenyl-1,3-benzodiazepines

Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.

PROCESS FOR THE PREPARATION OF ALKYLIMIDAZOLIDONE (METH) ACRYLATE.

A compound (I) is prepared by reacting at least one (meth)acrylate (II) with a heterocyclic alcohol (III) in the presence of at least one catalyst chosen from tin dialkyloxides and/or tin dialkyldialkoxides. <??>Alkylimidazolidone acrylates and methacrylates are known for the part they play in the constitution of polymers which are useful as coatings and adhesives and for paper and textile treatment, as well as for their use as leather treatment agents and in the production of emulsion paints. R1 = H, CH3; A,B = alkylene group with a straight or branched chain containing from 2 to 5 carbon atoms.