Optically active cyclobutyl pyrimidine

The compound of the formula см. иллюстрацию в PDF-документе [1R-(1α(E),2β,3α)]-1-[2,3-bis(hydroxymethyl)cyclobutyl]-5 - (2-bromoethenyl)-2,4(1H,3H)-pyrimidinedione, is an antiviral agent that is active against herpes simplex virus 1 and varicella-zoster virus.

Bis protected (hydroxymethyl)cyclobutanols

Cyclobutanols of the formula см. иллюстрацию в PDF-документе wherein P is a hydroxy protecting group are useful intermediates in the preparation of antiviral compounds.

6-Benzalimino-6-arylthio penicillanic acids and derivatives thereof

... 6-Amino and 6-benzalimino-6-arylthio penicillins are disclosed. These compounds are useful as intermediates in the preparation of 6-acylamino-6-arylthio penicillins.

7-(α-Cyanomethylthio)acetamido-3-cephem carboxylates

New 7-(α-cyanomethylthio)acetamido-3-cephem carboxylates which have the formula см. иллюстрацию в PDF-документе have antimicrobial activity.

Process for converting 3-methylene cephalosporins to 3-heterothiomethyl cephalosporins

This invention relates to the preparation of 3-heterothiomethyl cephalosporanic acid esters of the formula см. иллюстрацию в PDF-документе by treating a 3-methylene cephalosporin of the formula см. иллюстрацию в PDF-документе with a compound of the formula HETERO-S-S-hetero or X-S-hetero in the presence of a base wherein R is a readily removable ester group, R1 is in the α-configuration and is hydrogen or methoxy, and X is a leaving group. The resulting 3-heterothio cephalosporin esters are treated according to known methods to remove the ester protecting group and yield the corresponding free acids which have antibacterial activity.

6-Amino-6-arylthio penicillanic acids and derivatives thereof

... 6-Amino and 6-benzalimino-6-arylthio penicillins are disclosed. These compounds are useful as intermediates in the preparation of 6-acylamino-6-arylthio penicillins.

3-acylamino-2-oxo-1-azetidinyl esters of phosphonic acids, phosphoric acid and phosphoric acid esters

Antimicrobial activity is exhibited by β-lactams having a см. иллюстрацию в PDF-документе substituent in the 1-position and an acylamino substituent in the 3-position, or a pharmaceutically acceptable salt thereof; wherein Y is oxygen or sulfur and R5 is hydroxyl, alkyl, substituted alkyl, phenyl, substituted phenyl, alkoxy, alkylthio, (substituted alkyl)oxy, (substituted alkyl)thio, phenyloxy, phenylthio, (substituted phenyl)oxy or (substituted phenyl)thio.

Hydroxymethyl(methylenecyclopentyl) purines and pyrimidines

Antiviral activity is exhibited by compounds having the formula см. иллюстрацию в PDF-документе and its pharmaceutically acceptable salts.

2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines

Antibacterial activity is exhibited by 3-acylamino-2-oxoazetidines having in the 1-position an activating group of the formula см. иллюстрацию в PDF-документе wherein R is см. иллюстрацию в PDF-документе and R4 is см. иллюстрацию в PDF-документе ...

Bis (hydroxymethyl) cyclobutyl triazolopyrimidines

Antiviral activity is exhibited by compounds having the formula см. иллюстрацию в PDF-документе and its pharmaceutically acceptable salts wherein R1 is см. иллюстрацию в PDF-документе R6 is hydrogen, alkyl, substituted alkyl, or aryl; and R7 and R8 are independently hydrogen, см. иллюстрацию в PDF-документе ...

Bis (hydroxymethyl) cyclobutyl purines

Antiviral activity is exhibited by compounds having the formula см. иллюстрацию в PDF-документе and its pharmaceutically acceptable salts wherein R1 is см. иллюстрацию в PDF-документе wherein R2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; or trifluoromethyl; R5 is alkyl; R6 is hydrogen, alkyl, substituted alkyl, or aryl; and R7 and R8 are independently hydrogen, см. иллюстрацию в PDF-документе ...

[3S(Z)]-2-[[[1-(2-amino-4-thiazolyl)-2-[[2,2-dimethyl-4-oxo-1-(sulfoo xy)-3-azetidinyl]amino]-2-oxoethylidene]-amino]oxy] acetic acid and intermediate

Pharmaceutically acceptable salts of [3S(Z)]-2-[[[1-(2-amino-4-thiazolyl)-2-[[2,2-dimethyl-4-oxo-1-(sulfooxy)-3 -azetidinyl]amino]-2-oxoethylidene]amino]oxy] acetic acid and a process useful in the preparation of such salts are disclosed herein.

7-α substituted imino 7-β substituted thio cephalosporin derivatives

An improved, versatile method for producing 7-cephalosporin derivatives having a 7-alkylthio or 7-arylthio group which comprises treating a 7-substituted imino halide, imino ether or iminothio ether of 7-aminocephalosporanic acid, 7-amino-3-desacetoxycephalosporanic acid and the like with a thiolating agent in the presence of a base, to obtain the thio derivative. These products are particularly useful for conversion to 7α-alkylthio or 7α-arylthio-7-acylamino intermediates which are converted to lower alkoxy cephalosporin derivatives useful as antibacterial agents.

2-Oxoazetidin-1-yloxymethyl sulfonic acid and analogs

Antibiotic activity is exhibited by β-lactams having an см. иллюстрацию в PDF-документе substituent in the 1-position and an acylamino substituent in the 3-position.

Certain carbamate ester derivatives forming salts with pyridinium or picolinium cations which are useful as intermediates

Disclosed herein is a process for preparing a compound having the formula см. иллюстрацию в PDF-документе which comprises sulfonating a compound having the formula см. иллюстрацию в PDF-документе with a complex having the formula см. иллюстрацию в PDF-документе and cyclizing the resulting compound having the formula см. иллюстрацию в PDF-документе by treatment with a base.

Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method

Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure см. иллюстрацию в PDF-документе including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) --O--; or (3) см. иллюстрацию в PDF-документе B is: см. иллюстрацию в PDF-документе and wherein L2, L1, R1, R2, R3, R3', R3a, R3b, R4, R4', R5, X, см. иллюстрацию в PDF-документе are as defined herein.

Process for preparing a 2-oxo-1-azetidinesulfonic acid salt

A pharmaceutically acceptable salt of (R)-3-(acetylamino)-3-methoxy-2-oxo-1-azetidinesulfonic acid can be prepared by culturing Chromobacterium violaceum A.T.C.C. No. 31532 at about 25° C. under submerged aerobic conditions on an aqueous nutrient medium containing an assimilable carbohydrate and nitrogen source.

Hydroxymethyl (methylenecyclopentyl) purines and pyrimidines

Antiviral activity is exhibited by compounds having the formula см. иллюстрацию в PDF-документе and its pharmaceutically acceptable salts.

Process for chemically removing the acyl sidechain from cephalosporins and penicillins

A process for removing the acyl sidechain from penicillins and cephalosporins which comprises chlorinating the acyl compound and treating the resulting iminochloride with an o-aminothiophenol to obtain the corresponding 6β-aminopenicillin or 7β-aminocephalosporin.

3-Acylamino-1-carboxymethylaminocarbonyl-2-azetidinones

Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula см. иллюстрацию в PDF-документе (or a salt or ester thereof).

4-Thio substituted-Δ2 cephalosporin intermediates

Cephalosporin intermediates of the formulas см. иллюстрацию в PDF-документе wherein R is lower alkyl, 2,2,2-trichloroethyl, diphenylmethyl, p-methoxybenzyl, or p-nitrobenzyl; R1 is lower alkyl or phenyl; R2 is hydrogen or acetoxy; R4 is methyl or ethyl; and R5 is hydrogen, methyl, or methoxy; are disclosed. Methods of reacting these intermediates to prepare antibacterially active cephalosporins are disclosed.

6-Arylthio penicillanic acid and derivatives thereof

Disclosed herein are penicillanic acids and derivatives thereof which are substituted in the 6-position, processes for preparing such compounds and the utility thereof. The compounds of the invention have been found to be useful as antibacterial agents.

Derivatives of diumycin A and diumycin A'

This invention relates to lower alkyl or aryl lower alkyl esters of Diumycin A and Diumycin A', their basic hydrolysis products, and alkyl aminolysis hydrolysis products of Diumycin A and Diumycin A', which are effective against gram-positive bacteria.

Hydroxymethyl cyclobutyl purines

Antiviral activity is exhibited by compounds having the formula см. иллюстрацию в PDF-документе and their pharmaceutically acceptable salts. R1 is см. иллюстрацию в PDF-документе R2 is hydrogen, --PO3 H2, см. иллюстрацию в PDF-документе wherein R3 is hydrogen, alkyl, substituted alkyl, or aryl, and R4 is alkyl.

Process for preparing 4,4-dialkyl-2-azetidinones utilizing a pyridine (or substituted pyridine) sulfur trioxide complex

Disclosed herein is a process for preparing a compound having the formula см. иллюстрацию в PDF-документе which comprises sulfonating a compound having the formula см. иллюстрацию в PDF-документе with a complex having the formula см. иллюстрацию в PDF-документе and cyclizing the resulting compound having the formula см. иллюстрацию в PDF-документе by treatment with a base.

2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines

Antibacterial activity is exhibited by β-lactams having a см. иллюстрацию в PDF-документе substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur, and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (Rc), phenylalkyl, (substituted phenyl)alkyl, Rc -alkyl or --NRa Rb wherein Ra and Rb are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of Ra and Rb is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, Rc, Rc -alkyl, Rc -alkoxy, alkylsulfonyl, alkylmethyleneamino, phenylmethyleneamino ...

Mercury intermediates useful in the preparation of 2-alkoxy cephalosporins

Compounds of the formula см. иллюстрацию в PDF-документе WHEREIN R1 is lower alkyl, diphenylmethyl, 2,2,2-trichloro-ethyl, p-methoxybenzyl, or p-nitrobenzyl; R2 is hydrogen or acetoxy; R5 is lower alkyl; and R4 is см. иллюстрацию в PDF-документе wherein R3 is a heterocyclic group, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, substituted phenyl, phenyl-lower alkyl, or phenoxy and X is hydrogen, protected amino or protected hydroxy provided that X is protected amino or protected hydroxy only when R3 is phenyl, substituted phenyl, or cycloalkadienyl, are disclosed. These compounds are useful as intermediates in the preparation of antibacterially active 2-alkoxy cephalosporins.

Method for producing 2-(substituted thio)-3-cephem derivatives

Treatment of a 7-imido-3-cephem carboxylic acid ester with a thiolating agent in the presence of a strong base yields a 4-(substituted thio)-2-cephem derivative which can be made to rearrange by use of a strong acid to obtain a 2-substituted thio-2-cephem derivative which has antimicrobial activity.

Method for preparing 7-substituted cephalosporins and 6-substituted penicillins by replacement of sulfur-containing groups

Disclosed is a method for replacing 7-lower alkylthio and 7-arylthio groups from cephalosporins with lower alkanoyloxy,lower alkoxy, aryloxy, aroyloxy, amino, lower alkylamino and azido moieties, and for replacing 6-lower alkylthio and 6-arylthio groups from penicillins with lower alkanoyloxy, lower alkoxy, aryloxy, aroyloxy, amino, lower alkyl amino, and azido moieties.

Cyclobutane derivatives

Cyclobutane derivatives of the formulas см. иллюстрацию в PDF-документе wherein P is a hydroxy protecting group and X is a leaving group are useful intermediates in the preparation of antiviral compounds.

4-Thio substituted-Δ2 -cephalosporin intermediates

Cephalosporin intermediates of the formulas см. иллюстрацию в PDF-документе wherein R is lower alkyl, 2,2,2-trichloroethyl, diphenylmethyl, p-methoxybenzyl, or p-nitrobenzyl; R1 is lower alkyl or phenyl; R2 is hydrogen or acetoxy; R4 is methyl or ethyl; and R5 is hydrogen, methyl, or methoxy; are disclosed. Methods of reacting these intermediates to prepare antibacterially active cephalosporins are disclosed.

2-oxo-1-azetidinesulfonic acid salts

Antibacterial activity is exhibited by β-lactams having a sulfonic acid salt substituent in the 1-position and an amino or acylamino substituent in the 3-position.

Acid derivatives useful as serine protease inhibitors

Compounds having the formula (I), are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, IXa, Xa, and/or XIa, wherein ring B is phenyl or pyridyl, W is preferably C(═O)NR 4 R 5 , L is a linker group, X 2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification.

3-acylamino-2-oxo-1-azetidinyl esters of phosphonic acids, phosphoric acid and phosphoric acid esters

ABSTRACT Novel .beta.-lactams having the formula:

PROCESS FOR THE PREPARATION OF 4,4-DIALKYL-2-AZETIDINONES, AND NOVEL COMPOUNDS THUS PREPARED

PROCESS FOR THE PREPARATION OF 4,4-DIALKYL-2-AZETIDINONES, AND NOVEL COMPOUNDS THUS PREPARED

PROCEDE DE PREPARATION D'UN COMPOSE DE FORMULE (CF DESSIN DANS BOPI) QUI CONSISTE A SULFONER UN COMPOSE DE FORMULE (CF DESSIN DANS BOPI) AVEC UN COMPLEXE DE FORMULE (CF DESSIN DANS BOPI) ET A CYCLISER LE COMPOSE RESULTANT AYANT POUR FORMULE (CF DESSIN DANS BOPI) PAR TRAITEMENT AVEC UNE BASE; A ETANT UN RADICAL BENZYLOXYCARBONYLE, PARA-NITROBENZYLOXYCARBONYLE, T-BUTYLOXYCARBONYLE, O-NITROPHENYLSULFENYLE OU TRIPHENYLMETHYLE; R ET R ETANT IDENTIQUES OU DIFFERENTS ET ETANT CHACUN UN RADICAL ALKYLE DE 1 A 4 ATOMES DE CARBONE; R ETANT UN RADICAL BENZYLE, PARA-NITROBENZYLE, BENZYLOXYMETHYLE, 2-METHOXY-2-PROPYLE, 2-ETHOXY-2-PROPYLE, TETRAHYDROPYRAN-2-YLE, 2-TRIMETHYLSILYLETHYLE, T-BUTYLDIMETHYLSILYLE OU T-BUTYLDIPHENYLSILYLE; ET M ETANT EGAL A 0, 1, 2 OU 3. CERTAINS DE CES COMPOSES SONT DES AGENTS ANTIBACTERIENS. PROCESS FOR PREPARING A COMPOUND OF FORMULA (CF DRAWING IN BOPI) WHICH CONSISTS OF SULFONING A COMPOUND OF FORMULA (CF DRAWING IN BOPI) WITH A COMPLEX OF FORMULA (CF DRAWING IN BOPI) AND CYCLING THE RESULTING COMPOUND WITH FORMULA ( CF DRAWING IN BOPI) BY PROCESSING WITH A BASE; A BEING A BENZYLOXYCARBONYL, PARA-NITROBENZYLOXYCARBONYL, T-BUTYLOXYCARBONYL, O-NITROPHENYLSULFENYL, OR TRIPHENYLMETHYL RADICAL; R AND R BEING THE SAME OR DIFFERENT AND EACH BEING A RADICAL ALKYL OF 1 TO 4 CARBON ATOMS; R BEING A RADICAL BENZYL, PARA-NITROBENZYL, BENZYLOXYMETHYL, 2-METHOXY-2-PROPYL, 2-ETHOXY-2-PROPYL, TETRAHYDROPYRAN-2-YLE, 2-TRIMETHYLSILYLELSYLDIM-BUTHYLSILYLELSYLDIM-T-BUTHYLSILYLELSYLDIM-BUTHYLSILYLELSYLDIM-BUTHYLSILYLELSYLDIM-T-BUTHYLELSYLD-BUTHYLSILYLELSYLD-BUTHYLSILYLELSYLD-BUTHYLD-BUTHYLELSYL AND M BEING 0, 1, 2 OR 3. SOME OF THESE COMPOUNDS ARE ANTIBACTERIAL AGENTS.

PROCESS FOR TRANSFORMATION OF 3-METHYLENECEPHALOSPORINS INTO 3-HETEROTHIOMETHYLCEPHALOSPORINS

L'invention concerne la préparation d'esters d'acides 3-hétérothiométhylcéphalosporaniques de formule : The invention relates to the preparation of esters of 3-heterothiomethylcephalosporanic acids of the formula:

USEFUL MERCURIC INTERMEDIARIES IN THE PREPARATION OF 2-ALCOXYCEPHALOSPORINS

Diumycin a' and b' and salts thereof from streptomyces umbrinus

Derivatives of diumycin A and diumycin A'

This invention relates to lower alkyl or aryl lower alkyl esters of Diumycin A and Diumycin A', their basic hydrolysis products, and alkyl aminolysis hydrolysis products of Diumycin A and Diumycin A', which are effective against gram-positive bacteria.

Beta lactam compounds and their use as inhibitors of tryptase

Compounds of the formulas:are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.

2-OXO-1-SULPHONYLAMINOCARBONYL-AZETIDINES AND PROCEDURES FOR THEIR PREPARATION

Acid derivatives useful as serine protease inhibitors

Compounds having the formula (I), are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, Ixa, Xa, and/or Xia, wherein ring B is phenyl or pyridyl, W is preferably C(=O)NR4R5, L is a linker group, X2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R1, R2, R3, R4, R5 and R6 are as defined in the specification.

Process for chemically removing the acyl sidechain from cephalosporins and penicillins

A process is provided for removing the acyl sidechain from penicillins and cephalosporins which comprises chlorinating the acyl compound and treating the resulting iminochloride with an o-aminothiophenol to obtain the corresponding 6β-aminopenicillin or 7β-aminocephalosporin.

3-acylamino-2-oxo-1-azetidinyl esters of phosphonic acids phosphoric acid phosphoric acid esters

Mercury intermediates useful in the preparation of 2-alkoxy cephalosporins

Compounds of the formula ##STR1## WHEREIN R 1 is lower alkyl, diphenylmethyl, 2,2,2-trichloro-ethyl, p-methoxybenzyl, or p-nitrobenzyl; R 2 is hydrogen or acetoxy; R 5 is lower alkyl; and R 4 is ##STR2## wherein R 3 is a heterocyclic group, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, substituted phenyl, phenyl-lower alkyl, or phenoxy and X is hydrogen, protected amino or protected hydroxy provided that X is protected amino or protected hydroxy only when R 3 is phenyl, substituted phenyl, or cycloalkadienyl, are disclosed. These compounds are useful as intermediates in the preparation of antibacterially active 2-alkoxy cephalosporins.

Hydroxymethylcyclobutylpurine

Amidino and guanidino azetidinone tryptase inhibitors

Compounds of formulae (I), (II), (III).

Substituted methylene cyclopentyl-substituted purines and pyrimidines which exhibit antiviral activity

6-Arylthio penicillanic acid and derivatives thereof

Disclosed herein are penicillanic acids and derivatives thereof which are substituted in the 6-position, processes for preparing such compounds and the utility thereof. The compounds of the invention have been found to be useful as antibacterial agents.

Intermediates for production of bis (hydroxymethyl) cyclobutyl purines and pyrimidines

PROCESS FOR PREPARING 4,4-DIALKYL-2-AZETIDINONE COMPOUNDS

Die Erfindung betrifft ein Verfahren zur Herstellung von 4,4-Dialkyl-2-azetidinon-Verbindungen. Die Verbindungen sind Zwischenprodukte bei der Herstellung von Antibiotika. The invention relates to a process for the preparation of 4,4-dialkyl-2-azetidinone compounds. The compounds are intermediates in the production of antibiotics.

Zpusob vyroby beta laktamovych antibiotik

AMIDINO AND GUANIDINO-AZETIDINONE TRYPTASE INHIBITORS

PROCEDURE FOR THE PREPARATION OF ANTIBIOTIC ACTIVE BETA LACTAMES

Bis(hydroxymethyl)cyclobutylpurines and -pyrimidines, method of their preparation and use

Antiviral activity is exhibited by compounds having the formula and its pharmaceutically acceptable salts wherein R 1 is wherein R 2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; R 3 is fluoro, chloro, bromo, iodo, hydrogen, methyl, trifluoromethyl, ethyl, n-propyl, 2-fluoroethyl, 2-chloroethyl, or wherein R 4 is chloro, bromo, iodo, hydrogen methyl or trifluoromethyl; R s is alkyl; R 6 is hydrogen, alkyl, substituted alkyl, or aryl; and R 7 and R 8 are independently hydrogen,

4-Thio substituted-Δ2 cephalosporin intermediates

Cephalosporin intermediates of the formulas ##STR1## wherein R is lower alkyl, 2,2,2-trichloroethyl, diphenylmethyl, p-methoxybenzyl, or p-nitrobenzyl; R 1 is lower alkyl or phenyl; R 2 is hydrogen or acetoxy; R 4 is methyl or ethyl; and R 5 is hydrogen, methyl, or methoxy; are disclosed. Methods of reacting these intermediates to prepare antibacterially active cephalosporins are disclosed.

Azetidinones

ABSTRACT AZETIDINONES Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula

PROCEDURE FOR FRAMSTATION OF 4,4-DIALKYL-2-AZETIDINONER.

Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method

An optically active cyclobutyl pyrimidine

The compound of the formula [1 R-(1α(E),2β,3α)]-1-[2,3-bis(hydroxymethyl)cyclobutyl]-5-(2-bromoethenyl)-2,4(1H,3H)-pyrimidinedione, is an antiviral agent that is active against herpes simplex virus 1 and varicella-zoster virus.

AZETIDINYL SULFONIC ACID AND ANALOGS WITH THERAPEUTIC ACTION

B-LACTAMES PORTANT UN SUBSTITUANT (CF DESSIN DANS BOPI) EN POSITION 1 ET UN SUBSTITUANT ACYLAMINE EN POSITION 3. ILS REPONDENT A LA FORMULE : (CF DESSIN DANS BOPI) DANS LAQUELLE R EST UN RADICAL ACYLE, UN ATOME D'HYDROGENE OU UN GROUPEMENT PROTECTEUR DE LA FONCTION AMINE, R EST UN ATOME D'HYDROGENE OU UN RADICAL METHOXY, R, R, R ET R SONT IDENTIQUES OU DIFFERENTS ET SONT CHACUN, DE PREFERENCE, UN ATOME D'HYDROGENE OU UN RADICAL ALKYLE INFERIEUR. CES COMPOSES SONT UTILISABLES COMME AGENTS ANTIBACTERIENS. B-LACTAMES CARRYING A SUBSTITUTE (CF DRAWING IN BOPI) IN POSITION 1 AND AN ACYLAMINE SUBSTITUTE IN POSITION 3. THEY MEET THE FORMULA: (CF DRAWING IN BOPI) IN WHICH R IS A RADICAL ACYL, A HYDROGEN ATOM OR A A PROTECTIVE GROUP OF THE AMINE FUNCTION, R IS A HYDROGEN ATOM OR A RADICAL METHOXY, R, R, R AND R ARE THE SAME OR DIFFERENT AND ARE EACH, PREFERRED, A HYDROGEN ATOM OR A LOWER RADICAL ALKYL. THESE COMPOUNDS CAN BE USED AS ANTIBACTERIAL AGENTS.

Lactam compounds and their use as inhibitors of serine proteases and method

Lactam inhibitors are provided which have the structure X is wherein Y is O or S and R 4 is  R 7 O— or R 8 and R 1 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 8 , are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants, and are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating cardiovascular diseases associated with thromboses and for treating asthma and related diseases are also provided.

BETA-LACTAMANTIBIOTIC AGENTS

PROCESS FOR THE PREPARATION OF 4,4-DIALKYL-2-AZETIDINONES

Hydroxymethylcyclobutylpurine

Hydroxymethyl (methylenecyclopentyl) purines and pyrimidines

Antiviral activity is exhibited by compounds having the formula <CHEM> and its pharmaceutically acceptable salts. v

Procedimento per la preparazione di 4,4-dialchil-2-azetidinoni.

Esteri 3-acilammino-2-osso-1-azetidinilici di acidi fosfonici, acido fosforico e esteri dell'acido fosforico ad attivita'antimicrobica.

Method for preparing 7-substituted cephalosporins by replacement of o- or s-containing groups

Acido azetidinil solfonico ed analoghi.

Hydroxymethyl(methylencyclopentyl)purinen und pyrimidinen

Amidino- und guanidino-azetidinone tryptase- inhibitoren

Verfahren zur chemischen abspaltung des acylrestes von cephalosporinen und penicillinen.

Konformationseingeschränkte aromatische inhibitoren des microsomalen triglyceridtransferproteins und verfahren

Mikroszomális trigliceridtranszfer-proteint gátló aromás inhibitorok

A találmány tárgyát a mikrőszőmális trigliceridtranszfer-prőteintgátló (I), (IA) és (IB) általánős képletű, új vegyületek - ahől q= 0, 1 vagy 2; A őxigénatőm, iminőcsőpőrt, vagy A és R2 gyűrűt képez; B (m), (n) vagy (ő), illetve (p), (q), (r) vagy (s) általánős képletűcsőpőrt, amelyekben a gyűrűrendszer adőtt esetben szűbsztitűált (R3,R3', R4, R4', R3a és R3b különféle szűbsztitűenseket jelenthetnek)és/vagy heterőatőmő(ka)t tartalmaz (a Het jelölés 5 vagy 6 tagú, 1-4heterőatőmőt, azaz őxigén-, kén- vagy nitrőgénatőmőt tartalmazó gyűrűtjelez, és X előnyösen vegyértékvőnal, őxigén- vagy kénatőm); Rx hidrőgénatőm, alkil- vagy arilcsőpőrt; és R1 hidrőgénatőm, adőtt esetben szűbsztitűált és/vagy őxigén-, kén-vagy nitrőgénatőmőn keresztül kapcsőlódó és/vagy heterőatőmő(ka)ttartalmazó, nyílt láncú vagy gyűrűs, arőmás vagy nemarőmásszénhidrőgéncsőpőrt, szűbsztitűált főszfinilcsőpőrt, de alegelőnyösebb vegyületek képletében aril- vagy heterőaril-, különösenfenil-, imidazőlil-, benzimidazőlil-, indőlil- vagy piridilcsőpőrt,különösen (cő), (cp), (cq), (cr), (cs) vagy (ct) képletű csőpőrt; R2 űgyanaz, mint R1, de előnyösen pőliflűőr-alkil-, adőtt esetbenszűbsztitűált heterőciklőalkil- vagy dialkőxi-főszfinil-csőpőrt; L1 adőtt esetben szűbsztitűált és/vagy telítetlen kötés(eke)t és/vagyheterőatőmő(ka)t tartalmazó alkiléncsőpőrt; és L2 űgyanaz, mint L1, de előnyösen vegyértékvőnal vagy alkiléncsőpőrt -és N-őxidjaik vagy sóik, valamint a szérűmlipidszint csökkentésére ésaz aterőszklerózis vagy azzal rőkőn betegségek kezelésére valóalkalmazásűk képezik. ŕ

2-oxo-1-(((substituted sulfonyl)amino)-carbonyl)azetidines

Antibacterial activity is exhibited by beta -lactams having a -@-NH-SO2R substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (Rc), phenylalkyl, (substituted-phenyl)alkyl, Rc-alkyl or -NRaRb wherein Ra and Rb are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, (substituted phenyl)alkyl or one of Ra and Rb is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino (-NH2), alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl- amino, hydroxy, cyano (-C IDENTICAL N), alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, Rc as defined, above Rc-alkyl, Rc-alkoxy, alkylsulfonyl, alkylmethyleneamino, (alkyl-CH=N-), phenylmethyleneamino or (substituted phenyl)methyleneamino.

Process for producing 2-oxo-1-figure bracket-square bracket-bracket-substituted sulfonyl-bracket closed-amino-square bracket closed-carbonyl-figure bracket closedazetidines

Fremgangsmaade til fremstilling af 2-oxo-1(((substitueret sulfonyl)amino)-carbonyl)azetidiner

2-oxo-1-<<(substituted sulfonyl)amino>-carbonyl>azetidines

Lactam compounds and their use as inhibitors of serine proteases and method

Lactam compounds and their use as inhibitors of serine proteases and method

Lactam inhibitors are provided which have the structure (I), x is (a) or (b) wherein Y is O or S and R4 is (i), (ii) or R8 at least one of R?1 and R2¿ is hydrogen, and R?1, R2, R3, R5, R6, R7, and R8¿, are as defined herein. These compounds are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating asthma and related diseases are also provided.