Abstract: A cephalosporin derivative of the formula: ##STR1## in which R.sup.0 is a hydrogen atom or a methyl radical, R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is a hydrogen atom or a 1-6C alkoxy or 1-6C alkylthio radical; X.sup.1 is a sulphur or oxygen atom, a CH.sub.2 radical or a radical of the formula NR.sup.7 in which R.sup.7 is a hydrogen atom, a 1-6C alkyl, formyl or benzyl radical; X.sup.2 is a nitrogen atom or a radical of the formula N.sup..sym. -R.sup.7 ; R.sup.4 and R.sup.7, and R.sup.5 and R.sup.6 are a variety of substituents which are described in the specification; and the pharmaceutically-acceptable acid- or base-addition salts thereof. Pharmaceutical compositions, manufacturing processes and intermediates are also described.

Abstract: Naphthylglycyl and tetrahydronaphthylglycyl cephalosporins are potent antibacterial agents and are particularly useful as oral treatments for upper respiratory infections.

Abstract: Cysteic acid and homocysteic acid analogues of methotrexate and aminopterin having antitumor activity and low toxicity are soluble in water at a physiological pH ranging from 7.2-7.5.

Abstract: Compounds according to the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl or hydroxy lower alkyl;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;A is an amide forming group wherein the nitrogen substituents are: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms; cycloalkyl of 3 to 7 carbon atoms or cycloalkyl lower alkyl of 4 to 11 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, OH, --OCOR.sub.5, halo, --NH.sub.2, --N(R.sub.5).sub.2, --NHCOR.sub.5, --COOH, or --COO(R.sub.5) group wherein R.sub.

Abstract: Novel cephalosporins which has attached to the exomethylene group at the 3-position of the cephem ring a substituted or unsubstituted aryl, acylamino, aromatic heterocyclic, triazolyl or tetrazolyl group, said aromatic heterocyclic group being attached through a carbon-carbon bond and said triazolyl or tetrazolyl group being attached through a carbon-nitrogen bond, and has the following group attached to the amino group at the 7-position: ##STR1## wherein A represents a group of the formula, --CH.sub.2 -- or a group of the formula ##STR2## in which R.sup.5 represents a hydrogen atom or an alkyl group, and the bond represents syn or anti isomer or their mixture; R.sup.3 represents a hydrogen or halogen atom; and R.sup.4 represents a hydrogen atom or an amino group which may be protected or substituted. These cephalosporins have a broad antibacterial spectrum, are stable against .beta.-lactamase produced by bacteria, have a low toxicity, and are well absorbed when administered orally or parenterally.

Abstract: Bacteriostatic cephem compounds and processes for preparing same having the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkyl, esterified carbony(lower)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, lower alkenyl or lower alkynyl,R.sup.3 is a heterocyclic group substituted with amino(lower)alkyl, protected amino(lower)alkyl, hydroxy(lower)alkyl or both amino and lower alkyl,R.sup.4 is carboxy or protected carboxy, provided that R.sup.3 is a heterocyclic group substituted with hydroxy(lower)alkyl or both amino and lower alkyl, when R.sup.2 is lower alkyl, and its pharmaceutically acceptable salt.

Abstract: The invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl, andR.sup.3 is carboxy or protected carboxy,and a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to novel 7-acylamino-3-vinylcephalosporanic acid derivatives of high antimicrobial activity, to processes for preparation thereof from novel intermediates, and to said intermediates of the formula: ##STR1## in which R.sub.A is a group of the formula: ##STR2## wherein R.sup.1 is amino-substituted-heterocyclic group which may have halogen, protected amino-substituted-heterocyclic group which may have halogen, or a group of the formula: ##STR3## wherein R.sup.3 is lower alkyl,R.sup.8 is aryl,A is lower alkylene which may have a substituent selected from the group consisting of amino, a protected amino group, hydroxy, oxo and a group of the formula:.dbd.N.about.OR.sup.4,whereinR.sup.

Abstract: Novel syn isomers of 7-amino-thiazolyl-acetamido-3-acetoxymethyl-cephalosporanic acid derivatives of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of --CN, --CONH.sub.2 and --COOR.sub.1 ', R.sub.1 ' is selected from the group consisting of alkyl of 1 to 3 carbon atoms, hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, R' and R" are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms with the ##STR2## group in the syn position with the proviso that when R.sub.1 is --COOR.sub.1 ' and R.sub.1 ' is hydrogen, A is hydrogen and when R.sub.1 is --COOR.sub.1 ' and R.sub.

Abstract: Intermediates of the formula ##STR1## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl, Y is halogen, R.sup.3 is hydrogen, lower alkyl, aryl or aryl-(lower alkyl)--, R.sup.20 l is lower alkoxy and R.sup.42 is hydrogen, lower alkyl, aryl or aryl-(lower alkyl) or a group of the formula --A--Y in which A and Y are as above, are described.

Abstract: Amino derivatives of isochromans are described. These compounds exhibit antipsychotic and hypotensive activity.

Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 represents a lower alkyl group selected from methyl groups and ethyl groups;R.sup.2 represents a hydrogen atom or a methyl group; andR.sup.3 represents a group selected from C.sub.1 -C.sub.5 alkoxy groups,and pharmaceutically acceptable acid addition salts thereof have valuable antibiotic activity and are suitable for oral administration. They may be prepared by a variety of synthetic routes.

Abstract: Novel 4-hydroxy-3-quinoline-carboxamides of the formula ##STR1## wherein X is in the 5,6,7 or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --OCF.sub.3 and --SCF.sub.3, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of thiazolyl, 4,5-dihydro-thiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidinyl and tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.4 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.

Abstract: A process for preparing and controlling the M.sub.n in the range of 70 to 700 of a reaction product comprising at least 90 mole % linear alpha olefins which includes polymerizing an ethylene containing gas in the presence of the reaction product of a Zirconium metal compound with R.sub.2 AlX, wherein R is an alkyl group having about 1 to about 20 carbon atoms, preferably 1 to 5, most preferably ethyl, and X is Cl or Br, in the presence of a diluent at a temperature of about 75.degree. to 200.degree. C. and an ethylene pressure above about 50 psia, wherein the mole ratio of ethylene to olefin reaction product is above 0.8 throughout the reaction, wherein the product olefin concentration is greater than 5 wt. % based on the diluent and reaction product, wherein the M.sub.n of said reaction product is controlled by the molar ratio of said R.sub.2 AlX/ZrCl.sub.4, said molar ratio being between 100:1 to 0.1:1.

Abstract: A process is described for the catalytic gas phase reduction of 4-oxoalkanenitriles to form 2-alkylpyrroles in high yields and conversions.

Abstract: Substituted tetrahydrotetrazolo[5,1-a]phthalazine compounds such as 6-methylamino-7,8,9,10-tetrahydrotetrazolo[5,1-a]phthalazine are prepared by reacting a 6-halo-7,8,9,10-tetrahydrotetrazolo[5,1-a]phthalazine with an appropriate amine. The compounds are useful as bronchodilators.

Abstract: This invention relates to compounds having the formula ##STR1## wherein R.sub.1 represents hydrogen, halogen or alkoxy, R.sub.2 and R.sub.3 are hydrogen, alkanoyl or alkyl each being the same or different, R.sub.4 represents alkanoyloxyalkyl, hydroxyalkyl, hydrogen, alkyl, alkoxyalkyl, alkenyl, alkynyl, adamantanecarbonyloxyalkyl, bromoalkyl or benzoyloxyalkyl.

Abstract: 2,4-Diaminoquinazoline compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R is a pyrimidinyl, pyrazinyl, pyridazinyl or triazinyl group linked to the piperazine ring by one of its carbon atoms, and optionally substituted by hydroxy, halogen, alkyl, aralkyl, alkoxy, aralkoxy, alkylthio, aryl, aryloxy and certain amino groups; their use as an antihypertensive agent and pharmaceutical compositions containing them.

Abstract: Novel syn isomers of 7-amino-thiazolyl-acetamido-3-acetoxymethyl-cephalosporanic acid derivatives of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of --CN, --CONH.sub.2 and --COOR.sub.1 ', R.sub.1 ' is selected from the group consisting of alkyl of 1 to 3 carbon atoms, hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, R' and R" are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms with the ##STR2## in the syn position with the proviso that when R.sub.1 is --COOR.sub.1 ' and R.sub.1 ' is hydrogen, A is hydrogen and when R.sub.1 is --COOR.sub.1 ' and R.sub.

Abstract: 2,4-Diaminoquinazoline compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R is a pyrimidinyl, pyrazinyl, pyridazinyl or triazinyl group linked to the piperazine ring by one of its carbon atoms, and optionally substituted by hydroxy, halogen, alkyl, aralkyl, alkoxy, aralkoxy,alkylthio, aryl, aryloxy and certain amino groups; their use as an antihypertensive agent and pharmaceutical compositions containing them.