Abstract: 1-Carba(1-dethia)cephem antibacterial agents possessing a 3-(substituted or unsubstituted)thiazolo group are provided. Further provided is a method for treating bacterial infections in man and other animals and a pharmaceutical formulation utilizing said 1-carba(1-dethia)cephems.

Abstract: A method of combating pests which comprises applying to such pests or to a pest habitat a pesticidally effective amouht of a substituted 2-cyclohexen-1-yl-amine derivative of the formula ##STR1## and addition products thereof with acids and metal salts. Most of the compounds are new.

Abstract: Azlactone-functional Michael adducts are disclosed which are the Michael reaction products of 2-alkenyl azlactones and Michael donors selected from carbon and nitrogen nucleophiles. Reaction products which contain a plurality of azlactone groups are useful as step growth monomers in adhesives, sealants, and coatings.

Abstract: This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In another aspect, this invention is concerned with said intermediate. ##STR1## In the compounds of Scheme (A), R.sup.1 is a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.

Abstract: A process for the preparation of at least one compound of a formula selected from the group consisting of ##STR1## and their salts and esters wherein X is selected from the group consisting of hydrogen and a substituent such as halogen and acetoxy comprising diazotizing a compound of the formula ##STR2## and salts and esters thereof wherein X has the above definition and brominating the resulting diazotized compound with at least an equimolar amount of a nitrosating agent in the presence of 1 to 5 equivalents of a strong acid in solution or suspension in a mixture of water and an at least partially water-miscible organic solvent with the amount of water being 1 to 20% by volume containing at least equimolar amounts of hydrogen bromide and bromine which bromo compounds are useful intermediates for the preparation of penicillanic acid-1,1-dioxide and its derivatives and novel 6-diazo-intermediates.

Abstract: Derivatives of 2-spirocyclopropyl cephalosporin sulfone of the structural formula I ##STR1## are provided which are useful as potent elastase inhibitors.

Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --S--Q--(Y).sub.n --Pwherein Q is a 5- or 6-membered heterocyclic ring, P is a benzene ring substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or P is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl; said ring P being further optionally substituted; and --(Y).sub.n -- is a bond or various linking groups or --(Y)--.sub.n may be such so that rings Q and P are fused.The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

Abstract: There is provided a cephalosporin derivative represented by the general formula (1): ##STR1## wherein R.sup.101, R.sup.102, R.sup.103 and Y.sup.101 are as difined; the general formula (2): ##STR2## wherein R.sup.201, R.sup.202 and R.sup.203 are as defined above; the general formula (3): ##STR3## wherein R.sup.301, R.sup.302, Y.sup.301, Y.sup.302 and A.sup.301 are as defined; or pharmaceutically acceptable salt thereof. The compound is useful as an active ingredient of antimicrobial agent.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein the broken line represents a saturated or an olefinic bond, R.sup.1 and R.sup.4 are each hydrogen or C.sub.1 to C.sub.6 alkyl, and R.sup.2 and R.sup.3 are each hydrogen, C.sub.1 to C.sub.6 alkyl, halogen, C.sub.1 to C.sub.6 alkoxy or C.sub.1 to C.sub.6 alkylthio, and pharmaceutically acceptable salts thereof, pharmaceutical compounds containing the same, methods of preparing the foregoing compounds, and to novel intermediates in the preparation of the foregoing compounds. These compounds are useful as agents in the prevention of neuronal damage in the brain following cerebral ischemia and during the progression of Alzheimer's disease and also as anticonvulsants.

Abstract: (4-Piperidinylmethyl and -hetero)purines having antihistaminic properties and being useful agents in the treatment of allergic diseases.

Abstract: Derivatives of 2-spirocyclopropyl 4-acylcephem sulfones of the formula (I) ##STR1## are provided which are useful as potent elastase inhibitors and hence are useful in the prevention, control and treatment of inflammatory conditions, especially arthritis and emphysema.

Abstract: A cephalosporin derivative of the formula I: ##STR1## in which X is S, O, CH.sub.2 or SO, ##STR2## represents one of C-7 acyl groups known in the cephalosporin art, R3 is hydrogen or methoxy, R4 is hydrogen, optionally substituted alkyl or allyl, and R5 is an aromatic heterocyclic ring system which is linked via carbon, and which contains a quaternized nitrogen atom.

Abstract: 5-Substituted pyrrolo[2,3-d]pyrimidines are prepared from a nucleophile of the formula R.sup.2 -C(.dbd.NH)NH.sub.2 and a 2-amino-5-substituted-furan carrying a cyano or carboxy group in the 4-position. A typical example is the preparation of ethyl 4-(2-(2,4-diaminopyrrolo[2,3-d]pyrimidin-5-yl)ethyl}benzoate, an intermediate for the preparation of the known N-[4-{2-(2,4-diaminopyrrolo[2,3-d]pyrimidin-5-yl)ethyl}benzoyl]-L-glutamic acid, by allowing guanidine and ethyl 4-[2-(2-amino-3-cyanofur-4-yl)ethyl]benzoate to react under mild conditions.

Abstract: A preparation containing a cephalosporin medicament is disclosed. The preparation comprises a cephalosporin derivative represented by the following formula: ##STR1## namely, 7.beta.-{2-(5-amino-1,2,4-thiadiazol-3-yl)-(Z)-2-fluoromethoxyiminoacetami do}-3-{(E)-3-(carbamoylmethylethylmethylammonio) -1-propen-1-yl}-3-cephem-4-carboxylate or a pharmaceutically acceptable salt thereof salt, lactose, citric acid or a sodium salt thereof, and arginine or a hydrochloride thereof; or the cephalosporin derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof, lactose, citric acid or a sodium salt thereof, and sodium chloride.

Abstract: There is provided a process for preparing a compound of the formula (I): ##STR1## wherein R.sub.1 is an organic residue, R.sub.2 is a hydrogen or a chlorine atom, a methoxy, ethoxy or an acetoxy group, and n represents 0, 1 or 2.The process comprises reacting a compound of the formula (II): ##STR2## wherein R.sub.2 and n are as defined above, with an inorganic or organic nitrite, in an alcohol R.sub.1 OH, wherein R.sub.1 is as defined above, or in a mixture R.sub.1 OH-organic solvent in the presence of an inorganic or organic acid.The compounds of the formula (I) are known intermediates in the synthesis of human leucocyte elastase inhibitors (HLE).

Abstract: Intermediates of the following formula are disclosed: ##STR1## wherein R.sup.1 is aryl; R.sup.2 is carboxy or protected carboxy; Z.dbd.CH.dbd.CH.sub.2, CH.sub.2 --X.sup.2, --CH.sub.2 --P.sup.+ (R.sup.7).sub.3 .X.sup.3 or CH .dbd.P(R.sup.7).sub.3 wherein X.sup.2 and X.sup.3 are each halogen and R.sup.7 is aryl.The compounds are useful as intermediates for cephalosporins.

Abstract: A compound of formula (I) ##STR1## or a salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, acyl or phosphate, provided that when one of R.sub.1 or R.sub.2 is phosphate, the other is hydrogen; or R.sub.1 and R.sub.2 are joined together to form a cyclic acetal group, a cyclic carbonate group or a cyclic phosphate group.Processes for preparing these compounds and their use in therapy is also described.

Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen or --C(O)R.sup.7 wherein R.sup.7 is hydrogen, alkyl of one to nineteen carbon atoms, hydroxyalkyl of one to eight carbon atoms, alkoxyalkyl of two to nine carbon atoms, alkenyl of two to nineteen carbon atoms, phenyl, 1-adamantyl or 2-carboxyethyl and the pharmaceutically acceptable alkali metal salts thereof;R.sup.2 is --C(O)R.sup.7 wherein R.sup.7 is as defined above;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 wherein R.sup.9 and R.

Abstract: The present invention relates to novel cephalosporin derivatives with improved pharmacokinetics, corresponding to the formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3 represent a hydrogen atom, or R.sub.1 and R.sub.2 represent a hydrogen atom or a methyl group and R.sub.3 represents a carboxyl group, or ##STR2## form a cyclobutyl group and R.sub.3 represents a carboxyl group; and A and B are different and occupy the meta and para positions of the benzene ring, one representing a hydroxyl group and the other being selected from the groups ##STR3## and --NH--SO.sub.2 --Alk--NH.sub.2 in which Alk denotes a C.sub.2 -C.sub.4 lower alkylene group and also to the pharmaceutically acceptable salts and esters of the said derivatives.It further relates to a process for the preparation of such cephalosporins and to pharmaceutical compositions in which they are present.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.5 cycloalkyl or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.2 is H, C.sub.1 -C.sub.6 alkyl optionally substituted by OH, C.sub.1 -C.sub.3 alkoxy or C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 perfluoroalkyl or (C.sub.3 -C.sub.6 cycloalkyl)C.sub.1 -C.sub.6 alkyl; R.sup.4 taken together with the nitrogen atom to which it is attached completes a pyrrolidinyl, piperidino, morpholino, or 4-N-(R.sup.6)-piperazinyl group; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, NR.sup.7 R.sup.8, or CONR.sup.7 R.sup.8 ; R.sup.6 is H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.3 alkoxy) C.sub.2 - C.sub.6 alkyl, hydroxy C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 N)C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 NCO)C.sub.1 -C.sub.6 alkyl, CONR.sup.7 R.sup.8, CSNR.sup.7 R.sup.