Abstract: Novel amino acid derivatives of the formula ##STR1## wherein R.sup.1 is a protecting group removable under reducing or acid conditions, and R.sup.2 and R.sup.5 are hydrogen or carboxylic protecting groups, are useful as intermediates in preparing stereospecific carbapenam/carbapenem derivatives. R.sup.1 is removed under reducing conditions to form a pyrrolidine derivative, which is further cyclized from the R.sup.5 =H compound to form a .beta.-lactam ring. Stereospecificity at the 6-position is achieved by treatment with lithium diisopropylamide (LDA) and quenching at different temperatures. Compound (I) can be prepared by treating R.sup.1 -protected R.sup.3 -pyrrolidone carboxylic acid R.sup.2 -ester with a lithium enolate of the formula R.sup.4 CHLiCO.sub.2 R.sup.5. The lithium enolate can be formed from R.sup.4 CH.sub.2 CO.sub.2 R.sup.5 by treatment with LDA.

Abstract: 6-Fluoro-3,5-dihydroxy carboxylic acid derivatives of the formula I and the corresponding lactones of the formula II ##STR1## in which R.sup.1 and R.sup.2 have the specified meanings, a process for the preparation of these compounds, the use thereof as medicinal agents and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formula I or formula II are described.

Abstract: The present invention provides a process for preparing a cephem derivative characterized in that an allenyl .beta.-lactam compound represented by the formula (1) ##STR1## wherein R.sup.1 is amino or protected amino, R.sup.2 is a hydrogen atom or lower alkoxyl, R.sup.3 is a hydrogen atom or carboxylic acid protecting group and X is the group --SO.sub.2 R.sup.4 or --SR.sup.4, R.sup.4 being substituted or unsubstituted aryl or substituted or unsubstituted nitrogen-containing aromatic heterocyclic group is reacted with a nucleophilic agent to obtain the derivative, the cephem derivative being represented by the formula (2) ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, and Y is the residue of the nucleophilic agent.

Abstract: Treatment of an animal with calcium flux inhibitors results in a decrease in the number of epidermal Langerhans cells and a simultaneous decrease in the ability to respond to contact sensitizing agents. Also, topical application of calcium flux inhibitors will reduce inflammation in patients experiencing delayed-type hypersensitivity reaction or atopic eczema. Thus, calcium flux inhibitors represent a new class of therapeutic agents in the treatment of contact dermatitis and eczema.

Abstract: The present invention relates to new cephalosporin compounds of the formula(I), pharmaceutically acceptable non-toxic salts thereof, and physiologically hydrolyzable esters and solvates thereof, which have potent and broad antibacterial activities ##STR1## wherein R.sup.1 is a C.sub.1.about.4 alkyl, C.sub.3.about.4 alkenyl, C.sub.3.about.4 alkynyl group, or --C(R.sup.a)(R.sup.b)CO.sub.2 H.sub.1 wherein R.sup.a and R.sup.b are the same or different, and each is a hydrogen atom or a C.sub.1.about.4 alkyl group, or R.sup.a and R.sup.b form a C.sub.3.about.7 cycloalkyl group with the carbon atom to which they are linked;R.sup.2 is a C.sub.1.about.4 alkyl, C.sub.3.about.4 alkenyl or C.sub.3.about.4 cycloalkyl group, a substituted or unsubstituted amino group, or a substituted or unsubstituted phenyl group;R.sup.3 is hydrogen or a C.sub.1.about.4 alkyl group; andQ is N or CH.The invention further relates to a process for preparing said compounds, and to pharamaceutical compositions containing said compounds.

Abstract: A compound having the formula ##STR1## wherein R.sup.1 is hydrogen, NH.sub.2 or C.sub.1-6 -alkyl which may be branched;X is O, S, NCN;Y is O, S;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently of each other are hydrogen, halogen, CF.sub.3, NO.sub.2, NH.sub.2, OH, C.sub.1-6 -alkoxy, C(.dbd.O)-phenyl or SO.sub.2 NR.sup.I R.sup.II wherein R.sup.I and R.sup.II independently are hydrogen or C.sub.1-6 -alkyl;R.sup.11 is hydrogen, halogen, NO.sub.2 or SO.sub.2 NR'R" wherein R' and R" independently are hydrogen or C.sub.1-6 -alkyl;R.sup.13 is hydrogen, halogen, phenyl, CF.sub.3, NO.sub.2 ;R.sup.12 is hydrogen or together with R.sup.13 forms a C.sub.4-7 -carbocyclic ring which may be aromatic or partially saturated;R.sup.14 is hydrogen or together with R.sup.13 forms a C.sub.

Abstract: A compound of the formula (II): ##STR1## and pharmaceutically acceptable salts an in vivo hydrolysable esters are described as is their preparation and use as antibacterial agents.

Abstract: Compound I ##STR1## is obtained by reaction of compound II with compound III

Abstract: New derivatives of 1,2-dihydro 2-oxo quinoxalines corresponding to the general formula I: ##STR1## in which: R is a hydrogen or halogen atomR.sub.1 is a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 alkyl radicalR.sub.2 is:a hydrogen atoma C(O)R.sub.4 radical in which R.sub.4 is a straight or branched C.sub.1 -C.sub.4 alkyl groupa C(O)NHR.sub.5 radical in which R.sub.5 is a straight or branched C.sub.1 -C.sub.4 alkyl radical or a phenyl groupA is a C.sub.1 -C.sub.4 alkaline chainR.sub.3 represents:a hydrogen atom, a C.sub.1 -C.sub.4 alkyl radical, a C.sub.3 -C.sub.6 cycloalkyl radical, an alcynyl, nitrile, hydroxyl, carboxamido, pyridyl, phenyl group, or a phenyl group substituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group or a nitro groupan alkenyl radical of the formula: ##STR2## in which R.sub.6, R.sub.7 may, independently of each other, be a hydrogen atom, a C.sub.1 -C.sub.

Abstract: The present invention provides a process for preparing a 2-exo-methylenepenam derivative represented by the formula (2), the process being characterized by reacting an allenyl .beta.-lactum compound represented by the formula (1) with a metallic reducing agent, in which R.sup.1, R.sup.2, R.sup.3 and X are defined in the specification.

Abstract: 3-Piperidinyl-indazole derivatives and their pharmaceutically acceptable acid addition salts being useful antagonists of neurotransmitters; pharmaceutical compositions containing the same and a method of treating warm-blooded animals suffering from diseases associated with the release of said neutrotransmitters.

Abstract: The present invention provides compounds of the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl;A and A' are independently hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, amino, a 5-6 membered organic heterocycle containing 1, 2, or 3 hetero atoms selected from nitrogen or sulfur, C.sub.1 -C.sub.6 alkoxy, or phenyl; or A and A' taken together form a group of the formulae ##STR2## wherein X is hydrogen, halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, amino, nitro, or carboxy; and Y is nitrogen or carbon; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions and methods or treatment using the above compounds.

Abstract: This invention relates to novel antibiotic cephalosporin derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or a radical of the formula ##STR2## in which R.sup.3 and R.sup.4 are independently hydrogen, methyl or ethyl, or R.sup.3 and R.sup.4, taken together with the carbon atom to which they are attached, may be a cycloalkylidene ring containing from 3 to 6 carbon atoms;R.sup.2 is a radical selected from the group consisting of ##STR3## wherein R.sup.5 is hydrogen or C.sub.1-6 alkyl. This invention further relates to compounds of formula I and their pharmaceutically acceptable salts, physiologically hydrolyzable esters or solvates.

Abstract: Disclosed herein are processes for preparing a compound of the formula ##STR1## in which a novel compound of the formula ##STR2## is reacted with a beta lactam of the formula ##STR3## by treatment with a base, wherein the symbols are as defined in the specification.

Abstract: The invention relates to cephem compounds characterized by a substituted 2-pyrazolimethyl group and a 7-(aminothiazolyl) (hydroxyimino)-acetamido group and certain derivatives thereof, to pharmaceutical compositions comprising the same and to use for treatment of infectious diseases.

Abstract: Metal complexes of azines of the formula ##STR1## in which X denotes hydrogen or halogen,R denotes hydrogen or an organic radical,R.sub.1 denotes hydrogen or an organic radical,R.sub.2 denotes an organic radical, in which R.sub.1 and R.sub.2 together with the C atom linking them can also form a carbocyclic or heterocyclic ring or a carbocyclic or heterocyclic ring system in which the rings and ring systems mentioned can also be substituted, and one of the radicals R.sub.1, R.sub.2 or R.sub.1 and R.sub.2 together contain a group capable of forming a metal salt, and processes for pigmenting using these metal complexes.

Abstract: An efficient, multistep process for the synthesis of certain 6-(1-hydroxyethyl) 2-substituted penem antibiotics from 2-[4R-(triphenylmethylthio)-3S-(1R-(dimethyl-t-butylsilyloxy)ethyl)-2-azet idon-1-yl]acetic acid esters.

Abstract: 2-(Pyrimidyl or pyrazinyl)-imino-1,3-dithietanes ##STR1## wherein Ar is one of the radicals ##STR2## R is unsubstituted C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkyl which is substituted by halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio or cyano, independently of one another, or is unsubstituted or halo-substituted C.sub.3 -C.sub.7 alkenyl, unsubstituted or halo-substituted C.sub.3 -C.sub.7 alkynyl, or C.sub.3 -C.sub.5 cycloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylamino, nitro or halogen,n is a number from 0 to 3,X.sub.1 and X.sub.2 independently of each other are hydrogen or halogen, including the addition salts formed with acids of the formula H.sup..sym. X.sup..crclbar. in which the anion X.sup..crclbar. is Cl.sup..crclbar., Br.sup..crclbar., I.sup..crclbar., HSO.sub.4 -, H.sub.2 PO.sub.4 -, H.sub.2 PO.sub.3 -, NO.sub.3 -, CH.sub.3 COO.sup..crclbar., CH.sub.2 ClCOO-, CF.sub.3 COO-, HOCH.sub.2 COO-, CH.sub.3 CH(OH)COO.sup..crclbar., HOOCCOO.sup..crclbar.

Abstract: There are presented antibacterial cephalosporins having broad antimicrobial activity as well as intermediates for their formation, such compounds having the formula ##STR1## wherein X is ##STR2## R is hydrogen or a carboxylic acid protecting group; R.sub.1 is hydrogen or an acyl group;R.sub.2 is hydrogen or lower alkoxy; andR.sub.3 is carbocyclic aryl or alkyl carbocyclic aryl substituted on the ring with two or more of hydroxy and/or lower alkanoyl ester groups, with halogen being an optional additional ring substituent;as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds where R is hydrogen.

Abstract: A phthalocyanine compound of the Formula (1): ##STR1## wherein: Pc is a phthalocyanine nucleus which is metal free or contains a metal or oxymetal;X is S; NT or O;Y is S; NT or O;Z is S or Se; in which T in the above is H; alkyl or aryl;.sup.+ HA is an aliphatic polyamino ammonium ion or a substituted diguanidinium ion;each R independently is an aromatic radical linked to a peripheral carbon atom of the Pc nucleus through an atom Z;each R.sup.1 independently is optionally substituted phenylene or naphthylene in which the atoms X and Y are attached to adjacent nuclear carbon atoms in R.sup.1 and to adjacent peripheral carbon atoms of the Pc nucleus;a is 0 to 16; provided thatb is 0 to 8; a+b>0; andc+d is 1 to 16.