Abstract: A process for etherifying the hydroxymethyl group in position 3 of a cephalosporin by reaction of a 3-hydroxymethyl cephalosporin with an dioxycarbenium-tetrafluoroborate.

Abstract: A process for alkylating the 2'-OH of N.sup.6 -modified adenosine comprising the reacting of an unprotected N.sup.6 -alkyl adenosine with dimethyl sulfate and tetrabutylammonium hydrogen sulfate in a non-polar solvent, preferably dichloromethane, and 5% sodium hydroxide. The products of the reaction are useful as anti-diabetic, hypolipidemic, and analgesic agents.

Abstract: A cephalosporin intermediate of the formula ##STR1## where R.sub.3 is carboxyl, carboxylate, or a carboxylic acid ester group and,R.sub.8 and R.sub.9 are each independently hydrogen, halogen,(C.sub.1-4) alkyl, hydroxy, carboxamido,(C.sub.1-4) alkoxycarbonyl, amino,mono- (C.sub.1-4) alkylamino, di- (C.sub.1-4) alkylamino, ortogether are a 5 or 6-membered carbocyclic ring or an alkali metal, alkaline earth metal, or acid addition salt thereof. Valuable cephalosporin antibiotics can be produced from the cephalosporin intermediate products of formula I.

Abstract: The invention provides an improved process for the production of 7-amino-3-alkoxymethlycephem-4-carboxyl acid derivatives.

Abstract: Complexes and pharmaceutical preparations containing complexes of the pleuromutilin derivative of formula I ##STR1## in free base or in acid addition or quaternary salt form and cyclodextrin are described.They can be prepared by complexing the above pleuromutilin compound with an appropriate cyclodextrin.They are indicated for use as pharmaceuticals, e.g. as antibiotics, especially in veterinary medicine, e.g. as feed additives.

Abstract: The invention relates to a new process for the production of the disodium salt hemiheptahydrate of ceftriaxone by reacting 7-amino-3-{[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)thio] methyl}-3-cephem-4-carboxylic acid with 2-(2-aminothiazol-4-yl)-2-syn-methoximinoacetic acid-(2-benzthiazolyl)thiolester in the presence of a base, characterized in that the reaction and the crystallization of the disodium salt hemiheptahydrate of ceftriaxone are carried out in aqueous acetone.

Abstract: Pseudopeptides of formula I in free or salt form ##STR1## wherein A, B, R.sub.1, X, Y and m are defined as in claim 1, and their use in the prophylactic and acute treatment of thrombosis.

Abstract: A compound of formula (I), in which each of R.sub.1 and R.sub.2 is independently hydrogen, alkyi or, together with the carbon atom to which it is bonded, a cycloalkyl; and each of R.sub.3 and R.sub.4 is independently hydrogen, alkyl or substituted alkyl. The compounds are useful intermediates and prodrugs.

Abstract: Peptide derivatives selected from (i) a calcitonin peptide and a LHRH antagonist peptide modified by at least one sugar residue and/or at least one short polyhydroxy compound or derivative, and (ii) a calcitonin peptide modified by at least one formyl and/or at least C.sub.3-5 alkyl attached to an amino group other than a N-terminal amino group, and (iii) a calcitonin peptide modified by a combination of said substituents, with the provisos thati) when the calcitonin peptide comprises at least one sugar residue a), this sugar residue is attached by a coupling other than a direct N-glycosidic bond to an .omega.-amino group of an .omega.-amino substituted side chain in the 24 position, andii) when the LHRH antagonist comprises at least one sugar residue a), this sugar residue is an Amadori sugar residue attached by a coupling other than a direct N-glycosidic bond to an .omega.-amino group of an .omega.

Abstract: The invention relates to compounds of formula I ##STR1## wherein the substituents have various significances. They can be prepared by conventional methods, e.g. coupling, substitution, deprotection or protection reactions.They possess interesting pharmacological properties and are thus indicated for use in the treatment of retroviral infections, particularly as HIV proteinase inhibitors.

Abstract: Adenosines derivatives of the formula ##STR1## wherein R.sub.1 is allyl, methallyl, straight or branched chain (C.sub.3-7)alkynyl, (C.sub.3-8)cycloalkyl, or phenyl mono- or independently of one another di-substituted by halogen having an atomic number of from 9 to 35, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, or CF.sub.3 ; R.sub.2 is hydrogen or C(.sub.1-4)alkyl, and R.sub.3 is (C.sub.1-4)alkyl, are useful for protecting vascular endothelium, for lowering blood lipid levels, and for treating raised blood pressure.

Abstract: Cyclosporins wherein the residue at the 1-position (typically -MeBmt- or -dihydro-MeBmt-) is 3'O-acylated or 3'-oxo or -C.sub.1-4 alkoxyimino substituted, or wherein the residue at the 2-position is .beta.-O-acyl or .beta.-oxo substituted, or wherein the residue at the 2-position is -Ile-, or wherein the residue at the 11-position is -MeAls-, -MeIle- or -MealloIle- as well as various naturally occurring cyclosporins/dihydro-derivatives thereof, are useful in reversing resistance to chemotherapy, in particular resistance to cytostatic or anti-neoplastic therapy. Various of these cyclosporins and intermediates for their production are novel. Intermediates wherein the residue (e.g. -MeBmt-, -dihydro-MeBmt- etc.) at the 1-position is 8'-alkoxy or 7'-desmethyl-7'-hydrocarbyl substituted are novel and useful as immunosuppressants, anti-inflammatory and anti-parasitic agents.

Abstract: Compounds of the formula ##STR1## where X.sub.1 and X.sub.2 are independently O or S, andR.sub.1 is as defined in the descriptionR.sub.2, R.sub.3, and R.sub.4 are each independently straight orbranched chain (C.sub.1-4)alkyl, and pharmaceutically acceptable salts, physiological hydrolysable esters, and pro-drug forms thereof are useful as hypoglycemic agents.

Abstract: The invention concerns the compounds of formulae ##STR1## wherein the substituents have various significances. They can be prepared by various methods, e.g. acylation, reduction, alkylation, etc. They are indicated for use as pharmaceuticals, in particular as immunosuppressant, antiproliferative and antiinflammatory agents.

Abstract: The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances, in free form and, where such forms exist, in salt form.They can be prepared by various processes, e.g. by irradiation; oxidation; elimination; reduction; conversion by e.g. halogenation or acylation; deprotection of protected hydroxy groups; protection of free hydroxy groups; and separation of stereoisomeric mixtures into individual isomers.They are useful as pharmaceuticals, especially as antiinflammatory, and as antiproliferative and antiinflammatory agents.

Abstract: Compound of formula IVe ##STR1## where Het is 2-pyridyl or 2-benzothiazolyl, are useful as acylating agents in preparing 7-[2-(2-amino-4-thiazol)-2-oxoacetyl]-cephalosporin intermediates.

Abstract: A process for preparing compounds of the formula ##STR1## where X.sub.1 and X.sub.2 are independently O or S, andR.sub.1 is as defined herein,R.sub.2, R.sub.3, and R.sub.4 are each independently straight or branched chain (C.sub.1-4)alkyl,and pharmaceutically acceptable salts, physiological hydrolyzable esters, and pro-drug forms thereof, which are useful as hypoglycemic agents.

Abstract: Somatostatin analogues and derivatives in free form or in pharmaceutically acceptable salt or complex form are useful for preventing or reducing neointimal proleferation following angioplasty.

Abstract: The invention relates to a new, economical and simple process for the production of 3-vinylcephalosporin compounds of formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and denote hydrogen or an organic radical.

Abstract: Compound of the formula ##STR1## where R is CH.sub.3 (CH.sub.2).sub.m, A and B are hydrogen, a bond or --(CH.sub.2).sub.n,X is ##STR2## m is 0, 1 , 2 or 3, n is 1 , 2, or 3, R.sub.1 is hydrogen or lower alkyl, andY is --OH, --OR.sub.2 or --NR.sub.3 R.sub.4where R.sub.2, R.sub.3 and R.sub.4 are hydrogen or unsubstituted or substituted alkyl, aryl and aralkyl substituents.