PURPOSE: To obtain an intermediate for producing novel steroids having a 10-substituent and antiglucocorticoid activity and used for therapy or the like of the hypertension, glaucoma, atherosclerosis, osteoporosis, diabetes, immune depression, inflammatory diseases or the like. CONSTITUTION: This intermediate is an intermediate for producing a novel 10-substituted steroid expressed by formula I [when X is methylene, R is a (substituted) carbocyclic or a heterocyclic aryl, a (substituted) vinyl or ethynyl, or when X is S or a single bond, R is a (substituted) carbocyclic or heterocyclic aryl; R 2 is methyl or ethyl; K is a protecting group for ketone functional groups; K 2 is a (protected) ketone functional group or a group expressed by formula II (R 3 is a ≤3C alkyl, an alkenyl or an alkynyl)], having extraordinary antiglucocorticoid activity and used for curing or the like of inflammatory diseases. The compound is obtained by a method of reacting a compound of formula III (R 4 ' is H or an OH-protecting group) with a lithium compound, or the like of the formula R-X-Li or the like. COPYRIGHT: (C)1995,JPO

The synthesis of 2-isocephems bearing multiple bonds between the thiazoline ring and the 3-substituent is reported. When a leaving group was present, the E-vinylogous derivatives were shown to be more active than the parent compounds, essentially against staphylococci. Insertion of an aryl group in this position, however, sharply reduces the activity against Gram-negative bacteria.

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The aim of this paper is to describe the different structure-affinity and structure-activity relationships which led to the discovery of RU 43044, a pure antiglucocorticoid, and of the dissociated antiprogestins RU 46556 and RU 49295. Furthermore, a complete biochemical and pharmacological profile of these 3 compounds compared to that of RN 38486 will be presented

La reaction en milieu basique d'une N-carboxymethyl azetidinone convenablement fonctionnalisee, avec le sulfure de carbone ou l'oxysulfure de carbone, conduit a des isocephemes heterosubstitues en position 3

La reaction en milieu basique d'une N-carboxymethyl azetidinone convenablement fonctionnalisee, avec le sulfure de carbone ou l'oxysulfure de carbone, conduit a des isocephemes heterosubstitues en position 3

AbstractDerivatives of the title compounds (V) with nitrated phenyl ring are obtained from the reaction of the intermediate (II) with HNO3/AcOH followed by the reaction sequence (II)‐(V).

The synthesis of N-(1H-tetrazol-5-yl) azetidin-2-one and the racemic 4-methyl and 4-trifluoromethyl analogues starting with 5-amino tetrazole via two Independent pathways is described. The compounds were devoid of any useful antibacterial activity.

AbstractThe syntheses of the title compounds (XIV), (X) and (VII), resp., are described, all starting from the 5‐aminotetrazole (I).