The Hetero Ring Contains Two Chalcogens Which Are Bonded Directly At The 16 And 17-positions Of The Cyclopentanohydrophenanthrene Ring System Patents (Class 540/27)
Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
Type:
Grant
Filed:
August 17, 1999
Date of Patent:
August 8, 2000
Assignee:
Novo Nordisk A/S
Inventors:
Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
Abstract: Anthraquinone chiral ligands (AQN) are used in asymmetric aminohydroxylation addition reactions of cinnamate based olefins for synthesizing aryl serines. The anthraquinones impart a reverse regioselectivity as compared to the commonly employed phalazine chiral ligands (PHAL). Carbamates are employed as the oxidant nitrogen source. The yields and enantiomeric efficiencies are Excellent. .beta.-Hydroxyamines are obtained by deprotecting the corresponding .beta.-hydroxycarbamate.
Type:
Grant
Filed:
March 26, 1998
Date of Patent:
May 2, 2000
Assignee:
The Scripps Research Institute
Inventors:
K. Barry Sharpless, Beata Tao, Gunther Schlingloff
Abstract: The invention relates to antiinflammatory compounds of the formula (I), ##STR1## wherein A stands for hydrogen or hydroxyl group;X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;R stands for hydrogen, benzoyl or C.sub.1-8 alkanoyl group;R.sup.1 and R.sup.2, which are the same or different, stand for hydrogen or a C.sub.1-4 alkyl group; or one of R.sup.1 and R.sup.2 is hydrogen and the other is phenyl group; or R.sup.1 and R.sup.2 together form a C.sub.4-5 alkylene group;means a single or double bond between two adjacent carbon atoms,as well as pharmaceutical compositions containing these compounds and a process for their preparation.
Abstract: The invention involves a two step chemical transformation of a steroidal 17-cyanohydrin (II) ##STR1## to a 17.alpha.-hydroxy-21-halo-20-keto steroid (IV) ##STR2## intermediate which can readily be converted to pharmaceutically useful corticoids.