Hoffmann-La Roche Inc.

Gerard Schmid

Jean Ackermann

Kurt Hilpert

David Banner

Hans Peter Wessel

Klaus Gubernator

Thomas B Tschopp

Paul Hadvary

Beat Wirz

Klaus Muller

Ludvik Labler

Christian N Hubschwerlen

Hans P Marki

Marianne Rouge

Niggi Iberg

Michael Pech

Rita Muller

Jurgen Fingerle

Alexander Chucholowski

Johannes Aebi

Henrietta Dehmlow

Olivier Morand

Werner Hofheinz

Hans Lengsfeld

Jacques Himber

Harro Stohler

Synese Jolidon

Hans-Peter Marki

Yu-Hua Ji

Ku-Hua Ji

Tertiary amines of the formula ##STR1## wherein A.sup.1, A.sup.2, A.sup.3, A.sup.4, L, M, p, T, and Q are as defined herein, have antimycotic and cholesterol-lowering activity.

Tertiary amines

Aminoalkyl-substituted benzo-heterocyclic compounds of the formula ##STR1## wherein M, Q, R and T are as defined in the specification, as well as acid addition salts thereof. These compounds are useful as cholesterol level lowering agents and as antimycotic agents.

Aminoalkyl-substituted benzo-heterocyclic compounds

Compounds of the formula ##STR1## wherein n.sup.1 -n.sup.9 are each independently 0 or 1;

Sulfuric acid esters of sugar alcohols

Compounds of formulas ##STR1## wherein, B is lower alkylene or an optionally substituted aromatic ring system;

Sulfuric acid esters of amino sugars

Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.

Guanidine derivatives

Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.

Sulfonamidocarboxamides

The present invention is concerned with novel sulfuric acid esters of sugar alcohols and sugar alcohol-like compounds of the formula ##STR1## Also described are methods for the treatment and/or prophylaxis of arteriosclerotic changes in the vascular wall as well as a process for the manufacture of the compounds of formula I and their salts.

Guanidine derivatives compositions and use

Novel 4-substituted-4,8-dimethyl-2,3-dioxabicyclo[3.3.1] nonan-7-ones which have a pronounced activity against the causative organism of malaria and can be used for the prevention and control of malaria.

Bicyclic peroxides

Bicyclic peroxides compositions for and treatment of malaria therewith

The novel compounds of the formula ##STR1## wherein R.sup.11 signifies hydrogen, acyl or tri(lower alkyl)silyl, R.sup.2 signifies a phenyl group which is substituted in the o- and/or the p-position by halogen, lower alkyl, lower alkylthio or lower alkoxy and n signifies the number 0 or 2, and mixtures thereof with the corresponding optical antipodes are valuable intermediates for the manufacture of antimicrobially active penems and carbapenems which have as a common structural element a (R)-1-hydroxyethyl group in the 6-position. They can be manufactured by reacting a compound of the formula ##STR2## wherein R.sup.12 signifies acyl, tri(lower alkyl)silyl or a group of the formula --BR.sup.3 R.sup.4 and R.sup.3 and R.sup.4 have the same significance and each signify a branched-open chain, cyclic or bicyclic hydrocarbon residue with 5-10 carbon atoms or together signify an open chain or cyclic hydrocarbon residue with 5-10 carbon atoms and two free valencies and R.sup.2 has the above significance, or a mixture thereof with the corresponding optical antipode with chlorosulphonyl isocyanate and, if desired, S-oxidizing a resulting compound of formula I in which n signifies the number O and, previously or subsequently, cleaving off an acyl or tri(lower alkyl)silyl group which may be present.

4-(phenylthio or phenylsulfonyl) azetidinones and process of manufacture

Growing community of inventors

Kienberg, Switzerland

Gerard Schmid