Abstract: The present invention provides compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

Abstract: The present invention provides compounds of formula (I) 1

Abstract: The invention provides new macrolides antibiotics of formula I with improved biological properties and improved stability of the formula wherein R1 is hydrogen, cyano, —S(L)mR2, —S(O)(L)mR2, or —S(O)2(L)mR2; L represents —(CH2)n— or —(CH2)nZ(CH2)n′—; m is 0 or 1; n is 1, 2, 3, or 4; n′ is 0, 1, 2, 3, or 4; Z is O, S or NH; R2 is hydrogen, alkyl, heterocyclyl or aryl; which heterocyclyl and the aryl groups may be further substituted; * indicates a chiral center which is in the (R) or (S) form, as well as a pharmaceutically acceptable acid addition salts or in vivo cleavable esters thereof.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

Abstract: The invention provides new macrolides antibiotics of formula (I) with improved biological properties and improved stability formula (I): wherein R1 is hydrogen, cyano, —S(L)mR2, —S(O)(L)mR2, or —S(O)2(L)mR2; L represents —(CH2)n— or —(CH2)nZ(CH2)n′—-; m is 0 or 1; n is 1, 2, 3, or 4; n′ is 0, 1, 2, 3, or 4; Z is O, S or NH; R2 is hydrogen, alkyl, heterocyclyl or aryl; which heterocyclyl and the aryl groups may be further substituted; * indicates a chiral center which is in the (R) or (S) form and pharmaceutically acceptable acid addition salts or in vivo cleavable esters thereof.

Abstract: The present invention provides compounds of formula (I) 1

Abstract: The invention is concerned with compounds of formula ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is hydroxy or lower-alkoxy, R.sup.3 is hydrogen, cyano, alkyl, alkenyl, cycloalkyl, aryl, heterocycyl, aryl-Q-alkyl, or a group of the formula --CR.sup.4 R.sup.4 'COR.sup.5 --, Q is --SO-- or --SO.sub.2 --; R.sup.4, R.sup.4 ' are each independently hydrogen, alkyl, aryl or heterocyclyl, R.sup.5 is hydrogen, alkyl, alkoxy, hydroxy, aryl or heterocycyl, or R.sup.4 and R.sup.5 together form --(CH.sub.2).sub.n --, and n is a whole number between 2 to 5 inclusive and the enantiomers, epimers, and diastereomers thereof, as well as pharmaceutically acceptable salts thereof. These compounds have valuable antibacterial activity.

Abstract: This invention relates to novel imidazole derivatives of formula a ##STR1## and pharmaceutically acceptable salts of these compounds, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.7 and R.sup.8 are as disclosed herein. These compounds are protein kinase inhibitors useful in the treatment of atherosclerosis, psoriasis, alopecia, and tumors.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is bromine, lower-alkoxy or hydroxy, R.sup.3 is hydrogen, lower-alkyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclyl-lower-alkyl or cyano, R.sup.4 and R.sup.5 each independently are hydrogen, lower-alkyl, lower-alkoxy, halogen, hydroxy, amino, di(lower alkyl)amino, cyano or nitro and Q is ethynylene or vinylene, or pharmaceutically usable salts thereof, the use of these compounds and their salts as therapeutically active substances; medicaments based on these substances and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula I and their pharmaceutically acceptable salts and intermediates for their manufacture.

Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.

Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.

Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as herein described, and salts thereof, are described. The compounds of formula III have antibacterial activity, and are therefore useful as antibacterial agents.

Abstract: The novel retinoids of the formula ##STR1## wherein R represents a residue of a sugar attached ester-wise or a residue of an amino-sugar attached amide-wise or of derivatives of such sugars and n is 1 or 2,can be used as medicaments, e.g. for the treatment of neoplasms, acne and psoriasis. These compounds are obtained by reacting a sugar or an aminosugar or a derivative thereof with a reactive derivative of 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoic acid, optionally followed by the modification of reactive groups present in the reaction product.

Abstract: The invention relates to novel sugar esters and glycosides especially derivatives of D-glucopyranoside and D-glucopyranaronate suitable for the treatment of neoplasms, acne, psoriasis and dermatoses.

Abstract: Thiobenzamides of the formula ##STR1## wherein X' is bromine, fluorine, iodine, trifluoromethyl or C.sub.3-4 alkyl prepared from N-(2-aminoethyl)-morpholine and a compound of the formula ##STR2## wherein X' is as hereinbefore set forth and;Y is methoxy or ethoxy are described. The end products, including p-chloro-N-(2-morpholinoethyl)-thiobenzamide, are useful in the treatment of depressive conditions, that is, are useful as antidepressants.

Abstract: Benzamides of the formula ##STR1## wherein X is halogen, trifluoromethyl or C.sub.3-4 -alkyl and Y is hydrogen, halogen or nitro,and N-oxides thereof, prepared inter alia from N-(2-aminoethyl)-morpholine and an acid of the formula ##STR2## wherein X and Y are as hereinbefore set forth, are described. The end products are useful in the treatment of depressive conditions, that is, are useful as antidepressants.

Abstract: The present invention relates to a process for the manufacture of esters. More particularly, the invention is concerned with a process for the manufacture of esters of 2,2'-anhydro-1.beta.-D-arabinofuranosyl-5-fluorocytosine.

Abstract: Ribofuranoysl-imidazole derivatives of the formula ##STR1## wherein R, X, Y and Z have one of the meanings set forth hereinafter, are described. The ribofuranosyl-imidazole derivatives have cardiac and circulatory-dynamic properties and are useful in the treatment of angina pectoris.

Abstract: A novel class of glucose derivatives, i.e., 3,4,6-tri-o-acyl-2-deoxy-2-nicotinamido-1-0-nicotinoyl-D-glucopyranoses are disclosed. These compounds are pharmaceutically active and are useful as plasma lypid lowering agents.

Abstract: N-nicotinoylglucosamine as a lipid level lowering agent in plasma.