Abstract: The present invention is directed to a method of producing nanoparticles by the miniemulsion method, said nanoparticles being made by adding a defined amount of stabilizer to the reaction system. The present invention is further directed to nanoparticles made by this method and their use for the treatment of diseases and conditions, requiring a pharmaceutical agent to cross one or more physiological barriers, in particular the blood-brain barrier.

Abstract: The present invention is directed to a delivery vehicle containing nanoparticles. The present invention is further directed to a pharmaceutical composition, comprising said drug delivery vehicle. Further, the invention pertains to a method for manufacturing of said delivery vehicles as well as to the use of these vehicles in medicine.

Abstract: Diterpenes of the formula I ##STR1## in which R.sup.1 is --CH.sub.2 --C(CH.sub.3).dbd.CH--R.sup.3 or --CH.sub.2 --CH(CH.sub.3)--CH.sub.2 --R.sup.3,R.sup.3 is --CH.sub.2 OH, --CHO, --COOH or --COOR.sup.4,R.sup.4 is alkyl having 1 to 5 C atoms,A is ##STR2## and R.sup.2 is H, pentoses, hexoses, di-/oligosaccharides or amino sugars,are suitable for production of medicaments having immunomodulatory action, in particular stimulating T-cells.

Abstract: The invention relates to a process for the enantiomer-selective preparation of .gamma.-keto-.delta.-amino acid derivatives of the formula I ##STR1## characterized in that a compound of the formula II ##STR2## is converted, using a trialkylchlorosilane, into a compound of the formula III ##STR3## this compound is then reacted with a diazoacetate of the formula N.sub.2 CH.sub.2 COOR.sup.4 (R.sup.4 .noteq.H) to give a cyclopropane compound of the formula IV ##STR4## and then the compound IV is converted, by ring-opening and removal of the silyl groups, and where appropriate saponification, into the compound of the formula I, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 having the meanings indicated in claim 1.

Abstract: In a process for the reduction of ketones, the keto compounds are enantioselectively reduced to give secondary alcohols by means of microorganisms. Keto compounds of the formulaR.sup.3 NH--CHR.sup.1 --CO--CH.sub.2 --COOR.sup.2in which R.sup.1, R.sup.2 and R.sup.3 have the meanings defined herein are used as starting compounds.

Abstract: New salicylic acid derivatives of the general formula I ##STR1## in which R.sup.1 is H or CH.sub.3,R.sup.2 is 4-(4-methyl-2-thiazolyl)-piperazino, 4-(tetrahydro-2-furoyl)-piperazino, 4-(4-methyl-2-thiazolyl)-homopiperazino, 4-benzamidopiperidino, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolino, 1-imidazolyl, tribromo-1-imidazolyl or 2-(3-indolyl-1,1-dimethyl-ethylamino andR.sup.3 is alkoxy having 1-C atoms, NH.sub.2 or alkylamino having 1-4 C atoms,as well as the physiologically acceptable acid addition salts thereof, exhibit effects on the circulation, especially effects lowering the blood pressure and relieving the heart, and diuretic effects.

Abstract: New peptides of the formula IX--Z--W--E--W'--Y Iwherein X, Z, W, E, W' and Y are as defined herein and their salts inhibit the activity of human plasma renin.

Abstract: Compounds of the formula ##STR1## wherein A is C--C single bond, --CH.sub.2 --, --CH(CH.sub.3)--, --C(CH.sub.3).sub.2 --, --CH.sub.2 --CH.sub.2 --, CH(CH.sub.3)CH.sub.2 --, --C(CH.sub.3).sub.2 CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 O--; R.sup.1a and R.sup.1 each independently is hydrogen or a protective group which can be cleaved by solvolysis or by hydrogenolysis; R.sup.2 is H or alkyl of 1 to 3 C atoms; R.sup.3 is alkyl of 3 to 5 C atoms, phenyl or phenyl which is monosubstituted to trisubstituted by F, Cl, OH, OCH.sub.3, OC.sub.2 H.sub.5, CF.sub.3 or alkyl of 1 to 3 C atoms, or, when A is not --CH.sub.2 O--, can also be pyridyl, thienyl, naphthyl or alkoxy of 1 to 4 C atoms; indicates a bond in the .beta.-position and wavy line ( ) means that the bond can be in the .alpha.- or .beta.-position, are valuable intermediates for the stereospecific preparation of 13-thiaprostaglandin derivatives. The latter are prepared by U.V.

Abstract: Sulfur-containing 6-ketoprostaglandins of the formula I ##STR1## in which D is a bond, alkylene having 1-3 C atoms, cis-alkenylene having 2-5 C atoms or alkinylene having 2-5 C atoms,R.sup.1 is H, alkyl having 1-4 C atoms, aryl having 6-12 C atoms or --C.sub.6 H.sub.4 NHCOC.sub.6 H.sub.5,R.sup.2 is alkyl having 1-7 C atoms, alkyl having 1-7 C atoms which is substituted by halogen, cycloalkyl having 5-6 C atoms, cycloalkyl having 5-6 C atoms which is substituted by alkyl having 1-4 C atoms, phenyl, phenyl which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3, pyridyl, naphthyl, thienyl or, if D is alkylene having 1-3 C atoms, also is alkoxy having 1-4 C atoms, alkylthio having 1-4 C atoms, phenoxy or phenoxy which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3,R.sup.3 and R.sup.

Abstract: 13-thiaprostaglandins of Formula I ##STR1## wherein B is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,R.sup.1 is phenyl, CH.sub.3, or NH.sub.2,R.sup.2 is H or CH.sub.3, andR.sup.3 is pentyl, hexyl, 1-methylpentyl, or 1,1-dimethylpentylhave valuable pharmacological properties, e.g., as cytoprotective agents.

Abstract: 13-Thiaprostanoic acid derivatives of the general formula I ##STR1## wherein A is --CO-- or --CHOH--; B is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--; Q is 1,4-phenylene or 1,4-naphthylene; R.sup.1 is H or OH; R.sup.2 is H or CH.sub.3 ; R.sup.3 is alkyl with 1-8 carbon atoms or alkyl with 1-8 carbon atoms substituted by (a) phenyl, (b) phenyl substituted by at least one of CH.sub.3, F, Cl, Br, OH, OCH.sub.3 or CF.sub.3 ; (c) phenoxy or (d) phenoxy substituted by at least one of CH.sub.3, F, Cl, Br, OH, OCH.sub.3 or CF.sub.3 ; and R.sup.4 is NH.sub.2, CH.sub.3, phenyl, p-acetylaminophenyl, p-benzoylaminophenyl or phenylamino. These compounds are useful for lowering blood pressure as well as for other pharmaceutical purposes. They also are useful intermediates for the preparation of other known pharmaceuticals such s the 13-thiaprostaglandins.

Abstract: Benzothiazole derivatives of the formula I ##STR1## wherein R.sup.1 is H or CH.sub.3 ; R.sup.2 is phenyl, tolyl, xylyl or pyridyl; R.sup.3 is OH, alkoxy of 1-4 C atoms or -NHCH.sub.2 CH.sub.2 OH; and R.sup.4 is H, Cl, Br, OH or alkoxy of 1-4 C atoms,and physiologically acceptable salts thereof, have valuable pharmacological properties.

Abstract: Phenothiazine derivatives of the formula ##STR1## wherein R is H, F, Cl, Br, I, CH.sub.3, CF.sub.3, CN, CH.sub.3 O or CH.sub.3 CO; Y is S, SO, or SO.sub.2 ; Z is imidazol-1-yl, 2-methyl-imidazol-1-yl, pyrazol-1-yl or benzimidazol-1-yl; and n is 1, 2 or 3; or the physiologically acceptable acid addition salts thereof; are useful as antihypertensive agents, for example.

Abstract: Pyrazole derivatives of the formula ##STR1## wherein R.sup.1 is H or Cl; R.sup.2 is 1-methyl-4-piperidyloxy-carbonyl, 2-(4-phenylpiperazino)-ethoxycarbonyl, benzoxazol-2-yl, benzthiazol-2-yl, tetrazol-5-yl or 3-R.sup.3 -4-R.sup.4 -thiazolidin-2-yl; R.sup.3 is H, alkanoyl of 1-7 carbon atoms or benzoyl; and R.sup.4 is H or COOH,or a physiologically acceptable salt thereof;possess valuable pharmacological activities.

Abstract: 13-Thiaprostanoic acid derivatives of the formula ##STR1## wherein A is --CO-- or --CHOH--, B is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH-- R.sup.1 is H or alkyl of 1 to 4 carbon atoms, m is a whole number from 0 to 5, n is a whole number from 0 to 3 or, when B is --CH.dbd.CH--, additionally 4, 5, 6, 7, 8 or 9, R.sup.2 is alkoxy of 1 to 4 carbon atoms, phenoxy, pyridyl, thienyl, naphthyl, phenyl substituted by F, Cl, Br, OH, OCH.sub.3 or OF.sub.3 or phenoxy substituted by F, Cl, Br, OH, OCH.sub.3, CH.sub.3 or CF.sub.3 or, when B is --CH.dbd.CH--, additionally hydrogen, phenyl or tolyl, R.sup.3 is H, methyl or ethyl, possess pharmacological activity, including blood pressure lowering activity.

Abstract: Compounds of formula ##STR1## their mirror images and racemic mixtures, and the physiologically acceptable salts thereof,wherein A and D each are ketalized carbonyl groups; B is --CH.sub.2 --, --CH(CH.sub.3)--, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.sub.2 --, --CH(CH.sub.3)CH.sub.2 ----C(CH.sub.3).sub.2 CH.sub.2 -- or --CH.sub.2 O--; R.sup.1 is H or alkyl of 1-4 C-atoms; and R.sup.2 is alkyl of 3 to 5 C-atoms, phenyl or phenyl substituted one to three times by F, Cl, CF.sub.3, OH, OCH.sub.3, OC.sub.2 H.sub.5 or alkyl of 1 to 3 C-atoms inhibit aggregation and/or adhesion of thrombocytes.

Abstract: Compounds of the Formula ##STR1## and the physiologically acceptable salts thereof, wherein R.sup.1 and R.sub.2 each is hydrogen or benzyl; R.sup.3 is alkyl of 5-10 C-atoms or 2-hydroxyalkyl of 5-10 C-atoms; R.sup.4 is hydrogen, methyl or ethyl; R.sup.5 is alkyl of 5-10 C-atoms or --C.sub.n H.sub.2n COOR.sup.6 ; R.sup.6 is hydrogen or alkyl of 1-4 C-atoms; and n is 0, 4, 5 or 6 are effective for inhibiting adhesion and/or agglomeration of thrombocytes.

Abstract: 1,4-Oxathianes of the formula ##STR1## and the physiologically-acceptable salts thereof wherein R.sup.1 is H or alkyl with 1-4 C-atoms; R.sup.2 is H or alkyl with 1-4 C-atoms; R.sup.3 is H, alkyl with 1-8 C-atoms, phenyl or phenyl substituted by F, Cl, Br, OH, OCH.sub.3, CF.sub.3 or NO.sub.2 ; R.sup.4 is H or CH.sub.3 ; B is a single bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --CH.sub.2 O--; and a wavy line ( ) indicates that these bonds can be in the .alpha.- or .beta.- positions possess thrombocyte inhibition properties.

Abstract: Prostenoic acid derivatives of the general formula ##STR1## wherein R.sup.1 is H or alkyl of 1-4 carbon atoms;R.sup.2 is alkyl of 5 - 9 carbon atoms, phenoxymethyl or phenoxymethyl substituted by up to 3 of F, Cl, Br, CH.sub.3, CF.sub.3, or OCH.sub.3 ;R.sup.3 is H or alkyl of 1 - 5 carbon atoms, and physiologically acceptable salts thereof, as well as intermediates therefore are blood-pressure lowering, vasodilatory, diuretic, and nasal mucosa decongesting agents and are produced from intermediates of the formula ##STR2## wherein R.sup.4 is H or acyl of up to 5 carbon atoms and A is CH.sub.2 D or CH.dbd.C(OR.sup.5); D is carbonyl or dialkoxypolymethylene of up to 7 carbon atoms.

Abstract: Prostenoic acid derivatives of the general formula ##STR1## wherein R.sup.1 is H or alkyl or 1-4 carbon atoms;R.sup.2 is alkyl of 5 - 9 carbon atoms, phenoxymethyl or phenoxymethyl substituted by up to 3 of F, Cl, Br, CH.sub.3, CF.sub.3, or OCH.sub.3 ;R.sup.3 is H or alkyl or 1 - 5 carbon atoms, and physiologically acceptable salts thereof, as well as intermediates therefore are blood-pressure lowering, vasodilatory, diuretic and nasal mucosa decongesting agents.