Abstract: A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.

Abstract: A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.

Abstract: A process for the racemization of atropisomeric bis(phosphine oxide) compounds of formula I: in their (S) or (R) or non-racemic form, is useful for preparing optical active bisphosphine ligands, that form optical active complexes with transition metals. Racemization is thermal and carried out in high or low boiling solvent, under normal or elevated pressure at 105 to 3.5×107 Pa. Heating is performed in a system that allows heating up to 400° C. (reactor, autoclave, aluminum block, round-bottom flask with heating/stirring mantle and the like) or by microwave irradiation or in the melt at a temperature from 260 to 400° C.

Abstract: The invention relates to an improved process for preparing [(3aR,4S,7aS)4-bromooctahydro-7a-methyl-1H-indene-1,5-dione]. (S)-(+)-2,3,7,7a-tetrahydro-7a-methyl-1H-indene-1,5(6H)-dione is reduced by reaction with diisobutylaluminum hydride and hexamethylphosphoric triaminde in the presence of a catalyst of the formula R—Cu, wherein R is and R1, R2 and R3 are each, independently, selected from the group consisting of C1-7 alkyl, phenyl, phenyl substituted by at least one C1-4 alkyl group, benzyl, or benzyl substituted by at at least one C1-4 alkyl group to form a reductate. The reductate is then treated with a bromine-containing electrophile to yield (3aR,4S,7aS)4-bromooctahydro-7a-methyl-1H-indene-1,5-dione.

Abstract: The present invention provides a process for the manufacture of pyrimidines of formula I: wherein R1, R2, R3 each independently represent hydrogen, C1-7-alkyl, or C1-7-alkoxy, A signifies —CN, a carbanionic R4-alkynyl residue, in which R4 is hydrogen or C1-7-alkyl, or a carbanionic residue of the malonic acid derivative of formula III  in which B and B′ independently represent —CN, —COOR5, or —C(O)R5, wherein R5 is alkyl or aryl.

Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.

Abstract: A hypodermic injection system allows for the generation of a high pressure liquid jet capable of passing through the skin. The system uses two regions, the first region being flexible or squeezable and the second region having at least one exiting orifice through which the liquid jet can be expelled. The flexible region can be deformed by a pressure change in the surrounding container generated by an activatable gas generator that generates pressure within the first region that causes the liquid to be expelled.

Abstract: Methods for preparing antiosteoportic agents are disclosed. Compounds useful in the methods are also disclosed.

Abstract: The compounds of formula (I) wherein R1, R2 and X have the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.

Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.

Abstract: Osteoblast-specific mitogens and drugs containing such compounds can be used for treating metabolic bone diseases. These compounds include lysophosphatidylic acid derivatives selected from the group consisting of compounds of formula: wherein R1=alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen or NH; the compounds (all-cis-5,8,11,14)-eicosatetraenoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9, cis-12-octadecadienoic acid 2-hydroxy-3-phosphonooxypropyl ester; (all-cis-9,12,15)-octadecatrienoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9-octadecenoic acid 2-hydroxy-3-phosphonooxypropyl ester; and erucic acid 2-hydroxy-3-phosphonooxypropylester being excluded, and the physiologically tolerable salts, esters, optically active forms, and racemates of said compounds, and derivatives of said compounds, salts, esters, optically active forms and racemates which can be metabolized in vivo to yield the corresponding compound of formula (I).

Abstract: Compounds of formula (I) wherein R1 and R2 are as defined in the description and claims and pharmaceutically acceptable salts thereof, are useful for the treating diseases associated with restenosis, glaucoma, cardiac infarct, high blood pressure and end organ damage, for example, cardiac insufficiency and kidney insufficiency.

Abstract: Compounds of formula I wherein X is C═CH2 or CH2; Y and Z are independently of each other hydrogen, fluorine or hydroxy; A is —C≡C—, —CH═CH— or —CH2—CH2—, R1 and R2 are independently of each other alkyl or perfluoroalkyl; and R3 is lower alkyl are useful in the treatment or prevention of hyperproliferative skin diseases, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis; or for reversing the conditions associated with photodamage.

Abstract: A process manufactures of a compound of formula: and unique intermediates.

Abstract: The present invention relates to a method for the purification of the lipstatin.

Abstract: A process is useful for making compounds of the formula: wherein R is hydro, methyl, or fluoro.Valuable intermediates in this process include: ##STR1## wherein R is hydro, methyl, or fluoro, and L is a leaving group.

Abstract: Piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the piperidine derivatives of general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Z, m and n are as described herein.

Abstract: A method for treating or preventing type II diabetes mellitus comprising administering an effective amount of a gastrointestinal lipase inhibitor, such as, tetrahydrolipstatin.

Abstract: N-(4-carbamimidophenylamino) phenylglycineamide derivative compounds having the formula: ##STR1## in which E, g.sup.1, g.sup.2, Q, R and X.sup.1 to X.sup.4 are each as defined in the description, and hydrates or solvates and physiologically acceptable salts thereof can be used as inhibitors of the formation of the coagulation factors Xa, IXa and thrombin induced by the factor VIIa and by the tissue factor. These compounds can be used as medicaments for the treatment and/or prevention of thromboses, apoplexy, cardiac infarction, inflammation and arteriosclerosis or as antitumor agents.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;R.sup.2 signifies phenyl or substituted phenyl;R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ;R.sup.4 signifies hydrogen or lower-alkyl;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl;R.sup.a signifies hydrogen, lower-alkyl or hydroxy;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.