Abstract: A novel group of anti-inflammatory compounds are salts composed of the anion of a nonsteroidal anti-inflammatory acid drug (NSAID) and the cation N(1)-methylnicotinamide, which both anion and cation moieties alone exhibit anti-inflammatory activity, and which in this combination have advantages over the individual compounds and in comparison to commercial anti-inflammatory products. The compounds are produced in analogy to processes known in the art. They are used for the preparation of new pharmaceutical formulations with anti-inflammatory and analgesic activity. The new pharmaceutical formulations exhibit several advantageous properties over preparations of prior art.

Abstract: Amine hydrofluorides of the general formula (I): R—N(CH2CH2OH)2.HF   (I) In which R is a straight-chain hydrocarbon residue having 10 to 20 carbon atoms exhibit antibacterial and caries-prophylactic activity and can be prepared in high purity. The amine hydrofluorides of the formula (I) can be formulated, optionally in combination with tin fluoride, into oral hygiene compositions such as toothpastes, mouthwashes or chewable tablets.

Abstract: Amine hydrofluorides of the general formula (I):

Abstract: Described is a process for preparing triazolone compounds of the formula ##STR1## comprising heating a mixture of a compound of the formula ##STR2## and a hydrazine derivative of the formula R.sup.5 --NH--NH--CHO, R.sup.5 --NH--NH--C(O)OC(CH.sub.3).sub.3 or R.sup.5 --NH--NH--C(O)OCH.sub.2 C.sub.6 H.sub.5, optionally in the presence of an added base.

Abstract: 2-Substituted 5-chlorimidazoles of the general formula: ##STR1## are new intermediate products for the production of antihyperintensive pharmaceutical agents or of herbicidal compounds. A process for the production of these intermediate products as well as a new process for the further reaction of 2-substituted 5-chlorimidazoles of general formula I, wherein R.sub.

Abstract: A process for preparing 2-substituted 5-chloroimidazole-4-carbaldehydes of the general formula: ##STR1## In the process, a glycine ester hydrohalide is ring-closed with an imidate ester to obtain the intermediate 2-substituted 3,5-dihydroimidazol-4-one. This intermediate is converted with an N,N-substituted formamide acetel into an N,N-substituted aminomethyleneimidazolinone. This latter intermediate is chlorinated with phosphorus oxychloride or phosgene to obtain the final product 2-substituted 5-chlorimidazole-4-carbaldehydes of the general formula I.Also disclosed are N,N-substituted aminomethyleneimidazolinones of the general formula: ##STR2## wherein R is hydrogen or is an alkyl group, an alkenyl group, a cycloalkyl group, an arylalkyl group or an aryl group, and R.sub.5 and R.sub.6 are identical or different and each is an alkyl group or an aryl group, in the form of the E- or Z-isomer.

Abstract: The 2-substituted 5-chlorimidazoles of general formula: ##STR1## are new intermediate products for the production of antihypertensive pharmaceutical agents or of herbicidal compounds. A process for the production of these intermediate products as well as a new process for the further reaction of 2-substituted 5-chlorimidazoles of general formula I, wherein R.sub.

Abstract: A process for preparing 2-substituted 5-chloroimidazole-4-carbaldehydes of the general formula: ##STR1## In the process, a glycine ester hydrohalide is ring-closed with an imidate ester to obtain the intermediate 2-substituted 3,5-dihydroimidazol-4-one. This intermediate is converted with an N,N-substituted formamide acetal into an N,N-substituted aminomethyleneimidazolinone. This latter intermediate is chlorinated with phosphorus oxychloride or phosgene to obtain the final product 2-substituted 5-chlorimidazole-4-carbaldehydes of the general formula I.Also disclosed are N,N-substituted aminomethyleneimidazolinones of the general formula: ##STR2## wherein R is hydrogen or is an alkyl group, an alkenyl group, a cycloalkyl group, an arylalkyl group or an aryl group, and R.sub.5 and R.sub.6 are identical or different and each is an alkyl group or an aryl group, in the form of the E- or Z-isomer.

Abstract: The 2-substituted 5-chlorimidazoles of general formula: ##STR1## are new intermediate products for the production of antihypertensive pharmaceutical agents or of herbicidal compounds. A process for the production of these intermediate products as well as a new process for the further reaction of 2-substituted 5-chlorimidazoles of general formula I, wherein R.sub.

Abstract: Compounds of formula I are described, ##STR1## wherein n is equal to one or two, R.sub.1 stands for hydrogen or an amino protecting group, R.sub.2 represents hydrogen or a carboxyl protecting group and R.sub.3 4-methyltriphenylmethyl, 4,4'-dimethyltriphenylmethyl, 4,4',4"-trimethyltriphenylmethyl. Furthermore described are compounds of formula I which are reactive and suitable for coupling reactions and are derived from I with R.sub.2 =H by activation of the carboxyl group.The compounds mentioned above can be used as starting materials for the synthesis of peptides. They are more suitable than analogous compounds of formula I, wherein R.sub.3 represents hydrogen or a carbamoyl protecting group used hitherto.

Abstract: Process for the production of 2-substituted 5-chlorimidazole-4-carbaldehydes of general formula: ##STR1## wherein R is alkyl, cycloalkyl, benzyl, or phenyl. These compounds form valuable intermediate products for the production of antihypertensive pharmaceutical agents or herbicidal compounds.

Abstract: A process for the production of 2-substituted 5-chlorimidazole-4-carbaldehydes of the general formula: ##STR1## wherein R is hydrogen, an alkyl group, and alkenyl group, a cycloalkyl group, a benzyl group, a phenyl group or an aryl group. These compounds form important intermediate products for the production of antihypertensive pharmaceutical agents or herbicidal compounds.

Abstract: A process for preparing an (S,S) or (R,R) diastereoisomer of the formula: ##STR1## or salts, esters or amides thereof, wherein R.sup.3 and R.sup.4 independently represent hydrogen, alkyl, aryl or aryl substituted with halogen, alkyl, nitro or alkoxy, and n and m independently represent integers from one to six, comprising combining a cyanide compound of the formula:M.sup.1 C.tbd.N (III)wherein M.sup.1 is hydrogen, trimethylsilyl or a metal, with an optional proton source, a solvent and a Lewis acid of the formula:M.sup.2 X.sub.4, AlCl.sub.3 or BF.sub.3 (IV)wherein M.sup.2 is Sn or Ti and X represents chloro, bromo, fluoro or iodo, with an .alpha.-amino acid compound or salts or esters thereof, followed by addition of an acyl or acetal compound to give the diastereoisomer of formula (X).

Abstract: The following intermediate compounds, namely, 4-Oxo-3-(2-propenyl)-piperidine-3-carboxylic acid ester of the formula: ##STR1## wherein R is hydrogen, a formyl group, an acetyl group or a benzoyl group or is a benzyl group, whose aromatic ring optionally is ring-substituted by at least one halogen atom, and R.sub.1 is an alkyl group with 1 to 4 C atoms.4-Oxo-3-(2-propenyl)-piperidine of the formula: ##STR2## wherein R is hydrogen, a formyl group, and acetyl group or a benzoyl group or is a benzyl group, whose aromatic ring optionally is ring-substituted by at least one halogen atom.

Abstract: A process for the production of 4,5,6,7-tetrahydrothieno-[3,2-c]-pyridines of the formula: ##STR1## Thus, in the case of a 4-oxo-3-piperidine-3-carboxylic acid ester of the formula: ##STR2## an allyl group is introduced in the 3 position, the ester function in the 3 position is removed, the resultant compound of the formula: ##STR3## is ionized, reduced to the corresponding aldehyde of the formula: ##STR4## and with H.sub.2 S/HCl in the presence of a metal halide is cyclized to the end product. The synthesized compounds have antithrombotic action.

Abstract: The invention relates to azetidin-2-ones of the formula ##STR1## wherein R.sub.a represents hydroxy-lower alkyl, R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group, R.sub.2.sup.A together with the carbonyl group to which it is attached is a protected carboxyl group and Z' is oxygen, sulfhur or an optionally substituted methylidene group, functional groups in the radicals R.sub.a, R.sub.1 and Z' optionally being in protected form. The azetidinones are useful intermediates for the preparation of penem antibiotics.

Abstract: The present invention relates to a novel polymeric carrier, a process for its production and its use for the preparation of peptides and their intermediates. The process comprises reacting chloromethylated polystyrene (cross-linked with divinylbenzene) with a 4-hydroxy-2-substituted-benzyl alcohol (linker), attaching .alpha.-amino acids with amino and side-chain protection to the carrier thus obtained, and building up a peptide according to the method known in the field of solid phase peptide synthesis (SPPS). The method allows removal of intermediates or final products under extremely mild acidic conditions giving products in high state of purity and yield. The 2-substituent consists of an electron donating group, such as methoxy.

Abstract: The present invention relates to a novel polymeric carrier, a process for its production and its use for the preparation of peptides and their intermediates. The process comprises reacting chloromethylated polystyrene (cross-linked with divinylbenzene) with a 4-hydroxy-2-substituted-benzyl alcohol (linker), attaching .alpha.-amino acids with amino and side-chain protection to the carrier thus obtained, and building up a peptide according to the method known in the field of solid phase peptide synthesis (SPPS). The method allows removal of intermediates or final products under extremely mild acidic conditions giving products in high state of purity and yield. The 2-substituent consists of an electron donating group, such as methoxy.

Abstract: Process for the production of optically-active di-[3-chloro-2-oxy-propyltrimethylammonium]-tartrate. Racemic 3-chloro-2-oxy-propyltrimethylammonium-chloride is converted by racemate resolution with optically-active tartaric acid into the optically-active di-[3-chloro-2-oxy-propyltrimethylammonium]-tartrate. Such optically-active tartrate compound is dissociated in tartaric acid and optically-active 3-chloro-2-oxy-propyltrimethylammonium-chloride and the latter is converted with inorganic cyanides. From the product, the production of optically-active carnitine nitrile chloride can be achieved.

Abstract: Process for the production of optically-active di-[3-chloro-2-oxy-propyltrimethylammonium]-tartrate. Racemic 3-chloro-2-oxy-propyltrimethylammonium-chloride is converted by racemate resolution with optically-active tartaric acid into the optically-active di-[3-chloro-2-oxy-propyltrimethylammonium]-tartrate. Such optically-active tartrate compound is dissociated in tartaric acid to optically-active 3-chloro-2-oxy-propyltrimethylammonium-chloride and the latter is converted with inorganic cyanides. From the product, the production of optically-active carnitine nitrile chloride can be achieved.