Spofa United Pharmaceutical Works

Spofa, Spojene Podniky Pro Zdravotnickou Vyrobu

Spofa Spojene Podniky Pro Zdravotnickou

Vyzkumny Ustav Pro Farmacii a Biochemii, Statni Podnik

Vyzkumng, Ustav Pro Farmacii a Biochemii, Statni Podnik

Spojene Podniky Prozdravotnickou Vyrobu (spofa)

Jaroslava Grimova

Oldrich Nemecek

Miroslav Kuchar

Bohumila Brunova

Ludmila Fisnerova

Eva Maturova

Antonin Cerny

Zdenek Roubal

Jiri Krepelka

Miroslav Semonsky

Karel Rezabek

Miroslav Seda

Vaclav Trcka

Milan Melka

Stanislava Pokorna

Ruzena Reichlova

Milan Miko

Irena Kejhova

Darina Slukova

Jiri Kejha

Eva Knezova

Marta Beitova

Marie Poppova

This relates to substances represented by formula (I), wherein X stands for represented by either OR in which R is an alkyl of 1 to 4 carbon atoms, or NHR in which is an alkyl of 1 to 4 carbon atoms, or a (CH.sub.2).sub.n NR.sub.2 group wherein n is 2 or 3 while R.sup. is an methyl or an ethyl group; eventually X may represent morpholinyl. Also considered are salts of 4-(2,4-difluorbiphenylyl)-2-methyl-4-oxobutanoic acid with appropriate inorganic or organic bases represented by formula (II) wherein B.sup.+ is either an alkaline metal cation, alkaline earth metal cation, cyclohexylamine cation, or lysine cation. Said substances are characterized by antiinflamatory properties comparable to (and greater than) the initial acid while simultaneously said modifications of their physico-chemical properties broaden the posibilities of their therapeutic application. ##STR1##

Derivatives of 4-(2,4-difluorbiphenylyl)-2-methyl-4-oxobutanoic acid

This invention relates to 5-[4-[-(4,6-dimethyl-2-pyrimidinylsulfamoyl)phenylazo]acetylsalicylic acid (DISALAZINE) is provided as a new compound having anti-arthritic and immunomodulating properties. It can be produced via reaction of the diazonium salt of sulfadimidine reacted with salicylic acid and then acetylating the product anti-arthritic and immunomodulating properties.

5-[4-(4,6-dimethyl-2-pyrimidinylsulfamoyl)phenylazo]acetylsalicylic acid

An etheric derivative of 4(3H)-quinazolinone which is a fluorinated 3-[2-(4-biphenylyloxy)ethyl]-4(3H)-quinazolinone, produced by reacting said 4(3H)-quinazolinone with the corresponding fluorinated 4-(2-chloroethoxy)biphenyl, and its acid addition salts, especially the hydrochloride. This compound possesses substantially higher analgesic activity and lower acute toxicity than aminophenazone, ibuprofen, acetylosalicyclic acid and paracetamol.

Etheric derivative of 4(3H)-quinazolinone and a process for preparation

6-purinyl N-(2-chloroethyl) carbamate and thiocarbamate are disclosed of the general formula I, ##STR1## in which X stands for an oxygen or sulfur atom, and also a process for their preparation by reacting a purine derivative of the general formula II (hypoxanthine or 6-mercaptopurine, respectively) with 2-chloroethylisocyanate. The subject compounds of formula I show a remarkable antineoplastic effect in vitro and in vivo, and consequently have great potential for the treatment of malignant neoplastic diseases in mammals.

6-purinyl N-/2-chloroethyl/carbamate and thiocarbamate and process for

The invention relates to omega-(2',4'-dihalobiphenylyl)oxo alkanoic acids of Formula: ##STR1## wherein X.sup.1 and X.sup.2 each represent a fluorine or chlorine atom and Y represents a bivalent hydrocarbon chain selected from the group consisting of --CH.sub.2 --CH--CH.sub.3 and (CH.sub.2).sub.3, and to a process for their preparation. The compounds of the invention are highly active and longlasting anti-inflammatory agents.

Omega-(2,4-dihalobiphenylyl) oxo alkanoic acids

This invention relates to the compound 3-[2-(2-Benzimidazolyl) Benzoyloxyethyl]-4(3H)-Quinazolinone of Formula I, and a process for the preparation thereof. The compound exhibits strong analgesic activity and almost zero toxicity in laboratory mice. ##STR1## The compound of Formula I is prepared by acylation of the compound 3-(2-hydroxyethyl)-4(3H)-quinazolinone with a reactive derivative of 2-(2-benzimidazolyl)benzoic acid, preferably its imidazolide, formed by treatment of the acid of Formula III with 1,1'-carbonyldiimidazole. The compounds of Formula II and Formula III are reacted in situ, at room temperature, and in the presence of an inert organic solvent. The product compound is isolated and purified by common techniques.

3-(2-(2-benzimidazolyl) benzolyloxyethyl)-4(3H)-quinazolinone

Antiinflammatory substituted phenylacetic acids of low toxicity are prepared by reaction of a salt of an alkyl 3 chloro-4-hydroxyphenylacetate with a substituted benzyl halide in the presence of an inert organic solvent at elevated temperatures.

Antiinflammatory substituted phenylacetic acids

A technique is described for the preparation of a novel anti-inflammatory agent comprising 2-phenyl-2-carboxyethyl 1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetate. The preparative technique involves reacting indomethacin with tropic acid.

2-Phenyl-2-carboxyethyl

8-(.beta.-AMINOETHYL)ERGOLINES-I of the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or an acyl group of the general formula R.sup.3 --CO, R.sup.3 being a hydrogen atom, an alkyl group having from 1-5 carbon atoms, a phenyl group, a phenylalkyl group or a pyridyl group or substituents thereof, and R.sup.2 is a hydrogen atom or a methyl group. Acid addition salts of the described ergolines evidence pharmacological activity in the anti-inflammation and hypotensive fields.

8-(.beta.-AMINOETHYL)ERGOLINES-I

Growing community of inventors

Prague, Czechia

Jaroslava Grimova