Abstract: The erythromycin salt of 5-(3-carboxy-1-oxopropoxy)-.alpha.,.alpha., 4-trimethyl-3-cyclohesene-1-methanol acid is described.This salt shows a mucosecretolytic and fluidizing activity. There is further described a process for the preparation of said salt, as well as pharmaceutical compositions with mucosecretolytic and fluidizing action which contain the novel salt.
Abstract: A novel ester of (+) 6-methoxy-.alpha.-methyl-2-naphthalene acetic acid is described.Such ester is obtained by reaction of the (+)6-methoxy-.alpha.-methyl-2-naphthalene acetic acid chloride as prepared by a well known technique, with (-).alpha..sup.4, .alpha..sup.4 -dimethyl-1-cyclohexane-1,4-dimethanol.There are further described pharmaceutic compositions having mucosecretolytic, anti-inflammatory analgesic and antipyretic activity, which contain the novel ester.
Abstract: A novel theophylline-7- acetic acid ester is described. Said ester is obtained by reacting, at a temperature from 1.degree. to 20.degree. C., theophylline-7-acetic acid chloride with d,l-trans-sobrerol.There are further described pharmaceutical compositions with mucosecretolytic-fluidizing and antibronchospastic activity containing the novel ester.
Abstract: A novel derivative of (-)-6,6-dimethylbicyclo [3.1.1]ept-2-ene-2-ethanol (J. P. Bain, J. Am. Chem. Soc. 1946, vol. 68, page 638) is disclosed. The parent composition is marketed e.g. under the name nopol, v. The Aldrich-Europe Catalog Handbook of Fine Chemicals, item 3160-5 nopol 98% 128-50-7.The object of the present invention is the compound of formula (I): 4-(2-hydroxyethyl) -.alpha..alpha.dimethyl-5-hydroxy-3-cyclohexene-1-methanol, with the process for obtaining the same, which consists of the preparation of (-)-(6,6-dimethylbicyclo[3.1.1]ept-2-ene-2-ethanol epoxide, followed by hydration of the above compound. Finally, this invention comprises the pharmaceutical compositions containing the compound of formula (I) which have a mucosecretolytic pharmacological activity.
Abstract: A novel salicylic acid ester is described, which may be combined with inorganic or organic bases to give pharmaceutically acceptable salts. Such an ester is obtained by reaction of (-) campholenic acid chloride, as prepared by a well known technique, with salicylic acid.There are, further, described pharmaceutical compositions having mucosecretolytic, anti-inflammatory, analgesic, antipyretic activity, which contain the novel ester or the salts thereof.
Abstract: A novel derivative of (-)-6,6-dimethylbicyclo[3.3.1]ept-2-ene-2-methanol is disclosed.The compound which is an object of the present invention, is the derivative :.alpha.,.alpha.-dimethyl-5-hydroxy-3-cyclohexene-1,4-dimethanol.The present invention further discloses the process for obtaining the compound which consists in preparing the (-)-6,6-dimethylbicyclo[3.3.1]ept-2-ene-2-methanol epoxide, thereafter hydrating the above compound and separating the compound from the hydration products. Finally, this invention comprises the pharmaceutical compositions containing the compound which possess a pharmacological mucosecretolytic activity.
Abstract: The object of the present invention are the following diastereoisomer compounds (as derived from (-)-5-(1-hydroxy-1-methylethyl)-2-methyl-2-cyclohexene-1-one):(I): (1S-5R) 5-hydroxy-.alpha.,.alpha.-4,5-tetramethyl-3-cyclohexene-1-methanol (CO/1516)(II): (1S-5S) 5-hydroxy-.alpha.,.alpha.-4,5-tetramethyl-3-cyclohexene-1-methanol (CO/1517)which can be separated from the mixture of (I)+(II) at the % proportion of 44.44/55.55; said mixture will be hereinafter also designated either by the code CO/1483 or by (III).This invention provides, furthermore, the process for obtaining the mixture (III) (CO/1483) by reaction of (-)-5-(1-hydroxy-1-methylethyl)-2-methyl-2-cyclohexene-1-one with methyl-lithium and for separating the diastereoisomers (I) and (II) by a chromatographic method.Finally, the present invention comprises pharmaceutical compositions which contain the compounds (I), (II) and the mixture (III), when possess a pharmacologic mucosecretolytic activity.
Abstract: There is described a novel acylamide derivative of p-aminophenol as obtained by condensation of 5-(3-carboxy-1-oxo-propoxy)-.alpha.,.alpha.-4, trimethyl-3-cyclohexene-1-methanol acid with p-aminophenol.There are also described pharmaceutical compositions containing the novel p-aminophenol derivative with mucosecretolytic-fluidizing and antipyretic activity.
Abstract: The present invention concerns the new erythromycin salt of the o-carbonyl(1-thiazolidinyl)-benzoic acid having the formula ##STR1## wherein X represents the monovalent cation of erythromycin. The new salt constitutes a novel antibiotic complex for the selective therapy of the respiratory tract.
Abstract: The invention relates to complex salts of N-cyclohexyl-piperazino-acetamides or propionamides with dihydroxy aluminum-.alpha.-hydroxy-carboxylates, a process for preparing them and the use thereof as antiulcer-antisecretive-buffering drugs.
Abstract: Thiazolidine derivatives of formula ##STR1## in which R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 have the meanings as defined in the specification, Q is CH or N and X is H or a pharmacologically acceptable cation derived from an inorganic or organic base limited to amino acids. These derivatives are obtained by condensing phthalic or quinolinic anhydride, possibly substituted in the ring, with the thiazolidine, optionally substituted, in an aprotic solvent. Said derivatives as well as the salts thereof possess a fluidizing mucosecretolytic action.
Abstract: New piperazine derivatives and homologs thereof of formula ##STR1## wherein n is equal to 2 or 3 and m to 1, 2 or 3; X REPRESENTS HYDROGEN OR A METHYL GROUPR represents hydrogen or a C.sub.1 to C.sub.6 lower alkyl group or a C.sub.1 to C.sub.3 hydroxyalkyl group; andR.sub.1 is one of the following groups:A substituted cyclohexyl of formula ##STR2## wherein R.sub.2 is hydrogen or a C.sub.1 to C.sub.6 lower alkyl group, A SUBSTITUTED PHENYL OF FORMULA ##STR3## wheein R.sub.3 is hydrogen, methyl or ethyl, OR WHEREIN R.sub.1 is norbornyl, bornyl or cinnamyl, are useful as antiulcerous compounds.
Abstract: A process for the industrial production of terpene nitrolaminic derivatives, comprising a first step wherein the terpene nitroso-chlorides are prepared reacting in a concentrated organic acid medium, selected from formic acid or acetic acid, terpenic materials, selected from alpha-pinene, limonene, alpha-terpineol and the like, with concentrated hydrochloric acid, in the presence of compounds having the formula R--OH, wherein R is an alkyl group, having 1 to 7 carbon atoms, and of alkali nitrites; and a second step wherein the nitroso-chlorides, thus precipitated, are reacted after purification and recrystallization, with an aminic derivative, selected from ammonia, amines, amino-alcohols and amino-acids, in an organic solvent medium in a ratio of nitroso-chloride to aminic derivative of 1 : 1, at a temperature ranging between 50.degree. and 70.degree.