EP0124925B1
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EP
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Derivatives of d-2-(6-methoxy-2-naphthyl)-propionic acid having therapeutical activity, process for their preparation and pharmaceutical compositions containing them
Assignee: Farma Resa Srl
•
Filing: 1984-04-05
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Granted: 1986-11-26
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Expires: 2004-04-05
Abstract
Abstract Derivatives of d-2-(6-methoxy-2-naphtyl)-propionic acid with therapeutical activity having general formula: <CHEM> wherein X is selected in the group comprising H, and a radical selected among the radicals of organic or inorganic, non toxic and pharmaceutically acceptable bases, the radicals of basis aminoacids and the radicals of basic antibiotics. The invention relates also to the process for obtaining said therapeutically active derivatives and the pharmaceutical compositions containing them for anti-inflammatory, analgesic, antipyretic and mucolithic use.
Inventors
- 👤 Antonino Franchina
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-07 07:42
CPC Classifications
C; C07; C07H; C07H17/00; C07H17/04; C07H17/08; C07C; C07C51/00; C07C51/58; C07C51/60
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
46 words
Therapeutically active derivatives of d-2-(6-methoxy-2-naphthyl)-propionic acid having general formula: wherein X is selected from the group comprising H, and a radical selected among the radicals of organic or inorganic, non toxic and pharmaceutically acceptable bases, the radicals of basic aminoacids and the radicals of basic antibiotics.
Claim 2
Dependent Claim
46 words
Therapeutically active derivatives of d-2-(6-methoxy-2-naphthyl)-propionic acid having general formula: wherein X is selected from the group comprising H, and a radical selected among the radicals of organic or inorganic, non toxic and pharmaceutically acceptable bases, the radicals of basic aminoacids and the radicals of basic antibiotics.
Claim 3
Dependent Claim
27 words
Therapeutically active derivatives according to claim 1, characterized in that said organic bases are selected among primary and secondary amines and among primary, secondary and tertiary aminoalcohols.
Claim 4
Dependent Claim
19 words
Therapeutically active derivatives according to claim 2, characterized in that said organic bases are selected among diethanolamine and diethylamine.
Claim 5
Dependent Claim
21 words
Therapeutically active derivatives according to claim 1, characterized in that said inorganic bases are selected among sodium, potassium and silver hydroxides.
Claim 6
Dependent Claim
20 words
Therapeutically active derivatives according to claim 1, characterized in that said basic aminoacids are selected among arginine, lysine and histidine.
Claim 7
Dependent Claim
22 words
Therapeutically active derivatives according to claim 1, characterized in that said basic antibiotics are selected among erythromycin, propionylerythromycin, mechlocycline, clindamycine and josamycine.
Claim 8
Dependent Claim
9 words
Sodium salt of DL-2-(6-methoxy-2-naphthyl)-propionyl-alpha-thio-propionylglycinic acid according to claim 1.
Claim 9
Dependent Claim
9 words
Potassium salt of DL-2-(6-methoxy-2-naphthyl)-propionyl-alpha-thio-propionylglycinic acid according to claim 1.
Claim 10
Dependent Claim
9 words
Silver salt of DL-2-(6-methoxy-2-naphthyl)-propionyl-alpha-thio-propionylglicinic acid according to claim 1.
Claim 11
Dependent Claim
9 words
Lysine salt of DL-2-(6-methoxy-1-naphthyl-propionyl-alpha-thio-propionylglycinic acid according to claim 1.
Claim 12
Dependent Claim
8 words
Arginine salt of DL-2-(6-methoxy-2-naphthyl)-propionyl-alpha-thio-propionylglycinic according to claim 1.
Claim 13
Dependent Claim
9 words
Histidine salt of DL-2-(6-methoxy-2-naphthyl)-propionyl-alpha-thio-propionylglycinic acid according to claim 1.
Claim 14
Dependent Claim
9 words
Erythromycin salt of DL-2-(6-methoxy-2-naphthyl)-propionyl)-alpha-thio-propionylglycinic acid according to claim 1.
Claim 15
Dependent Claim
9 words
Propionylerythromycin salt of DL-2-(6-methoxy-2-naphthyl)-propionyl-alpha-thio-propionylglycinic acid according to claim 1.
Claim 16
Dependent Claim
9 words
Mechlocycline salt of DL-2-(6-methoxy-2-naphthyl)-propionyl-alpha-thio-propionylglycinic acid according to claim 1.
Claim 17
Dependent Claim
9 words
Clindamycin salt of DL-2-(6-methoxy-2-naphthyl)-propionyl-alpha-thio-propionylglycinic acid according to claim 1.
Claim 18
Dependent Claim
9 words
Josamycine salt of DL-2-(6-methoxy-2-naphthyl)-propionyl-alpha-thio-propionylglycinic acid according to claim 1.
Claim 19
Dependent Claim
59 words
A process for the preparation of the derivatives according to the preceding claims characterized by comprising the steps of: a) preparation of a reactive derivative of d-2-(6-methoxy-2-naphthyl)-propionic acid; b) reaction of said reactive derivative with an alkaline salt of alpha-mercaptopropionylglycine; c) isolation of the pure DL form of the thus obtained thio-derivative; and d) optional salification of the DL-thio-derivative.
Claim 20
Dependent Claim
42 words
A process according to claim 18, characterized in that said reactive derivative is selected among the chloride and the mixed anhydride, e.g. with ethyl chloroformate, of the d-2-(6-methoxy-2-naphthyl- propionic acid, and in that said alkaline salt is the sodium salt of alpha-mercaptopropionylglycine.
Claim 21
Dependent Claim
28 words
A process according to claim 19, characterized in that the chlorination of the d-2-(6-methoxy-2-naphthyl)propionic acid is carried out by adding thionyl chloride, in the presence of a solvent.
Claim 22
Dependent Claim
37 words
A process according to claim 20, characterized in that the reaction of the chloride of d-2-(6-methoxy-2-naphthyl-propionic acid with the sodium salt of alpha-mercaptopropionylglycine is carried out in aqueous medium at a temperature of between 0°C and +5°C.
Claim 23
Dependent Claim
25 words
Pharmaceutical composition for parenteral, oral, rectal or topical use, containing a therapeutically active amount of a derivative according to any of claims 1 to 5.
References Cited (Backward Citations)
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