Title:
MERCAPTO-ACETAMIDE DERIVATIVES
Document Type and Number:
WIPO Patent Application WO1993019024
Kind Code:
A3
Abstract:
New pharmacologically active derivatives of N-(2-mercapto-acetyl) homocysteine, both in its cyclised gamma -thiolactonic form or in the open chain form are described, such derivatives having formula (I) wherein R represents a hydrogen atom, a C1-3 alkyl, a C7-9 aralkyl or a group COR1 in which R1 is a C1-3 alkyl or a C7-9 aralkyl, the aralkyl groups being unsubstituted or substituted on the phenyl ring by one or more halogens, C1-3 alkyl or C1-3 alkoxy; L is hydrogen, Q is hydroxy, or L and Q, together, form a bond. The process for the preparation of the above compounds as well as the pharmaceutical compositions containing them are also described. The above compounds are potent free-radical scavenging agents. They can prevent the cellular damage induced by free radicals and they have additional local antiinflammatory, mucolytic and mucokinetic activities. Therefore, the compounds may be useful in the treatment of acute and chronic bronchitis, emphysema, acute and chronic ORL pathologies, as antidotes against drug-induced depletion of endogenous glutathione and in case of alteration of the biological oxidant-antioxidant balance.
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Inventors:
NICOLA MASSIMO (IT)
INGLESI MARCO (IT)
FREGNAN GIANCARLO B (IT)
VANDONI GUIDO (IT)
INGLESI MARCO (IT)
FREGNAN GIANCARLO B (IT)
VANDONI GUIDO (IT)
Application Number:
PCT/EP1993/000449
Publication Date:
October 28, 1993
Filing Date:
February 26, 1993
Export Citation:
Assignee:
EDMOND PHARMA SRL (IT)
International Classes:
A61K31/195; A61K31/19; A61K31/198; A61K31/38; A61K31/381; A61P11/08; A61P29/00; C07C319/14; C07C323/52; C07C323/56; C07C323/60; C07C327/22; C07D333/32; C07D333/36; (IPC1-7): C07C/
Foreign References:
| FR2518542A1 | 1983-06-24 | |||
| FR2561105A1 | 1985-09-20 | |||
| EP0061386A1 | 1982-09-29 | |||
| EP0192191A1 | 1986-08-27 |
Other References:
IL FARMACO EDIZIONE SCIENTIFICA vol. 41, no. 10, 1986, ITALY pages 758 - 780 G. PICCIOLA 'DERIVATI DELLA METIONINA AD ATTIVITA EPATOPROTETTRICE'
IL FARMACO EDIZIONE SCIENTIFICA vol. 41, no. 1, 1986, ITALY pages 69 - 79 M. GOBETTI 'DL-S-(2-(N-3-(2-OXO-TETRAHYDRO THIENYL)ACETAMIDO))-THIOGLYCOLIC ACID: A NOVEL MUCOLYTIC AGENT OF THE CLASS OF HOMOCYSTEINE THIOLACTONE DERIVATIVES'
CHEMICAL ABSTRACTS, vol. 109, no. 3, 1988, Columbus, Ohio, US; abstract no. 17008a, G.B. FREGNAN 'Proconvulsive and convulsive properties of methionine , homocysteine and related compounds in mice.'
IL FARMACO EDIZIONE SCIENTIFICA vol. 41, no. 1, 1986, ITALY pages 69 - 79 M. GOBETTI 'DL-S-(2-(N-3-(2-OXO-TETRAHYDRO THIENYL)ACETAMIDO))-THIOGLYCOLIC ACID: A NOVEL MUCOLYTIC AGENT OF THE CLASS OF HOMOCYSTEINE THIOLACTONE DERIVATIVES'
CHEMICAL ABSTRACTS, vol. 109, no. 3, 1988, Columbus, Ohio, US; abstract no. 17008a, G.B. FREGNAN 'Proconvulsive and convulsive properties of methionine , homocysteine and related compounds in mice.'
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