You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 28, 2024

Claims for Patent: 6,339,160


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 6,339,160
Title: Metalloproteinase inhibitors, their therapeutic use and process for the production of the starting compound in the synthesis thereof
Abstract:Objects of the present invention are compounds of a peptido-mimetic character having the capacity of acting as inhibitors of metalloproteinases produced by venom of snake, and of other metalloproteinases of human origin which have been put in relation with various pathologies in man, including tumoral growth and metastatization, aterosclerosis, multiple sclerosis, Alzheimer\'s disease, osteoporosis, hypertension, rheumatoid arthritis and other inflammatory diseases. Object of the present invention is also the procedure for the production of diethylester of (1)-phosphotryptophan, as an initial product necessary to synthesize all compounds mentioned above.
Inventor(s): Politi; Vincenzo (Rome, IT), Gavuzzo; Enrico (Rome, IT), Gallina; Carlo (Rome, IT), Stazio; Giovanni Di (Rome, IT), D\'Alessio; Silvana (Rome, IT), Sella; Antonio (Rome, IT), Piazza; Cinzia (Rome, IT), Giordano; Cesare (Rome, IT), Gorini; Barbara (Rome, IT), Panini; Gabriella (Rome, IT), Paradisi; Mario Paglialunga (Rome, IT), Cirilli; Maurizio (Rome, IT), Pochetti; Giorgio (Rome, IT), Mazza; Fernando (Rome, IT)
Assignee: Polifarma S.p.A. (Rome, IT) Consiglio Nazionale Delle Ricerche (Rome, IT)
Application Number:09/462,932
Patent Claims:1. Compound of formula: ##STR10##

in which R is H, or CH.sub.2 --C.sub.6 H.sub.5, and R' is a saturated or aromatic ring of five or six members, of which at least one is nitrogen, oxygen or sulphur.

2. Compound according to claim 1, in which R' is selected from the group consisting of : ##STR11##

3. Pharmaceutical composition useful for therapy of human pathologies in whose pathogenic mechanism or in whose symptomatology an involvment of at least one zinc-dependent metalloproteinase has been proven, comprising as an active principle at least one of the compounds as claimed in claim 2, and a pharmaceutically compatible vehicle.

4. In a method of inhibiting enzymatic activity of at least one snake zinc-dependent metalloproteinase extracted from snake venoms belonging to the families Crotalidae and Viperidae, also called hemorrhagines, and/or at least one zinc-dependent metalloproteinase of human origin whose active site presents a three-dimensional structure analogous to that of said snake metalloproteinase, comprising

administering an inhibition-effective amount of an inhibitor of metalloproteinase to be a patient in need thereof suffering from a pathology in which the pathogenic mechanism or in which the symptomatology thereof has been shown to involve at least one zinc-dependent metalloproteinase, the improvement wherein

said inhibitor is a compound according to claim 2.

5. A method according to claim 4, in which said human metalloproteinase is ADAM.

6. A method according to claim 4, in which said metalloproteinase is Adamlysin II, Collagenase or Gelatinase A.

7. The compound of claim 1 for inhibiting enzymatic activity of at least on snake zinc-dependent metalloproteinase extracted from snake venoms belonging to the families Crotalidae and Viperidae, also called hemorrhagines, and/or at least one zinc-dependent metalloproteinase of human origin whose active site presents a three-dimensional structure analogous to that of said snake metalloproteinase.

8. A compund according to claim 7, in which said human metalloproteinases are ADAM.

9. A compound according to claim 7, in which said metalloproteinase is Adamalysin II, and/or Collagenase and Gelatinase A.

10. Pharmaceutical composition useful for therapy of human pathologies in whose pathogenic mechanism or in whose sympotomatology an involvement of at least one zinc-dependent metalloproteinase has been proved, comprising as an active principle at least one of the compounds as claimed in claim 1 and a pharmaceutically compatible vehicle.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.