Patent US3885012A successfully refreshed from Google Patents.
US3885012A
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New protease-inhibiting substance, its extraction, and its use
Assignee: Bayer AG
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Filing: 1973-03-02
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Granted: 1975-05-20
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Expires: 1993-03-02
Abstract
Abstract There is disclosed a new protease-inhibiting substance obtained from edible snails, and particularly the edible snail, Helix pomatia, processes for extraction thereof from the edible snail, Helix promatia, and to its use as a medicine.
Inventors
- 👤 Harald Tschesche
- 👤 Hans Fritz
- 👤 Rudolf Christoph
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 10:50
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/16; A61K38/55; A61K38/57
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
98 words
A PROTEASE-INHIBITING SUBSTANCE CHARACTERIZED BY AN INHIBITING ACTION TOWARD TYRPSIN CHYMOTRYPSIN, PLASMIN AND KINIOGENASES; SAID SUBSTANCE CONTAINING AT LEAST ONE ISOINLHIBITOR HAVING AN ISOELECTRIC POINT BELOW 10.5, A CONTENT OF 55-70 AMINO ACID RESIDUES, AND A MOLECULAR WEIGHT OF ABOUT 6500, WHEREIN SAID PROTEASE-INHIBITING SUBSTANCE IS OBTAINED BY A PROCESS COMPRISING: I. HOMOGENIZING EDIBLE SNAILS OF THE GENUS HELIX OF THE FAMILY HELICIDAE TO PRODUCE A HOMOGENATE; II. SEPARATING THE HOMOGENATE INTO A PRECIPITATE AND SUPERNATANT LIQUID, AND III. MIXING THE SUPERNATANT LIQUID WITH AMMONIUM SULPHATE UP TO 63% OF THE SATURATION CENCENTRATION TO PRECIPITATE THE PROTEASE-INHIBITING SUBSTANCE.
Claim 2
Dependent Claim
98 words
A PROTEASE-INHIBITING SUBSTANCE CHARACTERIZED BY AN INHIBITING ACTION TOWARD TYRPSIN CHYMOTRYPSIN, PLASMIN AND KINIOGENASES; SAID SUBSTANCE CONTAINING AT LEAST ONE ISOINLHIBITOR HAVING AN ISOELECTRIC POINT BELOW 10.5, A CONTENT OF 55-70 AMINO ACID RESIDUES, AND A MOLECULAR WEIGHT OF ABOUT 6500, WHEREIN SAID PROTEASE-INHIBITING SUBSTANCE IS OBTAINED BY A PROCESS COMPRISING: I. HOMOGENIZING EDIBLE SNAILS OF THE GENUS HELIX OF THE FAMILY HELICIDAE TO PRODUCE A HOMOGENATE; II. SEPARATING THE HOMOGENATE INTO A PRECIPITATE AND SUPERNATANT LIQUID, AND III. MIXING THE SUPERNATANT LIQUID WITH AMMONIUM SULPHATE UP TO 63% OF THE SATURATION CENCENTRATION TO PRECIPITATE THE PROTEASE-INHIBITING SUBSTANCE.
Claim 3
Dependent Claim
90 words
A protease-inhibiting substance characterized by an inhibiting action towards trypsin, chymotrypsin, plasmin and kininogenases; said substance containing at least one iso-inhibitor having an isoelectric point below 10.5, a content of 55-70 amino acid residues, and a molecular weight of about 6,500, wherein said protease-inhibiting substance is obtained by a process comprising: i. homogenizing Helix pomatia to produce a homogenate; ii. separating the homogenate into a precipitate and a supernatant liquid, and iii. mixing the supernatant liquid with ammonium sulphate up to 63% of the saturation concentration precipitate the protease-inhibiting substance.
Claim 4
Dependent Claim
90 words
A protease-inhibiting substance characterized by an inhibiting action towards trypsin, chymotrypsin, plasmin and kininogenases; said substance containing at least one iso-inhibitor having an isoelectric point below 10.5, a content of 55-70 amino acid residues, and a molecular weight of about 6,500, wherein said protease-inhibiting substance is obtained by a process comprising: i. homogenizing Helix pomatia to produce a homogenate; ii. separating the homogenate into a precipitate and a supernatant liquid, and iii. mixing the supernatant liquid with ammonium sulphate up to 63% of the saturation concentration precipitate the protease-inhibiting substance.
Claim 5
Dependent Claim
36 words
A protease-inhibiting substance in accordance with claim 1 which contains a plurality of ios-inhibitors having at least in coommon isoelectric points below 10.5, contents of amino acid residues of 55-70 and molecular weights of about 6,500.
Claim 6
Dependent Claim
36 words
A protease-inhibiting substance in accordance with claim 2 which contains a plurality of iso-inhibitors having at least in common isoelectric points below 10.5, contents of amino acid residues of 55-70 and molecular weights of about 6,500.
Claim 7
Dependent Claim
36 words
A protease-inhibiting substance in accordance with claim 1 wherein said iso-inhibitor contains 58 amino acid residues, free of histidine and tryptophan residues and having an arginine residue essential to its inhibiting activity at its reactive center.
Claim 8
Dependent Claim
36 words
A protease-inhibiting substance in accordance with claim 2 wherein said iso-inhibitor contains 58 amino acid residues, free of histidine and tryptophan residues and having an arginine residue essential to its inhibiting activity at its reactive center.
Claim 9
Dependent Claim
41 words
A protease-inhibiting substance in accordance with claim 3 further characterized in that each of said iso-inhibitors contains 58 amino acid residues, free of histidine and tryptophan residues and having an arginine residue essential to its inhibiting activity at its reactive center.
Claim 10
Dependent Claim
41 words
A protease-inhibiting substance in accordance with claim 4 further characterized in that each of said iso-inhibitors contains 58 amino acid residues, free of histidine and tryptophan residues and having an arginine residue essential to its inhibiting activity at its reactive center.
Claim 11
Dependent Claim
76 words
A process for the extraction of a protease-inhibiting substance comprising: i. homogenizing edible snails of the genus Helix of the family Helicidae to produce a homogenate; ii. separating the homogenate into a precipitate and a supernatant liquid; iii. mixing the supernatant liquid with ammonium sulfate up to 63% of the saturation concentration to precipitate the protease-inhibiting substance; and iv. fractioning the protease-inhibiting substance by gel fractionation and selecting the most active protease-inhibiting fraction or fractions therefrom.
Claim 12
Dependent Claim
76 words
A process for the extraction of a protease-inhibiting substance comprising: i. homogenizing edible snails of the genus Helix of the family Helicidae to produce a homogenate; ii. separating the homogenate into a precipitate and a supernatant liquid; iii. mixing the supernatant liquid with ammonium sulfate up to 63% of the saturation concentration to precipitate the protease-inhibiting substance; and iv. fractioning the protease-inhibiting substance by gel fractionation and selecting the most active protease-inhibiting fraction or fractions therefrom.
Claim 13
Dependent Claim
86 words
A precess for the extraction of a protease-inhibiting substance comprising: i. homogenizing edible snails of the genus Helix of the family Helicidae to produce a homogenate; ii. separating the homogenate into a precipitAte and a supernatant liquid; iii. mixing the supernatant liquid with ammonium sulfate up to 63% of the saturation concentration to precipitate the protease-inhibiting substance; and iv. fractionating the protease-inhibiting substance on a cation exchange resin to obtain a plurality of fractions, each containing a different iso-inhibitor characterized by a peak of protease-inhibiting activity.
Claim 14
Dependent Claim
86 words
A precess for the extraction of a protease-inhibiting substance comprising: i. homogenizing edible snails of the genus Helix of the family Helicidae to produce a homogenate; ii. separating the homogenate into a precipitAte and a supernatant liquid; iii. mixing the supernatant liquid with ammonium sulfate up to 63% of the saturation concentration to precipitate the protease-inhibiting substance; and iv. fractionating the protease-inhibiting substance on a cation exchange resin to obtain a plurality of fractions, each containing a different iso-inhibitor characterized by a peak of protease-inhibiting activity.
Claim 15
Dependent Claim
16 words
A pharmaceutical composition containing as an active ingredient a protease-inhibiting substance in accordance with claim 1.
Claim 16
Dependent Claim
19 words
A pharmaceutical composition in accordance with claim 11 which is an injectable aqueous solution of the said protease-inhibiting substance.
Claim 17
Dependent Claim
19 words
A medicament in dosage unit form containing as an active ingredient a protease-inhibiting substance in accordance with claim 1.
Claim 18
Dependent Claim
21 words
A medicament in accordance with claim 13 in the form of an ampoule of injectable solution of the said protease-inhibiting substance.
Claim 19
Dependent Claim
30 words
A method of inhibiting fibrinolysis or treating pancreatitis which comprises administering to a human or non-human animal an effective therapeutic dosage of a pharmaceutical composition in accordance with claim 11.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1978-05-19 | 1978-11-18 | 1979-05-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1982-05-19 | 1982-11-18 | 1983-05-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1986-05-19 | 1986-11-18 | 1987-05-20 | $7700.00 | Window Closed / Lapsed |