Deep knowledge on
small-molecule drugs and
the 110,000 global patents
Drug patents …
… from Kazakhstan to Kalamazoo
Manage your formulary budget
Proactively manage your pharmacy inventory
Anticipate generic drug launch
Find generic entry opportunities
Flat-rate pricing for predictable budgeting
Short-term plans for project- or client-based billing
Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Title:||Hypocalcaemic peptides and process for their manufacture|
|Abstract:||Human calcitonin in the form of four components and process for their isolation from C-cells material.|
|Inventor(s):||Neher; Robert (Binningen, CH), Riniker; Bernhard (Frenkendorf, CH)|
|Assignee:||Ciba-Geigy Corp. (Ardsley, NY)|
1. The .Iadd.substantially pure .Iaddend.dotriacontapeptide amide of the formula ##STR3## its acid addition salts and complexes.
2. A pharmaceutical preparation suitable for treatment of hypercalcaemea, Paget's disease and osteoporosis comprising an effective amount of the dotriacontapeptide amide of the formula ##STR4## .Iadd.
3. The dotriacontapeptide amide of the formula Cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Gln-Asp-Phe-Asn-Lys-Phe-Hi s-Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-Val-Gly-Ala-Pro-NH.sub.2 which is substantially free of biological impurities. .Iaddend. .Iadd.4. The dotriacontapeptide amide of the formula Cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Gln-Asp-Phe-Asn-Lys-Phe-Hi s-Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-Val-Gly-Ala-Pro-NH.sub.2 which has a distribution coefficient of about 0.6 in a Craig liquid - liquid distribution system of glacial acetic acid, water and n-butanol having a volume to volume ratio of 4:1:5. .Iaddend. .Iadd.5. The dotriacontapeptide amide of the formula Cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Gln-Asp-Phe-Asn-Lys-Phe-Hi s-Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-Val-Gly-Ala-Pro-NH.sub.2 which is capable of producing a biological test activity of at least about 100 MRC units per mg in the rat calcium blood level test as described by Kumar. .Iaddend. .Iadd.6. The dotriacontrapeptide amide of the formula Cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Gln-Asp-Phe-Asn-Lys-Phe-Hi s-Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-Val-Gly-Ala-Pro-NH.sub.2 which is unitary as determined by thin layer chromatography and electrophoresis. .Iaddend. .Iadd.7. The dotriacontapeptide amide according to claim 6 wherein the thin layer chromatography is on a solid support of aluminum oxide using an eluting system of n-butanol, glacial acetic acid and water and the electrophoresis is on cellulose using an eluting system of glacial acetic
acid, formic acid and water. .Iaddend. .Iadd.8. The dotriacontapeptide amide according to claim 7 wherein the reference standard for chromatographic and electrophoretic measurement of the dotriacontapeptide amide movement is porcine calcitonin. .Iaddend. .Iadd.9. A pharmaceutical preparation suitable for treatment of hypercalcaemia, Paget's disease and osteoporosis comprising an effective amount of the dotriacontapeptide amide of the formula ##STR5## .Iaddend. or its pharmaceutically acceptable acid addition salt or its formulated, activity prolonging complex in a pharmaceutical excipient
suitable for enteral or parenteral administration. .Iadd.10. A pharmaceutical preparation according to claim 9 wherein the dotriacontapeptide amide is substantially pure. .Iaddend. .Iadd.11. A pharmaceutical preparation according to claim 9 wherein the pharmaceutical carrier is mannitol. .Iaddend. .Iadd.12. A pharmaceutically acceptable acid addition salt or a pharmaceutically acceptable formulated, activity prolonging complex of the dotriacontapeptide amide of the formula Cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Gln-Asp-Phe-Asn-Lys-Phe-Hi s-Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-Val-Gly-Ala-Pro-NH.sub.2. .Iaddend. .Iadd.13. A pharmaceutically acceptable salt or complex according to claim 12 wherein the dotriacontapeptide amide is substantially pure. .Iaddend. .Iadd.14. A pharmaceutically acceptable acid addition salt according to
claim 12. .Iaddend. .Iadd.15. A salt according to claim 14 wherein the acid is hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, phosphoric acid, acetic acid, propionic acid, stearic acid, glycollic acid, lactic acid, pyruvic acid, oxalic acid, citric acid, benzoic acid, cinnamic acid, salicylic acid, 2-phenoxybenzoic acid, 2-acetoxybenzoic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, hydroxyethanesulfonic acid, benzenesulfonic acid, toluenesulfonic acid, trichloroacetic acid or trifluoroacetic acid. .Iaddend. .Iadd.16. A salt according to claim 14 wherein the acid is acetic acid. .Iaddend. .Iadd.17. A pharmaceutically acceptable, formulated activity-prolonging complex according to claim 12. .Iaddend. .Iadd.18. A complex according to claim 17 wherein the complexing substance is nonantigenic gelatin, oxypolygelatin, polyvinyl-pyrrolidone, polyphloretinephosphate phytic acid, protamine, polyglutamic acid, or an inorganic metal compound having a cation selected from aluminum, magnesium, cobalt or zinc and an anion selected from phosphate, pyrophosphate or hydroxide. .Iaddend.
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 verifification 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.