Claims for Patent: 6,121,312
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Summary for Patent: 6,121,312
Title: | Cyclic ether vitamin D3 compounds and uses thereof |
Abstract: | Novel cyclic ether vitamin D3 compounds having a cyclic ether side chain are disclosed. These compounds were first identified as metabolites of 3-epi vitamin D3 produced via a tissue-specific metabolic pathway which catalyzes the formation of a cyclic ether structure. Also disclosed are 1.alpha.(OH) 3-epi vitamin D3 compounds, which are produced via the epimerization of a 3-.beta.-hydroxyl group of 1.alpha.(OH) vitamin D3 precursor in vivo. The vitamin D3 compounds of the present invention can be used as substitutes for natural and synthetic vitamin D3 compounds. |
Inventor(s): | Reddy; Satayanarayana G. (Barrington, RI) |
Assignee: | Woman and Infants Hospital (Providence, RI) |
Application Number: | 09/410,223 |
Patent Claims: | 1. An isolated cyclic ether vitamin D3 compound having the formula (I) as follows: ##STR8## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1,
R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group.
2. A method of treating a disorder characterized by an aberrant activity of a vitamin D.sub.3 -responsive cell, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D.sub.3 compound having the formula I as follows: ##STR9## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group, such that the aberrant activity of the vitamin D.sub.3 -responsive cell is reduced. 3. The method of claim 2, wherein the subject is a mammal. 4. The method of claim 3, wherein the mammal is a human. 5. The method of claim 2, wherein the disorder comprises an aberrant activity of an endocrine cell. 6. The method of claim 5, wherein the endocrine cell is a parathryoid cell and the aberrant activity is processing and/or secretion of parathyroid hormone. 7. A method of treating a disorder characterized by an aberrant activity of a hyperproliferative skin cell, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR10## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group, such that the aberrant activity of the hyperproliferative skin cell is reduced. 8. A method of treating secondary hyperparathyroidism, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR11## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 9. A method of treating a disorder characterized by an aberrant activity of a bone cell, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR12## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group, such that the aberrant activity of the bone cell is reduced. 10. A method of treating osteoporosis, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR13## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 11. A method of treating osteodystrophy, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR14## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 12. A method of treating senile osteoporosis, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR15## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 13. A method of treating osteomalacia, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR16## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 14. A method of treating rickets, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR17## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 15. A method of treating osteitis fibrosa cystica, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR18## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 16. A method of treating renal osteodystrophy, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR19## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 17. A method of treating cirrhosis, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR20## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 18. A method of treating chronic renal disease, comprising administering to a subject an effective amount of an isolated cyclic ether vitamin D3 compound having formula I as follows: ##STR21## wherein A.sub.1, A.sub.2 and A.sub.3 are a single or a double bond; X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of a hydrogen, a halogen, a haloalkyl, a hydroxy, a hydroxy-protecting group, an alkyl, an alkenyl, an alkynyl, an alkoxy, an aryl group and a heterocyclic group. 19. A pharmaceutical composition comprising a therapeutically effective amount of a cyclic ether vitamin D.sub.3 compound of claim 1 and a pharmaceutically acceptable carrier. 20. The composition of claim 19, which is suitable for topical or oral administration. |
Details for Patent 6,121,312
Applicant | Tradename | Biologic Ingredient | Dosage Form | BLA | Approval Date | Patent No. | Expiredate |
---|---|---|---|---|---|---|---|
Nps Pharmaceuticals, Inc. | NATPARA | parathyroid hormone | For Injection | 125511 | 01/23/2015 | ⤷ Try a Trial | 2017-05-16 |
>Applicant | >Tradename | >Biologic Ingredient | >Dosage Form | >BLA | >Approval Date | >Patent No. | >Expiredate |
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