Method of treating metabolic bone diseases with 18-nor-vitamin D compounds
First Claim
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1. A method of treating metabolic bone disease where it is desired to maintain or increase bone mass comprising administering to a patient with said disease a compound having the formula:
- ##STR9## where X1 and X2, which may be the same or different, are each selected from hydrogen and a hydroxy protecting group, and where the group R is represented by the structure;
##STR10## where the stereochemical center at carbon 20 may have the R or S configuration, and where Z is selected from Y, --OY, --CH2 OY, --C.tbd.CY and --CH═
CHY, where the double bond may have the cis or trans geometry, and where Y is selected from hydrogen, methyl, --CR5 O and a radical of the structure;
##STR11## where m and n, independently, represent the integers from 0 to 5, where R1 is selected from hydrogen, deuterium, hydroxy, protected hydroxy, fluoro, trifluoromethyl, and C1-5 -alkyl, which may be straight chain or branched and, optionally bear a hydroxy or protected-hydroxy substituent, and where each of R2, R3, and R4, independently, is selected from deuterium, deuteroalkyl, hydrogen, fluoro, trifluoromethyl and C1-5 alkyl, which may be straight-chain or branched, and optionally, bear a hydroxy or protected-hydroxy substituent, and where R1 and R2, taken together, represent an oxo group, or an alkylidene group, ═
CR2 R3, or the group --(CH2)p, where p is an integer from 2 to 5, and where R3 and R4, taken together, represent an oxo group, or the group --(CH2)q --, where q is an integer from 2 to 5, and where R5 represents hydrogen, hydroxy, protected hydroxy, or C1-5 alkyl.
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Abstract
18-nor-vitamin D3 analogs in which the angular methyl group attached to carbon 13 of the CD-ring has been removed and replaced by a hydrogen atom. The 18-nor vitamin D compounds are characterized by relatively high cell differentiation activity, while exhibiting much lower activity than 1α,25-dihydroxyvitamin D3 in their ability to mobilize calcium from bone. These compounds would be useful for the treatment of diseases where bone formation is desired, such as osteoporosis, because of their preferential calcemic activity, and for the treatment of psoriasis due to their cell differentiation activity.
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8 Claims
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1. A method of treating metabolic bone disease where it is desired to maintain or increase bone mass comprising administering to a patient with said disease a compound having the formula:
- ##STR9## where X1 and X2, which may be the same or different, are each selected from hydrogen and a hydroxy protecting group, and where the group R is represented by the structure;
##STR10## where the stereochemical center at carbon 20 may have the R or S configuration, and where Z is selected from Y, --OY, --CH2 OY, --C.tbd.CY and --CH═
CHY, where the double bond may have the cis or trans geometry, and where Y is selected from hydrogen, methyl, --CR5 O and a radical of the structure;
##STR11## where m and n, independently, represent the integers from 0 to 5, where R1 is selected from hydrogen, deuterium, hydroxy, protected hydroxy, fluoro, trifluoromethyl, and C1-5 -alkyl, which may be straight chain or branched and, optionally bear a hydroxy or protected-hydroxy substituent, and where each of R2, R3, and R4, independently, is selected from deuterium, deuteroalkyl, hydrogen, fluoro, trifluoromethyl and C1-5 alkyl, which may be straight-chain or branched, and optionally, bear a hydroxy or protected-hydroxy substituent, and where R1 and R2, taken together, represent an oxo group, or an alkylidene group, ═
CR2 R3, or the group --(CH2)p, where p is an integer from 2 to 5, and where R3 and R4, taken together, represent an oxo group, or the group --(CH2)q --, where q is an integer from 2 to 5, and where R5 represents hydrogen, hydroxy, protected hydroxy, or C1-5 alkyl. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
- ##STR9## where X1 and X2, which may be the same or different, are each selected from hydrogen and a hydroxy protecting group, and where the group R is represented by the structure;
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Current AssigneeWisconsin Alumni Research Foundation (University of Wisconsin System)
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Original AssigneeWisconsin Alumni Research Foundation (University of Wisconsin System)
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InventorsSicinski, Rafal R., Deluca, Hector F., Perlman, Kato L.
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Primary Examiner(s)PRIOR, KIMBERLY
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Application NumberUS08/810,887Time in Patent Office356 DaysField of Search514/167US Class Current514/167CPC Class CodesA61P 17/00 Drugs for dermatological di...A61P 19/10 for osteoporosisA61P 3/02 Nutrients, e.g. vitamins, m...A61P 35/00 Antineoplastic agentsA61P 43/00 Drugs for specific purposes...C07C 401/00 Irradiation products of cho...C07F 7/1804 Compounds having Si-O-C lin...
