(20R)-2a-Methyl-19,26,27-Trinor-Vitamin D Analogs
First Claim
Patent Images
1. A compound having the formula:
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where X1, X2 and X3, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group.
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Abstract
This invention discloses (20R)-2α-methyl-19,26,27-trinor-vitamin D analogs, and specifically (20R)-2α-methyl-19,26,27-trinor-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows very low activity in vivo on bone calcium mobilization and intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
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Citations
79 Claims
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1. A compound having the formula:
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where X1, X2 and X3, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group. - View Dependent Claims (2, 3, 4, 5, 6, 7)
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8. (20R)-2α
- -methyl-19,26,27-trinor-1α
,25-dihydroxyvitamin D3 having the formula;
- -methyl-19,26,27-trinor-1α
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9. A pharmaceutical composition containing an effective amount of (20R)-2α
- -methyl-19,26,27-trinor-1α
,25-dihydroxyvitamin D3 together with a pharmaceutically acceptable excipient. - View Dependent Claims (10, 11)
- -methyl-19,26,27-trinor-1α
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12. A method of treating psoriasis comprising administering to a subject with psoriasis an effective amount of a compound having the formula:
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where X1, X2 and X3 which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group. - View Dependent Claims (13, 14, 15, 16, 17, 18, 19, 20, 21)
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22. A method of treating a disease selected from the group consisting of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer comprising administering to a subject with said disease an effective amount of a compound having the formula:
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where X1, X2 and X3 which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group. - View Dependent Claims (23, 24, 25, 26, 27, 28, 29, 30)
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31. A method of treating an autoimmune disease selected from the group consisting of multiple sclerosis, lupus, diabetes mellitus, host versus graft rejection, and rejection of organ transplants, comprising administering to a subject with said disease an effective amount of a compound having the formula:
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where X1, X2 and X3 which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group. - View Dependent Claims (32, 33, 34, 35, 36, 37, 38, 39)
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40. A method of treating an inflammatory disease selected from the group consisting of rheumatoid arthritis, asthma, and inflammatory bowel diseases, comprising administering to a subject with said disease an effective amount of a compound having the formula:
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where X1, X2 and X3, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group. - View Dependent Claims (41, 42, 43, 44, 45, 46, 47, 48)
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49. A method of treating a skin condition selected from the group consisting of wrinkles, lack of adequate skin firmness, lack of adequate dermal hydration and insufficient sebum secretion which comprises administering to a subject with said skin condition an effective amount of a compound having the formula:
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where X1, X2 and X3 which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group. - View Dependent Claims (50, 51, 52, 53, 54, 55, 56, 57, 58)
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59. A method of treating renal osteodystrophy comprising administering to a subject with renal osteodystrophy an effective amount of a compound having the formula:
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where X1, X2 and X3, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group. - View Dependent Claims (60, 61, 62, 63, 64, 65, 66, 67)
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68. A method of treating or preventing obesity of an animal, inhibiting adipocyte differentiation, inhibiting SCD-1 gene transcription, and/or reducing body fat in an animal comprising administering to an animal in need thereof an effective amount of a compound having the formula:
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where X1, X2 and X3, which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group. - View Dependent Claims (69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79)
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77. The method of claim 68 wherein the animal is a human.
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78. The method of claim 68 wherein the animal is a domestic animal.
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79. The method of claim 68 wherein the animal is an agricultural animal.
Specification
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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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InventorsPlum, Lori A., DeLuca, Hector F., Clagett-Dame, Margaret, Grzywacz, Pawel
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Granted Patent
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Time in Patent OfficeDays
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Field of Search
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US Class Current514/167
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CPC Class CodesA61P 17/00 Drugs for dermatological di...A61P 3/10 for hyperglycaemia, e.g. an...A61P 35/00 Antineoplastic agentsA61P 37/00 Drugs for immunological or ...C07C 401/00 Irradiation products of cho...
