IPC분류정보
국가/구분 |
United States(US) Patent
등록
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국제특허분류(IPC7판) |
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출원번호 |
US-0651777
(2000-08-30)
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발명자
/ 주소 |
- Dudley, Robert E.
- Kottayil, S. George
- Palatchi, Olivier
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출원인 / 주소 |
- Unimed Pharmaceuticals, Inc., Laboratories Besins Iscovesco
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대리인 / 주소 |
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인용정보 |
피인용 횟수 :
70 인용 특허 :
76 |
초록
A pharmaceutical composition useful for treating hypogonadism is disclosed. The composition comprises an androgenic or anabolic steroid, a C1-C4 alcohol, a penetration enhancer such as isopropyl myristate, and water. Also disclosed is a method for treating hypogonadism utilizing the composition.
대표청구항
▼
A pharmaceutical composition useful for treating hypogonadism is disclosed. The composition comprises an androgenic or anabolic steroid, a C1-C4 alcohol, a penetration enhancer such as isopropyl myristate, and water. Also disclosed is a method for treating hypogonadism utilizing the composition. he
A pharmaceutical composition useful for treating hypogonadism is disclosed. The composition comprises an androgenic or anabolic steroid, a C1-C4 alcohol, a penetration enhancer such as isopropyl myristate, and water. Also disclosed is a method for treating hypogonadism utilizing the composition. he proviso that R1and R2cannot both be an alkenyl group, or taken together with the carbon to which they are bonded, form a C3-C8cyclocarbon ring; R3is lower alkyl, lower alkenyl, lower fluoroalkyl, lower fluoroalkenyl, O-lower alkyl, O-lower alkenyl, O-lower acyl, O-aromatic acyl or lower cycloalkyl; X1is hydrogen or hydroxyl, or, taken with R3,constitutes a bond when R3is an alkenyl group, and X2is hydrogen or hydroxyl, or, taken with R1or R2,constitutes a double bond. 6. A method of inhibiting the hyperproliferative activity of malignant or neoplastic cells, comprising administering to a patient suffering therefrom, an anitproliferarive amount of a hypocalcemic hydroxyvitamin D compound. 7. A method in accordance with claim 6, wherein the hypocalcemic vitamin D compound is administered in a daily regimen or an episodic regimen. 8. A method in accordance with claim 7, wherein the episodic regimen is a dose once every 2 to 7 days. 9. A method in accordance with claim 7, wherein the hypocalcemic vitamin D compound is administered daily at a dose of about 10 to 100 μg/day. 10. A method in accordance with claim 6, wherein the hypocalcemic vitamin D compound is administered orally, is administered intravenously, is directly injected to a cancer site or is regionally delivered to a cancer site. 11. A method in accordance with claim 10, wherein the hypocalcemic vitamin D compound is administered orally. 12. A method in accordance with claim 6, wherein the hypocalcemic vitamin D compound is co-administered with a cytotoxic agent. 13. A method in accordance with claim 12, wherein the cytotoxic agent is an antimetabolite, and antimicrotubule agent, an alkyating agent, a platinum agent, an anthracycline, a topoisomase inhibitor, or an antibiotic. 14. A method in accordance with claim 13, wherein the antimetabolite is 5-fluoro-uracil, methotrexate or fludarabine. 15. A method in accordance with claim 13, wherein the antimicrotubule agent is vincristine, vinblastine or a taxane. 16. A method in accordance with claim 14, wherein the taxane is paclitaxel or docetaxel. 17. A method in accordance with claim 12, wherein the alkylating agent is cyclophasphamide, melphalan, biochoroethylnitrosurea or hydroxyurea. 18. A method in accordance with claim 12, wherein the platinum agent is cisplatin, carboplatin, oxaliplatin, JM-216 or CI-973. 19. A method in accordance with claim 12, wherein the anthracycline is doxrubicin or daunorubicin. 20. A method in accordance with claim 12, wherein the antibiotic is mitomycin, idarubicin, adriamycin or daunomycin. 21. A method in accordance with claim 12, wherein the topoisomerase inhibitior is etoposide or camptothecins. 22. A method in accordance with claim 12, wherein the cytotoxic agent is estramustine phosphate or prednimustine. 23. A method in accordance with claim 11, wherein an antiproliferative effective amount of the cytotoxic agent is lower than the antiproliferative effective amount of the cytotoxic agent when administered alone. 24. The method of claim 5, wherein the compound of formula (III) is 1α,24-dihydroxyvitamin D2,1α,24-dihydroxyvitamin D4,1α,25-dihydroxyvitamin D2,1α,25-dihydroxyvitamin D4,1α-hydroxyvitamin D2or 1α-hydroxyvitamin D4. 25. A method of treating a human to alleviate the pathological effects of breast cancer, colon cancer, testicular cancer, pancreatic cancer, endometrial cancer, small cell and non-small cell cancer of the lung (including squamous, adneocarcinoma and large cell types), squamous cell of the head and neck, bladder, ovarian and cervical cancers, myeloid and lymphocyltic leukemia, lymphoma, hepatic tumors, medullary thyroid carcinoma, multiple myeloma, melanoma, retinoblastoma or sarcomas of the soft tissue and bone, comprising administering to the human an therapeutic amou nt of a hypocalcemic hydroxyvitamin D compound. 26. A method of claim 25, wherein said hypocalcemic vitamin D is a 1α-hydroxyvitamin D compound represented by formula (III) wherein A1and A2each are hydrogen or a carbon-carbon bond, thus forming a double bond between C-22 and C-23; R1and R2are identical or different and are hydrogen, hydroxyl, lower alkyl, lower fluoroalkyl, O-lower alkyl, lower alkenyl, lower fluoroalkenyl, O-lower alkenyl, O-lower acyl, O-aromatic acyl, lower cycloalkyl with the proviso that R1and R2cannot both be an alkenyl group, or taken together with the carbon to which they are bonded, form a C3-C8cyclocarbon ring; R3is lower alkyl, lower alkenyl, lower fluoroalkyl, lower fluoroalkenyl, O-lower alkyl, O-lower alkenyl, O-lower acyl, O-aromatic acyl or lower cycloalkyl; X1is hydrogen or hydroxyl, or, taken with R3,constitutes a bond when R3is an alkenyl group, and X2is hydrogen or hydroxyl, or, taken with R1or R2,costitutes a double bond. 27. The method of claim 26, wherein said therapeutic amount is 0.01 μg/kg/day to 2.0 μg/kg/day. 28. The method of claim 26, wherein the compound of formula (III) is 1α,24-dihydroxyvitamin D2,1α,24-dihydroxyvitamin D4,1α,25-dihydroxyvitamin D2,1α,25-dihydroxyvitamin D4,1α-hydroxyvitamin D2or 1α-hydroxyvitamin D4. 29. A method of enhancing the antiproliferative effect of a cytotoxic agent in a patient with a disease in need of treatment by a cytotoxic agent, comprising administering to the patient a therapeutic amount of hypocalcemic vitamin D compound and the cytotoxic agent. 30. A method in accordance with claim 29, wherein the hypocalcemic vitamin D compound is administered from 0.5 to 7 days prior to administration of the cytotoxic agent. 31. A method in accordance with claim 29, wherein the hypocalcemic vitamin D compound is administered 2 to 4 days prior to administration of the cytotoxic agent. 32. A method of claim 29, wherein said hypocalcemic vitamin D is a 1α-hydroxyvitamin D compound represented by formula (III) wherein A1and A2each are hydrogen or a carbon-carbon bond, thus forming a double bond between C-22 and C-23; R1and R2are identical or different and are hydrogen, hydroxyl, lower alkyl, lower fluoroalkyl, O-lower alkyl, lower alkenyl, lower fluoroalkenyl, O-lower alkenyl, O-lower acyl, O-aromatic acyl, lower cycloalkyl with the proviso that R1and R2cannot both be an alkenyl group, or taken together with the carbon to which they are bonded, form a C3-C8cyclocarbon ring; R3is lower alkyl, lower alkenyl, lower fluoroalkyl, lower fluoroalkenyl, O-lower alkyl, O-lower alkenyl, O-lower acyl, O-aromatic acyl or lower cycloalkyl; X1is hydrogen or hydroxyl, or, taken with R3,constitutes a bond when R3is an alkenyl group, and X2is hydrogen or hydroxyl, or, taken with R1or R2,constitutes a double bond. 33. The method of claim 32, wherein said therapeutic amount of the vitamin D compound is 0.01 μg/kg/day to 2.0 μg/kg/day. 34. The method of claim 32, wherein the compound of formula (III) is 1α,24-dihydroxyvitamin D2,1α,24-dihydroxyvitamin D4,1α25-dihydroxyvitamin D2,1α,25-dihydroxyvitamin D4,1α-hydroxyvitamin D2or 1α-hydroxyvitamin D4. 35. A method in accordance with claim 32, wherein the cytotoxic agent is an antimetabolite, and antimicrotubule agent, an alkyating agent, a platinum agent, an anthracycline, a topoisomase inhibitor, or an antibiotic. 36. A method of inducing differentiation in malignant or neoplastic cells, comprising treating to the cells with a prodifferentiative amount of a
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