JP4362442B2 - 女性における萎縮の抑制方法または萎縮関連症状の治療または予防方法 - Google Patents
女性における萎縮の抑制方法または萎縮関連症状の治療または予防方法 Download PDFInfo
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- JP4362442B2 JP4362442B2 JP2004510768A JP2004510768A JP4362442B2 JP 4362442 B2 JP4362442 B2 JP 4362442B2 JP 2004510768 A JP2004510768 A JP 2004510768A JP 2004510768 A JP2004510768 A JP 2004510768A JP 4362442 B2 JP4362442 B2 JP 4362442B2
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- toremifene
- tore
- atrophy
- urinary
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- LUMKNAVTFCDUIE-VHXPQNKSSA-N OCCOc(cc1)ccc1/C(/c1ccccc1)=C(/CCCl)\c1ccccc1 Chemical compound OCCOc(cc1)ccc1/C(/c1ccccc1)=C(/CCCl)\c1ccccc1 LUMKNAVTFCDUIE-VHXPQNKSSA-N 0.000 description 2
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/075—Ethers or acetals
- A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Gynecology & Obstetrics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Orthopedics, Nursing, And Contraception (AREA)
- Medicinal Preparation (AREA)
Description
以下の表1は、種々の用量のオスペミフェンまたはラロキシフェンの3ヵ月の投与後、傍基底細胞(MI1)に対する成熟指数および表在細胞(MI3)に対する成熟指数の変化を示す。
オスペミフェンは、子宮内膜組織学に弱いエストロゲン性作用を有した。この作用は、明らかにエストロゲン代替治療により見られるものより弱い。子宮内膜には悪性所見はみられなかった。超音波検査法により評価された子宮内膜の厚さは、用量レベル30、60および90mgでそれぞれ統計学的に有意でない軽微な厚さの増加(平均0.2mm、0.5mmおよび0.5mm)を示した。測定した値は、タモキシフェンなどのSERMsの生理的に有意なエストロゲン性を示す厚さとみなされている8mmより常に小さかった(Hann et al., 1997; Lahti et al, 1993)。
臨床フェーズIおよびII試験では、241人の閉経後の女性をオスペミフェンで治療した。77人を、オスペミフェンの日用量25〜30mgで、78人を50〜60mgで、78人を90〜100mgで、そして8人を200mgで治療した。対照群では、47人をプラシーボで、29人をラロキシフェンで処置した。被験者の何人かは、尿生殖器の萎縮に関連する症状の自発的な軽減を報告した。その症状には、過敏、かゆみ、やけどのような痛み、うずき、***後の出血、外陰のかゆみ、および/または悪臭のあるおりものによる膣の不快感および白帯下などの膣の症状と泌尿器の症状との両方が含まれる。個々のケースにおいて軽減される泌尿器の症状には、尿失禁、再発性***症、放尿障害、頻尿、夜間多尿症、尿意促迫感、切迫尿失禁および不随意尿漏れが含まれる。また、臨床医は、膣の蒼白、点状出血、破砕性(friability)、膣粘膜萎縮および潰瘍形成などの尿生殖器の萎縮の徴候がオスペミフェンによって軽減された症例を報告した。
Delmas PD, Bjarnason NH, Mitlak BH, Ravoux AC, Shah AS, Huster WJ, Draper M, Christiansen C: Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women. N Engl J Med 337: 1641-1647, 1997.
Ettinger B, Genant HK, Cann CE: Long-term estrogen replacement therapy prevents bone loss and fractures. Ann Intern Med 102: 319-324, 1985.
Hann LE, Giess CS, Bach AM, Tao Y, Baum HJ, Barakat RR: Endometrial thickness in tamoxifen-treated patients: correlation with clinical and pathologic findings. Am J Roentgenol 168: 657-661, 1997.
Gustafsson J-Å: Estrogen receptor β-getting in on the action? Nature Medicine 3: 493-494, 1997.
Kangas L: Biochemical and pharmacological effects of toremifene metabolites. Cancer Chemother Pharmacol 27: 8-12, 1990.
Kauffman RF, Bryant HU: Selective estrogen receptor modulators. Drug News Perspect 8: 531-539, 1995.
Lahti E, Blanco G, Kauppila A, Apaja-Sarkkinen M, Taskinen PJ, Laatikainen T: Endometrial changes in postmenopausal breast cancer patients receiving tamoxifen. Obstet Gynecol 81: 660-664, 1993.
Palkowitz AD, Glasebrook AL, Thraser KJ, Hauser KL, Short LL, Phillips DL, Muchi BS, Sato M, Shetler PK, Cullinan GJ, Pell TR, Bryant HU: Discovery and synthesis of [6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-2-(4-hydroxyphenyl)]benzo[b]thiophene: a novel, highly potent, selective estrogen receptor modulator. Med Chem 40: 1407-1416, 1997.
Payer L: The menopause in various cultures. In: A portrait of the menopause. Expert reports on medical and therapeutic strategies for the 1990s. Ed. Burger H & Boulet M, Parthenon Publishing, Park Ridge, NJ, USA, 1991. pp3-22.
Rekers H: Matering the menopause. In: A portrait of the menopause. Expert reports on medical and therapeutic strategies for the 1990s. Ed. Burger H & Boulet M, Parthenon Publishing, Park Ridge, NJ, USA, 1991. pp23-43.
Schneider LS, Finch CE: Can estrogens prevent neurodegeneration. Drugs & Aging 11: 87-95, 1997
Spector IP, Carey MP: Incidence and prevalence of sexual dysfunctions: a critical review of the empirical literature. Archives of Sexual Behaviour 19: 389-408, 1990.
Vuopala S, Kauppila A, Mikkonen M, Stenbaeck F: Screening of asymptomatic postmenopausal women for gynecological malignancies, with special reference to endometrial sampling methods. Arch Gyncol 231: 119-127, 1982.
Wakeling AE, Bowler J: Biology and mode of action of pure antiestrogens. J Steroid Biochem 30: 1-6, 1988.
Wickelgren I: Estrogen stakes claim to cognition. Science 276: 675-678, 1997.
Claims (11)
- 式(I)
- 化合物(I)がオスペミフェンまたはその薬学的に許容し得る塩である請求項1記載の薬剤。
- 化合物(I)がオスペミフェンである請求項1記載の薬剤。
- 式(I)
- 化合物(I)がオスペミフェンまたはその薬学的に許容し得る塩である請求項4記載の薬剤。
- 化合物(I)がオスペミフェンである請求項4記載の薬剤。
- 化合物が経口で投与される請求項1〜6のいずれかに記載の薬剤。
- 化合物が局所で投与される請求項1〜6のいずれかに記載の薬剤。
- 化合物が経皮で投与される請求項1〜6のいずれかに記載の薬剤。
- 化合物が30〜90mgの範囲の日用量で投与される請求項1〜7のいずれかに記載の薬剤。
- 化合物が60mgの日用量で投与される請求項1〜7のいずれかに記載の薬剤。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US38590402P | 2002-06-06 | 2002-06-06 | |
PCT/FI2003/000369 WO2003103649A1 (en) | 2002-06-06 | 2003-05-14 | Method for the inhibition of atrophy or for treatment or prevention of atrophy-related symptoms in women |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2005532353A JP2005532353A (ja) | 2005-10-27 |
JP4362442B2 true JP4362442B2 (ja) | 2009-11-11 |
Family
ID=29736123
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004510768A Expired - Lifetime JP4362442B2 (ja) | 2002-06-06 | 2003-05-14 | 女性における萎縮の抑制方法または萎縮関連症状の治療または予防方法 |
Country Status (24)
Country | Link |
---|---|
EP (1) | EP1509215B1 (ja) |
JP (1) | JP4362442B2 (ja) |
KR (1) | KR100991157B1 (ja) |
CN (2) | CN101406464A (ja) |
AT (1) | ATE344025T1 (ja) |
AU (1) | AU2003227790B2 (ja) |
BR (1) | BR0311613A (ja) |
CA (1) | CA2484542C (ja) |
CY (1) | CY1105787T1 (ja) |
DE (1) | DE60309465T2 (ja) |
DK (1) | DK1509215T3 (ja) |
ES (1) | ES2270025T3 (ja) |
HR (1) | HRP20041150B1 (ja) |
IL (1) | IL164528A (ja) |
MX (1) | MXPA04012220A (ja) |
NO (3) | NO334090B1 (ja) |
NZ (1) | NZ536118A (ja) |
PL (1) | PL214242B1 (ja) |
PT (1) | PT1509215E (ja) |
RU (1) | RU2317816C2 (ja) |
SI (1) | SI1509215T1 (ja) |
UA (1) | UA79797C2 (ja) |
WO (1) | WO2003103649A1 (ja) |
ZA (1) | ZA200408321B (ja) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8236861B2 (en) | 2004-02-13 | 2012-08-07 | Hormos Medical Corporation | Method for enhancing the bioavailablity of ospemifene |
US8642079B2 (en) | 2004-02-23 | 2014-02-04 | Hormos Medical Corporation | Solid formulations of ospemifene |
US8758821B2 (en) | 2004-05-04 | 2014-06-24 | Hormos Medical Ltd. | Oral formulations of ospemifene |
SI1742618T1 (sl) | 2004-05-04 | 2012-12-31 | Hormos Medical Ltd. | Tekoäśe oralne formulacije ospemifena |
CA2654152A1 (en) | 2006-06-02 | 2007-12-13 | Pear Tree Women's Health Care | Method of treating atrophic vaginitis |
EP2821385B1 (en) | 2007-02-14 | 2016-07-27 | Hormos Medical Ltd. | Method for the preparation of therapeutically valuable triphenylbutene derivatives |
US7504530B2 (en) | 2007-02-14 | 2009-03-17 | Hormos Medical Ltd. | Methods for the preparation of fispemifene from ospemifene |
EP2909164A1 (en) | 2012-10-19 | 2015-08-26 | Fermion Oy | A process for the preparation of ospemifene |
KR102052133B1 (ko) | 2017-08-10 | 2019-12-05 | 고려대학교 산학협력단 | 당 부가된 오스페미펜, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물 |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5352699A (en) * | 1992-04-30 | 1994-10-04 | University Of Massachusetts Medical Center | Use of retinioc acid to treat vaginal atrophy |
US5461064A (en) * | 1993-12-21 | 1995-10-24 | Eli Lilly And Company | Methods of inhibiting atrophy of the skin and vagina |
US5747059A (en) * | 1996-01-11 | 1998-05-05 | Novo Nordisk A/S | Atrophy of skin/mucous membrane |
IL149990A0 (en) * | 2000-01-28 | 2002-12-01 | Endorech Inc | Selective estrogen receptor modulators in combination with estrogens |
US20010034340A1 (en) * | 2000-03-20 | 2001-10-25 | American Home Products Corporation | Hormone replacement therapy |
US6245819B1 (en) * | 2000-07-21 | 2001-06-12 | Hormos Medical Oy, Ltd. | Method for the treatment of vaginal dryness and sexual dysfunction in women during or after the menopause |
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2003
- 2003-05-14 CA CA2484542A patent/CA2484542C/en not_active Expired - Lifetime
- 2003-05-14 RU RU2004138571/14A patent/RU2317816C2/ru active
- 2003-05-14 MX MXPA04012220A patent/MXPA04012220A/es active IP Right Grant
- 2003-05-14 NZ NZ536118A patent/NZ536118A/en not_active IP Right Cessation
- 2003-05-14 ES ES03725238T patent/ES2270025T3/es not_active Expired - Lifetime
- 2003-05-14 AU AU2003227790A patent/AU2003227790B2/en not_active Expired
- 2003-05-14 CN CNA2008101733358A patent/CN101406464A/zh active Pending
- 2003-05-14 CN CNB038128780A patent/CN100448437C/zh not_active Expired - Lifetime
- 2003-05-14 DK DK03725238T patent/DK1509215T3/da active
- 2003-05-14 PL PL372758A patent/PL214242B1/pl unknown
- 2003-05-14 EP EP03725238A patent/EP1509215B1/en not_active Expired - Lifetime
- 2003-05-14 KR KR1020047019843A patent/KR100991157B1/ko active IP Right Grant
- 2003-05-14 WO PCT/FI2003/000369 patent/WO2003103649A1/en active IP Right Grant
- 2003-05-14 UA UAA200500144A patent/UA79797C2/uk unknown
- 2003-05-14 DE DE60309465T patent/DE60309465T2/de not_active Expired - Lifetime
- 2003-05-14 PT PT03725238T patent/PT1509215E/pt unknown
- 2003-05-14 SI SI200330601T patent/SI1509215T1/sl unknown
- 2003-05-14 JP JP2004510768A patent/JP4362442B2/ja not_active Expired - Lifetime
- 2003-05-14 BR BR0311613-1A patent/BR0311613A/pt not_active Application Discontinuation
- 2003-05-14 AT AT03725238T patent/ATE344025T1/de active
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2004
- 2004-10-12 IL IL164528A patent/IL164528A/en active IP Right Grant
- 2004-10-14 ZA ZA200408321A patent/ZA200408321B/en unknown
- 2004-10-22 NO NO20044568A patent/NO334090B1/no not_active IP Right Cessation
- 2004-12-02 HR HR20041150A patent/HRP20041150B1/xx not_active IP Right Cessation
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2006
- 2006-11-15 CY CY20061101664T patent/CY1105787T1/el unknown
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2013
- 2013-09-04 NO NO20131189A patent/NO336612B1/no not_active IP Right Cessation
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2015
- 2015-04-22 NO NO20150487A patent/NO339194B1/no not_active IP Right Cessation
Also Published As
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JP5629746B2 (ja) | 閉経期または閉経後の女性における更年期障害の治療方法 | |
NO339194B1 (no) | Anvendelse av en forbindelse for fremstilling av en farmasøytisk sammensetning for hemming av urinveisinfeksjon hos en kvinne | |
AU2001258449A1 (en) | Method for the treatment of climacteric disorders in women during or after the menopause |
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