JP2008530110A5 - - Google Patents
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- JP2008530110A5 JP2008530110A5 JP2007555236A JP2007555236A JP2008530110A5 JP 2008530110 A5 JP2008530110 A5 JP 2008530110A5 JP 2007555236 A JP2007555236 A JP 2007555236A JP 2007555236 A JP2007555236 A JP 2007555236A JP 2008530110 A5 JP2008530110 A5 JP 2008530110A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutical composition
- lack
- effective amount
- skin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 150000001875 compounds Chemical class 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 208000006673 Asthma Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010012601 Diabetes mellitus Diseases 0.000 claims 2
- 206010021972 Inflammatory bowel disease Diseases 0.000 claims 2
- 206010024324 Leukaemias Diseases 0.000 claims 2
- 206010025135 Lupus erythematosus Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 210000002374 Sebum Anatomy 0.000 claims 2
- 210000003491 Skin Anatomy 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 200000000018 inflammatory disease Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 201000004681 psoriasis Diseases 0.000 claims 2
- 230000028327 secretion Effects 0.000 claims 2
- 230000037393 skin firmness Effects 0.000 claims 2
- 230000037067 skin hydration Effects 0.000 claims 2
- 230000037303 wrinkles Effects 0.000 claims 2
- 210000000481 Breast Anatomy 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 206010031240 Osteodystrophy Diseases 0.000 claims 1
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000000056 organs Anatomy 0.000 claims 1
- 201000006409 renal osteodystrophy Diseases 0.000 claims 1
- -1 t-butyldimethylsilyl groups Chemical group 0.000 claims 1
- XPJAYNDSNNJWDA-AWCUZLSVSA-N C[C@H]([C@@H](CC1)[C@@](C)(CCC2)[C@@H]1/C2=C/C=C(C[C@H](C1=C)O)C[C@H]1O)/C=C/[C@@H](C(C)(C)O)C=[IH] Chemical compound C[C@H]([C@@H](CC1)[C@@](C)(CCC2)[C@@H]1/C2=C/C=C(C[C@H](C1=C)O)C[C@H]1O)/C=C/[C@@H](C(C)(C)O)C=[IH] XPJAYNDSNNJWDA-AWCUZLSVSA-N 0.000 description 2
- 0 C[C@](C(CC1)[C@@](C)(CCC2)[C@@]1C2=CC=C(C[C@@](*)C1=C)C[C@]1*#C)C=C[C@](*)C(C)(C)* Chemical compound C[C@](C(CC1)[C@@](C)(CCC2)[C@@]1C2=CC=C(C[C@@](*)C1=C)C[C@]1*#C)C=C[C@](*)C(C)(C)* 0.000 description 2
Claims (10)
- 下記式Iを有する化合物。
- X1とX2が両方ともヒドロキシ保護基である、請求項１に記載の化合物。
- X1とX2が両方ともt-ブチルジメチルシリル基である、請求項２に記載の化合物。
- X1、X2、及びX3がすべてHであり、かつ該化合物が下記式IAを有する、請求項１に記載の化合物。
- 有効量の請求項４に記載の化合物と、医薬的に許容しうる担体とを含む医薬組成物。
- 前記有効量が、該組成物1g当たり約0.01μg〜約1mgの前記化合物を含む、請求項５に記載の医薬組成物。
- 前記有効量が、該組成物1g当たり約0.1μg〜約500μgの前記化合物を含む、請求項５に記載の医薬組成物。
- 有効量の請求項４に記載の化合物を含む生物学的状態に苦しむ対象を治療するための医薬組成物であって、前記生物学的状態が、乾癬；白血病；大腸癌；乳癌；前立腺癌；多発性硬化症；ループス；糖尿病；宿主対移植片反応；臓器移植の拒絶反応；リウマチ性関節炎、喘息、又は炎症性腸疾患から選択される炎症性疾患；しわ、十分な皮膚の堅固さの欠如、十分な皮膚の水分補給の欠如、又は不十分な皮脂分泌から選択される皮膚状態；腎性骨異栄養症；又は骨粗しょう症から選択される医薬組成物。
- X1、X2、及びX3がすべてHであり、かつ該化合物が下記式IBを有する、請求項１に記載の化合物。
- 請求項４又は請求項９に記載の化合物の、乾癬；白血病；大腸癌；乳癌；前立腺癌；多発性硬化症；ループス；糖尿病；宿主対移植片反応；臓器移植の拒絶反応；リウマチ性関節炎、喘息、又は炎症性腸疾患から選択される炎症性疾患；しわ、十分な皮膚の堅固さの欠如、十分な皮膚の水分補給の欠如、又は不十分な皮脂分泌から選択される皮膚状態；腎性骨異栄養症；又は骨粗しょう症から選択される生物学的状態の治療用薬物の調製における使用。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US65247305P | 2005-02-11 | 2005-02-11 | |
| US60/652,473 | 2005-02-11 | ||
| PCT/US2006/004699 WO2006086613A2 (en) | 2005-02-11 | 2006-02-10 | 2-METHYLENE-19-NOR- (20S-24S) - 1α, 25-D IHYDROXYVITAMIN-D2 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008530110A JP2008530110A (ja) | 2008-08-07 |
| JP2008530110A5 true JP2008530110A5 (ja) | 2009-03-05 |
| JP5036566B2 JP5036566B2 (ja) | 2012-09-26 |
Family
ID=36793746
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007555236A Expired - Fee Related JP5036566B2 (ja) | 2005-02-11 | 2006-02-10 | ２−メチレン−１９−ノル−（２０Ｓ−２４Ｓ）−１α，２５−ジヒドロキシビタミン−Ｄ２ |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7563783B2 (ja) |
| EP (1) | EP1853274B1 (ja) |
| JP (1) | JP5036566B2 (ja) |
| AU (1) | AU2006213727B2 (ja) |
| CA (1) | CA2597624C (ja) |
| ES (1) | ES2404061T3 (ja) |
| MX (1) | MX2007009726A (ja) |
| WO (1) | WO2006086613A2 (ja) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060079490A1 (en) * | 2001-01-25 | 2006-04-13 | Deluca Hector F | Method of treatment of type I diabetes |
| JP5009617B2 (ja) * | 2003-08-20 | 2012-08-22 | ウイスコンシン アラムニ リサーチ ファンデーション | ２−メチレン−１９−ノル−ビタミンｄ２化合物 |
| US7741314B2 (en) * | 2006-09-28 | 2010-06-22 | Wisconsin Alumni Research Foundation | 2-Methylene-(20R,25S)-19,27-Dinor-(22E)-Vitamin D Analogs |
| US20110034426A1 (en) * | 2009-08-03 | 2011-02-10 | Wisconsin Alumni Research Foundation | Method of Preventing Renal Disease and Treating Symptoms Thereof |
| US8445468B2 (en) * | 2009-10-02 | 2013-05-21 | Wisconsin Alumni Research Foundation | (20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3 |
| US8664206B2 (en) | 2010-03-23 | 2014-03-04 | Wisconsin Alumni Research Foundation | Diastereomers of 2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin D3 |
| JP5770261B2 (ja) * | 2010-03-23 | 2015-08-26 | ウイスコンシン アラムニ リサーチ ファンデーション | （２０Ｓ）−２−メチレン−１９−ノル−２２−ジメチル−１α，２５−ジヒドロキシビタミンＤ３および（２０Ｒ）−２−メチレン−１９−ノル−２２−ジメチル−１α，２５−ヒドロキシビタミンＤ３ |
| AU2011232562B2 (en) * | 2010-03-23 | 2014-10-02 | Wisconsin Alumni Research Foundation | Diastereomers of 2-methylene-19-nor-22-methyl-1alpha,25- dihydroxyvitamin D3 |
| JP6035331B2 (ja) * | 2011-06-14 | 2016-11-30 | ウイスコンシン アラムニ リサーチ ファンデーション | ３−デスオキシ−２−メチレン−１９−ノル−ビタミンｄ類似体およびそれらの使用 |
| RU2666995C2 (ru) | 2012-06-29 | 2018-09-13 | Висконсин Алюмни Рисерч Фаундейшн | ПРИМЕНЕНИЕ 2-МЕТИЛЕН-19-НОР-(20S)-1α,25-ДИГИДРОКСИВИТАМИНА D3 ДЛЯ ЛЕЧЕНИЯ ВТОРИЧНОГО ГИПЕРПАРАТИРЕОЗА |
| US10369161B2 (en) | 2014-12-30 | 2019-08-06 | Wisconsin Alumni Research Foundation | Use of 2-methylene-19-NOR-(20S)-1-alpha,25-dihydroxyvitamin D3 to treat primary hyperparathyroidism |
| US9539264B2 (en) | 2014-12-30 | 2017-01-10 | Wisconsin Alumni Research Foundation | Use of 2-methylene-19-nor-(20S)-1-alpha,25-dihydroxyvitamin D3 to treat secondary hyperparathyroidism in patients previously treated with calcimimetics |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4588716A (en) * | 1984-05-04 | 1986-05-13 | Wisconsin Alumni Research Foundation | Method for treating metabolic bone disease in mammals |
| US4666634A (en) | 1984-12-05 | 1987-05-19 | Chugai Seiyaku Kabushiki Kaisha | vitamin D3 derivatives having a substituent at 2-position |
| US5086191A (en) | 1991-05-28 | 1992-02-04 | Wisconsin Alumni Research Foundation | Intermediates for the synthesis of 19-nor vitamin D compounds |
| DE69400495T2 (de) | 1993-04-05 | 1997-04-30 | Wisconsin Alumni Res Found | 19-Nor-vitamin-D3-Verbindung mit einem Substituent an die 2. Stelle |
| US5552392A (en) | 1993-11-03 | 1996-09-03 | Wisconsin Alumni Research Foundation | Method of treating hypoparathyroidism with (20S) vitamin D compounds |
| US5843928A (en) * | 1997-03-17 | 1998-12-01 | Wisconsin Alumni Research Foundation | 2-alkylidene-19-nor-vitamin D compounds |
| US6392071B1 (en) * | 1997-03-17 | 2002-05-21 | Wisconsin Alumni: Research Foundation | 26,27-homologated-20-EPI-2-alkylidene-19-nor-vitamin D compounds |
| US5945410A (en) * | 1997-03-17 | 1999-08-31 | Wisconsin Alumni Research Foundation | 2-alkyl-19-nor-vitamin D compounds |
| US6673782B2 (en) * | 1999-04-29 | 2004-01-06 | Wisconsin Alumni Research Foundation | Treatment of systemic lupus erythematosis |
| US6479474B2 (en) * | 1999-07-08 | 2002-11-12 | Wisconsin Alumni Research Foundation | Dietary calcium as a supplement to vitamin D compound treatment of multiple sclerosis |
| US7704979B2 (en) | 2000-09-01 | 2010-04-27 | The University Of Tennessee Research Foundation | Materials and methods for the treatment or prevention of obesity |
| US6384087B1 (en) | 2000-09-01 | 2002-05-07 | University Of Tennesseee Research Corporation, Inc. | Materials and methods for the treatment or prevention of obesity |
| AU7544501A (en) | 2000-09-08 | 2002-03-22 | Wisconsin Alumni Res Found | 1alpha-hydroxy-2-methylene-19-nor-homopregnacalciferol and its therapeutic applications |
| US6627622B2 (en) * | 2002-02-18 | 2003-09-30 | Wisconsin Alumni Research Foundation | (20S)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol and its uses |
| US6566352B1 (en) | 2002-02-18 | 2003-05-20 | Wisconsin Alumni Research Foudation | 1 α-hydroxy-2-methylene-19-nor-pregnacalciferol and its uses |
| JP3957303B2 (ja) | 2002-03-29 | 2007-08-15 | ウィスコンシン・アルムニ・リサーチ・ファウンデーション | １α−ヒドロキシ−２−メチレン−１９−ノル−ホモプレグナカルシフェロールの合成法 |
| US7259143B2 (en) * | 2002-09-05 | 2007-08-21 | Wisconsin Alumni Research Foundation | Method of extending the dose range of vitamin D compounds |
| MXPA05009336A (es) * | 2003-04-10 | 2005-11-04 | Wisconsin Alumni Res Found | Compuestos de 2-propiliden-19-nor-vitamina d. |
| JP5009617B2 (ja) * | 2003-08-20 | 2012-08-22 | ウイスコンシン アラムニ リサーチ ファンデーション | ２−メチレン−１９−ノル−ビタミンｄ２化合物 |
| RU2331425C2 (ru) | 2003-09-19 | 2008-08-20 | Висконсин Эламнай Рисерч Фаундейшн (ВАРФ) | Фармацевтические композиции и способы, включающие комбинации производных 2-алкилиден-19-нор-витамина d и агониста/антагониста эстрогенов |
| AU2004273660B2 (en) | 2003-09-19 | 2010-08-19 | Wisconsin Alumni Research Foundation (Warf) | Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin D derivatives and parathyroid hormone |
| WO2005027931A1 (en) | 2003-09-19 | 2005-03-31 | Pfizer Products Inc. | Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and an ep2 or ep4 selective agonist |
| WO2005027913A1 (en) | 2003-09-19 | 2005-03-31 | Pfizer Products Inc. | Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and a growth hormone secretagogue |
| EP1694333A2 (en) * | 2003-11-25 | 2006-08-30 | Deltanoid Pharmaceuticals, Inc. | Methods for reducing body fat using vitamin d compounds |
-
2006
- 2006-02-10 EP EP06720601A patent/EP1853274B1/en not_active Not-in-force
- 2006-02-10 ES ES06720601T patent/ES2404061T3/es active Active
- 2006-02-10 WO PCT/US2006/004699 patent/WO2006086613A2/en active Application Filing
- 2006-02-10 CA CA2597624A patent/CA2597624C/en not_active Expired - Fee Related
- 2006-02-10 MX MX2007009726A patent/MX2007009726A/es active IP Right Grant
- 2006-02-10 US US11/352,454 patent/US7563783B2/en not_active Expired - Fee Related
- 2006-02-10 JP JP2007555236A patent/JP5036566B2/ja not_active Expired - Fee Related
- 2006-02-10 AU AU2006213727A patent/AU2006213727B2/en not_active Ceased
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