JP2008536807A5 - - Google Patents
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- JP2008536807A5 JP2008536807A5 JP2007558143A JP2007558143A JP2008536807A5 JP 2008536807 A5 JP2008536807 A5 JP 2008536807A5 JP 2007558143 A JP2007558143 A JP 2007558143A JP 2007558143 A JP2007558143 A JP 2007558143A JP 2008536807 A5 JP2008536807 A5 JP 2008536807A5
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- 150000001875 compounds Chemical class 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 201000002028 prostate disease Diseases 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 230000000699 topical Effects 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000443 aerosol Substances 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 238000001361 intraarterial administration Methods 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000007921 spray Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 241001465754 Metazoa Species 0.000 description 3
- 206010028980 Neoplasm Diseases 0.000 description 3
- 230000004614 tumor growth Effects 0.000 description 3
- 230000000259 anti-tumor Effects 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 230000000638 stimulation Effects 0.000 description 2
- 206010067482 No adverse event Diseases 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 102000001307 androgen receptors Human genes 0.000 description 1
- 108010080146 androgen receptors Proteins 0.000 description 1
- 230000002280 anti-androgenic Effects 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 230000000275 pharmacokinetic Effects 0.000 description 1
- 230000003389 potentiating Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 210000004881 tumor cells Anatomy 0.000 description 1
Description
去勢は対照と比較して最終腫瘍体積の５５％減少へ導く（図６）。５の０．１５ｍｍｏｌ／ｋｇ １日１回および０．１５ｍｍｏｌ／ｋｇ １日２回は、ビヒクル処理対照動物の腫瘍に比較してそれぞれ平均最終腫瘍体積の４１％および８６．５％減少をもたらした（図６）。５で処理したマウスのすぐれた腫瘍発育阻害とは対照的に、化合物６で処理したマウスは低投与量において効果がないか、または対照と比較して腫瘍発育の刺激を示す（図６）。この化合物はインビトロにおいてＰＣＡ細胞生育の阻害において非常に有効であり、そして高度に抗アンドロゲン性であったから（図１を見よ）、化合物６がインビボにおいてＬＡＰＣＡ腫瘍細胞の発育を阻害することができないことは特に失望的である。５および６のインビボ抗腫瘍有効性の高度に有意な不均衡な二つの化合物の薬物動態学的性質の差に安易に帰せしめることはできない。これら二つの密接に関連した化合物のインビボ抗腫瘍有効性の劇的な差に含まれる理由は現時点では未知である。しかしながら、６が動物においてアンドロゲン受容体の強力なアゴニストであり得る代謝産物へ変換され、そのため腫瘍生育刺激を生ぜしめることへ帰せしめることができる。この研究の間、すべてのマウスは週１回体重測定した。すべての処理グループの体重は僅かに増加し、そして対照グループで観察されたのと類似であった。すべての動物は健康に見え、そして有害効果は観察されず、化合物は有意な毒性を持たないことを示唆する。
Claims (5)
- 前立腺疾患を処置する際に使用するための式１（化１）の化合物および生理学的に許容し得る担体を含む医薬組成物。
- 前記前立腺疾患が前立腺癌又は前立腺肥大症であることを特徴とする請求項１に記載の医薬組成物。
- 経口投与のために処方された請求項１に記載の医薬組成物。
- 非経口、経腸、腹腔内、外用、経皮、眼内、経鼻、局所、そしてエアロゾル、スプレー、吸入のような非経口、皮下、静脈内、筋肉内、バッカル、舌下、経直腸、膣内、動脈内又は硬膜下腔内から選択される経路によって送達するために処方された請求項１に記載の医薬組成物。
- 式１（化１）の化合物又はその薬学的に許容し得る塩が任意の他の活性成分と組み合わせられることを特徴とする請求項１乃至４のいずれかに記載の医薬組成物。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US65739005P | 2005-03-02 | 2005-03-02 | |
| US60/657,390 | 2005-03-02 | ||
| PCT/US2006/007143 WO2006093993A1 (en) | 2005-03-02 | 2006-03-02 | Novel c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012196525A Division JP5613206B2 (ja) | 2005-03-02 | 2012-09-06 | 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008536807A JP2008536807A (ja) | 2008-09-11 |
| JP2008536807A5 true JP2008536807A5 (ja) | 2012-10-25 |
| JP5130453B2 JP5130453B2 (ja) | 2013-01-30 |
Family
ID=36941503
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007558143A Active JP5130453B2 (ja) | 2005-03-02 | 2006-03-02 | 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性 |
| JP2012196525A Active JP5613206B2 (ja) | 2005-03-02 | 2012-09-06 | 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012196525A Active JP5613206B2 (ja) | 2005-03-02 | 2012-09-06 | 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性 |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US7875599B2 (ja) |
| EP (2) | EP2206719B1 (ja) |
| JP (2) | JP5130453B2 (ja) |
| KR (1) | KR101380959B1 (ja) |
| CN (2) | CN101155823A (ja) |
| AT (1) | ATE482969T1 (ja) |
| AU (1) | AU2006218711B2 (ja) |
| BR (1) | BRPI0607523A2 (ja) |
| CA (1) | CA2599953C (ja) |
| DE (1) | DE602006017175D1 (ja) |
| DK (2) | DK1853619T3 (ja) |
| EA (1) | EA019560B1 (ja) |
| ES (2) | ES2353413T3 (ja) |
| HK (1) | HK1115387A1 (ja) |
| IL (3) | IL185608A (ja) |
| MX (1) | MX2007010593A (ja) |
| NZ (1) | NZ561571A (ja) |
| PL (2) | PL2206719T3 (ja) |
| PT (2) | PT2206719E (ja) |
| SI (2) | SI1853619T1 (ja) |
| WO (1) | WO2006093993A1 (ja) |
| ZA (1) | ZA200708106B (ja) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8569275B2 (en) | 2002-08-28 | 2013-10-29 | Harbor Therapeutics, Inc. | Steroids having 7-oxgen and 17-heteroaryl substitution |
| CA2599953C (en) * | 2005-03-02 | 2013-08-13 | Angela Brodie | Novel c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity |
| CA2726734C (en) | 2007-06-06 | 2014-10-07 | University Of Maryland, Baltimore | Hdac inhibitor ms-275 and aromatase inhibitors for the treatment of cancer |
| US20110105445A1 (en) * | 2008-03-12 | 2011-05-05 | University Of Maryland, Baltimore | Androgen receptor inactivation contributes to antitumor efficacy of cyp17 inhibitors in prostate cancer |
| US20100048913A1 (en) * | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
| US20110118219A1 (en) | 2008-03-25 | 2011-05-19 | University Of Maryland, Baltimore | Novel prodrugs of c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity |
| US8785423B2 (en) * | 2008-04-14 | 2014-07-22 | University Of Maryland, Baltimore | Compositions and methods of inducing endoplasmic reticulum stress response for the treatment of cell proliferative diseases |
| EP2334686B1 (en) | 2008-08-28 | 2019-02-27 | President and Fellows of Harvard College | Cortistatin analogues and syntheses therof |
| BRPI0920681A2 (pt) * | 2008-10-28 | 2015-12-29 | Biomarin Pharm Inc | inibidores de decahidro-1h-indenoquinolinona e decahidro-3h-ciclopentafenantridinona de cyp17 |
| US8791095B2 (en) | 2009-02-05 | 2014-07-29 | Tokai Pharmaceuticals, Inc. | Steroidal CYP17 inhibitors/antiandrogens |
| EP2393827B1 (en) * | 2009-02-05 | 2015-10-07 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens |
| WO2010091299A2 (en) * | 2009-02-05 | 2010-08-12 | Tokai Pharmaceuticals | Novel combination cancer therapies |
| KR101360725B1 (ko) | 2009-06-26 | 2014-02-07 | 노파르티스 아게 | Ｃｙｐ17의 억제제로서의 1,3-이치환된 이미다졸리딘-2-온 유도체 |
| EP2461814A4 (en) * | 2009-08-07 | 2012-12-05 | Tokai Pharmaceuticals Inc | PROSTATE CANCER TREATMENT |
| EP2499151A4 (en) * | 2009-11-13 | 2013-03-20 | Tokai Pharmaceuticals Inc | MAMMALIAN STEROID METABOLITES |
| WO2011066582A1 (en) * | 2009-11-30 | 2011-06-03 | Harbor Biosciences, Inc. | Anticancer compounds and screening method |
| US8946260B2 (en) | 2010-09-16 | 2015-02-03 | Novartis Ag | 17α-hydroxylase/C17,20-lyase inhibitors |
| US20130252930A1 (en) * | 2010-12-16 | 2013-09-26 | Biomarin Pharmaceutical Inc. | Cyp11b, cyp17, and/or cyp21 inhibitors |
| MX359399B (es) | 2011-04-28 | 2018-09-27 | Novartis Ag | Inhibidores de 17alfa-hidroxilasa/c17-20-liasa. |
| BR112014001440A2 (pt) * | 2011-07-18 | 2017-02-21 | Tokai Pharmaceuticals Inc | novas composições e métodos para o tratamento de câncer de próstata |
| EP2793896A4 (en) * | 2011-12-22 | 2015-06-24 | Tokai Pharmaceuticals Inc | METHODS AND COMPOSITIONS FOR POLYTHERAPY USING P13K / MTOR INHIBITORS |
| US9884067B2 (en) | 2013-03-14 | 2018-02-06 | University Of Maryland, Baltimore | Androgen receptor down-regulating agents and uses thereof |
| AU2014247941C1 (en) * | 2013-04-04 | 2019-10-31 | University Of Maryland, Baltimore | Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity |
| US9808472B2 (en) * | 2013-08-12 | 2017-11-07 | Tokai Pharmaceuticals, Inc. | Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies |
| MY180383A (en) | 2013-12-24 | 2020-11-28 | Harvard College | Cortistatin analogues and syntheses and uses thereof |
| CN103694299A (zh) * | 2014-01-13 | 2014-04-02 | 中国药科大学 | 甾体类雄激素受体抑制剂、其制备方法及其医药用途 |
| CN105732759A (zh) * | 2015-01-29 | 2016-07-06 | 苏州晶云药物科技有限公司 | (3β)-17-(1H-苯并咪唑-1-基)雄甾-5，16-二烯-3-醇的盐及其制备方法 |
| EP3294298A4 (en) | 2015-05-08 | 2018-10-17 | President and Fellows of Harvard College | Cortistatin analogues, syntheses, and uses thereof |
| EP3316889A4 (en) | 2015-07-01 | 2018-11-14 | President and Fellows of Harvard College | Cortistatin analogues and syntheses and uses thereof |
| WO2017066697A1 (en) | 2015-10-14 | 2017-04-20 | Dou Qingping | Treatments and diagnostics for cancers |
| IT201600121375A1 (it) * | 2016-11-30 | 2018-05-30 | Ind Chimica Srl | PROCESSO PER LA PREPARAZIONE DI 3ß-IDROSSI-17-(1H-BENZIMIDAZOL-1-IL)ANDROSTA-5,16-DIENE |
| RU2749134C1 (ru) * | 2016-08-08 | 2021-06-04 | Индустриале Кимика С.Р.Л. | СПОСОБ ПОЛУЧЕНИЯ 3β-ГИДРОКСИ-17-(1Н-БЕНЗИМИДАЗОЛ-1-ИЛ)АНДРОСТА-5,16-ДИЕНА |
| IT201600083406A1 (it) * | 2016-08-08 | 2018-02-08 | Ind Chimica Srl | PROCESSO PER LA PREPARAZIONE DI 3β-IDROSSI-17-(1H-BENZIMIDAZOL-1-IL)ANDROSTA-5,16-DIENE |
| WO2019160890A1 (en) * | 2018-02-13 | 2019-08-22 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase degraders and methods of use |
| EP3752518A4 (en) * | 2018-02-13 | 2021-10-20 | Dana Farber Cancer Institute, Inc. | CYCLINE DEPENDENT KINASE INHIBITORS AND METHOD OF USING |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA27440A (en) | 1887-08-16 | James T. Walsh | Art of making sheet metal cans, for packing meats, fruits, vegetables, etc. | |
| CH621803A5 (ja) * | 1974-08-08 | 1981-02-27 | Siphar Sa | |
| US5604213A (en) | 1992-03-31 | 1997-02-18 | British Technology Group Limited | 17-substituted steroids useful in cancer treatment |
| US5994335A (en) | 1997-10-17 | 1999-11-30 | The University Of Maryland, Baltimore | 17-azolyl steroids useful as androgen synthesis inhibitors |
| US20070036747A1 (en) | 2003-07-29 | 2007-02-15 | Dompe S.P.A. | Pharmaceutical combination useful for stem cell mobilization |
| CA2599953C (en) * | 2005-03-02 | 2013-08-13 | Angela Brodie | Novel c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity |
-
2006
- 2006-03-02 CA CA2599953A patent/CA2599953C/en active Active
- 2006-03-02 SI SI200630861T patent/SI1853619T1/sl unknown
- 2006-03-02 BR BRPI0607523-1A patent/BRPI0607523A2/pt not_active IP Right Cessation
- 2006-03-02 DK DK06736460.4T patent/DK1853619T3/da active
- 2006-03-02 SI SI200631883T patent/SI2206719T1/sl unknown
- 2006-03-02 AU AU2006218711A patent/AU2006218711B2/en active Active
- 2006-03-02 CN CNA2006800064632A patent/CN101155823A/zh active Pending
- 2006-03-02 ES ES06736460T patent/ES2353413T3/es active Active
- 2006-03-02 US US11/817,550 patent/US7875599B2/en active Active
- 2006-03-02 MX MX2007010593A patent/MX2007010593A/es active IP Right Grant
- 2006-03-02 JP JP2007558143A patent/JP5130453B2/ja active Active
- 2006-03-02 EP EP10150763.0A patent/EP2206719B1/en active Active
- 2006-03-02 PL PL10150763T patent/PL2206719T3/pl unknown
- 2006-03-02 NZ NZ561571A patent/NZ561571A/en not_active IP Right Cessation
- 2006-03-02 KR KR1020077022440A patent/KR101380959B1/ko not_active IP Right Cessation
- 2006-03-02 AT AT06736460T patent/ATE482969T1/de active
- 2006-03-02 PT PT101507630T patent/PT2206719E/pt unknown
- 2006-03-02 DK DK10150763.0T patent/DK2206719T3/en active
- 2006-03-02 EP EP06736460A patent/EP1853619B1/en active Active
- 2006-03-02 WO PCT/US2006/007143 patent/WO2006093993A1/en active Application Filing
- 2006-03-02 ES ES10150763.0T patent/ES2528055T3/es active Active
- 2006-03-02 PL PL06736460T patent/PL1853619T3/pl unknown
- 2006-03-02 CN CN2013101036754A patent/CN103349664A/zh active Pending
- 2006-03-02 PT PT06736460T patent/PT1853619E/pt unknown
- 2006-03-02 DE DE602006017175T patent/DE602006017175D1/de active Active
- 2006-03-02 EA EA200701872A patent/EA019560B1/ru not_active IP Right Cessation
-
2007
- 2007-08-30 IL IL185608A patent/IL185608A/en not_active IP Right Cessation
- 2007-09-20 ZA ZA200708106A patent/ZA200708106B/xx unknown
-
2008
- 2008-05-14 HK HK08105362.1A patent/HK1115387A1/xx not_active IP Right Cessation
-
2011
- 2011-01-06 IL IL210480A patent/IL210480A/en not_active IP Right Cessation
- 2011-01-06 IL IL210478A patent/IL210478A0/en unknown
-
2012
- 2012-09-06 JP JP2012196525A patent/JP5613206B2/ja active Active
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