NZ561571A - Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity - Google Patents
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activityInfo
- Publication number
- NZ561571A NZ561571A NZ561571A NZ56157106A NZ561571A NZ 561571 A NZ561571 A NZ 561571A NZ 561571 A NZ561571 A NZ 561571A NZ 56157106 A NZ56157106 A NZ 56157106A NZ 561571 A NZ561571 A NZ 561571A
- Authority
- NZ
- New Zealand
- Prior art keywords
- benzimidazol
- androsta
- compound
- diene
- heteroaryl
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract description 25
- 238000003786 synthesis reaction Methods 0.000 title abstract description 22
- 230000003637 steroidlike Effects 0.000 title abstract description 9
- 229940124766 Cyp17 inhibitor Drugs 0.000 title description 22
- 239000000051 antiandrogen Substances 0.000 title description 18
- 230000002280 anti-androgenic effect Effects 0.000 title description 17
- 238000000338 in vitro Methods 0.000 title description 13
- 229940030495 antiandrogen sex hormone and modulator of the genital system Drugs 0.000 title description 7
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- 150000003431 steroids Chemical group 0.000 claims description 27
- -1 heteroaryl steroid compound Chemical class 0.000 claims description 26
- 239000012964 benzotriazole Chemical class 0.000 claims description 24
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- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims description 18
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Classifications
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
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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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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|---|---|---|---|
| US65739005P | 2005-03-02 | 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 |
Publications (1)
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|---|---|
| NZ561571A true NZ561571A (en) | 2009-09-25 |
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| NZ561571A NZ561571A (en) | 2005-03-02 | 2006-03-02 | Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity |
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| US8569275B2 (en) | 2002-08-28 | 2013-10-29 | Harbor Therapeutics, Inc. | Steroids having 7-oxgen and 17-heteroaryl substitution |
| PT2206719E (pt) * | 2005-03-02 | 2015-02-05 | Univ Maryland | Composição farmacêutica compreendendo 3-beta-hidroxi-17- (1-h-benzimidazol-1-il)androsta-5,16-dieno |
| EP2359828A1 (en) | 2007-06-06 | 2011-08-24 | University of Maryland, Baltimore | HDAC inhibitors and hormone targeted drugs 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 |
| US20100048914A1 (en) * | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal Cyp17 Inhibitors/Antiandrogens, 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 |
| WO2010024930A2 (en) | 2008-08-28 | 2010-03-04 | 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 |
| GB201114153D0 (en) * | 2009-02-05 | 2011-10-05 | Tokai Pharmaceuticals Inc | Combination of a 17 alpha-hydroxylase/c17, 20-lyase inhibitor with an additional therapeutic agent |
| BRPI1008745A2 (pt) * | 2009-02-05 | 2019-09-17 | Tokai Pharmaceuticals Inc | pró-fármacos de inibidores esteroidais de cyp17/antiandrogênios |
| KR101360725B1 (ko) | 2009-06-26 | 2014-02-07 | 노파르티스 아게 | Ｃｙｐ17의 억제제로서의 1,3-이치환된 이미다졸리딘-2-온 유도체 |
| US8791094B2 (en) * | 2009-08-07 | 2014-07-29 | Tokai Pharmaceuticals, Inc. | Treatment of prostate cancer |
| JP5956928B2 (ja) * | 2009-11-13 | 2016-07-27 | トーカイ ファーマシューティカルズ，インク． | 哺乳類のステロイドの代謝物質 |
| WO2011066582A1 (en) * | 2009-11-30 | 2011-06-03 | Harbor Biosciences, Inc. | Anticancer compounds and screening method |
| EP2627648A1 (en) | 2010-09-16 | 2013-08-21 | Novartis AG | 17aHYDROXYLASE/C17,20-LYASE INHIBITORS |
| RU2013132766A (ru) * | 2010-12-16 | 2015-01-27 | Байомарин Фармасьютикал Инк. | Ингибиторы cyp11b, cyp17 и/или cyp21 |
| JP6002210B2 (ja) | 2011-04-28 | 2016-10-05 | ノバルティス アーゲー | １７α−ヒドロキシラーゼ／Ｃ１７，２０−リアーゼ阻害剤 |
| BR112014001440A2 (pt) * | 2011-07-18 | 2017-02-21 | Tokai Pharmaceuticals Inc | novas composições e métodos para o tratamento de câncer de próstata |
| AU2012358219A1 (en) * | 2011-12-22 | 2014-07-10 | Tokai Pharmaceuticals, Inc. | Methods and compositions for combination therapy using P13K/mTOR inhibitors |
| SG11201507093WA (en) | 2013-03-14 | 2015-10-29 | Univ Maryland Baltimore Office Of Technology Transfer | Androgen receptor down-regulating agents and uses thereof |
| WO2014165815A2 (en) | 2013-04-04 | 2014-10-09 | University Of Maryland, Baltimore | Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity |
| CA2920317A1 (en) | 2013-08-12 | 2015-02-19 | Tokai Pharmaceuticals, Inc. | Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies |
| KR20160101162A (ko) | 2013-12-24 | 2016-08-24 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 코르티스타틴 유사체 및 그의 합성 및 용도 |
| 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 |
| US10682362B2 (en) | 2015-10-14 | 2020-06-16 | Wayne State University | 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 |
| 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 |
| US11390645B2 (en) | 2016-08-08 | 2022-07-19 | Industriale Chimica S.R.L. | Process for the preparation of 3β-hydroxy-17-(1H-benzimidazol-1-YL) androsta-5,16-diene |
| US20200369715A1 (en) * | 2018-02-13 | 2020-11-26 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase inhibitors and methods of use |
| CA3087286C (en) | 2018-02-13 | 2023-06-27 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase degraders and methods of use |
| US12410194B2 (en) | 2019-11-26 | 2025-09-09 | Dana-Farber Cancer Institute, Inc. | Potent and selective azaindole inhibitors of CDK8 and CDK19 |
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| CA27440A (en) | 1887-08-16 | James T. Walsh | Art of making sheet metal cans, for packing meats, fruits, vegetables, etc. | |
| CH621803A5 (cg-RX-API-DMAC7.html) * | 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 |
| DK1660115T3 (da) | 2003-07-29 | 2011-10-10 | Dompe Spa | Farmaceutisk kombination af G-CSF og PLGF anvendelig til blodstamceller |
| PT2206719E (pt) | 2005-03-02 | 2015-02-05 | Univ Maryland | Composição farmacêutica compreendendo 3-beta-hidroxi-17- (1-h-benzimidazol-1-il)androsta-5,16-dieno |
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