ZA200708106B - Novel C-17 -heteroaryl steroidal CYP17 inhibitors/anti-androgens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity - Google Patents
Novel C-17 -heteroaryl steroidal CYP17 inhibitors/anti-androgens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activityInfo
- Publication number
- ZA200708106B ZA200708106B ZA200708106A ZA200708106A ZA200708106B ZA 200708106 B ZA200708106 B ZA 200708106B ZA 200708106 A ZA200708106 A ZA 200708106A ZA 200708106 A ZA200708106 A ZA 200708106A ZA 200708106 B ZA200708106 B ZA 200708106B
- Authority
- ZA
- South Africa
- Prior art keywords
- synthesis
- androgens
- pharmacokinetics
- novel
- biological activities
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 230000003637 steroidlike Effects 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- 229940124766 Cyp17 inhibitor Drugs 0.000 title 1
- 230000002280 anti-androgenic effect Effects 0.000 title 1
- 230000000259 anti-tumor effect Effects 0.000 title 1
- 239000000051 antiandrogen Substances 0.000 title 1
- 229940030495 antiandrogen sex hormone and modulator of the genital system Drugs 0.000 title 1
- 230000004071 biological effect Effects 0.000 title 1
- 238000000338 in vitro Methods 0.000 title 1
- 238000000034 method Methods 0.000 abstract 3
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 2
- KCTZOTUQSGYWLV-UHFFFAOYSA-N N1C=NC=C2N=CC=C21 Chemical class N1C=NC=C2N=CC=C21 KCTZOTUQSGYWLV-UHFFFAOYSA-N 0.000 abstract 2
- 102000001307 androgen receptors Human genes 0.000 abstract 2
- 108010080146 androgen receptors Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000003389 potentiating effect Effects 0.000 abstract 2
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 101100298362 Homo sapiens PPIG gene Proteins 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 150000004891 diazines Chemical class 0.000 abstract 1
- 238000003379 elimination reaction Methods 0.000 abstract 1
- 102000056262 human PPIG Human genes 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000012038 nucleophile Substances 0.000 abstract 1
- 230000000269 nucleophilic effect Effects 0.000 abstract 1
- 238000010651 palladium-catalyzed cross coupling reaction Methods 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- DBHSVKZZSWTSTN-UHFFFAOYSA-N tributyl(pyridazin-3-yl)stannane Chemical class CCCC[Sn](CCCC)(CCCC)C1=CC=CN=N1 DBHSVKZZSWTSTN-UHFFFAOYSA-N 0.000 abstract 1
- 125000002348 vinylic group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US65739005P | 2005-03-02 | 2005-03-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200708106B true ZA200708106B (en) | 2008-12-31 |
Family
ID=36941503
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200708106A ZA200708106B (en) | 2005-03-02 | 2007-09-20 | Novel C-17 -heteroaryl steroidal CYP17 inhibitors/anti-androgens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US7875599B2 (show.php) |
| EP (2) | EP1853619B1 (show.php) |
| JP (2) | JP5130453B2 (show.php) |
| KR (1) | KR101380959B1 (show.php) |
| CN (2) | CN103349664A (show.php) |
| AT (1) | ATE482969T1 (show.php) |
| AU (1) | AU2006218711B2 (show.php) |
| BR (1) | BRPI0607523A2 (show.php) |
| CA (1) | CA2599953C (show.php) |
| DE (1) | DE602006017175D1 (show.php) |
| DK (2) | DK2206719T3 (show.php) |
| EA (1) | EA019560B1 (show.php) |
| ES (2) | ES2528055T3 (show.php) |
| IL (3) | IL185608A (show.php) |
| MX (1) | MX2007010593A (show.php) |
| NZ (1) | NZ561571A (show.php) |
| PL (2) | PL1853619T3 (show.php) |
| PT (2) | PT1853619E (show.php) |
| SI (2) | SI2206719T1 (show.php) |
| WO (1) | WO2006093993A1 (show.php) |
| ZA (1) | ZA200708106B (show.php) |
Families Citing this family (36)
| 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 |
| NZ561571A (en) * | 2005-03-02 | 2009-09-25 | Univ Maryland | Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity |
| WO2008154402A2 (en) | 2007-06-06 | 2008-12-18 | University Of Maryland, Baltimore | Hdac inhibitors and hormone targeted drugs for the treatment of cancer |
| WO2009114658A2 (en) * | 2008-03-12 | 2009-09-17 | University Of Maryland, Baltimore | Androgen receptor inactivation contributes to antitumor efficacy of cyp17 inhibitors in prostate cancer |
| US20100048524A1 (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 |
| GB2470700B (en) | 2008-03-25 | 2012-08-08 | Univ Maryland | C-17 heteroaryl steroidal CYP17 inhibitors |
| 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 |
| EP2362872A4 (en) * | 2008-10-28 | 2012-05-30 | Biomarin Pharm Inc | DECAHYDRO-1H-INDENOCHINOLINONE AND DECAHYDRO-3H-CYCLOPENTAPHENANTHRIDINONE CYP17 HEMMER |
| WO2010091299A2 (en) * | 2009-02-05 | 2010-08-12 | Tokai Pharmaceuticals | Novel combination cancer therapies |
| GB2479693B (en) * | 2009-02-05 | 2014-04-09 | Tokai Pharmaceuticals Inc | Steroidal CYP17 inhibitors and their use in the treatment of cancer and prostate hyperplasia |
| CN102686600A (zh) * | 2009-02-05 | 2012-09-19 | 托凯药业股份有限公司 | 甾体cyp17抑制剂/抗雄激素物质的新型药物前体 |
| WO2010149755A1 (en) | 2009-06-26 | 2010-12-29 | Novartis Ag | 1, 3-disubstituted imidazolidin-2-one derivatives as inhibitors of cyp 17 |
| AU2010279398A1 (en) * | 2009-08-07 | 2012-03-08 | 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 |
| WO2012035078A1 (en) | 2010-09-16 | 2012-03-22 | Novartis Ag | 17α-HYDROXYLASE/C17,20-LYASE INHIBITORS |
| BR112013017635A2 (pt) * | 2010-12-16 | 2016-10-11 | Biomarin Pharm Inc | inibidores de cyp11b, cyp17 e/ou cyp21 |
| AU2012249421B9 (en) | 2011-04-28 | 2015-10-22 | Novartis Ag | 17alpha-hydroxylase/C17,20-lyase inhibitors |
| CN103813794A (zh) * | 2011-07-18 | 2014-05-21 | 拓凯制药公司 | 用于治疗前列腺癌的新型组合物及方法 |
| JP2015503508A (ja) * | 2011-12-22 | 2015-02-02 | トーカイ ファーマシューティカルズ，インク． | ＰＩ３Ｋ／ｍＴＯＲ阻害剤を使用する併用療法のための方法および組成物 |
| CA2904170A1 (en) | 2013-03-14 | 2014-09-25 | University Of Maryland, Baltimore | 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 |
| JP2016528252A (ja) | 2013-08-12 | 2016-09-15 | トーカイ ファーマシューティカルズ， インコーポレイテッド | アンドロゲン標的治療を使用する新生物障害の処置のためのバイオマーカー |
| EA030907B1 (ru) | 2013-12-24 | 2018-10-31 | Президент Энд Феллоус Оф Гарвард Колледж | Аналоги кортистатина, их синтез и применения |
| 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 |
| WO2017004411A1 (en) | 2015-07-01 | 2017-01-05 | 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 |
| CA3063339C (en) * | 2016-08-08 | 2024-05-28 | Industriale Chimica S.R.L. | Process for the preparation of 3b-hydroxy-17-(1h-benzimidazol-1-yl)androsta-5,16-diene |
| EP3752517B1 (en) * | 2018-02-13 | 2025-04-09 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase degraders and methods of use |
| WO2019160889A1 (en) * | 2018-02-13 | 2019-08-22 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase inhibitors and methods of use |
| CA3159284A1 (en) | 2019-11-26 | 2021-06-03 | Dana-Farber Cancer Institute, Inc. | Potent and selective azaindole inhibitors of cdk8 and cdk19 |
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 (show.php) * | 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 |
| ATE513555T1 (de) | 2003-07-29 | 2011-07-15 | Dompe Spa | Pharmazeutische kombination aus g-csf und plgf für blutstammzellen |
| NZ561571A (en) * | 2005-03-02 | 2009-09-25 | Univ Maryland | Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity |
-
2006
- 2006-03-02 NZ NZ561571A patent/NZ561571A/en not_active IP Right Cessation
- 2006-03-02 SI SI200631883T patent/SI2206719T1/sl unknown
- 2006-03-02 DK DK10150763.0T patent/DK2206719T3/en active
- 2006-03-02 BR BRPI0607523-1A patent/BRPI0607523A2/pt not_active IP Right Cessation
- 2006-03-02 ES ES10150763.0T patent/ES2528055T3/es active Active
- 2006-03-02 MX MX2007010593A patent/MX2007010593A/es active IP Right Grant
- 2006-03-02 PL PL06736460T patent/PL1853619T3/pl unknown
- 2006-03-02 WO PCT/US2006/007143 patent/WO2006093993A1/en not_active Ceased
- 2006-03-02 PL PL10150763T patent/PL2206719T3/pl unknown
- 2006-03-02 ES ES06736460T patent/ES2353413T3/es active Active
- 2006-03-02 KR KR1020077022440A patent/KR101380959B1/ko not_active Expired - Fee Related
- 2006-03-02 EA EA200701872A patent/EA019560B1/ru not_active IP Right Cessation
- 2006-03-02 US US11/817,550 patent/US7875599B2/en active Active
- 2006-03-02 PT PT06736460T patent/PT1853619E/pt unknown
- 2006-03-02 CN CN2013101036754A patent/CN103349664A/zh active Pending
- 2006-03-02 CA CA2599953A patent/CA2599953C/en active Active
- 2006-03-02 CN CNA2006800064632A patent/CN101155823A/zh active Pending
- 2006-03-02 JP JP2007558143A patent/JP5130453B2/ja active Active
- 2006-03-02 SI SI200630861T patent/SI1853619T1/sl unknown
- 2006-03-02 EP EP06736460A patent/EP1853619B1/en active Active
- 2006-03-02 AT AT06736460T patent/ATE482969T1/de active
- 2006-03-02 AU AU2006218711A patent/AU2006218711B2/en active Active
- 2006-03-02 EP EP10150763.0A patent/EP2206719B1/en active Active
- 2006-03-02 DK DK06736460.4T patent/DK1853619T3/da active
- 2006-03-02 DE DE602006017175T patent/DE602006017175D1/de active Active
- 2006-03-02 PT PT101507630T patent/PT2206719E/pt unknown
-
2007
- 2007-08-30 IL IL185608A patent/IL185608A/en not_active IP Right Cessation
- 2007-09-20 ZA ZA200708106A patent/ZA200708106B/xx unknown
-
2011
- 2011-01-06 IL IL210478A patent/IL210478A0/en unknown
- 2011-01-06 IL IL210480A patent/IL210480A/en not_active IP Right Cessation
-
2012
- 2012-09-06 JP JP2012196525A patent/JP5613206B2/ja active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200708106B (en) | Novel C-17 -heteroaryl steroidal CYP17 inhibitors/anti-androgens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity | |
| GB2470700A (en) | Novel prodrugs of C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogans: synthesis, in vitro biological activities, Pharmacokinetics and antitumor activity | |
| AU2010210422A8 (en) | Novel prodrugs of steroidal CYP17 inhibitors/antiandrogens | |
| WO2006044379A3 (en) | Novel curcumin analogues and uses thereof | |
| EA017278B9 (ru) | Соединения азаиндазола и способы применения | |
| SI2444085T1 (sl) | Diarilhidantoinske spojine kot antagonisti androgenega receptorja za zdravljenje raka | |
| PT1353672E (pt) | Síntese da 4-amino talidomida enantiómeros | |
| WO2003088927A3 (en) | Novel curcumin analogues and uses thereof | |
| EP2966065A3 (en) | Hydroxylated and methoxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors | |
| PT1928882E (pt) | (s)-n-metilnaltrexona, processo para a sua síntese e sua utilização farmacêutica | |
| IL195256A0 (en) | Compositions of r(+)and s(-)pramipexole and methods of using the same | |
| WO2007087548A3 (en) | Chemical compounds | |
| IL183160A0 (en) | Indazole-carboxamide compounds | |
| MX2009004096A (es) | Metabolitos de talarozol. | |
| MXPA06009475A (es) | Derivados de quinazolina y usos terapeuticos de los mismos. | |
| WO2006052889A3 (en) | Quinolinone-carboxamide compounds | |
| TW200724537A (en) | Pyrimidine derivatives for treatment of hyperproliferative disorders | |
| IL178261A0 (en) | Use of 5,10-methylene tetrahydrofolate for the treatment of cancer | |
| TW200612925A (en) | Prodrug substituted benzoxazoles as estrogenic agents | |
| WO2007048097A3 (en) | Anbrosteeone derivatives and method of use thereof | |
| TW200621703A (en) | Alkylidene-tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents | |
| WO2008073752A3 (en) | Cyclobutyl derivatives for the treatment of glaucoma | |
| CY1115910T1 (el) | ΦΑΡΜΑΚΕΥΤΙΚΗ ΣΥΝΘΕΣΗ ΠΟΥ ΠΕΡΙΛΑΜΒΑΝΕΙ 3-BETA-HYDROXY-17-(l-HBENZIMIDAZOLE-1-YL)ANDROSΤΑ-5,16-DIENE | |
| TW200603812A (en) | D-homo-17-chlor-16(17)-ene steroids | |
| TW200504044A (en) | Methods for preparing derivatives of fungicidal iodochromones and intermediate compounds |