JP2018062523A5 - - Google Patents
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- Publication number
- JP2018062523A5 JP2018062523A5 JP2017253315A JP2017253315A JP2018062523A5 JP 2018062523 A5 JP2018062523 A5 JP 2018062523A5 JP 2017253315 A JP2017253315 A JP 2017253315A JP 2017253315 A JP2017253315 A JP 2017253315A JP 2018062523 A5 JP2018062523 A5 JP 2018062523A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- inhibitor
- hsd1
- pharmaceutically acceptable
- tumor
- 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.)
- Granted
Links
- 239000003112 inhibitor Substances 0.000 claims 26
- 102100037426 17-beta-hydroxysteroid dehydrogenase type 1 Human genes 0.000 claims 19
- 108010070743 3(or 17)-beta-hydroxysteroid dehydrogenase Proteins 0.000 claims 19
- 206010028980 Neoplasm Diseases 0.000 claims 18
- 201000011510 cancer Diseases 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 239000003098 androgen Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 229940011871 estrogen Drugs 0.000 claims 2
- 239000000262 estrogen Substances 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 238000011275 oncology therapy Methods 0.000 claims 2
- 230000009467 reduction Effects 0.000 claims 2
- 208000011571 secondary malignant neoplasm Diseases 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- -1 -OCH 2 CH 2 Br Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 230000003388 anti-hormonal effect Effects 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 230000005880 cancer cell killing Effects 0.000 claims 1
- 230000005907 cancer growth Effects 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 238000000315 cryotherapy Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 150000002391 heterocyclic compounds Chemical class 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 238000009169 immunotherapy Methods 0.000 claims 1
- 238000001361 intraarterial administration Methods 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001394 metastastic effect Effects 0.000 claims 1
- 206010061289 metastatic neoplasm Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000002035 prolonged effect Effects 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 238000009094 second-line therapy Methods 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 230000004083 survival effect Effects 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161467764P | 2011-03-25 | 2011-03-25 | |
| US61/467,764 | 2011-03-25 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014500216A Division JP2014508784A (ja) | 2011-03-25 | 2012-03-26 | １７β−ＨＳＤ１、１７β−ＨＳＤ３、および１７β−ＨＳＤ１０の阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018062523A JP2018062523A (ja) | 2018-04-19 |
| JP2018062523A5 true JP2018062523A5 (enExample) | 2018-06-07 |
| JP6727184B2 JP6727184B2 (ja) | 2020-07-22 |
Family
ID=46929260
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014500216A Withdrawn JP2014508784A (ja) | 2011-03-25 | 2012-03-26 | １７β−ＨＳＤ１、１７β−ＨＳＤ３、および１７β−ＨＳＤ１０の阻害剤 |
| JP2017253315A Expired - Fee Related JP6727184B2 (ja) | 2011-03-25 | 2017-12-28 | １７β−ＨＳＤ１、１７β−ＨＳＤ３、および１７β−ＨＳＤ１０の阻害剤 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014500216A Withdrawn JP2014508784A (ja) | 2011-03-25 | 2012-03-26 | １７β−ＨＳＤ１、１７β−ＨＳＤ３、および１７β−ＨＳＤ１０の阻害剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11072632B2 (enExample) |
| EP (1) | EP2688901B1 (enExample) |
| JP (2) | JP2014508784A (enExample) |
| AU (1) | AU2012234682A1 (enExample) |
| CA (1) | CA2830984C (enExample) |
| WO (1) | WO2012129673A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6456373B2 (ja) * | 2013-06-25 | 2019-01-23 | フォレンド ファーマ リミテッド | １７β−ヒドロキシステロイドデヒドロゲナーゼ タイプ１の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体 |
| WO2014207309A1 (en) * | 2013-06-25 | 2014-12-31 | Forendo Pharma Ltd | Therapeutically active estratrienthiazole derivatives as inhibitors of 17 b-hydroxysteroid dehydrogenase, type 1 |
| AU2015257594A1 (en) * | 2014-05-09 | 2016-11-24 | Tangent Reprofiling Limited | Modulators of androgen synthesis |
| US20170260226A1 (en) * | 2014-09-11 | 2017-09-14 | Bayer Pharma Aktiengesellschaft | 3-nitrogen or sulphur substituted oestra-1,3,5(10),16-tetraene akr1c3 inhibitors |
| CZ307437B6 (cs) * | 2016-06-07 | 2018-08-22 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. | 15β-substituované deriváty estronu jako selektivní inhibitory 17β-hydroxysteoiddehydrogenáz |
| MX391234B (es) | 2017-06-08 | 2025-03-21 | Forendo Pharma Ltd | Compuestos de estra-1,3,5(10)-trien-17-ona sustituida con 15.beta.-[3-propanamido] y sus 17-oximas para usarse en la inhibicion de 17.beta.-hidroxiesteroides deshidrogenasas. |
| WO2024020520A2 (en) * | 2022-07-20 | 2024-01-25 | Board Of Regents, The University Of Texas System | Enzyme compositions, steroid derivatives, enzyme inhibitors, and methods of making same for pharmaceutical applications |
| WO2025035212A1 (en) * | 2023-08-15 | 2025-02-20 | UNIVERSITé LAVAL | Irreversible 17beta-hsd1 inhibitors |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5232917A (en) * | 1987-08-25 | 1993-08-03 | University Of Southern California | Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series |
| EP0559240B1 (en) | 1987-09-24 | 2001-12-05 | Jencap Research Limited | Contraceptive packages containing oestrogen and progestin |
| TW385308B (en) * | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| US5952319A (en) * | 1997-11-26 | 1999-09-14 | Research Triangle Institute | Androgenic steroid compounds and a method of making and using the same |
| US6933312B2 (en) * | 2002-10-07 | 2005-08-23 | Agouron Pharmaceuticals, Inc. | Pyrazole derivatives |
| TWI331154B (en) | 2003-11-12 | 2010-10-01 | Solvay Pharm Gmbh | Novel 17-hydroxysteroid dehydrogenase type i inhibitors |
| ES2388297T3 (es) * | 2005-05-26 | 2012-10-11 | Abbott Products Gmbh | Inhibidores de 17-HSD1 y STS |
| US10174070B2 (en) * | 2005-09-30 | 2019-01-08 | Endece Llc | 6-substituted estradiol derivatives and methods of use |
| JP5268917B2 (ja) * | 2006-09-19 | 2013-08-21 | アボット プロダクツ ゲゼルシャフト ミット ベシュレンクテル ハフツング | 治療学的に有効なトリアゾール類及びそれらの使用 |
| CA2671075A1 (en) | 2006-11-30 | 2008-06-05 | Solvay Pharmaceuticals Gmbh | Substituted estratrien derivatives as 17beta hsd inhibitors |
| US20080171728A1 (en) | 2007-01-12 | 2008-07-17 | Quatrx Pharmaceuticals Co. | Efficient Process for Preparing Steroids and Vitamin D Derivatives With the Unnatural Configuration at C20 (20 Alpha-Methyl) from Pregnenolone |
| EP2014672A1 (en) * | 2007-07-12 | 2009-01-14 | Bayer Schering Pharma Aktiengesellschaft | 8-beta-substituted estratrienes as selectively active estrogens |
-
2012
- 2012-03-26 CA CA2830984A patent/CA2830984C/en active Active
- 2012-03-26 AU AU2012234682A patent/AU2012234682A1/en not_active Abandoned
- 2012-03-26 EP EP12765822.7A patent/EP2688901B1/en active Active
- 2012-03-26 US US14/007,577 patent/US11072632B2/en not_active Expired - Fee Related
- 2012-03-26 JP JP2014500216A patent/JP2014508784A/ja not_active Withdrawn
- 2012-03-26 WO PCT/CA2012/000316 patent/WO2012129673A1/en not_active Ceased
-
2017
- 2017-12-28 JP JP2017253315A patent/JP6727184B2/ja not_active Expired - Fee Related
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