JP2016515630A5 - - Google Patents
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- Publication number
- JP2016515630A5 JP2016515630A5 JP2016506667A JP2016506667A JP2016515630A5 JP 2016515630 A5 JP2016515630 A5 JP 2016515630A5 JP 2016506667 A JP2016506667 A JP 2016506667A JP 2016506667 A JP2016506667 A JP 2016506667A JP 2016515630 A5 JP2016515630 A5 JP 2016515630A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- group
- cooet
- coome
- tetrazole
- 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
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 30
- KJUGUADJHNHALS-UHFFFAOYSA-N 1H-tetrazole Chemical compound C=1N=NNN=1 KJUGUADJHNHALS-UHFFFAOYSA-N 0.000 claims 20
- 238000000034 method Methods 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims 10
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 10
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 10
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 10
- -1 1H-benzimidazol-1-yl Chemical group 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 206010060862 Prostate cancer Diseases 0.000 claims 8
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 8
- MDHIWBNJNHUBJL-VMXHOPILSA-N (8s,9s,10r,13r,14s)-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15-decahydro-1h-cyclopenta[a]phenanthrene Chemical compound C1CCC[C@]2(C)[C@H]3CC[C@](C)(C=CC4)[C@@H]4[C@@H]3CC=C21 MDHIWBNJNHUBJL-VMXHOPILSA-N 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 4
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 4
- 239000003098 androgen Substances 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- GOBHVZIVCCFNFK-UHFFFAOYSA-N 6-[3-(1H-benzimidazol-2-yl)phenyl]naphthalen-2-ol Chemical compound N1=C(NC2=C1C=CC=C2)C=2C=C(C=CC2)C=2C=C1C=CC(=CC1=CC2)O GOBHVZIVCCFNFK-UHFFFAOYSA-N 0.000 claims 3
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 3
- 108091008715 AR-FL Proteins 0.000 claims 2
- 201000004384 Alopecia Diseases 0.000 claims 2
- 206010003694 Atrophy Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010068597 Bulbospinal muscular atrophy congenital Diseases 0.000 claims 2
- 208000027747 Kennedy disease Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 claims 2
- 108010080146 androgen receptors Proteins 0.000 claims 2
- 102000001307 androgen receptors Human genes 0.000 claims 2
- 201000002996 androgenic alopecia Diseases 0.000 claims 2
- 230000037444 atrophy Effects 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 230000000593 degrading effect Effects 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 210000003205 muscle Anatomy 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 208000037922 refractory disease Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 0 C*1C=CC(C(Nc2cc(-[n]3c4ccccc4nc3)ccc2)=O)=CC=C1 Chemical compound C*1C=CC(C(Nc2cc(-[n]3c4ccccc4nc3)ccc2)=O)=CC=C1 0.000 description 2
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361808345P | 2013-04-04 | 2013-04-04 | |
| US61/808,345 | 2013-04-04 | ||
| US201361808902P | 2013-04-05 | 2013-04-05 | |
| US61/808,902 | 2013-04-05 | ||
| PCT/US2014/033063 WO2014165815A2 (en) | 2013-04-04 | 2014-04-04 | Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016515630A JP2016515630A (ja) | 2016-05-30 |
| JP2016515630A5 true JP2016515630A5 (https=) | 2017-03-30 |
| JP6417392B2 JP6417392B2 (ja) | 2018-11-07 |
Family
ID=51659362
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016506667A Active JP6417392B2 (ja) | 2013-04-04 | 2014-04-04 | 強力なアンドロゲン受容体ダウンレギュレーションおよび抗前立腺ガン活性を伴う非ステロイド化合物およびステロイド化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9694005B2 (https=) |
| EP (2) | EP2991644B1 (https=) |
| JP (1) | JP6417392B2 (https=) |
| AU (1) | AU2014247941C1 (https=) |
| CA (2) | CA3151555A1 (https=) |
| WO (1) | WO2014165815A2 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10675289B2 (en) * | 2014-10-02 | 2020-06-09 | University Of Maryland, Baltimore | Methods of treating pancreatic cancer |
| WO2017201683A1 (en) * | 2016-05-25 | 2017-11-30 | Merck Sharp & Dohme Corp. | Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists |
| US12391725B2 (en) | 2016-06-22 | 2025-08-19 | National Institutes Of Health (Nih), U.S. Dept. Of Health And Human Services (Dhhs), U.S. Government | Method for production of novel galeterone analogs and uses thereof |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| CN106902112B (zh) * | 2017-03-07 | 2019-06-04 | 中国医学科学院医药生物技术研究所 | Imb-a6作为雄激素受体拮抗剂的应用 |
| CN111943889B (zh) * | 2020-07-24 | 2022-07-22 | 中国医学科学院医药生物技术研究所 | 一种双芳香基胺类化合物及其制备方法和应用 |
| CN116444599B (zh) * | 2022-01-07 | 2026-02-03 | 中国科学院上海药物研究所 | 甾体类化合物及制备方法和用途 |
| WO2024064026A1 (en) * | 2022-09-19 | 2024-03-28 | Alterome Therapeutics, Inc. | Akt1 modulators |
| CN120225521A (zh) * | 2022-09-26 | 2025-06-27 | 亚特罗姆医疗公司 | Akt1调节剂 |
| WO2024091899A1 (en) * | 2022-10-25 | 2024-05-02 | University Of Maryland, Baltimore | Salts of galeterone and salts of next generation galeterone analogs, and uses thereof |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA129379A (en) | 1910-10-18 | 1910-11-22 | John Clarence Bisland | Hoe |
| DE3928177A1 (de) * | 1989-04-08 | 1991-02-28 | Thomae Gmbh Dr K | Benzimidazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
| IL95975A (en) * | 1989-10-24 | 1997-06-10 | Takeda Chemical Industries Ltd | N-benzyl- 2-alkylbenzimidazole derivatives, their production and pharmaceutical compositions containing them |
| DK40192D0 (da) * | 1992-03-26 | 1992-03-26 | Neurosearch As | Imidazolforbindelser, deres fremstilling og anvendelse |
| DE10342503A1 (de) | 2003-09-12 | 2005-04-14 | Merck Patent Gmbh | Benzyl-Benzimidazolylderivate |
| US7875599B2 (en) * | 2005-03-02 | 2011-01-25 | University Of Maryland | C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity |
| EP2732819B1 (en) * | 2008-02-07 | 2019-10-16 | Massachusetts Eye & Ear Infirmary | Compounds that enhance Atoh-1 expression |
| 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 |
| GB2479337A (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 |
| WO2010091306A1 (en) * | 2009-02-05 | 2010-08-12 | Tokai Pharmaceuticals | Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens |
| BR112014001440A2 (pt) * | 2011-07-18 | 2017-02-21 | Tokai Pharmaceuticals Inc | novas composições e métodos para o tratamento de câncer de próstata |
| KR20150127720A (ko) * | 2013-03-14 | 2015-11-17 | 유니버시티 오브 매릴랜드, 발티모어 | 안드로겐 수용체 하향 조절제 및 그의 용도 |
-
2014
- 2014-04-04 US US14/781,437 patent/US9694005B2/en active Active
- 2014-04-04 CA CA3151555A patent/CA3151555A1/en active Pending
- 2014-04-04 WO PCT/US2014/033063 patent/WO2014165815A2/en not_active Ceased
- 2014-04-04 AU AU2014247941A patent/AU2014247941C1/en active Active
- 2014-04-04 CA CA2908577A patent/CA2908577C/en active Active
- 2014-04-04 EP EP14779540.5A patent/EP2991644B1/en active Active
- 2014-04-04 JP JP2016506667A patent/JP6417392B2/ja active Active
- 2014-04-04 EP EP19161938.6A patent/EP3514147B1/en active Active
-
2017
- 2017-05-31 US US15/609,803 patent/US10617685B2/en active Active
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