CA3151555A1 - Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity - Google Patents
Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activityInfo
- Publication number
- CA3151555A1 CA3151555A1 CA3151555A CA3151555A CA3151555A1 CA 3151555 A1 CA3151555 A1 CA 3151555A1 CA 3151555 A CA3151555 A CA 3151555A CA 3151555 A CA3151555 A CA 3151555A CA 3151555 A1 CA3151555 A1 CA 3151555A1
- Authority
- CA
- Canada
- Prior art keywords
- amd
- compound
- cancer
- mhz
- nmr
- 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.)
- Pending
Links
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
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- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/08—Radicals containing only hydrogen and carbon atoms
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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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| US61/808,902 | 2013-04-05 | ||
| CA2908577A CA2908577C (en) | 2013-04-04 | 2014-04-04 | Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity |
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| EP3200801B1 (en) | 2014-10-02 | 2024-04-24 | 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 |
| WO2017223320A1 (en) * | 2016-06-22 | 2017-12-28 | University Of Maryland, Baltimore | 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 |
| 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 |
| 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 |
| 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 |
| CN116444599A (zh) * | 2022-01-07 | 2023-07-18 | 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 |
| KR20250071251A (ko) * | 2022-09-26 | 2025-05-21 | 알테롬 테라퓨틱스, 인크. | Akt1 조절제 |
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| 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 |
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| DK2206719T3 (en) * | 2005-03-02 | 2015-01-26 | Univ Maryland | A pharmaceutical composition comprising 3-BETA-HYDROXY-17- (1-H-benzimidazol-1-yl) androsta-5, 16-DIEN |
| EP2732819B1 (en) | 2008-02-07 | 2019-10-16 | Massachusetts Eye & Ear Infirmary | Compounds that enhance Atoh-1 expression |
| 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 |
| EP2393827B1 (en) * | 2009-02-05 | 2015-10-07 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of 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 |
| CA2841960A1 (en) * | 2011-07-18 | 2013-01-24 | Tokai Pharmaceuticals, Inc. | Novel compositions and methods for treating prostate cancer |
| SG11201507093WA (en) * | 2013-03-14 | 2015-10-29 | Univ Maryland Baltimore Office Of Technology Transfer | Androgen receptor down-regulating agents and uses thereof |
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| CA2908577A1 (en) | 2014-10-09 |
| JP2016515630A (ja) | 2016-05-30 |
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| EP2991644B1 (en) | 2020-03-25 |
| CA2908577C (en) | 2022-05-31 |
| US20160038476A1 (en) | 2016-02-11 |
| AU2014247941A1 (en) | 2015-10-22 |
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