JP2011518843A5 - - Google Patents
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- Publication number
- JP2011518843A5 JP2011518843A5 JP2011506486A JP2011506486A JP2011518843A5 JP 2011518843 A5 JP2011518843 A5 JP 2011518843A5 JP 2011506486 A JP2011506486 A JP 2011506486A JP 2011506486 A JP2011506486 A JP 2011506486A JP 2011518843 A5 JP2011518843 A5 JP 2011518843A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- compound
- alkyl
- alkynyl
- alkenyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- -1 C 1-6 alkyl-OH Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims 2
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000005647 linker group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N 1H-pyrrole Natural products C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 230000002280 anti-androgenic effect Effects 0.000 claims 1
- 239000000051 antiandrogen Substances 0.000 claims 1
- 125000004980 cyclopropylene group Chemical group 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 150000002500 ions Chemical class 0.000 claims 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4755908P | 2008-04-24 | 2008-04-24 | |
| US61/047,559 | 2008-04-24 | ||
| PCT/US2009/041715 WO2009132307A1 (en) | 2008-04-24 | 2009-04-24 | Small-molecule inhibitors of the androgen receptor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011518843A JP2011518843A (ja) | 2011-06-30 |
| JP2011518843A5 true JP2011518843A5 (enExample) | 2012-06-14 |
| JP5599385B2 JP5599385B2 (ja) | 2014-10-01 |
Family
ID=41217163
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011506486A Expired - Fee Related JP5599385B2 (ja) | 2008-04-24 | 2009-04-24 | アンドロゲンレセプターの小分子阻害剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US8354538B2 (enExample) |
| EP (1) | EP2276345A4 (enExample) |
| JP (1) | JP5599385B2 (enExample) |
| KR (1) | KR101640512B1 (enExample) |
| AU (1) | AU2009240417B2 (enExample) |
| CA (1) | CA2722340A1 (enExample) |
| NZ (1) | NZ589299A (enExample) |
| WO (1) | WO2009132307A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2496135B (en) * | 2011-11-01 | 2015-03-18 | Valirx Plc | Inhibitors of the interaction between a Src family kinase and an androgen receptor or estradiol receptor for treatment of endometriosis |
| WO2014130932A2 (en) * | 2013-02-25 | 2014-08-28 | Novartis Ag | Novel androgen receptor mutation |
| GB2513615A (en) | 2013-05-01 | 2014-11-05 | Cancer Rec Tech Ltd | Medical use |
| US10428048B2 (en) | 2015-09-04 | 2019-10-01 | City Of Hope | Androgen receptor antagonists |
| WO2019126739A1 (en) | 2017-12-21 | 2019-06-27 | Shepherd Therapeutics, Inc. | Pyrvinium pamoate anti-cancer therapies |
| WO2019152731A1 (en) * | 2018-01-31 | 2019-08-08 | Alpine Androsciences, Inc. | Androgen receptor antagonists |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1166538A (en) * | 1967-06-10 | 1969-10-08 | Pfizer Ltd | Substituted Tetrahydroquinolines |
| DE2421382A1 (de) | 1974-05-03 | 1975-11-20 | Council Scient Ind Res | 1-substituierte 4-(beta-2-chinolylaethyl)- piperazine und deren 1,2,3,4-tetrahydrochinolinanaloge |
| US3983121A (en) * | 1974-07-01 | 1976-09-28 | Council Of Scientific And Industrial Research | 1-Substituted 4-(β-2-quinolylethyl)piperazines and 1,2,3,4-tetrahydroquinolyl-ethyl analogues thereof |
| US5840500A (en) * | 1996-07-11 | 1998-11-24 | Trega Biosciences, Inc. | Quinoline derivatives and quinoline combinatorial libraries |
| KR100826485B1 (ko) * | 1999-10-14 | 2008-05-02 | 가켄 세야쿠 가부시키가이샤 | 테트라히드로퀴놀린 유도체 |
| EP1325914A4 (en) | 2000-09-14 | 2004-11-17 | Kaken Pharma Co Ltd | TETRAHYDROQUINOLINE COMPOUNDS |
| ITMI20012060A1 (it) * | 2001-10-05 | 2003-04-05 | Recordati Chem Pharm | Nuovi eterocilcli n-acilati |
| CN1506359A (zh) * | 2002-12-05 | 2004-06-23 | �й�ҽѧ��ѧԺҩ���о��� | 新的香豆素酰胺衍生物及其制法和其药物组合物与用途 |
| WO2005090282A1 (en) * | 2004-03-12 | 2005-09-29 | Ligand Pharmaceuticals Incorporated | Androgen receptor modulator compounds and methods |
| US7482359B2 (en) * | 2004-08-25 | 2009-01-27 | Merck & Co., Inc. | Androgen receptor modulators |
| US20080281105A1 (en) | 2005-01-18 | 2008-11-13 | Immusol Incorporated | Novel Quinolinium Salts and Derivatives |
| WO2007117466A2 (en) | 2006-03-31 | 2007-10-18 | Massachusetts Institute Of Technology | Celastrol, gedunin, and derivatives thereof as hsp90 inhibitors |
| WO2008128100A1 (en) * | 2007-04-13 | 2008-10-23 | The Regents Of The University Of California | Small-molecule inhibitors of the androgen receptor |
-
2009
- 2009-04-24 EP EP09735196A patent/EP2276345A4/en not_active Withdrawn
- 2009-04-24 KR KR1020107026231A patent/KR101640512B1/ko not_active Expired - Fee Related
- 2009-04-24 US US12/989,389 patent/US8354538B2/en not_active Expired - Fee Related
- 2009-04-24 JP JP2011506486A patent/JP5599385B2/ja not_active Expired - Fee Related
- 2009-04-24 AU AU2009240417A patent/AU2009240417B2/en not_active Ceased
- 2009-04-24 WO PCT/US2009/041715 patent/WO2009132307A1/en not_active Ceased
- 2009-04-24 NZ NZ589299A patent/NZ589299A/xx not_active IP Right Cessation
- 2009-04-24 CA CA2722340A patent/CA2722340A1/en not_active Abandoned
-
2012
- 2012-12-06 US US13/706,647 patent/US8580773B2/en not_active Expired - Fee Related