JP2009506077A5 - - Google Patents
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- Publication number
- JP2009506077A5 JP2009506077A5 JP2008528257A JP2008528257A JP2009506077A5 JP 2009506077 A5 JP2009506077 A5 JP 2009506077A5 JP 2008528257 A JP2008528257 A JP 2008528257A JP 2008528257 A JP2008528257 A JP 2008528257A JP 2009506077 A5 JP2009506077 A5 JP 2009506077A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- aryl
- alkoxycarbonyl
- carbamoyl
- 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
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 76
- 125000003710 aryl alkyl group Chemical group 0.000 claims 76
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 76
- 125000001072 heteroaryl group Chemical group 0.000 claims 71
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 69
- 125000003282 alkyl amino group Chemical group 0.000 claims 68
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 68
- 125000004414 alkyl thio group Chemical group 0.000 claims 68
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 68
- 125000004663 dialkyl amino group Chemical group 0.000 claims 68
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 66
- 125000004404 heteroalkyl group Chemical group 0.000 claims 66
- 125000002252 acyl group Chemical group 0.000 claims 64
- 125000004442 acylamino group Chemical group 0.000 claims 64
- 239000001257 hydrogen Substances 0.000 claims 51
- 229910052739 hydrogen Inorganic materials 0.000 claims 51
- 125000000217 alkyl group Chemical group 0.000 claims 46
- 125000003118 aryl group Chemical group 0.000 claims 42
- 125000000547 substituted alkyl group Chemical group 0.000 claims 41
- 125000003107 substituted aryl group Chemical group 0.000 claims 41
- 150000002431 hydrogen Chemical class 0.000 claims 39
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 36
- 150000001875 compounds Chemical class 0.000 claims 36
- 229910052799 carbon Inorganic materials 0.000 claims 34
- 150000001721 carbon Chemical group 0.000 claims 34
- 125000004093 cyano group Chemical group *C#N 0.000 claims 34
- 125000001475 halogen functional group Chemical group 0.000 claims 34
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 34
- 125000003545 alkoxy group Chemical group 0.000 claims 28
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 28
- 125000004432 carbon atom Chemical group C* 0.000 claims 24
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 24
- -1 carboxy, cyano, nitro, chloro, bromo, iodo, thio Chemical group 0.000 claims 18
- 125000000449 nitro group Chemical class [O-][N+](*)=O 0.000 claims 18
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 8
- 239000001301 oxygen Chemical group 0.000 claims 8
- 229910052760 oxygen Chemical group 0.000 claims 8
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- SCVJRXQHFJXZFZ-KVQBGUIXSA-N 2-amino-9-[(2r,4s,5r)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3h-purine-6-thione Chemical compound C1=2NC(N)=NC(=S)C=2N=CN1[C@H]1C[C@H](O)[C@@H](CO)O1 SCVJRXQHFJXZFZ-KVQBGUIXSA-N 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 101150065749 Churc1 gene Proteins 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102100038239 Protein Churchill Human genes 0.000 claims 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 230000008484 agonism Effects 0.000 claims 1
- 239000003098 androgen Substances 0.000 claims 1
- 102000001307 androgen receptors Human genes 0.000 claims 1
- 108010080146 androgen receptors Proteins 0.000 claims 1
- 230000008485 antagonism Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 208000037922 refractory disease Diseases 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 208000002320 spinal muscular atrophy Diseases 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 0 C*C(*)(*)[C@@](*C(*)(*)*(C)C(C1(*)*)[C@]11[C@@]2([C@@]3C4(*)*)C4(*)C1(*)*)([C@@]2(*)C(*)(*)C1=C3*=NC1=O)[Rn] Chemical compound C*C(*)(*)[C@@](*C(*)(*)*(C)C(C1(*)*)[C@]11[C@@]2([C@@]3C4(*)*)C4(*)C1(*)*)([C@@]2(*)C(*)(*)C1=C3*=NC1=O)[Rn] 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71174905P | 2005-08-26 | 2005-08-26 | |
| PCT/US2006/033732 WO2007025303A2 (en) | 2005-08-26 | 2006-08-28 | Non-steroidal antiandrogens |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009506077A JP2009506077A (ja) | 2009-02-12 |
| JP2009506077A5 true JP2009506077A5 (https=) | 2009-10-15 |
Family
ID=37772542
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008528257A Pending JP2009506077A (ja) | 2005-08-26 | 2006-08-28 | 非ステロイド性抗アンドロゲン剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7645885B2 (https=) |
| EP (1) | EP1916896A4 (https=) |
| JP (1) | JP2009506077A (https=) |
| AU (1) | AU2006282767A1 (https=) |
| CA (1) | CA2620275A1 (https=) |
| WO (1) | WO2007025303A2 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2473886C (en) * | 2002-01-22 | 2012-08-21 | The Regents Of The University Of California | Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof |
| US9868705B2 (en) | 2013-09-27 | 2018-01-16 | The Board Of Trustees Of The University Of Illinois | Tetra-aryl cyclobutane inhibitors of androgen receptor action for the treatment of hormone refractory cancer |
| US10017471B2 (en) | 2015-04-21 | 2018-07-10 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10441570B2 (en) | 2015-04-21 | 2019-10-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) Ligands and methods of use thereof |
| US10035763B2 (en) | 2015-04-21 | 2018-07-31 | Gtx, Inc. | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10654809B2 (en) | 2016-06-10 | 2020-05-19 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10865184B2 (en) | 2015-04-21 | 2020-12-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10093613B2 (en) | 2015-04-21 | 2018-10-09 | Gtx, Inc. | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| CN107709290B (zh) | 2015-04-21 | 2023-02-28 | Gtx公司 | 选择性雄激素受体降解剂(sard)配体和其使用方法 |
| RU2724103C2 (ru) | 2015-04-21 | 2020-06-22 | Джи Ти Икс, ИНК. | Селективные лиганды-разрушители андрогенных рецептов (sard) и способы их применения |
| US10806720B2 (en) | 2015-04-21 | 2020-10-20 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US9834507B2 (en) | 2015-04-21 | 2017-12-05 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US11230523B2 (en) | 2016-06-10 | 2022-01-25 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| WO2020051344A1 (en) | 2018-09-05 | 2020-03-12 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (sard) ligands and methods of use thereof |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3135743A (en) * | 1960-06-29 | 1964-06-02 | Sterling Drug Inc | Steroido[2. 3-d]isoxazoles and preparation thereof |
| US5677336A (en) | 1993-10-21 | 1997-10-14 | Ligand Pharmaceuticals Incorporated | Non-steroid androgen receptor antagonist compounds and methods |
| US6696459B1 (en) | 1994-12-22 | 2004-02-24 | Ligand Pharmaceuticals Inc. | Steroid receptor modulator compounds and methods |
| US5696130A (en) | 1994-12-22 | 1997-12-09 | Ligand Pharmaceuticals Incorporated | Tricyclic steroid receptor modulator compounds and methods |
| US6017924A (en) | 1996-06-27 | 2000-01-25 | Ligand Pharmaceuticals Incorporated | Androgen receptor modulator compounds and methods |
| JP2001518501A (ja) | 1997-10-06 | 2001-10-16 | ビーエーエスエフ アクチェンゲゼルシャフト | インデノ［１，２−ｃ］−、ナフト［１，２−ｃ］−およびベンゾ［６，７］シクロへプタ［１，２−ｃ］ピラゾール誘導体 |
| US6372779B1 (en) | 1997-12-29 | 2002-04-16 | Ortho Pharmaceutical Corporation | Anti-inflammatory compounds |
| US6380207B2 (en) | 1998-02-13 | 2002-04-30 | Abbott Laboratories | Glucocortiocoid-selective antiinflammatory agents |
| US6462036B1 (en) | 1998-11-06 | 2002-10-08 | Basf Aktiengesellschaft | Tricyclic pyrazole derivatives |
| KR20020038741A (ko) | 1999-08-27 | 2002-05-23 | 윌리암 엘. 레스페스 | 안드로겐 수용체 조절 화합물 및 방법 |
| US6566372B1 (en) | 1999-08-27 | 2003-05-20 | Ligand Pharmaceuticals Incorporated | Bicyclic androgen and progesterone receptor modulator compounds and methods |
| JP2003508397A (ja) | 1999-08-27 | 2003-03-04 | リガンド・ファーマシューティカルズ・インコーポレイテッド | アンドロゲンレセプターモジュレーターとしての８−置換−６−トリフルオロメチル−９−ピリド［３，２−ｇ］キノリン化合物 |
| DE60201921T2 (de) | 2001-01-24 | 2005-10-06 | Yung Shin Pharmaceutical Ind. Co., Ltd. | Kondensierte Pyrazolverbindungen |
| US7026484B2 (en) | 2001-02-23 | 2006-04-11 | Ligand Pharmaceuticals Incorporated | Tricyclic androgen receptor modulator compounds and methods |
| US7214690B2 (en) | 2001-02-23 | 2007-05-08 | Ligand Pharmaceuticals Incorporated | Tricyclic quinolinone and tricyclic quinoline androgen receptor modulator compounds and methods |
| CN1578781A (zh) | 2001-09-26 | 2005-02-09 | 拜尔药品公司 | 用作抗糖尿病药物的1,8－萘啶衍生物 |
| DE10164564B4 (de) | 2001-12-14 | 2007-05-16 | Zentaris Gmbh | Tetrahydrocarbazolderivate als Liganden für G-Protein gekoppelte Rezeptoren (GPCR) |
| CA2473886C (en) | 2002-01-22 | 2012-08-21 | The Regents Of The University Of California | Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof |
| EP1496892B1 (en) * | 2002-04-11 | 2011-01-26 | Merck Sharp & Dohme Corp. | 1h-benzo(f)indazol-5-yl derivatives as selective glucocorticoid receptor modulators |
| AU2003270783C1 (en) | 2002-09-20 | 2010-05-20 | Merck Sharp & Dohme Corp. | Octahydro-2-H-naphtho[1,2-F] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators |
| JP3990718B2 (ja) | 2003-01-09 | 2007-10-17 | ファイザー・インク | キナーゼ阻害剤としてのジアゼピノインドール誘導体 |
| EP1599201B1 (en) * | 2003-02-25 | 2010-04-14 | Merck Sharp & Dohme Corp. | Selective non-steroidal glucocorticoid receptor modulators |
| ATE447575T1 (de) | 2003-04-23 | 2009-11-15 | Merck & Co Inc | Selektive spirocyclische glucocorticoid-rezeptor- modulatoren |
| US7071333B2 (en) | 2003-07-30 | 2006-07-04 | Bristol-Myers Squibb Company | Triazolopurine-based tricyclic compounds and pharmaceutical compositions comprising same |
| MXPA06001751A (es) | 2003-08-22 | 2006-05-12 | Ligand Pharm Inc | Derivados de 6-cicloamino-2-quinolinona como compuestos moduladores de receptor de androgeno. |
-
2006
- 2006-08-28 WO PCT/US2006/033732 patent/WO2007025303A2/en not_active Ceased
- 2006-08-28 EP EP06802564A patent/EP1916896A4/en not_active Withdrawn
- 2006-08-28 CA CA002620275A patent/CA2620275A1/en not_active Abandoned
- 2006-08-28 AU AU2006282767A patent/AU2006282767A1/en not_active Abandoned
- 2006-08-28 US US11/467,908 patent/US7645885B2/en not_active Expired - Fee Related
- 2006-08-28 JP JP2008528257A patent/JP2009506077A/ja active Pending
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