JP2005523254A5 - - Google Patents
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- Publication number
- JP2005523254A5 JP2005523254A5 JP2003561595A JP2003561595A JP2005523254A5 JP 2005523254 A5 JP2005523254 A5 JP 2005523254A5 JP 2003561595 A JP2003561595 A JP 2003561595A JP 2003561595 A JP2003561595 A JP 2003561595A JP 2005523254 A5 JP2005523254 A5 JP 2005523254A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- compound
- alkyl
- aryl
- heteroalkyl
- 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.)
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- 150000001875 compounds Chemical class 0.000 description 36
- 229910052739 hydrogen Inorganic materials 0.000 description 27
- 239000001257 hydrogen Substances 0.000 description 27
- 150000002431 hydrogen Chemical class 0.000 description 24
- 125000004404 heteroalkyl group Chemical group 0.000 description 21
- 125000001072 heteroaryl group Chemical group 0.000 description 21
- 125000002252 acyl group Chemical group 0.000 description 20
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 20
- 125000003710 aryl alkyl group Chemical group 0.000 description 19
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 17
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 16
- 125000000217 alkyl group Chemical group 0.000 description 16
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 16
- 125000003282 alkyl amino group Chemical group 0.000 description 13
- 125000004663 dialkyl amino group Chemical group 0.000 description 13
- 125000003545 alkoxy group Chemical group 0.000 description 12
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 description 12
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 12
- 125000000547 substituted alkyl group Chemical group 0.000 description 12
- 125000003118 aryl group Chemical group 0.000 description 11
- 125000005843 halogen group Chemical group 0.000 description 11
- 125000003107 substituted aryl group Chemical group 0.000 description 11
- 125000004442 acylamino group Chemical group 0.000 description 10
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 9
- 125000004093 cyano group Chemical group *C#N 0.000 description 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 9
- 229910052757 nitrogen Inorganic materials 0.000 description 8
- 125000004043 oxo group Chemical group O=* 0.000 description 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 7
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 7
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 7
- 125000004414 alkyl thio group Chemical group 0.000 description 7
- 229910052799 carbon Inorganic materials 0.000 description 7
- 239000000203 mixture Substances 0.000 description 7
- 125000005415 substituted alkoxy group Chemical group 0.000 description 7
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 6
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 5
- 239000008194 pharmaceutical composition Substances 0.000 description 5
- 102000003676 Glucocorticoid Receptors Human genes 0.000 description 4
- 108090000079 Glucocorticoid Receptors Proteins 0.000 description 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 4
- 229910052760 oxygen Inorganic materials 0.000 description 4
- 239000001301 oxygen Substances 0.000 description 4
- 125000000446 sulfanediyl group Chemical group *S* 0.000 description 4
- 229910052717 sulfur Inorganic materials 0.000 description 4
- 239000011593 sulfur Substances 0.000 description 4
- 208000019901 Anxiety disease Diseases 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- 208000008589 Obesity Diseases 0.000 description 3
- 230000036506 anxiety Effects 0.000 description 3
- 206010012601 diabetes mellitus Diseases 0.000 description 3
- 208000027866 inflammatory disease Diseases 0.000 description 3
- 235000020824 obesity Nutrition 0.000 description 3
- 230000004913 activation Effects 0.000 description 2
- 230000008484 agonism Effects 0.000 description 2
- 230000008485 antagonism Effects 0.000 description 2
- 125000000753 cycloalkyl group Chemical group 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 208000015122 neurodegenerative disease Diseases 0.000 description 2
- 230000000626 neurodegenerative effect Effects 0.000 description 2
- 230000000069 prophylactic effect Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 239000000556 agonist Substances 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- -1 carboxy, cyano, carbamoyl Chemical group 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 230000004770 neurodegeneration Effects 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35148402P | 2002-01-22 | 2002-01-22 | |
| US60/351,484 | 2002-01-22 | ||
| US37375702P | 2002-04-17 | 2002-04-17 | |
| US60/373,757 | 2002-04-17 | ||
| PCT/US2003/001997 WO2003061651A1 (en) | 2002-01-22 | 2003-01-22 | Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010006117A Division JP2010132672A (ja) | 2002-01-22 | 2010-01-14 | グルココルチコイドレセプターのための非ステロイド性リガンド、その組成物および使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005523254A JP2005523254A (ja) | 2005-08-04 |
| JP2005523254A5 true JP2005523254A5 (https=) | 2006-04-06 |
| JP4745609B2 JP4745609B2 (ja) | 2011-08-10 |
Family
ID=27616805
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003561595A Expired - Fee Related JP4745609B2 (ja) | 2002-01-22 | 2003-01-22 | グルココルチコイドレセプターのための非ステロイド性リガンド、その組成物および使用 |
| JP2010006117A Pending JP2010132672A (ja) | 2002-01-22 | 2010-01-14 | グルココルチコイドレセプターのための非ステロイド性リガンド、その組成物および使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010006117A Pending JP2010132672A (ja) | 2002-01-22 | 2010-01-14 | グルココルチコイドレセプターのための非ステロイド性リガンド、その組成物および使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (4) | US6831093B2 (https=) |
| EP (1) | EP1467730A4 (https=) |
| JP (2) | JP4745609B2 (https=) |
| AU (1) | AU2003214879B2 (https=) |
| CA (1) | CA2473886C (https=) |
| WO (1) | WO2003061651A1 (https=) |
Families Citing this family (91)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4745609B2 (ja) * | 2002-01-22 | 2011-08-10 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | グルココルチコイドレセプターのための非ステロイド性リガンド、その組成物および使用 |
| DE60335869D1 (de) | 2002-04-11 | 2011-03-10 | Merck Sharp & Dohme | 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren |
| US20040220153A1 (en) * | 2002-09-24 | 2004-11-04 | Jost-Price Edward Roydon | Methods and reagents for the treatment of diseases and disorders associated with increased levels of proinflammatory cytokines |
| WO2004075840A2 (en) * | 2003-02-25 | 2004-09-10 | Merck & Co. Inc. | Selective non-steroidal glucocorticoid receptor modulators |
| US20070088042A1 (en) | 2004-09-09 | 2007-04-19 | Meissner Robert S | Fluorinated 4-azasteroid derivatives as androgen receptor modulators |
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| CN113563163A (zh) * | 2021-07-07 | 2021-10-29 | 南京伊派森化学科技有限公司 | 一种5-溴-1，2，3-三甲氧基苯的合成方法 |
| KR20250073629A (ko) | 2022-10-06 | 2025-05-27 | 코어셉트 쎄라퓨틱스 인코포레이티드 | 글루코코르티코이드 수용체 조절제의 제형 |
| US12433882B2 (en) | 2022-10-28 | 2025-10-07 | Corcept Therapeutics Incorporated | Treatments for amyotrophic lateral sclerosis using dazucorilant |
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| US3135743A (en) * | 1960-06-29 | 1964-06-02 | Sterling Drug Inc | Steroido[2. 3-d]isoxazoles and preparation thereof |
| NL273722A (https=) * | 1961-01-18 | |||
| DE1169442B (de) * | 1962-05-05 | 1964-05-06 | Schering Ag | Verfahren zur Herstellung von Steroidthioaethern bzw. Aminothiazolosteroiden |
| GB1071124A (en) * | 1965-05-11 | 1967-06-07 | Biorex Laboratories Ltd | Derivatives of pyrazolo-[4',5'-b]-11-oxo-18ª‡- and 18ª‰-olean-12-en-30-oic acid |
| US4412995A (en) | 1981-02-19 | 1983-11-01 | Sterling Drug Inc. | Pentacyclic phenylpyrazole compounds as anti-inflammatory agents |
| EP0102404A1 (en) * | 1982-09-02 | 1984-03-14 | Sterling Drug Inc. | Novel polycyclic fused pyrazole compounds useful as antiinflammatory agents and preparation thereof |
| CA1178965A (en) | 1982-09-13 | 1984-12-04 | Sterling Drug Inc. | Polycyclic fused pyrazole compounds useful as anti- inflammatory agents and preparation thereof |
| US6139873A (en) * | 1996-07-10 | 2000-10-31 | Cedars-Sinai Medical Center | Combined pharmaceutical estrogen-androgen-progestin |
| 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 |
| AR014195A1 (es) | 1997-12-29 | 2001-02-07 | Ortho Mcneil Pharm Inc | Compuestos de trifenilpropanamida utiles para el tratamiento de procesos inflamatorios, composiciones anti-inflamatorias que los comprenden, ymetodos para prepararlos |
| US6380207B2 (en) | 1998-02-13 | 2002-04-30 | Abbott Laboratories | Glucocortiocoid-selective antiinflammatory agents |
| ES2230880T3 (es) | 1998-07-30 | 2005-05-01 | Abbott Laboratories | Agentes selectivos anti-inflmatorios de glucocorticoides. |
| GB9816935D0 (en) | 1998-08-05 | 1998-09-30 | Karobio Ab | Novel glucocortoid and thyroid receptor ligands for the treatment of metabolic disorders |
| US6462036B1 (en) * | 1998-11-06 | 2002-10-08 | Basf Aktiengesellschaft | Tricyclic pyrazole derivatives |
| 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 |
| BR0212864A (pt) * | 2001-09-26 | 2004-08-17 | Bayer Pharmaceuticals Corp | Derivados de 1,6-naftiridina como antidiabéticos |
| DE10164564B4 (de) * | 2001-12-14 | 2007-05-16 | Zentaris Gmbh | Tetrahydrocarbazolderivate als Liganden für G-Protein gekoppelte Rezeptoren (GPCR) |
| JP4745609B2 (ja) * | 2002-01-22 | 2011-08-10 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | グルココルチコイドレセプターのための非ステロイド性リガンド、その組成物および使用 |
| DE60335869D1 (de) | 2002-04-11 | 2011-03-10 | Merck Sharp & Dohme | 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren |
| CA2512683C (en) * | 2003-01-09 | 2010-03-16 | Pfizer Inc. | Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agents and radiation therapy |
| WO2004066920A2 (en) | 2003-01-21 | 2004-08-12 | Merck & Co. Inc. | 17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators |
| WO2004075840A2 (en) * | 2003-02-25 | 2004-09-10 | Merck & Co. Inc. | Selective non-steroidal glucocorticoid receptor modulators |
| US7662846B2 (en) | 2003-04-23 | 2010-02-16 | Merck Sharp & Dohme Corp. | Selective spirocyclic glucocorticoid receptor modulators |
| US7071333B2 (en) * | 2003-07-30 | 2006-07-04 | Bristol-Myers Squibb Company | Triazolopurine-based tricyclic compounds and pharmaceutical compositions comprising same |
| ATE463479T1 (de) | 2005-05-18 | 2010-04-15 | Merck Sharp & Dohme | D-homoandrosta-17-yl-carbamat-derivate als selektive glucocorticoid-rezeptor-liganden |
| CA2620275A1 (en) * | 2005-08-26 | 2007-03-01 | Thomas S. Scanlan | Non-steroidal antiandrogens |
-
2003
- 2003-01-22 JP JP2003561595A patent/JP4745609B2/ja not_active Expired - Fee Related
- 2003-01-22 CA CA2473886A patent/CA2473886C/en not_active Expired - Fee Related
- 2003-01-22 US US10/350,260 patent/US6831093B2/en not_active Expired - Fee Related
- 2003-01-22 WO PCT/US2003/001997 patent/WO2003061651A1/en not_active Ceased
- 2003-01-22 EP EP03710722A patent/EP1467730A4/en not_active Withdrawn
- 2003-01-22 AU AU2003214879A patent/AU2003214879B2/en not_active Ceased
-
2004
- 2004-10-22 US US10/972,250 patent/US7485660B2/en not_active Expired - Fee Related
-
2009
- 2009-02-03 US US12/365,106 patent/US7947726B2/en not_active Expired - Fee Related
-
2010
- 2010-01-14 JP JP2010006117A patent/JP2010132672A/ja active Pending
-
2011
- 2011-05-11 US US13/105,349 patent/US20110218225A1/en not_active Abandoned
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